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 ...
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 ...
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 formulationsencompassing"Ursolic 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 ...
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
Get to know more about the unprecedented reaction of Betulinic Acid Market Researchplayers analysis and their strategies. Impact of coronavirus on Consumer Spending to create intense volatility and speculative pricing bringing imbalance in demand and supply curve.
... 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
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 ...
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...
Fully Renovated 2 BR/1 BA on Sullivans Island. This charming red circa 1890 cottage on Sullivans Island has been lovingly restored into a cozy, elegant ret...
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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