Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases.
From the methanol extract of the bulbs of Pancratium illyricum L., three phenanthridine type alkaloids, ungeremine (1), (-)-lycorine (2) and (+)-vittatine (3) were isolated. For the evaluation of their anticancer and antibacterial potential, compounds 1-3 were tested against human (I, IIα) and bacterial (IA, IV) topoisomerases. Our data demonstrated that ungeremine impairs the activity of both, human and bacterial topoisomerases. Remarkably, ungeremine was found to largely increments the DNA cleavage promoted by bacterial topoisomerase IA, a new target in antimicrobial chemotherapy.
Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Cagliari, Italy.
Laura
L
Casu
Filippo
F
Cottiglia
Marco
M
Leonti
Alessandro
A
De Logu
Emanuela
E
Agus
Yuk-Ching
YC
Tse-Dinh
Valentina
V
Lombardo
Claudia
C
Sissi
D047151:Amaryllidaceae Alkaloids / Q000494:pharmacology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology; D001426:Bacterial Proteins / Q000378:metabolism; D016503:Drug Delivery Systems; D006801:Humans; D007212:Indolizines / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D019668:Liliaceae / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D059004:Topoisomerase I Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000737:chemistry / Q000494:pharmacology*
D047151:Amaryllidaceae Alkaloids; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D001426:Bacterial Proteins; D007212:Indolizines; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; C016175:ungeremine