Regulatory mechanism of gallic acid against advanced glycation end products induced cardiac remodeling in experimental rats.

Advanced glycation end products (AGEs) play a major role in the development of cardiovascular disorders in diabetic patients. Recent studies evidenced the beneficial role of phytochemicals in reducing the risk of cardiovascular diseases. Hence the present study was framed to investigate the protective role of Gallic acid (GA) on AGEs induced cardiac fibrosis. Rats were infused with in vitro prepared AGEs (50mg/kg BW-intravenous injection) for 30 days. Further, GA (25mg/kgBW) was administered to rats along with AGEs. On infusion of AGEs, induction of fibrotic markers, collagen deposition, oxidative marker NADPH oxidase (NOX-p47 phox subunit), AGE receptor (RAGE) and cytokines expression was evaluated in the heart tissues using RT-PCR, Western blot and immunostaining methods. AGEs infusion significantly (P<0.01) increased the HW/BW ratio and fibrosis (4-fold) with increased expression of matrix genes MMP-2 and -9 (P<0.01, respectively) in the heart tissues. Whereas, administration of GA along with AGEs infusion prevented the fibrosis induced by AGEs. Further, GA treatment effectively prevented the AGEs mediated up-regulation of pro-fibrotic genes and ECM proteins such as TNF-α, TGF-ß, MMP-2 and -9 expression. In addition, the increased expression of NOX (P<0.01), RAGE (P<0.01), NF-κB (P<0.01) and ERK 1/2 on AGEs infusion were normalized by GA treatment. Thus the present study shows the protective effect of GA on the fibrotic response and cardiac remodeling process induced by advanced glycation end products from external sources.

Gold nanoparticle conjugated PLGA-PEG-SA-PEG-PLGA multiblock copolymer nanoparticles: synthesis, characterization, in vivo release of rifampicin.

A series of succinate linearly linked PLGA-PEG-SA-PEG-PLGA multiblock copolymers were synthesized using direct melt polycondensation and characterized using inherent viscosity, gel permeation chromatography (GPC), FTIR and 1H-NMR spectroscopy techniques. Gold nanoparticles (AuNPs) were synthesized using an as-synthesized citrate-PEG (CPEG) hybrid dendron, which acts as a reducing agent as well as a stabilizing agent. The CPEG capped AuNPs were characterized using UV-visible spectroscopy and TEM analysis. The Au-conjugated PLGA-PEG-SA-PEG-PLGA multiblock copolymer NPs were loaded with the tuberculosis drug rifampicin (RIF) using ultrasonication followed by solvent evaporation and were characterized by TEM, powder XRD and XPS analyses. The RIF loading efficiency and percentage drug content of RIF loaded Au-conjugated multiblock copolymer NPs were evaluated using UV-visible spectroscopy. The RIF loading efficiency and RIF content of the AuNP conjugated multiblock copolymer NPs were 41.8-75.7% and 11.5-17.7% respectively. The in vivo drug release studies in male Wistar rats show that AuNP conjugated multiblock copolymer NPs exhibit drug release up to 240 h. The nanoconjugates exhibit 18.13-29.41 µg mL-1 of Cmax with a delayed Tmax of 72 h and the relative bioavailability is increased to 107-190.

Rapid synthesis of biocompatible silver nanoparticles using aqueous extract of Rosa damascena petals and evaluation of their anticancer activity

Objective: To optimize the process parameters involved in the green synthesis of silver nanoparticles (G-SNPs) by aqueous extract of Rosa damascena petals and to evaluate the biocompatibility and anti cancer activity of the synthesized silver nanoparticles against human lung adenocarcinoma (A549). Methods: The process variables that include concentration of extract, mixing ratio of reactants, silver salt concentration and interaction time were analyzed. The compatibility of the G-SNPs was verified by incubating with erythrocytes and the anticancer property of the G-SNPs against A549 cells was performed by MTT assay. Results: Formation of G-SNPs was confirmed by the visual change in the colour of the reaction mixture from pale yellow to brown yellow. Surface plasmon resonance of synthesized G-SNPs was observed at 420 nm; the size of G-SNPs were analyzed by DLS and found to be in the range of (84.00±10.08) nm. Field emission scanning electron microscope and high resolution transmission electron microscopy analysis confirmed that the G-SNPs were fairly spherical. Fourier transform infrared spectroscopy spectroscopy and X-ray diffraction revealed the characteristic peaks of G-SNPs. Energy dispersive X-ray analysis showed a signal of silver around 3 keV. The synthesized G-SNPs exhibited anticancer activity as evidenced by the MTT assay. IC

Rapid synthesis of biocompatible silver nanoparticles using aqueous extract of Rosa damascena petals and evaluation of their anticancer activity

OBJECTIVE@#To optimize the process parameters involved in the green synthesis of silver nanoparticles (G-SNPs) by aqueous extract of Rosa damascena petals and to evaluate the biocompatibility and anti cancer activity of the synthesized silver nanoparticles against human lung adenocarcinoma (A549).@*METHODS@#The process variables that include concentration of extract, mixing ratio of reactants, silver salt concentration and interaction time were analyzed. The compatibility of the G-SNPs was verified by incubating with erythrocytes and the anticancer property of the G-SNPs against A549 cells was performed by MTT assay.@*RESULTS@#Formation of G-SNPs was confirmed by the visual change in the colour of the reaction mixture from pale yellow to brown yellow. Surface plasmon resonance of synthesized G-SNPs was observed at 420 nm; the size of G-SNPs were analyzed by DLS and found to be in the range of (84.00±10.08) nm. Field emission scanning electron microscope and high resolution transmission electron microscopy analysis confirmed that the G-SNPs were fairly spherical. Fourier transform infrared spectroscopy spectroscopy and X-ray diffraction revealed the characteristic peaks of G-SNPs. Energy dispersive X-ray analysis showed a signal of silver around 3 keV. The synthesized G-SNPs exhibited anticancer activity as evidenced by the MTT assay. IC50 value of G-SNPs was found to be 80 μg/mL.@*CONCLUSION@#The results of the present study suggest that G-SNPs can be synthesized rapidly within first minute of the reaction; they are biocompatible and possess anticancer activity against human lung adenocarcinoma.

Isoniazid loaded core shell nanoparticles derived from PLGA-PEG-PLGA tri-block copolymers: in vitro and in vivo drug release.

A series of biodegradable low molecular weight PLGA-PEG-PLGA tri-block copolymers have been synthesized in powder form. The anti-tuberculosis drug Isoniazid (INH) loaded polymeric core-shell nanoparticles (CSNPs) have been prepared by sonication followed by water-in-oil-in-water (w/o/w) double emulsification technique. The nanoparticles (NPs) have been characterized by field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), powder X-ray diffraction (XRD) and X-ray photo electron spectroscopic (XPS) techniques. The drug loaded CSNPs were found to be 150-400 nm in size with spherical shape. The drug loading efficiency and drug content of the polymer NPs were determined by UV-vis spectrophotometry. The drug loading efficiency and drug content of the NPs were (12.8-18.67%) and (6.4-8.9%) respectively. The in vitro release behavior of the polymer NPs has been investigated by UV-vis spectrophotometry and the release kinetics mechanism has been evaluated by Korsemeyer-Peppas (KP) and Higuchi models. The in vitro release studies show initial burst release followed by controlled and uniform release for longer duration. The pharmacokinetic studies show that the INH bioavailability of INH loaded CSNPs is 28 fold higher than that of free INH and also the CSNPs show sustained drug release for longer duration.