scholarly journals Preliminary in vitro study of anti-oxidant activity and anti-diabetic potential of plant extracts from 4 herbal substances not traditionally used for treatment of diabetes mellitus

Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 755-762
Author(s):  
Dora Trifonova ◽  
Anna Gavrilova ◽  
Galina Dyakova ◽  
Genadi Gavrilov ◽  
Maya Yotova ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Biologically Active ◽  
Total Phenolic ◽  
Water Extracts ◽  
Sambucus Ebulus ◽  
Anti Oxidant ◽  
Treatment Of Diabetes

The focus of the presented study is the in vitro anti-oxidant activity and anti-diabetic potential of water extracts from the following four herbal substances, not traditionally used for treatment of diabetes mellitus – leaves of Sambucus ebulus L. and Prunus mahaleb L., and flowering stems of Cichorium intybus L. and Satureja kitaibelii Wierzb. ex Heuff. The water extracts are obtained through ultrasonication. The extract of S. kitaibelii stands out due to its highest values in all studied indicators – total phenolic content, scavenging potential (DPPH, ABTS) and α-glucosidase inhibitory activity which was six times higher than acarbose. The extract of C. intybus also showed significant α-glucosidase inhibitory activity compared to acarbose. The flowering stems of both species are promising sources of biologically active substances for blood sugar control in diabetes mellitus.

scholarly journals Machine Learning and In Vitro Chemical Screening of Potential α-Amylase and α-Glucosidase Inhibitors from Thai Indigenous Plants

Nutrients ◽  
2022 ◽  
Vol 14 (2) ◽  
pp. 267
Author(s):  
Tarapong Srisongkram ◽  
Sasisom Waithong ◽  
Thaweesak Thitimetharoch ◽  
Natthida Weerapreeyakul
Keyword(s):  
Diabetes Mellitus ◽  
Machine Learning ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Ethanolic Extract ◽  
Accuracy Score ◽  
Indigenous Plants ◽  
Predisposing Factor ◽  
Chemical Screening

Diabetes mellitus is a major predisposing factor for cardiovascular disease and mortality. α-Amylase and α-glucosidase enzymes are the rate-limiting steps for carbohydrate digestion. The inhibition of these two enzymes is clinically used for the treatment of diabetes mellitus. Here, in vitro study and machine learning models were employed for the chemical screening of inhibiting the activity of 31 plant samples on α-amylase and α-glucosidase enzymes. The results showed that the ethanolic twig extract of Pinus kesiya had the highest inhibitory activity against the α-amylase enzyme. The respective ethanolic extract of Croton oblongifolius stem, Parinari anamense twig, and Polyalthia evecta leaf showed high inhibitory activity against the α-glucosidase enzyme. The classification analysis revealed that the α-glucosidase inhibitory activity of Thai indigenous plants was more predictive based on phytochemical constituents, compared with the α-amylase inhibitory activity (1.00 versus 0.97 accuracy score). The correlation loading plot revealed that flavonoids and alkaloids contributed to the α-amylase inhibitory activity, while flavonoids, tannins, and reducing sugars contributed to the α-glucosidase inhibitory activity. In conclusion, the ethanolic extracts of P. kesiya, C. oblongifolius, P. anamense, and P. evecta have the potential for further chemical characterization and the development of anti-diabetic recipes.

scholarly journals Alpha Amylase, Alpha Glucosidase Inhibition and Profiling of Volatile Compounds of Biologically Active Extracts from Momordica cymbalaria (Hook, Fenzl) Skin and Seeds

2019 ◽  
Vol 8 (1) ◽  
pp. 67-73
Author(s):  
E. Abbirami . ◽  
L. Dinesh Kumar . ◽  
R. Guna .
Keyword(s):  
Vaccenic Acid ◽  
Ethanol Extract ◽  
Biologically Active ◽  
Bioactive Metabolites ◽  
Total Phenolic ◽  
Fruit Skin ◽  
Ic50 Values ◽  
Anti Oxidant ◽  
Alpha Glucosidase

Momordica cymbalaria (Hook, Fenzl) has been used in traditional medicine for diabetes in India. This study was designed to examine, total phenolic, total flavonoid contents and in vitro anti-oxidant activity by using seven different types of solvent extracts. The biologically active extracts, ethanol extract of fruit skin (EESK) and methanol extract of seed (MESE) were evaluated for in vitro anti-diabetic activity followed by detection of bioactive metabolites by GC-MS analysis. EESK and MESE exhibited IC50 values of 185.1 μg/ml against α – amylase and 224.4 μg/ml against α – glucosidase, respectively. GC-MS profiling of skin and seed portion of the vegetable revealed the presence of 40 compounds from EESK and 29 compounds from MESE. Thus, this study reveals that EESK and MESE exhibited in vitro anti-diabetic activity and GC-MC profiling confirms the presence of anti-diabetic phytocompounds such as L-Cysteine and cis- Vaccenic acid.

