Hundley S G, Freudenthal R I
Cancer Res. 1977 Jan;37(1):244-9.
The metabolism of benzo(a)pyrene was determined, using rhesus monkey hepatic and pulmonary microsomal enzymes. Metabolites were separated by high-pressure liquid chromatography and identified using known reference standards. Metabolites were quantitated by scintillation spectrometry. Both liver and lung microsomes metabolized benzo(a)pyrene to the following metabolites: 9,10-, 7,8-, and 4,5-dihydrodihydroxybenzo(a)pyrene; benzo(a)pyrene-1,6-dione, -3,6-dione, and -6,12-dione; and 9- and 3-hydroxybenzo(a)pyrene. Two unidentified metabolites and one metabolite region which chromatographed prior to 9,10-dihydrodihydroxybenzo(a)pyrene were produced by both liver and lung microsomes. The two unknown peaks were located between, 9,10- and 4,5-dihydrohidroxybenzo(a)pyrene. Two additional unknown metabolites were produced only in the liver and had retention times slightly greater than the 4,5- and 7,8-dihydrodihydroxybenzo(a)pyrene metabolites, respectively. Quantitative determination of benzo(a)pyrene metabolism revealed large differences for the three monkeys and the respective tissue activities. Liver activity for each animal was substantially higher than lung activity for all benzo(a)pyrene metabolites. The ratio of the metabolites also differed between the liver and lung. 3-Hdyroxybenzo(a) pyrene represented over 60% of the total liver metabolite fraction and 30% of the total lung metabolite fraction. The total quinone fraction represented between 7 and 13% of the total metabolites in the liver and comprised over 40% of the total lung metabolites. The metabolite ratios for the dihydrodiols were very similar for both tissues.
利用恒河猴肝脏和肺微粒体酶测定了苯并(a)芘的代谢情况。代谢产物通过高压液相色谱法分离，并使用已知参考标准进行鉴定。代谢产物通过闪烁光谱法进行定量。肝脏和肺微粒体均将苯并(a)芘代谢为以下代谢产物：9,10-、7,8-和4,5-二氢二羟基苯并(a)芘；苯并(a)芘-1,6-二酮、-3,6-二酮和-6,12-二酮；以及9-和3-羟基苯并(a)芘。肝脏和肺微粒体均产生了两种未鉴定的代谢产物以及一个在9,10-二氢二羟基苯并(a)芘之前色谱分离的代谢产物区域。这两个未知峰位于9,10-和4,5-二氢二羟基苯并(a)芘之间。另外两种未知代谢产物仅在肝脏中产生，其保留时间分别略大于4,5-和7,8-二氢二羟基苯并(a)芘代谢产物。苯并(a)芘代谢的定量测定显示，三只猴子以及各自组织活性存在很大差异。对于所有苯并(a)芘代谢产物，每只动物的肝脏活性均显著高于肺活性。肝脏和肺中代谢产物的比例也有所不同。3-羟基苯并(a)芘占肝脏总代谢产物比例的60%以上，占肺总代谢产物比例的30%。醌类总组分占肝脏总代谢产物的7%至13%，占肺总代谢产物的40%以上。两种组织中二氢二醇的代谢产物比例非常相似。
