keyword
MENU ▼
Read by QxMD icon Read
search

chloroquine resistance

keyword
https://www.readbyqxmd.com/read/28333961/phytochemical-investigation-of-aloe-pulcherrima-roots-and-evaluation-for-its-antibacterial-and-antiplasmodial-activities
#1
Dele Abdissa, Girma Geleta, Ketema Bacha, Negera Abdissa
Medicinal plants with documented traditional uses remain an important source for the treatment of a wide range of ailments. Evidence shows that majority of the Ethiopian population are still dependent on traditional medicine. Aloe pulcherrima Gilbert & Sebsebe is one of the endemic Aloe species traditionally used for the treatment of malaria and wound healing in central, Southern and Northern part of Ethiopia. The aim of the current study was, therefore, to isolate active compounds from roots of A. pulcherrima and evaluate for their antibacterial and antiplasmodial activities using standard test strains...
2017: PloS One
https://www.readbyqxmd.com/read/28333717/effect-of-resistance-exercise-on-muscle-metabolism-and-autophagy-in-sibm
#2
Jae-Hoon Jeong, Dae-Seung Yang, Dong-Ju Hwang, Joon-Yong Cho, Eun-Bum Kang
PURPOSE: Sporadic inclusion body myositis (sIBM), a muscular degenerative disease in the elderly, is an inflammatory myopathy characterized by muscle weakness in the wrist flexor, quadriceps, and tibialis anterior muscles. We aimed to identify the therapeutic effect of resistance exercise (RE) in improving sIBM symptoms in an sIBM animal model. METHODS: Six-week-old male Wistar rats were divided into a sham group (sham, n = 12), chloroquine-control group (CQ-con, n = 12), and chloroquine-RE group (CQ-RE, n = 12)...
March 23, 2017: Medicine and Science in Sports and Exercise
https://www.readbyqxmd.com/read/28332319/piperazine-linked-4-aminoquinoline-chalcone-ferrocenyl-chalcone-conjugates-synthesis-and-anti-plasmodial-evaluation
#3
Amandeep Singh, Anu Rani, Jiri Gut, Philip J Rosenthal, Vipan Kumar
A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41-2.38 μM against chloroquine-resistant and mefloquine sensitive W2 strain of P. falciparum. The sub-micromolar activities of most of the synthesized conjugates suggest that such molecular frameworks can act as therapeutic templates for the design and synthesis of new antimalarials...
March 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28320254/antimalarial-and-antiplasmodial-activity-of-husk-extract-and-fractions-of-zea-mays
#4
Jude E Okokon, Bassey S Antia, Dinesh Mohanakrishnan, Dinkar Sahal
CONTEXT: Zea mays L. (Poacae) husk decoctions are traditionally used in the treatment of malaria by various tribes in Nigeria. OBJECTIVE: To assess the antimalarial and antiplasmodial potentials of the husk extract and fractions on malaria parasites using in vivo and in vitro models. MATERIALS AND METHODS: The ethanol husk extract and fractions (187-748 mg/kg, p.o.) of Zea mays were investigated for antimalarial activity against Plasmodium berghei using rodent (mice) malaria models and in vitro activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using the SRBR green assay method...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28318947/docking-synthesis-and-antimalarial-activity-of-novel-4-anilinoquinoline-derivatives
#5
Shilpa Vijayaraghavan, Supriya Mahajan
A series of 4-anilinoquinoline triazine derivatives were designed, synthesized and screened for in vivo antimalarial activity against a chloroquine-sensitive strain of Plasmodium berghei. The compounds were further subjected to in vitro antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum and β-haematin inhibition studies. All the compounds exhibited in vivo antimalarial activity better than that shown by the standard drug, chloroquine. Twelve out of fifteen compounds showed better inhibition than that of chloroquine against chloroquine-resistant W2 strain of Plasmodium falciparum...
