Pyrrolo[1,2-a]azepines Coupled with Benzothiazole and Fluorinated Aryl Thiourea Scaffolds as Promising Antioxidant and Anticancer Agents

2019 ◽  
Vol 19 (15) ◽  
pp. 1855-1862
Author(s):  
Rahul V. Patel ◽  
Bhupendra M. Mistry ◽  
Riyaz Syed ◽  
Nikhil M. Parekh ◽  
Han-Seung Shin
Keyword(s):  
Anticancer Agents ◽  
Mdck Cells ◽  
Radical Scavenging Activity ◽  
Small Cell Lung Carcinoma ◽  
Radical Scavenging ◽  
Colon Adenocarcinoma ◽  
Cytotoxic Agents ◽  
Health Concern ◽  
Anticancer Activities ◽  
Cell Lung Carcinoma

Background: Cancer remains a major health concern throughout history and is responsible for huge numbers of deaths globally. The sensitivity of cancer cells to anticancer drugs is a crucial factor for developing effective treatments. Methods: Pyrrolo[1,2-a]azepines coupled with benzothiazole and fluorinated aryl thiourea scaffolds have been synthesized, and their potential as cytotoxic agents was investigated against different cancer cell lines such as human ovarian cancer (SK-OV-3), cervical cancer (HeLa), colon adenocarcinoma (HT-29) and non-small-cell lung carcinoma (A549). Cytotoxicity of new compounds was confirmed using SRB assay against non-cancer MDCK cell line. In addition, free radical scavenging activity of new pyrrolo[1,2-a]azepines was examined by adopting DPPH and ABTS assays. Results: The results concluded that the presence and position of fluorine atom(s) on the thiourea unit played a significant role in order to gain anticipated efficacies. Results of the cytotoxic assay against non-cancer MDCK cells showed that these new derivatives are safe to study further. New structures were confirmed using spectral and elemental analyses. Conclusion: Pyrrolo[1,2-a]azepines endowed with a benzothiazole entity and fluorinated aryl thiourea substituents were derived aiming to furnish remarkable antioxidant and anticancer activities. New molecules generated showed interesting biological result correlated with the structure and substituent of the final derivatives. Specifically, numbers and position of fluorine atoms on the thiourea unit influenced the biological profile of the mentioned compounds.

scholarly journals Investigation of antioxidant and anticancer activities of unsaturated oligo-galacturonic acids produced by pectinase of Streptomyces hydrogenans YAM1

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Afrouzossadat Hosseini Abari ◽  
Hamed Amini Rourani ◽  
Seyed Mahdi Ghasemi ◽  
Hyun Kim ◽  
Yun-Gon Kim
Keyword(s):  
Radical Scavenging Activity ◽  
Flow Cytometric Analysis ◽  
Radical Scavenging ◽  
Anticancer Activities ◽  
Pectin Degradation ◽  
New Approach ◽  
Flight Mass Spectrometry ◽  
Highly Active ◽  
Carbohydrate Polymer ◽  
Pectinase Activity

AbstractPectin, a diverse carbohydrate polymer in plants consists of a core of α-1,4-linked D-galacturonic acid units, includes a vast portion of fruit and agricultural wastes. Using the wastes to produce beneficial compounds is a new approach to control the negative environmental impacts of the accumulated wastes. In the present study, we report a pectinase producing bacterium Streptomyces hydrogenans YAM1 and evaluate antioxidative and anticancer effects of the oligosaccharides obtained from pectin degradation. The production of oligosaccharides due to pectinase activity was detected by thin layer chromatography (TLC) and matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF MS). Our results revealed that S. hydrogenans YAM1 can degrade pectin to unsaturated pectic oligo-galacturonic acids (POS) with approximately 93% radical scavenging activity in 20 mg/mL which it is more than 50% of the same concentration of pectin. Flow cytometric analysis revealed that MCF-7 cells viability decreased more than 32 and 92% following treatment with 6 and 20 mg/mL POS after 24 h, respectively. It is suggested that pectin degradation by S. hydrogenans YAM1 is not only a new approach to produce highly active compounds from fruit wastes, but also is an effective method to remove fibrous pollutants from different environments.

scholarly journals Antioxidant and Anticancer Activities of Wampee (Clausena lansium(Lour.) Skeels) Peel

2009 ◽  
Vol 2009 ◽  
pp. 1-6 ◽  
Author(s):  
K. Nagendra Prasad ◽  
Jing Hao ◽  
Chun Yi ◽  
Dandan Zhang ◽  
Shengxiang Qiu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Total Phenolic ◽  
Liver Carcinoma ◽  
Scavenging Activity ◽  
Anticancer Activities

