Antiinflammatory and antinociceptive activities of gossypin and procumbentin – cyclooxygenase‐2 (COX‐2) inhibition studies

Abstract

In the present study the antiinflammatory and antinociceptive activities of a few selected flavonoids were investigated. Procumbentin, gossypin, chrysin and methylhespiridin were studied for antiinflammatory and antinociceptive activities using in vitro enzymatic assays and in animal models utilizing acetic acid-induced writhing in mice and hind paw edema in rats. In vitro studies were performed using TMPD (NNN'N'-tetramethyl-p-phenylene diamine) and oxygraphic methods for COX-1 (cyclooxygenase-1), COX-2, 5-LOX (5-lipoxygenase) and 15-LOX. Gossypin and procumbentin showed COX-2 inhibitory activity and exhibited IC(50) (COX-2/COX-1) ratios of 0.14 and 0.11, respectively. None of the flavonoids tested in this study showed LOX inhibitory activity. Four groups were studied for each test compound following intraperitoneal (i.p.) administration of doses of 10, 30 and 100 mg/kg. Antiinflammatory activity was measured by the carrageenin-induced rat hind paw edema model and antinociceptive activity by acetic acid-induced writhing. Procumbentin and gossypin showed antinociceptive activity at the 100 mg/kg dose. Gossypin showed antiinflammatory activity at doses of 10, 30, 100 mg/kg. Procumbentin and gossypin exhibited COX-2 inhibitory activity when tested by in vitro methods. Procumbentin and gossypin showed antinociceptive, and gossypin showed antiinflammatory, activities.

Natural Flavonoids as Promising Analgesic Candidates: A Systematic Review

“…Perception and transmission of pain are complex processes that involve peripheral and central mechanisms. Different mediators, such as 5‐hydroxytryptamine (5‐HT), nitric oxide, prostaglandin, superoxide anion, and cyclooxygenase are involved in pathogenesis of pain . Effective multifaceted pain treatment relies on effective drugs to ensure minimal adverse effects and optimized rehabilitation.…”

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“…Some compounds such as flavonoids which are well known to display anti-inflammatory and antinociceptive activities 19,20 are common to both studies.…”

Gossypin: A phytochemical of multispectrum potential

“…Further in vitro studies also revealed that both procumbentin and gossypin have COX-2 inhibitory activity [26]. In another study, oral administration of flavonoids including gossypin inhibited paw oedema in carrageenin induced oedema in mice [27].…”