Withaferin A
(Synonyms: 醉茄素A) 目录号 : GC17309
Withaferin A是一种甾体内酯，通常从冬虫夏草（Withania somnifera (L.) Dunal）中提取。
Cas No.:5119-48-2
Sample solution is provided at 25 µL, 10mM.
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Withaferin A is a steroidal lactone generally obtained from Withania somnifera (L.) Dunal, commonly known as Ashwagandha[1]. Withaferin A can inhibits NF-κB at a very low concentration in endothelial cells[2] and exhibits a broad spectrum of biological activities, including antioxidant, anti-inflammatory, antibacterial, antistress, cardioprotective, neuroprotective, and anticancer activities[3]. Withaferin A is commonly utilized in cancer research due to its anticancer activities against various cancer cell lines and preclinical cancer models, achieved by modulating the expression and activity of different oncogenic proteins[4].
Withaferin A potently inhibited cell proliferation in human MPM cells, treatment with Withaferin A at 5µM for 72h significantly inhibit cell growth[5]. In MCF-7 cells, treatment with Withaferin A at 2.5µM for 24h can increase in the level of total as well as S15 phosphorylated p53, which has been implicated in apoptosis induction[6].
Withaferin A (4mg/kg; 14d; i.p.) treatment can inhibits Isoproterenol-induced myocardial fibrosis in mice and significantly reduce heart necrosis[7]. Treatment with Withaferin A (4mg/kg; 10d; i.p.) significantly reduced murine solid tumour growth and improved survival rate of tumour bearing mice[8].
References:
[1]. Paul S, Chakraborty S, Anand U, et al. Withania somnifera (L.) Dunal (Ashwagandha): A comprehensive review on ethnopharmacology, pharmacotherapeutics, biomedicinal and toxicological aspects. Biomed Pharmacother. 2021 Nov;143:112175. doi: 10.1016/j.biopha.2021.112175. Epub 2021 Sep 27. PMID: 34649336.
[2]. Mohan R, Hammers HJ, Bargagna-Mohan P, et al. Withaferin A is a potent inhibitor of angiogenesis. Angiogenesis. 2004;7(2):115-22. doi: 10.1007/s10456-004-1026-3. PMID: 15516832.
[3]Tewari D, Chander V, Dhyani A, et al. Withania somnifera (L.) Dunal: Phytochemistry, structure-activity relationship, and anticancer potential. Phytomedicine. 2022 Apr;98:153949. doi: 10.1016/j.phymed.2022.153949. Epub 2022 Jan 19. PMID: 35151215.
[4]. Kumar S, Mathew SO, Aharwal RP, et al. Withaferin A: A Pleiotropic Anticancer Agent from the Indian Medicinal Plant Withania somnifera (L.) Dunal. Pharmaceuticals (Basel). 2023 Jan 22;16(2):160. doi: 10.3390/ph16020160. PMID: 37259311; PMCID: PMC9966696.
[5]. Yang H, Wang Y, Cheryan VT, et al. Withaferin A inhibits the proteasome activity in mesothelioma in vitro and in vivo. PLoS One. 2012;7(8):e41214. doi: 10.1371/journal.pone.0041214. Epub 2012 Aug 17. PMID: 22912669; PMCID: PMC3422308.
[6]. Hahm ER, Lee J, Huang Y, et al. Withaferin a suppresses estrogen receptor-α expression in human breast cancer cells. Mol Carcinog. 2011 Aug;50(8):614-24. doi: 10.1002/mc.20760. Epub 2011 Mar 22. PMID: 21432907; PMCID: PMC3129407.
[7]. Challa AA, Vukmirovic M, Blackmon J, et al. Withaferin-A reduces type I collagen expression in vitro and inhibits development of myocardial fibrosis in vivo. PLoS One. 2012;7(8):e42989. doi: 10.1371/journal.pone.0042989. Epub 2012 Aug 10. PMID: 22900077; PMCID: PMC3416765.
