387485961 - EP 0943620 A3 2001-02-07 - Betulinic acid derivatives for inhibiting cancer growth - [origin: EP0943620A2] The invention relates to use of betulinic acid and/or its derivatives for treating, inhibiting, and/or preventing tumors or cancer growth more particularly, to treating leukemia, lymphomas, lung, prostate and ovarian cancer. This invention also relates to novel betulinic acid derivatives and a composition containing betulinic acid derivatives with or without betulinic acid. IMAGE [origin: EP0943620A2] The invention relates to use of betulinic acid and/or its derivatives for treating, inhibiting, and/or preventing tumors or cancer growth more particularly, to treating leukemia, lymphomas, lung, prostate and ovarian cancer. This invention also relates to novel betulinic acid derivatives and a composition containing betulinic acid derivatives with or without betulinic acid. IMAGE
Global ursolic acid market is anticipated to post a remarkable CAGR during the forecast period i.e. 2017-2024. Moreover, the global ursolic acid market is projected to reach noteworthy revenue by the end of 2024. Additionally, massive adoption of ursolic acid by pharmaceutical industry is one of the key growth drivers of global ursolic acid market.. In terms of geography, North America and Asia-Pacific are the notable regional markets of ursolic acid. Further, North America ursolic acid market is driven by various factors such as growing adoption of ursolic acid on the back of fitness and health concern. In North America, U.S. is the major contributor in the market of ursolic acid due to presence of large pharmaceutical and dietary supplement industry. Apart from this, Asia-Pacific region is believed to showcase tremendous growth over the forecast period owing to rising health awareness among the population along with rising per capita income support the population to spend more on healthcare. ...
Novel anti-HIV-1 agents derived from betulinic acid have been greatly concerned. 3D-QSAR and molecular docking studies were applied to rationalize the structural requirements responsible for the anti-HIV activity of these compounds. The CoMFA and CoMSIA models resulted from 28 molecules gave rcv² values of 0.599 and 0
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In the study of triterpene derivatives as potent anti-HIV agents, different C-3 conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized in order to explore the conformational space of the C-3 pharmacophore. 3-O-Monomethylsuccinyl-betulinic acid (MSB) analogues were also designed to better understand the contribution of the C-3 dimethyl group of bevirimat (2), the first-in-class HIV maturation inhibitor, which is currently in phase IIb clinical trials. In addition, another triterpene skeleton, moronic acid (MA, 3), was also employed to study the influence of the backbone and the C-3 modification toward the anti-HIV activity of this compound class, may lead to led to the design and synthesis of compound 12 (EC(50): 0.0006 microM), which displayed slightly better activity than 2 as a HIV-1 maturation inhibitor, according to Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as ...
Human immunodeficiency virus type 1 resistance to the small molecule maturation inhibitor 3-O-(3,3-dimethylsuccinyl)-betulinic acid is conferred by a variety of single amino acid substitutions at the CA-SP1 cleavage site in Gag.
The report generally describes ursolic acid acetate, examines its uses, production methods, patents. Ursolic acid acetate market situation is overviewed;
We demonstrate that hopanoids can determine order in the bacterial OM through their interaction with lipid A, analogous to the interaction of cholesterol with sphingolipids in eukaryotic plasma membranes. Hopanoids have been identified in the OM of diverse bacteria (29, 43⇓⇓-46), and two recent studies have reported a covalently linked hopanoid-lipid A compound in rhizobial plant-associated bacteria (47, 48). These observations suggest that hopanoid-lipid A ordering may be widespread among hopanoid-producing bacteria. Interestingly, hopanoids have also been observed in association with other specialized membranes, such as the thylakoid membranes in cyanobacteria and in the vesicle envelope of the root nodule symbionts Frankia spp. (44, 45, 49, 50). The exact role of hopanoids in these diverse bacterial membranes is not fully understood. Furthermore, bacteria that lack hopanoids may use other, possibly unknown, ordering lipids in their membranes. For instance, it has been shown that Borrelia ...
Triterpenes are a class of chemical compounds composed of three terpene units with the molecular formula C30H48; they may also be thought of as consisting of six isoprene units. Animals, plants and fungi all create triterpenes, with arguably the most important example being squalene as it forms the basis of almost all steroids. Triterpenes exist in a huge variety of structures with nearly 200 different skeletons known from natural sources or enzymatic reactions. These may be broadly divided according to the number of rings present; although in general pentacyclic structures (5 rings) tend to dominate. By definition triterpenes are hydrocarbons and possess no heteroatoms; functionalized triterpenes should instead be called triterpenoids. However this distinction is not always adhered to in scientific literature, with the two terms triterpene and triterpenoid often being used interchangeably. Triterpenoids possess a rich chemistry and pharmacology (e.g. cholesterol) with several pentacyclic ...
The results of this research, recently published in the renowned PloS ONE magazine, show without a doubt how maslinic acid is capable of early inducing the extrinsic cellular death pathway in Caco-2 cells that dont express protein p53 (known by its pro-apoptotic capacity).. Said research has been lead by professors José Antonio Lupiáñez Cara and Andrés Parra Sánchez from the University of Granada, Marta Cascante Serratosa from the University of Barcelona, and Juan Peragón Sánchez from the University of Jaen.. In previous works, professor Lupiáñez Caras research team had reported that maslinic acid induces apoptotic cell death via the mitochondrial apoptotic pathway in cancer cell lines.. In the paper published in PloS ONE, the researchers have shown that MA induces apoptosis in Caco-2 colon cancer cells via the extrinsic apoptotic pathway in a dose-dependent manner in the short term (4 hours).. A quick response. Maslinic acid triggers a series of effects associated with apoptosis and ...
TY - JOUR. T1 - Apoptosis as the basic mechanism of cytotoxic action of ursolic and pomolic acids in glioma cells. AU - Frolova, T. S.. AU - Lipeeva, A. V.. AU - Baev, D. S.. AU - Tsepilov, Y. A.. AU - Sinitsyna, O. I.. PY - 2017/9/1. Y1 - 2017/9/1. N2 - Pentacyclic triterpene acids are of great interest as compounds that exhibit selective cytotoxicity against malignant tumor cells. If earlier studies were carried out mainly in cancer cells of epithelial origin, in the present work the cytotoxic effect of ursolic and pomolic acids on the primary and permanent glioma cell lines was analyzed. Both compounds are toxic to oncotransformed cells and induce apoptosis in U-87 MG line. Using molecular docking, it has been shown that Akt1 and MDM2 may be potential targets of the studied triterpene acids. It has been suggested that ursolic and pomolic acids induce apoptosis in glioma cells through inhibition of the PI3K/Akt signaling pathway, and they can be considered as potentially promising agents for ...
