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Hua Yao, Jinqi Ma
The present paper investigates the enhancement of the therapeutic effect of Paclitaxel (a potent anticancer drug) by increasing its cellular uptake in the cancerous cells with subsequent reduction in its cytotoxic effects. To fulfill these goals the Paclitaxel (PTX)-Biotinylated PAMAM dendrimer complexes were prepared using biotinylation method. The primary parameter of Biotinylated PAMAM with a terminal HN2 group - the degree of biotinylation - was evaluated using HABA assay. The basic integrity of the complex was studied using DSC...
2018: Acta Biochimica Polonica
Rihab Khlifi, Zaineb Dhaouefi, Mouna Maatouk, Aicha Sassi, Najet Boudhiba, Irina Ioannou, Kamel Ghedira, Leila Chekir-Ghedira, Soumaya Kilani-Jaziri
Plants and natural molecules are generally consumed not in raw state but after different processing conditions (heating, mechanical agitation or cooking). The understanding of the chemistry and biological outcome of thermal treatment is still scarce. In the current study, Eriodictyol, a natural flavanone, has undergone heat treatment, generating hence three different products ((3-(3,4-dihydroxyphenyl)-3-hydroxypropanoic acid, (3-(3,4-dihydroxyphenyl) propanal) and an unidentified component). The consequences of aforementioned treatment on the immunomodulatory behavior of resulted molecules were evaluated...
June 15, 2018: International Immunopharmacology
Bruna Medeiros-Neves, Helder Ferreira Teixeira, Gilsane Lino von Poser
ETHNOPHARMACOLOGICAL RELEVANCE: Species of the genus Pterocaulon (Asteraceae) are used in different parts of the world for mainly to treat skin and liver diseases, as well as disorders of the respiratory system, among others. AIM OF THE STUDY: This review aims to discuss the present state of the art concerning the ethnobotanical uses, secondary metabolites and biological effects of Pterocaulon species and their chemical components. MATERIALS AND METHODS: The available information on the genus Pterocaulon was gathered from scientific databases (Web of Science, Pubmed, ScienceDirect, Scopus, ChemSpider, SciFinder ACS Publications, Wiley Online Library)...
June 15, 2018: Journal of Ethnopharmacology
Angel Josabad Alonso-Castro, Juan Ramón Zapata-Morales, Victor Arana-Argáez, Julio Cesar Torres-Romero, Eyra Ramírez-Villanueva, Sabino Eduardo Pérez-Medina, Marco Antonio Ramírez-Morales, Mario Alberto Juárez-Méndez, Yessica Paola Infante-Barrios, Fidel Martínez-Gutiérrez, Candy Carranza-Álvarez, Mario Alberto Isiordia-Espinoza, Andrés Flores-Santos
Eysenhardtia polystachya is used for the empirical treatment of cancer, infections, diarrhea, inflammation, and pain. This study identified, using GC-MS, the main chemical components in an ethanol extract of E. polystachya branches and leaves (EPE) and tested its cytotoxic, antimicrobial, anti-diarrheal, anti-inflammatory, and antinociceptive effects. The in vitro and in vivo toxicity of EPE was evaluated using the comet assay in human peripheral blood mononuclear cells (PBMC) and the acute toxicity test in mice, respectively...
June 15, 2018: Journal of Ethnopharmacology
Yuan-Chin Lee, Liang-Jun Wang, Chia-Hui Huang, Yi-Jun Shi, Long-Sen Chang
The present study aimed to investigate the pathway related to MCL1 expression in ABT-263-treated human leukemia U937 cells. ABT-263 upregulated MCL1 protein expression but did not affect its mRNA level and protein stability. Notably, ABT-263 increased 4EBP1 mRNA decay and thus reduced 4EBP1 expression. Overexpression of 4EBP1 abrogated ABT-263-induced MCL1 upregulation. ABT-263-induced activation of IKKα/β-NFκB axis elicited autophagy of U937 cells, leading to reduced mRNA stability of 4EBP1. Inhibition of the IKKα/β-NFκB axis or autophagy mitigated the effect of ABT-263 on 4EBP1 and MCL1 expression...
