RESUMEN

The aims of this study were to investigate the potential benefits of antioxidant, anti-inflammatory, anti-hepatotoxic, and anti-tyrosinase activities of a methanolic extract of fresh tea leaves (FTE) (Camellia sinensis L.). The antioxidant capacity was investigated using three different methods at different temperatures. The anti-inflammatory activity was studied in vitro by the inhibition of 5-lipoxygenase assay. The anti-hepatotoxic effect was investigated in CCl4-induced liver injury in rats. The anti-tyrosinase activities of the FTE and its principal phenolic compounds were investigated in l-3,4-dihydroxyphenylalanine (l-DOPA) oxidation by a mushroom tyrosinase. A molecular docking study was conducted to determine how the FTE's principal catechins interact with the tyrosinase. The FTE exhibited the best shelf life at low temperatures and demonstrated concentration-dependent antioxidant, anti-inflammatory, anti-hepatotoxic, and anti-tyrosinase effects compared to positive references. Treatment of rats with the FTE at 2000 mg/kg/day for 28 consecutive days reversed CCl4-induced oxidative damage in hepatic tissues by lowering the levels of alanine aminotransferase by 69% and malondialdehyde by 90%. Our findings suggest that the FTE has the capacity to scavenge free radicals and can protect against oxidative stress induced by CCl4 intoxication. The docking results were consistent with our in vitro data, indicating the anti-tyrosinase potency of the principal catechins.

Asunto(s)

Camellia sinensis/química , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/administración & dosificación , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antioxidantes/administración & dosificación , Antioxidantes/química , Antioxidantes/farmacología , Modelos Animales de Enfermedad , Inhibidores Enzimáticos/administración & dosificación , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Masculino , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa/química , Estrés Oxidativo/efectos de los fármacos , Fenoles/administración & dosificación , Fenoles/química , Fenoles/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ratas

RESUMEN

Methyl gallate (MG) and pentagalloyl glucopyranose (PGG) are bioactive phenolic compounds that possess various pharmacological activities. However, the knowledge of hepatic metabolism of MG and PGG is limited. The purpose of this study was to investigate the in vitro glucuronidation of MG and PGG using liver microsomes from human (HLMs) and rats (Sprague-Dawley, SDRLMs; Wistar, WRLMs; and Gunn, GRLMs), and recombinant human uridine 5'-diphospho-glucuronosyltransferases (UGT) 1A1 and 1A9. The results demonstrated that liver microsomes catalyzed two mono-glucuronided MG (M1 and M2) formations but that UGT1A1 and 1A9 catalyzed only M1 formation. For PGG, a mono-glucuronided metabolite was mediated by liver microsomes or UGT1A9. However, a PGG glucuronide was absent in the UGT1A1 system. Additionally, all metabolites showed susceptibility to ß-glucuronidases. Furthermore, the glucuronidation activities of PGG were lower than those of MG. The kinetic parameters of MG glucuronidation demonstrated that the SDRLMs and GRLMs were more similar to the HLMs than the WRLMs for the formations of M1 and M2, respectively and that the SDRLMs and HLMs preferentially contributed to M1, whereas the WRLMs and GRLMs showed the favored formation of M2. In conclusion, MG and PGG were subjectively glucuronided by liver microsomes to demonstrate species- and strain-dependent metabolism.

Asunto(s)

Ácido Gálico/análogos & derivados , Glucuronosiltransferasa/metabolismo , Taninos Hidrolizables/metabolismo , Microsomas Hepáticos/enzimología , Animales , Ácido Gálico/química , Ácido Gálico/metabolismo , Glucuronidasa/metabolismo , Humanos , Taninos Hidrolizables/química , Cinética , Ratas Gunn , Ratas Sprague-Dawley , Ratas Wistar , UDP Glucuronosiltransferasa 1A9

RESUMEN

Mango seed kernel extract (MSKE) and its key components (gallic acid, GA; methyl gallate, MG; and pentagalloyl glucopyranose, PGG) have generated interest because of their pharmacological activities. To develop the potential use of the key components in MSKE as natural therapeutic agents, their pharmacokinetic data are necessary. Therefore, this study was performed to evaluate the factors affecting their oral bioavailability as pure compounds and as components in MSKE. The in vitro chemical stability, biological stability, and absorption were evaluated in Hanks' Balanced Salt Solution, Caco-2 cell and rat fecal lysates, and the Caco-2 cell model, respectively. The in vivo oral pharmacokinetic behavior was elucidated in Sprague-Dawley rats. The key components were unstable under alkaline conditions and in Caco-2 cell lysates or rat fecal lysates. The absorptive permeability coefficient followed the order MG > GA > PGG. The in vivo results exhibited similar pharmacokinetic trends to the in vitro studies. Additionally, the co-components in MSKE may affect the pharmacokinetic behaviors of the key components in MSKE. In conclusion, chemical degradation under alkaline conditions, biological degradation by intestinal cell and colonic microflora enzymes, and low absorptive permeability could be important factors underlying the oral bioavailability of these polyphenols.

Asunto(s)

Ácido Gálico/análogos & derivados , Ácido Gálico/metabolismo , Taninos Hidrolizables/metabolismo , Mangifera/química , Extractos Vegetales/administración & dosificación , Semillas/química , Animales , Células CACO-2 , Heces/química , Humanos , Absorción Intestinal , Masculino , Estructura Molecular , Ratas , Ratas Sprague-Dawley

RESUMEN

Methyl gallate (MG) and pentagalloyl glucopyranose (PGG) are bioactive phenolic compounds that are widely distributed in herbs and plant foods. Their potential activities include anti-oxidant, anti-inflammatory, anti-cancer, anti-bacterial and anti-viral activities. However, knowledge concerning the pharmacokinetic characteristics of MG and PGG is limited. The purpose of this study was to develop a sensitive and reproducible ultra-performance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS) method to simultaneously quantify MG and PGG in rat blood samples. The linear response ranges for MG and PGG were 0.0195-20 and 0.0390-20 µM, respectively. The lower limit of quantification was 0.0195 µM for MG and 0.0390 µM for PGG. The intra- and inter-day variances were less than 15%, and accuracy was within 80-120%. This assay was successfully applied to pharmacokinetic studies in Sprague-Dawley rats after intraperitoneal administration of MG and PGG (20 mg/kg). The values of areas under the blood concentration time curves (AUC0₋24 h) for MG and PGG were 109.9 ± 73.40 and 38.78 ± 24.53 h*µM, respectively. The maximum blood concentrations (Cmax) of MG and PGG were 34.72 ± 17.32 and 6.39 ± 4.25 µM, respectively. The time required to reach the maximum concentration (Tmax) was 0.85 ± 0.70 h for both MG and PGG. The values of the elimination rate constant (Ke), elimination half-life (t1/2), volume of distribution (Vd), clearance (Cl) and mean resident time (MRTlast) were 0.056 ± 0.032 h(-1), 17.50 ± 12.25 h, 530.95 ± 247.54 L/kg, 159.91±76.05L/h/kg, 8.71 ± 2.53 h for MG and 0.023 ± 0.012 h(-1), 38.66 ± 22.89 h, 7838.89 ± 3474.72 L/kg, 30.98 ± 21.73 L/h/kg, 12.47 ± 2.77 h for PGG, respectively. In conclusion, a UPLC-MS/MS method was fully validated over a wide linear range and used to quantify the levels of MG and PGG in pharmacokinetic studies of MG and PGG in rats. The main advantages of this method are the use of small blood volumes (10 µL), rapid analysis (5 min) and excellent recoveries.

