Structure modification of mefenamic acid and evaluate their bioactivities
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Date
2015
Journal Title
Journal ISSN
Volume Title
Publisher
Uva Wellassa University of Sri Lanka
Abstract
Thousands of years medicine and natural products have been closely linked through the use of
traditional medicines and natural poisons (Phillipson et al., 2001). Lately, pharmaceutical industries
mainly pay their attention on natural products and their bioactivities to develop novel drugs which
shows promising activities on diseases in humans as well as in plants. Since biological assays are used
to detect the biological activity on synthetic compounds and natural products. There are several kinds
of bioassays such as, antioxidant, antifungal, phytotoxicity, cytotoxicity and enzyme inhibitory
activities (e.g. lipase, α-amylase, α-Glucosidase etc). Though there are several types of bioassays,
most pharmaceutical manufacturing industries limited their research activities only towards one or
few types of bioassays. There can be hidden bioactivities which are important in medicinally,
agriculturally and environmentally. Therefore it is important to study about the other bioactivities too
by doing the structure modifications of existing drugs and evaluate their bioactivities using various
types of bioassays. By doing the modification of the exiting drug that can be enhanced the efficiency
of the drug usage.
Mefenamic acid (MFA) which is used as a pain killer from many years ago. It is a Non-Steroidal Anti-
Inflammatory Drug (NSAID) which exhibits poor water solubility properties (Dixit et al., 2012). MFA
is a prescription medicine used for the relief of mild to moderate pain, including painful menstrual
periods (Asl et al., 2008). There can be some hidden important bioactivities which were not studied
yet in addition as a pain-killer. The aim of this study was to improve the usages of the drug for
industrially, agriculturally and environmentally. Therefore the drug was synthetically modified by
acetylation/acylation reaction methods.
Methodology
Pure MFA was separated from the tablet by using column chromatography technique. Separated pure
MFA was subjected to acetylation and acylation reactions according to Arnold et al., 2007. Acylation
was carried out with acid chlorides such as acetyl chloride (AC), benzoyl chloride (BC) and crotonoyl
chloride (CC), while acetylation with acetic anhydride. Efficiency of the drug and its synthetic
derivatives were tested by subjecting to bioassays such as α-amylase inhibition assay (Giancarlo et
al., 2006), antioxidant assay (DPPH radical scavenging assay) (Mensor et al., 2001), phytotoxicty
(bio-assay with lettuce seed germination) (Drewes et al., 1995) and cytotoxicity (brine shrimp
lethality assay) assay using Artemia salina (Subbaraju et al., 2005).
The Inhibition percentage was plotted against the sample concentration and the fitted line plot was
established. Then IC50value (Inhibitory Concentration) was calculated in order to the 50% inhibition.
Description
Keywords
Science and Technology, Technology, Bioactivities, Medicinal Plants