A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer.
Oil obtained from the seeds of Gossypium herbaceum L., the cotton plant. It is used in dietary products such as oleomargarine and many cooking oils. Cottonseed oil is commonly used in soaps and cosmetics.
Chemical substances or agents with contraceptive activity in males. Use for male contraceptive agents in general or for which there is no specific heading.
Biphasic dose responses of cells or organisms (including microorganisms) to an exogenous or intrinsic factor, in which the factor induces stimulatory or beneficial effects at low doses and inhibitory or adverse effects at high doses.
A highly caustic substance that is used to neutralize acids and make sodium salts. (From Merck Index, 11th ed)
A colorless liquid used as a solvent and an antiseptic. It is one of the ketone bodies produced during ketoacidosis.
The visually perceived property of objects created by absorption or reflection of specific wavelengths of light.
Hard, amorphous, brittle, inorganic, usually transparent, polymerous silicate of basic oxides, usually potassium or sodium. It is used in the form of hard sheets, vessels, tubing, fibers, ceramics, beads, etc.
Strong alkaline chemicals that destroy soft body tissues resulting in a deep, penetrating type of burn, in contrast to corrosives, that result in a more superficial type of damage via chemical means or inflammation. Caustics are usually hydroxides of light metals. SODIUM HYDROXIDE and potassium hydroxide are the most widely used caustic agents in industry. Medically, they have been used externally to remove diseased or dead tissues and destroy warts and small tumors. The accidental ingestion of products (household and industrial) containing caustic ingredients results in thousands of injuries per year.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The formation of crystalline substances from solutions or melts. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Inorganic or organic oxy acids of sulfur which contain the RSO2(OH) radical.
Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
Domesticated birds raised for food. It typically includes CHICKENS; TURKEYS, DUCKS; GEESE; and others.
The medical science concerned with the prevention, diagnosis, and treatment of diseases in animals.
A condition or physical state produced by the ingestion, injection, inhalation of or exposure to a deleterious agent.
Diseases of birds which are raised as a source of meat or eggs for human consumption and are usually found in barnyards, hatcheries, etc. The concept is differentiated from BIRD DISEASES which is for diseases of birds not considered poultry and usually found in zoos, parks, and the wild.
Food products manufactured from poultry.
Drugs used by veterinarians in the treatment of animal diseases. The veterinarian's pharmacological armamentarium is the counterpart of drugs treating human diseases, with dosage and administration adjusted to the size, weight, disease, and idiosyncrasies of the species. In the United States most drugs are subject to federal regulations with special reference to the safety of drugs and residues in edible animal products.
Use for general articles concerning veterinary medical education.
Individual's rights to obtain and use information collected or generated by others.
A publication issued at stated, more or less regular, intervals.
A quantitative measure of the frequency on average with which articles in a journal have been cited in a given period of time.
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
The evaluation by experts of the quality and pertinence of research or research proposals of other experts in the same field. Peer review is used by editors in deciding which submissions warrant publication, by granting agencies to determine which proposals should be funded, and by academic institutions in tenure decisions.
"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.
Process that is gone through in order for a drug to receive approval by a government regulatory agency. This includes any required pre-clinical or clinical testing, review, submission, and evaluation of the applications and test results, and post-marketing surveillance of the drug.
The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.
Surgical removal of the ductus deferens, or a portion of it. It is done in association with prostatectomy, or to induce infertility. (Dorland, 28th ed)
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Prevention of CONCEPTION by blocking fertility temporarily, or permanently (STERILIZATION, REPRODUCTIVE). Common means of reversible contraception include NATURAL FAMILY PLANNING METHODS; CONTRACEPTIVE AGENTS; or CONTRACEPTIVE DEVICES.
Sexual stimulation or gratification of the self.
Chemical substances which inhibit the process of spermatozoa formation at either the first stage, in which spermatogonia develop into spermatocytes and then into spermatids, or the second stage, in which spermatids transform into spermatozoa.
Compounds, usually hormonal, taken orally in order to block ovulation and prevent the occurrence of pregnancy. The hormones are generally estrogen or progesterone or both.
Insects of the suborder Heterocera of the order LEPIDOPTERA.
A large order of insects comprising the butterflies and moths.
Wormlike or grublike stage, following the egg in the life cycle of insects, worms, and other metamorphosing animals.
A suborder of HEMIPTERA, called true bugs, characterized by the possession of two pairs of wings. It includes the medically important families CIMICIDAE and REDUVIIDAE. (From Dorland, 28th ed)
A family of insect viruses causing disease in lepidopterous larvae, most commonly from species of the owlet moth family Noctuidae. There is one genus: Ascovirus.
Use of naturally-occuring or genetically-engineered organisms to reduce or eliminate populations of pests.
Regular course of eating and drinking adopted by a person or animal.
A plant genus in the family MYRTACEAE, order Myrtales, subclass Rosidae. It is best known for allspice from the dried berry of Pimenta diocia.
A plant species in the PIPERACEAE plant family. It is a common spice on foods and is used medicinally to increase gastrointestinal assimilation of other supplements and drugs. Piperine is a key component. Black pepper is picked unripe and heaped for a few days to ferment. White Pepper is the ripe fruit dehulled by maceration in water.
Proteins that bind to RNA molecules. Included here are RIBONUCLEOPROTEINS and other proteins whose function is to bind specifically to RNA.
Tumors or cancer of the COLON.
A biosensing technique in which biomolecules capable of binding to specific analytes or ligands are first immobilized on one side of a metallic film. Light is then focused on the opposite side of the film to excite the surface plasmons, that is, the oscillations of free electrons propagating along the film's surface. The refractive index of light reflecting off this surface is measured. When the immobilized biomolecules are bound by their ligands, an alteration in surface plasmons on the opposite side of the film is created which is directly proportional to the change in bound, or adsorbed, mass. Binding is measured by changes in the refractive index. The technique is used to study biomolecular interactions, such as antigen-antibody binding.
A polyposis syndrome due to an autosomal dominant mutation of the APC genes (GENES, APC) on CHROMOSOME 5. The syndrome is characterized by the development of hundreds of ADENOMATOUS POLYPS in the COLON and RECTUM of affected individuals by early adulthood.
Gossypol, an extract of cotton, has been studied as a male contraceptive pill. It decreased sperm production; however this is ... 1985). "Anti-implantation activity of some indigenous plants in rats". Acta Europaea Fertilitatis. 16 (6): 441-8. PMID 3832714 ... Hadley MA, Lin YC, Dym M (1981). "Effects of gossypol on the reproductive system of male rats". J. Androl. 2 (4): 190-9. doi: ... Deshpande VY, Mendulkar KN, Sadre NL; Mendulkar; Sadre (July 1980). "Male antifertility activity of Azadirachta Indica in mice ...
Gossypol and its derivatives - syntheses, spectroscopic investigations and biological tests. New compounds important in ... Ion channels, proton pumping - chemical modification, mechanism and biological activity, collective hydrogen bonds and bonds ... Ionophores (monensin, lasalocid), their structures, antibacterial activity and chemical modifications. ...
"Mitogenic activity of zeranol in human breast cancer cells is enhanced by leptin and suppressed by gossypol". Anticancer ...
NCI-sponsored clinical trials have demonstrated clinical activity against a number of different cancers including glioblastoma ... and gossypol. PARP inhibitors (e.g. Iniparib, Olaparib in clinical trials) PI3K inhibitors (e.g. perifosine in a phase III ... pyrimidines with anti-proliferative activity on pancreatic cancer cell lines". Bioorganic Chemisry. 94: 103472 - via Elsevier ... trial) Apatinib is a selective VEGF Receptor 2 inhibitor which has shown encouraging anti-tumor activity in a broad range of ...
