The synthesis of boronic-imine structured compounds and identification of their anticancer, antimicrobial and antioxidant activities

Boronic acid compounds with different substituted groups were handled to synthesize various ligands encoded as B1, B2, B3, B4, B5, B6, B7 and B8. B5 and B7 were tested for the cytotoxic activity against the prostate cancer cells and it was found that the cell viability of cancer cells was decreased while most of the healthy cells could still be viable. 5 µM solutions of B5 and B7 decreased the cell viability to 33% and 44% whereas healthy cells were 71% and 95%, respectively, after treatment. Antimicrobial properties were explored against the bacterial and fungal microorganisms with B1, B5 and B7. The inhibition zones were evaluated for all boronic structures, and the growth inhibition zones were determined in a range of 7–13 mm diameter for different microorganism species. Staphylococcus aureus was the common microorganism that three boronic compounds with imine ligands showed the activity. Antioxidant features of B2, B3, B4, B5, B6, B7 and B8 were investigated by different processes such as Beta-carotene bleaching (BCB), 2,2-diphenyl picryl hydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and CUPric reducing antioxidant capacity (CUPRAC) methods. Significant antioxidant activity was achieved by the phenyl boronic based ligands and these compounds demonstrated as much activity as standards (α-Toc and BHT). In addition, all structures were applied properly without any decomposition during the experiments. They were rather stable both in aqueous media and solid state

COMPARISON OF CANDIDA COLONIZATION IN INTENSIVE CARE UNIT PATIENTS WITH AND WITHOUT COVID-19: FIRST PROSPECTIVE COHORT STUDY FROM TURKEY

POSTER SESSION 3, SEPTEMBER 23, 2022, 12:30 PM - 1:30 PM:   OBJECTIVES: Candida species, as the main component of human mycobiome, are the most common cause of fungal infections in intensive care units (ICU). ICU patients with COVID-19 are more prone to fungal infections, due to various causes like mechanical ventilation, use of steroids, or long-term hospitalization. There is yet no extended prospective study examining Candida colonization rates, epidemiology of species, and predisposing factors in this population. This is the first prospective cohort study comparing the time-varying colonization features of Candida species in ICU patients with and without COVID-19. METHODS: This study was performed between March 2021-December 2021 in ICUs of Istanbul University, Istanbul Faculty of Medicine, Department of Anesthesiology and Reanimation. COVID-19 and non-COVID-19 ICU patients who were ≥ 18 years and expected to stay in the ICU for at least 7 days were included in the study. Samples were taken at certain time intervals from different body parts of the patients [mouth, skin (axilla), rectal, and urine] (Table 1) and evaluated at Istanbul University, Istanbul Faculty of Medicine, Department of Medical Microbiology, Mycology Laboratory. All specimens were inoculated on CHROMagar Candida media (CHROMagar Candida, France) to detect mixed growth and CHROMagar Candida Plus media (CHROMagar Candida Plus, France) to avoid missing Candida auris. Cultures were incubated at 35-37⁰C for 48 h and phenotypically different colonies on primary media were subcultured on corn meal-tween-80 agar for determining their morphology. All strains were identified to the species level using MALDI-TOF MS (Version 4.1.80; Biotyper Bruker) in Yeditepe University, Faculty of Engineering, Genetics and Bioengineering Department. Patient groups were compared statistically in terms of isolated Candida species and distribution according to regions. RESULTS: The study consisted of 122 ICU patients including 62 COVID-19 (25 female; 37 male; mean age:63.29 years) and 60 non-COVID-19 (24 female; 36 male; mean age:63.9 years). A total of 1464 samples (756 COVID-19 and 708 non-COVID-19 patients) were taken (Table 1) and fungi grew in 340 (23.2%) samples. Mixed growth was observed in 108 cultures; was more frequently in COVID-19 patients (P < .05), and significantly higher in oral specimens (P < .05). Out of a total of 471 strains that were obtained from fungal cultures, C. albicans (42.25%) and C. glabrata (24.2%) were most frequently isolated. Candida auris was not observed in this period (Table 2). Patients with COVID-19 were found more frequently colonized in oral (P < .001), rectal (P < .05) regions and urine (P < .001) compared with non-COVID-19 patients. There was no growth in the axillary region in any of the patients. Non-albicans Candida strains were found significantly more frequent in patients with COVID-19 in oral (P < .001) and rectal regions (P < .05). CONCLUSION: In this study, we found significantly higher oral, rectal, and urine Candida colonization rates in COVID-19 ICU patients compared with non-COVID-19 individuals. Increased oral Candida colonization can be the result of insufficient oral care application to these patients in the ICUs due to infection control anxiety, and also mechanical ventilation. Because non-albicans Candida strains were found significantly more frequent in COVID-19 patients, intrinsically resistant isolates should be kept in mind before administering antifungals. The high mixed growth rate detected in all individuals and especially in COVID-19 patients will affect the antifungal therapy and therefore emphasized the importance of using chromogenic media for routine evaluation

Design, synthesis, and molecular docking studies of a conjugated thiadiazole-thiourea scaffold as antituberculosis agents

In view of the emergence and frequency of multidrug-resistant and extensively drug-resistant tuberculosis and consequences of acquired resistance to clinically used drugs, we undertook the design and synthesis of novel prototypes that possess the advantage of the two pharmacophores of thiourea and 1,3,4-thiadiazole in a single molecular backbone. Three compounds from our series were distinguished from the others by their promising activity profiles against Mycobacterium tuberculosis strain H37Rv. Compounds 11 and 19 were the most active representatives with minimum inhibitory concentration (MIC) values of 10.96 and 11.48 µM, respectively. Compound 15 was shown to inhibit M. tuberculosis strain H37Rv with an MIC value of 17.81 µM. Cytotoxicity results in the Vero cell line showed that these three derivatives had selectivity indices between 1.8 and 8.7. In order to rationalize the biological results of our compounds, molecular docking studies with the enoyl acyl carrier protein reductase (InhA) of M. tuberculosis were performed and compounds 11, 15, and 19 were found to have good docking scores in the range of -7.12 to -7.83 kcal/mol.status: publishe