Khellinoflavanone, a Semisynthetic Derivative of Khellin, Overcomes Benzo[a]pyrene Toxicity in Human Normal and Cancer Cells That Express CYP1A1.

ABSTRACT: Cytochrome P450 family 1 (CYP1) enzymes catalyze the metabolic activation of environmental procarcinogens such as benzo[a]pyrene, B[a]P, into carcinogens, which initiates the process of carcinogenesis. Thus, stopping the metabolic activation of procarcinogens can possibly prevent the onset of cancer. Several natural products have been reported to show unique ability in inhibiting CYP1 enzymes. We found that khellin, a naturally occurring furanochromone from Ammi visnaga, inhibits CYP1A1 enzyme with an IC₅₀ value of 4.02 μM in CYP1A1-overexpressing human HEK293 suspension cells. To further explore this natural product for discovery of more potent and selective CYP1A1 inhibitors, two sets of semisynthetic derivatives were prepared. Treatment of khellin with al

SUBMITTER: Sharma R 

PROVIDER: S-EPMC6645225 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature