scholarly journals In-Vitro Evaluation of Antioxidant, Antiproliferative and Photo-Protective Activities of Benzimidazolehydrazone Derivatives

2020 ◽  
Vol 13 (4) ◽  
pp. 68
Author(s):  
Anna Baldisserotto ◽  
Monica Demurtas ◽  
Ilaria Lampronti ◽  
Massimo Tacchini ◽  
Davide Moi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antiproliferative Activity ◽  
Antioxidant Activities ◽  
Melanoma Cells ◽  
Benzimidazole Derivatives ◽  
Radical Scavenger ◽  
Correlation Pattern ◽  
Multifunctional Compounds ◽  
Antioxidant Agents ◽  
Hydroxy Groups

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.

scholarly journals HPLC-DAD Polyphenolic Profiling and Antioxidant Activities of Sorghum bicolor during Germination

Agronomy ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 417
Author(s):  
Ioana Otilia Ghinea ◽  
Maria Daniela Ionica Mihaila ◽  
Giorgiana-Valentina Blaga (Costea) ◽  
Sorin Marius Avramescu ◽  
Mihaela Cudalbeanu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Sorghum Bicolor ◽  
Antioxidant Activities ◽  
Total Phenolic ◽  
Radical Scavenger ◽  
Ultrasound Assisted Extraction ◽  
Food Ingredient ◽  
Radical Scavenger Activity ◽  
Scavenger Activity ◽  
Sorghum Grains

The purpose of this study was to assess the suitability of the Romanian Albanus hybrid of Sorghum bicolor as a potential functional food ingredient. Ultrasound-assisted extraction in different solvents, together with spectrophotometric and chromatographic methods, was used to monitor the variation in total phenolic and flavonoid content and the antioxidant activity of raw sorghum grains before and during short germination periods (24, 36 and 48 h). The High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) investigation of the extracts revealed that the ungerminated sorghum grains extracted with methanol had the highest diversity of phenolic compounds, while the total phenolic content (TPC) was the highest after 36 h of germination in both extract types: 1853 mg GAE/100 g for the methanolic extract and 1726 mg GAE/100 g for the ethanolic extract. The findings of this study showed that the TPC of sorghum extracts is strongly correlated with their antioxidant activity and, overall, that the studied extracts presented a good radical scavenger activity, which supports the benefits of alimentary uses of Sorghum bicolor grains.

scholarly journals Antioxidant Studies of Thiazole Ring Bearing Chalcone Derivatives

2021 ◽  
pp. 355-359
Author(s):  
Ashok Babu Kasetti ◽  
Jayesh Dwivedi ◽  
Ravindra Nagasuri
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Thiazole Ring ◽  
Chalcone Derivatives ◽  
Antioxidant Agents ◽  
Ic50 Values ◽  
The Common ◽  
Common Problems

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.

scholarly journals Production of eugenol from fungal endophytesNeopestalotiopsissp. andDiaporthesp. isolated fromCinnamomum loureiroileaves

PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e6427 ◽  
Author(s):  
Chutima Tanapichatsakul ◽  
Sarunpron Khruengsai ◽  
Sakon Monggoot ◽  
Patcharee Pripdeevech
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Endophytic Fungi ◽  
Antioxidant Activities ◽  
Chemical Constituents ◽  
Fungal Endophytes ◽  
Biologically Active ◽  
Crude Extracts ◽  
Antioxidant Agents ◽  
Fungal Extracts

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.

