Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza , acts as an inhibitor of human carboxylesterase ( CE ). Tanshinone IIA anhydride has a K i value of 1.9 nM against hCE1 and a K i value of 1.4 nM against hiCE . Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase , and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies.
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