Affordable Access

Publisher Website

The effect of an insulin releasing agent, BTS 67 582, on advanced glycation end product formationin vitro

Authors
Journal
Life Sciences
0024-3205
Publisher
Elsevier
Publication Date
Volume
64
Issue
16
Identifiers
DOI: 10.1016/s0024-3205(99)00076-4
Keywords
  • Bts 67 582
  • Advanced Glycation End Product
  • Amadori Products

Abstract

Abstract BTS 67 582 (1,1-dimethyl-2-(2-morpholinophenyl) guanidine fumarate) is an insulin-releasing agent currently in phase II clinical trials. Its effect on advanced glycation end product (AGE) formation was measured in the BSA/D-glucose and L-lysine/glucose-6-phosphate assay systems and Amadori product formation was measured in the BSA/D-glucose assay system, following a 3 week incubation period. In the BSA/D-glucose assay system, 200 mM BTS 67 582 caused an approximate 70 % inhibition in AGE formation (p < 0.001), whilst at 20 mM and 2 mM it caused a marginal inhibition (21 %, (p < 0.001) and 8 % respectively). 200 mM and 20 mM aminoguanidine-HCl inhibited AGE formation by 95 % and 69 % (p < 0.001), respectively, whereas 2 mM aminoguanidine-HCl had no significant effect. Tolbutamide (200 μM) and glibenclamide (100 μM) had significant, but only marginal, effects on AGE formation (16 % and 17 %, respectively, p < 0.01). In the BSA/D-glucose assay system 200 mM BTS 67 582 and 200 mM aminoguanidine-HCl retarded Amadori product formation by 88 % (p < 0.001) and 60 % (p < 0.01), respectively. BTS 67 582 at 20 mM and 2 mM was shown to inhibit Amadori product formation by 67 % and 57 %, respectively, (p < 0.01). In the lysine and glucose-6-phosphate assay system 200 mM BTS 67 582 and 200 mM aminoguanidine-HCl were shown to inhibit AGE formation by about 70% and 96% (p < 0.001), respectively. Tolbutamide (200 μM) and glibenclamide (100 μM) had no significant effect on AGE formation.

There are no comments yet on this publication. Be the first to share your thoughts.

Statistics

Seen <100 times
0 Comments

More articles like this

Biphasic insulin-releasing effect of BTS 67 582 in...

on The Journal of pharmacy and ph... December 1998

Insulin-releasing action of the novel antidiabetic...

on British Journal of Pharmacolog... February 1998

Glucose-lowering effect of BTS 67 582.

on British Journal of Pharmacolog... December 1997
More articles like this..