Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, And School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, PR China.
Wuya College of Innovation, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, PR China.
Eur J Med Chem. 2020 Mar 1;189:112087. doi: 10.1016/j.ejmech.2020.112087. Epub 2020 Jan 25.
Based on the definite therapeutic benefits, such as neuroprotective, cardioprotective, anticancer, anti-diabetic and so on, the Panax genus which contains many valuable plants, including ginseng (Panax ginseng C.A. Meyer), notoginseng (Panax notoginseng) and American ginseng (Panax quinquefolius L.), attracts research focus. Actually, the biological and pharmacological effects of the Panax genus are mainly attributed to the abundant ginsenosides. However, the low membrane permeability and the gastrointestinal tract influence seriously limit the absorption and bioavailability of ginsenosides. The acid or base hydrolysates of ginsenosides, 20 (R,S)-panaxadiol and 20 (R,S)-protopanaxadiol showed improved bioavailability and diverse pharmacological activities. Moreover, relative stable skeletons and active hydroxyl group at C-3 position and other reactive sites are suitable for structural modification to improve biological activities. In this review, the pharmacological activities of panaxadiol, protopanaxadiol and their structurally modified derivatives are comprehensively summarized.
基于明确的治疗益处，如神经保护、心脏保护、抗癌、抗糖尿病等，包含许多有价值植物的人参属（Panax ginseng C.A. Meyer）、三七（Panax notoginseng）和西洋参（Panax quinquefolius L.）引起了研究关注。实际上，人参属的生物学和药理学作用主要归因于丰富的人参皂苷。然而，人参皂苷的低膜通透性和胃肠道影响严重限制了其吸收和生物利用度。人参皂苷的酸或碱水解产物，20（R，S）-人参二醇和 20（R，S）-原人参二醇显示出改善的生物利用度和多样化的药理学活性。此外，相对稳定的骨架和 C-3 位及其他反应性位点的活性羟基基团适合进行结构修饰以提高生物活性。在这篇综述中，全面总结了人参二醇、原人参二醇及其结构修饰衍生物的药理学活性。
