整合生物学期刊网

应用天然产物 ›› 2017, Vol. 7 ›› Issue (4): 329-334.DOI: 10.1007/s13659-017-0136-8

• Original article • 上一篇    

α-Pyrone Derivatives from a Streptomyces Strain Resensitize Tamoxifen Resistance in Breast Cancer Cells

Rui-Min Yang1,2, Xiu-Lei Zhang1, Li Wang1, Jian-Ping Huang1, Jing Yang1, Yi-Jun Yan1, Jian-Ying Luo1, Xiang-Ting Wang1, Sheng-Xiong Huang1   

  1. 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China;
    2. University of the Chinese Academy of Sciences, Beijing 100049, People's Republic of China
  • 收稿日期:2017-05-31 修回日期:2017-06-05 出版日期:2017-08-24 发布日期:2018-02-07
  • 通讯作者: Sheng-Xiong Huang,e-mail:sxhuang@mail.kib.ac.cn
  • 基金资助:
    This research was financially supported by the National Natural Science Foundation of China to S-X.H (No. 81522044) and to X.W (No. 31471226), High-end Science and Technology Talents Program of Yunnan Province to S-X.H (No. 2013HA022), and a Grant from the Thousand Youth Talents Program of China.

α-Pyrone Derivatives from a Streptomyces Strain Resensitize Tamoxifen Resistance in Breast Cancer Cells

Rui-Min Yang1,2, Xiu-Lei Zhang1, Li Wang1, Jian-Ping Huang1, Jing Yang1, Yi-Jun Yan1, Jian-Ying Luo1, Xiang-Ting Wang1, Sheng-Xiong Huang1   

  1. 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China;
    2. University of the Chinese Academy of Sciences, Beijing 100049, People's Republic of China
  • Received:2017-05-31 Revised:2017-06-05 Online:2017-08-24 Published:2018-02-07
  • Supported by:
    This research was financially supported by the National Natural Science Foundation of China to S-X.H (No. 81522044) and to X.W (No. 31471226), High-end Science and Technology Talents Program of Yunnan Province to S-X.H (No. 2013HA022), and a Grant from the Thousand Youth Talents Program of China.

摘要: Tamoxifen resistance (TamR) is the underlying cause of treatment failure in many breast cancer patients receiving tamoxifen. In order to look for noncytotoxic natural products with the ability to reverse TamR, an extract from strain Streptomyces sp. KIB-H0495 was detected to be active. Subsequent large scale fermentation and isolation led to the isolation of four α-pyrone derivatives including two new compounds, violapyrones J (2) and K (3), and two known analogues, violapyrones B (1) and I (4). Further bioactivity assays indicated that only 1 and 3 exerted potent resensitization effects on MCF-7/TamR cells at a concentration of 1 μM. Owing to the simple structures of 1 and 3, these two compounds might have potential for further investigation as novel tamoxifen resensitization agent in breast cancer chemotherapy.

关键词: Breast cancer, Tamoxifen resistance, Resensitization, α-Pyrone derivatives, Streptomyces

Abstract: Tamoxifen resistance (TamR) is the underlying cause of treatment failure in many breast cancer patients receiving tamoxifen. In order to look for noncytotoxic natural products with the ability to reverse TamR, an extract from strain Streptomyces sp. KIB-H0495 was detected to be active. Subsequent large scale fermentation and isolation led to the isolation of four α-pyrone derivatives including two new compounds, violapyrones J (2) and K (3), and two known analogues, violapyrones B (1) and I (4). Further bioactivity assays indicated that only 1 and 3 exerted potent resensitization effects on MCF-7/TamR cells at a concentration of 1 μM. Owing to the simple structures of 1 and 3, these two compounds might have potential for further investigation as novel tamoxifen resensitization agent in breast cancer chemotherapy.

Key words: Breast cancer, Tamoxifen resistance, Resensitization, α-Pyrone derivatives, Streptomyces