Adebusayo E. Adedapo

Functionalized Benzimidazole Scaffolds: Privileged Heterocycle for Drug Design in Therapeutic Medicine

Benzimidazole derivatives are crucial structural scaffolds found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research. They are structural isosteres of naturally occurring nucleotides, which allows them to interact with the biopolymers of living systems. Hence, there is a need to couple the latest information with the earlier documentations to understand the current status of the benzimidazole nucleus in medicinal chemistry research. This present work unveils the benzimidazole core as a multifunctional nucleus that serves as a resourceful tool of information for synthetic modifications of old existing candidates in order to tackle drug resistance bottlenecks in therapeutic medicine. This manuscript deals with the recent advances in the synthesis of benzimidazole derivatives, the widespread biological activities as well as pharmacokinetic reports. These present them as a toolbox for fighting infectious diseases and also make them excellent candidates for future drug design.

Disinfection Byproducts in Drinking Water and Evaluation of Potential Health Risks of Long-Term Exposure in Nigeria

Levels of trihalomethanes (THMs) in drinking water from water treatment plants (WTPs) in Nigeria were studied using a gas chromatograph (GC Agilent 7890A with autosampler Agilent 7683B) equipped with electron capture detector (ECD). The mean concentrations of the trihalomethanes ranged from zero in raw water samples to 950 μg/L in treated water samples. Average concentration values of THMs in primary and secondary disinfection samples exceeded the standard maximum contaminant levels. Results for the average THMs concentrations followed the order TCM > BDCM > DBCM > TBM. EPA-developed models were adopted for the estimation of chronic daily intakes (CDI) and excess cancer incidence through ingestion pathway. Higher average intake was observed in adults (4.52 × 10−2 mg/kg-day), while the ingestion in children (3.99 × 10−2 mg/kg-day) showed comparable values. The total lifetime cancer incidence rate was relatively higher in adults than children with median values 244 and 199 times the negligible risk level.

A new method for assessment of sediment-associated contamination risks using multivariate statistical approach

Graphical abstract

Chemical Speciation and Characterization of Trace Metals in Dry Camellia sinensis and Herbal Tea Marketed in Nigeria

Background. Trace metals from anthropogenic activities have been found to occur in tea brands and pose potential human health risks to consumers. Objectives. The present study assessed the concentrations of trace metals in green, black and herbal tea brands using a modified Community Bureau of Reference sequential extraction method. Methods. Fifteen (15) Camellia sinensis and eight (8) herbal tea samples commonly consumed in Nigeria were collected and analyzed for trace metals. The concentrations of cadmium (Cd), chromium (Cr), copper (Cu), manganese (Mn), nickel (Ni), lead (Pb), vanadium (V), and zinc (Zn) in extract fractions were analyzed using microwave plasma atomic emission spectroscopy (MP-AES). Results. Trace metals were detected in all of the samples investigated. The concentrations of trace metals in 4 stages (soluble/exchangeable/carbonates bound fraction, reducible fraction, oxidizable fraction, residual fraction) of sequential and pseudo-total metal extraction procedures are presented. The concentrations of Cd, Cr, Cu, Mn, Ni, Pb, V, and Zn in the exchangeable/carbonate bound fraction for green tea ranged between 0.27–1.47, ND-0.33, ND-0.44, 7.05–33.04, 0.23–0.69, ND-0.51, ND-0.16 and 0.18–1.99 mg/kg, ND-0.73, 0.15–0.36, 0.36–0.59, 1.38–30.07, 0.15–0.54, 0.05–0.76, 0.15–0.34 and 0.27–0.77 mg/kg and 0.54–0.64, 0.25–0.41, 0.35–0.47, 18.72–23.98, 0.30–0.55, 0.15–0.21, 0.15–0.23 and 0.30–0.48 mg/kg for hebal tea, respectively. Conclusion. The metal content in the investigated tea indicated low to enhanced concentrations. Locally produced black teas recorded relatively low trace metal contents compared to the green and herbal tea samples. The most bioavailable trace metal was Mn, while Zn was most preferably bound to the residual fraction. Cadmium, Cr, Cu, Ni, Pb, and V were distributed at varied concentrations among other extractable phases. Daily consumption of the investigated tea products may expose consumers to potentially toxic metals as well as essential elements. Competing Interests. The authors declare no competing financial interests.

Trace and major elements distribution in coastal sediment cores from Lagos Lagoon, Nigeria

Heavy metals contamination in aquatic ecosystems has been a major concern, however, no information is available about the concentrations, depth distributions and ecological risks of heavy metals in sediments cores from microtidal lagoonal ecosystem in Lagos, Nigeria. Four sediment cores were collected using a 50 cm × 3.5 cm Wildco® hand corer. Elemental determinations were carried out using the Microwave Plasma Atomic Emission Spectrometry (4200 MP-AES) after extraction. The concentrations of heavy metals in the sediment cores indicated enhanced degree of contamination influenced by anthropogenic discharges especially industrial effluents. Vertical depth distributions indicated varied depositional periods largely controlled by increasing anthropogenic land-based activities. The remarkable metal pollution of core sediments raises the concern potential sources of metals to the lagoonal ecosystem and ecological risks to the biota, humans, and the environment. The results of elemental concentrations should be considered as baseline data for heavy metals in sediments in the region.

Characterisation of Polychlorinated Biphenyls in Coastal Inland Seawater, Nigeria

The concentrations of polychlorinated biphenyls (PCBs) were determined in samples of surface seawater collected from five (5) different locations along the coastline of a tropical lagoon. The surface water samples were analysed using gas chromatography coupled with electron capture detector (GC-ECD) with fifteen (15) PCB congeners detected across the studied area. The chlorobiphenyls levels are in the order Ebute Ero > Oko Baba > Ijora > Lagos Island > Unilag lagoon front with levels 107.89, 53.15, 34.90, 27.78, and 2.15 mg/L, respectively. The enhanced average concentration of PCBs at the Ebute Ero site is due to the predominance of PCB-180 and PCB-185. A negative correlation was found between the total PCB concentration and the level of dissolved oxygen. Although, the results indicated fairly high levels of PCBs, the anthropogenic contributions from industrial releases and domestic activities may be largely associated with the detected concentrations of the di-, tetra-, penta-, hexa-, hepta-, and octa-chlorobiphenyls