Casticin(Synonyms: 蔓荆子黄素; Vitexicarpin)

天然产物 黄酮类 Flavonoids

Casticin (Synonyms: 蔓荆子黄素; Vitexicarpin) 纯度: 99.67%

Casticin 是从蔓荆子中得到的甲氧基黄酮化合物,具有抗有丝分裂和抗炎活性。Casticin 能够抑制 STAT3 的活化。

Casticin(Synonyms: 蔓荆子黄素; Vitexicarpin)

Casticin Chemical Structure

CAS No. : 479-91-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1650 In-stock
5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
25 mg ¥5200 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.

IC50 & Target

STAT3[3]

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

374.34

Formula

C19H18O8

CAS 号

479-91-4

中文名称

蔓荆子黄素;紫花牡荆素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (267.14 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6714 mL 13.3568 mL 26.7137 mL
5 mM 0.5343 mL 2.6714 mL 5.3427 mL
10 mM 0.2671 mL 1.3357 mL 2.6714 mL

*

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, 6 months; -20°C, 1 month (protect from light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (16.70 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (16.70 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [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 Assay
[2]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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