Idea Proposed/Formulated by:Dr L Boominathan Ph.D.. Terms & Conditionsapplyhttp://genomediscovery.org/registration/terms-and-conditions/. Citation:Boominathan, Natural product-based therapy for p53-mutated human cancers: Ursolic acid increases the expression of tumor suppressor p53 homologue TAp63 via down regulation of its target gene, 4/March/2015, 8.31 am,Genome-2-Bio-MedicineDiscovery center(GBMD),http://genomediscovery.org. Significance:This study suggests, for the first time, that Ursolic acid,by decreasing the expression of its target gene,it may increase the expression of TAp63. Thereby, it may inhibit cancer progression.Thus,pharmacological formulationsencompassingUrsolic acid or its analogues can be used to inhibit the progression of human tumors.. Amount: $ 300*. Undisclosed information:How Ursolic acidincreases the expression ofTAp63. Web:http://genomediscovery.org. Courtesy:When you cite drop us a line [email protected] * Research cooperation. ...
Kvasnica, M., Urban, M., Dickinson, N. J., Sarek, J. Pentacyclic triterpenoids with nitrogen- and sulfur-containing heterocycles: synthesis and medicinal significance. Nat Prod Rep. 2015 Jun 1. PubMed PMID: 26030604 Borkova, L., Jasikova, L., Rehulka, J., Frisonsova, K., Urban, M., Frydrych, I., Popa, I.,Hajduch, M., Dickinson, N. J., Vlk, M., Dzubak, P., Sarek, J. Synthesis of cytotoxic 2,2-difluoroderivatives of dihydrobetulinic acid and allobetulin and study of their impact on cancer cells. Eur J Med Chem. 2015 May 26, doi: 10.1016/j.ejmech.2015.03.068. Epub 2015 Apr 1. PubMed PMID: 25942059. Urban, M., Vlk, M., Dzubak, P., Hajduch, M., Sarek, J.Cytotoxic Heterocyclic Triterpenoids Derived from Betulin and Betulinic Acid. Bioorg. Med. Chem. 2012, 20, 3666. Urban, M., Sarek, J., Kvasnica, M., Tislerova, I., Hajduch, M. Triterpenoid pyrazines and benzopyrazines with cytotoxic activity. J. Nat. Prod. 2007, 70, 526. Urban, M., Klinot, J., Tislerova, I., Biedermann, D., Hajduch, M., Cisarova, I., ...
Headline: Bitcoin & Blockchain Searches Exceed Trump! Blockchain Stocks Are Next!. 2017 Deep Research Report on Global Ursolic Acid Industry published through its high quality database available at ReportsnReports.com. The report provides key statistics on the market status of the Ursolic Acid manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry.. Complete report on Ursolic Acid market spreads across 152 pages profiling 18 companies and supported with 227 tables and figures @ http://www.reportsnreports.com/contacts/discount.aspx?name=903706 . Key Companies Analysis: - Sabinsa, Sami Labs, Changsha Staherb Natural Ingredients, Run Shaanxi Days of Bio-tech, Shaanxi Huike Botanical Development, Changsha Luyuan Bio-Tech, Xuancheng Baicao Pharmaceutical, Changsha E.K HERB etc. profiles overview.. Development policies and plans are discussed as well as manufacturing processes and cost structures are also analyzed. This report also ...
TY - JOUR. T1 - Ursolic Acid attenuates HMGB1-induced LOX-1 expression in vascular endothelial cells in vitro and inhibits atherogenesis in hypercholesterolemic mice in vivo. AU - Lee, Ai-Wei. AU - Huang, Chun-Yao. AU - Shih, Chun-Ming. AU - Lin, Yi Wen. AU - Tsao, Nai-Wen. AU - Chen, Yung Hsiang. AU - Chang, Yu-Jia. AU - Chang, Nen-Chung. AU - Li, Chi Yuan. AU - Fong, Tsorng-Harn. AU - Nien, Chih Hao. AU - Lin, Feng-Yen. PY - 2012. Y1 - 2012. N2 - Ursolic acid (UA), a triterpenoid compound found in plants, is used in both the human diet and in medicinal herbs and possesses a wide range of benefits, including antioxidative and anti-inflammatory effects. Additionally, UA may inhibit lipid absorption in pancreatic cells and enhance lipolysis in adipocytes. Oxidized LDL (oxLDL) acts as a major mediator of endothelium dysfunction, which mediates atherogenesis. Until now, we have not known what role UA plays in the absorption of oxidized LDL in vascular endothelial cells. Regardless of whether UA ...
Alaska chaga tea is also notable for containing a large variety of sterols, from botulin, lanosterol, ergosterol peroxide, and many more. Sterols are naturally occurring molecules that promote healthy cell division and growth. For example, inotodiol has been shown to enhance cell division and immune system function, as well as inflammation response, as does ergosterol peroxide.. Chaga is also notable for containing betulinic acid, a sterol that is vital for cell health. The betulinic acid found in Alaska chaga is superior to the betulin found in other staple foods of the human diet due to its greater bioavailability, which comes from the fact that chaga mushrooms extract betulin from birch trees and turn it into betulinic acid. Like the previously mentioned sterols, betulinic acid is vital in aiding cell division, immune health, and inflammation response.. Polysaccharides are another beneficial substance that is found in abundance in Alaska chaga. Polysaccharides are naturally-occurring ...
In this study, the relationships between the chemical structure and cytotoxic activity of betulinic acid (1) derivatives were investigated. Eight lupane derivatives (1-8), one of them new (6), five diosphenols (9-13), four of them new (10-13), two new norderivatives (14 and 15), five seco derivatives (16-20), four of them new (16, 17, 19, and 20), and three new seco-anhydrides (21-23) were synthesized from 1, and their activities were compared with the activities of known compounds. The effects of substitution on the A-ring and esterification of the carboxyl group in position 28 on cytotoxicity were of special interest. Significant cytotoxic activity against the T-lymphoblastic leukemia cell line CEM was found in diosphenols 9 and 13 (TCS(50) 4 and 5 micromol/L) and seco-anhydrides 22 and 23 (TCS(50) 7 and 6 micromol/L). All compounds were also tested on cancer cell lines HT 29, K562, K562 Tax, and PC-3, and these confirmed activity of diosphenols 9, 10, and 11 and anhydride 22. Diosphenols, as ...
