scholarly journals Antioxidant Studies of Thiazole Ring Bearing Chalcone Derivatives

Author(s):  
Ashok Babu Kasetti ◽  
Jayesh Dwivedi ◽  
Ravindra Nagasuri

Oxidative stress is one of the common problems seen in a variety of diseases. Chalcones and in particular heteroaryl chalcones had reported with promising antioxidant activities. Hence, in the present work, we reported the antioxidant activity of twenty thiazole ring bearing chalcone derivatives (1-20). Among the tested compounds, compounds 17, 19 and 20 containing 2-pyridinyl, 3-pyridinyl and 2-thiazolyl scaffolds showed superior antioxidant activity than the standard with their IC50 values 4±1µg/mL, 3±1 µg/mL and 5±1 µg/mL respectively. The compound 19 is an interesting lead for the development of newer antioxidant agents.

2021 ◽  
Vol 17 (6) ◽  
pp. 1123-1130
Author(s):  
Qichen Pan ◽  
Yunchao Ban ◽  
Lijun Xu

Alzheimer’s disease (AD) is strongly associated with oxidative stress which can damage neural cells. Silibinin has shown potential antioxidative effects. However, due to its low solubility in water, silibinin provides low biological activity and bioavailability. Therefore, to increase its pharmacological effects, silibilin was encapsulated into human serum albumin (HSA) nanoparticles and well-characterized by DLS and TEM techniques. The antioxidant activity of silibinin-HSA nanoparticles was evaluated on LPS-induced oxidative stress in neuron-like cells (SH-SY5Y) through MTT, antioxidant activity and apoptotic assay. It was shown that the mean diameter of HSA and silibinin-HSA nanoparticles were 88 and 105 nm, respectively with a drug loading of 24.08%, drug encapsulation rate of 94.72%, and the yield of silibinin-HSA nanoparticles of around 83.41% and the HSA nano-formulation released silibinin for 15 h. The results displayed that cell viability was reduced by LPS (10 μg/mL), who’s also determined to stimulate oxidative stress and apoptosis. However, co-incubation of cells with silibinin (50 μg/mL) or silibinin-HSA nanoparticles led to the recovery of cell viability, activation of SOD and CAT, increase of GSH content, and reduction of ROS level, Caspase-3 activity and fragmentation of DNA. It was also indicated that the neuroprotective and antioxidant activities of silibinin-HAS nanoparticles was greater than free silibinin, indicating that using albumin can be a potential formulation approach for improving the antioxidant efficacy of silibinin.


Author(s):  
Kavitha S ◽  
Parthasarathi Perumal

 Objective: The present study was undertaken to assess the α-amylase inhibitory activity and antidiabetic experimental catfish model and antioxidant properties of Piper betle L. ethanolic (PBE) extract.Methods: The phytochemical analysis of PBE extract was performed. The PBE extract was tested for their inhibitory effect on the α-amylase assay, which compared to the control, acarbose. The absorbance was read at 540 nm using a spectrophotometer, and IC50 values were calculated. In this present investigation, diabetes mellitus was induced in catfish, Clarias gariepinus by epaxial musculature injection to glucose and standard drug, Metformin hydrochloride. After 24-h incubation, the treated fishes were dissected, and the blood, liver, tissue samples, and epaxial musculature regions were collected. In addition, the antioxidant properties of PBE were determined by 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical scavenging and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging (ABTS) assays.Results: The phytochemical screening of PBE revealed the presence of alkaloid, flavonoids, tannins, phenol, glycosides, sterols, saponins, and quinines. Furthermore, the values of (μg/ml) 3.038 and 7.672 α-amylase enzyme inhibition were excellent activity when compared to the acarbose. Moreover, elevated the glucose level (mg/dl) was estimated in blood 1.9±0.35, liver 0.5±0.25, tissue 0.2±0.25, and epaxial musculature 0.8±0.2 after 24-h incubation. The antioxidant effect of maximum activity was found in PBE; IC50 values (μg/ml) of DPPH and ABTS were 9.362 and 6.606, respectively.Conclusions: These studies might be responsible for the P. betle L. that was used as the new source of antidiabetic and antioxidant agents. 


