Anti-Inflammatory Properties of Acerola (Malpighia emarginata) Leaf and Ripe Fruit Genotypes for Protection Against LPS-Induced Inflammation in Macrophage Cells and Their Selectivity to Cyclooxygenase-2 (COX-2) Activity
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Date
2015-04-30
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Abstract
Conventionally, NSAID has been proposed to have inhibitory action against COX and therefore has traditionally been used for treatment of acute and chronic inflammation. This study aims at exploring putative anti-inflammation mechanism of acerola. Previous studies have illustrated that phytochemicals like alkaloids, terpenoids, flavonoids, curcumin and phenolics have COX inhibitory activities as well. However, a natural occurring selective inhibitor of COX-2 that can modulate inflammation and can overcome the limitations of drugs like aspirin is still a priority. Aspirin is known to form an irreversible and non-competitive binding to COX which proves to be a potent cardiovascular protective agent. On the other hand, irreversible binding has implications by initiating inhibition of blood platelet aggregation.
Acerola has been earlier studied for its antioxidant, antimicrobial, anti-inflammatory, anticancer, antigenotoxic and antihyperglycemic properties. In the present study, anti-inflammatory properties of acerola have been established where different genotypes of acerola fruit and leaf fractions were studied for their biological properties. A comparative study using TLC, LC-MS and bioassays using macrophages is employed to identify which groups of phytochemicals are responsible for scavenging and inflammation inhibitory effect of acerola. Initially, phytochemicals were extracted using methanolic and methanolic/acetone/water solvents which isolated different groups of compounds in two fractions, including polyphenols and a mixture of polyphenols/terpenoids, respectively. The two fractions were explored to elucidate mode of action for different acerola genotypes. Results indicated that the methanolic fractions of acerola showed higher activity exhibited suppression of ROS and partial decrease of nitric oxide levels in LPS-stimulated RAW264.7 macrophage cell line. This fraction also demonstrated inhibition of enzyme expression of COX-1/2. Moreover, BRS-238, a ripe fruit genotypes of acerola had a selective action against COX-2 - confirming the hypothesis that acerola’s mode of anti-inflammatory action is through selective inhibition of COX-2.
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COX- Cyclooxygenase, NSAID: Non- Steroidal Anti-Inflammatory Drug, NO- nitric oxide, ROS-Reactive Oxygen Species