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首页> 外文期刊>Journal of Clinical Medicine >Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents
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Novel Pharmacological Activity of Artesunate and Artemisinin: Their Potential as Anti-Tubercular Agents

机译：青蒿琥酯和青蒿素的新型药理活性：作为抗结核剂的潜力。

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Tuberculosis is a major infectious disease that globally causes the highest human mortality. From this aspect, this study was carried out to evaluate novel pharmacological activities/effects of artesunate and artemisinin causing anti-tubercular activity/effects against Mycobacterium tuberculosis (Mtb). The anti-Mtb activities/effects of artesunate and artemisinin were evaluated using different anti-Mtb indicator assays, such as the resazurin microtiter assay, the Mycobacteria Growth Indicator Tube (MGIT) 960 system assay, and the Ogawa slant medium assay, as well as in vivo tests. Artesunate showed selective anti-Mtb effects by strongly inhibiting the growth of Mtb compared to artemisinin, and consistently induced anti-Mtb activity/effects by effectively inhibiting Mtb in the MGIT 960 system and in Ogawa slant medium for 21 days with a single dose; its minimum inhibitory concentration was 300 μg/mL in in vitro testing. Furthermore, artesunate demonstrated an anti-tubercular effect/action with a daily dose of 3.5 mg/kg in an in vivo test for four weeks, which did not indicate or induce toxicity and side effects. These results demonstrate that artesunate effectively inhibits the growth and/or proliferation of Mtb through novel pharmacological activities/actions, as well as induces anti-Mtb activity. This study shows its potential as a potent candidate agent for developing new anti-tuberculosis drugs of an effective/safe next generation, and suggests novel insights into its effective use by repurposing existing drugs through new pharmacological activity/effects as one of the substantive alternatives for inhibiting tuberculosis.
机译：结核病是一种主要的传染病，在全球范围内导致人类最高的死亡率。从这个方面出发，进行了这项研究以评估青蒿琥酯和青蒿素的新药理活性/效应，从而引起针对结核分枝杆菌（Mtb）的抗结核活性/效应。青蒿琥酯和青蒿素的抗Mtb活性/效果使用不同的抗Mtb指标测定方法进行了评估，例如刃天青微量滴定法，分枝杆菌生长指示剂管（MGIT）960系统测定法和小川倾斜培养基测定法以及体内测试。青蒿琥酯与青蒿素相比，通过强烈抑制Mtb的生长而表现出选择性的抗Mtb效应，并且通过有效抑制MGIT 960系统和Ogawa倾斜培养基中的Mtb持续21天，从而持续诱导抗Mtb活性/效应。在体外测试中，其最小抑菌浓度为300μg/ mL。此外，青蒿琥酯在体内试验中连续四周每日剂量为3.5 mg / kg表现出抗结核作用/作用，但未表明或诱发毒性和副作用。这些结果表明青蒿琥酯通过新颖的药理活性/作用有效抑制了Mtb的生长和/或增殖，并诱导了抗Mtb的活性。这项研究显示了其作为开发有效/安全的下一代抗结核药物的有效候选药物的潜力，并通过新的药理活性/作用重新利用现有药物作为该药物的实质性替代品之一，从而对其有效使用提出了新的见解。抑制结核病。

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