Ivermectin: An Anthelmintic, an Insecticide, and Much More

被引:112
作者
Martin, Richard J. [1 ]
Robertson, Alan P. [1 ]
Choudhary, Shivani [1 ]
机构
[1] Iowa State Univ, Dept Biomed Sci, Ames, IA 50011 USA
关键词
GATED CHLORIDE CHANNEL; P-GLYCOPROTEIN; CAENORHABDITIS-ELEGANS; BRAIN PENETRATION; NUCLEAR IMPORT; IN-VITRO; GENE; SENSITIVITY; RESISTANCE; PHARMACOKINETICS;
D O I
10.1016/j.pt.2020.10.005
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
Here we tell the story of ivermectin, describing its anthelmintic and insecticidal actions and recent studies that have sought to reposition ivermectin for the treatment of other diseases that are not caused by helminth and insect parasites. The standard theory of its anthelmintic and insecticidal mode of action is that it is a selective positive allosteric modulator of glutamate-gated chloride channels found in nematodes and insects. At higher concentrations, ivermectin also acts as an allosteric modulator of ion channels found in host central nervous systems. In addition, in tissue culture, at concentrations higher than anthelmintic concentrations, ivermectin shows antiviral, antimalarial, antimetabolic, and anticancer effects. Caution is required before extrapolating from these preliminary repositioning experiments to clinical use, particularly for Covid-19 treatment, because of the high concentrations of ivermectin used in tissue-culture experiments.
引用
收藏
页码:48 / 64
页数:17
相关论文
共 107 条
[1]   Curiouser and Curiouser: The Macrocyclic Lactone, Abamectin, Is also a Potent Inhibitor of Pyrantel/Tribendimidine Nicotinic Acetylcholine Receptors of Gastro-Intestinal Worms [J].
Abongwa, Melanie ;
Buxton, Samuel K. ;
Robertson, Alan P. ;
Martin, Richard J. .
PLOS ONE, 2016, 11 (01)
[2]   Activation of rat recombinant α1β2γ2S GABAA receptor by the insecticide ivermectin [J].
Adelsberger, H ;
Lepier, A ;
Dudel, J .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2000, 394 (2-3) :163-170
[3]   Effects of ivermectin and midecamycin on ryanodine receptors and the Ca2+-ATPase in sarcoplasmic reticulum of rabbit and rat skeletal muscle [J].
Ahern, GP ;
Junankar, PR ;
Pace, SM ;
Curtis, S ;
Mould, JA ;
Dulhunty, AF .
JOURNAL OF PHYSIOLOGY-LONDON, 1999, 514 (02) :313-326
[4]   FXR agonist activity of conformationally constrained analogs of GW 4064 [J].
Akwabi-Ameyaw, Adwoa ;
Bass, Jonathan Y. ;
Caldwell, Richard D. ;
Caravella, Justin A. ;
Chen, Lihong ;
Creech, Katrina L. ;
Deaton, David N. ;
Madauss, Kevin P. ;
Marr, Harry B. ;
McFadyen, Robert B. ;
Miller, Aaron B. ;
Navas, Frank, III ;
Parks, Derek J. ;
Spearing, Paul K. ;
Todd, Dan ;
Williams, Shawn P. ;
Wisely, G. Bruce .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (16) :4733-4739
[5]   Comment on: Measurements of the in vitro anti-mycobacterial activity of ivermectin are method-dependent [J].
Ameen, Sirwan Muhammed ;
Drancourt, Michel .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2014, 69 (06) :1724-1725
[6]   Old wine in new bottles: Drug repurposing in oncology [J].
Antoszczak, Michal ;
Markowska, Anna ;
Markowska, Janina ;
Huczynski, Adam .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2020, 866
[7]   Ivermectin: From theory to clinical application [J].
Ashour, Dalia S. .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2019, 54 (02) :134-142
[8]   Ivermectin exhibits potent anti-mitotic activity [J].
Ashraf, Shoaib ;
Prichard, Roger .
VETERINARY PARASITOLOGY, 2016, 226 :1-4
[9]   Effects of glutamate and ivermectin on single glutamate-gated chloride channels of the parasitic nematode H. contortus [J].
Atif, Mohammed ;
Estrada-Mondragon, Argel ;
Nguyen, Bindi ;
Lynch, Joseph W. ;
Keramidas, Angelo .
PLOS PATHOGENS, 2017, 13 (10)
[10]   Inhibition of Plasmodium sporogonic stages by ivermectin and other avermectins [J].
Azevedo, Raquel ;
Mendes, Antonio M. ;
Prudencio, Miguel .
PARASITES & VECTORS, 2019, 12 (01)