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
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 mo...
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| Format: | Article |
| Language: | English |
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Elsevier
2025-03-01
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| Series: | Scientific African |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2468227624004435 |
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| author | Menna B.Abdel Halim Ghada F. Metwally Areeg M. Abd-Elrazek Ahmed A. Al-Karmalawy Haidy H. El-Zoheiry Kadriya S.El Deeb Hanaa H. Eid |
| author_facet | Menna B.Abdel Halim Ghada F. Metwally Areeg M. Abd-Elrazek Ahmed A. Al-Karmalawy Haidy H. El-Zoheiry Kadriya S.El Deeb Hanaa H. Eid |
| author_sort | Menna B.Abdel Halim |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-4c9cd322fd7e4d598fc6f8c5e7478cd7 |
| institution | DOAJ |
| issn | 2468-2276 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Scientific African |
| spelling | doaj-art-4c9cd322fd7e4d598fc6f8c5e7478cd72025-08-20T02:56:02ZengElsevierScientific African2468-22762025-03-0127e0250110.1016/j.sciaf.2024.e02501Cognitive enhancement and anti-oxidant activities of Thespesia populnea L.: A bio-assay guided study using molecular docking for symptomatic alleviation of Alzheimer's diseaseMenna B.Abdel Halim0Ghada F. Metwally1Areeg M. Abd-Elrazek2Ahmed A. Al-Karmalawy3Haidy H. El-Zoheiry4Kadriya S.El Deeb5Hanaa H. Eid6Department of Medicinal plants and Natural Products, Egyptian Drug Authority (EDA; formerly: NODCAR), Egypt; Corresponding author.Department of Medicinal plants and Natural Products, Egyptian Drug Authority (EDA; formerly: NODCAR), EgyptDepartment of Physiology, Egyptian Drug Authority (EDA; formerly: NODCAR), EgyptDepartment of Pharmaceutical Chemistry, College of Pharmacy, The University of Mashreq, Baghdad 10023, Iraq; Departement of Pharmaceutical chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta 34518, EgyptDepartment of Pharmaceutical chemistry, Faculty of Pharmacy, Cairo University, 11562, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Cairo University, 11562, EgyptDepartment of Pharmacognosy, Faculty of Pharmacy, Cairo University, 11562, EgyptThespesia 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.http://www.sciencedirect.com/science/article/pii/S2468227624004435Acetylcholinesterase inhibitor activityAnti-inflammatoryAnti-oxidantMitochondrial complex I & IIIMolecular dockingPassive avoidance behavioral test & Thespesia populnea leaves |
| spellingShingle | Menna B.Abdel Halim Ghada F. Metwally Areeg M. Abd-Elrazek Ahmed A. Al-Karmalawy Haidy H. El-Zoheiry Kadriya S.El Deeb Hanaa H. Eid 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 Scientific African Acetylcholinesterase inhibitor activity Anti-inflammatory Anti-oxidant Mitochondrial complex I & III Molecular docking Passive avoidance behavioral test & Thespesia populnea leaves |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | Acetylcholinesterase inhibitor activity Anti-inflammatory Anti-oxidant Mitochondrial complex I & III Molecular docking Passive avoidance behavioral test & Thespesia populnea leaves |
| url | http://www.sciencedirect.com/science/article/pii/S2468227624004435 |
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