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麻黄非生物碱部位抗过敏性哮喘活性组分的化学成分分析
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| 篇名： | 麻黄非生物碱部位抗过敏性哮喘活性组分的化学成分分析 |
| TITLE： | Analysis of Chemical Components of Anti-allergic Asthma Active Fractions in Alkaloids-free Part of Ephedrae Herba |
| 摘要： | 目的：为阐明麻黄非生物碱部位抗过敏性哮喘的药效物质基础提供参考。方法：麻黄用85％乙醇提取、正庚烷萃取后经固相萃取（填料为AC18）前处理，对麻黄提取物进行非生物碱部位富集，并采用高效液相色谱法经UnitaryC18柱和EclipseXDB-C18色谱柱进行麻黄非生物碱类组分制备。以HT-29细胞中高表达的G蛋白偶联受体35（GPR35受体）为靶标、GPR35受体激动剂敏喘宁（1μmol/L）为阳性对照、动态质量重置（DMR）响应值为检测指标，通过无标记细胞整合药理学方法考察各组分（质量浓度均为100μg/mL）对GPR35受体的激动活性和脱敏活性，以筛选抗过敏性哮喘的活性组分。应用高效液相色谱-四极杆飞行时间质谱（HPLC-Q-TOF-MS）技术对活性组分的化学成分进行鉴定。结果：麻黄非生物碱部位主要分为固相萃取前处理的沉淀部分和95％甲醇洗脱部分，从上述两部分中共富集得到了20个组分。其中，沉淀部分中组分F1.5～F1.10及95％甲醇洗脱部分中组分F2.5～F2.10对GPR35受体有较强的激动活性，同时对GPR35受体激动剂敏喘宁显示出了较强的脱敏活性；并且沉淀部分中组分F1.5～F1.10在HT-29细胞上引起的DMR响应信号强度甚至超过了阳性对照药敏喘宁。经HPLC-Q-TOF-MS分析，共从活性组分中鉴定出了24个化合物，其中黄酮类14个、挥发油类2个、有机羧酸类7个、蒽醌类1个。结论：麻黄非生物碱部位主要以黄酮类成分为主，其具有一定的抗过敏性哮喘活性。 |
| ABSTRACT： | OBJECTIVE：To provide reference for elucidating the anti-allergic asthma constituents in alkaloids-free part of Ephedrae Herba. METHODS ：Ephedrae Herba was extracted with 85％ ethanol and n-heptane，and then subjected to solid-phase extraction（filler AC 18）for pretreatment to enrich alkaloids-free part from the extract of Ephedrae Herba. HPLC method was adopted，and alkaloids-free fractions of Ephedrae Herba were performed on Unitary C 18 column and Eclipse XDB-C 18 column. Using high expression G protein coupled-receptor 35（GPR35 receptor）in HT- 29 cell as target ，GPR35 receptor agonist zaprinast （1 μmol/L）as positive control ，DMR response value as the detection index ，the agonistic and desensitizing activity of each fraction（100 μg/mL）on GPR 35 receptor was screened by label-free integrated pharmacological method ，so as to screen active anti-allergic asthma fraction. HPLC-Q-TOF-MS method was used to identify the chemical composition of the selected active fractions. RESULTS ：The alkaloids-free part of Ephedrae Herba was divided into two parts ，involving the precipitated part before solid phase extraction and the 95％ methanol elution part ；from them ，20 fractions were screened. Among them ，the precipitated fraction F 1.5-F1.10 and 95％ methanol eluted fraction F 2.5-F2.10 had a strong agonistic activity on GPR 35 receptor；at the same time，GPR35 receptor agonist zaprinast showed a relatively strong desensitization activity. The signal intensity of DMR induced by F1.5-F1.10 in the precipitated part of HT- 29 cells was even higher than that of reference drug zaprinast. By HPLC-Q-TOF-MS analysis，24 chemical components were identified from active fractions ，involving 14 flavonoids，2 volatile oils ，7 organic carboxylic acids ，1 anthraquinones. CONCLUSIONS ：The alkaloid-free part of Ephedrae Herba is mainly flavonoids and has anti-allergic asthma activity. |
| 期刊： | 2020年第31卷第09期 |
| 作者： | 靳京妹，于大永，侯滔，张秀莉，史丽颖 |
| AUTHORS： | JIN Jingmei ，YU Dayong ，HOU Tao，ZHANG Xiuli，SHI Liying |
| 关键字： | 麻黄；非生物碱部位；G蛋白偶联受体35；过敏性哮喘；化学成分；鉴定 |
| KEYWORDS： | Ephedrae Herba ；Alkaloids-free part ；G protein coupled-receptor 35；Allergic asthma ；Chemical component ； |
| 阅读数： | 391 次 |
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