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ROS generating agent

Lorena Polloni, Ana Carolina de Seni Silva, Samuel Cota Teixeira, Fernanda Van Petten de Vasconcelos Azevedo, Mariana Alves Pereira Zóia, Marcelo Santos da Silva, Paula Marynella Alves Pereira Lima, Lucas Ian Veloso Correia, Janaina do Couto Almeida, Claudio Vieira da Silva, Veridiana de Melo Rodrigues Ávila, Luiz Ricardo Filho Goulart, Sandra Morelli, Wendell Guerra, Robson José de Oliveira Júnior
This work reports the biological evaluation of a copper complex of the type [Cu(O-O)(N-N)ClO4 ], in which O-O = 4,4,4-trifluoro-1-phenyl-1,3-butanedione (Hbta) and N-N = 1,10-phenanthroline (phen), whose generic name is CBP-01. The cytotoxic effect of CBP-01 was evaluated by resazurin assay and cell proliferation was determined by MTT assay. DNA fragmentation was analyzed by gel electrophoresis. Cell cycle progression was detected through propidium iodide (PI) staining. Apoptosis and autophagy were determined by, respectively, Annexin V and 7-AAD staining and monodansylcadaverine (MDC) staining...
February 18, 2019: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Hyung Ha Jang, Su Bum Park, Jeong Sup Hong, Hye Lim Lee, Yeon Hui Song, Jungsoo Kim, Yun Hye Jung, Chan Kim, Doo-Man Kim, Sang Eun Lee, Young-Il Jeong, Dae Hwan Kang
BACKGROUND: The aim of this study is to fabricate drug-eluting gastrointestinal (GI) stent using reactive oxygen species (ROS)-sensitive nanofiber mats for treatment of cholangiocarcinoma (CCA) cell. A ROS-producing agent, piperlongumine (PL)-incorporated nanofiber mats were investigated for drug-eluting stent (DES) application. METHODS: Selenocystamine-conjugated methoxy poly(ethylene glycol) (MePEG) was conjugated with poly(L-lactide) (PLA) to produce block copolymer (LEse block copolymer)...
February 18, 2019: Nanoscale Research Letters
Olivier Reelfs, Vincenzo Abbate, Agostino Cilibrizzi, Mark A Pook, Robert C Hider, Charareh Pourzand
Mitochondrial labile iron (LI) is a major contributor to the susceptibility of skin fibroblasts to ultraviolet A (UVA)-induced oxidative damage leading to necrotic cell death via ATP depletion. Mitochondria iron overload is a key feature of the neurodegenerative disease Friedreich's ataxia (FRDA). Here we show that cultured primary skin fibroblasts from FRDA patients are 4 to 10-fold more sensitive to UVA-induced death than their healthy counterparts. We demonstrate that FRDA cells display higher levels of mitochondrial LI (up to 6-fold on average compared to healthy counterparts) and show higher increase in mitochondrial reactive oxygen species (ROS) generation after UVA irradiation (up to 2-fold on average), consistent with their differential sensitivity to UVA...
February 19, 2019: Metallomics: Integrated Biometal Science
Rone Aparecido De Grandis, Patrick Wellington da Silva Dos Santos, Katia Mara de Oliveira, Ana Rita Tomazela Machado, Alexandre Ferro Aissa, Alzir Azevedo Batista, Lusânia Maria Greggi Antunes, Fernando Rogério Pavan
This study describes a series of newly synthesized phosphine/diimine ruthenium complexes containing the lawsone as bioligand with enhanced cytotoxicity against different cancer cells, and apoptosis induction in prostatic cancer cells DU-145. The complexes [Ru(law)(N-N)2 ]PF6 where N-N is 2,2'-bipyridine (1) or 1,10-phenanthroline (2) and [Ru(law)(dppm)(N-N)]PF6 , where dppm means bis(diphenylphosphino)methane, N-N is 2,2'-bipyridine (3) or 1,10-phenanthroline (4), and law is lawsone, were synthesized and fully characterized by elemental analysis, molar conductivity, NMR, UV-vis, IR spectroscopies and cyclic voltammetry...
