Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India.
Department of Neurodegenerative Science, Van Andel Institute, Grand Rapids, Michigan, 49503, USA.
Curr Pharm Des. 2023;29(17):1326-1340. doi: 10.2174/1381612829666230529164321.
Apigenin is a natural polyphenolic compound widely distributed as a glycoside in fruits and vegetables. Apigenin belongs to BCS class II with low solubility, which leads to poor absorption and bioavailability. It is mostly absorbed from the small intestine and extensively metabolized through glucuronidation and sulfation processes. Apigenin is known for its antioxidant and anti-inflammatory properties. It is also used as a chemopreventive drug in the management of various cancers. Pharmacological effects of apigenin have a wide range, from neuroprotective to treating renal disorders. Apigenin is non-toxic in nature and acts through various pathways (JAK/STAT, Wnt/β-catenin, MAPK/ERK, PI3K/Akt, and NF-κB) to exert its therapeutic efficacy. Numerous formulations have been researched to enhance the bioavailability and pharmacological effects of apigenin. Combinatorial therapies are also researched to minimize the side-effects of chemotherapeutic drugs. The review presents pharmacokinetic and pharmacodynamic aspects of apigenin. Apigenin is safe for the treatment and management of numerous diseases. It can be easily incorporated into nanoformulation alone or in combination with other active ingredients to widen the therapeutic window. This review intends to help in drug optimization and therapeutic efficacy maximization for future studies.
芹菜素是一种天然多酚类化合物，广泛分布于水果和蔬菜中，以糖苷的形式存在。芹菜素属于 BCS 分类 II 类，溶解度低，导致吸收不良和生物利用度差。它主要从小肠吸收，并通过葡萄糖醛酸化和硫酸化过程广泛代谢。芹菜素有抗氧化和抗炎特性。它也被用作各种癌症管理中的化学预防药物。芹菜素的药理作用广泛，从神经保护到治疗肾脏疾病。芹菜素性质无毒，通过各种途径（JAK/STAT、Wnt/β-catenin、MAPK/ERK、PI3K/Akt 和 NF-κB）发挥治疗功效。已经研究了许多制剂来提高芹菜素的生物利用度和药理作用。还研究了联合治疗以最小化化疗药物的副作用。该综述介绍了芹菜素的药代动力学和药效学方面。芹菜素可安全用于治疗和管理许多疾病。它可以单独或与其他活性成分一起轻松纳入纳米制剂，以扩大治疗窗口。本综述旨在帮助药物优化和治疗效果最大化，以用于未来的研究。
