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Cytotoxicity

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Luteolin Inhibits Proliferation, Triggers Apoptosis And Modulates Akt/Mtor And Map Kinase Pathways In Hela Cells, Ritu Raina, Sreepoorna Pramodh, Naushad Rais, Shafiul Haque, Jasmin Shafarin, Khuloud Bajbouj, Mawieh Hamad, Arif Hussain Jan 2021

Luteolin Inhibits Proliferation, Triggers Apoptosis And Modulates Akt/Mtor And Map Kinase Pathways In Hela Cells, Ritu Raina, Sreepoorna Pramodh, Naushad Rais, Shafiul Haque, Jasmin Shafarin, Khuloud Bajbouj, Mawieh Hamad, Arif Hussain

All Works

Flavonoids, a subclass of polyphenols, have been shown to be effective against several types of cancer, by decreasing proliferation and inducing apoptosis. Therefore, the aim of the present study was to assess the anti-carcinogenic potential of luteolin on HeLa human cervical cancer cells, through the use of a cell viability assay, DNA fragmentation assay, mitochondrial membrane potential assay, cell cycle analysis using Annexin/PI staining and flow cytometry, gene expression analysis and a protein profiling array. Luteolin treatment exhibited cytotoxicity towards HeLa cells in a dose- and time-dependent manner, and its anti-proliferative properties were confirmed by accumulation of luteolin-treated cells in …

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New Weldable 316l Stainless Flux-Cored Wires With Reduced Cr(Vi) Fume Emissions Part 1 – Health Aspects Of Particle Composition And Release Of Metals, Yolanda Hedberg Jan 2021

New Weldable 316l Stainless Flux-Cored Wires With Reduced Cr(Vi) Fume Emissions Part 1 – Health Aspects Of Particle Composition And Release Of Metals, Yolanda Hedberg

Chemistry Publications

Welding fumes have been found to be carcinogenic and stainless steel welders may be at higher risk due to increased formation of hexavalent chromium (Cr(VI)). The slag-shielded methods, identified to generate most airborne particles and Cr(VI), would potentially be most harmful. With ever-stricter limits set to protect workers, measures to minimize human exposure become crucial. Austenitic stainless steel flux-cored wires of 316L type have been developed with the aim to reduce the toxicity of the welding fume without compromised usability. Collected particles were compared with fumes formed using solid, metal-cored and standard flux-cored wires. The size, morphology and composition were …

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Investigation Of Olea Ferruginea Roylebark Extracts For Potential In Vitroantidiabetic And Anticancer Effects, Samra Liaqat, Muhammad Islam, Hamid Saeed, Mehwish Iqtedar, Azra Mehmood Jan 2021

Investigation Of Olea Ferruginea Roylebark Extracts For Potential In Vitroantidiabetic And Anticancer Effects, Samra Liaqat, Muhammad Islam, Hamid Saeed, Mehwish Iqtedar, Azra Mehmood

Turkish Journal of Chemistry

This study was conducted to investigate the physicochemical, phytochemical, in vitro antidiabetic and anticancer potential of Olea ferruginea R bark. After extraction using Soxhlet, in vitro antidiabetic and cytotoxic activity on human hepatocellular carcinoma (HepG2) cells was assessed by nonenzymatic glycosylation of hemoglobin assay, alpha-amylase inhibition assay, glucose uptake by yeast cells, and 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay, respectively, and gene expression via real-time polymerase chain reaction. Primary and secondary metabolites were present in the extractants; polyphenols (35.61 ± 0.03) and flavonoids (64.33 ± 0.35) in the chloroform; and polysaccharides in the ethanol (268.75 ± 0.34), and glycosaponins (78.01 ± …

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Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n Jan 2021

Synthesis And Biological Evaluation Of New Pyrazolebenzene-Sulphonamides As Potentialanticancer Agents And Hca I And Ii Inhibitors, Mehtap Tuğrak, Hali̇se İnci̇ Gül, Hi̇roshi̇ Sakagami̇, Rüya Kaya, İlhami̇ Gülçi̇n

