432 results match your criteria denaturation cytotoxicity

A supramolecular nanocarrier for efficient cancer imaging and therapy by targeting at matriptase.

J Control Release 2021 Apr 21;334:153-163. Epub 2021 Apr 21.

College of Chemistry, Fuzhou University, Fujian 350116, China. Electronic address:

Human serum albumin (HSA), a versatile protein carrier for endogenous and exogenous compounds, is a proven macromolecule to form nanoparticles for drug delivery. To render HSA carrier specificity toward tumors, we designed a recombinant HSA protein fused with Kunitz domain 1 (KD1) of hepatocyte growth factor activator inhibitor type 1, which targets to matriptase, a type II transmembrane serine protease overexpressed on tumor cell surface. The carrier was thus named matriptase targeting carrier (MTC). Read More

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Visible light-curable water-soluble chitosan derivative, chitosan hydrogel, and preparation method: a patent evaluation of US2019202998A1.

Expert Opin Ther Pat 2021 May 30;31(5):351-360. Epub 2021 Mar 30.

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Parktown, South Africa.

: Water soluble polysaccharides are versatile structural materials that can be used for the design of biocompatible hydrogels and wet dressings in wound healing applications. Glycol chitosan (GC) is an example of a multifunctional water-soluble chitosan derivative that has inherent wound healing properties and reactive sites for chemical modification.: United States (US) patent US2019202998A1 describes the preparation of a novel wound healing technology based on a three-dimensional (3D) crosslinked GC hydrogel (GCH) wet dressing, prepared via the synthesis of PEG1K-biscarboxylic acid--Glycol Chitosan--methacrylate using visible light induced photocrosslinking. Read More

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Design, synthesis and biological evaluation of water soluble and non-aggregated silicon phthalocyanines, naphthalocyanines against A549, SNU-398, SK-MEL128, DU-145, BT-20 and HFC cell lines as potential anticancer agents.

Bioorg Chem 2021 Feb 9;107:104637. Epub 2021 Jan 9.

Karadeniz Technical University, Department of Chemistry, Trabzon, Turkey. Electronic address:

Cancer has become an important public problem in worldwide since cancer incidence and mortality are growing rapidly. In this study, water soluble and non-aggregated silicon (IV) phthalocyanines and naphthalocyanines containing (3,5-bis{3-[3-(diethylamino)phenoxy]propoxy}phenyl)methoxy groups have been synthesized and characterized to investigate their anticancer potential. Their DNA binding/nuclease, topoisomerases inhibition were investigated using UV-Vis absorption, thermal denaturation and agarose gel electrophoresis. Read More

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February 2021

Methanolic Extract of (Caesalpiniaceae) Stem Bark Suppresses Ethanol/Indomethacin-Induced Chronic Gastric Injury in Rats.

Gastroenterol Res Pract 2020 28;2020:8180323. Epub 2020 Nov 28.

Laboratory of Animal Physiology and Phytopharmacology, Faculty of Science, University of Dschang, Cameroon.

(Caesalpiniaceae) is a plant from the Cameroon pharmacopoeia very widely used in the treatment of many pathologies among which are gastrointestinal disorders. The main purpose of this study was to assess the healing properties of gastric ulcer from the methanolic extract of and its mechanisms of action. The healing properties of gastric ulcers (chronic ulcer model induced by ethanol and indomethacin) were evaluated in adult male rats, while the mechanisms of action were evaluated by anti-inflammatory assay (protein denaturation, cyclooxygenase, and lipoxygenase assays) and immunomodulatory assay (ROS production (using technical chemiluminescence), cytokine (TNF-, IL-1, IL-6) production (using ELISA), proliferation of T cells (using liquid scintillation counter), and cytotoxicity (using MTT assay)). Read More

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November 2020

Nano-Bio Interaction between Blood Plasma Proteins and Water-Soluble Silicon Quantum Dots with Enabled Cellular Uptake and Minimal Cytotoxicity.

Nanomaterials (Basel) 2020 Nov 13;10(11). Epub 2020 Nov 13.

