scholarly journals Antioxidant Activity and Inhibitory Potential ofCistus salviifolius(L.) andCistus monspeliensis(L.) Aerial Parts Extracts against Key Enzymes Linked to Hyperglycemia

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Karima Sayah ◽  
Ilias Marmouzi ◽  
Hanae Naceiri Mrabti ◽  
Yahia Cherrah ◽  
My El Abbes Faouzi

Cistusgenus (Cistaceae) comprises several medicinal plants used in traditional medicines to treat several pathological conditions including hyperglycemia. These includeCistus salviifoliusL.(CS) andCistus monspeliensisL.(CM), still not fully explored as a source of metabolites with therapeutic potential for human diseases. In this study, the antioxidantα-amylase andα-glucosidase enzyme inhibitory effects of aqueous and hydromethanolic extracts from the aerial parts of Moroccan CS and CM were investigated. Antioxidant activity has been assessed using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radicals and ferric reducing/antioxidant power (FRAP) methods. Theα-amylase andα-glucosidase inhibitory activity has been assessed using an in vitro model. Moreover, mineral and phenolic contents of CS and CM were analyzed. The extracts of both species exhibited potent antioxidant activity in all used systems and possess strong inhibitory effect towardsα-glucosidase (IC50:0.95±0.14to14.58±1.26 μg/mL) and significant inhibitory potential againstα-amylase (IC50:217.10±0.15to886.10±0.10 μg/mL). Furthermore, the result showed high levels of phenolic content and unexpectedly some higher levels of mineral content in CS. The results suggest that the phenolic rich extracts of CS and CM may have a therapeutic potential against diseases associated with oxidative stress and may be useful in the management of hyperglycemia in diabetic patients.

2021 ◽  
Vol 11 (22) ◽  
pp. 11028
Author(s):  
Mohd W. A. Khan ◽  
Ahmed A. Otaibi ◽  
Arwa F. M. Alhumaid ◽  
Abdulmohsen K. D. Alsukaibi ◽  
Asma K. Alshamari ◽  
...  

Glycation of various biomolecules contributes to structural changes and formation of several high molecular weight fluorescent and non-fluorescent, advanced glycation end products (AGEs). AGEs and glycation are involved in various health complications. Synthetic medicines, including metformin, have several adverse effects. Natural products and their derivatives are used in the treatment of various diseases due to their significant therapeutic qualities. Allium sativum (garlic) is used in traditional medicines because of its antioxidant, anti-inflammatory, and anti-diabetic properties. This study aimed to determine the anti-glycating and AGEs inhibitory activities of garlic. Biochemical and biophysical analyses were performed for in vitro incubated human serum albumin (HSA) with 0.05 M of glucose for 1, 5, and 10 weeks. Anti-glycating and AGEs inhibitory effect of garlic was investigated in glycated samples. Increased biochemical and biophysical changes were observed in glycated HSA incubated for 10 weeks (G-HSA-10W) as compared to native HSA (N-HSA) as well as glycated HSA incubated for 1 (G-HSA-1W) and 5 weeks (G-HSA-5W). Garlic extract with a concentration of ≥6.25 µg/mL exhibited significant inhibition in biophysical and biochemical changes of G-HSA-10W. Our findings demonstrated that garlic extract has the ability to inhibit biochemical and biophysical changes in HSA that occurred due to glycation. Thus, garlic extract can be used against glycation and AGE-related health complications linked with chronic diseases in diabetic patients due to its broad therapeutic potential.


2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Nasreddine El Omari ◽  
Karima Sayah ◽  
Saad Fettach ◽  
Omar El Blidi ◽  
Abdelhakim Bouyahya ◽  
...  

Oxidative stress plays a major role in diabetic physiopathology; hence, the interest of using natural antioxidants as therapeutic tools exists. The aim of this study was the evaluation of in vitro antioxidant activity and inhibitory potential of organic extracts from Aristolochia longa roots against key enzymes linked to hyperglycemia. Antioxidant activity was performed using 2,2′-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radicals and ferric reducing/antioxidant power (FRAP) methods. The α-Glucosidase and β-Galactosidase inhibitory activities were investigated using an in vitro model. Moreover, phytochemical analysis of tested extracts was carried out. The aqueous fraction of this herb exhibited the highest antioxidant activity for both DPPH and ABTS methods, IC50=125.40±2.40 μg/mL and IC50=65.23±2.49 μg/mL, respectively. However, the ethyl acetate fraction possessed the strongest inhibitory effect towards α-Glucosidase (IC50=1.112±0.026 mg/mL). Furthermore, the result showed high levels of phenolic content. The results showed that this plant could be a significant source of medically important natural compounds.


