2. Academic Validation
  3. Discovery of highly oxygenated cytochalasans with antiproliferative activity from an endophytic fungus Boeremia exigua

Discovery of highly oxygenated cytochalasans with antiproliferative activity from an endophytic fungus Boeremia exigua

  • Bioorg Chem. 2025 Mar:156:108198. doi: 10.1016/j.bioorg.2025.108198.
Chun Tian 1,  Yuanyuan Feng 2,  Hanqi Zhang 2,  Xinyu Mao 1,  Xinyao Zhu 1,  Xiang Wang 1,  Chang Hou 1,  Xiaoyang Han 3,  Huixiang Yang 4,  Jikai Liu 5
Affiliations

Affiliations

  • 1 Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China.
  • 2 Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Science & Technology Industrial Parks of Anhui University of Chinese Medicine, Hefei 230012 China.
  • 3 Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Science & Technology Industrial Parks of Anhui University of Chinese Medicine, Hefei 230012 China. Electronic address: hanxy@ahtcm.edu.cn.
  • 4 Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Science & Technology Industrial Parks of Anhui University of Chinese Medicine, Hefei 230012 China. Electronic address: yanghuixiang@ahtcm.edu.cn.
  • 5 Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Science & Technology Industrial Parks of Anhui University of Chinese Medicine, Hefei 230012 China. Electronic address: liujikai@ahtcm.edu.cn.
PMID: 39864369 DOI: 10.1016/j.bioorg.2025.108198
Abstract

Eleven cytochalasans (1-11), including six undescribed analogues (1-3 and 5-7) and a new natural product (4), were obtained from the endophytic fungus Boeremia exigua. Their structures and absolute configurations were determined by a combination of extensive spectroscopic techniques, electron circular dichroism (ECD), and single-crystal X-ray diffraction. Boerelasin E (1) represented the first cytochalasan possessing a cis-configured Δ21(22) double bond. The growth-inhibitory activities of all the isolates 1-11 against five human tumor cells were examined. Boerelasin E (1) exhibited the most potent inhibitory effect on MCF-7 cells with an IC50 value of 4.89 μM, even about four times lower than positive control cis-platin (IC50 = 20.52 μM). Further mechanistic investigations revealed that 1 could inhibit the complete cell division of MCF-7 cells by arresting them in the G2/M phase and induced Apoptosis.

Keywords

Antiproliferative activity; Boeremia exigua; Cytochalasans; Endophytic fungi.

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