| 引用本文:王安琪1，田莉娟1，陈晓鹏2，张静1，邹立伟1，杨凌1.清肺排毒汤对二肽基肽酶-Ⅳ的抑制作用研究[J].世界中医药,2022,(08):. |
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| 清肺排毒汤对二肽基肽酶-Ⅳ的抑制作用研究 |
| Inhibitory Effect of Qingfei Paidu Decoction on DPP-Ⅳ |
| 投稿时间：2021-03-17 |
| DOI：10.3969/j.issn.1673-7202.2022.08.003 |
| 中文关键词: 二肽基肽酶-Ⅳ 抑制剂 2型糖尿病 清肺排毒汤 新型冠状病毒肺炎 芹菜素 槲皮素 山柰酚 |
| English Keywords:DPP-Ⅳ Inhibitor Type 2 diabetes mellitus Qingfei Paidu Decoction COVID-19 Apigenin Quercetin Kaempferol |
| 基金项目:国家重点研发计划项目“新冠肺炎应急项目”（2020YFC0845400）；国家科技重大专项“重大新药创制”(2018ZX09731016-004)；国家重点研发计划项目“中医药现代化研究”(2017YFC1702000) |
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| 中文摘要: |
| 目的：以自主研发的二肽基肽酶-Ⅳ（DPP-Ⅳ）特异性双光子荧光探针甘氨酰-脯氨酰-N-丁基-4-氨基-1,8-萘二甲酰亚胺（GP-BAN）为底物，人血浆为DPP-Ⅳ酶原，评价方剂清肺排毒汤及处方中中药材对DPP-Ⅳ的抑制作用，并进一步评价具有DPP-Ⅳ抑制活性中药材的成分单体化合物。方法：以建立的DPP-Ⅳ抑制剂筛选体系，分别将清肺排毒汤汤剂的喷干粉水溶液、中药颗粒水溶液、中药单体化合物与DPP-Ⅳ特异性探针GP-BAN在37 ℃条件下共同孵育，通过测定探针底物代谢产物BAN的荧光值来判断上述物质对DPP-Ⅳ的抑制程度。结果：清肺排毒汤具有较弱的DPP-Ⅳ活性的抑制作用，而其组分中药水溶液浓度为1 000 μg/mL时，麻黄、枳实、广藿香颗粒水溶液对DPP-Ⅳ的活性明显的抑制作用，酶残余活性分别为40.00%、61.05%、62.04%。橙皮素、芦丁、芹菜素、槲皮素、山柰酚、去甲基麻黄碱、川陈皮素对DPP-Ⅳ有一定的抑制作用，其中最强的3种单体成分槲皮素、山柰酚及芹菜素对DPP-Ⅳ的IC50值分别为(75.39±6.17）μmol/L、(9.16±0.69）μmol/L和(7.91±1.09）μmol/L。结论：清肺排毒汤对DPP-Ⅳ的有一定的抑制作用，存在抑制DPP-Ⅳ的成分群和单体化合物，这些发现为“清肺排毒汤”对感染新型冠状病毒肺炎（COVID-19）患者，尤其是COVID-19合并T2DM的患者的治疗提供了参考。 |
| English Summary: |
| With the self-developed two-photon fluorescent probe glycyl-prolyl-N-butyl-4-amino-1,8-naphthalimide(GP-BAN) for dipeptidyl peptidase-Ⅳ(DPP-Ⅳ) detection with high specificity and sensitivity as the substrate and human plasma as the source of DPP-Ⅳ，this study aims to evaluate the inhibitory effect of Qingfei Paidu Decoction and the medicinals in the prescription on DPP-Ⅳ，and to further explore the effective compounds in the medicinals.Methods:With the established DPP-Ⅳ inhibitor screening system，the solution of Qingfei Paidu Decoction powder，the aqueous solution of the Chinese medicinal granules，and the effective compounds in the medicinals were respectively incubated with GP-BAN at 37 ℃.The inhibition on DPP-Ⅳ was evaluated based on the fluorescence value of the probe metabolite BAN.Results:Qingfei Paidu Decoction showed mild inhibitory effect on DPP-Ⅳ.The aqueous solution of Herba Ephedrae，Fructus Aurantii Immaturus，and Herba Pogostemonis granules at 1 000 μg/mL had obvious inhibitory effect on DPP-Ⅳ，and the residual activity of the enzyme was 40.00%，61.05%，and 62.04%，separately.Hesperetin，rutin，apigenin，quercetin，kaempferol，norephedrine，and nobiletin significantly suppressed DPP-Ⅳ，particularly quercetin，kaempferol，and apigenin whose half maximal inhibitory concentration(IC50) on DPP-Ⅳ was(75.39±6.17) μmol/L,(9.16±0.69) μmol/L，and(8.29±0.93) μmol/L，respectively.Conclusion:Qingfei Paidu Decoction inhibits DPP-Ⅳ，and the medicinals in the prescription and the compounds in the medicinals also show inhibitory effect on DPP-Ⅳ.These findings can serve as a reference for the treatment of coronavirus disease 2019(COVID-19) with Qingfei Paidu Decoction，especially COVID-19 complicated with type 2 diabetes mellitus(T2DM). |
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