Labdane-type diterpenes from Hedychium gardnerianum with potent cytotoxicity against human small cell lung cancer cells.
Seven labdane-type diterpenes, coronarin E, coronarin A, yunnancoronarin A, yunnancoronarin B, hedyforrestin B, villosin, and hedyforrestin C were isolated from the rhizome of Hedychium gardnerianum and evaluated for cytotoxic activity against human small cell lung cancer (NCI-H187) and non-cancerous Vero cells. The results showed that villosin exhibited potent cytotoxic activity with IC(50) of 0.40 microM, which was higher than that of the drug ellipticine (IC(50) 1.79 microM). Moreover, ellipticine was very toxic to Vero cells (IC(50) 7.47 microM) whereas the toxicity of villosin was undetectable at concentration lower than 166.42 microM. The results have indicated that the lactone ring is essential for high cytotoxic activity and that the presence of a hydroxyl group at the 6 or 7 position causes decrease in activity. The very high cytotoxicity against the NCI-H187 cells and the exceptionally high selectivity index (>416) of villosin suggested that this compound may be used as a potential lead molecule for antitumor therapeutic development.
Kumrit
Iyared
I
Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai, 50200, Thailand.
Suksamrarn
Apichart
A
Meepawpan
Puttinan
P
Songsri
Sineenard
S
Nuntawong
Nuchnipa
N
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002522:Chlorocebus aethiops; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004611:Ellipticines / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry; D014709:Vero Cells; D030521:Zingiberaceae / Q000737:chemistry*
D000970:Antineoplastic Agents; D004224:Diterpenes; D004611:Ellipticines; C570588:hedyforrestin C; C443702:villosin, Hedychium villosum; C034192:ellipticine; D015107:4-Butyrolactone