Planta Med 2017; 83(01/02): 23-29
DOI: 10.1055/s-0042-107083
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Cytotoxic and Antitumor Effects of Curzerene from Curcuma longa

Youdi Wang*
1   College of Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, China
4   Novel Drug Screening Center, Department of Pharmacology, Guangdong Pharmaceutical University, Guangzhou, China
,
Jiahong Li*
1   College of Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, China
,
Jiquan Guo
2   Guangdong General Hospital, Guangzhou, China
,
Qiyou Wang
3   The Third Affiliated Hospital of Sun-Yat Shan University, Guangzhou, China
,
Shuguang Zhu
2   Guangdong General Hospital, Guangzhou, China
,
Siyuan Gao
4   Novel Drug Screening Center, Department of Pharmacology, Guangdong Pharmaceutical University, Guangzhou, China
,
Chen Yang
1   College of Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, China
,
Min Wei
5   College of Medicine, University of Kentucky, Lexington, Kentucky, USA
,
Xuediao Pan
4   Novel Drug Screening Center, Department of Pharmacology, Guangdong Pharmaceutical University, Guangzhou, China
,
Wei Zhu
6   Dshare Pharmaceutical Science & Technology Co., Ltd., Jiangsu, China
,
Dongmei Ding
7   Guangdong Food and Drug Vocational College, Guangzhou, China
,
Ruiping Gao
8   The First Affiliated Hospital, Pharmaceutical University, Guangzhou, China
,
Wei Zhang
8   The First Affiliated Hospital, Pharmaceutical University, Guangzhou, China
,
Junye Wang
9   State Key laboratory of Oncology in Southern China, Sun-Yat Shan University Cancer Center, Guangzhou, China
,
Linquan Zang
4   Novel Drug Screening Center, Department of Pharmacology, Guangdong Pharmaceutical University, Guangzhou, China
› Author Affiliations
Further Information

Publication History

received 05 November 2015
revised 07 April 2016

accepted 15 April 2016

Publication Date:
10 June 2016 (online)

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Abstract

Curzerene is a sesquiterpene and component used in oriental medicine. It was originally isolated from the traditional Chinese herbal medicine Curcuma rhizomes. In this study, anticancer activity of curzerene was examined in both in vitro and in vivo models. The result of the MTT assay showed that curzerene exhibited antiproliferative effects in SPC-A1 human lung adenocarcinoma cells in a time-dependent and dose-dependent manner. The anticancer IC50s were 403.8, 154.8, and 47.0 µM for 24, 48, and 72 hours, respectively. The flow cytometry analysis indicated curzerene arrested the cells in the G2/M cell cycle and promoted or induced apoptosis of SPC-A1 cells. The percentage of cells arrested in the G2/M phase increased from 9.26 % in the control group cells to 17.57 % in the cells treated with the highest dose (100 µM) of curzerene. Western blot and RT-PCR analysis demonstrated that curzerene induced the downregulation of GSTA1 protein and mRNA expressions in SPC-A1 cells. Tumor growth was significantly inhibited in SPC-A1 cell-bearing nude mice by using curzerene (135 mg/kg daily), meanwhile, curzerene did not significantly affect body mass and the organs of the mice, which may indicate that curzerene has limited toxicity and side effects in vivo. In conclusion, curzerene could inhibit the proliferation of SPC-A1 human lung adenocarcinoma cells line in both in vitro and in vivo models. Focusing on its relationship with GSTA1, curzerene could induce the downregulation of GSTA1 protein and mRNA expressions in SPC-A1 cells. Curzerene might be used as an anti-lung adenocarcinoma drug candidate compound for further development.

* These authors contributed equally to this work.


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