Structural Analysis of Mogrol and its Glycosides as Inhibitors of Animal DNA Polymerase and Human Cancer Cell Growth
Mogroside I E1 (compound 3), a steroidal glycoside (i.e., mogroside) isolated from traditional Chinese medicinal plants (Momordica grosvenori) selectively inhibited the activities of animal DNA polymerases from mammals, fish and insects in vitro. The compound showed no effect on the activities of DNA polymerases from plants and procaryotes, and other DNA metabolic enzymes tested. Compound 3 also inhibited human cancer cell growth. Since parts of compound 3 such as mogrol (compound 1) and D-glucose (compound 2) did not influence the activities of any enzymes tested, the converted structure of compounds 1 and 2 might be important for DNA polymerase inhibition and the suppression of cancer cell growth. The other four mogrolal glycosides (i.e., compounds 4 - 7) did not influence the inhibition of DNA polymerase activity and human cancer cell proliferation. The relationship between the three-dimensional molecular structure of mogrol-based compounds and these inhibitory activities is discussed.
No Supplementary Data
No Article Media
Document Type: Research Article
Affiliations: Laboratory of Food and Nutritional Sciences, Department of Nutritional Science, Kobe-Gakuin University, Nishi-ku, Kobe, Hyogo 651-2180, Japan.
Publication date: 01 May 2006
More about this publication?
- Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.