scholarly journals Kaempferol Rhamnosides from Geranium sibiricum as Aldose Reductase Inhibitors and Their Content by HPLC Analysis

Processes ◽  
2020 ◽  
Vol 8 (6) ◽  
pp. 694
Author(s):  
Norman G. Quilantang ◽  
Kyung Choi ◽  
Bog-Hieu Lee ◽  
Sanghyun Lee
Keyword(s):  
Solvent Extraction ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Hplc Analysis ◽  
Ethyl Acetate Fraction ◽  
Inhibitory Effect ◽  
Reductase Inhibitors ◽  
Potent Inhibition ◽  
Ic50 Value ◽  
Natural Therapy

The study aimed to assess the aldose reductase (AR) inhibition of selected Geranium species and determine the bioactive flavonoid constituents. Flavonoids are known to be good AR inhibitors. Among the species examined, G. sibiricum exhibited potent inhibition of AR (IC50 value, 2.4 µg/mL). Further examination of G. sibiricum, after solvent extraction and fractionation, revealed that the ethyl acetate fraction (IC50 value, 0.41 µg/mL) had a potent AR inhibitory effect. Kaempferol rhamnosides were the active compounds from this fraction. Moreover, G. sibiricum showed the highest content of kaempferol-7-O-rhamnoside and kaempferol-3,7-O-dirhamnoside among the samples examined with a concentration in the extracts of 28.1 and 2.2 mg/g, respectively. This study shows that G. sibiricum exhibits promising AR inhibitory activity, which can be explored further as a natural therapy for treating and managing complications associated with diabetes.

scholarly journals Screening and Isolating Major Aldose Reductase Inhibitors from the Seeds of Evening Primrose (Oenothera biennis)

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2709 ◽  
Author(s):  
Zhiqiang Wang ◽  
Shigang Shen ◽  
Ze Cui ◽  
Hailiang Nie ◽  
Dandan Han ◽  
...  
Keyword(s):  
Gallic Acid ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
High Speed ◽  
High Performance ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Oenothera Biennis ◽  
Evening Primrose ◽  
Ic50 Value

Aldose reductase (AR) is a drug target for therapies to treat complications caused by diabetes mellitus, and the development of effective AR inhibitors (ARIs) of natural origin is considered to be an attractive option for reducing these complications. In this research, the rat lens AR (RLAR) inhibitory activity of evening primrose (Oenothera biennis) seeds was investigated for the first time. In our results, the 50% (v/v) methanol extract of evening primrose seeds exhibits excellent RLAR inhibitory activity (IC50 value of 7.53 μg/mL). Moreover, after enrichment of its bioactive components, the ARIs are more likely to be present in the ethyl acetate fraction of 50% (v/v) methanol extract (EME) of evening primrose seeds, which exhibits superior RLAR inhibitory activity (IC50 value of 3.08 µg/mL). Finally, gallic acid (1), procyanidin B3 (2), catechin (3), and methyl gallate (4) were identified as the major ARIs from the EME by affinity-based ultrafiltration-high-performance liquid chromatography and were isolated by high speed countercurrent chromatography, with gallic acid (11.46 µmol/L) and catechin (14.78 µmol/L) being the more potent inhibitors of the four ARIs identified. The results demonstrated that evening primrose seeds may be a potent ingredient of ARIs.

scholarly journals Inhibitory Activities ofStauntonia hexaphyllaLeaf Constituents on Rat Lens Aldose Reductase and Formation of Advanced Glycation End Products and Antioxidant

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Seung Hwan Hwang ◽  
Shin Hwa Kwon ◽  
Set Byeol Kim ◽  
Soon Sung Lim
Keyword(s):  
Aldose Reductase ◽  
Advanced Glycation End Products ◽  
Inhibitory Activity ◽  
Solvent System ◽  
Inhibitory Effect ◽  
Advanced Glycation ◽  
Rat Lens Aldose Reductase ◽  
Glycation End Products ◽  
End Products ◽  
Etoac Fraction

