Zou W, Yang C, Liu M, Su W
School of Life Sciences, Sun Yat-sen University, Guangzhou, People's Republic of China.
Arzneimittelforschung. 2012 Apr;62(4):181-6. doi: 10.1055/s-0031-1299746. Epub 2012 Jan 23.
Naringin (CAS 10236-47-2), a flavanone glucoside widely present in fruits of citrus plants, has received extensive studies on its potential effects on health benefits and was recently demonstrated to be a putative antitussive. In this study, we determined the tissue distributions of naringin and its metabolites (naringenin and naringenin's conjugates) in rats to examine whether they undergo selective uptake by specific organs. Naringin was administered orally to rats at the dose of 42 mg/kg and the concentrations of naringin and its metabolites in tissue compartments were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The areas under curve values in the individual tissues decreased as follows: stomach, small intestine, liver, trachea, muscle, kidney, lung, fat, heart, spleen, ovary, testis, brain for naringin; and liver, stomach, small intestine, kidney, trachea, lung, testis, heart, ovary, fat, spleen, muscle, brain for total naringenin (including free and its conjugates). Naringin and total naringenin were rapidly and widely distributed to all the tissues except brain in rats. They had difficulties in crossing the blood-brain barrier. There are no accumulations in rats. This study identifying naringin in several organs including lung and trachea may explain its effects as antitussive.
柚皮苷（CAS 10236-47-2）是一种广泛存在于柑橘类植物果实中的黄酮醇苷，其对健康益处的潜在影响已得到广泛研究，最近被证明是一种假定的镇咳剂。在本研究中，我们测定了柚皮苷及其代谢产物（柚皮素及其结合物）在大鼠体内的组织分布，以检查它们是否被特定器官选择性摄取。以42 mg/kg的剂量给大鼠口服柚皮苷，并通过液相色谱-串联质谱法（LC-MS/MS）测定组织隔室中柚皮苷及其代谢产物的浓度。各组织中的曲线下面积值下降情况如下：柚皮苷：胃、小肠、肝脏、气管、肌肉、肾脏、肺、脂肪、心脏、脾脏、卵巢、睾丸、脑；总柚皮素（包括游离型及其结合物）：肝脏、胃、小肠、肾脏、气管、肺、睾丸、心脏、卵巢、脂肪、脾脏、肌肉、脑。柚皮苷和总柚皮素在大鼠体内迅速且广泛地分布到除脑以外的所有组织中。它们难以穿过血脑屏障。在大鼠体内无蓄积现象。本研究在包括肺和气管在内的多个器官中鉴定出柚皮苷，这可能解释了其作为镇咳剂的作用。
