Synthesis of gossypol atropisomers and derivatives and evaluation of their anti-proliferative and anti-oxidant activity |
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Authors: | Dodou Kalliopi Anderson Rosaleen J Lough W John Small David A P Shelley Michael D Groundwater Paul W |
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Institution: | Sunderland Pharmacy School, University of Sunderland, Wharncliffe Street, Sunderland SR1 3SD, UK. |
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Abstract: | Gossypol 1, gossypolone 2, and a series of bis 3 and half Schiff's bases 4 of gossypol were synthesised and tested for anti-proliferative and anti-oxidant activity. (-)-Gossypol (-)-1 was the most potent inhibitor of the proliferation of the HPV-16 keratinocyte cell line (using an MTT viability assay) with a GI50 of 4.8 microM. The bis Schiff's base of (-)-gossypol with L-tyrosine ethyl ester (-)-3b was the most potent inhibitor of iron/ascorbate dependent lipid peroxidation (using the thiobarbituric acid test), with an IC50 of 11.7 microM, with (-)-gossypol being the next most potent of the series, with an IC50 of 13.1 microM. The results from these initial assays suggest that gossypol, as either a racemic mixture rac-1, or the individual atropisomers (-)-1 or (+)-1, has potential for the treatment of psoriasis. |
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