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Jie Tao, Feng Jiang, Cheng Liu, Zhirui Liu, Yudan Zhu, Jian Xu, Yiqin Ge, Kan Xu, Peihao Yin
Chan-su (toad venom) has been used as an analgesic agent in China from ancient to modern times. Bufalin, a non-peptide toxin extracted from toad venom, is considered as one of the analgesic components. The molecular mechanism underlying the anti-nociceptive effects of bufalin remains unclear so far. In this study, we investigated the pharmacological effects of bufalin on pain-related ion channels as well as animal models through patch clamping, calcium imaging and animal behavior observation. Using the whole-cell recording, bufalin caused remarkable suppressive effect on the peak currents of Nav channels (voltage gated sodium channels, VGSCs) of dorsal root ganglion neuroblastomas (ND7-23 cell) in a dose-dependent manner...
June 21, 2018: Molecular Biology Reports
L Santhosh, S Durgamma, Shekharappa, Vommina V Sureshbabu
A unified approach to access Nβ-protected amino alkyl isothiocyanates using Nβ-protected amino alkyl azides through a general strategy of Staudinger/aza-Wittig reaction is described. The type of protocol used to access isothiocyanates depends on the availability of precursors and also, especially in the amino acid chemistry, on the behavior of other labile groups towards the reagents used in the protocols; fortunately, we were not concerned about both these factors as precursor-azides were prepared easily by standard protocols, and the present protocol can pave the way for accessing title compounds without affecting Boc, Cbz and Fmoc protecting groups, and benzyl and tertiary butyl groups in the side chains...
June 22, 2018: Organic & Biomolecular Chemistry
Michael J Workman, John P Gleeson, Elissa J Troisi, Hannah Q Estrada, S Jordan Kerns, Christopher D Hinojosa, Geraldine A Hamilton, Stephan R Targan, Clive N Svendsen, Robert J Barrett
Background and Aims: Human intestinal organoids derived from induced pluripotent stem cells have tremendous potential to elucidate the intestinal epithelium's role in health and disease, but it is difficult to directly assay these complex structures. This study sought to make this technology more amenable for study by obtaining epithelial cells from induced pluripotent stem cell-derived human intestinal organoids and incorporating them into small microengineered Chips. We then investigated if these cells within the Chip were polarized, had the 4 major intestinal epithelial subtypes, and were biologically responsive to exogenous stimuli...
2018: Cellular and Molecular Gastroenterology and Hepatology
Huan Liu, Zhouping Yang, Linquan Zang, Guixiang Wang, Sigui Zhou, Guifang Jin, Zhicheng Yang, Xuediao Pan
Glutathione S-transferase A1 (GSTA1) is a phase II detoxification enzyme and serves a crucial role in anti-cancer drug resistance. In our previous study, GSTA1 was identified to be highly expressed in various subtypes of non-small-cell lung cancer cell lines compared with human embryonic lung fibroblast cell line MRC-5. The aim of the present study was to investigate the effect of GSTA1 expression on the proliferation and apoptosis of A549 cells. GSTA1 expression was knocked down or with overexpressed using lentivirus particles...
July 2018: Oncology Letters
Ruthellen H Anderson, Cody J Lensing, Benjamin J Forred, Michael W Amolins, Cassandra L Aegerter, Peter F Vitiello, Jared R Mays
Consumption of Brassica vegetables provides beneficial effects due to organic isothiocyanates (ITCs), a resultant product of the enzymatic hydrolysis of glucosinolate secondary metabolites. The ITC L-sulforaphane (L-SFN) is the principle agent in broccoli that demonstrates several modes of anticancer action. While the anticancer properties of ITCs like L-SFN have been extensively studied and L-SFN has been the subject of multiple human clinical trials, the scope of this work has largely been limited to those derivatives found in nature...
June 20, 2018: ChemMedChem
Adaobi Okonkwo, Joy Mitra, Gavin S Johnson, Li Li, Wan Mohaiza Dashwood, Muralidhar Hegde, Chen Yue, Roderick H Dashwood, Praveen Rajendran
SCOPE: DNA repair inhibitors have broad clinical applications in tumor types with DNA repair defects, including colorectal cancer. Structural analogs of the anticancer agent sulforaphane (SFN) were investigated as modifiers of histone deacetylase (HDAC) and histone acetyltransferase (HAT) activity, and for effects on DNA damage/repair pertinent to human colorectal cancer. METHODS AND RESULTS: In the polyposis in rat colon (Pirc) model, single oral administration of SFN and structurally-related long-chain isothiocyanates (ITCs) decreased HDAC3 expression and increased pH2AX levels markedly in adenomatous colon polyps, extending our prior observations on HDAC3 inhibition/turnover in cell-based assays...
