Evaluation of in-vitro antidiabetic activity of leaf juice of Plectranthus amboinicus (lour.)

2020 ◽  
Vol 10 (1) ◽  
pp. 9-17
Author(s):  
Pavan Kumar Kurakula ◽  
Tharun D ◽  
Mahantesh S ◽  
Krishna O ◽  
Sudheer A ◽  
...  
Keyword(s):  
Side Effects ◽  
Enzyme Inhibitors ◽  
Antidiabetic Activity ◽  
Albino Rat ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Gastrointestinal Side Effects ◽  
Plectranthus Amboinicus ◽  
Leaf Juice

Diabetes mellitus ‘the disease of modern civilization’ is characterized by chronic hyperglycaemia. The management of elevated post prandial glucose is critical to control the sequale of complications and α-amylase, α-glucosidases are responsible for elevated plasma glucose. Enzyme inhibitors in current clinical practice like acarbose, voglibose etc. are known to cause various gastrointestinal side effects. The present study was aimed to screen for potential α-amylase and α-glucosidase inhibitors from natural sources by in–vitro antidiabetic assays to overcome the side effects and toxicity. Different concentrations of leaf juice of Plectranthus amboinicus Lour. (20, 40, 60, 80 &100 μg/ml) were tested against fungal α-amylase and α-glucosidases isolated from albino rat small intestine and a prominent dose dependent inhibition of the enzymes was observed comparable with the marketed product, Acarbose. The IC50 values of LJPA and acarbose on fungal α-amylase was found to be 83.15 &52.15 μg/ml respectively. The IC50 values of LJPA and acarbose on α-glucosidase was found to be 92.44 &54.84 μg/ml respectively. The protein concentration of leaf juice was found to be 10.6 mg/ml.

α-Glucosidase Inhibitory Activity of the Extracts and Major Phytochemical Components of Smilax glabra Roxb

2020 ◽  
Vol 10 (1) ◽  
pp. 26-32
Author(s):  
Phuong T.M. Nguyen ◽  
Quang V. Ngo ◽  
Minh T.H. Nguyen ◽  
Alan T. Maccarone ◽  
Stephen G. Pyne
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Cytotoxicity ◽  
Antidiabetic Activity ◽  
Ca 125 ◽  
Chemical Structures ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Phytochemical Components

Background: A therapeutic approach to treat diabetes is to decrease postprandial hyperglycemia. α-Glucosidase inhibitors from plant sources offer an attractive strategy for the control of hyperglycemia. Smilax glabra Roxb is a medicinal plant found in Asia, including Vietnam, which is used in the treatment of chronic diseases. However, the antidiabetic activity and the identification of α-glucosidase inhibitors from this plant have not been intensively investigated. This research was carried out to determine the α-glucosidase inhibitory activity of the extracts and that of the major phytochemical components of Smilax glabra Roxb. This could lead to further studies on the role of these compounds in hyperglycemia control, as well as identify their potential future applications. Methods: Column chromatography combined with crystallization procedures were used to isolate active fractions and two major compounds. The chemical structures of these compounds were determined by analysis of their NMR spectroscopic data, as well as MS data and comparisons made with the literature data. The α-glucosidase inhibitory activity was determined spectrophotometrically using p-nitrophenyl α-D-glucopyranoside as a substrate. The in vitro cytotoxicity of the isolated compounds and fractions was determined using the MTT assay. Results: The two major compounds, astilbin and 5-O-caffeoylshikimic acid together with two very active fractions, F7 and F8, were isolated from the rhizome. The two major compounds had α- glucosidase inhibitory activities with IC50 values of ca. 125 µg/mL and 38 µg/mL, respectively which are about 4 and 13 folds higher activity than the reference compound acarbose (IC50 of ca. 525 µg/mL). Fractions F7 and F8 showed very promising inhibitory activities towards α-glucosidase with IC50 values of 5.5 and 5.8 µg/mL, respectively. Cytotoxicity data on mouse fibroblast NIH3T3 cells indicated that the active compounds and fractions were not toxic at concentrations that are greater than their respective IC50 values. The α-glucosidase inhibitory activity of 5-Ocaffeoylshikimic acid and that of the two active fractions are reported here for the first time. Conclusion: The two major isolated compounds and fractions, F7 and F8, significantly contribute to the α-glucosidase inhibitory activity of S. glabra Roxb extract. Further work is needed to clarify their modes of action and potential application.

scholarly journals IN-VITRO HYPOGLYCEMIC EVALUATION OF FRACTIONS OF HYDRO-ACOHOLIC EXTRACT OF HEARTWOOD OF TECOMELLA UNDULATA LINN.