Antioxidant activities of wampee peel extracts using five different solvents (ethanol, hexane, ethyl acetate, butanol and water) were determined by using in-vitro antioxidant models including total antioxidant capability, 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity, reducing power, and superoxide scavenging activity. Ethyl acetate fraction (EAF) exhibited the highest antioxidant activity compared to other fractions, even higher than synthetic antioxidant butylated hydroxyl toluene (BHT). In addition, the EAF exhibited strong anticancer activities against human gastric carcinoma (SGC-7901), human hepatocellular liver carcinoma (HepG-2) and human lung adenocarcinoma (A-549) cancer cell lines, higher than cisplatin, a conventional anticancer drug. The total phenolic content of wampee fraction was positively correlated with the antioxidant activity. This is the first report on the antioxidant and anticancer activities of the wampee peel extract. Thus, wampee peel can be used potentially as a readily accessible source of natural antioxidants and a possible pharmaceutical supplement.

Synthesis and Evaluation of bis-Schiff Bases of Carbohydrazide as Antioxidant and Cytotoxic Agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Sarosh Iqbal ◽  
Shumaila Kiran ◽  
Shahida Perveen ◽  
Rizwana Malik ◽  
Muhammad Taha ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cytotoxic Agents ◽  
Scavenging Activity ◽  
Standard Drug ◽  
Age Related ◽  
Dpph Radical Scavenging ◽  
Better Than

Background & Introduction : Antioxidants are known to prevent oxidative stress-induced damage to the biomolecules and thus, delay the onset of cancers and many age-related diseases. Therefore, the development of novel and potent antioxidants is justified. Method: During this study, we synthesized symmetrical bis-Schiff bases of carbohydrazide 1-27, and evaluated their in vitro antioxidative activity and cytotoxic activity. Results: Among synthesized compounds, six compounds 20 (IC50 = 12.89 ± 0.02 µM), 16 (IC50 = 14.32 ± 0.43 µM), 17 (IC50 = 18.52 ± 0.83 µM), 19 (IC50 = 22.84 ± 0.62 µM), 24 (IC50 = 35.1 ± 0.82 µM) and 15 (IC50 = 40.03 ± 1.06 µM) showed an excellent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, better than the standard butylatedhydroxyanisole (BHA) (IC50 = 44.6 ± 0.6 µM). Likewise, two compounds 16 (IC50 = 4.3 ± 1.3 µM) and 20 (IC50 = 6.6 ± 1.6 µM) showed oxidative burst scavenging activity better than the standard drug ibuprofen (IC50 = 11.2 ± 1.9 µM). Some synthesized compounds showed good to moderate toxicity against prostate cancer (PC-3) cell lines. Conclusion: This study has identified potent antioxidants and good cytotoxic agents with the potential to further investigate.

scholarly journals Circulating Tumour Cells (CTCs) in NSCLC: From Prognosis to Therapy Design

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1879
Author(s):  
Zdeněk Kejík ◽  
Robert Kaplánek ◽  
Petr Dytrych ◽  
Michal Masařík ◽  
Kateřina Veselá ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Epithelial Mesenchymal Transition ◽  
Small Cell Lung Carcinoma ◽  
Meta Analysis ◽  
Tumour Cells ◽  
Circulating Tumour Cells ◽  
Cell Lung Carcinoma ◽  
Mesenchymal Transition ◽  
Standard Methods ◽  
The Impact

Designing optimal (neo)adjuvant therapy is a crucial aspect of the treatment of non-small-cell lung carcinoma (NSCLC). Standard methods of chemotherapy, radiotherapy, and immunotherapy represent effective strategies for treatment. However, in some cases with high metastatic activity and high levels of circulating tumour cells (CTCs), the efficacy of standard treatment methods is insufficient and results in treatment failure and reduced patient survival. CTCs are seen not only as an isolated phenomenon but also a key inherent part of the formation of metastasis and a key factor in cancer death. This review discusses the impact of NSCLC therapy strategies based on a meta-analysis of clinical studies. In addition, possible therapeutic strategies for repression when standard methods fail, such as the administration of low-toxicity natural anticancer agents targeting these phenomena (curcumin and flavonoids), are also discussed. These strategies are presented in the context of key mechanisms of tumour biology with a strong influence on CTC spread and metastasis (mechanisms related to tumour-associated and -infiltrating cells, epithelial–mesenchymal transition, and migration of cancer cells).

