OBJECTIVESThis study aimed to evaluate the in vitro antioxidant capacity, to determine the anti-inflammatory effect due to lipoxygenase inhibition and to test the antimicrobial activity of ethanolic extracts from leaves of seven climbing species belonging to the Bignoniaceae family. These species are Adenocalymma marginatum (Cham.) DC., Amphilophium vauthieri DC., Cuspidaria convoluta (Vell.) A. H. Gentry, Dolichandra dentata (K. Schum.) L. G. Lohmann, Fridericia caudigera (S. Moore) L. G. Lohmann, Fridericia chica (Bonpl.) L. G. Lohmann and Tanaecium selloi (Spreng.) L. G. Lohmann.

METHODSThe antioxidant activity was evaluated using three methods, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power. Lipoxygenase-inhibiting activity was assayed spectrophotometrically; the result was expressed as percent inhibition. The antimicrobial activity was assessed using the agar disk diffusion method. Minimal inhibitory concentration (MIC) and minimal bactericidal/fungicidal concentration were also determined for each extract against 12 pathogenic bacterial strains of Staphylococcus aureus and seven fungal strains of the Candida genus. The identification of the major compounds present in the most promising extract was established by high-performance liquid chromatography-tandem mass spectrometry.

RESULTSC. convoluta, F. caudigera, and F. chica exhibited the best antioxidant activity by scavenging DPPH and ABTS radicals and reducing Fe ion. These extracts showed a notable inhibition of lipoxygenase. F. caudigera was found to have the lower MIC value against S. aureus strains and six Candida species. The extracts of F. caudigera and C. convoluta were active even against methicillin-resistant S. aureus. C. convoluta had higher total phenol content, better antioxidant activity and superior anti-inflammatory and antimicrobial activity. The main phenolic compounds found in this extract were coumaric and hydroxybenzoic acid derivatives and glycosylated and nonglycosylated flavones.

CONCLUSIONMost of the extracts exhibited antioxidant activity as well as in vitro inhibition of lipoxygenase. The excellent antimicrobial activity of T. selloi and F. chica supports their use in traditional medicine as antiseptic agents. The extracts of F. caudigera and C. convoluta, both with notable biological activities in this study, could be used as herbal remedies for skin care. In addition, this study provides, for the first time, information about phenolic compounds present in C. convoluta.

Anti-Infective Agents ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Bignoniaceae ; chemistry ; Candida ; drug effects ; growth & development ; Humans ; Lipoxygenase ; chemistry ; Lipoxygenase Inhibitors ; chemistry ; pharmacology ; Medicine, Traditional ; Microbial Sensitivity Tests ; Plant Extracts ; chemistry ; pharmacology ; Staphylococcus aureus ; drug effects ; growth & development

BACKGROUND/AIMS: The unique role of enzyme 5-lipoxygenase (5-LO) in the production of leukotrienes makes it a therapeutic target for inflammatory bowel disease (IBD). The aim of this study was to evaluate the effects of B-98, a newly synthesized benzoxazole derivatives and a novel 5-LO inhibitor, in a mouse model of IBD induced by dextran sulfate sodium (DSS). METHODS: C57BL/6 mice were randomly assigned to four groups: normal control, DSS colitis (DSS+saline), low dose B-98 (DSS+B-98 20 mg/kg) and high dose B-98 (DSS+B-98 100 mg/kg). B-98 was administered with 3% DSS intraperitoneally. The severity of the colitis was assessed via the disease activity index (DAI), colon length, and histopathologic grading. The production of inflammatory cytokines interleukin (IL)-6 was determined by RT-PCR. Th cells were examined for the proportion of Th1 cell, Th2 cell, Th9 cell, Th17 cell and Treg cell using intracellular cytometry. RESULTS: The B-98 group showed lower DAI, less shortening of the colon length and lower histopathologic grading compared with the DSS colitis group (p<0.01). The expression of IL-6 in colonic tissue was significantly lower in the B-98 groups than the DSS colitis group (p<0.05). The cellular profiles revealed that the Th1, Th9 and Th17 cells were increased in the DSS colitis group compared to the B-98 group (p<0.05). CONCLUSIONS: Our results suggest that acute intestinal inflammation is reduced in the group treated with B-98 by Th1, Th9 and Th17 involved cellular immunity.
Acute Disease ; Animals ; Arachidonate 5-Lipoxygenase/chemistry/metabolism ; Benzoxazoles/chemistry/*pharmacology ; Colitis/chemically induced/pathology/*prevention & control ; Colon/drug effects/pathology/physiology ; Dextran Sulfate/toxicity ; Disease Models, Animal ; Forkhead Transcription Factors/metabolism ; Injections, Intraperitoneal ; Interleukin-6/genetics/metabolism ; Lipoxygenase Inhibitors/chemistry/*pharmacology ; Male ; Mice ; Mice, Inbred C57BL ; Severity of Illness Index ; T-Lymphocytes/classification/*drug effects/metabolism

Tepoxalin is a potent inhibitor of both the cyclooxygenase and lipoxygenase pathways of the arachidonic acid cascade, as well as a potent anti-inflammatory and control-pain (postoperation, arthritis et. al.) agent. The new method about the use of novel synthesis reagents and the first using ionic liquid as reactive solvent to synthesize tepoxalin were presented in this paper. The ionic liquid can be easily recycled and reused for several runs efficiently. The analgesic activity of tepoxalin was detected by acetic acid test on mice. The analysis of variance showed that oral administration of tepoxalin could significantly inhibit the number of writhing response within 1 hour and prolong the latent time in a dose dependent manner as compared with CMC control group (P < 0.05). At the same time, tepoxalin had the same analgesic activity as diclofenac sodium.
Administration, Oral ; Analgesics ; administration & dosage ; chemical synthesis ; pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; chemical synthesis ; pharmacology ; Cyclooxygenase Inhibitors ; administration & dosage ; chemical synthesis ; pharmacology ; Diclofenac ; pharmacology ; Imidazoles ; chemistry ; Ionic Liquids ; chemistry ; Lipoxygenase Inhibitors ; administration & dosage ; chemical synthesis ; pharmacology ; Mice ; Pain Measurement ; drug effects ; Pyrazoles ; administration & dosage ; chemical synthesis ; pharmacology ; Random Allocation