AI Article Synopsis
- Researchers isolated cytotoxic compounds from the plant Bridelia ferruginea using a method called bioactivity-guided fractionation, identifying several known substances including deoxypodophyllotoxin and neoechinulin.
- The study extended previous research on podophyllotoxin by investigating structural modifications of 4-aza-podophyllotoxin to improve its effectiveness.
- Some modified compounds showed strong cancer cell growth inhibitory activity, with GI50 values as low as 0.1 to <0.03 μg/mL, while 4'-demethylated versions were significantly less effective.
Article Abstract
Cytotoxic constituents of the terrestrial plant Bridelia ferruginea were isolated using bioactivity-guided fractionation, which revealed the presence of the previously known deoxypodophyllotoxin (1), isopicrodeoxypodophyllotoxin (2), β-peltatin (3), β-peltatin-5-O-β-D-glucopyranoside (3a), and the indole neoechinulin (4). As an extension of previous podophyllotoxin research, SAR studies were undertaken focused on 4-aza-podophyllotoxin structural modifications. A number of such derivatives were synthesized following modifications to the A and E rings. Such structural modifications with alkyl and 4-fluorobenzyl substituents at the 4-aza position provided the most potent cancer cell growth inhibitory activity (GI50 0.1 to <0.03 μg/mL) against a panel of six human cancer cell lines and one murine cancer cell line. Several compounds corresponding to 4'-demethylated modifications were also synthesized and found to be significantly less potent.
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| http://dx.doi.org/10.1021/acs.jnatprod.5b00873 | DOI Listing |
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