In vitro Antioxidant Capacities of Two Benzonaphthoxanthenones: Ohioensins F and G, Isolated from the Antarctic Moss Polytrichastrum alpinum

2009 ◽  
Vol 64 (3-4) ◽  
pp. 197-200 ◽  
Author(s):  
Hari Datta Bhattarai ◽  
Babita Paudel ◽  
Hong Kum Lee ◽  
Hyuncheol Oh ◽  
Joung Han Yim
Keyword(s):  
Antioxidant Activity ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Reducing Power ◽  
Commercial Application ◽  
Moss Species ◽  
Antioxidant Capacities ◽  
Antioxidant Agents ◽  
Antarctic Moss

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.

scholarly journals Bioactivities of plant extracts collected in Halmahera, Indonesia: A bioprospection study of underexplored plant species

2021 ◽  
pp. 376-384
Author(s):  
Marlin Megalestin Raunsai ◽  
Kartika Dyah Palupi ◽  
Ahmad Fathoni ◽  
Andria Agusta
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Plant Species ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Total Phenolic ◽  
Antioxidant Agents ◽  
Ethanolic Extracts ◽  
Potential Sources ◽  
Weak Antibacterial Activity

The discovery of new antibiotics to overcome the growing resistance problem as well as the discovery of new natural, safe antioxidants to combat oxidative stress are still urgently needed. Medicinal plants are known to produce potential therapeutic substances which are more biologically selective than synthetic compounds. Therefore, we explored the bioactivities of 35 ethanolic extracts from 24 underexplored plant species collected in Halmahera, to find potential sources for antibacterial and antioxidant agents.  Dried plant parts were extracted using ethanol 96%. Thin layer chromatography-direct-bioautography (TLC-DB) and minimum inhibitory concentration (MIC) determination were used to evaluate the antibacterial effect. Antioxidant activity was determined against DPPH using TLC-DB and microdilution assay. Total phenolic content (TPC) was determined using Folin-Ciocalteu’s method. The ethanolic extracts exhibited moderate to weak antibacterial activity against Escherichia coli and Staphylococcus aureus. However, the leaf extract of Elaeocarpus dolichostylus, Elaeocarpus multiflorus, and Psychotria celebica as well as the stem bark extract of Elaeocarpus dolichostylus, Cinnamomum sintoc, and Garcinia latissima displayed very strong antioxidant activities against DPPH with AAI values between 4.60 to 13.42. A strong correlation between TPC and antioxidant activity with r = 0.8712 was observed. Despite the moderate to weak antibacterial activity, eight underexplored plant species exhibit strong antioxidant activities. A high correlation between TPC and antioxidant activity indicating a prominent role of phenolic compounds in the plants’ antioxidant properties. These findings indicate that collected plants from Halmahera are potential to be studied and developed further as the potential sources for novel antioxidants.

scholarly journals Anti-Melanogenic Effect of Ethanolic Extract of Sorghum bicolor on IBMX–Induced Melanogenesis in B16/F10 Melanoma Cells

Nutrients ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 832 ◽  
Author(s):  
Hye Ju Han ◽  
Seon Kyeong Park ◽  
Jin Yong Kang ◽  
Jong Min Kim ◽  
Seul Ki Yoo ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Sorghum Bicolor ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Melanoma Cells ◽  
Total Phenolic ◽  
Skin Whitening

To evaluate possibility as a skin whitening agent of Sorghum bicolor (S. bicolor), its antioxidant activity and anti-melanogenic effect on 3-isobutyl-1-methylxanthine (IBMX)-induced melanogenesis in B16/F10 melanoma cells were investigated. The result of total phenolic contents (TPC) indicated that 60% ethanol extract of S. bicolor (ESB) has the highest contents than other ethanol extracts. Antioxidant activity was evaluated using the 2,2’-azino-bis-(3-ethylbenzothiazolin-6-sulfonic acid) diammonium salt (ABTS)/1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging activities and malondialdehyde (MDA) inhibitory effect. These results showed ESB has significant antioxidant activities. Inhibitory effect against tyrosinase was also assessed using L-tyrosine (IC50 value = 89.25 μg/mL) and 3,4-dihydroxy-L-phenylalanine (L-DOPA) as substrates. In addition, ESB treatment effectively inhibited melanin production in IBMX-induced B16/F10 melanoma cells. To confirm the mechanism on anti-melanogenic effect of ESB, we examined melanogenesis-related proteins. ESB downregulated melanogenesis by decreasing expression of microphthalmia-associated transcription factor (MITF), tyrosinase and tyrosinase-related protein (TRP)-1. Finally, 9-hydroxyoctadecadienoic acid (9-HODE), 1,3-O-dicaffeoylglycerol and tricin as the main compounds of ESB were analyzed using the ultra-performance liquid chromatography-ion mobility separation-quadrupole time of flight/tandem mass spectrometry (UPLC-IMS-QTOF/MS2). These findings suggest that ESB may have physiological potential to be used skin whitening material.

