A Quercetin Containing Supplement Reduces Niacin-Induced Flush in Humans

Abstract

Coronary artery disease is associated with increased serum levels of cholesterol, triglycerides and LDL, but low levels of HDL. The most potent agent capable of reversing this trend is the vitamin nicotinic acid (niacin). However, compliance even with extended-release preparations and addition of acetylsalicylic acid (ASA) is hampered by the development of a feeling of erythema and burning ("flush"), especially on the face. We recently showed that the natural flavonoids quercetin and luteolin can eliminate "flush", as well as inhibit both niacin-induced plasma prostaglandin D, (PGD z ) and serotonin increase in an animal model. We conducted a pilot clinical study in humans. Four normal male subjects received (a) 1 g immediate release niacin either alone or after (b) the dietary formulation (Algonot-plus") containing 150 mg quercetin per capsule. Subjects completed a visual scale (l=no, 5=worst response) symptom assessment. Erythema and burning sensation scores were both 4.75±0.50 and lasted for 3.63±1.11 hours. After Algonot-plus" administration, both scores were reduced to 2.5±0.58 and lasted for only 1.68±O.70 hours. Quercetin also inhibited methylnicotinate-induced human mast cell PGD z release. These preliminary results suggest that quercetin could reduce niacin-induced "flush" in humans.Ingestion of the B 3-vitamin niacin (nicotinic acid) has been repeatedly shown to improve hypercholesterolemia and other lipoprotein abnormalities, while it also-increases HOL levels (1). Moreover, the combination of niacin with lovastatin has been shown to be superior to either agent alone (2-4). However, a serious limiting adverse effect is the development of significant facial erythema and warmth, known as "flush" that is more intense with immediate release than with extended release niacin (2, 5-6). Moreover, most of the over-the-counter formulations either do not contain sufficient niacin to have any effect or contain niacin metabolites that are ineffective (7).Niacin is thought to induce flush by stimulating the release of prostaglandin 02 (PG0 2) from the skin (8-9), most likely from dermal macrophages (10). However, co-administration of acetylsalicylic acid (ASA) does not reduce PGD 2 levels more than about 30% (II). Other measures used to reduce flush have included avoidance of alcohol and spicy foods with little benefit (12).We recently used a rat model of flush (13) and showed that niacin-induced skin vasodilation was accompanied by increased plasma PGD 2 , but also serotonin increases, both of which were inhibited along with the flush by the f1avonoids quercetin and luteolin (14). We therefore conducted a pilot clinical trial to investigate if a quercetin containing dietary supplement could inhibit niacin-induced flush in humans. MATERIALS AND METHODS MaterialsImmediate release macin caplets (250 mg each, SLO-NIACIN<l<) were obtained commercially (UpsherSmith Laboratories, Inc., Minneapolis, MN). Quercetin were obtained from Sigma (St. Louis, MO) and were dissolved in olive kernel extract. Four normal male subjec...

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