PNAS：中国科学家发现小分子Boc5有助于控制2型糖尿病
生物谷报道：上海科学家最近发现一种关键化合物，该化合物可能能够用于合成II型糖尿病患者和减肥人群的口服药物。该研究中的发现（一种名为Boc5的化合物，它在自然界中并不存在）---发表于《美国国家科学院院报》本周的在线版本上。
受到当地及中央政府和其它来源的资金支持，上海药物研究所的研究人员开发了一种化合物被证明具有抗糖尿病特性。给予Boc5的正常老鼠食物摄取明显减少。该化合物同样可以预防体重增加，并使糖尿病动物的血糖水平正常化。该研究表明，Boc5可能代表一类无需通过注射即可治疗糖尿病、肥胖和相关代谢紊乱的新小分子家族。Boc5化合物口服有效，因为长期口服该药物后不会使糖尿病老鼠产生明显的副作用。
II型糖尿病是一类非胰岛素依赖性疾病。 根据该研究发现，研究人员将更进一步致力于研发含有该化合物的新型药物用于治疗糖尿病。
Fig. 3. The acute effect of Boc5 on food intake in female C57BL/6 mice.
(a) Cumulative food intake up to 12 h after various i.p. doses of Boc5. Exenatide (1 µg) was used as control. (b) Dose–response characteristics. ED50 was estimated based on 9–10 measurements per group as a shared parameter for all time points. Hill slope was also shared. (c) Blockade of the 30-min anorectic effect of i.p. Boc5 at 1 mg by prior i.p. injection of exendin(9–39) at 10 µg. (d and e) Time course (d) and dose–response (e) of gavaged Boc5 on cumulative food intake. (f) Blockade of the 90-min anorectic effect of gavaged Boc5 (10 mg) by prior i.p. injection of exendin(9–39) at 15 µg. Symbols are means ± SEM, and asterisks indicate P <
原文出处：
MEDICAL SCIENCES:
Desu Chen, Jiayu Liao, Na Li, Caihong Zhou, Qing Liu, Guangxing Wang, Rui Zhang, Song Zhang, Lilin Lin, Kaixian Chen, Xin Xie, Fajun Nan, Andrew A. Young, and Ming-Wei Wang
From the Cover: A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice
PNAS 2007 104: 943-948; published online before print as 10.1073/pnas.0610173104
Abstract Full Text PDF Supporting Information
COMMENTARIES:
K. G. Murphy and S. R. Bloom
Nonpeptidic glucagon-like peptide 1 receptor agonists: A magic bullet for diabetes?
PNAS 2007 104: 689-690; published online before print as 10.1073/pnas.0610679104
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