Abstract
Pain is one of the most common cause for hospital visits. It plays an important role in inflammation and serves as a warning sign to avoid further injury. Analgesics are used to manage pain and provide comfort to patients. However, prolonged usage of pain treatments like opioids and NSAIDs are accompanied with undesirable side effects. Therefore, research to identify novel compounds that produce analgesia with lesser side effects are necessary. The present study investigated the antinociceptive potentials of a natural compound, cardamonin, isolated from Boesenbergia rotunda (L) Mansf. using chemical and thermal models of nociception. Our findings showed that intraperitoneal and oral administration of cardamonin (0.3, 1, 3, and 10 mg/kg) produced significant and dose-dependent inhibition of pain in abdominal writhing responses induced by acetic acid. The present study also demonstrated that cardamonin produced significant analgesia in formalin-, capsaicin-, and glutamate-induced paw licking tests. In the thermal-induced nociception model, cardamonin exhibited significant increase in response latency time of animals subjected to hot-plate thermal stimuli. The rota-rod assessment confirmed that the antinociceptive activities elicited by cardamonin was not related to muscle relaxant or sedative effects of the compound. In conclusion, the present findings showed that cardamonin exerted significant peripheral and central antinociception through chemical- and thermal-induced nociception in mice through the involvement of TRPV1, glutamate, and opioid receptors.
Highlights
Cardamonin or 20,40 -dihydroxy-60 -methoxychalcone (C16 H14 O4 ) is a naturally occurring chalcone.Cardamonin was firstly isolated from the seeds of Amomum subulatum [1] and later from other plant species, such as Boesenbergia pandurata, Alpinia rafflesiana, Alpinia katsumadai, Alpinia henryi, and Campomanesia adamantium
In line with the in vitro finding where cardamonin exerted inhibitory action of PGE2 secretion and down regulation of COX-2 gene expression, we suggest that the antinociceptive mechanism of cardamonin may be linked partly to the disruption of the LOX and/or COX in the peripheral tissues, leading to decrease in PGE2 synthesis, which interferes with the mechanism of signal transduction in primary afferent nociceptors
The present study strongly suggests that antinociceptive activity induced by cardamonin in the glutamate test, at least in part, could be due to its interaction with the glutamatergic system or its ability to inhibit NO production
Summary
Cardamonin or 20 ,40 -dihydroxy-60 -methoxychalcone (C16 H14 O4 ) is a naturally occurring chalcone.Cardamonin was firstly isolated from the seeds of Amomum subulatum [1] and later from other plant species, such as Boesenbergia pandurata, Alpinia rafflesiana, Alpinia katsumadai, Alpinia henryi, and Campomanesia adamantium. Cardamonin or 20 ,40 -dihydroxy-60 -methoxychalcone (C16 H14 O4 ) is a naturally occurring chalcone. Previous report showed that cardamonin exerted antiproliferative activity and induced apoptosis in PC-3 [2], myeloma [3], and A549 cell lines [4]. Cardamonin was capable to protect lipopolysaccharide (LPS)-induced septic mice against acute lung injury [5] and showed nephroprotective effect against cisplatin-induced renal injury [6]. Cardamonin could exert inhibition of platelet aggregation [7], vasorelaxant effect [8], improvement in Molecules 2018, 23, 2237; doi:10.3390/molecules23092237 www.mdpi.com/journal/molecules. In vitro study showed that cardamonin inhibits the release of pro-inflammatory mediators [13] Molecules 2018, 23, 2237 insulin resistance and vascular complication in a high fructose-fed rat model [9], suppression of lipid accumulation in vitro [10], inhibition of pigmentation in human normal melanocytes [11], and anti-pruritic activity [12].
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