Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki- 54124, Greece.
Department of Pharmacy, School of Health Sciences, Frederick University, Nicosia 1036, Cyprus.
Curr Top Med Chem. 2019;19(4):276-291. doi: 10.2174/1568026619666190129122727.
The biotransformation of xenobiotics is a homeostatic defensive response of the body against bioactive invaders. Xenobiotic metabolizing enzymes, important for the metabolism, elimination and detoxification of exogenous agents, are found in most tissues and organs and are distinguished into phase I and phase II enzymes, as well as phase III transporters. The cytochrome P450 superfamily of enzymes plays a major role in the biotransformation of most xenobiotics as well as in the metabolism of important endogenous substrates such as steroids and fatty acids. The activity and the potential toxicity of numerous drugs are strongly influenced by their biotransformation, mainly accomplished by the cytochrome P450 enzymes, one of the most versatile enzyme systems.
In this review, considering the importance of drug metabolising enzymes in health and disease, some of our previous research results are presented, which, combined with newer findings, may assist in the elucidation of xenobiotic metabolism and in the development of more efficient drugs.
Study of drug metabolism is of major importance for the development of drugs and provides insight into the control of human health. This review is an effort towards this direction and may find useful applications in related medical interventions or help in the development of more efficient drugs.
外源性物质的生物转化是机体对抗生物活性入侵物的一种体内稳态防御反应。对于外源性物质的代谢、消除和解毒,生物转化酶非常重要,这些酶存在于大多数组织和器官中,并分为 I 相和 II 相酶以及 III 相转运体。细胞色素 P450 酶超家族在大多数外源性物质的生物转化以及固醇和脂肪酸等重要内源性底物的代谢中起着主要作用。许多药物的活性和潜在毒性受其生物转化的强烈影响,主要由细胞色素 P450 酶完成,该酶是最具多功能性的酶系统之一。
鉴于药物代谢酶在健康和疾病中的重要性,本文呈现了我们之前的一些研究结果,这些结果与新的发现相结合,可能有助于阐明外源性物质的代谢,并开发更有效的药物。
药物代谢的研究对药物的开发具有重要意义,并为人类健康的控制提供了深入的了解。本文的综述是朝着这个方向努力的,可能在相关的医学干预中具有实用价值,或有助于开发更有效的药物。