Faculty of Pharmacy, Integral University, Lucknow, Uttar Pradesh, India.
J Basic Clin Physiol Pharmacol. 2021 Feb 8;33(3):223-233. doi: 10.1515/jbcpp-2020-0099.
N-acetylcysteine (NAC) is considered as the body's major antioxidant molecules with diverse biological properties. In this review, the pharmacokinetics, safety and efficacy report on both the preclinical and clinical summary of NAC is discussed. Both and preclinical studies along with the clinical data have shown that NAC has enormous biological properties. NAC is used in the treatment of acetaminophen poisoning, diabetic nephropathy, Alzheimer's disease, schizophrenia, and ulcerative colitis, etc. Numerous analytical techniques, for instance, UPLC, LC-MS, HPLC, RP-IPC are primarily employed for the estimation of NAC in different single and fixed-dose combinations. The molecular docking studies on NAC demonstrate the binding within Sudlow's site-I hydrogen bonds and formation of NAC and BSA complexes. Various hydrophobic and hydrophilic amino acids generally exist in making contact with NAC as NAC-BSA complexes. Docking studies of NAC with the active site of the urease exposed an O-coordinated bond through nickel 3002 and a hydrogen bond through His-138. NAC and its analogs also made the allosteric pockets that helped to describe almost all favorable pose for the chaperone in a complex through the protein. Thus, we intended to highlight the several health benefits of this antioxidant compound and applications in pharmaceutical product development.
N-乙酰半胱氨酸(NAC)被认为是体内主要的抗氧化分子,具有多种生物学特性。本综述讨论了 NAC 的药代动力学、安全性和疗效报告,包括临床前和临床总结。临床前研究和临床数据均表明,NAC 具有巨大的生物学特性。NAC 用于治疗对乙酰氨基酚中毒、糖尿病肾病、阿尔茨海默病、精神分裂症和溃疡性结肠炎等疾病。目前主要采用 UPLC、LC-MS、HPLC、RP-IPC 等多种分析技术来测定 NAC 在不同单药和固定剂量组合中的含量。NAC 的分子对接研究表明,它与 Sudlow 位点 I 氢键结合,形成 NAC 和 BSA 复合物。作为 NAC-BSA 复合物,通常存在各种疏水性和亲水性氨基酸与 NAC 接触。NAC 与脲酶活性位点的对接研究表明,通过镍 3002 形成 O 配位键,并通过 His-138 形成氢键。NAC 及其类似物还形成了变构口袋,有助于通过蛋白质描述伴侣在复合物中的几乎所有有利构象。因此,我们旨在强调这种抗氧化化合物的多种健康益处及其在药物产品开发中的应用。