[8]. Abeesh P, Vishnu WK, Guruvayoorappan C. Preparation and characterization of withaferin A loaded pegylated nanoliposomal formulation with high loading efficacy: In vitro and in vivo anti-tumour study. Mater Sci Eng C Mater Biol Appl. 2021 Sep;128:112335. doi: 10.1016/j.msec.2021.112335. Epub 2021 Jul 27. Erratum in: Mater Sci Eng C Mater Biol Appl. 2021 Nov;130:112432. doi: 10.1016/j.msec.2021.112432. PMID: 34474886.
Withaferin A是一种甾体内酯，通常从冬虫夏草（Withania somnifera (L.) Dunal）中提取[1]。Withaferin A 在内皮细胞中能以极低浓度抑制NF-κB[2]，此外Withaferin A表现出广泛的生物活性，包括抗氧化、抗炎、抗菌、抗应激、心脏保护、神经保护和抗癌活性[3]。Withaferin A 常用于癌症研究，它可以通过调节不同致癌蛋白的表达和活性，对多种癌细胞系和临床前癌症模型具有抗癌活性[4]。
Withaferin A 在人类MPM细胞中强效抑制细胞增殖，使用5µM Withaferin A处理72小时可显著抑制细胞生长[5]。在MCF-7细胞中，使用2.5µM Withaferin A处理24小时可增加总p53蛋白及S15位点磷酸化p53蛋白的水平，这与诱导凋亡有关[6]。
使用Withaferin A（4mg/kg；连续14天；腹腔注射）处理可抑制异丙肾上腺素诱导的小鼠心肌纤维化，并显著减少心脏坏死[7]。使用Withaferin A（4mg/kg；连续10天；腹腔注射）处理可显著减少小鼠实体肿瘤生长，并提高肿瘤负荷小鼠的生存率[8]。
| Cell experiment [1]: | |
Cell lines | MPM |
Preparation Method | MPM cells were treated with 5µM dose of Withaferin A for 72h. Then viable/live cells were determined by MTT assay to evaluate cell proliferation. |
Reaction Conditions | 5µM; 72h |
Applications | Withaferin A treatment inhibits MPM cell proliferation. |
| Animal experiment [2]: | |
Animal models | 129 Svev male mice |
Preparation Method | Isoproterenol (50mg/kg) was injected subcutaneously into 129 Svev male mice for 2 consecutive days, while Withaferin A (4mg/kg) was administered intraperitoneally daily for 14 days. 24h after the last injection, hearts were removed, weighed, fixed and processed for histopathologic analysis. |
Dosage form | 4mg/kg; 14d; i.p. |
Applications | Withaferin A was greatly reduced Isoproterenol-induced heart necrosis compared to animals treated with Isoproterenol alone. |
References: | |
| Cas No. | 5119-48-2 | SDF | |
| 别名 | 醉茄素A | ||
| 化学名 | (4S,4aR,5aR,6aS,6bS,9R,9aS,11aS,11bR)-4-hydroxy-9-((S)-1-((R)-5-(hydroxymethyl)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)ethyl)-9a,11b-dimethyl-5a,6,6a,6b,7,8,9,9a,10,11,11a,11b-dodecahydrocyclopenta[1,2]phenanthro[8a,9-b]oxiren-1(4H)-one | ||
| Canonical SMILES | O[C@@H](C=C1)[C@@]23O[C@@H]2C[C@@H]([C@H]4[C@@]5(C)[C@@H]([C@H](C)[C@@H](CC(C)=C6CO)OC6=O)CC4)[C@H](CC5)[C@]3(C1=O)C | ||
| 分子式 | C28H38O6 | 分子量 | 470.6 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | 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。 |
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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 | 2.1249 mL | 10.6247 mL | 21.2495 mL |
| 5 mM | 0.425 mL | 2.1249 mL | 4.2499 mL |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 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。
Quality Control & SDS
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- Purity: >98.00%
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