Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul 06351, Korea.
Int J Mol Sci. 2022 May 18;23(10):5637. doi: 10.3390/ijms23105637.
Genipin is a protein cross-linking agent extracted from Gardenia ( Ellis) fruits. This fruit has conventionally been used as a Chinese herbal medicine for the treatment of inflammation and jaundice and as an edible colorant in oriental countries. Uncoupling protein (UCP)-2 is a member of the family of uncoupling proteins, which are anion transporters positioned in the mitochondrial inner membrane. Genipin has been shown to have hepatoprotective activity, acting as an effective antioxidant and inhibitor of mitochondrial UCP2, and is also reported to exert significant anticancer effects. In this review, the author presents the latest progress of genipin as an anticancer agent and concisely describes its various mechanisms of action. In brief, genipin inhibits UCP2 to attenuate generation of reactive oxygen species (ROS), leading to ROS/c-Jun N-terminal kinase-dependent apoptosis of cancer cells. Genipin also increases the tissue inhibitors of matrix metalloproteases (MMP)-2, a kind of tumor promoter in a variety of cancers, as well as induces caspase-dependent apoptosis in in vitro and in vivo models. These findings suggest that genipin can serve as a promising novel antitumor agent that could be applicable for chemotherapy and/or chemoprevention for cancers.
京尼平是一种从栀子（Ellis）果实中提取的蛋白质交联剂。这种水果传统上被用作中药，用于治疗炎症和黄疸，并且在东方国家被用作食用色素。解偶联蛋白（UCP）-2 是解偶联蛋白家族的成员，是位于线粒体内膜中的阴离子转运体。京尼平具有肝保护活性，作为一种有效的抗氧化剂和线粒体 UCP2 的抑制剂，并且据报道还具有显著的抗癌作用。在这篇综述中，作者介绍了京尼平作为抗癌剂的最新进展，并简要描述了其各种作用机制。简而言之，京尼平抑制 UCP2 以减轻活性氧（ROS）的产生，导致 ROS/c-Jun N-末端激酶依赖性癌细胞凋亡。京尼平还增加组织基质金属蛋白酶（MMP）-2 的抑制剂，MMP-2 是多种癌症中的一种肿瘤促进剂，并在体外和体内模型中诱导 caspase 依赖性细胞凋亡。这些发现表明，京尼平可以作为一种有前途的新型抗肿瘤药物，可适用于癌症的化疗和/或化学预防。
