NOTES

Discovery of Tiancimycin Congeners from Streptomyces sp. CB03234-S

  • Lu Xue ,
  • Lihua Zhang ,
  • Chengyu Zhang ,
  • Xin Zhao ,
  • Weifan Dang ,
  • Zhaoxin Wang ,
  • Chunhua Wang ,
  • Tongchuan Suo ,
  • Xiaohui Yan
Expand
  • a Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617
    b State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191
    c College of Pharmaceutical Engineering of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617

Received date: 2021-11-10

  Revised date: 2021-12-09

  Online published: 2021-12-31

Supported by

National Science Foundation of China(81872779); State Key Laboratory of Natural and Biomimetic Drugs(K202116)

Abstract

Tiancimycins (TNMs) are anthraquinone-fused enediynes with phenomenal antitumor activity. By heterologous expression of two cytochrome P450 hydroxylase genes, dynE10 and dynOrf19, in the TNMs high-producing strain Streptomyces sp. CB03234-S, three TNM derivatives 1~3 were isolated. Their chemical structures were determined by one-dimensional and two-dimensional NMR, high resolution mass spectrometry and circular dichroism. TNM H (1) is the C-9-hydroxylated product of TNM D, TNM T1 (2) is a cycloaromatized product, and TNM T3 (3) is a known compound. Compound 1 exhibited strong antitumor activity against the four tested cancer cell lines, including HeLa, MB49, B16 and BIU87.

Cite this article

Lu Xue , Lihua Zhang , Chengyu Zhang , Xin Zhao , Weifan Dang , Zhaoxin Wang , Chunhua Wang , Tongchuan Suo , Xiaohui Yan . Discovery of Tiancimycin Congeners from Streptomyces sp. CB03234-S[J]. Chinese Journal of Organic Chemistry, 2022 , 42(4) : 1241 -1247 . DOI: 10.6023/cjoc202111018

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