... is one of the key steps in the synthesis of gossypol, a toxic terpenoid produced in cotton seeds. ... Davis GD, Essenberg M (1995). "(+)-delta-Cadinene is a product of sesquiterpene cyclase activity in cotton". Phytochemistry. 39 ... "Engineering cottonseed for use in human nutrition by tissue-specific reduction of toxic gossypol". Proc Natl Acad Sci U S A. ...
These phosphorylation events are essential for the activity of the enzyme, and 3-phosphoinositide-dependent protein kinase-1 ( ... Other naturally occurring PKCIs are miyabenol C, myricitrin, gossypol. Other PKCIs : Verbascoside, BIM-1. Bryostatin 1 can act ...
Animal Activity Monitor and Behavioral Processor - Inventors: Czekajewski; Jan A., Hill; Harold L., Kober; Kenneth J. - Issued ... "Effects of Gossypol on Consumption and CO2 Production in Human Prostate Cells", Anticancer Research 22:1491-1496 (2002) ... "An Activity Meter for Small Laboratory Animals Maintained Singly or in the Groups", Laboratory Animals (1968),2,49-50 J. ... Patent 3,602,806 Selective Activity Meter for Laboratory Animals - Inventors: Czekajewski Jan A. - Issued: August 31, 1971 U.S ...
Daily sexual activity increases sperm quality in men minimizing DNA damage in the sperm-because it is speculated to result in ... Gossypol has been associated with reduced sperm production. It is present in crude cottonseed oil, and potentially the organ ... However, despite these compensations, there are activities that should not be performed too often, in order to prevent ... Depo-Provera, Adjudin, and gossypol are examples of substances used as male contraceptives or in chemical castration. Recent ...
Gossypol was one of the many substances found in all parts of the cotton plant, and it was described by scientists as ' ... Foster suggests that men and boys may have also been forced into unwanted sexual activity; one problem in documenting such ...
Gossypol can have various chemical structures. It can exist in three forms: gossypol, gossypol acetic acid, and gossypol formic ... Plant hormones, which are secondary metabolites, are often used to regulate the metabolic activity within cells and oversee the ... Gossypol is a type of aldehyde, meaning that it has a formyl group. The formation of gossypol occurs through an isoprenoid ... Gossypol's main function in the cotton plant is to act as an enzyme inhibitor. An example of gossypol's enzyme inhibition is ...
12 November 2010). "Gossypol induces death receptor-5 through activation of the ROS-ERK-CHOP pathway and sensitizes colon ... 2017). "Curcumin-Free Turmeric Exhibits Activity against Human HCT-116 Colon Tumor Xenograft: Comparison with Curcumin and ... 1 October 2010). "Cyclodextrin-complexed curcumin exhibits anti-inflammatory and antiproliferative activities superior to those ...
1988). Production Study of a Low Gossypol Protein Product From Cottonseed Meal. Journal of Agricultural and Food Chemistry ... Between 1986 & 1991 initiated and developed professional activities between the USSR All Grain Institute and the Department of ...
The Court of Appeals granted the petition, citing the precautionary principle stating "when human activities may lead to ... One variety of cottonseed has been genetically modified to remove the toxin gossypol, so that it would be safe for humans to ... and long-term effects on the microbiota and their activities in soil". The diversity and number of weed populations has been ... "Association of the Brazil nut protein gene and Kunitz trypsin inhibitor alleles with soybean protease inhibitor activity and ...
... a key enzyme in gossypol production, without affecting the enzyme's production in other parts of the plant, where gossypol is ... Most studies have focused on the mating-type region in fission yeast, which may not be representative of activities in other ... Cotton seeds are rich in dietary protein but naturally contain the toxic terpenoid product gossypol, making them unsuitable for ... In plants, the majority of genes regulated by miRNAs are transcription factors; thus miRNA activity is particularly wide- ...
... which is defined as a person who experiences no limitation in any activities and has no symptoms from ordinary activities. ... Gossypol can increase the effects of diuretics, leading to toxicity. Gynura can cause low blood pressure. Licorice can worsen ... With NYHA class III heart failure, a marked limitation occurs with any activity; the person is comfortable only at rest. A ... A person's risk of developing heart failure is inversely related to level of physical activity. Those who achieved at least 500 ...
... gossypol - gp100 - gp209-2M - GPX-100 - grade IV astrocytoma - graft-versus-host disease - graft-versus-tumor - granisetron - ... mitotic activity - mitotic index - mitotic inhibitor - mitoxantrone - mivobulin isethionate - mixed glioma - MLN2704 - ...
... a key enzyme in gossypol production, without affecting the enzyme's production in other parts of the plant, where gossypol is ... Most studies have focused on the mating-type region in fission yeast, which may not be representative of activities in other ... Cotton seeds are rich in dietary protein but naturally contain the toxic terpenoid product gossypol, making them unsuitable for ... miRNA activity is also clustered in P-bodies.[48] Disruption of P-bodies decreases the efficiency of RNA interference, ...
... peptides from the venom of possess divergent biological activity". Toxicon. 45 (6): 727-733. doi:10.1016/j.toxicon.2005.01.020 ...
... activity and hCYP1A2-mediated mutagenicity of aflatoxin B1". Food and Chemical Toxicology. 44 (9): 1474-84. doi:10.1016/j.fct. ... and functional characterization of cytochrome P450 3A37 from turkey liver with high aflatoxin B1 epoxidation activity". ...
The toxic activity of LPS was first discovered and termed "endotoxin" by Richard Friedrich Johannes Pfeiffer, who distinguished ... LPS is required for the proper conformation of omptin activity; however, smooth LPS will sterically hinder omptins. ... molecular relationships of structure to activity and function". FASEB J. 8 (2): 217-25. doi:10.1096/fasebj.8.2.8119492. PMID ... "Intrinsic conformation of lipid A is responsible for agonistic and antagonistic activity". Eur. J. Biochem. 267 (10): 3032-9. ...
The ADP-ribosylation causes the Gαs subunit to lose its catalytic activity of GTP hydrolization into GDP + Pi, thus maintaining ... Increased Gαs activation leads to increased adenylate cyclase activity, which increases the intracellular concentration of 3',5 ... binding to Arf6 drives a change in the shape of CTA1 which exposes its active site and enables its catalytic activity.[11] The ...
... with the activities of types A and B enduring longest in vivo (from several weeks to months).[35] ... the toxin's activity is also susceptible, post-exposure, to inhibition by protease inhibitors, e.g., zinc-coordinating ... This blockage is slowly reversed as the toxin loses activity and the SNARE proteins are slowly regenerated by the affected cell ...
... a key enzyme in gossypol production, without affecting the enzyme's production in other parts of the plant, where gossypol is ... Most studies have focused on the mating-type region in fission yeast, which may not be representative of activities in other ... Cotton seeds are rich in dietary protein but naturally contain the toxic terpenoid product gossypol, making them unsuitable for ... miRNA activity is also clustered in P-bodies.[49] Disruption of P-bodies decreases the efficiency of RNA interference, ...
... with the activities of types A and B enduring longest in vivo (from several weeks to months).[51] ... the toxin's activity is also susceptible, post-exposure, to inhibition by protease inhibitors, e.g., zinc-coordinating ... This blockage is slowly reversed as the toxin loses activity and the SNARE proteins are slowly regenerated by the affected cell ...
... gossypol and some aza-derivatives of gossypol [24]. From the structure activity relationship, inactivity or weak activity of ... gossypol and screened for in vitro cytotoxic activity against several human cancer cell lines and antibacterial activity ... gossypol and some other gossypol derivatives reported [16, 17]. Regarding mechanism of action, most of gossypol derivatives ... L. Tai-Shun, R. F. Schinazi, J. Zhu et al., "Anti-HIV-1 activity and cellular pharmacology of various analogs of gossypol," ...
