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Jasna Lojk, Vladimir Boštjan Bregar, Klemen Strojan, Samo Hudoklin, Peter Veranič, Mojca Pavlin, Mateja Erdani Kreft
The blood-urine barrier is the tightest and most impermeable barrier in the body and as such represents a problem for intravesical drug delivery applications. Differentiation-dependent low endocytotic rate of urothelial cells has already been noted; however, the differences in endocytosis of normal and cancer urothelial cells have not been exploited yet. Here we analysed the endocytosis of rhodamine B isothiocyanate-labelled polyacrylic acid-coated cobalt ferrite nanoparticles (NPs) in biomimetic urothelial in vitro models, i...
August 18, 2017: Histochemistry and Cell Biology
Yujia Liu, Momoko Yamanaka, Naomi Abe-Kanoh, Xiaoyang Liu, Beiwei Zhu, Shintaro Munemasa, Toshiyuki Nakamura, Yoshiyuki Murata, Yoshimasa Nakamura
In the present study, we assessed benzyl isothiocyanate (BITC), an organosulfur compound from cruciferous vegetables, as a potential inducer of aldehyde dehydrogenase (ALDH) activity using murine hepatoma Hepa1c1c7 cells. BITC was shown to enhance not only the total ALDH activity, but also the ALDH activity of the cytosolic/microsomal and mitochondrial fraction. BITC also significantly increased the gene and protein expression of ALDH1A1, ALDH2 and ALDH3A1 in a concentrationdependent manner. Simultaneously, the gene expression of phase 2 drugmetabolizing enzymes, such as NAD(P)H: quinone oxidoreductase 1 and heme oxygenase-1, was increased by the BITC treatment...
August 15, 2017: Food and Chemical Toxicology
Yuanshuang Xu, Bin Li, Xinying Zhang, Xuesen Fan
In this paper, a highly efficient and sustainable synthesis of 2-aminobenzothiazoles through the cascade reactions of isothiocyanatobenzenes with primary or secondary amines by using iodine as a catalyst and oxygen as an oxidant is presented. Mechanistically, the formation of the title compounds involves the in situ formation of the required benzothiourea intermediate followed by its intramolecular cross dehydrogenative coupling of a C(sp2)-H bond and a S-H bond. To our knowledge, this should be the first example in which 2-aminobenzothiazoles are efficiently prepared from simple and cheap isothiocyanates and amines under metal free conditions by using iodine as a catalyst and molecular oxygen as an oxidant with water as the byproduct...
August 16, 2017: Journal of Organic Chemistry
Shafinah Ahmad Suhaimi, Sok Lai Hong, Sri Nurestri Abdul Malek
BACKGROUND: Ruta angustifolia Pers. is a perennial herb that is cultivated worldwide, including Southeast Asia, for the treatment of various diseases as traditional medicine. OBJECTIVE: The purpose of the study was to identify an active principle of R. angustifolia and to investigate its effect on the HT29 cell death. MATERIALS AND METHODS: The methanol and fractionated extracts (hexane, chloroform, ethyl acetate, and water) of R. angustifolia Pers...
July 2017: Pharmacognosy Magazine
Hye-Jin Park, Jeong-Bin Park, Sang-Jae Lee, Minjung Song
Colon cancer is one of the most common types of cancer, and it has recently become a leading cause of death worldwide. Among colon cancers, the v-ki-ras2 Kirsten rat sarcoma viral oncogene homolog (KRAS)-mutated form is notorious for its non-druggable features. Cetuximab, a monoclonal antibody that binds to the epidermal growth factor receptor, has been introduced as an antitumor therapy; however, secondary resistance and side effects significantly limit its effective use in these cancers. In this study, we prepared Phellinuslinteus on germinated brown rice (PBR) extracts to increase the sensitivity of KRAS-mutated colon cancers to cetuximab...
August 11, 2017: International Journal of Molecular Sciences
Haniyeh Hemmatian, Michaël R Laurent, Samaneh Ghazanfari, Dirk Vanderschueren, Astrid D Bakker, Jenneke Klein-Nulend, G Harry van Lenthe
Bone's microporosity plays important roles in bone biology and bone mechanical quality. In this study, we explored the accuracy and reproducibility of nondestructive desktop μCT for 3D visualization and subsequent morphometric analysis of mouse cortical bone microporosity including the vascular canal network and osteocyte lacunae. The accuracy of measurements was evaluated in five murine fibula using confocal laser scanning microscopy (CLSM) in conjunction with Fluorescein isothiocyanate (FITC) staining as the reference method...
2017: PloS One
Mohamed K Al-Essa, Susanne Melzer, Attila Tarnok, Kamal A Hadidi, Mohammed El-Khateeb
This study was designed to load different antibodies (Abs) and a fluorescent dye onto the red blood cell (RBC) surface. We have used fluorescein isothiocyanate (FITC)-conjugate anti-human Ab, CD22-PE (B-cell marker-phycoerythrin Ab), and 4',6-diamidino-2-phenylindole (DAPI) for insertion over the RBC surface. In a first step, conjugation experiments were performed: in dimethyl sulfoxide (DMSO), RBCs were conserved and modified by succinic anhydride to create an additional -COOH group, and then activated with 3-(3-dimethylaminopropyl)carbodiimide-N-hydroxysuccinimide (EDC-NHS) in 2-(N-morpholino) ethanesulfonic acid hydrate buffer for insertion of labeled Abs or DAPI...