Author(s):  
Irfan Zamzani ◽  
Nita Triadisti

Antioxidants are substances that can slow down the oxidation process of free radicals. Limpasu plant (Baccaurea lanceolata (Miq) Muell. Arg), an indigenous plant of Borneo, is a natural antioxidant source. The purpose of this study was to determine the antioxidant activity of the limpasu pericarpium extract. The extraction of the limpasu pericarpium was done by maceration method using solvents with increasing polarity ranging from n-hexane, ethyl acetate, and methanol. Antioxidant activities of the three extracts were measured by the DPPH and FRAP methods. The IC50 values of n-hexane, ethyl acetate, and methanol extracts, as well as quercetin using the DPPH method were 517,45 µg/mL, 530,64 µg/mL, 10,63 µg/mL and 6,83 µg/mL, respectively. Meanwhile, the IC50 values obtained from FRAP method were 198,96 µg/mL, 190,07 µg/mL, 661,36 µg/mL, and 7,09 µg/mL, respectively. The results revealed that the methanol extract is more potent than other extracts tested for antioxidant activity.


2019 ◽  
Vol 17 (1) ◽  
pp. 1339-1344 ◽  
Author(s):  
T. M. Thant ◽  
N. S. Aminah ◽  
A. N. Kristanti ◽  
R. Ramadhan ◽  
H. T. Aung ◽  
...  

AbstractAll around the world, patients with diabetes and the prevalence of its disease are currently growing. Due to these side effects of oral hypoglycemic agents and oxidative stress in complicating diabetes, there is growing interest in drugs, which possess dual function as both type II diabetes mellitus treatment and oxidative stress treatment. The objective of this research is to search effective antidiabetes and antioxidant bioactive compounds from the Myanmar medicinal plant Clausena excavata. The root part of C. excavata was successfully extracted with 95% ethanol and followed by column chromatographic separation technique. The structure of isolated pure compounds was elucidated by using methods of spectroscopic such as UV-Vis, IR, NMR and HRFABMS spectrometry. The α-glucosidase inhibition assay was performed against baker’s yeast and rat intestine (sucrose and maltase) α-glucosidases. The activity of isolated compounds’ antioxidant was measured by using DPPH assay. Among the tested enzymes, the two isolated compounds, which were dentatin (1) and heptaphylline (2), exhibited highest inhibitory on maltase enzymes with IC50 values 6.75 and 11.46 μM; as positive control, acarbose (IC50, 2.35 μM) was utilized. Moreover, scavenging activity was found to be present upon seeing the result of antioxidant activity investigation of (1) and (2) (IC50 values 2.66 and 1.55 mM), where ascorbic acid (IC50 0.012 mM) was used as standard. Both compounds showed their antidiabetic and antioxidant activity with different fashion, especially exhibited strongest activity against on maltase α-glucosidase.


PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e6427 ◽  
Author(s):  
Chutima Tanapichatsakul ◽  
Sarunpron Khruengsai ◽  
Sakon Monggoot ◽  
Patcharee Pripdeevech

Endophytic fungi, which colonize within a host plant without causing any apparent diseases, have been considered as an important source of bioactive secondary metabolites containing antimicrobial and antioxidant activities. The aim of this research was to isolate the endophytic fungi ofCinnamomum loureiroiand then to screen their antimicrobial and antioxidant activities. A total of 11 fungal endophytes were isolated from healthy leaves ofCinnamomum loureiroibelonging to six genera:Botryosphaeria,Colletotrichum,Diaporthe,Fusarium,Neopestalotiopsis, andPestalotiopsis. All isolated strains were cultured and further extracted with ethyl acetate solvent. Antimicrobial activity of all crude endophytic fungal extracts was analyzed using disc diffusion assay against six bacterial and two fungal pathogens. Crude extracts of strains MFLUCC15-1130 and MFLUCC15-1131 showed broad-spectrum antimicrobial activity against all tested pathogens. Activity againstBacillus cereusandStaphylococcus epidermidiswas notable, showing the lowest minimum inhibitory concentration at 3.91 μg/mL. Antioxidant activity of all crude endophytic fungal extracts was also evaluated based on 2,2-diphenyl-1-picrylhydrazyl assay. Significant antioxidant activity was detected in the crude extracts of fungus MFLUCC15-1130 and MFLUCC15-1131 with IC50of 22.92 ± 0.67 and 37.61 ± 0.49 μg/mL, respectively. Using molecular identification, MFLUCC15-1130 and MFLUCC15-1131 were identified asNeopestalotiopsissp. andDiaporthesp., respectively. The major chemical constituents produced by both crude extracts were identified by gas chromatography-mass spectrometry. Eugenol, myristaldehyde, lauric acid, and caprylic acid were the primary antimicrobial and antioxidant compounds in both crude extracts. This is the first report of eugenol being a biologically active compound ofNeopestalotiopsissp. andDiaporthesp. fungal endophytes. Eugenol has been reported as antimicrobial and antioxidant agents with agronomic applications. Thus the two newly-isolated endophytes may be used for eugenol production, which in turn can be used in a variety of applications.


