RESUMEN
Redox-active quinones have been reported to show good potential for biological activities, while efforts are directed to explore the usefulness of these materials further in cancer management. Our previous study demonstrated that theaflavin and theaflavin-gallates (tea-extracted polyphenols) selectively induce apoptosis of tumour cells in vitro, but its concentration for showing half-maximal therapeutic response remains a matter of concern. In this report, we demonstrated that if theaflavin is conjugated with gold nanoparticles (AuNPs) to form a nanoconjugate AuNP@TfQ, its apoptotic ability increases significantly in comparison to the bare theaflavin (Tf). The nanoconjugate is prepared by following a one-step green synthesis ̶ a reaction between HAuCl4 and the aflavin at room temperature. AuNP@TfQ is characterized using particle size analysis, FESEM, UV-vis, FTIR, fluorescence, and X-ray photoelectron spectroscopytechniques. We assume that the enhanced anti-cancer effect of AuNP@TfQ appears due to the facile oxidation of the pristine theaflavin to its quinone derivative on the surface of AuNPs. The presence of quinone motif in AuNP@TfQ induces an increased level of ROS generation probably through the depolarization of mitochondria and resulted in the caspase-mediated apoptotic cell death which may hold the potential for a "magic bullet"-mediated ovarian cancer treatment.
Asunto(s)
Biflavonoides/farmacología , Catequina/farmacología , Oro/farmacología , Nanopartículas del Metal/química , Neoplasias Ováricas/patología , Apoptosis/efectos de los fármacos , Biflavonoides/síntesis química , Biflavonoides/química , Biomarcadores de Tumor/metabolismo , Catequina/síntesis química , Catequina/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Endocitosis/efectos de los fármacos , Femenino , Hemólisis/efectos de los fármacos , Humanos , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Espectroscopía de Fotoelectrones , Especies Reactivas de Oxígeno/metabolismoRESUMEN
Murraya koenigii (Mk) leaves possess a hypoglycemic effect. Activity of paraoxonase 1 (PON1), a HDL-associated antioxidant enzyme, was found to be decreased during hyperglycemia. The present study explored the effect of Murraya koenigii leaves (MkL) on paraoxonase 1 activity in order to control the oxidative stress in diabetes. Hyperglycemia was induced in mice by a single dose of streptozotocin (200 mg kg(-1) body weight). Diabetic mice were treated with the aqueous extract of MkL orally once daily for 15 days. Doses of 75 and 150 mg kg(-1) body weight of the aqueous MkL extract decreased the blood sugar level significantly in a dose dependant manner. MkL administration significantly reduced oxidative stress by decreasing the MDA level and by increasing GSH level, SOD as well as catalase activity. However, PON1 activity was found to be increased after administration of aqueous MkL extract. MkL treatment also possesses a hypolipidemic effect as inferred from the decrease in total cholesterol, triglyceride level and increase in HDL-C concentration. Here we conclude that after MkL treatment, not only the antioxidant parameters like SOD, CAT, GSH and MDA, but also PON1 may be involved in decreasing the oxidative stress associated with diabetes.
Asunto(s)
Arildialquilfosfatasa/genética , Diabetes Mellitus Experimental/tratamiento farmacológico , Murraya/química , Fitoterapia , Extractos Vegetales/farmacología , Hojas de la Planta/química , Animales , Antioxidantes/farmacología , Arildialquilfosfatasa/metabolismo , Glucemia/efectos de los fármacos , Peso Corporal/efectos de los fármacos , Catalasa/sangre , Colesterol/sangre , Diabetes Mellitus Experimental/sangre , Glutatión/sangre , Hiperglucemia/tratamiento farmacológico , Hipoglucemiantes/farmacología , Insulina/sangre , Ratones , Estrés Oxidativo/efectos de los fármacos , Superóxido Dismutasa/sangre , Triglicéridos/sangreRESUMEN
The ability of ethanol extract of Phyllanthus amarus root (EEPA) to decrease bilirubin level and oxidative stress in phenylhydrazine-induced neonatal jaundice in mice was investigated. Administration of phenylhydrazine (75 mg/kg b.w.) significantly elevated total and unconjugated serum bilirubin level compared to control mice. EEPA (5, 10, and 20 mg/kg b.w., oral) dose-dependently reduced the bilirubin level. EEPA treatment also upregulated hepatic CAR and CYP3A1, accounting for its ability to facilitate bilirubin clearance. A single dose of EEPA (20 mg/kg b.w.) induced higher level of bilirubin clearance than phototherapy, widely used for treating neonatal jaundice. Furthermore, phenylhydrazine administration significantly increased MDA, protein carbonyl, and total thiol content and lowered the GSH level along with superoxide dismutase and catalase activity in erythrocyte compared to the control group. Single administration of EEPA (20 mg/kg b.w.) significantly reversed the trend. Presence of gallic acid, gentisic acid, and ortho-coumaric acid in EEPA was identified by HPLC analysis. Amongst these, the major phenolic constituent, gallic acid, exhibited significant bilirubin-lowering effect. These results suggested that P. amarus may be beneficial in reducing bilirubin level as well as oxidative stress in neonatal jaundice.
