Axl, Immune Checkpoint Molecules and HIF Inhibitors from the Culture Broth of Lepista luscina

Mihaya Kotajima, Jae Hoon Choi, Mitsuru Kondo, Corina N. D’Alessandro-Gabazza, Masaaki Toda, Taro Yasuma, Esteban C. Gabazza, Yukihiro Miwa, Chiho Shoda, Deokho Lee, Ayaka Nakai, Toshihide Kurihara, Jing Wu, Hirofumi Hirai, Hirokazu Kawagishi

Research output: Contribution to journalArticlepeer-review

Abstract

Two compounds 1 and 2 were isolated from the culture broth of Lepista luscina. This is the first time that compound 1 was isolated from a natural source. The structure of compound 1 was identified via 1D and 2D NMR and HRESIMS data. Compounds 1 and 2 along with 8-nitrotryptanthrin (4) were evaluated for their biological activities using the A549 lung cancer cell line. As a result, 1 and 2 inhibited the expression of Axl and immune checkpoint molecules. In addition, compounds 1, 2 and 4 were tested for HIF inhibitory activity. Compound 2 demonstrated statistically significant HIF inhibitory effects on NIH3T3 cells and 1 and 2 against ARPE19 cells.

Original languageEnglish
Article number8925
JournalMolecules
Volume27
Issue number24
DOIs
Publication statusPublished - 2022 Dec

Keywords

  • Axl
  • Lepista luscina
  • hypoxia-inducible factor
  • immune checkpoint molecules
  • tryptanthrin

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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