---

The multi-targets integrated fingerprinting for screening anti-diabetic compounds from a Chinese medicine Jinqi Jiangtang Tablet

作者 Chang, Yan-xu; Ge, Ai-hua; Donnapee, Sineeporn; Li, Jin; Bai, Yang; Liu, Jiao; He, Jun; Yang, Xi; Song, Li-jiao; Zhang, Bo-li; Gao, Xiu-mei

期刊 JOURNAL OF ETHNOPHARMACOLOGY , APR 22 2015,:164

DOI 10.1016/j.jep.2015.02.018 PubMed 25698248

摘要 Ethnopharmacological relevance: Jinqi Jiangtang Tablet is a traditional Chinese anti-diabetic formula containing three ingredients: Coptis chinensis Franch. (dried rhizome of C. chinensis Franch., Coptis deltoidea C. Y. Cheng et Hsiao and Coptis teeta Wall.), Astragalus membranaceus (Fisch.) Bunge. (dried root of A. membranaceus (Fisch.) Bge. var. mongholicus (Bge.) Hsiao and A. membranaceus (Fisch.) Bge.) and Lonicera japonica Thunb. (dried alabastrum or with nascent flowers of L. japonica Thunb.). Free radicals, a-glucosidase, alpha-amylase, aldose reductase and lipase are different targets related with diabetes. However, there are no chromatographic methods employed in screening the anti-diabetic compounds from natural products basing on these targets simultaneously. The present study was aimed at the establishment of a multi-targets integrated fingerprinting to clarify the possible mechanism of the action of Traditional Chinese Medicines which simultaneously contained multiple chemical characteristics and effects of constitutions.Materials and methods: The multi-targets integrated fingerprinting was developed and validated to screen antidiabetic compounds from natural products by using ultra-high-performance liquid chromatography/quadruple-time-of-flight mass spectrometry, fraction collector and microplate reader. Ultra performance liquid chromatography was employed to separate the components in Jingi Jiangtang Tablet, which were identified by quadruple-time-of-flight mass spectrometry to acquire their structural information and collected by the fraction collector. Finally the active fractions were tested for scavenging 1, 1-dipheny1-2-picrylhydrazyl radical and inhibition of alpha-glucosidase, alpha-amylase, aldose reductase, and lipase activities in vitro by microplate reader.Results: Our tests revealed that the Jinqi Jiangtang Tablet showed inhibitory activity against a-glucosidase, a-amylase, aldose reductase and lipase with IC50 values of 0.80 +/- 0.02 mg/mL, 1.28 +/- 0.13 mg/mL, 0.80 +/- 0.02 mg/mL, 1.90 +/- 0.18 mg/mL respectively and the scavenging activity with IC50 value of 1.71 +/- 0.178 mg/mL The bioactive fractions were identified to be alkaloids, flavonoids and phenolic acids. The phenolic acids possessed antioxidant activities, namely the scavenging effect on 1, 1-diphenyl-2-piaylhydrazyl rull;). The alkaloids exhibited inhibitory activity against a-glucosidase, aldose reductase, alpha-amylase, and lipase. The flavonoids also showed mild inhibition on alpha-glucosidase, aldose reductase, alpha-amylase and lipase.Conclusions: The results demonstrate that Jinqi Jiangtang Tablet can scavenge free radicals and inhibit alpha-glucosidase, aldose reductase, alpha-amylase and lipase, which may be the possible mechanism of action of Jinqi/Jiangtang Tablet for the treatment of diabetes and associated complications. Compared with conventional chromatographic separation and activity assays, the multi-targets integrated fingerprinting, which simultaneously contains the chemical characteristics and multiple effects of constitutions could comprehensively and properly reveal the activity of Jinqi/Jiangtang Tablet. The results also show that the multi-targets integrated fingerprinting is a novel and powerful tool for screening and identifying active ingredients from Traditional Chinese Medicines. (C) 2015 Elsevier Ireland Ltd. All rights reserved.

涉及物种 黄连 Coptis chinensis 三角叶黄连 Coptis deltoidea 云南黄连 Coptis teeta 忍冬 Lonicera japonica 黄芪 Astragalus membranaceus