[关键词]
[摘要]
目的 建立全新结构化合物4-(5'-二甲氨基)-萘磺酰氧基苯并噁唑酮(W3D)的含量测定方法,并对其进行体内抗炎活性评价。方法 采用Diamonsil C18(250 mm×4.6 mm,5 μm)色谱柱,以甲醇-水(75∶25)为流动相,体积流量1.0 mL·min-1,检测波长257 nm,柱温28℃,测定W3D的峰面积,建立其含量测定方法;采用二甲苯致小鼠耳肿胀模型评价化合物W3D(25.000、12.500、6.250、3.125 mg·kg-1)体内抗炎活性。结果 供试品主峰专属性良好,在1~100 μg·mL-1线性关系良好(R2=0.999 9),精密度、重复性、稳定性的RSD分别为0.61%、0.19%、0.84%,回收率为99.55%(RSD=0.81%);与对照组比较,W3D各剂量组耳肿胀率均显著下降(P<0.05、0.01),12.5 mg·kg-1组抑制率可达53.88%,优于阳性药塞来昔布。结论 建立的HPLC法简便、准确,且专属性好,可用于W3D的含量检测;W3D具有较好的体内抗炎活性,作为新结构抗炎小分子化合物具有深入研究的价值。
[Key word]
[Abstract]
Objective To establish a method for determining the content of the novel compound 4- (5'-dimethylamino) - naphthalenesulfonyl-2(3H)-benzoxazolone (W3D), and to evaluate the anti-inflammatory activity in vivo. Methods HPLC method was performed on the Diamonsil C18 column (250 mm×4.6 mm, 5 μm) with the mobile phase consisted of methanol-water (75∶25) at a flow rate of 1.0 mL·min-1. The detection wavelength was set at 257 nm and the column temperature was 28 ℃. Xylene-induced mouse ear swelling model was used to evaluate the anti-inflammatory activity of W3D (25.000, 12.500, 6.250, and 3.125 mg·kg-1) in vivo. Results Under the above chromatographic conditions, the compound W3D could be completely separated. The linear range was 1—100 μg·mL-1 (R2 = 0.999 9). RSD of precision, repeatability and stability were 0.61%, 0.19% and 0.84% respectively, and the average recovery was 99.55% (RSD = 0.81%). Compared with control group, the ear swelling rate of each dose group of W3D significantly decreased (P < 0.05, 0.01), and the inhibition rate of the 12.5 mg·kg-1 group reached 53.88%, which was better than the positive drug celecoxib. Conclusion The analytical method was simple, accurate and specific which could be used on the determination of the content of compound W3D. As a new compound with determinate anti-inflammatory activity in vivo, it was worth to carry out further research.
[中图分类号]
R917
[基金项目]
国家自然科学基金资助项目(81602976);山西省应用基础研究项目(201901D211350)