Turkish Journal of Chemistry

Cancer is a disease characterized by the continuous growth of cells without adherence to the rules that healthy normal cells obey. Carbonic anhydrase I and II (CA I and CA II) inhibitors are used for the treatment of some diseases. The available drugs in the market have limitations or side effects, which bring about the need to develop new drug candidate compound(s) to overcome the problems at issue. In this study, new pyrazole-sulphonamide hybrid compounds 4-[5-(1,3-benzodioxol-5-yl)-3-aryl-4,5-dihydro-1Hpyrazol- 1-yl]benzenesulphonamides (4a - 4j) were designed to discover new drug candidate compounds. The compounds 4a - 4j were synthesized and their chemical structures were …

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Synthesis And Characterization Of Magnetic Nanocomposite For In Vitro Evaluation Of Irinotecan Using Human Cell Lines, Tuba Tarhan Jan 2021

Synthesis And Characterization Of Magnetic Nanocomposite For In Vitro Evaluation Of Irinotecan Using Human Cell Lines, Tuba Tarhan

Turkish Journal of Chemistry

In this study, magnetic O-carboxymethyl chitosan (MOCC) nanocomposite was synthesized and characterized as a drug delivery system for loading the anticancer drug irinotecan (CPT-11). To increase the drug loading capacity, MOCC was synthesized by linking the carboxyl group functionally to chitosan. Also, several critical factors such as concentration, the dose of MOCC, and contact time for optimum drug loading condition were investigated. The loading capacity of CPT-11 onto MOCC was calculated as 5.6 mg/g, and the loaded drug concentration was calculated as 0.04787 mM at pH value of 5. Besides, the cytotoxic properties of MOCC, CPT- 11 loaded MOCC (MOCC-CPT-11), …

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Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç Jan 2021

Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç

Turkish Journal of Chemistry

The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure with 1H NMR, 13C NMR and FT-IR spectral foundations, which were compatible with literature informations. Antimicrobial activity and cytotoxicity studies were done by disc diffusion and NCI-60 sulphordamine B assay methods. The antimicrobial test results revealed that synthesized compounds have better activity against gram-positive species than gram-negative ones. A total analysis of the antibacterial, antifungal, and antiyeast activity revealed that newly synthesized compounds were really active against Bacillus cereus, Bacillus …

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Biomolecules As Model Indicators Of In Vitro And In Vivo Cold Plasma Safety, Caitlin Heslin, Daniela Boehm, Brendan F. Gilmore, Julianne Megaw, Theresa A. Freeman, Noreen Hickok, Patrick J. Cullen, Paula Bourke Jan 2021

Biomolecules As Model Indicators Of In Vitro And In Vivo Cold Plasma Safety, Caitlin Heslin, Daniela Boehm, Brendan F. Gilmore, Julianne Megaw, Theresa A. Freeman, Noreen Hickok, Patrick J. Cullen, Paula Bourke

Articles

The potential applications for cold plasma in medicine are extensive, from microbial inactivation and induction of apoptosis in cancer cells to stimulating wound healing and enhancing the blood coagulation cascade. The safe bio-medical application of cold plasma and subsequent effect on complex biological pathways requires precision and a distinct understanding of how physiological redox chemistry is manipulated. Chemical modification of biomolecules such as carbohydrates, proteins, and lipids treated with cold plasma have been characterized, however, the context of how alterations of these molecules affect cell behavior or in vivo functionality has not been determined. Thus, this study examines the cytotoxic …

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Screening Of The Small Molecule Library Of Meinox Enables The Identification Of Anticancer Compounds In Pathologically Distinct Cancers, Aynura Mammadova, Ari̇f Mermer, Fati̇h Kocabaş Jan 2021

Screening Of The Small Molecule Library Of Meinox Enables The Identification Of Anticancer Compounds In Pathologically Distinct Cancers, Aynura Mammadova, Ari̇f Mermer, Fati̇h Kocabaş

Turkish Journal of Biology

Small molecules are widely used for the modulation of the molecular basis of diseases. This makes them the perfect tool for discovering and developing new therapeutics. In this work, we have established a library of small molecules in house and characterized its molecular and druglike properties. We have shown that most small molecules have molecular weights less than 450. They have pharmaceutically relevant cLogP, cLogS, and druglikeness value distributions. In addition, Meinox's small molecule library contained small molecules with polar surface areas that are less than 60 square angstroms, suggesting their potent ability to cross the blood-brain barrier. Meinox's small …

