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1.
Front Nutr ; 9: 868209, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35662938

RESUMEN

Asparagus [Asparagus cochinchinensis (Lour.) Merr.] is a traditional herbal medicine plant commonly used to nourish yin, moisten dryness, and clear fire cough symptoms. Drying is an excellent option to conserve food materials, i.e., grains, fruits, vegetables, and herbs, reducing the raw materials volume and weight. This study aims to evaluate different drying approaches that could increase the value of asparagus, particularly as an ingredient in fast foods or as nutraceutical byproducts. The volatile components of asparagus roots were analyzed by using headspace-gas chromatography-ion mobility spectroscopy under different drying conditions, i.e., natural drying (ND) at ambient air temperature in the dark, well-ventilated room, temperature range 28-32°C, blast or oven drying at 50°C, heat pump or hot-air drying at temperature 50°C and air velocity at 1.5 ms-1 and vacuum freeze-drying at the temperature of -45°C and vacuum pressure of 10-30 Pa for 24 h. The findings revealed that the various drying processes had multiple effects on the color, odor index, and volatile compounds of the asparagus roots. As a result of the investigations, multiple characteristics of components, therefore, exploitation and comparison of various flavors; a total of 22 compounds were identified, such as alcohols, ketones, aldehydes, acids, esters, heterocyclic, and terpene. The present findings may help understand the flavor of the processed asparagus roots and find a better option for drying and processing.

2.
Front Plant Sci ; 13: 1025974, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36618645

RESUMEN

Abiotic stresses causing extensive yield loss in various crops globally. Over the past few decades, the application of silicon nanoparticles (nSi) has emerged as one of the abiotic stress mitigators. The initial responses of plants are shown by the biogenesis of reactive oxygen species (ROS) to sustain cellular/organellar integrity to ensure in vivo operation of metabolic functions by regulating physiological and biochemical pathways during stress conditions. Plants have evolved various antioxidative systems to balance/maintain the process of homeostasis via enzymatic and non-enzymatic activities to repair the losses. In the adverse environment, supplementation of Si mitigates the stress condition and improved the growth and development of plants. Its ameliorative effects were correlated with the enhanced antioxidant enzymes activities to maintain the equilibrium between the ROS generation and reduction. However, there are limited studies covered the role of nSi in the abiotic stress condition. This review addresses the accumulation and/or uptake of nSi in several crops and its mode of action linked with improved plants' growth and tolerance capabilities to confer sustainable agriculture.

3.
Cent Nerv Syst Agents Med Chem ; 20(1): 41-48, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31814557

RESUMEN

OBJECTIVE: In the present study, we synthesized fifteen 4, 5-disubstituted 1, 2, 4-triazol- 3-thione derivatives and evaluated for anticonvulsant activity with neurotoxicity determination. METHODS: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The molecular docking study was also performed to study the interactions of compounds with LYS329 residue of gamma amino butyric acid aminotransferase (GABA-AT) using Autodock 4.2 software. The anticonvulsant activity was assessed by maximal electroshock (MES) test and subcutaneous pentylenetetrazol (scPTZ) tests. The neurotoxicity was assessed by rotarod ataxia test. RESULTS: In MES test, compounds 5a, 8a and 9a were found active at 100 mg/kg and five compounds were found active at 300 mg/kg dose after 1 hr of administration. After 4 hr of drug administration, only two compounds 8a and 9a exhibited protection at 100 mg/kg. In scPTZ test, three compounds 2a, 6a and 8a were found active at 100 mg/kg and 7a was active at 300 mg/kg after 1 hr of test drug administration. Most of the compounds were found active in MES test with 8a and 9a being the most active among all. In docking study, 2a was found to be best compound based on the binding energy of -6.5 kcal/mol and estimated inhibition constant of 17.2 µM. CONCLUSION: Majority of synthesized compounds were found active in MES test, whereas only few were found to possess anti scPTZ activity. Among all compounds, only 14a caused motor coordination impairment in rotarod ataxia test at 300 mg/kg 1 hr duration.


Asunto(s)
Anticonvulsivantes/farmacología , Triazoles/farmacología , 4-Aminobutirato Transaminasa/efectos de los fármacos , Animales , Anticonvulsivantes/síntesis química , Anticonvulsivantes/toxicidad , Ataxia/inducido químicamente , Ataxia/psicología , Convulsivantes , Evaluación Preclínica de Medicamentos , Electrochoque , Masculino , Ratones , Simulación del Acoplamiento Molecular , Pentilenotetrazol , Prueba de Desempeño de Rotación con Aceleración Constante , Convulsiones/inducido químicamente , Convulsiones/prevención & control , Relación Estructura-Actividad , Triazoles/síntesis química , Triazoles/toxicidad
4.
J Nat Prod ; 79(4): 691-6, 2016 Apr 22.
Artículo en Inglés | MEDLINE | ID: mdl-27057812

