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INTRODUCTION: Health-related quality of life (HRQOL) in human immunodeficiency virus (HIV)-positive individuals is substantially challenged due to disease, opportunistic infections, lifelong commitment, and tolerability to antiretroviral therapy (ART) and various social, physical, and psychological domains. AIM: This study was conducted to assess the magnitude of the impact on HRQOL in HIV-positive people from early access to ART. SETTINGS AND DESIGN: This was a randomized, prospective, open-label study, conducted at the ART center attached to the Government Medical College, Amritsar. SUBJECTS AND METHODS: This study comprised 240 HIV-infected adults in the age group >18 years who presented to the ART center. Approval from the Institutional Ethics Committee was obtained. Informed consent was taken from all the enrolled participants after explaining the study therapy and its benefits and side effects. Patients who presented early in their course of disease and had baseline CD4 count ≥350/mm3 were recruited in early arm and those with <350/mm3 or the development of symptomatic HIV-related disease in the late arm. Following stratification, both groups were 1:1 randomized by permuted block randomization. The primary objective was to assess HRQOL using the World Health Organization Quality of Life-HIV brief instrument (WHOQOL-HIV). STATISTICAL ANALYSIS USED: The summary domain and total HRQOL scores were calculated using method developed by the WHOQOL-HIV group. Unpaired t-test was applied for statistical analysis, with level of significance expressed as P < 0.05. RESULTS: Out of the total 240 HIV-positive patients, 120 who met eligibility criteria were recruited for the final analysis. There was a significant difference between HRQOL score of Physical domains and Psychological domains, between early and late arms at baseline and at the end of 9 months. CONCLUSIONS: Quality of life is an important holistic measure for assessing the health of people living with HIV/AIDS.
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OBJECTIVES: In this retrospective study, we evaluated the diagnostic accuracy of molecular tests (MT) for the detection of DR-TB, compared to the gold standard liquid-based drug susceptibility testing (DST) in Karakalpakstan. METHODS: A total of 6670 specimens received in the Republican TB No 1 Hospital Laboratory of Karakalpakstan between January and July 2017 from new and retreatment patients were analysed. Samples were tested using Xpert MTB/RIF and line probe assays (LPA) for the detection of mutations associated with resistance. The sensitivity and specificity of MTs were calculated relative to results based on DST. RESULTS: The accuracy of MT for detection of rifampicin resistance was high, with sensitivity and specificity over 98%. However, we observed reduced sensitivity of LPA for detection of resistance; 86% for isoniazid (95% CI 82-90%), 86% for fluoroquinolones (95% CI 68-96%), 70% for capreomycin (95% CI 46-88%) and 23% for kanamycin (95% CI 13-35%). CONCLUSIONS: We show that MTs are a useful tool for rapid and safe diagnosis of DR-TB; however, clinicians should be aware of their limitations. Although detection of rifampicin resistance was highly accurate, our data suggest that resistance mutations circulating in the Republic of Karakalpakstan for other drugs were not detected by the methods used here. This merits further investigation.
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Antibióticos Antituberculosos/uso terapéutico , Farmacorresistencia Bacteriana , Pruebas de Sensibilidad Microbiana/métodos , Mycobacterium tuberculosis/crecimiento & desarrollo , Tuberculosis/tratamiento farmacológico , Capreomicina/uso terapéutico , Fluoroquinolonas/uso terapéutico , Humanos , Isoniazida/uso terapéutico , Kanamicina/uso terapéutico , Mutación , Mycobacterium tuberculosis/genética , Reacción en Cadena de la Polimerasa , Reproducibilidad de los Resultados , Estudios Retrospectivos , Rifampin/uso terapéutico , Tuberculosis/microbiología , Tuberculosis Resistente a Múltiples Medicamentos/tratamiento farmacológico , Tuberculosis Resistente a Múltiples Medicamentos/microbiología , Tuberculosis Pulmonar/tratamiento farmacológico , Tuberculosis Pulmonar/microbiología , UzbekistánRESUMEN
The screening of aqueous extract of Clerodendrum serratum revealed its broad-spectrum antimicrobial potential against Gram positive, Gram negative bacteria, and yeast. Optimizing the extraction strategies, revealed 15% concentration of aqueous extract prepared at 40 °C by extracting for 40 min, as optimum parameters and its statistical optimization by Box-Behnken design led to 1.16-1.35 folds enhancement in activity. Organic solvent extraction further improved the activity where methanol proved to be the best organic extractant which was effective against all the 13 pathogens tested with inhibition zone ranging from 14 to 32 mm. Minimum Inhibitory Concentration (MIC) study endorsed the methanolic extract to be the best organic extractant, as it showed the lowest MIC (0.5-10 mg/ml) in comparison to aqueous extract (1-10 mg/ml) as well as Partially Purified Phytoconstituents i.e., flavonoids (1-5 mg/ml), diterpenes (5-10 mg/ml) and cardiac glycosides (5-10 mg/ml). All these were found to be biosafe in both In-vitro (Ames and MTT assay) and In-vivo toxicity studies. Acute oral toxicity testing of flavonoids (2000 mg/ml) on Wistar rats did not reveal any significant change in relative organ weight, biochemical, hematological parameters and organs' architecture in comparison to control. Antiproliferative potential of flavonoids against human cancerous cell lines i.e., HeLa, HCT-15, and U87-MG, further increase the importance of this plant as a promising candidate for drug development. The overall study justified the medicinal importance of this plant.
