Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Phytother Res. 2022 Nov;36(11):4063-4079. doi: 10.1002/ptr.7589. Epub 2022 Oct 11.
Barberry (Berberis vulgaris L.) is a medicinal plant and its main constituent is an isoquinoline alkaloid named berberine that has multiple pharmacological effects such as antioxidant, anti-microbial, antiinflammatory, anticancer, anti-diabetes, anti-dyslipidemia, and anti-obesity. However, it has restricted clinical uses due to its very poor solubility and bioavailability (less than 1%). It undergoes demethylenation, reduction, and cleavage of the dioxymethylene group in the first phase of metabolism. Its phase two reactions include glucuronidation, sulfation, and methylation. The liver is the main site for berberine distribution. Berberine could excrete in feces, urine, and bile. Fecal excretion of berberine (11-23%) is higher than urinary and biliary excretion routes. However, a major berberine metabolite is excreted in urine greater than in feces. Concomitant administration of berberine with other drugs such as metformin, cyclosporine A, digoxin, etc. may result in important interactions. Thus, in this review, we gathered and dissected any related animal and human research articles regarding the pharmacokinetic parameters of berberine including bioavailability, metabolism, distribution, excretion, and drug-drug interactions. Also, we discussed and gathered various animal and human studies regarding the developed products of berberine with better bioavailability and consequently, better therapeutic effects.
小檗（Berberis vulgaris L.）是一种药用植物，其主要成分是一种异喹啉生物碱，名为黄连素，具有多种药理作用，如抗氧化、抗菌、抗炎、抗癌、抗糖尿病、抗血脂异常和抗肥胖。然而，由于其溶解度和生物利用度极低（低于 1%），其临床应用受到限制。它在代谢的第一阶段经历去甲烯化、还原和二氧亚甲基基团的裂解。其二期反应包括葡萄糖醛酸化、硫酸化和甲基化。肝脏是黄连素分布的主要部位。黄连素可以通过粪便、尿液和胆汁排出体外。黄连素的粪便排泄（11-23%）高于尿液和胆汁排泄途径。然而，一种主要的黄连素代谢物在尿液中的排泄量大于粪便。黄连素与其他药物如二甲双胍、环孢素 A、地高辛等同时给药可能会导致重要的相互作用。因此，在这篇综述中，我们收集并剖析了任何与黄连素的药代动力学参数相关的动物和人体研究文章，包括生物利用度、代谢、分布、排泄和药物相互作用。此外，我们还讨论和收集了各种关于具有更好生物利用度的黄连素开发产品的动物和人体研究，从而具有更好的治疗效果。
