An antagonist of the retinoid X receptor reduces the viability of Trichuris muris in vitro

作者：Hurst Rebecca J M^*; Hopwood Thomas; Gallagher Amanda L; Partridge Frederick A; Burgis Timothy; Sattelle David B; Else Kathryn J

来源：BMC Infectious Diseases, 2014, 14(1): 520.

DOI：10.1186/1471-2334-14-520

• RXR
• HX531
• Trichuris muris
• Nematode
• Viability
• Anthelmintic

Background: Trichuriasis is a parasitic disease caused by the human whipworm, Trichuris trichiura. It affects millions worldwide, particularly in the tropics. This nematode parasite burrows into the colonic epithelium resulting in inflammation and morbidity, especially in children. Current treatment relies mainly on general anthelmintics such as mebendazole but resistance to these drugs is increasingly problematic. Therefore, new treatments are urgently required.
Methods: The prospect of using the retinoid X receptor (RXR) antagonist HX531 as a novel anthelmintic was investigated by carrying out multiple viability assays with the mouse whipworm Trichuris muris.
Results: HX531 reduced both the motility and viability of T. muris at its L3, L4 and adult stages. Further, bioinformatic analyses show that the T. muris genome possesses an RXR-like receptor, a possible target for HX531.
Conclusions: The study suggested that Trichuris-specific RXR antagonists may be a source of much-needed novel anthelmintic candidates for the treatment of trichuriasis. The identification of an RXR-like sequence in the T. muris genome also paves the way for further research based on this new anthelmintic lead compound.

• 出版日期2014-9-27