Han Si-Wen, Shi Sheng-Ming, Zou Yu-Xiao, Wang Zhi-Cheng, Wang Yan-Qun, Shi Lin, Yan Ting-Cai
College of Food Science, Shenyang Agricultural University, Shenyang 110866, China.
Tianjin Press of Chinese Herbal Medicines, Tianjin Institute of Pharmaceutical Research, Tianjin 300462, China.
Chin Herb Med. 2020 Mar 14;12(2):195-199. doi: 10.1016/j.chmed.2020.03.003. eCollection 2020 Apr.
To investigate the hypoglycemic components from the acid hydrolyzates of total saponins, and screen the active compounds by inhibitory activities to α-glycosidase enzymes and protein tyrosine phosphatase-1B (PTP1B).
The hydrolyzates were chromatographed repeatedly over silica gel column, and the structures of the compounds were determined by means of NMR. The bioassay was performed through the inhibitory effects on α-glucosidase or/and PTP1B.
Eight compounds were isolated, which identified as 20()-panaxadiol (), (20,24)-dammarane-20,24-epoxy-3β,6α,12β,25-tetraol (), 20()-dammarane-3β,12β,20,25-tetraol (), 20()-dammarane-3β,6α,12β,20,25-pentol (), 20()-dammarane-3β,12β,20,25-tetrahydroxy-3β--β--glucopyranoside (), β-sitosterol (), oleanolic acid () and 20()-protopanaxadiol (). Compound was ginseng triterpenoid isolated from the acid hydrolysates of total saponins from for the first time. In this paper, the possible inhibitory activities were investigated. Compound exhibited significantly inhibitory activity against α-glucosidase, and the IC value [(0.22 ± 0.21) µmol/L] was about 43-fold lower than positive control. For the PTP1B inhibition assay, compound indicated the strongest inhibitory effect with IC of (5.91 ± 0.38) µmol/L, followed by compound with IC of (6.21 ± 0.21) µmol/L, which were all showed competitive inhibitory pattern by using a Lineweaver-Burk plot.
These results supported the potential application of dammaranes from acid hydrolyzates of total saponins can be used as ingredients of ancillary anti-diabetic agent or functional factor.
研究总皂苷酸水解产物中的降血糖成分，并通过对α-糖苷酶和蛋白酪氨酸磷酸酶-1B（PTP1B）的抑制活性筛选活性化合物。
水解产物在硅胶柱上反复进行柱色谱分离，通过核磁共振确定化合物结构。通过对α-葡萄糖苷酶或/和PTP1B的抑制作用进行生物活性测定。
分离得到8个化合物，分别鉴定为20（S）-人参二醇、（20S，24R）-达玛烷-20，24-环氧-3β，6α，12β，25-四醇、20（S）-达玛烷-3β，12β，20，25-四醇、20（S）-达玛烷-3β，6α，12β，20，25-五醇、20（S）-达玛烷-3β，12β，20，25-四羟基-3β-O-β-D-吡喃葡萄糖苷、β-谷甾醇、齐墩果酸和20（S）-原人参二醇。化合物是首次从人参总皂苷酸水解产物中分离得到的人参三萜类化合物。本文研究了其可能的抑制活性。化合物对α-葡萄糖苷酶表现出显著的抑制活性，IC50值[（0.22±0.21）μmol/L]比阳性对照低约43倍。在PTP1B抑制试验中，化合物表现出最强的抑制作用，IC50为（5.91±0.38）μmol/L，其次是化合物，IC50为（6.21±0.21）μmol/L，通过Lineweaver-Burk图均显示为竞争性抑制模式。
这些结果支持了人参总皂苷酸水解产物中的达玛烷类化合物可作为辅助抗糖尿病药物成分或功能因子的潜在应用。
