Molecules 2014, 19(4), 4941-4955; doi:10.3390/molecules19044941
Article

Anti-Proliferative and Apoptosis-Inducing Effects of Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic Ester in Human Breast Tumor MCF-7 Cells

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Received: 22 January 2014; in revised form: 2 April 2014 / Accepted: 3 April 2014 / Published: 17 April 2014
(This article belongs to the Section Medicinal Chemistry)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester (CPT6) is a novel semi-synthetic analog of camptothecin. In a previous report, CPT6 possessed higher cytotoxic activity in vitro towards human breast tumor MCF-7 cells than topotecan. In this study, the antitumor activity of CPT6 on the human breast tumor MCF-7 cell line was analyzed using the MTT method. The underlying mechanism of CPT6 action was investigated by analyzing the cell cycle distribution, apoptotic proportion, changes in mitochondrial membrane potential, and intracellular Ca2+ concentration using flow cytometry. Nuclear and mitochondrial morphologies were also observed by laser scanning confocal and transmission electron microscopy. DNA damage was observed in MCF-7 cells treated with CPT6. Low-dose CPT6 had a significant cytotoxic effect and could inhibit proliferation and induce apoptosis in MCF-7 cells, possibly through cell nucleus fragmentation and DNA damage. CPT6 thus appears to display potent antitumor activity against human breast tumor MCF-7 cells via the induction of apoptosis, and may be a useful alternative drug for breast cancer therapy.
Keywords: Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester; MCF-7 cell line; anti-proliferative; apoptosis
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MDPI and ACS Style

Chu, C.; Xu, J.; Cheng, D.; Li, X.; Tong, S.; Yan, J.; Li, Q. Anti-Proliferative and Apoptosis-Inducing Effects of Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic Ester in Human Breast Tumor MCF-7 Cells. Molecules 2014, 19, 4941-4955.

AMA Style

Chu C, Xu J, Cheng D, Li X, Tong S, Yan J, Li Q. Anti-Proliferative and Apoptosis-Inducing Effects of Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic Ester in Human Breast Tumor MCF-7 Cells. Molecules. 2014; 19(4):4941-4955.

Chicago/Turabian Style

Chu, Chu; Xu, Jialin; Cheng, Dongping; Li, Xingnuo; Tong, Shengqiang; Yan, Jizong; Li, Qingyong. 2014. "Anti-Proliferative and Apoptosis-Inducing Effects of Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic Ester in Human Breast Tumor MCF-7 Cells." Molecules 19, no. 4: 4941-4955.

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