August 9, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Asha Jaja-Chimedza, Brittany L Graf, Charlotte Simmler, Youjin Kim, Peter Kuhn, Guido F Pauli, Ilya Raskin
Moringa oleifera Lam. is a tropical plant, used for centuries as food and traditional medicine. The aim of this study was to develop, validate and biochemically characterize an isothiocyanate-enriched moringa seed extract (MSE), and to compare the anti-inflammatory effects of MSE-containing moringa isothiocyanate-1 (MIC-1) with a curcuminoid-enriched turmeric extract (CTE), and a material further enriched in its primary phytochemical, curcumin (curcumin-enriched material; CEM). MSE was prepared by incubating ground moringa seeds with water to allow myrosinase-catalyzed enzymatic formation of bioactive MIC-1, the predominant isothiocyanate in moringa seeds...
2017: PloS One
Jochen-Frederick Hernekamp, Florian Neubrech, Tomke Cordts, Volker J Schmidt, Ulrich Kneser, Thomas Kremer
PURPOSE: The clinical course after major burns is characterized by microcirculatory changes and consecutive capillary leakage. However, current clinical monitoring does not properly assess microcirculation, whereas macrohemodynamic changes are continuously evaluated. Here, we assess if macrohemodynamic and microhemodynamic parameters after burn trauma are correlated in a rat model. METHODS: Burn plasma harvested from donor rats 4 hours after thermal injury (30% total body surface area, 100 °C water, 12 seconds) was administered intravenously to healthy animals during 2 hours of intravital microscopy (burn group [BG])...
November 2016: Annals of Plastic Surgery
Lijuan Zhang, Gang Feng, Xinyan Zhang, Yawen Ding, Xiaojuan Wang
Dysregulation of microRNAs (miRNAs) in colorectal cancer provides important opportunities for the development of future miRNA‑based therapies. The present study aimed to assess the role of miRNA‑630 (miR‑630) expression in colorectal cancer. HCT116 human colorectal cancer cells were transfected with miR‑630 inhibitor, mimic or control miRNA, and the effects of miR‑630 dysregulation on cell viability, proliferation and apoptosis were analyzed using MTT and bromodeoxyuridine assays, and an annexin V‑fluorescein isothiocyanate cell apoptosis kit, respectively...
August 3, 2017: Molecular Medicine Reports
Wei Chen, Jie Yang, Shuhua Chen, Hong Xiang, Hengdao Liu, Dan Lin, Shaoli Zhao, Hui Peng, Pan Chen, Alex F Chen, Hongwei Lu
OBJECTIVE: Mitochondrial Ca(2+) overload is implicated in hyperglycaemia-induced endothelial cell dysfunction, but the key molecular events responsible remain unclear. We examined the involvement of mitochondrial calcium uniporter, which mediates mitochondrial Ca(2+) uptake, in endothelial cell dysfunction resulting from high-glucose treatment. METHODS: Human umbilical vein endothelial cells were exposed to various glucose concentrations and to high glucose (30 mM) following mitochondrial calcium uniporter inhibition or activation with ruthenium red and spermine, respectively...
August 1, 2017: Diabetes & Vascular Disease Research
Kuang-Chi Lai, Yung-Ting Hsiao, Jiun-Long Yang, Yi-Shih Ma, Yi-Ping Huang, Tai-An Chiang, Jing-Gung Chung
Benzyl isothiocyanate (BITC), and phenethyl isothiocyanate (PEITC) have been demonstrated to induce anticancer function in many human cancer cells and also inhibit cancer cell migration and invasion. However, there are no studies that show BITC and PEITC to inhibit cell migration and invasion in mouse melanoma B16F10 cells. In this study, we investigated anti-metastasis effects of BITC and PEITC in melanoma cancer cells in vitro. Under sub-lethal concentrations (from 1, 2.5 up to 5 µM), BITC and PEITC significantly inhibited cell mobility, migration and invasion nature of B16F10 cells...
September 2017: International Journal of Oncology
Stephen J Geier, James H W LaFortune, Diya Zhu, Stephanie C Kosnik, Charles L B Macdonald, Douglas W Stephan, Stephen A Westcott
The transition metal-free addition of phosphinoboronate ester Ph2PBpin (pin = 1,2-O2C2Me4) to heterocumulenes including carbodiimides, isocyanates, isothiocyanates and carbon dioxide has been investigated. The corresponding 1,2-addition products were readily prepared at room temperature without the need of a catalyst or added base. Addition of methanol to the compounds derived from addition of Ph2PBpin to carbodiimides, isocyanates, and isothiocyanates resulted in traditional hydrophosphination products. The methodology developed in this study provides a simple and elegant route for the generation of a wide range of functionalized phosphines...
