Molecules (Dec 2022)

Axl, Immune Checkpoint Molecules and HIF Inhibitors from the Culture Broth of <i>Lepista luscina</i>

  • 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

DOI
https://doi.org/10.3390/molecules27248925
Journal volume & issue
Vol. 27, no. 24
p. 8925

Abstract

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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.

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