Search Results (7)

Flos sophorae immaturus (FSI) is considered to be a natural hypoglycemic product with the potential for a-glucosidase inhibitory activity. In this work, the polyphenols with α-glucosidase inhibition in FSI were identified, and then their potential mechanisms were investigated by omission assay, interaction, type of inhibition, fluorescence spectroscopy, circular dichroism, isothermal titration calorimetry and molecular docking analysis. The results showed that five polyphenols, namely rutin, quercetin, hyperoside, quercitrin and kaempferol, were identified as a-glucosidase inhibitors with IC₅₀ values of 57, 0.21, 12.77, 25.37 and 0.55 mg/mL, respectively. Quercetin plays a considerable a-glucosidase inhibition role in FSI. Furthermore, the combination of quercetin with kaempferol generated a subadditive effect, and the combination of quercetin with rutin, hyperoside and quercitrin exhibited an interference effect. The results of inhibition kinetics, fluorescence spectroscopy, isothermal titration calorimetry and molecular docking analysis showed that the five polyphenols were mixed inhibitors and significantly burst the fluorescence intensity of α-glucosidase. Moreover, the isothermal titration calorimetry and molecular docking analysis showed that the binding to α-glucosidase was a spontaneous heat-trapping process, with hydrophobic interactions and hydrogen bonding being the key drivers. In general, rutin, quercetin, hyperoside, quercitrin and kaempferol in FSI are potential α-glucosidase inhibitors. Full article

Flos Sophorae Immaturus (FSI) contains a large number of bioactive substances with antioxidant and hypoglycaemic activity. However, a feasible drying process plays an important role in the retention of its biological activity. The present work investigated the effects of ultrasound-assisted vacuum drying (UAVD) on FSI samples in terms of drying time, colour, microstructure, and total flavonoid content (TFC). Meanwhile, the antioxidant activity and α-glucosidase inhibition activity were also evaluated. The results show that the drying time of UVAD samples was decreased by 40% compared to that of the single vacuum-dried (VD) samples (600 W for 10 min). The cellular porous structures of FSI tissue were formed by UAVD, which promoted the migration of water from the inside to the outside. Furthermore, samples treated by UAVD exhibited better antioxidant activities and α-glucosidase and α-amylase inhibition capacities, with DPPH (81.86%), ABTS (88.61%), FRAP (83.05%), α-glucosidase inhibition capacity (89%), α-amylase (85%), drying time (3 h), and total aberration (ΔE) (1.63) being the highest characteristic traits. In this condition, the highest levels of total flavonoid content (TFC), rutin, quercetin, kaempferol, isorhamnetin, and genistein were obtained with 266.94, 239.46, 35.56, 8.54, 10.37, and 5.64 mg/g DW, respectively. The results confirm that UAVD is a novel method that significantly reduced the VD time and promoted the release of the bioactive substances of FSI. Full article

Flos Sophorae Immaturus (FSI) serves as one of the Chinese medicinal herbs of homologous provenance, whose polysaccharides constitute part of the active compounds that exert their pharmacological properties. Single-factor and response surface methodology were employed to investigate optimal extraction conditions for the ultrasonic-microwave synergistic extraction (UMSE) of polysaccharides from FSI (PFSI), which were deproteinized by Sevage, papain, and trichloroacetic acid methods, and the antioxidant potential of PFSI by contrasting deproteinization methods based on free-radical scavenging capacity. The optimum conditions for UMSE extraction of PFSI were 500 W microwave power, 265.887 W ultrasonic power, 20.078 min extraction time, and 94.995:1 liquid-to-material ratio. Meanwhile, the sequence of the single factors on the yield of polysaccharides indicated that microwave power > extraction time > D liquid to material ratio > B ultrasonic power, and that the obtained average value of polysaccharide yield was 37.05%, which was analogous to the predicted value of 37.17%, indicating that the optimization method was reasonable. In vitro, the antioxidant assay demonstrated that PFSI, with or without deproteinization, had a definite capability to scavenge oxidative free radicals. This research provides a theoretical basis for the industrial production of PFSI as a natural antioxidant, and a scientific basis for its industrial development. Full article

Polysaccharides from Flos Sophorae Immaturus (FSI) are one of its pharmacological compounds that can perform effective activities. Aiming to extract the most effective polysaccharides against hepatocellular carcinoma (HCC), the polysaccharides were separated from FSI through ultrasonic microwave extraction, and the first comparison was carried out on the characterization of the structure and its cytotoxic properties on HCC SMMC 7721 cells of undeproteinized purified polysaccharides (PFSI-1) and papain-deproteinized polysaccharides (PFSI-2) from FSI. The findings indicated that PFSI-1 and PFSI-2 had characteristic absorption peaks of polysaccharides; PFSI-1 contained three monosaccharides and PFSI-2 contained ten; and SEM, AFM, and NMR were consistent with the verification of IR polysaccharide characteristics, suggesting probable additional latent activities. The pharmacotoxic effects of both PFSI-1 and PFSI-2 on SMMC 7721 cells (p < 0.05), attenuated the migration ability of SMMC 7721 cells (p < 0.05) and promoted apoptosis (p < 0.05), with an increase in G0/G1-phase cells and decrease in S-phase cells in the PFSI-1 as well as a decrease in G0/G1-phase cells, increase in S-phase cells, and decrease in apoptosis in the PFSI-2 (p < 0.05). The significant cytotoxic effect of PFSI-2 on SMMC 7721 cells (p < 0.05) and its protective effect on human hepatic L02 cells (HL-7702) at low concentrations (p > 0.05) could indicate its potential as a new drug for the treatment of HCC. Full article

