Gymnemic Acid I
(Synonyms: 匙羹藤酸I) 目录号 : GC45719
A triterpene glycoside
Cas No.:122168-40-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Gymnemic acid I is a triterpene glycoside that has been found in G. sylvestre and has antihyperglycemic activities.1,2 It inhibits glucose-induced phosphorylation of serine 70 on S6 kinase (S6K1) and serine 2448 on mTOR, caspase-3 activity, and apoptosis, as well as increases autophagy in MIN-6 pancreatic β cells when used at a concentration of 5 μg/ml.1 Gymnemic acid I has been used as a reference compound to compare the potency of plant-derived sweet taste inhibitors.2
|1. Wu, Y., Hu, Y., Yuan, Y., et al. Gymnemic acid I triggers mechanistic target of rapamycin-mediated β cells cytoprotection through the promotion of autophagy under high glucose stress. J. Cell. Physiol. 234(6), 9370-9377 (2019).
| Cas No. | 122168-40-5 | SDF | |
| 别名 | 匙羹藤酸I | ||
| Canonical SMILES | CC1(C)[C@@H](OC(/C(C)=C/C)=O)[C@H](O)[C@]2(COC(C)=O)[C@@H](O)C[C@@]3(C)[C@]4(C)CC[C@@]5([H])[C@](C)(CO)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O6)CC[C@]5(C)[C@@]4([H])CC=C3[C@]2([H])C1 | ||
| 分子式 | C43H66O14 | 分子量 | 807 |
| 溶解度 | DMSO : 50 mg/mL (61.96 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2392 mL | 6.1958 mL | 12.3916 mL |
| 5 mM | 0.2478 mL | 1.2392 mL | 2.4783 mL |
| 10 mM | 0.1239 mL | 0.6196 mL | 1.2392 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Gymnemic Acid I triggers mechanistic target of rapamycin-mediated β cells cytoprotection through the promotion of autophagy under high glucose stress
J Cell Physiol 2019 Jun;234(6):9370-9377.PMID:30370588DOI:10.1002/jcp.27621.
Gymnemic Acid I (GA I) is a bioactive component of Gymnema sylvestre. It is an Indian traditional medicinal herb which has antidiabetic effect. However, the molecular mechanism is remaining to be elucidated. Here, we showed that high glucose promoted the rate of apoptosis, GA I decreased the apoptosis under the high glucose stress. Our further study explored that GA I increased the number of autophagosome and the ratio of light chain 3-I (LC3-I)/LC3-II in MIN-6 cells under the normal or high glucose stress by the methods of western blot analysis and immunofluorescence. It induced autophagy flux and inhibited the phosphorylation of mammalian target of rapamycin (mTOR) and ribosomal protein S6 kinase β-1 (p70 S6K/S6K1), which is a substrate of mTOR. GA I decreased the rate of apoptosis and the activity of caspase-3 under the high glucose stress. The inhibition of apoptosis and caspase-3 activity by GA I were increased after treating with autophagy inhibitor in mouse islet β cells MIN-6. Our data suggested that GA I-induced autophagy protected MIN-6 cells from apoptosis under high glucose stress via inhibition the phosphorylation activity of mTOR.
Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics
J Nat Prod 2017 Apr 28;80(4):909-915.PMID:28256837DOI:10.1021/acs.jnatprod.6b00793.
The plant Gymnema sylvestre has been used widely in traditional medicine as a remedy for several diseases, and its leaf extract is known to contain a group of bioactive triterpene saponins belonging to the gymnemic acid class. Gymnemic Acid I (1) is one of the main components among this group of secondary metabolites and is endowed with an interesting bioactivity profile. Since there is a lack of information about its specific biological targets, the full interactome of 1 was investigated through a quantitative chemical proteomic approach, based on stable-isotope dimethyl labeling. The ribosome complex was found to be the main partner of compound 1, and a full validation of the proteomics results was achieved by orthogonal approaches. Further biochemical and biological investigations revealed an inhibitory effect of 1 on the ribosome machinery.
Structure Activity Relationship Studies of Gymnemic Acid Analogues for Antidiabetic Activity Targeting PPARγ
Curr Comput Aided Drug Des 2015;11(1):57-71.PMID:26058590DOI:10.2174/1573409911666150610093611.
Diabetes accounts for high mortality rate worldwide affecting million of lives annually. Global prevalence of diabetes and its rising frequency makes it a key area of research in drug discovery programs. The research article describes the development of quantitative structure activity relationship model against PPARγ, a promising drug target for diabetes. Multiple linear regression approach was adopted for statistical model development and the QSAR relationship suggested the regression coefficient (r2) of 0.84 and the cross validation coefficient (rCV2) of 0.77. Further, the study suggested that chemical descriptors viz., dipole moment, electron affinity, dielectric energy, secondary amine group count and LogP correlated well with the activity. The docking studies showed that most active gymnemic acid analogues viz., gymnemasin D and gymnemic acid VII possess higher binding affinity to PPARγ. QSAR and ADMET studies based other predicted active gymnemc acid analogues were Gymnemic Acid I, gymnemic acid II, gymnemic acid III, gymnemic acid VIII, gymnemic acid X, gymnemic acid XII, gymnemic acid XIV, gymnemic acid XVIII and gymnemoside W2. Predicted activity results of three query compounds were found comparable to experimental in vivo data. Oral bioavailability of these active analogues is still a limiting factor and therefore further lead optimization required. Also, such study would be of great help in active pharmacophore discovery and lead optimization, and offering new insights into therapeutics for diabetes mellitus.