世界中医药

作者	单位
张永欣1，朱童1，2，杨丹1，滕菲1，朱晶晶1，王智民1，陈两绵1，高慧敏1，冯伟红1	1 中国中医科学院中药研究所,中药质量控制技术国家工程实验室,北京,100700 2 安徽中医药大学药学院,合肥,230012

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中文摘要:

目的:在黄连的采收加工过程中,大量的黄连须作为农业废弃物而丢弃,为探索其在植物源农药方面的应用价值和前景,对黄连须根的化学成分及其含量进行测定,并对其提取物和单体成分进行活性筛选。方法:采用酸水提取,制备黄连须根提取物,采用超高效液相色谱-高分辨质谱联用技术(UPLC-Q-TOF-MS)对其生物碱类成分进行定性分析,指认黄连须根中的主要化学成分;采用一测多评方法,对其中的盐酸小檗碱、盐酸黄连碱、盐酸药根碱、盐酸表小檗碱、盐酸巴马汀等5个成分进行定量研究;采用抑菌圈法,评价须根提取物及部分单体成分对农业病原菌的抑制活性。结果:通过质谱指认了黄连须根酸水提取物中14种生物碱类成分,其中5种主要生物碱含量总和是6.9%～9.1%,其含量约为主根提取物的26%,具有开发利用价值。通过对黄连、须根2种提取物以及黄连须根中的主要成分盐酸黄连碱的活性筛选,发现黄连须根提取物在1、10、50、100 mg/L 4个浓度下对农业中常见病原菌(小麦赤霉菌、番茄灰霉菌、辣椒疫霉菌、小麦纹枯病、番茄早疫病、苹果斑点落叶病、辣椒炭疽菌、水稻稻瘟病)抑制活性较弱,仅有黄连提取物在高浓度(100 mg/L)时对辣椒疫霉菌的抑制活性达50%,其余抑菌活性均低于50%。须根中的盐酸黄连碱在50 mg/L对辣椒疫霉菌、小麦纹枯病均具有较强的抑制活性(>80%),对水稻稻瘟病、辣椒炭疽菌也有较强的抑制活性,分别达71.43%和63.64%。结论:黄连须根中的生物碱成分含量较高,且对农业中常见病原菌有一定的抑制活性,尤其是盐酸黄连碱对辣椒疫霉菌、小麦纹枯病均具有较强的抑制活性,具备开发利用潜力,可以为黄连须根的综合利用提供依据。

English Summary:

During the harvesting and processing of Rhizoma Coptidis，a large number of Rhizoma Coptidis whiskers are discarded as agricultural wastes，in order to explore the application value and Prospect of Coptis whiskers in botanical pesticides，the chemical composition and content of Coptis whiskers were determined，and the activity of extracts and monomers were screened.Methods:In this study，the fibrous root extract of Rhizoma Coptidis was prepared by acid water extraction，the alkaloids were qualitatively analyzed by UPLC-q-TOF/MS，the main chemical components in the fibrous root extract of Rhizoma Coptidis were identified by combining reference substance with literature.The quantitative analysis of berberine hydrochloride，berberine hydrochloride，jatrorrhizine hydrochloride，epiberberine hydrochloride and palmatine hydrochloride was carried out by quantitative analysis of multi-components with single marker，and the inhibition activity of fibrous root extracts and some monomers against agricultural pathogens was evaluated by inhibition zone method.Results:A total of 14 alkaloids in the fibrous root extract of Rhizoma Coptidis were identified by mass spectrometry.The total content of 5 main alkaloids was 6.9%～9.1%，which was about 26% of the main root extract，and has development and utilization value.Through the active screening of the 2 extracts of Coptis root and fibrous roots，and the main component of Rhizoma Coptidis root--berberine hydrochloride，it was found that the extracts from Rhizoma Coptidis had significant inhibitory effect on common pathogenic bacteria in agriculture(Gibberella graminearum，Botrytis cinerea，Phytophthora capsici，Wheat Sheath Blight，Tomato early blight，Alternaria mali，Colletotrichum capsicum and rice blast) under four concentrations of 1 mg/L,10 mg/L,50 mg/L and 100 mg/L.Only the extract of Rhizoma Coptidis at high concentration(100 mg/L) had 50% inhibitory activity against Phytophthora capsici，and the other antibacterial activities were less than 50%.Berberine hydrochloride in fibrous roots had strong inhibitory activity against Phytophthora capsici and Wheat Sheath Blight(>80%) at 50 mg/L.It also had strong inhibitory activity against rice blast and Colletotrichum capsici，reaching 71.43% and 63.64% respectively.Conclusion:The content of alkaloids in the fibrous roots of Rhizoma Coptidis is still high，and it has certain inhibitory activity to the common pathogenic bacteria in agriculture，especially the strong inhibitory activity of berberine hydrochloride to Phytophthora capsici and sharp eyespot of wheat，which has the potential of development and utilization.The results of this study provide the basis for the comprehensive utilization of fibrous roots of Rhizoma Coptidis.

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