Twelve new pyridine-4(1)-one derivatives, namely, 8-demethoxywaltherione F (), waltheriones R-V (, , , , and ), 1-methoxywaltherione O (), ()-15-hydroxywaltherione G (), (8)-8-hydroxywaltherione M (), (9,13)-2-hydroxymethylwaltherione C (), (9,10,13)-10-hydroxywaltherione C (), and ()-13-methoxywaltherione V (), as well as melovinone () and 5'-methoxywaltherione A () were isolated from the CHCl extract of the aerial parts of Their chemical structures were determined by means of a comprehensive analysis including H NMR, DEPTQ, HSQC, HMBC, H-H COSY, ROESY, and HRESIMS data. The absolute configurations were assigned via comparison of the experimental and calculated ECD data. In addition, the isolated constituents as well as the known waltheriones M-Q were evaluated for their in vitro antitrypanosomal activity. Compounds , , and as well as waltheriones M, P, and Q showed potent growth inhibition toward with IC values of 2.1, 0.8, 2.1, 1.3, 0.5, and 0.1 μM, respectively, and selectivity indices of >12, >33, >13, 5, 25, and 14. These findings further demonstrate that the waltheriones are a promising class of antichagasic compounds worthy of further investigations.
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http://dx.doi.org/10.1021/acs.jnatprod.0c00671 | DOI Listing |
J Fungi (Basel)
May 2021
Department of Botany, Breeding and Agricultural Technology of Medicinal Plants, Institute of Natural Fibres and Medicinal Plants, National Research Institute, Kolejowa 2, 62-064 Plewiska, Poland.
Fungi from the genus are very important human and animal pathogens. Many strains can produce biofilms, which inhibit the activity of antifungal drugs and increase the tolerance or resistance to them as well. Clinically, this process leads to persistent infections and increased mortality.
View Article and Find Full Text PDFJ Nat Prod
November 2020
School of Pharmaceutical Sciences, University of Geneva, 1211 Geneva 4, Switzerland.
Twelve new pyridine-4(1)-one derivatives, namely, 8-demethoxywaltherione F (), waltheriones R-V (, , , , and ), 1-methoxywaltherione O (), ()-15-hydroxywaltherione G (), (8)-8-hydroxywaltherione M (), (9,13)-2-hydroxymethylwaltherione C (), (9,10,13)-10-hydroxywaltherione C (), and ()-13-methoxywaltherione V (), as well as melovinone () and 5'-methoxywaltherione A () were isolated from the CHCl extract of the aerial parts of Their chemical structures were determined by means of a comprehensive analysis including H NMR, DEPTQ, HSQC, HMBC, H-H COSY, ROESY, and HRESIMS data. The absolute configurations were assigned via comparison of the experimental and calculated ECD data. In addition, the isolated constituents as well as the known waltheriones M-Q were evaluated for their in vitro antitrypanosomal activity.
View Article and Find Full Text PDFFitoterapia
September 2015
School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, CH-1211 Geneva 4, Switzerland. Electronic address:
Six extracts from the roots and the aerial parts of Waltheria indica L. (Malvaceae) were screened for their in vitro antitrypanosomal activity towards Trypanosoma brucei brucei STIB 427 strain, T. brucei rhodesiense STIB 900 and Trypanosoma cruzi Tulahuen C4.
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