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https://www.readbyqxmd.com/read/29924131/synthesis-and-molecular-modelling-studies-of-pyrimidinones-and-pyrrolo-3-4-d-pyrimidinodiones-as-new-antiplasmodial-compounds
#1
Kamilla Rodrigues Rogerio, Leonardo J M Carvalho, Luiza Helena Pinto Domingues, Bruno Junior Neves, José Teófilo Moreira Filho, Rosane Nora Castro, Cesare Bianco Júnior, Claudio Tadeu Daniel-Ribeiro, Carolina Horta Andrade, Cedric Stephan Graebin
BACKGROUND Malaria is responsible for 429,000 deaths per year worldwide, and more than 200 million cases were reported in 2015. Increasing parasite resistance has imposed restrictions to the currently available antimalarial drugs. Thus, the search for new, effective and safe antimalarial drugs is crucial. Heterocyclic compounds, such as dihydropyrimidinones (DHPM), synthesised via the Biginelli multicomponent reaction, as well as bicyclic compounds synthesised from DHPMs, have emerged as potential antimalarial candidates in the last few years...
2018: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/29923307/corilagin-inhibits-breast-cancer-growth-via-reactive-oxygen-species-dependent-apoptosis-and-autophagy
#2
Yinping Tong, Gongye Zhang, Yang Li, Jiajia Xu, Jiahui Yuan, Bing Zhang, Tianhui Hu, Gang Song
Corilagin is a component of Phyllanthus urinaria extract and has been found of possessing anti-inflammatory, anti-oxidative, and anti-tumour properties in clinic treatments. However, the underlying mechanisms in anti-cancer particularly of its induction of cell death in human breast cancer remain undefined. Our research found that corilagin-induced apoptotic and autophagic cell death depending on reactive oxygen species (ROS) in human breast cancer cell, and it occurred in human breast cancer cell (MCF-7) only comparing with normal cells...
June 19, 2018: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29917191/autophagy-regulates-chemoresistance-of-gastric-cancer-stem-cells-via-the-notch-signaling-pathway
#3
L-Q Li, D Pan, S-W Zhang, D -Y-Xie, X-L Zheng, H Chen
OBJECTIVE: Gastric cancer is the most common gastrointestinal malignancy and the leading cause of cancer-related deaths in East Asia. Increasing evidence has revealed that autophagy is closely associated with tumor initiation and progression. The present work aimed to investigate the role of autophagy in adjuvant chemotherapy for gastric cancer. MATERIALS AND METHODS: Gastric cancer stem cells (CSCs) were isolated from gastric cancer cell lines using the cell surface markers CD44 and CD54 and cultured in a three-dimensional cell culture system...
June 2018: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29909287/prazosin-induced-lysosomal-tubulation-interferes-with-cytokinesis-and-the-endocytic-sorting-of-the-tumour-antigen-cd98hc
#4
Robert Fuchs, Anika Stracke, Viktoria Holzmann, Gerfried Luschin-Ebengreuth, Nathalie Meier-Allard, Nadine Ebner, Teresa Maria Lassacher, Markus Absenger-Novak, Eleonore Fröhlich, Matthias Schittmayer, Sara Cano Crespo, Manuel Palacin, Beate Rinner, Ruth Birner-Gruenberger
The quinazoline based drug prazosin (PRZ) is a potent inducer of apoptosis in human cancer cells. We recently reported that PRZ enters cells via endocytosis and induces tubulation of the endolysosomal system. In a proteomics approach aimed at identifying potential membrane proteins with binding affinity to quinazolines, we detected the oncoprotein CD98hc. We confirmed shuttling of CD98hc towards lysosomes and upregulation of CD98hc expression in PRZ treated cells. Gene knockout (KO) experiments revealed that endocytosis of PRZ still occurs in the absence of CD98hc - suggesting that PRZ does not enter the cell via CD98hc but misroutes the protein towards tubular lysosomes...
June 14, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29902340/autophagy-inhibition-synergizes-with-calcium-mobilization-to-achieve-efficient-therapy-of-malignant-gliomas
#5
Ha Thi Vu, Masahiko Kobayashi, Ahmed M Hegazy, Yuko Tadokoro, Masaya Ueno, Atsuko Kasahara, Yusuke Takase, Naho Nomura, Hui Peng, Chiaki Ito, Yasushi Ino, Tomoki Todo, Mitsutoshi Nakada, Atsushi Hirao
Autophagy plays a critical role in tumorigenesis, but how autophagy contributes to cancer cells' responses to chemotherapeutics remains controversial. To investigate the roles of autophagy in malignant gliomas, we used CRISPR/CAS9 to knock out the ATG5 gene, which is essential for autophagosome formation, in tumor cells derived from glioblastoma patients. While ATG5 disruption inhibited autophagy, it did not change the phenotypes of glioma cells and did not alter their sensitivity to temozolomide, an agent used for glioblastoma patient therapy...
