RESUMO
Three previously undescribed isoflavones, derrisrobustones A-C, and a previously undescribed natural isoflavone, derrisrobustone D, along with eight known isoflavones, were isolated from the twig extract of Derris robusta (DC.) Benth. All structures were identified by extensive spectroscopic analysis. Derrisrobustones A-C were obtained as scalemic mixtures and were resolved by chiral HPLC. The (1â³R, 2â³R) absolute configuration of (+)-derrisrobustone B was established by single-crystal X-ray crystallography using Cu Kα radiation. The absolute configurations of derrisrobustones A and C were determined by analysis of experimental and calculated ECD data. All compounds were evaluated for their α-glucosidase inhibitory activity. Of these, derrubone displayed the best α-glucosidase inhibitory activity with an IC50 value of 64.2 µM.
Assuntos
Derris , Isoflavonas , Derris/química , Derris/metabolismo , Isoflavonas/química , Isoflavonas/farmacologia , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases/metabolismoRESUMO
Due to the increased development of resistance of vectors against synthetic insecticides and chemical drugs, plant based insecticides serve as promising biocontrol agents for effective vector control. Green approach for the synthesis of nanoparticles has been attained using environmentally safe, non-toxic plant extracts. The present study was aimed to investigate the potent larvicidal activity of silver nanoparticles (AgNPs) produced by Derris trifoliata leaf extract in relation to the various concentrations of methanol and chloroform extracts for 24h against 3rd and 4th instar larvae of Aedes aegypti. AgNPs were synthesized using D. trifoliata leaf extract as reducing and stabilizing agent. Synthesized AgNPs were characterized by UV-Vis spectroscopy, FTIR spectroscopy, SEM, EDX, XRD and HRTEM. The size of AgNPs as estimated from the full width at half-maximum of (200) peak of silver was 16.13nm, the average crystalline size of the synthesized AgNPs was approximately 20nm, which was correlated with the HRTEM results (20nm). SEM and TEM images have shown the formation of polydispersed nanoparticles with an average size of 20nm. The FTIR spectra of AgNPs exhibited prominent peaks at 2360.7, 1606.2, 1095.6 and 785.9cm-1. The spectral peak observed at 1606.2, assigned to stretching vibration (C=O) in carbonyl compounds characterized by the presence of major constituents of flavonoids and terpenoids. The results obtained in FTIR spectroscopy correlated with the GC-MS analysis of methanol and chloroform extracts and indicates the presence of phytosteroids, flavonoids and terpenoids. The highest larvicidal activity was observed for the synthesized AgNPs against the 3rd instar larvae with LC50 values of 5.87mg/l and LC90 of 12.11mg/l, while against 4th instar larvae these values were7.00 and17.76mg/l respectively. The chloroform extracts also showed increased larvicidal activity than methanol extracts against 3rd instar larvae (LC50=54.42mg/l, LC90=140.83mg/l) and 4th instar larvae (LC50=62.47mg/l, LC90=145.06mg/l) of A. aegypti. Besides, the synthesized AgNPs also exhibited potent antibacterial activity against certain food borne pathogens. These results infer that the biologically synthesized AgNPs and organic solvent extracts have the potential to be used as an excellent eco-friendly approach for vector control against A. aegypti.
Assuntos
Aedes , Antibacterianos/química , Derris/química , Inseticidas , Nanopartículas Metálicas/química , Extratos Vegetais/química , Prata/química , Animais , Antibacterianos/farmacologia , Derris/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Química Verde , Larva , Luz , Nanopartículas Metálicas/toxicidade , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismo , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
To investigate allelopathic activity of a leguminous mangrove plant, Derris indica, the 'Protoplasts Co-culture Method' for bioassay of allelopathy was developed using suspension culture. A suspension culture was induced from immature seed and sub-cultured in Murashige and Skoog's (MS) basal medium containing 10 µM each of 2,4-dichlorophenoxyacetic acid (2,4-D) and 6-benzyladenine (BA). The protoplasts were isolated using the separate wells method with 2% each of Cellulase RS, Driselase 20 and Macerozyme R10 in 0.4 M mannitol solution. Protoplast cultures of D. indica revealed that high concentrations of cytokinins, BA and thidiazuron, were effective for cell divisions. The co-cultures of D. indica protoplasts with recipient lettuce protoplasts using 96 multi-well culture plates were performed in MS basal medium containing 0.4 M mannitol solution and 1 µM 2,4-D and 0.1 µM BA. The protoplast density of D. indica used in co-culturing varied from 6 x 10(3) - 10(5) / mL. Very strong inhibitory allelopathic effects of D. indica protoplasts on lettuce protoplast growth were found. A similar strong inhibitory allelopathic activity of dried young leaves on lettuce seedling growth was also observed by using the sandwich method. Rotenone, which is a component of Derris root, dissolved in DMSO, was highly inhibitory on the growth of lettuce protoplasts in culture and this could be one of the causes of the strong allelopathic activity of D. indica.
Assuntos
Bioensaio/métodos , Técnicas de Cocultura/métodos , Derris/química , Lactuca/crescimento & desenvolvimento , Protoplastos/efeitos dos fármacos , Rotenona/farmacologia , Alelopatia , Células Cultivadas , Derris/crescimento & desenvolvimento , Derris/metabolismo , Lactuca/efeitos dos fármacos , Rotenona/metabolismoRESUMO
Enhancing of radioresponsiveness of tumors by using radiosensitizers is a promising approach to increase the efficacy of radiation therapy. Recently, the ethanolic extract of the medicinal plant, Derris scandens Benth has been identified as a potent radiosensitizer of human colon cancer HT29 cells. However, cell death mechanisms underlying radiosensitization activity of D scandens extract have not been identified. Here, we show that treatment of HT-29 cells with D scandens extract in combination with gamma irradiation synergistically sensitizes HT-29 cells to cell lethality by apoptosis and mitotic catastrophe. Furthermore, the extract was found to decrease Erk1/2 activation. These findings suggest that D scandens extract mediates radiosensitization via at least two distinct modes of cell death and silences pro-survival signaling in HT-29 cells.
Assuntos
Apoptose/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Derris/metabolismo , Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos , Radiossensibilizantes/farmacologia , Apoptose/efeitos da radiação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos da radiação , Neoplasias do Colo/radioterapia , MAP Quinases Reguladas por Sinal Extracelular/biossíntese , Células HT29 , Humanos , Marcação In Situ das Extremidades Cortadas , Pontos de Checagem da Fase M do Ciclo Celular/efeitos da radiação , Extratos Vegetais/farmacologiaRESUMO
The aim of this study was to reveal the pyridine metabolism in leaves of two mangrove legumes, Derris indica (= Millettia pinnata or Pongamia pinnata) and Caesalpinia crista. Radioactivity from [carbonyl-14C]nicotinamide supplied exogenously to young leaf disks was recovered in nicotinic acid, nicotinic acid mononucleotide, NAD, NADP, nicotinamide mononucleotide and trigonelline. These mangrove species, especially D. indica, have strong ability to convert nicotinamide to trigonelline, but not to nicotinic acid glucoside. The endogenous trigonelline content in leaves of D. indica was more than 830 microg/g dry weight. This value is 5-12 times greater than that in leaves of Glycine max. There was little short-term effect of 250 and 500 mM NaCl (equivalent to ca. 50% and 100% sea water) on nicotinamide metabolism.