Hopanoids are pentacyclic triterpenoids produced by a wide range of bacteria. Within modern settings, hopanoids mostly occur in the biological 17 beta, 21 beta(H) configuration ...
Ursolic acid (UA), a natural pentacyclic triterpenoid carboxylic acid distributed in medical herbs, exerts antitumor effects and is emerging as a promising compound for cancer prevention and therapy, but its excise mechanisms of action in colon cancer cells remains largely unknown. Here, we identified the molecular mechanisms by which UA inhibited cell proliferation and induced apoptosis in human colon cancer SW480 and LoVo cells. Treatment with UA led to significant inhibitions in cell viability and clone formation and changes in cell morphology and spreading. UA also suppressed colon cancer cell migration by inhibiting MMP9 and upregulating CDH1 expression. Further studies showed that UA inhibited the phosphorylation of Akt and ERK proteins. Pretreatment with an Akt or ERK-specific inhibitor considerably abrogated the proliferation inhibition by UA. UA also significantly inhibited colon cancer cell COX-2 expression and PGE2 production. Pretreatment with a COX-2 inhibitor (celecoxib) abrogated ...
Chemical investigation of Maesa lanceolata leaves aqueous MeOH extract has led to the isolation of eight new triterpene glycosides identified as 16-oxo-28-hydroxyolean-12-ene 3- O - β -glucopyranosyl-(1 → 6)- β -glucopyranoside 1 , 16 α , 28-dihydroxyolean-12-ene 3 - O - β -[(6- O -galloylglucopyranosyl-(1 → 2)][ β -glucopyranosyl-(1 → 6)]- β -glucopyranoside 2, 16 α , 22 α , 28-trihydroxyolean-12-ene 3- O -[ β -glucopyranosyl-(1 → 2)] [ α -rhamnopyranosyl- (1 → 6]- β -glucopyranoside 3 , 22 α -acetyl-16 α -hydroxyolean-12-en-28-al 3- O -[ α -rhamnopyranosyl- (1  6)- β -glucopyranosyl-(1  3)] [ β -glucopyranosyl-(1  2)]- β -arabinopyranoside 4 , 22 α -acetyl-16 α ,21 β -dihydroxyoleanane-13 β :28-olide 3- O -[ β -glucopyranosyl-(1 → 6)] [6- O -coumaroylglucopyranosyl-(1 → 2)]- β -glucopyranoside 5 , 16 α ,22 α -diacetyl-21 β - angeloyloleanane-13 β :28-olide 3 β - O -[ β -glucopyranosyl-(1 → 2)][ ...
Natural Ursolic Acid CAS No: 77-52-1 picture from Nanjing Zelang Medical Technology Co., Ltd. view photo of Ursolic Acid, Rosemary Extract, Plant Extract.Contact China Suppliers for More Products and Price.
This topic has 6 study abstracts on Betulinic acid indicating that it may have therapeutic value in the treatment of HIV Infections, Leukemia: Chronic myelogenous leukemia (CML), and Promyelocytic leukemia
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Ursolic acid is a compound that exists in many herbs and other plants. In recent research, ursolic acid has been shown to have an anti-tumor effects.
Eucalyptus nitens crops are used in Portugal mainly by the pulp and paper industries, producing substantial bark residues with no added value use [1]. They can, however, be an interesting source of bioactive triterpenic compounds. Here, a lipophilic crude extract (CE) from bark of E. nitens prepared with dichloromethane [1] with about 70% (w/w) of triterpenoids, and a fraction of this (F2) more enriched in triterpenoids (93% w/w), as well as their main compounds betulinic acid (BiA) and betulonic acid (BoA), were used to determine their potential cytotoxicity against the colorectal HCT116 cancer cells. After 48h of incubation, the extracts/compounds inhibited significantly cell growth in a concentration-dependent manner (assessed by the MTT assay), with a GI50 s of 1.3 µg/mL and 2.2 µg/mL for F2 and CE extracts, respectively, and of 0.8µM and 3.9µM for BoA and BiA, respectively. The inhibition of cell growth was shown to be dependent on both the arrest of cell cycle at the G2/M phase, and ...
The small GTPase Rac1 has been widely implicated in mammary tumorigenesis and metastasis. Previous studies established that stimulation of ErbB receptors in breast cancer cells activates Rac1 and enhances motility via the Rac-GEF P-Rex1. As the Jak2/Stat3 pathway has been shown to be functionally associated with ErbB receptors, we asked if this pathway could mediate P-Rex1/Rac1 activation in response to ErbB ligands. Here we found that the anticancer agent cucurbitacin I, a Jak2 inhibitor, reduced the activation of Rac1 and motility in response to the ErbB3 ligand heregulin in breast cancer cells. However, Rac1 activation was not affected by Jak2 or Stat3 RNAi, suggesting that the effect of cucurbitacin I occurs through a Jak2-independent mechanism. Cucurbitacin I also failed to affect the activation of P-Rex1 by heregulin. Subsequent analysis revealed that cucurbitacin I strongly activates RhoA and the Rho effector ROCK in breast cancer cells and induces the formation of stress fibers. ...
The SDU researchers set up a co-culture system with both drug-susceptible and azole-resistant strains of C. albicans. They applied green fluorescent proteins on the susceptible version to make it stand out.. Next, they screened natural molecules found in lung moss for their potential as anti-fungal agents. They compared the results among the candidates and to the azole-type anti-fungal drug fluconazole.. They identified five lung moss-derived molecules with anti-fungal effects against susceptible and drug-resistant C. albicans strains. Of the candidates, two caught their eye.. Retigeric acid B and riccardin D displayed a preference for targeting C. albicans strains with activated efflux pump MDR1 protein. The researchers believe that the two molecules sought out the higher intracellular accumulation of the drugs in the resistant strains.. Furthermore, the drug-resistant strains changed the make-up of their lipids and sterols. The alterations might have made it easier for the lung moss molecules ...
Maturation inhibitors act at the last step of the HIV life cycle and keep the protein known as Gag from helping the virus to mature and become infectious. ...
