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类药性膳食香草素通过抑制增殖和调节 bcl 相关凋亡蛋白诱导抗癌活性。

Drug-like dietary vanilloids induce anticancer activity through proliferation inhibition and regulation of bcl-related apoptotic proteins.

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia.

Department of Human Biology, School of Medicine, International Medical University, Kuala Lumpur, Malaysia.

出版信息

Phytother Res. 2018 Jun;32(6):1108-1118. doi: 10.1002/ptr.6051. Epub 2018 Feb 21.

DOI:10.1002/ptr.6051
PMID:29464796
Abstract

In this study, a series of 20 structurally similar vanilloids (Vn) were tested for their antiproliferative effects against 12 human cancer cells: human breast (MCF-7 and MDA-MB-231), cervical (HeLa), ovarian (Caov-3), lung (A549), liver (HepG2), colorectal (HT-29 and HCT116), nasopharyngeal (CNE-1 and HK-1), and leukemic (K562 and CEM-SS) cancer cells. Among all the tested vanilloids, Vn16 (6-shogaol) exhibited the most potent cytotoxic effects against human colorectal cancer cells (HT-29). The apoptotic induction effects exhibited by Vn16 on HT-29 cells were confirmed using dual staining fluorescence microscopy and enzyme-linked immunosorbent assay. The effects of Vn16 on regulation of 43 apoptotic-related markers were determined in HT-29. The results suggested that 8 apoptotic markers (caspase 8, BAD, BAX, second mitochondrial-derived activator, caspase 3, survivin, bcl-2, and cIAP-2) were either upregulated or downregulated. These results further support the chemopreventive properties of foods that contain vanilloids.

摘要

在这项研究中,测试了一系列 20 种结构相似的香草素(Vn)对 12 种人类癌细胞的抗增殖作用:人乳腺癌(MCF-7 和 MDA-MB-231)、宫颈癌(HeLa)、卵巢癌(Caov-3)、肺癌(A549)、肝癌(HepG2)、结直肠癌(HT-29 和 HCT116)、鼻咽癌(CNE-1 和 HK-1)和白血病(K562 和 CEM-SS)。在所有测试的香草素中,Vn16(6-姜烯酚)对人结直肠癌细胞(HT-29)表现出最强的细胞毒性作用。通过双染色荧光显微镜和酶联免疫吸附试验证实了 Vn16 对 HT-29 细胞的凋亡诱导作用。在 HT-29 中测定了 Vn16 对调节 43 个凋亡相关标记物的影响。结果表明,8 个凋亡标记物(半胱天冬酶 8、BAD、BAX、线粒体衍生的第二激活物、半胱天冬酶 3、存活素、bcl-2 和 cIAP-2)被上调或下调。这些结果进一步支持了含有香草素的食物的化学预防特性。

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