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Antiinfecciosos , Clerodendrum , Extractos Vegetales , Animales , Antiinfecciosos/uso terapéutico , Antiinfecciosos/toxicidad , Contención de Riesgos Biológicos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/uso terapéutico , Extractos Vegetales/toxicidad , Ratas , Ratas WistarRESUMEN
Pathogenesis of Parkinson's disease (PD) specifically involves the degeneration of dopaminergic neurons in the substantia nigra region, which mainly begun with the overwhelmed oxidative stress and neuroinflammation. Considering the antioxidant and other pharmacological properties, Eclipta alba needs to be exploited for its possible neuroprotective efficacy against PD and other neurological disorders. Therefore, the current study was conducted to exemplify the remedial effects of hydro-alcoholic extract of E. alba (EA-MEx) against MPP+-elicited in vitro and in vivo PD models. SH-SY5Y, a neuroblastoma cell culture and male Wistar rats were used to impersonate the hallmarks of PD. Qualitative and quantitative analyses of EA-MEx revealed the presence of quercetin, ellagic acid, catechin, kaempferol, and epicatechin at varying concentrations. EA-MEx was found to deliver considerable protection against MPP+-induced oxidative damages in SH-SY5Y cells. Furthermore, in vivo study also supported the neuroprotective efficacy of EA-MEx, with significant mitigation of behavioral deficits induced by intrastriatal injection of MPP+. Furthermore, the disturbed levels of cellular antioxidant machinery have been significantly improved with the pre-treatment of EA-MEx. Mechanistically, the expression of α-synuclein, tyrosine hydroxylase, and mortalin were also found to be improved with the prior treatment of EA-MEx. Hence, the study suggests Eclipta alba as a suitable candidate for the development of better neuropathological therapeutics.
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Eclipta , Fármacos Neuroprotectores , Enfermedad de Parkinson , 1-Metil-4-fenilpiridinio/farmacología , Animales , Apoptosis , Línea Celular Tumoral , Masculino , Fármacos Neuroprotectores/farmacología , Enfermedad de Parkinson/tratamiento farmacológico , Extractos Vegetales/farmacología , Ratas , Ratas WistarRESUMEN
Hansen's disease is a chronic infectious granulomatous disease with varied clinical presentation. In the postelimination era, histoid Hansen's disease is an important emerging lepromatous subset known to mimic varied dermatoses, thereby making clinical diagnosis difficult and often delayed. We report two cases of histoid Hansen's disease bereft of clinical cardinal signs of leprosy.
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Enfermedad Granulomatosa Crónica/diagnóstico , Enfermedad Granulomatosa Crónica/microbiología , Lepra/microbiología , Abdomen/microbiología , Abdomen/patología , Adulto , Antituberculosos/uso terapéutico , Enfermedad Granulomatosa Crónica/tratamiento farmacológico , Humanos , Lepra/clasificación , MasculinoRESUMEN
Citrus peel (CP) forms around 40-50% of the total fruit mass but is generally thought to be a waste. However, it is a substantial source of naturally occurring health enhancing compounds, particularly phenolic compounds and carotenoids. Phenolic compounds in CP mainly comprise phenolic acids (primarily caffeic, p-coumaric, ferulic and sinapic acid), flavanones (generally naringin and hesperidin) and polymethoxylated flavones (notably nobiletin and tangeretin). It has also been noted that CP's contain more amounts of these compounds than corresponding edible parts of the fruits. Phenolic compounds present in CP act as antioxidants (by either donation of protons or electrons) and protect cells against free radical damage as well as help in reducing the risk of many chronic diseases. Owing to the more abundance of polyphenols in CP's, their antioxidant activity is also higher than other edible fruit parts. Therefore, peels from citrus fruits can be used as sources of functional compounds and preservatives for the development of newer food products, that are not only safe but also have health-promoting activities. The present review provides in-depth knowledge about the phenolic composition, antioxidant potential and health benefits of CP.
