Anti-leukemic activity of semisynthetic derivatives of lupeol

Abstract

In our previous work, lupeol was isolated from aerial parts of V. scorpioides and modified by semisynthetic approach. The purpose of this study was to investigate the cytotoxicity of lupeol and its derivatives previously prepared on the human K562 acute myeloid leukemia cell and human Jurkat acute lymphoid leukemia cell in vitro. Compounds 3β-hydroxylup-20(29)-en-30-al (2), lup-20(30)-en-3β,29-diol (3), 3β-acetoxylup-20(29)-en-30-al (5) and 3β-acetoxy-30-hydroxylup-20(29)-ene (6) presented cytotoxicity with IC₅₀ ranging from 11.72 to 56.15 µM at 24 h of incubation for both cell lines. Most of the active compounds (3, 5 and 6) were selective to leukemia cells, in compare with healthy cells. The hemolysis assay showed high blood compatibility of the cytotoxic lupeol derivatives which makes possible an intravenous administration of these compounds aiming to the potential to development of anti-leukemic drugs.

Graphical Abstract

Keywords:

• Leukemia
• K562 cells
• Jurkat cells
• lupeol
• hemolysis assay

Disclosure statement

The authors have declared no conflict of interest.

Additional information

Funding

The authors thank the financial support from CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico), CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior), and Polydoro Ernani de São Thiago University Hospital (HU/UFSC).