Kalogeromitros D, Makris M, Chliva C, Aggelides X, Kempuraj D, Theoharides T C
Allergy Clinical Research Center, Allergy Section, Attikon Hospital, University of Athens Medical School, Athens, Greece.
Int J Immunopathol Pharmacol. 2008 Jul-Sep;21(3):509-14. doi: 10.1177/039463200802100304.
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 D2 (PGD2) 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 (1 = 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 only for 1.68+/-0.70 hours. Quercetin also inhibited methylnicotinate-induced human mast cell PGD2 release. These preliminary results suggest that quercetin could reduce niacin-induced "flush" in humans.
冠状动脉疾病与血清胆固醇、甘油三酯和低密度脂蛋白水平升高相关,但高密度脂蛋白水平较低。能够逆转这种趋势的最有效药物是维生素烟酸。然而,即使使用缓释制剂并添加乙酰水杨酸(ASA),患者仍会因出现红斑和烧灼感(“潮红”),尤其是面部潮红,而影响依从性。我们最近发现,天然类黄酮槲皮素和木犀草素可以消除“潮红”,并在动物模型中抑制烟酸诱导的血浆前列腺素D2(PGD2)和血清素升高。我们在人体上进行了一项初步临床研究。四名正常男性受试者接受了(a)单独服用1克速释烟酸,或(b)服用每粒胶囊含150毫克槲皮素的膳食配方(Algonot-plus)后再服用1克速释烟酸。受试者完成了视觉量表(1=无,5=最差反应)症状评估。红斑和烧灼感评分均为4.75±0.50,持续3.63±1.11小时。服用Algonot-plus后,两项评分均降至2.5±0.58,仅持续1.68±0.70小时。槲皮素还抑制了甲基烟酸酯诱导的人肥大细胞PGD2释放。这些初步结果表明,槲皮素可以减轻人体中烟酸诱导的“潮红”。