Rice Protein Matrix Enhances Circulating Levels of Xanthohumol Following Acute Oral Intake of Spent Hops in Humans

O’Connor, Annalouise; Konda, Veera Reddy; Reed, Ralph L.; Christensen, J. Mark; Stevens, Jan F.; Contractor, Nikhat

doi:10.1002/mnfr.201700692

Cited by 6 publications

(10 citation statements)

References 28 publications

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“…Of note, XN was combined with rice protein because rice protein has been shown to significantly increase the bioavailability of XN and its metabolites in humans. [ 15 ] To maintain blinding, the study material was encapsulated in orange‐colored gelatin capsules. The 99+% pure xanthohumol was provided by Hopsteiner (New York, NY, USA).…”

Section: Methodsmentioning

confidence: 99%

Xanthohumol Microbiome and Signature in Healthy Adults (the XMaS Trial): Safety and Tolerability Results of a Phase I Triple‐Masked, Placebo‐Controlled Clinical Trial

Langley

Ryan

Hanes

et al. 2021

Molecular Nutrition Food Res

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Scope: Xanthohumol, a prenylflavonoid from hops, has been extensively studied preclinically but has undergone limited research in human subjects. A triple-masked, placebo-controlled phase I clinical trial was conducted to examine the safety and tolerability of xanthohumol. Methods and Results: Thirty healthy volunteers were randomized to 24 mg day −1 xanthohumol (99.8% pure) or placebo for eight weeks. Comprehensive metabolic panels, complete blood counts, body weight, vital signs, and health-related quality of life questionnaires were assessed every two weeks. Participants were interviewed for adverse events (AEs) throughout the trial. Thirteen of 14 (93%) and 14 of 16 (88%) participants completed the trial in the placebo and xanthohumol groups, respectively. There were no withdrawals due to AEs. There were no clinically relevant, between-group differences in laboratory biomarkers, body weight, vital signs, or health-related quality of life. There were no severe or FDA-defined serious AEs, but non-serious AEs are documented in both the placebo (n = 42) and xanthohumol (n = 58) groups. Conclusion: Over an eight-week period, 24 mg daily xanthohumol was safe and well-tolerated by healthy adults.

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Section: Methodsmentioning

confidence: 99%

Xanthohumol Microbiome and Signature in Healthy Adults (the XMaS Trial): Safety and Tolerability Results of a Phase I Triple‐Masked, Placebo‐Controlled Clinical Trial

Langley

Ryan

Hanes

et al. 2021

Molecular Nutrition Food Res

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“…Intervention description {11a} and choice of comparators {6b} [26]. Participants randomized to placebo will be administered 288 mg of rice protein, 109.3 mg microcrystalline cellulose, 4.3 mg silica, and 4.3 mg magnesium stearate combined in an identical capsule.…”

Section: Interventionsmentioning

confidence: 99%

Xanthohumol microbiome and signature in healthy adults (the XMaS trial): a phase I triple-masked, placebo-controlled clinical trial

Bradley

Langley

Ryan

et al. 2020

Trials

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Background Natural products may provide a source for the discovery and development of adjunctive pharmacological interventions to modulate the inflammatory pathways contributing to chronic disease. Xanthohumol, a flavonoid from the hops plant (Humulus lupulus), has antioxidant and anti-inflammatory properties and may act as a prebiotic to the intestinal microbiota. Xanthohumol is not currently approved as a drug by the US Food and Drug Administration (FDA), but is available as a dietary supplement and ingredient in medical foods. To formally test the safety of xanthohumol, a phase I clinical trial (“XMaS”) was designed and approved under an Investigational New Drug application to the US FDA. The main objective is to examine the clinical safety and subjective tolerability of xanthohumol in healthy adults compared to placebo. Additional aims are to monitor biomarkers related to inflammation, gut permeability, bile acid metabolism, routes, and in vivo products of xanthohumol metabolism, and to evaluate xanthohumol’s impact on gut microbial composition. Methods The safety and tolerability of xanthohumol in healthy adults will be evaluated in a triple-masked, randomized, placebo-controlled trial. Participants will be randomized to either 24 mg/day of xanthohumol or placebo for 8 weeks. Blood cell counts, hepatic and renal function tests, electrolytes, and self-reported health-related quality of life measures will be collected every 2 weeks. Participants will be queried for adverse events throughout the trial. Xanthohumol metabolites in blood, urine, and stool will be measured. Biomarkers to be evaluated include plasma tumor necrosis factor-alpha, various interleukins, soluble CD14, lipopolysaccharide-binding protein, fecal calprotectin, and bile acids to assess impact on inflammatory and gut permeability-related mechanisms in vivo. Stool samples will be analyzed to determine effects on the gut microbiome. Discussion This phase I clinical trial of xanthohumol will assess safety and tolerability in healthy adults, collect extensive biomarker data for assessment of potential mechanism(s), and provide comparison data necessary for future phase II trials in chronic disease(s). The design and robustness of the planned safety and mechanistic evaluations planned provide a model for drug discovery pursuits from natural products. Trial registration ClinicalTrials.gov NCT03735420. Registered on November 8, 2018

