Antiplasmodial activity of quinine-zinc complex and chloroquine: A comparative in vitro assessment

The evolving and complicating drug resistance exhibited by strains of Plasmodium falciparum to existing antimalarials like chloroquine and quinine (which are relatively more affordable than recent drugs) and advances in metal-drug complex research instigated this work. The antiplasmodial activity of the Quinine-Zinc complex (QZ) synthesized by a modification of the method of Singla and Wadhwa was assessed relative to that of Chloroquine diphosphate (C) in vitro. Measurement of antiplasmodial activity was carried out based on the inhibition of parasite growth measured by the inhibition of schizont formation in freshly collected infected blood samples from malaria patients. A comparative analysis of the antiplasmodial activity of QZ against C showed that its antiplasmodial activity was significantly better than that of C (p < 0.05). The result of this study suggests that the QZ could have a better therapeutic activity against malaria than C

Anti-tuberculosis activities of the crude methanolic extract and purified fractions of the bulb of Crinum jagus

Summary: Tuberculosis (TB) is of great public health burden globally especially in developing countries of Africa and Asia . Current TB regimen involves multiple therapies and of long duration leading to poor patient adherence. There is also the challenge of multidrug resistant TB. Hence, there is a need for discovery of new anti- TB drugs. This study was designed to investigate the in –vitro activity of the crude methanolic extract and chromatographic fractions of the bulb of Crinum jagus against Mycobacterium tuberculosis isolates. The extracts were screened for anti- TB activity against three different M. tuberculosis isolates and a drug susceptible reference strain H37Rv using Lowenstein Jensen (L-J) medium and Middlebrook 7H10agar. The crude extract was prepared using soxhlet extraction apparatus while the purified fractions were obtained by column chromatography. The two media were inoculated with M. tuberculosis strains, after which the crude and purified extracts were added. After 4-6 weeks incubation, colony forming units were counted and percentage inhibition calculated. The crude extract and the purified fractions showed inhibitory activity on all the isolates tested including the reference strain. Fraction 3 showed the highest inhibitory percentage (86%) among the extracts. At a concentration of 1.0mg/ml, the percentage inhibition of fraction 3, rifampicin and isoniazid against M. tuberculosis strain 3 were 83%, 95% and 86% in L-J medium respectively while 86%, 96% and 89% were obtained respectively in Middle brook medium. Results showed that the crude methanolic extract and the purified fractions of the bulb of Crinum jagus exhibited anti-mycobacterial activity which is an indication of promising potential of this plant for the development of anti-tuberculosis agent.Keywords: Crinum jagus, Chromatographic fractions, Mycobacterium tuberculosis, In-vitr

DISCOURSE ON MORALITY, CORRUPTION AND CHANGE IN CONTEMPORARY AFRICA: DOES INTENTION MATTER?

Corruption is widely regarded as a condemnable act because of its effects on the wellbeing of the populace. More than the reason(s) for the supposed act of corruption, most scholars are of the view that the very act of „diverting‟ public funds, with likely severe consequence(s), is unacceptable, and therefore immoral. But the question is: should the morality of an act be decided strictly based on the consequence(s) of such an action or should the intent of the „performer‟ be considered? In this paper we shall be examining the „consequences versus intent‟ factor in the definition of corruption within the public space, using T.M. Scalon‟s „Predictive Significance‟. In the final analysis, the work suggests that neither consequences nor intent is solely sufficient in evaluating the morality of corruption. We therefore suggest that both intent and consequences should be duly considered within the ambit of Scalon‟s „Predictive Significance‟ when moralising corruption, most especially in Africa where change is much needed

Potential toxicity of Chlorpheniramine plus chloroquine for the treatment of childhood malaria

