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chloroquine resistance

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https://www.readbyqxmd.com/read/29351800/drug-resistance-genes-pvcrt-o-and-pvmdr-1-polymorphism-in-patients-from-malaria-endemic-south-western-coastal-region-of-india
#1
Shiny Joy, Benudhar Mukhi, Susanta K Ghosh, Rajeshwara N Achur, D Channe Gowda, Namita Surolia
BACKGROUND: Malaria is highly prevalent in many parts of India and is mostly caused by the parasite species Plasmodium vivax followed by Plasmodium falciparum. Chloroquine (CQ) is the first-line treatment for blood stage P. vivax parasites, but cases of drug resistance to CQ have been reported from India. One of the surveillance strategies which is used to monitor CQ drug resistance, is the analysis of single nucleotide polymorphisms (SNPs) of the associated gene markers. Susceptibility to CQ can also be determined by copy number assessment of multidrug resistant gene (mdr-1)...
January 19, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29330980/comparison-of-efficacy-of-chloroquine-and-artemether-lumafantrine-in-treating-vivax-malaria-in-thall-and-surrounding-area
#2
Syed Mohammad Abrar, Syed Sajid Ali Shah, Raja Jibran Akbar, Sheema Rahim, Faizan Malik, Fakhar Uzzaman Khan
BACKGROUND: Fever is the main complaint in patients reporting to our hospital and the most common cause of fever in our set up is malaria. The aim of this study was to know about the clinical response, efficacy and resistance of vivax malaria to chloroquine in patients reporting to Thall Scouts Hospital. METHODS: All the adult male patients reporting to Thall Scouts Hospital with fever and other symptoms of malaria having slide positive vivax malaria were included in the study...
October 2017: Journal of Ayub Medical College, Abbottabad: JAMC
https://www.readbyqxmd.com/read/29326018/semisynthesis-cytotoxicity-antimalarial-evaluation-and-structure-activity-relationship-of-two-series-of-triterpene-derivatives
#3
Simone Tasca Cargnin, Andressa Finkler Staudt, Patrícia Medeiros, Daniel de Medeiros Sol Sol, Ana Paula de Azevedo Dos Santos, Fernando Berton Zanchi, Grace Gosmann, Antonio Puyet, Carolina Bioni Garcia Teles, Simone Baggio Gnoatto
In this report, we describe the semisynthesis of two series of ursolic and betulinic acid derivatives through designed by modifications at the C-3 and C-28 positions and demonstrate their antimalarial activity against chloroquine-resistant P. falciparum (W2 strain). Structural modifications at C-3 were more advantageous to antimalarial activity than simultaneous modifications at C-3 and C-28 positions. The ester derivative, 3β-butanoyl betulinic acid (7b), was the most active compound (IC50 = 3.4 µM) and it did not exhibit cytotoxicity against VERO nor HepG2 cells (CC50 > 400 µM), showing selectivity towards parasites (selectivity index > 117...
December 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29324340/antimalarial-naphthoquinones-synthesis-via-click-chemistry-in%C3%A2-vitro-activity-docking-to-pfdhodh-and-sar-of-lapachol-based-compounds
#4
Geraldo Célio Brandão, Franciele C Rocha Missias, Lucas Miquéias Arantes, Luciana Ferreira Soares, Kuldeep K Roy, Robert J Doerksen, Alaide Braga de Oliveira, Guilherme Rocha Pereira
Lapachol is an abundant prenyl naphthoquinone occurring in Brazilian Bignoniaceae that was clinically used, in former times, as an antimalarial drug, despite its moderate effect. Aiming to search for potentially better antimalarials, a series of 1,2,3-triazole derivatives was synthesized by chemical modification of lapachol. Alkylation of the hydroxyl group gave its propargyl ether which, via copper-catalyzed cycloaddition (CuAAC) click chemistry with different organic azides, afforded 17 naphthoquinonolyl triazole derivatives...
December 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29320822/antimalarial-activity-of-c-10-substituted-triazolyl-artemisinin
#5
Gab-Man Park, Hyun Park, Sangtae Oh, Seokjoon Lee
We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate...