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Antioxidantes/análisis , Citrus/química , Frutas/química , Fenoles/análisis , Disponibilidad Biológica , Ácidos Cumáricos/análisis , Flavanonas , Flavonas/análisis , Hesperidina , Hidroxibenzoatos , Extractos Vegetales/análisis , PolifenolesRESUMEN
Plants have been the basis of traditional medicine since the dawn of civilizations. Different plant parts possess various phytochemicals, playing important roles in preventing and curing diseases. Scientists, through extensive experimental studies, are playing an important part in establishing the use of phytochemicals in medicine. However, there are still a large number of medicinal plants which need to be studied for their phytochemical profile. In this study, the objective was to isolate phytochemicals from bark of Bauhinia variegata L. and to study them for their antioxidant and cytotoxic activities. The bark was extracted with methanol, followed by column chromatography and thus isolating kaempferol, stigmasterol, protocatechuic acid-methyl ester (PCA-ME) and protocatechuic acid (PCA). 2,2-azinobis-3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) and 2, 2'-diphenyl-1-picrylhydrazyl radical (DPPH) radical scavenging assays were utilized for assessment of antioxidant activity, and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye reduction assay was used to determine cytotoxic activity against C-6 glioma rat brain, MCF-7 breast cancer, and HCT-15 colon cancer cell lines. The compounds were found to have significant antioxidant and cytotoxic activity. Since there is a considerable increase in characterizing novel chemical compounds from plant parts, the present study might be helpful for chemotaxonomic determinations, for understanding of medicinal properties as well as for the quality assessment of herbal supplements containing B. variegata bark, thus establishing its use in traditional medicine.
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ETHNOPHARMACOLOGICAL RELEVANCE: The neem tree (Azadirachta indica A.Juss), of the Meliaceae family, has been used in India for millennia in traditional medicine. Parts of the tree are used to treat problems with the gastrointestinal tract, urinary tract, and hair; to combat infections of smallpox and plasmodium; and to treat ulcers, diabetes, blood pressure, headache, and heartburn. Natural products and extracts from the tree have been reported to have antimicrobial, antifungal, and antiparasitic activities. AIM OF THE STUDY: Antibiotic resistance in the gastric pathogen Helicobacter pylori is increasing, and novel therapeutics to eradicate this bacterium are needed. Given the growing interest in the use of natural products as antimicrobials, this study was designed to examine the bactericidal effects of an extract of neem oil against H. pylori. MATERIALS AND METHODS: Neem oil was obtained from a commercial source and subjected to liquid-liquid extraction with diethyl ether and aqueous methanol; the methanol-soluble fraction was retained. The minimum inhibitory (MIC) and bactericidal (MBC) concentrations were determined against nine strains of H. pylori. Additionally, specific properties of the extract were characterized using H. pylori strain G27: bactericidal kinetics, reversibility, and effectiveness under growth arrest conditions and at low pH. The hemolytic activity of the extract was measured in vitro. RESULTS: The MIC and MBC of the extract against the H. pylori strains were between 25 and 51⯵g/mL and 43-68⯵g/mL, respectively. The bactericidal activity was time- and concentration-dependent, and at the highest concentrations (75-105⯵g/mL), no detectable bacteria were present by 6â¯h. The activity of the extract was reversible, independent of H. pylori growth, and increased at low pH. The extract exhibited no appreciable hemolytic activity. CONCLUSIONS: Neem oil extract has significant bactericidal activity against H. pylori. The extract has several favorable pharmacological properties, including ability to kill non-growing bacteria, increased activity at low pH, and no hemolytic activity. The compound(s) present in the extract could potentially be used as a future treatment for H. pylori infection.
