Islam Dilara, Lombardini Eric, Ruamsap Nattaya, Imerbsin Rawiwan, Khantapura Patchariya, Teo Ian, Neesanant Pimmnapar, Gonwong Siriphan, Yongvanitchit Kosol, Swierczewski Brett E, Mason Carl J, Shaunak Sunil
Department of Enteric Diseases, Armed Forces Research Institute of Medical Sciences (AFRIMS), Bangkok, Thailand.
Department of Veterinary Medicine, Armed Forces Research Institute of Medical Sciences (AFRIMS), Bangkok, Thailand.
Immunology. 2016 Feb;147(2):178-89. doi: 10.1111/imm.12549. Epub 2015 Nov 24.
Shigella dysenteriae causes the most severe of all infectious diarrhoeas and colitis. We infected rhesus macaques orally and also treated them orally with a small and non-absorbable polypropyletherimine dendrimer glucosamine that is a Toll-like receptor-4 (TLR4) antagonist. Antibiotics were not given for this life-threatening infection. Six days later, the clinical score for diarrhoea, mucus and blood was 54% lower, colon interleukin-8 and interleukin-6 were both 77% lower, and colon neutrophil infiltration was 75% less. Strikingly, vasculitis did not occur and tissue fibrin thrombi were reduced by 67%. There was no clinical toxicity or adverse effect of dendrimer glucosamine on systemic immunity. This is the first report in non-human primates of the therapeutic efficacy of a small and orally bioavailable TLR antagonist in severe infection. Our results show that an oral TLR4 antagonist can enable controlled resolution of the infection-related-inflammatory response and can also prevent neutrophil-mediated gut wall necrosis in severe infectious diarrhoeas.
痢疾志贺菌可引发所有感染性腹泻和结肠炎中最为严重的病症。我们对恒河猴进行口服感染,并口服给予一种小型且不可吸收的聚丙醚亚胺树枝状大分子葡糖胺,它是一种Toll样受体4(TLR4)拮抗剂。对于这种危及生命的感染未给予抗生素治疗。六天后,腹泻、黏液和便血的临床评分降低了54%,结肠白细胞介素-8和白细胞介素-6均降低了77%,结肠中性粒细胞浸润减少了75%。引人注目的是,未发生血管炎,组织纤维蛋白血栓减少了67%。葡糖胺树枝状大分子对全身免疫没有临床毒性或不良反应。这是在非人灵长类动物中关于一种小型且口服生物可利用的TLR拮抗剂在严重感染中的治疗效果的首次报告。我们的结果表明,口服TLR4拮抗剂能够实现对感染相关炎症反应的可控消退,并且还能预防严重感染性腹泻中中性粒细胞介导的肠壁坏死。