Anticancer effects of a novel class rosin-derivatives with different mechanisms

作者：Xing Yanhong; Zhang Wei; Song Jingjing; Zhang Yixin; Jiang Xianxing; Wang Rui^*

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(13): 3868-3872.

DOI：10.1016/j.bmcl.2013.04.069

• Rosin
• Dehydroabietic acid
• Apoptosis
• Necrosis
• Caspase
• Cancer

In this Letter, the anticancer activity of novel rosin-derivatives introducing indicated side chains at position C18 of dehydroabietic acid (DHAA) was reported. Gratifyingly, all of these derivatives showed significantly cytotoxicity toward diverse human carcinoma cell lines. We found the compound 4 could induce cell membrane damage at high concentration as well as cell apoptosis at low concentration. However, compound 5, attachment of quinidine to dehydroabietic acid via thiourea bond, only induced apoptotic cell death. In addition, all these active compounds induced apoptosis mainly through mitochondrial-dependent pathway. Interestingly, compound 5 exhibited the highest anticancer activity and little toxicity to normal cells compared with the other derivatives. Therefore, 5 merits further investigation as a potential agent for future anticancer treatment.

• 出版日期2013-7-1
• 单位兰州大学