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Antibacterianos/farmacología , Glicéridos/farmacología , Helicobacter pylori/efectos de los fármacos , Terpenos/farmacología , Animales , Eritrocitos/efectos de los fármacos , Helicobacter pylori/crecimiento & desarrollo , Caballos , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad MicrobianaRESUMEN
Legumes are a good source of bioactive phenolic compounds which play significant roles in many physiological as well as metabolic processes. Phenolic acids, flavonoids and condensed tannins are the primary phenolic compounds that are present in legume seeds. Majority of the phenolic compounds are present in the legume seed coats. The seed coat of legume seeds primarily contains phenolic acids and flavonoids (mainly catechins and procyanidins). Gallic and protocatechuic acids are common in kidney bean and mung bean. Catechins and procyanidins represent almost 70% of total phenolic compounds in lentils and cranberry beans (seed coat). The antioxidant activity of phenolic compounds is in direct relation with their chemical structures such as number as well as position of the hydroxyl groups. Processing mostly leads to the reduction of phenolic compounds in legumes owing to chemical rearrangements. Phenolic content also decreases due to leaching of water-soluble phenolic compounds into the cooking water. The health benefits of phenolic compounds include acting as anticarcinogenic, anti-thrombotic, anti-ulcer, anti-artherogenic, anti-allergenic, anti-inflammatory, antioxidant, immunemodulating, anti-microbial, cardioprotective and analgesic agents. This review provides comprehensive information of phenolic compounds identified in grain legume seeds along with discussing their antioxidant and health promoting activities.
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Antioxidantes/análisis , Grano Comestible/química , Fenoles/análisis , Semillas/química , Antocianinas/análisis , Catequina/análisis , Flavanonas/análisis , Flavonas/análisis , Flavonoides/análisis , Flavonoles/análisis , Hidroxibenzoatos/análisis , Phaseolus/química , Extractos Vegetales/análisis , Proantocianidinas/análisis , Taninos/química , Vaccinium macrocarpon/químicaRESUMEN
In view of developing effective xanthine oxidase (XO) enzyme inhibitors, a series of 100 pyrano[3,2-d]pyrimidine derivatives was synthesized and evaluated for its in vitro XO enzyme inhibition. Structure activity relationship has also been established. Among all the synthesized compounds, 4d, 8d and 9d were found to be the most potent enzyme inhibitors with IC50 values of 8µM, 8.5µM and 7µM, respectively. Compound 9d was further investigated in enzyme kinetic studies and the Lineweaver-Burk plot revealed that the compound 9d was mixed type inhibitor. Molecular properties of the most potent compounds 4d, 8d and 9d, have also been calculated. Docking study was performed to investigate the recognition pattern between xanthine oxidase and the most potent XO inhibitor, 9d. The study suggests that 9d may block the activity of XO sufficiently enough to prevent the substrate from binding to its active site.
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Inhibidores Enzimáticos/farmacología , Simulación del Acoplamiento Molecular , Piranos/farmacología , Pirimidinas/farmacología , Xantina Oxidasa/antagonistas & inhibidores , Animales , Bovinos , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Leche/enzimología , Estructura Molecular , Piranos/síntesis química , Piranos/química , Pirimidinas/síntesis química , Pirimidinas/química , Relación Estructura-Actividad , Xantina Oxidasa/metabolismoRESUMEN
Neurodegenerative diseases are the consequences of imbalance between the production of oxidative stress and its nullification by cellular defense mechanisms. Hydrogen peroxide (H2O2), a precursor of deleterious reactive oxygen species, elicits oxidative stress, resulting in severe brain injuries. Bacopa monnieri is well known for its nerve relaxing and memory enhancing properties. The present study was designed to evaluate the protective effects of extracts from Bacopa monnieri against H2O2 induced oxidative stress using a cellular model, neuroblastoma IMR32 cell line. The protective potential of methanolic, ethanolic, and water extracts of B. monnieri (BM-MEx, BM-EEx, and BM-WEx) was evaluated using MTT assay. Although, all the B. monnieri extracts were found to protect cells against H2O2-mediated stress but BM-MEx showed significantly greater protection. UPLC analysis of BM-MEx revealed various polyphenols, including quercetin, catechin, umbelliferone, and caffeic acid predominance. Further, BM-MEx was found to possess considerable greater neuroprotective potential in comparison to the standard polyphenols such as quercetin, catechin, umbelliferone, and caffeic acid. The levels of antioxidant enzymes were significantly elevated after the pretreatment of BM-MEx and quercetin. The expression levels of oxidative stress markers, such as NF200, HSP70, and mortalin, were significantly alleviated after the pretreatment of BM-MEx as shown by immunofluorescence and RT-PCR. In conclusion, the present study demonstrated the protective effects of BM-MEx, suggesting that it could be a candidate for the development of neuropathological therapeutics.
