不同中药单体的急性毒性及抗肿瘤活性评价研究  

Study on Evaluation of Acute Toxicity and Antitumor Activity of Different Chinese Medicinal Monomers

作　　者：高妍 尚诚彰 沈月雷 GAO Yan;SHANG Chengzhang;SHEN Yuelei(Jiangxi University of Chinese Medicine,Nanchang,Jiangxi,China,330000;Yangtze Delta Drug Advanced Research,Nantong Jiangsu,China,226133;Biocytogen Pharmaceuticals(Beijing)Co.,Ltd.,Beijing,China,102600)

机构地区：[1]江西中医药大学,江西南昌330000 [2]长三角药物高等研究院,江苏南通226133 [3]百奥赛图(北京)医药科技股份有限公司,北京102600

出　　处：《河南中医》2024年第9期1361-1372,共12页Henan Traditional Chinese Medicine

基　　金：湖南省教育厅科学研究项目(21B0229)。

摘　　要：目的:本研究旨在考察姜黄素、黄芩素、白桦脂酸、白藜芦醇和双氢青蒿素等5种中药单体的急性毒性,并初步探讨不同中药单体的抗肿瘤活性。方法:采用IncuCyte活细胞成像技术检测肿瘤细胞的增殖;采用流式细胞术检测肿瘤细胞凋亡;通过小鼠急性毒性实验初步评价不同中药单体的毒性。取健康8周龄B-NDG雌性小鼠,建立胃癌、结直肠癌和乳腺癌的PDX模型,采用腹腔注射和静脉注射两种给药方式,比较姜黄素、黄芩素、白藜芦醇和双氢青蒿素的抗肿瘤活性。结果:姜黄素、黄芩素、白藜芦醇和双氢青蒿素4种中药单体均有不同程度的抑制肿瘤细胞增殖和促进肿瘤细胞凋亡的作用(P<0.05),其中姜黄素活性最强。急性毒性实验显示,小鼠对黄芩素耐受度最好,姜黄素次之。静脉注射姜黄素在BP0880胃癌PDX模型中体现出了明显的抗肿瘤活性(P<0.05)。结论:在5种中药单体中,姜黄素的抗肿瘤活性最强,且在急性毒性中表现出较高的耐受性。Objective:To investigate the acute toxicity of five Chinese medicinal monomers:curcumin,baicalein,betulinic acid,resveratrol,and dihydroartemisinin,and to preliminarily explore their antitumor activities.Methods:The IncuCyte live-cell imaging technology was used to assess tumor cell proliferation,and flow cytometry was employed to detect tumor cell apoptosis.The acute toxicity of different Chinese medicinal monomers was preliminarily evaluated through a mouse acute toxicity test.Healthy 8-week-old female B-NDG mice were used to establish patient-derived xenograft(PDX) models of gastric cancer,colorectal cancer,and breast cancer.The antitumor activities of curcumin,baicalein,resveratrol,and dihydroartemisinin were compared using intraperitoneal and intravenous injection methods.Results:All four Chinese medicinal monomers:curcumin,baicalein,resveratrol,and dihydroartemisinin,showed varying degrees of inhibition of tumor cell proliferation and promotion of tumor cell apoptosis(P<0.05),with curcumin exhibiting the strongest activity.Acute toxicity tests indicated that mice had the highest tolerance to baicalein,followed by curcumin.Intravenous injection of curcumin demonstrated significant antitumor activity in the BP0880 gastric cancer PDX model(P<0.05).Conclusion:Among the five monomers,curcumin exhibits the strongest antitumor activity and shows a relatively high tolerance in acute toxicity tests.

关 键 词：姜黄素 黄芩素 白桦脂酸 白藜芦醇 双氢青蒿素 抗肿瘤活性 中药单体 急性毒性 PDX模型 小鼠 

分 类 号：R285.5[医药卫生—中药学]