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

2021 ◽  
Vol 19 (1) ◽  
pp. 1-13
Author(s):  
L.A. Adeniran ◽  
C.P. Palanisamy ◽  
A.O.T. Ashafa

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

2014 ◽  
Vol 10 (2) ◽  
pp. 2305-2316 ◽  
Author(s):  
Manel Ben Ali ◽  
Kais Mnafgui ◽  
Abdelfattah Feki ◽  
Mohamed Damak ◽  
Noureddine Allouche

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.


Author(s):  
E. I. Akpakpan ◽  
E. N. Onyeike ◽  
C. U. Ogunka-Nnoka

Dennettia tripetala fruit is a popular Nigerian fruit from the family of plant known as Annonaceae. The whole fruit (flesh and seed) is usually consumed as snacks and it is oftentimes consumed with local gin (ufofop in Ibibio or kaikai in Igbo) or added to dishes as spice due to its peculiar strong pepperish taste and sweet aroma. The present study is aimed at evaluating the antioxidant potentials of ethanol extract of ripe and unripe D. tripetala (DT) fruit in vitro. The antioxidant activity of the ethanol extract of DT was evaluated spectrophotometrically using various in vitro models like 1, 1-diphenyl-2-picryl-hydrazyl (DPPH) and hydrogen peroxide scavenging activity; metal chelating activity and reducing power. Vitamin C was used as the standard antioxidant.Unripe and ripe DT fruits, as well as vitamin C showed a competitive inhibition of DPPH and H2O2 free radicals. As concentration of the extracts increased from 20 to100 µg/mL, the % scavenging activity for vitamin C increased from 87.86 ± 0.11 to 90.66 ± 0.07 and for ripe DT fruits from 15.15 ± 0.24 to 25.52 ± 0.23, while for unripe, fruits values increased from 12.09 ± 0.35 to 23.06 ± 0.12. The IC50 values was highest in unripe (549.23) followed by ripe (276.63) and lowest in vitamin C (12.92) indicating that vitamin C was the best scavenger of DPPH radical. Similar trend was obtained for H2O2 scavenging activity as well as reducing power. Unripe DT fruit extract was more potent at chelating metal ions (IC50 was 95.38), followed by the standard ascorbic acid with IC50 of 97.03 and was lowest in ripe DT fruit extract with IC50 value of 124.66. Unripe and ripe DT are potent antioxidants in nature and may be used to supplement our diets as rich sources of natural antioxidants for health protection.


2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Urmeela Taukoorah ◽  
M. Fawzi Mahomoodally

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.


2020 ◽  
Vol 2 (2) ◽  
pp. 105-120
Author(s):  
L. A. Adeniran ◽  
A. O. T. Ashafa

The scientific investigation of the folkloric use of Hermannia geniculata roots in the management of diabetes mellitus was conducted. Phytochemical analyses, in vitro antioxidant and hyperglycaemic studies were carried out on the crude extracts of H. geniculata. Qualitative phytochemical analysis revealed the presence of saponins, phenols, flavonoids, alkaloids, tannins, phytosterols, triterpenes and anthraquinones. The ethanol extract exhibited the highest free radical scavenging capability with the lowest IC values (0.52, 0.38, 0.59, 0.63, 0.39) mg/mL for 50 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2-Azino-bis(3-ethylbenzothiazoline-6-Sulphonic acid (ABTS), hydroxyl radical, superoxide anion radical and metal chelating ability which is significantly different (p<0.05) from the standard (silymarin). In antidiabetic studies, ethanol extract is a potent inhibitor of α-glucosidase (IC : 0.15 mg/mL) which is lower and significantly 50 different (p<0.05) from the standard (acarbose) IC value of (0.52 mg/mL). Ethanol extract 50 exhibited a milder inhibition of α-amylase enzyme with IC (0.57mg/mL) which is higher and 50 significantly different (p<0.05) from acarbose with IC (0.47 mg/mL). Kinetic studies revealed H. 50 geniculata ethanol extract exhibited competitive inhibition of α-amylase and uncompetitive inhibition of α-glucosidase enzymes. All these findings provided the scientific basis which support the use of the root extract of H. geniculata in the management of diabetes mellitus and oxidative stress induced ailments like colitis and ulcers by the Basotho traditional medicine of South Africa.


Antibiotics ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 518
Author(s):  
Fadia S. Youssef ◽  
Munira A. Mamatkhanova ◽  
Nilufar Z. Mamadalieva ◽  
Gokhan Zengin ◽  
Salima F. Aripova ◽  
...  

The differences in the composition of essential oils obtained from the aerial parts of six Ferula species viz., F. caratavica (Fc), F. kuchistanica (Fk), F. pseudoreoselinum (Fp), F. samarcandica (Fs), F. tenuisecta (Ft) and F. varia (Fv) were detected both qualitatively and semi-quantitatively using GC-MS and GC-FID analyses. One hundred and six metabolites were identified that account for 92.1, 96.43, 87.43, 95.95, 92.90 and 89.48% of Fc, Fk, Fp, Fs, Ft and Fv whole essential oils, respectively. The data from the GC-MS analyses were subjected to unsupervised pattern recognition chemometric analysis utilizing principal component analysis (PCA) to improve the visualization of such differences among the six species. Fk and Ft are very closely related to each other and were gathered together in one cluster. The antioxidant potential was assessed in vitro using different assays including 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and phosphomolybdenum (PM) assays. Ft and Fp exhibited the most notable antioxidant properties as evidenced by their pronounced activities in most of the antioxidant assays performed, followed by Fc. Fk showed the most effective tyrosinase inhibitory potential, which was estimated as 119.67 mgKAE/g oil, while Fp exhibited the most potent α-amylase inhibitory potential, which was equivalent to 2.61 mmol ACAE/g oil. Thus, it was concluded that Ferula species could serve as a promising natural antioxidant drug that could be included in different products and spices to alleviate hyperglycemia and used as a natural ingredient in pharmaceutical cosmetics to counteract hyperpigmentation.


Viruses ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 873
Author(s):  
Raphael J. Eberle ◽  
Danilo S. Olivier ◽  
Marcos S. Amaral ◽  
Ian Gering ◽  
Dieter Willbold ◽  
...  

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.


2016 ◽  
Vol 3 ◽  
pp. 160-163
Author(s):  
Muhammad Amir Masruhim ◽  
Wisnu Cahyo Prabowo ◽  
Dita Paramitha

Hyperuricemia is a condition in which increased levels of uric acid in the blood. Xanthine oxidase role in the oxidation of hypoxanthine and xanthine to uric acid. One treatment of hyperuricemia is inhibiting xanthine oxidase in the process of formation of uric acid. The purpose of this study to determine the inhibitory activity of xanthine oxidase in the ethanol extract of black betel leaf (Piper sp). Xanthine oxidase inhibitory activity test using UV-Vis spectrophotometry in vitro with a concentration of 5 ppm, 10 ppm and 20 ppm. The data obtained were analyzed using one-way ANOVA. The result is the ethanol extract of black betel leaf has a different activity significantly and IC50 values obtained is 65.96 ppm.


2021 ◽  
Vol 15 (5) ◽  
pp. 571-579
Author(s):  
Rokayya Sami ◽  
Ebtihal Khojah ◽  
Mona Alharbi ◽  
Amina A. M. Al-Mushhin ◽  
Mohammed Saeed Alkaltham ◽  
...  

Consumers are interested in antimicrobial by-products from natural sources. The present study aims to estimate the antibacterial effects of different concentrations and solvent extracts such as methanol, ethanol, and water extract of pomegranate peels with the milk quality application in-vitro. Listeria monocytogens, E. coli, Salmonella, and Staphylococcus aureus were used as bacteria growth indicators in two pomegranate varieties (i.e., Wonderful and Francis). Besides, evaluating somephysical characterization, antibacterial and antioxidant activities. Results showed that the highest inhibition zone of 18.88 mm was observed with 90% ethanol extract of Wonderful variety against Listeria monocytogens, at 0, 12.5, 25, and 50 mg/mL concentrations, while the lowest inhibition zone of 11.29 mm was observed with 90% methanol extract of Francis variety, at 12.5 mg/mL concentration. The milk treated with WPE of Wonderful variety maintained the bacterial growth from 1.19 ±0.29 x 109 to 1.43 x 1011 CFU/mL at 4 °C. Punicalagin was the most abundant polyphenolic compound (165.05–190.43 µg/mL) followed by gallic acid (153.08–177.65 µg/mL), and p-Hydroxybenzoic acid (91.29–92.5 mg/mL). Acetaldehyde (23.09–27.15 PPM), followed by acetoin (9.65–15.33 PPM) were the most predominant volatile compounds. The WPE treated milk maintained the sensory evaluations such as taste, color, texture, and overall acceptance longer time longer time (i.e., 144 h) than FPE treated milk (i.e., 168 h) at 4°C. DPPH and ABTS radical scavenging of capacity (IC50 values) of FPE treated milk were found to be lower than WPE treated milk (i.e., 159.65 µg/mL and 131.87 µg/mL), respectively. While, FPE treated milk reported a higher viscosity content than WPE treated milk (13.11 cP). In conclusion, pomegranate peel extracts especially Wonderful variety may be used to prolong the shelf-life of milk in dairy products manufacturers.


Antioxidants ◽  
2018 ◽  
Vol 8 (1) ◽  
pp. 2 ◽  
Author(s):  
Marco Bonesi ◽  
Maria Tenuta ◽  
Monica Loizzo ◽  
Vincenzo Sicari ◽  
Rosa Tundis

The aim of this work is to investigate the in vitro acetylcholinesterase (AChE) and butyrycholinesterase (BChE) inhibitory activities of essential oils obtained by hydrodistillation from the leaves of Prunus armeniaca and P. domestica in relation to their composition, analysed by Gas Chromatography–Flame Ionization Detector (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS) analyses, at different times. Moreover, considering the role of free radicals in the progression of neurodegenerative disorders, the antioxidant properties of essential oils were investigated by using, 2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and β-carotene bleaching tests. The relative antioxidant capacity index (RACI) was used to achieve more comprehensive comparison between analysed antioxidant effects of essential oils. P. armeniaca oils were more active than P. domestica oils against AChE. Against BChE, the most active was the essential oil from P. domestica leaves collected in August with an IC50 value of 95.80 μg/mL. This oil exerted the highest inhibitory activity of lipid peroxidation with IC50 values of 11.15 and 11.39 μg/mL after 30 and 60 min of incubation, respectively. All samples demonstrated a remarkable ABTS radicals scavenging activity, with IC50 values in the range 0.45–0.57 μg/mL in comparison to the positive control, ascorbic acid.


2019 ◽  
Vol 65 (4) ◽  
pp. 316-323
Author(s):  
T.V. Sirota

The superoxide-generating reaction of adrenaline autoxidation in an alkaline medium, used in vitro to identify the antioxidant properties of various compounds, simulates the complex multistep process of quinoid oxidation of catecholamines (CA) in the body. Sulfur-containing cysteine (Cys) and reduced glutathione (GSH), as well as oxidized glutathione (GSSG), have been shown to inhibit this process. The studied substances were considered as inhibitors of quinoid oxidation and are evaluated as antioxidants. The IC50 values for Cys and GSH were close to 7.5 mM. Inhibition by GSSG was weaker; represented approximately 50-70% of Cys and GSH. Other sulfur-containing compounds that differ in chemical structure, the amino acids taurine and methionine were ineffective. The interest in this model and the search for effective compounds acting on this reaction is associated with one of the mechanisms of the etiopathogenesis of Parkinson's disease (PD) discussed in the literature, which occurs when the biochemical transformations of dopamine CA and its quinoid oxidation process are violated. Cys, GSH and GSSG in the model system inhibit quinoid oxidation of adrenaline, as a result of which the formation of superoxide (O2 ·-) is also inhibited. Experiments with the superoxide-generating enzymatic reaction xanthine xanthioxidase, the chemistry of which is different and not related to formation of quinoid metabolites, showed that the studied substances did not inhibit O2 ·- formation in this model. Thus, it was established that the biologically active sulfur-containing compounds Cys, GSH and GSSG are specific inhibitors of quinoid oxidation of CA, and are likely to be able to play the role of a neuroprotector. It is proposed to use these compounds in the treatment and prevention of PD by activating their biosynthesis in the body.


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