Biological Reactive Intermediates VI: Chemical and by John D. Robertson, Joya Chandra, Vladimir Gogvadze (auth.),

By John D. Robertson, Joya Chandra, Vladimir Gogvadze (auth.), Patrick M. Dansette, Robert Snyder, Marcel Delaforge, G. Gordon Gibson, Helmut Greim, David J. Jollow, Terrence J. Monks, I. Glenn Sipes (eds.)

This quantity provides a dialogue of the organic results produced following the metabolism of xenobiotic chemical compounds to chemically reactive metabolites, i.e., poisonous and carcinogenic results, which were the root of all 5 previous volumes during this sequence. particularly, this quantity devotes sections to structure-activity relationships, fresh advances within the realizing of the chemistry of reactive metabolites, and the iteration and task of reactive oxygen species with designated emphasis on nitric oxide. There also are segments on DNA harm via reactive metabolites and DNA fix, tissue particular responses to BRIs, and human healthiness results of BRIs. The papers that contain this quantity have been submitted by way of global category scientists who have been in attendance on the Symposium on organic Reactive Intermediates VI on the Université René Descartes, July 16-20, 2000.

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26: 107 (1999). G. Block, S. Patterson and A. Subar. Fruit, vegetables and cancer prevention: a review of the epidemiological evidence. Nutr. Cancer 19: 1 (1992). T. Diplock, The Leon Goldberg memorial lecture: Antioxidants and disease prevention. Fd. Chern. Toxicol. 34: 1013 (1996). S. Omenn, Micronutrients (vitamins and minerals) as cancer-preventive agents. fARC Sci. Pub!. 139: 33 (1997). T. MacGregor and L. Jurd, Mutagenicity of plant flavonoids: structural requirements for mutagenic activity in Salmonella typhimurium.

57:27 (1999). 24. G. Y. Gadaska, A. Gallegos, K. Sherrill and D. Goodman. Over-expression of DTdiaphorase in transfected NIH 3T3 cells does not lead to increased anticancer quinone drug sensitivity: A questionable role for the enzyme as a target for bioreductively activated anticancer drugs. Anticancer Res. 15: 1141 (1995). 21 USE OF STRUCTURE-ACTIVITY RELATIONSHIPS FOR PROBING BIOCHEMICAL MECHANISMS: GLUTATHIONE TRANSFERASE ZETA CONJUGATION OF HALOACIDS Paul D. Swartz and Ann M. Richard US Environmental Protection Agency Office of Research and Development National Health and Environmental Effects Research Lab Research Triangle Park, NC 27111 USA INTRODUCTION A structure-activity relationship (SAR) represents an empirical means for generalizing chemical information relative to biological activity, rationalizing existing data, and, ideally, providing an effective linkage between theory and experiment.

Energetic stability is presented relative to the most stable isomer for each flavonoid, electrophilic reactivity is indicated as the energy of the lowest unoccupied molecular orbital (E(LUMO». Numbering of the quinone methides is as indicated in Figure 5. 60 Pro-oxidant toxicity and biotransformation of flavonoids The pro-oxidant toxicity of the flavonoids was investigated in HL-60 cells and revealed that in addition to the pro-oxidant effects and their ease of oxidation especially an increase in polyphenol lipophilicity increases their cytotoxicityl8.

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