CAJ | 학술논문

目的:呋喃香豆素类(补骨脂素类)是导致葡萄柚汁与药物相互作用的重要成分.本研究拟调查该类化合物在其它柑橘类果汁中的存在,并比较这些果汁对细胞色素P450(CYP)3A活性的抑制强度.方法:用梯度高压液相色谱法测定柑橘类的鲜榨果汁中6种呋喃香豆素化合物的组成与含量.以雄性Sprague-Dawley大鼠肝微粒体的睾酮6β-羟化活性测试每种果汁对CYP3A的抑制作用.结果:与葡萄柚汁比较,Jaffa sweetie果汁中呋喃香豆素的组成与含量基本相同,对CYP3A的抑制强度也相当;日本红柚、溪蜜柚和金柚的果汁中呋喃香豆素组成相似但含量较低,对CYP3A的抑制强度也较弱;常山胡柚、甜橙与宽皮橘果汁中呋喃香豆素种类少且含量极低,且多数对CYP3A无抑制作用.结论:根据呋喃香豆素组成可以预测柑橘类果汁因为抑制CYP3A引起的药物相互作用;琯溪蜜柚及近缘品种的果汁可能导致类似于葡萄柚汁的药物相互作用,有必要在临床上加以验证.
목적:부남향두소류(보골지소류)시도치포도유즙여약물상호작용적중요성분.본연구의조사해류화합물재기타감귤류과즙중적존재,병비교저사과즙대세포색소P450(CYP)3A활성적억제강도.방법:용제도고압액상색보법측정감귤류적선자과즙중6충부남향두소화합물적조성여함량.이웅성Sprague-Dawley대서간미립체적고동6β-간화활성측시매충과즙대CYP3A적억제작용.결과:여포도유즙비교,Jaffa sweetie과즙중부남향두소적조성여함량기본상동,대CYP3A적억제강도야상당;일본홍유、계밀유화금유적과즙중부남향두소조성상사단함량교저,대CYP3A적억제강도야교약;상산호유、첨등여관피귤과즙중부남향두소충류소차함량겁저,차다수대CYP3A무억제작용.결론:근거부남향두소조성가이예측감귤류과즙인위억제CYP3A인기적약물상호작용;관계밀유급근연품충적과즙가능도치유사우포도유즙적약물상호작용,유필요재림상상가이험증.
AIM: To investigate the existence of these compounds in other citrus fruit juices, and check their inhibitory intensities on activity of cytochrome P450(CYP) 3A. METHODS: Freshly squeezed citrus fruit juices were determined separately for their composition and levels of six furanocoumarins with a gradient highpressure liquid chromatographic (HPLC) method. Inhibition of CYP3A by each juice sample was tested with the activity of testosterone 6β-hydroxylation in liver microsoms of male Sprague-Dawley rats. RESULTS: Comparing with grapefruit juices, the Jaffa sweetie showed almost the same composition and levels of furanocoumarins, and a comparable inhibitory intensity of CYP3A; the Japanese showed similar compositions but lower levels of furanocoumarins, and weaker inhibiting intensities of CYP3A;mandarins showed less varieties and much lower levels of furanocoumarins, and most of them showed no inhibition of CYP3A. CONCLUSION: Furanocoumarin composition can be an index to predict citrus fruit juice-drug interaction based on CYP3A inhibition; Clinical validations closely related accessions for their possible drug interactions similar to grapefruit juice.