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“…A modulation of molecular targets that act in multiple metabolic processes (e.g., PPAR𝛾, LXR) might explain the various effects of xanthohumol in living organisms. Nevertheless, mainly due to poor bioavailability of orally administered xanthohumol, [29,50,56] and a strong metabolization in the body, [30,44,47,48] it remains uncertain whether in vitro observations can be translated to effects in the living organism.…”

Section: Discussion Conclusion and Further Directionsmentioning

confidence: 99%

“…[43] In metabolically healthy subjects, the plasma concentration of xanthohumol and its metabolites was higher when xanthohumol (12 mg) was consumed in a proteinrich spent hops matrix than in a spent hops powder preparation (Table 1). [50] Micellar solubilization, which has been successfully employed to increase the transport of curcumin through intestinal cells [51] and to enhance the bioavailability of curcumin [52][53][54] and resveratrol [55] in humans, also increased concentrations of xanthohumol and its biological activities (on biomarkers of the metabolic syndrome and chronic low-grade inflammation) in mice and rats. [29,56] However, enhanced bioavailability of xanthohumol by micellar solubilization remains to be confirmed in human studies.…”

Section: Methods To Enhance the Bioavailability Of Xanthohumolmentioning

confidence: 99%

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Bioavailability and Cardiometabolic Effects of Xanthohumol: Evidence from Animal and Human Studies

Neumann

Frank

Venturelli

et al. 2022

Molecular Nutrition Food Res

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Xanthohumol is the main prenylflavonoid in hops and has been associated with a wide range of health benefits, due to its anti-inflammatory, anti-oxidative, and cancer-preventive properties. Increasing evidence suggests that xanthohumol positively affects biomarkers associated with metabolic syndrome and cardiovascular diseases (CVDs). This review summarizes the effects of xanthohumol supplementation on body weight, lipid and glucose metabolism, systemic inflammation, and redox status. In addition, it provides insights into the pharmacokinetics of xanthohumol intake. Animal studies show that xanthohumol exerts beneficial effects on body weight, lipid profile, glucose metabolism, and other biochemical parameters associated with metabolic syndrome and CVDs. Although in vitro studies are increasingly elucidating the responsible mechanisms, the overall in vivo results are currently inconsistent and quantitatively insufficient. Pharmacokinetic and safety studies confirm that intake of xanthohumol is safe and well tolerated in both animals and humans. However, little is known about the metabolism of xanthohumol in the human body, and even less about its effects on body weight and CVD risk factors. There is an urgent need for studies investigating whether the effects of xanthohumol on body weight and cardiometabolic parameters observe in animal studies are reproducible in humans, and what dosage, formulation, and intervention period are required.

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Rice Protein Matrix Enhances Circulating Levels of Xanthohumol Following Acute Oral Intake of Spent Hops in Humans

Abstract: Compared to a standard spent hops powder, a protein-rich spent hops matrix demonstrates enhanced plasma levels of XN and metabolites following acute oral intake.

Cited by 6 publications

References 28 publications

Xanthohumol Microbiome and Signature in Healthy Adults (the XMaS Trial): Safety and Tolerability Results of a Phase I Triple‐Masked, Placebo‐Controlled Clinical Trial

Xanthohumol Microbiome and Signature in Healthy Adults (the XMaS Trial): Safety and Tolerability Results of a Phase I Triple‐Masked, Placebo‐Controlled Clinical Trial

Xanthohumol microbiome and signature in healthy adults (the XMaS trial): a phase I triple-masked, placebo-controlled clinical trial

Bioavailability and Cardiometabolic Effects of Xanthohumol: Evidence from Animal and Human Studies

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