scholarly journals Antioxidant, Antidiabetic, and Anticholinesterase Activities and Phytochemical Profile of Azorella glabra Wedd

Plants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 265 ◽  
Author(s):  
Immacolata Faraone ◽  
Dilip K. Rai ◽  
Daniela Russo ◽  
Lucia Chiummiento ◽  
Eloy Fernandez ◽  
...  

Oxidative stress is involved in different diseases, such as diabetes and neurodegenerative diseases. The genus Azorella includes about 70 species of flowering plant species; most of them are commonly used as food and in particular as a tea infusion in the Andean region of South America in folk medicine to treat various chronic diseases. Azorella glabra Wedd. aerial parts were firstly analyzed for their in vitro antioxidant activity using different complementary assays. In particular, radical scavenging activity was tested against biological neutral radical DPPH; ferric reducing power and lipid peroxidation inhibitory capacity (FRAP and Beta-Carotene Bleaching tests) were also determined. The Relative Antioxidant Capacity Index (RACI) was used to compare data obtained by different assays. Then, the inhibitory ability of samples was investigated against α-amylase and α-glucosidase enzymes involved in diabetes and against acetylcholinesterase and butyrylcholinesterase enzymes considered as strategy for the treatment of Parkinson’s or Alzheimer’s diseases. Moreover, the phytochemical profile of the sample showing the highest RACI (1.35) and interesting enzymatic activities (IC50 of 163.54 ± 9.72 and 215.29 ± 17.10 μg/mL in α-glucosidase and acetylcholinesterase inhibition, respectively) was subjected to characterization and quantification of its phenolic composition using LC-MS/MS analysis. In fact, the ethyl acetate fraction derived from ethanol extract by liquid/liquid extraction showed 29 compounds, most of them are cinnamic acid derivatives, flavonoid derivatives, and a terpene. To the best of our knowledge, this is the first report about the evaluation of significant biological activities and phytochemical profile of A. glabra, an important source of health-promoting phytochemicals.

Author(s):  
Saira Tabassum ◽  
Muhammad Zia ◽  
Esperanza J. Carcahe de Blanco ◽  
Riffat Batool ◽  
Roohi Aslam ◽  
...  

Abstract Background Arisaema jacquemontii is traditionally used in treatment of different diseases. In this study, phytochemical, in vitro biological and chemo-preventive screening of A. jacquemontii was carried out to explore its pharmacological potential. Methods The dried tuber of A. jacquemontii was extracted in 11 organic solvent mixture of different polarity. The extracts were screened for phytochemical assays (phenolics and flavonoids), antioxidants potential (free radical scavenging activity, total antioxidant activity, reducing power), biological activities (antibacterial, antifungal, cytotoxic, antileishmanial, protein kinase inhibition), and chemopreventive activities using different cell lines through standard protocols. Results Significant amount phenolic contents were determined in EtOH and MeOH extracts (210.3 ± 3.05 and 193.2 ± 3.15 μg GAE/mg, respectively). Maximum flavonoid content was determined in MeOH extract (22.4 ± 4.04 μg QE/mg). Noteworthy, DPPH scavenging activity was also recorded for MeOH extract (87.66%) followed by MeOH+EtOAc extract (85.11%). Considerable antioxidant capacity (7.8 ± 0.12 μg AAE/mg) and reducing power (3.1 ± 0.15 μg AAE/mg) was observed in extract of MeOH. The LC50 against brine shrimp and leishmanial parasite was found 9.01 and 12.87 μg/mL for n-Hex and CHCl3 extracts, respectively. The highest zone of inhibition against Streptomyces hyphae formation (12.5 ± 1.77 mm) by n-Hex extract. Growth zone of inhibition 13.8 ± 1.08 mm was recorded for EtOAc and MeOH extracts, respectively against Micrococcus luteus while 10.0 ± 0.11 mm for MeOH extract against Aspergillus flavus. In-vitro cytotoxic assay showed that n-Hex extract had higher cytotoxicity against DU-145 prostate cancer and HL-60 cancer cell lines. NF-kB and MTP potential showed 34.01 and 44.87 μg/mL for n-Hex and CHCl3 extracts, respectively in chemo-preventive potential. Conclusion The study concludes that Arisaema jacquemontii bears significant phytochemical activity and pharmacological activities, this plant can be further explored for isolation of active component against a number of aliments.


