Evaluation of cytotoxic and antitumor activity of perillaldehyde 1,2-epoxide

Abstract

The study aimed to evaluate cytotoxicity and antitumor activity of perillaldehyde 1,2-epoxide (PE), a pmenthane monoterpene derivative against four human tumor cell lines ovarian cancer (OVCAR-8), colon carcinoma (HCT-116), glioblastoma (SF-295) and leukemia (HL-60) using the colorimetric MTT assay. PE showed a high degree of inhibition of cell proliferation (GI = 95.66 to 99.71%) and IC 50 16.14 μM (± 1.86), 23.61 μM (± 1.13), 21.99 μM (± 2.64) and, 9.70 μM (± 1.01) against tumor cells, respectively. Then, in vivo antitumor activity of the PE was assessed in sarcoma 180-bearing mice. Tumor growth inhibition rates were 33.4, 56.4 and 66.6% at doses of 100 and 200 mg/kg/day for the PE and 25 mg/kg/day for 5-FU intraperitoneal treatments, respectively. Toxicological effects related to the spleen, kidneys, liver, and hematological were investigated in mice submitted to treatment. Furthermore, histopathological analyses of these organs were absent of any morphological changes in the animals treated with PE. The viability of HL-60 cells was affected by perillaldehyde 1, 2-epoxide after an exposure period of 72 h when analyzed by trypan blue exclusion. PE reduced the number of viable cells associated with an increase in non-viable cells, which contributes to the increased number of dead cells in the morphological analysis. The incorporation of ethidium bromide/acridine orange, the treated cells suggests cytotoxicity via apoptosis and necrosis. So on the results, we conclude that PE presents cytotoxic and antitumoral activity through apoptotic and necrotic processes.

Selected Monocyclic Monoterpenes and Their Derivatives as Effective Anticancer Therapeutic Agents

“…Histopathological analyses of the spleen, liver and kidney showed no morphological changes in mice dosed with PE. Hence, the authors concluded the PE (28) exhibits cytotoxic and anticancer properties via necrosis and apoptosis [55]. Andrade and co-workers [24] prepared several compounds occurring in essential oils of various groups of plants.…”

“…Histopathological analyses of the spleen, liver and kidney showed no morphological changes in mice dosed with PE. Hence, the authors concluded the PE (28) exhibits cytotoxic and anticancer properties via necrosis and apoptosis [55]. A novel agent, perillaldehyde 1,2-epoxide (PE) 28 (Figure 15) was studied to estimate its cytotoxicity and antitumor activity against a few human tumor cell lines.…”