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Antioxidantes/farmacología , Bacopa/química , Fármacos Neuroprotectores/farmacología , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Polifenoles/farmacología , Antioxidantes/metabolismo , Línea Celular , Humanos , Peróxido de Hidrógeno , Neuroblastoma , Enfermedades Neurodegenerativas/metabolismo , Polifenoles/análisis , Especies Reactivas de Oxígeno/metabolismoRESUMEN
Nicotinamide adenine dinucleotide (NAD) is an essential co-factor in glycolysis and is a key molecule involved in maintaining cellular energy metabolism. Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step of an important salvage pathway in which nicotinamide is recycled into NAD. NAMPT is up-regulated in many types of cancer and NAMPT inhibitors (NAMPTi) have potential therapeutic benefit in cancer by impairing tumor metabolism. Clinical trials with NAMPTi APO-866 and GMX-1778, however, failed to reach projected efficacious exposures due to dose-limiting thrombocytopenia. We evaluated preclinical models for thrombocytopenia that could be used in candidate drug selection and risk mitigation strategies for NAMPTi-related toxicity. Rats treated with a suite of structurally diverse and potent NAMPTi at maximum tolerated doses had decreased reticulocyte and lymphocyte counts, but no thrombocytopenia. We therefore evaluated and qualified a human colony forming unit-megakaryocyte (CFU-MK) as in vitro predictive model of NAMPTi-induced MK toxicity and thrombocytopenia. We further demonstrate that the MK toxicity is on-target based on the evidence that nicotinic acid (NA), which is converted to NAD via a NAMPT-independent pathway, can mitigate NAMPTi toxicity to human CFU-MK in vitro and was also protective for the hematotoxicity in rats in vivo. Finally, assessment of CFU-MK and human platelet bioenergetics and function show that NAMPTi was toxic to MK and not platelets, which is consistent with the clinically observed time-course of thrombocytopenia.
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Antineoplásicos/efectos adversos , Inhibidores Enzimáticos/efectos adversos , Hematopoyesis/efectos de los fármacos , Megacariocitos/efectos de los fármacos , Niacina/metabolismo , Nicotinamida Fosforribosiltransferasa/antagonistas & inhibidores , Trombocitopenia/inducido químicamente , Animales , Antineoplásicos/química , Plaquetas/efectos de los fármacos , Plaquetas/metabolismo , Células Cultivadas , Ensayo de Unidades Formadoras de Colonias , Suplementos Dietéticos , Evaluación Preclínica de Medicamentos , Inhibidores Enzimáticos/química , Interacciones Alimento-Droga , Humanos , Leucocitos Mononucleares/citología , Leucocitos Mononucleares/efectos de los fármacos , Leucocitos Mononucleares/metabolismo , Leucocitos Mononucleares/patología , Macaca fascicularis , Masculino , Megacariocitos/citología , Megacariocitos/metabolismo , Megacariocitos/patología , Ratones , Estructura Molecular , Niacina/uso terapéutico , Nicotinamida Fosforribosiltransferasa/genética , Nicotinamida Fosforribosiltransferasa/metabolismo , Pentosiltransferasa/genética , Pentosiltransferasa/metabolismo , Ratas Sprague-Dawley , Trombocitopenia/metabolismo , Trombocitopenia/prevención & controlRESUMEN
Diabetic nephropathy (DN) has a complex pathogenesis and poor prognosis due to the lack of therapeutic interventions. The present study investigates the effect of A. marmelos leaf extract (AME) on early alloxan induced DN. The treatment with AME was found to significantly decrease the fasting blood sugar, total cholesterol, blood urea, creatinine and renal TBARS and increased the levels of renal reduced glutathione and catalase significantly as compared to the diabetic control group. The maximum dose-dependent protection was observed at a dose of 200 mg kg(-1). Histological examination revealed marked reversal of the morphological derangements with AME treatment as indicated by a decrease in glomerular expansion, tubular dilatation and inflammatory cells. The present results conclude that AME treatment has a significant ameliorative effect on early changes induced in the kidneys by alloxan and improves the outcome of DN.
