News Column

Researchers from University of Birjand Describe Findings in Leflunomide Therapy

June 18, 2014



By a News Reporter-Staff News Editor at Biotech Week -- Investigators publish new report on Drugs and Therapies. According to news reporting originating in Birjand, Iran, by NewsRx journalists, research stated, "Leflunomide [HWA 486 or RS-34821, 5-methyl-N-(4trifluoromethylphenyl)-4-isoxazole carboximide] is an immunosuppressive agent effective in the treatment of rheumatoid arthritis. Dihydroortate dehydrogenase (DHODH, EC 1.3.3.1) immobilization on the nanotubes was carried out and biochemical characterization of free and immobilized enzyme was determined."

The news reporters obtained a quote from the research from the University of Birjand, "In comparison with free enzyme, the immobilized DHODH showed improved stability and reusability for investigation of inhibition pattern of drugs such as leflunomide. The experimental data showed that, DHODH was inhibited by the active metabolite of leflunomide (RS-61980) with a K-i and K-I of 0.82 and 0.06 mM, respectively. Results exhibited mixed-type inhibition kinetics towards dihydroorotate as a substrate in the free and immobilized enzyme. Furthermore, the behavior of anticancer drug leflunomide adsorbed on the external surface of zigzag single walled (6,0) carbon and boron nitride nanotubes (SWCNT and SWBNNT) was studied by means of DFT calculations at the B3LYP/6-31G(*) level of theory. The larger adsorption energies and charges transfer showed that the adsorption of leflunomide onto SWBNNT is more stable than that the adsorption of leflunomide onto SWCNT. Frontier molecular orbitals (HOMO and LUMO) suggest that adsorption of leflunomide onto SWBNNT behave as charge transfer compounds with leflunomide as an electron donor and SWBNNT as an electron acceptor. Thus, nanotubes (NTs) have been proposed and actively explored as multipurpose innovative carriers for drug delivery and diagnostic application. The theory has been also applied to analyze the properties of the bond critical points: their electron densities and their laplacians."

According to the news reporters, the research concluded: "Also, the natural bond orbital (NBO) calculations were performed to derive natural atomic orbital occupancies, and partial charges of the interacting atoms in the equilibrium tube-molecule distance."

For more information on this research see: Immunosuppressive agent leflunomide: A SWNTs-immobilized dihydroortate dehydrogenase inhibitory effect and computational study of its adsorption properties on zigzag single walled (6,0) carbon and boron nitride nanotubes as controlled drug delivery d. European Journal of Pharmaceutical Sciences, 2014;56():37-54. European Journal of Pharmaceutical Sciences can be contacted at: Elsevier Science Bv, PO Box 211, 1000 Ae Amsterdam, Netherlands. (Elsevier - www.elsevier.com; European Journal of Pharmaceutical Sciences - www.elsevier.com/wps/product/cws_home/523997)

Our news correspondents report that additional information may be obtained by contacting H. Raissi, Univ Birjand, Dept. of Chem, Birjand, Iran (see also Drugs and Therapies).

Keywords for this news article include: Iran, Asia, Antirheumatics, Pharmaceuticals, Birjand, Chemicals, Chemistry, Leflunomide, Boron Nitride, Dehydrogenase, Drugs and Therapies, Enzymes and Coenzymes

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Source: Biotech Week