Affiliation:
1. Institute of Chemistry, College of Science, University of the Philippines, Diliman 1101, Quezon City, Philippines
2. Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Stadium Road, Karachi-74800, Pakistan
3. International Center for the Chemical Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi-75270, Pakistan
Abstract
The hexane extract of Syzygium samarangense (Ss.Hex) dose-dependently (10D1000 μg/ ml) relaxed the spontaneously contracting isolated rabbit jejunum. Four rare C-methylated flavonoids with a chalcone and a flavanone skeleton were isolated from Ss.Hex and were subsequently tested for spasmolytic activity. All flavonoids, identified as 2′-hydroxy-4′,6′- dimethoxy-3′-methylchalcone (1), 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (2), 2′,4′-dihydroxy-6′-methoxy-3′-methylchalcone (3), and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (4), showed dose-dependent spasmolytic activity in the rabbit jejunum with IC50 values of 148.3 ± 69.4, 77.2 ± 43.5, 142.4 ± 58.6 and 178.5 ± 37.5 μg/ml (mean ± SEM), respectively. The dihydrochalcone derivative of compound 1, 2′-hydroxy-4′,6′-dimethoxy-3′- methyldihydrochalcone (5), when tested for spasmolytic activity, did not significantly relax the smooth muscle relative to the other compounds. Verapamil, a standard spasmolytic, has an IC50 value of 0.16 ± 0.04 μg/ml. This is the first report of the relaxant activity of chalcones, specifically of compounds 1-3.
Subject
General Biochemistry, Genetics and Molecular Biology
Cited by
21 articles.
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