Inhibition and Structural Changes of Liver Alkaline Phosphatase by Tramadol

Title:Inhibition and Structural Changes of Liver Alkaline Phosphatase by Tramadol

Volume: 8 Issue: 2

Author(s): Dariush Minai-Tehrani, Mahya Eslami, Nafsa Khazaei, Elmira Katebian, Leila Azizi, Fatemeh Yazdi, Akram Sadat Hosseini and Mohammadreza Taheri

Affiliation:

Keywords: Conformational changes, drug, enzyme, inhibition.

Abstract: Tramadol is a potent analgesic drug which interacts with mu-opioid and has low effect on other opioid receptors. Unlike other opioids, it has no clinically significant effect on respiratory or cardiovascular parameters. Alakaline phosphatase is a hydrolase enzyme that prefers alkaline condition and removes phosphate group from different substrates. In this study, the interaction between tramadol and calf liver alkaline phosphatase was investigated. The results showed that tramadol can bind to alakaline phosphatase and inhibit the enzyme in an un-competitive manner. Ki and IC50 values of tramadol were determined as about 91 and 92 μM, respectively. After enzyme purification, structural changes on alakaline phosphatase-drug interaction were studied by circular dichroism and fluorescence measurement. These data revealed the alteration in the content of secondary structures and also conformational changes in enzyme occurred when the drug bound to enzyme-substrate complex.

Cite this article as:

Minai-Tehrani Dariush, Eslami Mahya, Khazaei Nafsa, Katebian Elmira, Azizi Leila, Yazdi Fatemeh, Hosseini Sadat Akram and Taheri Mohammadreza, Inhibition and Structural Changes of Liver Alkaline Phosphatase by Tramadol, Drug Metabolism Letters 2014; 8 (2) . https://dx.doi.org/10.2174/1872312808666140506093756