Graduate School of Chemical Sciences and Engineering, Hokkaido University, Sapporo 060-0814, Japan.

A better understanding of the compatibility of water-soluble semiconductor quantum dots (QDs) upon contact with the bloodstream is important for biological applications, including biomarkers working in the first therapeutic spectral window for deep tissue imaging. Herein, we investigated the conformational changes of blood plasma proteins during the interaction with near-infrared light-emitting nanoparticles, consisting of Pluronic F127 shells and cores comprised of assembled silicon QDs terminated with decane monolayers. Albumin and transferrin have high quenching constants and form a hard protein corona on the nanoparticle. Read More

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November 2020

Purification, characterization and anticancer evaluation of l-methioninase from .

3 Biotech 2020 Nov 2;10(11):501. Epub 2020 Nov 2.

Bioprocess Laboratory, School of Biotechnology, National Institute of Technology, Calicut, India.

The l-methioninase was purified 7.15-fold with a recovery of 47.9% and the specific activity of 74. Read More

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November 2020

Implication of a positive virtual crossmatch with negative flow crossmatch: A mind-boggler.

Asian J Transfus Sci 2020 Jan-Jun;14(1):79-82. Epub 2020 Jul 24.

Department of Transfusion Medicine, Molecular Biology and Transplant Immunology, Indraprastha Apollo Hospital, New Delhi, India.

There are occasions when tests performed before considering a patient for transplant are ambiguous and require further workup. One such condition is the presence of a positive virtual crossmatch (VXm) (anti-human leukocyte antigen [HLA-A]*26: 01 antibody in this case) with a negative complement-dependent cytotoxicity, Luminex, and flow crossmatch. To ascertain the nature of the antibody, the beads used in single-antigen bead assay (SAB) were treated by acid to denature the antigens and retested with the control and test sample. Read More

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Ethnomedicinal documentation and anti-inflammatory effects of n-butanol extract and of four compounds isolated from the stems of Pituranthos scoparius: An in vitro and in vivo investigation.

J Ethnopharmacol 2021 Mar 20;267:113488. Epub 2020 Oct 20.

Department of Chemistry, The University of Jordan, Amman, 11942, Jordan; Department of Chemistry, Indiana University, Bloomington, IN, 47405, United States. Electronic address:

Ethnopharmacological Relevance: Pituranthos scoparius is a medicinal plant belonging to the Apiaceae family. It thrives in North Africa, and is widely distributed in the high plateau of most parts of the Sahara in Algeria. This plant is widely used in the Algerian traditional medicine to treat numerous infectious diseases, dermatoses, nervous breakdowns, digestive disorders, and calm abdominal pain. Read More

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A novel petasin-modified zinc oxide eugenol sealer.

J Conserv Dent 2019 Sep-Oct;22(5):490-494. Epub 2020 Aug 4.

Department of Conservative Dentistry and Endodontics, SRM Dental College, Ramapuram, Chennai, India.

Objective: Zinc oxide eugenol (ZOE) is one of the most commonly used root canal sealer. However, it has few drawbacks such as cytotoxicity, solubility, and irritation to periapical tissues. The scope of this study was to investigate the setting time, solubility, cytotoxic effects, and anti-inflammatory action of ZOE sealer with the modification of its liquid component by the addition of petasin extract in the ratios 1:1, 5:1, and 10:1. Read More

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Design and synthesis of pyrazole-pyrazoline hybrids as cancer-associated selective COX-2 inhibitors.

Arch Pharm (Weinheim) 2021 Jan 4;354(1):e2000116. Epub 2020 Oct 4.

Drug Design and Medicinal Chemistry Laboratory, Jamia Hamdard, New Delhi, India.

In continuation of our previous work on cancer and inflammation, 15 novel pyrazole-pyrazoline hybrids (WSPP1-15) were synthesized and fully characterized. The formation of the pyrazoline ring was confirmed by the appearance of three doublets of doublets in H nuclear magnetic resonance spectra exhibiting an AMX pattern for three protons (H , H , and H ) of the pyrazoline ring. All the synthesized compounds were screened for their in vitro anticancer activity against five cell lines, that is, MCF-7, A549, SiHa, COLO205, and HepG2 cells, using the MTT growth inhibition assay. Read More

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January 2021

Discovery of novel dehydroabietic acid derivatives as DNA/BSA binding and anticancer agents.

