| Autor: |
Keerthana Morusu, Vidyavathi Maravajhala |
| Rok vydání: |
2021 |
| Předmět: |
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| Zdroj: |
Lecture Notes in Networks and Systems ISBN: 9789811619403 |
| DOI: |
10.1007/978-981-16-1941-0_28 |
| Popis: |
Loratadine is an antihistaminic nonsedating drug that acts on H1 receptors. Loratadine shows rapid absorption and subjected to pervasive first-pass metabolism and majorly converted to its metabolite descarboethoxyloratadine, which is also known as desloratadine. The Cytochrome P450-catalyzed reactions are sufficiently described by classical Michaelis–Menten kinetic parameters (e.g., Km and Vmax). In turn, these parameters may be used to predict pharmacokinetics. Microorganisms especially fungi can also have the capability to mimic the biotransformation reactions that occur in mammals. The present study was emphasized to estimate the enzyme kinetic parameters of loratadine biotransformation by fungi. In preliminary fungal screening studies, it was revealed that two Cunnighmella fungi and one Aspergillus fungus proved their capability for loratadine transformation. These three fungi were further used to evaluate the enzyme kinetics of loratadine biotransformation. The kinetic parameters Km and V max were obtained from Graph pad prism-5 software upon application of HPLC data of all samples. The results of these enzyme kinetic studies showed that the product (metabolite) formation by both Cunnighamella elegans and Cunnighamella echinulata was increased with increasing substrate concentration up to saturation level indicated that these follow classical Michaelis–Menten kinetics. The product formed by Aspergillus niger showed atypical kinetics due to substrate autoinhibition at high concentrations of substrates. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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