2017 ◽  
Vol 10 (2) ◽  
pp. 266
Author(s):  
Munish Garg ◽  
Ruby Rohilla ◽  
Chanchal Garg
Keyword(s):  
Postprandial Hyperglycemia ◽  
Alcoholic Extract ◽  
Phytochemical Screening ◽  
Bioactive Components ◽  
Standard Drug ◽  
Minimal Inhibitory Concentrations ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Tecomella Undulata

Objective: To screen α-amylase and α-glucosidase inhibitors from the different fractions of crude hydro-alcoholic extract of heartwood of Tecomella undulata Linn.Methods: Four fractions of crude hydro-alcoholic extract of heartwood of plant were used for in-vitro inhibitory assays against digestive enzymes: α-amylase and α-glucosidase. For assay, different concentrations (20, 40, 60, 80, 100 µg/ml) were used for all fractions. Standard protocol was used for preliminary phytochemical screening of different bioactive components present in all fractions.Results: The fractions have shown moderate to highest inhibitory activity against both enzymes. But, the strong inhibition was revealed by acetone fraction against α-amylase with very minimal inhibitory concentrations at IC50 values when compared with a standard drug acarbose. Several medicinally active phytocomponents such as flavanoids, saponin, anthraquinones, tannins, triterpenoids and phenols were observed in all studied fractions.Conclusion: The different fractions prepared from crude hydro-alcoholic extract of heartwood of plant are capable of inhibiting α-amylase and α-glucosidase and it can be concluded that heartwood of Tecomella undulata Linn. is partially active against postprandial hyperglycemia, thus diabetes mellitus.Keywords: Tecomella undulata Linn., Diabetes mellitus, α-Amylase, α-Glucosidase. 

scholarly journals LC-QTOF-MS/MS Based Molecular Networking Approach for the Isolation of α-Glucosidase Inhibitors and Virucidal Agents from Coccinia grandis (L.) Voigt

Foods ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3041
Author(s):  
Maharani A. Astiti ◽  
Akanitt Jittmittraphap ◽  
Pornsawan Leaungwutiwong ◽  
Nopporn Chutiwitoonchai ◽  
Patcharee Pripdeevech ◽  
...  
Keyword(s):  
Influenza A ◽  
2D Nmr ◽  
Antidiabetic Activity ◽  
Flavonoid Glycosides ◽  
Edible Plant ◽  
Molecular Networking ◽  
Coccinia Grandis ◽  
Glucosidase Inhibitors

Coccinia grandis or ivy gourd is an edible plant. Its leaves and fruits are used as vegetable in many countries. Many works on antidiabetic activity of a crude extract of C. grandis, i.e., in vitro, in vivo, and clinical trials studies, have been reported. Profiles of the antidiabetic compounds were previously proposed by using LC-MS or GC-MS. However, the compounds responsible for antidiabetic activity have rarely been isolated and characterized by analysis of 1D and 2D NMR data. In the present work, UHPLC-ESI-QTOF-MS/MS analysis and GNPS molecular networking were used to guide the isolation of α-glucosidase inhibitors from an extract of C. grandis leaves. Seven flavonoid glycosides including rutin (1), kaempferol 3-O-rutinoside (2) or nicotiflorin, kaempferol 3-O-robinobioside (3), quercetin 3-O-robinobioside (4), quercetin 3-O-β-D-apiofuranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside (5) or CTN-986, kaempferol 3-O-β-D-api-furanosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside (6), and kaempferol 3-O-β-D-apiofuranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranoside (7) were isolated from C. grandis leaves. This is the first report of glycosides containing apiose sugar in the genus Coccinia. These glycosides exhibited remarkable α-glucosidase inhibitory activity, being 4.4–10.3 times more potent than acarbose. Moreover, they also displayed virucidal activity against influenza A virus H1N1, as revealed by the ASTM E1053-20 method.

