ABSTRACT
BACKGROUND PROBLEM: Antibiotic resistance is considered a global problem, where highly emerging antibacterial resistance is posing a great threat to treat infections. OBJECTIVES: The present study is aimed to highlight emerging resistance of bacteria to commonly used antibiotics in Pakistan. METHODS: The samples for bacterial culture were obtained using high vaginal swabs (HVS) from female genitalia. The specimens were incubated and identified for subsequent pathogenic bacterial growth. There were 370 bacterial isolates from 520 females provisionally diagnosed for gynecological infections. RESULTS: Out of total 9 isolated bacteria, Escherichia coli were most common isolates (41.6%) followed by Staphylococcus aureus (15.4%), and coagulase negative staphylococci (12.2%). E. coli exhibited maximum susceptibility to meropenem (98.2%) and imipenem (97.7%) and least to amoxicillin (9.8%) and ampicillin (9.6%). The highest incidence of bacterial infection was found in age group of 26-35 years. Among Gram-positive bacteria, 98.7%, 88.2% and 81.3% were susceptible to vancomycin, cefuroxime and linezolid respectively. For Gram-negative bacteria, 94.3%, 93.6% were susceptible to cefoperazone/sulbactam and meropenem respectively. Recurrence of infection developed among 3.27% of the patients, while two patients died with the infection. CONCLUSION: Maximum resistance was shown by co-trimoxazole (81.4%), followed by amoxicillin (80.2%). After identifying the causative strain, the susceptible antibiotic should be administered to reduce antibiotic resistance and better control of gynecological infections in female Pakistani population.
Subject(s)
Bacterial Infections , Gram-Negative Bacterial Infections , Adult , Anti-Bacterial Agents/pharmacology , Bacterial Infections/epidemiology , Drug Resistance, Bacterial , Escherichia coli , Female , Gram-Negative Bacteria , Humans , Microbial Sensitivity Tests , Pakistan/epidemiologyABSTRACT
BACKGROUND: Due to the pressing need and adverse effects associated with the available anti-cancer agents, an attempt was made to develop the new anti-cancer agents with better activity and lesser adverse effects. OBJECTIVE: Synthetic approaches based on chemical modification of quinoline derivatives have been undertaken with the aim of improving anti-cancer agents' safety profile. METHODS: In the present study, quinoline derivatives 6-hydroxy-2-(4-methoxyphenyl) quinoline-4-carboxylic acid (M1) and 2-(4-chlorophenyl)-6-hydroxyquinoline-4-carboxylic acid (M3) were synthesized by the reaction of aldehyde and pyruvic acid. The complete reaction was indicated by thin-layer chromatography. Newly synthesized M1and M3were tested for in silico and in vitro studies. RESULTS: M1 and M3 were docked against selected targets. Both the test compounds showed good affinity against all targets except the p300\CBP-associated factor target as there was no H-bond formed by M1. IC50 values of M1 and M3 against 1, 1-diphenyl-picrylhydrazyl free radical scavenging activity were 562 and 136.56ng/mL, respectively. In brine shrimp lethality assay, M1 and M3 showed IC50 value of 81.98 and 139.2ng/mL, respectively. IC50 values recorded for M1 and M3 in tumor inhibition activity were 129 and 219µg/mL, respectively. M1 and M3 exhibited concentration-dependent anti-cancer effects against human cell lines of hepatocellular carcinoma (HepG2) and colon cancer (HCT-116). Against HepG2 cells, M1 and M3 exhibited IC50 of 88.6 and 43.62µg/mL, respectively. M1 and M3 utilized against HCT-116 cell lines possessed IC50 values of 62.5 and 15.3µg/mL. M1 and M3 also showed an anti-leishmanial effect with IC50 values of 336.64 and 530.142µg/mL, respectively. CONCLUSION: From the results of pharmacological studies, we conclude that the newly synthesized compound showed enhanced anti-oxidant, anti-cancer and anti-leishmanial profile with good yield.
Subject(s)
Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Antiprotozoal Agents/pharmacology , Leishmania tropica/drug effects , Molecular Docking Simulation , Quinolines/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Artemia , Biphenyl Compounds/antagonists & inhibitors , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Molecular Structure , Picrates/antagonists & inhibitors , Quinolines/chemical synthesis , Quinolines/chemistry , Structure-Activity RelationshipABSTRACT
Though, herbal medicines are prone to deterioration upon storage due to their complex nature, but less attention has been paid to investigating stability of such products to assign shelf-life. Therefore, the present study aimed to assess the accelerated stability of methanolic extract of seeds of Syzygium cumini. The extract was kept at three different storage conditions (30oC/60% RH, 40oC/75% RH and 60oC/85% RH) for a period of 6 months. The samples withdrawn at 0 (before starting the study), 1, 2, 3, 4 and 6 months were analyzed to get UV-Visible metabolomics fingerprints and determine caffeic acid contents using RP-HPLC. The comparison of metabolomics fingerprints indicated that the extract was stable for 1 month at all the three storage conditions. However, caffeic acid contents were found to be intact for a longer period of time. Following the zero order degradation, caffeic acid was predicted to be stable for more than 3 years, if kept at 25oC. The results of the present study indicate that metabolomes of methanol extract of seeds of Syzygium cumini change very fast, suggesting the development of stable formulations.
