Epoxy-guaiane Cancer Inhibitors: New Class of Natural Products Isolated from the African Plant Phyllanthus englerii
Description of Invention:
The present invention involves the observation of renal selective inhibitory activity by the extracts of the African plant Phyllanthus englerii. Bioassay-guided fractionation of the purified extracts revealed a series of novel chemical entities which are named Englerin A-F. The englerins and their derivatives are useful in the treatment of a number of cancers, particularly renal cancer. The englerins exhibit selective and potent renal cell inhibitory activity in vitro.
These compounds are recoverable in reasonable yield from natural product extracts and are considered to be reasonably tractable for synthetic chemistry schemes. Sufficient supply of several analogs had been extracted from repository samples for identification and initial biological characterization. Subsequent five-dose testing in the NCI60 screening panel indicated and confirmed impressive renal-selective activity.
Applications:
The new chemical entities can be potential cancer therapeutics, especially for renal cancer.
Advantages:
There is reasonable yield and recovery of the compounds from the natural product extracts.
The synthetic chemistry schemes for synthesis of these compounds are considered to be reasonably tractable.
Development Status:
Proof of concept in vitro studies have been completed and further in vitro and in vivo animal model studies are ongoing.
Patent Status:
DHHS Reference No. E-064-2008/0 --
U.S. Provisional Application No. 61/018,938 filed 04 Jan 2008
Relevant Publication: S Sutthivaiyakit et al. A novel 29-nor-3,4-seco-friedelane triterpene and a new guaiane sesquiterpene from the roots of Phyllanthus oxyphyllus. Tetrahedron 2003 Dec 8;59(50:9991-9995.
Licensing Status: Available for exclusive or non-exclusive licensing.
Collaborative Research Opportunity:
The National Cancer Institute Molecular Targets Development Program is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize epoxy-guaiane cancer inhibitors. Please contact John D. Hewes, Ph.D. at 301-435-3121 or hewesj@mail.nih.gov for more information.
Portfolios: Cancer
Cancer -Therapeutics-Conventional Chemotherapy-Alkylating Agents Cancer -Therapeutics-Conventional Chemotherapy-Other Cancer -Therapeutics
For Additional Information Please Contact: Surekha Vathyam Ph.D.
Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/435-4076
Email: vathyams@mail.nih.gov
Fax: 301/402-0220
