延胡索药材质量控制的关键技术研究
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摘要
延胡索为紫堇科植物延胡索(Corydalis yanhusuo W. T. Wang ex Z. Y. Su et C.Y Wu)的干燥块茎,是著名的“浙八味”中的一种,性味辛、苦、温,具有活血散瘀、理气止痛等功效,其主要的活性化学成分是生物碱。本研究对延胡索药材生产的各个环节的质量控制的关键技术进行研究,为延胡索质量评价和质量控制提出科学的建议,为延胡索药材的可持续发展奠定研究基础。主要研究结果如下：
1)利用HPLC-DAD分析技术和多变量数据处理方法构建了延胡索化学指纹图谱与生物碱成分定量分析相结合的化学多样性评价体系,为本文后续研究及延胡索药材质量评价提供了技术手段。
2)通过不同产地延胡索样品及不同种源同质园样品的化学多样性分析比较,揭示栽培延胡索的化学多样性受环境的影响较大,可能跟其遗传多样性低有关。就指标成分延胡索乙素来说,南通的环境更有利于其积累,具体哪个环境因子起主要作用有待进一步研究。但是从资源的长期可持续利用的角度出发,需引进遗传多样性高的野生群体进行种质改良,提高其有效成分含量的同时增加其对环境的适应能力。
3)通过水煮机理的探讨,进一步证实了水煮对延胡索质量具有显著影响,并揭示了延胡索水煮过程中生物碱含量的变化机制,其主要机理是热溶出作用,同时还伴随着部分生物碱单体的热降解作用,本研究结果支持中国药典规定的水煮工艺,并进一步建议在加工过程中,用80℃以上热(沸)水快速煮延胡索至白心消失。
4)通过对延胡索干燥方法和规格等级的化学多样性的考察,认为应优先考虑空气干燥,同时研究发现生物碱主要分布在块茎的皮层,所以块茎越小,指标成分含量越高。该结果并不支持目前药材规范中延胡索药材规格越大,质量等级越高的规定。
Rhizoma Corydalis, the dry rhizome of Corydalis yanhusuo (Fumariaceae), is one of the famous traditional herb medicine named as "Zhe ba wei". It is widely used in China for promoting blood circulation, reinforcing vital energy and alleviating pain. The alkaloids are considered to be the main bioactive components. In the present research, several key techniques of quality control in production links were studied, so that scientific suggestions can be proprosed for quality assessment and quality control of Rhizoma Corydalis, as well as its sustainable development. The main results are listed as following:
1. Applying HPLC-DAD technique and multivariate statistic analysis, both chemical fingerprints and four alkaloid components quantitative analysis were combined to construct the chemical diversity evaluation system of Rhizoma Corydalis. This evaluation system provides technical means for the present study and quality evaluation of Rhizoma Corydalis.
2. Through analysis and comparison of the chemical diversity of Rhizoma Corydalis from different regions and different geo-sources in a common garden experiment, we found that environment played a more important role in chemical diversity of cultivated populations than genetic background which may be due to low genetic diversity and Nantong environment is more conductive to its accumulation based on the content of THP which is the index component of Rhizoma Corydalis. But which specific factor in environment playing a major role should further study. And from a long-term sustainable use point of view, we should collect wild germplasm resources with high genetic diversity which can be applied to agricultural practice for breeding, so as to increase the active ingredient contents of C. yanhusuo and their ability of adaption to the environment.
3. Study on the boiled mechanism of C. yanhusuo confirmed that boiling have a significant impact on the quality of Rhizoma Corydalis and revealed a process of changes of alkaloid contents during boiling. The mechanism during boiling of C. yanhusuo relates to that the leaching of alkaloids into boiling water mainly and thermal degradation of some alkaloids. The results support the processing method of Rhizoma Corydalis stipulated in Pharmacopeia of China, and further suggest that the processing method is boiling to the point when the white color of the central part of the rhizome disappears rapidly with water above 80℃.
