桑枝生物碱对糖脂代谢的作用

Effect of Sangzhi alkaloids on glucose and lipid metabolism

桑枝提取物是以桑树枝为原材料,经提取、分离、纯化得到的有效提取物,主要包含生物碱、黄酮、多糖和氨基酸等成分。其中,降糖有效部位即桑枝总生物碱(SZ-A)具有双糖酶抑制活性,由1-脱氧野尻霉素(1-DNJ)、荞麦碱(FAG)和1,4双脱氧-1,4-亚氨基-D-阿拉伯糖醇(DAB)组成,DNJ占70%,FAG和DAB各占15%。口服SZ-A后,DNJ、FAG和DAB分别在0.67、1.30和0.67 h内达到最大血浆浓度。SZ-A对小肠糖苷酶有高选择性的抑制作用,单药使用有效降低HbA1c 1.0%,在用药早期即可降低1 hPG,胃肠道副作用比阿卡波糖减少50%。此外SZ-A还具有调节糖脂代谢和肠道菌群、保护胰岛β细胞、改善葡萄糖刺激的胰岛素分泌功能、刺激GLP-1分泌等作用,适用于T2DM餐后高血糖患者,特别是T2DM新诊断患者、有社交需求的患者、伴脂代谢异常患者、偏好天然药物的患者、使用糖苷酶抑制剂胃肠副作用明显的患者。今后期待更多的临床试验,以进一步验证其有效性、与其他药物的相互作用、药物不良反应、降糖以外的疗效等,为临床应用提供更多的循证证据。

Mulberry branch extract is extracted from the waste“mulberry branch”of mulberry management in the industry of mulberry planting and silkworm rearing.This effective extract obtained by extraction,separation,and purification,mainly includes alkaloids,flavonoids,polysaccharides,and amino acids.Among them,Sangzhi alkaloids(SZ-A),which is considered as the effective part of the hypoglycemic activity,has disaccharidase inhibitory activity.SZ-A consisted of 1-deoxynojirimycin(1-DNJ),soba(FAG)and 1-4 dideoxy 1-4-Imino-D-Arabinitol(DAB).In SZ-A,DNJ accounts for 70%,FAG and DAB account for 15%each.The maximum plasma concentrations(Cmax)of DNJ,FAG and DAB reached within 0.67,1.30,and 0.67 h after oral intake of SZ-A.Sz-a has a highly selective inhibitory effect on small intestinal glycosidase,and the single administration of SZ-A effectively reduced HbA1 c by 1.0%.In the early administration,SZ-A reduced 1 hPG and reduced gastrointestinal side effects by 50%than acarbose.In addition,SZ-A also has the functions of regulating glucose and lipid metabolism and intestinal flora,protecting pancreaticβcells,improving insulin secretion function stimulated by glucose,and stimulating GLP-1 secretion.SZ-a is suitable for typ 2 diabetes mellitus(T2 DM)patients with postprandial hyperglycemia,especially newly diagnosed T2 DM patients,patients with social needs,patients with abnormal lipid metabolism,patients who prefer natural drugs,and patients with obvious gastrointestinal side effects from the use of glucoside-enzyme inhibitors.In the future,more clinical trials are expected to further verify its effectiveness,interactions with other drugs,side effects,and other efficacy other than hypoglycemic effects,to provide more evidence-based evidence for clinical application.