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6,7-二羟基佛手柑素(6,7-DHB)是CYP3A4的强效抑制剂(IC50 = 25 µM)。它似乎是葡萄柚汁中主要负责抑制睾酮6β-羟化酶活性的化合物。在使用通常由CYP3A亚家族细胞色素P450酶代谢的药物治疗期间,摄入葡萄柚汁会导致这些药物的血浆浓度显著增加。然而,在药物被CYP3A4代谢过快的情况下,给予患者葡萄柚汁或单独使用6,7-DHB可能具有一定的优势。6,7-dihydroxy Bergamottin (6,7-DHB) is a potent inhibitor of CYP3A4 (IC50 = 25 µM). It appears to be the primary compound in grapefruit juice that is responsible for inhibition of testosterone 6β-hydrolase activity. Ingestion of grapefruit juice during treatment regimes with drugs normally metabolized by cytochrome P450 enzymes of the CYP3A subfamily results in a substantial increase in plasma concentration of these agents. However, giving a patient grapefruit juice or just 6,7-DHB could be advantageous in cases where a drug is metabolized too quickly by CYP3A4.
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6,7-dihydroxy Bergamottin
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