海恩酮性质、用途与生产工艺
Hycanthone 是噻吨酮类的 DNA 嵌入剂 (DNA intercalator)，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。Hycanthone 通过直接蛋白质结合来抑制核酸生物合成并抑制嘌呤内切核酸酶1 (APE1)，KD 为 10 nM。Hycanthone 是 Lucanthone (HY-B2098) 的生物活性代谢产物，具有抗血吸虫病药物。
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Topoisomerase I
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Topoisomerase II
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Hycanthone has an IC
50
of 80 nM for inhibition of APE1 incision of depurinated plasmid DNA.
Hycanthone (0.05-100 µM; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO.
Hycanthone at 20 mg/mL or more is progressively more detrimental to cell viability. Results reveal that increased concentrations of Hycanthone, ranging from 0.1 to 10 μg/mL, progressively reduces viral interferon yields as much as 73% compare to that of controls.
Results show that the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease after treatment with Hycanthone. Immature worms are totally unaffected by Hycanthone at all times tested. Male worms treated with Hycanthone show signs of a possible partial recovery from the initial low levels of incorporation. The incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50% in the first four days after treatment. Results show that, 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.
化学性质
淡黄色至黄橙色结晶粉末。
用途
海恩酮（Hycanthone）是一种具有抗血吸虫活性和潜在抗肿瘤活性的Lucanthorne的硫杂吨衍生物。海恩酮干扰寄生虫的神经功能，导致寄生虫瘫痪和死亡。它也能插入DNA并在体外抑制RNA的合成。
参考资料
[1] 陈建新, 刘泽鑫, 曾振灵, et al. 海恩酮在制备防治非洲猪瘟药物中的用途.
[2] 张继瑜, 邱燕华, 翟斌涛, et al. 海恩酮在制备治疗弓形虫感染疾病药物中的应用.
[3] D. CLIVE M. R M W G Flamm. Mutagenicity of hycanthone in mammalian cells[J]. Mutation Research-Fundamental and Molecular Mechanisms of Mutagenesis, 1972, 14 2: Pages 262-264. DOI:
10.1016/0027-5107(72)90055-3.
[4] PHILIP E. HARTMAN. Hycanthone: A Frameshift Mutagen[J]. Science, 1971, 172 3987. DOI:
10.1126/science.172.3987.1058.
海恩酮
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