RESUMEN
BACKGROUND: The plant Euphorbia hirta is widely used against snake envenomations in rural areas and it was proved to be effective in animal models. Therefore, the scientific validation of its phytoconstituents for their antiophidian activity is aimed in the present study. METHODS: E. hirta extract was subjected to bioactivity guided fractionation and the fractions that inhibited different enzyme activities of Naja naja venom in vitro was structurally characterized using UV, FT-IR, LC-MS and NMR spectroscopy. Edema, hemorrhage and lethality inhibition activity of the compound were studied in mice model. In addition, molecular docking and molecular dynamic simulations were also performed in silico. RESULTS: The bioactive fraction was identified as Quercetin-3-O-α-rhamnoside (QR, 448.38 Da). In vitro experiments indicated that protease, phospholipase-A(2), hemolytic activity and hemorrhage inducing activity of the venom were inhibited completely at a ratio of 1:20 (venom: QR) w/w. At the same concentration, the edema ratio was drastically reduced from 187% to 107%. Significant inhibition (93%) of hyaluronidase activity was also observed at a slightly higher concentration of QR (1:50). Further, in in vivo analysis, QR significantly prolonged the survival time of mice injected with snake venom. CONCLUSION: For the first time Quercetin-3-O-α-rhamnoside, isolated from E. hirta, has been shown to exhibit anti-snake venom activity against Naja naja venom induced toxicity. GENERAL SIGNIFICANCE: Exploring such multifunctional lead molecules with anti-venom activity would help in developing complementary medicine for snakebite treatments especially in rural areas where anti-snake venom is not readily available.
Asunto(s)
Venenos Elapídicos , Elapidae , Inhibidores Enzimáticos/farmacología , Euphorbia/química , Extractos Vegetales/farmacología , Quercetina/análogos & derivados , Mordeduras de Serpientes/tratamiento farmacológico , Animales , Bioensayo , Fraccionamiento Químico/métodos , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Edema/enzimología , Edema/prevención & control , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Hemólisis/efectos de los fármacos , Hemorragia/enzimología , Hemorragia/prevención & control , Hialuronoglucosaminidasa/antagonistas & inhibidores , Hialuronoglucosaminidasa/metabolismo , Masculino , Ratones , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Estructura Molecular , Inhibidores de Fosfolipasa A2/aislamiento & purificación , Inhibidores de Fosfolipasa A2/farmacología , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Inhibidores de Proteasas/aislamiento & purificación , Inhibidores de Proteasas/farmacología , Quercetina/química , Quercetina/aislamiento & purificación , Quercetina/farmacología , Mordeduras de Serpientes/enzimología , Relación Estructura-Actividad , Factores de TiempoRESUMEN
OBJECTIVE: To investigate the efficacy of ethanolic extract of nilavembu kudineer choornam (EENKC) in inflammation, pain and fever using animal models to support its actions. METHODS: Acute toxicity study of EENKC was performed in mice to fix the effective dose. The antipyretic, anti-inflammatory and analgesic activity of EENKC was evaluated in brewer's yeast induced pyrexia in rats, carrageenan-induced inflammation in rats and acetic-acid induced writhing in mice model. RESULTS: Acute toxicity revealed that EENKC didn't show death and toxic signs up to 2 000 mg/kg. In brewer's yeast induced pyrexia and carrageenan-induced inflammation EENKC at the doses of 200 and 400 mg/kg inhibited fever and inflammation significantly (P<0.01 and <0.05) compared to control animals. In mice, the number of writhing induced by acetic-acid was significantly (P<0.01) reduced after treatment with both the dose of EENKC than control animals. EENKC 200 mg/kg inhibits inflammation higher level in carrageenan-induced paw edema, but there is no significant difference when compared to indomethacin 10 mg/kg. CONCLUSIONS: The present findings revealed that EENKC possesses antipyretic, anti-inflammatory and analgesic activity which supports nilavembu kudineer choornam efficacy in chikungunya fever.
Asunto(s)
Fiebre/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Medicina Tradicional/métodos , Dolor/tratamiento farmacológico , Fitoterapia , Plantas Medicinales , Ácido Acético , Animales , Carragenina , Estudios de Casos y Controles , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Femenino , Fiebre/inducido químicamente , Alimentos , Miembro Posterior , India , Inflamación/inducido químicamente , Masculino , Ratones , Dolor/inducido químicamente , Dimensión del Dolor/efectos de los fármacos , Ratas , Ratas Wistar , Saccharomyces cerevisiae , Resultado del TratamientoRESUMEN
A nutrition survey carried out in India revealed that the diets of the rural population are inadequate and deficient in most of the nutrients especially protein. India being the 5th-largest producer of soybean, a protein-rich cereal, can redress protein-energy malnutrition through diversification of soybean uses by developing high-value and health-based food products. Tofu, a nonfermented soybean product rich in high-quality protein, B-vitamins, and isoflavones, could be an excellent substitute for meat in Indian recipes. Tofu being rich in protein has a very short shelf life. Hence an attempt was made to improve the shelf life using extracts of tulsi (Ocimum sanctum) commonly available in rural areas. Tofu was prepared traditionally using MgCl(2):CaSO(4) as coagulating agents. Aqueous extract of Ocimum sanctum (tulsi) was added during the preparation and storage of tofu to prolong its shelf life. Water used in this study was free from microflora, plant extract used contained mesophilic count of 2.527 x 10(4) CFU/g, and no yeasts and molds were detected. Tofu with tulsi extract had 76.4% moisture and was softer than control. Not much difference in mesophilic count was observed between control and treated samples during storage; however, treated tofu was organoleptically good until the end of the study with less lipid-peroxidation and exhibited 50% (4.7 units) less protease activity than control (9.6 units) after 7 d. By using extracts of naturally available, easily cultivable tulsi, the shelf life was successfully extended to 7 to 8 d from 3 to 4 d of normal storage without refrigeration.
Asunto(s)
Conservación de Alimentos/métodos , Conservantes de Alimentos/farmacología , Ocimum/química , Extractos Vegetales/farmacología , Alimentos de Soja/normas , Proteínas en la Dieta/administración & dosificación , Proteínas en la Dieta/normas , Humanos , India , Peroxidación de Lípido/efectos de los fármacos , Valor Nutritivo , Péptido Hidrolasas/metabolismo , Factores de TiempoRESUMEN
Ascorbic acid is one of the essential vitamins for normal physiological activities of any organism. The present study demonstrates an immunostimulatory effect of vitamin C on the humoral and cell mediated immunity of the bagrid catfish, Mystus gulio, determined using different bacterins of Aeromonas hydrophila. Humoral as well as cell mediated immune responses were elucidated in the vitamin supplemented, vaccinated and unvaccinated groups. The vitamin supplemented lipopolysaccharide (LPS) vaccinated group exhibited greater immune (both humoral and cell mediated) responses than its formalin killed (FK) and heat killed (HK) bacterin vaccinated counterparts. Nevertheless, in the challenge study, the relative percent survival (RPS) was found to be the same for both FK and LPS immunised vitamin treated groups while lower for the HK immunised vitamin treated group.