Binding of phenochalasin A, an inhibitor of lipid droplet formation in mouse macrophages, on G-actin

  • Drug Discov Ther. 2022 Sep 17;16(4):148-153. doi: 10.5582/ddt.2022.01053.
Keisuke Kobayashi  1  2 ,  Daisuke Matsuda  1 ,  Hiroshi Tomoda  1  3 ,  Taichi Ohshiro  1  2
Affiliations
  • 1. Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
  • 2. Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo, Japan.
  • 3. Laboratory of Drug Discovery, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
PMID: 36002309 DOI: 10.5582/ddt.2022.01053
Abstract

Phenochalasin A, a unique phenol-containing cytochalasin produced by the marine-derived fungus Phomopsis sp. FT-0211, was originally discovered in a cell morphological assay of observing the inhibition of lipid droplet formation in mouse peritoneal macrophages. To investigate the mode of action and binding proteins, phenochalasin A was radio-labeled by 125I. Iodinated phenochalasin A exhibited the same biological activity as phenochalasin A. [125I]Phenochalasin A was found to be associated with an approximately 40 kDa protein, which was identified as G-actin. Furthermore, detail analyses of F-actin formation in Chinese hamster ovary cells (CHO-K1 cells) indicated that phenochalasin A (2 µM) caused elimination of F-actin formation on the apical site of the cells, suggesting that actin-oriented specific function(s) in cytoskeletal processes are affected by phenochalasin A.

Keywords
Phenochalasin; actin; cytochalasin; lipid droplet; macrophages.
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