Asunto(s)

Cromatografía Liquida/métodos , Ácido Gálico/análogos & derivados , Taninos Hidrolizables/sangre , Taninos Hidrolizables/farmacocinética , Espectrometría de Masas en Tándem/métodos , Animales , Ácido Gálico/sangre , Ácido Gálico/química , Ácido Gálico/farmacocinética , Taninos Hidrolizables/química , Modelos Lineales , Masculino , Ratas , Ratas Sprague-Dawley , Reproducibilidad de los Resultados , Sensibilidad y Especificidad

RESUMEN

A microemulsion system containing Thai mango seed kernel extract (MSKE, cultivar "Fahlun") was developed and characterised for the purpose of topical skin delivery. The MSKE-loaded microemulsions were prepared by using the spontaneous emulsification method. Isopropyl myristate (IPM) was selected as the oil phase. A polyoxyethylene sorbitan monooleate and sorbitan monododecanoate (1:1, w/w) system was used as the surfactant phase; an aqueous mixture of different cosurfactants (absolute ethanol, 96.3% v/v ethanol, 1-propanol, 2-propanol or 1,2-propanediol) at a weight ratio of 1:1 was used as the aqueous phase. Among the cosurfactants studied, the 1-propanol aqueous mixture had the largest microemulsion region (48.93%) in the pseudo-ternary phase diagram. Microemulsions containing 1% MSKE demonstrated good physicochemical stability during a six-month study period at 25 ± 2 °C/60% ± 5% RH. The ex vivo skin permeation study demonstrated that the microemulsions exhibited a potent skin enhancement effect allowing MSKE to penetrate skin layers up to 60-fold higher compared with the control. Neither skin irritation nor skin corrosion was observed in ex vivo studies. The present study revealed that IPM-based microemulsion systems may be promising carriers to enhance skin penetration and delivering MSKE for topical treatment.

Asunto(s)

Emulsiones/administración & dosificación , Emulsiones/química , Mangifera/química , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Semillas/química , Piel/metabolismo , 1-Propanol/química , Células Cultivadas , Sistemas de Liberación de Medicamentos/métodos , Fibroblastos/metabolismo , Humanos , Miristatos/química , Permeabilidad , Absorción Cutánea , Tensoactivos/química

RESUMEN

Pectinate gel beads containing Thai mango seed kernel extract (MSKE, cultivar 'Fahlun') were developed and characterised for the purpose of colon-targeted delivery. The MSKE-loaded pectinate beads were prepared using ionotropic gelation with varying pectin-to-MSKE ratios, MSKE concentrations, and concentrations of two cross-linkers (calcium chloride and zinc acetate). The formulated beads were spherical in shape and ranged in size between 1.13 mm and 1.88 mm. Zinc-pectinate (ZPG) beads containing high amounts of MSKE showed complete entrapment efficiency (EE) of MSKE (100%), while calcium-pectinate (CPG) beads demonstrated 70% EE. The in vitro release tests indicated that MSKE-loaded CPG beads were unstable in both simulated gastric medium (SGM) and simulated intestinal medium (SIM), while MSKE-loaded ZPG beads were stable in SIM but unable to prevent the release of MSKE in SGM. The protection of ZPG beads with gastro-resistant capsules (Eudragit® L 100-55) resulted in stability in both SGM and SIM; they disintegrated immediately in simulated colonic medium containing pectinolytic enzymes. MSKE-loaded ZPG beads were stable at 4, 25 and 45 °C during the study period of four months. The present study revealed that ZPG beads in enteric-coated capsules might be a promising carrier for delivering MSKE to the colon.

