RESUMEN
Four carbazoles (girinimbine, mahanimbine, murrayafoline and murrayanine), isolated from Murraya koenigii, and one kavalactone (5,6-dehydrokawain) and one flavonoid (pinostrobin) isolated, from Alpinia mutica, were tested for their antitrypanosomal activity using in vitro cultured Trypanosoma evansi cell lines. The cytotoxic activities of these compounds were also investigated against mammalian Vero cells using the MTT (3-(4,5- Dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide)-cell proliferation assay. Three carbazole compounds, namely mahanimbine, murrayafoline, and girinimbine, showed a potent antitrypanosomal activity, scoring a median inhibitory concentration (IC50) of 3.13, 6.35 and 10.16 µg/ml, respectively. Girinimbine was the least toxic to Vero cells, and the mean cytotoxic concentration (CC50) and the selectivity index (SI) of this compound were 745.58 ± 42.38 µg/ ml and 73.38, respectively. Girinimbine and the other carbazole compounds possess potential antitrypanosomal activity with comparably low toxicity against mammalian cells. Girinimbine, in particular, is a good candidate to be further investigated as a potential antitrypanosomal agent using in vivo models.
RESUMEN
@#Four carbazoles (girinimbine, mahanimbine, murrayafoline and murrayanine), isolated from Murraya koenigii, and one kavalactone (5,6-dehydrokawain) and one flavonoid (pinostrobin) isolated, from Alpinia mutica, were tested for their antitrypanosomal activity using in vitro cultured Trypanosoma evansi cell lines. The cytotoxic activities of these compounds were also investigated against mammalian Vero cells using the MTT (3-(4,5- Dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide)-cell proliferation assay. Three carbazole compounds, namely mahanimbine, murrayafoline, and girinimbine, showed a potent antitrypanosomal activity, scoring a median inhibitory concentration (IC50) of 3.13, 6.35 and 10.16 μg/ml, respectively. Girinimbine was the least toxic to Vero cells, and the mean cytotoxic concentration (CC50) and the selectivity index (SI) of this compound were 745.58 ± 42.38 μg/ ml and 73.38, respectively. Girinimbine and the other carbazole compounds possess potential antitrypanosomal activity with comparably low toxicity against mammalian cells. Girinimbine, in particular, is a good candidate to be further investigated as a potential antitrypanosomal agent using in vivo models.
RESUMEN
The current in vitro study was designed to investigate the anti-inflammatory, cytotoxic and antioxidant activities of boesenbergin A (BA), a chalcone derivative of known structure isolated from Boesenbergia rotunda. Human hepatocellular carcinoma (HepG2), colon adenocarcinoma (HT-29), non-small cell lung cancer (A549), prostate adenocarcinoma (PC3), and normal hepatic cells (WRL-68) were used to evaluate the cytotoxicity of BA using the MTT assay. The antioxidant activity of BA was assessed by the ORAC assay and compared to quercetin as a standard reference antioxidant. ORAC results are reported as the equivalent concentration of Trolox that produces the same level of antioxidant activity as the sample tested at 20 µg/mL. The toxic effect of BA on different cell types, reported as IC50, yielded 20.22 ± 3.15, 10.69 ± 2.64, 20.31 ± 1.34, 94.10 ± 1.19, and 9.324 ± 0.24 µg/mL for A549, PC3, HepG2, HT-29, and WRL-68, respectively. BA displayed considerable antioxidant activity, when the results of ORAC assay were reported as Trolox equivalents. BA (20 µg/mL) and quercetin (5 µg/mL) were equivalent to a Trolox concentration of 11.91 ± 0.23 and 160.32 ± 2.75 µM, respectively. Moreover, the anti-inflammatory activity of BA was significant at 12.5 to 50 µM and without any significant cytotoxicity for the murine macrophage cell line RAW 264.7 at 50 µM. The significant biological activities observed in this study indicated that BA may be one of the agents responsible for the reported biological activities of B. rotunda crude extract.
