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·药学研究·

基于黄酮类成分含量构成特征和体外抗病毒活性的不同产地黄

芩的质-效评价研究 Δ

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李 化 ，张明晓，白羽琦，杨 滨（中国中医科学院中药研究所，北京 100700）
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中图分类号 R282 文献标志码 A 文章编号 1001-0408（2020）10-1166-06
DOI 10.6039/j.issn.1001-0408.2020.10.03

摘 要 目的：评价黄芩道地药材与非道地药材中主要黄酮类成分含量构成特征及其抗病毒活性，以探讨黄芩药材的质-效关系
及药效物质基础。方法：制备8批不同产地黄芩（S1～S8）的水提物冻干粉，采用超高效液相色谱法测定水提物中黄芩苷、汉黄芩
苷、黄芩素、汉黄芩素等4种黄酮类成分的含量并计算其含量构成比。按不同产地黄芩的黄酮类成分含量构成比，制备上述4种成
分混合物作为对应的黄酮类成分模拟样品（E1～E8）。以利巴韦林为阳性对照，采用MTT法和细胞病变程度法，考察8批黄芩水
提物样品及其对应的模拟样品对人喉癌细胞Hep-2的半数有毒浓度（TD50 ）和对呼吸道合胞病毒（RSV）的半数抑制浓度（IC50 ），并
计算治疗指数（TI）。采用SPSS 17.0软件对黄芩苷、汉黄芩苷、黄芩素、汉黄芩素含量与其抗RSV活性（IC50值）进行Pearson相关性
分析。结果：样品S4（产地为河北承德）的黄芩苷、汉黄芩苷含量最高，样品S6（产地为内蒙古-2）的黄芩素、汉黄芩素含量最高；上
述4种成分含量最低的分别为样品S6、S6、S7（产地为北京）、S4。样品S4中黄酮苷类成分含量较高，相应的苷元类成分含量较低，
其黄芩苷、汉黄芩苷、黄芩素、汉黄芩素的含量构成比为1∶0.224∶0.111∶0.013；样品S6中黄酮苷类成分含量较低，相应的苷元类成
分含量较高，上述4种成分的含量构成比为1 ∶ 0.241 ∶ 0.713 ∶ 0.106。不同产地黄芩水提物对Hep-2细胞的TC50均高于50 μg/mL，对
RSV的IC50为11.11～51.74 μg/mL，TI为1.86～5.20；其对应的黄酮类成分模拟样品的TC50为23.11～52.23 μg/mL，对RSV的IC50为
4.87～14.61 μg/mL，TI为1.85～4.75。道地产区（河北承德）黄芩（S4）的水提物及其对应模拟样品（E4）的抗RSV作用最强。相关
性分析显示，4种黄酮类成分的含量与其抗病毒活性的相关系数均小于0.5，两者无显著相关性。结论：当黄芩中4种主要黄酮类
成分的含量构成比为1 ∶ 0.224 ∶ 0.111 ∶ 0.013时，其对RSV的抑制作用较强。道地产区黄芩样品具有较优的黄酮类成分构成特征，
该特征可能是道地药材发挥最佳抗病毒疗效的重要物质基础。
关键词 黄芩；道地药材；黄酮类成分；含量测定；抗病毒活性；质-效关系

Study on Quality-efficiency Evaluation of Scutellaria baicalensis from Different Origins Based on Content
Constituent Characteristics of Flavonoids and in vitro Antiviral Activity
LI Hua，ZHANG Mingxiao，BAI Yuqi，YANG Bin（Institute of Chinese Materia Medica，China Academy of
Chinese Medical Sciences，Beijing 100700，China）

ABSTRACT OBJECTIVE：To evaluate content constituent characteristics and antiviral activity of main flavonnoids in genuine
and non-genuine Scutellaria baicalensis，and to investigate quality-efficiency relationship and effective substance. METHODS：
Totally 8 batches of S. baicalensis from different origins（S1-S8）were collected to prepare its water extract lyophilized powder.
UPLC method was used to determine the contents of baicalin，wogonoside，baicalein and wogonin，and calculate their content
constituent ratio. According to the content constituent ratio of flavonoids in S. baicalensis from different origins，the mixture of the
above four components was prepared as the corresponding simulated sample of flavonoids （E1-E8）. Using ribavirin as positive
control，MTT assay and CPE method were used to investigate half toxic concentration（TD50 ）of the water extract from 8 batches
of S. baicalensis and their corresponding simulated samples to human laryngeal carcinoma cell Hep-2 and their half inhibition
concentration（IC50 ）to respiratory syncytial virus（RSV）；treatment indexes（TI）were calculated. Pearson correlation analysis for
the content of baicalin，wogonoside，baicalein and wogonin with their anti-RSV activity （IC50 ） was performed by SPSS 17.0
software. RESULTS：The contents of baicalin and wogonoside in sample S4（from Hebei Chengde）were the highest，and the
contents of baicalein and wogonin in sample S6（from Inner Mongolia-2）were the highest. The contents of above 4 components
were the lowest in sample S6，S6，S7（from Beijing），S4. The contents of flavonoid glycosides in sample S4 were relatively
higher， while those of corresponding glycosides were
Δ 基金项目：国家自然科学基金资助项目（No.81573534）
relatively lower； the content constituent ratio of baicalin，
＊副研究员，硕士生导师，博士。研究方向：中药质量评价及其药
wogonoside，baicalein and wogonin was 1 ∶ 0.224 ∶ 0.111 ∶ 0.013.
效物质基础。电话：010-64014411-2848。E-mail：xiariyuji1@163.com
The contents of flavonoid glycosides in sample S6 were
# 通信作者：研究员，博士生导师，博士。研究方向：中药质量评
价及其药效物质基础。电话：010-64014411-2848。E-mail：ybinmm@ relatively lower， while those of glycosides were relatively
126.com higher；the content constituent ratio of above 4 components

·1166 · China Pharmacy 2020 Vol. 31 No. 10 中国药房 2020年第31卷第10期