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Some Sulfanoquinoxaline-2,3-diones hydrazone derivatives (1-8) were synthesized from the reactions of 2,3-dioxoquinoxaline-6-sulfonohydrazine with seven substituted benzaldehydes and acetophenone. All the synthesized compounds were biologically evaluated against cholinesterase’s (acetylcholinesterase and butyryl cholinesterase). Compounds 1-8 were found to be a good selective inhibitor for acetylcholinesterase and butyryl cholinesterase. Among the series, compounds 3 (IC50 = 75 ± 10 µg/mL) and 5 (IC50 = 80 ± 10 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 6 (IC50 = 110 ± 10 µg/mL), 8 (IC50 = 130 ± 10 µg/mL) and 7 (IC50 = 150 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase. The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50 = 70 ± 20 µg/mL). Their considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities make them a good candidate for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties. Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The acetylcholinesterase and butyryl cholinesterase inhibitions were determined by Spectro photochemical analysis of acetylthiocholine and butyryl choline chloride. Results: Compounds 6 (IC50 = 30±3 µg/mL) and 4 (IC50 = 141±60 µg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 4 (IC50 = 102±10 µg/mL), 5 (IC50 = 105 ± 20 µg/mL) and 2 (IC50 = 190 ± 10 µg/mL), were found to be most active inhibitor against butyryl cholinesterase. Conclusion: The considerable acetylcholinesterase and butyryl cholinesterase inhibitory activities of the synthesized compounds makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

Aims: To synthesize some phthalimides derivatives and evaluate the compounds for their possible biological properties. Methods: The substituted phenylisoindoline-1,3-dione were synthesized from the reactions of N-phenyl phthalimide with different substituted aromatic aldehyde. The synthesized compounds were characterized using nuclear magnetic resonance spectroscopic analysis. The Nitric oxide and Ferric reducing antioxidant properties (FRAP) were determined by spectrophochemical method. Results: The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50 = 15 ± 2 µg/mL) against Nitric oxide inhibition. Compounds 3 (FRAP = 205±8 µg/ML) and 6 (FRAP = 118±1 µg/ML) were found to exhibit higher FRAP analysis results which were comparable to the results obtained for serine. (FRAP = 202±7 µg/ML). Conclusion: The considerable activity of the compounds shown by its Nitric oxide and Ferric reducing antioxidant properties (FRAP) makes them good candidates for the development of selective acetylcholinesterase and butyryl cholinesterase inhibitors.

Aminoethanoic acid undergoes condensation with 1,4-benzenedicarboxaldehyde to form an O, N, N, O donor Schiff base, N,N'-di(carboxymethylene) terephthalaldehyde, Ligand L. Coordination compounds of this Schiff base using Ni (II), Cu (II), VO (IV) and Co (II) were then obtained in-situ. The Schiff base and the complexes were evaluated for their antimicrobial and DNA binding abilities. Molecular docking studies of the ligand and synthesized compounds were also carried out. Evidence for the formation of the Schiff base coordination compounds and the coordinating atoms was obtained from 1H NMR, infrared and ultraviolet spectral data, EDX, EDTA complexometric titration and magnetic susceptibility measurement. The results obtained are consistent with octahedral geometry for Ni (II) complex, the metal ion coordinating to one molecule of Ligand L and with additional coordination with two oxygen atoms of two molecules of the solvent. A square-planar geometry was suggested for both Co (II), and Cu (II) complexes and a five-coordinate, square pyramidal geometry for the VO (IV) complex. The results further indicated that the carboxylic acid of Ligand L was not deprotonated both in the free base and also the complexes. In addition, the results showed that Compound 2 elicited the best antimicrobial activity potential. Generally, the compounds exhibited considerable good affinity to CT-DNA.

Heliotropium indicum L. has been shown to be very important in traditional healing medicine. However, many reports have indicated that the toxicity is not unconnected with pharmaceutical properties. This study therefore investigated the cytotoxic, genotoxic and biotoxic activities of methanolic leaf extract of H. indicum using Brine Shrimp lethality assay. The results revealed that the leaf extract of H. indicum showed lethality against the Brine Shrimps nauplii. The highest mortality was recorded at a concentration of 1000 μg/ml. The LC50 value of the Brine Shrimps mortality of the extract was recorded to be 461.04±10.02 μg/ml. In addition, the extract inhibited mitotic division in A. cepa root meristematic cells. The mitotic index was reduced from 59.99% in the control to 2.2% at 1000 μg/ml of the leaf extract. Chromosomal aberrations were observed at different concentrations. These include sticky chromosomes at metaphase and anaphase, chromosome breakage, degenerated and disoriented chromosomes at metaphase plate. It can be concluded from this present study that methanolic leaf extract of H. indicum was cytotoxic and genotoxic to Brine Shrimps and A. cepa cells respectively. Hence, caution should be exercised with respect to the consumption of H. indicum leaf in any form. © 2020 International Formulae Group. All rights reserved. Keywords: Mitotic index, chromosome aberrations, Brine Shrimps Lethality assay, Allium cepa assay, leaf extract

