Sesquiterpene Antitumor Agents: Inhibitors of Cellular Metabolism
| Autor: | Eng Chun Mar, Salwa A. Elgebaly, Ivonne Weidner, Robert I. Hadgraft, Thomas G. Waddell, Iris H. Hall, Charles G. Ruffner, C.O. Starnes, Kuo Hsiung Lee |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Male
Antimetabolites Antineoplastic Alkylation Biology Sesquiterpene lactone Lactones Sesquiterpenes Guaiane Structure-Activity Relationship chemistry.chemical_compound Oxygen Consumption Cyclic AMP medicine Animals Glycolysis Cysteine RNA Neoplasm Sulfhydryl Compounds Carcinoma Ehrlich Tumor Nucleic Acid Synthesis Inhibitors chemistry.chemical_classification Multidisciplinary DNA synthesis DNA Neoplasm Metabolism Glutathione Adenosine Rats Cholesterol Enzyme chemistry Biochemistry Sesquiterpenes medicine.drug Helenalin |
| Zdroj: | Science. 196:533-536 |
| ISSN: | 1095-9203 0036-8075 |
| DOI: | 10.1126/science.191909 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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