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

来自 Lepista luscina 培养液的 Axl、免疫检查点分子和 HIF 抑制剂

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作者: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

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.

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