Piperine

Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL^[1][2][3]. IC50 & Target:IC50: 61.94±0.054 μg/mL (P-glycoprotein, HeLa cell)^[1] 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^[1]. Piperine has been found to have immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogenic, anti-inflammatory, anti-ulcer, and anti-amoebic properties^[2]. Piperine could enhance the bioavailabilities of other drugs including rosuvastatin, peurarin and docetaxel (DOX) via inhibition of CYP3A and P-glycoprotein activity^[3]. 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^[3]. 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^[4].