Cytisine-Pterocarpan-Derived Compounds: Biomimetic Synthesis and Apoptosis-Inducing Activity in Human Breast Cancer Cells
Cytisine-pterocarpan-derived compounds were biomimetically synthesized with (-)-cytisine and (-)-maackiain via a , -4-dimethyl-4-aminopyridine (DMAP)-mediated synthetic strategy in a mild manner. In the present study, tonkinensine B ( ) was elaborated in good and high yields with the optimized react...
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Published in | Molecules (Basel, Switzerland) Vol. 23; no. 12; p. 3059 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
Switzerland
MDPI AG
22.11.2018
MDPI |
Subjects | |
Online Access | Get full text |
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Summary: | Cytisine-pterocarpan-derived compounds were biomimetically synthesized with (-)-cytisine and (-)-maackiain via a
,
-4-dimethyl-4-aminopyridine (DMAP)-mediated synthetic strategy in a mild manner. In the present study, tonkinensine B (
) was elaborated in good and high yields with the optimized reaction conditions. The in vitro cytotoxicity of compound
was evaluated against breast cancer cell lines and showed that
had a better cytotoxicity against MDA-MB-231 cells (IC
= 19.2 μM). Depending on the research on cytotoxicities of
against RAW 264.7 and BV2 cells, it was suggested that
produced low cytotoxic effects on the central nervous system. Further study indicated that
demonstrated cytotoxic activity against MDA-MB-231 cells and the cytotoxic activity was induced by apoptosis. The results implied that the apoptosis might be induced by mitochondrion-mediated apoptosis via regulating the ratio of Bax/Bcl-2 and promoting the release of cytochrome c from the mitochondrion to the cytoplasm in MDA-MB-231 cells. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 1420-3049 1420-3049 |
DOI: | 10.3390/molecules23123059 |