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《美国科学院院刊(PNAS)》新闻发布原文和译文

时间: 2006-11-21 15:04 字号:|| 点击:

Small molecule diabetes therapy

An orally available “small molecule” may represent a new class of therapies for diabetes and other metabolic disorders, researchers report. The recently approved diabetes drug, exenatide belongs to a class of “incretin mimetics”, agents that mimic one of the body’s own glucose-regulating peptide hormones, called glucagon-like peptide-1 (GLP-1). While effective in treating type II (adult onset) diabetes, peptide-based incretin mimetics must be injected, limiting their usefulness. Efforts to develop orally-available small molecules with GLP1-like activity have failed, leading researchers to search for alternatives. Ming-Wei Wang and colleagues screened more than 48,000 compounds and identified two promising candidates with the ability to mimic the actions of GLP-1 in cultured cells and in live animals. The researchers found that one compound, called Boc5, decreased food intake when administered to mice by injection and orally. Daily injections of Boc5 also prevented weight gain and reduced levels of HbA1c, a marker of long-term glucose control, in a mouse model of type II diabetes. The results suggest that Boc5 may represent a new class of small molecules with potential for treating diabetes, obesity, and related metabolic disorders without the need for injection.


小分子糖尿病疗法

研究人员报道,一类口服有效的“小分子”可能成为糖尿病和其他代谢性疾病的一种新型疗法。最近获准上市的糖尿病治疗药物Exenatide为“肠降糖素类似物”,可以模拟体内的肽类激素 — 胰高血糖素样肽-1(GLP-1)而发挥血糖调节作用。肠降糖素的多肽类似物治疗成人2型糖尿病有效,但由于必须采用注射给药方式,使其应用受到限制。以往试图开发口服有效、具有胰高血糖素样肽-1活性的小分子之努力均未成功,促使科研人员寻找其他途径。王明伟和同事们通过对48,000多个化合物进行筛选,发现了两个颇有希望的候选结构。它们能在细胞培养和活体动物模型上模拟胰高血糖素样肽-1的活性。研究人员证实,其中一个代号为Boc5的化合物在注射或口服给药后降低了小鼠的摄食量。在2型糖尿病小鼠模型中,每日注射Boc5可以防止体重增长,降低糖化血红蛋白(血糖长期控制指标)。研究结果提示,Boc5可能代表一类全新、无需注射的小分子用于治疗糖尿病、肥胖症及相关代谢性疾病。
 

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