Scientific African (Mar 2025)
Cognitive enhancement and anti-oxidant activities of Thespesia populnea L.: A bio-assay guided study using molecular docking for symptomatic alleviation of Alzheimer's disease
Abstract
Thespesia populnea L., known for its diverse pharmacological properties, has been identified as a potential mitigator of oxidative stress and cognitive impairment. A bioassay guided study was performed on ethanolic extracts of different organs (bark, wood and leaves) of the plant to determine the most active organ through both in-vitro and in-vivo tests. Through in-vitro studies, ethanolic leaves extract (ELE) showed the highest activity as acetylcholinesterase inhibitor and anti-oxidant in increasing mitochondrial complex I & III, hence, these studies were further performed on the successive fractions of ELE. Petroleum ether fraction of the leaves (Pet-L) exhibited the highest activity in nearly all tests. Thus, in-vivo testing; including behavioral, biochemical and histopathological studies was performed on two doses level (100 and 200 mg/kg b.wt.) and the highest dose showed potent activities. The highly bioactive Pet-L was subjected to phytochemical study which led to the isolation of fourteen compounds (L1-L14), Diosgenin-3-O-β-d-galactopyranoside, betulinic acid, catacerebroside, Mansonone C, Mansonone E & thespesenone were the major isolated compounds. Molecular docking study of the isolated and identified compounds on acetylcholinesterase enzyme revealed that thespesenone, mansonone C and mansonone E exerted the strongest binding affinity to the enzyme, where thespesenone and mansonone C displayed a mixed-type inhibition via binding both peripheral anionic site “PAS” as well as catalytic active site “CAS”. Our findings highlighted Thespesia populnea L. ELE together with its Pet-L fraction to be considered as promising candidates in the management of memory impairment caused by oxidative stress in Alzheimer's disease.
