文章摘要
李会伟,段金廒,刘培,张森,江曙,陶伟伟.莲藕中白桦脂酸的微生物转化及其产物的抗肿瘤活性研究[J].南京中医药大学学报(自然科学版),2017,33(2):144-149.
莲藕中白桦脂酸的微生物转化及其产物的抗肿瘤活性研究
Biotransformation of Betulinic Acid From Nelumbinis Rhizoma and Cytotoxicity Determination of the Fermentation Products Against Cancer Cell Lines
投稿时间:2017-01-05  修订日期:2017-02-23
DOI:
中文关键词: 白桦脂酸  生物转化  莲藕  解淀粉芽孢杆菌
英文关键词: betulinic acid  biotransformation  Nelumbinis Rhizoma  Bacillus amyloliquefaciens
基金项目:
作者单位
李会伟,段金廒*,刘培*,张森,江曙,陶伟伟 南京中医药大学江苏省中药资源产业化过程协同创新中心中药资源产业化与方剂创新药物国家地方联合工程研究中心中药品质与效能国家重点实验室培育江苏 南京 ;210023 
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中文摘要:
      目的 对莲藕中的白桦脂酸进行微生物转化,并对转化产物分离纯化,解析其结构特征,评价其抗肿瘤活性,以提高莲藕资源的利用率。方法 采用HPLC-PDA法测定莲藕根茎不同部位白桦脂酸的含量;筛选具有转化作用的菌种,采用UPLC-Q-TOF/MS方法对发酵产物进行分析;采用硅胶柱层析法分离转化产物,NMR和MS法解析发酵产物结构特征;利用细胞分子生物学技术测定衍生物抗肿瘤活性。结果 莲藕不同部位(藕尖、藕肉、藕皮、藕节、藕尾)中白桦脂酸含量以藕节中最高,为0.621%,筛选得到一株具有转化白桦脂酸的菌种Bacillus amyloliquefaciens FJ18,该菌转化藕节中的白桦脂酸(1),获得2个转化产物,分别为3β-hydroxy-lup-20(29)-en-28-oic acid 28-O-(4-oxy-4-oxobutanoic acid-4-O-β-D-glucopyranosyl) ester(2)和28-O-β-D-glucopyranosyl-3β-hydroxy-lup-20(29)-en-28-oate(3),其中化合物2为新化合物。体外细胞毒性实验表明转化产物对A375、Hela、U251、SH-SY5Y和MCF-7等肿瘤细胞均有一定的细胞毒活性。结论 通过微生物发酵从藕节中获得具有抗肿瘤活性的白桦脂酸转化产物,其中一个为新化合物。
英文摘要:
      OBJECTIVE Betulinic acid (BA) from the waste of Nelumbinis Rhizoma (NR) was introduce sugar groups at specific positions by biotransformation. The fermentation products were isolated and purified. Their structural characterization and antitumor activities were also investigated, which may improve utilization of NR. METHODS The content levels of BA in different parts of NR were analyzed by the modified HPLC-PDA method. With the transformation ability of strains screened, the transformation products were analyzed using a UPLC-QTOF-MS method, isolated and purified by silica gel column chromatography repeatedly. The structure characteristics were analyzed by NMR and MS. Cell viability was evaluated by the methylthiazolyl tetrazolium (MTT) assay. RESULTS The content of BA(1) in the nodus was measured to be 0.621%, the highest in the parts of NR. The strain, identified as Bacillus amyloliquefaciens FJ18, was used in the biotransformation. A novel glycosylation derivative of betulinic acid (BA) derivative, 3β-hydroxy-lup-20(29)-en-28-oic acid 28-O-(4-oxy-4-oxobutanoic acid-4-O-β-D-glucopyranosyl) ester, together with a known derivative, 28-O-β-D-glucopyranosyl-3β-hydroxy-lup-20(29)-en-28-oate were obtained by bioconversion of BA. Their structures were determined on the basis of spectroscopic data. The biotransformation products showed in vitro cytotoxic activity against A375 (melanoma), HeLa (cervical carcinoma), U251 (glioma), SH-SY5Y (neuroblastoma) and MCF-7 (breast cancer) cell lines. CONCLUSION The biotransformation of betulinic acid to the derivatives featuring D- glucopyranosyl moieties was accomplished. The in vitro cytotoxicity study revealed that the derivatives exhibit potent cytotoxic activity against cancer cell lines.
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