Morin sulfates/glucuronides exert anti-inflammatory activity on activated macrophages and decreased the incidence of septic shock
Morin sulfates/glucuronides exert anti-inflammatory activity on activated macrophages and decreased the incidence of septic shock
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DOI：
10.1016/j.lfs.2003.07.017
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发表时间：
2003-12-26
期刊：
影响因子：
6.1
通讯作者：
Chiang, BL
中科院分区：
文献类型：
--
作者：
Fang, SH;Hou, YC;Chiang, BL
桑色素是一种存在于水果和中草药中的类黄酮。基于体外研究，已报道桑色素显示出各种有益的生物活性。然而，越来越多的证据表明，共轭代谢是黄酮类化合物生物命运的核心。因此，桑色素的生物学效应主要取决于其结合代谢产物。在这项研究中，桑色素及其硫酸盐/葡萄糖醛酸苷对脂多糖（LPS）激活的巨噬细胞产生一氧化氮（NO）和细胞因子的影响进行了单独研究和比较。结果表明，1.25 mM桑色素和1.25 μ M桑色素硫酸盐/葡萄糖醛酸苷可抑制LPS激活的RAW 264.7细胞产生50%的NO。同时，桑色素和桑色素硫酸盐/葡萄糖醛酸苷在活化的腹腔巨噬细胞中的50%抑制浓度（IC 50）值分别为1.5 mM桑色素和1.5 μ M桑色素硫酸盐/葡萄糖醛酸苷。此外，30%的肿瘤坏死因子-α（TNF-α）和35%的白细胞介素（IL）-12从激活的巨噬细胞的生产被抑制2类似于2.5 mM桑色素和2类似于2.5 μ M桑色素硫酸盐/葡萄糖醛酸苷，分别。此外，给药桑色素两个月的小鼠外周血中的吞噬细胞活性约为65%，与对照组的70%相似。较低的NO产生和减少的巨噬细胞吞噬活性对应于LPS抵抗状态。这些结果表明，桑色素可能通过降低巨噬细胞的功能，表现出抗炎活性，降低实验性感染性休克的发生率，并可能通过调节细胞因子谱来调节免疫反应。因此，桑色素可能是一个有前途的治疗候选人的炎症性疾病，由于其代谢产物的强活性。(C)2003年由Elsevier Inc.出版
Morin is a flavonoid present in fruits and Chinese herbs. Based on in vitro studies, morin has been reported to show various beneficial biological activities. However, there is growing evidence that conjugative metabolism is central to the biological fate of flavonoids. Therefore, the biological effects of morin could be primarily determined by its conjugated metabolites. In this study, the effects of morin and its sulfates/glucuronides on the production of nitric oxide (NO) and cytokines from lipopolysaccharide (LPS)-activated macrophages were individually investigated and compared. The results indicated that the 50% NO production was inhibited from LPS-activated RAW 264.7 cells by 1.25 mM morin and 1.25 muM morin sulfates/glucuronides. Meanwhile, the 50% inhibition concentration (IC50) values of morin and morin sulfates/glucuronides in activated peritoneal macrophages were 1.5 mM morin and 1.5 muM morin sulfates/glucuronides, respectively. In addition, 30% of the tumor necrosis factor-alpha (TNF-alpha) and 35% of the interleukin (IL)-12 productions from activated macrophages were inhibited by 2 similar to 2.5 mM morin and 2 similar to 2.5 gM morin sulfates/glucuronides, respectively. Furthermore, phagocyte activities in the peripheral blood of those for mice dosed with morin for two months were about 65 similar to 70% of controls. Lower NO production and reduced macrophage phagocytic activities corresponded to LPS-resistant state. These findings indicated that morin may exhibit anti-inflammatory activity and reduced the incidence of experimental septic shock through decreasing the functions of macrophages and may regulate immune response through modulating the cytokine profiles. Therefore, morin could be a promising therapeutic candidate for inflammatory disease due to the strong activity of its metabolites. (C) 2003 Published by Elsevier Inc.