21.

Antiproliferative Activity and Constituents of Aspidosperma macrocarpon (Apocynaceae) Leaves

Geanderson Bannwart 1, Cecília M. A. de Oliveira 2, Lucilia Kato 2, Cleuza C. da Silva 1, Ana Lúcia T. G. Ruiz 3, João E. de Carvalho 3 and Silvana M. O. Santin

Departamento de Química, Universidade Estadual de Maringá, Av. Colombo 5790, 87020-900, Maringá, Paraná, Brazil

Instituto de Química, Universidade Federal de Goiás, Campus Samambaia; P.O. Box 131, 74001-970, Goiânia, Goiás, Brazil

Centro Pluridisciplinar de Pesquisa Químicas, Biológicas e Agrícolas, Universidade Estadual de Campinas, P.O. Box 6171, 13081-970, Campinas, São Paulo, Brazil .

Abstract: Aspidosperma macrocarpon belongs to the family Apocynaceae and is endemic to Americas and mainly found from Mexico to Argentina. It is known in Brazil as “guatambu” or “peroba”. Crude extracts and their fractions from leaves were assayed against human cancer cells lines: glioma (U251), melanoma (UACC-62), mammary (MCF-7), ovarian expressing the multidrug resistance phenotype (NCI-ADR/RES), lung (NCI-H460), prostate (PC-3), kidney (786-0), ovarian (OVCAR-3), colon (HT-29) and leukemia (K-562). The crude extract (EAM), hexane (HA) and chloroform (CA) fractions were the most active fractions against K-562 with GI50 values low than 1 µg/mL. Also, CA was moderate active against OVCAR-3 and NCI-ADR/RES cells lines. This phytochemical study allowed to identify the known kopsanone, kopsinine, ursolic acid, rutin, 5-O-caffeoylquinic acid, and 3,5-O-dicaffeoylquinic acid. The kopsanone was also evaluated against human cancer cell lines and showed activity to the U251 and K-562 cell lines, with GI50 values of 20.6 µg/mL and 8.7 µg/mL, respectively.

Keywords: Aspidosperma macrocarpon ; antiproliferative activity; alkaloids ./p>