June 15, 2018: Cancer Letters
Céline Parmentier, Delilah F G Hendriks, Bruno Heyd, Philippe Bachellier, Magnus Ingelman-Sundberg, Lysiane Richert
Cholestasis represents a major subtype of drug-induced liver injury and novel preclinical models for its prediction are needed. Here we used primary human hepatocytes (PHH) from different donors in 2D-sandwich (2D-sw) and/or 3D-spheroid cultures to study inter-individual differences in response towards cholestatic hepatotoxins after short-term (48-72 h) and long-term repeated exposures (14 days). Cholestatic liabilities were determined by comparing cell viability upon exposure to the highest non-cytotoxic drug concentration in the presence and absence of a non-cytotoxic concentrated bile acid (BA) mixture...
June 15, 2018: Toxicology Letters
Roberto Marques Damiani, Dinara Jaqueline Moura, Cassiana Macagnan Viau, Verônica Brito, Ana Moira Morás, João Antonio Pêgas Henriques, Jenifer Saffi
Doxorubicin (DOX) and Mitoxantrone (MTX) are very effective drugs for a range of tumors despite being highly cardiotoxic. DNA topoisomerase 2 beta (Top2ß) was revealed as key mediator of DOX-induced cardiotoxicity, although ROS generation is also an important mechanism. Oxidative stress is also an important issue in MTX-induced cardiotoxicity that is manifested by mitochondrial dysfunction. Studies have demonstrated the relationship between PARP-1 overactivation and cell viability in DOX-treated cardiomyocytes...
June 15, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
Nan Jiang, Chengjie Meng, Xiao Han, Guo Jun, Haoming Li, Zhengquan Yu
Astrocytes are the most abundant cell type in the central nervous system. Defects in astrocyte function have been implicated in a variety of diseases. Cisplatin (CDDP) is a chemotherapeutic drug that is widely used to treat various cancers. However, it causes neurocognitive impairment in patients. Little is known about the damaging effects of chemotherapeutic drugs like CDDP on astrocytes. Presently, we found that a low dose of CDDP distinctly inhibited astrocyte proliferation and induced delayed cell death...
June 15, 2018: Neuroscience Letters
Ningombam Swapana, Takehiro Tominaga, Abdelsamed I Elshamy, Mahmoud A A Ibrahim, Mohamed-Elamir F Hegazy, Ch Brajakishor Singh, Midori Suenaga, Hiroshi Imagawa, Masaaki Noji, Akemi Umeyama
A new unusual seco-isopimarane, kaemgalangol A (1) and 12 usual analogs (2-13) were isolated from the rhizomes of Kaempferia galanga (Family: Zingiberaceae). KaemgalangolA (1) represented a rarely isolated 9,10-seco-isopimarane skeleton. The chemical structures of the isolated compounds were mainlyinvestigated by spectroscopic techniques such as 1D, 2D NMR, and HRMS. The absolute configuration of 1-3 was studied by X-ray diffraction analysis as well as experimental and TDDFT-calculated electronic circular dichroism...
June 15, 2018: Fitoterapia
Kim Min, Seung Cheol Jee, Jung-Suk Sung, Avinash A Kadam
Owing to the ubiquitous availability and simple biocatalysis, the anti-proliferative laccase holds enormous opportunities for anti-cancer applications. However, accessing efficient and specific (super-magnetically targetable) new delivery system for anti-proliferative laccase is vital step towards laccase based anti-cancer approach. Therefore, in this investigation, super-magnetized (Fe3 O4 ) and chitosan (CS) functionalized halloysite nanotubes (HNTs) (termed as Fe3 O4 -HNTs-CS) was facile synthesized. Further, laccase from Trametes versicolor was immobilized on Fe3 O4 -HNTs-CS (termed as Fe3 O4 -HNTs-CS-Lac)...