4. Having finished study about the effect of different drying methods and grades on chemical diversity, we suggest that air drying is prior to other drying methods and found that alkaloids of bulbs mainly distribute in the cortex, so the smaller the bulbs, the higher the content of index components. The results do not support the current requirement that the higher the specifications, the higher quality level.
1)利用HPLC-DAD分析技术和多变量数据处理方法构建了延胡索化学指纹图谱与生物碱成分定量分析相结合的化学多样性评价体系,为本文后续研究及延胡索药材质量评价提供了技术手段。
2)通过不同产地延胡索样品及不同种源同质园样品的化学多样性分析比较,揭示栽培延胡索的化学多样性受环境的影响较大,可能跟其遗传多样性低有关。就指标成分延胡索乙素来说,南通的环境更有利于其积累,具体哪个环境因子起主要作用有待进一步研究。但是从资源的长期可持续利用的角度出发,需引进遗传多样性高的野生群体进行种质改良,提高其有效成分含量的同时增加其对环境的适应能力。
3)通过水煮机理的探讨,进一步证实了水煮对延胡索质量具有显著影响,并揭示了延胡索水煮过程中生物碱含量的变化机制,其主要机理是热溶出作用,同时还伴随着部分生物碱单体的热降解作用,本研究结果支持中国药典规定的水煮工艺,并进一步建议在加工过程中,用80℃以上热(沸)水快速煮延胡索至白心消失。
4)通过对延胡索干燥方法和规格等级的化学多样性的考察,认为应优先考虑空气干燥,同时研究发现生物碱主要分布在块茎的皮层,所以块茎越小,指标成分含量越高。该结果并不支持目前药材规范中延胡索药材规格越大,质量等级越高的规定。
Rhizoma Corydalis, the dry rhizome of Corydalis yanhusuo (Fumariaceae), is one of the famous traditional herb medicine named as "Zhe ba wei". It is widely used in China for promoting blood circulation, reinforcing vital energy and alleviating pain. The alkaloids are considered to be the main bioactive components. In the present research, several key techniques of quality control in production links were studied, so that scientific suggestions can be proprosed for quality assessment and quality control of Rhizoma Corydalis, as well as its sustainable development. The main results are listed as following:
1. Applying HPLC-DAD technique and multivariate statistic analysis, both chemical fingerprints and four alkaloid components quantitative analysis were combined to construct the chemical diversity evaluation system of Rhizoma Corydalis. This evaluation system provides technical means for the present study and quality evaluation of Rhizoma Corydalis.
2. Through analysis and comparison of the chemical diversity of Rhizoma Corydalis from different regions and different geo-sources in a common garden experiment, we found that environment played a more important role in chemical diversity of cultivated populations than genetic background which may be due to low genetic diversity and Nantong environment is more conductive to its accumulation based on the content of THP which is the index component of Rhizoma Corydalis. But which specific factor in environment playing a major role should further study. And from a long-term sustainable use point of view, we should collect wild germplasm resources with high genetic diversity which can be applied to agricultural practice for breeding, so as to increase the active ingredient contents of C. yanhusuo and their ability of adaption to the environment.
3. Study on the boiled mechanism of C. yanhusuo confirmed that boiling have a significant impact on the quality of Rhizoma Corydalis and revealed a process of changes of alkaloid contents during boiling. The mechanism during boiling of C. yanhusuo relates to that the leaching of alkaloids into boiling water mainly and thermal degradation of some alkaloids. The results support the processing method of Rhizoma Corydalis stipulated in Pharmacopeia of China, and further suggest that the processing method is boiling to the point when the white color of the central part of the rhizome disappears rapidly with water above 80℃.
4. Having finished study about the effect of different drying methods and grades on chemical diversity, we suggest that air drying is prior to other drying methods and found that alkaloids of bulbs mainly distribute in the cortex, so the smaller the bulbs, the higher the content of index components. The results do not support the current requirement that the higher the specifications, the higher quality level.
引文
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