March 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28315598/n-piperonyl-substitution-on-aminoquinoline-pyrimidine-hybrids-effect-on-the-antiplasmodial-potency
#6
Rohit Kholiya, Shabana I Khan, Aparna Bahuguna, Mohit Tripathi, Diwan S Rawat
A series of 4-aminoquinoline-piperonyl-pyrimidine hybrids were synthesized with the aim of identifying compounds with enhanced antimalarial activity. All the synthesized molecules were evaluated in vitro against cultured Plasmodium falciparum W2 and D6 strains and exhibited potent antiplasmodial activities with IC50 values in the range of 0.02-5.16 μM. Out of the 22 synthesised hybrids, 12 were found to be better (up to eight-fold more active) than chloroquine (CQ), particularly against the CQ-resistant W2 strain of P...
March 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28302108/confirmation-of-plasmodium-falciparum-in-vitro-resistance-to-monodesethylamodiaquine-and-chloroquine-in-dakar-senegal-in-2015
#7
Silman Diawara, Marylin Madamet, Mame Bou Kounta, Gora Lo, Khalifa Ababacar Wade, Aminata Nakoulima, Raymond Bercion, Rémy Amalvict, Mamadou Wague Gueye, Bécaye Fall, Bakary Diatta, Bruno Pradines
BACKGROUND: In response to increasing resistance to anti-malarial drugs, Senegal adopted artemisinin-based combination therapy (ACT) as the first-line treatment for uncomplicated malaria in 2006. However, resistance of Plasmodium falciparum parasites to artemisinin derivatives, characterized by delayed parasite clearance after treatment with ACT or artesunate monotherapy, has recently emerged and rapidly spread in Southeast Asia. After 10 years of stability with rates ranging from 5.6 to 11...
March 16, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28301876/autophagy-inhibitor-chloroquine-increases-sensitivity-to-cisplatin-in-qbc939-cholangiocarcinoma-cells-by-mitochondrial-ros
#8
Xianzhi Qu, Jiyao Sheng, Luyan Shen, Jing Su, Yunjie Xu, Qi Xie, Yao Wu, Xuewen Zhang, Liankun Sun
The tumor cells have some metabolic characteristics of the original tissues, and the metabolism of the tumor cells is closely related to autophagy. However, the mechanism of autophagy and metabolism in chemotherapeutic drug resistance is still poorly understood. In this study, we investigated the role and mechanism of autophagy and glucose metabolism in chemotherapeutic drug resistance by using cholangiocarcinoma QBC939 cells with primary cisplatin resistance and hepatocellular carcinoma HepG2 cells. We found that QBC939 cells with cisplatin resistance had a higher capacity for glucose uptake, consumption, and lactic acid generation, and higher activity of the pentose phosphate pathway compared with HepG2 cells, and the activity of PPP was further increased after cisplatin treatment in QBC939 cells...
2017: PloS One
https://www.readbyqxmd.com/read/28300558/therapeutic-efficacy-of-chloroquine-for-the-treatment-of-plasmodium-vivax-malaria-among-outpatients-at-shawa-robit-health-care-center-north-east-ethiopia
#9
Seble Seifu, Ahmed Zeynudin, Endalew Zemene, Sultan Suleman, Abdissa Biruksew
Nearly 40% of all malaria infection in Ethiopia is caused by Plasmodium vivax (P. vivax). Chloroquine (CQ) is the first line treatment for confirmed P. vivax malaria in the country. However, the efficacy of this drug has been compromised by CQ resistant P. vivax (CRPv) strains. Therefore, the present study was aimed at assessing the therapeutic efficacy of CQ for treatment of P. vivax malaria at Shawa Robit Health Care Centre, North-Ease Ethiopia. A one-arm, 28-day follow-up, in vivo therapeutic efficacy study was conducted from October 2013 to February 2014...
March 11, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28298235/clinical-and-molecular-surveillance-of-drug-resistant-vivax-malaria-in-myanmar-2009-2016
#10
Myat Htut Nyunt, Jin-Hee Han, Bo Wang, Khin Myo Aye, Kyin Hla Aye, Seong-Kyun Lee, Ye Htut, Myat Phone Kyaw, Kay Thwe Han, Eun-Taek Han
BACKGROUND: One of the major challenges for control and elimination of malaria is ongoing spread and emergence of drug resistance. While epidemiology and surveillance of the drug resistance in falciparum malaria is being explored globally, there are few studies on drug resistance vivax malaria. METHODS: To assess the spread of drug-resistant vivax malaria in Myanmar, a multisite, prospective, longitudinal study with retrospective analysis of previous therapeutic efficacy studies, was conducted...