Antioxidants ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 69 ◽  
Author(s):  
Agnieszka Kicel ◽  
Aleksandra Owczarek ◽  
Paulina Kapusta ◽  
Joanna Kolodziejczyk-Czepas ◽  
Monika A. Olszewska

Cotoneaster plants are sources of traditional medicines and dietary products, with health benefits resulting from their phenolic contents and antioxidant activity. In this work, active markers of the leaves of C. bullatus and C. zabelii were characterized and evaluated in an integrated phytochemical and biological activity study. Based on UHPLC-PDA-ESI-MS3 analysis, twelve analytes were preselected from the constituents of the hydromethanolic leaf extracts, and two of them—caffeoylmalic acid and quercetin 3--O-β-d-(2″--O-β-d-xylopyranosyl)galactopyranoside (QPH)—were isolated for full identification (NMR spectroscopy: 1H, 13C, COSY, HMBC, HMQC). All selected phenolics contributed to the antioxidant activity of the extracts, which was demonstrated in chemical in vitro tests (DPPH, FRAP, and TBARS) and in a biological model of human plasma exposed to oxidative/nitrative stress induced by peroxynitrite. This contribution was partly due to the synergy between individual polyphenols, evidenced by an isobolographic analysis of the interactions of (–)-epicatechin, chlorogenic acid, and QPH as representatives of three classes of Cotoneaster polyphenols. All twelve markers, including also neochlorogenic acid, cryptochlorogenic acid, procyanidin B2, procyanidin C1, rutin, hyperoside, isoquercitrin, and quercitrin, were thus applied as calibration standards, and a fast, accurate, reproducible, and fully validated RP-HPLC-PDA method for quality control and standardization of the target extracts was proposed.


2019 ◽  
Vol 6 (1) ◽  
pp. 17-25
Author(s):  
Ibtissem Boulacel ◽  
Brahim Harkati ◽  
Radia Ayad ◽  
Ibrahim Demirtas ◽  
Hocine Laouer ◽  
...  

Abstract The focus of this paper was to assess the phytochemical composition, the antioxidant and antibacterial activities of the crude extracts of the aerial parts of Ferula lutea. Four new compounds were isolated from this genus, and their structures were primarily established by extensive spectroscopic analysis including 1D and 2D spectroscopic techniques. Total phenolics and flavonoids containing in ethyl acetate (AcOEt) and n-butanol (n-BuOH) extracts were quantified [199.1-184.02 mg gallic acid equivalent / g of dry weight], flavonoids [70.24-65.95 mg quercetin / g dry weight]. DDPH scavenging and phosphomolybdenum methods were used to evaluate in vitro antioxidant activity. The obtained results showed a significant antioxidant activity of the two aerial parts. Correlation analysis between the DPPH values and those for TAC indicates the possibility of the two models for evaluating antioxidants power from medicinal plants. Dichloromethane (CH2Cl2), AcOEt and n-BuOH extracts were screened against two gram-negative [Escherichia coli (E.coli) and Pseudo aeruginosa (P.aer)] and two gram-positive [Staphylococcus aureus (S.aur) and Bacillus (Bacil.)] bacteria using disc diffusion method. The results indicate a good inhibition of CH2Cl2 and EtAct extracts on the growth of (Bacil. and E.coli). Furthermore n-but extract showed a significant inhibitory effect only against E.coli.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3134
Author(s):  
Fadoua Asraoui ◽  
Ayoub Kounnoun ◽  
Francesco Cacciola ◽  
Fouad El Mansouri ◽  
Imad Kabach ◽  
...  

