药学学报, 2019, 54(1): 117-121
引用本文:
齐欢, 马正, 薛正莲, 阮海宁, 高美越, 张辉, 俞晓平, 王继栋. 利福霉素抗性突变菌Streptomyces sp.HS-NF-1046R中的两个新化合物[J]. 药学学报, 2019, 54(1): 117-121.
QI Huan, MA Zheng, XUE Zheng-lian, RUAN Hai-ning, GAO Mei-yue, ZHANG Hui, YU Xiao-ping, WANG Ji-dong. Two new compounds from rifamycin resistant mutant strain Streptomyces sp. HS-NF-1046R[J]. Acta Pharmaceutica Sinica, 2019, 54(1): 117-121.

利福霉素抗性突变菌Streptomyces sp.HS-NF-1046R中的两个新化合物
齐欢1,3, 马正1, 薛正莲2, 阮海宁3, 高美越3, 张辉3, 俞晓平1, 王继栋2,3
1. 中国计量大学生命科学学院, 浙江省生物计量与检疫检验重点实验室, 浙江 杭州 310018;
2. 安徽工程大学生物与化学工程学院, 微生物发酵安徽省工程技术中心, 安徽 芜湖 241000;
3. 浙江海正药业股份有限公司, 浙江省抗真菌药物重点实验室, 浙江 台州 318000
摘要:
采用硅胶色谱、凝胶色谱及液相色谱分离纯化一株利福霉素抗性突变菌Streptomyces sp.HS-NF-1046R发酵物中的次级代谢产物,通过波谱技术鉴定了3个化合物:3-hydroxyl-2-N-propionyl-anthranilamide(1)、2,3-dihydro-8-hydroxy-2,2-dimethyl quinazolin-4-(1H)-one(2)和2-aminobenzamide(3),其中12是新化合物。通过SRB法评价新化合物的细胞毒活性,化合物12对人肺癌细胞A549、人肝癌细胞HepG2、人结肠癌细胞HCT-116和白血病细胞K562的IC50值均大于100 μmol·L-1,未表现出明显的细胞毒性。
关键词:    链霉菌      利福霉素抗性筛选      次级代谢产物      结构解析     
Two new compounds from rifamycin resistant mutant strain Streptomyces sp. HS-NF-1046R
QI Huan1,3, MA Zheng1, XUE Zheng-lian2, RUAN Hai-ning3, GAO Mei-yue3, ZHANG Hui3, YU Xiao-ping1, WANG Ji-dong2,3
1. Zhejiang Provincial Key Laboratory of Biometrology and Inspection and Quarantine, College of Life Sciences, China Jiliang University, Hangzhou 310018, China;
2. Microorganism Fermentation Engineering and Technology Research Center of Anhui Province, Institute of Biologic and Chemical Engineering of Anhui Polytechnic University, Wuhu 241000, China;
3. Zhejiang Key Laboratory of Antifungal Drugs, Zhejiang Hisun Pharmaceutical Co., Ltd., Taizhou 318000, China
Abstract:
Using silica gel column chromatography, gel chromatography and HPLC, we isolated secondary metabolites in fermentation broth of a rifamycin resistant mutation strain Streptomyces sp. HS-NF-1046R. Based on spectroscopic data, the chemical structures of three compounds were identified as 3-hydroxyl-2-N-propionyl-anthranilamide (1), 2,3-dihydro-8-hydroxy-2,2-dimethyl quinazolin-4-(1H)-one (2) and 2-aminobenzamide (3). Compounds 1 and 2, as new entities, were evaluated for cytotoxicity against A549, HepG2, HCT-116 and K562 cells using the SRB assay. Compounds 1 and 2 exhibited no cytotoxicity with IC50 over 100 μmol·L-1.
Key words:    Streptomyces    rifamycin resistant screening    secondary metabolites    structure elucidation   
收稿日期: 2018-10-29
DOI: 10.16438/j.0513-4870.2018-0974
基金项目: 国家自然科学基金资助项目(31772213);浙江省杰出青年基金资助项目(LR17C140002).
通讯作者: 俞晓平,Tel:86-571-87676258,E-mail:yuxiaoping19630306@163.com;王继栋,Tel:86-576-88827216,E-mail:jdwang@hisunpharm.com
Email: yuxiaoping19630306@163.com;jdwang@hisunpharm.com
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