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Naphthoquinones from Catalpa bungei "Jinsi" as potent antiproliferation agents inducing DNA damage.
- Source :
-
Fitoterapia [Fitoterapia] 2022 Jul; Vol. 160, pp. 105196. Date of Electronic Publication: 2022 Apr 12. - Publication Year :
- 2022
-
Abstract
- Structure-guided isolation of a CH <subscript>2</subscript> Cl <subscript>2</subscript> -soluble fraction of the heartwood of Catalpa bungei "Jinsi" provided two new naphthoquinones, 9-hydroxy-4-oxo-α-lapachone (1) and 6-hydroxy-4-oxo-α-lapachone (2), together with three undescribed ones (3-5) and six known ones (6-11). The structures were elucidated on the basis of spectroscopic methods including electronic circular dichroism calculation. The antiproliferative effects of these isolates were evaluated in human breast adenocarcinoma cells MCF7. (4R)-4,9-dihydroxy-α-lapachone (5) and (4S)-4,9-dihydroxy-α-lapachone (6) exhibited the significant activities with IC <subscript>50</subscript> values of 2.19 and 2.41 μM, respectively. The structure-activity relationship of 1-11 in the antiproliferative assay was then discussed. The most potent 5 and 6 were found to induce cell arrest in G1 phage through DNA damage. The findings provided some valuable insights for the discovery and structural modification of α-lapachone as antiproliferative lead compounds against human breast adenocarcinoma cells.<br /> (Copyright © 2022. Published by Elsevier B.V.)
Details
- Language :
- English
- ISSN :
- 1873-6971
- Volume :
- 160
- Database :
- MEDLINE
- Journal :
- Fitoterapia
- Publication Type :
- Academic Journal
- Accession number :
- 35427755
- Full Text :
- https://doi.org/10.1016/j.fitote.2022.105196