首页> 外文期刊>Chemical biology and drug design >Chemotherapeutic potentials of β‐ionone against Trypanosoma congolense infection: Inhibition of parasite proliferation, anemia development, trans‐sialidase (TconTS3 and TconTS4) gene expressions, and phospholipase A2
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Chemotherapeutic potentials of β‐ionone against Trypanosoma congolense infection: Inhibition of parasite proliferation, anemia development, trans‐sialidase (TconTS3 and TconTS4) gene expressions, and phospholipase A2

机译:β-紫罗兰酮对刚果锥虫感染的化疗潜力:抑制寄生虫增殖、贫血发展、反式唾液酸酶(TconTS3 和 TconTS4)基因表达和磷脂酶 A2

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摘要

Abstract Trypanosoma congolense is a pathogenic African animal trypanosome species causing devastating conditions leading to death of an infected host. The drawbacks of the existing trypanocidal drugs have led to the search for new drug candidates. In this study, β‐ionone at 15 and 30 mg/kg body weight (BW) was orally administered to T. congolense infected rats for 14 days followed by an assessment of anemia, organ damages, and the expression of T. congolense trans‐sialidase gene variants. A significant decrease in parasitemia (p  .05) between FSA with the TconTS gene expressions. In addition, the compound inhibited partially purified T. congolense sialidase and phospholipase A2 via mixed inhibition pattern with inhibition binding constants of 25.325 and 4.550 µM, respectively, while molecular docking predicted binding energies of −5.6 kcal/mol for both enzymes. In conclusion, treatment with β‐ionone suppressed T. congolense proliferation and protected the animals against some of the parasite‐induced pathologies whilst the effect on anemia development might be due to inhibition of sialidase and PLA2 activities as well as the expression levels of TconTS3 and TconTS4.
机译:摘要 刚果锥虫是一种致病性非洲动物锥虫,可引起毁灭性的疾病,导致受感染宿主死亡。现有锥虫杀虫药物的缺点导致了寻找新的候选药物。在这项研究中,将 15 和 30 mg/kg 体重 (BW) 的 β-紫罗兰酮口服给受 T. congolense 感染的大鼠 14 天,然后评估贫血、器官损伤和 T. congolense 反唾液酸酶基因变异的表达。在用15mg / kg BW β-紫罗兰酮治疗的动物中观察到寄生虫血症显着降低(p .05)基因表达。此外,该化合物通过混合抑制模式抑制部分纯化的刚果锥虫唾液酸酶和磷脂酶 A2,抑制结合常数分别为 25.325 和 4.550 μM,而分子对接预测两种酶的结合能为 -5.6 kcal/mol。总之,β-紫罗兰酮治疗抑制了T。刚果增殖并保护动物免受一些寄生虫诱导的病理,而对贫血发展的影响可能是由于抑制唾液酸酶和PLA2活性以及TconTS3和TconTS4的表达水平。

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