Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis

Department of Animal and Dairy Science, 444 Edgar L. Rhodes Center for Animal and Dairy Science, University of Georgia, Athens, GA 30602-2771, USA.
APOPTOSIS (Impact Factor: 3.61). 12/2007; 12(11):1953-63. DOI: 10.1007/s10495-007-0130-4
Source: PubMed

ABSTRACT Xanthohumol (XN), the chalcone from beer hops has several biological activities. XN has been shown to induce apoptosis in cancer cells and also has been reported to be involved in lipid metabolism. Based on these studies and our previous work with natural compounds, we hypothesized that XN and its isomeric flavanone, isoxanthohumol (IXN), would induce apoptosis in adipocytes through the mitochondrial pathway and would inhibit maturation of preadipocytes. Adipocytes were treated with various concentrations of XN or IXN. In mature adipocytes both XN and IXN decreased viability, increased apoptosis and increased ROS production, XN being more effective. Furthermore, the antioxidants ascorbic acid and 2-mercaptoethanol prevented XN and IXN-induced ROS generation and apoptosis. Immunoblotting analysis showed an increase in the levels of cytoplasmic cytochrome c and cleaved poly (ADP-ribose) polymerase (PARP) by XN and IXN. Concomitantly, we observed activation of the effectors caspase-3/7. In maturing preadipocytes both XN and IXN were effective in reducing lipid content, XN being more potent. Moreover, the major adipocyte marker proteins such as PPARgamma, C/EBPalpha, and aP2 decreased after treatment with XN during the maturation period and that of DGAT1 decreased after treatment with XN and IXN. Taken together, our data indicate that both XN and IXN inhibit differentiation of preadipocytes, and induce apoptosis in mature adipocytes, but XN is more potent.

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    ABSTRACT: The female inflorescences of hops (Humulus lupulus L.), a well-known bittering agent used in the brewing industry, have long been used in traditional medicines. Xanthohumol (XN) is one of the bioactive substances contributing to its medical applications. Among foodstuffs XN is found primarily in beer and its natural occurrence is surveyed. In recent years, XN has received much attention for its biological effects. The present review describes the pharmacological aspects of XN and summarizes the most interesting findings obtained in the preclinical research related to this compound, including the pharmacological activity, the pharmacokinetics, and the safety of XN. Furthermore, the potential use of XN as a food additive considering its many positive biological effects is discussed.
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    ABSTRACT: In recent years, interest in hop-derived constituents, esp. for prenylflavonoids has grown, as they have a wide range of biol. properties including antioxidant, anticarcinogenic and antimicrobial activities. Two main hop prenylflavonoids, xanthohumol and isoxanthohumol, and hop ext. enriched in prenylflavonoids, were tested for their antiproliferative activities on colon cancer cell lines, HT-29 and SW620, and a noncancerous cell line, IEC-6. It was confirmed that both xanthohumol and isoxanthohumol inhibited cell proliferation, even at micromolar concns. For cell line HT-29, the IC50 was 1.2 ± 0.9 and 16.9 ± 0.9 μmol dm-3 for xanthohumol and isoxanthohumol, resp. Similar values were obtained for SW620 cells (2.5 ± 0.2 and 37.3 ± 3.2 μmol dm-3). None of the pure prenylflavonoids that were tested affected the proliferation of the noncancerous cell line, IEC-6. The effect of the hop ext. contg. xanthohumol was also tested for antiproliferative activities on the cancer cell lines, HT-29 (IC50
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