In Vitro Activity of Geldanamycin Derivatives against Schistosoma japonicum and Brugia malayi

المؤلفون المشاركون

Shen, Yuehai
Ramirez, Bernadette
Wenkert, David
Kron, Michael A.

المصدر

Journal of Parasitology Research

العدد

المجلد 2010، العدد 2010 (31 ديسمبر/كانون الأول 2010)، ص ص. 1-7، 7ص.

الناشر

Hindawi Publishing Corporation

تاريخ النشر

2010-12-29

دولة النشر

مصر

عدد الصفحات

7

التخصصات الرئيسية

علم الحيوان
الأمراض

الملخص EN

Geldanamycin (GA) is a benzoquinone-containing ansamycin that inhibits heat shock protein 90.

GA derivatives are being evaluated as anti-neoplastic agents, but their utility against parasites whose heat shock proteins (Hsps) have homology with human Hsp90 is unknown.

The activities of four synthetic GA derivatives were tested in vitro using adult Brugia malayi and Schistosoma japonicum.

Two of the derivatives, 17-N-allyl-17-demethoxygeldanamycin (17-AAG) and 17-N-(2-dimethylaminoethylamino)-17-demethoxygeldanamycin (DMAG), are currently in human clinical trials as anticancer drugs.

Using concentrations considered safe peak plasma concentrations for these two derivatives, all four derivatives were active against both parasites.

The less toxic derivative 17-AAG was as effective as GA in killing S.

japonicum, and both DMAG and 5′-bromogeldanoxazinone were more active than 17-AAG against B.

malayi.

This work supports continued evaluation of ansamycin derivatives as broad spectrum antiparasitic agents.

نمط استشهاد جمعية علماء النفس الأمريكية (APA)

Wenkert, David& Ramirez, Bernadette& Shen, Yuehai& Kron, Michael A.. 2010. In Vitro Activity of Geldanamycin Derivatives against Schistosoma japonicum and Brugia malayi. Journal of Parasitology Research،Vol. 2010, no. 2010, pp.1-7.
https://search.emarefa.net/detail/BIM-492915

نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)

Wenkert, David…[et al.]. In Vitro Activity of Geldanamycin Derivatives against Schistosoma japonicum and Brugia malayi. Journal of Parasitology Research No. 2010 (2010), pp.1-7.
https://search.emarefa.net/detail/BIM-492915

نمط استشهاد الجمعية الطبية الأمريكية (AMA)

Wenkert, David& Ramirez, Bernadette& Shen, Yuehai& Kron, Michael A.. In Vitro Activity of Geldanamycin Derivatives against Schistosoma japonicum and Brugia malayi. Journal of Parasitology Research. 2010. Vol. 2010, no. 2010, pp.1-7.
https://search.emarefa.net/detail/BIM-492915

نوع البيانات

مقالات

لغة النص

الإنجليزية

الملاحظات

Includes bibliographical references

رقم السجل

BIM-492915