Pestalotinones A-D, new benzophenone antibiotics from endophytic fungus Pestalotiopsis trachicarpicola SC-J551

  • J Antibiot (Tokyo). 2022 Apr;75(4):207-212. doi: 10.1038/s41429-022-00510-0.
Zhiming Jiang  1  2 ,  Ping Wu  3 ,  Hanxiang Li  1 ,  Jinghua Xue  1 ,  Xiaoyi Wei  1
Affiliations
  • 1. Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Xingke Road 723, Tianhe District, Guangzhou, 510650, People's Republic of China.
  • 2. School of Life Sciences, University of Chinese Academy of Sciences, Yuquanlu 19A, Beijing, 100049, People's Republic of China.
  • 3. Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Xingke Road 723, Tianhe District, Guangzhou, 510650, People's Republic of China. [email protected].
PMID: 35115699 DOI: 10.1038/s41429-022-00510-0
Abstract

Four new pestalone-type benzophenones, pestalotinones A-D (1-4), along with six known congeners, pestalone, pestalone E-F, SB87-Cl, SB87-H, and pestalachloride B, were isolated from the endophytic fungus Pestalotiopsis trachicarpicola SC-J551 cultivated on rice grains. Their structures were established by extensive spectroscopic analysis. Compounds 1-3 exhibited potent activity against Staphylococcus aureus and MRSA (MIC: 1.25-2.5 μg ml-1) while no cytotoxicity against Vero cells (IC50 > 50 μM). The activity profile of this group of compounds suggested that replacement of the C-14 aldehyde with an oxymethyl greatly increases their activity and selectivity towards the bacteria and chlorine substitutions result in the increase of Antibacterial activity and slight decrease of cytotoxicity against the mammalian cells.

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