Diphyllin 是一种从Justicia procumbens中分离的芳基萘木脂素，是HIV-1的有效抑制剂，IC50 为 0.38 μM。它是V-ATPase抑制剂，IC50值为 17 nM，可抑制人破骨细胞中的溶酶体酸化。它抑制NO产生，IC50值为 50 μM ，具有抗癌和抗炎活性。

Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling.

The in vitro inhibitory effects of these compounds were evaluated on the production of nitric oxide (NO) and cytokines (tumor necrosis factor (TNF)-alpha and interleukin (IL)-12), from LPS/IFN-gamma activated murine peritoneal macrophages. The results indicated that the 50% inhibition concentration (IC(50)) values of NO production from activated peritoneal macrophages by compounds 1-4 were 100, 25, 12.5 and 50 microM, respectively. In parallel, these dilutions were approximately inhibited in a similar manner to that observed for cytokines (TNF-alpha, and IL-12) production. On the other hand, at 100 microM concentration compounds 3 and 4 showed 50% inhibition of NO production from peritoneal macrophages that had been pre-activated with LPS/IFN-gamma for 24h, whereas compounds 1 and 2 inhibited only about 20 and 10%, respectively.

22055-22-7

C21H16O7

380.35

二叶草素;山荷叶素

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