Asunto(s)
Animales , Humanos , Ratones , Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Chalcona/farmacología , Técnicas In Vitro , Neoplasias/tratamiento farmacológico , Fitoterapia/métodos , Zingiberaceae/química , Análisis de Varianza , Antiinflamatorios/uso terapéutico , Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/uso terapéutico , Línea Celular Tumoral , Cromatografía , Chalcona/aislamiento & purificación , Ensayos de Selección de Medicamentos Antitumorales/métodos , RizomaRESUMEN
The current in vitro study was designed to investigate the anti-inflammatory, cytotoxic and antioxidant activities of boesenbergin A (BA), a chalcone derivative of known structure isolated from Boesenbergia rotunda. Human hepatocellular carcinoma (HepG2), colon adenocarcinoma (HT-29), non-small cell lung cancer (A549), prostate adenocarcinoma (PC3), and normal hepatic cells (WRL-68) were used to evaluate the cytotoxicity of BA using the MTT assay. The antioxidant activity of BA was assessed by the ORAC assay and compared to quercetin as a standard reference antioxidant. ORAC results are reported as the equivalent concentration of Trolox that produces the same level of antioxidant activity as the sample tested at 20 µg/mL. The toxic effect of BA on different cell types, reported as IC50, yielded 20.22 ± 3.15, 10.69 ± 2.64, 20.31 ± 1.34, 94.10 ± 1.19, and 9.324 ± 0.24 µg/mL for A549, PC3, HepG2, HT-29, and WRL-68, respectively. BA displayed considerable antioxidant activity, when the results of ORAC assay were reported as Trolox equivalents. BA (20 µg/mL) and quercetin (5 µg/mL) were equivalent to a Trolox concentration of 11.91 ± 0.23 and 160.32 ± 2.75 µM, respectively. Moreover, the anti-inflammatory activity of BA was significant at 12.5 to 50 µM and without any significant cytotoxicity for the murine macrophage cell line RAW 264.7 at 50 µM. The significant biological activities observed in this study indicated that BA may be one of the agents responsible for the reported biological activities of B. rotunda crude extract.
Asunto(s)
Antiinflamatorios/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Chalcona/farmacología , Neoplasias/tratamiento farmacológico , Fitoterapia/métodos , Zingiberaceae/química , Análisis de Varianza , Animales , Antiinflamatorios/uso terapéutico , Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/uso terapéutico , Línea Celular Tumoral , Chalcona/aislamiento & purificación , Cromatografía , Ensayos de Selección de Medicamentos Antitumorales/métodos , Humanos , Técnicas In Vitro , Ratones , RizomaRESUMEN
A detailed chemical study on the stem bark of Garcinia nitida has led to the isolation of five xanthones. They are 1,6-dihydroxy-5-methoxy-6,6-dimethylpyrano[2',3':2,3]-xanthone (1), inophyllin B (2), osajaxanthone (3), 3-isomangostin (4) and rubraxanthone (5). The structures of these compounds were established using mainly 1-D and 2-D NMR spectroscopy ((1)H, (13)C, DEPT, COSY, HMBC and HMQC) while molecular masses were determined via MS techniques; 1 is a new compound.
Asunto(s)
Garcinia/química , Xantonas/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Infrarroja , Espectrofotometría UltravioletaRESUMEN
An investigation of Morinda citrifolia roots afforded a new anthraquinone, 2-ethoxy-1-hydroxyanthraquinone (1), along with five other known anthraquinones: 1-hydroxy-2-methylanthraquinone (2), damnacanthal (3), nordamnacanthal (4), 2-formyl-1-hydroxyanthraquinone (5) and morindone-6-methyl-ether (6). This is the first report on the isolation of morindone-6-methyl-ether (6) from this plant. The structures of these compounds were elucidated based on spectroscopic analyses such as NMR, MS and IR. Biological evaluation of five pure compounds and all the extracts against the larvae of Aedes aegypti indicated 1-hydroxy-2-methylanthraquinone (2) and damnacanthal (3) were the extracts to exhibit promising larvicidal activities.
Asunto(s)
Antraquinonas/química , Morinda/química , Raíces de Plantas/química , Aedes/efectos de los fármacos , Aldehídos/química , Aldehídos/farmacología , Animales , Antraquinonas/farmacología , Insecticidas/química , Insecticidas/farmacología , Larva/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura MolecularRESUMEN
A new carbazole alkaloid, 3-carbomethoxy-2-hydroxy-7-methoxycarbazole, Clausine-TY (1), together with two known carbazole alkaloid, Clausine-H (2) and Clausine-B (3), were isolated from the ethyl acetate extract of the stem bark of the Malaysian Clausena excavata. The structures of these compounds were elucidated by spectroscopic analyses. The new carbazole alkaloid shows significant cytotoxicity against CEM-SS cell line.
Asunto(s)
Carbazoles/aislamiento & purificación , Corteza de la Planta/química , Rutaceae/química , Carbazoles/química , Carbazoles/uso terapéutico , Línea Celular Tumoral , Compuestos Heterocíclicos con 3 Anillos/aislamiento & purificación , Compuestos Heterocíclicos con 3 Anillos/uso terapéutico , Humanos , Leucemia Linfoide/tratamiento farmacológico , Espectroscopía de Resonancia Magnética , Estructura MolecularRESUMEN
A new tetraoxygenated xanthone, daphnifolin (1,3,5-trihydroxy-4-methoxyxanthone), along with three other xanthones, were isolated from the stem bark extracts of Mesua daphnifolia. Their structures were characterized on the basis of 1D and 2D NMR spectral data.