The buckthorn "Rhamnus alaternus" is a plant used in traditional medicine especially in the treatment of certain diseases such as diabetes, cardiovascular disease and dyslipidemia. The aim of our study was to analysed and evaluate the effects of buckthorn on nephroangiosclerosis Wistar rats. Thirty male Wistar rats, adult weighing between 120g and 250g were distributed as follows Five control animals received a standard laboratory diet, thirty four experimental rats received the standard laboratory diet supplemented with palm oil and 4% of NaCl (High Sold Fat Diet). After six month of this diet the HSFD group was subdivided into rats treated for 45 days with aqueous extract of buckthorn or animals HSFD only. Plasma metabolites and endothelin-1 concentration were measured by standard methods, section of kidney were stained by Heindenhain-azan and periodic acid shiff. The examination of renal parenchyma of HSFD rats showed a prominent structural changes such as, obstruction of vascular lumen, ischemia of the glomerular and tubulo-interstitial fibrosis the biochemical and hormonal parameters were significantly improved in the HSFD rats treated with decoction of buckthorn. Moreover, the morphogical changes of the renal parenchyma were attenuated in rats HSFD decoction. The buckthorn attenuates renal parenchymal lesions by aggregating at different levels of rats maintained on HSFD.Among the physicochemical properties, pKa and LogP values help us in studying drug parameters like ADME and could be predicted to some extent. https://www.selleckchem.com/ With this view, here we wish to predict these two properties of our previously synthesized biologically active derivatives of isoniazid using on-line available program Marvin, a Java-based chemical software application frequently used for chemical modeling. According to Marvin, pKa values predicted 99.99% unionized states of INH and some derivatives at physiological pH 7.4. Marvin calculated LogP values estimated good oral absorption for all the synthesized compounds. Therefore it can be said that the findings of the study emerged in an ideal region that permits the formulation of these derivatives. Since this was just a theoretical study, it demands more experimentation to determine accurate situation.Human diseases like viral organisms for example, hepatitis, HIV and etc., attack the health and caused large mortality in populations by many years. So finding novel delivery vehicles based antiviral drugs employing nano-materials is of high universal interest. In current approach a very biocompatible biodegradable nano-biopolymer anionic linear globular dendrimer second generation G2 was elaborately conjugated to a well-known anti-HIV drug Azidovudine and thereafter was characterized by different analytical techniques like AFM, Zeta sizer, 1HNMR, FTIR and LC-Mass spectroscopy. Then, Anionic Linear Globular DendrimerG2-Zidovudine Nano-Conjugate was assessed on human normal cells (toxicity assay by XTT test) and also HIV cell model and the results showed that Anionic Linear Globular DendrimerG2-Zidovudine Nano-Conjugate Significantly Decreased Retroviral Activity without any human cell toxicity respectively. Based on current experimental data such nano-compositions is proposed for further in vivo anti-HIV assays as well.The DPPH radical scavenging potentials of the fractions were determined in comparison to positive controls such as quercetin with EC50 = 4.12±1.27, ascorbic acid with EC50 = 6.20±1.67, gallic acid with EC50 = 4.75±1.24 and α-tocopherol with EC50 = 32.50±1.57 μg/mL. The experiment showed that aqueous fractions of the bark extracts of Abies pindrow (fraction C2) and Cedrus deodara (fraction E2) showed significantly lower EC50 values of 2.5±0.5 and 2.5±0.6 μg/mL, respectively. In reducing power assay, lower EC50 values of 5.5 and 4.5μg/mL were recorded for the aqueous fraction (fraction C 2) and final residue (fraction C5), of Abies pindrow, respectively. The ethyl acetate, acetone and final fractions of knot wood of Picea smithiana were found significantly active against all bacterial strains. Of the most sensitive fractions towards all the fungal strains was ethyl acetate fraction obtained from the bark of Cedrus deodara with a zone of inhibition ranging from 75 to 88 % that was more than the standard fluconazole.Curcumin (Diferuloylmethane) is a natural product extracted from the root of Curcuma longa. 