June 20, 2018: Molecular Nutrition & Food Research
Bo-Liang Zhao, Da-Ming Du
This study demonstrates that novel isothiocyanates derived from 1-indanones are useful building blocks in heteroannulation reactions with isatinimines. This convenient Mannich/cyclization cascade reaction serves as a powerful tool for the enantioselective construction of bispirocyclic indanone-thioimidazolidine-oxindoles bearing two adjacent spiro-quaternary stereocenters in good to excellent yields with excellent diastereo- and enantioselectivities. Versatile transformations of the products into other potential bioactive bispirocyclic heterocycles have also been demonstrated...
June 20, 2018: Organic Letters
Shu-Jian Zheng, Shi-Jie Liu, Quan-Fei Zhu, Ning Guo, Ya-Lan Wang, Bi-Feng Yuan, Yu-Qi Feng
Chemical labeling (CL) in combination with liquid chromatography-mass spectrometry (LC-MS) analysis has been demonstrated to be a promising technology in metabolomic analysis. However, identification of chemically-labeled metabolites remains to be challenging. Retention time (RT) is one of the most important parameters for the identification of metabolites, but it could vary greatly in LC-MS analysis. In this work, we developed a chemical labeling-based HPLC retention index (CL-HPLC RI) strategy to facilitate the identification of metabolites...
June 20, 2018: Analytical Chemistry
Aroonwan Lam-Ubol, Alison Lea Fitzgerald, Arnat Ritdej, Tawaree Phonyiam, Hui Zhang, Jeffrey N Myers, Peng Huang, Dunyaporn Trachootham
High doses of β-phenylethyl isothiocyanate (PEITC), a phytochemical in cruciferous vegetables, are not feasible for consumption due to a strong mouth-tingling effect. This study investigated the anti-cancer effect of PEITC at sensory acceptable doses. In vitro, PEITC was selectively toxic to oral cancer cells (CAL-27, FaDu, SCC4, SCC 9, SCC15, SCC25 and TU138), compared to oral keratinocytes (OKF6/TERT2 and NOK/Si). In vivo, 5 and 10 mg kg-1 PEITC, equivalent to human organoleptically acceptable doses, retarded tumor growth and prolonged the survival of mice bearing p53-mutated oral cancer cells - TU138 xenograft...
June 20, 2018: Food & Function
Pedram Madadkar, Rahul Sadavarte, Raja Ghosh
Enrichment and immobilization of analytes by chemical bonding or physical adsorption is typically the first step in many commonly used analytical techniques. In this paper, we discuss a permeation drag based technique as an alternative approach for carrying out location-specific immobilization of macromolecular analytes. Fluorescein isothiocyanate (FITC) labeled macromolecules and their complexes were enriched near the surface of ultrafiltration membranes and detected by direct visual observation and fluorescence imaging...
June 2018: Journal of Pharmaceutical Analysis
Sreekar B Marpu, Erin N Benton
Chitosan (CS) is a natural polymer derived from chitin that has found its usage both in research and commercial applications due to its unique solubility and chemical and biological attributes. The biocompatibility and biodegradability of CS have helped researchers identify its utility in the delivery of therapeutic agents, tissue engineering, wound healing, and more. Industrial applications include cosmetic and personal care products, wastewater treatment, and corrosion protection, to name a few. Many researchers have published numerous reviews outlining the physical and chemical properties of CS, as well as its use for many of the above-mentioned applications...
June 17, 2018: International Journal of Molecular Sciences
Umme Salma, Taous Khan, Abdul Jabbar Shah
ETHNOPHARMACOLOGICAL RELEVANCE: Eruca sativa Mill., (Brassicaceae) is a popular remedy for the treatment of hypertension in Pakistan. However, direct effect of the extract and its fractions on blood pressure and vascular tone are unknown. AIM OF THE STUDY: This investigation was aimed to explore the pharmacological base for the traditional use of E. sativa in hypertension. MATERIALS AND METHODS: In-vivo blood pressure study was carried out using normotensive and high salt-induced hypertensive rats under anaesthesia...
June 15, 2018: Journal of Ethnopharmacology
E Zhang, Fulong Chu, Lixu Xu, Hao Liang, Shuliang Song, Aiguo Ji
A new method to label fucoidan sulfate was established with tyramine and fluorescein isothiocyanate isomer I (FITC). The fluorescence spectrophotometry and high performance liquid chromatography verified the successful labelling of fucoidan by FITC. The results of the single-pass intestinal perfusion indicated jejunum and ileum as the main absorption sites, and there was carrier saturation. In addition, fucoidan sulfate at 1 mg/mL had no inhibitory effect on Caco-2 cell proliferation. Studies on the transmembrane transport mechanism showed that fucoidan can be absorbed because the apparent permeability coefficient of drugs (Papp ) A→B was 3...
