Isosilybin A 是从水飞蓟中分离出来的一种黄酮木脂素，可抑制癌细胞增殖并诱导 G1 期停滞和凋亡，通过靶向Akt-NF-Κb-雄激素受体轴激活前列腺癌细胞的凋亡机制，具有抗前列腺癌活性。

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC50=12.1-44.9μM) of tyrosinase. Isosilybin A shows anti-angiogenic efficacy, it has anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction.

To investigate the effects of milk thistle extract and its main flavonolignans (silybin A, silybin B, Isosilybin A and isosilybin B) on CYP2C8 activity at relevant concentrations, the effect of milk thistle extract and the flavonolignans on CYP2C8 enzyme activity was studied in vitro using human liver microsomes (HLM) incorporating an enzyme-selective substrate for CYP2C8, amodiaquine. Metabolite formation was analyzed using liquid chromatography-tandem mass spectrometry (LC/MS-MS). The concentration causing 50% inhibition of enzyme activity (IC50) was used to express the degree of inhibition. Isosilibinin, a mixture of the diastereoisomers Isosilybin A and isosilybin B, was found to be the most potent inhibitor, followed by isosilybin B with IC50 values (mean ± SE) of 1.64 ± 0.66 μg/mL and 2.67 ± 1.18 μg/mL, respectively. The rank order of observed inhibitory potency after isosilibinin was silibinin >Isosilybin A >silybin A >milk thistle extract >and silybin B[1]

142796-21-2

C25H22O10

482.44

异水飞蓟素 A;异水飞蓟宾A;水飞蓟素 B2

DMSO:90mg/ml(186.55mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years