Asunto(s)
Bilirrubina/sangre , Ictericia Neonatal/tratamiento farmacológico , Phyllanthus/química , Fitoterapia , Extractos Vegetales/farmacología , Raíces de Plantas/química , Administración Oral , Animales , Catalasa/metabolismo , Receptor de Androstano Constitutivo , Citocromo P-450 CYP3A/metabolismo , Relación Dosis-Respuesta a Droga , Etanol , Glutatión/metabolismo , Humanos , Recién Nacido , Ictericia Neonatal/sangre , Ictericia Neonatal/inducido químicamente , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Ratones , Estrés Oxidativo/efectos de los fármacos , Fenilhidrazinas , Receptores Citoplasmáticos y Nucleares/metabolismo , Superóxido Dismutasa/metabolismo , Regulación hacia ArribaRESUMEN
The antioxidant property of the 70% aqueous ethanol extract of Phyllanthus amarus roots and its ether-soluble, ethyl acetate-soluble, and aqueous fractions were investigated by various in vitro assays. The root extracts showed higher DPPH, hydroxyl, superoxide, and nitric oxide radical scavenging and reducing power activity. Among all the samples, the ethyl acetate-soluble fraction demonstrated highest radical scavenging activity and total phenolics content. Twenty-eight different phenolic compounds were identified by LCMS/MS analysis of the ethyl acetate-soluble fraction. The majority of the compounds were found to exist as their glycosides, and many of these were gallic acid derivatives. Free epicatechin and gallic acid were also identified in the ethyl acetate-soluble fraction. The present investigation suggested that P. amarus root is a potent antioxidant and can be used for the prevention of diseases related to oxidative stress.
Asunto(s)
Antioxidantes/análisis , Fenoles/análisis , Phyllanthus/química , Raíces de Plantas/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Catequina/análisis , Catequina/química , Catequina/aislamiento & purificación , Depuradores de Radicales Libres/análisis , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Ácido Gálico/análisis , Ácido Gálico/química , Ácido Gálico/aislamiento & purificación , India , Fenoles/química , Fenoles/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificaciónRESUMEN
AIM OF THE STUDY: We sought to determine the efficacy as antioxidant and safety profile of the polyherbal formulation in geriatric patients of eastern India. MATERIALS AND METHODS: The study was double-blind, randomized including placebo controlled and was approved by the ethical committee of SSKM hospital. Geriatric patients attending the OPD (outpatient department) of SSKM hospital formed the study group. The patients were randomized to receive either the polyherbal formulation or the identical-looking placebo at a dose of 2 tablets twice daily for a period of 6 months. Follow-up of patient status was done monthly. The clinical parameters were assessed before and after 6 months of medication or placebo intake. RESULTS: The results showed that significant rejuvenation of the anti-oxidant property which is determined by the enzymatic and non enzymatic anti oxidants, superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, reduced glutathione and malondialdehyde in the geriatric patients were seen in patients treated with Geriforte tablets as compared to patients treated with placebo and control group. There were no significant adverse effects experienced by cases in any group. CONCLUSION: Polyherbal formulation is effective in rejuvenating geriatric age group compared to the placebo. This formulation is safe and compliance to the treatment was good. In ancient Ayurveda the constituents of polyherbal formulation were prescribed for different diseases including cardiological, neurological, sepsis, etc.
Asunto(s)
Antioxidantes/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Estrés Fisiológico/efectos de los fármacos , Adulto , Anciano , Antioxidantes/administración & dosificación , Antioxidantes/metabolismo , Método Doble Ciego , Combinación de Medicamentos , Femenino , Humanos , Magnoliopsida , Masculino , Malondialdehído/sangre , Persona de Mediana Edad , Extractos Vegetales/administración & dosificación , Adulto JovenRESUMEN
The ability of ethanol extract of Phyllanthus amarus root (EEPA) to decrease bilirubin level and oxidative stress in phenylhydrazine-induced neonatal jaundice in mice was investigated. Administration of phenylhydrazine (75 mg/kg b.w.) significantly elevated total and unconjugated serum bilirubin level compared to control mice. EEPA (5, 10, and 20 mg/kg b.w., oral) dose-dependently reduced the bilirubin level. EEPA treatment also upregulated hepatic CAR and CYP3A1, accounting for its ability to facilitate bilirubin clearance. A single dose of EEPA (20 mg/kg b.w.) induced higher level of bilirubin clearance than phototherapy, widely used for treating neonatal jaundice. Furthermore, phenylhydrazine administration significantly increased MDA, protein carbonyl, and total thiol content and lowered the GSH level along with superoxide dismutase and catalase activity in erythrocyte compared to the control group. Single administration of EEPA (20 mg/kg b.w.) significantly reversed the trend. Presence of gallic acid, gentisic acid, and ortho-coumaric acid in EEPA was identified by HPLC analysis. Amongst these, the major phenolic constituent, gallic acid, exhibited significant bilirubin-lowering effect. These results suggested that P. amarus may be beneficial in reducing bilirubin level as well as oxidative stress in neonatal jaundice (AU)