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Research ArticleDrug Discovery and Translational Medicine

LG308, a Novel Synthetic Compound with Antimicrotubule Activity in Prostate Cancer Cells, Exerts Effective Antitumor Activity

Min Qin, Shihong Peng, Ning Liu, Meichun Hu, Yundong He, Guoliang Li, Huang Chen, Yuan He, Ang Chen, Xin Wang, Mingyao Liu, Yihua Chen and Zhengfang Yi
Journal of Pharmacology and Experimental Therapeutics December 2015, 355 (3) 473-483; DOI: https://doi.org/10.1124/jpet.115.225912
Min Qin
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Shihong Peng
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Ning Liu
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Meichun Hu
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Yundong He
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Guoliang Li
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Huang Chen
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Yuan He
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Ang Chen
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Xin Wang
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Mingyao Liu
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Yihua Chen
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Zhengfang Yi
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China (M.Q., S.P., N.L., M.H., Y.H., G.L., H.C., Y.H., A.C., X.W., M.L., Y.C., Z.Y.); and Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology and Department of Molecular and Cellular Medicine, Texas A & M University Health Science Center, Houston, Texas (M.L.)
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Abstract

Microtubule plays many different essential roles in the process of tumorigenesis in many eukaryotes, and targeting mitotic progression by disturbing microtubule dynamics is used as a common strategy for cancer treatment. Microtubule-targeted drugs, including paclitaxel and Vinca alkaloids, were previously considered to work primarily by increasing or decreasing the cellular microtubule mass. The tubulin/microtubule system, which is an integral component of the cytoskeleton, is a therapeutic target for prostate cancer. In this study, we found a novel synthetic compound, 8-fluoro-N-phenylacetyl-1, 3, 4, 9-tetrahydro-β-carboline (LG308), which disrupted the microtubule organization via inhibiting the polymerization of microtubule in PC-3M and LNCaP prostate cancer cell lines. Further study proved that LG308 induced mitotic phase arrest and inhibited G2/M progression significantly in LNCaP and PC-3M cell lines in a dose-dependent manner, and these were associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. Besides, the cell proliferation and colony formation of PC-3M and LNCaP cells were effectively inhibited by LG308. Furthermore, LG308 induced apoptosis and cell death in PC-3M and LNCaP cell lines in vitro. In vivo, LG308 dramatically suppressed the growth and metastasis of prostate cancer in both xenograft and orthotopic models. All these data indicate that LG308 is a promising anticancer candidate with antimitotic activity for the treatment of prostate cancer.

Footnotes

    • Received May 13, 2015.
    • Accepted September 14, 2015.
  • M.Q. and S.P. contributed equally to this work.

  • This work was supported by the Major State Basic Research Development Program of China [Grants 2015CB910400, 2012CB910400]; National Natural Science Foundation of China [Grants 81272463, 81472788, 81330049, 81202407]; and Innovation Program of Shanghai Municipal Education Commission [Grant 13zz034].

  • dx.doi.org/10.1124/jpet.115.225912.

  • ↵Embedded ImageThis article has supplemental material available at jpet.aspetjournals.org.

  • Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 355 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 355, Issue 3
1 Dec 2015
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Research ArticleDrug Discovery and Translational Medicine

LG308 Suppresses PCa by Blocking Microtubule Polymerization

Min Qin, Shihong Peng, Ning Liu, Meichun Hu, Yundong He, Guoliang Li, Huang Chen, Yuan He, Ang Chen, Xin Wang, Mingyao Liu, Yihua Chen and Zhengfang Yi
Journal of Pharmacology and Experimental Therapeutics December 1, 2015, 355 (3) 473-483; DOI: https://doi.org/10.1124/jpet.115.225912

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Research ArticleDrug Discovery and Translational Medicine

LG308 Suppresses PCa by Blocking Microtubule Polymerization

Min Qin, Shihong Peng, Ning Liu, Meichun Hu, Yundong He, Guoliang Li, Huang Chen, Yuan He, Ang Chen, Xin Wang, Mingyao Liu, Yihua Chen and Zhengfang Yi
Journal of Pharmacology and Experimental Therapeutics December 1, 2015, 355 (3) 473-483; DOI: https://doi.org/10.1124/jpet.115.225912
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