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Isosilybin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Isosilybin图片
CAS NO:72581-71-6
包装与价格:
包装价格(元)
20 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Isosilibinin
Isosilybinin
Silymarin
异水飞蓟宾
Q-100795
Silybin B
产品介绍
Isosilybin 是一种类黄酮,来源于乳蓟;能够抑制CYP3A4诱导(IC50:74 μM)。

产品描述

Isosilybin and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.

体外活性

The reporter gene assay shows that milk thistle’s components silybin and isosilybin are responsible for the inhibition of PXR-mediated CYP3A4 induction by milk thistle. The isomer isosilybin is a stronger inhibitor of PXR-mediated CYP3A4 induction compared with silybin. A solution of 89, 133, and 200 μM isosilybin significantly inhibits CYP3A4 induction by 64, 82, and 88%, respectively. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM[1]. Isosilybin B and isosilybin A, two diastereoisomers isolated from silymarin, have anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction. Isosilybin B and isosilybin A treatment results in growth inhibition and cell death together with a strong G(1) arrest and apoptosis in human prostate cancer LNCaP and 22Rv1 cells[2]. Isosilybin B causes increased phosphorylation of Akt (Ser-473 and Thr-308) and Mdm2 (Ser-166), which is linked with androgen receptor degradation as pretreatment with PI3K inhibitor (LY294002)-restored androgen receptor level. Isosilybin B treatment enhances the formation of complex between Akt, Mdm2 and AR, which promotes phosphorylation-dependent AR ubiquitination and its degradation by proteasome[3]. Isosilybin A is able to significantly activate PPARγ at a concentration of 30 μM (2.08±0.48 fold, p<0.01). Isosilybin A causes transactivation of a PPARγ-dependent luciferase reporter in a concentration-dependent manner. In silico docking studies suggests a binding mode for 3 distinct from that of the inactive silymarin constituents, with one additional hydrogen bond to Ser342 in the entrance region of the ligand-binding domain of the receptor[4].

细胞实验

LNCaP cells and 22Rv1 cells are plated and treated at 40–50% confluency with different doses of isosilybin B and isosilybin A (10–90 μM in medium) dissolved originally in Dimethyl sulfoxide (DMSO) for the desired time periods (24–48 h) in serum condition. An equal amount of DMSO (vehicle) is present in each treatment, including control; DMSO concentration did not exceed 0.1% (v/v) in any treatment. At the end of desired treatments, total cell number is determined by counting each sample in duplicate using a hemocytometer under an inverted microscope. Cell viability is determined using trypan blue exclusion method[2].

Cas No.

72581-71-6

分子式

C25H22O10

分子量

482.441

别名

Isosilibinin;Isosilybinin;Silymarin;异水飞蓟宾;Q-100795;Silybin B

储存和溶解度

DMSO:88 mg/mL(182.4 mM)
Chloroform, Dichloromethane, Ethyl Acetate:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years