Cytotoxic 4-nerolidylcatechol from Pothomorphe peltata inhibits topoisomerase I activity.
Bioactivity-guided fractionation of the leaf methanolic extract of P. peltata (Piperaceae), using the brine shrimp lethality test, led to the isolation of catechol derivative 4-nerolidylcatechol (4-NC). The methanolic extract was active against crown gall tumour in potato discs, showing a 22% crown gall tumour inhibition (SD = 4%), while 4-NC was cytotoxic against KB tumour cells growth (EC50 = 1.3 micrograms/ml). No interaction with DNA could be observed when tested using the methyl green-DNA (MG-DNA) bioassay. An inhibition in the activity of topoisomerase I using agarose gel electrophoresis was detected in the presence of the purified compound (IC50 = 20 micrograms/ml), suggesting that this could be a possible mechanism for the cytotoxicity observed in KB cells.
Mongelli
E
E
Romano
A
A
Desmarchelier
C
C
Coussio
J
J
Ciccia
G
G
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D002396:Catechols / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D010944:Plants / Q000737:chemistry*; D059004:Topoisomerase I Inhibitors; D014407:Tumor Cells, Cultured
C110583:4-nerolidylcatechol; D000972:Antineoplastic Agents, Phytogenic; D002396:Catechols; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors