Arizona Board of Regents, a Body Corporate

Arizona State University

Feng Gao

George R Pettit

Rui Tan

An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 1, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Phakellia carteri. Halistatin 1 (8.8.times.10.sup.-7 % yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulin.

Isolation and structure of Halistatin 1

An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 2, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Axinella cf. carteri (Dendy). Halistatin 2 (1.4.times.10.sup.-6 % yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulino. Further, Halistatin 2 displayed significant activity against selected human tumor cell lines.

Isolation and structure of Halistatin 2

The marine bryozoan Bugula neritina has been found to contain a novel 22-membered macrocyclic lactone which is an inhibitor of lymphocytic leukemia as measured by the US National Cancer Institute's P 388 and in vitro evaluation system. The novel lactone is herein denominated 'neristatin 1' and is elucidated.

Growing community of inventors

Tempe, AZ, United States of America

Feng Gao