February 8, 2019: Bioorganic Chemistry
Om P S Patel, Ashutosh Arun, Pankaj K Singh, Deepika Saini, Sharanbasappa Shrimant Karade, Manish K Chourasia, Rituraj Konwar, Prem P Yadav
A series of new pyranocarbazole derivatives were synthesized via semi-synthetic modification of koenimbine (1a) and koenidine (1b) isolated from the leaves of Murraya koenigii. Among all, compound 3bg displayed significant anti-cancer activity against MDA-MB-231, DU145 and PC3 cell lines with the IC50 values of 3.8, 7.6 and 5.8 μM, respectively. It was also observed that the halogenated-benzyl substitution at N-9 position, C-3 Methyl and C-7 methoxy group on carbazole motif are favoured for anti-cancer activity...
February 7, 2019: European Journal of Medicinal Chemistry
Jia Wen, Kui Yang, Xingcheng Ding, Hongjuan Li, Yongqian Xu, Fengyu Liu, Shiguo Sun
A folic acid (FA) functional drug delivery system (MT@L-PTX@FA) based on in situ formation of tellurium nanodots (Te NDs) in paclitaxel (PTX)-loaded MgAl layered double hydroxide (LDHs) gated mesoporous silica nanoparticles (MSNs) has been designed and fabricated for targeted chemo/PDT/PTT trimode combinatorial therapy. X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM), high-resolution transmission electron microscopy (HRTEM), N2 adsorption-desorption, Fourier transform infrared (FT-IR) spectra, and UV-vis spectra were used to demonstrate the successful fabrication of MT@L-PTX@FA...
February 15, 2019: Inorganic Chemistry
Yingchao Zhu, Ming Li, Yawen Lu, Jun Li, Ye Ke, Jie Yang
Atherosclerosis (AS) is one of important events involving in the pathological process of coronary artery disease. Many traditional Chinese medicines have been widely used for the treatment of AS. Previous studies have demonstrated that Ilexgenin A (IA) obtained from Ilex hainanensis Merr. could improve AS development. However, its underlying mechanism is still unknown. This study was conducted to explore the possible targets and mechanisms involving in the anti-atheroclerosis effect of IA. The results showed IA significantly promoted NO production, reduced reactive oxygen species (ROS) generation, and inflammatory cytokine production induced by palmitate (PA) in endothelial cells, demonstrating IA could improve endothelial dysfunction...
February 14, 2019: Drug Development Research
M Carmen Ortega-Liebana, M Mar Encabo-Berzosa, Alvaro Casanova, M Desiree Pereboom, Octavio Alda, Jose Luis Hueso, Jesus Santamaria
This work describes the synthesis of nitrogen-doped carbon nanodots (CNDs) synthesized from ethylene diamine tetra acetic acid (EDTA) as a precursor and their application as luminescent agents with a dual-mode theranostic role as near-infrared (NIR) triggered imaging and photodynamic therapy agents. Interestingly, these fluorescent CNDs are more rapidly and selectively internalized in tumor cells and exhibit no cytotoxicity until remotely activated with a NIR illumination source. These CNDs are excellent candidates for photo-theranostic purposes, i...
February 11, 2019: Chemistry: a European Journal
Raimundo Gonçalves de Oliveira Júnior, Antoine Bonnet, Estelle Braconnier, Hugo Groult, Grégoire Prunier, Laureen Beaugeard, Raphäel Grougnet, Jackson Roberto Guedes da Silva Almeida, Christiane Adrielly Alves Ferraz, Laurent Picot
Cutaneous melanoma has a high capacity to metastasize and significant resistance to conventional therapeutic protocols, which makes its treatment difficult. The combination of conventional drugs with cytostatic molecules of low toxicity has been shown to be an interesting alternative for sensitization of tumor cells to chemotherapy. In this study, we evaluated the effect of bixin, an abundant apocarotenoid present in Bixa orellana, on the sensitization of human melanoma cells (A2058) to dacarbazine treatment, an anticancer agent clinically used for the therapy of metastatic melanoma...
February 7, 2019: Food and Chemical Toxicology
Anees Rahman, Siraj Pallichankandy, Faisal Thayyullathil, Sehamuddin Galadari
Natural products are a major source of potential anticancer agents, and in order to develop improved and more effective cancer treatments, there is an immense need in exploring and elucidating their mechanism of action. Sanguinarine (SNG), a quaternary benzophenanthridine alkaloid, has been shown to induce cytotoxicity in various human cancers and suppresses various pro-tumorigenic processes such as invasion, angiogenesis, and metastasis in different cancers. Lack of understanding the anticancer mechanism(s) of SNG has impeded the development of this molecule as a potential anticancer agent...
February 5, 2019: Free Radical Biology & Medicine
Nerella Sridhar Goud, S Mahammad Ghouse, Jatoth Vishnu, Jakkula Pranay, Ravi Alvala, Venu Talla, Insaf A Qureshi, Mallika Alvala
BACKGROUND: Human Galectin-1, protein of lectin family showing affinity towards β-galactosides has emerged as critical regulator of tumor progression and metastasis, by modulating diverse biological events including homotypic cell aggregation, migration, apoptosis, angiogenesis and immune escape. Therefore, galectin-1 inhibitors might represent novel therapeutic agents for cancer. METHODS: A new series of heterocyclic imines linked coumarin-thiazole hybrids (6a-6r) has been synthesized and evaluated for their cytotoxic potential against a panel of six human cancer cell lines namely, lung (A549), prostate (DU-145), breast (MCF-7 & MDA-MB-231), colon (HCT-15 & HT-29) using MTT assay...
February 7, 2019: Anti-cancer Agents in Medicinal Chemistry
Chunyan Chen, Jiangchuan Sun, Shuning Chen, Yujiao Liu, Shenyin Zhu, Zhigang Wang, Shufang Chang
Purpose: Nanomedicine has emerged as a novel therapeutic modality for cancer treatment and diagnosis. Lipid-polymer hybrid nanoparticles (LPHNPs) are core-shell nanoparticle (NP) structures comprising polymer cores and lipid shells, which exhibit complementary characteristics of both polymeric NPs and liposomes. However, it is difficult to wrap perfluoropentane (PFP) into core-shell NPs in the existing preparation process, which limits its application in the integration of diagnosis and treatment...
2019: International Journal of Nanomedicine
Jin-Can Chen, Yao Zhang, Xin-Ming Jie, Ji She, Guang-Zhi Dongye, Yu Zhong, Yuan-Yuan Deng, Jie Wang, Bo-Yang Guo, Lan-Mei Chen
Thioredoxin reductase (TrxR), a major component of the thioredoxin system, makes a critical role in regulating cellular redox signaling and is found to be overexpressed in many human cancer cells. TrxR has become an attractive target for anticancer agents. In this work, three Ru(II) complexes with salicylate as ligand, [Ru(phen)2 (SA)] (phen = 1,10-phenanthroline, SA = salicylate, 1), [Ru(dmb)2 (SA)] (dmb = 4,4'-dimethyl-2,2'-bipyridine, 2) and [Ru(bpy)2 (SA)] (bpy = 2,2'-bipyridine, 3), were synthesized and characterized...
January 25, 2019: Journal of Inorganic Biochemistry
Minako Nyui, Ikuo Nakanishi, Kazunori Anzai, Toshihiko Ozawa, Ken-Ichiro Matsumoto
The reactivity of nitroxyl free radicals, 4-hydroxyl-2,2,6,6-tetramethylpiperidine- N -oxyl (TEMPOL) and 3-carbamoyl-2,2,5,5-tetramethylpyrrolidine- N -oxyl (CmP), with reactive oxygen species (ROS) were compared as typical 6-membered and 5-membered ring nitroxyl compounds, respectively. The reactivity of the hydroxylamine forms of both these nitroxyl radicals (TEMPOL-H and CmP-H) was also assessed. Two free radical species of ROS, hydroxyl radical (• OH) and superoxide (O2 •- ), were subjected to a competing reaction...
