In vitro Antidiabetic, anti-obesity and antioxidant proprities of Rosemary extracts

Diabetes mellitus is a serious health problem worldwide that has adverse and long-lasting consequences for individuals, families, and communities. Hence, this study sought to investigate the inhibitory potential of rosemary extracts on key-enzymes related to diabetes such as α-amylase and pancreatic lipase activities, as well as to assess their antioxidant properties in vitro. The IC50 values of Rosemary essential oil, ethyl acetate and methanolic extracts against α-amylase were 28.36, 34.11 and 30.39 µg/mL respectively, and those against pancreatic lipase were 32.25, 36.64 and 34.07 µg/mL, suggesting strong anti-diabetic and anti-obesity effects of Rosemary. The methanolic extract was found to be the highest in levels of phenolic (282.98 µgGAE/mg extract) and flavonoids (161.05 µg QE /mg extract) contents as well as in the antioxidant activity (IC50 = 15.82 µg/mL) as compared to other extracts ethyl acetate (IC50 = 32.23 µg/mL) and essential oil (IC50 = 96.12 µg/mL).Antioxidant efficacy of Rosemary extracts has been estimated in the stabilization of sunflower oil (SFO) at three different concentrations, i.e. 200 (SFO-200), 500 (SFO-500) and 1000 ppm (SFO-1000). Results showed the highest efficiency of SFO-1000.The results obtained in this study demonstrated for the first time that Rosemary is a potent source of natural inhibitors of α-amylase and pancreatic lipase with powerful antioxidants proprieties that might be used in the food stabilization and the prevention of diabetes and obesity complications as a complementary pharmacological drug.

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Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽

10.3390/molecules26061694 ◽

2021 ◽

Vol 26 (6) ◽

pp. 1694

Author(s):

Kamel Arraki ◽

Perle Totoson ◽

Alain Decendit ◽

Andy Zedet ◽

Justine Maroilley ◽

...

Keyword(s):

Inhibitory Activity ◽

Methanolic Extract ◽

Significant Inhibition ◽

Isolation And Identification ◽

Vasorelaxant Effect ◽

Methanolic Extracts ◽

Phytochemical Investigation ◽

Ic50 Values ◽

First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

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CrudeAloe veraGel Shows Antioxidant Propensities and Inhibits Pancreatic Lipase and Glucose MovementIn Vitro

Advances in Pharmacological Sciences ◽

10.1155/2016/3720850 ◽

2016 ◽

Vol 2016 ◽

pp. 1-9 ◽

Cited By ~ 5

Author(s):

Urmeela Taukoorah ◽

M. Fawzi Mahomoodally

Keyword(s):

Pancreatic Lipase ◽

Antioxidant Properties ◽

Aloe Vera ◽

Reducing Power ◽

Kinetic Studies ◽

Total Phenolic ◽

Anthocyanin Content ◽

Maximal Velocity ◽

Inhibitory Potential

Aloe veragel (AVG) is traditionally used in the management of diabetes, obesity, and infectious diseases. The present study aimed to investigate the inhibitory potential of AVG againstα-amylase,α-glucosidase, and pancreatic lipase activityin vitro. Enzyme kinetic studies using Michaelis-Menten (Km) and Lineweaver-Burk equations were used to establish the type of inhibition. The antioxidant capacity of AVG was evaluated for its ferric reducing power, 2-diphenyl-2-picrylhydrazyl hydrate scavenging ability, nitric oxide scavenging power, and xanthine oxidase inhibitory activity. The glucose entrapment ability, antimicrobial activity, and total phenolic, flavonoid, tannin, and anthocyanin content were also determined. AVG showed a significantly higher percentage inhibition (85.56±0.91) of pancreatic lipase compared to Orlistat. AVG was found to increase the Michaelis-Menten constant and decreased the maximal velocity (Vmax) of lipase, indicating mixed inhibition. AVG considerably inhibits glucose movement across dialysis tubes and was comparable to Arabic gum. AVG was ineffective against the tested microorganisms. Total phenolic and flavonoid contents were66.06±1.14 (GAE)/mg and60.95±0.97 (RE)/mg, respectively. AVG also showed interesting antioxidant properties. The biological activity observed in this study tends to validate some of the traditional claims of AVG as a functional food.

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Chemical profiling, in vitro antioxidant and antidiabetic assessment of flavonoids from the ethanol extract of Hermannia geniculata root

Sokoto Journal of Veterinary Sciences ◽

10.4314/sokjvs.v19i1.1 ◽

2021 ◽

Vol 19 (1) ◽

pp. 1-13

Author(s):

L.A. Adeniran ◽

C.P. Palanisamy ◽

A.O.T. Ashafa

Keyword(s):

Competitive Inhibition ◽

Antioxidant Properties ◽

Reactive Oxygen ◽

Ethanol Extract ◽

Kinetic Studies ◽

Retention Factor ◽

Chemical Profiling ◽

Ic50 Values ◽

Inhibitory Potential

Determination of the in vitro antioxidant and the inhibitory potential of flavonoids from Hermannia geniculata (FHG) roots on diabetes-linked enzymes was carried out. The chemical profiling of FHG roots extract was investigated using High Pressure Thin Layer Chromatography (HPTLC) fingerprint analysis. The reactive oxygen scavenging potential of the extract was analyzed. Starch solution (1%) was reacted with different concentrations of FHG extract to determine the α-amylase inhibitory potential of the extract while α- glucosidase inhibition assay was carried out through incubation of different concentrations of the extract followed by addition of p-ntrophenyl-α-Dglucopyranoside solution. HPTLC results indicated the presence of flavonoids/ phenolcarboxylic acid, and Kaemferol (Rf 0.80) were detected in the extract with retention factor Rf. ranging from 0.08 to 0.95. FHG extract showed commendable antioxidant properties with IC50 values (3.07± 0.12, 2.13± 0.67) µg/mL for 1, 1-diphenyl-2- picrylhydrazyl (DPPH) and 2, 2-azino-bis (3- ethylbenzothiazoline-6-sulphonic) acid (ABTS) radicals which were lower and significantly different (p<0.05) compared to standard silymarin with IC50: (3.55± 0.10, 2.77± 0.75) µg/mL for DPPH and ABTS respectively. The results indicated mild inhibition of α-amylase with IC50: (5.55± 0.37) µg/mL which was higher and significantly different (p<0.05) from acarbose with IC50: (3.81± 0.29) µg/mL. Moreover, the extract showed 73% inhibition of α-glucosidase. Kinetic studies of FHG extract revealed competitive and mixed non-competitive inhibition of α- amylase and α-glucosidase respectively. This study indicated FHG capabilities of scavenging reactive oxygen species and reducing hydrolysis of starch responsible for post-prandial hyperglyceamia seen in type 2 diabetes mellitus. Keywords: Antidiabetic, Antioxidant, Flavonoids, Hermannia geniculate, HPTLC

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Pancreatic Lipase Inhibitory Alkaloids of Murraya koenigii Leaves

Natural Product Communications ◽

10.1177/1934578x0900400814 ◽

2009 ◽

Vol 4 (8) ◽

pp. 1934578X0900400 ◽

Cited By ~ 10

Author(s):

Rahul Birari ◽

Somendu Kumar Roy ◽

Anubha Singh ◽

Kamlesh Kumar Bhutani

Keyword(s):

Pancreatic Lipase ◽

Inhibitory Activity ◽

Murraya Koenigii ◽

Etoac Extract ◽

Inhibitory Potential ◽

Pancreatic Lipase Inhibitors ◽

First Time ◽

Carbazole Alkaloids

In the continuing search for newer pancreatic lipase inhibitors from plants, a total of 63 extracts from 21 different plants were screened to study their pancreatic lipase (PL) inhibitory activity in vitro. All three extracts (DCM, EtOAc and MeOH) of Murraya koenigii (L.) Spreng leaves (Rutaceae) exhibited antilipase activity greater than 80%. Further, bioactivity guided fractionation of the EtOAc extract led to the isolation of four alkaloids, namely mahanimbin, koenimbin, koenigicine and clausazoline-K, with IC50 values of 17.9 μM, 168.6 μM, 428.6 μM and ≤500 μM, respectively. This study reports for the first time the PL inhibitory potential of carbazole alkaloids from plants.

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Phytochemical and Biological Profile of Moricandia arvensis (L.) DC.: An Inhibitor of Pancreatic Lipase

Molecules ◽

10.3390/molecules23112829 ◽

2018 ◽

Vol 23 (11) ◽

pp. 2829 ◽

Cited By ~ 10

Author(s):

Mariangela Marrelli ◽

Federica Morrone ◽

Maria Argentieri ◽

Lucia Gambacorta ◽

Filomena Conforti ◽

...

Keyword(s):

Ethyl Acetate ◽

Pancreatic Lipase ◽

Inhibitory Activity ◽

Methanolic Extract ◽

Dietary Lipids ◽

Lipid Absorption ◽

Flavonoid Glycosides ◽

Moricandia Arvensis ◽

Ic50 Values

Pancreatic lipase, a key enzyme for lipid absorption, is one of the most important targets for the treatment of obesity, while natural compounds have recently attracted much interest as potential inhibitors of this enzyme. Here, in an attempt to find new effective agents, the methanolic extract from Moricandia arvensis (L.) DC. and its sub-extracts were investigated for their potential inhibitory activity. The ability to inhibit pancreatic lipase was verified through the in vitro evaluation of the prevention of p-nitrophenyl caprylate hydrolysis. The antioxidant activity was also verified by means of DPPH and β-carotene bleaching tests. Compositional profiling revealed that flavonoid glycosides were the main specialized metabolites present in the methanolic extract from the aerial parts of the plant with kaempferol and quercetin representing the two O-glycosylated aglycones. Kaempferol-3-O-β-(2″-O-glucosyl)-rutinoside and kaempferol-3-O-a-arabinosyl-7-O-rhamnoside were the most abundant flavonols. The crude methanolic extract and the dichloromethane and ethyl acetate sub-extracts showed a strong lipase inhibitory activity, with IC50 values of 2.06 ± 0.02, 1.52 ± 0.02 and 1.31 ± 0.02 mg/mL, respectively. The best capacity to scavenge DPPH radical was detected for the ethyl acetate sub-extract (IC50 = 171.9 ± 1.0 µg/mL), which was also effective in protecting linoleic acid from peroxidation (IC50 = 35.69 ± 2.30 µg/mL). Obtained results support the hypothesis that M. arvensis can be a source of bioactive phytochemicals for the pharmacological inhibition of dietary lipids absorption.

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Helichrysum italicum (Roth) G. Don subsp. italicum from Herzegovina

Croatica Chemica Acta ◽

10.5562/cca3475 ◽

2019 ◽

Vol 92 (1) ◽

pp. 69-77

Author(s):

Stanislava Talić ◽

Ilijana Odak ◽

Anita Martinović Bevanda ◽

Nikolina Crnjac ◽

Mate Paštar

Keyword(s):

Antioxidant Activity ◽

Chemical Composition ◽

Essential Oil ◽

Inhibition Activity ◽

Complex Chemical ◽

Methanolic Extracts ◽

Complex Chemical Composition ◽

Ic50 Values ◽

Vegetative Cycle ◽

Inhibitory Potential

The chemical composition of essential oils isolated from immortelle (Helicrysum italicum subsp. italicum) collected in Herzegovina during five different periods, was investigated by GC/MS analysis. The main compounds were a-pinene (15.7 %) and γ-curcumene (12.8 %), followed by 4,6,9-trimethyldec-8-en-3,5-dione (8.7 %), neryl acetate (6.9 %), limonene (6.4 %) and β-selinene (5.3 %). In total, 69 components were identified whose share changed over the vegetative cycle. Antioxidant activity of methanolic extracts of immortelle were determined according to DPPH (IC50 = 23–34 μg/mL) and FRAP (29 μg/mL is equivalent to 1.1‒2.2 mM Fe2+) methods. Acetylcholinesterase inhibitory potential, investigated by modified Ellman’s assay and determined as IC50 values, were 340–440 μg/mL for methanol extracts and 135 μg/mL for essential oil. Metanolic extracts showed strong antioxidant activity and potential to inhibit AChE. Essential oil possesses complex chemical composition, inhibition activity of AChE and weak antioxidant capacity.

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Antioxidant, Anti-Inflammatory, and Inhibition of Acetylcholinesterase Potentials of Cassia timoriensis DC. Flowers

Molecules ◽

10.3390/molecules26092594 ◽

2021 ◽

Vol 26 (9) ◽

pp. 2594

Author(s):

Maram B. Alhawarri ◽

Roza Dianita ◽

Khairul Niza Abd Razak ◽

Suriani Mohamad ◽

Toshihiko Nogawa ◽

...

Keyword(s):

Ethyl Acetate ◽

Radical Scavenging ◽

Acetylcholinesterase Activity ◽

Phytochemical Analysis ◽

Methanol Extracts ◽

Anti Inflammatory ◽

Inhibitory Potential ◽

Radical Scavenging Ability ◽

First Time

Despite being widely used traditionally as a general tonic, especially in South East Asia, scientific research on Cassia timoriensis, remains scarce. In this study, the aim was to evaluate the in vitro activities for acetylcholinesterase (AChE) inhibitory potential, radical scavenging ability, and the anti-inflammatory properties of different extracts of C. timoriensis flowers using Ellman’s assay, a DPPH assay, and an albumin denaturation assay, respectively. With the exception of the acetylcholinesterase activity, to the best of our knowledge, these activities were reported for the first time for C. timoriensis flowers. The phytochemical analysis confirmed the existence of tannins, flavonoids, saponins, terpenoids, and steroids in the C. timoriensis flower extracts. The ethyl acetate extract possessed the highest phenolic and flavonoid contents (527.43 ± 5.83 mg GAE/g DW and 851.83 ± 10.08 mg QE/g DW, respectively) as compared to the other extracts. In addition, the ethyl acetate and methanol extracts exhibited the highest antioxidant (IC50 20.12 ± 0.12 and 34.48 ± 0.07 µg/mL, respectively), anti-inflammatory (92.50 ± 1.38 and 92.22 ± 1.09, respectively), and anti-AChE (IC50 6.91 ± 0.38 and 6.40 ± 0.27 µg/mL, respectively) activities. These results suggest that ethyl acetate and methanol extracts may contain bioactive compounds that can control neurodegenerative disorders, including Alzheimer’s disease, through high antioxidant, anti-inflammatory, and anti-AChE activities.

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Chemical composition and biological activities of the essential oil from the leaves of Vaccinium myrtillus L.

Bangladesh Journal of Botany ◽

10.3329/bjb.v49i1.49098 ◽

2020 ◽

Vol 49 (1) ◽

pp. 91-96

Author(s):

Omer Elkiran ◽

Cumhur Avşar

Keyword(s):

Antioxidant Activity ◽

Chemical Composition ◽

Essential Oil ◽

Antioxidant Activities ◽

Biological Activities ◽

Antioxidant Properties ◽

Antimicrobial Activities ◽

Vaccinium Myrtillus ◽

First Time

The chemical composition, antimicrobial and antioxidant properties of the essential oil (EO), obtained from the leaves of Vaccinium myrtillus naturally grown in the northernmost of Turkey were determined by GC and GC-MS and chemical differences were discussed with the help of chemotaxonomy. The leaves of the plant samples were hydro-distilled to produce oil in the yields of 1%. Nineteen components were identified representing 96.4% of the oil. The main compounds in the EO of V. myrtillus were; 1,8-cineole (38.6%), α- pinene (21%), linalool (19.5%), α-terpineol (5.8%). The EO extract was screened for their antimicrobial activities against the 9 bacteria and 3 yeast species by using disc-diffusion and MIC procedure. The EO extract displayed more effective against all the tested bacteria (especially, S. aureus ATCC 6538 and MRSA) and yeast (only C. krusei). The MIC values of sample against tested microorganisms were found to be in the range of 320 to ≥1280 μg/ml. The most effective MIC values were observed against the S. aureus and MRSA (320 μg/ml). In vitro the antioxidant activity based on the 1,1-diphenly-2-picrylhydrazyl (DPPH) free radical was evaluated for the EO extract, and it was found that the extract had good antioxidant activity in the range of the IC50 = 583.4 ±11 μg ml. Antibacterial and antioxidant activities of the EO from the leaves of V. myrtillus has been reported for the first time.

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Antimutagenic, Antiproliferative and Antioxidant Properties of Sea Grape Leaf Extract Fractions (Coccoloba uvifera L.)

