Methylnissolin
(Synonyms: 黄芪紫檀烷苷; Astrapterocarpan) 目录号 : GC36596
A flavonoid with antiproliferative activity
Cas No.:73340-41-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
3-hydroxy-9,10-Dimethoxypterocarpan is a flavonoid that has been found in A. membranaceus and has antiproliferative activity.1 It inhibits PDGF-BB-induced proliferation of, and DNA synthesis in, A-10 vascular smooth muscle cells (IC50s = 10 and 1 ?M, respectively).
1.Onhawara, S., Okuma, Y., Uehara, T., et al.Astrapterocarpan isolated from Astragalus membranaceus inhibits proliferation of vascular smooth muscle cellsEur. J. Pharmacol.525(1-3)41-47(2005)
| Cas No. | 73340-41-7 | SDF | |
| 别名 | 黄芪紫檀烷苷; Astrapterocarpan | ||
| Canonical SMILES | COC1=C2O[C@]3([H])[C@](COC4=CC(O)=CC=C34)([H])C2=CC=C1OC | ||
| 分子式 | C17H16O5 | 分子量 | 300.31 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3299 mL | 16.6495 mL | 33.2989 mL |
| 5 mM | 0.666 mL | 3.3299 mL | 6.6598 mL |
| 10 mM | 0.333 mL | 1.6649 mL | 3.3299 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。
Danggui Buxue Decoction in the Treatment of Metastatic Colon Cancer: Network Pharmacology Analysis and Experimental Validation
Drug Des Devel Ther 2021 Feb 24;15:705-720.PMID:33658761DOI:10.2147/DDDT.S293046.
Purpose: This study aimed to reveal Danggui Buxue Decoction (DBD) candidate targets and mechanisms in the treatment of metastatic colon cancer (MCC), using network pharmacology-based analyses and experimental validation. Methods: Traditional Chinese Medicine Systems Pharmacology (TCMSP) database query and text mining were used to screen active compounds in DBD, and the Swiss target prediction platform was applied to predict compound-related target proteins. Targets likely associated with MCC were determined using GeneCards and OMIM databases. Targets common to DBD and MCC were obtained from the Venn platform; subsequently, Cytoscape was used to construct drug-compound-target-disease and protein-protein interaction networks. The hub gene was determined by R, while GO and KEGG enrichment analyses were performed on common targets to elucidate biological processes and signaling pathways involved in DBD against MCC. Finally, the metastatic colon cancer mouse model was used to detect the levels of expression of protein Bax, Bcl2, Caspase3, and Cleaved caspase3 by Western blot. Results: A total of 28 active compounds and 61 common targets were predicted. The main compounds were quercetin, hederagenin, jaranol, Methylnissolin, formononetin, calycosin, kaempferol, 3.9-di-O-methylnissolin, 24-propylcholesterol, and 7-O-methylisomucronulatol, present in Astragalus membranaceus (Huangqi, HQ). In addition, beta-sitosterol, ferulic acid, and stigmasterol, present in Angelica sinensis (Danggui, DG), were detected. JUN, PTSG2, EGFR, ESR1and, CASP3 genes were the top 5 hub genes in the PPI network. GO and KEGG enrichment analyses indicated that apoptosis played a major role in the biological processes and signaling pathways involved. Moreover, the in vivo experiment revealed that DBD inhibited MCC by up-regulating the expression of Bax, Caspase3, and Cleaved caspase3, and by down-regulating the expression of Bcl2. Conclusion: This study revealed candidate DBD targets and mechanisms in the treatment of MCC, using network pharmacology-based analyses and experimental validation. The present findings provide a reference for tumor treatment during the perioperative period.
Rapid Quantitative Analysis of 19 Bioactive Components in Fangji Huangqi Decoction Based on UHPLC-MS/MS
J Chromatogr Sci 2022 Oct 15;bmac085.PMID:36250324DOI:10.1093/chromsci/bmac085.
Fangji Huangqi Decoction (FHD) is a classic prescription of traditional Chinese medicine which is recorded in "Jin Gui Yao Lue". The purpose of this study is to develop a method for simultaneous determination multicomponent in FHD. The separation of the 19 compounds that included calycosin, calycosin-7-O-β-D-glucoside, formononetin, ononin, Methylnissolin, methylnissolin-3-O-glucoside, isomucronulatol, tetrandrine, fangchinoline, atractylenolide-I, atractylenolide-III, liquiritigenin, liquiritin, isomucronulatol-7-O-β-D-glucoside, astragaloside-I, astragaloside-II, astragaloside-III, astragaloside-IV and glycyrrhetinic acid were achieved by linear gradient elution. The 19 components were identified by comparing the chromatographic peaks with the reference compounds and were quantitatively analyzed by multiple reaction monitoring. This method was strict validated with recovery (96.10-101.70%), precision [relative standard deviation (RSD), 1.34-3.34%], stability (RSD, 1.49-3.80%) and repeatability (RSD, 1.60-3.49%), respectively. All the compounds showed good linearities (R2 > 0.999). The limit of detection (LOD) and limit of quantitation (LOQ) for the 19 compounds were in the range of 0.03-0.27 μg/mL (LODs) and 0.05-1.23 μg/mL (LOQs). The correlation analysis indicated that astragalus flavonoids were negatively correlated with astragalosides, tetrandrine and their corresponding flavonoid glycosides, and atractylenolides were positively correlated with astragalosides and fangchinoline. This method proved to be reliable and effective, which would give a helpful basis for the quality control, pharmacological and pharmacokinetic of FHD.
