Minai-Tehrani Dariush, Masoudnia Allaleh, Alavi Sana, Osmani Raheleh, Lotfi Leila, Asghari Mitra, Pirsalehi Mahdi, Sobhani-Damavandifar Zahra
Biology Department, Payam Noor University of Mashhad, Mashhad, Iran.
Drug Metabol Drug Interact. 2012;27(4):225-8. doi: 10.1515/dmdi-2012-0030.
Methocarbamol is a skeletal muscle relaxant and is widely used to relieve pain in muscles. Many drugs may have interactions with each other when used at the same time. Yeast sucrase is taken as a drug by patients with congenital sucrase-isomaltase deficiency (CSID).
In this study, the interaction between methocarbamol and yeast sucrase was investigated.
Our results showed that methocarbamol can inhibit sucrase activity and reduce the maximum reaction velocity (Vmax) of the enzyme by a non-competitive pattern. Measurement of IC50 and Ki of the drug revealed that methocarbamol did not bind the enzyme with high affinity. Fluorescence measurement showed that the drug binds to free enzyme and enzyme-substrate complexes that were accompanied by structural changes on the enzyme. Guaifenesin, which has a similar structure to methocarbamol, does not affect the activity of sucrase.
Methocarbamol inhibits sucrase activity and its carbamate group plays a main role in the binding of drug to sucrase.
美索巴莫是一种骨骼肌松弛剂，广泛用于缓解肌肉疼痛。多种药物同时使用时可能会相互作用。先天性蔗糖酶-异麦芽糖酶缺乏症（CSID）患者会将酵母蔗糖酶作为药物服用。
在本研究中，对美索巴莫与酵母蔗糖酶之间的相互作用进行了研究。
我们的结果表明，美索巴莫可抑制蔗糖酶活性，并以非竞争性模式降低该酶的最大反应速度（Vmax）。对该药物的半数抑制浓度（IC50）和抑制常数（Ki）的测定表明，美索巴莫与该酶的结合亲和力不高。荧光测量显示，该药物与游离酶和酶-底物复合物结合，同时酶的结构发生变化。与美索巴莫结构相似的愈创甘油醚不影响蔗糖酶的活性。
美索巴莫抑制蔗糖酶活性，其氨基甲酸酯基团在药物与蔗糖酶的结合中起主要作用。