Recent years have witnessed a breakthrough in identification of a trimer-of-hairpins motif within viral envelopes that triggers a broad range of virus-host fusion. Identifying a domain capable of controlling virus-host fusion remains a challenge due to sequence diversity, heavy glycan shielding and multiple conformations. Here, we report that HR2, a prevalent heptad repeat sequence comprising an alpha-helical coil anchored in viral membranes, is an accessible site to triterpenes, a class of widely distributed natural products. Triterpenes and their derivatives inhibit the entry of Ebola, HIV, and influenza A viruses with distinct structure-activity relationships. Specifically, triterpenoid probes, upon activation by ultraviolet light, capture the viral envelope via crosslinking the HR2 coil. Profiling the Ebola HR2 sequence using amino acid substitution, surface plasmon resonance (SPR) and nuclear magnetic resonance (NMR) spectroscopy disclosed six constitutive residues that are accessible to
Ursolic acid is one of those ingredients that shows huge potential as a bodybuilding supplement, yet struggles to get the kind of academic attention
Celastrol, a natural triterpene, exhibits potential anti-inflammatory activity in a variety of inflammatory diseases. The present study aimed to investigate its biological effect on activated fibroblast-like synoviocytes (FLSs) from patients with rheumatoid arthritis (RA). The primary FLSs of the synovial tissues were obtained from synovial biopsies of patients with RA. The normal human FLS line (HFLS) was used as a control. After the RA-FLSs and HFLSs were treated with or without celastrol, various approaches, including the WST-1 assay, transwell assay, real-time PCR and ELISA analysis, were performed to estimate proliferation, invasion and expression of pro-inflammatory cytokines of the RA-FLSs ...
Scientifics of the University of Granada have found that maslinic acid, present in olive skins leaf and wax, acts on antitumor cells controlling their alterations in growth processes. At present, the only production plant of this substance at a semi-industrial level in the whole world is at the faculty of sciences of the UGR. This research group has published results related with this release in the specialized journal FEBS Letters.
Apoptosis is an evolutionarily conserved and genetically regulated process of critical importance for embryonic development and maintenance of tissue homeostasis in the adult organism.1 Apoptosis and cancer are antagonistic processes in cell physiology. Stimulation of apoptosis is responsible for the elimination of potentially harmful or premalignant cells, whereas suppression of apoptotic pathways can lead to uncontrolled cell proliferation and formation of malignancies. Thus, searching for compounds that can specifically stimulate tumor cell death is very important for developing antitumor strategies.2,3 Although it appears that distinct pathways leading to cell death are triggered by different signals, they often merge at a common regulator of this multistep process - mitochondria. Specifically, permeabilization of the outer mitochondrial membrane (OMM) and the release of certain proteins (including cytochrome c) from the intermembrane space of mitochondria are regarded as key events in ...
This master formula is created to penetrate the deepest layers of the skin and from there, due to the high concentrations and properties of its active ingredients, achieve a balancing, repairing, anti-wrinkle, anti-stress and a smoothing of the superficial layers keeping hydrated the complexion. Coenzyme Q10 has a superficial antioxidant effect but also within the same cell, in the mitochondria, helps neutralize free radicals before they damage the cell. The hyaluronic acid that we contribute to this formula has a molecular weight so small that it penetrates in the deepest layers of the skin, increasing the synthesis of collagen. Another activator of collagen regeneration is maslinic acid, which comes from olive and has a natural antibacterial effect among other beneficial actions. 30ml ...
PHYTO BIOTECH PVT. LTD. - Exporter, Manufacturer & Supplier of AKBA ( 3-acetyl-11-keto-beta-boswallic acid ) based in Kolkata, India
Ursolic acid is a very potent anti-aging compound. Ursolic acid has been used to treat photo-aged skin, because it suppresses production of UV-A induced free radicals and inhibits the appearance of wrinkles and age spots by restoring the skins collagen bundle structures and elasticity. Scientific studies have shown that ursolic acid contains biological actives that give it anti-microbial, anti-cancer and anti-inflammatory properties.. In the skin it increases skin collagen content by increasing its production by skin fibroblast cells in the dermis, as well as increasing the ceramides content in the epidermis.. ...
Metabolic disorders including obesity, dyslipidemia and diabetes appear to be associated with monocyte dysfunction, yet the molecular mechanisms underlying mono...
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Das DECHEMA-Forschungsinstitut betreibt interdisziplinäre Forschung für nachhaltige Technologien auf den Themen Werkstoff- und Korrosionsforschung, chemische Technik, Elektrochemie und Biotechnologie
Ursolic acid encapsulated in liposomes has demonstrated an ability to stimulate ceramide synthesis in keratinocytes, resulting in a barrier that is stronger and recovers more quickly from disruption.
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Beta-boswellic acid, keto-beta-boswellic acid, and acetyl-keto-beta-boswellic acid (AKBA) have been indicated in apoptosis of cancer cells, in particular brain tumors and cells affected by leukemia or colon cancer.[5] Acetyl-boswellic acids also exhibit anti-inflammatory behaviour by inhibiting leukotriene synthesis.[6] To be specific, it inhibits the activity of the enzyme 5-lipoxygenase through a non-redox reaction. Clinical trials[7][8] have investigated the effectiveness of boswellic acids in treating ulcerative colitis, but a study on chemically induced colitis in mouse models[9] showed little effectiveness. A latter study showed that low doses of Boswellia serrata extract may have hepatoprotective effects. The higher dose was found to have a milder hepatoprotective effect than the lower dose.[10] Boswellic acids are also thought to decrease the symptoms of asthma; a small 1998 placebo-controlled trial of Boswellia extract for the treatment of asthma showed good results.[11] Boswellia ...
Huo Luo Xiao Ling Dan (HLXLD), a Chinese herbal formula composed of 11 different herbs, has been used traditionally for the treatment of arthritis and other chronic inflammatory diseases. However, the pharmacokinetic profile of its anti-inflammatory bioactive compounds has not been elucidated. Boswellic acids are the bioactive compounds with potent anti-inflammatory activity isolated from Boswellia serrate which is one of the 11 herbs of HLXLD. The objective of the study was to compare the pharmacokinetics of the two bioactive bowsellic acids: 11-keto-β-boswellic acid and 3-O-acetyl-11-keto-β-boswellic following oral administration of HLXLD or Boswellia serrata extract alone in normal and arthritic rats. An LC-MS method was developed and validated for the determination of 11-keto-β-boswellic acid and 3-O-acetyl-11-keto-β-boswellic in the comparative pharmacokinetic study. The results showed that there were significant differences in pharmacokinetic parameters between normal and arthritic groups.
