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This study aimed to optimize subcritical water extraction process, characterize chemical composition and investigate the biological activities of Nitraria sibirica Pall. (NSP) anthocyanin. Overall, the optimization was achieved under following conditions: extraction temperature 140 °C, extraction time 45 min and flow rate 7 mL/min with the extraction yield of 1.075 mg/g. 3 cyanidin, 3 petunidin, 1 delphinidin and 1 pelargonidin compounds were identified in the anthocyanic extract from NSP via UPLC–Triple–TOF–MS/MS. NSP anthocyanin exhibited better DPPH free-radical scavenging activity than ascorbic acid. It displayed superior α-glucosidase inhibition activity, which was ∼14 times higher than that of acarbose. Moreover, enzyme kinetics results indicated that NSP anthocyanin behaved as a reversible, mixed-type inhibitor. Molecular docking and molecular dynamics simulation results revealed that NSP anthocyanin interacted with α-glucosidase mainly via van der Waals forces, hydrogen bond and possessed fairly stable configuration. Therefore, NSP anthocyanin is a promising α-glucosidase inhibitor for diabetes mellitus.

Objective: The purpose of this study was to compare the activity difference of polyphenols in banana pulp of different varieties and to provide scientific basis for the exploitation and utilization of banana pulp polyphenols. Methods: Five banana pulp polyphenols were extracted by ultrasonic extraction, and the phenolic components were analyzed by ultra-high performance liquid chromatography （UHPLC）. The antioxidant capacity and inhibition ability of α-glucosidase were determined. Results: The total polyphenols, flavonoids and tannins content were significant differences among five varieties （P＜0.05）. Eight phenolic compounds were identified in five banana pulps, including four phenolic acids and their derivatives, and four flavonoid compounds. The five kinds of banana pulp polyphenols had certain antioxidant activities of scavenging DPPH, ABTS free radical, and reducing iron ion. All the five kinds of banana pulp polyphenols could inhibit α-glucosidase. The major bioactive components in banana pulp, catechin acid and rutin, were signiflcantly positively correlated with the ability of α-glucosidase inhibition （P＜0.05）. The antioxidative ability and inhibitory activity of α-glucosidase were the strongest in the pulp polyphenols of Nanjiao No.42 banana. The enzyme activity was inhibited by mixed inhibition, and the interaction with α-glucosidase was exothermic. Conclusion: Banana pulp polyphenols have good antioxidant ability and inhibition ability to α-glucosidase activity, and are expected to be a good selective inhibitor of α-glucosidase.

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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. [ABSTRACT FROM AUTHOR]

Plant-derived phytochemicals have recently drawn interest in the prevention and treatment of diabetes mellitus (DM). The seeds of Moringa oleifera Lam. are widely used in food and herbal medicine for their health-promoting properties against various diseases, including DM, but many of their effective constituents are still unknown. In this study, 6 new phenolic glycosides, moringaside B–G (1–6), together with 10 known phenolic glycosides (7–16) were isolated from M. oleifera seeds. The structures were elucidated by 1D and 2D NMR spectroscopy and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) data analysis. The absolute configurations of compounds 2 and 3 were determined by electronic circular dichroism (ECD) calculations. Compounds 2 and 3 especially are combined with a 1,3-dioxocyclopentane moiety at the rhamnose group, which are rarely reported in phenolic glycoside backbones. A biosynthetic pathway of 2 and 3 was assumed. Moreover, all the isolated compounds were evaluated for their inhibitory activities against α-glucosidase. Compounds 4 and 16 exhibited marked activities with IC50 values of 382.8 ± 1.42 and 301.4 ± 6.22 μM, and the acarbose was the positive control with an IC50 value of 324.1 ± 4.99 μM. Compound 16 revealed better activity than acarbose.

In our current investigation, 37 constituents (1–37), including 11 megastigmanes (1–11), 17 flavonoids (12–28) and 9 phenylpropanoids (29–37), were isolated from a 70%-EtOH extract of Diaphragma juglandis Fructus. Among them, compounds 1–3, 12 and 29 were new compounds and their structures were elucidated on the basis of physicochemical evidence and meticulous spectroscopic analysis (NMR, HRESIMS and CD). Compounds 13, 16, 21 and 28 showed moderate inhibitory effect on α-glycosidase inhibitory activities, with IC50 values being in the range of 29.47–54.82 µM and stronger than the positive control (acarbose, 60.01 ± 4.82 µM). [ABSTRACT FROM AUTHOR]

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.

