美洲大蠊提取物CⅡ-3的抗肝癌谱效关系研究
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篇名: 美洲大蠊提取物CⅡ-3的抗肝癌谱效关系研究
TITLE: Study on Spectrum-effect Relationship of Anti-hepatoma Effect of C Ⅱ-3 Extract from Periplaneta americana
摘要: 目的:研究美洲大蠊提取物CⅡ-3与其体外抗肝癌活性的谱效关系,并初步明确其抗肝癌活性成分。方法:在已建立10批CⅡ-3样品的超高效液相色谱(UHPLC)指纹图谱的基础上,借助超高效液相色谱-四极杆-飞行时间质谱联用法(UHPLC-Q-TOF/MS),通过标准品和相关文献定性鉴定各色谱峰对应的化合物;以各批CⅡ-3样品对人肝癌细胞HepG2的半数抑制浓度(IC50)为抗肝癌活性指标,采用灰色关联度分析法(GRA)与正交偏最小二乘法(OPLS)建立并分析指纹图谱与抗肝癌活性之间的谱效关系。结果:10批CⅡ-3样品的UHPLC指纹谱图中有共有峰25个,指认出其中10个,分别为环(酪氨酸-脯氨酸)(峰24)、环(甘氨酸-苯丙氨酸)(峰15)、次黄嘌呤(峰3)、腺嘌呤(峰7)、苯丙氨酸(峰10)、肌苷(峰11)、N-乙酰多巴胺(峰16)、环(脯氨酸-丙氨酸)(峰13)、2-羟基马尿酸(峰22)、环(脯氨酸-丝氨酸)(峰6)。10批CⅡ-3样品对HepG2细胞的IC50为70.550~200.303μg/mL。25个共有峰中,以抗肝癌活性的GRA分析关联度(r)排序为峰20>23>24>15,且其r值均大于0.7;以OPLS分析变量重要性投影(VIP)值排序为峰23>18>15>24>7>14>6>2>20,且VIP值均大于1,其中峰7、15、20、23、24的标准回归系数均大于0,峰2、6、14、18的标准回归系数均小于0。联合分析显示,CⅡ-3样品抗肝癌活性主要成分依次为峰20>23>24>15。结论:CⅡ-3中两个未知化合物(峰20、23)和环(酪氨酸-脯氨酸)(峰24)、环(甘氨酸-苯丙氨酸)(峰15)可能是其抗肝癌活性的主要成分。
ABSTRACT: OBJECTIVE:To study the spectrum-ef fect relationship of anti-hepatoma effect of C Ⅱ-3 extract from Periplaneta americana,and to preliminarily clarify the anti-hepatoma active components of it. METHODS :Based on UHPLC fingerprints of 10 batches of C Ⅱ-3 samples,with the help of UHPL C-Q-TOF/MS,the compounds corresponding to each chromatographic peak were identified qualitatively by standard substances and related literatures. Using the IC 50 value of each batch of C Ⅱ-3 sample against human hepatoma cells HepG 2 as anti-hepatoma activity index ,the spectrum-effect relationship of fingerprint and anti-hepatoma effect was established and analyzed by the combination of grey relational analysis (GRA)and orthogonal partial least squares(OPLS). RESULTS :There were 25 common peaks in UHPLC fingerprints of 10 batches of C Ⅱ-3 samples,and 10 chemical compounds were identified ,which were cyclo- (Tyr-Pro)(peak 24),cyclo-(Gly-Phe)(peak 15),hypoxanthine(peak 3), adenine(peak 7),phenylalanine(peak 10),inosine(peak 11),N-acetyldopamine(peak 16),cyclo-(Pro-Ala)(peak 13),2-hydroxy propionyl(peak 22),cyclo-(Pro-Ser)(peak 6). The IC 50 of 10 batches of C Ⅱ-3 samples to HepG 2 cells was 70.550-200.303 μg/mL. Among 25 common peaks ,the order of GRA correlation (r)of anti-hepatoma activity was peak 20>23>24>15,all of r values were greater than 0.7;the order of variable importance projection (VIP)of OPLS analysis was peak 23>18>15>24>7>14>6> 2>20,all of VIP values were greater than 1. The standard regression coefficients of peak 7,15,20,23,24 were all greater than 0;while the standard regression coefficients of peak 2,6,14,18 were all less than 0. Conjoint analysis shows that the order of anti-hepatoma activity was peak 20>23>24>15. CONCLUSIONS:unknown chemical ingredients (peak 20, ),cyclo-(Tyr-Pro)(peak 24)and cyclo- (Gly-Phe)(peak 15) in C Ⅱ-3 may be main anti-hepatoma active components.
期刊: 2020年第31卷第16期
作者: 周姣姣,何正春,夏从龙,张成桂,刘湘,刘光明
AUTHORS: ZHOU Jiaojiao,HE Zhengchun,XIA Conglong,ZHANG Chenggui,LIU Xiang,LIU Guangming
关键字: 美洲大蠊;抗肝癌作用;灰色关联度法;正交偏最小二乘法;谱效关系;超高效液相色谱-四极杆-飞行时间质谱联用法
KEYWORDS: Periplaneta american;Anti-hepatoma effect ; Grey relational analysis ; Orthogonal partial least squares ;
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