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.

中文翻译：

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脱氧Shikonin可逆地抑制细胞色素P450 2B6。

Deoxyshikonin，天然紫草衍生物，是的主要成分紫草并表现出各种药理作用如lymphangiogenetic，抗菌，伤口愈合，和抗癌作用。为研究与脱氧Shikonin相关的草药-药物相互作用潜力，使用鸡尾酒基质孵育的人肝微粒体检测了脱氧Shikonin对八种主要细胞色素P450（CYP）酶的抑制作用。脱氧Shikonin强烈抑制CYP2B6催化的安非他酮羟基化，K _iCYP2B6为3.5μM，使用纯化的人CYP2B6确认抑制。该抑制作用是可逆的，因为脱氧Shikonin的抑制作用不依赖于预孵育时间。结果表明，当任何含有脱氧shikonin的草药用作常规药物时，应考虑脱氧shikonin诱导的药物相互作用。