January 2019: Journal of Clinical Biochemistry and Nutrition
Hyun Ji Lim, Moon Nyeo Park, Changmin Kim, Beomku Kang, Hyo-Sook Song, Hyemin Lee, Sung-Hoon Kim, Bum-Sang Shim, Bonglee Kim
Though Spatholobus suberectus Dunn (SSD) has been reported to have anti-virus, anti-osteoclastogenesis, and anti-inflammation activities, its underlying anti-cancer mechanism has never been elucidated in association with the role of miR-657 in endoplasmic reticulum (ER) stress-related apoptosis to date. SSD treatment exerted cytotoxicity in U266 and U937 cells in a dose-dependent manner. Also, apoptosis-related proteins such as PARP, procaspase-3, and Bax were regulated by SSD treatment. Furthermore, Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay revealed that a number of apoptotic bodies were increased by SSD...
January 28, 2019: Cancers
Li Ma, Yilin Liu, Yi Liu, Shuyi Jiang, Ping Li, Yuchen Hao, Pengpeng Shao, Anxiang Yin, Xiao Feng, Bo Wang
Conjugated microporous polymers (CMPs) have full access to the organic synthesis toolbox and feature-rich functionality, structural diversity, and high surface area. We incorporated ferrocene (Fc) into the backbones of CMPs and systematically engineered their optical energy gaps. Compared with the CMPs without Fc units yet adopting similar molecular orbital level, Fc-based CMPs can sufficiently generate reactive oxygen species (ROS) under visible light. The resultant ROS are able to effectively decompose the absorbed pollutants, including organic dyes and chemical warfare agents...
January 29, 2019: Angewandte Chemie
Perumal Sathiyachandran, Jabastin Jayamanoharan, Vladimir N Nesterov, Karnam Jayarampillai Rajendra Prasad
A simple and one-pot approach for the synthesis of highly functionalized novel (E)-2-benzylideno-(Z)-carbazolylideno cyanoacetamide derivatives from different 2-(2',3',4',9'-tetrahydro-carbazol-1'-ylidene)-propanedinitriles and aryl/heteroaryl carbaldehydes via vinylogous aldol reaction. The structures of the molecules were designated by FT-IR, 1 H NMR, 13 C NMR studies, elemental and X-ray crystallographic analysis. The synthesized pure products have been screened for in vitro antibiofilm inhibitory activity towards antibiotic-resistant pathogenic organisms...
January 17, 2019: Bioorganic & Medicinal Chemistry
Qing-Qing Liu, Ke Lu, Hai-Miao Zhu, Shi-Lin Kong, Jing-Mei Yuan, Guo-Hai Zhang, Nan-Ying Chen, Chen-Xi Gu, Cheng-Xue Pan, Dong-Liang Mo, Gui-Fa Su
Inspired by the common structural characteristics of numerous known antitumor compounds targeting DNA or topoisomerase I, 3-(benzazol-2-yl)-quinoxaline-based scaffold was designed via the combination of two important privileged structure units -quinoxaline and benzazole. Thirty novel 3-(benzazol-2-yl)-quinoxaline derivatives were synthesized and evaluated for their biological activities. The MTT assay indicated that most compounds possessed moderate to potent antiproliferation effects against MGC-803, HepG2, A549, HeLa, T-24 and WI-38 cell lines...
January 11, 2019: European Journal of Medicinal Chemistry
T O Ajiboye
2-(2-nitrovinyl) furan is a broad-spectrum antibacterial agent with activity against Gram-positive and Gram-negative bacteria. In this study, the contributions of reactive oxygen species, oxidative DNA damage and glutathione depletion on its activity against Acinetobacter baumannii was investigated. Inactivation of sodB, katG and recA lowered the minimum inhibitory concentration of 2-(2-nitrovinyl) furan. Furthermore, the inactivation increased the superoxide anion radical and hydrogen peroxide contents of 2-(2-nitrovinyl) furan-treated A...
January 22, 2019: Microbial Pathogenesis
Saniyya Khan, Mohammed Rayis P, Asim Rizvi, Md Maroof Alam, Meher Rizvi, Imrana Naseem
Nosocomial infections are a major threat to modern therapeutics. The major causative agent of these infections is multidrug-resistant gram-negative bacteria, which impart high morbidity and mortality rate. This has led to an urge for the development of new antibiotics. Antimicrobial photodynamic therapy is a promising strategy to which till date no resistant strain has been reported. Since the efficacy of photodynamic therapy largely depends on the selection and administration of an appropriate photosensitizer, therefore, the realization of clinically active photosensitizers is an immediate need...
2019: Toxicology Reports
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