Stauntonia hexaphylla(Thunb.) Decne. (Lardizabalaceae) leaves (SHL) have been used traditionally as analgesics, sedatives, diuretics, and so on, in China. To date, no data have been reported on the inhibitory effect of SHL and its constituents on rat lens aldose reductase (RLAR) and advanced glycation end products (AGEs). Therefore, the inhibitory effect of compounds isolated from SHL extract on RLAR and AGEs was investigated to evaluate potential treatments of diabetic complications. The ethyl acetate (EtOAC) fraction of SHL extract showed strong inhibitory activity on RLAR and AGEs; therefore, EtOAc fraction (3.0 g) was subjected to Sephadex LH-20 column chromatography, for further fractionation, with 100% MeOH solvent system to investigate its effect on RLAR and AGEs. Phytochemical investigation of SHL led to the isolation of seven compounds. Among the isolated compounds, chlorogenic acid, calceolarioside B, luteolin-3′-O-β-D-glucopyranoside, quercetin-3-O-β-D-glucopyranoside, and luteolin-7-O-β-D-glucopyranoside exhibited significant inhibitory activity against RLAR with IC50in the range of 7.34–23.99 μM. In addition, 3-(3,4-dihydroxyphenyl) propionic acid, neochlorogenic acid, and luteolin-3′-O-β-D-glucopyranoside exhibited the most potent inhibitory activity against formation of AGEs, with an IC50value of 115.07–184.06 μM, compared to the positive control aminoguanidine (820.44 μM). Based on these findings, SHL dietary supplements could be considered for the prevention and/or treatment of diabetes complication.

scholarly journals The Inhibitory Effect ofPrunella vulgarisL. on Aldose Reductase and Protein Glycation

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Hong Mei Li ◽  
Jin Kyu Kim ◽  
Jai Man Jang ◽  
Sang Oh Kwon ◽  
Cheng Bi Cui ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Inhibitory Effect ◽  
Protein Glycation ◽  
Prunella Vulgaris ◽  
Inhibitory Effects ◽  
Advanced Glycation ◽  
High Concentration ◽  
Potent Inhibition ◽  
Glycation End Products

To evaluate the aldose reductase (AR) enzyme inhibitory ability ofPrunella vulgarisL. extract, six compounds were isolated and tested for their effects. The components were subjected toin vitrobioassays to investigate their inhibitory assays using rat lens aldose reductase (rAR) and human recombinant AR (rhAR). Among them, caffeic acid ethylene ester showed the potent inhibition, with the IC50values of rAR and rhAR at3.2±0.55 μM and12.58±0.32 μM, respectively. In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, this compound showed noncompetitive inhibition against rhAR. Furthermore, it inhibited galactitol formation in a rat lens incubated with a high concentration of galactose. Also it has antioxidative as well as advanced glycation end products (AGEs) inhibitory effects. As a result, this compound could be offered as a leading compound for further study as a new natural products drug for diabetic complications.

scholarly journals α-Amylase Inhibition, Antioxidant Activity and Phytochemical Analysis of Calotropis gigantea (L.) Dryand

2020 ◽  
Vol 10 (1) ◽  
pp. 77-81
Author(s):  
Rajendra Gyawali ◽  
Bijay Bhattarai ◽  
Susan Bajracharya ◽  
Surakshya Bhandari ◽  
Puja Bhetwal ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Ethyl Acetate Fraction ◽  
Gas Chromatography Mass Spectrometry ◽  
Phytochemical Analysis ◽  
Calotropis Gigantea ◽  
Ic50 Value ◽  
Loaded Column ◽  
Chloroform Methanol

Introduction: Antioxidant and α-Amylase inhibitory activity of methanolic extract of Calotropis gigantea (L.) Dryand leaves were evaluated. Methods: The antioxidant activity was evaluated by DPPH assay. The extract was fractionated in Silica gel loaded column chromatography (CC). All fractions were evaluated for their purity by TLC. Out of 11 fractions from CC, one fraction was analyzed by Gas Chromatography-Mass Spectrometry (GC-MS). Results: The antioxidant activity of methanolic extract was found satisfactory (IC50268.80 µg/ml) as compared with ascorbic acid (141.82 µg/ml). TLC of a fractions showed a compound at Rf value at 0.45 in toluene: chloroform: methanol with mobile phase ratio 7:2:1 respectively. Conclusions: Total 17 compounds were identified by GC-MS of ethyl acetate fraction and 5-hydroxyl methyl furfural was major furan compound (59.49%). α-Amylase inhibitory activity of the same fraction showed IC50 value of 0.94 mg/ ml. The Nepalese originated C. gigentea (L.) Dryand possesses antioxidant and α-Amylase inhibitory property.