The ethyl acetate partition of dried methanolic extract of aerial parts of Euphorbia microsciadia (Euphorbiaceae) afforded three pentacyclic triterpenes, betulinic acid (1) from lupane type, oleanolic acid (2) from oleane type and ursolic acid (3) from ursane type triterpenes that are reported for the first time in this plant. These three compounds were structurally compared through their mass fragmentation pattern, nuclear magnetic resonance (NMR) data and their biologic immunomodulatory effects. The structures of the isolated compounds were elucidated by 13C- and 1H-NMR as well as 2D-NMR, IR and by the aid of mass fragmentation pattern and comparing with the literature. After running T-Cell proliferation assay, oleanolic acid stimulated proliferation of T-Cells at lower concentration 0.5 µg/mL, while betulinic acid and ursolic acid showed inhibitory activity against T-Cell proliferation with IC50- value | 50 µg/mL and 3.01 ± 0.47 µg/mL, respectively.
Sometimes referred to as Indian frankincense, this deciduous tree is native to arid mountainous regions of India. A member of the Burseraceae family, which includes myrrh and frankincense, the plant provides a notable incense fragrance and is distinguished by its aromatic resin and oil. Like standard frankincense, Boswellia extract is collected from an incision in the trunk, with a sap-like oleoresin emerging from the tree. In long-held Ayurvedic traditions, Boswellia serrata is known as Salai guggul or Shallaki, and has been used for ages due to its health-supporting qualities. Today, science has validated many of Indian frankincenses benefits and shown them to largely stem from its ability to modulate inflammation.**. Research has reinforced the inflammation-modulating properties of Boswellia serrata, which have been attributed to beneficial compounds called triterpenes, most notably boswellic acid. Boswellia serratas active compounds are believed to influence the creation of inflammatory ...
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Resin from the Boswellia serrata tree found in Asia and Africa is commonly used in traditional natural medicine for a variety of disorders associated with inflammation. It has been used medicinally for centuries and is now gaining support through research. The main ingredients of the resin are boswellic acids. Boswellic acids have anti-inflammatory effects when applied topically.. Research shows boswellic acids also inhibit the actions of inflammatory mediators that cause loss of collagen and elastin fibers in the scalp. Boswellic acids also increase the activity of fibroblasts, cells that make collagen.. The accepted mechanism for the anti-inflammatory effect of boswellic acids is through inhibiting the formation of leukotrienes (1, 6, 7). Leukotrienes are immune mediators produced by immune cells and play an important role in inflammation. Boswellic acids are unique in that they specifically target an enzyme that forms leukotrienes, 5-LO (6). Research shows boswellic acids also inhibit the ...
AIM: To investigate the chemical constituents of Isodon xerophilus. METHODS: The constituents were isolated by various chromatographic methods, and the chemical structures were elucidated on the basis of spectral analyses. Their cytotoxicity was evaluated by the MTT method in 96-well microplates. RESULTS: Ten triterpenes were isolated and identified as oleanolic acid (1), ursolic acid (2), maslinic acid (3), 2 alpha-hydroxyursolic acid (4), hederagenin (5), 3 beta, 23-dihydroxy-urs-12-en-28-oic acid (6), arjunolic acid (7), asiatic acid (8), 2 alpha, 3 alpha, 24-trihydroxyolean-12-en-28-oic acid (9), and 2 alpha, 3 alpha, 24-trihydroxyurs-12-en-28-oic acid (10). All compounds were tested against three human tumor cell lines, K562, MKN45, and HepG2. CONCLUSION: All of the compounds were isolated from this plant for the first time. The proposed biosynthetic pathway of these triterpenes was discussed. All of the triterpenes showed noncytotoxic activity against the above-mentioned three human tumor ...
Each Boswellia Capsule contains 300 mg of extract (as dry extract) from Shallaki (Boswellia serrata) (6:1) (equivalent to 1800 mg of Shallaki resin). When assayed these capsules contain Boswellic Acid NLT 65%. Sanskrit name of Boswellia Serrata is Salai g
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TY - JOUR. T1 - Inhibition of rat brain Na+-K+-ATPase by triterpene glycosides from holothurians. AU - Gorshkova, I. A.. AU - Gorshkov, B. A.. AU - Stonik, V. A.. PY - 1989/1/1. Y1 - 1989/1/1. N2 - I. A. Gorshkova, B. A. Gorshkov and V. A. Stonik. Inhibition of rat brain Na+-K+-ATPase by triterpene glycosides from holothurians. Toxicon 27, 927-936, 1989.-The effect of triterpene glycosides from holothurians on Na+-K+-ATPase of rat brain was investigated. The marine glycosides are irreversible inhibitors of the enzyme with an average I50 value of 10-4 M. ATP had a low protective effect against inhibition. The inhibitory effect was increased by preincubation with MgCl2. There was alteration of the activation curve of Na+-K+-ATPase by NaCl and KCl in the presence of glycosides. Triterpene glycosides inhibited the K+-phosphatase activity, but to a smaller degree than the ATPase activity. Na+-K+-ATPase of pig kidney was less sensitive to the marine triterpene glycosides than the brain enzyme. The ...
Authors: NAZLI BÖKE SARIKAHYA, SÜHEYLA KIRMIZIGÜL Abstract: Two new triterpene glycosides, 3-O-\beta-D-glucopyranosyl- (1\to 4)-\beta-D-xylopyranosyl-(1\to 3)-\alpha-L-rhamnopyranosyl- (1\to 3)-\alpha-L-arabinopyranosyl olean-12-ene 28-O-\beta -D- glucopyranosyl-(1\to 6)-\beta-D-glucopyranosyl ester (gazipashoside A, 1) and 3-O-\beta-D-glucopyranosyl-(1\to 4)-\beta-D-xylopyranosyl- (1\to 3)-\alpha-L-rhamnopyranosyl-(1\to 2)-\alpha-L-arabinopyranosyl hederagenin 28-O-\beta -D-glucopyranosyl-(1\to 6)-\beta-D-glucopyranosyl ester (gazipashoside B, 2), were isolated together with 11 known compounds including 7 triterpene, 1 flavonoid, and 3 iridoidal metabolites from the aerial parts of Cephalaria gazipashensis (Dipsacaceae). The structures of all compounds were elucidated by extensive evaluation of the spectroscopic data (1D- and 2D- NMR, HRESI-MS), as well as chemical examinations. The antimicrobial effects of all pure compounds were tested against gram-positive and gram-negative bacteria. The ...