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Understanding The Potential Of Plasma Activated Liquids For Biomedical Applications, Evanthia Tsoukou Jan 2021

Understanding The Potential Of Plasma Activated Liquids For Biomedical Applications, Evanthia Tsoukou

Doctoral

Atmospheric cold plasma has evolved as a new technology for applications used in biomedicine, agriculture and food industry. Recently, treatment of liquids using various atmospheric pressure plasmas has attracted much attention owing to multiple practical applications such as water purification, surface cleaning and decontamination with impact in dentistry, wound healing and sterilisation, or cancer therapy. The over-arching aim of this study is to build a better understanding of the parameters which govern the liquid chemistry generated in a liquid exposed to cold plasma and how these translate into biological effects on pro- and eu-karyotic organisms. The objective was to investigate …

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Anticancer Activities Of Plant Secondary Metabolites: Rice Callus Suspension Culture As A New Paradigm, Wusirika Ramakrishna, Anuradha Kumari, Nafeesa Rahman, Pallavi Mandave Jan 2021

Anticancer Activities Of Plant Secondary Metabolites: Rice Callus Suspension Culture As A New Paradigm, Wusirika Ramakrishna, Anuradha Kumari, Nafeesa Rahman, Pallavi Mandave

Michigan Tech Publications, Part 1

Plant natural products including alkaloids, polyphenols, terpenoids and flavonoids have been reported to exert anticancer activity by targeting various metabolic pathways. The biological pathways regulated by plant products can serve as novel drug targets. Plant natural compounds or their derivatives used for cancer treatment and some novel plant-based compounds which are used in clinical trials were discussed. Callus suspension culture with secondary metabolites can provide a continuous source of plant pharmaceuticals without time and space limitations. Previous research has shown that rice callus suspension culture can kill >95% cancer cells with no significant effect on the growth of normal cells. …

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Origins Of Amyloid Oligomers And Novel Approaches For Their Detection, Jeremy Barton Nov 2020

Origins Of Amyloid Oligomers And Novel Approaches For Their Detection, Jeremy Barton

USF Tampa Graduate Theses and Dissertations

Alzheimer’s disease, type II diabetes, and other amyloid diseases are known to be associated with the formation of amyloid aggregates. It has been thoroughly researched whether amyloid fibrils or oligomers are the main culprit for these diseases, and recent evidence has connected oligomers as the most disease relevant aggregate species. However, many difficulties have arose in confirming this hypothesis. Techniques for oligomer detection are often limited in their sensitivity, and in many cases are unable to distinguish oligomers from rigid fibrils. Additionally, the role oligomer splay in fibril assembly is still unclear, and has led to the belief that different …

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Nadph-Quinone Oxidoreductase-1 Mediates Benzo-[A]-Pyrene-1,6-Quinone-Induced Cytotoxicity And Reactive Oxygen Species Production In Human Ea.Hy926 Endothelial Cells, Halley Shukla, Gabriella Gaje, Ashkon Koucheki, Ho Young Lee, Xiaolun Sun, Michael A. Trush, Hong Zhu, Y R. Li, Zhenquan Jia Oct 2020

Nadph-Quinone Oxidoreductase-1 Mediates Benzo-[A]-Pyrene-1,6-Quinone-Induced Cytotoxicity And Reactive Oxygen Species Production In Human Ea.Hy926 Endothelial Cells, Halley Shukla, Gabriella Gaje, Ashkon Koucheki, Ho Young Lee, Xiaolun Sun, Michael A. Trush, Hong Zhu, Y R. Li, Zhenquan Jia

Osteopathic Medicine, Jerry M. Wallace School of

Numerous studies conducted in the past have reported deaths in the human population due to cardiovascular diseases (CVD) on exposure to air particulate matter (APM). BP-1,6-quinone (BP-1,6-Q) is one of the significant components of APM. However, the mechanism(s) by which it can exert its toxicity in endothelial cells is not yet completely understood. NAD(P)H: quinone oxidoreductase-1 (NQO1) is expressed highly in myocardium and vasculature tissues of the heart and plays a vital role in maintaining vascular homeostasis. This study, demonstrated that BP-1,6-Q diminishes NQO1 enzyme activity in a dose-dependent manner in human EA.hy926 endothelial cells. The decrease in the NQO1 …

