TY - JOUR
T1 - Carvacrol/β-cyclodextrin inclusion complex inhibits cell proliferation and migration of prostate cancer cells
AU - Trindade, Gabriela G.G.
AU - Thrivikraman, Greeshma
AU - Menezes, Paula P.
AU - França, Cristiane M.
AU - Lima, Bruno S.
AU - Carvalho, Yasmim M.B.G.
AU - Souza, Eloísa P.B.S.S.
AU - Duarte, Marcelo C.
AU - Shanmugam, Saravanan
AU - Quintans-Júnior, Lucindo J.
AU - Bezerra, Daniel P.
AU - Bertassoni, Luiz E.
AU - Araújo, Adriano A.S.
N1 - Funding Information:
We wish to acknowledge Dr. Ryan Gordon (OHSU Knight Cancer Research Institute, Portland, Oregon) for PC3 cells. We also thank the CAPES (grant numbers 88881.134368/2016-01 and 88881.134337/2016–01 ), CNPq and FAPITEC/SE for financial support.
Publisher Copyright:
© 2019
PY - 2019/3
Y1 - 2019/3
N2 - Carvacrol, a phenolic monoterpene derived from thyme oil has gained wide interest recently because of its anticancer activities. To improve the solubility of carvacrol, the formation of inclusion complexes with β-cyclodextrin was performed by ultrasound and freeze-drying methods and characterized using thermal analysis, FTIR, XRD, SEM, NMR and HPLC analysis. From these results, carvacrol was successfully complexed within β-cyclodextrin cavity. Moreover, HPLC analysis demonstrated a higher entrapment efficiency for freeze-drying method (81.20 ± 0.52%) in contrast to ultrasound method (34.02 ± 0.67%). Hence, freeze-drying inclusion complex was evaluated for its antiproliferative effect and cytotoxicity against prostate cancer cell line (PC3) in vitro. Further, freeze-drying complex led to a dose-dependent inhibition in tumor cell growth in 2D and 3D cell culture systems. Altogether, the inclusion of carvacrol in β-cyclodextrin led to the formation of stable complexes with potent antiproliferative effects against PC3 cells, in vitro. Such an improved cytotoxic effect can be attributed to the enhanced the aqueous solubility and bioavailability of carvacrol by effective complexation in β-cyclodextrin.
AB - Carvacrol, a phenolic monoterpene derived from thyme oil has gained wide interest recently because of its anticancer activities. To improve the solubility of carvacrol, the formation of inclusion complexes with β-cyclodextrin was performed by ultrasound and freeze-drying methods and characterized using thermal analysis, FTIR, XRD, SEM, NMR and HPLC analysis. From these results, carvacrol was successfully complexed within β-cyclodextrin cavity. Moreover, HPLC analysis demonstrated a higher entrapment efficiency for freeze-drying method (81.20 ± 0.52%) in contrast to ultrasound method (34.02 ± 0.67%). Hence, freeze-drying inclusion complex was evaluated for its antiproliferative effect and cytotoxicity against prostate cancer cell line (PC3) in vitro. Further, freeze-drying complex led to a dose-dependent inhibition in tumor cell growth in 2D and 3D cell culture systems. Altogether, the inclusion of carvacrol in β-cyclodextrin led to the formation of stable complexes with potent antiproliferative effects against PC3 cells, in vitro. Such an improved cytotoxic effect can be attributed to the enhanced the aqueous solubility and bioavailability of carvacrol by effective complexation in β-cyclodextrin.
KW - Carvacrol
KW - Cell viability
KW - Inclusion complex
KW - Prostate cancer
KW - β-cyclodextrin
UR - http://www.scopus.com/inward/record.url?scp=85059626134&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85059626134&partnerID=8YFLogxK
U2 - 10.1016/j.fct.2019.01.003
DO - 10.1016/j.fct.2019.01.003
M3 - Article
C2 - 30615955
AN - SCOPUS:85059626134
SN - 0278-6915
VL - 125
SP - 198
EP - 209
JO - Food and Chemical Toxicology
JF - Food and Chemical Toxicology
ER -