scholarly journals Antioxidant Activity of Bacterial Cellulose Based Edible Films Incorporated with Catechin and Citrus aurantium L (Bergamot) Essential Oil

2018 ◽  
Vol 2 (6) ◽  
pp. 30-36
Author(s):  
Keyword(s):  
Antioxidant Activity ◽  
Bacterial Cellulose ◽  
Food Packaging ◽  
Antioxidant Activities ◽  
Edible Films ◽  
Antioxidant Compounds ◽  
Natural Material ◽  
Antioxidant Agents ◽  
Dpph Method ◽  
Bergamot Oil

Bacterial cellulose-based edible films have been known as natural material and eco-friendly fibers for food packaging. The edible films contain carboxymethyl cellulose (CMC), Tween 80 and glycerol as an external food protection. The edible films as carriers of ingredients agents (antimicrobial, antioxidant) preserve the quality of food product. Incorporating antioxidant compounds into edible films provide the novel approach to improve the safety, shelf-life of foods and physical properties. In present study, the antioxidant agents are cathechin and bergamot oil. The study was aimed to investigate the antioxidant activities of edible films incorporated with catechin (FC), bergamot oil (FB) and both cathechin and bergamot oil (FCB). Antioxidant activity was carried out using DPPH method. The results showed that antioxidant activities of FC, FB and FCB with various concentrations antioxidant agents (1-2.5%) were 65.78%, 73.16% and 81.07% respectively. GC-MS showed bergamot oil contained compounds limonene (23,66%) , linalool (19.44), and lynalil acetate (37,88). SEM showed the surface of edible films FB and FCB were fine and smooth. Edible film only and FC revealed the cracks on the surfaces of films. Alll compounds of edible films were still available based on FTIR results.

Synthesis, Antimicrobial, Antioxidant and Molecular Docking Studies on Novel 6-Methoxybenzothiazole-piperazine Derivatives with Propanamide Chain

2020 ◽  
Vol 20 (19) ◽  
pp. 1733-1741
Author(s):  
Nesrin Atiah Alhusadi ◽  
Bengisu Turgutalp ◽  
Inci Deniz ◽  
Ebru Turkoz Acar ◽  
Hande Sipahi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Antioxidant Activities ◽  
Docking Studies ◽  
Superoxide Dismutase 1 ◽  
Disc Diffusion ◽  
Disc Diffusion Assay ◽  
Piperazine Derivatives ◽  
Antioxidant Agents ◽  
Diffusion Assay

Background: Infectious diseases are a major threat in the developing world and the discovery of novel antimicrobial agents remains to be crucial due to acquired resistance by the microorganisms. Additionally, various diseases can be prevented with antioxidant agents as they can eliminate the harmful effects of reactive oxygen species. Objective: In this study, it was aimed to synthesize novel compounds bearing N-(6- methoxybenzothiazol-2-yl)-3-(4-substitued piperazinyl)propanamide backbone that had antimicrobial and antioxidant activities. Mechanisms of activity were aimed to be revealed by docking studies. Methods: Antimicrobial activities were tested by agar-based disc diffusion assay, and antioxidant activities were determined by CUPRAC assay. Results: In agar-based disc diffusion assay, the most active compounds were 2b and 2e against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. Compounds 2e and 2j showed promising antioxidant activity in CUPRAC assay. Docking studies were performed to optimize the interactions of compounds with DNA gyrase subunit B of S. aureus. Under the light of docking studies, a new compound with potential GyrB inhibition was designed. Antioxidant activity was also supported by docking studies on superoxide dismutase 1 enzyme in which interactions with key residues were observed. Conclusion: Ten novel benzothiazole-piperazine derivatives were synthesized and their antimicrobial and antioxidant activities were evaluated. Superoxide dismutase 1 enzyme was suggested to be a possible target for the antioxidant activity of the series.