Spectrochim Acta A Mol Biomol Spectrosc 2021 Feb 15;246:118944. Epub 2020 Sep 15.

College of Science, Nanjing Forestry University, Nanjing 210037, China.

To explore the biological properties of rosin derivatives, two dehydroabietic acid derivatives N-(5-dehydroabietyl-1,3,4-thiadiazole)-yl-pyridine-2-carboxamide (DTPC) and di-N-(5-dehydroabietyl-1,3,4-thiadiazole)-yl-pyridine-2,6-carboxamide (DDTPC) with 1,3,4-thiadiazole, pyridine and amide moieties were designed and synthesized according to superposition principle of activity group. They interact with calf thymus DNA (CT DNA) via intercalation based on the results of circular dichroism (CD) and fluorescence spectroscopy, DNA denaturation and viscosity studies. Fluorescence and CD spectral experiments indicate that they might be transported and stored by protein like bovine serum albumin (BSA). Read More

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February 2021

Interaction of memantine with calf thymus DNA: an and approach and cytotoxic effect on the cancerous cell lines.

J Biomol Struct Dyn 2020 Sep 21:1-14. Epub 2020 Sep 21.

Department of Biochemistry, Faculty of Life Sciences, A.M. University, Aligarh, India.

Memantine belongs to the class of cognition enhancers that functions as NMDA receptor antagonist, used to treat Alzheimer's disease. The interaction of memantine with DNA was not investigated. In the present study, the interaction of memantine with ct-DNA, as well as its cytotoxicity on cancer cells, was evaluated. Read More

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September 2020

Use of collagen and auricular cartilage in bioengineering: scaffolds for tissue regeneration.

Cell Tissue Bank 2020 Sep 2. Epub 2020 Sep 2.

Interunit Graduate Program in Bioengineering, University of São Paulo, São Carlos, SP, Brazil.

The aim of this study was the development of collagen and collagen/auricular cartilage scaffolds for application in dermal regeneration. Collagen was obtained from bovine tendon by a 72 h-long treatment, while bovine auricular cartilage was treated for 24 h and divided into two parts, external (perichondrium, E) and internal (elastic cartilage, I). The scaffolds were prepared by mixing collagen (C) with the internal part (CI) or the external part (CE) in a 3:1 ratio. Read More

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September 2020

Pro-Oxidant Activity of an ALS-Linked SOD1 Mutant in Zn-Deficient Form.

Molecules 2020 Aug 7;25(16). Epub 2020 Aug 7.

Faculty of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan.

Cu, Zn superoxide dismutase (SOD1) is a representative antioxidant enzyme that catalyzes dismutation of reactive oxygen species in cells. However, (E,E)-SOD1 mutants in which both copper and zinc ions were deleted exhibit pro-oxidant activity, contrary to their antioxidant nature, at physiological temperatures, following denaturation and subsequent recombination of Cu. This oxidative property is likely related to the pathogenesis of amyotrophic lateral sclerosis (ALS); however, the mechanism by which Cu re-binds to the denatured (E,E)-SOD1 has not been elucidated, since the concentration of free copper ions in cells is almost zero. Read More

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An EdU-based flow cytometry assay to evaluate chicken T lymphocyte proliferation.

BMC Vet Res 2020 Jul 6;16(1):230. Epub 2020 Jul 6.

Research and Development Laboratories, FARVET, Carretera Panamericana Sur N°766 Km 198.5, Ica, Peru.

Background: In the poultry industry, quantitative analysis of chicken T cell proliferation is important in many biological applications such as drug screening, vaccine production, and cytotoxicity assessment. Several assays have been established to evaluate this immunological response in chicken cells. However, these assays have some disadvantages including use of radioactive labels ([3H]-Thymidine assay), necessity of DNA denaturation or digestion (BrdU incorporation assay), lack of sensitivity and underestimation of anti-proliferative effects (MTT assay), and modulation of activation molecules and cell viability reduction (CFSE assay). Read More

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Experimental and quantum chemical study оn the DNA/protein binding and the biological activity of a rhodium(iii) complex with 1,2,4-triazole as an inert ligand.