March 16, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28291694/new-hydrazine-and-hydrazide-quinoxaline-1-4-di-n-oxide-derivatives-in-silico-admet-antiplasmodial-and-antileishmanial-activity
#11
Miguel Quiliano, Adriana Pabón, Gustavo Ramirez-Calderon, Carlos Barea, Eric Deharo, Silvia Galiano, Ignacio Aldana
We report the design (in silico ADMET criteria), synthesis, cytotoxicity studies (HepG-2 cells), and biological evaluation of 15 hydrazine/hydrazide quinoxaline 1,4-di-N-oxide derivatives against the 3D7 chloroquine sensitive strain and FCR-3 multidrug resistant strain of Plasmodium falciparum and Leishmania infantum (axenic amastigotes). Fourteen of derivatives are novel quinoxaline 1,4-di-N-oxide derivatives. Compounds 18 (3D7 IC50=1.40μM, FCR-3 IC50=2.56μM) and 19 (3D7 IC50=0.24μM, FCR-3 IC50=2.8μM) were identified as the most active against P...
February 21, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28289248/antimalarial-drug-resistance-a-threat-to-malaria-elimination
#12
Didier Menard, Arjen Dondorp
Increasing antimalarial drug resistance once again threatens effective antimalarial drug treatment, malaria control, and elimination. Artemisinin combination therapies (ACTs) are first-line treatment for uncomplicated falciparum malaria in all endemic countries, yet partial resistance to artemisinins has emerged in the Greater Mekong Subregion. Concomitant emergence of partner drug resistance is now causing high ACT treatment failure rates in several areas. Genetic markers for artemisinin resistance and several of the partner drugs have been established, greatly facilitating surveillance...
March 13, 2017: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/28288632/unexpected-selections-of-plasmodium-falciparum-polymorphisms-in-previously-treatment-na%C3%A3-ve-areas-after-monthly-presumptive-administration-of-three-different-anti-malarial-drugs-in-liberia-1976-78
#13
Irina T Jovel, Anders Björkman, Cally Roper, Andreas Mårtensson, Johan Ursing
BACKGROUND: To assess the effect on malaria prevalence, village specific monthly administrations of pyrimethamine, chlorproguanil, chloroquine or placebo were given to children in four previously treatment-naïve Liberian villages, 1976-78. Plasmodium falciparum in vivo resistance developed to pyrimethamine only. Selection of molecular markers of P. falciparum resistance after 2 years of treatment are reported. METHODS: Blood samples were collected from 191 study children in a survey in 1978...
March 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28282266/autophagy-is-dispensable-for-kmt2a-mll-mllt3-af9-aml-maintenance-and-anti-leukemic-effect-of-chloroquine
#14
Xiaoyi Chen, Jason Clark, Mark Wunderlich, Cuiqing Fan, Ashley Davis, Song Chen, Jun-Lin Guan, James C Mulloy, Ashish Kumar, Yi Zheng
Recently, macroautophagy/autophagy has emerged as a promising target in various types of solid tumor treatment. However, the impact of autophagy on acute myeloid leukemia (AML) maintenance and the validity of autophagy as a viable target in AML therapy remain unclear. Here we show that Kmt2a/Mll-Mllt3/Af9 AML (MA9-AML) cells have high autophagy flux compared with normal bone marrow cells, but autophagy-specific targeting, either through Rb1cc1-disruption to abolish autophagy initiation, or via Atg5-disruption to prevent phagophore (the autophagosome precursor) membrane elongation, does not affect the growth or survival of MA9-AML cells, either in vitro or in vivo...
