Abstract:
:We have analyzed the effect of quinolizidine alkaloids from Lupinus species upon insulin secretion. Isolated normal rat islets were incubated with 3.3, 8.3, and 16.7 mM glucose, in the presence or absence of different concentrations of lupanine (0.05, 0.5, and 1.0 mM), 13-alpha-OH lupanine, 17-oxo-lupanine, and 2-thionosparteine. Insulin release was measured by radioimmunoassay. While 2-thionosparteine enhanced insulin secretion at all glucose concentrations, lupanine did at 8.3 and 16.7 mM, and 13-alpha-OH lupanine or 17-oxo-lupanine only at 16.7 mM glucose. Diazoxide (0.1 mM) decreased the effect of all alkaloids, without suppressing it completely. Consequently, blockage of beta-cell K(ATP)-sensitive channels is at least one of the mechanisms involved in the enhancing secretagogue effects of quinolizidine alkaloids. The fact that 13-alpha-OH lupanine and 17-oxo-lupanine only exert their secretagogue effect at high glucose concentrations could be of additional value when considering their potential use in the treatment of type 2 diabetes.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
García López PM,de la Mora PG,Wysocka W,Maiztegui B,Alzugaray ME,Del Zotto H,Borelli MIdoi
10.1016/j.ejphar.2004.09.008keywords:
subject
Has Abstractpub_date
2004-11-03 00:00:00pages
139-42issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(04)01014-3journal_volume
504pub_type
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