December 2017: Korean Journal of Parasitology
https://www.readbyqxmd.com/read/29317166/synthesis-in-vitro-antimalarial-activities-and-cytotoxicities-of-amino-artemisinin-ferrocene-derivatives
#6
Christo de Lange, Dina Coertzen, Frans J Smit, Johannes F Wentzel, Ho Ning Wong, Lyn-Marie Birkholtz, Richard K Haynes, David D N'Da
Novel derivatives bearing a ferrocene attached via a piperazine linker to C-10 of the artemisinin nucleus were prepared from dihydroartemisinin and screened against chloroquine (CQ) sensitive NF54 and CQ resistant K1 and W2 strains of Plasmodium falciparum (Pf) parasites. The overall aim is to imprint oxidant (from the artemisinin) and redox (from the ferrocene) activities. In a preliminary assessment, these compounds were shown to possess activities in the low nM range with the most active being compound 6 with IC50 values of 2...
December 26, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29311064/high-content-screening-of-mmv-pathogen-box-for-plasmodium-falciparum-digestive-vacuole-disrupting-molecules-reveals-valuable-starting-points-for-drug-discovery
#7
Jie Xin Tong, Rajesh Chandramohanadas, Kevin Shyong-Wei Tan
Plasmodium falciparum infections leading to malaria have severe clinical manifestations and high mortality rates. Chloroquine (CQ), a former mainstay of malaria chemotherapy, has been rendered ineffective due to the emergence of wide-spread resistance. Recent studies, however, have unveiled a novel mode of action in which low micromolar levels of CQ permeabilized the parasite's digestive vacuole (DV) membrane, leading to calcium efflux, mitochondrial depolarization and DNA degradation. These phenotypes implicate the DV as an alternative target of CQ and suggests that DV disruption is an attractive target for exploitation through the screening for DV-disruptive antimalarials...
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29289595/monitoring-autophagic-flux-using-p62-sqstm1-based-luciferase-reporters-in-glioma-cells
#8
Zhang Min, Yao Ting, Gong Mingtao, Tang Xiaofei, Yan Dong, Zhang Chenguang, Ding Wei
Autophagy is a highly dynamic process characterized with the term of autophagic flux. In the present study, we developed a quantifiable luciferase reporter system to measure the capacity as well as the dynamics of autophagic flux. Briefly, a luciferase variant of Luc2p was fused with p62/SQSTM1 or its UBA domain deletion mutant (p62ΔU) and transfected into cells. The expressed Luc2p-p62 fusion protein was primarily degraded via autophagy, while Luc2p-p62ΔU was employed as a normalization control due to its resistance to autophagic degradation...
December 28, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/29285270/metformin-alleviates-nickel-induced-autophagy-and-apoptosis-via-inhibition-of-hexokinase-2-activating-lipocalin-2-in-human-bronchial-epithelial-cells
#9
Yu-Ting Kang, Wen-Cheng Hsu, Chih-Hsien Wu, I-Lun Hsin, Pei-Ru Wu, Kun-Tu Yeh, Jiunn-Liang Ko
Autophagy is an intracellular recycling and degradation process for regulating tumor progression, survival and drug resistance. Nickel compounds have been identified as human carcinogens. However, the role of nickel-induced autophagy in lung carcinogenesis has not yet been fully elucidated. In this study, we determined that hexokinase 2 (HK2), which phosphorylates glucose and regulates autophagy, is the key mediator in nickel-induced autophagy in lung bronchial epithelial cells. We attempted to investigate the effects of the antidiabetic drug metformin on HK2 expression and lung cancer chemoprevention...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29276062/targeting-urothelial-carcinoma-cells-by-combining-cisplatin-with-a-specific-inhibitor-of-the-autophagy-inducing-class-iii-ptdins3k-complex
#10
David Schlütermann, Margaretha A Skowron, Niklas Berleth, Philip Böhler, Jana Deitersen, Fabian Stuhldreier, Nora Wallot-Hieke, Wenxian Wu, Christoph Peter, Michèle J Hoffmann, Günter Niegisch, Björn Stork
BACKGROUND: Cisplatin-based regimens are routinely employed for the treatment of urothelial carcinoma. However, therapeutic success is hampered by the primary presence of or the development of cisplatin resistance. This chemoresistance is executed by multiple cellular pathways. In recent years, the cellular process of autophagy has been identified as a prosurvival pathway of cancer cells. On the one hand, autophagy enables cancer cells to survive conditions of low oxygen or nutrient supply, frequently found in tumors...