5-Bis (4-hydroxy-3-methoxybenzylidene)-N-methyl-4-piperidone, the piperidone analogue of curcumin (PAC), was one of the analogues that, demonstrated potential anticancer effects against breast and colon cancers compared with native curcumin. A simple, accurate, and rapid isocratic reverse phase high performance liquid chromatography (HPLC) analytical method utilizing UV detection was developed and validated for the determination of PAC utilizing C18 column with run time was 7 min. Chromatogram showed a peak of PAC at retention time of 5.8±0.92 min. The method was validated for linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. Linear relationship (r > 0.99) was observed between AUP of PAC and the corresponding concentrations over 100-10000μg/mL. The LOQ of this assay was 3.9ng/mL with a corresponding relative standard deviation of 4.8 and 4.0%. The LOD was 13.1ng/mL at a signal-to-noise ratio of >3.The present work reports the synthesis of Schiff base series of nicotinic hydrazide (C-1-C-5) and it's antibacterial and wound healing evaluation. The synthetic molecules were characterized with different spectroscopic techniques and explored for their antibacterial potential. The objective of this work was to explore antimicrobial agent using two types of microorganisms, one Gram-positive (S. aureus ATCC 9144) and one Gram-negative (E. coli ATCC 10536). C-2, C-4 and C-5 potentially inhibit bacterial growth (p less then 0.001). Atomic force microscopy (AFM) imaging was obtained to get high-resolution images of the effect of treated drugs on the bacterial morphology. The images obtained also revealed the antibacterial effects of potent molecule. The magnified pictures captured under AFM suggest significantly damaged cell surface and disturbed morphology. The compounds were further analyzed for in vivo wound healing potential on ****. The compound C-2, C-4 and C-5 heal the wounds comparatively in less time duration as compared to control group (p less then 0.
The buckthorn "Rhamnus alaternus" is a plant used in traditional medicine especially in the treatment of certain diseases such as diabetes, cardiovascular disease and dyslipidemia. The aim of our study was to analysed and evaluate the effects of buckthorn on nephroangiosclerosis Wistar rats. Thirty male Wistar rats, adult weighing between 120g and 250g were distributed as follows Five control animals received a standard laboratory diet, thirty four experimental rats received the standard laboratory diet supplemented with palm oil and 4% of NaCl (High Sold Fat Diet). After six month of this diet the HSFD group was subdivided into rats treated for 45 days with aqueous extract of buckthorn or animals HSFD only. Plasma metabolites and endothelin-1 concentration were measured by standard methods, section of kidney were stained by Heindenhain-azan and periodic acid shiff. The examination of renal parenchyma of HSFD rats showed a prominent structural changes such as, obstruction of vascular lumen, ischemia of the glomerular and tubulo-interstitial fibrosis the biochemical and hormonal parameters were significantly improved in the HSFD rats treated with decoction of buckthorn. Moreover, the morphogical changes of the renal parenchyma were attenuated in rats HSFD decoction. The buckthorn attenuates renal parenchymal lesions by aggregating at different levels of rats maintained on HSFD.Among the physicochemical properties, pKa and LogP values help us in studying drug parameters like ADME and could be predicted to some extent. https://www.selleckchem.com/ With this view, here we wish to predict these two properties of our previously synthesized biologically active derivatives of isoniazid using on-line available program Marvin, a Java-based chemical software application frequently used for chemical modeling. According to Marvin, pKa values predicted 99.99% unionized states of INH and some derivatives at physiological pH 7.4. Marvin calculated LogP values estimated good oral absorption for all the synthesized compounds. Therefore it can be said that the findings of the study emerged in an ideal region that permits the formulation of these derivatives. Since