Salak (Salacca zalacca) is well-known as snake fruit and it is immensely studied for its antioxidative and antidiabetic active metabolites throughout the southeast Asian countries. However, there are many remaining unidentified metabolites due to very low abundance and natural variation, which need to be further explored. Nowadays mass spectrometry (MS/MS) facilitates the tentative identification of unknown compounds in the crude herbal extracts. This study described the metabolite profiling of hydroalcoholic extracts of S. zalacca analysed by LC-QTOF-MS/MS. The 60% ethanolic extract exhibited the highest α-glucosidase inhibition and ferric reducing antioxidant power activities with IC50 of 15.94 µg/mL and 78.13 μg AAE/g, respectively. Multivariate data analysis (MVDA) by an orthogonal partial least-squares (OPLS) algorithm was conducted to correlate the α-glucosidase inhibition activity with the LC- QTOF-MS data. A total of 4 compounds were reported for first time in this fruit and identified based on the molecular mass and fragment ions. LC-QTOF-MS analysis indicated the presence of carexane I, 5-phenoxytetrazol-1-yl)-2,3,5,6-hexahydrofurofuran-3-ethylurea, 3-acetylphenoxy)-N-[(2)-1-amino-4-methyl-1-oxopentan-2-yl]-4,5-dihydroxycyclohexene-1-carboxamide and Ethyl 4-[5-methyl-2-oxo-1′,2′,5′,6′,7′,7′a-hexahydro-1H-spiro[indole-3,3′-pyrrolizine]-2′-ylamido] benzoate. Molecular docking of those compounds with the α–glucosidase enzyme was performed to confirm their antidiabetic potential. These bioactive compounds could be suggested as α-glucosidase inhibitors and functional food additives.

A new triterpene glycoside, 3-O-[(α-L-rhamnopyranosyl)(1→2)]-[β-D-glucuronopyranosyl-6-O-methyl ester]-olean-12-ene-28-olic acid (1) and a new indole alkaloid, 5-methoxy-2-oxoindolin-3-acetic acid methyl ester (5) were isolated from the leaves of Acanthopanax senticosus Harms along with six known compounds. The structures of the new compounds were determined by means of 2D-NMR experiments and chemical methods. All the isolated compounds were evaluated for their glycosidase inhibition activities and compound 6 showed significant α-glucosidase inhibition activity.

Six new phragmalin limonoids, named moluccensin Z1 (1), moluccensin Z2 (2), carapanolide Y (3), tabulalin N (4), chukvelutilide A1 (5), and velutinasin J (6), as well as two known compounds, chukvelutilide A (7) and velutinasin D (8) were isolated from the stems of Chukrasia tabularis A. Juss. The structures of the new compounds 1⁻6 were confirmed by spectroscopic methods, including IR and HRESIMS, as well as 1D and 2D NMR, and by comparisons with the data of known analogues. All compounds were tested for α-glucosidase and acetylcholinesterase inhibitory activities. However, none of the compounds was active against α-glucosidase and acetylcholinesterase in vitro.

Phytochemical investigation on the stems of C. tabularis led to the isolation of five new phragmalin-type limonoids and six known ones. The structures of the new compounds 1-5, named chukbularisins A-E, were elucidated by spectroscopic techniques (IR, HRESIMS, 1D and 2D NMR) and comparisons with published data. All the compounds were evaluated for in vitro α-glucosidase inhibitory activity. Compounds 2, 3, 4, 5, and 8 exhibited inhibitory activity against α-glucosidase with IC50 values of 0.06 ± 0.008, 0.04 ± 0.002, 0.52 ± 0.039, 1.09 ± 0.040, and 0.20 ± 0.057 mM, respectively (using acarbose as positive control, IC50 0.95 ± 0.092 mM). [ABSTRACT FROM AUTHOR]

A new triterpene glycoside, 3-O-[(α-L-rhamnopyranosyl)(1→2)]-[β-Dglucuronopyranosyl- 6-O-methyl ester]-olean-12-ene-28-olic acid (1) and a new indole alkaloid, 5-methoxy-2-oxoindolin-3-acetic acid methyl ester (5) were isolated from the leaves of Acanthopanax senticosus Harms along with six known compounds. The structures of the new compounds were determined by means of 2D-NMR experiments and chemical methods. All the isolated compounds were evaluated for their glycosidase inhibition activities and compound 6 showed significant α-glucosidase inhibition activity. [ABSTRACT FROM AUTHOR]

