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chloroquine resistance

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https://www.readbyqxmd.com/read/29128848/antimalarial-activity-of-malaria-box-compounds-against-plasmodium-falciparum-clinical-isolates
#1
Jersley D Chirawurah, Felix Ansah, Prince B Nyarko, Samuel Duodu, Yaw Aniweh, Gordon A Awandare
Malaria remains a major cause of childhood deaths in resource-limited settings. In the absence of an effective vaccine, drugs and other interventions have played very significant roles in combating the scourge of malaria. The recent reports of resistance to artemisinin necessitate the need for new antimalarial drugs with novel mechanisms of action. Towards the development of new, affordable and easily accessible antimalarial drugs for endemic regions, the Medicines for Malaria Venture (MMV) assembled a total of 400 active antimalarial compounds called the Malaria Box...
October 16, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29127189/autophagy-promotes-escape-from-phosphatidylinositol-3-kinase-inhibition-in-estrogen-receptor-positive-breast-cancer
#2
Wei Yang, Sarah R Hosford, Nicole A Traphagen, Kevin Shee, Eugene Demidenko, Stephanie Liu, Todd W Miller
Hyperactivation of the PI3K pathway has been implicated in resistance to antiestrogen therapies in estrogen receptor α (ER)-positive breast cancer, prompting the development of therapeutic strategies to inhibit this pathway. Autophagy has tumor-promoting and -suppressing roles and has been broadly implicated in resistance to anticancer therapies, including antiestrogens. Chloroquine (CQ) is an antimalarial and amebicidal drug that inhibits autophagy in mammalian cells and human tumors. Herein, we observed that CQ inhibited proliferation and autophagy in ER(+) breast cancer cells...
November 10, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29125042/molecular-surveillance-of-chloroquine-drug-resistance-markers-pfcrt-and-pfmdr1-among-imported-plasmodium-falciparum-malaria-in-qatar
#3
Anushree Acharya, Devendra Bansal, Praveen K Bharti, Fahmi Y Khan, Salem Abusalah, Ashraf Elmalik, Mohammed ElKhalifa, Pradyumna K Mohapatra, Jagadish Mahanta, Rakesh Sehgal, Neeru Singh, Ali A Sultan
Imported malaria has been a great challenge for public health in Qatar due to influx of large number of migrant workers. Antimalarial drug resistance has emerged as one of the greatest challenges facing malaria control today. Monitoring parasite haplotypes that predict susceptibility to major antimalarial can guide treatment policies. This study aimed to determine molecular drug resistance pattern in imported malaria cases in Qatar. Blood samples from the uncomplicated P. falciparum malaria patients were collected at Hamad General Hospital, HMC, Doha, Qatar...
November 10, 2017: Pathogens and Global Health
https://www.readbyqxmd.com/read/29121061/a-randomized-double-blind-active-control-trial-to-evaluate-the-efficacy-and-safety-of-a-three-day-course-of-tafenoquine-monotherapy-for-the-treatment-of-plasmodium-vivax-malaria
#4
Mark M Fukuda, Srivicha Krudsood, Khadeeja Mohamed, Justin A Green, Sukhuma Warrasak, Harald Noedl, Ataya Euswas, Mali Ittiverakul, Nillawan Buathong, Sabaithip Sriwichai, R Scott Miller, Colin Ohrt
BACKGROUND: Tafenoquine is an investigational 8-aminoquinoline for the prevention of Plasmodium vivax relapse. Tafenoquine has a long half-life and the potential for more convenient dosing, compared with the currently recommended 14-day primaquine regimen. METHODS: This randomized, active-control, double-blind trial was conducted in Bangkok, Thailand. Seventy patients with microscopically confirmed P. vivax were randomized (2:1) to tafenoquine 400 mg once daily for 3 days or 2500 mg total dose chloroquine phosphate (1500 mg chloroquine base) given over 3 days plus primaquine 15 mg daily for 14 days...
2017: PloS One
https://www.readbyqxmd.com/read/29111368/discovery-of-new-antimalarial-agents-second-generation-dual-inhibitors-against-fp-2-and-pfdhfr-via-fragments-assembely
#5
Wenhua Chen, Zhenghui Huang, Wanyan Wang, Fei Mao, Longfei Guan, Yun Tang, Hualiang Jiang, Jian Li, Jin Huang, Lubin Jiang, Jin Zhu
Malaria parasites are a leading cause of worldwide mortality from infectious disease. Cysteine protease falcipain-2 (FP-2) and Plasmodium falciparum dihydrofolate reductase (PfDHFR) play vital roles, which are absolutely essential, in the parasite life cycle. In this study, based on the structures of uniform fragments of reported PfDHFR inhibitors and the first-generation dual inhibitors against FP-2 and PfDHFR, we identified a novel series of dual inhibitors through fragments assembly. Lead optimization led to the discovery of 24, which showed high potency against FP-2 (IC50 = 10...