Asunto(s)

Sistemas de Liberación de Medicamentos , Mangifera/química , Microesferas , Extractos Vegetales/química , Semillas/química , Calcio/química , Cápsulas/química , Portadores de Fármacos/química , Geles/química , Tamaño de la Partícula , Zinc/química

RESUMEN

Plant extracts are a valuable source of novel antibacterial compounds to combat pathogenic isolates of methicillin-resistant Staphylococcus aureus (MRSA), a global nosocomial infection. In this study, the alcoholic extract from Thai mango (Mangifera indica L. cv. 'Fahlun') seed kernel extract (MSKE) and its phenolic principles (gallic acid, methyl gallate and pentagalloylglucopyranose) demonstrated potent in vitro antibacterial activity against Staphylococcus aureus and 19 clinical MRSA isolates in studies of disc diffusion, broth microdilution and time-kill assays. Electron microscopy studies using scanning electron microscopy and transmission electron microscopy revealed impaired cell division and ultra-structural changes in bacterial cell morphology, including the thickening of cell walls, of microorganisms treated with MSKE; these damaging effects were increased with increasing concentrations of MSKE. MSKE and its phenolic principles enhanced and intensified the antibacterial activity of penicillin G against 19 clinical MRSA isolates by lowering the minimum inhibitory concentration by at least 5-fold. The major phenolic principle, pentagalloylglucopyranose, was demonstrated to be the major contributor to the antibacterial activity of MSKE. These results suggest that MSKE may potentially be useful as an alternative therapeutic agent or an adjunctive therapy along with penicillin G in the treatment of MRSA infections.

Asunto(s)

Antibacterianos/farmacología , Infección Hospitalaria , Mangifera/química , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Fenoles/farmacología , Fitoterapia/métodos , Extractos Vegetales/farmacología , Infecciones Estafilocócicas , Antibacterianos/análisis , División Celular/efectos de los fármacos , Infección Hospitalaria/tratamiento farmacológico , Infección Hospitalaria/microbiología , Relación Dosis-Respuesta a Droga , Sinergismo Farmacológico , Ácido Gálico/análogos & derivados , Ácido Gálico/farmacología , Staphylococcus aureus Resistente a Meticilina/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana , Microscopía Electrónica de Rastreo , Microscopía Electrónica de Transmisión , Penicilina G/farmacología , Extractos Vegetales/química , Semillas/química , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/microbiología , Tailandia

RESUMEN

Aqueous extracts from seeds of Areca catechu L. (Arecaceae) (AC) and nutgalls of Quercus infectoria Oliv. (Fagaceae) (QI) were investigated for their hepatoprotective potential by studying their antioxidant capacity using four different methods, by determining their in vitro anti-inflammatory activity against 5-lipoxygenase, and by evaluating their hepatoprotective potential against liver injury induced by carbon tetrachloride (CCl(4)) in rats. AC and QI extracts exhibited potent antioxidant and anti-inflammatory activities. Treatment of rats with AC and QI extracts reversed oxidative damage in hepatic tissues induced by CCl(4). It is suggested that extracts rich in either condensed or hydrolysable tannins and known for their potent antioxidant and anti-inflammatory activities, may potentially confer protection against oxidative stress-induced liver injury. These data should contribute to evidence-based traditional medicines for anti-inflammatory and hepatoprotective effects of both extracts.

Asunto(s)

Areca/embriología , Hígado/efectos de los fármacos , Extractos Vegetales/farmacología , Quercus/embriología , Semillas/química , Animales , Masculino , Ratas , Ratas Wistar

RESUMEN

Polyphenols from the extracts of Areca catechu L. and Quercus infectoria Oliv. inhibited phospholipase A(2), proteases, hyaluronidase and L-amino acid oxidase of Naja naja kaouthia Lesson (NK) and Calloselasma rhodostoma Kuhl (CR) venoms by in vitro tests. Both extracts inhibited the hemorrhagic activity of CR venom and the dermonecrotic activity of NK venom by in vivo tests. The inhibitory activity of plant polyphenols against local tissue necrosis induced by snake venoms may be caused by inhibition of inflammatory reactions, hemorrhage, and necrosis. The result implies the therapeutic potential of plant polyphenols against necrosis in snakebite victims.