Salak (Salacca zalacca) is well-known as snake fruit and it is immensely studied for its antioxidative and antidiabetic active metabolites throughout the southeast Asian countries. However, there are many remaining unidentified metabolites due to very low abundance and natural variation, which need to be further explored. Nowadays mass spectrometry (MS/MS) facilitates the tentative identification of unknown compounds in the crude herbal extracts. This study described the metabolite profiling of hydroalcoholic extracts of S. zalacca analysed by LC-QTOF-MS/MS. The 60% ethanolic extract exhibited the highest α-glucosidase inhibition and ferric reducing antioxidant power activities with IC 50 of 15.94 µg/mL and 78.13 μg AAE/g, respectively. Multivariate data analysis (MVDA) by an orthogonal partial least-squares (OPLS) algorithm was conducted to correlate the α-glucosidase inhibition activity with the LC- QTOF-MS data. A total of 4 compounds were reported for first time in this fruit and identified based on the molecular mass and fragment ions. LC-QTOF-MS analysis indicated the presence of carexane I, 5-phenoxytetrazol-1-yl)-2,3,5,6-hexahydrofurofuran-3-ethylurea, 3-acetylphenoxy)-N-[(2)-1-amino-4-methyl-1-oxopentan-2-yl]-4,5-dihydroxycyclohexene-1-carboxamide and Ethyl 4-[5-methyl-2-oxo-1′,2′,5′,6′,7′,7′a-hexahydro-1H-spiro[indole-3,3′-pyrrolizine]-2′-ylamido] benzoate. Molecular docking of those compounds with the α–glucosidase enzyme was performed to confirm their antidiabetic potential. These bioactive compounds could be suggested as α-glucosidase inhibitors and functional food additives. [ABSTRACT FROM AUTHOR]

• New pyrazole-triazolopyrimidines were designed, synthesized and well characterized. • The compound 4j confirmed by the SCXRD. • a-glucosidase inhibition activity evaluated and 4h , 4f and 4l identified as potent acitve compounds. • SAR studies and molecular docking studies were carried out for all the compounds. • 4h , 4f and 4l exhibited good binding interactions and drug-likeness properties, which could be promising hits for anti-diabetic The aim of the present study is to design and synthesis of new pyrazole-triazolopyrimidine hybrids as potent α-glucosidase inhibitors. The target compounds 4a-n were synthesized by one-pot multicomponent approach with good yields and were characterized by various spectroscopic techniques and finally by single crystal X-ray diffraction method (4j). All the newly-synthesized derivatives have been screened for their α-glucosidase enzyme inhibition activity and acarbose taken as a standard drug. Among all the tested compounds, 4h has displayed excellent α-glucosidase enzyme inhibition activity with IC 50 value 12.45 μM to the standard drug acarbose (IC 50 : 12.68 μM). Similarly, the compounds 4f and 4l have exhibited potent activity with IC 50 values 14.47 μM and 17.27 μM respectively. Structure-activity relationship (SAR) studies of all the title compounds were established. The mode of binding interactions between the α-glucosidase enzyme and the compounds were studied. The drug-likeness properties (Lipinski parameters and in silico ADME properties) have predicted for the target compounds. The α-glucosidase inhibition, molecular docking and drug-likeness properties of the compounds 4h , 4f and 4l were suggested that these are promising hits for anti-diabetic activity. [ABSTRACT FROM AUTHOR]

Six new phragmalin limonoids, named moluccensin Z1 (1), moluccensin Z2 (2), carapanolide Y (3), tabulalin N (4), chukvelutilide A1 (5), and velutinasin J (6), as well as two known compounds, chukvelutilide A (7) and velutinasin D (8) were isolated from the stems of Chukrasia tabularis A. Juss. The structures of the new compounds 1–6 were confirmed by spectroscopic methods, including IR and HRESIMS, as well as 1D and 2D NMR, and by comparisons with the data of known analogues. All compounds were tested for α-glucosidase and acetylcholinesterase inhibitory activities. However, none of the compounds was active against α-glucosidase and acetylcholinesterase in vitro. [ABSTRACT FROM AUTHOR]

The aim of this study was to compare the quality and physicochemical characteristics of blue-shelled eggs (BE) and conventional eggs (CE). Proximate composition, quality, pH value, shell color, collagen content, fatty acid composition, total cholesterol, α-glucosidase inhibition activity, and antioxidation activity were determined. The proximate composition, general qualities, and pH values of CE and BE showed no significant differences, except in moisture composition, weight, and shell thickness. Moisture content and weight of BE were significantly lower than those of CE. However, shell thickness and weight of BE were higher than those of CE ( p <0.05). Lightness of BE was significantly higher than that of CE (85.20 vs. 58.80), while redness ( a *) and yellowness ( b *) of BE were lower than those of CE ( a *: -4.75 vs. 14.20; b *: 10.45 vs. 30.63). The fatty acid [C18:1n7 (cis-vaccenic acid) and C18:3n6 (gamma-linolenic acid)] contents of BE were significantly higher than those of CE. The total cholesterol contents of BE and CE were similar. DPPH radical scavenging activity of BE was significantly higher than that of CE (40.78 vs. 35.35). Interestingly, α-glucosidase inhibition activity of whole egg and egg yolk in BE (19.27 and 36.06) was significantly higher than that of whole egg and egg yolk in CE (13.95 and 32.46). This result indicated that BE could potentially be used as a functional food material. Further studies are required to evaluate the specific compounds that affect functional activity.