October 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29110722/molecular-markers-for-artemisinin-and-partner-drug-resistance-in-natural-plasmodium-falciparum-populations-following-increased-insecticide-treated-net-coverage-along-the-slope-of-mount-cameroon-cross-sectional-study
#6
Tobias O Apinjoh, Regina N Mugri, Olivo Miotto, Hanesh F Chi, Rolland B Tata, Judith K Anchang-Kimbi, Eleanor M Fon, Delphine A Tangoh, Robert V Nyingchu, Christopher Jacob, Roberto Amato, Abdoulaye Djimde, Dominic Kwiatkowski, Eric A Achidi, Alfred Amambua-Ngwa
BACKGROUND: Drug resistance is one of the greatest challenges of malaria control programmes, with the monitoring of parasite resistance to artemisinins or to Artemisinin Combination Therapy (ACT) partner drugs critical to elimination efforts. Markers of resistance to a wide panel of antimalarials were assessed in natural parasite populations from southwestern Cameroon. METHODS: Individuals with asymptomatic parasitaemia or uncomplicated malaria were enrolled through cross-sectional surveys from May 2013 to March 2014 along the slope of mount Cameroon...
November 6, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/29099265/analysis-of-defective-protein-ubiquitylation-associated-to-adriamycin-resistant-cells
#7
Valérie Lang, Fabienne Aillet, Wendy Xolalpa, Sonia Serna, Laurie Ceccato, Rosa G Lopez-Reyes, Maria Paz Lopez-Mato, Radosław Januchowski, Niels-Christian Reichardt, Manuel S Rodriguez
DNA damage activated by Adriamycin (ADR) promotes ubiquitin-proteasome system-mediated proteolysis by stimulating both the activity of ubiquitylating enzymes and the proteasome. In ADR-resistant breast cancer MCF7 (MCF7(ADR)) cells, protein ubiquitylation is significantly reduced compared to the parental MCF7 cells. Here, we used tandem ubiquitin-binding entities (TUBEs) to analyze the ubiquitylation pattern observed in MCF7 or MCF7(ADR) cells. While in MCF7, the level of total ubiquitylation increased up to six-fold in response to ADR, in MCF7(ADR) cells only a two-fold response was found...
November 3, 2017: Cell Cycle
https://www.readbyqxmd.com/read/29097636/antiplasmodial-efficacy-of-calotropis-gigantea-l-against-plasmodium-falciparum-3d7-strain-and-plasmodium-berghei-anka
#8
P V V Satish, D Santha Kumari, K Sunita
BACKGROUND & OBJECTIVES: Malaria is a deadly parasitic disease, having a high rate of incidence and mortality across the world. The spread and development of resistance against chemical insecticides is one of the major problems associated with malaria treatment and control. Hence, plant based formulations may serve as an alternative source towards development of new drugs for treatment of malaria. The present study was aimed to evaluate the in vitro antiplasmodial activities of leaf, stem and flower of Calotropis gigantea against chloroquine-sensitive Plasmodium falciparum (3D7 strain) and its cytotoxicity against THP-1 cell lines...
July 2017: Journal of Vector Borne Diseases
https://www.readbyqxmd.com/read/29096443/characteristics-of-artemether-loaded-poly-lactic-co-glycolic-acid-microparticles-fabricated-by-coaxial-electrospray-validation-of-enhanced-encapsulation-efficiency-and-bioavailability
#9
Farhana Akbar Mangrio, Pankaj Dwivedi, Shuya Han, Gang Zhao, Dayong Gao, Ting Si, Ronald X Xu
Artemether is one of the most effective drugs for the treatment of chloroquine-resistant and Plasmodium falciparum strains of malaria. However, its therapeutic potency is hindered by its poor bioavailability. To overcome this limitation, we have encapsulated artemether in poly(lactic-co-glycolic) acid (PLGA) core-shell microparticles (MPs) using the coaxial electrospray method. With optimized process parameters including liquid flow rates and applied electric voltages, experiments are systematically carried out to generate a stable cone-jet mode to produce artemether-loaded PLGA-MPs with an average size of 2 μm, an encapsulation efficiency of 78 ± 5...
