Influence of chalcone analogues on serum glucose levels in hyperglycemic rats

被引：38

作者：

Alberton, Elga Heloisa ^{[1
]}

Damazio, Rosangela Guollo ^{[1
]}

Cazarolli, Luisa Helena ^{[1
]}

Chiaradia, Louise Domeneghini ^{[2
]}

Leal, Paulo Cesar ^{[2
]}

Nunes, Ricardo Jose ^{[2
]}

Yunes, Rosendo Augusto ^{[2
]}

Mena Barreto Silva, Fatima Regina ^{[1
]}

机构：

[1] Univ Fed Santa Catarina, Dept Bioquim, Ctr Ciencias Biol, Campus Univ,Cx Postal 5069, BR-88040970 Florianopolis, SC, Brazil

[2] Univ Fed Santa Catarina, Dept Quim, Ctr Ciencias Fis & Matemat, BR-88040900 Florianopolis, SC, Brazil

来源：

CHEMICO-BIOLOGICAL INTERACTIONS | 2008年 / 171卷 / 03期

关键词：

chalcone; hyperglycemia; analogues; insulin; tolbutamide;

D O I：

10.1016/j.cbi.2007.11.001

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A series of chalcone derivatives from 3,4-methylenedioxybenzaldehyde and substituted acetophenones have been synthesized and investigated as antihyperglycemic agents in a glucose loaded animal model. Chalcones with biological activity were compared with lispro, regular insulin and tolbutamide effects on serum glucose levels. Compound 01, without substituent in the A-ring was not able to change glycemic levels. On the other hand, compounds 03, 04, 05, 09 and 10 with substitutions at position 3' and/or 4' in the A-ring caused significant reduction in serum glucose levels. Concerning the antihyperglycemic effect, compounds 03 and 05 (methoxy substituent) inhibited the hyperglycemia induced by glucose around 96% similar to that demonstrated for lispro insulin and tolbutamide at 60 min. A rapid and lasting antihyperglycemic effect was found with compound 09 and 10 (nitro substituent). In conclusion, besides the nature of the functional groups electron-donor substituent, as methoxy and hydroxyl or electron-acceptor, as nitro groups, the position of the group may be mandatory for biological activity. (c) 2007 Elsevier Ireland Ltd. All rights reserved.

引用

页码：355 / 362

页数：8

共 34 条

[1]

Cardamonin, inhibits pro-inflammatory mediators in activated RAW 264.7 cells and whole blood [J].