“Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies”
Malaria claims over 600,000 deaths annually with a disproportionately high burden in the WHO African Region. The development of parasite resistance has warranted the search for novel anti-plasmodial drug candidates. This research aimed at validating the efficacy of Senegalia ataxacantha and tracking...
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| Language: | English |
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Elsevier
2024-12-01
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| Series: | Scientific African |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2468227624003971 |
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| author | Kennedy Ameyaw Baah Akwasi Acheampong Isaac Kingsley Amponsah Silas Adjei Yakubu Jibira Reinhard Isaac Nketia Linda Mensah Sarpong Emmanuel Quaye Kontoh |
| author_facet | Kennedy Ameyaw Baah Akwasi Acheampong Isaac Kingsley Amponsah Silas Adjei Yakubu Jibira Reinhard Isaac Nketia Linda Mensah Sarpong Emmanuel Quaye Kontoh |
| author_sort | Kennedy Ameyaw Baah |
| collection | DOAJ |
| description | Malaria claims over 600,000 deaths annually with a disproportionately high burden in the WHO African Region. The development of parasite resistance has warranted the search for novel anti-plasmodial drug candidates. This research aimed at validating the efficacy of Senegalia ataxacantha and tracking down its bioactive constituents. In vivo antiplasmodial activity of the extract was assessed using suppressive and curative protocols. Yeast-induced pyrexia was employed to evaluate the antipyretic activity of the extract. In vitro anti-plasmodial activity of isolated compounds was done using SYBR green I fluorescence assay on chloroquine sensitive (3D7) and resistant (Dd2) strains of P falciparum. In silico pharmacokinetic and interactions with parasites lactate dehydrogenase predictions of isolated compounds was conducted through molecular docking studies. Ethanol (70 %) extract of the plant showed in vitro and in vivo anti-plasmodial effect. The extract demonstrated significant (p < 0.05) dose-dependent suppression of 63.39 % and 63.32 % respectively at the highest dose (300 mg kg-1). Artesunate (4 mg kg-1/day) had considerably better curative potential (85.25%). The compounds showed in vitro anti-plasmodial activity in the order lupeol> friedelin/ friedelinol mixture>friedelin>β-sitosterol based on IC50 measurement. Friedelinol and lupeol exhibited higher binding affinities with pfLDH compared to Chloroquine. The extract and acetaminophen (positve control) showed significant (p < 0.05) reduction in rectal temperature compared to the control group. In silico studies of the compounds revealed moderate interactions with some cytochrome P450 metabolizing enzymes. S. ataxacantha stem extract shows anti-plasmodial and antipyretic activities which may be due to its pentacyclic triterpenoid constituents inhibiting pfLDH. |
| format | Article |
| id | doaj-art-bd4a4757290b47a0bb19df7add8b6519 |
| institution | Kabale University |
| issn | 2468-2276 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Scientific African |
| spelling | doaj-art-bd4a4757290b47a0bb19df7add8b65192024-12-21T04:29:16ZengElsevierScientific African2468-22762024-12-0126e02455“Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies”Kennedy Ameyaw Baah0Akwasi Acheampong1Isaac Kingsley Amponsah2Silas Adjei3Yakubu Jibira4Reinhard Isaac Nketia5Linda Mensah Sarpong6Emmanuel Quaye Kontoh7Department of Chemistry, Faculty of Physical and Computational Sciences, College of Science, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana; Department of Science Education, Wesley College of Education, Kumasi, GhanaDepartment of Chemistry, Faculty of Physical and Computational Sciences, College of Science, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana; Corresponding author at: Department of Chemistry, Faculty of Physical and Computational Sciences, College of Science, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.Department of Herbal Medicine, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Science, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Herbal Medicine, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Science, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Pharmacology and Toxicology, School of Pharmacy and Pharmaceutical Sciences, University for Development Studies, Tamale, GhanaDepartment of Pharmacognosy, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Science, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Chemistry, Faculty of Physical and Computational Sciences, College of Science, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaDepartment of Herbal Medicine, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Science, Kwame Nkrumah University of Science and Technology, Kumasi, GhanaMalaria claims over 600,000 deaths annually with a disproportionately high burden in the WHO African Region. The development of parasite resistance has warranted the search for novel anti-plasmodial drug candidates. This research aimed at validating the efficacy of Senegalia ataxacantha and tracking down its bioactive constituents. In vivo antiplasmodial activity of the extract was assessed using suppressive and curative protocols. Yeast-induced pyrexia was employed to evaluate the antipyretic activity of the extract. In vitro anti-plasmodial activity of isolated compounds was done using SYBR green I fluorescence assay on chloroquine sensitive (3D7) and resistant (Dd2) strains of P falciparum. In silico pharmacokinetic and interactions with parasites lactate dehydrogenase predictions of isolated compounds was conducted through molecular docking studies. Ethanol (70 %) extract of the plant showed in vitro and in vivo anti-plasmodial effect. The extract demonstrated significant (p < 0.05) dose-dependent suppression of 63.39 % and 63.32 % respectively at the highest dose (300 mg kg-1). Artesunate (4 mg kg-1/day) had considerably better curative potential (85.25%). The compounds showed in vitro anti-plasmodial activity in the order lupeol> friedelin/ friedelinol mixture>friedelin>β-sitosterol based on IC50 measurement. Friedelinol and lupeol exhibited higher binding affinities with pfLDH compared to Chloroquine. The extract and acetaminophen (positve control) showed significant (p < 0.05) reduction in rectal temperature compared to the control group. In silico studies of the compounds revealed moderate interactions with some cytochrome P450 metabolizing enzymes. S. ataxacantha stem extract shows anti-plasmodial and antipyretic activities which may be due to its pentacyclic triterpenoid constituents inhibiting pfLDH.http://www.sciencedirect.com/science/article/pii/S2468227624003971AntipyreticIn silicoStructural elucidationChromatographic fractionationAntimalariaPharmacokinetic profile |
| spellingShingle | Kennedy Ameyaw Baah Akwasi Acheampong Isaac Kingsley Amponsah Silas Adjei Yakubu Jibira Reinhard Isaac Nketia Linda Mensah Sarpong Emmanuel Quaye Kontoh “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” Scientific African Antipyretic In silico Structural elucidation Chromatographic fractionation Antimalaria Pharmacokinetic profile |
| title | “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” |
| title_full | “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” |
| title_fullStr | “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” |
| title_full_unstemmed | “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” |
| title_short | “Hydroethanol extract and triterpenoids of Senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase (pfLDH) as indicated by molecular docking studies” |
| title_sort | hydroethanol extract and triterpenoids of senegalia ataxacantha show antiplasmodial activity and the compounds are predicted to inhibit parasite lactate dehydrogenase pfldh as indicated by molecular docking studies |
| topic | Antipyretic In silico Structural elucidation Chromatographic fractionation Antimalaria Pharmacokinetic profile |
| url | http://www.sciencedirect.com/science/article/pii/S2468227624003971 |
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