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 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.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

scholarly journals GALLIC ACID: A PHENOLIC ACID AND ITS ANTIOXIDANT ACTIVITY FROM STEM BARK OF CHLOROFORM EXTRACTS OF SYZYGIUM LITORALE (BLUME) AMSHOFF (MYRTACEAE)

Molekul ◽  
2016 ◽  
Vol 11 (2) ◽  
pp. 180 ◽  
Author(s):  
Tukiran Tukiran ◽  
Fitriyatul Mahmudah ◽  
Nurul Hidayati ◽  
Kuniyoshi Shimizu
Keyword(s):  
Antioxidant Activity ◽  
Gallic Acid ◽  
Phenolic Acid ◽  
Methanol Extract ◽  
Authentic Sample ◽  
Stem Bark ◽  
Spectroscopic Studies ◽  
Chloroform Fraction ◽  
Ic50 Value ◽  
Isolated Compound

A phenolic acid had been isolated from chloroform soluble fractions of a methanol extract of stem bark of Syzygium litorale, Fam. Myrtaceae. The structure of the isolated compound was elucidated and established as gallic acid through extensive spectroscopic studies (UV-Vis, FTIR, and NMR) and by comparison with literature data and authentic sample. This is the first report of the isolation of compound from this plant, although it has previously been found in Myrtaceae family such as S. aromaticum, S. cumini, S. polyanthum, S. cordatum, etc. The chloroform fraction, isolated compound, and vitamin C showed very strong antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) with IC50 value of 23.2, 7.5, and 12.5 mg/mL, respectively.

scholarly journals Rapid Identification and Isolation of Inhibitors of Rat Lens Aldose Reductase and Antioxidant inMaackia amurensis

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Set Byeol Kim ◽  
Seung Hwan Hwang ◽  
Zhiqiang Wang ◽  
Jae Myung Yu ◽  
Soon Sung Lim
Keyword(s):  
Ethyl Acetate ◽  
Chlorogenic Acid ◽  
Aldose Reductase ◽  
Diabetic Complications ◽  
High Speed ◽  
Reductase Activity ◽  
Ethyl Acetate Fraction ◽  
Rapid Identification ◽  
Active Components ◽  
Abts Assay

Oxidative stress and aldose reductase activity have been implicated in the development of diabetic complications. In this study, the antioxidant and aldose reductase (AR) inhibitory effects ofMaackia amurensis(MA) were investigated. The ethyl acetate fraction of the MA extract showed the highest inhibitory activity in antioxidant and rat lens AR (RLAR). To identify and isolate the active components in the ethyl acetate fraction of the MA extract, high-speed countercurrent chromatography and Sephadex LH-20 column chromatography were performed and guided by an offline HPLC-ABTS assay and HPLC microfractionation AR assay. Four antioxidants, namely, piceatannol (IC50= 6.73 μM), resveratrol (IC50= 11.05 μM),trans-ferulic acid (IC50= 13.51 μM), and chlorogenic acid (IC50= 27.23 μM), and six AR inhibitors, namely, chlorogenic acid (IC50= 4.2 μM), tectoridin (IC50= 50.4 μM), genistein (IC50= 57.1 μM), formononetin (IC50= 69.2 μM), resveratrol (IC50= 117.6 μM), and daidzein (IC50= 151.9 μM), were isolated and identified. The screening results of the offline HPLC-ABTS assay and HPLC microfractionation AR assay matched the activity of isolated compounds. Thus, MA is potentially valuable for antioxidant and AR inhibitor discovery and efficient drug design for the prevention and treatment of diabetic complications.

scholarly journals Triterpenoid Glycosides from Olax imbricata

2019 ◽  
Vol 22 (3) ◽  
pp. 324-334
Author(s):  
Nga Thi Vo ◽  
Suong Thi Minh Huynh ◽  
Huong Thi My Nguyen ◽  
Huy Thuc Duong ◽  
Phung Kim Phi Nguyen
Keyword(s):  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Methanol Extract ◽  
Colorimetric Method ◽  
2D Nmr ◽  
Pure Compound ◽  
Ic50 Value ◽  
2D Nmr Spectra ◽  
Pure Compounds ◽  
Triterpenoid Glycosides