November 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29066501/knockdown-of-brca2-enhances-cisplatin-and-cisplatin-induced-autophagy-in-ovarian-cancer-cells
#10
B Wan, L Dai, L Wang, Y Zhang, H Huang, G Qian, T Yu
Clinical implications of the BRCA2 expression level on treatments of ovarian cancer are controversial. Here we demonstrated that platinum-resistant cancer had a higher percentage of high BRCA2 level (87.5% vs. 43.6%, p = 0.001), and that patients with a low BRCA2 level in cancer tissues had longer progression-free survival (with a median time of 28.0 vs. 12.0 mon, p < 0.001) and platinum-free duration (with a median time of 19.0 vs. 5.0 mon, p < 0.001) compared with those with a high BRCA2 level. In human ovarian cancer cell lines CAOV-3 and ES-2, cisplatin induced an up-regulation of the RAD51 protein, which was inhibited after silencing BRCA2; silencing BRCA2 enhanced the action of cisplatin in vitro and in vivo...
October 24, 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/29057679/optimisation-of-chloroquine-phosphate-loaded-nanostructured-lipid-carriers-using-box-behnken-design-and-its-antimalarial-efficacy
#11
Uday Krishna Baruah, Kuppusamy Gowthamarajan, Vanka Ravisankar, Veera Venkata Satyanarayana Reddy Karri, Praveen Kumar Simhadri, Vineeta Singh
Chloroquine was once the most widely used antimalarial for nearly eight decades for its safety, efficiency, stability, low cost and finally for its less toxic nature. But its use and efficacy got slowly decreased with the increase of chloroquine resistant strains of Plasmodium species throughout the world. Lipid based nanodrug delivery systems have been very popular in the recent times as they are very less toxic, have drug targeting capabilities and also reduces the dosing frequency by increasing efficacy of the drug...
October 23, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29050671/gambogic-acid-improves-non-small-cell-lung-cancer-progression-by-inhibition-of-mtor-signaling-pathway
#12
Teng Zhao, Hong-Jian Wang, Wen-Wen Zhao, Yi-Ling Sun, Li-Kuan Hu
Gambogic acid (GA) has been shown to inhibit cancer cell proliferation, induce apoptosis, and enhance reactive oxygen species accumulation. However, whether GA could improve multidrug resistance through modulating autophagy has never been explored. We demonstrated that the combination of GA and cisplatin (CDDP) resulted in a stronger growth inhibition effect on A549 and NCI-H460 cells using the MTT assay. Furthermore, treatment with GA significantly increased autophagy in these cells. More importantly, GA-induced cell death could be largely abolished by 3-methyladenine (3-MA) or chloroquine (CQ) treatment, suggesting that GA-induced cell death was dependent on autophagy...
November 2017: Kaohsiung Journal of Medical Sciences
https://www.readbyqxmd.com/read/29035245/in-vivo-and-in-vitro-models-for-scanning-drug-substances-in-malaria-prestudy
#13
Ahmet Özbilgin, İbrahim Çavuş, Alicem Nuraydın, Tuğba Kaya
OBJECTIVE: The Wolrd Health Organization (WHO) encourages all countries to investigate antimalarial drug substances derived from herbal sources with the slogan "Hunt of the Next Artemisinin" due to the emergence of resistant strains of Plasmodium species to artemisinin. In the broad and simple sense, it was planned to help guide the young researchers set in-vitro and in-vivo models of malaria in order to be used in drug research and active ingredient studies. METHODS: In-vitro study, young Plasmodium berghei trophozoites were removed from the liquid nitrogen tank and resuspended in appropriate conditions, followed by incubation with chloroquine and tetracycline at concentrations of 0...
September 2017: Türkiye Parazitolojii Dergisi
https://www.readbyqxmd.com/read/29018598/the-plasmodium-berghei-rc-strain-is-highly-diverged-and-harbors-putatively-novel-drug-resistance-variants
#14
Warangkhana Songsungthong, Supasak Kulawonganunchai, Alisa Wilantho, Sissades Tongsima, Pongpisid Koonyosying, Chairat Uthaipibull, Sumalee Kamchonwongpaisan, Philip J Shaw
BACKGROUND: The current first line drugs for treating uncomplicated malaria are artemisinin (ART) combination therapies. However, Plasmodium falciparum parasites resistant to ART and partner drugs are spreading, which threatens malaria control efforts. Rodent malaria species are useful models for understanding antimalarial resistance, in particular genetic variants responsible for cross resistance to different compounds. METHODS: The Plasmodium berghei RC strain (PbRC) is described as resistant to different antimalarials, including chloroquine (CQ) and ART...
