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Epoxy-guaiane Cancer Inhibitors: New Class of Natural Products Isolated from the African Plant Phyllanthus englerii

Posted Apr 28 2011 8:00pm

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.

The new chemical entities can be potential cancer therapeutics, especially for renal cancer.

  • 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.

John A Beutler (NCI)

Patent Status:
HHS, Reference No. E-064-2008/2
US, Application No. 12/811,245 filed 29 Jul 2010

and related international filings

Relevant Publication:
  1. 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 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 for more information. Click here to view the NCI collaborative opportunity announcement.

Cancer - Therapeutics
In-vitro Data

For Licensing Information Please Contact:
Surekha Vathyam Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4076
Fax: 301-402-0220

Ref No: 1721

Updated: 04/2011

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