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In vitro effects of garlic compounds on human CYPs (2A6, 2E1 and 3A4)

In vitro effects of garlic compounds on human CYPs (2A6, 2E1 and 3A4). Anticarcinogenic properties of garlic compounds could be explained by the inhibition of the activities of CYPs which are able to activate carcinogens.

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In vitro effects of garlic compounds on human CYPs (2A6, 2E1 and 3A4)

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  1. In vitro effects of garlic compounds on human CYPs (2A6, 2E1 and 3A4) Anticarcinogenic properties of garlic compounds could be explained by the inhibition of the activities of CYPs which are able to activate carcinogens Objective : to determine and to compare the inactivation capacities of DADSO and DADS on these human CYPs (in vitro)

  2. Procedure for monitoring the inactivation of human CYPs DADSO, DADS NADPH Microsomes Substrate Cofactors Preincubation Enzyme assay

  3. Results : inactivation of human CYP 2A6 by DADSO Without DADSO 0 µM 50 µM DADSO + GSH 100 µM 200 µM 400 µM DADSO Criteria for mechanism-based inactivation: - time dependent loss of activity - rate of inactivation is proportional to the concentration of inhibitor Prevention of CYP inactivation by glutathione Hypothesis : DADSO reacts directly with SH of the enzyme

  4. Conclusions : Inactivation of human CYPs by DADSO and DADS DADSO and DADS inactivate CYPs 2A6, 2E1 and 3A4, involved in carcinogen activation The rate of inactivation is more important for DADSO as compared with DADS (No inactivation of CYP 2E1 by DADS) The affinity of DADSO for different CYPs is higher as compared with DADS

  5. In vivo effects of garlic extracts on several carcinogen metabolizing enzymes in the rat liver Objective: to better understand the anticarcinogenic capacities of garlic extracts. These enzymes are involved either in the activation (CYPs) or in the detoxification (Phase II) of carcinogens

  6. liver Garlic extracts Printanor Experimental protocol CytosolsMicrosomes Enzyme assaysCYPs 1A, 2B, 2E1, 3A Phase II: Glutathione transferase Quinone reductase UDP-glucuronyl transferase Immunodetectionof isoenzymes

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