Dalton Trans 2020 Jul;49(26):9070-9085

University of Kragujevac, Faculty of Science, Radoja Domanovića 12, 34000 Kragujevac, Serbia.

The synthesis and structural characterization of a newly synthesized mononuclear rhodium(iii) complex, Rhtrz, with a ligand (2,2,6-bis((4S,7R)-7,8,8-trimethyl-4,5,6,7-tetrahydro-1H-4,7-methanoindazol-3-yl)pyridine) and a ligand of 1,2,4-triazole, are presented in this paper. The kinetic interactions of the Rhtrz complex with essential biomolecules such as 5-GMP, L-Met, and GSH were examined. The study of the biological interactions was focused on the binding properties of the Rhtrz complex with CT-DNA and serum albumin. Read More

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Computational stabilization of T cell receptors allows pairing with antibodies to form bispecifics.

Nat Commun 2020 05 11;11(1):2330. Epub 2020 May 11.

Eli Lilly Biotechnology Center, 10300 Campus Point Drive, San Diego, CA, 92121, USA.

Recombinant T cell receptors (TCRs) can be used to redirect naïve T cells to eliminate virally infected or cancerous cells; however, they are plagued by low stability and uneven expression. Here, we use molecular modeling to identify mutations in the TCR constant domains (Cα/Cβ) that increase the unfolding temperature of Cα/Cβ by 20 °C, improve the expression of four separate α/β TCRs by 3- to 10-fold, and improve the assembly and stability of TCRs with poor intrinsic stability. The stabilizing mutations rescue the expression of TCRs destabilized through variable domain mutation. Read More

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α-amylase and α-glucosidase Inhibition, Antioxidant, Anti- Inflammatory Activity and GC-MS Profiling of Blume.

Comb Chem High Throughput Screen 2020 ;23(9):945-954

Research Institute of Biotechnology & Medical Converged Science, Dongguk University-Seoul, Goyangsi 10326, Korea.

Background: Avicennia alba Blume, is a well-known mangrove plant used in traditional medicinal practices for several human ailments.

Objective: The study aimed at the evaluation of antidiabetic, antioxidant, anti-inflammatory and cytotoxic activities of A. alba ethanolic leaf (AAL) and bark (AAB) extract along with phytochemical investigation. Read More

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January 2020

Specific stabilization of promoter G-Quadruplex DNA by 2,6-disubstituted amidoanthracene-9,10-dione based dimeric distamycin analogues and their selective cancer cell cytotoxicity.

Eur J Med Chem 2020 Jun 16;195:112202. Epub 2020 Mar 16.

Department of Organic Chemistry, Indian Institute of Science, Bangalore, 560012, India; School of Applied & Interdisciplinary Sciences, Indian Association for the Cultivation of Science, Kolkata, 700032, India. Electronic address:

We have designed and synthesized anthraquinone containing compounds which have oligopyrrole side chains of varying lengths. These compounds stabilized the G-quadruplex DNA formed in the promoter regions of c-MYC oncogenes selectively over the duplex DNA. These observations were recorded using UV-vis spectroscopic titrations, fluorescence measurements and circular dichroism (CD) spectral titrations. Read More

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Synthesis, cytotoxicity, pharmacokinetic profile, binding with DNA and BSA of new imidazo[1,2-a]pyrazine-benzo[d]imidazol-5-yl hybrids.

Sci Rep 2020 04 16;10(1):6534. Epub 2020 Apr 16.

School of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala, 147001, India.

Novel derivatives possessing imidazo[1,2-a]pyrazine and 1H-benzo[d]imidazole scaffolds were synthesized using Suzuki-Miyaura cross-coupling reactions. In vitro anticancer activities against NCI-60 cancer cell panels were tested at 10 µM concentration. The best results were obtained from substitution of two 1-cyclohexyl-1H-benzo[d]imidazole groups present at C-6 and C-8 positions of imidazo[1,2-a]pyrazine (31). Read More

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Anti-melanoma potential of two benzoquinone homologues embelin and rapanone - a comparative in vitro study.