June 14, 2018: Biopharmaceutics & Drug Disposition
Letizia Romeo, Francesca Diomede, Agnese Gugliandolo, Domenico Scionti, Fabrizio Lo Giudice, Veronica Lanza Cariccio, Renato Iori, Placido Bramanti, Oriana Trubiani, Emanuela Mazzon
The therapeutic strategies for neurodegenerative diseases still represent a vast research field because of the lack of targeted, effective and resolutive treatment for neurodegenerative diseases. The use of stem cell-based therapy is an alternative approach that could lead to the replacement of damaged neuronal tissue. For this purpose, adult mesenchymal stem cells (MSC), including periodontal ligament stem cells (PDLSCs), could be very useful for their differentiation capacity, easy isolation and the ability to perform an autologous implant...
June 14, 2018: Scientific Reports
Daiki Nomura, Masaaki Saito, Yosuke Takahashi, Yuki Takahashi, Yoshinobu Takakura, Makiya Nishikawa
Self-gelling DNA hydrogels with cytosine-phosphate-guanine (CpG) motifs have been shown to exhibit high potency as vaccine adjuvants. However, their oral use is limited because of their thermodynamic and chemical instability in the gastrointestinal tract. In this study, we aimed to develop DNA hydrogel microspheres (Dgel-MS) coated with chitosan to improve their stability. Chitosan-coated Dgel-MS (Cs-Dgel-MS) was prepared by emulsifying Dgel to obtain the D-gel core, followed by mixing with microemulsions of chitosan for electrostatic coating...
June 11, 2018: International Journal of Pharmaceutics
Teresa Oliviero, Ruud Verkerk, Matthijs Dekker
The formation of health-beneficial isothiocyanates (ITCs) from glucosinolates depends on a wide variety of plant-intrinsic factors (e.g., concentration of glucosinolates, activity of myrosinase and specifier proteins) and on a multitude of extrinsic post-harvest factors such as the conditions used during industrial processing, domestic preparation, mastication and digestion. All of these factors contribute to a large variability in the formation of ITCs (and other breakdown products), as well as their intake and absorption upon consumption of Brassica vegetables...
June 13, 2018: Molecular Nutrition & Food Research
Makoto Shirakawa, Ikuko Hara-Nishimura
Plant vacuoles display many versatile functions. Vacuoles in vegetative tissues are generally involved in protein degradation, and are called lytic vacuoles. However, vegetative vacuoles in specialized cells can accumulate large concentrations of proteins, such as those in idioblast myrosin cells along veins in the order Brassicales, which store large amounts of myrosinases (thioglucoside glucohydrolase, TGG). Myrosinases cleave the bond between sulfur and glucose in sulfur-rich compounds (glucosinolates) to produce toxic compounds (isothiocyanates) when plants are damaged by pests...
April 20, 2018: Plant & Cell Physiology
Meifen Chu, Tongtong Wang, Aihua Sun, Yu Chen
Pancreatic cancer is the fourth leading cause of cancer-associated cases of mortality worldwide. Prostaglandin-endoperoxide synthase 2 (COX-2) is considered a therapeutic target for prevention of pancreatic cancer. Nimesulide, a selective COX-2 inhibitor, can induce cell apoptosis, resulting in an anti-cancer effect. However, the mechanism underlying this effect remains to be elucidated. The present study aimed to evaluate the effects of nimesulide on proliferation of PANC-1 cells using an MTT assay. Apoptosis was evaluated by DNA laddering and Annexin V-fluorescein isothiocyanate/propidium iodide-stained flow cytometry...
July 2018: Experimental and Therapeutic Medicine
Lian-Wei Li, Chao Na, Song-Yu Tian, Jie Chen, Rong Ma, Ying Gao, Ge Lou
Ellagic acid has been reported to possess various activities, including anti-inflammatory, anti-oxidative, antiviral and anticancer abilities. However, the effect and underlying molecular mechanism of ellagic acid on cervical carcinoma remain unclear. Therefore, the present study aimed to investigate the effects of ellagic acid on human cervical carcinoma cells and the molecular mechanism involved. The present study assessed the survival of HeLa cells cultured in vitro using an MTT assay. Apoptosis rate and cell cycle of HaLa cells were measured using an Annexin V-Fluorescein isothiocyanate/propidium iodide Apoptosis Detection and Cell Cycle Analysis kits, respectively, following treatment with varying concentrations of ellagic acid...
July 2018: Experimental and Therapeutic Medicine
In Heon Lee, Matthew S Palombo, Xiaoping Zhang, Zoltan Szekely, Patrick J Sinko
The feasibility of utilizing the cell surface chemokine receptor CXCR4 for human immunodeficiency virus (HIV) entry inhibition and as an intracellular portal for targeted drug delivery was evaluated. Novel DV3 ligands (1DV3, 2DV3, and 4DV3) were designed, synthesized and conjugated to various probes (fluorescein isothiocyanate (FITC) or biotin) and cargos with sizes ranging from 10 to 50 nm (polyethylene glycol (PEG), streptavidin, and a polymeric nanoparticle). 4DV3 conjugated probes inhibited HIV-1 entry into the CXCR4-expressing reporter cell line TZM-bl (IC50 at 553 nM) whereas 1DV3 and 2DV3 did not...
June 9, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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