Vitexicarpin (Casticin)
(Synonyms: 蔓荆子黄素; Vitexicarpin) 目录号 : GN10282
An anticancer flavonol
Cas No.:479-91-4
Sample solution is provided at 25 µL, 10mM.
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Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
Casticin (0.2-1.0 μM) dose-dependently inhibits the proliferation of KB cells, with an IC50 of 0.23 μM on day 3, while shows no significant inhibition on 3T3 Swiss Albino and TIG-103 cells. Casticin (0.6 μM) alters spindle morphology with partial mitotic spindle breakdown or with disordered spindles[1]. Casticin (0-40 μM) dose-dependently inhibits the proliferation of LX2 cells. Casticin (40 μM) suppresses L02 cells proliferation and induces apoptosis. Casticin inhibits fibrotic effects of TGF-β1 on ECM deposition in LX2 cells by evaluating the mRNA levels of TGF-β, collagen α1(I), MMP-2, MMP-9, TIMP-1 and TIMP-2[2]. Casticin (0-8 μM) reduces the viability of 786-O, YD-8, and HN-9 cells, but shows no significant effect on that of the normal HEL 299 cells. Casticin (5 μM) increases cleavage caspase-3 and PPAR, diminishes the levels of B-cell lymphoma-extra large (Bcl-xl), Bcl-2, IAP-1/-2, vascular endothelial growth factor (VEGF), matrix metallopeptidase 9 (MMP-9), and cyclooxygenase 2 (COX-2) proteins in 786-O, YD-8, and HN-9 cells. Casticin (5 μM) also promotes apoptotic cell death, inhibits constitutively active STAT3 in tumor cells, modulates STAT3 activation by altering the activity of upstream STAT3 regulators, and abrogates IL-6-induced STAT3 activation. In addition, Casticin (2.5 μM) enhances the effect of ionizing radiation in 786-O cells and potentiates the therapeutic effect of radiotherapy[3].
Casticin (20 mg/kg, p.o.) has toxic effect on the liver in mice with CCl4-and BDL-induced hepatic injury. Casticin attenuates liver fibrosis induced by CCl4 or BDL in vivo. Casticin inhibits HSC activation and collagen matrix expression by blocking TGF-β/Smad signaling in vivo[2].
References:
[1]. Kobayakawa J, et al. G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.). Cancer Lett. 2004 May 10;208(1):59-64.
[2]. Zhou L, et al. Casticin attenuates liver fibrosis and hepatic stellate cell activation by blocking TGF-β/Smad signaling pathway. Oncotarget. 2017 Apr 27;8(34):56267-56280.
[3]. Lee JH, et al. Casticin inhibits growth and enhances ionizing radiation-induced apoptosis through the suppression of STAT3 signaling cascade. J Cell Biochem. 2018 Dec 5.
Cell experiment: | LX-2 cells or L02 cells are plated at a density of 5 × 103 cells per well in a 96-well plate and treated with Casticin (0-40 μM) for 48 h in growth medium containing serum. Cell proliferation is determined using a CCK-8 assay kit[2]. |
Animal experiment: | Mice[2]Male mice 6-8 weeks of age weighing 20-30 g are kept in a temperature-controlled room with an alternating 12 h dark and light cycle. A total of 32 mice are divided randomly into four groups of 8 animals each: control, Casticin, CCl4, and CCl4 + Casticin. To induce liver fibrosis, CCl4 dissolved in olive oil (20%) is injected intraperitoneally into mice (1.0 mL/kg body weight) in the CCl4 and CCl4 + Casticin groups twice a week for six weeks. Mice in the control group and Casticin group are injected with an equivalent volume of olive oil. Casticin is dissolved in 0.25% Tween-80. After treatment with CCl4 or olive oil for six weeks, mice in the Casticin group and CCl4 + Casticin group receives Casticin (20 mg/kg) by gastric gavage daily for two weeks, and the other two groups are given the equivalent volume of 0.25% Tween-80. After the eight week intervention period, mice are euthanatized under 3% pentobarbital sodium anesthesia (40 mg/kg ip), and the livers and blood from all animals are collected. Serum is obtained by centrifugation (1600 g, 15 min) and stored at −20°C for further examination[2]. |
References: [1]. Kobayakawa J, et al. G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.). Cancer Lett. 2004 May 10;208(1):59-64. | |
| Cas No. | 479-91-4 | SDF | |
| 别名 | 蔓荆子黄素; Vitexicarpin | ||
| 化学名 | 5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-3,6,7-trimethoxychromen-4-one | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C2=C(C(=O)C3=C(C(=C(C=C3O2)OC)OC)O)OC)O | ||
| 分子式 | C19H18O8 | 分子量 | 374.35 |
| 溶解度 | ≥ 37.4mg/mL 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。 |
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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 | 2.6713 mL | 13.3565 mL | 26.713 mL |
| 5 mM | 0.5343 mL | 2.6713 mL | 5.3426 mL |
| 10 mM | 0.2671 mL | 1.3356 mL | 2.6713 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet