Chang Chi-Chang, Hsu Hsia-Fen, Huang Kuo-Hung, Wu Jing-Mei, Kuo Shyh-Ming, Ling Xue-Hua, Houng Jer-Yiing
Institute of Biotechnology and Chemical Engineering, I-Shou University, Kaohsiung 84001, Taiwan.
Department of Nutrition, I-Shou University, Kaohsiung 82445, Taiwan.
Molecules. 2014 Dec 1;19(12):19980-94. doi: 10.3390/molecules191219980.
Endometrial cancer is a common malignancy of the female genital tract. This study demonstrates that Siegesbeckia orientalis ethanol extract (SOE) significantly inhibited the proliferation of RL95-2 human endometrial cancer cells. Treating RL95-2 cells with SOE caused cell arrest in the G2/M phase and induced apoptosis of RL95-2 cells by up-regulating Bad, Bak and Bax protein expression and down-regulation of Bcl-2 and Bcl-xL protein expression. Treatment with SOE increased protein expression of caspase-3, -8 and -9 dose-dependently, indicating that apoptosis was through the intrinsic and extrinsic apoptotic pathways. Moreover, SOE was also effective against A549 (lung cancer), Hep G2 (hepatoma), FaDu (pharynx squamous cancer), MDA-MB-231 (breast cancer), and especially on LNCaP (prostate cancer) cell lines. In total, 10 constituents of SOE were identified by Gas chromatography-mass analysis. Caryophyllene oxide and caryophyllene are largely responsible for most cytotoxic activity of SOE against RL95-2 cells. Overall, this study suggests that SOE is a promising anticancer agent for treating endometrial cancer.
子宫内膜癌是女性生殖道常见的恶性肿瘤。本研究表明,豨莶草乙醇提取物(SOE)显著抑制RL95-2人子宫内膜癌细胞的增殖。用SOE处理RL95-2细胞导致细胞停滞于G2/M期,并通过上调Bad、Bak和Bax蛋白表达以及下调Bcl-2和Bcl-xL蛋白表达诱导RL95-2细胞凋亡。用SOE处理剂量依赖性地增加了caspase-3、-8和-9的蛋白表达,表明凋亡是通过内源性和外源性凋亡途径进行的。此外,SOE对A549(肺癌)、Hep G2(肝癌)、FaDu(咽鳞癌)、MDA-MB-231(乳腺癌)细胞系也有效,尤其是对LNCaP(前列腺癌)细胞系。通过气相色谱-质谱分析共鉴定出SOE的10种成分。氧化石竹烯和石竹烯在很大程度上是SOE对RL95-2细胞的大部分细胞毒性活性的原因。总体而言,本研究表明SOE是一种有前途的治疗子宫内膜癌的抗癌药物。