In vitro cytotoxic activity of isolated acridones alkaloids from Zanthoxylum leprieurii Guill. et Perr.
Chemical investigation of the roots and fruits of Zanthoxylumleprieurii Guill. et Perr. led to the isolation of three new alkaloids including two acridone derivatives, 3-hydroxy-1,4-dimethoxy-10-methyl-9-acridone (2) and 3-hydroxy-1,2-dimethoxy-10-methyl-9-acridone (3) named helebelicine A and B, respectively, and one secobenzo[c]phenantridine, 10-O-demethyl-12-O-methylarnottianamide (10), together with thirteen other compounds. The structures of compounds 2, 3 and 10 as well as those of the known compounds were elucidated by using spectroscopic methods and by comparison with reported data. The brine-shrimp (artemia salina) lethality bioassay of the chloroform extract of the fruits showed modest cytotoxicity with LD(50) at 13.1microg/mL. Isolated compounds 1, 4-6 were found to be moderately active against lung carcinoma cells (A549), colorectal adenocarcinoma cells (DLD-1) and normal cells (WS1) with IC(50) values ranging from 27 to 77microM. In contrast to the positive control etoposide used, the cytotoxicity of the most active compound 4 was found to be selective against cancer cells in comparison to normal cells WS1 with IC(50) of 51+/-8microM and 4.3+/-0.4microM, respectively.
Ngoumfo
Rostand M
RM
Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, PO Box 812, Yaoundé, Cameroon. manfouo@yahoo.fr
Jouda
Jean-Bosco
JB
Mouafo
Ferdinand T
FT
Komguem
Justin
J
Mbazoa
Céline D
CD
Shiao
Tze Chieh
TC
Choudhary
Mohammed I
MI
Laatsch
Hartmut
H
Legault
Jean
J
Pichette
André
A
Roy
René
R
D054831:Acridones / Q000494:pharmacology*; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001156:Artemia / Q000187:drug effects; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008517:Phytotherapy / Q000379:methods; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry*; D014407:Tumor Cells, Cultured; D032106:Zanthoxylum / Q000737:chemistry*
D054831:Acridones; D000470:Alkaloids; D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts