ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN

被引:14
作者
CONDER, GA [1 ]
ZIELINSKI, RJ [1 ]
JOHNSON, SS [1 ]
KUO, MST [1 ]
COX, DL [1 ]
MARSHALL, VP [1 ]
HABER, CL [1 ]
DIROMA, PJ [1 ]
NELSON, SJ [1 ]
CONKLIN, RD [1 ]
LEE, BL [1 ]
GEARY, TG [1 ]
ROTHWELL, JT [1 ]
SANGSTER, NC [1 ]
机构
[1] UNIV SYDNEY,DEPT VET PATHOL,SYDNEY,NSW 2006,AUSTRALIA
关键词
D O I
10.7164/antibiotics.45.977
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostrongylus colubriformis) from jirds, and clearance of Haemonchus contortus from lambs. A crude extract of UC 11065 containing dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 was active against C. elegans and against H. contortus in the jird. Purified and/or synthetic samples of dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 were tested in the jird model; only dioxapyrrolomycin exhibited appreciable activity against H. contortus (greater-than-or-equal-to 90.9% clearance at 0.33 mg/jird), while none of the compounds showed appreciable activity against T. colubriformis. Dioxapyrrolomycin cleared 99.9% of H. contortus from lambs at 12.5 mg/kg. An in vitro migration study using susceptible and closantel-resistant H. contortus showed there is cross-resistance between dioxapyrrolomycin and closantel. Dioxapyrrolomycin appears to be a narrow-spectrum anthelmintic which works through a closantel-like mode-of-action.
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收藏
页码:977 / 983
页数:7
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