Objective: Vigna unguiculata ssp. dekindtiana (L.) Walp is used in traditional practice to treat depression-like disorders in some communities of Southwest Nigeria. This study investigated the antidepressant-like effects of the aqueous fraction of the dried aerial parts of V. unguiculata ssp. dekindtiana (AFVU). Methodology: AFVU was evaluated for antidepressant effect on the force-swimming test (FST), tail suspension test (TST) and locomotor activity (LC) in the open field test (OFT) using mice; and its probable neural mechanism(s) investigated using various receptor antagonists. Elemental composition (EC) and phyto-constituents of AFVU were analyzed using standard methods. Results: The AFVU (600 and 800 mg/kg, p.o.) significantly (p

This study evaluated the spectroscopic and anti-inflammatory properties of the ethanol leaf extract ofMilicia excelsaand fractions. The anti-inflammatory activities of the extract and various organic fractions were investigated using bovine erythrocyte membrane stabilizing assay. Ultraviolet‐visible (UV-VIS) and Fourier transform-infrared (FT-IR) methods were used to detect the characteristic peak values and their functional groups. The results showed that the crude extract and ethyl acetate fraction showed minimum percentage inhibitions of 0.88 ± 0.30 and 72.05 ± 0.45% and maximum percentage inhibitions of 81.66 ± 0.23% and 99.07 ± 0.30% respectively compared to the standard anti-inflammatory drug (Indomethacin) which exhibited minimum and maximum percentage inhibitions of 52.64 ± 0.83 and 75.51 ± 1.52% respectively. The UV-VIS profile showed the peaks ranging from 270 to 670 nm with the absorption values from 0.040 – 0.720 which could confirm the presence of aromatic compounds, alkaloids, flavonoids, unsaturated conjugated compounds in the plant. In addition, the FT-IR revealed diagnostic peaks around 3570-3200, 3000-2800, 2865-2845, 2850-2815, 2820-2780, 2070-2000, 1630-1750, 1640-1450, 1340-1250, 1200-1000, 800-700 nm-1which could confirm the presence of phenols/alcohol/carboxylic acids, alkanes, diazocompounds, aldehyde /ketone/ amide/ester, alkenes/aromatic compounds, ethers/phosphate compounds, aliphatic/chloro compounds respectively inMilicia excelsa.This study therefore demonstrated that ethyl acetate fraction with the highest percentage inhibition contained bioactive principles that protected the erythrocyte membranes effectively from lyses and also exhibited both monophasic and biphasic modes. The study also produced the UV-VIS and FT-IR spectrum profile forMilicia excelsaleaf which could be used to identify the plant biomarkers and chemical markers.

Alzheimer’s disease is a chronic and progressive neurodegenerative disease which occurs due to lower levels of acetylcholine neurotransmitters, and results in a gradual decline in memory and other cognitive processes. Acetylcholinesterase and butyrylcholinesterase have been reported to be the primary regulators of the acetylcholine levels in the brain. Evidence shows that acetylcholinesterase activity decreases in Alzheimer’s disease, while activity of butyrylcholinesterase elevate in advanced Alzheimer’s disease, which suggests a key involvement of butyrylcholinesterase in acetylcholine hydrolysis during Alzheimer’s disease symptoms. In order to sustain the level of remaining acetylcholine, acetylcholinesterase and butyrylcholinesterase inhibitors may be used. Therefore, inhibiting the activity of butyrylcholinesterase may be an effective way to control Alzheimer’s disease associated disorders. In this study, eleven 3-methylquinoxaline-2-hdrazones were synthesized from the reactions of 3-methylquinoxaline-2-hydrazine with different substituted aromatic ketones and aromatic aldehyde. All the newly synthesized compounds have been characterized on the basis of IR, 1H-NMR and 13H-NMR spectral data as well as physical data. All the synthesized compounds were biologically evaluated against cholinesterases (acetylcholinesterase and butyrylcholinesterase). Compounds 2-12 were found to be a good selective inhibitor for acetycholinesterase and butyrylcholinesterase. Among the series, compounds 6 (IC50=170 ± 30 μg/mL) and 10 (IC50=180 ± 10 μg/mL) were found to be the most active inhibitors against acetylcholinesterase, while compounds 2 (IC50=780 ± 10 μg/mL), 5 (IC50=550 ± 10 μg/mL) and 6 (IC50=790 ± 10 μg/mL), were found to be most active inhibitor against butyrylcholinesterase. The IC50 values for all the synthesized compounds were lower than standard, eserine (IC50=70 ± 20 μg/mL). Their considerable acetylcholinesterase and butyrylcholinesterase inhibitory activities makes them a good candidate for the development of selective acetycholinesterase and butyrylcholinesterase inhibitors.