2016 ◽  
Vol 78 (6-12) ◽  
Author(s):  
Amir H. M. S. ◽  
Nurun N. ◽  
Nida Iqbal ◽  
Nur F. R. ◽  
Lee L. H. ◽  
...  

Natural sources of antioxidants are derived from fruits, vegetables and wine, whilst artificial supplements are from teas and spices. Sweet potato (Ipomoea batatas) is an excellent natural source of vitamins and minerals, and likely a great source of antioxidant. The objective of this study  is to analyze the antioxidant activity of orange sweet potato (Vitato) and  purple sweet potato (All purple), prepared as heat dry and  moist heat for 30 minutes at 100oC. All the samples were obtained from Pasir Puteh and MARDI Telong, Bachok, Kelantan, respectively. Both samples were soaked into methanol to obtain the crude extract prior to analyzing for antioxidant activity by using 2, 2-diphenyl-1-picryl hydrazyl (DPPH). IC50 values of dry heat and moist heat Vitato were 0.40mg/L and 0.20mg/L while dry heat and moist heat, All purple were 0.32mg/L and 0.19mg/L, respectively. Both moist heat samples enjoyed higher scavenging activities compared to dry heat samples. However, the All purple sample of moist heat is the most superior one. Significant difference of IC50values between dry heat and moist heat sample differ significantly. Thus, this study clearly demonstrated that moist heat sweet potato exhibited  excellent increase in antioxidant activity.


2020 ◽  
Vol 13 (4) ◽  
pp. 68
Author(s):  
Anna Baldisserotto ◽  
Monica Demurtas ◽  
Ilaria Lampronti ◽  
Massimo Tacchini ◽  
Davide Moi ◽  
...  

In the search of multifunctional compounds we designed benzimidazole derivatives endowed with phenolic hydroxy groups and a hydrazone moiety as potential radical-scavenger and the antioxidant agents. The target molecules have been prepared by a simple synthetic procedure and tested for their antioxidant activity by DPPH, FRAP, and ORAC test, for photoprotective activity against UV rays and for antiproliferative activity against Colo-38 melanoma cells. Furthermore, two different dermocosmetic formulations were prepared with the compounds endowed with the best antioxidant and photoprotective profile and their release from formulation evaluated using Franz Cells system. High antioxidant activity is related to the presence of at least two hydroxy groups on arylidene moiety of benzimidazoles. Structure activity analysis revealed that the position of hydroxy groups is crucial for antioxidant activity as well as the presence of a 2-hydroxy-4-(diethylamino)arylidene group. The same correlation pattern was found to be related to photoprotective activity resulting in an UVA Protection Factor better than the commercial solar filter PBSA and antiproliferative activity against melanoma cells without producing cytotoxicity on normal keratinocytes. The release analysis indicated that high antioxidant activities are achieved with limited release at concentration compatible with the use as UV sunscreen filter.


2016 ◽  
Vol 2016 ◽  
pp. 1-17 ◽  
Author(s):  
Anna Maria Mileo ◽  
Stefania Miccadei