The atropisomers differ in their biological activities. (-)-(R)-Gossypol is more toxic ... Gossypol occurs naturally in the seed, foliage, and roots of the cotton plant ( Gossypium ) as atropisomers due to restricted ... R)-Gossypol is more toxic and exhibits significantly greater anticancer activity than the (+)-(S)-atropisomer. Most commercial ... Total and percent atropisomers of gossypol and gossypol-6-methyl ether in seeds from pima cottons and accessions of Gossypium ...
Both DNA fragmentation by ELISA assay and caspase 3/7 activity measurement were used for demonstrating apoptosis. To elucidate ... Gossypol, in combination with zoledronic acid, may provide a rational treatment option for ovarian cancer, not only by direct ... Combined gossypol and zoledronic acid treatment results in synergistic induction of cell death and regulates angiogenic ... In the present study, we aimed to evaluate the possible synergistic, cytotoxic effects of combination treatment of gossypol and ...
The invention also relates to the use of co-crystals of (-)-gossypol with a C.sub.1-8 carboxylic acid or C.sub.1-8 sulfonic ... gossypol with a C.sub.1-8 carboxylic acid or C.sub.1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. ... Gossypol has been shown to bind to Bcl-2 and Bcl-X.sub.L at the BH3 binding groove and to have significant anticancer activity ... gossypol. Moreover, (-)-gossypol is a more potent inhibitor than racemic gossypol. Thus, compositions comprising (-)-gossypol ...
Gossypol, Proapoptotic agent; alters cell cycle and apoptosis proteins. (CAS 303-45-7), with ,98% purity. Join researchers ... Exhibits a wide range of biological effects including anticancer and antifertility activity. Downregulates Bcl-2, p53 and ... Molecular mechanism of gossypol-induced cell growth inhibition and cell death of HT-29 human colon carcinoma cells.. Biochem ... Gossypol: prototype of inhibitors targeted to dinucleotide folds.. Curr Med Chem 7:479-98 (2000). Read more (PubMed: 10702620 ...
Calculate urease activity as mg/litre urea in urea blank less mg/litre urea in sample. 4.8.2 Free gossypol in cottonseed meal ... e) Standard gossypol solution (i) Dissolve 25 mg of pure gossypol in aniline-free acetone and transfer to a 250 ml volumetric ... A - mg apparent free gossypol in sample aliquot (a). B - mg apparent free gossypol in sample aliquot (b). W - sample weight. V ... 4.8.1 Urease activity in soybean meal Reagents: (a) dimethylaminobenzaldehyde solution (DMAB) Dissolve 16 g DMAB in 1 litre 95 ...
Diagnosis can be confirmed by testing brain for cholinesterase activity.. Gossypol:. Cottonseed meal contains appreciable ... amounts of gossypol, which produces severe cardiac edema that results in dyspnea, weakness, and anorexia. When fed to laying ...
... a novel derivate of gossypol, suppresses the c-Myc signaling pathway [26]; gossypol also suppresses NF-kappaB activity and NF- ... D. Moon, M. Kim, J. Lee, and G. Kim, "Gossypol suppresses NF-κB activity and NF-κB-related gene expression in human leukemia ... Significant necrosis was observed with 20 μmol/L gossypol-treatment. for and for . ... To profile gossypol-induced changes in proteomes of untreated and gossypol-treated cells, we have carried out a SILAC-based ...
Gossypol and its derivatives - syntheses, spectroscopic investigations and biological tests. New compounds important in ... Ion channels, proton pumping - chemical modification, mechanism and biological activity, collective hydrogen bonds and bonds ... Ionophores (monensin, lasalocid), their structures, antibacterial activity and chemical modifications. ...
Identification of a novel potential antitumor activity of gossypol as an APE1/Ref-1 inhibitor Qian CY, Li MX, Sui JD, Ren T, Li ... Synthesis and antibacterial activities of acylide derivatives bearing an aryl-tetrazolyl chain Shan LX, Sun PH, Guo BQ, Xu XJ, ... Neurotherapeutic activity of the recombinant heat shock protein Hsp70 in a model of focal cerebral ischemia in rats Shevtsov MA ... Triazole derivatives with improved in vitro antifungal activity over azole drugs Yu S, Chai X, Wang Y, Cao Y, Zhang J, Wu Q, ...
Inhibition of lactate dehydrogenase-X by imino-derivatives of gossypol:structure activity relationship. ... Comparative in vitro spermicidal effects of (+/-)-gossypol, (+)-gossypol, (-)-gossypol and gossypolone.. Kim IC, Waller DP, ... Analysis of gossypol and gossypol-acetic acid by high-performance liquid chromatography. ... Vaginal contraceptive activity of aryl 4-guanidinobenzoates (acrosin inhibitors) in rabbits.. Kaminski JM, Nuzzo NA, Bauer L, ...
... three lignans and one gossypol derivative, were isolated from the branches of Polyalthia rumphii (Blume ... Two novel alkaloids from the stem of Saprosma hainanense and their cytotoxic activities in vitro. Chem. Pharm. Bull. 59, 338- ... Twelve known compounds, including eight alkaloids, three lignans and one gossypol derivative, were isolated from the branches ... Anticancer activities of constituents from the stem oiPolyalthia rumphii. Pak. J. Pharm. Sci. 25, 353-356. ...
However, gossypol, a toxic terpenoid present in the glands, renders cottonseed unfit as food and as feed for non-ruminant ... Results from enzyme activity and molecular analyses on developing embryos were consistent with the observed phenotype in the ... Therefore, elimination of gossypol from cottonseed has been a long-standing goal of geneticists. We have successfully used RNAi ... We demonstrate that it is possible to reduce significantly the levels of cottonseed-gossypol in a stable and heritable manner. ...
Surface activity of cotton dust components: catechin (120809), rutin (153184), and gossypol (303457) was measured alone and ... The authors conclude that gossypol may be the cotton dust component responsible for surface activity of cotton dust. The role ... on surface activity was determined. All three cotton components were surface active. Gossypol was the most active. Surface ... Repeated washings reduced the surface activity to 10 percent. Repeated washings of cotton dust with sodium-hydroxide removed ...
Stability and antioxidant activity of gossypol derivative immobilized on N-polyvinylpyrrolidone.. *M. Ionov, N. Gordiyenko, +6 ... The objective of this study is analysis of stability and antioxidant and antiradical activities of the gossypol derivative… ... gossypol beta-aminoethyl sodium sulfate. Known as: megosine, (2,2-Binaphthalene)-1,1,6,6,7,7-hexol, 3,3-dimethyl-5,5-bis( ... The immobilization of gossypol derivative on N-polyvinylpyrrolidone increases its water solubility and modifies membrane-active ...
Bioactivities of gossypol, 6-methoxy gossypol and 6,6-dimethoxy gossypol. Journal of Agricultural and Food Chemistry. 2008, 56 ... Anticancer activity of branched-chain derivatives of oleic acid. Anticancer Research, 2011,31:3165-3170 83. S.Z. Yang, L.T. ... Anticancer activity of limonoid from Khaya senegalensis. Phytotherapy Research. 2007. 21:731-734. 129. Hua Yin Chung, Chi Wang ... Review: Gossypol-A polyphenolic compound from cotton plant. Advances in Food and Nutrition Research. 2009, 58, chapter 6, p213- ...
Primary mitochondrial activity of gossypol in yeast and mammalian cells. Biochem. Pharmacol.37:4217-4224. ... Antimicrobial activity of aerial parts of Drosera peltata Smith on oral bacteria. J. Ethnopharmacol.60:91-96. ... Wild-type strain EC16, as well as the tolC mutant strain, was resistant to relatively high levels (,2 mg/ml) of gossypol, a ... Activity of anthraquinonic and naphthoquinonic compounds on oral bacteria. Pharmazie49:681-683. ...
