Cytotoxic and anti-HIV-1 constituents of Gardenia obtusifolia and their modified compounds

摘要: Abstract 5α-Cycloart-24-ene-3,23-dione ( 1 ), 5α-cycloart-24-ene-3,16,23-trione 2 ) and methyl 3,4- seco -cycloart-4(28),24-diene-29-hydroxy-23-oxo-3-oate 3 together with five known flavones 5,7,4′-trihydroxy-3,8-dimethoxyflavone 4 5,7,4′-trihydroxy-3,8,3′-tri-methoxyflavone 5 5,7,4′-trihydroxy-3,6,8-trimethoxyflavone 6 5,4′-dihydroxy-3,6,7,8-tetramethoxyflavone 7 5,3′-dihydroxy-3,6,7,8,4′-pentamethoxyflavone 8 have been isolated from the leaves twigs of Gardenia obtusifolia . The structures were assigned on basis spectroscopic methods. Compounds – some modified compounds showed significant cytotoxic activities in several mammalian cell lines, especially its diacetate 21 which exhibited potent cytotoxicities (compound : P-388 0.05 μg/mL, KB 0.09 μg/mL, BCA-1 0.63 μg/mL, Lu-1 ASK 0.70 μg/mL; diacetate: 0.27 μg/mL, 0.06 μg/mL, 0.53 μg/mL, 0.49 μg/mL). It was also found that , antimitotic acitivity assay. displayed interesting anti-HIV activity syncytium assay, but inactive or weak HIV-1 RT assay; while compound to be active assay (99.9 % inhibition at 200 μg/mL),