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FOOD CHEMISTRY · 2017 · IF 4.529

Phenolic compounds of the Australian native herb Prostanthera rotundifolia and their biological activities

Kitty S.C. Tang,Izabela Konczak,Jian Zhao

The chemical identity and bioactivities of phenolic components of the Australian native herb Prostanthera rotundifolia were studied. Phenolic compounds were extracted with 80% (v/v) aqueous methanol and purified by liquid chromatography. The antioxidant capacity of the extract and its inhibiting activity against α-glucosidase, pancreatic lipase and hyaluronidase were determined. Phenolic compounds were identified by a combination of HPLC-PDA, LC-high resolution MS (LC-HRMS), LC-tandem MS (LC–MS/MS) and nuclear magnetic resonance (NMR) spectroscopy. Compared to spearmint, mint bush showed comparable antioxidant capacity, stronger inhibitory activity on pancreatic lipase and comparable and lower activity on α-glucosidase and hyaluronidase, respectively. Major compounds identified were verbascoside (48.8%), 4-methoxycinnamic acid (36.4%), p -coumaric acid glucose ester (9.2%) and 1- O -β- d -glucopyranosyl sinapate (5.6%), while caffeic acid, p -coumaric acid, hesperidin and naringenin were present in trace quantities. 4-Methoxycinnamic acid, p -coumaric acid glucose ester and 1- O -β- d -glucopyranosyl sinapate were identified for the first time in the genus of Prostanthera .

CAS / MDL: 480-41-1 67604-48-2
研究领域: 植物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD RESEARCH INTERNATIONAL · 2024 · IF 7

Identification of procyanidins as α-glucosidase inhibitors, pancreatic lipase inhibitors, and antioxidants from the bark of Cinnamomum cassia by multi-bioactivity-labeled molecular networking

Jun Dai,Zihan Liu,Lei Ma,Chunliu Yang,Ligai Bai,Dandan Han,Qi Song,Hongyuan Yan,Zhiqiang Wang

This study examined the suppressive effects of 16 selected plant-based foods on α-glucosidase and pancreatic lipase and their antioxidant properties. Among these, the bark of Cinnamomum cassia (Cinnamon, WLN-FM 15) showed the highest inhibitory activity against α-glucosidase and the highest antioxidant activity. Additionally, WLN-FM 15 showed promising results in the other tests. To further identify the bioactive constituents of WLN-FM 15, a multi-bioactivity-labeled molecular networking approach was used through a combination of GNPS-based molecular networking, DPPH-HPLC, and affinity-based ultrafiltration-HPLC. A total of nine procyanidins were identified as antioxidants and inhibitors of α-glucosidase and pancreatic lipase in WLN-FM 15. Subsequently, procyanidins A1, A2, B1, and C1 were isolated, and their efficacy was confirmed through functional assays. In summary, WLN-FM 15 has the potential to serve as a functional food ingredient with the procyanidins as its bioactive constituents. These results also suggest that the multi-bioactivity-labeled molecular networking approach is reliable for identifying bioactive constituents in plant-based foods.

研究领域: 植物化学 · 食品科学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Waste and Biomass Valorization · 2024 ·Vol. 15 ·期 7 ·4353-4372 · IF 2.6

Bioactive Potential of Baby Corn Silk: In-Vitro Evaluation of Antioxidant, Antimicrobial, Anti-diabetic, and Anti-gout Activities

Shankaranarayana Sahana Hosanagara,Gajanana Vijayalaxmi Karki,Chavan Mohan,Chavannavar Suvarna V.,Doddanagappa Shobha

