Literature DB >> 18226810

In vitro trypanocidal activity of the anti-helminthic drug niclosamide.

Karin Merschjohann1, Dietmar Steverding.   

Abstract

Only a few drugs are available for chemotherapy of African trypanosomiasis and there is an urgent need for the development of new anti-trypanosomal agents. In this study, the anti-helminthic drug niclosamide was tested for its trypanocidal activity in vitro using culture-adapted bloodstream forms of Trypanosoma brucei brucei and Trypanosoma congolense. The concentrations of niclosamide to reduce the growth rate by 50% and to kill all cells were in the low- and mid micromolar ranges for T. b. brucei and T. congolense, respectively. The very low toxicity of niclosamide for mammals makes the compound interesting for drug development for African trypanosomiasis.

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Year:  2007        PMID: 18226810     DOI: 10.1016/j.exppara.2007.12.001

Source DB:  PubMed          Journal:  Exp Parasitol        ISSN: 0014-4894            Impact factor:   2.011


  25 in total

1.  Structure-activity studies of Wnt/β-catenin inhibition in the Niclosamide chemotype: Identification of derivatives with improved drug exposure.

Authors:  Robert A Mook; Jiangbo Wang; Xiu-Rong Ren; Minyong Chen; Ivan Spasojevic; Larry S Barak; H Kim Lyerly; Wei Chen
Journal:  Bioorg Med Chem       Date:  2015-08-10       Impact factor: 3.641

2.  On the photooxidation of the multifunctional drug niclosamide. A kinetic study in the presence of vitamin B2 and visible light.

Authors:  José Natera; Eduardo Gatica; Cecilia Challier; David Possetto; Walter Massad; Sandra Miskoski; Adriana Pajares; Norman A García
Journal:  Redox Rep       Date:  2015-04-21       Impact factor: 4.412

3.  Benzimidazole inhibitors from the Niclosamide chemotype inhibit Wnt/β-catenin signaling with selectivity over effects on ATP homeostasis.

Authors:  Robert A Mook; Xiu-Rong Ren; Jiangbo Wang; Hailan Piao; Larry S Barak; H Kim Lyerly; Wei Chen
Journal:  Bioorg Med Chem       Date:  2017-02-03       Impact factor: 3.641

4.  Small molecule modulators of Wnt/β-catenin signaling.

Authors:  Robert A Mook; Minyong Chen; Jiuyi Lu; Larry S Barak; H Kim Lyerly; Wei Chen
Journal:  Bioorg Med Chem Lett       Date:  2013-01-30       Impact factor: 2.823

5.  Disruption of STAT3 by niclosamide reverses radioresistance of human lung cancer.

Authors:  Shuo You; Rui Li; Dongkyoo Park; Maohua Xie; Gabriel L Sica; Ya Cao; Zhi-Qiang Xiao; Xingming Deng
Journal:  Mol Cancer Ther       Date:  2013-12-20       Impact factor: 6.261

6.  Niclosamide inhibits androgen receptor variants expression and overcomes enzalutamide resistance in castration-resistant prostate cancer.

Authors:  Chengfei Liu; Wei Lou; Yezi Zhu; Nagalakshmi Nadiminty; Chad T Schwartz; Christopher P Evans; Allen C Gao
Journal:  Clin Cancer Res       Date:  2014-04-16       Impact factor: 12.531

7.  Niclosamide overcomes acquired resistance to erlotinib through suppression of STAT3 in non-small cell lung cancer.

Authors:  Rui Li; Zhongliang Hu; Shi-Yong Sun; Zhuo G Chen; Taofeek K Owonikoko; Gabriel L Sica; Suresh S Ramalingam; Walter J Curran; Fadlo R Khuri; Xingming Deng
Journal:  Mol Cancer Ther       Date:  2013-07-26       Impact factor: 6.261

8.  Combined niclosamide with cisplatin inhibits epithelial-mesenchymal transition and tumor growth in cisplatin-resistant triple-negative breast cancer.

Authors:  Junjun Liu; Xiaosong Chen; Toby Ward; Mark Pegram; Kunwei Shen
Journal:  Tumour Biol       Date:  2016-01-26

9.  Niclosamide suppresses macrophage-induced inflammation in endometriosis†.

Authors:  Nikola Sekulovski; Allison E Whorton; Tomoki Tanaka; Yasushi Hirota; Mingxin Shi; James A MacLean; Julio Ricardo Loret de Mola; Kathleen Groesch; Paula Diaz-Sylvester; Teresa Wilson; Kanako Hayashi
Journal:  Biol Reprod       Date:  2020-04-24       Impact factor: 4.285

10.  Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling.

Authors:  Aruna D Balgi; Bruno D Fonseca; Elizabeth Donohue; Trevor C F Tsang; Patrick Lajoie; Christopher G Proud; Ivan R Nabi; Michel Roberge
Journal:  PLoS One       Date:  2009-09-22       Impact factor: 3.240

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