December 21, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/29258566/5-fu-resistant-emt-like-pancreatic-cancer-cells-are-hypersensitive-to-photochemical-internalization-of-the-novel-endoglin-targeting-immunotoxin-cd105-saporin
#11
Kaja Lund, Cathrine Elisabeth Olsen, Judith Jing Wen Wong, Petter Angell Olsen, Nina Therese Solberg, Anders Høgset, Stefan Krauss, Pål Kristian Selbo
BACKGROUND: Development of resistance to 5-fluorouracil (5-FU) is a major problem in treatment of various cancers including pancreatic cancer. In this study, we reveal important resistance mechanisms and photochemical strategies to overcome 5-FU resistance in pancreatic adenocarcinoma. METHODS: 5-FU resistant (5-FUR), epithelial-to-mesenchymal-like sub-clones of the wild type pancreatic cancer cell line Panc03.27 were previously generated in our lab. We investigated the cytotoxic effect of the endosomal/lysosomal-localizing photosensitizer TPCS2a (fimaporfin) combined with light (photochemical treatment, PCT) using MTS viability assay, and used fluorescence microscopy to show localization of TPCS2a and to investigate the effect of photodamage of lysosomes...
December 19, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/29236492/pimentelamines-a-c-indole-alkaloids-isolated-from-the-leaves-of-the-australian-tree-flindersia-pimenteliana
#12
Luke P Robertson, Sandra Duffy, Yun Wang, Dongdong Wang, Vicky M Avery, Anthony R Carroll
Three members of a new class of ascorbic acid-adduct indole alkaloids (1-3), a new prenylated indole alkaloid (4), and five known compounds (5-9) were isolated from the leaves of Flindersia pimenteliana. The structures of 1-4 were elucidated on the basis of their (+)-HRESIMS and 2D NMR spectroscopic data. Antiplasmodial activity was also reported for the natural products against chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum with IC50 values ranging from 0.19 to 3.6 μM.
December 13, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/29227011/synthesis-of-novel-benzimidazole-acrylonitriles-for-inhibition-of-plasmodium-falciparum-growth-by-dual-target-inhibition
#13
Kalicharan Sharma, Apeksha Shrivastava, Ram N Mehra, Girdhar S Deora, Mohammad M Alam, Mohammad S Zaman, Mymoona Akhter
Antimalarial drug resistance has emerged as a threat for treating malaria, generating a need to design and develop newer, more efficient antimalarial agents. This research aimed to identify novel leads as antimalarials. Dual receptor mechanism could be a good strategy to combat developing drug resistance. A series of benzimidazole acrylonitriles containing 18 compounds were designed, synthesized and evaluated for cytotoxicity, heme binding, ferriprotoporphyrin IX biomineralisation inhibition, and falcipain-2 enzyme assay...
December 11, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29225629/synthesis-sar-and-docking-studies-disclose-2-arylfuran-1-4-naphthoquinones-as-in-vitro-antiplasmodial-hits
#14
Tatiane Freitas Borgati, Maria Fernanda Alves do Nascimento, Juma Fortunato Bernardino, Lunamaura Claudia Oliveira Martins, Alex Gutterres Taranto, Alaíde Braga de Oliveira
A total of 28 lapachol-related naphthoquinones with four different scaffolds were synthesized and spectroscopically characterized. In vitro antiplasmodial activity was assayed against the chloroquine-resistant Plasmodium falciparum W2 strain by the parasite lactate dehydrogenase (pLDH) method. Cytotoxicity against Hep G2A16 cell was determined by the MTT assay. All compounds disclosed higher in vitro antiplasmodial activity than lapachol. Ortho- and para-naphthoquinones with a furan ring fused to the quinonoid moiety were more potent than 2-hydroxy-3-(1'-alkenyl)-1,4-naphthoquinones, while ortho-furanonaphthoquinones were more cytotoxic...
2017: Journal of Tropical Medicine
https://www.readbyqxmd.com/read/29223887/a-minimalistic-approach-to-develop-new-anti-apicomplexa-polyamines-analogs
#15
Esteban A Panozzo-Zénere, Exequiel O J Porta, Gustavo Arrizabalaga, Lucía Fargnoli, Shabana I Khan, Babu L Tekwani, Guillermo R Labadie
The development of new chemical entities against the major diseases caused by parasites is highly desired. A library of thirty diamines analogs following a minimalist approach and supported by chemoinformatics tools have been prepared and evaluated against apicomplexan parasites. Different member of the series of N,N'-disubstituted aliphatic diamines shown in vitro activities at submicromolar concentrations and high levels of selectivity against Toxoplasma gondii and in chloroquine-sensitive and resistant-strains of Plasmodium falciparum...
