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Evaluation of the Antidiabetic Activity and Chemical Composition of Geranium collinum Root Extracts-Computational and Experimental Investigations.

ABSTRACT: The root of Geranium collinum Steph is known in Tajik traditional medicine for its hepatoprotective, antioxidant, and anti-inflammatory therapeutic effects. The present study was conducted to evaluate of potential antidiabetic, antioxidant activities, total polyphenolic and flavonoid content from the different extracts (aqueous, aqueous-ethanolic) and individual compounds isolated of the root parts of G. collinum. The 50% aqueous-ethanolic extract possesses potent antidiabetic activity, with IC50 values of 0.10 ?g/mL and 0.09 ?g/mL for the enzymes protein-tyrosine phosphatase (1B PTP-1B) and ?-glucosidase, respectively. Phytochemical investigations of the 50% aqueous-ethanolic extract of G. collinum, led to the isolation of ten pure compounds identified as 3,3',4,4'-tetra-O-methylellagic acid (1), 3,3'-di-O-methylellagic acid (2), quercetin (3), caffeic acid (4), (+)-catechin (5), (-)-epicatechin (6), (-)-epigallocatechin (7), gallic acid (8), ?-sitosterol-3-O-?-d-glucopyranoside (9), and corilagin (10). Their structures were determined based on 1D and 2D NMR and mass spectrometric analyses. Three isolated compounds exhibited strong inhibitory activity against PTP-1B, with IC50 values below 0.9 ?g/mL, more effective than the positive control (1.46 ?g/mL). Molecular docking analysis suggests polyphenolic compounds such as corilagin, catechin and caffeic acid inhibit PTP-1B and ?-sitosterol-3-O-?-d-gluco-pyranoside inhibits ?-glucosidase. The experimental results suggest that the biological activity of G. collinum is related to its polyphenol contents. The results are also in agreement with computational investigations. Furthermore, the potent antidiabetic activity of the 50% aqueous-ethanolic extract from G. collinum shows promise for its future application in medicine. To the best of our knowledge, we hereby report, for the first time, the antidiabetic activity of G. collinum.

SUBMITTER: Numonov S

PROVIDER: S-EPMC6152703 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Evaluation of the Antidiabetic Activity and Chemical Composition of Geranium collinum Root Extracts-Computational and Experimental Investigations.

Numonov Sodik S Edirs Salamet S Bobakulov Khayrulla K Qureshi Muhammad Nasimullah MN Bozorov Khurshed K Sharopov Farukh F Setzer William N WN Zhao Haiqing H Habasi Maidina M Sharofova Mizhgona M Aisa Haji Akber HA

Molecules (Basel, Switzerland) 20170613 6

The root of <i>Geranium collinum</i> Steph is known in Tajik traditional medicine for its hepatoprotective, antioxidant, and anti-inflammatory therapeutic effects. The present study was conducted to evaluate of potential antidiabetic, antioxidant activities, total polyphenolic and flavonoid content from the different extracts (aqueous, aqueous-ethanolic) and individual compounds isolated of the root parts of <i>G. collinum</i>. The 50% aqueous-ethanolic extract possesses potent antidiabetic acti ...[more]

PMID: 28608836

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Project description:Irvingia gabonensis commonly referred to as wild mango or ogbono is a tropical plant with both nutritional and medicinal uses. The present study was designed to evaluate the chemical composition, in vitro antioxidant activity, and inhibitory activity of carbohydrate hydrolyzing enzymes related to diabetes by different extracts of the plant. From the results of the study, Total Phenolic Content (TPC) was highest in the aqueous and ethanol extracts (367.30 ± 00 mg/100g GAE) compared to the chloroform and n-hexane extracts whereas the Total Flavonoid Content (TFC) was highest (230.69 ± 0.18 mg/100g QE) in the ethanol extract. Analysis of the in vitro antioxidant activity showed that the ethanol extract also possessed the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity (IC50: 21.42 ± 0.05 μg/ml) and hydroxyl radical scavenging activity (81.43 ± 0.11%) compared to other solvent extracts. The aqueous extract had the highest (23.91 ± 0.04 mM Fe++ equivalent) ferric antioxidant reducing power (FRAP). However, the antioxidant activity of the extracts was significantly lower than that of the reference compounds used for the study (butylated hydroxytoluene and Gallic acid). In vitro antidiabetic activity of the extracts was measured based on inhibition of α-amylase and α-glucosidase. The aqueous extract had the highest α-amylase and α-glucosidase inhibitory activity followed by the ethanol extract compared to the chloroform and n-hexane extracts. The inhibitory activity of the aqueous extract against both enzymes was higher compared to the reference compound Acarbose. Gas Chromatography-Mass Spectrometry analysis of the extracts revealed the presence of chemical constituents including fatty acids, vitamin, phytosterols, aromatic compounds, glycosides. The interaction of these compounds with α-amylase and α-glucosidase was evaluated in silico by molecular docking. Phytosterols namely, campesterol, stimasterol and γ-sitosterol had the best binding affinities to α-amylase and α-glucosidase. In conclusion, the results of this study revealed that the aqueous and ethanol extracts of Irvingia gabonensis had the highest phenolic content, antioxidant activity, and in vitro antidiabetic activity. These results offer a scientific explanation for the mode of preparation and traditional use of the plant in the treatment of diabetes.

Dataset Information

Evaluation of the Antidiabetic Activity and Chemical Composition of Geranium collinum Root Extracts-Computational and Experimental Investigations.

Publications

Evaluation of the Antidiabetic Activity and Chemical Composition of Geranium collinum Root Extracts-Computational and Experimental Investigations.

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