Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan.
Chemistry of Natural Compounds Department, National Research Centre, Giza 12622, Egypt.
Molecules. 2023 Jul 27;28(15):5677. doi: 10.3390/molecules28155677.
In the last decade, gypsogenin has attracted widespread attention from medicinal chemists by virtue of its prominent anti-cancer potential. Despite its late identification, gypsogenin has proved itself as a new anti-proliferative player battling for a frontline position among other classic pentacyclic triterpenes such as oleanolic acid, glycyrrhetinic acid, ursolic acid, betulinic acid, and celastrol. Herein, we present the most important reactions of gypsogenin via modification of its four functional groups. Furthermore, we demonstrate insights into the anti-cancer activity of gypsogenin and its semisynthetic derivatives and go further by introducing our perspective to judiciously guide the prospective rational design. The present article opens a new venue for a better exploitation of gypsogenin chemical entity as a lead compound in cancer chemotherapy. To the best of our knowledge, this is the first review article exploring the anti-cancer activity of gypsogenin derivatives.
在过去的十年中，桂莪醇因其显著的抗癌潜力引起了药物化学家的广泛关注。尽管发现较晚，但桂莪醇已被证明是一种新型的抗增殖剂，它在其他经典五环三萜如齐墩果酸、甘草次酸、熊果酸、白桦脂酸和雷公藤红素等中占据一线地位。在此，我们通过修饰其四个官能团展示了桂莪醇最重要的反应。此外，我们展示了桂莪醇及其半合成衍生物的抗癌活性，并进一步引入了我们的观点，以明智地指导预期的合理设计。本文为更好地利用桂莪醇作为癌症化疗的先导化合物开辟了新的途径。据我们所知，这是第一篇探讨桂莪醇衍生物抗癌活性的综述文章。