scholarly journals ANTI-DIABETIC AND ALDOSE REDUCTASE INHIBITORY POTENTIAL OF PSIDIUM GUAJAVA BY IN VITRO ANALYSIS

2016 ◽  
Vol 8 (9) ◽  
pp. 271 ◽  
Author(s):  
Singaravelu Anand ◽  
Munichetty Arasakumari ◽  
Panneervelu Prabu ◽  
Arul Joseph Amalraj
Keyword(s):  
Glucose Uptake ◽  
Aldose Reductase ◽  
Inhibitory Activity ◽  
Psidium Guajava ◽  
Inhibitory Effect ◽  
Cellular Level ◽  
L6 Myotubes ◽  
Successive Extraction ◽  
Vitro Analysis

<p><strong>Objective: </strong>The objective of the present study was to determine the cellular level effect on glucose uptake and aldose reductase inhibitory activity of different extracts of traditional medicinal plant <em>Psidium guajava</em>.</p><p><strong>Methods: </strong><em>Psidium guajava</em> was selected and subjected for successive extraction from non-polar to polar solvents and subjected to glucose uptake and aldose reductase inhibition assay.</p><p><strong>Results: </strong>Based on the results <em>Psidium guajava</em><em> </em>methanolic extract (PGME) showed an enhancement in the glucose uptake and also up-regulates the gene and protein level expression of IRβ, IRS-1, PI3K and GLUT4. Wortmannin, a specific PI3K inhibitor confirms that the active PGME recruits glucose uptake through a PI3K dependent pathway. In the assay of aldose reductase inhibitory activity, the results suggested that PGME possesses a significant inhibitory effect.</p><p><strong>Conclusion: </strong>The result obtained in the present study focuses on the anti-diabetic effect of PGME by studying cellular level glucose uptake in L6 myotubes and aldose reductase inhibitory activity.<strong></strong></p>

scholarly journals Ranirestat has a stronger inhibitory activity on aldose reductase and suppresses inflammatory reactions in high glucose–exposed endothelial cells

2016 ◽  
Vol 13 (4) ◽  
pp. 312-315 ◽  
Author(s):  
Yuji Ishibashi ◽  
Takanori Matsui ◽  
Takafumi Matsumoto ◽  
Hiroshi Kato ◽  
Sho-ichi Yamagishi
Keyword(s):  
Endothelial Cells ◽  
Cell Adhesion ◽  
Aldose Reductase ◽  
High Glucose ◽  
Inhibitory Activity ◽  
Umbilical Vein ◽  
Inflammatory Reactions ◽  
Human Umbilical Vein ◽  
Reductase Inhibitors ◽  
Umbilical Vein Endothelial Cells

Objective: Under diabetic conditions, glucose is converted to sorbitol via aldose reductase, whose process could contribute to diabetic vascular complications. However, effects of aldose reductase inhibitors are modest in diabetic patients. This may be attributed to weak inhibitory activity of aldose reductase inhibitors. We compared effects of ranirestat on endothelial cell damage with those of epalrestat. Materials and methods: Intracellular formations of sorbitol and superoxide were measured by liquid chromatography–mass spectrometry–mass spectrometry and dihydroethidium staining, respectively. Vascular cell adhesion molecule-1 gene expression was analysed by reverse transcription polymerase chain reaction. THP-1 cell adhesion to human umbilical vein endothelial cells was evaluated using a fluorescent probe. Results: High glucose significantly increased sorbitol levels, superoxide generation and vascular cell adhesion molecule-1 mRNA levels in, and THP-1 cell adhesion to, human umbilical vein endothelial cells, all of which were prevented by 500 nM ranirestat, but not epalrestat except for superoxide production. Conclusion: Our present results suggest that ranirestat has a stronger inhibitory activity on aldose reductase than epalrestat and suppresses inflammatory reactions in high glucose–exposed human umbilical vein endothelial cells.

scholarly journals Heme Polymerization Inhibitory Activity And Phytochemical Screening Of Ethyl Acetate Fraction In Manuran (Coptosapelta tomentosa Valeton ex K. Heyne) Stem

2021 ◽  
Vol 6 (1) ◽  
pp. 1-7
Author(s):  
Arnida ◽  
Siti Humairah Z.A ◽  
Sutomo ◽  
Fadlillahturrahmah
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Chemical Compound ◽  
Methyl Acetate ◽  
Ethyl Acetate Fraction ◽  
Compound Identification ◽  
Ic50 Value ◽  
Significant Difference ◽  
Chloroquine Diphosphate