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Aegle/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Nefropatías Diabéticas/tratamiento farmacológico , Hipoglucemiantes/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Aloxano , Animales , Glucemia/análisis , Catalasa/metabolismo , Nefropatías Diabéticas/inducido químicamente , Femenino , Glutatión/metabolismo , Riñón/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Masculino , Hojas de la Planta/química , Ratas , Ratas Wistar , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismoRESUMEN
Oxidative stress has been implicated as an important factor in the process of neurodegeneration and hydrogen peroxide (H2O2) is one of the most important precursors of reactive oxygen species (ROS), responsible for many neurodegenerative diseases. This study used extracts from Nardostachys jatamansi rhizomes, known for nerve relaxing properties in Ayurvedic medicine, to ascertain their protective role in H2O2-induced oxidative stress in C6 glioma cells. The protective effect of methanolic, ethanolic and water extracts of N. jatamansi (NJ-MEx, NJ-EEx and NJ-WEx respectively) was determined by MTT assay. NJ-MEx significantly protected against H2O2 cytotoxicity when cells were pretreated for 24 h. The level of antioxidant enzymes, catalase, superoxide dismutase (Cu-ZnSOD), glutathione peroxidase (GPx), and a direct scavenger of free radicals, glutathione (GSH), significantly increased following pre-treatment with NJ-MEx. Lipid peroxidation (LPx) significantly decreased in NJ-MEx-pretreated cultures. The expression of a C6 differentiation marker, GFAP (glial fibrillary acidic protein), stress markers HSP70 (heat shock protein) and mortalin (also called glucose regulated protein 75, Grp75) significantly decreased when cells were pre-treated with NJ-MEx before being subjected to H2O2 treatment as shown by immunofluorescence, western blotting and RT-PCR results. The present study suggests that NJ-MEx could serve as a potential treatment and/or preventive measure against neurodegenerative diseases.
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Antioxidantes/farmacología , Nardostachys , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Antioxidantes/aislamiento & purificación , Western Blotting , Línea Celular Tumoral , Citoprotección/efectos de los fármacos , Peróxido de Hidrógeno/química , Inmunohistoquímica , Metanol/química , Nardostachys/química , Neoplasias/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Reacción en Cadena de la Polimerasa , Ratas , Rizoma/químicaRESUMEN
OBJECTIVE: The pathogenesis of diabetic cardiomyopathy (DCM) is complex, and the therapeutic options available to treat DCM are limited. The present study was designed to investigate the effect of Aegle marmelos (L.) Correa (Rutaceae) leaf extract on early stage DCM in alloxan-induced diabetic rats. METHODS: Diabetes was induced in Wistar rats (150-200 g) by injecting alloxan (150 mg kg(-1); i.p.). Ethanol extract of A. marmelos leaves was administered at varying doses (100, 200, and 400 mg kg(-1)) and tolbutamide (100 mg kg(-1)) as standard. Fasting blood glucose (FBG), total cholesterol, thiobarbituric acid reactive substances (TBARS), reduced glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), lactate dehydrogenase (LDH) and creatine kinase (CK) were determined by standard methods. RESULTS: A. marmelos extract (AME) was found to decrease the levels of FBG, total cholesterol, TBARS, LDH and CK, and increase the levels of GSH, CAT and SOD dose dependently as compared to diabetic control groups. The maximum dose-dependent decrease in TBARS (63.46%), LDH (34.04%), CK (53.14%), and increase in GSH (64.91%), CAT (59.34%), SOD (69.65%) was evident at an optimum dose of 200 mg kg(-1). Histopathological studies revealed salvage in the morphological derangements as indicated by absence of necrosis and marked decrease in inflammatory cells in AME-treated groups as compared to diabetic control. CONCLUSIONS: The present investigations conclude that treatment with AME attenuates the severity and improves the myocardium in the early stages of alloxan-induced DCM at a dose of 200 mg kg(-1).
