Anti-Tumor Efficiency of Perillylalcohol/beta-Cyclodextrin Inclusion Complexes in a Sarcoma S180-Induced Mice Model


The low solubility and high volatility of perillyl alcohol (POH) compromise its bioavailability and potential use as chemotherapeutic drug. In this work, we have evaluated the anticancer activity of POH complexed with beta-cyclodextrin (beta-CD) using three complexation approaches. Molecular docking suggests the hydrogen-bond between POH and beta-cyclodextrin in molar proportion was 1:1. Thermal analysis and Fourier-transform infrared spectroscopy (FTIR) confirmed that the POH was enclosed in the beta-CD cavity. Also, there was a significant reduction of particle size thereof, indicating a modification of the beta-cyclodextrin crystals. The complexes were tested against human L929 fibroblasts after 24 h of incubation showing no signs of cytotoxicity. Concerning the histopathological results, the treatment with POH/beta-CD at a dose of 50 mg/kg promoted approximately 60% inhibition of tumor growth in a sarcoma S180-induced mice model and the reduction of nuclear immunoexpression of the Ki67 antigen compared to the control group. Obtained data suggest a significant reduction of cycling cells and tumor proliferation. Our results confirm that complexation of POH/beta-CD not only solves the problem related to the volatility of the monoterpene but also increases its efficiency as an antitumor agent.



subject category

Pharmacology & Pharmacy


Rezende, AA; Santos, RS; Andrade, LN; Amaral, RG; Pereira, MM; Bani, C; Chen, M; Priefer, R; da Silva, CF; de Albuquerque, RLC; Souto, EB; Severino, P

our authors


This work was supported by the Banco do Nordeste (grant FUNDECI/2016.0015), Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq), Fundacao de Apoio a Pesquisa e a Inovacao Tecnologica do Estado de Sergipe (Fapitec) and Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES). Eliana B. Souto would like to acknowledge the Portuguese Science and Technology Foundation (FCT/MCT) and from European Funds (PRODER/COMPETE) for the project UIDB/04469/2020 (strategic fund), co-financed by FEDER, under the Partnership Agreement PT2020.

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