Changchun Center of Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, P. R., China.
Phytochem Anal. 2012 Jul-Aug;23(4):315-23. doi: 10.1002/pca.1360. Epub 2011 Sep 26.
Acanthopanax senticosus Harms is a typical Chinese herb with flavonoids existing in all parts of the plant but with the largest content in leaves. However, leaves have been neglected in past research. To investigate the potential use of leaves of A. senticosus Harms for discovering lead compounds to treat type 2 diabetes, the herb leaves were selected for screening the potential of α-glucosidase inhibitors.
To screen for candidates of α-glucosidase inhibitors from leaves of A. senticosus Harms and evaluate the structure-activity relationship of the α-glucosidase inhibitors.
Ultrafiltration liquid chromatography/mass spectrometry (UF-LC/MS) assay was developed for screening candidates of α-glucosidase inhibitors from leaves of A. senticosus Harms. The interesting compounds were identified by using reversed-phase high performance liquid chromatography with diode array detector and electrospray ionisation multiple-stage tandem mass spectrometry (RP-HPLC-DAD-ESI-MS(n) ), and confirmed by using electrospray ionisation Fourier transform ion cyclotron resonance multiple-stage tandem mass spectrometry (ESI-FT-ICR-MS(n)). Furthermore, the α-glucosidase inhibitory activity of the compounds detected was estimated using in vitro assays.
Eight compounds that might bind to α-glucosidase were screened and seven of them were identified successfully. The α-glucosidase inhibitory activity of the related compounds in leaves of A. senticosus Harms was determined.
The results obtained provided new information for the discovery of potential α-glucosidase inhibitors and the potential anti-diabetic application of the leaves of A. senticosus Harms.
刺五加是一种典型的中国草药,其黄酮类化合物存在于植物的各个部位,但在叶片中的含量最大。然而,在过去的研究中,叶片一直被忽视。为了研究刺五加叶片作为发现治疗 2 型糖尿病的潜在先导化合物的用途,选择该草药叶片进行筛选潜在的α-葡萄糖苷酶抑制剂。
从刺五加叶片中筛选α-葡萄糖苷酶抑制剂候选物,并评价α-葡萄糖苷酶抑制剂的构效关系。
建立超滤液相色谱/质谱(UF-LC/MS)测定法,从刺五加叶片中筛选α-葡萄糖苷酶抑制剂候选物。采用反相高效液相色谱-二极管阵列检测器-电喷雾离子化多级串联质谱(RP-HPLC-DAD-ESI-MS(n))鉴定有意义的化合物,并采用电喷雾离子化傅里叶变换离子回旋共振多级串联质谱(ESI-FT-ICR-MS(n))进行确证。此外,还采用体外试验测定了所检测化合物的α-葡萄糖苷酶抑制活性。
筛选出 8 种可能与α-葡萄糖苷酶结合的化合物,其中 7 种成功鉴定。测定了刺五加叶片中相关化合物对α-葡萄糖苷酶的抑制活性。
研究结果为发现潜在的α-葡萄糖苷酶抑制剂和刺五加叶片的潜在抗糖尿病应用提供了新的信息。