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Aegle , Antioxidantes/farmacología , Diabetes Mellitus Experimental/tratamiento farmacológico , Cardiomiopatías Diabéticas/prevención & control , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Aegle/química , Animales , Antioxidantes/aislamiento & purificación , Glucemia/efectos de los fármacos , Glucemia/metabolismo , Catalasa/metabolismo , Colesterol/sangre , Creatina Quinasa/metabolismo , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/complicaciones , Cardiomiopatías Diabéticas/sangre , Cardiomiopatías Diabéticas/etiología , Cardiomiopatías Diabéticas/patología , Relación Dosis-Respuesta a Droga , Etanol/química , Femenino , Glutatión/metabolismo , Hipoglucemiantes/aislamiento & purificación , L-Lactato Deshidrogenasa/metabolismo , Masculino , Miocardio/metabolismo , Miocardio/patología , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta , Plantas Medicinales , Ratas , Ratas Wistar , Solventes/química , Superóxido Dismutasa/metabolismo , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo , Factores de TiempoRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Eclipta alba is traditionally used as hepatoprotective agent. The study was designed to explore its antiproliferative activity on liver and other related cancer. AIM OF THE STUDY: The present study was designed to assess and establish the role of Eclipta alba as anti-cancer agent using HepG2, C6 glioma and A498 cell lines as model system. MATERIALS AND METHODS: Antiproliferative and cytotoxic effects of the Eclipta alba hydroalcoholic extract (EAE) was determined using MTT assay. The expression level of NF-kB was analysed by western blotting and RT PCR. Gelatin zymography was done for gelatinase matrix metalloproteinases (MMP-2 and 9) analysis. RESULTS: EAE inhibited the cell proliferation in dose dependent manner in HepG2, A498 and C6 glioma cell lines with an IC50 of 22±2.9, 25±3.6 and 50±8.7 µg/ml, respectively. The expression of MMP (2 and 9) was down-regulated with EAE treatment. DNA damage was observed following 72h of extract treatment, leading to apoptosis. Additionally, the expression level of NF-kB was evaluated with western blotting and RT-PCR and was found to be down-regulated/inactivated. CONCLUSIONS: The data establish the existence of anti-proliferative, DNA damaging and anti-metastasis properties in EAE which is yet unexplored and hold high therapeutic impact.
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Antineoplásicos Fitogénicos/uso terapéutico , Eclipta , Neoplasias/tratamiento farmacológico , Fitoterapia , Extractos Vegetales/uso terapéutico , Antineoplásicos Fitogénicos/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Daño del ADN , Regulación hacia Abajo , Glioma/tratamiento farmacológico , Glioma/metabolismo , Células Hep G2 , Hepatoblastoma/tratamiento farmacológico , Hepatoblastoma/metabolismo , Humanos , Concentración 50 Inhibidora , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/metabolismo , Metaloproteinasas de la Matriz/metabolismo , FN-kappa B/metabolismo , Neoplasias/metabolismo , Extractos Vegetales/farmacología , Hojas de la PlantaRESUMEN
Three monomeric monocot lectins from Zephyranthes carinata, Zephyranthes candida, and Gloriosa superba with carbohydrate specificity towards mannose derivatives and (or) oligomannose have been isolated and purified from their storage tissues. The lectins were purified by anion-exchange chromatography on DEAE-Sephacyl and by gel filtration chromatography on Biogel P-200 followed by high-performance liquid chromatography. The purified lectins, Z. carinata, Z. candida, and G. superba had molecular masses of 12, 11.5, and 12.5 kDa, respectively, as determined by gel filtration and SDS-PAGE, indicating that they are monomers. In a hapten inhibition assay, methyl-alpha-D-mannopyranoside inhibited agglutination of both Z. candida and Z. carinata; the latter was also inhibited by Man(alpha1-2)Man and Man(alpha1-3)Man. Gloriosa superba showed inhibition only with Man(alpha1-4)Man of all of the sugars and glycoproteins tested. All purified lectins agglutinated red blood cells from rabbit, whereas G. superba was also reactive towards erythrocytes from guinea pig. All of the lectins were nonglycosylated and did not require metal ions for their activity. They were labile above 60 degrees C and were affected by denaturing agents such as urea, thiourea, and guanidine-HCl. The lectins were virtually nonmitogenic, like other members of Amaryllidaceae and Liliaceae. Of the 3 lectins, G. superba was found to be highly toxic to the BSC-1 cell line (African green monkey kidney epithelial cells), while both of the Zephyranthes species showed significant in vitro inhibition of poxvirus replication in BSC-1 cells without any toxic effects to the cells. In addition, Z. candida also exhibited significant anticancer activity against SNB-78, a CNS human cancer cell line.