this was just a theoretical study, it demands more experimentation to determine accurate situation.Human diseases like viral organisms for example, hepatitis, HIV and etc., attack the health and caused large mortality in populations by many years. So finding novel delivery vehicles based antiviral drugs employing nano-materials is of high universal interest. In current approach a very biocompatible biodegradable nano-biopolymer anionic linear globular dendrimer second generation G2 was elaborately conjugated to a well-known anti-HIV drug Azidovudine and thereafter was characterized by different analytical techniques like AFM, Zeta sizer, 1HNMR, FTIR and LC-Mass spectroscopy. Then, Anionic Linear Globular DendrimerG2-Zidovudine Nano-Conjugate was assessed on human normal cells (toxicity assay by XTT test) and also HIV cell model and the results showed that Anionic Linear Globular DendrimerG2-Zidovudine Nano-Conjugate Significantly Decreased Retroviral Activity without any human cell toxicity respectively. Based on current experimental data such nano-compositions is proposed for further in vivo anti-HIV assays as well.The DPPH radical scavenging potentials of the fractions were determined in comparison to positive controls such as quercetin with EC50 = 4.12±1.27, ascorbic acid with EC50 = 6.20±1.67, gallic acid with EC50 = 4.75±1.24 and α-tocopherol with EC50 = 32.50±1.57 μg/mL. The experiment showed that aqueous fractions of the bark extracts of Abies pindrow (fraction C2) and Cedrus deodara (fraction E2) showed significantly lower EC50 values of 2.5±0.5 and 2.5±0.6 μg/mL, respectively. In reducing power assay, lower EC50 values of 5.5 and 4.5μg/mL were recorded for the aqueous fraction (fraction C 2) and final residue (fraction C5), of Abies pindrow, respectively. The ethyl acetate, acetone and final fractions of knot wood of Picea smithiana were found significantly active against all bacterial strains. Of the most sensitive fractions towards all the fungal strains was ethyl acetate fraction obtained from the bark of Cedrus deodara with a zone of inhibition ranging from 75 to 88 % that was more than the standard fluconazole.Curcumin (Diferuloylmethane) is a natural product extracted from the root of Curcuma longa. 5-Bis (4-hydroxy-3-methoxybenzylidene)-N-methyl-4-piperidone, the piperidone analogue of curcumin (PAC), was one of the analogues that, demonstrated potential anticancer effects against breast and colon cancers compared with native curcumin. A simple, accurate, and rapid isocratic reverse phase high performance liquid chromatography (HPLC) analytical method utilizing UV detection was developed and validated for the determination of PAC utilizing C18 column with run time was 7 min. Chromatogram showed a peak of PAC at retention time of 5.8±0.92 min. The method was validated for linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. Linear relationship (r > 0.99) was observed between AUP of PAC and the corresponding concentrations over 100-10000μg/mL. The LOQ of this assay was 3.9ng/mL with a corresponding relative standard deviation of 4.8 and 4.0%. The LOD was 13.1ng/mL at a signal-to-noise ratio of >3.The present work reports the synthesis of Schiff base series of nicotinic hydrazide (C-1-C-5) and it's antibacterial and wound healing evaluation. The synthetic molecules were characterized with different spectroscopic techniques and explored for their antibacterial potential. The objective of this work was to explore antimicrobial agent using two types of microorganisms, one Gram-positive (S. aureus ATCC 9144) and one Gram-negative (E. coli ATCC 10536). C-2, C-4 and C-5 potentially inhibit bacterial growth (p less then 0.001). Atomic force microscopy (AFM) imaging was obtained to get high-resolution images of the effect of treated drugs on the bacterial morphology. The images obtained also revealed the antibacterial effects of potent molecule. The magnified pictures captured under AFM suggest significantly damaged cell surface and disturbed morphology. The compounds were further analyzed for in vivo wound healing potential on mice. The compound C-2, C-4 and C-5 heal the wounds comparatively in less time duration as compared to control group (p less then 0.
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