Deoxyshikonin reversibly inhibits cytochrome P450 2B6

Ju Hyun Kim; Su Min Choi; Riya Shreatha; Gil Saeng Jeong; Tae Cheon Jeong; Sangkyu Lee

doi:10.1002/bdd.2230

Deoxyshikonin reversibly inhibits cytochrome P450 2B6

Ju Hyun Kim
, Su Min Choi
, Riya Shreatha
, Gil Saeng Jeong
, Tae Cheon Jeong
, Sangkyu Lee

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	221-225
Number of pages	5
Journal	Biopharmaceutics and Drug Disposition
Volume	41
Issue number	4-5
DOIs	https://doi.org/10.1002/bdd.2230
State	Published - 1 Apr 2020
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

cytochrome P450 2B6
deoxyshikonin
herb–drug interaction
reversible inhibition

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10.1002/bdd.2230

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title = "Deoxyshikonin reversibly inhibits cytochrome P450 2B6",

abstract = "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 Ki 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.",

keywords = "cytochrome P450 2B6, deoxyshikonin, herb–drug interaction, reversible inhibition",

author = "Kim, \{Ju Hyun\} and Choi, \{Su Min\} and Riya Shreatha and Jeong, \{Gil Saeng\} and Jeong, \{Tae Cheon\} and Sangkyu Lee",

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year = "2020",

month = apr,

day = "1",

doi = "10.1002/bdd.2230",

language = "English",

volume = "41",

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journal = "Biopharmaceutics and Drug Disposition",

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TY - JOUR

T1 - Deoxyshikonin reversibly inhibits cytochrome P450 2B6

AU - Kim, Ju Hyun

AU - Choi, Su Min

AU - Shreatha, Riya

AU - Jeong, Gil Saeng

AU - Jeong, Tae Cheon

AU - Lee, Sangkyu

PY - 2020/4/1

Y1 - 2020/4/1

N2 - 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 Ki 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.

AB - 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 Ki 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.

KW - cytochrome P450 2B6

KW - deoxyshikonin

KW - herb–drug interaction

KW - reversible inhibition

UR - https://www.scopus.com/pages/publications/85085060306

U2 - 10.1002/bdd.2230

DO - 10.1002/bdd.2230

M3 - Article

C2 - 32364297

AN - SCOPUS:85085060306

SN - 0142-2782

VL - 41

SP - 221

EP - 225

JO - Biopharmaceutics and Drug Disposition

JF - Biopharmaceutics and Drug Disposition

IS - 4-5

ER -

Deoxyshikonin reversibly inhibits cytochrome P450 2B6

Abstract

UN SDGs

Keywords

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