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Deoxyshikonin reversibly inhibits cytochrome P450 2B6
Author(s) -
Kim JuHyun,
Choi Su Min,
Shreatha Riya,
Jeong GilSaeng,
Jeong Tae Cheon,
Lee Sangkyu
Publication year - 2020
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2230
Subject(s) - cytochrome p450 , cyp2b6 , hydroxylation , microsome , chemistry , pharmacology , drug , enzyme , cytochrome , herb , drug interaction , biochemistry , traditional medicine , biology , medicinal herbs , cyp3a4 , medicine
Deoxyshikonin, a natural shikonin derivative, is the major component of Lithospermum erythrorhizon and exhibits various pharmacological effects such as lymphangiogenetic, antibacterial, wound healing, and anticancer effects. To investigate the herb–drug interaction potential associated with deoxyshikonin, the inhibitory effects of deoxyshikonin on eight major cytochrome P450 (CYP) enzymes were examined using cocktail substrate‐incubated human liver microsomes. Deoxyshikonin strongly inhibited CYP2B6‐catalyzed bupropion hydroxylation, with a K i value of 3.5 μM, and the inhibition was confirmed using purified human CYP2B6. The inhibition was reversible because the inhibitory effect of deoxyshikonin was not dependent on the preincubation time. The results indicated that deoxyshikonin‐induced drug–drug interaction should be considered when any herb containing deoxyshikonin is used for conventional medications.