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9种通络祛风中药提取物对黄嘌呤氧化酶的体外抑制活性研究 Δ

1，2 #
李 芮 1，2＊ ，马良会 ，王 栋 ，张春雷 ，周 孟 ，廖尚高 （1.贵州医科大学药学院/省部共建药用植物功效与利
2
1
1
1
用国家重点实验室，贵阳 550025；2.贵州医科大学民族药与中药开发应用教育部工程研究中心/贵州省药物制
剂重点实验室，贵阳 550004）
中图分类号 R285.1 文献标志码 A 文章编号 1001-0408（2020）06-0677-06
DOI 10.6039/j.issn.1001-0408.2020.06.08

摘 要 目的：研究9种通络祛风中药的提取物对黄嘌呤氧化酶（XO）的体外抑制活性，以筛选活性突出的中药提取物。方法：以
黄嘌呤为底物、XO为反应酶，以别嘌醇为阳性对照，以三角风、石胡椒、山莓、金雀花根、紫藤根、牛迭肚根、梓木皮、凌霄花根、爬岩
香等药材的水提物和甲醇提取物（以下简称“醇提物”）以及活性提取物的石油醚、二氯甲烷、乙酸乙酯、正丁醇、水等萃取部位为对
象，采用紫外分光光度法检测各样品对XO的抑制率，采用Graphpad prism 6.0软件计算半数抑制浓度（IC50 ）以筛选活性提取物/部
位；采用双倒数法判断药材的酶抑制作用的类型。结果：9 种中药共 18 个提取物中，500 μg/mL 各中药提取物（除石胡椒醇提物
外），250 μg/mL三角风、石胡椒、山莓、爬岩香的水提物和醇提物，250 μg/mL梓木皮水提物，250 μg/mL金雀花根、牛迭肚根、凌霄
花根醇提物，125 μg/mL金雀花根、牛迭肚根醇提物以及62.5 μg/mL金雀花根醇提物对XO的抑制率均超过了50％；其中，金雀花
根醇提物的IC50值为43.43 μg/mL，低于其他药材的提取物，为活性提取物。金雀花根醇提物石油醚、二氯甲烷、乙酸乙酯、正丁醇、
水等萃取部位的IC50值分别为＞200、193.35、7.67、14.80、＞200 μg/mL，其中乙酸乙酯提取部位的IC50值与阳性对照（5.11 μg/mL）
接近。金雀花根醇提物对XO的抑制类型为竞争-非竞争性抑制，不同于阳性对照的竞争性抑制。结论：金雀花根、牛迭肚根、石胡
椒、山莓、爬岩香、三角风等醇提物及三角风、石胡椒、梓木皮等水提物对 XO 均具有一定的体外抑制活性，以金雀花根醇提物最
强，且该提取物的乙酸乙酯萃取部位的抑制活性与别嘌醇相当，但抑制类型有所差异。
关键词 黄嘌呤氧化酶抑制活性；痛风；中药；提取物；金雀花根；体外

Study on in vitro Inhibitory Activity of the Extracts from 9 Kinds of TCM for Dredging Collaterals and
Dispelling Wind on Xanthine Oxidase
1
1
LI Rui ，MA Lianghui ，WANG Dong ，ZHANG Chunlei ，ZHOU Meng ，LIAO Shanggao （1. School of
1，2
1
2
1，2
Pharmacy， Guizhou Medical University/State Key Laboratory of Functions and Applications of Medicinal
Plants，Guiyang 550025，China；2. Engineering Research Center for the Development and Application of Ethnic
Medicine and TCM，Ministry of Education/Guizhou Provincial Key Laboratory of Pharmaceutics，Guizhou
Medical University，Guiyang 550004，China）
ABSTRACT OBJECTIVE：To study in vitro inhibitory activities of 9 kinds of TCM for dredging collaterals and dispelling wind
on xanthine oxidase（XO），and to screen TCM with outstanding activity. METHODS：Using xanthine as substrate and xanthinase
as reaction enzyme，allopurinol as positive control，with water extract and methanol extract（hereinafter referred to as“ethanol
extract”）from the stem and leaves of Hedera nepalensis，the whole plant of Piper wallichii，the fruits of Rubus corchorifolius，the
root of Caragana sinica，the root of Wisteria sinensis，the root of Rubus crataegifolius，the bark of Catalpa ovata，the root of
Campsis grandiflora，the stem of P. hancei（hereinafter referred to by plant name）and petroleum ether，dichloromethane，ethyl
acetate，n-butanol and water fraction of active extract as the objects，inhibition rate of each sample to XO was detected by
spectrophotometry；IC50 values were calculated with Graphpad prism 6.0 software to screen active extract/fraction. Double reciprocal
method was used to determine the type of enzyme inhibition. RESULTS：Among 9 kinds of TCM and 18 kinds of the extracts，the
inhibitory rates to XO of 500 μg/mL extracts from each TCM（except for ethanol extract of P. wallichii），250 μg/mL water extract
and ethanol extract of H. nepalensis，P. wallichii ，R. corchorifolius and P. hancei ，250 μg/mL water extract of C. ovata ，250
μ g/mL ethanol extract of C. sinica ，R. crataegifolius and C. grandiflora ，125 μ g/mL ethanol extract of C. sinica and R.
crataegifolius ，62.5 μg/mL ethanol extract of C. sinica were more than 50％. The IC50 value of the ethanol extract from C. sinica
was 43.43 μg/mL，which was lower than the extracts of other TCM，and which was the active extract. The IC50 values of petroleum
ether，dichloromethane，ethyl acetate，n-butanol and water fraction of ethanol extract from C. sinica were ＞200，193.35，7.67，
14.80 and ＞200 μg/mL，respectively. The IC50 value of ethyl
Δ 基金项目：国家自然科学基金资助项目（No.81860690）
acetate extract was close to that of positive control（5.11
＊硕士研究生。研究方向：药物体内代谢。E-mail：787403723@qq.
μ g/mL）. Inhibitory type of ethanol extract from C. sinica to
com
# 通信作者：教授，博士生导师，博士。研究方向：天然药物化学、 XO was competitive-noncompetitive inhibition， which was
中草药药效物质基础及药物开发。E-mail：lshangg@163.com different from competitive inhibition of positive control.

中国药房 2020年第31卷第6期 China Pharmacy 2020 Vol. 31 No. 6 ·677 ·