Pharmacotherapeutics Unit, Department of Medicine, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 UPM, Serdang, Selangor, Malaysia.
Department of Pharmaceutical Chemistry, School of Pharmacy, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.
Drug Discov Today. 2019 Sep;24(9):1890-1898. doi: 10.1016/j.drudis.2019.05.017. Epub 2019 May 30.
Andrographolide (AGP), a naturally occurring bioactive compound, has been investigated as a lead compound in cancer drug development. Its multidimensional therapeutic effects have raised interest among medicinal chemists, which has led to extensive structural modification of the compound, resulting in analogues with improved pharmacological and pharmaceutical properties. Nevertheless, the analogues with the improved properties need to be rigorously studied to identify drug-like lead compounds. We scrutinised articles published from 2012 to 2018, to objectively provide opinions on the mechanisms of action of AGP and its analogues, as well as their potential as viable anticancer drugs. Preclinical and clinical data, along with the extensive medicinal chemistry efforts, indicate the compounds are potential anticancer agents with specific value in treating recalcitrant cancers such as pancreatic and lung cancers.
穿心莲内酯（AGP）是一种天然存在的生物活性化合物，已被研究作为癌症药物开发的先导化合物。其多维治疗效果引起了药物化学家的兴趣，这导致了对该化合物的广泛结构修饰，产生了具有改善的药理学和药物特性的类似物。然而，具有改善特性的类似物需要经过严格的研究，以确定类似物是否具有药物样的先导化合物。我们仔细研究了 2012 年至 2018 年发表的文章，客观地提供了关于 AGP 及其类似物的作用机制的意见，以及它们作为可行的抗癌药物的潜力。临床前和临床数据以及广泛的药物化学研究表明，这些化合物是具有特定价值的潜在抗癌药物，特别适用于治疗难治性癌症，如胰腺癌和肺癌。
