Abstract

This study investigated the anticancer effect of zerumbone (ZER) and zerumbone-loaded nanostructured lipid carrier (ZER-NLC) on the human mammary gland adenocarcinoma (MDA-MB-231) cell line. The effect of ZER and ZER-NLC on MDA-MB-231 cells was determined via electron and fluorescent microscopy and flow cytometry using the Annexin V, cell cycle, and Tdt-mediated dUTP nick-end labeling assays. We demonstrated that ZER and ZER-NLC significantly suppressed the proliferation of MDA-MB-231 cells with an IC50of 5.96 ± 0.13 and 6.01 ± 0.11 μg/mL, respectively. ZER and ZER-NLC arrested MDA-MB-231 cell cycle at the G2/M phase. The induction of apoptosis by ZER and ZER-NLC was via the intrinsic pathway through the release of cytochrome c and activation of caspase-3 and caspase-9. The treatments also caused the downregulation of antiapoptotic Bcl-2, Bcl-xL proteins, and proliferating cell nuclear protein and upregulation of proapoptotic Bax protein. Therefore, loading of ZER into NLC did not compromise the anticancer effects of ZER on MDA-MB-231 cells. In conclusion, ZER-NLC, which increased the bioavailability of ZER, is an effective agent in the treatment of cancers.

Highlights

  • The main life-threatening and the most prevalent diseases in women are breast cancers [1]

  • This study suggests that incorporation of ZER into nanostructured lipid carriers (NLC) did not change the cytotoxic effect of the compound on MDA-MB-231 cells, maintaining its anticancer activity

  • The results show that both ZER and zerumbone-loaded nanostructured lipid carrier (ZER-NLC) are potent in the induction of apoptosis of the MDA-MD-231 cells

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Summary

Introduction

The main life-threatening and the most prevalent diseases in women are breast cancers [1]. There are several treatment methods currently being instituted for breast cancers to include chemotherapy, hormonal therapy using tamoxifen and doxorubicin, radiotherapy, and surgery. Most of these treatment methods are not specific for cancer cells and more often damage normal cells. Current studies are increasingly providing evidences that therapeutic compounds from natural sources are promising for effective treatment of chronic human diseases including cancers, without significant sideeffect [2]. Among these compounds is zerumbone (ZER), extracted from the essential oils of Zingiber zerumbet Smith rhizome

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