Medicinal plants offer imperative sources of innovative chemical substances with important potential therapeutic effects. Among them, the members of the genus Inula have been widely used in traditional medicine for the treatment of several diseases. The present study investigated the antioxidant (DPPH, ABTS and FRAP assays) and the in vitro anti-hyperglycemic potential of aerial parts of Inula viscosa (L.) Aiton (I. viscosa) extracts through the inhibition of digestive enzymes (α-amylase and α-glucosidase), responsible of the digestion of poly and oligosaccharides. The polyphenolic profile of the Inula viscosa (L.) Aiton EtOAc extract was also investigated using HPLC-DAD/ESI-MS analysis, whereas the volatile composition was elucidated by GC-MS. The chemical analysis resulted in the detection of twenty-one polyphenolic compounds, whereas the volatile profile highlighted the occurrence of forty-eight different compounds. Inula viscosa (L.) Aiton presented values as high as 87.2 ± 0.50 mg GAE/g and 78.6 ± 0.55mg CE/g, for gallic acid and catechin, respectively. The EtOAc extract exhibited the higher antioxidant activity compared to methanol and chloroform extracts in different tests with (IC50 = 0.6 ± 0.03 µg/mL; IC50 = 8.6 ± 0.08 µg/mL; 634.8 mg ± 1.45 AAE/g extract) in DPPH, ABTS and FRAP tests. Moreover, Inula viscosa (L.) Aiton leaves did show an important inhibitory effect against α-amylase and α-glucosidase. On the basis of the results achieved, such a species represents a promising traditional medicine, thanks to its remarkable content of functional bioactive compounds, thus opening new prospects for research and innovative phytopharmaceuticals developments.


2015 ◽  
Vol 10 (3) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Agnieszka Kicel ◽  
Monika Anna Olszewska

This study was designed to evaluate the flavonoid, saponin (TSC) and phenolic (TPC) contents and in vitro antioxidant activity of the crude (CME) and dry extracts and fractions of Medicago lupulina L. aerial parts. A validated RP-HPLC method led to quantitation of flavonols (kaempferol, quercetin and myricetin) and flavones (apigenin and luteolin) in the hydrolyzed extract. TSC and TPC were assayed spectrophotometrically at 560 and 760 nm, respectively. The antioxidant activity of the CME and the dry fractions were followed in vitro by DPPH free radical and ferric reducing antioxidant power (FRAP) methods. The flavonoid content of CME was 1.27 mg/g dw. The prevailing flavonoids were luteolin and myricetin, at concentrations of 0.37 and 0.36 mg/g dw, respectively. TSC and TPC were detected in CME at the level of 90.4 mg ESE/g dw, and 12.9 mg GAE/g dw, respectively. In the DPPH and FRAP tests, the CME exhibited antioxidant capacity with TEAA and FRAP values of 45.4 μmol Trolox®/g dw and 0.2 mmol Fe2+/g dw, respectively. The diethyl ether dry fraction was the most valuable one, showing the highest antioxidant activity (TEAA = 726.1 μmol Trolox®/g dw, FRAP = 2349.4 μmol Fe2+/g dw) that was in accordance with its high TPC (162.4 mg/g dw).


2013 ◽  
Vol 14 (1) ◽  
pp. 87-94 ◽  
Author(s):  
Gan B Bajracharya ◽  
Rokesh Maharjan

This study was aimed to evaluate the cytotoxicity of methanolic extract (ME) and aqueous extract (AE) of the rhizomes of Bergenia purpurascens through the Brine-shrimp bioassay, which revealed that ME possessed cytotoxicity with LC50 = 181.97 ìg/ml value. The plant extracts were also evaluated in vitro for antioxidant activity using different redox [Folin-Ciocalteu (FC) and Ferric Reducing Antioxidant Power (FRAP)] and radical scavenging [(2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS)] assays. Both ME and AE possessed antioxidant activity and ME displayed comparatively a greater potential. The total phenolic contents in ME and AE was 1.27 and 0.06 g gallic acid equivalent (GAE)/100 g dry mass (DM), respectively. The FRAP values determined for ME and AE were 15.82 and 2.58 ìmol Fe(II)/100 g DM, respectively. The DPPH radical scavenging effect (IC50) was for ME 19.86 ìg/ml and 295.91 ìg/ml for AE. At 100 ìg/ml concentration, up to 94% inhibition of ABTS+ was observed in 6 min incubation. Nepal Journal of Science and Technology Vol. 14, No. 1 (2013) 87-94 DOI: http://dx.doi.org/10.3126/njst.v14i1.8927


2021 ◽  
Vol 18 ◽  
Author(s):  
Allaoua Nouri ◽  
Lakhder Gasmi ◽  
Chawki Bensebini ◽  
Daoud Harzallah ◽  
Seddik Khennouf ◽  
...  

