To investigate the composition and hypoglycemic activity of polyphenols in Gastrodia elata, this study utilized ultra-high performance liquid chromatography coupled with quadrupole and electrostatic field Orbitrap high-resolution mass spectrometry (UPLC-Q-Exactive Orbitrap-MS) to identify the components of the purified polyphenols. In vitro experiments were conducted to evaluate the inhibitory effects of G. elata polyphenols on α-amylase and α-glucosidase activities and to explore the mechanism underlying their hypoglycemic effects. The results indicated that G. elata polyphenols contained 30 compounds, including 23 flavonoids, 2 phenolic acids, and 5 phenolic compounds. In vitro hypoglycemic experiments showed that G. elata polyphenols exhibited significantly inhibitory effects on both α-amylase and α-glucosidase, which were positively correlated with polyphenol concentration. At a concentration of 0.5 mg/mL, the inhibitory rates of G. elata polyphenols on α-amylase and α-glucosidase were (79.71 ± 2.51) % and (77.33 ± 2.31) %, respectively. The half-maximal inhibitory concentrations (IC₅₀) were (0.057 ± 0.011) and (0.189 ± 0.017) mg/mL, respectively. The types of inhibition were determined to be mixed uncompetitive-noncompetitive inhibition for α-amylase and mixed competitive-noncompetitive inhibition for α-glucosidase. These findings could provide a theoretical foundation for further research into the hypoglycemic mechanisms of G. elata polyphenols and for their development and utilization.

This study was carried out in order to explore the anti-inflammatory constituents of the tuber of Gastrodia elata B1 and their mechanisms of action. The petroleum ether extract and its sequential fractions: dichloromethane, ethyl acetate, n-butanol and water-soluble fractions were determined for their active ingredients as well as assessed for their bioactivities. The bioactive ingredients were identified by ultra-high performance liquid chromatography-quadrupole-time of flight-mass spectrometry (UPLC-Q-TOF-MS/MS), and network pharmacology was utilized to predict the potential anti-inflammatory components of the selected fraction and their targets. Furthermore, molecular docking was used to investigate the binding of the potential anti-inflammatory components to the core targets for treating inflammation. The results showed that the ethyl acetate fraction possessed the highest content of bioactive ingredients, with total polyphenol, total flavonoid and polysaccharide contents of (164.69 ± 1.57), (64.81 ± 3.21) and (279.64 ± 3.11) mg/g, respectively. The ethanol extract and its fractions possessed strong in vitro antioxidant and anti-inflammatory activities, among which the ethyl acetate fraction demonstrated the strongest 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging capacity and in vitro anti-inflammatory activity. Correlation analysis showed that the total polyphenol content was significantly (P < 0.05) and highly significantly (P < 0.01) correlated with the half maximal inhibitory concentration (IC₅₀) against DPPH radical and 2,2’-biazobis(3-ethylbenzothiazoline-6-sulfonic acid) cationic radical, with correlation coefficients of −0.587 and −0.873, respectively. The total flavonoid content was significantly (P < 0.05) and highly significantly (P < 0.01) correlated with the IC₅₀ values against NO and the denaturation of bovine serum albumin (BSA), with correlation coefficients of -0.780 and -0.842, respectively. Meanwhile, a total of 164 chemical constituents were identified from the ethyl acetate fraction, and core active ingredients including 5-(5-methoxycarbonyl-5,8a-dimethyl-2-methylidene-3,4,4a,6,7,8-hexahydro-1H-naphthalen-1-yl)-3-methylpentanoic acid, 4,4,8,10,14-pentamethyl-17-(4,5,6-trihydroxy-6-methylheptan-2-yl)-2,5,6,7,9,15-hexahydro-1Hcyclopenta[a]phenanthrene-3,16-dione, and simvastatin and key targets including TP53, SRC, PIK3R1, PIK3CA, and AKT1, which were mainly involved in cancer-related signaling pathways as well as the mitogen-activated protein kinase (MAPK) and cyclic adenosine monophosphate (cAMP) signaling pathways, were obtained by network pharmacology. The results of molecular docking showed that the core active ingredients had good binding activity with the key targets.