Didemnins
From Wikipedia, the free encyclopedia
Didemnins are cyclodepsipeptide compounds isolated from a tunicate (sea-squirt) of the genus Trididemnum (family of Didemnidæ) that were collected in the Caribbean Sea. They were first isolated in 1978 at the University of Illinois. <ref>Rinehart L., K. et al.. J. Am. Chem. Soc. 1981, 103, 1857-1859.</ref>
Although more than nine Didemnins (Didemnins A-E, G, X and Y) have been isolated from the extract of Trididemnum solidum, Didemnin B is the one that possesses the most potent biological activities. <ref>Rinehart L., K. et al.. J. Nat. Prod. 1988, 51, 1-21.</ref> It is a strong antiviral agent against both DNA and RNA viruses like Herpes simplex virus type 1, a strong immunosuppressant that shows some potential in skin graft <ref>Montgomery, D.; Zukoshi, C. F. Transplantation 1985, 40, 49.</ref> and is also very cytotoxic. It shows strong activity against murine leukemia cells. Large amounts of Didemnin B were chemically synthesized and it was advanced to clinical trials by the National Cancer Institute. It has completed phase II human clinical trials against adenocarcinoma of the kidney <ref>Taylor, S. A.; Goodman, P.; Stuckey, W. J. Stephens, R. L.; Gaynor, E. R. Invest. New Drugs 1992, 10, 55.</ref>, advanced epithelial ovarian cancer <ref>Cain, J. M.; Liu, P. Y.; Alberta, D.E.; Gallion, J.J.; Laufman, L.; O'Sullivan, J.; Weiss, G.; Bickers, J. N. Invest. New Drugs 1992, 10, 113.</ref>, and metastatic breast cancer <ref>Montgomery, D.; Zukoshi, C. F. Transplantation 1985, 40, 49.</ref>. Unfortunately, the compound exhibited high toxicity through a high incidence of anaphylactic reactions in patients and trials were terminated <ref>Nuijen, B.; Bouma, M.; Manada, C.; Jimeno, J.M.; Schellens, J. H. M.; Bult, A.; Beijnen, J. H. Anti-Cancer Drugs 2000, 11, 793.</ref>.
[edit] References
<references/>
