INDONESIAN JOURNAL OF PHARMACY
Vol 17 No 2, 2006

Activity of propyl p-benzoyloxybenzoate as mu-class glutathione s-transferase inhibitor

Agnes Nora Iska Harnita (Pharmaceutical Chemistry Lab., Faculty of Pharmacy Sanata Dharma University Yogyakarta)
Enade Perdana Istyastono (Pharmaceutical Chemistry Lab., Faculty of Pharmacy Sanata Dharma University Yogyakarta)
Sudibyo Martono (Department of Pharmaceutical Chemistry, Faculty of Pharmacy Universias Gadjah Mada Yogyakarta)



Article Info

Publish Date
01 Apr 2006

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed medicines. Anti-inflammatory activity was reported to have relationship with the inhibition of prostaglandin synthesis, one of the inflammation mediators. The inhibition mechanism might be through the cyclooxygenase (COX) inhibition, oxygen radical scavenging, and mu-class glutathione S-transferase (GST) inhibition. Aspirin has been used as a NSAID since a hundred years ago and was reported as cyclooxigenase-1 (COX-1) selective inhibitor. The selectivity leds to gastrointestinal ulceration. Propyl p-benzoyloxybenzoate was a new compound which was predicted to have anti-inflammatory activity and would be developed to be an NSAID with minimum side effect.mu-class GST inhibition was examined using formation reaction model of GS-CNB conjugate through conjugation of 1,2-dichloro-4-nitrobenzene (DCNB) and glutathione (GSH) with GST (prepared from rat’s liver) as a catalyst. GSTs were isolated from the rat liver cytosolic fraction by centrifugation according to Lundgren. Protein concentration of the cytosol was determined spectrophotometrically by using bovine serum albumin as a standard. The GST activity was determined using conjugation reaction rate between DCNB and GSH, followed by determination of IC50 of propyl p-benzoyloxybenzoate. The result showed that propyl p-benzoyloxybenzoate has activity as  mu-class GST inhibitor with IC50 = 111.77 μM as the result from extrapolation.Key words: Anti-inflammatory, propyl p-benzoyloxybenzoate, inhibitor, mu-class glutathione S-transferase (GST).

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Journal Info

Abbrev

3

Publisher

Subject

Medicine & Pharmacology

Description

Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas ...