Devipriya Sankarasharma, Ganapathy Vani, Shyamaladevi Chennam Srinivasulu
Department of Biochemistry, University of Madras, Guindy Campus, Chennai, India.
Chem Biol Interact. 2006 Aug 25;162(2):106-13. doi: 10.1016/j.cbi.2006.04.002. Epub 2006 Jul 17.
Administration of quercetin, a common polyphenolic component of many vascular and edible plants including vegetables, fruits and tea significantly reduced the tumor volume in rats induced for mammary carcinoma using dimethyl benz (a) anthracene (DMBA). Dose response was assessed, by treating the animals with different doses (15-45 mg/kgbw) of quercetin and 25 mg/kgbw was taken as effective dose. Quercetin was administered as an intra tumoral injection once a week for 4 weeks. Serum levels of carcino embryonic antigen (CEA), a potent marker for tumor growth and invasion was significantly decreased on quercetin treatment. Quercetin caused a significant decrease in the activities of acid phosphatase and Cathepsin D in serum of experimental animals. Activities of lysosomal enzymes- (beta-D galactosidase, beta-D glucuronidase, beta-D glucosidase and sialidase), in serum and tissue were significantly altered in DMBA animals compared to control animals. However, quercetin treatment caused no significant change in lysosomal enzyme activities in tissues, whereas the activities were significantly lowered in serum. Partial purification of tissue type plasminogen activator (t-PA) from the tumor and kidney showed increased activity in the DMBA induced animals. Serum urokinase, -like plasminogen activator (u-PA) was also increased in animals with tumor, indicating tumor invasion. Administration of quercetin caused a significant decrease of both t-PA and u-PA. In conclusion, the present study suggests the possible role of quercetin in primary and invasive mammary tumor treatment. The above observations in vivo warrant further studies, due to the easy availability, common occurrence and low toxicity of this dietary bioflavonoid.
槲皮素是许多维管植物和可食用植物(包括蔬菜、水果和茶)中常见的多酚类成分。给用二甲基苯并(a)蒽(DMBA)诱导患乳腺癌的大鼠施用槲皮素,可显著减小肿瘤体积。通过用不同剂量(15 - 45毫克/千克体重)的槲皮素处理动物来评估剂量反应,25毫克/千克体重被视为有效剂量。槲皮素每周进行一次瘤内注射,共注射4周。肿瘤生长和侵袭的有效标志物癌胚抗原(CEA)的血清水平在槲皮素处理后显著降低。槲皮素使实验动物血清中的酸性磷酸酶和组织蛋白酶D的活性显著降低。与对照动物相比,DMBA处理的动物血清和组织中的溶酶体酶(β - D半乳糖苷酶、β - D葡萄糖醛酸酶、β - D葡萄糖苷酶和唾液酸酶)活性发生了显著改变。然而,槲皮素处理对组织中的溶酶体酶活性没有显著影响,而血清中的活性则显著降低。从肿瘤和肾脏中对组织型纤溶酶原激活剂(t - PA)进行部分纯化后发现,在DMBA诱导的动物中其活性增加。患有肿瘤的动物血清中尿激酶样纤溶酶原激活剂(u - PA)也增加,表明肿瘤发生侵袭。施用槲皮素可使t - PA和u - PA均显著降低。总之,本研究表明槲皮素在原发性和侵袭性乳腺肿瘤治疗中可能发挥作用。鉴于这种膳食生物黄酮易于获取、普遍存在且毒性低,上述体内观察结果值得进一步研究。