College of Horticulture and Forestry Sciences, Key Laboratory of Horticultural Plant Biology, Huazhong Agricultural University, Ministry of Education, Wuhan, 430070, China.
Inflammation. 2013 Dec;36(6):1525-32. doi: 10.1007/s10753-013-9695-y.
Poncirus trifoliate is a traditional Chinese medicinal plant used for treating inflammation-related diseases for a long time and trifoliate orange contains abundant auraptene. The present study was to evaluate auraptene as a potential anti-inflammatory agent and investigate the mechanism of auraptene against prostaglandins E2 (PGE2) and cyclooxygenase-2 (COX-2) on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by comparing it with aspirin as a positive control group. The methods of enzyme-linked immunosorbent assay, reverse transcriptive polymerase chain reaction, real-time PCR, and western-blotting were used in the study. The results showed that auraptene exhibited better biocompatibility and lower cytotoxicity. At the same time, it significantly inhibited the production of PGE2 on LPS-stimulated macrophage cells. The auraptene-treated group had a higher COX-2 mRNA expression but relatively lower COX-2 protein level which implied that auraptene suppressed the post-transcriptional expression of COX-2 protein but not the transcriptional process. Compared with aspirin, the lower cytotoxicity of auraptene can make it a potential source for medicine that can benefit patients who are suffering from chronic inflammatory diseases and need long-term medication.
枳实为一种传统的中药,长期以来一直被用于治疗与炎症相关的疾病,且枳实中含有丰富的佛手柑内酯。本研究通过与阿司匹林作为阳性对照组进行比较,旨在评估佛手柑内酯作为一种潜在的抗炎剂,以及研究佛手柑内酯对脂多糖(LPS)刺激的 RAW264.7 细胞中前列腺素 E2(PGE2)和环氧化酶-2(COX-2)的作用机制。本研究采用酶联免疫吸附测定法、逆转录聚合酶链反应、实时 PCR 和 Western-blotting 等方法。结果表明,佛手柑内酯表现出更好的生物相容性和更低的细胞毒性。同时,它能显著抑制 LPS 刺激的巨噬细胞中 PGE2 的产生。佛手柑内酯处理组 COX-2mRNA 表达较高,但 COX-2 蛋白水平相对较低,这表明佛手柑内酯抑制了 COX-2 蛋白的转录后表达,但没有影响转录过程。与阿司匹林相比,佛手柑内酯较低的细胞毒性使其成为一种潜在的药物来源,可以造福于患有慢性炎症性疾病且需要长期用药的患者。