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Salvia Ceratophylla L. From South Of Jordan: New Insights On Chemical Composition And Biological Activities, Mohammad Sanad Abu-Darwish, Célia Cabral, Zulfigar Ali, Mei Wang, Shabana I. Khan, Melissa R. Jacob, Surendra K. Jain, Babu L. Tekwani, Fazila Zulfiqar, Ikhlas A. Khan, Hatem Taifour, Lígia Salgueiro, Thomas Efferth Oct 2020

Salvia Ceratophylla L. From South Of Jordan: New Insights On Chemical Composition And Biological Activities, Mohammad Sanad Abu-Darwish, Célia Cabral, Zulfigar Ali, Mei Wang, Shabana I. Khan, Melissa R. Jacob, Surendra K. Jain, Babu L. Tekwani, Fazila Zulfiqar, Ikhlas A. Khan, Hatem Taifour, Lígia Salgueiro, Thomas Efferth

Faculty and Student Publications

© 2020, The Author(s). In Jordan, Salvia ceratophylla L. is traditionally used in the treatment of cancer, microbial infections, and urinary disorders. This study aimed: (1) to chemically characterize S. ceratophylla essential oil (EO) from South Jordan, by gas chromatography (GC) and gas chromatography-mass spectrometry (GC–MS); and (2) to evaluate in vitro the cytotoxic, anti-inflammatory, and antiprotozoal activities of the EO, it’s predominant components, and the hexane (A), ethyl acetate (B), methanol (C) and crude-methanol extracts (D). The analysis revealed that the EO has 71 compounds, with linalool (54.8%) as main constituent. Only the hexane extract (A) showed some cytotoxic …

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Prevalence And Characterization Of Some Colibactin Genes In Clinical Enterobacteriaceae Isolates From Iraqi Patients, Mohammed T. Hussein, Safaa A. S. Al-Qaysi, Munther H. Rathi, Qasim I. Hussein, Tarek A.A. Moussa Sep 2020

Prevalence And Characterization Of Some Colibactin Genes In Clinical Enterobacteriaceae Isolates From Iraqi Patients, Mohammed T. Hussein, Safaa A. S. Al-Qaysi, Munther H. Rathi, Qasim I. Hussein, Tarek A.A. Moussa

Baghdad Science Journal

The members of the family of Eentrobacteriaceae harbour a gene cluster called polyketide synthase (pks) island. This cluster is responsible for the synthesis of the genotoxin colibactin that might have an important role in the induction of double-strand DNA breaks, leading to promote human colorectal cancer (CRC). Eleven out of the eighty eight isolates (12.5%) were pks+, distributed as 7 (8%) isolates of E. coli, 2 (2.25%) of K. pneumoniae and 2 (2.25%) of E. aerogenes. The cytotoxic effects of selected pks+ isolates (E. coli and E. aerogenes) on HeLa cells were represented by decreasing cell numbers and enlarged cell …

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Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang Sep 2020

Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

The cellular delivery of cell-impermeable and water-insoluble molecules remains an ongoing challenge to overcome. Previously, we reported amphipathic cyclic peptides c[WR]4 and c[WR]5 consisting of alternate arginine and tryptophan residues as nuclear-targeting molecular transporters. These peptides contain an optimal balance of positive charge and hydrophobicity, which is required for interactions with the phospholipid bilayer to facilitate their application as a drug delivery system. To further optimize them, we synthesized and evaluated a multivalent tricyclic peptide as an efficient molecular transporter. The monomeric cyclic peptide building blocks were synthesized using Fmoc/tBu solid-phase chemistry and cyclization in the …

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Characterizing Human Receptor-Mediated Cytotoxicity By Staphylococcal Bi-Component Leucocidins In S. Aureus Pathogenesis, Jaime Rutter Aug 2020

Characterizing Human Receptor-Mediated Cytotoxicity By Staphylococcal Bi-Component Leucocidins In S. Aureus Pathogenesis, Jaime Rutter

