ABSTRACT
The antioxidant and larvicidal activities of Tephrosia egregia extracts and its major component, dehydrorotenone, were studied. High antioxidant activity was found for dehydrorotenone and methanol and ethyl acetate extracts from roots and stems, respectively. Among the tested extracts, the hexane extract from stems showed potent larvicidal activity (LC50 12.88 +/- 0.64) while low activity was found for dehydrorotenone.
Subject(s)
Aedes , Insecticides/chemistry , Tephrosia/chemistry , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacology , Insecticides/isolation & purification , Lethal Dose 50 , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Stems/chemistryABSTRACT
(1)H and (13)C NMR chemical shifts of praecansone B, pongaflavone and dehydrorotenone isolated from Tephrosia egregia Sandw and obovatin from T. toxicaria Pers. were unambiguously assigned by 1D and 2D NMR experiments including (1)H, (1)H COSY, gHMQC and gHMBC, allowing the correction of literature assignments.
Subject(s)
Flavones/chemistry , Flavonoids/chemistry , Protons , Tephrosia/chemistry , Carbon Isotopes , Flavonoids/isolation & purification , Magnetic Resonance Spectroscopy , Molecular Structure , Reference Standards , StereoisomerismABSTRACT
One- and two-dimensional NMR experiments were used for the unambiguous assignment of the (1)H and (13)C NMR chemical shifts of the furoquinoline alkaloid maculine (1) and the new furanocoumarin 3,8-dimethoxyfuro[3,2-g]coumarin (2).
Subject(s)
Coumarins/chemistry , Dioxoles/chemistry , Furans/chemistry , Magnetic Resonance Spectroscopy/methods , Magnetic Resonance Spectroscopy/standards , Quinolines/chemistry , Rutaceae/chemistry , Carbon Isotopes , Molecular Conformation , Protons , Reference StandardsABSTRACT
One- and two-dimensional NMR experiments were used for the unambiguous assignment of the 1H and 13C NMR chemical shifts of 3,3-diisopentenyl-N-methyl-2,4-quinoldione and five novel reaction derivatives.
Subject(s)
Alkaloids/chemistry , Isoquinolines/chemistry , Sapindus/chemistry , Magnetic Resonance Spectroscopy/methods , Molecular Conformation , WoodABSTRACT
The structure of the glycosomal glyceraldehyde-3-phosphate dehydrogenase (gGAPDH) from Trypanosoma cruzi complexed with chalepin, a natural product from Pilocarpus spicatus, has been determined by X-ray crystallography to 1.95 A resolution. The structure is in the apo form without cofactors in the subunits of the tetrameric gGAPDH in the asymmetric unit. Unequivocal density corresponding to the inhibitor was clearly identified in one monomer. The final refined model of the complex shows extensive conformational changes when compared with the native structure. The mode of binding of chalepin to gGAPDH and its implications for inhibitor design are discussed.
Subject(s)
Furocoumarins/chemistry , Glyceraldehyde-3-Phosphate Dehydrogenases/chemistry , Microbodies/enzymology , Trypanosoma cruzi/enzymology , Animals , Crystallization , Crystallography, X-Ray , Furocoumarins/metabolism , Glyceraldehyde-3-Phosphate Dehydrogenases/genetics , Glyceraldehyde-3-Phosphate Dehydrogenases/metabolism , Macromolecular Substances , Molecular Structure , Protein Binding , Structure-Activity Relationship , Trypanosoma cruzi/geneticsABSTRACT
The activity of crude plant extracts of nine species of Rutaceae against the trypomastigote form of Trypanosoma cruzi was evaluated at 4 mg/ml. Thirty-two crude extracts were tested and eight of them showed significant activity (>80%). The most active extract was obtained from the stems of Pilocarpus spicatus (97.3%). Fractionation of the active crude extracts provided 25 fractions which were tested against the trypomastigote form of T. cruzi at 2 mg/ml. Of these six showed significant activity (>80%). The most active fractions (100%) were obtained from the leaves of Almeidea coerulea (butanol fraction) and Conchocarpus inopinatus (dichloromethane fraction).
