Laboratory of Clinical Pharmacy, Showa Pharmaceutical University, Higashi Tamagawa Gakuen, Machida, Tokyo 194-8543, Japan.
Laboratory of Clinical Pharmacy, Showa Pharmaceutical University, Higashi Tamagawa Gakuen, Machida, Tokyo 194-8543, Japan.
Phytomedicine. 2015 May 15;22(5):545-52. doi: 10.1016/j.phymed.2015.03.008. Epub 2015 Mar 27.
Natural products are one of the most important sources of drugs used in pharmaceutical therapeutics. Screening of several natural products in the search for novel anticancer agents against human leukemia HL-60 cells led us to identify potent apoptosis-inducing activity in the essential oil fraction from Artemisia capillaris Thunb. flower.
The cytotoxic effects of extracts were assessed on human leukemia HL-60 cells by XTT assay. Induction of apoptosis was assessed by analysis of DNA fragmentation and nuclear morphological change. The plant name was checked with the plant list website (http://www.theplantlist.org).
A purified compound from the essential oil fraction from Artemisia capillaris Thunb. flower that potently inhibited cell growth in human leukemia HL-60 cells was identified as capillin. The cytotoxic effect of capillin in cells was associated with apoptosis. When HL-60 cells were treated with 10(-6) M capillin for 6 h, characteristic features of apoptosis such as DNA fragmentation and nuclear fragmentation were observed. Moreover, activation of c-Jun N-terminal kinase (JNK) was detected after treatment with capillin preceding the appearance of characteristic properties of apoptosis. Release of cytochrome c from mitochondria was also observed in HL-60 cells that had been treated with capillin.
Capillin induces apoptosis in HL-60 cells via the mitochondrial apoptotic pathway, which might be controlled through JNK signaling. Our results indicate that capillin may be a potentially useful anticancer drug that could enhance therapeutic efficacy.
天然产物是药物治疗中使用的药物的最重要来源之一。在寻找针对人白血病 HL-60 细胞的新型抗癌剂的过程中,对几种天然产物进行筛选,导致我们在青蒿花的精油部分中发现了具有强大诱导细胞凋亡活性的物质。
通过 XTT 测定法评估提取物对人白血病 HL-60 细胞的细胞毒性作用。通过分析 DNA 片段化和核形态变化来评估细胞凋亡的诱导。植物名称通过植物名录网站(http://www.theplantlist.org)进行核对。
从青蒿花的精油部分中分离出的一种能有效抑制人白血病 HL-60 细胞生长的纯化化合物被鉴定为青蒿素。青蒿素在细胞中的细胞毒性作用与细胞凋亡有关。当 HL-60 细胞用 10(-6) M 的青蒿素处理 6 小时时,观察到 DNA 片段化和核片段化等凋亡的特征。此外,在用青蒿素处理后,检测到 c-Jun N-末端激酶 (JNK) 的激活,随后出现凋亡的特征。在用青蒿素处理的 HL-60 细胞中还观察到线粒体细胞色素 c 的释放。
青蒿素通过线粒体凋亡途径诱导 HL-60 细胞凋亡,这可能通过 JNK 信号通路进行调控。我们的结果表明,青蒿素可能是一种有潜在用途的抗癌药物,可增强治疗效果。