Ultrasound-assisted extraction (UAE) was applied to extract rutin (RU), nicotiflorin (NI), narcissoside (NA), kaempferol (KA), isorhamnetin (IS), quercetin (QU), and total flavonoids of Flos Sophorae Immaturus (TFFSI) from Flos Sophorae Immaturus (FSI). Through single factor test and response surface methodology (RSM), the optimal extraction conditions were concluded as follows: ethanol concentration 70%, time 30 min, temperature 61 °C, and liquid/solid ratio 15.30 mL/g, respectively. The actual extraction rates of RU, NI, NA, KA, IS, QU, and TFFSI were 14.6101%, 2.9310%, 7.1987%, 0.1041%, 0.4920%, 2.7998%, and 26.4260%, respectively. The experimental results demonstrated that the extraction method with accuracy and efficiency could be used for the comprehensive evaluation quality control of extracts from FSI. The antioxidant activities of hydroalcoholic extraction from FSI on 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•⁺), superoxide anion (•O²⁻) free radicals, and ferric reducing/antioxidant power (FRAP) were assessed. The results showed that the antioxidation activities of extracts on DPPH, ABTS•⁺, and •O²⁻ free radicals were reached 89.29%, 97.86%, and 56.61%, and 81.4% in FRAP at 1.0 mg/mL, respectively. The antioxidant capacity of FSI extract was positively correlated with the amount of total flavonoids. Full article

An efficient microwave-assisted extraction (MAE) combined with in-capillary [Fe(ferrozine)3]2+-capillary electrophoresis-Diode Array Detector (in-capillary [Fe(ferrozine)3]2+-CE-DAD) was developed to screen active components with the ability to chelate ferrous ions and determine the total antioxidant activity. The MAE conditions, including methanol concentration, extraction power, extraction time, and the ratio of material to liquid, were optimized by an L₉(3⁴) orthogonal experiment. Background buffer, voltage, and cartridge temperature that affect the separation of six compounds were optimized. It was found that rutin and quercetin were the main components chelating ferrous ions in Flos Sophorae Immaturus (Flos Sophorae) by the in-capillary [Fe(ferrozine)₃]²⁺-CE-DAD. The recoveries were ranged from 95.2% to 104%. It was concluded that the MAE combined with in-capillary [Fe(ferrozine)₃]²⁺-CE-DAD method was a simple, reliable, and efficient tool for screening active components from the complex traditional Chinese medicine samples and evaluating their ability to chelate ferrous ions. Full article

Microwave-assisted extraction was applied to extract rutin; quercetin; genistein; kaempferol; and isorhamnetin from Flos Sophorae Immaturus. Six independent variables; namely; solvent type; particle size; extraction frequency; liquid-to-solid ratio; microwave power; and extraction time were examined. Response surface methodology using a central composite design was employed to optimize experimental conditions (liquid-to-solid ratio; microwave power; and extraction time) based on the results of single factor tests to extract the five major components in Flos Sophorae Immaturus. Experimental data were fitted to a second-order polynomial equation using multiple regression analysis. Data were also analyzed using appropriate statistical methods. Optimal extraction conditions were as follows: extraction solvent; 100% methanol; particle size; 100 mesh; extraction frequency; 1; liquid-to-solid ratio; 50:1; microwave power; 287 W; and extraction time; 80 s. A rapid and sensitive ultra-high performance liquid chromatography method coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (EIS-Q-TOF MS/MS) was developed and validated for the simultaneous determination of rutin; quercetin; genistein; kaempferol; and isorhamnetin in Flos Sophorae Immaturus. Chromatographic separation was accomplished on a Kinetex C₁₈ column (100 mm × 2.1 mm; 2.6 μm) at 40 °C within 5 min. The mobile phase consisted of 0.1% aqueous formic acid and acetonitrile (71:29; v/v). Isocratic elution was carried out at a flow rate of 0.35 mL/min. The constituents of Flos Sophorae Immaturus were simultaneously identified by EIS-Q-TOF MS/MS in multiple reaction monitoring mode. During quantitative analysis; all of the calibration curves showed good linear relationships (R² > 0.999) within the tested ranges; and mean recoveries ranged from 96.0216% to 101.0601%. The precision determined through intra- and inter-day studies showed an RSD% of <2.833%. These results demonstrate that the developed method is accurate and effective and could be readily utilized for the comprehensive quality control of Flos Sophorae Immaturus. Full article