Synthesis and antibacterial study of some s-substituted aliphatic analogues of 2-mercapto-5-(1-(4-toluenesulfonyl) piperidin-4-yl)-1,3,4-oxadiazole

Purpose: To synthesize a series of analogues of 1,3,4-oxadiazole and to evaluate their antibacterial activity. Methods: Ethyl piperidin-4-carboxylate (1) was mixed with 4-toluenesulfonyl chloride (2) in benignant conditions to yield ethyl 1-(4-toluenesulfonyl)piperidin-4-carboxylate (3) and then 1-(4- toluenesulfonyl)piperidin-4-carbohydrazide (4). Intermolecular cyclization of 4 into 2-mercapto-5-(1-(4- toluenesulfonyl) piperidin-4-yl)-1,3,4-oxadiazole (5) was obtained on reflux with CS2 in the presence of KOH. Molecule 5 was stirred with alkyl halides, 6a-i, in DMF in the presence of LiH to synthesize the final compounds, 7a-i. The structures of these molecules were elucidated by Fourier transform infra-red (FTIR) spectroscopy, proton nuclear magnetic resonance (1H-NMR) and electron impact mass spectrometry (EI-MS). Antibacterial activity was evaluated against five bacterial strains, namely, Salmonella typhi, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis, with ciprofloxacin used as standard antibacterial agent. Results: Out of nine synthesized derivatives, compound 7a was the most active against three bacterial strains, S. typhi, E. coli and P. aeruginosa, with minimum inhibitory concentration (MIC) of 9.11 ± 0.40, 9.89 ± 0.45 and 9.14 ± 0.72 μM, respectively, compared with 7.45 ± 0.58, 7.16 ± 0.58 and 7.14 ± 0.18 μM, respectively, for the reference standard (ciprofloxacin). Similarly, compounds 7a - 7c showed relatively good antibacterial activity against B. subtilis strain while compound 7e - 7g revealed good results against S. typhi bacterial strain. Conclusion: The results indicate that S-substituted derivatives of the parent compound are more effective antibacterial agents than the parent compound, even with minor differences in substituents

Awareness and Coverage of the National Health Insurance Scheme among Formal Sector Workers in Ilorin, Nigeria

A prepayment scheme for health through the National Health Insurance Scheme (NHIS) was commenced in Nigeria about ten years ago. Nigeria operates a federal system of government. Sub- national levels possess a high degree of autonomy in a number of sectors including health. It is important to assess the level of coverage of the scheme among the formal sector workers in Nigeria as a proxy to gauge the extent of coverage of the scheme and derive suitable lessons that could be used in its expansion. This is a cross-sectional, descriptive survey carried out among formal sector workers in Ilorin Kwara State, Nigeria. A stratified sampling technique was used to select study participants. A self-administered questionnaire was used to collect data from respondents. Data was analysed with the SPSS. Ethical approval to conduct the study was obtained from the Bowen University Teaching Hospital Research Ethics Committee. A total of 370 people participated in the study. Majority, (78.9%) of the respondents were aware of the NHIS, however only 13.5 % paid for health care services through the NHIS. Logistic regression analysis shows that respondents with post-secondary education (OR = 9.032, CI = 2.562 – 31.847, p = 0.001) and in federal civil service (OR = 2.679, CI = 1.036 – 6.929, p = 0.042) were over nine and three times more likely to be aware of the scheme than others. Coverage of the scheme among the respondents was unimpressive. A lot still need to be done to fast-track the expansion of the scheme among this sector of the population.

NUTRITIONAL COMPOSITION AND ANTIOXIDANT PROPERTIES OF RAPHIONACME SPLENDENS (SCHL.) TUBERS

People of Western Kordofan (Sudan) are endowed with a deep knowledge concerning the use of wild plants. Tubers of Raphionacme splendens Schl. subspecies splendens Flickr (family Apocynaceae), locally known as Elfayo, are used as a food reserve during times of famine or poor harvest. The aim of this study was to analyze the nutritional composition and antioxidant capacity of root tubers of R. splendens. Samples were collected from South-West Kordofan. Analyses included determination of moisture, carbohydrate, crude protein, fat, fibre, ash, minerals, vitamin C, amino acids and fatty acids composition. Antioxidant activity was determined by the DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2.2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) assays. The total phenolic content was also assessed. The results, which are referred to as (%) dry weight, showed that the tubers contained 3.2% protein, 18% carbohydrate, 0.5% lipid, 2.4% crude fibre, 3.5% ash, 79.2% moisture and gross energy 101.7 kJ/g. The total amino acids were 10776 mg/100g where the essential amino acids represented 28.2%. The more abundant essential amino acids were leucine (792mg/100g), isoleucine (712mg/100g) and threonine (536mg/100g). Methionine and lysine were the limiting amino acids. Minerals were potassium (259mg/100g), calcium (183mg/100g), magnesium (64mg/100g), phosphorus (37mg/100g), copper (3.6mg/100g), manganese (2.4mg/100g), zinc (1.8mg/100g) and iron (1.2mg/100g). Total saturated fatty acids were 45.6% whereas total unsaturated fatty acids were 54.4%. Oleic acid (32.56%) and palmitic acid (30.23%) were the most abundant fatty acids. Tubers displayed good antioxidant activity with IC50 values 0.987 and 1.559mg/mL against DPPH and ABTS radicals respectively. Vitamin C was 31.5mg/100g and total phenolic content was 60mg gallic acid equivalent (GAE) per 100g dry sample and they could be the main contributor to the antioxidant capacity of the tubers. In conclusion, the results of this study suggested that tubers of R. splendens could have beneficial effect for food and/or nutraceutical application for normal growth and adequate protection against diseases associated with reactions of free radicals.

In vitro antioxidative activity of moss extract, and effect of moss on serum lipid level of mice fed with high-fat diet

Purpose: To evaluate the potential of active compounds derived from moss in the prevention and treatment of various diseases. Methods: Three species of moss were extracted with deionized water at 95 °C, and with 70.5 % ethanol at 85 °C. Analysis of total phenolic contents (TPC) of the extracts were performed by FolinCiocalteu (FC) method. The antioxidant activity of the extracts were determined using three methods, namely, by 2,2\'-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP). In vivo effects were evaluated in mice fed high fat diet (HFD) supplemented with 20 % ground moss. Cholesterol levels in HFD were evaluated by ophthalaldehyde method. Serum triglyceride levels were measured using triglyceride (TG) kit, while blood insulin level and leptin concentration were measured by enzyme-linked immunosorbent assay (ELISA) kit. Results: The moss extracts exhibited antioxidative effects, as evidenced of . TPC of 47.20 ± 11.20 to 119.87 ± 11.51 mg GAE/mg, respectively. ABTS scavenging activity was 1078.11 ± 18.95 to 2587.33 ± 46.19 μmol Trolox/mg, DPPH scavenging activity of were 42.11 ± 8.22 to 298.78 ± 20.02 μmol Trolox/mg, and FRAP value of 393.19 ± 24.64 to 1070.14 ± 17.92 μmol Trolox/mg, respectively. Mice fed with 20 % ground moss did not show any significant effect (p < 0.05) on visceral weight and blood lipid levels of HFD, while leptin concentrations reduced significantly to 4.74 ± 0.00 and 0.20 ± 0.00 ng/dL) relative to HFD alone (26.72 ± 6.53 ng/dL). Conclusion: Moss can potentially be used as an antioxidative ingredient, for the improvement of overall human health, suggesting that important medical benefits associated with moss consumption. However, further investigations are required to ascertain this.