June 14, 2018: Cancer Science
https://www.readbyqxmd.com/read/29901280/role-of-toll-like-receptor-9-signaling-on-activation-of-nasal-polyp-derived-fibroblasts-and-its-association-with-nasal-polypogenesis
#6
Soo Kyoung Park, Soung Yong Jin, Sun Hee Yeon, Sung Bok Lee, Jun Xu, Young Hoon Yoon, Ki Sang Rha, Yong Min Kim
BACKGROUND: Nasal polyposis is characterized by persistent inflammation and remodeling in sinonasal mucosa. Toll-like receptor 9 (TLR9) is a DNA receptor of the innate immune system that plays a pivotal role in fibrosis and inflammatory responses. The aim of this study is to explore the expression, activity, and potential pathogenic role of TLR9 signaling in tissue remodeling in nasal polyp-derived fibroblasts (NPDFs). METHODS: Fibrotic and inflammatory responses elicited by type A CpG oligonucleotides were examined in the NPDFs by a combination of real-time quantitative polymerase chain reaction, Western blot analysis, enzyme-linked immunosorbent assay, and immunofluorescence staining...
June 14, 2018: International Forum of Allergy & Rhinology
https://www.readbyqxmd.com/read/29896171/autophagy-benefits-the-replication-of-egg-drop-syndrome-virus-in-duck-embryo-fibroblasts
#7
Xueping Wang, Xuefeng Qi, Bo Yang, Shuying Chen, Jingyu Wang
Egg drop syndrome virus (EDSV) is an economically important pathogen with a broad host range, and it causes disease that leads to markedly decreased egg production. Although EDSV is known to induce apoptosis in duck embryo fibroblasts (DEFs), the interaction between EDSV and its host needs to be further researched. Here, we provide the first evidence that EDSV infection triggers autophagy in DEFs through increases in autophagosome-like double-membrane vesicles, the conversion of LC3-I to LC3-II, and LC3 colocalization with viral hexon proteins...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29895768/antiplasmodial-properties-and-cytotoxicity-of-endophytic-fungi-from-symphonia-globulifera-clusiaceae
#8
Joël E T Ateba, Rufin M K Toghueo, Angelbert F Awantu, Brice M Mba'ning, Sebastian Gohlke, Dinkar Sahal, Edson Rodrigues-Filho, Etienne Tsamo, Fabrice F Boyom, Norbert Sewald, Bruno N Lenta
There is continuing need for new and improved drugs to tackle malaria, which remains a major public health problem, especially in tropical and subtropical regions of the world. Natural products represent credible sources of new antiplasmodial agents for antimalarial drug development. Endophytes that widely colonize healthy tissues of plants have been shown to synthesize a great variety of secondary metabolites that might possess antiplasmodial benefits. The present study was carried out to evaluate the antiplasmodial potential of extracts from endophytic fungi isolated from Symphonia globulifera against a chloroquine-resistant strain of Plasmodium falciparum (PfINDO )...
June 12, 2018: Journal of Fungi (Basel, Switzerland)
https://www.readbyqxmd.com/read/29890129/microrna-199a-b-5p-enhance-imatinib-efficacy-via-repressing-wnt2-signaling-mediated-protective-autophagy-in-imatinib-resistant-chronic-myeloid-leukemia-cells
#9
Peng-Hsu Chen, Ann-Jeng Liu, Kuo-Hao Ho, Ya-Ting Chiu, Zhe-Harn Anne Lin, Yi-Ting Lee, Chwen-Ming Shih, Ku-Chung Chen
Imatinib (IM) is a first-line therapeutic drug for chronic myeloid leukemia (CML), a hematological disease. Mutations in the BCR-ABL domain increase formation of IM resistance in CML. However, not all patients are BCR-ABL domain-mutant dependent. Investigating non-mutant mechanisms in the development of acquired IM resistance is a critical issue. We explored the mechanisms which influence IM efficacy and resistance in CML. Higher protective autophagy was identified in IM-resistant K562 (K562R) cells. Inhibition of autophagy by the inhibitors, chloroquine and 3-methyladenine, enhanced IM's efficacy in K562R cells...
