目的 建立全新結(jié)構(gòu)化合物4-（5'-二甲氨基）-萘磺酰氧基苯并噁唑酮（W3D）的含量測定方法，并對其進(jìn)行體內(nèi)抗炎活性評價。方法 采用Diamonsil C₁₈（250 mm×4.6 mm，5 μm）色譜柱，以甲醇-水（75∶25）為流動相，體積流量1.0 mL·min^-1，檢測波長257 nm，柱溫28℃，測定W3D的峰面積，建立其含量測定方法；采用二甲苯致小鼠耳腫脹模型評價化合物W3D（25.000、12.500、6.250、3.125 mg·kg^-1）體內(nèi)抗炎活性。結(jié)果 供試品主峰專屬性良好，在1～100 μg·mL^-1線性關(guān)系良好（R²＝0.999 9），精密度、重復(fù)性、穩(wěn)定性的RSD分別為0.61%、0.19%、0.84%，回收率為99.55%（RSD＝0.81%）；與對照組比較，W3D各劑量組耳腫脹率均顯著下降（P＜0.05、0.01），12.5 mg·kg^-1組抑制率可達(dá)53.88%，優(yōu)于陽性藥塞來昔布。結(jié)論 建立的HPLC法簡便、準(zhǔn)確，且專屬性好，可用于W3D的含量檢測；W3D具有較好的體內(nèi)抗炎活性，作為新結(jié)構(gòu)抗炎小分子化合物具有深入研究的價值。

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.

R917

國家自然科學(xué)基金資助項(xiàng)目（81602976）；山西省應(yīng)用基礎(chǔ)研究項(xiàng)目（201901D211350）