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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Cytotoxic activity of azulenequinones against human oral tumor cell lines.
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Cytotoxic activity of azulenequinones against human oral tumor cell lines.

机译：天青石烯酮对人口腔肿瘤细胞系的细胞毒活性。

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We investigated twenty-seven azulenequinone derivatives for their relative cytotoxicity against three human normal cell lines (HGF, HPC, HPLF) and four human tumor cell lines (HSG, HSC-2, HSC-3, HL-60). Parent 1,5-azulenequinone showed potent and some tumor-specific cytotoxicity. Halogenated derivatives of 1,5- and 1,7-azulenequinone showed potent cytotoxicity, but lower tumor-specific cytotoxicity. In contrast to other azulenequinones, amino derivatives such as 3-amino-1,5- and 1, 7-azulenequinones showed relatively lower cytotoxic activity. The 3-Phenoxy-1,5-azuleneqinone derivative showed higher cytotoxicity than the 3-phenoxy-1, 7-azulenequinone derivative. 1,5- and 1,7-Azulenequinones generally showed higher cytotoxicity, as compared with tropolones and azulene derivatives. 3- (3-Guaiazulenyl)-1, 5-azulenequinone [12] and 7-isopropyl-3- (4-methylanilino)-2-methyl- 1, 5-azulenequinone [24] showed a relatively higher TS value and induced apoptosis (internucleosomal DNA fragmentation, activation of caspases 3, 8 and 9) in HL-60 and HSC-2 cells, possibly via the activation of both mitochondria-independent (extrinsic) and -dependent (intrinsic) pathways. Western blot analysis showed that [24] slightly increased the intracellular concentration of pro-apoptotic proteins (Bad, Bax) in HSC-2 cells, whereas [12] was much less active. None of the twenty-seven azulenequinones showed anti-HIV activity. These results suggest [12] and [24] as possible candidates for future cancer chemotherapy.
机译：我们研究了二十七个氮杂醌衍生物对三种人类正常细胞系（HGF，HPC，HPLF）和四种人类肿瘤细胞系（HSG，HSC-2，HSC-3，HL-60）的相对细胞毒性。母体1，5-氮杂苯醌显示出强效的和某些肿瘤特异性的细胞毒性。 1,5-和1,7-azulenequinone的卤代衍生物显示出强大的细胞毒性，但较低的肿瘤特异性细胞毒性。与其他天青石烯酮相反，氨基衍生物，例如3-氨基-1,5-和1，7-azulenequinones显示出相对较低的细胞毒活性。 3-苯氧基-1,5-azulenequininone衍生物显示出比3-苯氧基-1，7-azulenequinone衍生物更高的细胞毒性。 1，5-和1，7-Azulenequinoneses通常显示出更高的细胞毒性，与对偶氮酮和azulene衍生物。 3-（3-瓜杂氮烯基）-1、5-氮杂苯醌[12]和7-异丙基-3-（4-甲基苯胺基）-2-甲基-1、5-氮杂苯醌[24]显示相对较高的TS值并诱导凋亡HL-60和HSC-2细胞中的核糖体间DNA片段化，胱天蛋白酶3、8和9的激活）可能是通过线粒体非依赖性（内在）和非依赖性（内在）途径的激活来实现的。蛋白质印迹分析表明[24]略微增加了HSC-2细胞中促凋亡蛋白（Bad，Bax）的细胞内浓度，而[12]则活性低得多。二十七个氮烯马龙没有一个显示出抗HIV活性。这些结果表明[12]和[24]可能是未来癌症化疗的候选者。

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