scholarly journals Synthesis and In Vitro Study of Antiviral Activity of Glycyrrhizin Nicotinate Derivatives against HIV-1 Pseudoviruses and SARS-CoV-2 Viruses

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 295
Author(s):  
Vladislav V. Fomenko ◽  
Nadezhda B. Rudometova ◽  
Olga I. Yarovaya ◽  
Artem D. Rogachev ◽  
Anastasia A. Fando ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Broad Spectrum ◽  
Inhibitory Activity ◽  
Antiviral Agents ◽  
In Vitro Study ◽  
Biologically Active ◽  
Component Mixture ◽  
Control Drug ◽  
Hiv 1

When developing drugs against SARS-CoV-2, it is important to consider the characteristics of patients with different co-morbidities. People infected with HIV-1 are a particularly vulnerable group, as they may be at a higher risk than the general population of contracting COVID-19 with clinical complications. For such patients, drugs with a broad spectrum of antiviral activity are of paramount importance. Glycyrrhizinic acid (Glyc) and its derivatives are promising biologically active compounds for the development of such broad-spectrum antiviral agents. In this work, derivatives of Glyc obtained by acylation with nicotinic acid were investigated. The resulting preparation, Glycyvir, is a multi-component mixture containing mainly mono-, di-, tri- and tetranicotinates. The composition of Glycyvir was characterized by HPLC-MS/MS and its toxicity assessed in cell culture. Antiviral activity against three strains of SARS-CoV-2 was tested in vitro on Vero E6 cells by MTT assay. Glycyvir was shown to inhibit SARS-CoV-2 replication in vitro (IC502–8 μM) with an antiviral activity comparable to the control drug Remdesivir. In addition, Glycyvir exhibited marked inhibitory activity against HIV pseudoviruses of subtypes B, A6 and the recombinant form CRF63_02A (IC50 range 3.9–27.5 µM). The time-dependence of Glycyvir inhibitory activity on HIV pseudovirus infection of TZM-bl cells suggested that the compound interfered with virus entry into the target cell. Glycyvir is a promising candidate as an agent with low toxicity and a broad spectrum of antiviral action.

scholarly journals WATER EXTRACTS FROM THE COMBINATION OF COCCINIA GRANDIS (L.) VOIGT LEAVES AND AVERRHOA BILIMBI L. FRUITS WITH ANTIDIABETIC PROPERTIES: AN IN VITRO STUDY

2020 ◽  
pp. 24-28
Author(s):  
MADE WISNU ADHI PUTRA I ◽  
OLYN TIEN ATE ◽  
GUSTI AYU WITA KUSUMAWATI I ◽  
WAYAN NURSINI NI
Keyword(s):  
Phenolic Content ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
In Vitro Study ◽  
Total Phenolic ◽  
Flavonoid Content ◽  
Water Extracts ◽  
Coccinia Grandis ◽  
Gallic Acid Equivalent

Objective: The combination of two or more plants in a product can improve the nature of the activity of the compounds contained and reduce toxicity. This study was aimed to make water extracts from the combination of Coccinia grandis (L.) CG Voigt and Averrhoa bilimbi L. (AB) with antidiabetic properties. Methods: The water extracts were made by decocting the combination of powdered CG Voigt leaves and AB fruits at various mass ratios (1:0, 1:3, 1:1, 3:1, and 0:1) and various amounts of powdered samples (1–5 g). The process was done in 100 ml of boiling water for 5 min. Results: The results showed that the highest total flavonoid content and total phenolic content of 135.1±0.18 mg quercetin equivalent micrograms d.m. and 48.5±3.09 mg gallic acid equivalent/g d.m., respectively, were found in the sample with a combination ratio of 1:3 (1 g). The antioxidant activity test using the 2,2-diphenyl-1-picrylhydrazyl method showed that the sample with a combination ratio of 3:1 had the lowest value of IC50 (4.447±0.446 mg/ml), which indicated the strongest radical scavenging activity, while the highest inhibition of α-amylase activity in the sample with a combination ratio of 1:1 amounted to 1.086±0.264 mg/ml. Conclusion: In general, all combinations of CG Voigt leaves and AB fruits had the potential as antidiabetic health beverages.

scholarly journals IN VITRO ANTIDIABETIC EFFECTS OF FERULA ASSA-FOETIDA EXTRACTS THROUGH DIPEPTIDYL PEPTIDASE IV AND α-GLUCOSIDASE INHIBITORY ACTIVITY

