RESUMEN
The aim of this paper was to observe the effect of gambogenic acid on angiogenesis of lung cancer and its preliminary mechanism. After culturing lung adenocarcinoma A549 cells, the conditioned medium was treated with gambogenic acid and then used to culture human umbilical vein endothelial cells (HUVECs) to establish the indirect contact cell co-culture system. A two-dimensional culture model of HUVEC was established with matrigel to observe the effect of gambogenic acid on angiogenesis. DAPI staining was used to observe the morphological changes in HUVEC cells after treatment with gambogenic acid under the fluorescence microscope. Annexin V-FITC/PI staining and flow cytometry analysis were used to determine gambogenic acid's effect on HUVEC cell apoptosis rate. The protein expressions of PI3K, p-PI3K, Akt, p-Akt were measured by Western blot. PTEN-siRNA was transfected into cells, and RT-PCR was used to detect the expression levels of PI3K and Akt genes. Gambogenic acid can significantly inhibit angiogenesis, and its inhibitory effect was dose-dependent. DAPI staining showed apoptotic morphological features of HUVEC cells under fluorescence microscope. Annexin V-FITC/PI staining showed that gambogenic acid induced apoptosis in HUVECs. The results of Western blot showed that the expressions of p-PI3K and p-Akt protein were down-regulated with gambogenic acid, while the expressions of PI3K and Akt protein was insignificant. The results of RT-PCR indicated that the expressions of PI3K and Akt protein were up-regulated by PTEN siRNA. Gambogenic acid can inhibit angiogenesis in lung cancer in vitro, and the mechanism of inhibiting angiogenesis may be related to the PI3K/Akt signaling pathway.
Asunto(s)
Apoptosis , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Neoplasias Pulmonares/patología , Neovascularización Patológica/patología , Xantenos/farmacología , Células A549 , Técnicas de Cocultivo , Humanos , Neoplasias Pulmonares/tratamiento farmacológico , Fosfohidrolasa PTEN/genética , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , TransfecciónRESUMEN
The purpose of this study is to investigate the applicability of a natural swelling matrix derived from boat-fruited sterculia seed (SMS) as the propellant of osmotic pump tablets. The sugar components, static swelling, water uptake and viscosity of SMS were determined and compared with that of polythylene oxide (WSR-N10 and WSR-303). Both ribavirin and glipizide were used as water-soluble and water-insoluble model drugs. Then, the monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide were prepared using SMS as the osmotically active substance and propellant. SMS was mainly composed of rhamnose, arabinose, xylose and galactose and exhibited relatively high swelling ability. The area of the disintegrated matrix tablet was 20.1 times as that at initial after swelling for 600 s. SMS swelled rapidly and was fully swelled (0.5%) in aqueous solution with relative low viscosity (3.66 +/- 0.03) mPa x s at 25 degrees C. The monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide using SMS as propellant exhibited typical drug release features of osmotic pumps. In conclusion, the swelling matrix derived from boat-fruited sterculia seed, with low viscosity and high swelling, is a potential propellant in the application of osmotic pump tablets.
Asunto(s)
Glipizida/administración & dosificación , Malvaceae/química , Ribavirina/administración & dosificación , Tecnología Farmacéutica/métodos , Arabinosa/química , Arabinosa/aislamiento & purificación , Química Farmacéutica , Preparaciones de Acción Retardada , Portadores de Fármacos , Galactosa/química , Galactosa/aislamiento & purificación , Glipizida/química , Ósmosis , Plantas Medicinales/química , Ramnosa/química , Ramnosa/aislamiento & purificación , Ribavirina/química , Semillas/química , Solubilidad , Comprimidos , Viscosidad , Agua , Xilosa/química , Xilosa/aislamiento & purificaciónRESUMEN
To explore the absorption mechanism of paeonol-beta-CD from various intestinal segments and offer biopharmaceutics data for paeonol new dosage form. The absorption kinetics and permeability rate consatants were investigated by the in situ perfusing method in rats. The absorption of the drug conforms to the firt-order kinetics and passive transport mechanism . The results indicate that paeonol-beta-CD absorption mechanism wasn't change.
Asunto(s)
Acetofenonas/farmacocinética , Absorción Intestinal/fisiología , Mucosa Intestinal/metabolismo , Animales , Cinética , Masculino , Ratas , Ratas Sprague-DawleyRESUMEN
OBJECTIVE: To optimize the formulation of immediate release tablet. METHOD: The immediate release tablet was prepared by using dry granules. The preparation was optimized by using orthogonal design which took the flow property of granules, the hardness, the disintegrating time and the dissolution rate of the tablet as indices. RESULT: The optimized formulation contained 40% microcrystalline cellulose, 10% sodium carboxymethyl starch and 15% dextrin. The hardness disintegrating time and T50 of the tablet were 4.5 kg, 3 min, 5 min respectively. CONCLUSION: It is successful to prepare on immediate release tablet using the optimized formula above.