民族药四数九里香药效部位筛选及咔唑生物碱含量测定研究  

Study on the antitumor activity of carbazole alkaloid from Murraya tetramera Huang and its content analysis

作　　者：周永福 姚如杰[1] 黎学明 李应[3] ZHOU Yongfu;YAO Rujie;LI Xueming;LI Ying(Technology Center of Chongqing Zi-Guang Chemical Co.,Ltd.,Chongqing 401121,China;College of Chemistry and Chemical Engineering,Chongqing University,Chongqing 400044,China;School of Chemistry and Pharmaceutical Engineering,Chongqing Industry Polytechnic College,Chongqing 401120,China)

机构地区：[1]重庆紫光化工股份有限公司技术中心,重庆401121 [2]重庆大学化学化工学院,重庆400044 [3]重庆工业职业技术学院化学与制药工程学院,重庆401120

出　　处：《药学研究》2023年第7期457-461,共5页Journal of Pharmaceutical Research

基　　金：重庆紫光化工股份有限公司博士后项目(No.KQY20220530)。

摘　　要：目的筛选民族药四数九里香抑制肿瘤细胞增殖作用的药效部位及测定质量标准控制物含量。方法采用MTS法筛选萃取馏分及单体化合物的细胞毒活性,利用高效液相色谱法测定质量标准物的含量。结果在初试浓度为100μg·mL^(-1)时,5个馏分中乙酸乙酯萃取馏分对5株肿瘤细胞(HL-60、A-549、SMMC-7721、MCF-7、SW-480)的抑制率最大,故确定其为民族药四数九里香的有效部位,IC 50(μg·mL^(-1))依次为52.84±1.63、78.34±4.79、43.29±1.74、64.19±1.24、43.75±2.20;从药效部位分离和鉴定7个咔唑生物碱化合物,并研究了这些化合物的细胞毒活性,分析得化合物7的抑制作用最大,其抑制肿瘤细胞HL-60、A-549、MCF-7、SW-480的IC 50(μmol·L^(-1))值依次为15.11±1.14、18.11±1.11、24.13±1.32、31.12±1.12;选择咔唑生物碱mahanimbine(化合物7)作为民族药四数九里香的质量标准控制物,分析得到化合物7在四数九里香中的含量为61.08μg·g^(-1)。结论本法对样品前期处理要求不高,设备条件简便,结果可靠,为民族药四数九里香抑制肿瘤细胞增殖作用质量标准建立提供理论支撑。Objective To screen the effective part of the national drug Murraya tetramera Huang for inhibiting the proliferation of tumor cells and determinate the content of quality standard control substance.Methods MTS method was used to screen the cytotoxicity of the extract fractions and carbazole monomers and HPLC method was used to determine the content of the standard substance of the national medicine of Murraya tetramera Huang.Results The initial concentration was 100μg·mL^(-1),the inhibitory rate of the ethyl acetate extract fraction in the extract fraction on five tumor cells(HL-60,A-549,SMMC-7721,MCF-7,SW-480)was the highest,so it was determined as the effective part,IC 50(μg·mL^(-1))were 52.84±1.63,78.34±4.79,43.29±1.74,64.19±1.24,43.75±2.20,respectively;Seven carbazole alkaloids showed inhibitory effects on four column tumor cells,and compound 7 had the largest inhibitory effect;The IC 50(μmol·L^(-1))values of tumor cells HL-60,A-549,MCF-7,SW-480 were 15.11±1.14,18.11±1.11,24.13±1.32,31.12±1.12,respectively.The content of carbazole alkaloid mahanimbine(compound 7),which was the quality standard control substance,in Murraya tetramera Huang was 61.08μg·g^(-1).Conclusion This method had low requirements for sample pretreatment,simple equipment conditions,and stable results,to provide theoretical support for the establishment of the quality standard for the inhibition of tumor cell proliferation by the national drug Murraya tetramera Huang.

关 键 词：民族药 四数九里香 细胞毒活性 咔唑生物碱 质量控制标准物 

分 类 号：R284.2[医药卫生—中药学]