Cancer onset and progression have been linked to oxidative stress by increasing DNA mutations or inducing DNA damage, genome instability, and cell proliferation and therefore antioxidant agents could interfere with carcinogenesis. It is well known that conventional radio-/chemotherapies influence tumour outcome through ROS modulation. Since these antitumour treatments have important side effects, the challenge is to develop new anticancer therapeutic strategies more effective and less toxic for patients. To this purpose, many natural polyphenols have emerged as very promising anticancer bioactive compounds. Beside their well-known antioxidant activities, several polyphenols target epigenetic processes involved in cancer development through the modulation of oxidative stress. An alternative strategy to the cytotoxic treatment is an approach leading to cytostasis through the induction of therapy-induced senescence. Many anticancer polyphenols cause cellular growth arrest through the induction of a ROS-dependent premature senescence and are considered promising antitumour therapeutic tools. Furthermore, one of the most innovative and interesting topics is the evaluation of efficacy of prooxidant therapies on cancer stem cells (CSCs). Several ROS inducers-polyphenols can impact CSCs metabolisms and self-renewal related pathways. Natural polyphenol roles, mainly in chemoprevention and cancer therapies, are described and discussed in the light of the current literature data.


Author(s):  
Resmi Mustarichie

Objective: The aim of this study is to investigate antioxidant activity and phytochemical screening of ethanol extract, fractions of water, ethyl acetate, and n-hexane from mistletoe tea (Scurrula atropurpurea Bl. Dans).Methods: Simplicia extracted using soxhlet equipment with 96% ethanol. Fractionation was conducted using liquid-liquid extraction using a solvent of water, ethyl acetate and n-hexane. Screening of phytochemical and antioxidant activity was performed against these fractions. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl method using ultraviolet-visible spectrophotometry with ascorbic acid as standard. Phytochemical screening was conducted based on the method of Farnsworth.Results: The IC50 values of ethanol extract, water fraction, fraction of ethyl acetate, and n-hexane fraction were 21.92 ppm, 89.57 ppm, 14.08 ppm, and 162.09 ppm, respectively, whereas for ascorbic acid was 4.41 ppm. The ethanol extract and ethyl acetate fraction contained compounds were the same group, polyphenolic, tannins, flavonoids, monoterpenoid, steroids, triterpenoids, and quinones. Fraction of water contained compounds such as polyphenolic group, flavonoids, monoterpenoids, sesquiterpenoids, steroids, and triterpenoids. n-hexane fraction compounds contained steroids and triterpenoids.Conclusion: The ethanol extract, water fraction, ethyl acetate fraction, and n-hexane fraction showed antioxidant activities. The ethanol extract, fractions of water, and ethyl acetate fraction contained flavonoids and polyphenolic potential as antioxidants.Keywords: Mistletoe tea, Scurrula atropurpurea, Antioxidant, 2,2-diphenyl-1-picrylhydrazyl, Ascorbic acid.


2009 ◽  
Vol 64 (3-4) ◽  
pp. 197-200 ◽  
Author(s):  
Hari Datta Bhattarai ◽  
Babita Paudel ◽  
Hong Kum Lee ◽  
Hyuncheol Oh ◽  
Joung Han Yim

Antioxidant agents against reactive oxygen species can be used for several cosmetic and medicinal applications. This study’s objective was to evaluate the antioxidant activities of Polytrichastrum alpinum (Hedw.) G. L. Sm. (Polytrichaceae), an Antarctic moss species collected from King George Island (Antarctica). The identifi cation of the moss species was performed on the basis of morphological characteristics and molecular sequencing of the 18S rRNA gene. Two benzonaphthoxanthenones: ohioensins F and G, were isolated from the extract after several chromatographic procedures. The various in vitro antioxidant capacities of a methanolic extract of P. alpinum and the isolated compounds were evaluated by analyzing the scavenging capacities of free radicals of 2,2-azino-bis(3-ethylbenzthiazoline- 6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH), the total phenol assay with Folin-Ciocalteu reagent, the ferric ion (Fe3+) reducing power and the nitric oxide (NO) scavenging activity and compared to those of commercial standards for each assay. The experimental data showed that even the crude extract of P. alpinum exhibited potent antioxidant activity. The antioxidant activity was increased two- to seven-fold for the purified compounds. The antioxidant activities of both purified compounds were found to be more or less the same in all experiments. However, the obtained data showed that the Fe3+ reducing power of the purified compounds and crude methanolic extract was almost the same suggesting the presence of other stronger reducing agents in the methanolic extract which could not be isolated in the present experiment. Therefore, further work on the isolation of these stronger antioxidant agents from this moss specimen of the extreme environment is warranted. Developments of laboratory mass culture techniques are anticipated to achieve bulk production of the active constituents for commercial application.


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