Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

APE1:10 nM(Kd)

Hycanthone at 20 mg/mL or more is progressively more detrimental to cell viability. Compared to that of controls, results show that increased concentrations of Hycanthone, ranging from 0.1 to 10 μg/mL, progressively decreases viral interferon yields as much as 73% [2].

Male worms treated with Hycanthone display signs of possible partial recovery from the initial low levels of incorporation. After treatment with Hycanthone, the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease. Immature worms are totally unaffected by Hycanthone at all times tested. In the first four days after treatment, incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50%. 7 days after Hycanthone treatment, both ribosomal RNA species are reduced by at least 80% with respect to untreated worms, with some indication of a possible accumulation of heavier precursor molecules [1].

H2O: < 0.1 mg/mL (insoluble)

DMSO: 18 mg/mL (50.49 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.81 mM), Sonication is recommended.