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Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 8
May 14-15, 2018 | Montreal, Canada
Global Summit on
Biopharma & Biotherapeutics
C
urcumin has shown pharmacological properties against
different phenotypes of various disease models. Different
synthetic routes have been employed to develop its
numerous derivatives for diverse and improved therapeutic
roles. In present study, we have synthesized curcumin
derivatives containing isoxazole, pyrazoles and pyrimidines
then the synthesized molecules were evaluated for their anti-
inflammatory and antinociceptive activities in experimental
animal models. Acute toxicity of synthesized molecules
was evaluated in albino mice by oral administration. Any
behavioral and neurological changes were observed at dose
of 10mg/kg body weight. Additionally, cyclooxygenase-2
(COX-2) enzyme inhibition studies were performed through
in vitro
assays.
In vivo
anti-inflammatory studies showed
that curcumin with pyrimidines were most potent anti-
inflammatory agents which inhibited induced edema from
74.7-75.9%. Compound 7, 9 and 12 exhibited relatively
higher prevention of writhing episodes than any other
compound with antinociceptive activity of 73.2, 74.9 and
71.8% respectively. This was better than diclofenac sodium
(reference drug, 67.1% inhibition). Similarly, COX-2
in vitro
inhibition assays results revealed that compound 12 (75.3%
inhibition) was the most potent compound. Molecular
docking studies of 10, 11 and 12 compounds in human COX-
2 binding site revealed the similar binding mode as that of
other COX-2 selective inhibitors.
e:
mahmoodresearchscholar@gmail.comCurcumin derivatives: Anti-inflammatory, analgesic, ulcerogenic, cyclooxygenase-2 inhibition and
molecular docking studies
Mahmood Ahmed
University of the Punjab, Pakistan