Asunto(s)

Venenos Elapídicos/antagonistas & inhibidores , Flavonoides/uso terapéutico , Fenoles/uso terapéutico , Piel/patología , Mordeduras de Serpientes/patología , Venenos de Serpiente/antagonistas & inhibidores , Venenos de Serpiente/toxicidad , Venenos de Víboras/antagonistas & inhibidores , Animales , Venenos Elapídicos/toxicidad , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Masculino , Ratones , Necrosis , Fenoles/aislamiento & purificación , Fenoles/farmacología , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Polifenoles , Ratas , Ratas Sprague-Dawley , Piel/efectos de los fármacos , Mordeduras de Serpientes/tratamiento farmacológico , Venenos de Víboras/toxicidad

RESUMEN

The ethanolic extract from seed kernels of Thai mango (MSKE) (Mangifera indica L. cv. 'Fahlun') (Anacardiaceae) and its major phenolic principle (pentagalloyl glucopyranose) exhibited dose-dependent inhibitory effects on enzymatic activities of phospholipase A(2) (PLA(2)), hyaluronidase and L-amino acid oxidase (LAAO) of Calloselasma rhodostoma (CR) and Naja naja kaouthia (NK)venoms by in vitro tests. The anti-hemorrhagic and anti-dermonecrotic activities of MSKE against both venoms were clearly supported by in vivo tests. Molecular docking studies indicated that the phenolic molecules of the MSKE could selectively bind to the active sites or their proximity, or modify conserved residues that are critical for the catalysis of PLA(2), and selectively bind to the LAAO binding pocket of both CR and NK venoms and thereby inhibit their enzymatic activities. The results imply a potential use of MSKE against snake venoms.

Asunto(s)

Simulación por Computador , Inhibidores Enzimáticos , Mangifera/química , Extractos Vegetales , Semillas/química , Venenos de Serpiente/enzimología , Animales , Antivenenos/química , Antivenenos/metabolismo , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/metabolismo , Humanos , Hialuronoglucosaminidasa/antagonistas & inhibidores , Taninos Hidrolizables/química , L-Aminoácido Oxidasa/antagonistas & inhibidores , Masculino , Mangifera/anatomía & histología , Ratones , Modelos Moleculares , Estructura Molecular , Fenoles/química , Inhibidores de Fosfolipasa A2 , Extractos Vegetales/química , Extractos Vegetales/metabolismo , Estructura Terciaria de Proteína , Ratas , Ratas Sprague-Dawley , Serpientes , Tailandia

RESUMEN

Three polyphenolic principles, 1,2,3,4,6-penta- O-galloyl-beta-D-glucopyranose (PGG), methyl gallate (MG), and gallic acid (GA), were isolated from the ethanolic extract of seed kernels of Thai mango (MSKE) ( MANGIFERA INDICA L. cv. "Fahlun") and quantified using a TLC scanning densitometric method. The MSKE and its isolates were investigated by studying their antioxidant capacities using four different methods, by determining their IN VITRO anti-inflammatory activities, and by evaluating their hepatoprotective potential against liver injury in rats induced by carbon tetrachloride (CCl (4)). The hepatoprotective effect of MSKE is clearly supported by its polyphenolic nature of the main principle, PGG, which exhibited potent antioxidant and anti-inflammatory activities.

Asunto(s)

Antioxidantes/farmacología , Hígado/efectos de los fármacos , Mangifera/embriología , Extractos Vegetales/farmacología , Semillas/química , Animales , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Inhibidores de la Lipooxigenasa , Hígado/enzimología , Hígado/patología , Masculino , Extractos Vegetales/normas , Ratas , Ratas Wistar , Análisis Espectral/métodos

RESUMEN

The alcoholic extract from seed kernels of Thai mango (Mangifera indica L. cv. 'Fahlun') (Anacardiaceae) and its major phenolic principle (pentagalloylglucopyranose) exhibited potent, dose-dependent inhibitory effects on tyrosinase with respect to L-DOPA. Molecular docking studies revealed that the binding orientations of the phenolic principles were in the tyrosinase binding pocket and their orientations were located in the hydrophobic binding pocket surrounding the binuclear copper active site. The results indicated a possible mechanism for their anti-tyrosinase activity which may involve an ability to chelate the copper atoms which are required for the catalytic activity of tyrosinase.