Introduction: Olax imbricata, owning antibacterial, antioxidant, and anti-inflammatory activities, has been investigated as one of traditional diabetic plants in Vietnam. In our previous publications on Olax imbricata, the structure analysis of the isolated compounds were reported, including two phenolic compounds, three phenolic glycosidic compounds, a sesquiterpenoid tropolone and 1,2,3,4-tetrahydronaphthalene derivatives. This article described the isolation and structure elucidation of three triterpenoid glycosides isolated from the methanol extract of Olax imbricata growing in Phu Yen province. Additionally, the evaluation of inhibitory activity for a-glucosidase was performed on a pure compound. Method: The methanol extract of this plant applied the chromatographic techniques, including thin-layer chromatography and silica gel column chromatography, led to the isolation of three pure compounds. The structures of three isolated compounds were elucidated by the spectroscopic data, including 1D and 2D NMR spectra in a combination of HRESIMS, and the sugar moieties were elucidated by acid hydrolysis. The a-glucosidase inhibitory assay was applied to a pure compound by the colorimetric method. Results: Three triterpenoid glycosides, namely 3-O-a-L-rhamnopyranosyl-(1->4)-b -D-glucopyranosyl-(1->3)-6′- O-ethyl-b -Dglucuronyl oleanolic acid (1), oleanolic acid 28-O-b -D-glucopyranoside (2) and spergulacin (3) were isolated and elucidated. The compound 2 showed its strong potentiala-glucosidase inhibitory activity with the IC50 value of 56.15+/-1.31 mM. Conclusion: Among them, compound 1 is a new one, the compounds 2 and 3 were isolated for the first time from the genus Olax. The compound 2 exhibited the potential a-glucosidase inhibition activity, contributing to demonstrating the diabetes treatment ability of Olax imbricata in the folklore.  

AKTIVITAS ANTIOKSIDAN DAN FLAVONOID EKSTRAK BIJI KURMA

EKOLOGIA ◽  
2020 ◽  
Vol 19 (1) ◽  
pp. 34-38
Author(s):  
Siti Warnasih ◽  
Diana Widiastuti ◽  
Uswatun Hasanah ◽  
Laksmi Ambarsari ◽  
Purwantiningsih Sugita
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Methanol Extract ◽  
Soxhlet Extraction ◽  
Ethyl Acetate Fraction ◽  
Positive Control ◽  
Palm Fruit ◽  
Ic50 Value ◽  
Dpph Method ◽  
Fruit Processing

Date seeds are waste from palm fruit processing that has not been utilized optimally. Date seeds contain flavonoids which are known to act as antioxidants. The aim of this study was to determine the antioxidant activity and flavonoid of methanol extract which was carried out by soxhletation and its fractionation results. Date seeds are made into simplicia, soxhlet extraction with methanol, then the methanol extract is fractionated in stages by liquid-liquid partition with n-hexane, ethyl acetate, and n-butanol. Each fraction and extract was determined by its antioxidant activity with the DPPH method and its flavonoid was determined by spectrophotometry. Ethyl acetate fraction has the strongest antioxidant activity with the lowest IC50 value, that is equal to 5.74 ± 0.05μg/mL, followed by methanol extract of 9.55±0.53 μg/mL, n-butanol fraction 19.73±0,58 μg/mL, and n-hexane fraction of 289.59±10.52 μg/mL, while the IC50 value for vitamin C as a positive control was 4.29±0.74 μg/mL. The highest flavonoids were produced from ethyl acetate fractions which amounted to 1484.33 ± 161.47 mg Quercetin Equivalent (QE) / 100 g, followed respectively by methanol extract of 282.84±13.72 mg QE/100 g.

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 Identification and Determination of Berberine from Arcangelisia Flava, East Borneo

2021 ◽  
Vol 5 (4) ◽  
pp. 381-386
Author(s):  
Riski Sulistiarini
Keyword(s):  
High Performance Liquid Chromatography ◽  
High Performance ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Hplc Method ◽  
Processed Food ◽  
Chelidonium Majus ◽  
Water Fraction ◽  
Traditional Medicines

