Chauhan Ayesha, Gupta Shiffalli, Mahmood Akhtar
Department of Biochemistry, Panjab University, Chandigarh 160 014, India.
Indian J Exp Biol. 2007 Apr;45(4):353-8.
Tannic acid is a glucoside (penta-m-digallolyl-glucose), which exhibits a wide variety of physiological functions. Around neutral pH, 0.4 mM tannic acid produced 84% inhibition of rat brush border sucrase activity, but 35-40% enzyme inhibition was observed in the rabbit intestine at 0.08 mM concentration. In the mice, 74-77% enzyme inhibition was observed at 0.05 mM concentration of tannic acid. The observed inhibition was reversible in rat intestine. Tannic acid (0.2 mM) also inhibited lactase (18% in adult and 71% in suckling animals), maltase (76%) and trehalase (88%) activities in rat intestine. pH versus activity curves showed that 0.2 mM tannic acid inhibited enzyme activity in rat by 91% at pH 5.5 which was reduced to 14% at pH 8.5 compared to the respective controls. In the rabbit 18-60% enzyme inhibition was noticed below pH 7.0, however at pH 8.5, it was of the order of 38%. Kinetic analysis revealed that tannic acid is a competitive inhibitor of rat brush border sucrase at pH 6.8. Effect of tannic acid together with various -SH group reacting reagents revealed that the enzyme inhibition is additive in nature, suggesting the distinct nature of binding sites on the enzyme for these compounds. The results suggest that tannic acid is a potent inhibitor of intestinal brush border disaccharidases, and could modulate the intestinal functions.
鞣酸是一种糖苷(五 - 间 - 没食子酰基 - 葡萄糖),具有多种生理功能。在接近中性pH值时,0.4 mM的鞣酸可使大鼠刷状缘蔗糖酶活性受到84%的抑制,但在兔肠道中,0.08 mM浓度时可观察到35 - 40%的酶抑制作用。在小鼠中,0.05 mM浓度的鞣酸可观察到74 - 77%的酶抑制作用。在大鼠肠道中观察到的抑制作用是可逆的。鞣酸(0.2 mM)还可抑制大鼠肠道中的乳糖酶(成年动物中为18%,哺乳动物中为71%)、麦芽糖酶(76%)和海藻糖酶(88%)的活性。pH与活性曲线表明,0.2 mM鞣酸在pH 5.5时可使大鼠酶活性受到91%的抑制,与各自的对照相比,在pH 8.5时降至14%。在兔中,在pH 7.0以下可观察到18 - 60%的酶抑制作用,然而在pH 8.5时,约为38%。动力学分析表明,在pH 6.8时,鞣酸是大鼠刷状缘蔗糖酶的竞争性抑制剂。鞣酸与各种 -SH基团反应试剂共同作用的结果表明,酶抑制作用本质上是相加的,这表明这些化合物在酶上的结合位点具有不同的性质。结果表明,鞣酸是肠道刷状缘二糖酶的有效抑制剂,并可调节肠道功能。