Toxicol In Vitro 2020 Jun 10;65:104826. Epub 2020 Mar 10.

Department of Pharmacognosy, Pharmaceutical Faculty, Medical College, Jagiellonian University, Medyczna 9, 30-688 Cracow, Poland. Electronic address:

Rapanone and embelin are simple alkyl benzoquinone derivatives, mainly distributed in the Primulaceae. They have an interesting scope of biological activities including cytotoxicity. As melanoma is one of the most common types of cancer, in many cases resistant to current treatment regimens, the aim of this study was to assess and compare anti-melanoma activity of the two benzoquinones. Read More

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Synthesis of naphthalimide derivatives with potential anticancer activity, their comparative ds- and G-quadruplex-DNA binding studies and related biological activities.

Mol Biol Rep 2020 Mar 25;47(3):1563-1572. Epub 2020 Feb 25.

Department of Chemistry, Faculty of Arts and Sciences, Zonguldak Bulent Ecevit University, 67100, Zonguldak, Turkey.

Two new cytotoxic 1,8-naphthalimide derivatives have been synthesized and characterized. Their biological activities as cytotoxicity and antimicrobial activities and inhibitory activities against DNA-polymerase were evaluated. The interactions of compounds with double-stranded- and quadruple-DNA have been studied by UV-Vis, fluorescent intercalator displacement, competition dialysis, circular dichroism and the findings were compared with the parent naphthalimide and the other compounds. Read More

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Effect of the Application of a Dehydrothermal Treatment on the Structure and the Mechanical Properties of Collagen Film.

Materials (Basel) 2020 Jan 14;13(2). Epub 2020 Jan 14.

Department of Biobased Materials Science, Kyoto Institute of Technology, Kyoto 606-8585, Japan.

Dehydrothermal (DHT) treatment was used to improve the properties of collagen casings because of its non-cytotoxicity. Understanding the effects of DHT treatment on the structure and mechanical properties of collagen films is beneficial to developing satisfying collagen casings. Herein, DHT treatment with various temperatures (85-145 °C) and timescales (1-7 days) were investigated. Read More

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January 2020

Fabrication of Collagen Films with Enhanced Mechanical and Enzymatic Stability through Thermal Treatment in Fluorous Media.

ACS Appl Mater Interfaces 2020 Feb 27;12(5):6590-6597. Epub 2020 Jan 27.

Department of Chemistry , University of Massachusetts, Amherst , Massachusetts 01003 , United States.

Collagen I (Col-I) is widely used in the fabrication of biomaterials due to its biocompatibility; however, Col-I based biomaterials are susceptible to mechanical failure during handling, which limits their applicability to biomaterials. Chemical or physical treatment can improve the mechanical properties of collagen; however, these processes can create issues of cytotoxicity or denaturation. We report here an alternative strategy to improve the stability and mechanical properties of Col-I while preserving its native structure, through thermal treatment in fluorous media. Read More

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February 2020

Cytotoxic and anti-inflammatory resorcinol and alkylbenzoquinone derivatives from the leaves of Ardisia sieboldii.

Z Naturforsch C J Biosci 2019 Nov;74(11-12):303-311

PAK Research Center, University of the Ryukyus, Okinawa, Japan.

Medicinal plants belonging to the genus Ardisia are traditionally used to cure various human diseases including inflammation and cancer. This study aimed to purify and characterize cytotoxic and anti-inflammatory compounds from Ardisia sieboldii leaves. Bioassay-guided chromatographic analyses yielded three compounds, 2-methyl-5-(8Z-heptadecenyl) resorcinol (1), 5-(8Z-heptadecenyl) resorcinol (2), and ardisiaquinone A (3), whereas liquid chromatography-electrospray ionisation-mass spectrometry chemical profiling revealed the presence of diverse resorcinol and alkylbenzoquinone derivatives in cytotoxic 70% methanol extracts. Read More

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November 2019

Structure-activity relationships of new Organotin(IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7 and HeLa human cancer cell lines.

Eur J Med Chem 2019 Nov 16;181:111544. Epub 2019 Jul 16.

School of Chemistry, Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse Street, Dublin 2, Ireland. Electronic address:

There is a growing interest in the cancer cell growth inhibitory effects of organotin (IV) compounds and, accordingly, a new series of dimethyl-, di-(n-butyl)-, diphenyl- and chloro-phenyl tin(IV) complexes with a Schiff base core were prepared. Their binding to DNA was assessed by UV thermal denaturation showing no interaction and by UV-vis titration exhibiting moderate interaction by intercalation. Complexes having n-butyl substituents were more potent and cytotoxic against human leukemia, breast and cervical cancer cell lines than other organotin(IV) complexes tested. Read More

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November 2019

Effects of molecular crowding environment on the acquisition of toxic properties of wild-type SOD1.

Biochim Biophys Acta Gen Subj 2020 02 23;1864(2):129401. Epub 2019 Jul 23.

Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan; Faculty of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan. Electronic address:

Background: Mutants of Cu,Zn-superoxide dismutase (SOD1) exhibit cytotoxicity such as aggregation and pro-oxidation after denaturation, which is thought to be involved in the pathogenesis of amyotrophic lateral sclerosis (ALS). In the present study, we investigated the possibility of the acquisition of toxic properties for wild-type SOD1 (WT) in the demetalated (apo) form after denaturation.

Methods: Denaturation and subsequent pro-oxidant activity of SOD1 were confirmed by circular dichroism (CD) spectroscopy and fluorescence assay, respectively. Read More

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February 2020

Efficient synthesis of amino acid polymers for protein stabilization.

Biomater Sci 2019 Aug;7(9):3675-3682

State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, China.

Proteins are fragile such that even freezing, drying and dehydration may induce their denaturation, aggregation, and activity loss. To protect proteins from these kinds of damage, we prepared two types of amino acid polymers, poly-(l-glutamate)-r-poly-(l-lysine) (PLG-r-PLL) and poly-l-glutamate (PLG), from the efficient ring-opening polymerization of α-amino acid N-carboxyanhydride (NCA) using lithium hexamethyldisilazide (LiHMDS) as the initiator. β-galactosidase (β-Gal) was used in this study to examine the protein protecting effect of the synthesized amino acid polymers during lyophilization. Read More

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Co-precipitation Synthesis of Near-infrared Iron Oxide Nanocrystals on Magnetically Targeted Imaging and Photothermal Cancer Therapy via Photoablative Protein Denature.

Nanotheranostics 2019 25;3(3):236-254. Epub 2019 May 25.

Department of Chemistry, National Chung Hsing University, Taichung City 402, Taiwan.

Near-infrared (NIR)-based nanomaterials that provide efficient tumor ablation for cancer therapy have been reported. However, the issues of biocompatibility of metals or ions in inorganic nanoparticles systems such as copper and gold nanoparticles are still a matter of concern. In this study, we developed a facile and ligand-assisted co-precipitation method to synthesize biocompatible iron oxide (IO) nanocrystals with NIR absorption that provided T2-weighted magnetic resonance (MR) images and photothermal ablation characteristics suitable for cancer theranostics. Read More

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Cellular and Molecular Level Mechanisms against Electrochemical Cancer Therapy.

J Pathog 2019 14;2019:3431674. Epub 2019 Apr 14.

Department of Radiation Oncology, Gyeongsang National University School of Medicine and Gyeongsang National University Changwon Hospital, 11 Sangjeongja-ro, Seongsan-gu, Changwon City, Gyeongsangnam-do, Changwon 642120, Republic of Korea.

Electrochemical treatment (ECT) is a promising new way to induce tumor regression by flowing direct current into the cancer tissue. ECT was applied to different kinds of tumors in clinical studies and showed good results. In addition, basic research has almost not been done in the field of evaluation of efficacy, dose-response, and cytotoxicity. Read More

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