白术的水溶性化学成分及其促肠动力活性研究

WATER-SOLUBLE CONSTITUENTS AND THEIR PROKINETIC ACTIVITY FROM ATRACTYLODES MACROCEPHAL

实验采用超高效液相色谱离子淌度-四极杆串联飞行时间质谱仪(UPLC-IMS-QTOF-MS)技术分析白术水溶性化学成分,并评估其主要成分的促肠动力活性。白术水提取物经溶剂萃取(石油醚/水、乙酸乙酯/水)和D-101大孔树脂纯化后,得到的白术水溶性部位采用UPLC BEH C18色谱柱(2.1 mm×100 mm,1.7μm),以0.1%甲酸水溶液(A)-乙腈(B)为流动相进行梯度洗脱,ESI源负离子模式下采集质谱数据;采用小鼠整体肠传输和离体兔回肠收缩实验进行活性评估。结果确定了20个化合物,主要为愈创木烷型倍半萜醇糖苷,其中苍术苷A占鉴定的白术水溶性成分总峰面积的49.68%。促肠动力作用的实验结果表明,37.5μg/mL苍术苷A显著促进家兔离体回肠的自发性收缩,收缩促进率为38.1%;5 mg/kg苍术苷A明显加速正常小鼠的小肠推进和全胃肠传输。研究结果确定,白术的水溶性部位主要含愈创木烷型倍半萜醇糖苷,其主要成分苍术苷A具有促肠动力活性。

Water-soluble chemical constituents from Atractylodes macrocephala were identified by using UPLC(ultra-high performance liquid chromatography)system coupled to ion mobility spectroscopy quadrupole-time of flight mass spectrometer(UPLC-IMS-QTOF-MS),and the activity of the main components was determined in vitro and vivo experiments.The water extract of A.macrocephala was subjected to liquid-liquid extraction(petroleum ether/water,ethyl acetate/water)and purification by D-101 macroporous resin to obtain the water-soluble portion,then UPLC was performed on BEH C18 column with 0.1%formic acid in water(A)-acetonitrile(A)as mobile phase in a gradient elution mode.The mass spectrometer equipped with electrospray ionization source was used as a detector under the negative ion mode.Assessment of prokinetic potential included whole gut transit in mice and isolated rabbit ileal contraction.The results showed that twenty compounds were identified,including 18 glycosides,mainly guaiane-type sesquiterpene alcohol glycosides and atractyloside A accounted for 49.68%of the total peak area of the identified water-soluble components in A.macrocephala.The experimental results of prokinetic actions indicate that 37.5μg/mL atractyloside A significantly promotes spontaneous contraction of the isolated ileum in rabbits,with an increasing contraction rate of 38.1%;5 mg/kg atractyloside A significantly accelerates the small intestine propulsion and whole GI transit in normal mice.This study illustrates that the water-soluble compounds of A.macrocephala mainly contain the guaiane-type sesquiterpene alcohol glycosides,and the main components possess the prokinetic activity.