June 15, 2018: International Journal of Biological Macromolecules
Chisato Hoshina, Tomohiro Omura, Katsuhiro Okuda, Hiroki Tanaka, Masaru Asari, Shotaro Isozaki, Kie Horioka, Hiromi Yamada, Hiroki Doi, Hiroshi Shiono, Kazuo Matsubara, Keiko Shimizu
Paraquat (PQ) is a widely used herbicide in the world despite being highly toxic to humans. PQ causes fatal damage to multiple organs, especially the lungs. While oxidative stress is the main toxic mechanism of PQ, there is no established standard therapy for PQ poisoning. In this study, we investigated the cytoprotective effect of 4-phenylbutyrate (4PBA) on PQ toxicity in human lung adenocarcinoma A549 cells. Phosphorylation levels of major survival signaling kinases Akt and ERK, as well as expression levels of antioxidant enzymes catalase and superoxide dismutase 2 (SOD2) were examined...
June 15, 2018: Biochemical and Biophysical Research Communications
Wensi Xu, Shunya Saiki, Takumi Myojin, Yujia Liu, Beiwei Zhu, Yoshiyuki Murata, Hitoshi Ashida, Makoto Tsunenaga, Yoshimasa Nakamura
Lycii Fructus is the dried ripe fruits of Lycium chinense and L. barbarum, which has long been used as a traditional food material in East Asia. The purpose of this study was to investigate the role of the indirect antioxidative action in the Lycii fructus extract (LFE)-induced cytoprotective effect in vitro. LFE significantly enhanced the expression of the drug-metabolizing enzyme genes and intracellular glutathione level in mouse hepatoma Hepa1c1c7 cells. LFE stimulated the nuclear translocation of aryl hydrocarbon receptor as well as nuclear factor (erythroid-derived 2)-like 2...
June 18, 2018: Bioscience, Biotechnology, and Biochemistry
Rory D de Vries, Arwen F Altenburg, Nella J Nieuwkoop, Erwin de Bruin, Stella E van Trierum, Mark R Pronk, Mart M Lamers, Mathilde Richard, David F Nieuwenhuijse, Marion P G Koopmans, Joost H C M Kreijtz, Ron A M Fouchier, Albert D M E Osterhaus, Gerd Sutter, Guus F Rimmelzwaan
Background: Highly pathogenic avian influenza viruses continue to circulate in poultry and wild birds and occasionally infect humans, sometimes with fatal outcome. Development of vaccines is a priority to prepare for potential pandemics, however complicated by antigenic variation of the surface glycoprotein hemagglutinin. We report the immunological profile induced by human immunization with Modified Vaccinia virus Ankara expressing the hemagglutinin gene of H5N1 virus A/Vietnam/1194/04 (rMVA-H5)...
April 18, 2018: Journal of Infectious Diseases
Aubrie O'Rourke, Stephan Kremb, Brendan M Duggan, Salim Sioud, Najeh Kharbatia, Misjudeen Raji, Abdul-Hamid Emwas, William H Gerwick, Christian R Voolstra
Viruses are underrepresented as targets in pharmacological screening efforts, given the difficulties of devising suitable cell-based and biochemical assays. In this study we found that a pre-fractionated organic extract of the Red Sea sponge Amphimedon chloros was able to inhibit the West Nile Virus NS3 protease (WNV NS3). Using liquid chromatography⁻mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR) spectroscopy, the identity of the bioactive compound was determined as a 3-alkylpyridinium with m / z = 190...
June 18, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Katie Palen, Monica Thakar, Bryon D Johnson, Jill A Gershan
Adoptive cell therapy (ACT) of chimeric antigen receptor T cells has demonstrated remarkable success for the treatment of pediatric B-cell leukemia. For patients who are not candidates for chimeric antigen receptor T-cell therapy, ACT using tumor antigen-experienced polyclonal T cells may be a treatment option. Since leukemic blasts reside in the bone marrow and bone marrow is a preferred site for homeostatic proliferation of cytotoxic memory CD8 T cells, we hypothesized that bone marrow would be a source of activated T cells...
