Diacylglycerol acyltransferase-inhibitory compounds from Erythrina senegalensis
Inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT) is proposed to be a drug target for the treatment of obesity and type 2 diabetes. Bioassay-guided fractionation of the CH 2 Cl 2 -soluble extract of the stem bark of Erythrina senegalensis , using an in vitro DGAT enzyme assay, resulted in...
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| Veröffentlicht in: | Archives of pharmacal research 2009, 32(1), , pp.43-47 |
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| Hauptverfasser: | , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
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| Zusammenfassung: | Inhibition of acyl CoA:diacylglycerol acyltransferase (DGAT) is proposed to be a drug target for the treatment of obesity and type 2 diabetes. Bioassay-guided fractionation of the CH
2
Cl
2
-soluble extract of the stem bark of
Erythrina senegalensis
, using an
in vitro
DGAT enzyme assay, resulted in the isolation of eight known prenylflavonoids, 8-prenylleutone (
1
), auriculatin (
2
), erysenegalensein O (
3
), erysenegalensein D (
4
), erysenegalensein N (
5
), derrone (
6
), alpinumisoflavone (
7
), and 6,8-diprenylgenistein (
8
). Compounds
1
,
2–4
,
6
, and
8
inhibited DGAT activity, with IC
50
values ranging from 1.1 ± 0.3 to 15.1 ± 1.1 μg/mL. On the basis of the data obtained, we propose isoflavonoids with isoprenyl groups as a novel class of DGAT inhibitors. |
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| ISSN: | 0253-6269 1976-3786 |
| DOI: | 10.1007/s12272-009-1116-2 |