Asunto(s)
Antivirales/farmacología , Liliaceae/química , Lectinas de Unión a Manosa/farmacología , Lectinas de Plantas/farmacología , Poxviridae/efectos de los fármacos , Replicación Viral/fisiología , Animales , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Antivirales/química , Antivirales/aislamiento & purificación , Línea Celular , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Agregación Eritrocitaria/efectos de los fármacos , Glicosilación , Cobayas , Humanos , Lectinas de Unión a Manosa/química , Lectinas de Unión a Manosa/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Lectinas de Plantas/química , Lectinas de Plantas/aislamiento & purificación , Poxviridae/fisiología , Conejos , Replicación Viral/efectos de los fármacosRESUMEN
A lectin from the seeds of Amaranthus viridis Linn has been purified by affinity chromatography on asialofetuin-linked amino activated silica. Amaranthus viridis lectin (AVL) has a native molecular mass of 67 kDa. It is a homodimer composed of two 36.6 kDa subunits. The lectin gave a single band in non-denaturing PAGE at pH 4.5 and pH 8.3 and a single peak on HPLC size exclusion and cation exchange columns. The purified lectin was specific for both T-antigen and N-acetyl-D-lactosamine, markers for various carcinomas, in addition to N-acetyl-D-galactosamine, asialofetuin and fetuin. This lectin reacted strongly with red blood cells (RBCs) from human ABO blood groups and rat. It also reacted with rabbit, sheep, goat and guinea pig RBCs. The lectin is a glycoprotein having no metal ion requirement for its activity. Denaturing agents such as urea, thiourea and guanidine-HCl had no effect on its activity when treated for 15 minutes. AVL showed significant antiproliferative activity towards HB98 and P388D1 murine cancer cell lines. It also exerted antifungal activity against phytopathogenic fungi Botrytis cincerea and Fusarium oxysporum but not against Rhizoctonia solani, Trichoderma reesei, Alternaria solani and Fusarium graminearum.
Asunto(s)
Amaranthus/química , Antifúngicos/farmacología , Proliferación Celular/efectos de los fármacos , Extractos Vegetales/farmacología , Lectinas de Plantas/farmacología , Semillas/química , Animales , Antifúngicos/química , Carbohidratos/química , Línea Celular Tumoral , Eritrocitos/efectos de los fármacos , Hongos/efectos de los fármacos , Hongos/metabolismo , Calor , Humanos , Metales/química , Ratones , Extractos Vegetales/química , Lectinas de Plantas/químicaRESUMEN
A lectin with antiproliferative activity towards human cancer cell lines and mitogenic towards human peripheral blood mononuclear cells was purified from the rhizomes of Arundo donax (Linn.) by affinity chromatography on N-acetyl-d-glucosamine linked to epoxy-activated sepharose-6B. The pure preparation apparently yielded a single band of approximately 15 kDa on SDS-PAGE, pH 8.3, under both reducing and non-reducing conditions. The molecular mass of native lectin was 32 kDa as determined by gel filtration chromatography. This showed the lectin to be a dimer, with subunits not held together by disulphide linkages. The A. donax lectin (ADL) agglutinated rabbit erythrocytes and the agglutination was inhibited by N-acetyl-d-glucosamine and its di- and trimer. The lectin was thermostable upto 55 degrees C and showed optimum activity in the range of pH 7.0-9.0 and comprised of 2.1% carbohydrate content.
Asunto(s)
Acetilglucosamina/química , Acetilglucosamina/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Lectinas/farmacología , Poaceae/química , Rizoma/química , Antineoplásicos Fitogénicos/farmacología , Línea Celular Tumoral , Humanos , Concentración de Iones de Hidrógeno , Lectinas/química , Lectinas/aislamiento & purificación , Leucocitos Mononucleares/efectos de los fármacos , Mitógenos/química , Mitógenos/farmacología , Neoplasias/tratamiento farmacológico , Neoplasias/patología , FitoterapiaRESUMEN
PURPOSE: To evaluate the efficacy and safety of transpupillary thermotherapy (TTT) for subfoveal neovascularization (SRNVM) in patients with group 2A Idiopathic Juxtafoveolar Telangiectasis (IJFT). DESIGN: Nonrandomized interventional case series. METHODS: We performed TTT for subfoveal SRNVM in 14 eyes of 13 patients with group 2A IJFT, who were referred to our tertiary care center. We evaluated visual outcome and SRNVM closure rate in these patients. RESULTS: After a mean follow-up period of 8.65 months, 92.3% of treated eyes had stabilization or improvement in visual acuity as well as regression of SRNVM by fluorescein angiography (FA). One SRNVM showed persistent leakage. One patient worsened by more than 2 Snellen lines; one required retreatment. CONCLUSION: Transpupillary thermotherapy may be a safe and useful alternative treatment option for patients with group 2A IJFT with subfoveal SRNVM.