February 15, 2017: Autophagy
https://www.readbyqxmd.com/read/28279945/quantitative-characterization-of-hemozoin-in-plasmodium-berghei-and-vivax
#15
John M Pisciotta, Peter F Scholl, Joel L Shuman, Vladimir Shualev, David J Sullivan
The incidence and global distribution of chloroquine resistant (CR) Plasmodium vivax infection has increased since emerging in 1989. The mechanism of resistance in CR P. vivax has not been defined. The resistance likely relates to the formation and disposition of hemozoin as chloroquine's primary mechanism of action involves disruption of hemozoin formation. CR P. berghei strains, like CR P. vivax strains, are confined to reticulocyte host cells and reportedly they do not accumulate appreciable intraerythrocytic hemozoin...
February 8, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28264857/the-malaria-taqman-array-card-87-assays-for-plasmodium-falciparum-drug-resistance-speciation-and-genotyping-in-a-single-reaction
#16
Suporn Pholwat, Jie Liu, Suzanne Stroup, Shevin Jacob, Patrick Banura, Christopher Moore, Fang Huang, Miriam Laufer, Eric Houpt, Jennifer Guler
Antimalarial drug resistance exacerbates the global disease burden and complicates eradication efforts. To facilitate the surveillance of resistance markers in malaria-endemic countries, we developed a suite of TaqMan assays for known resistance markers and compartmentalized them into a single array card (TAC). We included 87 assays for species identification, the detection of Plasmodium falciparum mutations associated with chloroquine, atovaquone, pyrimethamine, sulfadoxine, and artemisinin resistance, and neutral single nucleotide polymorphism (SNP) genotyping...
March 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28263085/exploration-of-thiaheterocyclic-hhdac6-inhibitors-as-potential-antiplasmodial-agents
#17
Rob De Vreese, Carmen de Kock, Peter J Smith, Kelly Chibale, Matthias D'hooghe
AIM: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan-histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoform-selective HDACis. RESULTS: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity...
March 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28259160/in-vivo-efficacy-of-top-five-surveyed-ghanaian-herbal-anti-malarial-products
#18
Dennis Wilmot, Elvis Ofori Ameyaw, Daniel Amoako-Sakyi, Johnson Nyarko Boampong, Neils Ben Quashie
BACKGROUND: Anti-malarial herbal preparations (HPs) continue to enjoy high patronage in Ghana despite reports that the artemisinin-based combination therapy (ACT), the recommended first choice for treatment of uncomplicated malaria in the country, remains efficacious. A major issue with the use of these preparations is inadequate or unreliable data on their efficacy and quality. An assessment of the potency and quality of the most popular commercial anti-malarial HPs in Ghana was, therefore, carried out...
March 4, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28258239/the-pushmi-pullyu-of-resistance-to-chloroquine-in-malaria
#19
REVIEW
Ruth Skrzypek, Richard Callaghan
Malarial infection continues to impart devastating health problems in the developing world. Treatment of malaria has involved chemotherapy since 168 BC, with the most prevalent and successful forms using plant alkaloids. Perhaps the greatest treatment success against malaria was by chloroquine, a synthetic derivative of the quinines found in the Cinchona tree bark. Chloroquine is able to kill parasites by interfering with haem metabolism in the parasite's digestive vacuole. The widespread use of chloroquine predictably resulted in the development of drug-resistant malaria and the most highly implicated resistance mediators are the transporter proteins P-glycoprotein (P-gp) homologue 1 (P-gh1) and Plasmodium falciparum chloroquine-resistance transporter (PfCRT), which reside on the parasite's digestive vacuole...
February 28, 2017: Essays in Biochemistry
https://www.readbyqxmd.com/read/28250867/new-triterpenoidal-saponins-from-koelreuteria-paniculata
#20
Ahmad E Mostafa, Atef A El-Hela, Abd-Elsalam I Mohammad, Stephen J Cutler, Samir A Ross
Bioassay guided fractionation and chemical investigation of the ethanolic extract of the aerial parts of Koelreuteria paniculata Laxm. (Sapindaceae), resulted in the isolation and identification of three new triterpenoid saponins 1-3 named Paniculatosoid A-C, along with eleven known compounds. The structures of the isolated compounds were elucidated using 1D and 2D NMR experiments, HRESIMS, and comparison with literature data. The occurrence of tridesmosidic saponin is reported for the first time from family Sapindaceae, as well as it is rarely found in natural saponins...
September 2016: Phytochemistry Letters
keyword
keyword
46679
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"