Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity
A combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from <i>Phyllanthus muellarianus.</i> Phytocomponents responsible for the...
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MDPI AG
2021-07-01
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| Series: | Molecules |
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| author | Marina Naldi Gloria Brusotti Gabriella Massolini Vincenza Andrisano Caterina Temporini Manuela Bartolini |
| author_facet | Marina Naldi Gloria Brusotti Gabriella Massolini Vincenza Andrisano Caterina Temporini Manuela Bartolini |
| author_sort | Marina Naldi |
| collection | DOAJ |
| description | A combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from <i>Phyllanthus muellarianus.</i> Phytocomponents responsible for the anti-cholinesterase activity of subfractions PMF1 and PMF4 were identified and re-assayed to confirm their activity. Magnoflorine was identified as an active phytocomponent from PMF1 while nitidine was isolated from PMF4. Magnoflorine was shown to be a selective inhibitor of human butyrylcholinesterase—hBChE (IC<sub>50</sub> = 131 ± 9 μM and IC<sub>50</sub> = 1120 ± 83 μM, for hBuChE and human acetylcholinesterase—hAChE, respectively), while nitidine showed comparable inhibitory potencies against both enzymes (IC<sub>50</sub> = 6.68 ± 0.13 μM and IC<sub>50</sub> = 5.31 ± 0.50 μM, for hBChE and hAChE, respectively). When compared with the commercial anti-Alzheimer drug galanthamine, nitidine was as potent as galanthamine against hAChE and one order of magnitude more potent against hBuChE. Furthermore, nitidine also showed significant, although weak, antiaggregating activity towards amyloid-β self-aggregation. |
| first_indexed | 2024-03-10T09:30:48Z |
| format | Article |
| id | doaj.art-b12c08cf263942eda1bee6f07b268490 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T09:30:48Z |
| publishDate | 2021-07-01 |
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| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b12c08cf263942eda1bee6f07b2684902023-11-22T04:32:53ZengMDPI AGMolecules1420-30492021-07-012614437610.3390/molecules26144376Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase ActivityMarina Naldi0Gloria Brusotti1Gabriella Massolini2Vincenza Andrisano3Caterina Temporini4Manuela Bartolini5Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro 6, 40126 Bologna, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum University of Bologna, Corso D’Augusto 237, 47921 Rimini, ItalyDepartment of Drug Sciences, University of Pavia, Viale Taramelli 12, 27100 Pavia, ItalyDepartment of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro 6, 40126 Bologna, ItalyA combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from <i>Phyllanthus muellarianus.</i> Phytocomponents responsible for the anti-cholinesterase activity of subfractions PMF1 and PMF4 were identified and re-assayed to confirm their activity. Magnoflorine was identified as an active phytocomponent from PMF1 while nitidine was isolated from PMF4. Magnoflorine was shown to be a selective inhibitor of human butyrylcholinesterase—hBChE (IC<sub>50</sub> = 131 ± 9 μM and IC<sub>50</sub> = 1120 ± 83 μM, for hBuChE and human acetylcholinesterase—hAChE, respectively), while nitidine showed comparable inhibitory potencies against both enzymes (IC<sub>50</sub> = 6.68 ± 0.13 μM and IC<sub>50</sub> = 5.31 ± 0.50 μM, for hBChE and hAChE, respectively). When compared with the commercial anti-Alzheimer drug galanthamine, nitidine was as potent as galanthamine against hAChE and one order of magnitude more potent against hBuChE. Furthermore, nitidine also showed significant, although weak, antiaggregating activity towards amyloid-β self-aggregation.https://www.mdpi.com/1420-3049/26/14/4376<i>Phyllanthus muellarianus</i>bioassay-guided fractionationanticholinesterase activityanti-amyloid properties |
| spellingShingle | Marina Naldi Gloria Brusotti Gabriella Massolini Vincenza Andrisano Caterina Temporini Manuela Bartolini Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity Molecules <i>Phyllanthus muellarianus</i> bioassay-guided fractionation anticholinesterase activity anti-amyloid properties |
| title | Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity |
| title_full | Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity |
| title_fullStr | Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity |
| title_full_unstemmed | Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity |
| title_short | Bio-Guided Fractionation of Stem Bark Extracts from <i>Phyllanthus muellarianus</i>: Identification of Phytocomponents with Anti-Cholinesterase Activity |
| title_sort | bio guided fractionation of stem bark extracts from i phyllanthus muellarianus i identification of phytocomponents with anti cholinesterase activity |
| topic | <i>Phyllanthus muellarianus</i> bioassay-guided fractionation anticholinesterase activity anti-amyloid properties |
| url | https://www.mdpi.com/1420-3049/26/14/4376 |
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