Humulon, a Bitter in the Hop, Inhibits Tumor Promotion by 12-O-Tetradecanoylphorbol-13-Acetate in Two-Stage Carcinogenesis in Mouse Skin

Yasukawa, Ken; Takeuchi, Mieko; Takido, Michio

doi:10.1159/000227448

Cited by 52 publications

(34 citation statements)

References 10 publications

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“…Hop extracts and/or compounds have been reported to be "active" or the equivalent by the authors of the given studies in the following assays: various antioxidant and/or chemoprevention (Gerhäuser et al, 2002;Gerhäuser et al, 2001;Liegeois et al, 2000;Masaki et al, 1995;Oyaizu et al, 1994;Stevens et al, 2002;Tagashira et al, 1995), antimicrobial, particularly against Gram positive bacteria (Grange and Davey, 1990;Langezaal et al, 1992;Matos et al, 2001;Ohsugi et al, 1997;Racz et al, 1980;Simpson and Smith, 1992;Tagashira et al, 1997), and cytotoxicity (Bae et al, 1996;Liu et al, 2001;Miranda et al, 1999;Shipp et al, 1994). Many constituents have been reported from hops (Farnsworth, 2003), among which in addition to the aforementioned estrogenic properties, many have been shown to possess other types of biological activity (Honma et al, 1998;Shipp et al, 1994;Tabata et al, 1998;Tobe et al, 1995;Tobe et al, 1997;Yasukawa et al, 1995) such as potential cancer chemopreventive activity (Gerhäuser et al, 2001a;Miranda et al, 2000a) and suppression of COX-2 gene transcription (Yamamoto et al, 2000). The major chalcone xanthohumol, as well as the flavanones isoxanthohumol, and 6PN and 8PN show various forms of antioxidant activity in vitro in the micromolar range, and are weakly cytotoxic to certain cancer cell lines (Gerhäuser et al, 2001a;Gerhäuser et al, 2001b;Milligan et al, 1999;Miranda et al, 2000a;Miranda et al, 2000b).…”

Section: Other Activitiesmentioning

confidence: 99%

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

2006

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SummaryAs the population ages, there is an ever-increasing need for therapeutic agents that can be used safely and efficaciously to manage symptoms related to postmenopausal estrogen deficiency. Endogenous estrogens, e.g., 17β-estradiol, of exogenous mammalian origin, e.g., horses, have long been used to manage such symptoms. There are more than twenty different classes of phytochemicals that have demonstrated affinity for human estrogen receptors in vitro. Some studies on exogenous estrogenic substances of botanical origin ("phytoestrogens"), such as standardized formulations of plant extracts with in vitro and in vivo estrogenic activity from soy (Glycine max Merill.) and red clover (Trifolium pratense L.), suggest clinical efficacy. Few clinical data for phytoestrogens other than isoflavonoids are available. In an exhaustive review of the literature through 2003, only two clinical trials were identified that were designed to evaluate the effect of hops (Humulus lupulus L.) on symptoms related to manopause. Folkloric, chemical, and biological literature relating primarily to the use of hops for their estrogenic activity, and two human clinical trials, are reviewed.

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Section: Other Activitiesmentioning

confidence: 99%

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

2006

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“…Hops, which have been used as an herbal medicine for many years, were shown to contain several compounds that have significant biological effects, such as 8-prenylnaringenin, which has estrogenic activity (37), and xanthohumol and hexahydro-colupulone, which were shown to inhibit the growth of cancers (38). Humulone was also shown to have anti-tumor effects (10,11,39). Isohumulones, which are isomerized humulones, are present in beer.…”

Section: Isohumulones Up-regulated the Expression Of Genes Involved Imentioning

confidence: 99%

Isohumulones, Bitter Acids Derived from Hops, Activate Both Peroxisome Proliferator-activated Receptor α and γ and Reduce Insulin Resistance

Yajima

Ikeshima

Shiraki

et al. 2004

Journal of Biological Chemistry

151

132

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The peroxisome proliferator-activated receptors (PPARs) are dietary lipid sensors that regulate fatty acid and carbohydrate metabolism. The hypolipidemic effects of fibrate drugs and the therapeutic benefits of the thiazolidinedione drugs are due to their activation of PPAR␣ and -␥, respectively. In this study, isohumulones, the bitter compounds derived from hops that are present in beer, were found to activate PPAR␣ and -␥ in transient co-transfection studies. Among the three major isohumulone homologs, isohumulone and isocohumulone were found to activate PPAR␣ and -␥. Diabetic KK-A y mice that were treated with isohumulones (isohumulone and isocohumulone) showed reduced plasma glucose, triglyceride, and free fatty acid levels (65.3, 62.6, and 73.1%, respectively, for isohumulone); similar reductions were found following treatment with the thiazolidinedione drug, pioglitazone. Isohumulone treatment did not result in significant body weight gain, although pioglitazone treatment did increase body weight (10.6% increase versus control group). C57BL/6N mice fed a high fat diet that were treated with isohumulones showed improved glucose tolerance and reduced insulin resistance. Furthermore, these animals showed increased liver fatty acid oxidation and a decrease in size and an increase in apoptosis of their hypertrophic adipocytes. A double-blind, placebo-controlled pilot study for studying the effect of isohumulones on diabetes suggested that isohumulones significantly decreased blood glucose and hemoglobin A1c levels after 8 weeks (by 10.1 and 6.4%, respectively, versus week 0). These results suggest that isohumulones can improve insulin sensitivity in high fat diet-fed mice with insulin resistance and in patients with type 2 diabetes.

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“…[8][9][10][11] Hops is widely available as an OTC drug having effects of depression of the central nervous system or activation of gastric function, or as a healthy food in Japan. However, there have been few reports about the effect of hops on gastric function and related mechanisms.…”

Section: Discussionmentioning

confidence: 99%

Effect of humulus lupulus on Gastric Secretion in a Rat Pylorus-Ligated Model

Kurasawa

Chikaraishi

Naito

et al. 2005

Biological & Pharmaceutical Bulletin

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In this study, we investigated the pharmacological effect of humulus lupulus (hops) on gastric juice volume and acidity using a rat pylorus-ligated model. In an intraorally administered experiment, hops clearly increased gastric juice volume without affecting acidity. On the other hand, hops had no influence on gastric juice volume when it was intragastrically administered. A cholinergic agonist, carbachol, increased gastric juice volume without affecting acidity, whereas histamine increased gastric juice volume and acidity. The increase of gastric juice volume induced by carbachol was completely inhibited by atropine. On the other hand, atropine did not inhibit the increase in gastric juice volume induced by histamine. The increase in gastric juice volume induced by hops was completely inhibited by atropine. These results suggested that the increase in gastric juice volume induced by intraorally administered hops could be mediated by the cholinergic nervous system.

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Humulon, a Bitter in the Hop, Inhibits Tumor Promotion by 12-O-Tetradecanoylphorbol-13-Acetate in Two-Stage Carcinogenesis in Mouse Skin

Cited by 52 publications

References 10 publications

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

The pharmacognosy of Humulus lupulus L. (hops) with an emphasis on estrogenic properties

Isohumulones, Bitter Acids Derived from Hops, Activate Both Peroxisome Proliferator-activated Receptor α and γ and Reduce Insulin Resistance

Effect of humulus lupulus on Gastric Secretion in a Rat Pylorus-Ligated Model

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