Objectives: To compare the adverse effects of two regimens of chlorpheniramine plus chloroquine (CP+CQ) in childrenwho live in a countrywhere chloroquine resistantmalaria is endemic. Methods: 99 children with acute uncomplicated malaria were randomised into two treatment groups. Group I received high dose chlorpheniramine (6mg +12mg/day for 7days in children = 5years; 8mg + 18mg/day for 7days in those >5years) plus chloroquine 10mg/kg daily for 3 days. Group II received a 50% higher dose of chlorpheniramine plus chloroquine 10mg/kg daily for 3 days. Outcome measures were vital signs, clinical response and parasite clearance on days 0-7 and day 14. Results: Parasite clearance, fever clearance and cure rate were comparable for the two groups. Drowsiness occurred in 66.7% of high dose and 86.3% of higher dose CP+CQ subjects (p = 0.05). Compared to children treated with high dose, those treated with higher dose CP+CQhad significantly lower respiratory rates on day 2 (p = 0.001), day 6 (p = 0.015), and on day 14 (p = 0.003). Conclusion: The higher rates of drowsiness and lower respiratory rates in children treated with higher dose CP+CQ calls for caution in the clinical application of the higher dose combination. The higher dose has no additional benefit andmay in fact be dangerous.Keywords: Chloroquine resistant malaria, chlorpheniramine-chloroquine, treatment, adverse effects, drowsiness, respiratory depressio

Evaluation of the comparative efficacy and safety of artemether-lumefantrine, artesunate-amodiaquine and artesunate-amodiaquine-chlorpheniramine (Artemoclo™) for the treatment of acute uncomplicated malaria in Nigerian children.

OBJECTIVE: To evaluate the comparative efficacy and safety of artemether-lumefantrine (AL), artesunate-amodiaquine (ASAQ) and artesunate-amodiaquine-chlorpheniramine (AQC) for the treatment of acute uncomplicated malaria among Southwest Nigerian children. SUBJECTS AND METHODS: One hundred and sixty children aged 6 months to 14 years with acute uncomplicated malaria were randomized to AL (n = 53), ASAQ (n = 53), or AQC (n = 54). Enrollees were seen daily on days 0-3 and then on days 7, 14, 21, 28 and 42 for clinical and parasitological evaluations. Paired samples of genomic DNA at enrolment and at the time of recurrent parasitaemia were genotyped using nested PCR to distinguish between reinfection and recrudescence. Detailed haematological and biochemical evaluations were carried out in a subset of enrollees on days 0, 7 and 28 as part of a safety evaluation. RESULTS: Of the 160 children, 144 (90%) completed the study. The mean fever clearance times and parasite clearance times for AL, ASAQ and AQC were comparable (p = 0.94 and p = 0.122, respectively). On day 14, the adequate clinical and parasitological response (ACPR) for AL and AQC was 100% and for ASAQ it was 90% (p = 0.39). The PCR-uncorrected results on days 28 and 42 and the ACPR-corrected results on day 42 were similar for all drugs (p = 0.62 and p = 0.56, respectively). AQC resulted in the best parasite clearance and haematological recovery on day 2 (p = 0.022 and p = 0.018, respectively). Biochemical parameters were not adversely affected by the three artemisinin-based combination therapies (ACTs) and these were well tolerated. CONCLUSION: The three ACTs were efficacious and safe, but AQC resulted in a better haematological recovery on day 2 and higher cure rates throughout the study period

PROVERBS, VALUES AND THE DEVELOPMENT QUESTION IN CONTEMPORARY AFRICA: A CASE STUDY OF YORUBA PROVERBS

If culture is a veritable instrument of development, if language is a carrier of culture and if the relationship between language and culture is like that between two sides of the same coin, then the role of proverb as a metaphorical use of language cannot be overemphasized in any development discourse. The paper examines this invaluable nexus between language and development, with particular emphasis on how the use of proverb and its lessons could help revive moral/cultural values, and thus be used as a veritable instrument of development. This is done by taking as a foil a content analysis of some of Yoruba proverbs, particularly the proverbs whose subject matter is centered on development-related themes such as care for others and cooperation, leadership qualities, advice, reproach and punishment, conflict resolution and warning

