NDLI: Synthesis, characterization and in-vitro antitubercular activity of isoniazid-gelatin conjugate.

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Synthesis, characterization and in-vitro antitubercular activity of isoniazid-gelatin conjugate.

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Synthesis, characterization and in-vitro antitubercular activity of isoniazid-gelatin conjugate.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Cassano, Roberta Trombino, Sonia Ferrarelli, Teresa Cavalcanti, Paolina Giraldi, Cristina Lai, Francesco Loy, Giuseppe Picci, Nevio
Description	Country affiliation: Italy Author Affiliation: Cassano R ( Department of Pharmaceutical Sciences, University of Calabria, Cosenza, Italy.)
Abstract	OBJECTIVES: A novel and simple method to synthesize antitubercular-protein conjugate by solid phase synthesis was developed employing a carboxypolystyrene resin. The aim was to covalently bind a drug with antitubercular activity, isoniazid, to a biomacromolecule, gelatin, widely used in the pharmaceutical, cosmetic and food industry. METHODS: Calorimetric and (1) H NMR analyses were performed to verify the bond formation between the antitubercular drug and gelatin. After absorption isoniazid delivers toxic metabolites and so an oxidation test with tert-butyl hydroperoxide was performed to assess the amount of toxic metabolites released from the prodrug (gelatin linked to isoniazid), compared with isoniazid itself. KEY FINDINGS: Spectrophotometric analysis revealed that the protein derivative was an excellent isoniazid prodrug since there was a 40% reduction in release of toxic metabolites (isonicotinic acid) by the prodrug. The results clearly showed that antitubercular moieties, covalently linked to a natural polymer, allowed the introduction of peculiar features for specific pharmaceutical applications into the macromolecule. In addition, antitubercular activity of the new polymer was determined by Middlebrook 7H11 medium against Mycobacterium tuberculosis complex. CONCLUSIONS: The new isoniazid-gelatin conjugate showed significant antitubercular activity and for this reason should be useful as an efficacious tool in the treatment of tuberculosis.
File Format	HTM / HTML
ISSN	00223573
Issue Number	5
Volume Number	64
e-ISSN	20427158
Journal	Journal of Pharmacy and Pharmacology
Language	English
Publisher	Wiley
Publisher Date	2012-05-01
Publisher Place	Great Britain (UK)
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology Antitubercular Agents Pharmacology Isoniazid Mycobacterium Tuberculosis Drug Effects Prodrugs Administration & Dosage Chemistry, Pharmaceutical Gelatin Chemical Synthesis Solid-phase Synthesis Techniques Methods Evaluation Studies Journal Article Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Pharmacology Pharmaceutical Science

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