Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H+-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 12 mg/mL|
Anti-HIV lignans from Justicia procumbens
Xin-Ya Xu, et al. Chin J Nat Med. 2019 Dec;17(12):945-952. PMID: 31882050.
Diphyllin, a novel and naturally potent V-ATPase inhibitor, abrogates acidification of the osteoclastic resorption lacunae and bone resorption
Mette G Sorensen, et al. J Bone Miner Res. 2007 Oct;22(10):1640-8. PMID: 17576165.
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