Author(s):  
Anindita Banerjee ◽  
Bithin Maji ◽  
Sandip Mukherjee ◽  
Kausik Chaudhuri ◽  
Tapan Seal

Objective: The aim of the present study was to evaluate the alpha (α)-amylase and alpha (α)-glucosidase inhibitory activities and in vitro antioxidant activities of the 80 % aqueous ethanol extracts of Tinosporasinensis Lour (Merr.).Methods: The 80% aq. ethanol extract of the plant was prepared. The plant extract was examined for its antioxidant activity by using free radical 1,1-diphenyl-2-picryl hydrazyl (DPPH) scavenging method, ABTS radical scavenging ability, reducing power capacity, estimation of total phenolic content, flavonoid content and flavonol content. Different concentrations (2, 4, 8,10and 15 μg/ml) of the extract was subjected to α-amylase inhibitory and α-glucosidase inhibitory activities and IC50were calculated.Results: The study revealed that the different concentrations of the plant extract possessed a very good amount of total phenolics, flavonoid and flavonol and exhibited potent radical scavenging activity using DPPH and ABTS as a substrate. The ethanol extracts exhibited significant α-amylase and α-glucosidase inhibitory activities with an IC50 value1.093µg and 1.04µg dry extract respectively and well compared with standard acarbose drug.Conclusion: Thus, it could be concluded that due to the presence of antioxidant components the plant extracts could be used for the treatment of hyperglycemia, diabetes and the related condition of oxidative stress. This knowledge will be useful in finding more potent components from the natural resources for the clinical development of antidiabetic therapeutics.


2021 ◽  
pp. 10-12
Author(s):  
S Srinivasan ◽  
A Rayar

Introduction:Medicinal plants have been used for the treatment of diseases all over the world before the advent of articial clinical drugs and are known to contain substances that can be used for therapeutic uses. Antioxidations act asreducing agents, free radical scavengers, quenchers of singlet oxygen molecule, and activators for antioxidative enzyme to reduce the damage caused by free radicals in biological pattern. Materials and Methods:The isolated organic compound from Mimosa nilotica was subjected to column chromatographic separation and was characterized 1 13 by UV, IR, H-NMR and C-NMR.DPPH assay was conducted to assess the effect of the ethanolic extract and 7-hydroxy–4-methylcoumarin. Result and Discussion:The reports of the in-vitro antioxidation assay indicated that the ethanol extract was more potent than 7-hydroxy–4- methylcoumarin. 7-hydroxy–4-methylcoumarin and ethanolic extractexpress excellent free radical scavenging activity. From the reports it is proved that the reducing power of bioactive constituent is associated with antioxidationpotential. Thus a correlation is proved between reducing power and the antioxidation effect. Conclusion:Previous reports are conrmed that the reducing power of bioactive constituents is associated with antioxidation potential. People who eat various parts of fruits and herbs have a lower risk of heart disease and some neurological diseases and there is evidence that some types of herbs, and fruits in general, protect against some malignant.


2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.


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 42 (1) ◽  
pp. 109-109
Author(s):  
Hao Zang Hao Zang ◽  
Qian Xu Qian Xu ◽  
Luyun Zhang Luyun Zhang ◽  
Guangqing Xia Guangqing Xia ◽  
Jiaming Sun and Junyi Zhu Jiaming Sun and Junyi Zhu

A series of hydroxytyrosol (HT) derivatives were synthesized by modification of alcohol hydroxyl group of HT, twenty-five target compounds were obtained and characterized by NMR and HRMS. The antioxidant activities of those compounds were evaluated in three different assays. Except 3e and 3y, all other compounds demonstrated significant 2,2and#39;-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radical cation scavenging activity ranging from IC50 3.4 to 24.4 μM, which were more potent than L-ascorbic acid (IC50=24.8 μM). Compounds 3b-3d, 3f-3k, 3m-3x were better than Trolox (18.3 M). Moreover, the ferric reducing antioxidant power (FRAP) of all compounds were discovered to be more potent than L-ascorbic acid (40.7 mmol/g), except 3e, all other compounds (141.5-202.1 mmol/g) were better than Trolox (94.7 mmol/g). Compounds 3a-3d, 3f-3j, 3l-3m, 3o, 3q, 3t, 3v-3y exhibited more potent hydroxyl radical scavenging activity (IC50=245.1-475.1 M) than L-ascorbic acid (554.4 M) and Trolox (500.4 M). Compounds 3q, 3t and 3y exhibited more potent -Glucosidase inhibition activity (39.1-52.4 M) than Acarbose (60.9 M). Compounds 3a, 3d, 3f-3m, 3s-3t, 3v-3y showed some acetylcholinesterase inhibition activities, compounds 3a, 3d, 3f-3j, 3l-3m, 3o-3p, 3s-3t, 3w showed some butyrylcholinesterase inhibition activities.