Purpose To analyse phytochemical composition, antioxidant potential, antimicrobial activity and α-amylase, α-glucosidase and xanthine oxidase inhibitory potential of corn silk extracts derived from the Syngenta 5414 corn variety. Methods Corn silk sample was lyophilized and extracted using 80% ethanol, methanol, water or acetone. Phytochemicals were qualitatively screened and bioactive compounds were identified through GCMS. Antimicrobial activities were evaluated using the agar well method for bacteria and fungal biomass method for fungi. The extracts were subjected to evaluation for their antidiabetic activity through α-amylase and α-glucosidase inhibitory assays, while their anti-gout potential was assessed through xanthine oxidase inhibitory assay, encompassing all four solvent extracts in the study. Results Phytochemical screening revealed the presence of phenols, flavonoids, tannins, alkaloids, sterols, protein xanthoproteic, and cardiac glycosides in the extracts. The Folin-Ciocalteu and AlCl 3 assays demonstrated higher yields of phenolics and flavonoids in 80% ethanolic extract. Furthermore, the extracts remarkably scavenged reactive oxygen species like DPPH, ABTS and elicited considerable ferric ion reducing antioxidant power. GC–MS analysis identified 21 compounds in the 80% ethanolic extract, with 1,2,3-Propanetriol-1-acetate, n-Hexadecanoic acid, and 4H-Pyran-4-one,2,3-dihydro-3,5-dihydroxy-6-methyl- as major components. Antimicrobial assays demonstrated the ethanolic (80%) and methanolic extract's remarkable ability to inhibit the growth of Gram-positive bacteria and exhibit anti-fungal properties. The ethanolic (80%) extract exhibited an IC 50 value of 0.70 ± 0.02 and 0.71 ± 0.01 mg against α-amylase and α-glucosidase, respectively, and 33.76 ± 0.43 mg against xanthine oxidase. Conclusion Corn silk exhibits potential as a valuable reservoir of natural bioactive compounds endowed with a wide array of health-promoting properties. Graphical

研究领域: 天然产物化学 · 药用植物学 · 生物化学 · 药物代谢 · 微生物学 · 内分泌药理学 · 代谢性疾病
✓ 已验证 DOI 高影响因子
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Food & Function · 2015 ·Vol. 6 ·期 12 ·3693-3701 · IF 2.791

Separation and characterization of polyphenolics from underutilized byproducts of fruit production (Choerospondias axillaris peels): inhibitory activity of proanthocyanidins against glycolysis enzymes

Qian Li,Jun Chen,Ti Li,Chengmei Liu,Yuxin Zhai,David Julian McClements,Jiyan Liu

Bioactive proanthocyanidins were isolated from the peel of Choerospondias axillaris fruit, which is a waste product of the food processing industry. Compositional analysis indicated that the proanthocyanidins had extension units mainly consisting of epicatechin gallate or epicatechin, and terminal units mainly consisting of catechin. Numerous polymeric forms of the molecules were detected, including monomers, dimers, and trimers. Certain fractions exhibited strong α-amylase or α-glucosidase inhibition in a dose-dependent manner. Furthermore, their inhibitory activities depended on their degree of polymerization and galloylation. For example, the most bioactive fraction had α-amylase and α-glucosidase inhibitory activities (IC50 values) of 541 and 3.1 μg mL−1, respectively. This study demonstrates that proanthocyanidins from C. axillaris peels can inhibit carbohydrate digestive enzymes in vitro and may therefore serve as antidiabetic ingredients in functional or medical foods.

研究领域: 食品科学 · 植物化学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2019 ·Vol. 54 ·期 6 ·2084-2093 · IF 2.281

Extraction optimisation, antioxidant activity and inhibition on α-amylase and pancreatic lipase of polyphenols from the seeds of Syzygium cumini

Mohamed Abdin,Yahya Saud Hamed,Hafiz Muhammad Saleem Akhtar,Dan Chen,Shanza Mukhtar,Peng Wan,Asad Riaz,Xiaoxiong Zeng

Summary The objectives of this study were to determine the optimal extraction conditions of polyphenols from Syzygium cumini seeds by response surface methodology and investigate their antioxidant activity and inhibition on α-amylase and pancreatic lipase. As results, the optimal extraction conditions in the ultrasonic extraction process which maximised total polyphenols content, minimised the IC 50 values of α-amylase and pancreatic lipase were determined as follows: extraction time 60 min, ethanol concentration 63% and solvent/solid ratio 44 mL g −1 . The main phenolic compounds in partially purified fraction of Syzygium cumini seeds were catechin, epicatechin, kaempferol, gallic, 5-caffeoylquinic, caffeic and ferulic acids. In addition, the partially purified fraction inhibited 87.66 ± 5.55 and 86.61 ± 3.15% of α-amylase and pancreatic lipase, respectively. The results suggested that Syzygium cumini seeds could be explored as a natural antioxidant and could be used as a source of highly antidiabetic and anti-obesity bioactive compounds.

