Acarviosine-simmondsin, a novel compound obtained from acarviosine-glucose and simmondsin by Thermus maltogenic amylase and its in vivo effect on food intake and hyperglycemia.
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| Abstract |
Simmondsin was modified with acarviosine-glucose using the transglycosylation activity of Thermus maltogenic amylase to synthesize a novel compound with both antiobesity and hypoglycemic activity. The LC/MS and 13C NMR analyses confirmed that the structure of the major transglycosylation product was acarviosine-simmondsin (Acv-simmondsin), in which acarviosine was attached to the glucose moiety of simmondsin by an alpha-(1,6)-glycosidic linkage. It was found that Acv-simmondsin was a potent competitive inhibitor of alpha-glucosidase with the Ki value of 0.69 microM and a mixed type inhibitor of alpha-amylase with the Ki and KI of 20.78 microM and 26.31 microM, respectively. The administration of Acv-simmondsin (0.1 g/100 g diet/day) to mice for 5 days significantly reduced food intake by 35%, compared to 25% with simmondsin in control obese mice. Acv-simmondsin (50 mg/kg BW) suppressed the postprandial blood glucose response to sucrose (1 g/kg BW) by 74%, compared to 71% with acarbose, in normal rats.
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| Authors | Jin-Sook Baek, Hye-Young Kim, Thomas P Abbott, Tae-Wha Moon, Soo-Bok Lee, Cheon-Seok Park, Kwan-Hwa Park |
| Journal | Bioscience, biotechnology, and biochemistry (Biosci Biotechnol Biochem) Vol. 67 Issue 3 Pg. 532-9 (Mar 2003) ISSN: 0916-8451 [Print] England |
| PMID | 12723600 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't) |
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