scholarly journals In-vitro Anti-diabetic and Antioxidant Efficacy of Methanolic Extract of Canthium coromandelicum Leaves

2020 ◽  
pp. 12-18
Author(s):  
S. Thiripura Salini ◽  
S. Shankar
Keyword(s):  
Diabetic Complications ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Antidiabetic Activity ◽  
Dpph Radical ◽  
Dpph Assay ◽  
Ic50 Value ◽  
Ic50 Values ◽  
In Vitro Antioxidant Activity

Oxidative stress plays a major role in diabetic complications. The study aim was to investigate the in-vitro antidiabetic and antioxidant activities of methanolic extract of Canthium coromandelicum leaves. The plant material was extracted with methanol and the methanolic extract was screened for in-vitro antioxidant activity using 1, 1-diphenyl-2-picryl hydrazyl (DPPH) assay. The efficiency of the antidiabetic activity of the plant extract was evaluated against α-amylase and α-glucosidase digestive enzymes. The study revealed that the C. coromandelicum extract exhibited significant α-amylase and α-glucosidase inhibitory activities with an IC50 value of 31.52 ± 0.42 and 41.49 ± 0.28 µg/mL respectively and compared with standard acarbose drug. The extract efficiently scavenging DPPH radical with IC50 values of 65.46 ± 0.50 µg/ml. Therefore, the extract could be a promising therapeutic in management of diabetic complications.

scholarly journals Antioxidant, Antimicrobial, Antidiabetic and Cytotoxic Activity of Crocus sativus L. Petals

2020 ◽  
Vol 10 (4) ◽  
pp. 1519
Author(s):  
Adil Farooq Wali ◽  
Houda Ahmed Abou Alchamat ◽  
Huda Khaled Hariri ◽  
Bushra Khaled Hariri ◽  
Godfred A. Menezes ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Cytotoxic Activity ◽  
Inhibitory Concentration ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Crocus Sativus ◽  
Antidiabetic Activity ◽  
Ic50 Values ◽  
Crocus Sativus L

The purpose of this research is to examine in vitro antioxidant, antimicrobial, antidiabetic and cytotoxic efficacy of different extracts of Crocus sativus L. petals. Antioxidant activity of extracts was assessed by DPPH and ABTS (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) assay. Among all extracts, ethanol (SPE) had the maximum radical scavenging activity with IC50 values 86.63 ± 7.53 μg/mL. The antimicrobial activity was determined by the evaluation of the minimum inhibitory concentration using the agar well plate procedure. The most effective extract was SPE with a minimum inhibitory concentration varying between 500 µg/mL, 250 µg/mL, 125 µg/mL, 62.5 µg/mL, 31.25 µg/mL, 15.63 µg/mL. Cytotoxic activity was tested against MDA-MB-231 cell lines using the MTT method whereas, antidiabetic activity was evaluated using an alpha-glucosidase inhibition assay. All extracts were found to have significant antidiabetic activity.

COMPARATIVE IN VITRO ANTIDIABETIC ACTIVITY OF PRUNUS AMYGDALUS (BAIL.) AND HIBISCUS ROSA-SINENSIS (LINN.)

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (04) ◽  
pp. 29-31
Author(s):  
Keyword(s):  
Aqueous Extract ◽  
Ethanolic Extract ◽  
Antidiabetic Activity ◽  
Assay Method ◽  
Inhibition Assay ◽  
Phytochemical Screening ◽  
Prunus Amygdalus ◽  
Hibiscus Rosa Sinensis ◽  
Ic50 Values

A comparative study was designed to evaluate the in vitro antidiabetic activity from the aqueous extract of dried pericarp of Prunus amygdalus Bail and ethanolic extract of dried flower of Hibiscus rosa-sinensis L. against the standard Acarbose.The aqueous extract of P. amygdalus and ethanolic extract of H. rosa-sinensis were extracted by the continuous hot extraction process.The qualitative phytochemical screening of aqueous extract and ethanolic extract reveals the presence of phytosterols, phenols, carbohydrates, flavanoids, saponins, amino acids and alkaloids, phenol, tannins, cardiac glycoside, saponin and flavonoids, respectively. In vitro pharmacological activity of P. amygdalus and H.rosa-sinensis were performed and compared by α-amylase inhibition assay method. The percentage inhibition of α-amylase by P. amygdalus, H. rosa-sinensis and Acarbose (50 &100 μg/mL) at dose of 50mg/mL and 100mg/mL were found to be 60.11±2.74%,74.86±0.31*%, 71.36± 1.86%, 81.49±1.72%, 82.33±1.10% and 95.37±0.56*%, respectively. The IC50 values were found to be 40.26μg/mL for acarbose, 49.63mg/mL for ethanolic extract of H. rosa-sinensis and 56.42mg/mL for aqueous extract of P. amygdalus.

