Diphyllin is an orally active V-ATPase inhibitor ( IC 50 =17 nM) and HIV-1 inhibitor (IC 50 =0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC 50 =0.6 nM for acid influx inhibition), thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption.
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