Chitkara College of Pharmacy, Chitkara University, Punjab, India.
NCRD'S Sterling Institute of Pharmacy, Navi Mumbai, India.
Curr Mol Pharmacol. 2021 Oct 25;14(4):477-486. doi: 10.2174/1874467213666200722152636.
Piperine is a key bioactive alkaloid found in plants of piperaceae family. The compound possesses various medicinal and pharmacological activities (cholesterol-lowering, anti-cancer, Alzheimer's disease etc.). Owing to its various target receptors (TRPV1, P-gp, CYP3A4 etc.) and several mechanisms, piperine has been studied as bio-enhancer for other drugs and its role has been evidenced in the literature. When administered with other drugs, it increases the absorption of other drugs, thereby reducing the dose and dose-related toxic potential. There are various mechanisms of piperine as a bio-enhancer and the common ones are i) prevention of efflux of drug molecules out of the cells; ii) decreased metabolism of drugs, thereby prolonging the halflife of drugs resulting in reduced urinary excretion. The detailed mechanism indicating the bio-enhancing role of piperine along with various target receptors has not been comprehensively summarised to date.
Literature related to the molecular, enzymatic and receptor targets of piperine were studied, and database was collected using various search engines such as j-gate, google scholar, scihub, pubmed, sciencedirect, etc. The literature related to therapeutic activities of piperine and its bio-enhancer role for other drugs has been thoroughly studied and compiled in brief.
A detailed summary of piperine targets, along with related mechanisms, has been stated. A brief therapeutic profile of piperine alone has been produced with supporting literature. Piperine role as a potential bio-enhancer for other drugs has been summarized.
Piperine is a fascinating molecule of natural origin with several modes of its action, not only possesses its own therapeutic activity but also enhances the therapeutic efficacy of other synthetic and natural drug molecules. Combination dosage forms of various API incorporating piperine as a bio-enhancer can be a potential area of thrust for upcoming drug design and development.
胡椒碱是胡椒科植物中的一种主要生物活性生物碱。该化合物具有多种药用和药理活性（降低胆固醇、抗癌、阿尔茨海默病等）。由于其多种靶受体（TRPV1、P-gp、CYP3A4 等）和几种机制，胡椒碱已被研究作为其他药物的生物增强剂，其作用在文献中已有证据。当与其他药物一起给药时，它会增加其他药物的吸收，从而减少剂量和剂量相关的毒性潜力。胡椒碱作为生物增强剂有多种机制，常见的机制有：i）防止药物分子从细胞中流出；ii）减少药物代谢，从而延长药物半衰期，减少尿液排泄。迄今为止，尚未全面总结胡椒碱作为生物增强剂的详细机制及其与各种靶受体的相互作用。
研究了与胡椒碱的分子、酶和受体靶标相关的文献，并使用各种搜索引擎（如 j-gate、google scholar、scihub、pubmed、sciencedirect 等）收集数据库。深入研究了胡椒碱的治疗活性及其作为其他药物生物增强剂的作用，并简要汇编。
详细说明了胡椒碱的靶标及其相关机制。并简要介绍了胡椒碱的单独治疗概况，并提供了相关文献支持。总结了胡椒碱作为其他药物潜在生物增强剂的作用。
胡椒碱是一种具有多种作用方式的天然来源的迷人分子，不仅具有自身的治疗活性，而且还增强了其他合成和天然药物分子的治疗效果。将含有胡椒碱作为生物增强剂的各种 API 组合成剂型可能是未来药物设计和开发的一个有潜力的领域。
