疟疾:仅需一剂药物就可治愈受感染的小鼠 |
| http://www.maydeal.com 【 2007-7-11发布 】 |
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研究者使用一种长效的合成药物已经治愈了疟疾感染的小鼠,这种药物是在一种古老的中国民间草药的基础上加工完成的。 这种古老的过氧化物抗疟药疗效很快。这种药物的主要成分是青缟素。几千年来,一直用于治疗疟疾和多种发热疾病。 第一代药物有很多缺点,包括半衰期短于一小时。Posner和其团队会逐渐改善这些缺点。“我们这种半-合成的药物已经克服了第一代药物的很多缺点。” Posner教授说,“最重要的是这些成分疗效所持续的时间,但根据我们的设计,这些药物在体内具有更长的半衰期。我们在设计时使这些药物变得更具亲脂性,这意味着药物在脂肪中的溶解能力更强并且能迅速到达疟原虫感染的血红细胞。” 除外,新的药物通过代谢不会降解为毒性物质,与传统的配方相比更加具有安全性。 Malaria: Infected Mice Cured By One Dose of New Drug Researchers have cured malaria-infected mice with single shots of a new series of potent, long lasting synthetic drugs modelled on an ancient Chinese herbal folk remedy.01/06/2007The team also has developed several other compounds which defeated the febrile disease in rodents after three oral doses. These peroxide compounds, containing a crucial oxygen-oxygen unit, promise not only to be more effective than today’s best malaria remedies, but also potentially safer and more efficient, said research team leader Gary Posner, Scowe Professor of Chemistry in the Krieger School of Arts and Sciences at Johns Hopkins. The oxygen-oxygen unit in the peroxides causes malaria parasites essentially to self-destruct. The parasites digest hemoglobin, the oxygen-carrying pigment of red blood cells, and, in the process, release a substance called heme, a deep-red iron-containing blood pigment. When the heme encounters peroxides, a powerful chemical reaction occurs, releasing carbon-free radicals and oxidizing agents that eventually kill the parasites. The first generation of trioxane drugs had a number of shortcomings, including a half-life of less than one hour. Posner and team believe that their new compounds address those disadvantages. "Our semi-synthetic artemisinin-derived compounds successfully overcome the disadvantages of their first-generation predecessors," he said. "Most important is their curative activity after a single, low dose, which is distinctly unusual. But based on our intentional design, they may also have a longer half-life in animals. We also designed them to be more lipophilic, meaning they have an enhanced ability to dissolve in fats and thus to arrive inside malaria-infected red blood cells." In addition, the new compounds are far less likely to break down into toxic substances when they are metabolized in the test animals’ bodies, making them potentially safer than their predecessors. ---本文由美迪医疗网乔永霞编译 |
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