June 8, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29889526/identification-characterization-and-optimization-of-2-8-disubstituted-1-5-naphthyridines-as-novel-plasmodium-falciparum-phosphatidylinositol-4-kinase-inhibitors-with-in-vivo-efficacy-in-a-humanized-mouse-model-of-malaria
#10
Nishanth Kandepedu, Diego Gonzalez Cabrera, Srinivas Eedubilli, Dale Taylor, Christel Brunschwig, Liezl Gibhard, Mathew Njoroge, Nina Lawrence, Tanya Paquet, Charles J Eyermann, Thomas Spangenberg, Gregory S Basarab, Leslie J Street, Kelly Chibale
A novel 2,8-disubstituted-1,5-naphthyridine hit compound stemming from the open access Medicines for Malaria Venture Pathogen Box, formed a basis for a hit-to-lead medicinal chemistry program. Structure-activity relationship investigations resulted in compounds with potent antiplasmodial activity against both chloroquine sensitive (NF54) and multi-drug resistant (K1) strains of the human malaria parasite Plasmodium falciparum. In the humanized P. falciparum mouse efficacy model, one of the frontrunner compounds showed in vivo efficacy at an oral dose of 4 × 50 mg...
June 11, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29889239/comparison-of-the-cumulative-efficacy-and-safety-of-chloroquine-artesunate-and-chloroquine-primaquine-in-plasmodium-vivax-malaria
#11
Cindy S Chu, Aung Pyae Phyo, Khin Maung Lwin, Htun Htun Win, Thida San, Aye Aye Aung, Rattanaporn Raksapraidee, Verena I Carrara, Germana Bancone, James Watson, Kerryn A Moore, Jacher Wiladphaingern, Stéphane Proux, Kanlaya Sriprawat, Markus Winterberg, Phaik Yeong Cheah, Amy L Chue, Joel Tarning, Mallika Imwong, François Nosten, Nicholas J White
Background: Chloroquine has been recommended for Plasmodium vivax infections for >60 years, but resistance is increasing. To guide future therapies, the cumulative benefits of using slowly eliminated (chloroquine) vs rapidly eliminated (artesunate) antimalarials, and the risks and benefits of adding radical cure (primaquine) were assessed in a 3-way randomized comparison conducted on the Thailand-Myanmar border. Methods: Patients with uncomplicated P. vivax malaria were given artesunate (2 mg/kg/day for 5 days), chloroquine (25 mg base/kg over 3 days), or chloroquine-primaquine (0...
June 8, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29887605/the-royal-college-of-ophthalmologists-recommendations-on-screening-for-hydroxychloroquine-and-chloroquine-users-in-the-united-kingdom-executive-summary
#12
REVIEW
Imran H Yusuf, Barny Foot, James Galloway, Michael R Ardern-Jones, Sarah-Lucie Watson, Cathy Yelf, Michael A Burdon, Paul N Bishop, Andrew J Lotery
No abstract text is available yet for this article.
June 11, 2018: Eye
https://www.readbyqxmd.com/read/29887512/access-to-new-highly-potent-antileukemia-antiviral-and-antimalarial-agents-via-hybridization-of-natural-products-homo-egonol-thymoquinone-and-artemisinin
#13
Aysun Çapcı Karagöz, Christoph Reiter, Ean-Jeong Seo, Lisa Gruber, Friedrich Hahn, Maria Leidenberger, Volker Klein, Frank Hampel, Oliver Friedrich, Manfred Marschall, Barbara Kappes, Thomas Efferth, Svetlana B Tsogoeva
Hybridization of natural products has high potential to further improve their activities and may produce synergistic effects between linked pharmacophores. Here we report synthesis of nine new hybrids of natural products egonol, homoegonol, thymoquinone and artemisinin and evaluation of their activities against P. falciparum 3D7 parasites, human cytomegalovirus, sensitive and multidrug-resistant human leukemia cells. Most of the new hybrids exceed their parent compounds in antimalarial, antiviral and antileukemia activities and in some cases show higher in vitro efficacy than clinically used reference drugs chloroquine, ganciclovir and doxorubicin...
May 24, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29885293/polyhexamethylene-biguanide-and-chloroquine-induce-programmed-cell-death-in-acanthamoeba-castellanii
#14
Eun-Kyung Moon, Hyun-Seo Choi, Hyun-Hee Kong, Fu-Shi Quan
Several chemotherapeutic drugs have been described as amoebicidal agents acting against Acanthamoeba trophozoites and cysts. However, the underlying mechanism of action is poorly characterized. Here, we describe programmed cell death (PCD) in A. castellanii induced by polyhexamethylene biguanide (PHMB) and chloroquine. We used four types of amoebicidal agents including 0.02% PHMB, 0.02% chlorhexidine digluconate, 100 μM chloroquine, and 100 μM 2,6-dichlorobenzonitrile to kill Acanthamoeba trophozoites and cysts...