scholarly journals Antidiabetic Activity ofGnidia glaucaandDioscorea bulbifera: Potent Amylase and Glucosidase Inhibitors

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Sougata Ghosh ◽  
Mehul Ahire ◽  
Sumersing Patil ◽  
Amit Jabgunde ◽  
Meenakshi Bhat Dusane ◽  
...  
Keyword(s):  
Petroleum Ether ◽  
Therapeutic Potential ◽  
Low Cost ◽  
Petroleum Ether Extract ◽  
Antidiabetic Activity ◽  
Biochemical Basis ◽  
Glucosidase Inhibitors ◽  
Treatment Of Diabetes

Diabetes is a metabolic disorder affecting about 220 million people worldwide. One of the most critical complications of diabetes is post-prandial hyper-glycemia (PPHG). Glucosidase inhibitor andα-amylase inhibitors are class of compounds that help in managing PPHG. Low-cost herbal treatment is recommended due to their lesser side effect for treatment of diabetes. Two plants with significant traditional therapeutic potential, namely,Gnidia glaucaandDioscorea bulbifera, were tested for their efficiency to inhibitα-amylase andα-glucosidase. Stem, leaf, and flower ofG. glaucaand bulb ofD. bulbiferawere sequentially extracted with petroleum ether, ethyl acetate, and methanol as well as separately with 70% ethanol. Petroleum ether extract of flower ofG. glaucawas found to inhibitα-amylase significantly (78.56%). Extracts were further tested against crude murine pancreatic, small intestinal, and liver glucosidase enzyme which revealed excellent inhibitory properties.α-glucosidase inhibition provided a strongin vitroevidence for confirmation of bothG. glaucaandD. bulbiferaas excellent antidiabetic remedy. This is the first report of its kind that provides a strong biochemical basis for management of type II diabetes usingG. glaucaandD. bulbifera. These results provide intense rationale for furtherin vivoand clinical study.

scholarly journals Identification of Digestive Enzyme Inhibitors from Ludwigia octovalvis (Jacq.) P.H.Raven

2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Dulce Morales ◽  
Guillermo Ramirez ◽  
Armando Herrera-Arellano ◽  
Jaime Tortoriello ◽  
Miguel Zavala ◽  
...  
Keyword(s):  
High Performance ◽  
Inhibitory Concentration ◽  
Enzyme Inhibitors ◽  
Competitive Inhibition ◽  
Digestive Enzyme ◽  
Chemical Compounds ◽  
Ethyl Acetate Fraction ◽  
Hydroalcoholic Extract ◽  
Glucosidase Inhibitors

Current antiobesity and antidiabetic tools have been insufficient to curb these diseases and frequently cause side effects; therefore, new pancreatic lipase and α–glucosidase inhibitors could be excellent aids for the prevention and treatment of these diseases. The aim of this study was to identify, quantify, and characterize the chemical compounds with the highest degree of inhibitory activity of these enzymes, contained in a Ludwigia octovalvis hydroalcoholic extract. Chemical purification was performed by liquid–liquid separation and column chromatography. Inhibitory activities were measured in vitro, employing acarbose, orlistat, and a Camellia sinensis hydroalcoholic extract as references. For structural elucidation, Nuclear Magnetic Resonance was carried out, and High Performance Liquid Chromatography was used to quantify the compounds. For α–glucosidases, L. octovalvis hydroalcoholic extract and its ethyl acetate fraction showed half–maximal Inhibitory Concentration (IC50) values of 700 and 250 μg/mL, for lipase, 480 and 718 μg/mL, while C. sinensis showed 260 and 587 μg/mL. The most active compounds were identified as ethyl gallate (1, IC50 832 μM) and gallic acid (2, IC50 969 μM); both displayed competitive inhibition of α–glucosidases and isoorientin (3, IC50 201 μM), which displayed uncompetitive inhibition of lipase. These data could be useful in the development of a novel phytopharmaceutical drug.

