Anti-inflammatory, free radical scavenging and alpha-glucosidase inhibitory activities of Hamelia patens and its chemical constituents
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ContextHamelia patens Jacq. (Rubiaceae) is traditionally used to treat wounds, inflammation and diabetes. However, there is still a lack of scientific evidence to support these applications. Objective The objective of this study is to evaluate the anti-inflammatory, antioxidant and antidiabetic activities of Hamelia patens, and identify its bioactive compounds. Materials and methods Four extracts were obtained by maceration and liquid–liquid extraction: HEX, DCM–EtOAc, MeOH–EtOAc and MeOH–Aq. The anti-inflammatory effect was evaluated orally on rat paw carrageenan-induced oedema over 6 h (50, 200 and 500 mg/kg), and topically in mouse ear oedema induced by 12-tetradecanoylphorbol-13-acetate (TPA) after 4 h (0.5 and 1 mg/ear). We also evaluated myeloperoxidase levels in ear tissue, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability, and in vitro α-glucosidase inhibition. The chemical compounds were separated by column chromatography and identified by spectroscopic analysis. Results We found that the oral administration of the HEX extract at 500 and 200 mg/kg significantly decreased the carrageenan-induced inflammation after 1 and 3 h, respectively. The MeOH–EtOAc extract significantly inhibited myeloperoxidase activity (83.5%25), followed by the DCM–EtOAc extract (76%25), β-sitosterol/stigmasterol (72.7%25) and the HEX extract (55%25), which significantly decreased oedema induced by TPA at both doses, giving a similar effect to indomethacin. We also found that the MeOH–EtOAc, MeOH–Aq and DCM–EtOAc extracts showed good DPPH scavenging activity (IC50 values of 18.6, 93.9 and 158.2 μg/mL, respectively). The HEX extract showed the lowest α-glucosidase inhibition (an IC50 value of 26.07 μg/mL), followed by the MeOH–EtOAc extract (an IC50 value of 30.18 μg/mL), β-sitosterol/stigmasterol (IC50 34.6 μg/mL) and compound A ((6E,10E,14E,18E)-2,6,10,14,18,23-hexamethyl-2,6,10,14,18,22-tetracosahexaene, an IC50 value of 114.6 μg/mL), which were isolated for the first time from Hamelia patens. Discussion and conclusionHamelia patens possesses anti-inflammatory, antioxidant and α-glucosidase inhibitory activities, which support its traditional use. These effects can be attributed to the identified compounds. © 2015 Informa UK Limited, trading as Taylor %26 Francis Group.
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12-tetradecanoylphorbol-13-acetate; Antidiabetic; antioxidant; carrageenan; myeloperoxidase; squalene isomer; stigmasterol; β-sitosterol 1,1 diphenyl 2 picrylhydrazyl; 2,6,10,14,18,23 hexamethyl 2,6,10,14,18,22 tetracosahexaene; acetic acid ethyl ester; alpha glucosidase; dichloromethane; Hamelia patens extract; hexane; indometacin; methanol; myeloperoxidase; phorbol 13 acetate 12 myristate; plant extract; plant medicinal product; sitosterol; stigmasterol; unclassified drug; 1,1-diphenyl-2-picrylhydrazyl; alpha glucosidase; antiinflammatory agent; biphenyl derivative; carrageenan; glycosidase inhibitor; peroxidase; picric acid; Saccharomyces cerevisiae protein; scavenger; solvent; animal experiment; animal model; animal tissue; antidiabetic activity; antiinflammatory activity; antioxidant activity; Article; carrageenan-induced paw edema; chemical composition; column chromatography; controlled study; drug identification; drug isolation; drug structure; ear edema; enzyme inhibition; female; Hamelia; Hamelia patens; IC50; in vitro study; liquid liquid extraction; mouse; nonhuman; rat; spectroscopy; structure analysis; animal; antagonists and inhibitors; chemically induced; chemistry; comparative study; disease model; dose response; edema; isolation and purification; medicinal plant; metabolism; phytotherapy; plant leaf; time factor; Wistar rat; alpha-Glucosidases; Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Carrageenan; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Female; Free Radical Scavengers; Glycoside Hydrolase Inhibitors; Hamelia; Peroxidase; Phytotherapy; Picrates; Plant Leaves; Plants, Medicinal; Rats, Wistar; Saccharomyces cerevisiae Proteins; Solvents; Tetradecanoylphorbol Acetate; Time Factors
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