RESUMEN

The sesquiterpene lactones dehydroleucodine (1) and leucodine (2) were isolated from Gynoxys verrucosa, a species used in traditional medicine in southern Ecuador. The activity of these compounds was determined against eight acute myeloid leukemia (AML) cell lines and compared with their activity against normal peripheral blood mononuclear cells. Compound 1 showed cytotoxic activity against the tested cell lines, with LD50 values between 5.0 and 18.9 µM. Compound 2 was inactive against all of the tested cell lines, demonstrating that the exocyclic methylene in the lactone ring is required for cytotoxic activity. Importantly, compound 1 induced less toxicity to normal blood cells than to AML cell lines and was active against human AML cell samples from five patients, with an average LD50 of 9.4 µM. Mechanistic assays suggest that compound 1 has a similar mechanism of action to parthenolide (3). Although these compounds have significant structural differences, their lipophilic surface signatures show striking similarities.


Asunto(s)
Antineoplásicos/aislamiento & purificación , Antineoplásicos/farmacología , Asteraceae/química , Lactonas/aislamiento & purificación , Lactonas/farmacología , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología , Antineoplásicos/química , Western Blotting , Ensayos de Selección de Medicamentos Antitumorales , Ecuador , Células HL-60 , Células HeLa , Humanos , Lactonas/química , Leucemia Mieloide Aguda/tratamiento farmacológico , Leucocitos Mononucleares/efectos de los fármacos , Medicina Tradicional , Estructura Molecular , Sesquiterpenos/química
5.
Prostate ; 71(15): 1638-45, 2011 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-21432866

RESUMEN

BACKGROUND: Men with positive margins after radical prostatectomy (RP) for localized prostate cancer (PC) have a 40-50% biochemical relapse rate at 5 years. Adjuvant radiotherapy improves biochemical progression-free and overall survival in men with positive margins, but is associated with increased toxicity. There is an urgent need to identify new prognostic markers to define the group of patients who would benefit from multimodality therapy. METHODS: Nuclear ß-catenin, membranous secreted frizzled-related protein 4 (sFRP4), zinc-alpha 2-glycoprotein (AZGP1), and macrophage inhibitory cytokine-1 (MIC-1) have previously been identified as molecular markers of outcome in localized PC. From these published studies, we identified a subset of patients with positive margins. The aim of this study was to assess the association between these four molecular markers and outcome in men with margin-positive, localized PC. RESULTS: We identified 186 men with positive margins from 330 men with localized PC; 53% had preoperative PSA >10 ng/ml, 72% extraprostatic extension (EPE), 24% seminal vesicles involvement (SVI), and 57% RP Gleason score ≥ 7. AZGP1 (P = 0.009), membranous sFRP4 (P = 0.03) and MIC-1 (P = 0.04) expression predicted for biochemical relapse on univariate analysis. Only absent/low AZGP1 expression (P = 0.01) was an independent predictor of recurrence in margin-positive, localized PC when modeled with preoperative PSA (P = 0.2), EPE (P = 0.2), SVI (P = 0.4), Gleason score ≥ 7 (P = 0.5) and adjuvant treatment (P = 0.4). Furthermore, there was an association between absent/low AZGP1 expression and clinical recurrence (P = 0.007). CONCLUSIONS: AZGP1 is a potential molecular marker for biochemical relapse in men with margin-positive, localized PC. Routine assessment of this biomarker may lead to better selection of patients who will benefit from post-RP radiotherapy.


Asunto(s)
Biomarcadores de Tumor/biosíntesis , Proteínas Portadoras/biosíntesis , Glicoproteínas/biosíntesis , Recurrencia Local de Neoplasia/metabolismo , Neoplasias de la Próstata/metabolismo , Adipoquinas , Anciano , Biomarcadores de Tumor/análisis , Proteínas Portadoras/análisis , Estudios de Cohortes , Supervivencia sin Enfermedad , Glicoproteínas/análisis , Factor 15 de Diferenciación de Crecimiento/análisis , Factor 15 de Diferenciación de Crecimiento/biosíntesis , Humanos , Inmunohistoquímica , Masculino , Persona de Mediana Edad , Análisis Multivariante , Recurrencia Local de Neoplasia/patología , Valor Predictivo de las Pruebas , Modelos de Riesgos Proporcionales , Neoplasias de la Próstata/patología , Neoplasias de la Próstata/cirugía , Proteínas Proto-Oncogénicas/análisis , Proteínas Proto-Oncogénicas/biosíntesis , Estudios Retrospectivos , beta Catenina/análisis , beta Catenina/biosíntesis
6.
Indian J Tuberc ; 56(1): 48-50, 2009 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-19402272

RESUMEN

The chance of incidence of XDR TB is on the rise due to improper use of second line anti-tubercular drugs. XDR-TB is very difficult to treat successfully and is often referred to as "virtually untreatable form of TB". We herein report a case of XDR TB confirmed by bacteriological examination in a WHO recognised laboratory who after 12 months of regular treatment improved both clinically and radiologically with sputum smear conversion. To the best of our knowledge, there has been no previous report of any similar case in literature.


