In vitro trypanocidal activity of the anti-helminthic drug niclosamide

Merschjohann, Karin; Steverding, Dietmar

doi:10.1016/j.exppara.2007.12.001

Cited by 34 publications

(33 citation statements)

References 20 publications

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“…It is deduced that 3 easily enters into the cercarial body and distributes uniformly. This result is in agreement with previous studies by Merschjohann et al, [7] to a certain extent, which finds that niclosamide can penetrate into the body of rats elsewhere beyond the circulatory system. We could deduce that 3 was effectively absorbed by cercariae through its tegument, which led to cercaria's rapid death.…”

Section: Cercaria Imagingsupporting

confidence: 95%

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Novel derivatives of niclosamide synthesis: Its bioactivity and interaction with Schistosoma japonicum cercariae

Yang

et al. 2011

Dyes and Pigments

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Section: Cercaria Imagingsupporting

confidence: 95%

“…Niclosamide (see Scheme 1, compound 1) has a long trackrecord as a killer of the tapeworm and snails that harbor Schistosome [7]. Moreover, niclosamide can effectively prevent Schistosoma japonicum cercariae from entering a human host by rendering cercariae uninfective with very short contact time [8].…”

Section: Introductionmentioning

confidence: 99%

Novel derivatives of niclosamide synthesis: Its bioactivity and interaction with Schistosoma japonicum cercariae

Yang

et al. 2011

Dyes and Pigments

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“…In a study of the antitrypanosomal activities of 34 different alkaloids, T. congolense was found to be less susceptible than T. b. brucei (Merschjohann et al, 2001). In another study involving the antitrypanosomal activity of niclosamide, T. congolense was found to be 10 times less susceptible than T. b. brucei (Merschjohann and Steverding, 2008). The susceptibility of different trypanosome species to different chemotherapeutic agents vary.…”

Section: Discussionmentioning

confidence: 99%

Investigation of the Antitrypanosomal Activity of <i>Buchholzia coriacea</i> Seed Extract against a Field Strain of <i>Trypanosoma congolense</i>

Nweze

Anene

Asuzu

2011

Afr. J. Trad. Compl. Alt. Med.

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The antitrypanosomal activity of the methanol extract of Buchholzia coriacea seed against a field strain of Trypanosoma congolense was investigated using experimentally infected mice of both sexes. Monitoring of parasitaemia was by the rapid matching technique. When parasitaemia was approximately log 7.8 (63 x 10 6 parasites/ml), treatment with graded doses of the extract (250, 500 and 1000 mg/kg) was instituted for 5 consecutive days. Diminazene diaceturate (Dimivet ® SKM Pharma Pvt. Ltd.) was given at 3.5 mg/kg i.p. to the positive control mice. No significant differences in body weights were observed. The rectal temperatures of infected mice showed fluctuations. The PCV of infected mice were significantly (p < 0.05) lower than those of the uninfected controls. There was no significant difference between the PCV of the extract-treated and untreated animals. Parasitaemia increased steadily in the extract-treated and untreated mice groups till all the animals died. Three days post-treatment with diminazene diaceturate parasitaemia was cleared. Six days later, there was a relapse of infection. By the end of the experiment, a 50 % relapse rate was recorded in the diminazene diaceturatetreated group. The methanol extract of Buchholzia coriacea seeds did not show any antitrypanosomal activity in mice infected with Trypanosoma congolense at the doses tested.

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“…Niclosamide has low toxicity in mammals (oral LD 50 in rats, >5,000 mg/kg; ref. 33) and is inexpensive and readily available. Here, we report on niclosamide as an antileukemic agent with two independent antineoplastic mechanisms: NF-κB pathway inactivation and ROS generation.…”

Section: Discussionmentioning

confidence: 99%

Antineoplastic Mechanisms of Niclosamide in Acute Myelogenous Leukemia Stem Cells: Inactivation of the NF-κB Pathway and Generation of Reactive Oxygen Species

Jin

Lu²,

Ding³

et al. 2010

Cancer Research

299

305

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NF-κB may be a potential therapeutic target for acute myelogenous leukemia (AML) because NF-κB activation is found in primitive human AML blast cells. In this report, we initially discovered that the potent antineoplastic effect of niclosamide, a Food and Drug Administration-approved antihelminthic agent, was through inhibition of the NF-κB pathway in AML cells. Niclosamide inhibited the transcription and DNA binding of NF-κB. It blocked tumor necrosis factor-induced IκBα phosphorylation, translocation of p65, and expression of NF-κB-regulated genes. Niclosamide inhibited the steps TAK1→IκB kinase (IKK) and IKK→IκBα. Niclosamide also increased the levels of reactive oxygen species (ROS) in AML cells. Quenching ROS by the glutathione precursor N-acetylcysteine attenuated niclosamide-induced apoptosis. Our results together suggest that niclosamide inhibited the NF-κB pathway and increased ROS levels to induce apoptosis in AML cells. On translational study of the efficacy of niclosamide against AML, niclosamide killed progenitor/stem cells from AML patients but spared those from normal bone marrow. Niclosamide was synergistic with the frontline chemotherapeutic agents cytarabine, etoposide, and daunorubicin. It potently inhibited the growth of AML cells in vitro and in nude mice. Our results support further investigation of niclosamide in clinical trials of AML patients. Cancer Res; 70(6); 2516-27. ©2010 AACR.

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In vitro trypanocidal activity of the anti-helminthic drug niclosamide

Cited by 34 publications

References 20 publications

Novel derivatives of niclosamide synthesis: Its bioactivity and interaction with Schistosoma japonicum cercariae

Novel derivatives of niclosamide synthesis: Its bioactivity and interaction with Schistosoma japonicum cercariae

Investigation of the Antitrypanosomal Activity of <i>Buchholzia coriacea</i> Seed Extract against a Field Strain of <i>Trypanosoma congolense</i>

Antineoplastic Mechanisms of Niclosamide in Acute Myelogenous Leukemia Stem Cells: Inactivation of the NF-κB Pathway and Generation of Reactive Oxygen Species

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