Background: Species of Echium trygorrhizum Pomel , are used traditionally in Algeria folk medicine for the treatment of Diabetes, Jaundice and Tonsillitis. To our knowledge, no previous study has been conducted out on the pharmacological activities of this species. Objective: The objective of the present research was to evaluate the content of polyphenols , flavonoids and condensed tannins compounds and to assess in vitro the antioxidant activity and the inhibitory effect of the hydroalcoholic extract of this plant, on α-amylase activity, an enzyme responsible for digestion of carbohydrate before the process of intestinal absorption. Methods: Polyphenols, flavonoids and condensed tannins were evaluated spectrophotometrically using Folin–Ciocalteu, the Aluminum chloride and vanillin methods respectively. The antioxidant activity using DPPH radical scavenging, ABTS, Ferric reducing antioxidant power and β- carotene bleaching tests and the assessment of in vitro α- amylase inhibitory potential by an Aspergillus oryzae α- amylase have been studied. Results: The hydroalcoholic crude extract was able to inhibit the α-amylase enzyme in vitro, with an IC50 of 0.56 ± 0.044 mg/ml, in addition the contents of polyphenols and flavonoids were found to be 157.403 ± 0.835 µg GAE/mg extract and 30.156±2.634µg Q E / mg extract, respectively, Whereas the amount of tannins was 65.293 ± 0.883µg Cat E/ mg of dry extract. Conclusion: The present study revealed that the extract is rich in phenolic compounds, which play a really important role in the scavenging of free radicals. It has been reported the inhibitory capacity of hydroalcoholic roots extract on Aspergillus oryzae α-amylase enzyme might be used as a natural agent within the management of diabetes mellitus.


2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.


2020 ◽  
Vol 16 ◽  
Author(s):  
Benedetta Bocchini ◽  
Bruna Goldani ◽  
Fernanda S.S. Sousa ◽  
Paloma T. Birmann ◽  
Cesar A. Brüning ◽  
...  

Background: Quinoline derivatives have been attracted much attention in drug discovery and synthetic derivatives of these scaffolds present a range of pharmacological activities. Therefore, organoselenium compounds are valuable scaffolds in organic synthesis because their pharmacological activities and their use as versatile building blocks for regio-, chemio-and stereoselective reactions. Thus, the synthesis of selenium-containing quinolines has great significance, and their applicability range from simple antioxidant agents, to selective DNA-binding and photocleaving agents. Objective: In the present study we describe the synthesis and antioxidant activity in vitro of new 7-chloroN(arylselanyl)quinolin-4-amines 5 by the reaction of 4,7-dichloroquinoline 4 with (arylselanyl)-amines 3. Methods: For the synthesis of 7-chloro-N(arylselanyl)quinolin-4-amines 5, we performed the reaction of (arylselanyl)- amines 3 with 4,7-dichloroquinoline 4 in the presence of Et3N at 120 °C in a sealed tube. The antioxidant activities of the compounds 5 were evaluated by the following in vitro assays: 2,2- diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric ion reducing antioxidant power (FRAP), nitric oxide (NO) scavenging and superoxide dismutase-like activity (SOD-Like). Results: 7-Chloro-N(arylselanyl)quinolin-4-amines 5a-d has been synthesized in yields ranging from 68% to 82% by the reaction of 4,7-dichloroquinoline 4 with arylselanyl-amines 3a-d using Et3N as base, at 120 °C, in a sealed tube for 24 hours and tolerates different substituents, such as -OMe and -Cl, in the arylselanyl moiety. The obtained compounds 5a-d presented significant results with respect to the antioxidant potential, which had effect in the tests of inhibition of radical’s DPPH, ABTS+ and NO, as well as in the test that evaluates the capacity (FRAP) and in the superoxide dismutase-like activity assay (SOD-Like). It is worth mentioning that 7-chloro-N(arylselanyl)quinolin-4-amine 5b presented excellent results, demonstrating a better antioxidant capacity when compared to the others. Conclusion: According to the obtained results 7-chloro-N(arylselanyl)quinolin-4-amines 5 were synthesized in good yields by the reaction of 4,7-dichloroquinoline with arylselanyl-amines and tolerates different substituents in the arylselanyl moiety. The tested compounds presented significant antioxidant potential in the tests of inhibition of DPPH, ABTS+ and NO radicals, as well as in the FRAP and superoxide dismutase-like activity assays (SOD-Like).


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