Rapid Screening Alpha-Glucosidase Inhibitors from Polygoni Vivipari Rhizoma by Multi-Step Matrix Solid-Phase Dispersion, Ultrafiltration and HPLC

Li, Haoxiang; He, Zhuobin; Shen, Qianhui; Fan, Weifeng; Tan, Guoying; Zou, Yuansheng; Mei, Quanxi; Qian, Zhengming

doi:10.3390/molecules26206111

Cited by 10 publications

(13 citation statements)

References 21 publications

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“…UF-HPLC is a rapid enzyme inhibitor screening method that has been used in studies on several herbal medicines [ 3 , 4 , 6 , 9 ]. By comparing the chromatograms of herbal extracts with active and inactive enzymes, peak areas of active components show a significant decrease.…”

Section: Resultsmentioning

confidence: 99%

“…The UF experiment was performed according to the method described in the literature, with slight modifications [ 4 ]. In the experimental group, 200 µL of the PCR extraction (5 mg/mL) was mixed with 200 µL of 3 enzyme solutions (200 U/mL of TYR, 4 U/mL of XOD, and 6 U/mL of α-GLU, respectively).…”

Section: Methodsmentioning

confidence: 99%

“…Currently, the enzyme inhibitors majorly originate from chemical synthetic, and natural products [ 1 ]. Chemical synthetic enzyme inhibitors usually have some side effects; for example, acarbose carries the risk of skin allergy and liver damage, while allopurinol carries the risk of liver and kidney damage [ 3 , 4 , 5 , 6 ]. To find safer enzyme inhibitors, screening enzyme inhibitors from natural products has become a research hotspot, and many natural inhibitors, such as huperzine-A, ursolic acid, and resveratrol, have been discovered [ 1 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

“…As a result, it is urgent that a rapid and efficient method be developed for screening enzyme inhibitors from natural products. Ultrafiltration coupled with high performance liquid chromatography (UF-HPLC), which combines enzyme affinity, HPLC separation, and identification, is a powerful tool for screening potential bioactive ingredients from complex natural products [ 3 , 4 , 6 ]. In UF-HPLC analysis, UF is carried out on a semipermeable membrane with a certain molecular weight cut-off which can separate the micro-molecule components and enzyme mixture into two parts.…”

Section: Introductionmentioning

confidence: 99%

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Screening of Tyrosinase, Xanthine Oxidase, and α-Glucosidase Inhibitors from Polygoni Cuspidati Rhizoma et Radix by Ultrafiltration and HPLC Analysis

Chen

Huang

et al. 2023

Molecules

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Polygoni Cuspidati Rhizoma et Radix (PCR), the rhizome and root of Polygonum cuspidatum Sieb. et Zucc., has been used as an herbal medicine for a long time. In this study, the ultrafiltration combined with high performance liquid chromatography (UF-HPLC) method was developed to screen tyrosinase (TYR), α-glucosidase (α-GLU), and xanthine oxidase (XOD) inhibitors from PCR. Firstly, the inhibitory activity of 50% methanol PCR extract on TYR, α-GLU, XOD, and acetylcholinesterase (ACHE) was tested. The extract showed a good inhibition on the enzymes, except for ACHE. Therefore, UF-HPLC experiments were carried out to screen TYR, α-GLU, and XOD inhibitors from PCR extract. Seven potential bioactive components were discovered, including methylgallate (1), 1,6-di-O-galloyl-D-glucose (2), polydatin-4′-O-D-glucoside (3), resveratrol-4′-O-D-glucoside (4), polydatin (5), malonyl glucoside resveratrol (6), and resveratrol-5-O-D-glucoside (7). Most of them were found as enzyme inhibitors from PCR for the first time, except polydatin (5), which had been reported as an α-GLUI in PCR in the literature. Finally, molecular docking analysis was applied to validate the interactions of these seven potential active components with the enzymes. Compounds 1–7 were proven as TYR inhibitors, compounds 2, 4–7 were identified as XOD inhibitors, and compounds 4–6 were confirmed as α-GLU inhibitors. In short, the current study provides a good reference for the screening of enzyme inhibitors through UF-HPLC, and provides scientific data for future studies of PCR.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Screening of Tyrosinase, Xanthine Oxidase, and α-Glucosidase Inhibitors from Polygoni Cuspidati Rhizoma et Radix by Ultrafiltration and HPLC Analysis

Chen

Huang

et al. 2023

Molecules

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“…The virtual simulations were done following some typical steps previously presented in the earlier reports [ 41 , 42 , 43 , 44 , 45 ]:…”

Section: Methodsmentioning

confidence: 99%

Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam

et al. 2023

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Among ten extracts of indigenous medicinal plants, the MeOH extract of Terminalia triptera Stapf. (TTS) showed the most efficient mammalian α-glucosidase inhibition for the first time. The data of screening bioactive parts used indicated that the TTS trunk bark and leaves extracts demonstrated comparable and higher effects compared to acarbose, a commercial anti-diabetic drug, with half-maximal inhibitory concentration (IC50) values of 181, 331, and 309 µg/mL, respectively. Further bioassay-guided purification led to the isolation of three active compounds from the TTS trunk bark extract and identified as (−)-epicatechin (1), eschweilenol C (2), and gallic acid (3). Of these, compounds 1 and 2 were determined as novel and potent mammalian α-glucosidase inhibitors. The virtual study indicated that these compounds bind to α-glucosidase (Q6P7A9) with acceptable RMSD values (1.16–1.56 Å) and good binding energy (DS values in the range of −11.4 to −12.8 kcal/mol) by interacting with various prominent amino acids to generate five and six linkages, respectively. The data of Lipinski’s rule of five and absorption, distribution, metabolism, excretion and toxicity (ADMET)-based pharmacokinetics and pharmacology revealed that these purified compounds possess anti-diabetic drug properties, and the compounds are almost not toxic for human use. Thus, the findings of this work suggested that (−)-epicatechin and eschweilenol C are novel potential mammalian α-glucosidase inhibitor candidates for type 2 diabetes treatment.

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New record of reusing brewing by-product for biosynthesis of prodigiosin and its novel anti-pathogen fungi via in vitro tests and molecular docking study

Nguyen,

Wang,

Phan

et al. 2024

Res Chem Intermed

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Rapid Screening Alpha-Glucosidase Inhibitors from Polygoni Vivipari Rhizoma by Multi-Step Matrix Solid-Phase Dispersion, Ultrafiltration and HPLC

Cited by 10 publications

References 21 publications

Screening of Tyrosinase, Xanthine Oxidase, and α-Glucosidase Inhibitors from Polygoni Cuspidati Rhizoma et Radix by Ultrafiltration and HPLC Analysis

Screening of Tyrosinase, Xanthine Oxidase, and α-Glucosidase Inhibitors from Polygoni Cuspidati Rhizoma et Radix by Ultrafiltration and HPLC Analysis

Screening and Elucidation of Chemical Structures of Novel Mammalian α-Glucosidase Inhibitors Targeting Anti-Diabetes Drug from Herbals Used by E De Ethnic Tribe in Vietnam

New record of reusing brewing by-product for biosynthesis of prodigiosin and its novel anti-pathogen fungi via in vitro tests and molecular docking study

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