Microbial Transformation of Memantine by Penicillum sp.

ROXANA ACIAR, LISANDRO HERGERT, NOELIA SANTANDREU, PAMELA BUSTOS, GABRIELA ORTEGA, GABRIELA PARAJE, DANIEL BUSTOS, SOLEDAD RAVETTI

Cartagena de Indias

Congreso; Congreso de la Federación Farmacéutica Sudamericana. VIII Congreso de Ciencias Farmacéuticas. XII Simposio Colombiano de Ciencia y Tecnología Cosmética.; 2012

Federación Farmacéutica Sudamericana

Microbial Transformation of Memantine by Penicillum sp. Area: Biotechnology 1. Instituto de Cs. Básicas, FFHA, Universidad Nacional de San Juan, San Juan, Argentina. 2. Facultad de Ciencias de la Alimentación, Bioquímicas y Farmacias, Universidad Católica de Cuyo, San Juan, Argentina. 3. Instituto Académico Pedagógico de Ciencias Básicas y Aplicadas, Universidad Nacional de Villa María, Córdoba, Argentina. 4. Departamento de Farmacia, IMBIV-CONICET, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina. In the chemical and pharmaceutical industry, the innovation and productivity in drug development is one of the most important processes, taking place by chemical synthesis, semi-synthesis or by friendly biotechnological techniques known as biotransformation or bioconversion.1 Biotransformation is defined as anyone biotransformation process in which catalyst is used as a microorganism or an isolated enzyme for conversion of a substrate to another product. In recent years, this method has allowed, in aqueous and biphasic, transform and derivatized through simple processes, selective, low cost and without damaging the environment, a variety of biologically active compounds.1,2 In this work we developed different microbial biotransformation reactions using the fungus Penicillium sp, with the aim of obtaining new derivatives of memantine showing better pharmacological and biopharmaceutical properties. Memantine (1-amino-3,5-dimethyladamantane) is a tricyclic amine structurally that is used to treat Parkinson?s disease, movement disorders and dementia syndrome. We performed a preliminary mapping of the biotransformation of memantine by action of the enzymes produced by the fungus Penicillium sp. Then the biotransformation was taken to a preparative scale, based on the criteria of purity and quantity of compounds detected by thin layer chromatographic (CCD) and gas chromatography (GC), the structural elucidation of the new derivative was performed by nuclear magnetic resonance spectroscopy. We also determined the antioxidant activity by different techniques obtained very promising results.3,4 1- Leuenberger, H.G.W. Biotransformation-A useful tool in organic chemistry. Pure & Appl. Chem. 1990; 753-768. 2- Xie ZY, Huang HH, Zhong D. Biotransformation of pantoprazole by the fungus Cunninghamella blakesleeana. Xenobiotica. 2005; 35(5): 467-477. 3- Potterat O. Antioxidants and free radical scavengers of natural origin. Curr Org Chem. 1997; 1: 415 ? 440. 4- Molyneux P. The use of the stable free radical diphenylpicrylhydrazyl (DPPH) for estimating antioxidant activity. Songklanakarin J Sci Technol. 2004; 26: 211 ? 219.