ABSTRACT
BACKGROUND: Acacia farnesiana (AF) pods have been traditionally used to treat dyspepsia, diarrhea and topically for dermal inflammation. Main objectives: (1) investigate the antioxidant activity and protection against oxidative-induced damage of six extracts from AF pods and (2) their capacity to curb the inflammation process as well as to down-regulate the pro-inflammatory mediators. METHODS: Five organic extracts (chloroformic, hexanic, ketonic, methanolic, methanolic:aqueous and one aqueous extract) were obtained and analyzed by UPLC-ESI-Q-oa/TOF-MS. Antioxidant activity (DPPHâ¢, ORAC and FRAP assays) and lipid peroxidation (TBARS assay) were performed. Assessment of anti-inflammatory properties was made by the ear edema induced model in CD-1 mice and MPO activity assay. Likewise, histological analysis, IL-1ß, IL-6, IL-10, TNF-α, COX measurements plus nitrite and immunohistochemistry analysis were carried out. RESULTS: Methyl gallate, gallic acid, galloyl glucose isomer 1, galloyl glucose isomer 2, galloyl glucose isomer 3, digalloyl glucose isomer 1, digalloyl glucose isomer 2, digalloyl glucose isomer 3, digalloyl glucose isomer 4, hydroxytyrosol acetate, quinic acid, and caffeoylmalic acid were identified. Both organic and aqueous extracts displayed antioxidant activity. All extracts exhibited a positive effect on the interleukins, COX and immunohistochemistry assays. CONCLUSION: All AF pod extracts can be effective as antioxidant and topical anti-inflammatory agents.
Subject(s)
Acacia/chemistry , Phenols/chemistry , Phenols/isolation & purification , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacology , Cell Survival/drug effects , Chromatography, High Pressure Liquid , Disease Models, Animal , Dose-Response Relationship, Drug , Edema/drug therapy , Edema/pathology , Lipid Peroxidation , Male , Mice , Nitrites/metabolism , Phenols/pharmacology , Plant Extracts/pharmacology , Polyphenols/chemistry , Polyphenols/isolation & purification , Polyphenols/pharmacology , Prostaglandin-Endoperoxide Synthases/metabolism , Rats , Spectrometry, Mass, Electrospray Ionization , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization , Tumor Necrosis Factor-alpha/genetics , Tumor Necrosis Factor-alpha/metabolismABSTRACT
Aliphatic and aromatic ferrocenylthiosemicarbazones were synthesized. The characterization of the new ferrocenylthiosemicarbazones was done by IR, (1)H-NMR and (13)C-NMR spectroscopy, elemental analysis and X-ray diffraction studies. The biological activity of the obtained compounds was assessed in terms of anticancer activity. Their activity against U251 (human glyoblastoma), PC-3 (human prostatic adenocarcinoma), K562 (human chronic myelogenous leukemia), HCT-15 (human colorectal adenocarcinoma), MCF-7 (human mammary adenocarcinoma) and SKLU-1 (human lung adenocarcinoma) cell lines was studied and compared with cisplatin. All tested compounds showed good activity and the aryl-chloro substituted ferrocenylthiosemicarbazones showed the best anticancer activity.
Subject(s)
Antineoplastic Agents/pharmacology , Coordination Complexes/pharmacology , Ferrous Compounds/pharmacology , Thiosemicarbazones/pharmacology , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Cisplatin/pharmacology , Coordination Complexes/chemical synthesis , Crystallography, X-Ray , Drug Screening Assays, Antitumor , Ferrous Compounds/chemical synthesis , Humans , Magnetic Resonance Spectroscopy , Metallocenes , Structure-Activity Relationship , Thiosemicarbazones/chemical synthesisABSTRACT
A series of 5-aryl-1,4-benzodiazepines with chloro- or fluoro-substituents in the second ring have been synthesized and their anti-inflammatory, myeloperoxidase and anticancer properties studied. The synthesized compounds showed potential anti-inflammatory and anticancer activities, which were enhanced in the presence of a chloro-substituent in the second ring of the 5-aryl-1,4- benzodiazepine.