June 14, 2018: Journal of Pediatric Hematology/oncology
Zhen-Tao Song, Leshuai W Zhang, Li-Qiang Fan, Jing-Wen Kong, Jun-Hua Mao, Jian Zhao, Fu-Jun Wang
Cyclosporin A (CsA) is a calcium antagonist and can enhance the efficacy of some protein drugs, but its mechanism remains unknown. In this study, MAP30, a ribosome-inactivating protein reported to have apoptotic effects on cancer cells, was fused with S3, an epidermal growth factor receptor (EGFR)-targeting peptide. In addition, CsA was used to investigate whether it can further promote the apoptotic effects of S3 fused MAP30 (MAP30-S3). Our result showed that the internalization of FITC-labeled MAP30-S3 was increased significantly by S3 in HeLa cells...
June 14, 2018: Anti-cancer Drugs
Xiao-Yan Yang, Wan-Rong Niu, Rui-Ting Li, Xiu-Ming Cui, Ji-Kai Liu
Two new sesquiterpenes (1-2), along with one known sesquiterpene (3), were isolated from cultures of the higher fungus Pholiota nameko. The structures of new compounds were elucidated by extensive spectroscopic methods. The known compound was identified by comparing its spectroscopic data with those reported in the literature. All compounds were evaluated for their cytotoxicities against five human cancer cell lines.
June 18, 2018: Natural Product Research
Hao-Bing Yu, Heng Jiao, Yu-Ping Zhu, Jian-Peng Zhang, Xiao-Ling Lu, Xiao-Yu Liu
Two new cyclohexanone derivatives, nectriatones A-B (1-2), and one new natural product, nectriatone C (3), together with three known phenolic sesquiterpene derivatives (4-6), were isolated from the culture of Nectria sp. B-13 obtained from high-latitude soil of the Arctic. The structures of all compounds were unambiguously elucidated by extensive spectroscopic analysis, as well as by comparison with the literature. These compounds were evaluated in cytotoxic and antibacterial activities. Compounds 1-6 showed cytotoxicities against SW1990, HCT-116, MCF-7, and K562 cells, with IC50 values in the range of 0...
June 18, 2018: Journal of Asian Natural Products Research
Abolfazl Shakeri, Milena Masullo, Alfredo Bottone, Javad Asili, Seyed Ahmad Emami, Sonia Piacente, Mehrdad Iranshahi
Two new sesquiterpene lactones, rhizantholide A (1) and rhizantholide B (2), together with five known compounds (3-7) have been isolated from the aerial parts of Centaurea rhizantha (Asteraceae). Sesquiterpene lactones belong to guaianolide class, and rhizantholide B is a rare guaianolide characterized by a free primary alcoholic function at C-10 along with a 3β,10β-epoxy function. Their structures have been established on the basis of 1D and 2D NMR experiments, as well as HR-ESIMS. The antimicrobial activity of compounds 1-7 has been evaluated against Gram-positive and Gram-negative strains...
June 18, 2018: Natural Product Research
F Ghaffarifar
DNA vaccines are considered as third-generation vaccines. The recombinant DNA technology plays an important role in the production of DNA vaccines. These vaccines are intended to increase DNA insertion and translation in the cell, activate CD4+ T cells, and enhance cytotoxic T-lymphocyte induction and antibody production. DNA vaccines are safe with few side effects in humans and animals. Their immunogenicity can be improved by the use of suitable adjuvants and proper delivery systems. In recent years, strategies have been developed to increase the efficacy of DNA vaccines through electroporation, as well as the use of cytokines, genetically engineered vectors, liposomes, and micro- or nanoparticles...
May 2018: Drugs of Today
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