Gamma-pyrone compounds as potential anti-cancer drugs.
The gamma-pyrones, artomunoxanthotrione epoxide, cyclocommunol, cyclomulberrin, and cyclocommunin exhibited potent inhibition of human PLC/PRF/5 and KB cells in-vitro. Dihydroisocycloartomunin showed significant and potent inhibition of human PLC/PRF/5 and KB cells in-vitro, respectively. Cyclomorusin, dihydrocycloartomunin and artomunoxanthone showed significant inhibition of KB cells in-vitro. Based on the above finding and the reported antileukaemic activity of xanthone psorospermin, a series of natural gamma-pyrones was prepared and the inhibition of human PLC/PRF/5 and KB cells in-vitro was measured. Structure-activity analysis indicated the epoxide group substituted at 3-hydroxyl and 2,6-; 3,6-; and 3,5-dihydroxyl xanthone enhanced the anti-tumour activity. The epoxide group substituted at the 6-hydroxyl group of 1,6-dihydroxyxanthone did not show anti-tumour activity.
Liou
S S
SS
Natural Products Research Center, Kaohsiung Medical College, Taiwan, Republic of China.
Shieh
W L
WL
Cheng
T H
TH
Won
S J
SJ
Lin
C N
CN
D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000473:pathology; D002470:Cell Survival / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007624:KB Cells; D008113:Liver Neoplasms / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts; D011753:Pyrones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014966:Xanthenes / Q000302:isolation & purification / Q000494:pharmacology
D000970:Antineoplastic Agents; D010936:Plant Extracts; D011753:Pyrones; D014966:Xanthenes