(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol
CYCLOASTRAGENOL
CAS: 78574-94-4
Molecular Formula: C30H50O5
(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol - Names and Identifiers
(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol - Physico-chemical Properties
| Molecular Formula | C30H50O5 |
| Molar Mass | 490.72 |
| Density | 1.20±0.1 g/cm3(Predicted) |
| Melting Point | 241.0 to 245.0 °C |
| Boling Point | 617.2±55.0 °C(Predicted) |
| Storage Condition | 2-8℃ |
| Use | Use a kind of sapogenin and aglycone in radix astragali. It is a natural triterpenoid. |
(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol - Determination of Astragaloside and Astragaloside Ⅳ in radix astragali
From HowNet
Author:
Summary:
the main active ingredient of astragalus on cardiovascular system is astragalus saponins. most of astragalus saponins are saponins with astragalus saponins as aglycone, of which astragalus A has the highest content. In this paper, double-wavelength thin-layer scanning & lambda;_s = 500nm,& lambda;_R = 700nm to determine the content of cycloastragaloside and astragaloside.
keywords:
astragalus cycloastragaloside astragaloside a> thin layer scanning method
DOI:
10.3969/j.issn.1006-3765.2009.02.015
cited:
Year:
2009
Last Update：2024-01-02 23:10:35
(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol - Study on in vitro and in vivo metabolism of Astragaloside and Astragaloside
From HowNet
Author:
Summary:
Nowadays, the aging of the population in various countries in the world is accelerating. Preventing aging and prolonging life has become an urgent need for people. The search for effective anti-aging drugs has become a hot spot. At present, the mechanism of aging has an impact on telomere theory. If telomerase is activated, it can increase the number of cell divisions and prolong life. In recent years, studies have confirmed that the sapogenin cycloastragaloside (Astragaloside Ⅳ, AST) has significant telomerase activation effect, and AST has long been confirmed to have obvious anti-aging activity. As the fourth generation of natural health products and anti-aging drugs, they have attracted widespread attention, so their research has become a hot spot. At present, many studies have confirmed that saponins can undergo glycosyl hydrolysis in the body, and metabolites including saponin as the main substances enter the blood to play a greater pharmacological effect. AST is both macromolecular saponins, and its oral bioavailability is very low; its absorption, metabolic transformation in the body and the components that really exert its efficacy are still unclear. CAG is its sapogenin, and their physical and chemical properties are different, which may directly lead to the difference in bioavailability, affect the absorption distribution and metabolism in the body, and then further affect the pharmacodynamic effect. Therefore, this topic studies the metabolic transformation process, transformation site and metabolites of AST and CAG in vivo, and clarifies the pharmacodynamic components. This paper first studies the physical and chemical properties of AST and CAG, and then discusses the metabolic characteristics of AST and CAG respectively in vitro and in vivo, clarifies the metabolic pathways, and provides experimental basis for the rational development of new drugs and health products. This paper mainly includes three parts: the first part of the literature review on aging and anti-aging drugs and health products, and summarizes the research on the metabolic transformation of saponin drugs in vitro and in vivo, the research status of AST and CAG is summarized and analyzed. The second part of the experiment part of the physical and chemical properties of AST and CAG and the study of their metabolism in vitro and in vivo, including the study of metabolites, the analysis of metabolic pathways, etc. 1AST and CAG physical and chemical properties evaluation of the two approximate solubility, water equilibrium solubility experimental results show that, the physical and chemical properties of the two are different. Study on metabolism of AST in vivo and in vitro (1) Analysis of metabolites in vivo The urine and feces of rats were collected by gavage of AST (40mg kg-1), and the prototype and metabolites were detected by LC-MS/MS. No prototype drug was detected in the urine and feces of rats. Among them, two metabolites were detected in rat urine: A(vivo)1(m/z513) and A(vivo)2(m/z543). According to multistage mass spectrometry, A(vivo)1 may be an isomer of CAG or a ternary ring-opening product. A(vivo)2 may be a methoxylated metabolite. Four new substances were detected in rat feces, namely A(vivo)1 '(m/z513), A(vivo)2'(m/z513), A(vivo)3 '(m/z543) and A(vivo)4'(m/z511). It is speculated that A(vivo)1 'may be CAG:A(vivo)2',A(vivo)3 'is consistent with A(vivo)1 and A(vivo)2 in urine. A(vivo)4' may be CAG dehydrogenation oxidation product. (2) In vitro metabolic characteristics and analysis of metabolites. Firstly, the