scholarly journals Phenolic Fractions from Vaccinium vitis-idaea L. and Their Antioxidant and Anticancer Activities Assessment

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1261
Author(s):  
Gabriele Vilkickyte ◽  
Lina Raudone ◽  
Vilma Petrikaite
Keyword(s):  
Antioxidant Activity ◽  
Biological Activity ◽  
Cell Lines ◽  
Radical Scavenging ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Anticancer Activities ◽  
Cell Renal Cell Carcinoma ◽  
Human Malignant Melanoma ◽  
Ht 29

Lingonberry leaves and fruits are associated with a range of potential bioactivities related to their phenolic content and composition, but the identification of major biological activity markers remains limited. The present study aimed at the isolation of lingonberry phenolic fractions and biological activity evaluation of them. Crude dry extracts of lingonberry leaves and fruits were fractionated by chromatography using Sephadex LH-20 and analyzed by validated HPLC-PDA method. For each fraction, the anticancer activity against human clear cell renal cell carcinoma (CaKi-1), human colon adenocarcinoma (HT-29), and human malignant melanoma (IGR39) cell lines was determined using MTT assay, and the radical scavenging, reducing, and chelating activities were investigated using ABTS, FRAP, and FIC assays, respectively. Further, 28 phenolics were identified and quantified in the crude extract of lingonberry leaves and 37 in the extract of fruits. These compounds, during fractionation steps, were selectively eluted into active fractions, enriched with different groups of phenolics—monophenols, anthocyanins, phenolic acids, catechins, flavonols, or proanthocyanidins. Fractions of lingonberry leaves and fruits, obtained by the last fractionation step, proved to be the most active against tested cancer cell lines and possessed the greatest antioxidant activity. In this perspective, the predominant compounds of these fractions—polymeric and mainly A-type dimeric proanthocyanidins—also quercetin can be considered to be anticancer and antioxidant activity markers of lingonberries.

Comparative Real Time EPR Investigation of Natural and Synthetic Antioxidants: As Potential Anticancer Agents and Radio-protectors

2017 ◽  
Vol 2 (3) ◽  
pp. 301
Author(s):  
Yanka Karamalakova ◽  
Galina Nikolova ◽  
Rakesh Kumar Sharma ◽  
Raj Kumar ◽  
Rajesh Arora ◽  
...  
Keyword(s):  
Free Radical ◽  
Anticancer Agents ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Natural Antioxidants ◽  
Synthetic Antioxidants ◽  
Anticancer Chemotherapy ◽  
Natural And Synthetic

<p>The purpose of this study was to evaluate and compare the free-radical scavenging activity against DPPH stable radical and protective properties of the natural products SQGD and P. corylifolia and synthetic nitroxyl- free radical containing nitrosoureas SLENU and SLCNUgly against in vivo oxidative toxicity of antitumor drug CCNU. It was found statistically significant increase in the DPPH radical-scavenging capacity of both extracts with increase of radiation. The natural antioxidants were localised mainly in the organs and blood after EPR biodistribution study. All combinations of natural extracts/ synthetics agents exhibited considerably lower levels of Asc. radicals as compared to controls. It should be mentioned that the natural antioxidants possess higher oxidative protection in comparison with the synthetic antioxidants. Considerable decrease in ROS production in livers of mice was found after treatment with SQGD, P. corylifolia and SLENU, alone, compared to controls.In conclusion, because of well-expressed antioxidant activities of natural and synthetic antioxidants they might be used in the combination anticancer chemotherapy for reducing toxicity caused by anticancer drugs and/or low levels radiation therapy.</p>

scholarly journals TheConyza trilobaExtracts with High Chlorophyll Content and Free Radical Scavenging Activity Had Anticancer Activity in Cell Lines

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Wael M. El-Sayed ◽  
Warda A. Hussin ◽  
Ahmed A. Mahmoud ◽  
Mohamed A. AlFredan
Keyword(s):  
Free Radical ◽  
Chlorophyll Content ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Methylene Chloride ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Antimutagenic Activity ◽  
Metal Chelating

