RESUMEN
A number of drugs as well as lead molecules are isolated from natural sources. Phytol is one of such lead molecule belongs to terpenes group distributed widely in medicinal plants. In the present work, we investigated the cytotoxic behavior of phytol on human lung carcinoma cells (A549). Phytol was found to cause characteristic apoptotic morphological changes and generation of ROS in A549 cells. The mechanism of phytol involved the activation of TRAIL, FAS and TNF-α receptors along with caspase 9 and 3. In silico molecular docking studies revealed that phytol has a good binding affinity with glucose-6-phosphate dehydrogenase (G6PD), which is known to promote tumor proliferation. The ability of phytol to become potential drug candidate has been revealed from the pharmacokinetic study performed in the present study.
Asunto(s)
Caspasa 3/biosíntesis , Caspasa 9/biosíntesis , Glucosafosfato Deshidrogenasa/metabolismo , Neoplasias Pulmonares/metabolismo , Fitol/farmacología , Especies Reactivas de Oxígeno/metabolismo , Células A549 , Apoptosis/efectos de los fármacos , Apoptosis/fisiología , Línea Celular Tumoral , Inducción Enzimática/efectos de los fármacos , Inducción Enzimática/fisiología , Humanos , Fitol/química , Fitol/uso terapéutico , Estructura Secundaria de Proteína , Receptores del Ligando Inductor de Apoptosis Relacionado con TNF/metabolismo , Receptores del Factor de Necrosis Tumoral/metabolismo , Receptor fas/metabolismoRESUMEN
Novel series of 2-morpholinoquinoline scaffolds (6a-n), containing the 1,2,4-oxadiazole and moiety, was designed and synthesized in good yield (76-86%). The synthesized compounds were screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains of bacteria and fungi. Molecular docking and pharmacokinetic study were carried out for the prepared compounds. The cytotoxicity of the synthesized compounds was tested at different concentrations using bioassay of S. pombe cells at the cellular level. The effect of synthesized compounds on the DNA integrity of S. pombe was observed on agarose gel. Compounds 6d, 6e, 6g, 6h, 6j and 6n exhibited excellent antimicrobial potency as compared to the standard drugs (i.e Ampicillin, Norfloxacin, Chloramphenicol, Ciprofloxacin). Compounds 6d, 6e, 6g, 6k and 6n were found to have significant antifungal activity as compared to griseofulvin. Compounds 6f, 6i, 6k, 6l were found very less cytotoxic, while compounds 6d, 6e, 6g, 6h were found to exhibit maximum toxicity. The rest of the synthesized compounds were found to be moderately toxic.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Oxadiazoles/química , Quinolinas/síntesis química , Quinolinas/farmacología , Antiinfecciosos/química , Antiinfecciosos/metabolismo , Bacterias/efectos de los fármacos , Proteínas Bacterianas/química , Proteínas Bacterianas/metabolismo , Dominio Catalítico , Técnicas de Química Sintética , Evaluación Preclínica de Medicamentos , Hongos/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Quinolinas/química , Quinolinas/metabolismo , Relación Estructura-ActividadRESUMEN
This study was intended to compare pulmonary function parameters in tea garden factory workers who are on chronic exposure to tea dust with tea garden plantation workers on the basis of dynamic ventilatory pulmonary function tests. The pulmonary function tests done on 128 subjects included 64 tea garden factory workers and 64 tea garden plantation workers. In tea factory workers the values of vital capacity (VC), forced vital capacity (FVC), forced expiratory volume in one second (FEV1), forced expiratory volume in first 0.75 second (FEV0.75), FEV1/FVC%, peak expiratory flow rate (PEFR) were found significantly lower (p < 0.001) than those of tea garden plantation workers. It may be concluded that pulmonary functions are more affected in tea factory workers than those of tea plantation workers.
Asunto(s)
Enfermedades de los Trabajadores Agrícolas/fisiopatología , Polvo , Exposición Profesional/efectos adversos , Té , Enfermedades de los Trabajadores Agrícolas/epidemiología , Estudios de Casos y Controles , Humanos , India/epidemiología , Masculino , Pruebas de Función RespiratoriaRESUMEN
Indian women of reproductive age groups commonly suffer from hypothyroidism which may be due to iodine or non iodine deficiency causes. This study was undertaken with a view to ascertain the leading cause of hypothyroidism in women of reproductive age group residing in the sub-Himalayan plain areas of Darjeeling district of West Bengal. Serum TSH, T4, T3 and Urinary Iodine Excretion (UIE) levels were measured in 101 non pregnant women. Our results reveal that among 37.62% (n=38) of bio-chemically established hypothyroid women; majority 76.32% (n=29) are suffering from iodine deficiency and the rest 23.68% (n=9) have Hypothyroidism due to other causes. Moreover, iodine deficiency persists among 57.42% (n=58) of the women in our study. We conclude that iodine deficiency disorders are still a major problem in this region and hypothyroidism due to iodine deficiency is more prevalent than the non iodine deficiency causes. Hence lacunae in the iodine supplementation process needs to be reviewed.