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Antiplasmodial and antileishmanial flavonoids from Mundulea sericea

  • Five known compounds (1-5) were isolated from the extract of Mundulea sericea leaves. Similar investigation of the roots of this plant afforded an additional three known compounds (6-8). The structures were elucidated using NMR spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was established using ECD spectroscopy. In an antiplasmodial activity assay, compound 1 showed good activity with an IC50 of 2.0 mu M against chloroquine-resistant W2, and 6.6 mu M against the chloroquine-sensitive 3D7 strains of Plasmodium falciparum. Some of the compounds were also tested for antileishmanial activity. Dehydrolupinifolinol (2) and sericetin (5) were active against drug-sensitive Leishmania donovani (MHOM/IN/83/AG83) with IC50 values of 9.0 and 5.0 mu M, respectively. In a cytotoxicity assay, lupinifolin (3) showed significant activity on BEAS-2B (IC50 4.9 mu M) and HePG2 (IC50 10.8 mu M) human cell lines. All the other compounds showed low cytotoxicity (IC50 > 30 mu M) against human lung adenocarcinoma cells (A549),Five known compounds (1-5) were isolated from the extract of Mundulea sericea leaves. Similar investigation of the roots of this plant afforded an additional three known compounds (6-8). The structures were elucidated using NMR spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was established using ECD spectroscopy. In an antiplasmodial activity assay, compound 1 showed good activity with an IC50 of 2.0 mu M against chloroquine-resistant W2, and 6.6 mu M against the chloroquine-sensitive 3D7 strains of Plasmodium falciparum. Some of the compounds were also tested for antileishmanial activity. Dehydrolupinifolinol (2) and sericetin (5) were active against drug-sensitive Leishmania donovani (MHOM/IN/83/AG83) with IC50 values of 9.0 and 5.0 mu M, respectively. In a cytotoxicity assay, lupinifolin (3) showed significant activity on BEAS-2B (IC50 4.9 mu M) and HePG2 (IC50 10.8 mu M) human cell lines. All the other compounds showed low cytotoxicity (IC50 > 30 mu M) against human lung adenocarcinoma cells (A549), human liver cancer cells (HepG2), lung/bronchus cells (epithelial virus transformed) (BEAS-2B) and immortal human hepatocytes (LO2)zeige mehrzeige weniger

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Metadaten
Verfasserangaben:Carolyne Chepkirui, Purity J. Ochieng, Biswajyoti Sarkar, Aabid Hussain, Chiranjib PalORCiD, Li Jun Yang, Paolo Coghi, Hoseah M. AkalaORCiD, Solomon DereseORCiD, Albert NdakalaORCiD, Matthias HeydenreichORCiD, Vincent K. W. Wong, Mate ErdelyiORCiD, Abiy YenesewORCiD
DOI:https://doi.org/10.1016/j.fitote.2020.104796
ISSN:0367-326X
ISSN:1873-6971
Pubmed ID:https://pubmed.ncbi.nlm.nih.gov/33271256
Titel des übergeordneten Werks (Englisch):Fitoterapia
Verlag:Elsevier
Verlagsort:Amsterdam
Publikationstyp:Wissenschaftlicher Artikel
Sprache:Englisch
Datum der Erstveröffentlichung:30.11.2020
Erscheinungsjahr:2020
Datum der Freischaltung:24.03.2023
Freies Schlagwort / Tag:Mundulea sericea; antileishmanial; antiplasmodial; cytotoxicity; flavanonol; flavonol; leguminosae
Band:149
Aufsatznummer:104796
Seitenanzahl:6
Fördernde Institution:Swedish Research CouncilSwedish Research CouncilEuropean Commission [2016-05857, 2019-03715]; International Science Program, Sweden [KEN-02]
Organisationseinheiten:Mathematisch-Naturwissenschaftliche Fakultät / Institut für Chemie
DDC-Klassifikation:5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften
Peer Review:Referiert
Publikationsweg:Open Access / Hybrid Open-Access
Lizenz (Deutsch):License LogoCC-BY - Namensnennung 4.0 International
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