α-葡萄糖苷酶是治疗糖尿病与肥胖症的关键靶标酶,抑制其活性可有效实现治疗作用。为高效发掘天然产物中靶向α-葡萄糖苷酶的抑制剂,该研究采用磁性纳米颗粒与α-葡萄糖苷酶结合的策略,选择性捕获潜在生物活性化合物,并利用超高效液相色...α-葡萄糖苷酶是治疗糖尿病与肥胖症的关键靶标酶,抑制其活性可有效实现治疗作用。为高效发掘天然产物中靶向α-葡萄糖苷酶的抑制剂,该研究采用磁性纳米颗粒与α-葡萄糖苷酶结合的策略,选择性捕获潜在生物活性化合物,并利用超高效液相色谱-四极杆-飞行时间串联质谱(ultra-high performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry,UHPLC-Q-TOF/MS)对捕获成分进行快速鉴定。通过单因素试验确定,当戊二醛体积分数为15%、α-葡萄糖苷酶浓度为7 U/mL、固定反应时间为4 h时,固定化酶的相对活性达最大值。基于优化后的固定化酶体系,经UHPLC-Q-TOF/MS鉴定从青钱柳(Cyclocarya paliurus)提取物中筛选出14种化合物,其中10种活性成分对α-葡萄糖苷酶具有较强的抑制作用,各活性化合物和阿卡波糖IC_(50)值如下:异绿原酸A(870.3μg/mL)、杨梅素-3-O-β-D-葡萄糖苷(123.9μg/mL)、槲皮素-3-O-葡萄糖醛酸苷(587.2μg/mL)、槲皮苷(320.9μg/mL)、杨梅素(25.7μg/mL)、金丝桃苷(394.1μg/mL)、阿福豆苷(272.7μg/mL)、山柰酚-3-O-β-D-吡喃葡萄糖醛酸苷(524.9μg/mL)、山柰酚(21.6μg/mL)、槲皮素(31.0μg/mL)和阿卡波糖(0.62μg/mL)。结果表明,固定化酶技术在药用植物潜在治疗化合物的高效发掘中具有重要应用前景。展开更多
Background:Cyperi Rhizoma,derived from Cyperus rotundus L.,is a widely used medicinal herb in traditional Chinese medicine(TCM),with Shandong Province recognized as its geo-authentic habitat.However,the quality of Cyp...Background:Cyperi Rhizoma,derived from Cyperus rotundus L.,is a widely used medicinal herb in traditional Chinese medicine(TCM),with Shandong Province recognized as its geo-authentic habitat.However,the quality of Cyperi Rhizoma varies significantly across different regions,potentially influencing its therapeutic efficacy.This study investigates the influence of geographic origin on the chemical composition and overall quality of Cyperi Rhizoma.Methods:A comprehensive approach,including traditional quality assessment,GC-MS(g as c hromatography-m ass s pectrometry),RP-HPLC(r everse p hase h igh-p erformance l iquid c hromatography),and FT-IR(f ourier t ransform i nfrared s pectroscopy)techniques,was employed to analyze Cyperi Rhizoma samples from Shandong Province.These methods examined the physical appearance,chemical profile,and content variations,particularly focusing onα-cyperone.Results:Traditional quality assessments revealed noticeable differences in the external characteristics of the samples.GC-MS analysis identified a variety of unique chemical constituents,while RP-HPLC and FT-IR showed significant variations inα-cyperone content,with higher levels found in Shandong samples.Conclusion:These results demonstrate that geographic origin is a critical determinant of Cyperi Rhizoma quality,with Shandong specimens exhibiting superiorα-cyperone levels and characteristic phytochemical profiles.This validates the geo-authenticity concept in TCM and provides actionable data for developing evidence-based quality standards,suggesting that provenance should be prioritized in medicinal material selection and pharmacopeial specifications.展开更多
文摘α-葡萄糖苷酶是治疗糖尿病与肥胖症的关键靶标酶,抑制其活性可有效实现治疗作用。为高效发掘天然产物中靶向α-葡萄糖苷酶的抑制剂,该研究采用磁性纳米颗粒与α-葡萄糖苷酶结合的策略,选择性捕获潜在生物活性化合物,并利用超高效液相色谱-四极杆-飞行时间串联质谱(ultra-high performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry,UHPLC-Q-TOF/MS)对捕获成分进行快速鉴定。通过单因素试验确定,当戊二醛体积分数为15%、α-葡萄糖苷酶浓度为7 U/mL、固定反应时间为4 h时,固定化酶的相对活性达最大值。基于优化后的固定化酶体系,经UHPLC-Q-TOF/MS鉴定从青钱柳(Cyclocarya paliurus)提取物中筛选出14种化合物,其中10种活性成分对α-葡萄糖苷酶具有较强的抑制作用,各活性化合物和阿卡波糖IC_(50)值如下:异绿原酸A(870.3μg/mL)、杨梅素-3-O-β-D-葡萄糖苷(123.9μg/mL)、槲皮素-3-O-葡萄糖醛酸苷(587.2μg/mL)、槲皮苷(320.9μg/mL)、杨梅素(25.7μg/mL)、金丝桃苷(394.1μg/mL)、阿福豆苷(272.7μg/mL)、山柰酚-3-O-β-D-吡喃葡萄糖醛酸苷(524.9μg/mL)、山柰酚(21.6μg/mL)、槲皮素(31.0μg/mL)和阿卡波糖(0.62μg/mL)。结果表明,固定化酶技术在药用植物潜在治疗化合物的高效发掘中具有重要应用前景。
基金supported by the National Natural Science Foundation of China(No.82204610)Qihang Talent Program(L2022046)+1 种基金the Scientific and Technological Innovation Project of China Academy of Chinese Medical Sciences(CI2021A04013)Fundamental Research Funds for the Central Public Welfare Research Institutes(ZZ15-YQ-041 and L2021029).
文摘Background:Cyperi Rhizoma,derived from Cyperus rotundus L.,is a widely used medicinal herb in traditional Chinese medicine(TCM),with Shandong Province recognized as its geo-authentic habitat.However,the quality of Cyperi Rhizoma varies significantly across different regions,potentially influencing its therapeutic efficacy.This study investigates the influence of geographic origin on the chemical composition and overall quality of Cyperi Rhizoma.Methods:A comprehensive approach,including traditional quality assessment,GC-MS(g as c hromatography-m ass s pectrometry),RP-HPLC(r everse p hase h igh-p erformance l iquid c hromatography),and FT-IR(f ourier t ransform i nfrared s pectroscopy)techniques,was employed to analyze Cyperi Rhizoma samples from Shandong Province.These methods examined the physical appearance,chemical profile,and content variations,particularly focusing onα-cyperone.Results:Traditional quality assessments revealed noticeable differences in the external characteristics of the samples.GC-MS analysis identified a variety of unique chemical constituents,while RP-HPLC and FT-IR showed significant variations inα-cyperone content,with higher levels found in Shandong samples.Conclusion:These results demonstrate that geographic origin is a critical determinant of Cyperi Rhizoma quality,with Shandong specimens exhibiting superiorα-cyperone levels and characteristic phytochemical profiles.This validates the geo-authenticity concept in TCM and provides actionable data for developing evidence-based quality standards,suggesting that provenance should be prioritized in medicinal material selection and pharmacopeial specifications.
