Related Experiment Videos
Cytotoxic quassinoids from Cedronia granatensis
M Tischler1, J H Cardellina, M R Boyd
1Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, Maryland 21702-1201.
Journal of Natural Products
|May 1, 1992
Summary
Researchers isolated two quassinoids, sergiolide and isobrucein B, from Cedronia granatensis. These compounds show significant antitumor activity against melanoma and other solid tumor cell lines in vitro.
Area of Science:
- Natural Products Chemistry
- Pharmacology
- Oncology
Background:
- The National Cancer Institute (NCI) employs in vitro screening to identify novel anticancer agents.
- Cedronia granatensis is a plant source with potential for bioactive compound discovery.
- Quassinoids are a class of natural products known for diverse biological activities.
Purpose of the Study:
- To isolate and characterize bioactive compounds from Cedronia granatensis using the NCI's antitumor screen.
- To evaluate the in vitro antitumor activity of isolated compounds against a panel of cancer cell lines.
Main Methods:
- Fractionation and isolation of organic and aqueous extracts of Cedronia granatensis.
- In vitro antitumor screening using NCI's disease-oriented panel.
- Determination of differential sensitivity and LC50 levels for isolated compounds.
Main Results:
- Two quassinoids, sergiolide and isobrucein B, were successfully isolated.
- These compounds exhibited a 1000-fold range of differential sensitivity across tested cell lines.
- Sergiolide and isobrucein B demonstrated LC50-level responses against melanoma, colon, lung, and other solid tumor cell lines at 10(-5)-10(-8) M concentrations.
Conclusions:
- Sergiolide and isobrucein B possess significant in vitro antitumor activity.
- The differential sensitivity suggests potential for targeted therapy development.
- Further in vivo evaluation in xenograft models is warranted for these quassinoids.