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目的利用菜籽粕制备芥子碱氯化盐,探讨其对自发性高血压大鼠(spontaneous hypertension rat,SHR)的降压作用。方法菜籽粕经水提法制备芥子碱硫氰酸盐,用氯型717阴离子交换树脂转换为芥子碱氯化盐,并通过理化性质和波谱数据对其进行结构鉴定。对随机分组的SHR大鼠连续给药28 d,间隔4 d测定其收缩压、舒张压、平均脉压和心率。结果采用1H-NMR、13C-NMR和IR法鉴定芥子碱硫氰酸盐与芥子碱氯化盐,HPLC归一化法测定芥子碱氯化盐纯度质量分数达99%。芥子碱氯化盐能显著降低SHR大鼠的收缩压、舒张压和平均脉压(P<0.05～0.01),但对心率无明显影响。结论该制备工艺简单,所得产品纯度高,对SHR大鼠降压作用显著,具备较好的药物开发前景。
Objective To prepare crude sinapine chloride by rapeseed meal and investigate its antihypertensive effect on spontaneous hypertensive rats (SHR). Method Rapeseed meal was prepared by water extraction, and converted to sinapine chloride by chlorine 717 anion exchange resin. The structure was identified by its physicochemical properties and spectral data. SHR rats were randomized to receive continuous administration for 28 days and measured systolic, diastolic, mean pulse pressure, and heart rate at 4-day intervals. Results Sinapine thiocyanate and sinapine chloride were identified by 1H-NMR, 13C-NMR and IR. The purity of sinapine chloride was 99% by HPLC. Sinapine chloride can significantly reduce systolic blood pressure, diastolic blood pressure and mean pulse pressure in SHR rats (P <0.05 ~ 0.01), but had no significant effect on heart rate. Conclusion The preparation process is simple, the purity of the product obtained is high, the antihypertensive effect is obvious to SHR rats, and the drug has good prospect of drug development.