Implant of polymer containing pentacyclic triterpenes from Eugenia punicifolia inhibits inflammation and activates skeletal muscle remodeling.: Sustained chroni
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Boswellia serrata contains triterpenoids, alleged Boswellic acids, which are actual able non-competitive and non-oxyreductive inhibitors of 5-lipoxygenase. This agitator gives acceleration to the assembly of leukotrienes; some of them (5 - HETE -ydroxyeicosatetraenoic acerbic and leukotriene LTB4) are mediators of anarchic processes and allergic reactions. Leukotrienes could cause chemotaxis, chemokinesis, chargeless abolitionist synthesis, access the…
Oleanolic acid and ursolic acid are triterpenoid compounds that exist widely in food, medicinal herbs and other plants. This review summarizes the pharmacological studies on these two triterpenoids. Both oleanolic acid and ursolic acid are effective in protecting against chemically induced liver inj …
Willow bark has a long history of traditional use for reducing minor pain. Several randomized human trials illustrate its ability to do so primarily through the actions of salicin, a source of salicylic acid. Additionally, it helps to maintain healthy prostaglandin metabolism and blood flow. Boswellia serrata has also revealed the potential to provide statistically significant support for reducing mild pain. AKBA, or 3-acetyl-11-keto-beta-boswellic acid, may be particularly supportive in maintaining healthy 5-lipoxygenase enzyme activity and leukotriene metabolism to maintain tissue comfort. Curcumin maintains healthy cyclooxygenase-2 enzyme activity while supporting healthy prostaglandin, leukotriene and thromboxane metabolism. Devils claw promotes both healthy cyclooxygenase-2 and 5-lipoxygenase enzyme activity. A review of 12 human studies indicates that devils claw may reduce mild pain to promote musculoskeletal comfort and function. dl-Phenylalanine supports enkephalin activity, which ...
Synthetic oleanane triterpenoids are multifunctional drugs being developed for the prevention and treatment of a variety of chronic diseases driven by inflammation and oxidative stress. Low nanomolar concentrations of triterpenoids inhibit the induction of inflammatory cytokines, and these drugs are potent activators of the Nrf2 cytoprotective pathway. In contrast, low micromolar concentrations of triterpenoids increased the production of ROS and induced apoptosis in a dose-dependent manner in malignant MCF10 CA1a breast cancer cells. Because cancer cells respond differently to ROS than normal cells, it should be possible to exploit these differences therapeutically. In an experimental model of lung cancer, the triterpenoids activated the Nrf2 pathway, as seen by induction of the cytoprotective enzyme NQO1, and reduced the toxicity of carboplatin and paclitaxel. The induction of the Nrf2 pathway in the lung did not suppress the efficacy of treatment with carboplatin and paclitaxel, as the average tumor
Man is a microcosm or a little world, because he is an extract from all the stars and planets of the whole firmament, from the earth and the elements and so he is their quintessence(the most perfect example of class). - Phillipus Paracelsus. From a linear and scientific stance, Frankincense Sacra is a potent anti-tumor agent causing apoptosis in cancer cells. The main compound is acetyl-11-keto-beta-boswellic acid, or AKBA. It is a potent cancer fighting triterpene produced by this incredible varietal. No wonder it was fit for a king. The antiquity of this incredible oil is something to hold reverence for.. Our bodies love the turpenes from medicinal trees and plants. We uptake the healing medicine into the cell and decode their powerful messages. They are a perfect fit for mans cellular structure. The body is an intelligent machine and the plants/trees and herbal kingdom are potent attendants to creating wholeness here on earth.. Lastly, Frankincense Sacra offers an anti-aging solution with ...
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The boswellia herb, also known as Indian frankincense, comes from the resin found deep inside of the boswellia serrata trees wood. Incredibly rare, this resin has been used as a priceless natural remedy in Ayurveda and other natural remedies. Compounds found in boswellia serrata extract called boswellic acids mat help
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Boswellia serrata extract ingestion and glomerular filtration rate. Clin Nephrol. 2020 Jan 27;: Authors: Lhotta K, Sprenger-Mähr H, Zitt E PMID: 31983384 [PubMed - as supplied by publisher]...
Background Ursolic acid (UA) is a triterpenoid compound with multiple biological functions. This compound has recently been reported to possess an anti-obesity effect; however, the mechanisms are less understood. Objective As adipogenesis plays a critical role in obesity, the present study was conducted to investigate the effect of UA on adipogenesis and mechanisms of action in 3T3-L1 preadipocytes. Methods and Results The 3T3-L1 preadipocytes were induced to differentiate in the presence or absence of UA for 6 days. The cells were determined for proliferation, differentiation, fat accumulation as well as the protein expressions of molecular targets that regulate or are involved in fatty acid synthesis and oxidation. The results demonstrated that ursolic acid at concentrations ranging from 2.5 µM to 10 µM dose-dependently attenuated adipogenesis, accompanied by reduced protein expression of CCAAT element binding protein β (C/EBPβ), peroxisome proliferator-activated receptor γ (PPARγ), CCAAT
1Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Universitas Airlangga, Surabaya 60115, Indonesia DOI : 10.35333/jrp.2020.138 Breast cancer and cervical cancer were ranked first and fourth of the leading cause of death of women in the world. One of natural compounds that was reported on having cytotoxic activity against various cancer cells with high selectivity is betulinic acid. In our previous study, it was found that the acetone extract of Solanum mammosum callus culture contains betulinic acid. The aims of the current study were firstly to investigate the anticancer activity of the acetone extract of S. mammosum as well as betulinic acid, and secondly to quantitatively determine the betulinic acid content in the acetone extract of S. mammosum culture. The anticancer activity was carried out using the MTT method against HeLa and Vero cells. The determination of betulinic acid content was done using the TLC densitometry method. The results showed that the acetone extract ...
TY - JOUR. T1 - Two different modes of inhibition of the rat brain Na+, K+-ATPase by triterpene glycosides, psolusosides A and B from the holothurian Psolus fabricii. AU - Gorshkova, Irina A.. AU - Kalinin, Vladimir I.. AU - Gorshkov, Boris A.. AU - Stonik, Valentin A.. PY - 1999/1/1. Y1 - 1999/1/1. N2 - Effects of two triterpene glycosides, isolated from the holothurian Psolus fabricii, on rat brain Na+, K+-ATPase (Na, K-pump; EC 3.6.1.3) were investigated. Psolusosides A and B (PsA and PsB) inhibited rat brain Na+, K+-ATPase with I50 values of 1 x 10-4 M and 3 x 10-4 M, respectively. PsA significantly stimulated [3H]ATP binding to Na+, K+-ATPase, weakly increased [3H]ouabain binding to the enzyme, and inhibited K+-phosphatase activity to a smaller degree than the total reaction of ATP hydrolysis. In contrast, PsB decreased [3H]ATP binding to Na+, K+-ATPase, and had no effect on [3H]ouabain binding to the enzyme. K+-Phosphatase activity was inhibited by PsB in parallel with Na+, K+-ATPase ...
