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Screening Acerola ( Malpighia emarginata ) Genotypes for Protection against LPS‐Induced Inflammation in Macrophage Cells and Selectivity to Cyclooxygenase‐2 (COX‐2) Activity
Author(s) -
Bhargava Prerna,
Nair Vimal,
Bang Woo Young,
Schreckinger Maria Elisa,
Alves Ricardo Elesbao,
CisnerosZevallos Luis
Publication year - 2016
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.30.1_supplement.1174.24
Subject(s) - chemistry , polyphenol , terpenoid , antioxidant , cyclooxygenase , anti inflammatory , pharmacology , inflammation , biochemistry , nitric oxide , aspirin , mode of action , enzyme , biology , organic chemistry , immunology
Acerola has been extensively studied for its antioxidant, antimicrobial, anti‐inflammatory, anticancer, antigenotoxic and antihyperglycemic properties. The aim of this investigation has been to study the putative anti‐inflammatory mechanism of various genotypes of acerola (fruit and leaves) fractions and project acerola as natural substitute for aspirin and ibuprofen. Conventionally, NSAID has been known to have preventive action against acute and chronic inflammation by inhibiting cyclooxygenases. Previous studies have illustrated that phytochemicals like alkaloids, terpenoids, flavonoids, curcumin and phenolics have COX inhibitory action. However, there is a necessity to seek for a naturally occurring selective inhibitor of COX‐2, that can modulate inflammation and could overcome the limitations of drugs like aspirin. 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 inhibits blood platelet aggregation. For characterization of phytochemicals that are responsible for scavenging and anti‐inflammatory effect of acerola a comparative study using TLC and LC‐MS was employed. Phytochemicals of acerola were extracted using two different solvents ‐ methanol and methanolic/ acetone/ water. Each solvent extracted different category of compounds. One of the two fractions included polyphenols and other one was polyphenols/terpenoids. The two fractions were explored to elucidate mode of action for different acerola genotypes in an in‐vitro system of macrophages. Results indicated with p‐ value < 0.05, which means that the methanolic fractions of acerola 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, with p‐ value < 0.05, BRS‐238, a ripe fruit genotype of acerola, displayed a selective action against COX‐2. This confirms that acerola's anti‐inflammatory action is through selective inhibition of COX‐2.