Mangumpenn7335

Although Hydroxyurea is one of the most widely used drugs in treating breast cancer, the use of it leads to some side effects. Hence, in order to reduce complications of treatment and increase its efficiency, drug delivery has been attracted more attention. Present study included three stages. The first stage was involved in the synthesis of nanoparticles-loaded Hydroxyurea that its characteristics were evaluated by using scanning electron microscopy and Zetasizer system. In the second stage, cultured MCF-7 cells were undergone treatments by Hydroxyurea and Nanoparticles-loaded Hydroxyurea in various concentrations. In the third stage, the MCF-7 was treated by IC50 of Hydroxyurea and nanoparticles-loaded Hydroxyurea which are in combination with radiation and hyperthermia. Afterward, the viable of cell, apoptosis, and levels of caspase-8 and-9 proteins were assessed. The average size and the potential surface of nanoparticles and nanoparticles-loaded Hydroxyurea were 26 nm, 48 nm, 3.86 mV, and -29.3 mV, respectively. Results of MTT assay and apoptosis represented that the percentage of cytotoxicity in the treated groups by in combination group and nanoparticles-loaded Hydroxyurea was significantly increased in comparison with Hydroxyurea. This increase was dependent on the concentration of nanoparticles-loaded Hydroxyurea. Nevertheless, the activity of caspase-8 shows any significant changes, the activity of caspase-9 was significantly increased in the control and treatment groups. We concluded that nanoparticles-loaded Hydroxyurea and it in combination with radiation and hyperthermia induces mitochondrial-dependent apoptosis by down-regulation of caspase-8 and up-regulation of caspase-9 expressions and have higher toxicity effect on MCF-7 cells in comparison with pure Hydroxyurea.LED light is used for many medical and cosmetic applications such as phototherapy and skin rejuvenation. Such physical methods can be combined with drug therapy, such as LED-responsive drug delivery system, the subject of present investigation. To perform this investigation, a nanoliposome composed of DPPC, DSPE-PEG2000, and DC8,9PC, was prepared as LED-sensitive systems. Calcein was loaded in the liposomes as a fluorescent probe for drug release studies. Different LED wavelengths (blue, green and red) were used for triggering release of calcein from nanoliposome. Indoor daylight, darkness, and sunlight were applied as controls. Results showed that liposomes do not release their cargo in darkness, but they released it in response to indoor daylight, sunlight and LEDs, with the blue light showing the highest effect. Results also showed that release of calcein was sensitive to wavelength. Our results reveal potential of LED-sensitive liposomes for medical and cosmetic applications and that such system can be combined with phototherapy. Such concomitant therapies can increase medical/cosmetic effects and decrease adverse reactions to phototherapy.In order to expand the application of Fe3O4@SiO2-SnCl4 in the synthesis of heterocyclic compounds, in this study, we wish to report the use of one-pot three component synthesis of pyrimido [4,5-b]quinolone derivatives ( D1-D16 ) through reaction of 6-amino-2-(methylthio)pyrimidin-4 (3H)-one, dimedone, or 1,3-cyclohexadione and aldehydes in the presence of Fe3O4@SiO2-SnCl4 as an efficient eco-friendly catalyst under ultrasound irradiation. The final aim of this study is evaluation of antifungal activity of resulted products. Synthesis of pyrimido [4,5-b]quinolin derivatives were done via three components coupling reaction of aldehyde, dimedone or 1,3-cyclohexadione and 6-amino-2-(methylthio)pyrimidin-4 (3H)-one in the presence of Fe3O4@SiO2-SnCl4 under ultrasonic irradiation in water at 60 °C. The products structure were studied by FT-IRI, 1H NMR,II and 13C NMRII. All the compounds were screened for antimicrobial activity by broth microdilution methods as recommended by CLSIIII. Considering our results showed that compound ( D13 ) had the most antifungal activity against C. dubliniensis, C. Albicans, C. Tropicalis, and C. Neoformance at concentrations ranging (MIC90) from 1-4 μg/mL. Compounds ( D9 ), ( D10 ), ( D14 ), and ( D15 ) had significant inhibitory activities against C. dubliniensis at concentrations ranging (MIC90) from 4-8 μg/mL, respectively. 5-(3,4-dihydroxyphenyl)-8,8-dimethyl-2-(methylthio)-5,8,9,10-tetrahydropyrimido[4,5-b]quinoline-4,6(3H,7H)-dione ( D13 ) exhibited inhibitory and fungicidal activities against the tested yeasts. The specific binding mode or the binding orientation of more efficient compounds to CYP51 active site, have been also performed by molecular modeling investigations and showed that there is a good correlation with biological test.Levisticum officinale (Apiaceae) is a favorite food spice. Iranian folk medicine claims that it has a prominent antidyslipidemic property but this is not documented scientifically so far. This study evaluated antidyslipidemic and the other antidiabetic aspects of the stem and leaf hydroalcoholic extract of it (LOE). Regarding oral glucose tolerance test results, LOE (500 mg/kg) administration 30 min before glucose loading significantly decreased the blood glucose level (13%) at 90 min in male rats. Additionally, LOE treatment (500 mg/kg, orally, once a day) for 14 days significantly reduced the serum glucose level (24.97%) and markedly improved the lipid profile and the insulin, creatinine, alanine aminotransferase and aspartate aminotransferase serum levels in diabetic rats. Moreover, LOE effectively amended the impaired antioxidant status and ameliorated lipid peroxidation in the plasma and pancreas and liver tissues of diabetics. Also, 14 days LOE treatment, significantly decreased the renal sodium-glucose cotransporter 2 and facilitated glucose transporter 2 (GLUT2) mRNA levels and GLUT2 gene expression in the enterocytes of jejunum tissue in comparison with diabetic untreated rats. PF-07104091 HPLC method revealed the presence of chlorogenic acid, rosmarinic acid, caffeic acid, quercetin and luteolin and GC-MS analysis detected bioactive compounds like phthalides, thymol, phytol, hexanoic acid, carene and menthofuran. LOE showed α-amylase (αΑ) inhibitory activity and in silico studies predicted that among extract ingredients luteolin, quercetin, rosmarinic, caffeic, and hexanoic acids have the greatest αΑ inhibition potecy. Thus, current results justify antidyslipidemic value of L. officinale and shed light on more antidiabetic health benefits of it.