2017 ◽  
Vol 10 (5) ◽  
pp. 357 ◽  
Author(s):  
Adel Yarizade ◽  
Hsan Hasani Kumle ◽  
Ali Niazi
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
Postprandial Glucose ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Dpp Iv ◽  
Glucosidase Inhibitors ◽  
Treatment Of Diabetes ◽  
Ethanol Ethanol

Objective: Diabetes mellitus (DM) causes hyperglycemia, which is one of the most common diseases in the world. One of the strategies for the treatment of diabetes is maintaining postprandial glucose level through inhibition of dipeptidyl peptidase IV (DPP-IV) and α-glucosidase enzymes. The aim of this study was to determine in vitro antidiabetic potential of Ferula assa-foetida via DPP-IV and α-glucosidase inhibitory activities.Methods: F. assa-foetida seeds were extracted in methanol, ethanol, ethanol-methanol, and water. Inhibitory activity on DPP-IV and α-glucosidase wasperformed in vitro and measured spectrophotometrically at λ=405 nm.Results: The result showed that the F. assa-foetida seed extract is effective against both enzymes. All fractions had DPP-IV inhibitory activity, but the ethanolic fraction had the highest inhibitory activity on DPP-IV enzyme and significantly decreased DPP-IV activity (24.5%). With respect to α-glucosidase inhibitory activity, the aqueous extract has the highest inhibitory activity (28%).Conclusion: According to the results of this study, F. assa-foetida contains DPP-IV and α-glucosidase inhibitors and could be a potential source for the discovery of active constituents as α-glucosidase and DPP-IV inhibitors to treat Type 2 DM.Keywords: Diabetes mellitus, Herbal medicine, Dipeptidyl peptidase IV, α-glucosidase.

scholarly journals Inhibition of Haemoglobin Glycosylation, Glucose Uptake and In Vitro Antidiabetic Activities of Solvent Fractions from Daucus carota Seed

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Habibu Tijjani ◽  
Sadiq Adamu Imam
Keyword(s):  
Diabetes Mellitus ◽  
Glucose Uptake ◽  
Daucus Carota ◽  
Inhibitory Activity ◽  
Seed Extract ◽  
Insulin Deficiency ◽  
Inhibitory Effects ◽  
Organ Systems ◽  
Treatment Of Diabetes

Abstract Diabetes mellitus (DM) is a metabolic disorder which result from either absolute or relative insulin deficiency and may lead to dysfunction in some organ systems. Pancreatic α- glucosidase and α- amylase inhibition are an effective strategy to decrease levels of postprandial hyperglycemia through starch control breakdown. The aim of the study is to assess the in vitro antidiabetic activities of fractions from Daucus carota seed extract, a plant used traditionally for the treatment of diabetes mellitus. The aqueous extract (AQE) of Daucus carota seed was partitioned in ethyl acetate (EAE), n – hexane (HEX) and diethyl ether (DEE) to obtain the various fractions. The AQE and EAE expressed significant α – amylase inhibitory activity with IC50 values of 637.0±18.6 μg/mL and 603.0±25.8 μg/mL respectively. AQE, EAE, HEX and DEE expressed α – glucosidase inhibitory activity with IC50 value of 135.85±1.21, 147.59±0.57, 132.64±1.17, and 143.56±0.49 μg/mL respective compared with acarbose (ACA) with 5.42±0.20 μg/mL. Furthermore, DEE fraction expressed inhibitory effects on % glucose uptake in yeast cell comparable with metronidazole. All Daucus carota fractions expressed various inhibitory effects on haemoglobin glycosylation at a concentration of 200 – 1000 μg/mL. The results show that fractions from the aqueous seed extract of Daucus carota possess in vitro antidiabetic potentials with EAE and HEX fractions having most promising inhibitory activities against α-amylase and α-glucosidase respectively.

scholarly journals Potential Anticancer Lipoxygenase Inhibitors from the Red Sea-Derived Brown Algae Sargassum cinereum: An In-Silico-Supported In-Vitro Study

Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 416
Author(s):  
Sami I. Alzarea ◽  
Abeer H. Elmaidomy ◽  
Hani Saber ◽  
Arafa Musa ◽  
Mohammad M. Al-Sanea ◽  
...  
Keyword(s):  
Red Sea ◽  
Antiproliferative Activity ◽  
Inhibitory Activity ◽  
Brown Algae ◽  
In Silico ◽  
Active Sites ◽  
In Vitro Study ◽  
Lipoxygenase Inhibitors ◽  
Phytochemical Investigation

LC-MS-assisted metabolomic profiling of the Red Sea-derived brown algae Sargassum cinereum “Sargassaceae” dereplicated eleven compounds 1–11. Further phytochemical investigation afforded two new aryl cresol 12–13, along with eight known compounds 14–21. Both new metabolites, along with 19, showed moderate in vitro antiproliferative activity against HepG2, MCF-7, and Caco-2. Pharmacophore-based virtual screening suggested both 5-LOX and 15-LOX as the most probable target linked to their observed antiproliferative activity. The in vitro enzyme assays revealed 12 and 13 were able to inhibit 5-LOX more preferentially than 15-LOX, while 19 showed a convergent inhibitory activity toward both enzymes. Further in-depth in silico investigation revealed the molecular interactions inside both enzymes’ active sites and explained the varying inhibitory activity for 12 and 13 toward 5-LOX and 15-LOX.