Synthesis, Antiproliferative, and Antioxidant Activities of Substituted N-[(1,3,4-Oxadiazol-2-yl) Methyl] Benzamines

2020 ◽  
Vol 17 (2) ◽  
pp. 145-154 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Lakshya Bhandari ◽  
Shally Makkar ◽  
Rajan Singh ◽  
Mohd. Zaheen Hassan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Drug Concentrations ◽  
Antioxidant Agents ◽  
Ic50 Value ◽  
Mcf 7

Background: Oxadiazole emerged as an important class of heterocyclic compound with diverse biological activities like anticancer, antitubercular, anticonvulsant, anti-tubulin, antimicrobial, anti-inflammatory, antioxidant etc. Objective: The objective of this study is to synthesis series of twelve substituted N-[(1,3,4-oxadiazol-2- yl)methyl]benzamines (6a-l) and their evaluation as antiproliferative and antioxidant agents. Methods: The substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines (6a-l) analogues were synthesized as per the reported procedure. The antiproliferative activity was tested against nine different panels cancer cell lines (leukemia, colon, renal, non-small cell lung, breast, CNS, melanoma, prostate, and ovarian cancer) at 10 µM drug concentrations as per the NCI US Protocol. Results: 2-(5-((3-Chloro-4-fluorophenylamino)methyl)-1,3,4-oxadiazol-2-yl)phenol (6e) revealed the significant antiproliferative activity among the series of title compounds (6a-l). The compound, 6e showed maximum sensitivity towards CCRF-CEM, MCF-7, MOLT-4, T-47D, and SR cell lines with percent growth inhibitions (%GIs) of 79.92, 56.67, 39.62, 34.71 and 33.35, respectively. Furthermore, the compounds, 6e and 6c showed promising antioxidant activity with an IC50 value of 15.09 and 19.02 µM, respectively in DPPH free radicals (FR) scavenging activity.R Conclusion: The present study may support a significant value in cancer drug discovery programme.

scholarly journals Synthesis and Structure-Activity Relationship of Daphnetin Derivatives as Potent Antioxidant Agents

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2476 ◽  
Author(s):  
Yangliu Xia ◽  
Chen Chen ◽  
Yong Liu ◽  
Guangbo Ge ◽  
Tongyi Dou ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Phenyl Group ◽  
Negative Effects ◽  
Scavenging Effect ◽  
Chemical Structures ◽  
Antioxidant Agents ◽  
Pharmaceutical Properties

In this study, daphnetin 1 was chosen as the lead compound, and C-3 or C-4-substituted daphnetins were designed and synthesized to explore the potential relationship between the antioxidant activities and the chemical structures of daphnetin derivatives. The antioxidant activities of the generated compounds were evaluated utilizing the free radical scavenging effect on 2,2′-diphenyl-1-picrylhydrazyl, 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulfonate) cation, and the ferric reducing power assays, and were then compared with those of the standard antioxidant Trolox. The results showed that the catechol group was the key pharmacophore for the antioxidant activity of the daphnetins. The introduction of an electron-withdrawing hydrophilic group at the C-4 position of daphnetin enhanced the antioxidative capacity, but this trend was not observed for C-3 substitution. In addition, introduction of a a hydrophobic phenyl group exerted negative effects on the antioxidant activity in both the C-3 and C-4 substitutions. Among all of the derivatives tested, the most powerful antioxidant was 4-carboxymethyl daphnetin (compound 9), for which the strongest antioxidant activity was observed in all of the assays. In addition, compound 9 also displayed strong pharmaceutical properties in the form of metabolic stability. To summarize, compound 9 holds great potential to be developed as an antioxidant agent with excellent antioxidant activity and proper pharmacokinetic behavior.

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