[Determination of eight active components of Bufei Huoxue Capsules in rat plasma and their pharmacokinetics by UHPLC-MS/MS]
Zhongguo Zhong Yao Za Zhi 2022 Jan;47(1):215-223.PMID:35178928DOI:10.19540/j.cnki.cjcmm.20211109.201.
An ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS) method was established to investigate the pharmacokinetic behaviors of psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, psoralen, isopsoralen, Methylnissolin, and neobavaisoflavone in rat plasma after oral administration of Bufei Huoxue Capsules. After SD rats were administered with Bufei Huoxue Capsules suspension by gavage, blood samples were collected from the inner canthus at different time points. After protein precipitation, plasma samples were separated on ACQUITY UPLC BEH C_(18) column(2.1 mm×100 mm, 1.7 μm). The mobile phase consisted of acetonitrile(A) and water(B) containing 0.1% formic acid in gradient elution. The positive and negative ions were measured simultaneously in the multi-reaction monitoring(MRM) mode. The pharmacokinetic parameters were calculated and fitted by DAS 3.2.8. Psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, psoralen, isopsoralen, Methylnissolin, and neobavaisoflavone were detected in the rat plasma after drug administration, with AUC_(0-t) of(3 357±1 348),(3 555±1 696),(3.03±0.88),(2.21±0.33),(1 787±522),(2 295±539),(5.69±1.41) and(3.40±0.75) μg·L~(-1)·h, and T_(max) of(1.56±0.62),(1.40±0.70),(0.21±0.05),(0.25±0.12),(0.26±0.11),(0.34±0.29),(0.74±0.59), and 0.25 h. The method is proved specific and repeatable and is suitable for the determination of psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, pso-ralen, isopsoralen, Methylnissolin, and neobavaisoflavone in the rat plasma, which can be applied to pharmacokinetic study.
Methodological Verification-based Screening of the Representative Ingredients for Traditional Chinese Medicine: Taking Astragalus as an Example for Interfering with Cervical Cancer
Curr Comput Aided Drug Des 2022;18(5):347-362.PMID:36017857DOI:10.2174/1573409918666220823120304.
Background: The screening of effective ingredients is the bridge between the research of efficacy and the mechanism of traditional Chinese medicine. Although promising virtual screening has emerged as an attractive alternative, an ideal strategy is still urgently required due to the characteristics of multi-ingredients and multi-targets of traditional Chinese medicine. Objective: The aim of the study was to develop a methodological verification-based novel screening strategy capable of comprehensively assessing the ability of compounds to perturb disease networks, thereby identifying representative ingredients of traditional Chinese medicine interventions in complex diseases. Methods: In this article, we take astragalus interfering with cervical cancer as an example. First, a multifunctional clustering disease network model was constructed; second, the several drugs and their decoys were used for molecular docking with disease network clusters for methodological verification and determining the best scoring criteria. Third, the representative ingredients of astragalus were screened according to the best scoring criteria. Finally, the effects of the representative ingredients on cervical cancer SiHa cells were evaluated by CCK-8 assay, flow cytometry, and western blot analysis. Results: Three representative ingredients of astragalus were betulinic acid, hederagenin and Methylnissolin, which perturbed the apoptosis, stabilization of p53, and G1/S transition cluster as a whole, respectively. CCK-8 assay showed that the IC50 value of betulinic acid, hederagenin and Methylnissolin at 48 h was 28.84, 101.90, and 187.40 μM, respectively. Flow cytometry showed that these three representative ingredients could significantly induce early apoptosis and cell cycle arrest. Western blot analysis showed that betulinic acid treatment significantly increased p53 expression, while hederagenin and Methylnissolin did not. Conclusion: This study has provided new ideas for the screening of effective ingredients in traditional Chinese medicine, and established a foundation for elucidating the overall mechanism of action of traditional Chinese medicine.
The Anti-inflammatory Effects of Isoflavonoids from Radix Astragali in Hepatoprotective Potential against LPS/D-gal-induced Acute Liver Injury
Planta Med 2023 Apr;89(4):385-396.PMID:36509104DOI:10.1055/a-1953-0369.
Radix Astragali (RA) is an important Traditional Chinese Medicine widely used in the treatment of various diseases, such as pneumonia, atherosclerosis, diabetes, kidney and liver fibrosis. The role of isoflavonoids from RA in the treatment of liver injury remains unclear. The study aimed to explore hepatoprotective and anti-inflammatory effects of isoflavonoids from Astragalus mongholicus. Network pharmacological analysis showed that RA had a multi-target regulating effect on alleviating liver injury and inhibiting inflammation through its active ingredients, among which isoflavones were closely related to its key molecular targets. The anti-inflammatory and liver protection effects of isoflavonoids of RA were investigated using lipopolysaccharide (LPS)-induced RAW 264.7 cells in vitro and LPS/D-galactosamine (D-gal)-induced acute liver injury mice in vivo. The experimental results showed that Methylnissolin (ML) and methylnissolin-3-O-β-D-glucoside (MLG) presented more notable anti-inflammatory effects. Both of them suppressed the release of pro-inflammatory cytokines, such as iNOS, COX-2, IL-1β, IL-6, and TNF-α in LPS-stimulated RAW 264.7 cells. In vivo investigation demonstrated that ML markedly meliorated liver injury in LPS/D-gal-induced mice. Western blot results revealed that ML and MLG down-regulated the expression of proinflammatory cytokines via NF-κB signaling pathway. The isoflavonoids, Methylnissolin (ML), and methylnissolin-3-O-β-D-glucoside (MLG), play a vital role in the hepatoprotective and anti-inflammatory effects of RA.