Berberine is a compound that has various benefits but also has dangerous toxic effects. In Indonesia, the Regulation of the Head of the Food and Drug Supervisory Agency No. 10 of 2014 concerning the Prohibition of Producing and Circulating Traditional Medicines and Health Supplements Containing Coptis Sp, Berberis Sp, Mahonia Sp, Chelidonium Majus, Phellodendron Sp, Arcangelica Flava, Tinosporae Radix, and Catharanthus Roseus. Regulation No. 7 of 2018 (BPOM, 2018) also prohibits the presence of berberine in processed food. This research was conducted to determine the content of berberine compounds from the extract and stem fraction of Arcangelisia flava. The research was conducted by identifying the content of berberine by TLC method compared with Rf Berberine sulfate and determination of berberine content by HPLC method (High-Performance Liquid Chromatography) using column C-18 (ODS). Berberine content of methanol extract, n-hexane fraction, ethyl acetate fraction and Arcangelisia Flava methanol-water fraction were 0.0040, respectively; 0.0010; 0.0041, 0.0044%.

scholarly journals ANTIHEPATITIS C VIRUS ACTIVITY OF INDONESIAN MAHOGANY (TOONA SURENI)

2018 ◽  
Vol 11 (2) ◽  
pp. 87
Author(s):  
Achmad Fuad Hafid ◽  
Tutik Sri Wahyuni ◽  
Lidya Tumewu ◽  
Evhy Apryani ◽  
Adita Ayu Permanasari ◽  
...  
Keyword(s):  
Hepatitis C ◽  
Gallic Acid ◽  
Inhibitory Concentration ◽  
Ethyl Acetate Fraction ◽  
Ethyl Gallate ◽  
Methyl Gallate ◽  
Virus Activity ◽  
Ic50 Value ◽  
Isolated Compound ◽  
Active Substances

 Objective: Toona sureni (Indonesian mahogany) is a member of Meliaceae family and locally known as suren. Previous study reported that T. sureni leaves extract exhibited antiviral activity with 50% inhibitory concentration (IC50) value of 13.9 ± 1.6 μg/ml against hepatitis C virus (HCV) J6/JFH1. Cytotoxicity analysis of T. sureni leaves extract did not reveal any cytotoxicity effect; therefore, further study was taken to investigate the active substances from the extract.Methods: Bioassay-guided isolation of anti-HCV was conducted using Huh-7.5 cells infected with HCV J6/JFH1 in the presence of extracts, fractions, or compounds from the plant.Results: Ethyl acetate fraction (Fr E) exhibited high anti-HCV activity with IC50 value of 1.7 μg/ml. Further, separation of Fr E by open column chromatography resulted in nine sub-fractions (sub-Fr E1-E9). Sub-Fr E3 and E4 have IC50 value of 29.90 μg/ml and 7.68 μg/ml, respectively. Polyphenols compounds have been isolated from sub-Fr E3 and E4. The structures have been determined to be ethyl gallate (1), methyl gallate (2), catechin (3), gallic acid (4), and quercetin 3-O-rhamnoside (5). Among the isolated compounds, gallic acid showed to possess strong anti-HCV activity with IC50 value of 15.9 μg/ml.Conclusion: T. sureni and its isolated compound, gallic acid, may be good candidates to develop for alternative and/or complementary agents of anti-HCV infection.

Neuroprotective constituents of Actaea acuminata (Wall. ex Royle) H. Hara roots

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Deepak Kumar ◽  
Suresh Kumar
Keyword(s):  
Spectral Analysis ◽  
Phenolic Compounds ◽  
Gallic Acid ◽  
Anticonvulsant Activity ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Polyphenolic Compounds ◽  
Racemic Mixture ◽  
Sedative Activity ◽  
Scientific Validation

AbstractThe methanol extract and its ethyl acetate fraction (EAF) of Actaea acuminata (Wall. ex. Royle) H. Hara roots were reported to exhibit significant antianxiety, anticonvulsant and antidepressant activities, and mild sedative activity. But the constituents responsible for these activities have not been isolated. The present study was undertaken to isolate neuroprotective compounds of A. acuminata following bioactivity-guided-fractionation. The column chromatography of EAF and its sub-fractions led to the isolation of four phenolic compounds (bergenin, gallic acid, acetyl bergenin and racemic mixture of diacetyl bergenin), which were characterized by IR and NMR spectral analysis. All the compounds exhibited significant antianxiety and antidepressant activities with respect to control. The gallic acid and bergenin did not show anticonvulsant activity, whereas acetyl bergenin and racemic mixture of diacetyl bergenin exhibited significant anticonvulsant activity. Neuropharmacological activities of A. acuminata are attributed due to polyphenolic compounds. Scientific validation of traditional claims of A. acuminata has opened up roadmap of research for the development of CNS affecting lead molecules.

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