2021 ◽  
Vol 18 ◽  
Author(s):  
Nayla Javed ◽  
Shakeel Ijaz ◽  
Naveed Akhtar ◽  
Haji Muhammad Shoaib Khan

Background: Arctostaphylos uva-ursi (AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts. Objective: The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation. Methods: AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (scanning electron microscopy), vesicular size, zeta potential, and entrapment efficiency (%EE). The optimized formulation was subjected to non-invasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation. Results: Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (polydispersity index), % EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity. Conclusion: A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation etc.


2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.


2019 ◽  
Vol 20 (1) ◽  
Author(s):  
Magdalena Woźniak ◽  
Lucyna Mrówczyńska ◽  
Agnieszka Waśkiewicz ◽  
Marta Babicka ◽  
Elżbieta Hołderna-Kędzia ◽  
...  

Introduction. Propolis (bee glue) is a natural product collected by honeybees from buds of various trees, shrubs and other plant species. Extracts of propolis possess numerous biological activities, including antioxidant, antibacterial, antifungal and anticancer. For this reason, propolis is currently used in many applications, such as preparations for cold syndrome, dermatological preparations or as a constituent of nutritional supplements and health food. The chemical composition of this natural material is very complex and depending on many factors, including method of extraction and selection of the solvent for the extraction process. Aim. The aim of the study was to determine concentration of selected phenolic compounds (flavonoids and phenolic acids) in extract of Polish propolis and estimate its antioxidant activity and effect on human red blood cells. Material and methods. In the propolis extract was determined concentration of 14 flavonoids and 9 phenolic acids using ultra-performance liquid chromatography equipped with a photodiode detector and a triple quadrupole mass spectrometer. The antioxidant potential of propolis extract was evaluated applying DPPH˙ free radical scavenging activity assay and Fe3+ reducing power assay. Moreover, the cytotoxicity and cytoprotective potential of propolis extract was estimated using human erythrocytes in vitro. Results. The propolis extract contained high concentration of pinocembrin, galangin, chrysin, apigenin, kaempferol, coumaric acid and cinnamic acid. It exhibited also high antioxidant potential. The antiradical activity of examined propolis extract was equal to 75% approx. activity of both standard antioxidants used in the study, namely Trolox and BHT. The reducing power of extract was equal to 65% approx. of Trolox and 80% of BHT, respectively. The propolis extract had no hemolytic activity, moreover, effectively protected human erythrocytes against free radicals-induced damage in vitro. Conclusions. The results of this study indicate that the propolis extract of national origin is a rich source of flavonoids and phenolic acids. Therefore, the propolis extract possesses a high antioxidant potential and can protect erythrocytes against free radicals-induced oxidative hemolysis.


2021 ◽  
pp. 28-38
Author(s):  
Henry Bulama ◽  
Daniel Dahiru ◽  
Joshua Madu

Background: Cataract is a major cause of visual impairment and blindness around the world. This study evaluated the in vitro antioxidant and anti-cataract activities of Cnidoscolus aconitifolius leaves extract and fractions. Antioxidant activities were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis (3-ethylbenzothiozoline-6-sulfonic acid) (ABTS), total reducing power, and hydrogen peroxide scavenging assays. Anti-cataract potential was evaluated in vitro using goat lenses divided into eight groups of different treatments and incubated in artificial aqueous humor at 37 °C for 72 hours. Glucose-induced opacity in the lenses was observed and biochemical indices quantified (catalase, Malondialdehyde (MDA) and total protein in the lens homogenate). Results: The crude extract and its fractions possess substantial antioxidant activities. The aqueous fraction exhibited the best DPPH radical scavenging activity (IC50 value 78.599 µg/ml); while the dichloromethane fraction exhibited the highest ABTS radical scavenging activity with IC50 66.68 µg/ml. The anti-cataract evaluation of crude and fractions at 250 μg/ml showed a significant increase (p<0.05) in the total protein and catalase activity compared to the cataract control group. The malonaldehyde level decreased significantly (p<0.05) in all the treated groups.


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