研究领域: 食品科学 · 药理学 · 生物化学
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2022 · IF 6.056

Development of yacon syrup fermented by Lactiplantibacillus plantarum NCU001043: Metabolite profiling, antioxidant and glycosidase inhibition activity

Fei Peng,Hui Huang,Jia-Xin Lin,Tao Yang,Mingyong Xie,Tao Xiong,Zhen Peng

The effects of Lactiplantibacillus plantarum NCU001043 fermentation on the physicochemical and biological properties of yacon tubers were investigated. The fermentation parameters were first optimized by single-factor tests, then an orthogonal experimental design, which resulted in production of a fermented yacon syrup with excellent sensory attributes and increased antimicrobial activity against Helicobacter pylori . The physicochemical characteristics of the yacon syrup were determined after fermentation under the optimum conditions. Although the total phenolic content of the fermented yacon syrup decreased after fermentation, its antioxidant capacity and glycosidase inhibition activity increased. Spearman correlation analysis indicated that one of the phenolic compounds, 4-hexyloxyphenol, might be the main α-amylase and α-glucosidase inhibitor. Molecular docking indicated that 4-hexyloxyphenol has a strong binding affinity for the active-sites of both enzymes. These findings will facilitate the development of yacon-based functional foods by microbial fermentation and application of Lactiplantibacillus plantarum NCU001043 in food fermentation.

研究领域: 食品科学 · 微生物学
✓ 已验证 DOI 高影响因子
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CHEMISTRY & BIODIVERSITY · 2023 ·Vol. 20 ·期 7 ·e202300387 · IF 2.9

Phytoconstituents of Selaginella effusa Alston and Their α-Glucosidase as well as Urease Inhibitory Activities

Wentao Sun,Li Luo,Jiazi Luo,Xixi Song,Demin Tang,Zishuo Song,Meishan Li,Hengshan Wang

Three new compounds ( 1 – 2 , 14 ), as well as 22 known compounds ( 3 – 13 , 15 – 25 ), were extracted for the first time from the Selaginella effusa Alston ( S. effusa ). For the unknown compounds, the planar configurations were determined via NMR and by high-resolution mass spectrometry, while their absolute configurations were determined by calculated electronic circular dichroism (ECD), and the configuration of the stereogenic center of biflavones 4 – 5 were established for the first time. The pure compounds ( 1 – 25 ) were tested in vitro to determine the inhibitory activity of the enzyme-catalyzed reactions. Compounds 1 – 9 inhibited α -glucosidase with IC 50 values ranging from 0.30±0.02 to 4.65±0.04 μM and kinetic analysis of enzyme inhibition indicated that biflavones 1 – 3 were mixed-type α -glucosidase inhibitors. Compounds 12 – 13 showed excellent inhibitory activity against urease, with compound 12 (IC 50 =4.38±0.31 μM) showing better inhibitory activity than the positive control drug AHA (IC 50 13.52±0.61 μM). In addition, molecular docking techniques were used to simulate inhibitor-enzyme binding and to estimate the binding posture of the α -glucosidase and urease catalytic sites. Graphical

CAS / MDL: 75-05-8
研究领域: 植物化学 · 药理学 · 酶学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2025 · IF 5.4

Green ultrasound‑assisted deep eutectic solvent extraction of flavonoid enzyme inhibitors from Blumea aromatica: process optimization, characterization, and mechanistic insights into α‑glucosidase and tyrosinase inhibition

Wei Dai,Liping Dai,Tao Su,Qin Lin,Zhiwen Lin,Shuxin Ye,Peihao Xu,Hongfeng Chen,Xilong Zheng