scholarly journals Design, Synthesis and Biological Screening of Novel 1,5-Diphenyl-3-(4-(trifluoromethyl)phenyl)-2-pyrazoline Derivatives

2020 ◽  
Vol 67 (4) ◽  
pp. 1139-1147
Author(s):  
Fatih Tok ◽  
Bedia Koçyiğit-Kaymakçıoğlu
Keyword(s):  
Inflammatory Activity ◽  
Antidiabetic Activity ◽  
Spectroscopic Methods ◽  
Design Synthesis ◽  
Reference Drug ◽  
Ic50 Values ◽  
Adme Properties ◽  
Anti Inflammatory ◽  
In Vitro Antioxidant Activity

1-Phenyl-5-substituted-3-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-pyrazole derivatives were synthesized from chalcone derivatives. The structures of compounds were characterized by IR, 1H NMR spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro antioxidant activity using DPPH and ABTS methods, anti-inflammatory activity using lipoxygenase inhibitory method and antidiabetic activity using the α-glucosidase inhibitory method. Especially, pyrazoline derivatives exhibited stronger anti-inflammatory activity than the reference drug indomethacin (IC50: 50.45 μM) and their IC50 values were in the range of 0.68 and 4.45 μM. In addition, the ADME properties of all chalcone and pyrazoline derivatives were calculated by Lipinski’s and Veber’s rules.

Feruloyl Sucrose Esters: Potent and Selective Inhibitors of α-glucosidase and α-amylase.

2021 ◽  
Vol 28 ◽  
Author(s):  
Surabhi Devaraj ◽  
Yew Mun Yip ◽  
Parthasarathi Panda ◽  
Li Lin Ong ◽  
Pooi Wen Kathy Wong ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Blood Glucose ◽  
Side Effects ◽  
Docking Studies ◽  
Sucrose Esters ◽  
Molecular Docking Studies ◽  
Gastrointestinal Side Effects ◽  
Lead Candidate

Introduction: Feruloyl Sucrose Esters (FSEs) are a class of Phenylpropanoid Sucrose Esters (PSEs) widely distributed in plants. They were investigated as potential selective Alpha Glucosidase Inhibitors (AGIs) to eliminate the side effects associated with the current commercial AGIs. The latter effectively lowers blood glucose levels in diabetic patients but causes severe gastrointestinal side effects. Methods: Systematic structure-activity relationship (SAR) studies using in silico, in vitro and in vivo experiments were used to accomplish this aim. FSEs were evaluated for their in vitro inhibition of starch and oligosaccharide digesting enzymes α-glucosidase and α-amylase followed by in silico docking studies to identify the binding modes. A lead candidate, FSE 12 was investigated in an STZ mouse model. Results: All active FSEs showed desired higher % inhibition of α-glucosidase and desired lower inhibition of α-amylase in comparison to AGI gold standard acarbose. This suggests a greater selectivity of the FSEs towards α-glucosidase than α-amylase, which is proposed to eliminate the gastrointestinal side effects. From the in vitro studies, the position and number of the feruloyl substituents on the sucrose core, the aromatic ‘OH’ group, and the diisopropylidene bridges were key determinants of the % inhibition of α-glucosidase and α-amylase. In particular, the diisopropylidene bridges are critical for achieving inhibition selectivity. Molecular docking studies of the FSEs corroborates the in vitro results. The molecular docking studies further reveal that the presence of free aromatic ‘OH’ groups and the substitution at position 3 on the sucrose core are critical for the inhibition of both the enzymes. From the in vitro and molecular docking studies, FSE 12 was selected as a lead candidate for validation in vivo. The oral co-administration of FSE 12 with starch abrogated the increase in post-prandial glucose and significantly reduced blood glucose excursion in STZ-treated mice compared to control (starch only) mice. Conclusion: Our studies reveal the potential of FSEs as selective AGIs for the treatment of diabetes, with a hypothetical reduction of side effects associated with commercial AGIs.

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