Cytofluorometric analysis of chondrotoxicity of fluoroquinolone antimicrobial agents |
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Authors: | G Hayem PX Petit M Levacher C Gaudin MF Kahn JJ Pocidalo |
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Affiliation: | Natural Products Laboratory, Division of Medicinal Chemistry, University of North Carolina, Chapel Hill 27599. |
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Abstract: | Betulinic acid [1] and platanic acid [2], isolated from the leaves of Syzigium claviforum, were found to be inhibitors of HIV replication in H9 lymphocyte cells. Evaluation of anti-HIV activity with eight derivatives of 1 revealed that dihydrobetulinic acid [3] was also a potent inhibitor of HIV replication. The C-3 hydroxy group and C-17 carboxylic acid group, as well as the C-19 substituents, contribute to enhanced anti-HIV activity. The inhibitory activity of these compounds against protein kinase C (PKC) was also examined, since a correlation between anti-HIV and anti-PKC activities has been suggested. However, there was no apparent correlation between anti-HIV activity and the inhibition of PKC among these compounds. |
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