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Eucalyptus camaldulensisis a medicinal plant used as insect repellant and antimalarial agent in ethnomedicine. This study examined the antiplasmodial and larvicidal potential of E. camaldulensisleaf extract and also identified the plant extract's most active fraction(s). The acute oral toxicity test of the methanol extract was evaluated using Lorke’s method. The larvicidal assay was performed on the extract and partitioned fractions according to the 2005 World Health Organization guidelines, while the 4-day chemosuppressive and curative antimalarial assays were carried out against Plasmodium bergei bergei. Endosulphan and chloroquine (10 mg/kg) was used as the positive controls for the larvicidal and antiplasmodial assays, respectively, while tween 80 in normal saline (1%) was the negative control. The methanol leaf extract of EC showed good larvicidal activity across all tested concentrations (LC503.79 ± 0.64 mg/mL), while the aqueous fraction with LC50of 2.80 ± 0.14 mg/mL was the most active. Its acute toxicity test showed it was safe up to 5000 mg/kg. The extract significantly increased dose-dependent antiplasmodial activity for the chemosuppressive and curative models (p< 0.05) than the negative control. At 800 mg/kg, EC gave chemosuppressive (53.69 ± 1.62%) and curative (81.26 ± 1.87%) activities, which was significantly lower than that of 10 mg/kg chloroquine (82.00 ± 0.57% and 92.51 ± 0.22% respectively). The aqueous partitioned fraction gave the highest chemosuppression (73.84 ± 2.73%) at 80 mg/kg, which was comparable to the positive control. The methanol extract of E. camaldulensisleaf is a promising larvicidal and antimalarial agent that could proffer a solution to vector control and the prevalence of malaria.

AbstractAlzheimer’s disease is among the major health challenges that currently attract the attention of health care givers and drug discovery and development experts worldwide. This study investigated the acetylcholinesterase inhibitory activity of sappanin-type homisoflavonoids isolated from the inter-bulb surface of Scilla nervosa. Molecular docking, molecular dynamics simulation, ADMET and in vitro studies were performed to identify the hit molecules, understand their binding mode and interaction, druggability and establish their inhibitory potentials against acetylcholinesterase enzyme. The hit compounds 5, 2, 1and 4were identified as the hit molecules through the molecular docking. The molecular dynamics simulation and MM-PBSA analysis showed the hit homoisoflavonoids established stability and good binding affinity against the acetylcholinesterase enzyme. Also, 5elicited the best inhibitory activity followed by 2, 1and 4in the in vitro experiment. Furthermore, the selected homoisoflavonoids exhibit interesting drug likeness and pharmacokinetic properties as drug candidate. The results suggest further investigations towards the development of the phytochemicals as possible acetylcholinesterase inhibitors.Communicated by Ramaswamy H. Sarma

Background of the study This study established the antidiabetic efficacy of Alternantera brasiliana in vitroand in vivo, identified the most active fraction and profiled the chemical constituents of the most active fraction.Methodology The leaf of A. brasilianawas air-dried, pulverized and extracted with methanol and evaluated for its α-amylase activity at different concentrations using in vitromethod. The in vivoantidiabetic activity of the extract and glibenclamide was evaluated in glucose loaded and streptozotocin-induced diabetic rats using various doses, while the most active partitioned fraction was identified using glucose loaded method followed by identification of its chemical constituents through GC-MS analysis.Results The extract elicited good α-amylase inhibitory potential with IC50 = 0.45 mg/mL. Also, the 50 mg/kg dose demonstrated the highest percentage blood glucose level reduction and significantly (P> 0.05) comparable to glibenclamide (5 mg/kg) from 0.5 to 4 h. The streptozotocin-induced antidiabetic assay showed that the 50 mg/kg demonstrated better activity than glibenclamide (5 mg/kg) and was significantly comparable on days 10 and 14. The aqueous methanol fraction was the most active fraction with 53% blood glucose level reduction at 4 h. The secondary metabolite profiling identified 30 chemical compounds whereby 1H-Indole-2-carboxylic acid, 6-(4-ethoxyphenyl)-3-methyl-4-oxo-4,5,6,7-tetrahydro-, isopropyl ester, Benzo[h]quinoline, 2,4-dimethyl-, thymol and 13,5-trioxane as the major constituents.Conclusion The antidiabetic activity demonstrated by the A. brasilianaextract established its antidiabetic efficacy

Background/Objectives Diabetes mellitus is among the leading cause of death worldwide. This study evaluated the alpha amylase and alpha glucosidase inhibitory properties of kaurane diterpenoids (kauran-13-ol (D1), xylopic acid (D2) and kauran-16α-ol (D3)) from the fruit of X. aethiopica.Methodology In vitroalpha amylase and alpha glucosidase inhibitory assays were performed on D1, D2 and D3 (0.03125, 0.0625, 0.125, 0.25, 0.5, 1.0 and 2.0 mg/mL) and acarbose (0.003125, 0.00625, 0.0125, 0.025, 0.05 and 0.1 mg/mL) followed by molecular docking studies, molecular dynamics simulation and MMPBSA to examine their mode of interaction, binding affinity, binding mode and binding energy established with the enzymes. Also, ADMET properties of the studied diterpenes were examined to explain their druggability potential.Result The in vitroalpha-amylase and alpha-glucosidase studies identified D3 as the most promising inhibitor among the kaurane diterpenes with lower IC50values of 0.65 and 0.17 mg/mL. The molecular docking analysis showed that D1, D2 and D3 established vital hydrogen bond, hydrophobic and pi-interaction with the receptors, while the molecular dynamics simulation showed the kaurane diterpenes exhibited good stability at the enzymes’ binding pocket. The MMPBSA binding energy values showed the diterpenes had good binding energies that corroborated that of molecular docking. The ADMET properties identified the compounds as promising drug candidate.Conclusion The study demonstrated that the kaurane diterpenoids have good inhibitory effect on the diabetes enzymes. Further comprehensive investigation into the antidiabetic properties of the diterpenes may lead to the identification of new hit molecule.

Background and objectives This study validated the antimalarial efficacy of Laportea aestuansextract using chemosuppressive and curative models, identified its most active fraction, and performed chemical profiling of the active fraction.Methodology The aerial part of L. aestuans(LA) was extracted with 80% methanol and assayed for its chemosuppressive and curative antimalarial activities through the oral administration of the extract (100, 200, 400 and 800 mg/kg) to groups consisting of five mice each. The extract was thereafter suspended in water and partitioned with dichloromethane to afford the dichloromethane (DLA) and aqueous (ALA) fractions. The fractions (10, 20, 40, and 80 mg/kg) were thereafter tested for their antimalarial activity followed by GC-MS analysis of the most active fraction.Results The toxicity level was found to be above 2000 mg/kg. The activity recorded for the four-day chemosuppressive antimalarial tests showed a dose-dependent activity up to 400 mg/kg. The activity was significantly lower than that of chloroquine. The antimalarial activity of the extract at the lowest dose of 100 mg/kg was 42%. In the curative test, the extract of LA gave a dose-dependent activity that was significantly higher than the negative control. The DLA and ALA fractions gave a comparable curative activity across all doses. At 10 mg/kg, ALA and DLA gave percentage clearance of 81.25 ± 1.84 and 87.45 ± 1.35, respectively, which were significantly higher than that of the negative control (0.00 ± 0.00) and significantly lower than that of the positive control (94.93 ± 0.26). The chemical profiling revealed the presence of non-polar and medium-polar constituents in the dichloromethane fraction.Conclusion The good antimalarial activity elicited by LA extractives supports its usage in ethnomedicine as an antimalarial agent.