Niranthin 是一种木脂素，具有广泛的药理活性。它是L. donovaniIB 拓扑异构酶的非竞争性抑制剂，可用于研究耐药利什曼病的治疗。

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

This study was designed to evaluate the anti-hepatitis B virus activity of Niranthin using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models. METHODS AND RESULTS:: Niranthin was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after Niranthin was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100 mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks. In the human HBV-transfected liver cell line HepG2.2.15, the secretion of HBsAg and HBeAg were significantly decreased after treatment with Niranthin for 144 h, with IC50 values for HBsAg of 15.6 μM, IC50 values for HBeAg of 25.1 μM. In DHBV-infected ducklings, Niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of Niranthin. CONCLUSIONS:The experimental data demonstrated that Niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo. values for HBsAg of 15.6 μM, IC50 values for HBeAg of 25.1 μM. In DHBV-infected ducklings, Niranthin significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. Furthermore, analysis of the liver pathological changes confirmed the hepatoprotective effect of Niranthin. CONCLUSION: The experimental data demonstrated that Niranthin exhibits anti-hepatitis B virus activity both in vitro and in vivo.

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C24H32O7

432.51

DMSO:65 mg/ml (150.29 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years