Design and synthesis of a gossypol derivative with improved antitumor activities. Arch. Pharm. Chem. Life Sci. 342, 223-229. ... 2015). In vitro and in vivo anticancer activity of root extracts of Sansevieria liberica Gerome and Labroy (Agavaceae). Evid. ... 2015). Antiproliferative activity of flavonoids from croton sphaerogynus Baill (Euphorbiaceae). Biomed Res. Int. 2015, 1-7. doi ... Batanai, M., and Stanley, M. (2015). Antiproliferative activity of T welwitschii extract on Jurkat T cells in vitro. Biomed Res ...
Following effects of gossypol acetic acid (GA) in mice were determined in the present study: influence on the total number of ... Gossypol is a yellow polyphenolic compound from cotton plant. It has been shown to exert a potential for anti-cancer, anti- ... Hu CY, Jiang CH (1997): The biological activities and mechanisms of gossypol. Foreign Medical Sciences (Family Planning/ ... Free gossypol is the major toxic ingredient of cotton-seed meal [1]. Gossypol is generally known as a male anti-fertility and ...
1985). "Anti-implantation activity of some indigenous plants in rats". Acta Europaea Fertilitatis. 16 (6): 441-8. PMID 3832714. ... Hadley MA, Lin YC, Dym M (1981). "Effects of gossypol on the reproductive system of male rats". J. Androl. 2 (4): 190-9. doi: ... Gossypol, an extract of cotton, has been studied as a male contraceptive pill. It decreased sperm production; however this is ... Coutinho EM (Apr 2002). "Gossypol: a contraceptive for men". Contraception. 65 (4): 259-63. doi:10.1016/S0010-7824(02)00294-9. ...
Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity. ... Gossypol is a di-sesquiterpene natural-product in the form of a functionalised binaphthyl and is isolated from cotton plants. ... Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity. ... Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity. J ...
In vitro spermicidal activity of gossypol. US5527534A (en) 1996-06-18. Vaginal sponge delivery system ... This type of anti-viral activity (often called virucidal activity, even though viruses arent regarded as alive by most ... It has been known for years that surfactants such as nonoxynol and octoxynol have certain types of anti-viral activity; they ... Without intending to be bound by theory or limited to any specific cellular or biological mechanism of activity either here or ...
... gossypol acetic acid when given together with cisplatin and etoposide in treating ... To evaluate the antitumor activity of this combination per tumor measurements using the. Response Evaluation Criteria In Solid ... OUTLINE: This is a dose-escalation study of R-(-)-gossypol.. Patients receive oral R-(-)-gossypol twice daily on days 1-3, ... AT-101 (R-(-)-gossypol) when combined with cisplatin and etoposide in patients with. advanced, refractory solid tumors and/or ...
Respiratory burst activity of blood and milk neutrophils in dairy cows during different stages of lactation. Journal of Dairy ... Effects of gossypol and raffinose on lysine content and nutritive quality of proteins in meals from glandless cottonseed. ... The presence of gossypol and raffinose in cottonseed makes this protein particularly susceptible to heat damage by binding, ... These may have adverse effects on intestinal morphology, on intestinal myoelectric activity affecting the rate of passage of ...
Gossypol was found to induce a dose-dependent inhibition of invasive activity and cell viability and reduced the level of ... Moreover, (-)-gossypol treatment induced a dose-dependent inhibition of invasive activity and cell viability and reduced Bcl-2 ... The effects of (-)-gossypol on cell viability, colony formation, invasive ability and cell migration in MAT-LyLu and MLL cells ... Gossypol, a polyphenolic compound present in cottonseeds, possesses anti-proliferation and pro-apoptotic effects in various ...
65). (-)- Gossypol was found to effectively improve antitumor activity in radioresistant prostate cancer (66), breast cancer ( ... displays single-agent activity in Bcl-2-transgenic mice and has superior efficacy with less toxicity compared with gossypol ( ... which has been linked to protumor activity in chronic inflammation as well as pro-angiogenic activity (55). It has been found ... Reactive oxygen species are essential for autophagy and specifically regulate the activity of Atg4. EMBO J 2007;26:1749-60. ...
Gossypol has been shown to have an anti-HCC effect, but the underlying mechanism requires further study. In this study, we ... Resveratrol (Res), a natural phytoalexin found in a variety of plants, has significant antitumor activity. Pyruvate kinase M2 ( ... Dual effects of gossypol on human hepatocellular carcinoma via endoplasmic reticulum stress and autophagy. ...
The activity of these substances was evident on 2 levels: rate of development and weight of pupae. Gossypol and quercetin ... Secondary substances were tested: nicotine, quercetin and gossypol which are resistance factors that showed obvious activity on ... In combination with gossypol, the S-containing amino acids maintain the weight of pupae, but do not shorten development time in ... Immobilized luciferase from the fireflies luciola mingrelica change in the ph dependence of the catalytic activity and ...
Compared to (−)-gossypol, the same concentration of Gn is less active in all the cell assays tested. To increase Gn ... gossypol. We validated Gn binding to MSI1 using surface plasmon resonance, nuclear magnetic resonance, and cellular thermal ... Previously, we have shown that the natural product (−)-gossypol as the first known small molecule inhibitor of MSI1 that down- ... Synthesis of gossypol atropisomers and derivatives and evaluation of their anti-proliferative and anti-oxidant activity. Bioorg ...
