Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga-142001, Punjab, India.
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga-142001, Punjab, India.
Bioorg Med Chem. 2021 May 15;38:116143. doi: 10.1016/j.bmc.2021.116143. Epub 2021 Apr 2.
In the last few decades, traditional natural products have been the center of attention for the scientific community and exploration of their therapeutic abilities is proceeding perpetually. Berberine, with remarkable therapeutic diversity, is a plant derived isoquinoline alkaloid which is widely used as a traditional medicine in China. Berberine has been tackled as a fascinating pharmacophore to make great contributions to the discovery and development of new therapeutic agents against variegated diseases. Despite its tremendous therapeutic potential, clinical utility of this alkaloid was significantly compromised due to undesirable pharmacokinetic properties. To overcome this limitation, several structural modifications were performed on this scaffold to improve its therapeutic efficacy. The collective efforts of the community have achieved the tremendous advancements, bringing berberine to clinical use and discovering new therapeutic opportunities by structural modifications on the berberine scaffold. In this review, recent advancements in the medicinal chemistry of berberine and its derivatives in the last few years (2016-2020) have been compiled to represent inclusive data associated with various biological activities of this alkaloid. The comprehensive structure-activity relationship studies along with molecular modelling and mechanistic studies have also been summarized. This article would be highly helpful for the scientific community to get better insight into medicinal research of berberine and become a compelling guide for the rational design of berberine based compounds.
在过去的几十年中，传统天然产物一直是科学界关注的焦点，对其治疗能力的探索一直在不断进行。小檗碱是一种具有显著治疗多样性的植物衍生的异喹啉生物碱，在中国被广泛用作传统药物。小檗碱已被视为一种引人注目的药效团，为发现和开发针对各种疾病的新型治疗药物做出了巨大贡献。尽管具有巨大的治疗潜力，但由于不理想的药代动力学特性，这种生物碱的临床应用受到了严重限制。为了克服这一限制，对该支架进行了几种结构修饰，以提高其治疗效果。通过对小檗碱支架进行结构修饰，该领域的集体努力取得了巨大进展，使小檗碱得以临床应用，并发现了新的治疗机会。在这篇综述中，我们编译了过去几年（2016-2020 年）小檗碱及其衍生物在药物化学方面的最新进展，以展示与该生物碱各种生物活性相关的综合数据。还总结了全面的构效关系研究以及分子建模和机制研究。这篇文章将对科学界深入了解小檗碱的医学研究非常有帮助，并成为基于小檗碱的化合物合理设计的有力指南。