ANTIMICROBIAL ACTIVITIES OF CRUDE METHANOLIC EXTRACT AND FRACTIONS OF THE BULB OF CRINUM JAGUS (LINN)

Crinum jagus is a medicinal plant used traditionally in Nigeria to treat infectious diseases such astuberculosis andmalaria. In the present study, the antimicrobial properties of the crude extract and chromatographic fractions from the bulb of Crinum jaguswere investigated against clinical and laboratoryisolates of bacteria and fungi using both agar well diffusion and agar dilution methods.Ampicillin (antibacterial) and tiaconazole(antifungal) were used as positive reference standard drugs.The crude plant extract and its fractionsdemonstrated broad spectrum activityagainst all the bacteriaand fungi isolatestested. Fraction 1 (24.00 mm zone of inhibition, MIC: 0.20 μg/mL, MBC:0.39μg/mL, MFC: 0.78μg/mL)demonstrated the highest activity, followed by Fraction 2 (24.00mm zone of inhibition, MIC: 0.39μg/mL, MBC: 0.78μg/mL, MFC: 1.56μg/mL. Fraction 3 (20:00mm zone of inhibition, MIC: 0.78μg/mL, MBC: 0.78μg/mL, MFC: 1.56μg/mL,). The crude extract howeverdemonstratedthe least activity against the test bacteria and fungi (18.00 mm zone of inhibition,MIC: 6.25mg/mL, MB: 25.00mg/mL, MFC: 50mg/mL.Preliminary phytochemical analysis revealed the presence of alkaloids, phenols, flavonoids,saponinsand steroids which may account for the antimicrobialactivity of theplant. The result of the study demonstrated that the extractand fractions of the bulb of Crinum jagus has appreciable antimicrobial properties and suggest that it may be useful in the treatment of microbial infections

Partial Mitigation of Oxidized Phospholipid-Mediated Mitochondrial Dysfunction in Neuronal Cells by Oxocarotenoids

Mitochondria are important (patho)physiological sources of reactive oxygen species (ROS) that mediate mitochondrial dysfunction and phospholipid oxidation; an increase in mitochondrial content of oxidized phospholipid (OxPL) associates with cell death. Previously we showed that the circulating OxPL 1-palmitoyl-2-(5’-oxo-valeroyl)-sn-glycero-3-phosphocholine (POVPC) increases in patients with Alzheimer’s disease (AD), and associates with lower plasma antioxidant oxocarotenoids, zeaxanthin, and lutein. Since oxocarotenoids are metabolized in mitochondria, we propose that during AD, lower concentrations of mitochondrial zeaxanthin and lutein may result in greater phospholipid oxidation and predispose to neurodegeneration. Here, we have investigated whether non-toxic POVPC concentrations impair mitochondrial metabolism in differentiated (d)SH-SY5Y neuronal cells and whether there is any protective role for oxocarotenoids against mitochondrial dysfunction. After 24 hours, glutathione (GSH) concentration was lower in neuronal cells exposed to POVPC (1–20μM) compared with vehicle control without loss of viability compared to control. However, mitochondrial ROS production (determined by MitoSOX oxidation) was increased by 50% only after 20μM POVPC. Following delivery of lutein (0.1-1μM) and zeaxanthin (0.5-5μM) over 24 hours in vitro, oxocarotenoid recovery from dSH-SY5Y cells was >  50%. Co-incubation with oxocarotenoids prevented loss of GSH after 1μM but not 20μM POVPC, whereas the increase in ROS production induced by 20μM POVPC was prevented by lutein and zeaxanthin. Mitochondrial uncoupling increases and ATP production is inhibited by 20μM but not 1μM POVPC; carotenoids protected against uncoupling although did not restore ATP production. In summary, 20μM POVPC induced loss of GSH and a mitochondrial bioenergetic deficit in neuronal cells that was not mitigated by oxocarotenoids