Theses and Dissertations

Staphylococcus aureus employs an array of virulence factors to aid in its pathogenesis. A subset of cytotoxins termed bi-component leucocidins have been characterized as important determinants in the host-pathogen interaction in S. aureus infections. While they have been studied over a century, bi-component leucocidins’ complex mechanisms in pathogenesis have not been fully elucidated. Secreted as monomers, with the exception of LukAB/GH, many combinations of the S- (HlgA, HlgC, LukE, LukS, LukA/H) and F- (HlgB, LukD, LukF, LukB/G) components have demonstrated cell lysis via pore formation and a magnified proinflammatory response at sublytic concentrations. While studies have described various host cellular …

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The Great Debate At 'Immunotherapy Bridge', Naples, December 5, 2019., Paolo A Ascierto, Carlo Bifulco, Jerome Galon, Claus Garbe, Samir N Khleif, Jennifer Mcquade, Kunle Odunsi, Hideho Okada, Chrystal M Paulos, Sergio A Quezada, Hussein A Tawbi, John Timmerman, Giorgio Trinchieri, Lisa H Butterfield, Igor Puzanov Aug 2020

The Great Debate At 'Immunotherapy Bridge', Naples, December 5, 2019., Paolo A Ascierto, Carlo Bifulco, Jerome Galon, Claus Garbe, Samir N Khleif, Jennifer Mcquade, Kunle Odunsi, Hideho Okada, Chrystal M Paulos, Sergio A Quezada, Hussein A Tawbi, John Timmerman, Giorgio Trinchieri, Lisa H Butterfield, Igor Puzanov

Articles, Abstracts, and Reports

As part of the 2019 Immunotherapy Bridge congress (December 4-5, Naples, Italy), the Great Debate session featured counterpoint views from leading experts on six topical issues in immunotherapy today. These were the use of chimeric antigen receptor T cell therapy in solid tumors, whether the Immunoscore should be more widely used in clinical practice, whether antibody-dependent cellular cytotoxicity is important in the mode of action of anticytotoxic T-lymphocyte-associated protein 4 antibodies, whether the brain is immunologically unique or just another organ, the role of microbiome versus nutrition in affecting responses to immunotherapy, and whether chemotherapy is immunostimulatory or immunosuppressive. Discussion …

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N-Acetyltranserase 2 (Nat2) Genotype Polymorphism In Cryopreserved Human Hepatocytes And Chinese Hamster Ovary (Cho) Cells., Mariam Refaat Zaky Habil Aug 2020

N-Acetyltranserase 2 (Nat2) Genotype Polymorphism In Cryopreserved Human Hepatocytes And Chinese Hamster Ovary (Cho) Cells., Mariam Refaat Zaky Habil

Electronic Theses and Dissertations

Arylamine N-acetyltransferases, NAT1 and NAT2, catalyze the detoxification and/or activation of drugs and aromatic amine carcinogens. Single nucleotide polymorphisms or SNPs result in different human NAT2 genotypes thus dividing the population into rapid, intermediate, and slow acetylators. We hypothesize allelic variants of NAT2 genotype will decrease levels of N-acetylation, cytotoxicity, oxidative stress, DNA adduct formation, and mutagenesis compared to the reference allele NAT2*4. Cryopreserved human hepatocytes expressing different NAT2 genotypes and NER-deficient Chinese hamster ovary (CHO) cells transfected with human CYP1A2 and human NAT2*4, NAT2*5B or NAT2*7B have been used to investigate N-acetylation of different xenobiotics. In …

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Anticancer Properties Of Recipes Derived From Nigeria And African Medicinal Plants On Breast Cancer Cells In Vitro, Mutiu A. Alabi, Annamalai Muthusamy, Shama P. Kabekkodu, Olugbenga O. Adebawo Jul 2020

Anticancer Properties Of Recipes Derived From Nigeria And African Medicinal Plants On Breast Cancer Cells In Vitro, Mutiu A. Alabi, Annamalai Muthusamy, Shama P. Kabekkodu, Olugbenga O. Adebawo

