Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Liaoning Province, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, 110016, China; Jilin Yizheng Pharmaceutical Group Co., Ltd., Jilin Province, Siping, 136001, China.
Phytochemistry. 2021 Nov;191:112895. doi: 10.1016/j.phytochem.2021.112895. Epub 2021 Aug 14.
Prenylated flavonoids, a unique class of flavonoids which combine a flavonoid skeleton and a lipophilic prenyl side-chain, possess great potential biological activities including cytotoxicity, anti-inflammation, anti-Alzheimer, anti-microbial, anti-oxidant, anti-diabetes, estrogenic, vasorelaxant and enzyme inhibition. Recently, prenylated flavonoids have become an indispensable anchor for the development of new therapeutic agents, and have received increasing from medicinal chemists. The prenylated flavonoids have been outstanding developed through isolation, semi or fully synthesis in a very short period of time, which proves the great value in medicinal chemistry researches. In this review, research progress of prenylated flavonoids including natural prenylated flavonoids, structural modification, synthetic methodologies and pharmacological activities was summarized comprehensively. Furthermore, the structure-activity relationships (SARs) of prenylated flavonoids were summarized which provided a basis for the selective design and optimization of multifunctional prenylated flavonoid derivatives for the treatment of multi-factorial diseases in clinic.
烯丙基化黄酮类化合物是一类独特的黄酮类化合物，它结合了黄酮骨架和脂溶性烯丙基侧链，具有巨大的潜在生物学活性，包括细胞毒性、抗炎、抗阿尔茨海默病、抗菌、抗氧化、抗糖尿病、雌激素、血管舒张和酶抑制作用。最近，烯丙基化黄酮类化合物已成为开发新治疗剂不可或缺的基础，受到越来越多的药物化学家的关注。在很短的时间内，通过分离、半合成或全合成，烯丙基化黄酮类化合物得到了显著的发展，这证明了其在药物化学研究中的巨大价值。本综述全面总结了烯丙基化黄酮类化合物的研究进展，包括天然烯丙基化黄酮类化合物、结构修饰、合成方法和药理活性。此外，还总结了烯丙基化黄酮类化合物的构效关系（SAR），为选择性设计和优化多功能烯丙基化黄酮类衍生物治疗多因素疾病提供了依据。
