Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (7): 1376-1381.DOI: 10.6023/cjoc201403032 Previous Articles     Next Articles



漆丽华a, 张媚b, 潘海学b, 陈晓东a, 唐功利b   

  1. a 江西中医药大学药学院 南昌 330004;
    b 中国科学院上海有机化学研究所 生命有机化学国家重点实验室 上海 200032
  • 收稿日期:2014-03-13 修回日期:2014-03-24 发布日期:2014-04-02
  • 通讯作者: 唐功利;
  • 基金资助:


Production of a Trioxacarcin Analogue by Engineering of Its Biosynthetic Pathway

Qi Li-Huaa, Zhang Meib, Pan Hai-Xueb, Chen Xiao-Donga, Tang Gong-Lib   

  1. a College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004;
    b State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032
  • Received:2014-03-13 Revised:2014-03-24 Published:2014-04-02
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 81202442).

Trioxacarcins, derived from streptomyces, are aromatic polyketide natural products with antitumor activity. The production of trioxacarcins was improved significantly by optimizing the fermentation and purification processes. The biosynthetic pathway of trioxacarcins was changed by inactivating an acyltransferase (Trx49) gene in the trioxacarcin cluster, and an analogue compound 1 lacking the O-acetyl group of sugar on C-4 was obtained. The influence of the O-acetyl group on biological activity of trioxacarcins was investigated by in vitro cytotoxicity test. Compared with trioxacarcin A, the activity of compound 1 decreases to some extent but still persists an excellent anti-tumor activity level with IC50 value of 4.86 nmol·L-1.

Key words: trioxacarcin, biosynthesis, natural product, acyltransferase