ABSTRACT
Antimicrobial activity of dichloromethane and ethanol extracts and five compounds: pinostrobin (I), pinocembrin (II), tectochrysin (III), galangin 3-methyl ether (IV) and tiliroside (V) isolated from Lychnophora markgravii aerial parts against fifteen microorganisms was determined. The structures of these compounds were elucidated based on ESI-MS and NMR spectroscopic data. Both extracts showed antimicrobial activity against several tested microorganisms. Pinostrobin, tectochrysin and galangin 3-methyl ether showed the strongest antibacterial and antifungal effects.
Subject(s)
Anti-Bacterial Agents/isolation & purification , Antifungal Agents/isolation & purification , Asteraceae/chemistry , Plant Extracts/chemistry , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Flavanones/analysis , Flavanones/chemistry , Flavonoids/analysis , Flavonoids/chemistry , Microbial Sensitivity Tests , Molecular StructureABSTRACT
Two new sesquiterpene lactones 8alpha-(2',3'-dihydroxy-2'-methylbutanoyl)-15-desoxygoyazensolide and 16alpha-(1',2'-dihydroxy-1'-methylpropyl)-eremantholide have been identified as constituents of Eremanthus argenteus aerial parts. In addition, two known sesquiterpene lactones and three flavonoids were isolated. Their structures were established on the basis of spectroscopic and spectrometric data.
Subject(s)
Asteraceae/chemistry , Flavonoids/isolation & purification , Lactones/isolation & purification , Plant Components, Aerial/chemistry , Plant Extracts/isolation & purification , Sesquiterpenes/isolation & purification , Brazil , Chemical Fractionation , Chromatography , Flavonoids/chemistry , Lactones/chemistry , Molecular Structure , Plant Extracts/chemistry , Sesquiterpenes/chemistryABSTRACT
The bioactivity of the flavonoids pinostrobin (1), pinocembrin (2), tectochrysin (3), galangin 3-methyl ether (4), and tiliroside (5) isolated from Lychnophora markgravii aerial parts was investigated in vitro against amastigote stages of Leishmania amazonensis. The compounds were isolated by several chromatographic techniques and their chemical structures were established by ESI-MS and NMR spectroscopic data. The flavonoids 1 and 3 were the most active compounds; they markedly reduced the viability of Leishmania amastigotes.
Subject(s)
Antiprotozoal Agents/pharmacology , Asteraceae/chemistry , Flavonoids/pharmacology , Leishmania/drug effects , Amphotericin B/pharmacology , Animals , Antiprotozoal Agents/chemistry , Flavanones/chemistry , Flavonoids/chemistry , Flavonoids/isolation & purification , Models, MolecularABSTRACT
Two Brazilian species of Dimerostemma (Asteraceae) were chemically investigated. Two known sesquiterpene lactones (STLs), a germacrolide and an eudesmanolide, were isolated from D. episcopale while D. brasilianum afforded the new germacranolide 1beta,5beta/10alpha-trihy-droxy-8alpha-angeloyloxy-germacra-3,11(13)-dien-6alpha,12-olide in addition to a known one. Structure identification based on NMR and MS analyses. 1beta,10alpha,4alpha,5beta-Diepoxy-8alpha-angeloyloxy-costunolide isolated from D. brasilianum was studied for its anti-inflammatory activity. This STL completely inhibited DNA binding of the transcription factor NF-kappaB at a concentration of 5 microm and 10 microM in Jurkat T and Raw 264.7 cells, respectively. Elastase release from human neutrophils was reduced to 50% at a concentrations of 23 microM after stimulation with PAF and of 27 microM after stimulation with fMLP without showing cytotoxic effects. Additionally, elastase was also directly inhibited.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Asteraceae/chemistry , Lactones/isolation & purification , Plant Extracts/isolation & purification , Sesquiterpenes/isolation & purification , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Cell Line , Granulocytes/drug effects , Granulocytes/physiology , Humans , Lactones/pharmacology , Macrophages/cytology , Macrophages/drug effects , Mice , Pancreatic Elastase/blood , Plant Extracts/pharmacology , Plant Leaves/chemistry , Sesquiterpenes/pharmacologyABSTRACT
The ethyl acetate extract from leaves plus inflorescences of L. salicifolia showed significant trypanocidal activity against trypomastigote forms of T. cruzi, which was due to the flavonoid quercetin-7,3',4'-trimethyl ether and the sesquiterpenoid lychnopholic acid. Despite the use of some species of Lychnophora in folk medicine for pain relief, crude extracts from L. salicifolia Mart. showed no antinociceptive activity in the mouse writhing test.
Subject(s)
Asteraceae , Phytotherapy , Plant Extracts/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Animals , Chagas Disease/prevention & control , Parasitic Sensitivity Tests , Plant Extracts/administration & dosage , Plant Extracts/therapeutic use , Plant Leaves , Trypanocidal Agents/administration & dosage , Trypanocidal Agents/therapeutic useABSTRACT
A lactona sesquiterpênica goyazensolide apresenta atividades esquistossomicida e citotóxica. Essa substância química foi testada em sistemas de mamíferos in vitro (cultura de linfócitos do sangue periférico humano) e in vivo (células de medula óssea de ratos Wistar) para determinar seu efeito clastogênico. In vitro foram testadas as concentraçöes de 0,1; 0,3; 0,6 e 1,0 µg/ml de meio de cultura, e in vivo as concentraçöes de 0,4; 0,8; 1,6 e 3,2 mg/100g de peso corpóreo. A análise do número de células com gaps cromossômicos demonstrou que todos tratamentos com goyazensolide in vitro e somente o tratamento com 0,8 mg in vivo foram significativamente maiores do que nos controles. Contudo, na análise estatística do número de células com quebras cromossômicas demonstramos, somente in vitro, que o tratamento com 0,6 mg goyazensolide/ml de meio de cultura tem uma açäo clastogênica. O goyazensolide näo causou efeito sobre a induçäo de SCE in vitro. A dose tóxica foi determinada tanto in vitro (1,0 µg/ml) como in vivo (3,2 mg/100g)
