Agnes Nora Iska Harnita
Pharmaceutical Chemistry Lab., Faculty of Pharmacy Sanata Dharma University Yogyakarta

Published : 2 Documents
Articles

Found 2 Documents
Search

Activity of propyl p-benzoyloxybenzoate as mu-class glutathione s-transferase inhibitor Harnita, Agnes Nora Iska; Istyastono, Enade Perdana; Martono, Sudibyo
INDONESIAN JOURNAL OF PHARMACY Vol 17 No 2, 2006
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (173.279 KB) | DOI: 10.14499/indonesianjpharm0iss0pp76-80

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).
ACTIVITY OF PROPYL p-BENZOYLOXYBENZOATE AS A GLUTATHIONE S-TRANSFERASE(S) INHIBITOR: THE COMPARISON BETWEEN COMPUTATIONAL CHEMISTRY APPROACH AND EMPIRICAL OBSERVATION Istyastono, Enade Perdana; Harnita, Agnes Nora Iska; Martono, Sudibyo
Indonesian Journal of Chemistry Vol 6, No 1 (2006)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (250.6 KB) | DOI: 10.22146/ijc.21781

Abstract

The activity of propyl p-benzoyloxybenzoate as a glutathione S-transferase(s) (GSTs) inhibitor has been examined through computational chemistry based theoretical approach and laboratory experiment. This research was related to the nature of GSTs as multifunctional enzymes, which play an important role in the detoxification of electrophilic compounds, the process of inflammation and the effectivities of anticancer compounds. Quantitative Structure-Activity Relationship (QSAR) study, which was established on curcumin and its derivatives using computational chemistry approach, was used to examine the theoretical activity of p-benzoyloxybenzoate as a GSTs inhibitor. Empirical observation on GSTs inhibition was examined using formation reaction model of GS-CNB conjugate through conjugation of 1-chloro-2,4-dinitrobenzene (CDNB) and glutathione (GSH) with GSTs (prepared from rats liver) as catalysts. The result showed that the difference between the activities of propyl p-benzoyloxybenzoate as a GSTs inhibitor obtained from the computational chemistry approach and the empirical observation were not statistically significant at 95% level of confidence.   Keywords: Propyl p-benzoyloxybenzoate, inhibitor,  glutathione S-transferase (GSTs), QSAR