State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, PR China.
College of Pharmacy, Henan University of Chinese Medicine, Zhengzhou, P. R. China.
J Sep Sci. 2022 Jul;45(14):2591-2602. doi: 10.1002/jssc.202200221. Epub 2022 May 31.
In this work, the hypoglycemic components in Platycladi Cacumen, an essential traditional Chinese medicine, were evaluated by combining phytochemical investigation, spectrum-effect relationship analysis, and chemometric methods. The phytochemical studies on Platycladi Cacumen extract lead to the isolation of 21 potential bioactive compounds. The chromatographic fingerprints of Platycladi Cacumen samples were established by high-performance liquid chromatography. The hypoglycemic effects of Platycladi Cacumen samples were further evaluated by inhibition of α-glucosidase and detected by the high-performance liquid chromatography method. The spectrum-effect relationship study by bivariate correlations analysis and orthogonal partial least squares regression revealed that myricitrin (P9), quercitrin (P13), afzelin (P18), and amentoflavone (P24) were more relevant to the α-glucosidase inhibitory activity. The results of α-glucosidase inhibitory activity of 21 isolated compounds and molecular docking studies also indicated these flavonoids had potent α-glucosidase inhibitory activity. Collectively, the present study established the spectrum-effect relationship mode of Platycladi Cacumen and discovered the major hypoglycemic components, which provides a feasible method for screening bioactive components.
在这项工作中，我们通过结合植物化学研究、谱效关系分析和化学计量学方法，评估了柏科植物柏子仁中的降血糖成分。对柏科植物提取物的植物化学研究导致分离出 21 种潜在的生物活性化合物。通过高效液相色谱法建立了柏科植物样品的色谱指纹图谱。通过高效液相色谱法检测α-葡萄糖苷酶抑制作用进一步评价柏科植物样品的降血糖作用。通过二元相关分析和正交偏最小二乘回归的谱效关系研究表明，杨梅素（P9）、槲皮素（P13）、圣草酚（P18）和芹菜素（P24）与α-葡萄糖苷酶抑制活性的相关性更强。21 种分离化合物的α-葡萄糖苷酶抑制活性和分子对接研究的结果也表明，这些类黄酮具有很强的α-葡萄糖苷酶抑制活性。综上所述，本研究建立了柏科植物的谱效关系模式，并发现了主要的降血糖成分，为筛选生物活性成分提供了一种可行的方法。
