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Science 29 April 1977:
Vol. 196. no. 4289, pp. 533 - 536
DOI: 10.1126/science.191909
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Articles

Science, Vol 196, Issue 4289, 533-536
Copyright © 1977 by American Association for the Advancement of Science

articles

Sesquiterpene antitumor agents: inhibitors of cellular metabolism

KH Lee, IH Hall, EC Mar, CO Starnes, SA ElGebaly, TG Waddell, RI HADGRAFT, CG Ruffner, and I Weidner

Helenalin and tenulin injected into CF1 male mice bearing Ehrlich ascites tumors inhibit DNA synthesis and DNA polymerase enzymatic activity in the tumor cells. Helenalin inhibited protein synthesis. Both drugs increased the concentration of adenosine 3',5'-monophosphate, and interfered with glycolytic and mitochondrial energy processes. Cholesterol synthesis was also inhibited, resulting in lower serum cholesterol levels in tumor-bearing animals. Data obtained in vitro indicate that the cyclopentenone-bearing sesquiterpene lactone and related compounds do not alkylate puring bases of nucleic acids but rather undergo a Michael-type addition reaction with the sulfhydryl groups of reduced glutathione and l-cysteine. Thus, the inhibition of cellular enzyme activities and metabolism that has been observed with these drugs might be explained by the occurrence of a Michael-type teaction.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Dual mechanisms of action of the 5-benzylidene-hydantoin UPR1024 on lung cancer cell lines.
A. Cavazzoni, R. R. Alfieri, C. Carmi, V. Zuliani, M. Galetti, C. Fumarola, R. Frazzi, M. Bonelli, F. Bordi, A. Lodola, et al. (2008)
Mol. Cancer Ther. 7, 361-370
   Abstract »    Full Text »    PDF »
Oxidative Stress-mediated Apoptosis. THE ANTICANCER EFFECT OF THE SESQUITERPENE LACTONE PARTHENOLIDE.
J. Wen, K.-R. You, S.-Y. Lee, C.-H. Song, and D.-G. Kim (2002)
J. Biol. Chem. 277, 38954-38964
   Abstract »    Full Text »    PDF »
Helenalin Triggers a CD95 Death Receptor-independent Apoptosis That Is Not Affected by Overexpression of Bcl-xL or Bcl-2.
V. M. Dirsch, H. Stuppner, and A. M. Vollmar (2001)
Cancer Res. 61, 5817-5823
   Abstract »    Full Text »    PDF »


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