2017: PeerJ
https://www.readbyqxmd.com/read/29016333/distribution-of-mutations-associated-with-antifolate-and-chloroquine-resistance-among-imported-plasmodium-vivax-in-the-state-of-qatar
#15
Devendra Bansal, Anushree Acharya, Praveen K Bharti, Mohamed H Abdelraheem, Ashraf Elmalik, Salem Abosalah, Fahmi Y Khan, Mohamed ElKhalifa, Hargobinder Kaur, Pradyumna K Mohapatra, Rakesh Sehgal, Mohammed A Idris, Jagadish Mahanta, Neeru Singh, Hamza A Babiker, Ali A Sultan
Plasmodium vivax is the most prevalent parasite worldwide, escalating by spread of drug resistance. Currently, in Qatar, chloroquine (CQ) plus primaquine are recommended for the treatment of P. vivax malaria. The present study examined the prevalence of mutations in dihydrofolate reductase (dhfr), dihydropteroate synthase (dhps) genes and CQ resistance transporter (crt-o) genes, associated with sulphadoxine-pyrimethamine (SP) and chloroquine resistance, among imported P. vivax cases in Qatar. Blood samples were collected from patients positive for P...
October 2, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28988153/synthesis-and-antimalarial-evaluation-of-artesunate-polyamine-and-trioxolane-polyamine-conjugates
#16
A Norrie Pearce, Marcel Kaiser, Brent R Copp
A series of artesunate-polyamine and trioxolane-polyamine conjugates have been prepared. The conjugates were evaluated for antimalarial activity towards the K1 dual drug resistant and NF54 chloroquine-sensitive strains of Plasmodium falciparum (Pf) and for cytotoxicity towards the rat myoblast cell line L6. (Bis)-Boc-(bis)-artesunate-polyamine and (tetra)-artesunate-polyamine conjugates exhibited potent in vitro activity towards both strains of Pf, with IC50 values in the range of 0.3-1.1 nM, comparable to the parent artesunate...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28981387/aldh1a1-and-hltf-modulate-the-activity-of-lysosomal-autophagy-inhibitors-in-cancer-cells
#17
Shengfu Piao, Rani Ojha, Vito W Rebecca, Arabinda Samanta, Xiao-Hong Ma, Quentin Mcafee, Michael C Nicastri, Meghan Buckley, Eric Brown, Jeffrey D Winkler, Phyllis A Gimotty, Ravi K Amaravadi
Lysosomal autophagy inhibitors (LAI) such as hydroxychloroquine (HCQ) have significant activity in a subset of cancer cell lines. LAIs are being evaluated in cancer clinical trials, but genetic determinants of sensitivity to LAIs are unknown, making it difficult to predict which tumors would be most susceptible. Here we characterize differentially expressed genes in HCQ-sensitive (-S) and -resistant (-R) cancer cells. Notably, expression of canonical macroautophagy/autophagy genes was not associated with sensitivity to HCQ...
October 5, 2017: Autophagy
https://www.readbyqxmd.com/read/28981103/a-novel-acridine-derivative-ls-1-10-inhibits-autophagic-degradation-and-triggers-apoptosis-in-colon-cancer-cells
#18
Wan Fu, Xue Li, Xiaopeng Lu, Luyao Zhang, Ran Li, Nan Zhang, Shan Liu, Xin Yang, Yue Wang, Ying Zhao, Xiangbao Meng, Wei-Guo Zhu
Autophagy promotes cancer cell survival and drug resistance by degrading harmful cellular components and maintaining cellular energy levels. Disruption of autophagy may be a promising approach to sensitize cancer cells to anticancer drugs. The combination of autophagic inhibitors, such as chloroquine (CQ) and lucanthone with conventional cancer therapeutics has been investigated in clinical trials, but adverse drug-drug interactions are a high possibility. Here we designed and synthesized a novel, small-molecule library based on an acridine skeleton and the CQ structure with various modifications and substitutions and screened the compounds for effective autophagy inhibition...
October 5, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28978341/mab-mdr1-modified-chitosan-nanoparticles-overcome-acquired-egfr-tki-resistance-through-two-potential-therapeutic-targets-modulation-of-mdr1-and-autophagy
#19
Yan Zheng, Chang Su, Liang Zhao, Yijie Shi
BACKGROUND: Tyrosine kinase inhibitors (TKIs) that act against the epithelial growth factor receptor (EGFR) were once widely used in chemotherapy for many human cancers. However, acquired chemoresistance occurred in almost all patients, limiting the clinical application of EGFR-TKI. Thus far, no effective methods existing can resolve this problem. Designing a therapeutic treatment with a specific multi-target profile has been regarded as a possible strategy to overcome acquired EGFR-TKI resistance...
October 4, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/28978032/vitamin-c-and-doxycycline-a-synthetic-lethal-combination-therapy-targeting-metabolic-flexibility-in-cancer-stem-cells-cscs
#20
Ernestina Marianna De Francesco, Gloria Bonuccelli, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression of four mitochondrial DNA encoded proteins (MT-ND3, MT-CO2, MT-ATP6 and MT-ATP8) is suppressed, by up to 35-fold. This high selection pressure metabolically synchronizes the surviving cancer cell sub-population towards a predominantly glycolytic phenotype, resulting in metabolic inflexibility...
September 15, 2017: Oncotarget
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