Triterpenes possess anti-inflammatory and anti-nociceptive effects. In this study anti-inflammatory activities of
Asparacosin A were evaluated' using in-vitro
cyclooxygenases 1 and 2 (COX-1/2) inhibition assays. Moreover, anti-nociceptive activities were assessed in-vivo by
carrageenan-induced paw
edema test,
xylene-induced ear
edema tests, and
acetic acid-induced writhing and
formalin tests. Additionally molecular docking was conducted to elucidate the binding mechanism of the compound and to correlate the in-vitro findings with the in-silico data.
Oral administration of
Asparacosin A at the doses of 10, 20, and 40 mg/kg induced significant anti-inflammatory effects (*p < 0.05, **p < 0.01, and ***p < 0.001) in a dose-dependent manner in both models.
Asparacosin A also inhibited the human recombinant COX-2
enzyme and caused a dose-dependent decrease in the levels of TNF-α, IL-1β, and
PGE2 in the
carrageenan-induced paws. Moreover,
Asparacosin A displayed significant anti-nociceptive effects (*p < 0.05, **p < 0.01, ***p < 0.001) at the doses of 10, 20, and 40 mg/kg in
acetic-acid induced writhing test. However, in
formalin test,
Asparacosin A (10-40 mg/kg, p.o) produced anti-nociceptive effects only in the late phase, similar to the effect observed with the reference drug
celecoxib (50 mg/kg, p.o). Molecular docking was carried out on both COX-1 and COX-2 structures which revealed that
Asparacosin A targets allosteric binding site similar to the binding mode of the selective COX inhibitor. In conclusion,
Asparacosin A exhibits anti-inflammatory and peripheral anti-nociceptive activities which are likely mediated via inhibition of COX-2
enzyme and inflammatory
cytokines. Furthermore,
Asparacosin A can serve as a model to obtain new and more selective potent anti-inflammatory and anti-nociceptive drugs.