Open Access archive

The study was carried out to examine the effects of two recipes prepared from Nigerian and African medicinal plants on the cell cytotoxicity, cell cycle distribution and apoptosis on breast cancer (MCF-7 and MDA-MB-231) cells and normal human fibroblasts. In vitro cytotoxicity and anti-proliferative effect was evaluated by 3-[4, 5-dimethylthizol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) assay while cell cycle and apoptosis were evaluated by flow cytometry using propidium iodide (PI) staining. The reactive oxygen species analysis by DCFDA staining and flow cytometry analysis while alterations in Mitochondrial Membrane Potential (MMP, ∆Ψm) were determined by staining the cells with Rhodamine 123 then FACS …

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Disinfection Byproduct Drivers Of Cytotoxicity In Drinking Water And Swimming Pools, Joshua M. Allen Jul 2020

Disinfection Byproduct Drivers Of Cytotoxicity In Drinking Water And Swimming Pools, Joshua M. Allen

Theses and Dissertations

Water disinfection was cited as the greatest public health achievement of the 20th Century. By inactivating pathogens, disinfection has significantly reduced waterborne diseases in drinking water and swimming pools. However, chemical disinfection has also raised a public health issue: the potential for cancer induction, reproductive and developmental effects, and asthma-related risks associated with exposure to chemical disinfection byproducts (DBPs), which are formed by the reaction of disinfectants with organic matter (natural or anthropogenic), bromide, and iodide. In the U.S., four trihalomethanes (THMs) and five haloacetic acids (HAAs) are currently regulated in drinking water, although no DBPs are regulated in pools, …

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Preparation, Evaluation And Metabolites Study In Rats Of Novel Isoginkgetin-Loaded Tpgs/Soluplus Mixed Nanomicelles, Xue Feng, Yu-Ting Chen, Lu-Ya Li, Yu-Peng Sun, Hai-Rong Wang, Lan-Tong Zhang Jun 2020

Preparation, Evaluation And Metabolites Study In Rats Of Novel Isoginkgetin-Loaded Tpgs/Soluplus Mixed Nanomicelles, Xue Feng, Yu-Ting Chen, Lu-Ya Li, Yu-Peng Sun, Hai-Rong Wang, Lan-Tong Zhang

Journal of Food and Drug Analysis

At present, cancer is one of the most lethal diseases in the world, and researchers are committed to developing effective anticancer drugs. Isoginkgetin (IGG) is a kind of biflavone with the potential to treat cancer due to the features of altering the cell cycle and inhibiting tumor cell infiltration. However, its solubility, absorbability and bioavailability are poor, so in this study, IGG was prepared into mixed nanomicelles and evaluated in vitro and in vivo. After condition optimization, IGG-loaded TPGS/soluplus mixed nanomicelles with particle size of 62.34 ± 1.10 nm, entrapment efficiency of 96.92 ± 0.66% and drug loading of 2.42 …

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Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang Jun 2020

Comparative Molecular Transporter Properties Of Cyclic Peptides Containing Tryptophan And Arginine Residues Formed Through Disulfide Cyclization, Eman H. M. Mohammed, Dindyal Mandal, Saghar Mozaffari, Magdy Abdel-Hamied Zahran, Amany Mostafa Osman, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

We have previously reported cyclic cell-penetrating peptides [WR]5 and [WR]4 as molecular transporters. To optimize further the utility of our developed peptides for targeted therapy in cancer cells using the redox condition, we designed a new generation of peptides and evaluated their cytotoxicity as well as uptake behavior against different cancer cell lines. Thus, cyclic [C(WR)xC] and linear counterparts (C(WR)xC), where x = 4–5, were synthesized using Fmoc/tBu solid-phase peptide synthesis, purified, and characterized. The compounds did not show any significant cytotoxicity (at 25 µM) against ovarian (SK-OV-3), leukemia (CCRF-CEM), gastric adenocarcinoma (CRL-1739), breast …

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Cytotoxic Analysis Of Old Drugs: New Drugs For Alzheimer’S Disease, Sebastian Yumiseba May 2020

Cytotoxic Analysis Of Old Drugs: New Drugs For Alzheimer’S Disease, Sebastian Yumiseba

Theses and Dissertations

Microglia are the resident immune cells of the CNS and constitute about 10% of all cells in the CNS. They have a vital role in Alzheimer’s pathogenesis as either cytotoxic or neuroprotective. Recent efforts are being put into repurposing drugs to target the microglia to treat Alzheimer’s disease.

