RESUMEN
The synthesized 4-(4-hydroxy benzyl)-2-amino-6-hydroxy pyrimidine-5-carboxamide was chosen to perform in silico modeling with identified drug target AGT, TNF, F2 and BCL2L1. The identified human proteins are vital in the pain management and also an important target for the study of wound healing activity. The enzymes were identified by using BioGRID, string database and network analysis through Cytoscape software. The wound healing activity was evaluated by excision wound model. The observed results revealed that, the pyrimidine nanoparticles showed significant wound healing activity compared to standard and synthesized compound. The detailed synthesis of nanoparticles formulation spectral analysis and pharmacological screening data's were reported. The revealed reports of synthesized analogues and formulated nanoparticles will generate a very good impact to the chemists and research scholars for further investigations in wound healing and pain management.
Asunto(s)
Nanopartículas/química , Pirimidinas/química , Pirimidinas/farmacología , Animales , Química Farmacéutica/métodos , Simulación por Computador , Humanos , Manejo del Dolor/métodos , Ratas , Cicatrización de Heridas/efectos de los fármacosRESUMEN
CONTEXT: Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) are used in folk medicine for various stomach disorders. OBJECTIVE: The chloroform and ethanol extracts of both plants were evaluated for antioxidant, gastric antisecretory, and gastroprotective properties. METHODS: Antioxidant properties of the extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide (NO) scavenging assay. The gastric antisecretory properties of the extracts were assessed, at a dose of 100 and 200 mg/kg, using aspirin-pylorus ligation induced gastric ulcer models and the gastroprotective activity of the extracts was assessed, at a dose of 100 and 200 mg/kg, using HCl-ethanol induced ulcer models in rats. RESULTS AND DISCUSSION: Ethanol extract of BM (EBM) possessed good antioxidant property with IC50 values of 37.4 and 44.1 µg/mL in DPPH and NO scavenging assays respectively, where 25-250 µg/mL concentration in DPPH assay and 30-300 µg/mL concentration in NO scavenging assay were used. Ethanol extract of AB (EAB) at a dose of 200 mg/kg reduced the free acidity to 142.66 mEq/L and total acidity to 451.22 mEq/L. It reduced the gastric secretion with increase in pH from 2.2 to 3.15. Possessing good antisecretory activity, it also reduced the ulcer by 92.2% in aspirin and pylorus ligation induced gastric ulcer models. EAB increased the mucus secretion and adherent mucus in the tissues with a 71.43% reduction of ulcerin HCl-ethanol induced ulcer models, at a dose of 200 mg/kg. This activity can be attributed to the various flavonoids like rutin and kaempferol-3-O-ß-glucopyranoside, and the phytosterol, ß-sitosterol-3-O-ß-glucopyranoside, and phenolics present in the extracts. CONCLUSION: EBM possessed significant antioxidant property while EAB possessed good antisecretory and gastroprotective activity.
Asunto(s)
Acanthaceae/química , Antiulcerosos/uso terapéutico , Depuradores de Radicales Libres/uso terapéutico , Mucosa Gástrica/efectos de los fármacos , Lythraceae/química , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/prevención & control , Adhesividad , Animales , Antiulcerosos/química , Antiulcerosos/aislamiento & purificación , Antiulcerosos/farmacología , Etnofarmacología , Femenino , Flavonoides/efectos adversos , Flavonoides/análisis , Flavonoides/farmacología , Flavonoides/uso terapéutico , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Ácido Gástrico/química , Ácido Gástrico/metabolismo , Mucosa Gástrica/inmunología , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patología , India , Masculino , Moco/química , Moco/metabolismo , Fitosteroles/efectos adversos , Fitosteroles/análisis , Fitosteroles/farmacología , Fitosteroles/uso terapéutico , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Hojas de la Planta/química , Ratas , Ratas Wistar , Úlcera Gástrica/inmunología , Úlcera Gástrica/patología , Pruebas de Toxicidad AgudaRESUMEN
Wound healing activity of the leaf extracts of Ammannia baccifera L., Lythraceae, and Blepharis maderaspatensis (L.) B.Heyne ex Roth., Acanthaceae, was investigated by excision and incision wound healing models in rats. A phytochemical screening was done to determine the major constituents of the chloroform, ethyl acetate and ethanolic fractions of ethanolic leaf extracts. The excision and incision models were used to assess the effect of the plant extracts on wound healing in rats. Phytochemical screening reveals the presence of tannins, saponins, steroids, terpenoids, and flavonoids in the extract. The wound healing effect was comparatively evaluated with a standard drug Framycetin cream. Significant wound healing activity was observed for the creams prepared with 5% ethanol fraction of B. maderaspatensis and 5% chloroform fraction of A. baccifera ethanolic leaf extracts. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Ethanolic fraction of B. maderaspatensis and chloroform fraction of A. baccifera exhibited marked wound healing activity. B. maderaspatensis extract displayed a remarkable wound healing activity compared to A. baccifera.
RESUMEN
The major objectives of the current study were (i) to prepare carvedilol-loaded buccal tablets by direct compression technique, and (ii) to study the influence of low and high proportions of sodium carboxy methylcellulose (SCMC) in conjunction with the corresponding high and low proportions of sodium alginate, polyvinyl pyrrolidone (PVP-K-30), carbopol 974P, and hydroxypropyl methylcellulose (HPMC) on the basic properties (hardness, friability, weight variation, thickness uniformity, drug content, mucoadhesive strength, surface pH, swelling property, and drug release behavior) of the tablets. Altering the polymer combinations did not affect the physical properties of the buccal tablets. However, the presence of SCMC and sodium alginate at 1:2 ratio in the tablet showed a sustained drug release. In addition, this polymer combination at 2:1 ratio did release the drug completely during the stipulated dissolution time. Swelling study indicated the tablet structure collapse over time at 2:1 polymer ratio, thus exposing the drug molecules directly to the dissolution medium to attain the complete drug release from the SCMC and sodium alginate-based tablets. On the other hand, whatever the polymer ratios, the SCMC and carbopol 974P combination always retarded the drug release in an almost similar manner. Though the SCMC- and carbopol 974P-based tablets did display an impressive mucoadhesion property, the surface pH value determined for this polymer combination was found to decrease considerably due to the liberation of the free carboxylic acid over the time period.