Inhibition of intestinal glucose uptake by aporphines and secoaporphines.

Abstract:

:The effects of aporphines and secoaporphines on glucose uptake by isolated intestinal brush-border membrane vesicles (BBMV) or basolateral membrane vesicles (BLMV) and glucose absorption during in situ intestinal perfusion were studied. Of the tested compounds, N-allylsecoboldine was the most potent glucose uptake inhibitor, with IC50 values of 159 microM and 121 microM, respectively, for uptake by BBMV and BLMV. While thaliporphine competitively inhibited glucose uptake by both membrane preparations, inhibition by N-allylsecoboldine was competitive using BBMV and noncompetitive using BLMV. In addition, N-allylsecoboldine significantly reduced both glucose absorption during in situ intestinal perfusion and blood glucose levels in the oral glucose tolerance test. The results demonstrate that levels of both aporphines and secoaporphines achievable by oral administration have an inhibitory effect on intestinal glucose uptake and suggest that the hypoglycemic effects of these compounds merit attention.

journal_name

Life Sci

journal_title

Life sciences

authors

Lin CJ,Chen CH,Liu FW,Kang JJ,Chen CK,Lee SL,Lee SS

doi

10.1016/j.lfs.2005.12.031

subject

Has Abstract

pub_date

2006-06-06 00:00:00

pages

144-53

issue

2

eissn

0024-3205

issn

1879-0631

pii

S0024-3205(05)01277-4

journal_volume

79

pub_type

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