RESUMEN
Tea (Camellia sinensis) has several reported health benefits, including that on bone health attributed to catechins of which the most abundant is epigallocatechin-3-gallate (EGCG). However, several preclinical and clinical studies raise safety concerns about EGCG in tea extract causing acute liver failure. Tea also contains kaempferol, albeit scanty, and it has hepatoprotective and osteogenic effects. Here, we utilized a novel extraction procedure of acid hydrolysis to enhance the osteogenic effect of tea extract while reducing its hepatotoxicity. The resultant extract (USKECSE) has a ~40-fold increase in kaempferol and a 2.5-fold reduction in EGCG content compared with the hydroethanolic extract (USCSE). In a female Sprague Dawley (SD) rat femur osteotomy model, USKECSE (100 mg/kg) but not USCSE promoted bone regeneration. In a rat postmenopausal osteoporosis model induced by bilateral ovariectomy (OVX), USKECSE through an osteogenic mechanism maintained bone mass, strength, and microarchitecture to the levels of ovary-intact rats with no hepatotoxic effect. After a single oral dose (100 mg/kg) of USKECSE to adult rats, kaempferol was detectable for 48 hours, suggesting its significant absorption and distribution in plasma. Peak kaempferol concentration in plasma (Cmax) was 483 ng/ml (2 µM), and at this concentration, kaempferol induces osteoblast differentiation. USKECSE had no genotoxicity, and its safety index assessed by preclinical toxicity studies, including safety pharmacology, was >20-fold. Taken together, we report a novel extraction process that enhanced the osteogenicity and concomitantly reduced hepatotoxicity of tea extract with significant kaempferol bioavailability and a favorable systemic safety profile. Based on these data, we propose assessing the USKECSE effect for postmenopausal osteoporosis treatment.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Osteoporosis Posmenopáusica , Osteoporosis , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Femenino , Humanos , Quempferoles/farmacología , Quempferoles/uso terapéutico , Osteoporosis/tratamiento farmacológico , Osteoporosis Posmenopáusica/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Sprague-Dawley , TéRESUMEN
The antibacterial property of Rumex nepalensis Spreng. was evaluated against some strains of bacteria. The methanol extract of the roots (tested at 200-1000 micro g/disc) showed significant concentration-dependent antibacterial activity.
Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Extractos Vegetales/farmacología , Rumex , Antibacterianos/administración & dosificación , Bacillus subtilis/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/administración & dosificación , Shigella dysenteriae/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Vibrio cholerae/efectos de los fármacosRESUMEN
The antidiarrhoeal activity of the methanol extract of the dried seeds of Strychnos potatorum (MESP) has been evaluated out in rats using different models (castor oil-induced diarrhoea, effects on gastrointestinal motility and on PGE(2)-induced gastric enteropooling. MESP (100, 200 and 400 mg/kg, p.o.) significantly (P<0.001) inhibited the frequency of defaecation and reduced the wetness of faecal droppings in castor oil-induced diarrhoea, decreased the propulsion of charcoal meal through the gastrointestinal tract, and also reduced the PGE(2)-induced enteropooling.