The discovery of anticancer agents paradigm has been shifted to natural resources to overcome the toxicity of many synthetic agents at early clinical stages. In the present study, the antimutagenic, anticancer, phytochemistry, and free radical scavenging activities of five extracts ofConyza trilobawere investigated. Extracts II (water : methanol), III (methylene chloride), and IV (methylene chloride : methanol) had the highest chlorophyll content and the highest superoxide scavenging, and metal chelating activities comparable to that of trolox. They also showed DPPH•scavenging activities better than that ofα-tocopherol. Virtually all extracts exerted a strong (>40% reduction) antimutagenic activity against sodium azide and benzopyrene. Extracts II, III, and IV showed a remarkable growth inhibition profile with GI50of 0.07–0.87 μg for Hepa1c1c7 and H4IIE1, A549, HT29, and PC3 cell lines and totally abated the growth of all cell lines, except for the breast cells, at 0.3–7.0 μg. The present study found a strong correlation between the chlorophyll content ofConyzaextracts and their DDPH scavenging, metal chelating, and in vitro cytotoxic and cytostatic activities most probably through triggering apoptosis. This study could offer a platform for future studies and help selecting the vital features that identify the extract with potential anticancer activities.

scholarly journals Antibacterial, antioxidant and cytotoxic activities of different fractions of acetone extract from flowers of Dipterocarpus intricatus Dyer (Dipterocarpaceae)

2021 ◽  
Vol 8 (2) ◽  
pp. 273-277
Author(s):  
Hong Thia Le ◽  
Thao Nguyen Luu ◽  
Huynh Mai Thu Nguyen ◽  
Dang HoaiTrang Nguyen ◽  
Pham Tan Quoc Le ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Salmonella Enteritidis ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Acetone Extract ◽  
Cytotoxic Agents ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
First Time

This study has shown for the first time the antimicrobial, antioxidant and cytotoxicity of 3 fractions of acetone extract, including hexane, chloroform and ethyl acetate from flowers of Dipterocarpus intricatus. Antibacterial test using disc diffusion method showed that the chloroform and ethyl acetate fractions inhibited the growth of all the tested bacteria, including Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis, Salmonella typhimurium, Bacillus cereus and Staphylococcus aureus while the hexane fraction showed the antibacterial activity against B. cereus and S. enteritidis. Antioxidant activity and cancer cell resistance of those extracts were conducted using DPPH and MTT methods respectively. As a result, the DPPH radical scavenging activity of the hexane, chloroform and ethyl acetate fractions were determined with the IC50 values of 0.508, 0.22 and 0.075 mg/mL respectively while the cytotoxicity to HepG2 cell line of those fractions was 163.3 ppm, 106.7 ppm and 459.3 ppm. These results suggested the potential application of these fractions isolated from D. intricatus flowers as the natural antimicrobial, antioxidant and cytotoxic agents for medicine.

scholarly journals Evaluation of Selected Nigerian Medicinal Plants for Antioxidant, Antimicrobial and Cytotoxic activities

2021 ◽  
Author(s):  
Samuel Oguntimehin ◽  
Edith Ajaiyeoba ◽  
Omonike Ogbole ◽  
Hannah Dada-Adegbola ◽  
Bosede Oluremi ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Broad Spectrum ◽  
Anticancer Agents ◽  
Phenolic Content ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Medicinal Uses ◽  
Incidence And Mortality

Abstract Background: Increased exposure to pathogens and free radicals contributed to the high incidence and mortality rate of various cancers in Nigeria and globally. Promotion of scientific research on medicinal plants in collaboration with traditional health practitioners to validate claims made on safety, efficacy and quality of traditional medicinal plants in the treatment of cancer is imperative. This study aims at screening extracts of selected Nigerian medicinal plants used traditionally for cancer treatment for antioxidant, antimicrobial and cytotoxic activities towards identification of potential source of new anticancer agents.Methods: Twenty-one extracts from sixteen medicinal plants species were screened for their cytotoxicity on RD, HeLa and Hep-2 cancer cell lines using MTT assay. The DPPH radical scavenging activity of the extracts as well as their Total Phenolic Content (TPC) were evaluated. The extracts were also evaluated for their antimicrobial activity using spectrophotometric growth inhibition method. Results: Extracts of Tetrapleura tetrapleura and Xylopia aethiopica showed high DPPH inhibitory activity and phenolic content. Extracts of X. aethiopica and Anchomanes difformis showed broad spectrum of antibacterial activities while root extracts of Crotolaria retusa and T. tetraptera exhibited antifungal activities comparable (P<0.05) to Ketoconazole. Extracts of Capcicum frutescens, Aspilia africana, X. aethiopica, T. tetraptera and C. retusa showed broad spectrum of cytotoxic activities.Conclusions: Extracts of T. tetraptera and X. aethiopica demonstrated satisfactory activities in all the biological tests which could be linked to their high phenolic contents. The findings support the ethno-medicinal uses of most of the tested medicinal plants.

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