90 CapsulesÊ This is the richest, full spectrum, frankincense (boswellia, AKBA) formula available. The main active ingredient of boswellia - AKBA- is the most potent natural 5-lipoxygenase enzyme inhibitor. This enzyme is crucial in maintaining a normal inflammatory response. AKBA promotes: a healthy respiratory system; a healthy joint function with a good range of motion, less stiffness; a healthy digestive tract ; a high energy level, and much more Common market available boswellia is not standardized at all or at best has 1-3% AKBA. The True Botanica AKBA PlusTMÊis std. to 90% AKBA, and offers 54mg of AKBA in every serving!! The addition of the frankincense gum, fenugreek and Bioperine¨ improve bioavailability even more. This allows a person to finally be able to take enough to reach the blood levels that have been found to be effective. Our research has shown that our formula creates blood levels of several hundred ng/ml while most of our competitors showed blood levels close to zero! Rudolf
en] An accurate and sensitive method, combining soxhlet extraction, solid phase-extraction and capillary gas chromatography is described for the quantitative determination of one triterpene (lupeol) and three sterols (stigmasterol, campesterol and beta-sitosterol) and the detection of another triterpene (alpha-amyrin) from the aerial part of Justicia anselliana. This is the first method allowing the quantification of sterols and triterpenes in this plant. It has been fully validated in order to be able to compare the sterol and triterpene composition of different samples of J. anselliana and therefore help to explain the allelopathic activity due to these compounds. This method showed that the aerial part of J. anselliana contained (292+/-2)mg/kg of lupeol, (206+/-1)mg/kg of stigmasterol, (266+/-2)mg/kg of campesterol and (184+/-9)mg/kg of beta-sitosterol ...
Frankincense (and Roxb. cell collection panel from the U.S. Country wide Cancer tumor Institute (NCI), using the IC50 beliefs for boswellic acids through bioinformatic methods to recognize novel molecular determinants for response towards these substances. 2.?Experimental Section 2.1. Phytochemicals Boswellic acids had been extracted from Sigma-Aldrich (Taufkirchen, Germany). The chemical substance structures are proven in Amount 1. Open up in another window Amount 1 Chemical buildings of - and -boswellic acidity (http://en.wikipedia.org/wiki/Boswellic_acid). 2.2. Cell Lines The -panel of individual tumor cell lines from the Developmental Therapeutics Plan of NCI includes leukemia, melanoma, non-small cell lung cancers, cancer of the colon, renal cancers, ovarian malignancy cells, tumor cells of the central nervous system, prostate carcinoma, and breast cancer. Their source and processing possess previously been explained [11]. These cell lines were employed to determine the cytotoxicity Rabbit ...
3-O-alpha-L-rhamnopyranosyl-(1-2)(beta-D-glucopyranosyl-(1- 4))-alpha-L-arabinopyranosyl-27-hydroxyoleanolic acid 28-O-alpha-L-rhamnopyranosyl (1-4)-beta-D-glucopyranosyl (1- 6)-beta-D- ...
Betulinic acid (BA) is a novel antineoplastic agent under evaluation for tumor therapy. Because of the selective cytotoxic effects of BA in tumor cells (including gliomas), the combination of this agent with conservative therapies (such as radiotherapy and chemotherapy) may be useful. Previously, the combination of BA with irradiation under hypoxic conditions had never been studied. In this study, the effects of 3 to 30 μM BA on cytotoxicity, migration, the protein expression of PARP, survivin and HIF-1α, as well as radiosensitivity under normoxic and hypoxic conditions were analyzed in the human malignant glioma cell lines U251MG and U343MG. Cytotoxicity and radiosensitivity were analyzed with clonogenic survival assays, migration was analyzed with Boyden chamber assays (or scratch assays) and protein expression was examined with Western blot analyses. Under normoxic conditions, a half maximal inhibitory concentration (IC50) of 23 μM was observed in U251MG cells and 24 μM was observed in U343MG
quercetin 3-O-alpha-L-rhamnopyranosyl-(1-2)-(beta-D-glucopyranosyl-(1-3)-alpha-L-(4-O-trans-p-coumaroylrhamnopyranosyl)-(1-6))-beta-D-galactopyranoside-7-O-alpha-L- ...
Biochemistry Research International is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles covering all areas of biological chemistry. Studies involving the structure, function, and/or dynamics of biological molecules, molecular pathways, organelles, cells, and/or tissues are welcomed.
Catherines lab focuses on virology with a specific interest in antiviral drugs. Antiviral drugs can be used to combat important viral diseases that cause medical and economic burdens; in addition they can be used as valuable tools to address basic research questions in virology.. Prior to her current position as Lecturer in Molecular Medicine at the University of St Andrews, Catherine worked as a Postdoctoral Research Fellow with Dr Eric Freed within the US National Institutes of Health (NIH) HIV Drug Resistance Program. During this time Catherine performed internationally recognized work on the novel HIV-1 maturation inhibitor bevirimat and made significant contributions to understanding the drugs mechanism of action, acquisition of drug resistance and performance in phase II clinical trials. Research into HIV-1 maturation inhibitors is on going in St Andrews; we are dissecting the relationship between drug binding and Gag-Gag multimerization during virus assembly and using a panel of ...
Ursolic acid (UA), a pentacyclic triterpenoid, is known to have anti-tumor activity in various cancers including human non small cell lung cancer (NSCLC). However, the molecular mechanisms underlying the action of UA remain largely unknown. Cell viability was measured by MTT assays. Apoptosis was analyzed with Annexin V-FITC/PI Apoptosis Detection Kit by Flow cytometry. Western blot analysis was performed to measure the phosphorylation and protein expression of stress-activated protein kinase/c-Jun N-terminal kinase (SAPK/JNK), DNMT1 [DNA (cytosine-5)-methyltransferase 1], enhancer of zeste 2 polycomb repressive complex 2 subunit (EZH2) and SP1. Exogenous expression of SP1 and DNMT1 was carried out by transient transfection assays. We showed that UA inhibited the growth and induced apoptosis of NSCLC cells in the dose- and time-dependent fashion. Furthermore, we found that UA induced phosphorylation of SAPK/JNK and suppressed the protein expression of DNMT1 and EZH2. The inhibitor of SAPK/JNK (SP600125)
Approaches to Improve the Oral Bioavailability and Effects of Novel Anticancer Drugs Berberine and Betulinic Acid. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Anti-oxidant, anti-inflammatory and antiacetylcholinesterase activity of betulinic acid and 3β- acetoxybetulinic acid from Melaleuca bracteata Revolution Gold
Staherb Natural Ingredients Co., Ltd always supply you high quality plant extract, herb extract, etc with reasonable price. What is the ursolic acid Ursolic Acid , a carboxylic acid present in a wide variety of plants in the form of a free acid or...
