Veselovský J, Oláh Z, Veselovská Z, Veselá A
Katedra zivocísnej fyziológie a etológie Prírodovedeckej fakulty Univerzity Komenského, Bratislava.
Cesk Slov Oftalmol. 1998 Jan;54(1):10-7.
On the basis of the proofs of pilocarpine interaction with free amino acids, the mechanism of this alkaloid effect in the tissue structures of the eye anterior segment is explained. Differences of colour reactions of amino acids mixtures with pilocarpine, decrease of radioactivity of Na[I125]tyrosine mixture with pilocarpine, unsteadiness of radioactivity of Na[I125]protein A mixture with pilocarpine and rise of 16 radioactivity fractions after adding pilocarpine to Na[I125]proteins A a) show the specificity of interaction of each amino acid with pilocarpine; b) give evidence of a strong covalent bond between pilocarpine and free amino acid and give rise to new biologically active metabolite; c) show non-cholinergic pathway of pilocarpine effect; d) for ophthalmo-physiological practice it is said that with respect to the rate between pilocarpine quantity and concentration and free amino acid quantity and concentration requested therapeutical effect by lower pilocarpine dose in glaucoma disease treatment might be achieved. Thus free amino acids being reactants can be identified as mechanism by which pilocarpine becomes biologically active.
基于毛果芸香碱与游离氨基酸相互作用的证据,解释了这种生物碱在眼前节组织结构中的作用机制。氨基酸混合物与毛果芸香碱的颜色反应差异、毛果芸香碱存在时Na[I125]酪氨酸混合物放射性的降低、毛果芸香碱存在时Na[I125]蛋白A混合物放射性的不稳定以及向Na[I125]蛋白A中添加毛果芸香碱后16个放射性组分的增加:a) 表明每种氨基酸与毛果芸香碱相互作用的特异性;b) 证明毛果芸香碱与游离氨基酸之间存在强共价键并产生新的生物活性代谢物;c) 显示毛果芸香碱作用的非胆碱能途径;d) 对于眼科生理实践而言,就毛果芸香碱的量和浓度与游离氨基酸的量和浓度之间的比率而言,在青光眼疾病治疗中通过较低剂量的毛果芸香碱可能实现所需的治疗效果。因此,作为反应物的游离氨基酸可被确定为毛果芸香碱具有生物活性的机制。