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Sesamol Protects Min6 Pancreatic Beta Cells Against Simvastatin-Induced Toxicity By Restoring Mitochondrial Membrane Potentials, Girish A. Ghadge, Karthik Gourishetti, Mallikarjuna Rao Chamallamudi, Gopalan Kutty Nampurath Apr 2020

Sesamol Protects Min6 Pancreatic Beta Cells Against Simvastatin-Induced Toxicity By Restoring Mitochondrial Membrane Potentials, Girish A. Ghadge, Karthik Gourishetti, Mallikarjuna Rao Chamallamudi, Gopalan Kutty Nampurath

Open Access archive

Statins, the drugs for the treatment of dyslipidemia, have been suggested to impact insulin sensitivity, resulting in pancreatic β-cell dysfunction, and consequently, lead to new onset of diabetes. Taking this as a clue, the present study was designed to evaluate the protective effect of sesamol (a known antioxidant, antidiabetic and antidyslipidemic agent) against the diabetogenic potential of simvastatin. The toxic effects of simvastatin and sesamol on MIN6 insulinoma (Mouse pancreatic β cells) cells were evaluated separately by MTT assay. The protective effect of sesamol was evaluated at the IC50 value of simvastatin at doses ranging from 7.8 to 62.5 micromolar …

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Responses Of Swine Associated Methicillin-Resistant Staphylococcus Aureus Against Human Lung Carcinoma Epithelial Cell Line A549, Min Tao Wan, Chin Cheng Chou Mar 2020

Responses Of Swine Associated Methicillin-Resistant Staphylococcus Aureus Against Human Lung Carcinoma Epithelial Cell Line A549, Min Tao Wan, Chin Cheng Chou

The Thai Journal of Veterinary Medicine

Staphylococcus aureus (S. aureus) has been shown to adhere, invade, and induce the death of various host cells. The prominent lineage of livestock-associated methicillin-resistant S. aureus (LA-MRSA) in Asia is the sequence type (ST) 9 that has emerged as a potential zoonotic pathogen. However, the virulence of LA-MRSA ST9 remains not clear. In this study, sixteen representative Taiwan LA-MRSA isolates were selected for adherence, invasion, and cytotoxicity studies against the human lung carcinoma epithelial cell line A549. The isolates showed 100% of cytotoxicity, 35.2% - 61% of adhesion, and 18% - 52.5% of invasion against A549 cells. Different adherent abilities …

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Xuetonglactones A–F: Highly Oxidized Lanostane And Cycloartane Triterpenoids From Kadsura Heteroclita Roxb. Craib, Nuzhat Shehla, Bin Li, Liang Cao, Jianping Zhao, Yuqing Jian, Muhammad Daniyal, Atia Tul Wahab, Ikhlas A. Khan, Duan Fang Liao, Atta Ur Rahman, M. Iqbal Choudhary, Wei Wang Jan 2020

Xuetonglactones A–F: Highly Oxidized Lanostane And Cycloartane Triterpenoids From Kadsura Heteroclita Roxb. Craib, Nuzhat Shehla, Bin Li, Liang Cao, Jianping Zhao, Yuqing Jian, Muhammad Daniyal, Atia Tul Wahab, Ikhlas A. Khan, Duan Fang Liao, Atta Ur Rahman, M. Iqbal Choudhary, Wei Wang

Faculty and Student Publications

© Copyright © 2020 Shehla, Li, Cao, Zhao, Jian, Daniyal, Wahab, Khan, Liao, Rahman, Choudhary and Wang. Xuetonglactones A–F (1–6), six unreported highly oxidized lanostane- and cycloartane-type triterpenoids along with 22 known scaffolds (7–28) were isolated from the stems of Kadsura heteroclita (Roxb.) Craib. Compared with previous congeners, xuetonglactone A (1), possesses an unprecedented 20,21-α-epoxide, and xuetonglactone D (4) features an unusual 19-α-hydroperoxyl moiety. The structures and the absolute configurations of the compounds were established by extensive one- and two-dimensional NMR, and electronic circular dichroism (ECD) spectroscopic analysis, with those of 1 and 5 confirmed by single-crystal X-ray diffraction technique. …

