Antiproliferative Activity and Constituents of Aspidosperma macrocarpon (Apocynaceae) Leaves

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.