June 6, 2018: Experimental Parasitology
https://www.readbyqxmd.com/read/29884802/chloroquine-and-amodiaquine-enhance-ampk-phosphorylation-and-improve-mitochondrial-fragmentation-in-diabetic-tubulopathy
#15
Hye Yun Jeong, Jun Mo Kang, Hak Hoon Jun, Dong-Jin Kim, Seon Hwa Park, Min Ji Sung, Jin Hyung Heo, Dong Ho Yang, Sang Ho Lee, So-Young Lee
We investigated the effects of chloroquine (CQ) and amodiaquine (AQ) on AMPK phosphorylation in renal tubular cells in a diabetic environment in vivo and in vitro. We also examined whether CQ- or AQ-mediated AMPK activity restoration attenuated diabetic tubulopathy by normalizing mitochondrial fragmentation. Human renal proximal epithelial cells (HKC8) were incubated in high-glucose conditions. Diabetes was induced with streptozotocin in male C57/BL6J mice. Treatment with CQ or AQ abolished high-glucose-induced phospho-AMPK and phosph-PGC1α down-regulation in HKC8 cells...
June 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29881426/phytochemical-analysis-and-in-vitro-bioactivity-of-scrophularia-umbrosa-rhizome-scrophulariaceae
#16
Elhameh Nikkhah, Fariba Heshmati Afshar, Hossein Babaei, Parina Asgharian, Abbas Delazar
Scrophularia umbrosa is a medicinal plant used as a traditional herb. This study was designed to investigate the phytochemical analysis of methanol (MeOH), DCM, and n-Hexane extracts of rhizome as well as total phenol and total flavonoid contents (TPC and TFC). In-vitro β-hematin formation assay and DPPH method were applied for analyzing antimalarial and free-radical scavenging activities of the extracts, respectively. The formation of hemozoin has been proposed as an ideal drug target for antimalarial screening programs...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29879220/therapeutic-potential-of-cpi-613-for-targeting-tumorous-mitochondrial-energy-metabolism-and-inhibiting-autophagy-in-clear-cell-sarcoma
#17
Yuki Egawa, Chiemi Saigo, Yusuke Kito, Toshiaki Moriki, Tamotsu Takeuchi
Clear cell sarcoma (CCS) is an aggressive type of soft tissue tumor that is associated with high rates of metastasis. In the present study, we found that CPI-613, which targets tumorous mitochondrial energy metabolism, induced autophagosome formation followed by lysosome fusion in HS-MM CCS cells in vitro. Interestingly, CPI-613 along with chloroquine, which inhibits the fusion of autophagosomes with lysosomes, significantly induced necrosis of HS-MM CCS cell growth in vitro. Subsequently, we established a murine orthotropic metastatic model of CCS and evaluated the putative suppressive effect of a combination of CPI-613 and chloroquine on CCS progression...
2018: PloS One
https://www.readbyqxmd.com/read/29877619/hemozoin-induced-activation-of-human-monocytes-toward-m2-like-phenotype-is-partially-reversed-by-antimalarial-drugs-chloroquine-and-artemisinin
#18
Deepali Bobade, Ashwin V Khandare, Mangesh Deval, Padma Shastry, Prakash Deshpande
Plasmodium falciparum malaria is the most severe form of malaria with several complications. The malaria pigment-hemozoin (Hz) is associated with severe anemia, cytokine dysfunction, and immunosuppression, thus making it an interesting target for developing new strategies for antimalarial therapy. Monocytes (MO) in circulation actively ingest Hz released by Plasmodium parasites and secrete pro- and anti-inflammatory cytokines. M1 and M2 types represent the two major forms of MO/macrophages (MQ) with distinct phenotypes and opposing functions...
June 7, 2018: MicrobiologyOpen
https://www.readbyqxmd.com/read/29874341/inhibitory-effect-of-chloroquine-derivatives-on-presenilin-1-and-ubiquilin-1-expression-in-alzheimer-s-disease-retraction
#19
(no author information available yet)
[This retracts the article on p. 7640 in vol. 8, PMID: 26261684.].
2018: International Journal of Clinical and Experimental Pathology
https://www.readbyqxmd.com/read/29873617/responses-of-thalamic-neurons-to-itch-and-pain-producing-stimuli-in-rats
#20
Brett Lipshetz, Sergey G Khasabov, Hai Truong, Theoden I Netoff, Donald A Simone, Glenn J Giesler
Understanding of processing and transmission of information related to itch and pain in the thalamus are incomplete. In fact, no single unit studies of pruriceptive transmission in the thalamus have yet appeared. In urethane-anesthetized rats, we examined responses of 66 thalamic neurons to itch- and pain- inducing stimuli including chloroquine, serotonin, b-alanine, histamine, and capsaicin. Eighty percent of all cells were activated by intradermal injections of one or more pruritogens. Forty percent of tested neurons responded to injection of three, four or even five agents...
June 6, 2018: Journal of Neurophysiology
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