ピペリン  (Synonyms: Piperine; Bioperine; 1-Piperoylpiperidine)

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: 61.94±0.054 μg/mL (P-glycoprotein, HeLa cell)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

285.34

C₁₇H₁₉NO₃

94-62-2

Solid

White to light yellow

O=C(N1CCCCC1)/C=C/C=C/C2=CC=C(OCO3)C3=C2

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Paarakh PM, et al. In vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn. In Silico Pharmacol. 2015 Dec;3(1):9. Epub 2015 Oct 29.  [Content Brief]

  [2]. Meghwal M,et al. Piper nigrum and piperine: an update. Phytother Res. 2013 Aug;27(8):1121-30.  [Content Brief]

  [3]. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93.  [Content Brief]

  [4]. Zhai WJ, et al. Piperine Plays an Anti-Inflammatory Role in Staphylococcus aureus Endometritis by Inhibiting Activation of NF-κB and MAPK Pathways in Mice. Evid Based Complement Alternat Med. 2016;2016:8597208.  [Content Brief]