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Regio-specific biotransformation of alizarin to alizarin methoxide with enhanced cytotoxicity against proliferative cells.
Journal of Industrial Microbiology & Biotechnology ( IF 3.2 ) Pub Date : 2020-06-25 , DOI: 10.1007/s10295-020-02286-4
Trang Thi Huyen Nguyen 1 , Jang Mi Han 1 , Hye Jin Jung 1, 2 , Ramesh Prasad Pandey 1, 2 , Yong Il Park 3 , Jae Kyung Sohng 1, 2
Affiliation  

Alizarin has been reported to have an antigenotoxic activity along with an inhibitory effect on the tumor cell growth of human colon carcinoma cells. Alizarin was biotransformed into an O-methoxide derivative using O-methyltransferase from Streptomyces avermitilis MA4680 (SaOMT2) to enhance its bioefficacy. The biotransformed product was extracted, purified, and characterized using various chromatographic and spectroscopic analyses, and confirmed to be an alizarin 2-O-methoxide. The antiproliferative activity of the compound against gastric cancer cells (AGS), uterine cervical cancer (Hela), liver cancer (HepG2), and normal cell lines was investigated. Alizarin 2-O-methoxide showed an inhibitory effect on all three cancer-cell lines at very low concentrations, from 0.078 µM, with no cytotoxicity against 267B1 (human prostate epithelial) and MRC-5 (normal human fetal lung fibroblast).



中文翻译:

茜素向合成茜素甲醇盐的区域特异性生物转化,对增殖细胞的细胞毒性增强。

据报道茜素具有对人结肠癌细胞的肿瘤细胞生长具有抑制作用的抗原毒性活性。使用来自阿维链霉菌MA4680(SaOMT2)的O-甲基转移酶将茜素生物转化为O-甲醇衍生物,以增强其生物功效。使用各种色谱和光谱分析对生物转化的产物进行提取,纯化和表征,并确认其为茜素2- O-甲醇盐。研究了该化合物对胃癌细胞(AGS),子宫宫颈癌(Hela),肝癌(HepG2)和正常细胞系的抗增殖活性。茜素2- O-甲醇盐在0.078 µM的极低浓度下对所有三种癌细胞系均表现出抑制作用,对267B1(人前列腺上皮)和MRC-5(正常人胎肺成纤维细胞)没有细胞毒性。

更新日期:2020-06-26
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