  • The purpose of the present study was to determine the immunomodulatory effects of gossypol acetic acid (GA) in mice, both in vitro and in vivo . (termedia.pl)
  • Zhang, J. B., Yang, Y. Z., Yuan, J., and Xue, S. P. [Observations of in vitro fertilization capacity and the transformation of human sperm nuclei before and after administration of gossypol acetic acid]. (webmd.com)
  • 17. The method of claim 15, wherein said (-)-gossypol comprises (-)-gossypol acetic acid co-crystals. (patentsencyclopedia.com)
  • R-(-)-gossypol acetic acid - The orally bioavailable solvate of the R-(-) enantiomer of gossypol and acetic acid with potential antineoplastic activity. (wikimd.org)
  • Both DNA fragmentation by ELISA assay and caspase 3/7 activity measurement were used for demonstrating apoptosis. (nih.gov)
  • Involvement of Smac, p53, and caspase pathways in induction of apoptosis by gossypol in human retinoblastoma cells. (abcam.com)
  • Gossypol is a phenolic aldehyde extracted from plants and is known to be an antitumor agent to induce cancer cell apoptosis. (hindawi.com)
  • Importantly, proteomic and western blot analysis showed that apoptosis regulators BAK and Bax were upregulated in gossypol-treated cells, indicating that Bcl-2 associated death pathway was activated. (hindawi.com)
  • Gossypol has been identified as a BH3-mimetic (BH3 stands for Bcl-2 homology domain 3) inhibitors of antiapoptotic Bcl-2 family members, including Bcl-2, Bcl-xL, and Mcl-1, and induces apoptosis in various types of cancer [ 15 - 18 ]. (hindawi.com)
  • Gossypol is more potent than (+)-Gossypol in inhibition of cell growth and induction of apoptosis. (medchemexpress.com)
  • AT-101 is a more potent inhibitor of B cell lymphoma 2 family apoptosis-related proteins than its racemic form, gossypol, which showed preliminary clinical activity in ACC. (elsevier.com)
  • Many therapeutic agents have been proposed with robust anticancer activity capable of inducing apoptosis in cancer cells, but the mechanisms defining their mode of action remain a mystery. (nature.com)
  • Upon administration, radgocitabine is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis. (wikimd.org)
  • Gossypol family Gossypol, a natural polyphenol, and its synthetic isomer AT-101 [21, 22] are also putative pan-BH3 mimetics: they do not fully meet the criteria for a BH3 mimetic and induce apoptosis via multiple mechanisms [19, 20, 23]. (immune-source.com)
  • TW-37, a rationally designed benzoylsulphonyl analog of gossypol [22, 27], was also known to operate only in part as a pan-BH3 mimetic: it binds to BCL-2, BCL-XL and MCL-1 with moderate affinity (sub-M), induces apoptosis depending partially on BAX/BAK activation and shows several off-target effects. (immune-source.com)
  • Gossypol, in combination with zoledronic acid, may provide a rational treatment option for ovarian cancer, not only by direct inhibition of cell proliferation, but also inhibition of angiogenesis-related molecules. (nih.gov)
  • Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol", J. Biol. (patentgenius.com)
  • Molecular mechanism of gossypol-induced cell growth inhibition and cell death of HT-29 human colon carcinoma cells. (abcam.com)
  • The anti-inflammatory activity of the compound could be demonstrated on exhausting neutrophils and by preventing vasodilatation which induces inhibition of leukocyte extravasation [13]. (termedia.pl)
  • Gossypolone and apogossypolone were more effective fungal growth inhibitors than gossypol, with the former producing 100% inhibition in all fungi tested except A. flavus. (usda.gov)
  • Apogossypolone displayed the most potent antiaflatoxigenic activity of the tested compounds, yielding greater than 94% inhibition in A. flavus and greater than 65% inhibition in A. parasiticus. (usda.gov)
  • Racemic gossypol and derivatives gossypolone and apogossypolone demonstrated significant growth inhibition against a diverse collection of filamentous fungi that included Aspergillus flavus, A. parasiticus, A. alliaceus, A. fumigatus, Fusarium graminearum, F. moniliforme, Penicillium chrysogenum, P. corylophilum and Stachybotrys atra. (usda.gov)
  • Racemic gossypol and apogossypolone induced growth inhibition values of up to 95%, whereas gossypolone effected 100% growth inhibition in all fungal isolates except A. flavus. (usda.gov)
  • In addition, Smac/Diablo is released and can block IAP inhibition of caspase activity. (sigmaaldrich.com)
  • Analysis of the kinetic parameters showed gossypol to inhibit two fragments of the mitochondrial electron transfer chain: a) between coenzyme Q and cytochrome b with K IIIi of 118.3 μM (inhibition by the noncompetitive type), and b) at the level of exogenous NADH dehydrogenase with of K Ii 17.2 μM (inhibition by the mixed type). (openbiochemistryjournal.com)
  • Kennedy WP, Vander Ven HH, Straus JW, Bhattacharya AK, Waller DP, Zaneveld LJD, Polakoski KL (1983) Gossypol inhibition of acrosin and proacrosin and oocyte penetration by human spermatozoa. (thefreedictionary.com)
  • A variety of lactate dehydrogenases are found throughout the body and gossypol exerts a degree of inhibition on many of these. (diff.org)
  • 1960). Later Chinese scientists demonstrated that administration of gossypol to males in humans and rats a t a low concentration (5-10 mg/kg) for several weeks results in inhibition of spermatogenesis, which leads to infertility without significant toxic effects (National Coordinating Group on Male Fertility, 1978). (docme.su)
  • YU, T. W. [Ultrastructural study of the testis in 22 persons based on the effect of gossypol]. (webmd.com)
  • This work studied the effect of gossypol on the mitochondrial respiratory chain of Yarrowia lipolytica . (openbiochemistryjournal.com)
  • 1970). Oral administration of gossypol was found to stimulate liver microsomal oxidative activity and concomitantly the ability to dealkylate carbaryl (Abou-Donia and Dieckert, 1971). (inchem.org)
  • 1981). In studies of antifertility induced by gossypol, administration of gossypol at 80 mgkg on each of the 3 days prior to expected ovulation failed to inhibit ovulation in the female rat (Hahn et al. (docme.su)
  • 1980) also reported that in the female mouse administration of gossypol a t 40-80 mgikg during days 1-13 of pregnancy results in nonviable offspring (26-100% of the litters). (docme.su)
  • We have previously reported that intramuscular administration of gossypol to normally cycling female rats induces an irregularity of the cyclic pattern for as long as the treatment is continued (Lin et al. (docme.su)
  • 1985).Furthermore, administration of gossypol from days 0 (day of if-) 1985 ALAN R. LISS, INC sperm-positive vaginal smear) to 8 of pregnancy results in the absence of implantation sites as determined by laparotomy. (docme.su)
  • More recently, significant attention has been focused on the potential therapeutic value of gossypol as a promising starting point for the development of antitumor or antiviral derivatives for medicinal applications with enhanced bioactivity and reduced side effects [ 14 - 18 ], in which the aldehyde groups are altered to give gossypol derivatives (e.g. (hindawi.com)
  • Study on chemical constituents and antitumor activity of Oxytropic falcata . (springer.com)
  • Resveratrol (Res), a natural phytoalexin found in a variety of plants, has significant antitumor activity. (sigmaaldrich.com)
  • To evaluate the antitumor activity of this combination per tumor measurements using the Response Evaluation Criteria In Solid Tumors (RECIST) criteria. (knowcancer.com)
  • Apogossypolone (ApoG2), a novel derivative of gossypol, exhibits superior antitumor activity in Bcl-2 transgenic mice, and induces autophagy in several cancer cells. (ku.edu)
  • Zoledronic acid has robust antitumor and antiangiogenic activity and merits further clinical development as ovarian cancer treatment. (aacrjournals.org)
  • Identification of a novel potential antitumor activity of gossypol as an APE1/Ref-1 inhibitor. (hellobio.com)
  • Rabusertib binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. (wikimd.org)
  • Moreover, it may be suggested that the antitumor activity of Lonidamine is enhanced if it is used in combination with other drugs and/or treatments, such as hyperthermia, which modify the energy status of mitochondria. (elsevier.com)
  • However, the application of gossypol as a therapeutic agent has been limited because of a number of serious side effects [ 13 ] that have been shown to be associated with the aldehyde groups. (hindawi.com)
