Related Experiment Video
Updated: Jun 16, 2026

Bioluminescence Imaging to Detect Late Stage Infection of African Trypanosomiasis
Published on: May 18, 2016
Podophyllotoxin analogues active versus Trypanosoma brucei
Md Jashim Uddin1, David C Smithson, Kristin M Brown
1Department of Biochemistry, Chemistry and Pharmacology, Vanderbilt Institute of Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Abstract:
In an effort to discover novel anti-trypanosomal compounds, a series of podophyllotoxin analogues coupled to non-steroidal anti-inflammatory drugs (NSAIDs) has been synthesized and evaluated for activity versus Trypanosoma brucei and a panel of human cell lines, revealing compounds with low nano-molar potencies. It was discovered that coupling of NSAIDs to podophyllotoxin increased the potencies of both compounds over 1300-fold. The compounds were shown to be cytostatic in nature and seem to act via de-polymerization of tubulin in a manner consistent with the known activities of podophyllotoxin. The potencies against T. brucei correlated directly with LogP values of the compounds, suggesting that the conjugates are acting as hydrophobic tags allowing podophyllotoxin to enter the cell.
Related Concept Videos
Antiprotozoal Agents
Anthelminthic Agents
American Trypanosomiasis
Antifungal Agents
Physical Properties of Amines
Directly Acting Muscle Relaxants: Dantrolene and Botulinum Toxin
The binding of dantrolene to the RYR1...

