Harapu Camelia Diaconu, Miron Anca, Cuciureanu Magdalena, Cuciureanu Rodica
Facultatea de Farmacie, Disciplina de Chimia mediului si alimentului, Universitatea de Medicină si Farmacie Gr.T. Popa Iaşi.
Rev Med Chir Soc Med Nat Iasi. 2010 Oct-Dec;114(4):1209-14.
Since 1989, grapefruit juice is reported to modify, with clinical implications, the pharmacokinetic of a series of drugs such as calcium channel blockers that are dihydropyridine derivates and/or some HMGCoA reductase inhibitors. All these drugs are metabolized to a large extent by the most abundant human isoform of cytochrome P450, CYP3A4. Grapefruit inhibits the cytochrome P450 3A4 enzyme system responsible for the oxidative metabolism of many orally administered drugs. The most important compounds of GFJ considered to be involved in the pharmacokinetic interaction are flavonoids (naringin, naringenin, narirutin, quercetin, kaempferol, hesperidin, neohesperidin, didymin, and poncirin), furanocoumarins (6',7'-dihydroxy-bergamottin, bergamottin, bergamottin-6',7'-epoxide, bergapten, epoxy-bergamottin) and sesquiterpens (noot-katone).
The experimental researches had as object the comparative study of total content of flavonoidic compounds, like naringin in different fruit juices: citric fruit (white, pink and red grapefruit), apples, pears--industrial or laboratory prepared juices (by squeezing). They praised a different content in flavonoidic compounds for citric and for the rest of analyzed fruits.
For grapefruit juices the concentrations in flavonoidic compounds are higher in total fruit juice: 143.86 mg/100 mL in red, 131.47 mg/100 mL in pink and 84.21 mg/100 mL in white grapefruit juice. In juice prepared from fruit pulp, the concentrations were 81.92 mg/100 mL, 108.23 mg/100 mL and 65.76 mg/100 mL, respectively. The content in naringin, the most important flavanone in citrus fruit, varied between 1.98 and 51.2 mg/100 mL juice.
自1989年以来，据报道葡萄柚汁会改变一系列药物的药代动力学，并产生临床影响，这些药物包括二氢吡啶衍生物类钙通道阻滞剂和/或一些HMGCoA还原酶抑制剂。所有这些药物在很大程度上由人体中最丰富的细胞色素P450同工型CYP3A4代谢。葡萄柚会抑制负责许多口服药物氧化代谢的细胞色素P450 3A4酶系统。葡萄柚汁中被认为参与药代动力学相互作用的最重要化合物是黄酮类化合物（柚皮苷、柚皮素、橙皮芸香苷、槲皮素、山奈酚、橙皮苷、新橙皮苷、地奥明和枳属苷）、呋喃香豆素（6',7'-二羟基-佛手柑内酯、佛手柑内酯、佛手柑内酯-6',7'-环氧化物、补骨脂素、环氧佛手柑内酯）和倍半萜（诺卡酮）。
实验研究的对象是比较不同果汁（工业或实验室制备的果汁（通过压榨））中黄酮类化合物的总含量，如不同柑橘类水果（白色、粉色和红色葡萄柚）、苹果、梨中的柚皮苷。他们发现柑橘类水果和其他分析水果中黄酮类化合物的含量不同。
对于葡萄柚汁，总果汁中黄酮类化合物的浓度更高：红色葡萄柚汁中为143.86毫克/100毫升，粉色葡萄柚汁中为131.47毫克/100毫升，白色葡萄柚汁中为84.21毫克/100毫升。在果肉制备的果汁中，浓度分别为81.92毫克/100毫升、108.23毫克/100毫升和65.76毫克/100毫升。柑橘类水果中最重要的黄烷酮柚皮苷的含量在1.98至51.2毫克/100毫升果汁之间。