Asunto(s)

Inhibidores Enzimáticos/química , Taninos Hidrolizables/farmacología , Mangifera/química , Monofenol Monooxigenasa/antagonistas & inhibidores , Semillas/química , Agaricales/enzimología , Sitios de Unión , Cobre/química , Inhibidores Enzimáticos/farmacología , Taninos Hidrolizables/química , Levodopa/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Conformación Proteica

RESUMEN

A new oleanane-triterpene, 3beta-acetoxy-11alpha-benzoyloxy-13beta-hydroxyolean-12-one (1), was isolated along with a known quinone-methide triterpene, pristimerin (2), from the root bark of Siphonodon celastrineus Griff., a Thai medicinal plant of the family Celastraceae. Their structures were determined based on spectroscopic analysis.

Asunto(s)

Antineoplásicos Fitogénicos/aislamiento & purificación , Corteza de la Planta/química , Plantas Medicinales/química , Triterpenos/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Triterpenos/química , Triterpenos/farmacología

RESUMEN

Plant polyphenols from the aqueous extracts of Pentace burmanica, Pithecellobium dulce, Areca catechu and Quercus infectoria were tested for their inhibitory activities against Naja kaouthia (NK) venom by in vitro neutralization method. The first three extracts could completely inhibit the lethality of the venom at 4 LD50 concentration and the venom necrotizing activity at the minimum necrotizing dose while also inhibited up to 90% of the acetylcholinesterase activity of NK venom at much lower tannin concentrations than that of Quercus infectoria. The ED50 of plant tannins in inhibiting NK venom activities varied according to condensed tannins and their content in the extracts. Molecular docking of the complexes between alpha-cobratoxin and either hydrolysable or condensed tannins at their lowest energetic conformations were proposed. The anti-venom activities of these plant polyphenols by selectively blocking the nicotinic acetylcholine receptor and non-selectively by precipitation of the venom proteins were suggested.

Asunto(s)

Antivenenos/farmacología , Venenos Elapídicos/antagonistas & inhibidores , Flavonoides/farmacología , Fenoles/farmacología , Animales , Antivenenos/química , Antivenenos/metabolismo , Sitios de Unión/fisiología , Relación Dosis-Respuesta a Droga , Venenos Elapídicos/metabolismo , Femenino , Flavonoides/química , Flavonoides/metabolismo , Masculino , Ratones , Fenoles/química , Fenoles/metabolismo , Corteza de la Planta , Extractos Vegetales/química , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacología , Polifenoles , Ratas , Ratas Sprague-Dawley , Semillas

RESUMEN

From the stem of Strychnos vanprukii, two new lignan glucosides, vanprukoside (1) and strychnoside (2), were isolated together with the known lignan glucoside, (+)-lyoniresinol-3 alpha-O-beta-glucopyranoside (3). The structures of these compounds were elucidated on the basis of their spectroscopic data. All three compounds exhibited antioxidant activity.

Asunto(s)

Antioxidantes/química , Fitoterapia , Extractos Vegetales/química , Strychnos , Compuestos de Bifenilo , Glucósidos/química , Humanos , Lignanos/química , Picratos/química , Tallos de la Planta

RESUMEN

Two new compounds, 6-oxo-20-hydroxy-20-epi-tingenol (1) and 2R*,3R*,5S*-trihydroxy-6R*-nonadecyltetrahydropyran-4-one (2), were isolated from the pericarp of Glyptopetalum sclerocarpum along with other 10 constituents.

