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Piperine

CAS No. : 94-62-2

MCE 国际站：Piperine

产品活性：Piperine是从胡椒中分离的天然生物碱，可以抑制P-glycoprotein and CYP3A4的活性，在HeLa细胞中的IC₅₀值为61.94±0.054 μg/mL。

研究领域：Membrane Transporter/Ion Channel  |  Autophagy  |  Metabolic Enzyme/Protease

作用靶点：P-glycoprotein  |  Autophagy  |  Endogenous Metabolite

结构分类：生物碱  |  哌啶类生物碱  |  结构分类

来源：植物  |  胡椒科  |  胡椒

In Vitro: Piperine has shown to possess in vitro cytotoxic activity and in silico studies. The IC₅₀ value is found to be 61.94±0.054 μg/mL and in silico studies, it has more number of hydrogen bonds with minimum binding and docking energy and may be considered as inhibitor of EGFR tyrosine kinase. Piperine has been found to have immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogenic, anti-inflammatory, anti-ulcer, and anti-amoebic properties. Piperine could enhance the bioavailabilities of other drugs including rosuvastatin, peurarin and docetaxel (DOX) via inhibition of CYP3A and P-glycoprotein activity.

In Vivo: At the dose of 3.5 mg/kg, the bioavailability of piperine is calculated to be 25.36%. Its AUC_0→t is unproportionally increased with doses, indicating a potential non-linear pharmacokinetics profile of piperine. It is found that the AUC_0→t and C₀ of Docetaxel (HY-B0011) and t_1/2 of piperine are significantly increased after their combination use, suggesting potential enhanced bioavailability of not only Docetaxel but also Piperine, which may lead to the overall enhanced pharmacological effects. The phosphorylation of I-κB, p65, p38, ERK, and JNK is inhibited by piperine in a dose-dependent manner, indicating that piperine may be a potential anti-inflammatory drug both in endometritis and in other S. aureus-induced diseases.

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