Cytotoxic effect of some natural compounds isolated from Lauraceae plants and synthetic derivatives.
BACKGROUND
The antiproliferative effect of eleven neolignans, two lignans and one diterpene isolated from three Lauraceae plants, four benzofurans and two bicyclooctanes synthetic derivatives was evaluated in vitro on a set of five human cancer cells from solid tumors with a high incidence in Colombia.


OBJECTIVE
To evaluate the cytotoxic effect of twenty compounds on the tumor cell lines HeLa, A-549, Hep-2, PC-3, and MCF-7. MATERIALS AND METHODS. Fourteen natural compounds were isolated by chromatographic techniques from three native Colombian plants (Pleurothyrium cinereum, Ocotea macrophylla and Nectandra amazonum), whose structures were established by spectroscopic methods; six synthetic derivatives were prepared by oxyarylation and diazomethane methylation. Antiproliferative effect and cell recovery were performed by means of in vitro treatment of tumor cell lines with test compounds, evaluating cell viability by resazurin staining.


RESULTS
Among test compounds, only neolignans ocophyllal A, cinerin D, kaurenoic acid, two benzofuran-derivatives, and synthetic (-)-cinerin A were found to have antiproliferative effect at different levels. Bicyclooctanoids as well as kaurenoic acid exhibited activity against all human cancer cells while benzofuranoids showed selective activity against HeLa. Furthermore, compounds (-)-cinerin A and kaurenoic acid exhibited total lethal effect against all-five cell lines and PC-3, Hep-2, and A549 cell lines, respectively.


CONCLUSIONS
Test compounds exhibiting antiproliferative activity showed interesting results, which would promote their use as lead compounds on further studies for anticancer agents development.
Laboratorio de Investigación en Productos Naturales Vegetales, Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá, D.C., Colombia.
Luis Enrique
LE
Cuca
Ericsson David
ED
Coy
Marlén Andrea
MA
Alarcón
Andrés
A
Fernández
Fabio Ancízar
FA
Aristizábal
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000302:isolation & purification* / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis / Q000494:pharmacology; D001643:Bridged Bicyclo Compounds / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor / Q000187:drug effects; D003105:Colombia; D003603:Cytotoxins / Q000138:chemical synthesis / Q000302:isolation & purification* / Q000494:pharmacology; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D019770:Lauraceae / Q000737:chemistry*; D017705:Lignans / Q000302:isolation & purification / Q000494:pharmacology; D015394:Molecular Structure; D027444:Ocotea / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D001572:Benzofurans; D001643:Bridged Bicyclo Compounds; D003603:Cytotoxins; D004224:Diterpenes; D017705:Lignans; D010936:Plant Extracts; C550759:cinerin A; C051436:kaurenoic acid