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1.
Molecules ; 26(13)2021 Jun 22.
Artículo en Inglés | MEDLINE | ID: mdl-34206529

RESUMEN

Urease is an enzyme that plays a significant role in the hydrolysis of urea into carbonic acid and ammonia via the carbamic acid formation. The resultant increase in pH leads to the onset of various pathologies such as gastric cancer, urolithiasis, hepatic coma, hepatic encephalopathy, duodenal ulcers and peptic ulcers. Urease inhibitors can reduce the urea hydrolysis rate and development of various diseases. The Cinnamomum genus is used in a large number of traditional medicines. It is well established that stem bark of Cinnamomum cassia exhibits antiulcerogenic potential. The present study evaluated the inhibitory effect of seven extracts of Cinnamomum camphora, Cinnamomum verum and two pure compounds Camphene and Cuminaldehyde on urease enzyme. Kinetic studies of potential inhibitors were carried out. Methanol extract (IC50 980 µg/mL) of C. camphora and a monoterpene Camphene (IC50 0.147 µg/mL) possess significant inhibitory activity. The Lineweaver Burk plot analysis suggested the competitive inhibition by methanol extract, hexane fraction and Camphene. The Gas Chromatography-Mass Spectroscopy (GC-MS) analysis of hexane fraction revealed the contribution of various terpenes. The present study targets terpenes as a new class of inhibitors that have potential therapeutic value for further development as novel drugs.


Asunto(s)
Proteínas Bacterianas , Cinnamomum/química , Inhibidores Enzimáticos/química , Simulación del Acoplamiento Molecular , Extractos Vegetales/química , Ureasa , Proteínas Bacterianas/antagonistas & inhibidores , Proteínas Bacterianas/química , Ureasa/antagonistas & inhibidores , Ureasa/química
2.
Molecules ; 26(11)2021 May 28.
Artículo en Inglés | MEDLINE | ID: mdl-34071722

RESUMEN

Obesity is a serious health complication in almost every corner of the world. Excessive weight gain results in the onset of several other health issues such as type II diabetes, cancer, respiratory diseases, musculoskeletal disorders (especially osteoarthritis), and cardiovascular diseases. As allopathic medications and derived pharmaceuticals are partially successful in overcoming this health complication, there is an incessant need to develop new alternative anti-obesity strategies with long term efficacy and less side effects. Plants harbor secondary metabolites such as phenolics, flavonoids, terpenoids and other specific compounds that have been shown to have effective anti-obesity properties. Nanoencapsulation of these secondary metabolites enhances the anti-obesity efficacy of these natural compounds due to their speculated property of target specificity and enhanced efficiency. These nanoencapsulated and naive secondary metabolites show anti-obesity properties mainly by inhibiting the lipid and carbohydrate metabolizing enzymes, suppression of adipogenesis and appetite, and enhancing energy metabolism. This review focuses on the plants and their secondary metabolites, along with their nanoencapsulation, that have anti-obesity effects, with their possible acting mechanisms, for better human health.


Asunto(s)
Productos Biológicos/química , Tecnología Química Verde , Nanomedicina/métodos , Obesidad/tratamiento farmacológico , Obesidad/metabolismo , Adipocitos/citología , Adipogénesis , Animales , Fármacos Antiobesidad/química , Diferenciación Celular , Flavonoides/química , Humanos , Ratones , Nanopartículas/química , Fenol/química , Extractos Vegetales/química , Poliésteres/química , Polietilenglicoles/química , Polifenoles/química , Terpenos/química
3.
Pharm Biol ; 53(3): 326-33, 2015 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-25366133

RESUMEN

CONTEXT: Bacterial ureases play an important role in pathogenesis of urinary infections. Selection of plants was done on the basis of their uses by the local people for the treatment of various bacterial and urinary infections. OBJECTIVE: Our investigation screens and evaluates 15 Indian medicinal plants for their possible urease inhibitory activity as well as their ability to inhibit bacteria causing urinary infections. MATERIALS AND METHODS: Plant extracts in three different solvents (methanol, aqueous, and cow urine) were screened for their effect on Jack-bean urease using the phenol-hypochlorite method. Subsequently, seven bacterial strains were screened for their ability to release urease and further antimicrobial-linked urease inhibition activity and minimum inhibitory concentration of the tested extracts were evaluated by the agar well diffusion and microdilution method, respectively. RESULTS: Five plants out of 15 crude extracts revealed good urease inhibitory activity (≥ 20% at 1 mg/ml conc.) and IC50 values for these extracts ranged from 2.77 to 0.70 mg/ml. Further testing of these extracts on urease-producing bacterial strains (Staphylococcus aureus NCDC 109, S. aureus MTCC 3160, Proteus vulgaris MTCC 426, Klebsiella pneumoniae MTCC 4030, and Pseudomonas aeruginosa MTCC 7453) showed good anti-urease potency with an MIC ranging from 500 to 7.3 µg/ml. DISCUSSION AND CONCLUSION: The results of screening as well as susceptibility assay clearly revealed a strong urease inhibitory effect of Acacia nilotica L. (Fabaceae), Emblica officinalis Gaertn. (Phyllanthaceae), Psidium guajava L. (Myrtaceae), Rosa indica L. (Rosaceae), and Terminalia chebula Retz. (Combretaceae). Our findings may help to explain the beneficial effect of these plants against infections associated with the urease enzyme.


Asunto(s)
Antibacterianos/farmacología , Canavalia/enzimología , Plantas Medicinales , Ureasa/antagonistas & inhibidores , Infecciones Urinarias/enzimología , Animales , Antibacterianos/aislamiento & purificación , Antibacterianos/uso terapéutico , Proteínas Bacterianas/antagonistas & inhibidores , Proteínas Bacterianas/metabolismo , Canavalia/efectos de los fármacos , Bovinos , Evaluación Preclínica de Medicamentos/métodos , India , Pseudomonas aeruginosa/crecimiento & desarrollo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Ureasa/metabolismo , Infecciones Urinarias/tratamiento farmacológico , Infecciones Urinarias/microbiología
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