  • Synthesis of mono-aldehyde gossypol and its analogues", Yao Xue Xue Bao, 22:597-602 (1987). (patentgenius.com)
  • Gossypol, a phenolic aldehyde extracted from the cotton and the tropical plants, can permeate cells. (hindawi.com)
  • Gossypol forms an extensive hydrogen bonding network with residues Arg146 and Asn143 in Bcl-2 through the aldehyde group and the adjacent hydroxyl group on the right naphthalene ring [ 14 ]. (hindawi.com)
  • Gossypol is a terpenoid aldehyde, which is formed metabolically through acetate via the isoprenoid pathway. (diff.org)
  • Gossypol is polyphenolic aldehyde, a toxic substance naturally present in cotton plant to protect it from insects, pests and diseases. (sciendo.com)
  • We have successfully used RNAi to disrupt gossypol biosynthesis in the seed by interfering with the expression of the o-cadinene synthase gene during embryo development. (usda.gov)
  • Gossypol was an ineffectual inhibitor of aflatoxin biosynthesis in both A. flavus and A. parasiticus. (usda.gov)
  • Biosynthesis of Gossypol. (diff.org)
  • The biosynthesis of gossypol is summarized in figure below. (diff.org)
  • And both glanded and glandless cotton roots had the ability of gossypol biosynthesis. (biomedcentral.com)
  • But the pigment glands, the main storage of gossypol, had indirect effects on gossypol biosynthesis. (biomedcentral.com)
  • In vitro culture of root and rootless seedling confirmed the strong gossypol biosynthesis ability in root system and the relatively weak gossypol biosynthesis ability in other organs of the seedling. (biomedcentral.com)
  • Expression profiling of the key genes involved in the gossypol biosynthetic pathway also supported the root as the major organ of gossypol biosynthesis. (biomedcentral.com)
  • Gossypol biosynthesis is not directed related to the expression of pigment glands, but the presence of pigment glands is essential for gossypol accumulation. (biomedcentral.com)
  • Zavos, P. M. and Zarmakoupis-Zavos, P. N. The inhibitory effects of gossypol on human sperm motility characteristics: possible modes of reversibility of those effects. (webmd.com)
  • Supplementation with acornhination ofexogenousprogesterone and estradiol 17p eliminates the inhibitory effects of gossypol on the maintenance of pregnancy (Lin et al. (docme.su)
  • Many of these derivatives exhibit a variety of unusual disease-inhibiting activities, especially anticancer activity [ 19 ]. (hindawi.com)
  • R)-Gossypol is more toxic and exhibits significantly greater anticancer activity than the (+)-(S)-atropisomer. (biomedsearch.com)
  • Structure-activity studies on gossypol in tumor cell lines," Anticancer Drugs, 11:209-216 (2000). (patentgenius.com)
  • Exhibits a wide range of biological effects including anticancer and antifertility activity. (abcam.com)
  • Anticancer activities of constituents from the stem oiPolyalthia rumphii . (springer.com)
  • Exhibits multiple biological effects including antifertility and anticancer activity. (timtec.net)
  • Like obatoclax, they showed limited anticancer activity in clinical trials [15]. (immune-source.com)
  • In haematopoietic cell system, the agents which inhibit PKC activity can suppress the growth of both normal and leukemic progenitors [10]. (termedia.pl)
  • It has been shown to inhibit the reverse transcriptase activity of human immunodeficiency virus (HIV) ( 31 ) and to protect mice challenged with Chlamydia trachomatis ( 22 ). (asm.org)
  • While several approaches were considered to selectively inhibit Bcl-2 family anti-apoptotic proteins, the discovery that gossypol binds and antagonizes anti-apoptotic effect of Bcl-2 family proteins was a major breakthrough in identifying specific Bcl-2 antagonists. (springer.com)
  • Acrosin antibodies present in the sera of infertile women inhibit spermzona pellucida binding through protease activity (8). (thefreedictionary.com)
  • Oxamic acid did not inhibit PfMDH, while gossypol, which interacts at the nucleotide binding site of oxido-reductases and shows antimalarial activity, inhibited PfMDH also. (elsevier.com)
  • 12 13 Hemoglobin, gossypol, and arginine analogues, such as nitro- l -arginine, inhibit NO-mediated relaxations but do not alter EDHF. (ahajournals.org)
  • Higher concentrations inhibit the enzyme activity. (elsevier.com)
  • Total and percent atropisomers of gossypol and gossypol-6-methyl ether in seeds from pima cottons and accessions of Gossypium barbadense L. (biomedsearch.com)
  • Gossypol occurs naturally in the seed, foliage, and roots of the cotton plant ( Gossypium ) as atropisomers due to restricted rotation around the binaphthyl bond. (biomedsearch.com)
  • Most commercial Upland ( Gossypium hirsutum ) cottonseeds have an (R)- to (S)-gossypol ratio of approximately 2:3, but some Pima ( Gossypium barbadense ) seeds have an excess of (R)-gossypol. (biomedsearch.com)
  • [25] However, the compound isolated from Gossypium , as well as other cotton seeds and okra ( gossypol ) has been abandoned for contraceptive use because it was found to cause permanent infertility in ten to twenty percent of users. (wikipedia.org)
  • Gossypol is a yellow polyphenolic compound originally isolated from seeds and roots of the cotton plant (Gossypium sp. (termedia.pl)
  • Gossypol is a yellow pigment derived from cotton seeds (Gossypium genus, Malvaceae). (diff.org)
  • Gossypol is a polyphenol of two naphthalenes, deriving from the plant pigment glands of the cotton genus Malvaceae gossypium . (ajas.info)
  • Gossypol is a specific secondary metabolite in Gossypium species. (biomedcentral.com)
  • S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity. (medchemexpress.com)
  • Gossypol and (-)-Gossypol binds to Bcl-2 or Bcl-xL with similar binding affinities. (medchemexpress.com)
  • Upon oral administration, the RAD51 inhibitor CYT-0851 targets, binds to and inhibits the activity of RAD51. (wikimd.org)
  • AT101 [R-(-)-enantiomer of gossypol] is an orally available and well-tolerated natural BH3-mimetic that activates Bax and also induces mitochondrial Smac release. (sigmaaldrich.com)
  • In vitro effects of the BH3 mimetic, (-)-Gossypol, on head and neck squamous cell carcinoma cells. (medchemexpress.com)
  • It is now known that obatoclax does not meet the two main criteria defining an authentic BH3 mimetic and that its proapoptotic activities result from off-target mechanisms [19, 20]. (immune-source.com)
  • Most importantly, the levels of gossypol and related terpenoids that are derived from the same pathway were not diminished in the foliage and floral parts of these plants and thus remain available for defense against insects and diseases. (usda.gov)
  • Cotton plants contain high levels of gossypol that provides protection against insect predation and possibly additional defense functions. (usda.gov)
  • Most relevant, the levels of gossypol and related terpenoids in the foliage and floral parts were not diminished, and thus their potential function in plant defense against insects and diseases remained untouched. (pnas.org)
  • Lonidamine does not affect state 4 respiration, but in the presence of gossypol, it determines a marked decrease in the rate of oxygen consumption. (elsevier.com)
  • Twelve known compounds, including eight alkaloids, three lignans and one gossypol derivative, were isolated from the branches of Polyalthia rumphii (Blume ex Hensch. (springer.com)
  • Stability and antioxidant activity of gossypol derivative immobilized on N-polyvinylpyrrolidone. (semanticscholar.org)
  • The immobilization of gossypol derivative on N-polyvinylpyrrolidone increases its water solubility and modifies membrane-active properties. (semanticscholar.org)
  • The conjugate of the gossypol derivative megosin (1) with N-polyvinylpyrrolidone named rometin (2) was synthesized. (semanticscholar.org)
  • apogossypolone is another oxidative derivative of gossypol. (usda.gov)
  • Stahelin H (1973) Activity of a new glycosidic lignan derivative (VP 16-213) related to podophyllotoxin in experimental tumors. (springer.com)
  • Synthesis and antifertility actions of gossypol derivatives and phenol aldehydes", Yao Xue Xue Bao, 24:502-511 (1989). (patentgenius.com)
  • Antifertility, spermicidal and ultrastructural effects of gossypol and derivatives administered orally and by intratesticular injections", Contraception, 37:301-331 (1988). (patentgenius.com)
  • Synthesis and in vitro spermicidal activity of isomeric hemigossypol derivatives", Experientia, 39:1276-1277 (1983). (patentgenius.com)
