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Abstract
Xanthohumol (XN), a prenylated chalcone unique to hops (Humulus lupulus) and two derived prenylflavanones, isoxanthohumol (IX) and 8-prenylnaringenin (8-PN) gained increasing attention as potential anti-diabetic and cancer preventive compounds. Two enzymes of the aldo-keto reductase (AKR) superfamily are notable pharmacological targets in cancer therapy (AKR1B10) and in the treatment of diabetic complications (AKR1B1). Our results show that XN, IX and 8-PN are potent uncompetitive, tight-binding inhibitors of human aldose reductase AKR1B1 (Ki = 15.08 μM, 0.34 μM, 0.71 μM) and of human AKR1B10 (Ki = 20.11 μM, 2.25 μM, 1.95 μM). The activity of the related enzyme AKR1A1 was left unaffected by all three compounds. This is the first time these three substances have been tested on AKRs. The results of this study may provide a basis for further quantitative structure–activity relationship models and promising scaffolds for future anti-diabetic or carcinopreventive drugs.
Highlights
The female inflorescences of hops (Humulus lupulus) have long been used in traditional Chinese and Ayurvedic medicine mainly to treat sleep disturbances[1] and are known for their antibiotic properties[2]
We investigated the inhibitory potential of three hopderived substances on three members of the aldo-keto reductase (AKR) superfamily
The activity of AKR1A1 was unaffected by all three substances (IC50 > 50 mM)
Summary
The female inflorescences of hops (Humulus lupulus) have long been used in traditional Chinese and Ayurvedic medicine mainly to treat sleep disturbances[1] and are known for their antibiotic properties[2]. Among the secondary plant compounds that occur in the resinous inflorescences of H. lupulus are prenylated chalcones and other flavonoids[3]. These compounds are well known for their bittering and preserving qualities in the brewing process of beer[3,4], as well as for their bioactivity (antibiotic, anti-viral and antioxidant properties)[5–7]. Since XN is a unique prenylflavonoid occurring in hops, beer is the only noteworthy dietary source for XN in central Europe. In addition to XN, hops inflorescences contain flavanones like isoxanthohumol (IX) and 8-prenylnaringenin (8-PN)[9]
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