Lee Magnolia Muk-Lan, Chan Brandon Dow, Wong Wing-Yan, Leung Tsz-Wing, Qu Zhao, Huang Junrong, Zhu Lizhi, Lee Chi-Sing, Chen Sibao, Tai William Chi-Shing
Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China.
State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen 518057, China.
ACS Omega. 2020 Jun 15;5(24):14586-14596. doi: 10.1021/acsomega.0c01276. eCollection 2020 Jun 23.
Cancer is the second leading cause of death globally, responsible for an estimated 9.6 million deaths in 2018, and this burden continues to increase. Therefore, there is a clear and urgent need for novel drugs with increased efficacy for the treatment of different cancers. Previous research has demonstrated that brevilin A () exerts anticancer activity in various cancers, including human multiple myeloma, breast cancer, lung cancer, and colon carcinoma, suggesting the anticancer potential present in the chemical scaffold of . Here, we designed and synthesized a small library of 12 novel BA derivatives and evaluated the biological anticancer effects of the compounds in various cancer cell lines. The results of this structure-activity relationship study demonstrated that BA derivatives and possessed significantly improved anticancer activity toward lung, colon, and breast cancer cell lines. and could more effectively reduce cancer cell viability and induce DNA damage, cell-cycle arrest, and apoptosis when compared with . Our findings represent a significant step forward in the development of novel anticancer entities.
癌症是全球第二大致死原因，2018年估计导致960万人死亡，且这一负担仍在持续增加。因此，迫切需要研发出疗效更佳的新型抗癌药物。先前的研究表明，短叶苏木酚A（）在多种癌症中发挥抗癌活性，包括人类多发性骨髓瘤、乳腺癌、肺癌和结肠癌，这表明其化学结构中存在抗癌潜力。在此，我们设计并合成了一个包含12种新型BA衍生物的小型文库，并评估了这些化合物在多种癌细胞系中的生物抗癌作用。这项构效关系研究的结果表明，BA衍生物和对肺癌、结肠癌和乳腺癌细胞系具有显著增强的抗癌活性。与相比，和能更有效地降低癌细胞活力，诱导DNA损伤、细胞周期停滞和细胞凋亡。我们的研究结果代表了新型抗癌实体研发方面的重大进展。