A green ultrasound-assisted deep eutectic solvent (UAE–DES) method was optimised for extracting flavonoid enzyme inhibitors from Blumea aromatica. Optimal conditions (choline chloride-1,4-butanediol 1:3 molar ratio, 43% water content, 50 mL/g liquid-to-solid ratio, 80 °C ultrasound for 48 min) yielded 3.15% total flavonoids, 45.2% higher than 50% ethanol extraction. Scanning electron microscopy confirmed cell wall disruption. The UAE–DES extract showed the strongest enzyme inhibition among all extracts tested (IC50 35.872 ± 0.294 µg/mL for α-glucosidase, 9.126 ± 0.285 μg/mL for tyrosinase), though the α-glucosidase inhibition was much weaker than acarbose, while tyrosinase inhibition was comparable to kojic acid. Six flavonoids were identified via UPLC-Q-Orbitrap HRMS, including scutellarein and corylin. Molecular docking revealed strong binding affinities (≤ −5 kcal/mol), with corylin showing the highest binding to both enzymes through hydrogen bonds and van der Waals interactions. This approach supports sustainable discovery of natural enzyme inhibitors for antidiabetic and skin-whitening applications.

CAS / MDL: 153-18-4
研究领域: 植物化学 · 酶学 · 绿色化学 · 药学 · 分析化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2023 · IF 6

Natural α-glucosidase and α-amylase inhibitors from raspberry (Rubus corchorifolius L.) leaf-tea: Screening, identification and molecular docking analysis

Fangliang Li,Tongjie Luo,Jiale Hou,Tao Fei,Jiachao Zhang,Lu Wang

Raspberry leaf as a tea substitute has been consumed in China for long time. In this work, the inhibitory activities of raspberry leaf-tea (RLT) extract on α -glucosidase ( α -GLU)/ α -amylase ( α -AMY) were measured, and the effects of the RLT extract on the glucose consumption of 3T-3L1 cells were also investigated. Results confirmed that RLT 70% ethanol extract (REE) exhibited strong inhibitory activities on α -GLU/ α -AMY in vitro . In addition, REE remarkably improved the glucose consumption of 3T-3L1 cells. Subsequently, eight major inhibitors including epigallocatechin gallate (EGCG), delphinidin-3- O -glucoside, cyanidin-3-rutinoside, isoorientin, procyanidin C3, dihydromyricetin, rutin, and isovitexin were screened and identified through affinity ultrafiltration combined with HPLC-MS/MS. Confirmation tests verified that these major compounds were responsible the inhibitory activities of the REE on α -GLU/ α -AMY. Molecular docking studies revealed that these inhibitors can well interact with α -GLU/ α -AMY via van der Waals force or hydrogen bonding, thus inhibiting their activities. In a short, raspberry leaf can be exploited as a promising anti-hypoglycemic material. This study provides a theoretical basis for discovering active components from medicinal plants using affinity ultra-filtration with multi-targets.

研究领域: 食品科学 · 植物化学 · 分子生物学
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Food Bioscience · 2022 · IF 5.318

Characterization and potential bioactivity of polyphenols of Rosa rugosa

Lan Wei,Jingjing Li,Yun Yang,Mei Zhu,Mengke Zhao,Jianhua Yang,Zhiyun Yang,Luyao Zhou,Shenyue Zhou,Jiajia Gong,Xiaogang Jiang,Jiangyun Liu,Yali Li,Jian Zhang

Rosa rugosa is widely cultivated in China, and the blossom of R. rugosa is used to extract rose essential oil or directly make into various foods, such as mei gui hua cake, mei gui hua sauce. Rose dregs are mostly used as fertilizer after extracting essential oil and the polar part has not been fully utilized. There is still much to be done in the products and deep processing of rose. In this study the content of total flavonol glycosides , the extractable polyphenols, the non-extractable polyphenols, the total phenolic and the total anthocyanins in R. rugosa from five major production areas in China was analyzed; the biological activities of the total extract, the polyphenols fraction, the flavonol glycosides fraction and the isolated compounds of R. rugosa were evaluated, including antioxidant, anti-ultraviolet, inhibitory activities of α -glucosidase, lipase , alveolar epithelial cell senescence and tyrosinase , together with regulating activities on intestinal flora . The components content of R. rugosa in different producing areas was significantly different. The total flavonol glycosides in Yunnan, the extractable polyphenols and the total phenolics in Shandong, the non-extractable polyphenols in Xinjiang, the total anthocyanins in Gansu was the higher than other areas. The polyphenols fraction showed antioxidant and anti-ultraviolet properties, inhibition of alveolar epithelial cell senescence, lipase and tyrosinase activities, and regulation of intestinal flora. The flavonol glycosides fraction showed α -glucosidase inhibitory activity. The results showed the polyphenols fraction and the flavonol glycosides fraction of R. rugosa could be used as skin care products and healthy food ingredient.