Novel Anti-Cancer, Anti-Bacterial Coatings for Biomaterial Applications: Selenium Nanoclusters

2009 ◽  
Vol 1209 ◽  
Author(s):  
Phong Anh Tran ◽  
Erik Taylor ◽  
Love Sarin ◽  
Robert H. Hurt ◽  
Thomas J Webster
Keyword(s):  
Bone Cells ◽  
Tumor Resection ◽  
Active Agent ◽  
In Vitro Study ◽  
Biologically Active ◽  
Elemental Selenium ◽  
Orthopedic Implant ◽  
Functional Coating ◽  
Anti Cancer

AbstractTwo common problems with implantation after cancerous tumor resection are cancer recurrence and bacteria infection at the implant site. Tumor resection surgery sometimes can not remove all the cancerous cells, thus, cancer can return after implantation. In addition, bacteria infection is one of the leading causes of implant failure. Therefore, it is desirable to have anti-cancer and anti-bacterial molecules which both rapidly (for anti-infection purposes) and continuously (for anti-cancer purposes) are available at the implant site following implantation. Therefore, the objective of the present in vitro study was to create a multi-functional coating for anti-cancer and anti-bacterial orthopedic implant applications. Elemental selenium was chosen as the biologically active agent in this effort because of its known chemopreventive and anti-bacterial properties. To achieve that objective, titanium (Ti), a conventional orthopedic implant material was coated with selenium (Se) nanoclusters. Different coating densities were achieved by varying Se concentration in the reaction mixture. Titanium substrates coated with Se nanoclusters were shown to enhance healthy osteoblast (bone-forming cell) and inhibit cancerous osteoblast proliferation in co-culture experiments. Functions of S. epidermidis (one of the leading bacteria that infect implants) were inhibited on Ti coated with Se-nanoclusters compared to uncoated materials. Thus, this study provided for the first time a coating material (selenium nanoclusters) to the biomaterials’ community to promote healthy bone cells’ functions, inhibit cancer growth and prevent bacteria infection.

scholarly journals In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Colorimetric Assay ◽  
Hypotensive Effect ◽  
Ace Inhibition ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Total Phenolic ◽  
Before And After

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

scholarly journals In Vitro α-Amylase and Protein Glycation Inhibitory Activity of the Aqueous Extract of Flueggea leucopyrus Willd

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Vishmi Sachindra Thrikawala ◽  
Srianthie A. Deraniyagala ◽  
Chamira Dilanka Fernando ◽  
Dinusha Nishani Udukala
Keyword(s):  
Aqueous Extract ◽  
Diabetic Complications ◽  
Inhibitory Activity ◽  
Radical Scavenging ◽  
Vital Role ◽  
Protein Glycation ◽  
Total Phenolic ◽  
Chronic Hyperglycemia ◽  
Body Tissues

There is much interest in plant-based medicine with antidiabetic and antiglycation properties. Chronic hyperglycemia plays a vital role in the development of long-term diabetic complications by inducing protein glycation and the gradual formation of advanced glycation end products (AGEs) in various body tissues. The main objectives of this study were to investigate the aqueous extract of the whole plant of Flueggea leucopyrus Willd (FLAE), a medicinal plant used in traditional medicine in Sri Lanka for its in vitro α-amylase inhibitory activity and its inhibitory potential on the formation of AGEs. α-Amylase inhibitory activity determined by 3,5-dinitrosalicylic acid method revealed that FLAE possesses 29%–91% inhibitory activity at a concentration range of 2.5–400 μg/mL, respectively. Nonenzymatic protein glycation inhibitory capacity assessed by bovine serum albumin-fructose fluorescence spectrometric assay showed that FLAE at 15.6–250.0 μg/mL inhibited AGE formation by 0.9%–98%, respectively. Radical scavenging ability of FLAE using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and total phenolic and flavonoid contents of FLAE were also determined. This study shows that Flueggea leucopyrus Willd not only inhibits α-amylase enzyme, which is known to break starch to glucose, but also inhibits the formation of AGEs, which occur due to chronic hyperglycemia that leads to the onset of diabetic complications.

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