December 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29207624/autophagy-suppression-potentiates-the-anti-glioblastoma-effect-of-asparaginase-in-vitro-and-in-vivo
#16
Qicheng Chen, Li Ye, Jiajun Fan, Xuyao Zhang, Huan Wang, Siyang Liao, Ping Song, Ziyu Wang, Shaofei Wang, Yubin Li, Jingyun Luan, Yichen Wang, Wei Chen, Wenjing Zai, Ping Yang, Zhonglian Cao, Dianwen Ju
Asparaginase has been reported to be effective in the treatment of various leukemia and several malignant solid cancers. However, the anti-tumor effect of asparaginase is always restricted due to complicated mechanisms. Herein, we investigated the mechanisms of how glioblastoma resisted asparaginase treatment and reported a novel approach to enhance the anti-glioblastoma effect of asparaginase. We found that asparaginase could induce growth inhibition and caspase-dependent apoptosis in U87MG/U251MG glioblastoma cells...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29207150/inhibition-of-autophagy-enhances-the-targeted-therapeutic-effect-of-sorafenib-in-thyroid-cancer
#17
Heqing Yi, Ting Ye, Minghua Ge, Mengdi Yang, Lijun Zhang, Shui Jin, Xuemei Ye, Bin Long, Linfa Li
The multi-target kinase inhibitor sorafenib has been approved for the treatment of patients with advanced differentiated thyroid cancer. However, different sensitivities to sorafenib have been observed, and few patients have benefited from sorafenib treatment in the long term. In the event of acquired resistance to sorafenib it is not beneficial to continue treatment in most patients. Autophagy can be induced in a variety of cancer treatments and plays an important role in cancer treatment. The role of autophagy in sorafenib treatment of thyroid cancer has not been fully demonstrated...
November 28, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29201083/evaluation-of-novel-%C3%AE-acyloxy-%C3%AE-quinolin-4-yl-acetamides-as-antiplasmodial-agents
#18
Ali Ramazani, Behnam Khosravani, Jafar Taran, Ali Ramazani
Because of expanding resistance to efficient and affordable antimalarial drugs like chloroquine, the search is continuing for more effective drugs against this disease. In-vitro antiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides on Plasmodiumfalciparum and structure-activity relationships of this new class of Passerini adducts is described. The in-vitro antiplasmodial activity of compounds was tested against chloroquine sensitive 3D7 strain. Toxicity of active compounds was investigated on HepG2 cell line...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29201061/selective-and-irreversible-induction-of-necroptotic-cell-death-in-lung-tumorspheres-by-short-term-exposure-to-verapamil-in-combination-with-sorafenib
#19
Juan Sebastian Yakisich, Yogesh Kulkarni, Neelam Azad, Anand Krishnan V Iyer
The presence of highly resistant cancer cells and the toxicity to normal cells are key factors that limit chemotherapy. Here, we used two models of highly resistant lung cancer cells: (1) adherent cells growing under prolonged periods of serum starvation (PPSS) and (2) cells growing as floating tumorspheres (FTs) to evaluate the effect of Verapamil (VP) in combination with Sorafenib (SF). Compared to cells growing under routine culture conditions (RCCs), PPPS cells or FTs were highly sensitive to short-term exposure (24 h) to VP 100 μM + SF 5 μM (VP100 + SF5)...
2017: Stem Cells International
https://www.readbyqxmd.com/read/29200731/brazilian-cerrado-qualea-grandiflora-mart-leaves-exhibit-antiplasmodial-and-trypanocidal-activities-in-vitro
#20
Thuany de Moura Cordeiro, Fabian Borghetti, Sarah C Caldas Oliveira, Izabela Marques Dourado Bastos, Jaime Martins de Santana, Philippe Grellier, Sébastien Charneau
Background: The rapid spread of drug-resistant strains of protozoan parasites required the urgent need for new effective drugs. Natural products offer a variety of chemical structures, which make them a valuable source of lead compounds for the development of such new drugs. Cerrado is the second largest biome in Brazil and has the richest flora of all the world savannahs. We selected Qualea grandiflora, a plant species known for its proprieties in folk medicine and its antibacterial activity...
October 2017: Pharmacognosy Magazine
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