Asunto(s)

Celastraceae , Fitoterapia , Extractos Vegetales/química , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Tallos de la Planta

RESUMEN

Azaphilone pigments, monascusones A (1) and B (2), together with two known azaphilones, monascin (3) and FK17-P2b2 (4), were isolated from the CH2Cl2 extract of a yellow mutant of the fungus M. kaoliang grown on rice. Structures of the isolated compounds were elucidated by analyses of spectroscopic data. Monascusone A (1), the major metabolite of M. kaoliang, showed no antimalarial (against Plasmodium falciparum), antitubercular (against Mycobacterium tuberculosis H37Ra), and antifungal (toward Candida albicans) activities. Compound 1 exhibited no cytotoxicity against BC (breast cancer) and KB (human epidermoid carcinoma of cavity) cell lines.

Asunto(s)

Benzopiranos/química , Benzopiranos/aislamiento & purificación , Monascus/química , Monascus/genética , Mutación/genética , Pigmentos Biológicos/química , Pigmentos Biológicos/aislamiento & purificación , Benzopiranos/farmacología , Línea Celular Tumoral , Color , Humanos , Espectroscopía de Resonancia Magnética , Estructura Molecular , Pigmentos Biológicos/farmacología

RESUMEN

The butanolic and purified butanolic extracts (PBEs) of Eclipta prostrata were evaluated for their anti-venom potential. Inhibition of lethal, hemorrhagic, proteolytic, and phospholipase A2 activities of Calloselasma rhodostoma (Malayan pit viper (MPV)) venom by these extracts were determined. Demethylwedelolactone was identified as their major constituent. The butanolic extract, at 2.5 mg per mouse, was able to completely neutralize the lethal activity of 2LD50 of MPV venom, but increasing the dose diminished the effect. The PBE, at 1.5-4.5 mg per mouse, was able to neutralize the lethality of the venom at around 50-58%. Both extracts partially inhibited the hemorrhagic activity but displayed very low anti-phospholipase A2 activity and did not inhibit proteolytic activity of MPV venom.

Asunto(s)

Antivenenos/farmacología , Venenos de Crotálidos/antagonistas & inhibidores , Eclipta , Animales , Antivenenos/química , Antivenenos/uso terapéutico , Butanoles/química , Butanoles/farmacología , Butanoles/uso terapéutico , Venenos de Crotálidos/toxicidad , Relación Dosis-Respuesta a Droga , Femenino , Hemorragia/inducido químicamente , Hemorragia/tratamiento farmacológico , Masculino , Ratones , Componentes Aéreos de las Plantas , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Viperidae

RESUMEN

From the stem of Strychnos vanprukii, a gluco-indole alkaloid, 3,4-dehydropalicoside, and a pimarane diterpenoid, 7 beta-hydroxypimara-8,15-dien-14-one, were isolated together with four known alkaloids: palicoside, 3,4,5,6-tetradehydropalicoside, akagerine and 17-O-methylakagerine. The structures of these compounds were elucidated based on spectroscopic evidence.

Asunto(s)

Abietanos , Diterpenos/química , Diterpenos/aislamiento & purificación , Alcaloides Indólicos/química , Alcaloides Indólicos/aislamiento & purificación , Strychnos/química , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Estructura Molecular , Tallos de la Planta/química , Espectrometría de Masa por Ionización de Electrospray

RESUMEN

Nine novel quinone-methide triterpenoids: 20-hydroxytingenone, 20,22beta-dihydroxytingenone, 20,22beta-dihydroxy-20-epi-tingenone, 20,21alpha-dihydroxy-22-oxo-21-desoxotingenone, 20-hydroxy-22-oxotingenone, 20-hydroxy-22-oxo-20-epi-tingenone, 21alpha-hydroxy-20,22-dioxo-30(20-->21)abeo-21-desoxotingenone, 20-oxo-20,21-seco-tingen-21-oic acid and 20-oxo-21-nor-20,21-seco-tingen-22-al, were isolated from the stem bark of Glyptopetalum sclerocarpum. Their structures were determined on the basis of spectroscopic evidence.