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621999210104201242 ◽

2021 ◽

Vol 21 ◽

Author(s):

Jorge A. Ramos-Hernández ◽

Montserrat Calderón-Santoyo ◽

Armando Burgos-Hernández ◽

Joel S. García- Romo ◽

Arturo Navarro-Ocaña ◽

...

Keyword(s):

Antioxidant Properties ◽

In Vitro Tests ◽

Antimutagenic Activity ◽

Hexane Extraction ◽

Biological Potential ◽

Hct 116 ◽

Pharmaceutical Industries ◽

Grape Leaf ◽

First Time

Background: Cancer is a disease characterized by the invasion and uncontrolled growth of cells. One of the best ways to minimize the harmful effects of mutagens is through the use of natural antimutagens. In this regard, the search for new antimutagens that act in the chemoprevention could represent a promising field in this area. Objective: In this study biological potential of 11 fractions from Coccoloba uvifera L. leaf hexane extract was evaluated by several in vitro tests. Methods: Leaves were lyophilized and hexane extraction was performed. The extract was fractionated by column chromatography with hexane, ethyl acetate, and methanol. The antimutagenic (Ames test), antiproliferative (MTT test), and antioxidant capacity (DPPH, ABTS, and ferrous ion chelation) of the fractions were evaluated. Results: Fractions 4, 6, 8, and 9 have antimutagenic activity (against sodium azide in strain TA100), fraction 11 showed antiproliferative capacity (IC50 of 24 ± 9 μg/mL in cells of HCT 116). The fractions with the highest activity were analyzed by HPLC-MS and lupeol, acacetin, and β-sitosterol were identified. Conclusion: This study demonstrates, for the first time, the bioactivity of C. uvifera leaf as a new source of high biological value compounds (HBVC), which can be of interest to the food and pharmaceutical industries.

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The Repurposed Drugs Suramin and Quinacrine Cooperatively Inhibit SARS-CoV-2 3CLpro In Vitro

Viruses ◽

10.3390/v13050873 ◽

2021 ◽

Vol 13 (5) ◽

pp. 873

Author(s):

Raphael J. Eberle ◽

Danilo S. Olivier ◽

Marcos S. Amaral ◽

Ian Gering ◽

Dieter Willbold ◽

...

Keyword(s):

Binding Mode ◽

Drug Candidates ◽

Main Protease ◽

Ic50 Values ◽

Repurposed Drugs ◽

Antiparasitic Drugs ◽

Inhibitory Potential ◽

Dynamics Simulations ◽

Micromolar Range

Since the first report of a new pneumonia disease in December 2019 (Wuhan, China) the WHO reported more than 148 million confirmed cases and 3.1 million losses globally up to now. The causative agent of COVID-19 (SARS-CoV-2) has spread worldwide, resulting in a pandemic of unprecedented magnitude. To date, several clinically safe and efficient vaccines (e.g., Pfizer-BioNTech, Moderna, Johnson & Johnson, and AstraZeneca COVID-19 vaccines) as well as drugs for emergency use have been approved. However, increasing numbers of SARS-Cov-2 variants make it imminent to identify an alternative way to treat SARS-CoV-2 infections. A well-known strategy to identify molecules with inhibitory potential against SARS-CoV-2 proteins is repurposing clinically developed drugs, e.g., antiparasitic drugs. The results described in this study demonstrated the inhibitory potential of quinacrine and suramin against SARS-CoV-2 main protease (3CLpro). Quinacrine and suramin molecules presented a competitive and noncompetitive inhibition mode, respectively, with IC50 values in the low micromolar range. Surface plasmon resonance (SPR) experiments demonstrated that quinacrine and suramin alone possessed a moderate or weak affinity with SARS-CoV-2 3CLpro but suramin binding increased quinacrine interaction by around a factor of eight. Using docking and molecular dynamics simulations, we identified a possible binding mode and the amino acids involved in these interactions. Our results suggested that suramin, in combination with quinacrine, showed promising synergistic efficacy to inhibit SARS-CoV-2 3CLpro. We suppose that the identification of effective, synergistic drug combinations could lead to the design of better treatments for the COVID-19 disease and repurposable drug candidates offer fast therapeutic breakthroughs, mainly in a pandemic moment.

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