  • Synthesis and antifertility actions of gossypol derivatives and phenol aldehydes. (springer.com)
  • Gossypol and its derivatives - syntheses, spectroscopic investigations and biological tests. (wikipedia.org)
  • Derivatives of phenol, called phenolics, contain a molecule of phenol that has been altered chemically to reduce its ability to irritate and/or to increase its antimicrobial activity. (thefreedictionary.com)
  • Free gossypol is the major toxic ingredient of cotton-seed meal [1]. (termedia.pl)
  • The crude protein (CP), total gossypol (TG), and free gossypol (FG) were determined in CSM after fermentation with isolated strain at 39°C for 72 h. (ajas.info)
  • It is a secondary metabolite in cottonseed, found as either bound gossypol (BG) or free gossypol (FG). (ajas.info)
  • Also related to the mechanism of action, (−)-gossypol has been reported to target Bcl-2, Bcl-xL, and Mcl-1 proteins with high affinities and is now in clinical trials as an orally administered agent for the treatment of several types of human cancer [ 21 , 22 ]. (hindawi.com)
  • Quantitative proteomic analysis was carried out to identify differentially expressed proteins between untreated and gossypol-treated cells. (hindawi.com)
  • Proteomic analysis identified 4330 proteins, in which 202 proteins are upregulated and 383 proteins are downregulated in gossypol-treated cells as compared to the untreated cells. (hindawi.com)
  • Similarly, gossypol also induced upregulations of DNA mismatch repair proteins and DNA replication licensing factor, suggesting that gossypol caused significant DNA damage. (hindawi.com)
  • 17-AAG inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185 erB2 . (sigmaaldrich.com)
  • Additionally, activity and localization of calcineurin is modulated by endogenous proteins, such as RCANs, Cabin1 or AKAP79. (biomedcentral.com)
  • Several autophagy-related proteins have tumor suppressor activity (Beclin 1, Atg5, Bif-1, Atg4C, UVRAG) and some autophagy gene mutations can lead to an accumulation of DNA damage and genome instability. (ac.ir)
  • These accessions may be useful in a breeding program to reduce (R)-gossypol in Pima seed, which is a concern to the dairy industry because of the toxicity and male antifertility activity of this atropisomer. (biomedsearch.com)
  • Yu, Y. W. Probing into the mechanism of action, metabolism and toxicity of gossypol by studying its (+)- and (-)-stereoisomers. (webmd.com)
  • Although parent compound gossypol did not sustain in the clinic, its structural modifications led to the development of additional analogues that demonstrated improved efficacy and reduced toxicity in preclinical and clinical investigations. (springer.com)
  • However, due to the toxicity of gossypol for human beings and monogastric animals, the consumption of cottonseeds was limited. (biomedcentral.com)
  • Focusing on the benefit of different therapeutic strategies, this article reviews recent advancements, the most effective therapy combinations and potential activity of novel agent in the treatment of CLL. (springermedizin.de)
  • Therapeutic potential of gossypol: an overview. (hellobio.com)
  • Conclusions AT-101 had no meaningful clinical activity in this study in patients with advanced ACC, but demonstrated feasibility of prospective therapeutic clinical trials in this rare cancer. (elsevier.com)
  • The therapeutic activity of navitoclax in patients with hematologic malignancies (particularly chronic lymphocytic leukemia) and some solid cancers is now well established [15, 16]. (immune-source.com)
  • However, gossypol, a toxic terpenoid present in the glands, renders cottonseed unfit as food and as feed for non-ruminant animals. (usda.gov)
  • however, it is woefully underutilized because of the presence of toxic gossypol within seed glands. (pnas.org)
  • however, the glandless varieties were commercially unviable because of the increased susceptibility of the plant to insect pests due to the systemic absence of glands that contain gossypol and other protective terpenoids. (pnas.org)
  • Gossypol and related terpenoids are present throughout the cotton plant in the glands of foliage, floral organs, and bolls, as well as in the roots. (pnas.org)
  • Stenberg (1970) reported that 0.7 mg/kg administered orally for 3-1/2 months induced tension and stimulation of the thyroid activity (increase of PSI, thyroid weight increase, and proliferation of colloid content of RNA). (inchem.org)
  • Rad51 inhibitor cyt-0851 - An orally bioavailable inhibitor of the DNA damage repair protein RAD51, with potential antineoplastic and sensitizing activities. (wikimd.org)
  • phenol coefficient a measure of the bactericidal activity of a chemical compound in relation to phenol. (thefreedictionary.com)
  • The activity of the compound is expressed as the ratio of dilution in which it kills in 10 minutes but not in 5 minutes under the specified conditions. (thefreedictionary.com)
  • High levels of 5AR activity gossypol, a compound that has use need abuse, as they are easy to obtain. (furoshiki.com)
  • This compound goes through various oxidative processes to make deoxyhemigossypol which is oxidized by one-electron into hemigossypol and then undergoes a phenolic oxidative coupling ortho to the phenol groups to form gossypol. (diff.org)
  • Gossypol is a nonsteroidal compound that inhibits sperm production and motility in a variety of male animals and in humans. (diff.org)
  • Racemic gossypol is a polyphenolic compound isolated from cottonseed. (wikimd.org)
  • 5'-diisopropyl3, Gossypol [1,1t,6,6',7,7'-hexahydroxy-5, 3 '-dimethyl-(2,2'-binaphthalene)-8,8'-dicarboxaldehyde] is a yellow phenolic compound (518.5 MW) found in the cotton plant that is especially concentrated in the seed. (docme.su)
  • Gossypol was originally studied as a toxic compound in cotton seed meal used for feeding livestock (Adams et al. (docme.su)
  • Gossypol: a contraceptive for men. (hellobio.com)
  • Gossypol has been used as oral contraceptive for man in People's Republic of China. (thenakedscientists.com)
  • In this study we used tablet preparation of gossypol, which is actually used as oral contraceptive for male in People's Republic of China, on a volunteer. (thenakedscientists.com)
  • Our study suggests gossypol may be effective as a male oral contraceptive with no acute side effect. (thenakedscientists.com)
  • Gossypol exerts its contraceptive action by inhibiting an enzyme that plays a crucial role in energy metabolism in sperm and spermatogenic cells. (diff.org)
  • Results from enzyme activity and molecular analyses on developing embryos were consistent with the observed phenotype in the mature seeds. (usda.gov)
  • A number of attempts have been made using different solvents to extract gossypol from the seeds. (sciendo.com)
  • Since proton affinities (PAs) are much lower than the bond dissociation enthalpies (BDEs) of phenolic hydrogens, we consider that direct antioxidant activity in these species is mainly due to the sequential proton loss electron transfer (SPLET) mechanism. (frontiersin.org)
  • Further investigation revealed that the antifertility component was gossypol, a potentially toxic phenolic pigment found in the seed, stem, and root of the cotton plant. (diff.org)
  • The racemic form and each of the enantiomers of Gossypol are tested against UM-SCC-6 and UM-SCC-14A in 6-day MTT assays. (medchemexpress.com)
  • The effect of the association of gossypol and Lonidamine on the electron transport in Ehrlich ascites tumor mitochondria has been investigated by addition of drugs to isolated mitochondria. (elsevier.com)
  • Monkey lactate dehydrogenase-C4 as a model for the interaction of enzymes with gossypol", Contraception, 33:605-616 (1986). (patentgenius.com)
  • 0.05) improve the VCL-decreased semen quality and improved the sperm DNA integrity and chromatin condensation.Conclusion:Our data suggest that Vit E by up-regulating the antioxidant status and DEX by reducing inflammation-dependent oxidative and nitrosative stresses could improve the VCL-reduced Hsp70-2 chaperone expression and ultimately protected the testicular endocrine activities and promoted the spermatogenesis process. (bvsalud.org)
  • These activities augment lactate production, albeit to a lesser extent than the lactate derived from glucose catabolism. (jci.org)