August 2, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Paz Trillo, Tove Slagbrand, Fredrik Tinnis, Hans Adolfsson
The development of an efficient protocol for the reductive functionalization of amides into pyrimidinediones and amino-substituted thioacrylamides is presented. Enamines are generated in a highly chemoselective amide hydrosilylation reaction catalyzed by molybdenum hexacarbonyl in combination with 1,1,3,3-tetramethyldisiloxane. The direct addition of either isocyanate or isothiocyanate generates the corresponding pyrimidinediones and 3-aminothioacrylamides in high yields.
August 2, 2017: Chemical Communications: Chem Comm
Yan Lin, Wenbin Kuang, Bitao Wu, Changli Xie, Cuiyin Liu, Zhiguang Tu
Interleukin-12 (IL-12) serves an important role in immune responses and antitumor activity. The study of the association between autophagy and cancer cells remains controversial. The present study aimed to investigate the effect of IL‑12 on autophagy in the human breast cancer cell lines MDA‑MB‑231 and MCF‑7, and the possible molecular mechanism. Breast cancer cells were treated with different concentrations of recombinant IL‑12. The expression of the autophagy-associated protein microtubule‑associated protein light chain 3 (LC3) was determined using western blot analysis, fluorescein isothiocyanate‑labeled LC3 was detected using fluorescence microscopy and autophagosomes were examined using transmission electron microscopy...
July 31, 2017: Molecular Medicine Reports
Saiman Zhang, Huilong Ou, Chunyun Liu, Yuan Zhang, Samir Mitragotri, Dexiang Wang, Ming Chen
We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of Fluorescein isothiocyanate-Dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (~120 μm in length and ~7 μm in diameter). SHS can physically disrupt skin in a dose-dependent manner and retain within the skin over at least 72 hours, which allows sustained skin penetration of hydrophilic biomacromolecules. The magnitude of enhancement of FD delivery into skin induced by SHS treatment was dependent on its molecular weight...
August 1, 2017: Molecular Pharmaceutics
Peng Zhang, Yuxin Liu
Sample enrichment or molecules concentration is considered as an essential step for sample processing in miniaturized devices aiming at biosensing and bioanalysis. Among all the means involved to achieve this aim, dielectrophoresis (DEP) is increasingly employed in molecules manipulation and concentration because it is non-destructive and high efficiency. This paper presents a methodology to achieve protein concentration utilizing the combination effects of electrokinetics and low frequency insulator-based dielectrophoresis (iDEP) generated within a microfluidic device, in which a submicron constricted channel was fabricated using DNA molecular combing and replica molding...
July 28, 2017: Biofabrication
Yun-Jeong Jeong, Hyun-Ji Cho, Fung-Lung Chung, Xiantao Wang, Hyang-Sook Hoe, Kwan-Kyu Park, Cheorl-Ho Kim, Hyeun-Wook Chang, Sang-Rae Lee, Young-Chae Chang
Isothiocyanates, which are present as glucosinolate precursors in cruciferous vegetables, have strong activity against various cancers. Here, we compared the anti-metastatic effects of isothiocyanates (benzyl isothiocyanate (BITC), phenethyl isothiocyanate (PEITC), and sulforaphane (SFN)) by examining how they regulate MMP-9 expression. Isothiocyanates, particularly PEITC, suppressed 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced MMP-9 activity and invasion in various cancer cell lines. By contrast, N-methyl phenethylamine, a PEITC analog without an isothiocyanate functional group, had no effect...
July 12, 2017: Oncotarget
Maciej Wos, Małgorzata Miazga-Karska, Agnieszka A Kaczor, Katarzyna Klimek, Zbigniew Karczmarzyk, Dorota Kowalczuk, Waldemar Wysocki, Grazyna Ginalska, Zofia Urbanczyk-Lipkowska, Maja Morawiak, Monika Pitucha
A series of thiosemicarbazides with 4-nitrophenyl group was obtained in the reaction of carboxylic acid hydrazides with isothiocyanates. All compounds were checked for their antibacterial and antiproliferative activity. Our results have shown that derivatives 6-8 possessed antibacterial activity against S. aureus, S. epidermidis, S. mutans and S. sanguinis, moderate cytotoxicity and good therapeutic safety in vitro. Additionally, compounds 1 and 4 significantly inhibited A549, HepG2 and MCF-7 cell division...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Diego Romano Perinelli, Driton Vllasaliu, Giulia Bonacucina, Benedetta Come, Stefania Pucciarelli, Massimo Ricciutelli, Marco Cespi, Rosangela Itri, Francesco Spinozzi, Giovanni Filippo Palmieri, Luca Casettari
The use of surfactants as drug permeability enhancers across epithelial barriers remains a challenge. Although many studies have been performed in this field using synthetic surfactants, the possibility of employing surfactants produced by bacteria (the so called biosurfactants") has not been completely explored. Among them, one of the most well characterized class of biosurfactants are rhamnolipids. The aim of the study was to investigate the effect of rhamnolipids on the epithelial permeability of fluorescein isothiocyanate-labelled dextrans 4kDa and 10kDa (named FD4 and FD10, respectively) as model for macromolecular drugs, across Caco-2 and Calu-3 monolayers...
July 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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