Coordination compounds of 4-hydroxy-3-nitro-2H-chromen-2-one and their mixed ligand complexes with aminoethanoic acid and pyrrolidine-2-carboxylic acid were synthesized by the reaction of Cu(II) and Zn(II) salts in molar ratio 1 : 2 for the coumarin complexes and 1 : 1 : 1 for the mixed ligand complexes, in basic media. The compounds formed were characterized using infrared, Uv-vis spectrophotometric analyses, mass spectrometry, magnetic susceptibility measurements, and EDX analyses. It was concluded that 4-hydroxy-3-nitro-2H-chromen-2-one coordinated as a monobasic ligand for all the complexes; it also coordinated via the carbonyl moiety in the case of the Cu(II) mixed ligand complexes. Similarly it was proposed that the amino acids also coordinated in a bidentate fashion via their amino nitrogen and carboxylate oxygen atoms. The synthesized compounds were screened for their antimicrobial and cytotoxic activities. The complexes exhibited marginal antimicrobial activity but good cytotoxic activity.

A new ligand namely 3-hydroxybenzaldehyde-4-nitrobenzoic acid hydrazone, its Nickel(II) and Copper(II) complexes were synthesised and characterised by spectroscopic methods: 1H NMR, Infrared (IR), UV-Vis, magnetic susceptibility measurement and % metal analysis. 1H NMR spectroscopy showed the diagnostic N-H signal at 12.10 ppm indicating the formation of the ligand. Infrared spectra showed that the ligand coordinated to the metal ion in keto form through the carbonyl oxygen (C=O) and the azomethine nitrogen (C=N). The UV-Vis spectrum of the ligand displayed two prominent bands at 47169 cm-1 and 30303 cm-1 which were ascribed to the intraligand transitions of π-π*, and n-π* respectively. These bands had hypsochromic shifts in the metal complexes indicating coordination with the metal ion. The nickel complex had a magnetic moment of 2.92 B.M, suggesting an octahedral geometry, while the copper complex had a value of 1.65 B.M. which is close to the expected value for a d9 copper(II) complex with possibility antiferromagnetic interactions. The % metal calculated had a good agreement with the observed values. The acetylcholinesterase inhibition activity of the ligand measured was 190 ± 20 μg/mL compared to the standard Eserin that had 68 ± 1.13 μg/mL. The copper(II) complex had a value of 220 ± 20 μg/mL, while the Nickel(II) complex had the least inhibitory value at 390 ± 80 μg/mL. The compounds could serve as primary target in the study of acetylcholinesterase inhibitors

Objective: The mechanism of ethanol-induced gastrointestinal mucosal lesions is known to include direct damage to mucus synthesis. The present study histochemically evaluated the activity of mucus secreting cells and determined the concentration of nitric oxide (NO) in ethanol injured pylorus and duodenum of rats pretreated with ethanol extract of Moringa oleifera (MO) leaves. Methods: Male adult rats were randomly assigned into five groups: group A served as control; group B received single dose of 5 ml/kg ethanol orally; group C received 200 mg/kg MO only orally for five days; group D and E received MO at 200 mg/kg and cimetidine at 100 mg/kg orally for five days, respectively, and then ethanol was administered at 5 ml/kg orally on the 6 th day to these groups. Results: Ethanol significantly reduced NO concentration in pylorus, and this was attenuated with MO pretreatment. Pretreatment with both MO and cimetidine significantly attenuated the hemorrhagic injuries induced by ethanol. Pretreatment with MO increased activity of mucus secreting cells compared to ethanol only group. Conclusion: The present study demonstrated that the antiulcer activity of Moringa oleifera may be attributed to preservation of mucus secreting cells and maintenance of endogenous NO concentrations in ethanol injured gastroduodenal tissues. © 2014 GESDAV