The native Indonesian plant that is empirically used as an antimalarial agent is manuran (Coptosapelta tomentosa Valeton ex K. Heyne). This study aims to determine chemical compound and heme polymerization inhibitory activity of ethyl acetate fraction of C. Tomentosa stem based on IC50 value. The method identification of chemical compound used tube test, and the method of heme polymerization inhibitory activity was Basilico through in vitro method. The results of chemical compound identification of the ethyl acetate fraction of C. Tomentosa showed the presence of flavonoids, terpenoids, saponins, tannins, and anthraquinones. The average percentages of heme polymerization inhibitory activity of ethyl acetate fraction of C. Tomentosa stem from concentration 20; 10; 5; 2.5; 1.25; 0.625; 0.3125 mg / mL were 98.507; 97,872; 96,407; 93,560; 88,419; 80,680; and 45.467%.The averages of IC50 of ethyl acetate fraction and chloroquine diphosphate were 0.24 ± 0.018 mg/mL and 0.214 ± 0.012 mg/mL. This shows that the ethyl acetate fraction of C. Tomentosa stem has heme polymerization inhibitory activity. The result of the independent sample t-Test obtained the significance value of 0.111 (p more than 0.05) that there was no significant difference. It means that the ethyl acetate fraction of C. Tomentosa stem has heme polymerization inhibitory activity as well as chloroquine diphosphate. This suggests the potentiation of the methyl acetate fraction of the stem C. Tomentosa as anti-malarial.

scholarly journals ACYLATED FLAVONOIDS OF SPIRAEA GENUS AS α-AMYLASE INHIBITORS

2017 ◽  
pp. 81-90 ◽  
Author(s):  
Нина (Nina) Игоревна (Igorevna) Кащенко (Kashchenko) ◽  
Надежда (Nadezhda) Константиновна (Konstantinovna) Чирикова (Chirikova) ◽  
Даниил (Daniil) Николаевич (Nikolaevich) Оленников (Olennikov)
Keyword(s):  
Ethyl Acetate Fraction ◽  
Inhibitory Effect ◽  
Leading Role ◽  
Ic50 Value ◽  
Extractive Substances ◽  
Deciduous Shrubs ◽  
Rosaceae Family ◽  
Amylase Inhibitors ◽  
First Time

Spiraea L. is a genus of deciduous shrubs of Rosaceae family widespread on the territory of Eastern Siberia. As a result of the study of six Spiraea species growing on the Baikal region, it was shown that they characterized by a high content of phenolic compounds and their extracts had an inhibitory effect on α-amylase. The use of correlation analysis made it possible to reveal the leading role of flavonoids as carriers of the biological effect of extracts. The most active was the extract of S. salicifolia leaves with an IC50 value 69,30 μg/mL After fractionation and chromatographic separation of the extractive substances, 18 compounds were isolated from the ethyl acetate fraction of S. salicifolia and fifteen of them for the first time for the species, including trifolin, 6′′-O-caffeoyl-hyperoside, 6′′-O-caffeoyl-isoquercitrin, 6′′-O-caffeoyl-astragalin, 1-O-p-hydroxybenzoyl-6-O-p-coumaroyl-β-d-glucopyranoside, 3,4,5-tri-O-caffeoylquinic acid, isoramnetinin-3-O-β-d-glucopyranoside, tiliroside, isoramnetin-3-O-α-l-rhamnopyranoside, 1-O-cis-cinnamoyl-6-O-(2′-methylene-4′-hydroxybutyroyl)-β-d-glucopyranose, 1-О-(4′′-hydroxy-3′′-methylfurane-2′′-one)-6-О-trans-cinnamoyl-β-d-glucopyranose, 1-О-(4′′-hydroxy-3′′-methylfurane-2′′-one)-6-О-cis-cinnamoyl-β-d-glucopyranose, 6-tuliposide A and tulipalin A. The most active inhibitors of α-amylase were flavonoid caffeoyl glycosides with 6′′-O-caffeoyl-hyperoside as a most effective inhibitor with IC50 value 46.18 μg/mL. Latter compound determined the total anti-α-amylase effect of S. salicifolia. The content of 6′′-O-caffeoyl-hyperoside in leaves of S. salicifolia was 0,60-10,53 mg/g and flavonoids – 12,02-23,17 mg/g. This study demonstrated the fact that the acylated flavonoids of Spiraea are effective inhibitors of α-amylase.

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