Background The search for pharmacologically effective agents among molecules bearing multiple functionalities is commonly practiced. In continuation of the search for new anti-malarial agents, new pyrazole-hydrazine coupled Schiff-base derivatives previously synthesized were screened for anti-malarial property. Methods Here, in vivo prophylactic and curative activities of the compounds were assessed while their binding affinity for falcipain-2, a crucial enzyme in Plasmodium survival, was done using computational techniques. Results The two derivatives (BepINH and BepBeH) respectively led to a significant (p < 0.05) reduction in parasitaemia count (0.76 ± 1.11 and 0.79 ± 1.19) at day 3 post-treatment relative to the negative control (16.37 ± 1.25). For the prophylactic study, it was observed that the highest parasitaemia suppression level of 95.35% and 95.17% for BepINH and BepBeH at 15 mg/kg was slightly comparable to that obtained for ACT-Lonart (99.38%). In addition, their haematological profiles indicate that they are potentially beneficial in suppressing haemolytic damage to RBC, thereby protecting the body against infection-induced anaemia. Docking calculations on the derivatives toward the Plasmodium falciparum falcipain-2 revealed that they favourably interacted with a binding affinity higher than that of a known cocrystallized inhibitor. Conclusion This study confirms the relevance of multi-functional molecules in the search for new and effective anti-plasmodial agent and lay the foundation for further development of these compound series to potent anti-plasmodial agent that interacts with falcipain-2.
Objective: In southeastern Nigeria, Nauclea diderrichii (De Wild) Merr is used in the treatment of a wide range of ailments including diabetes mellitus (DM). This study evaluates the antidiabetic activity and toxicological profile of the methanol-dichloromethane root bark extract of N. diderrichii in normoglycemic and alloxan-induced diabetic models.Methods: Dried root barks of N. diderrichii were extracted using methanol and dichloromethane (1:1) to obtain N. diderrichii extract (NDE). The acute and sub-chronic toxicity tests were performed using standard procedures. The effect on alanine aminotransferase (ALT) aspartate aminotransferase (AST), alkaline phosphatase (ALP), total protein (TP), packed cell volume (PCV), hemoglobin concentration (HB) and total white blood cell (TWBC) count was determined in the rats after treatment. In order to elucidate its antidiabetic mode of action, an oral glucose tolerance test (OGTT) was performed using glucose (2 g/kg) as substrate and alloxan (100 mg/kg; i. v.) induced diabetic model. Glibenclamide (GLI 0.2 mg/kg) was used as the reference standard drug. Results:The results indicated that the LD50 of the extract is>5000 mg/kg. ALT, AST, ALP PCV, HB and TWBC were insignificantly (p>0.05) different compared with the control. No significant changes were observed in the organ weights compared with the control. In the acute and prolonged antidiabetic study, NDE (100, 200 and 400 mg/kg) significantly reduced the blood glucose level (BGL) by 14.66, 18.9, 25.80% and 75.11, 80.24, 83.74% respectively. In comparison, GLI, when administered, reduced BGL by 38.18 and 92.86% respectively. Conclusion:N. diderrichii possesses antidiabetic activity with good toxicological profile.
Background: Geophagy is the consumption of earth materials which occurs across several cultures. For several reasons, pregnant women in many parts of West Africa including Nigeria frequently consume kaolin. This study was carried out to determine the influence of kaolin consumption on serum electrolytes, glucose and amylase levels of pregnant women attending antenatal clinic in a Teaching Hospital in the south east Nigeria. Methods: A total of eighty pregnant women recruited for this study were grouped as follows; Group 1, (30 geophagic pregnant women in the first trimester), Group 2 (30 geophagic pregnant women in the second trimester) and Group 3 (20 non-geophagic pregnant women that served as control). Subjects in Groups 1 and 2 were subdivided into three based on the quantity of kaolin consumed per week: group A (100 g/week), group B (150 g/week) and group C (200 g/week). Preliminary analysis of the calcium content of kaolin was carried out. Serum levels of potassium, sodium, chloride, bicarbonate, glucose and amylase of the subjects were determined. Results: Calcium level in kaolin was below the recommended daily intake in food. The concentrations of potassium in geophagic pregnant women who consumed 150 g and 200 g of kaolin per week were significantly (p < 0.05) lower in both 1 st and 2 nd trimester groups., There was a significant (p < 0.05) decrease in sodium concentration (132.2 ± 2.0) of the 2 nd trimester pregnant women that consumed 200 g of kaolin per week. The concentrations of chloride and bicarbonate were not significantly (p > 0.05) affected in all the groups. Serum amylase concentration decreased significantly (p < 0.05) in the 1 st and 2 nd trimester pregnant women on 150 g and 200 g of kaolin per week, while the plasma glucose concentration was significantly (p < 0.05) elevated in the same groups. Conclusion: This study concludes that kaolin consumption in pregnant women may predispose to gestational diabetes, electrolytes imbalance and reduced intes-
Intracellular pathogens are mainly eliminated by cell-mediated immunity offered by phagocytic cells like neutrophils, macrophages and monocytes. Two tannin glycosides, 1-O-galloyl-6-O-luteoyl-α-D-glucopyranoside (1) and 3-O-methylellagic acid 3'-O-α-rhamnopyranoside (2) were isolated from the ethyl acetate fraction (EF) of the methanol leaf extract of Phyllanthus muellerianus. The structures of the isolated compounds were elucidated by 1H-NMR and by mass spectroscopy. The effects of the isolated compounds on phagocytic competence of macrophages and neutrophils using in vitro models were evaluated. Compounds 1 and 2 significantly (p
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