| Description: |
Xanthohumol has anti-hepatitis C virus, anti-carcinogenic, free radical-scavenging, and anti-inflammatory activities, it can inhibit HIV-1 induced cytopathic effects, the production of viral p24 antigen and reverse transcriptase in C8166 lymphocytes at non-cytotoxic concentration. Xanthohumol may play a role in improving cognitive flexability in young animals. Xanthohumol has beneficial effects on markers of metabolic syndrome, it lowers body weight and fasting plasma glucose in obese male Zucker fa/fa rats.
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| Targets: |
NMDAR | Caspase | PARP | p53 | Bcl-2/Bax | HCV | HIV | XIAP | AIF |
| In vitro: |
| Antiviral Res. 2004 Dec;64(3):189-94. | | Xanthohumol, a novel anti-HIV-1 agent purified from Hops Humulus lupulus.[Pubmed: 15550272 ] | Xanthohumol, prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus. Its anti-HIV-1 activity was tested in the present study.
METHODS AND RESULTS:
Results showed that xanthohumol inhibited HIV-1 induced cytopathic effects, the production of viral p24 antigen and reverse transcriptase in C8166 lymphocytes at non-cytotoxic concentration. The EC50 values were 0.82, 1.28 and 0.50 microg/ml, respectively. The therapeutic index (TI) was about 10.8. Xanthohumol also inhibited HIV-1 replication in PBMC with EC50 value of 20.74 microg/ml. The activity of recombinant HIV-1 reverse transcriptase and the HIV-1 entry were not inhibited by xanthohumol.
CONCLUSIONS:
The results from this study suggested that xanthohumol is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection. However, the mechanism of its anti-HIV-1 effect needs to be further clarified. |
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| In vivo: |
| Behav Brain Res. 2014 Dec 15;275:1-10. | | Xanthohumol improved cognitive flexibility in young mice.[Pubmed: 25192637] | The protein palmitoylation cycle has been shown to be important for protein signaling and synaptic plasticity. Data from our lab showed a change in the palmitoylation status of certain proteins with age. A greater percentage of the NMDA receptor subunits GluN2A and GluN2B, along with Fyn and PSD95 proteins, were palmitoylated in the old mice. The higher level of protein palmitoylation was also associated with poorer learning scores. Xanthohumol is a prenylated flavonoid that has been shown to increase beta-oxidation in the livers of rodents, decreasing circulating free fatty acids in the serum. What is not known is whether the application of xanthohumol could influence the palmitoylation status of proteins.
METHODS AND RESULTS:
In this study, young and old mice were fed a diet supplemented with xanthohumol for 8 weeks. Spatial memory was assessed with the Morris water maze and protein palmitoylation quantified. The young xanthohumol-treated mice showed a significant improvement in cognitive flexibility. However, this appeared to be associated with the young control mice, on a defined, phytoestrogen-deficient diet, performing as poorly as the old mice and xanthohumol reversing this effect. The old mice receiving xanthohumol did not significantly improve their learning scores. Xanthohumol treatment was unable to affect the palmitoylation of NMDA receptor subunits and associated proteins assessed in this study.
CONCLUSIONS:
This evidence suggests that xanthohumol may play a role in improving cognitive flexability in young animals, but it appears to be ineffective in adjusting the palmitoylation status of neuronal proteins in aged individuals. | | J Oleo Sci. 2014;63(2):159-68. | | Effects of xanthohumol-rich extract from the hop on fatty acid metabolism in rats fed a high-fat diet.[Pubmed: 24420065 ] | Xanthohumol is the major prenylated flavonoid of female inflorescences of the hop plant (Humulus lupulus L.) and is a hydrophobic flavonoid. We examined the effects of dietary xanthohumol-rich hop extract in obese rats that was induced by feeding a high-fat diet.
METHODS AND RESULTS:
Dietary xanthohumol-rich hop extract significantly lowered the body weight gain of these rats compared to rats fed a high-fat diet without the extract. The increase of body weight, liver weight, and triacylglycerol levels in the plasma and liver of the rats fed a high-fat diet was ameliorated by dietary xanthohumol-rich hop extract. Dietary xanthohumol-rich hop extract tended to reduce hepatic fatty acid synthesis through the reduction of hepatic SREBP1c mRNA expression in the rats fed a high-fat diet. The excreted of triacylglycerol into feces also was promoted by dietary xanthohumol-rich hop extract. Plasma adiponectin levels in the rats fed a high-fat diet also tended to be elevated by dietary xanthohumol-rich hop extract. Thus, xanthohumol-rich hop extract may inhibit the increase of body weight, liver weight, and triacylglycerol in the plasma and liver induced by feeding high-fat diet through the regulation of hepatic fatty acid metabolism and inhibition of intestinal fat absorption.
CONCLUSIONS:
Therefore, xanthohumol-rich hop extract may exert preventive function on the increase of body weight and tissue triacylglycerol levels by overnutrition. |
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