Cancer now is one of the leading causes of mortality in the world. There has been a lot of effort to discover new anticarcinogenic agents that allow treatment with fewer side effects. A series of isoxazole-carboxamide derivatives (2a–2g) were synthesised and evaluated for their cytotoxic activity against breast (MCF-7), cervical (HeLa), and liver (Hep3B) cancer cell lines and their antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The results showed that 2d and 2e were the most active compounds against Hep3B cells, with a half-maximal inhibitory concentration (IC50) of around 23 μg/ml; 2d showed the highest activity against HeLa cells, with an IC50 15.48 μg/ml. However, 2a had the lowest IC50 (39.80 μg/ml) against MCF-7 cells. By contrast, compound 2g was inactive against all cancer cell lines, with IC50 values >400 μg/ml. Both 2d and 2e reduced Hep3B secretion of alpha-fetoprotein (to 1829.33 ± 65.91 ng / ml and 1758.66 ± 54.04 ng / ml , respectively). Furthermore, in cell cycle analysis, 2d and 2e induced a delay in the G2/M phase of 18.07%, which is similar to the doxorubicin positive control. Moreover, 2d and 2e reduced the necrosis rate of Hep3B threefold and instead shifted the cells to apoptosis. Our results indicate that 2d and 2e have potent and promising anticancer activity. However, compound 2a was the most active as antioxidant agent ( I C 50 = 7.8 ± 1.21 μ g / ml ) compared with Trolox as a positive control (IC50 2.75 μg/ml).
The in vitro activity of azithromycin, an orally active azalide, was compared with that of erythromycin and oral beta-lactams against 893 clinical isolates of staphylococci, streptococci, enterococci, Haemophilus influenzae and Salmonella typhi. MIC 90 of azithromycin for streptococci was 0.12 mg/L, 0. Azithromycin is an orally active azalide antibiotic with a chemical structure of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, molecular formula of C 38 H 72 O 12 N 2 , 2H 2 O and molecular weight of 785.01 Kd.1 It contains an aza-methyl substitution at position 9a of the 15-member aglycone ring as compared to 14-member erythromycin.24 Insertion of nitrogen into the lactone ring has been reported to increase its antibacterial activity against gram negative bacteria.1,2 We compared the in vitro activity of this compound with erythromycin and other oral beta-lactam drugs against clinical isolates of staphylococci, streptococci, enterococci, Haemophilus influenzae and Salmonella typhi. Material and MethodsClinical isolates from 893 patients at the King Faisal Specialist Hospital and Research Centre (KFSH&RC) were used for comparative in vitro evaluation of azithromycin. KFSH&RC is a 500-bed tertiary care referral facility in Riyadh, Saudi Arabia. Bacterial isolates were identified by standard routine laboratory procedures.5 Antimicrobial susceptibility testing was performed by the agar dilution method as recommended by the National Committee for Clinical Laboratory Standards.6 Mueller-Hinton agar with or without 5% sheep blood (Difco Laboratories, Detroit, MI, USA) with a pH between 7.2 and 7.4, was used throughout the study except for H. influenzae, where chocolate agar was used. The bacterial suspensions were adjusted to 10 7 CFU/ml and inoculated onto the agarsurface with a multipoint inoculator to contain 10 4 CFU/spot. All incubations were at 35°C for 18 to 24 hours. Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and Staphylococcus aureus ATCC 29213 were used as quality control (QC) organisms. The QC results were found to be within the normal expected range during the period of this study. ResultsA total of 893 isolates, consisting of 393 staphylococci, 228 streptococci, 210 H. influenzae and 62 strains of S. typhi were used to evaluate the in vitro activity of azithromycin and the results were compared with erythromycin, ampicillin, augmentin and cephalexin (Table). MIC 90 of azithromycin for members of the genus Streptococcus was 0.12 mg/L, which was comparable to that of erythromycin. Erythromycin-resistant enterococci had an MIC of >32 mg/L for azithromycin. MIC 50 and MIC 90 of azithromycin for methicillin-susceptible S. aureus were four to eight times higher than erythromycin; like erythromycin, azithromycin had virtually no activity against methicillinresistant S. aureus. All the 210 isolates of H. influenzae were inhibited by <0.5 mg/L of azithromycin, its activity being superior to erythromycin and the beta-lactams tested. A single concentration of 8.0 mg/L of this drug inhibited 97% i...
The pericardial space should not be irrigated with betadine'0.Constriction may be less common in pneumococcal than in tuberculous effusions where fibrosis is marked. The main advantage of catheter drainage is avoiding pericardial surgery in ill patients, particularly those with m3ycarditis or biventricular dysfunction'. In a n, in patients with limited recurrence oftheir effusion, an indwellingtcatheter may be removed at an early stage. More reports of.this promising, relatively non-invasive, inexpesive approach to the treatment of pericardial effusion are required.References 1 Kauffman CA, Watanakunakorn C, Phair JP. Purulent pneumococcal pericarditis, a continuing psvblem in the antibiotic era. Am
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