Chen Zhiyong, Du Xia, Yang Yuanyuan, Cui Xiaomin, Zhang Zijia, Li Ye
Shaanxi Academy of Traditional Chinese Medicine, Xi'an, Shaanxi, China.
The MOE Key Laboratory for Standardization of Chinese Medicines and The Shanghai Key Laboratory for Compound Chinese medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Biomed Chromatogr. 2018 Nov;32(11):e4328. doi: 10.1002/bmc.4328. Epub 2018 Aug 21.
Morus alba L has long been used as fodder and as a traditional medicine. The different parts of M. alba (Cortex Mori, Ramulus Mori, Folium Mori and Fructus Mori) have different bioactivities; however, most current evidence is focused on anti-diabetic properties. In spite of their widespread use, few studies have compared the chemical composition and activity against α-glucosidase of the various medicinal parts of M. alba. In this study, we developed an HPLC method for simultaneous quality control and discrimination of Cortex Mori, Ramulus Mori, Folium Mori and Fructus Mori using 13 marker compounds. We found that quercetin, morin, kuwanon G, sanggenon C, morusin, mulberroside A and rutin were chemically distinct among the various medicinal parts of M. alba. A spectrum-effect relationship method was established to compare α-glucosidase inhibitory activity of various batches of samples to determine the activity of the primary active components against α-glucosidase. Taken together with molecular docking data, we found that prenylated flavonoids (morin, sanggenon C, kuwanon G and morusin), flavonols (kaempferol, quercetin, rutin and isoquercitrin) and alkaloids (1-deoxynojirimycin) were small molecule α-glucosidase inhibitory ingredients. In conclusion, we laid a solid foundation for effective substance identification in various parts of M. alba, and simultaneously provided a basis for their quality control.
桑白皮长期以来一直被用作饲料和传统药物。桑白皮的不同部位（桑白皮、桑枝、桑叶和桑椹）具有不同的生物活性；然而，目前大多数证据都集中在抗糖尿病特性上。尽管它们被广泛使用，但很少有研究比较桑白皮不同药用部位的化学成分及其对α-葡萄糖苷酶的活性。在本研究中，我们开发了一种高效液相色谱法，用于使用13种标记化合物同时对桑白皮、桑枝、桑叶和桑椹进行质量控制和鉴别。我们发现槲皮素、桑色素、kuwanon G、桑根酮C、桑辛素、桑皮苷A和芦丁在桑白皮的不同药用部位中化学性质不同。建立了一种谱效关系方法，比较不同批次样品的α-葡萄糖苷酶抑制活性，以确定主要活性成分对α-葡萄糖苷酶的活性。结合分子对接数据，我们发现异戊烯基黄酮（桑色素、桑根酮C、kuwanon G和桑辛素）、黄酮醇（山柰酚、槲皮素、芦丁和异槲皮苷）和生物碱（1-脱氧野尻霉素）是小分子α-葡萄糖苷酶抑制成分。总之，我们为桑白皮不同部位有效成分的鉴定奠定了坚实基础，同时为其质量控制提供了依据。
