雌激素相关受体α特异性拮抗剂XCT790对H22荷瘤小鼠的体内抗肿瘤作用  

Antitumor effects of specific antagonist of estrogen-related receptor alpha XCT790 on H22 tumor-bearing mice in vivo

作　　者：叶丽香[1] 阮冠宇[2] 董滨华[2] 康雅芳 林芬[2] 毛晓丹[2] 孙蓬明[2] YE Li-xiang;RUAN Guan-yu;DONG Bin-hua;KANG Ya-fang;LIN Fen;MAO Xiao-dan;SUN Peng-ming(Fujian Center for Safety Evaluation of New Drug;Fujian Medical University,Fuzhou 350122,China;2 Laboratory of Gynecological Oncology,Fujian Provincial Maternal and Children Hospita;Affiliated Hospital of Fujian Medical University,Fuzhou 350001,China)

机构地区：[1]福建医科大学福建省新药安全性评价中心,福州350122 [2]福建省妇幼保健院妇科肿瘤实验室福建医科大学附属医院,福州350001

出　　处：《中国临床药理学杂志》2018年第19期2317-2319,共3页The Chinese Journal of Clinical Pharmacology

基　　金：福建省自然科学基金资助项目(2016J01491;2017J01233);福建省卫计委青年课题基金资助项目(2015-1-16);福建省妇幼保健院课题基金资助项目(妇保院研15-07;17-32)

摘　　要：目的研究雌激素相关受体α(ERRα)特异性拮抗剂——XCT790对2种H22荷瘤小鼠模型的体内抗肿瘤作用。方法建立H22腹水瘤和实体瘤小鼠模型,按体重将模型小鼠随机分为5组:模型组,对照组(环磷酰胺:30mg·kg^(-1)),低、中、高3个剂量实验组(XCT790:2,4,6 mg·kg^(-1))。各组用腹腔注射给药,给药体积为20 mL·kg^(-1),连续给药7 d。记录腹水量、实体瘤重,计算肝、脾、肾系数。结果给药后,腹水瘤模型组、对照组和低、中、高3个剂量实验组的腹水量分别为(6.17±3.04),(3.28±1.62),(3.60±1.67),(4.67±2.57),(4.73±2.66)mL,对照组和低剂量实验组与模型组比较,差异均有统计学意义(均P<0.05);实体瘤模型组、对照组和低、中、高3个剂量实验组的瘤重分别为(2.53±0.39),(1.25±0.45),(1.27±0.61),(1.14±0.56),(1.24±0.39)g,对照组和低、中、高3个剂量实验组与模型组比较,差异均有统计学意义(均P<0.05)。腹水瘤、实体瘤小鼠的肝、脾、肾系数组间比较差异均无统计学意义(均P>0.05)。结论 XCT790对H22荷瘤小鼠具有一定的抗肿瘤作用,对肝与脾和肾系数的影响较小。Objective To explore the effect of specific antagonist of estrogen-related receptor alpha——XCT790 on tumor growth,weight,liver index（ LI）,spleen index（ SI） and kidney index（ KI） in the different models of tumor-bearing mice. Methods The H22 ascitic and solid tumor-bearing mice models were established,then mice were randomized into five groups,including model group（ 20% DMSO）,control group（ cyclophosphamide： CTX 30 mg·kg^-1）,experimental-L,-M,-H groups（ XCT790： 2,4,6 mg·kg^-1）. The samples were obtained in 24 h after continuous intraperitoneal administration of drug or solvent to mice for 7 d. The ascitic volume and tumor weight were measured. The ratios of LI,SI,KI were calculated. Results The ascitic volume of mice in model group,control group,and experimental-L,-M,-H groups were（ 6. 17 ± 3. 04）,（ 3. 28 ± 1. 62）,（ 3. 60 ± 1. 67）,（ 4. 67 ± 2. 57）,（ 4. 73 ± 2. 66） mL; comparing between control group,experimental-L group and model group,the differences were significant（ all P〈0. 01）. In H22 solid tumor-bearing mice,the tumor weight of mice in model group, control group,experimental-L,-M,-H groups were（ 2. 53 ± 0. 39）,（ 1. 25 ± 0. 45）,（ 1. 27 ± 0. 61）,（ 1. 14 ± 0. 56）,（ 1. 24 ± 0. 39） g with significant difference compared with model group（ all P〈0. 05）. LI,SI and KI had no statistically significant differences in ascitic or solid tumor-bearing groups（ all P〉0. 05）. Conclusion XCT790 had anti-tumor effect on H22 tumor-bearing mice without influences on ratios of liver,spleen and kidney.

关 键 词：雌激素相关受体α XCT790 H22肝癌 抗肿瘤 抑瘤率 

分 类 号：R979.1[医药卫生—药品]