Nagalski Andrzej, Bryła Jadwiga
Zakład Regulacji Metabolizmu, Instytut Biochemii, Wydział Biologii, Uniwersytet Warszawski, Warszawa, Poland.
Postepy Hig Med Dosw (Online). 2007 May 15;61:288-302.
Niacin (nicotinic acid and nicotinamide) is a vitamin used as a source of the NAD+ and NADP+ coenzymes required for many metabolic processes. Its low dietary levels induce the development of pellagra. Niacin has been used for decades in the treatment of patients with disturbed lipid and lipoprotein metabolism, this being the main cause of atherosclerotic changes in cardiovascular diseases. It is still the most efficacious drug in terms of its ability to increase HDL cholesterol content accompanied by a decrease in all atherogenic lipoproteins (VLDL, LDL, and L(a)) as well as fatty acids and triglycerides. Niacin also increases adiponectin level, which might result in additional atheroprotection. There are studies confirming the beneficial action of niacin against migraine and hyperphosphatemia associated with renal failure, ethanol-induced neurodegeneration, and loss of beta-cell function in type 1 diabetes. Moreover, it augments plasma tryptophan concentrations in HIV-infected patients and thyroid radiosensitivity to 131I. Inhibition of the invasion of hepatoma cells has also been proven. However, it is necessary to point out that the currently applied niacin preparations might exhibit such side effects as cutaneous flushing, gastrointestinal disturbances, and hepatotoxicity, particularly during treatment with sustained-release niacin preparations. The recent discovery of the G-protein-coupled receptor GPR109A, which mediates the antilipolytic effects induced by nicotinic acid in adipocytes as well as cutaneous vasodilation, allows the development of new agents interacting with this receptor. In view of these observations, niacin therapy must be accompanied by control of the choice of niacin preparation and its dose in order to eliminate or at least limit its side effects.
烟酸(尼克酸和烟酰胺)是一种维生素,用作许多代谢过程所需的NAD +和NADP +辅酶的来源。其低膳食水平会诱发糙皮病的发展。几十年来,烟酸一直用于治疗脂质和脂蛋白代谢紊乱的患者,这是心血管疾病中动脉粥样硬化变化的主要原因。就增加高密度脂蛋白胆固醇含量以及降低所有致动脉粥样硬化脂蛋白(极低密度脂蛋白、低密度脂蛋白和L(a))以及脂肪酸和甘油三酯的能力而言,它仍然是最有效的药物。烟酸还会增加脂联素水平,这可能会带来额外的抗动脉粥样硬化保护作用。有研究证实了烟酸对偏头痛以及与肾衰竭、乙醇诱导的神经变性和1型糖尿病中β细胞功能丧失相关的高磷血症具有有益作用。此外,它会提高HIV感染患者的血浆色氨酸浓度以及甲状腺对131I的放射敏感性。还证实了其对肝癌细胞侵袭的抑制作用。然而,必须指出的是,目前应用的烟酸制剂可能会出现诸如皮肤潮红、胃肠道紊乱和肝毒性等副作用,特别是在使用缓释烟酸制剂治疗期间。最近发现的G蛋白偶联受体GPR109A介导了烟酸在脂肪细胞中诱导的抗脂解作用以及皮肤血管舒张,这使得能够开发与该受体相互作用的新型药物。鉴于这些观察结果,烟酸治疗必须同时控制烟酸制剂的选择及其剂量,以消除或至少限制其副作用。