stability in artificial gastric juice and artificial intestinal juice was investigated. It can be seen that AST basically remained stable within 4 hours of reaction between artificial gastric juice and intestinal juice. Through the metabolism of AST in vitro intestinal flora, it was found that AST was easily hydrolyzed and deglycosylated reaction occurred to generate CAG-6-O-β-D-glucoside and CAG. It shows that AST is unstable in the intestine and can be metabolized by intestinal flora. Experiments on AST metabolism in rat liver showed that AST was almost non-metabolized in rat liver, indicating that after oral administration of AST, there was almost no liver primary effect. Studies on metabolism of 3CAG in vitro and in vivo (1) Analysis of metabolites in vivo collected 24h urine and feces by gavage of rat CAG (40mg kg-1) and detected by LC-MS/MS. CAG(CO) and 7 metabolites C1-C7 were detected in rat urine, namely C1(m/z529), C2(m/z529), C3(m/z527), C4(m/z543), C5(m/z485), C6(m/z469) and C7(m/z353). according to multistage mass spectrometry, it is estimated that several metabolites are mostly oxidized and methyl. CAG(CO-1 ',C0-2') and nine metabolites C1'-C9', C1'(m/z527), C2'(m/z527), C3'(m/z529), C4'(m/z485), C5'(m/z499), C6'(m/z543), C7'(m/z455), c8 '(m/z469) and C9'(m/z453). The metabolites of CAG in vivo are mostly methylation and oxidation metabolites. (2) In vitro liver metabolism kinetics in rat liver homogenate, the optimal incubation time was 40min, the optimal protein concentration was 2.0mg · mL-1, and the optimal substrate concentration was 0.05mg · mL-1. The calculated Vmax is 6.88 × 10-5μmol ·(min · mg protein)-1 and Km is 18.8 μmol · L-1. The comparison of CAG metabolism in different tissues of rats shows that the metabolic capacity in heart, spleen, lung and kidney is relatively low and far inferior to that in liver. Part III Conclusion and discussion AST is prone to biotransformation in vivo to generate sapogenin CAG; CAG is metabolized in vivo. It is speculated that AST is transformed into metabolites with strong pharmacological activity by intestinal flora, mainly through aglycone CAG.
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keywords:
metabolism Cycloastragalus alcohol Astragaloside A In vivo <= "https://xueshu.baidu.com/s?wd=体外&tn=SE_baiduxueshu_c1gjeupa&ie=utf-8" target = "_blank"> In vitro
cited:
Year:
2013
Last Update：2023-08-16 22:09:50
(3beta,6alpha,16beta,20R,24S) 20,24-Epoxy-9,19-cyclolanostane-3,6,16,25-tetrol - Research progress on pharmacological effects of cycloastragalol
From Wanfang Medicine
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Summary:
Cycloastragalus alcohol, as a secondary metabolite with great medicinal value in Astragalus membranaceus, has protective effect on cardiovascular diseases, stroke, fatty liver, abdominal aortic aneurysm and other diseases, can activate telomerase, regulate immunity, promote wound healing and hair growth, etc. However, there are still some problems in the current research on the pharmacological effects of Cycloastragalol: ①Related in vitro experiments have found that Cycloastragalol has a cytotoxic effect at a certain concentration, suggesting that Cycloastragalol is not absolutely safe, and its toxicity to cells It still needs in-depth study, and its safety in animals needs further verification; ②The research on Cycloastragalol is mostly limited to activating telomerase, although it has advantages in the development of related health care products, it limits its deeper and wider research to a certain extent. At present, although there have been researches on the regulatory effects of cyclothrin on AMP activiated protein kinase (AMPK) pathway, farnicol X receptor (famesoid X receptor,FXR) transcription factor and silent mapping type information regulation,SIRT1) protein, it has made some supplements to its pharmacological targets, but there is still a lack of relevant pharmacological activities and mechanism of action. Although there are still some problems in the study of the pharmacological effects of Cycloastragalus alcohol, it is undeniable that its medicinal value should be further strengthened in the future, and its protective effects on cardiac fibrosis, congestive heart failure, arrhythmia and other diseases, as well as theoretical and experimental studies on improving cardiovascular disease risk indicators and regulating endothelial cell homeostasis, so as to be better applied in clinical practice. At the same time, fully tap the potential of Cycloastragalol in the treatment of cerebral ischemia and mental diseases, and take its effect on brain neurovascular diseases as a new direction of future research.
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keywords:
cycloastragalol astragalus pharmacological action drug metabolic dynamics safety cerebral ischemia mental diseases drug target
DOI:
10.16368/j.issn.1674-8999.2020.05.222
Year:
2020
Last Update：2023-08-16 22:09:50
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