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Your search keyword '"Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester"' showing total 2 results
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2 results on '"Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester"'

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

Author

Chu Chu, Jialin Xu, Dongping Cheng, Xingnuo Li, Shengqiang Tong, Jizong Yan, and Qingyong Li

Subjects
Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester, MCF-7 cell line, anti-proliferative, apoptosis, Organic chemistry, QD241-441
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.

Published
2014
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2. Anti-proliferative and apoptosis-inducing effects of camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester in human breast tumor MCF-7 cells

Author

Jialin Xu, Dongping Cheng, Shengqiang Tong, Chu Chu, Qingyong Li, Xing-Nuo Li, and Jizong Yan

Subjects
anti-proliferative, DNA damage, Cell Survival, Camptothecin-20(s)-O-(2-pyrazolyl-1)acetic ester, MCF-7 cell line, apoptosis, Pharmaceutical Science, DNA Fragmentation, Biology, Article, Analytical Chemistry, Flow cytometry, lcsh:QD241-441, lcsh:Organic chemistry, Drug Discovery, medicine, Cytotoxic T cell, Humans, Physical and Theoretical Chemistry, Fragmentation (cell biology), skin and connective tissue diseases, Cell Nucleus, Membrane Potential, Mitochondrial, medicine.diagnostic_test, Dose-Response Relationship, Drug, Organic Chemistry, Cell Cycle, Cell cycle, Antineoplastic Agents, Phytogenic, Mitochondria, Biochemistry, MCF-7, Chemistry (miscellaneous), Apoptosis, Cancer research, MCF-7 Cells, Molecular Medicine, Calcium, Camptothecin, Female, Topotecan, medicine.drug
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.

Published
2014

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