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本文报道波叶大黄多糖(Rheum hotaoense polysaccharide,RHP)对胰腺五种酶的抑制作用。结果表明。(1)RHP对胰蛋白酶、胰脂肪酶、胰淀粉酶、胰弹性蛋白酶和胰激肽释放酶均有很明显的抑制作用。IC_(50)分别为250μg/mL、21μg/mL、18μg/mL,189μg/mL和300μg/mL。(2)动力学研究表明,RHP对胰蛋白酶和胰脂肪酶的抑制均是非竞争性的,Km值分别为1.2×10~(-4)μmol/mL和1.2mg/mL,Ki值分别为355.0μg/mL和63.85μg/mL。(3)牛血清白蛋白(BSA)对RHP抑制胰蛋白晦和胰脂肪酶具有拮抗作用。当BSA浓度达72.0mg/mL时,对胰蛋白酶活性的恢复率为71.54％。当BSA浓度达20.0mg/mL时,对胰脂肪酶活性的恢复率为63.64％。上述结果表明,RHP对胰腺五种酶的抑制作用,可能是大黄治疗急性胰腺炎作用的生化机制之一,预示RHP在临床上将有重要应用前景。
This article reports the inhibitory effect of rheum hotaoense polysaccharide (RHP) on five enzymes in the pancreas. The results show. (1) RHP has a significant inhibitory effect on trypsin, pancreatic lipase, pancreatic amylase, pancreatic elastase and pancreatic kallikrein. IC 50 were 250 μg / mL, 21 μg / mL, 18 μg / mL, 189 μg / mL and 300 μg / mL, respectively. (2) Kinetic studies showed that inhibition of trypsin and pancreatic lipase by RHP were noncompetitive with Km values of 1.2 × 10 ~ (-4) μmol / mL and 1.2 mg / mL, respectively, with Ki values of 355.0 μg / mL and 63.85 μg / mL. (3) Bovine serum albumin (BSA) has antagonistic effect of RHP on trypsin and pancreatic lipase. The recovery of trypsin activity was 71.54% when the BSA concentration reached 72.0 mg / mL. When BSA concentration reached 20.0mg / mL, the recovery rate of pancreatic lipase activity was 63.64%. The above results show that the inhibitory effect of RHP on the five enzymes of the pancreas may be one of the biochemical mechanisms of rhubarb in the treatment of acute pancreatitis, indicating that RHP will have important clinical application prospects.