A novel series of meta-substituted ethanediamide and 2-butenediamide derivatives were synthesized and tested for their ability to inhibit electric eel acetylcholinesterase (AChE) and equine serum butyrylcholinesterase (BuChE). The synthesized compounds were evaluated against ChE enzymes using the colorimetric method described by Ellman et al. (Biochem. Pharmacol., 7, 1961). It was revealed that...

Zapoteca portoricensis (Jacq) HM Hernández is used with remarkable efficacy in ethnomedicinal management of tonsillitis in the Eastern part of Nigeria. Previous pharmacological studies have validated the antiinflammatory and antimicrobial activities of the crude extract. In this study, two dipeptides, saropeptate (aurantiamide acetate) and anabellamide, were isolated from the methanol root extr...

Novel enzyme-luminescence method is used for the rapid and sensitive in vitro detection of natural neurotoxins (e.g., shellfish and mushroom toxins) using model brain cells. Paralytic shellfish poisons gonyautoxins (e.g., GTX2,3 and GTX1,4) were detected at 1 nM level by their inhibition of glutamate release from C6 glioma cells upon drug stimulation (IC50: GTX2,3 = 30 nM and GTX1,4 = 8 nM). Ac...

Human acid beta-glucosidase (D-glucosyl-N-acylsphingosine glucohydrolase, EC 3.2.1.45) cleaves the beta-glucosidic bonds of glucosylceramide and synthetic beta-glucosides. The specificity of binding to the active site of this enzyme was evaluated using series of inhibitors including synthetic sphingosines, N-alkyl(Cn)-deoxynojirimycins (1,5-dideoxy-5-iminoglucose) and N-Cn-glucosylamines. The s...

Crude rhizome extracts and volatile oils of Curcuma aromatica were evaluated for chemical composition and anti-mosquito potential, including larvicidal, adulticidal, and repellent activities against the Aedes aegypti mosquito. Chemical identification achieved by GC/MS analysis revealed that xanthorrhizol, 1H-3a, 7-methanoazulene and curcumene at 35.08 and 13.65%, 21.81 and 30.02%, and 13.75 and...

A series of novel J147 derivatives were synthesized, and their inhibitory activities against β-amyloid (Aβ) aggregation and toxicity were evaluated by using the oligomer-specific antibody assay, the thioflavin-T fluorescence assay, and a cell viability assay in the transformed SH-SY5Y cell culture. Among the synthesized J147 derivatives, 3j with a 2,2-dicyanovinyl substituent showed the most po...

Lupeol (1), epilupeol (2) and β-sitosterol (3) were isolated from the n-hexane and the carbon tetrachloride soluble fraction of a methanol extract of the leaves of Phoenix paludosa Roxb. The n-hexane, carbon tetrachloride and chloroform soluble materials from the concentrated methanol extract were subjected to antimicrobial screening and brine shrimp lethality bioassay. All of the partitionates...