Asunto(s)
Antituberculosos/uso terapéutico , Tuberculosis Extensivamente Resistente a Drogas/tratamiento farmacológico , Adulto , Ácido Aminosalicílico/uso terapéutico , Compuestos Aza/uso terapéutico , Capreomicina/uso terapéutico , Claritromicina/uso terapéutico , Clofazimina/uso terapéutico , Quimioterapia Combinada , Etambutol/uso terapéutico , Tuberculosis Extensivamente Resistente a Drogas/diagnóstico , Fluoroquinolonas , Humanos , India , Inyecciones , Masculino , Moxifloxacino , Quinolinas/uso terapéutico , Esputo/microbiología , Resultado del Tratamiento
7.
Mol Endocrinol ; 17(12): 1792-1804, 2003 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-14680004

RESUMEN

Immortalized GnRH neurons (GT1-7) express receptors for estrogen [estrogen receptor-alpha and-13(ERa and ERI3)] and progesterone (progesterone receptor A) and exhibit positive immunostaining for both intracellular and plasma membrane ERs. Exposure of GT1-7 cells to picomolar estradiol concentrations for 5-60 min caused rapid, sustained,and dose-dependent inhibition of cAMP production. In contrast, treatment with nanomolar estradiol concentrations for 60 min increased cAMP production. The inhibitory and stimulatory actions of estradiol on cAMP formation were abolished by the ER antagonist, ICI 182,780. The estradiol-induced inhibition of cAMP production was prevented by treatment with pertussis toxin, consistent with coupling of the plasma membrane ER to an inhibitory G protein. Coimmunoprecipitation studies demonstrated an estradiol-regulated stimulatory interaction between ERa and G,3 that was prevented by the ER antagonist, ICI 182,780. Exposure of perifused GT1-7 cells and hypothalamic neurons to picomolar estradiol levels increased the GnRH peak interval, shortened peak duration, and increased peak amplitude. These findings indicate that occupancy of the plasma membrane-associated ERs expressed in GT1-7 neurons by physio-logical estradiol levels causes activation of a G, protein and modulates cAMP signaling and neuropeptide secretion.


Asunto(s)
AMP Cíclico/fisiología , Hipotálamo/embriología , Neuronas/fisiología , Receptores de Estrógenos/genética , Receptores de Progesterona/genética , Transducción de Señal/fisiología , Animales , Sitios de Unión , Células Cultivadas , Cartilla de ADN , Estradiol/farmacología , Receptor alfa de Estrógeno , Receptor beta de Estrógeno , Estrógenos/metabolismo , Femenino , Feto , Regulación del Desarrollo de la Expresión Génica , Hormona Liberadora de Gonadotropina/efectos de los fármacos , Hormona Liberadora de Gonadotropina/metabolismo , Hipotálamo/fisiología , Inmunohistoquímica , Neuronas/citología , Neuronas/efectos de los fármacos , Nervio Óptico/fisiología , Embarazo , Progesterona/farmacología , Ratas , Ratas Sprague-Dawley , Receptores de Estrógenos/metabolismo , Transducción de Señal/efectos de los fármacos , Útero/fisiología
8.
Mol Endocrinol ; 17(9): 1792-804, 2003 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-12819297

RESUMEN

Immortalized GnRH neurons (GT1-7) express receptors for estrogen [estrogen receptor-alpha and -beta(ERalpha and ERbeta)] and progesterone (progesterone receptor A) and exhibit positive immunostaining for both intracellular and plasma membrane ERs. Exposure of GT1-7 cells to picomolar estradiol concentrations for 5-60 min caused rapid, sustained, and dose-dependent inhibition of cAMP production. In contrast, treatment with nanomolar estradiol concentrations for 60 min increased cAMP production. The inhibitory and stimulatory actions of estradiol on cAMP formation were abolished by the ER antagonist, ICI 182,780. The estradiol-induced inhibition of cAMP production was prevented by treatment with pertussis toxin, consistent with coupling of the plasma membrane ER to an inhibitory G protein. Coimmunoprecipitation studies demonstrated an estradiol-regulated stimulatory interaction between ERalpha and Galphai3 that was prevented by the ER antagonist, ICI 182,780. Exposure of perifused GT1-7 cells and hypothalamic neurons to picomolar estradiol levels increased the GnRH peak interval, shortened peak duration, and increased peak amplitude. These findings indicate that occupancy of the plasma membrane-associated ERs expressed in GT1-7 neurons by physiological estradiol levels causes activation of a Gi protein and modulates cAMP signaling and neuropeptide secretion.