  • LDH -X, an isoenzyme of lactate dehydrogenase specific for germinal epithelium activity, has been measured in the seminal plasma of infertile subjects whose infertility had different origins. (diff.org)
  • Gossypol: prototype of inhibitors targeted to dinucleotide folds. (abcam.com)
  • Research regarding the biological effects of gossypol both in vitro and in vivo showed that the (−)-enantiomer is more potent than the (+)-enantiomer or the racemic mixture (1) [ 20 ]. (hindawi.com)
  • Intrigued by this observation, we synthesized and evaluated new (−)-gossypol hydrazones for their cytotoxic effects against three human cancer cell lines. (hindawi.com)
  • In the present study, we aimed to evaluate the possible synergistic, cytotoxic effects of combination treatment of gossypol and zoledronic acid, in human ovarian cancer cell lines, OVCAR-3 and MDAH-2774, and to elucidate the role of this novel combination treatment on angiogenesis-related molecules in ovarian cancer. (nih.gov)
  • Kinetic patterns of megosin and gossypol effects on properties of highly purified Na+, K+-ATPase were studied. (semanticscholar.org)
  • Dual effects of gossypol on human hepatocellular carcinoma via endoplasmic reticulum stress and autophagy. (sigmaaldrich.com)
  • An investigation was undertaken to determine effects of these gossypol related compounds on fungal growth in a collection of agriculturally important filamentous fungi that included both plant and human pathogens. (usda.gov)
  • The aim of this study was to evaluate the in vivo activity of the anti-inflammatory and analgesic effects of a suspension of the complex composed of dexamethasone acetate (DMA) with β-cyclodextrin in comparison to a suspension of the pure DMA. (scielo.br)
  • Yu, Z. H. and Chan, H. C. Gossypol as a male antifertility agent--why studies should have been continued. (webmd.com)
  • Gossypol prolongs skin allograft survival in mice without affecting the bone marrow function [14]. (termedia.pl)
  • Considering the requirement of AR signaling to drive prostate growth and survival, and because CRPC still retains AR activity, in this study we explored the impact of tubulin and microtubule-targeting drugs on AR signaling in prostate cancer. (aacrjournals.org)
  • Two representative UM-SCC cell lines, UM-SCC-6 and UM-SCC-14A , are continuously exposed to 0 (vehicle control), 5 or 10 μM (±)-Gossypol, (-)-Gossypol or (S)-Gossypol ((+)-Gossypol) in a 6-day MTT cell survival assay [1] . (medchemexpress.com)
  • Gn is a major metabolite of gossypol [ 44 ], and is oxidized in the liver by P450 enzyme [ 45 ]. (biomedcentral.com)
  • Gossypol, a cotton metabolite, was found to be the agent probably responsible for most of the surface activity of cotton dusts. (cdc.gov)
  • The natural racemic Gossypol has two enantiomers, namely the (-)-Gossypol and (S)-Gossypol ((+)-Gossypol) enantiomers. (medchemexpress.com)
  • There are two different enantiomers of gossypol, (+)-gossypol and (−)-gossypol. (biomedcentral.com)
  • Le Blanc et al, "An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines", Pharmacol. (patentgenius.com)
  • In the present study, multiple myeloma cells were treated with gossypol, which resulted in an increase of cellular reactive oxygen species (ROS) and cell necrosis. (hindawi.com)
  • Gossypol has been shown to have an anti-HCC effect, but the underlying mechanism requires further study. (sigmaaldrich.com)
  • OUTLINE: This is a dose-escalation study of R-(-)-gossypol. (knowcancer.com)
  • The aim of the study was to isolate gossypol-degrading bacteria and to assess its potential for gossypol degradation. (ajas.info)
  • In this study, we found that cotyledon was the primary source of gossypol at the seed germination stage. (biomedcentral.com)
  • Our study provide evidence that the cotton root system is the major source of gossypol in both glanded and glandless cottons, while other organs have a relatively weak ability to synthesize gossypol. (biomedcentral.com)
  • In this study ethanol has been used as the solvent at temperature below 323K for removal of gossypol from the defatted seed. (sciendo.com)
  • The aim of the present study was to evaluate the wound healing activity and phytochemical screening of Thespesia populnea barks extract. (ukjpb.com)
  • After extraction of oil from the cottonseed, the defatted cottonseed meal which contains both the gossypol and proteinous matter is left behind. (sciendo.com)
  • Gossypol is also reported to be a small-molecule Bcl-2 inhibitor [7] and nonspecific protein kinase C (PKC) inhibitor [8]. (termedia.pl)
  • Previously, we have shown that the natural product (−)-gossypol as the first known small molecule inhibitor of MSI1 that down-regulates Notch/Wnt signaling and inhibits tumor xenograft growth in vivo. (biomedcentral.com)
  • Similarly, an Mcl-1 small-molecule inhibitor synergized with MDA-7/IL24 and induced robust antibone metastatic activity. (aacrjournals.org)
  • Maximum gossypol is concentrated in the seed. (sciendo.com)
  • Gossypol was first identified as an antifertility agent as a result of epidemiologic studies conducted in China during the 1950s. (diff.org)
  • We demonstrate that it is possible to reduce significantly the levels of cottonseed-gossypol in a stable and heritable manner. (usda.gov)
  • It was recently shown that, when tested in cellular systems, quercetin oxidized products (Qox) have significantly better antioxidant activity than quercetin (Q) itself. (frontiersin.org)
  • Thus, gossypol-free cottonseed would significantly contribute to human nutrition and health, particularly in developing countries ( 3 - 5 ), and would help meet the requirements of the predicted 50% increase in the world population in the next 50 years. (pnas.org)
  • Serum progesterone and estradiol 176 values in normally cycling and pregnant rats treated with gossypol were significantly lower than control levels. (docme.su)
  • Moreover, the protein kinase, Akt, can be activated by various growth factors and its activity can be blocked by PTEN. (sigmaaldrich.com)
  • Gossypol can be detected in various products weak anabolic activity of Methenolone (its dose of testosterone for 4-8 and protein supplements. (gomiso.com)
  • Standardised extract of Bacopa monniera (CDRI-08) improves contextual fear memory by differentially regulating the activity of histone acetylation and protein phosphatases (PP1α, PP2A) in hippocampus. (thegoodscentscompany.com)
  • The similarities found between the kinetics parameters and other properties of the Ca(2+)-ATPase and the Ca2+ transport activity strongly suggest a common molecular entity. (bvsalud.org)
  • 3) The addition of gossypol to mitochondria respiring on pyruvate plus malate or succinate induces a more oxidized state of NAD + and cytochrome b, respectively. (elsevier.com)
  • The antiprotozoal activity of the methanol extract and its fractions were evaluated comparing growth in cultures with and without extracts. (scirp.org)
  • The methanol extract fraction containing ursolic acid obtained from Thymus vulgaris has antiprotozoal activity against G. lamblia and T. vaginalis trophozoites. (scirp.org)
  • Evidence for involvement of the monoaminergic system in antidepressant-like activity of an ethanol extract of Boerhaavia diffusa and its isolated constituent, punarnavine, in mice. (thegoodscentscompany.com)
  • Excision wound models were used to evaluate the wound healing activity of extract. (ukjpb.com)
  • 2) Gossypol, at concentrations at which it exerts its uncoupling effect, stimulates ATPase activity. (elsevier.com)
  • Combined gossypol and zoledronic acid treatment results in synergistic induction of cell death and regulates angiogenic molecules in ovarian cancer. (nih.gov)
  • Treatment of a synchronized culture of P. falciparum trophozoites with gossypol caused induction in expression of PfMDH, while expression of PfLDH was reduced and expression of malate:quinone oxidoreductase remained unchanged. (elsevier.com)
  • Gossypol is now in phases II and IIb clinical trials for hormone-refractory prostate cancer and other types of cancer including lung cancer, breast cancer, and ovarian cancer with promising initial results [ 19 , 20 ]. (hindawi.com)
  • Marinopyrrole A (Maritoclax) is a potent and selective inhibitor of Bcl-2 family member Mcl-1, originally isolated from marine streptomycetes for its antimicrobial activity against methicillin-resistant Staphylococcus aureus . (sigmaaldrich.com)
  • carbolic acid, C6H5OH, which has been used as an antiseptic and DISINFECTANT because of its antimicrobial activity. (thefreedictionary.com)