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The Employment Of A Conformal Polydopamine Thin Layer Reduces The Cytotoxicity Ofsilver Nanoparticles, Asli Yilmaz Jan 2020

The Employment Of A Conformal Polydopamine Thin Layer Reduces The Cytotoxicity Ofsilver Nanoparticles, Asli Yilmaz

Turkish Journal of Zoology

Silver nanoparticles (AgNPs) with their unique properties represent great promise in biological applications. However, the high toxicity of AgNPs still remains a major bottleneck and hinders their basic usage. In the present study, to improve the cytotoxicity of AgNPs, a thin layer of polydopamine (PDOP) was proposed as shell material. For this, the as-prepared citrate-stabilized AgNPs were dispersed in dopamine solution under alkaline conditions. The thickness of the PDOP layer could be manipulated simply by tuning the polymerization time. It was indicated that all NP systems (PDOP, AgNP, and AgNP@PDOP) were efficiently synthesized in the desired size and morphology. Cytotoxicity …

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Synthesis, Cytotoxic Assessment, And Molecular Docking Studies Of2,6-Diaryl-Substituted Pyridine And 3,4- Dihydropyrimidine-2(1h)-One Scaffolds, Zahra Hosseinzadeh, Nima Razzaghi-Asl, Ali Ramazani, Hamideh Aghahosseini, Ali Ramazani Jan 2020

Synthesis, Cytotoxic Assessment, And Molecular Docking Studies Of2,6-Diaryl-Substituted Pyridine And 3,4- Dihydropyrimidine-2(1h)-One Scaffolds, Zahra Hosseinzadeh, Nima Razzaghi-Asl, Ali Ramazani, Hamideh Aghahosseini, Ali Ramazani

Turkish Journal of Chemistry

Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytotoxic effects against several cancer cell lines. An easy and convenient method is reported for the synthesis of these derivatives, employing cobalt ferrite (CoFe$_{2}$ O$_{4}$ @SiO$_{2}$ -SO$_{3}$ H) magnetic nanoparticles under microwave irradiation and solvent-free conditions. The structural characteristics of the prepared nanocatalyst were investigated by FTIR, XRD, SEM, and TGA techniques. In vitro cytotoxic effects of the synthesized products were assessed against the human breast adenocarcinoma cell line …

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Design, Synthesis, Cytotoxic Activity, And Apoptosis Inducing Effects Of 4- And N-Substituted Benzoyltaurinamide Derivatives, Özlem Akgül, Mümi̇n Alper Erdoğan, Dervi̇ş Bi̇ri̇m, Çağla Kayabaşi, Cumhur Gündüz, Güli̇z Armagan Jan 2020

Design, Synthesis, Cytotoxic Activity, And Apoptosis Inducing Effects Of 4- And N-Substituted Benzoyltaurinamide Derivatives, Özlem Akgül, Mümi̇n Alper Erdoğan, Dervi̇ş Bi̇ri̇m, Çağla Kayabaşi, Cumhur Gündüz, Güli̇z Armagan

Turkish Journal of Chemistry

In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test. Compound 14 (in SH-SY5Y and MDA-MB-231 cell lines) and 15 (in SH-SY5Y cell line) were found to induce intrinsic …

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Synthesis, Evaluation, And In Silico Studies Of 2-Mercapto-5-Substituted Styryl-1,3,4-Oxadiazoles As Potential Cytotoxic Agents, Anitha Kumari Vinjavarapu, Shaheen Begum, Bharathi Koganti Jan 2020

Synthesis, Evaluation, And In Silico Studies Of 2-Mercapto-5-Substituted Styryl-1,3,4-Oxadiazoles As Potential Cytotoxic Agents, Anitha Kumari Vinjavarapu, Shaheen Begum, Bharathi Koganti

The Thai Journal of Pharmaceutical Sciences

Objective: The objective of the present study is to design, synthesize and evaluate 2-mercapto-5-styryl-1,3,4-oxadiazoles with an aim of developing potential cytotoxic agents and to carryout in silico studies to understand the possible interactions with .

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