研究领域: 药理学 · 生物化学 · 食品科学 · 化妆品科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Proanthocyanidin polymers (condensed tannins) from lychee seeds exhibit antioxidant, anticancer, anti-α-amylase, and anti-tyrosinase activities

Jie Hao,Yuanshuo Wang,Yang Xiao,Songhua He,Mingqi Chen,Xin Mao,Qiuju Huang,Zhiheng Su,Qinpei Lu,Hongwei Guo

Lychee ( Litchi chinensis ) is a subtropical fruit known for its potential health benefits. In this study, proanthocyanidins (condensed tannins) from lychee seeds (LSPAs) were isolated using a bioactivity-guided approach. Their structural characteristics, as well as antioxidant, anticancer, anti-α-amylase, and anti-tyrosinase activities, were comprehensively analyzed. Structural analysis using mass spectrometry revealed that LSPAs are polymeric compounds predominantly composed of procyanidins (PCs), with a number-average molecular weight (Mn) of 5803 Da as determined by gel permeation chromatography (GPC). LSPAs exhibited significant antioxidant activity in DPPH, ABTS, and hydroxyl radical scavenging assays, with IC 50 values of 28.8 ± 1.3, 24.29 ± 1.93, and 119.67 ± 32.85 μg/mL, respectively. The FRAP assay showed antioxidant activity of 0.45 ± 0.01 μM Fe(II) equivalent/g DW. The CCK-8 assay demonstrated potent anti-breast cancer efficacy of LSPAs (IC 50  = 25.78 ± 0.37 μg/mL). Notably, LSPAs suppressed mammosphere formation and downregulated Sox2 and NICD1 expression in breast cancer stem cells (BCSCs). Molecular docking and dynamics simulations confirmed stable interactions between LSPAs and Sox2, primarily mediated by van der Waals forces. Enzyme kinetics and fluorescence spectroscopy further revealed that LSPAs effectively inhibited both α-amylase (IC 50  = 0.12 ± 0.004 μg/mL) and tyrosinase (IC 50  = 66.34 ± 0.37 μg/mL) activities by inducing conformational alterations and modifying the amino acid microenvironment of these enzymes. These findings establish LSPAs as promising multifunctional inhibitors with potential applications in food, cosmetics, and pharmaceuticals.

CAS / MDL: 100-53-8
研究领域: 食品科学 · 药理学 · 植物化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Novel polysaccharide from Chaenomeles speciosa seeds: Structural characterization, α-amylase and α-glucosidase inhibitory activity evaluation

Yejun Deng,Lixin Huang,Caihong Zhang,Pujun Xie,Jiang Cheng,Xiang Wang,Lujie Liu

Purification and structural characterization of a novel polysaccharide fraction from Chaenomeles speciosa seeds were investigated. After hot water extraction and ethanol precipitation, the crude polysaccharide was sequentially purified with Cellulose DEAE-52 and gel-filtration chromatography, and a highly purified polysaccharide fraction (F3) was obtained. The structure of F3 was characterized by high-performance gel permeation chromatography (HPGPC), high performance liquid chromatography (HPLC), ultraviolet-visible (UV), Fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectrum, together with methylation, scanning electron microscopy (SEM), atomic force microscope (AFM), and Congo-red test analysis. The results indicated that F3 was a homogeneous polysaccharide fraction with a molecular weight of 8.65 × 10 6  Da, and it was composed of Rha, GlcA, Gal, and Ara in a molar ratio of 6.34:5.73:47.14:40.13. The backbone of F3 was consisted of →3,6)-Gal p -(1→, and the side chains of F3 were composed of Ara f -(1→, →4)-Glc p A-(1→, →4)-Gal p -(1→ and →3)-Rha p -(1→. The hypoglycemic assays demonstrated F3 had good α-amylase and α-glucosidase inhibition activities, and their IC 50 values were 6.24 mg/mL and 4.59 mg/mL respectively. Thus, the polysaccharide from Chaenomeles speciose could be applied as a potential natural source in retarding postprandial hyperglycemia effects.

研究领域: 药学 · 生物化学 · 食品科学
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