Ursolic acid (loquat leaf extract) can be found in plants that are used for cosmetics additives. Ursolic acid can serve as a starting material for synthesis of more potent bioactive derivatives.
TY - JOUR. T1 - UV-induced damages eliminated by arbutin and ursolic acid in cell model of human dermal fibroblast WS-1 cells. AU - Chen, Kuan-Chou. AU - Chang, Ho-Hsing AU - Ko, Wang Sheng. AU - Wu, Charng-Lin AU - Chiu, Wen-Ta. AU - Hsieh, Chiu Lan. AU - Peng, Robert Y.. PY - 2009/6. Y1 - 2009/6. N2 - Objectives: UV irradiation may cause dermal ageing and carcinoma. The molecular action mechanism of such an effect and the methods for prevention are still lacking. Materials and Methods: UVA (320-400 nm) plus UVB (290-320 nm) (hereafter denoted as UVAB) was used to induce skin damages in human fibroblast WS1 (hfWS1) cells. The parameters evaluated included the cell viability, expressions of relevant enzymes including MMP-1, MMP-2, catalase, and LDH; some biochemical indices such as elastin content and lipid peroxidation. Arbutin (AB) and ursolic acid (UA) were used to evaluate whether they could show any protective effect. Results: UVAB inhibited the viability of hfWS1 cells, leading to a ...
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Journal of Pharmaceutical and Biological Sciences-JPBS-Print ISSN No:- Online ISSN No:-2320-1924Article DOI No:-10.18231,Aliphatic alcohols, alkylated aromatic and triterpenic constituents from the aerial parts of Rhus chinensis Mill-IP Innovative Publication Pvt Limited, Medical Journals Publication, Open Access Jou
BA is a novel antineoplastic agent with cytotoxicity against melanoma and neuroectodermal tumor cells. Here, we report that BA triggers an apoptotic cascade in human malignant glioma cells as well. BA-induced apoptosis of glioma cells involves sequentially new protein synthesis, formation of reactive oxygen species, and caspase processing. In detail, we show that BA toxicity depends on new protein but not mRNA synthesis, suggesting that translation of preexisting mRNA mediates BA toxicity. Caspase 8 and 3 activation are critical steps in the killing cascade triggered by BA because cell death ensues whenever caspase activation is detected. Furthermore, pharmacological (PBN, NAC, DEVD-CHO) or genetic (BCL-2) manipulations that inhibit apoptosis do so at the level of, or upstream of, caspase activation. Cytotoxic, cytokine-resistant glioma cells do not exhibit cross-resistance to BA, suggesting that caspase activation is independent of interactions of endogenous CD95/CD95L or related pairs of death ...
Objective: To study the chemical constituents of dried fruits of Chaenomeles sinensis (Thouin.) Koehne and provide the evidence for the exploitation and utilization of this plant resources. Methods: Isolation and purification of chemical constituents of Chaenomeles sinensis (Thouin.) Koehne by solvent extraction and chromatography, and their structures were identified by physicochemical properties and spectroscopic analysis. Results and Conclusion: Seven compounds were isolated from the ethanol extract of the fruits and identified as: palmitic acid(Ⅴ), ursolic acid 3 O behenate(Ⅵ), ursolic acid(Ⅶ), 3 acetyl ursolic acid(Ⅷ), 3 acetyl pomolic acid(Ⅸ), daucosterol(Ⅹ), betulinic acid(Ⅺ). All of these compounds were obtained from the plant for the first time. Among themⅥ is a new compound.
BosPro Boswellia, clinically studied optimized boswellia supplement with 10x more AKBA boswellic acids (BosPure), extra-strength anti-inflammatory for gut, lungs, joints
TY - JOUR. T1 - Triterpene glycosides from the tubers of Leontice smirnowii. AU - Tabatadze, N.. AU - Tabidze, B.. AU - Mshvildadze, V.. AU - Elias, R.. AU - Dekanosidze, G.. AU - Balansard, G.. AU - Kemertelidze, E.. PY - 2009/5/1. Y1 - 2009/5/1. UR - http://www.scopus.com/inward/record.url?scp=69249202266&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=69249202266&partnerID=8YFLogxK. U2 - 10.1007/s10600-009-9313-2. DO - 10.1007/s10600-009-9313-2. M3 - Article. AN - SCOPUS:69249202266. VL - 45. SP - 453. EP - 454. JO - Chemistry of Natural Compounds. JF - Chemistry of Natural Compounds. SN - 0009-3130. IS - 3. ER - ...
Phytochemical investigation of the ethanol extract of the roots of Sanguisorba officinalis resulted in the isolation of three new triterpene glycosides, 3β-[(α-L-arabinopyranosyl)oxy]-19α,23-dihydroxyolean-12-en-28-oic acid 28-[6-O-acetyl-β-D-glucopyranosyl] ester (1), 2α,3β,19α,23-tetrahydroxyurs-12-en-28-oic acid 28-[6-O-acetyl-β-D-glucopyranosyl] ester (2), and 3β-[(α-L-arabinopyranosyl)oxy]-19α-hydroxyurs-12,20(30)-dien-28-oic acid 28-[6-O-acetyl-β-D-glucopyranosyl] ester (3). All the triterpene glycosides exhibited the significant cytotoxic potential with low IC50 values ...
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Development of new agents is needed for the prevention and treatment of cancer, and we have developed novel synthetic triterpenoids for this purpose. The potent anti-inflammatory, growth-suppressive, and differentiative activities of CDDO, a prototypic synthetic triterpenoid, have been described previously (8 , 14) . Here, we show that the C-28 imidazolide derivative of CDDO, CDDO-Im, is significantly more potent than CDDO in vitro. Furthermore, we report for the first time the potent in vivo activity of CDDO-Im in three mouse models that are relevant to carcinogenesis and cancer therapy.. CDDO-Im is approximately 10-fold more potent than CDDO as an inhibitor of human cancer cell proliferation and inducer of differentiation in human leukemia cells. Interestingly, CDDO-Im was found to synergize strongly with ligands for RXR and VDR nuclear receptors in inducing monocytic differentiation in U937 cells. Nuclear receptors control cancer cell growth and differentiation (34, 35, 36) , and their ...