Asunto(s)
Membrana Celular/metabolismo , AMP Cíclico/metabolismo , Neuronas/metabolismo , Neurosecreción/fisiología , Receptores de Estrógenos/metabolismo , Animales , Retículo Endoplásmico/metabolismo , Femenino , Feto/metabolismo , Hipotálamo/metabolismo , Inmunohistoquímica , Embarazo , Ratas , Receptores de Progesterona/metabolismo , Transducción de Señal/fisiología
9.
Proc Natl Acad Sci U S A ; 100(5): 2969-74, 2003 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-12591945

RESUMEN

The pulsatile secretion of gonadotropin-releasing hormone (GnRH) from normal and immortalized hypothalamic GnRH neurons is highly calcium-dependent and is stimulated by cAMP. It is also influenced by agonist activation of the endogenous GnRH receptor (GnRH-R), which couples to G(q/11) as indicated by release of membrane-bound alpha(q/11) subunits and increased inositol phosphate/Ca(2+) signaling. Conversely, GnRH antagonists increase membrane-associated alpha(q/11) subunits and abolish pulsatile GnRH secretion. GnRH also stimulates cAMP production but at high concentrations has a pertussis toxin-sensitive inhibitory effect, indicative of receptor coupling to G(i). Coupling of the agonist-activated GnRH-R to both G(s) and G(i) proteins was demonstrated by the ability of nanomolar GnRH concentrations to reduce membrane-associated alpha(s) and alpha(i3) levels and of higher concentrations to diminish alpha(i3) levels. Conversely, alpha(i3) was increased during GnRH antagonist and pertussis toxin treatment, with concomitant loss of pulsatile GnRH secretion. In cholera toxin-treated GnRH neurons, decreases in alpha(s) immunoreactivity and increases in cAMP production paralleled the responses to nanomolar GnRH concentrations. Treatment with cholera toxin and 8-bromo-cAMP amplified episodic GnRH pulses but did not affect their frequency. These findings suggest that an agonist concentration-dependent switch in coupling of the GnRH-R between specific G proteins modulates neuronal Ca(2+) signaling via G(s)-cAMP stimulatory and G(i)-cAMP inhibitory mechanisms. Activation of G(i) may also inhibit GnRH neuronal function and episodic secretion by regulating membrane ion currents. This autocrine mechanism could serve as a timer to determine the frequency of pulsatile GnRH release by regulating Ca(2+)- and cAMP-dependent signaling and GnRH neuronal firing.


Asunto(s)
Proteínas de Unión al GTP/metabolismo , Hipotálamo/embriología , Neuropéptidos/metabolismo , Receptores LHRH/metabolismo , 8-Bromo Monofosfato de Adenosina Cíclica/metabolismo , Adenilil Ciclasas/metabolismo , Animales , Western Blotting , Calcio/metabolismo , Membrana Celular/metabolismo , AMP Cíclico/metabolismo , Relación Dosis-Respuesta a Droga , Proteínas de Unión al GTP/química , Regulación de la Expresión Génica , Humanos , Hipotálamo/citología , Hipotálamo/metabolismo , Fosfatos de Inositol/metabolismo , Iones , Modelos Biológicos , Neuronas/citología , Neuronas/metabolismo , Péptidos/química , Péptidos/farmacología , Toxina del Pertussis/farmacología , Unión Proteica , Ratas , Ratas Sprague-Dawley , Receptores LHRH/agonistas , Receptores LHRH/química , Transducción de Señal , Factores de Tiempo
10.
Indian J Physiol Pharmacol ; 29(4): 199-206, 1985.
Artículo en Inglés | MEDLINE | ID: mdl-3842372

RESUMEN

An investigation was undertaken to study the circadian rhythmicity in pulse rate, systolic and diastolic blood pressure, rectal temperature and urine output in eight traumatic tetraplegics in view of the fact that diurnal rhythmicity in prolactin response to thyrotropin-releasing hormone was absent in such patients. The data, analysed by single cosinor procedure, showed absence of rhythmicity in all five parameters. Analysis of variance also showed no significant difference in these parameters at various time points. Knowledge of the alterations in circadian biology subsequent to cervical spinal cord trauma would provide useful guidelines towards chronotherapy and vocational rehabilitation of tetraplegics besides possible restoration of euchronism by pharmacological means.


Asunto(s)
Ritmo Circadiano , Cuadriplejía/fisiopatología , Traumatismos de la Médula Espinal/fisiopatología , Adolescente , Adulto , Anciano , Presión Sanguínea , Temperatura Corporal , Humanos , Masculino , Persona de Mediana Edad , Pulso Arterial , Micción
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