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Nat Prod Res. 2017 Nov 13:1-5. doi: 10.1080/14786419.2017.1402312. [Epub ahead of print]

Topoisomerases inhibitory activities and DNA binding properties of 9-methoxycamptothecin from Nothapodytes nimmoniana (J. Graham) Mabberly.

Wang H1,2,3,4, Ao M1,2,3, Liu W5, Bai Y1,2,3, Zhu Y1,2,3, Yu L1,2,3.

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a Department of Biotechnology, College of Life Science and Technology , Institute of Resource Biology and Biotechnology, Huazhong University of Science and Technology , Wuhan , China.
b Key Laboratory of Molecular Biophysics, Ministry of Education , Wuhan , China.
c Wuhan Institute of Biotechnology , Wuhan , China.
d Department of Chemical Engineering and Food Science , Hubei University of Arts and Science , Xiang yang , China.
e Innovation & Development Center , Fresenius Kabi , Wuhan , China.


We have reported previously that 9-methoxycamptothecin (MCPT) showed significant antitumor activity in vitro. Here, agarose gel electrophoresis experiments were performed to evaluate MCPT's unwinding ability toward plasmid DNA and inhibitory activities against topoisomerases (Topo) I and II. Binding properties of MCPT to calf thymus DNA (CT-DNA) were evaluated by UV-vis, melting temperature, fluorescence, circular dichroism methodologies and molecular docking technique. Results showed that MCPT at 100 μM inhibited Topo I activity, but had no effect on Topo II. Studies on the binding properties indicated that minor groove binding was the most probable binding mode of MCPT to DNA. The abilities of MCPT to act as Topo I inhibitor and minor groove binding agent may be related to its strong antitumor activity.


9-methoxycamptothecin (MCPT); DNA; Topoisomerases

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