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https://www.readbyqxmd.com/read/27919892/significant-divergence-in-sensitivity-to-antimalarial-drugs-between-neighboring-plasmodium-falciparum-populations-along-the-eastern-border-of-myanmar
#1
Weilin Zeng, Yao Bai, Meilian Wang, Zenglei Wang, Shuang Deng, Yonghua Ruan, Shi Feng, Zhaoqing Yang, Liwang Cui
Malaria parasites in different endemic areas display different levels of resistance to antimalarial drugs as the result of varied drug use histories. To provide updated knowledge of drug sensitivities during the malaria elimination phase in Southeast Asia, an epicenter of multidrug resistance, we determined in vitro susceptibilities of culture-adapted Plasmodium falciparum isolates from two eastern border regions (Wa and Kachin) of Myanmar to ten drugs. Despite their close proximity, the Kachin parasites displayed higher IC50 values than the Wa parasites to chloroquine, piperaquine, naphthoquine, mefloquine, quinine, pyrimethamine, pyronaridine, lumefantrine and dihydroartemisinin...
December 5, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27895848/four-artemisinin-based-treatments-in-african-pregnant-women-with-malaria
#2
Divine Pekyi, Akua A Ampromfi, Halidou Tinto, Maminata Traoré-Coulibaly, Marc C Tahita, Innocent Valéa, Victor Mwapasa, Linda Kalilani-Phiri, Gertrude Kalanda, Mwayiwawo Madanitsa, Raffaella Ravinetto, Theonest Mutabingwa, Prosper Gbekor, Harry Tagbor, Gifty Antwi, Joris Menten, Maaike De Crop, Yves Claeys, Celine Schurmans, Chantal Van Overmeir, Kamala Thriemer, Jean-Pierre Van Geertruyden, Umberto D'Alessandro, Michael Nambozi, Modest Mulenga, Sebastian Hachizovu, Jean-Bertin B Kabuya, Joyce Mulenga
BACKGROUND: Information regarding the safety and efficacy of artemisinin combination treatments for malaria in pregnant women is limited, particularly among women who live in sub-Saharan Africa. METHODS: We conducted a multicenter, randomized, open-label trial of treatments for malaria in pregnant women in four African countries. A total of 3428 pregnant women in the second or third trimester who had falciparum malaria (at any parasite density and regardless of symptoms) were treated with artemether-lumefantrine, amodiaquine-artesunate, mefloquine-artesunate, or dihydroartemisinin-piperaquine...
September 2016: Malawi Medical Journal: the Journal of Medical Association of Malawi
https://www.readbyqxmd.com/read/27890675/synergistic-drug-combination-effectively-blocks-ebola-virus-infection
#3
Wei Sun, Shihua He, Carles Martínez-Romero, Jennifer Kouznetsova, Gregory Tawa, Miao Xu, Paul Shinn, Ethan Fisher, Yan Long, Omid Motabar, Shu Yang, Philip E Sanderson, Peter R Williamson, Adolfo García-Sastre, Xiangguo Qiu, Wei Zheng
Although a group of FDA-approved drugs were previously identified with activity against Ebola virus, most of them are not clinically useful because their human blood concentrations are not high enough to inhibit EBOV infection. We screened 795 unique three-drug combinations in an EBOV entry assay. Two sets of three-drug combinations, toremifene-mefloquine-posaconazole and toremifene-clarithromycin-posaconazole, were identified that effectively blocked EBOV entry and were further validated for inhibition of live EBOV infection...
November 24, 2016: Antiviral Research
https://www.readbyqxmd.com/read/27889812/research-progress-of-hydroxychloroquine-and-autophagy-inhibitors-on-cancer
#4
REVIEW
Ting-Ting Shi, Xiao-Xu Yu, Li-Jun Yan, Hong-Tao Xiao
PURPOSE: Hydroxychloroquine (HCQ), the analog of chloroquine, augments the effect of chemotherapies and radiotherapy on various tumors identified in the current clinical trials. Meanwhile, the toxicity of HCQ retinopathy raises concern worldwide. Thus, the potent autophagy inhibitors are urgently needed. METHODS: A systematic review was related to 'hydroxychloroquine' or 'chloroquine' with 'clinical trials,' 'retinopathy' and 'new autophagy inhibitors.' This led to many cross-references involving HCQ, and these data have been incorporated into the following study...
November 26, 2016: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/27889529/antiviral-activities-of-selected-antimalarials-against-dengue-virus-type-2-and-zika-virus
#5
Anuradha Balasubramanian, Tadahisa Teramoto, Amol A Kulkarni, Apurba K Bhattacharjee, Radhakrishnan Padmanabhan
In a previous study, twelve antimalarial compounds, amodiaquine (AQ) and derivatives, were shown to have potent anti-dengue viral (DENV) activity by using the stable DENV2 Renilla luciferase reporter replicon expressing BHK-21 cells, infectivity (plaque), and the qRT-PCR assays. In this study, we performed molecular modeling on these compounds to determine their stereo-electronic properties required for optimal antiviral activity. Based on the similarity of calculated stereo-electronic profiles, specifically the electrostatic potential profiles of the compounds, and in silico screening of related compounds from literature, we identified three additional compounds, Quinacrine (QC), Mefloquine (MQ), and GSK369796...
November 23, 2016: Antiviral Research
https://www.readbyqxmd.com/read/27866919/in-vitro-sensitivity-of-antimalarial-drugs-and-correlation-with-clinico-parasitological-response-following-treatment-with-a-3-day-artesunate-mefloquine-combination-in-patients-with-falciparum-malaria-along-the-thai-myanmar-border
#6
Phunuch Muhamad, Artitaya Thiengsusuk, Papichaya Phompradit, Kesara Na-Bangchang
A 3-day artesunate-mefloquine combination therapy has been using as first-line treatment for acute uncomplicated Plasmodium falciparum malaria in Thailand since 1995 on the background of mefloquine resistance. The aim of the present study was to assess sensitivity of P. falciparum isolates (n=44) in an area along the Thai-Myanmar border (year 2009) to artesunate, mefloquine, chloroquine and quinine, including their correlation with clinico-parasitological response. Twenty, 19, and 5 isolates were collected from patients with 'Adequate Clinical and Parasitological Response (ACPR)', 'Late Parasitological Failure (LPF)' and 're-infection', respectively...
November 17, 2016: Acta Tropica
https://www.readbyqxmd.com/read/27853090/steroid-pulse-therapy-may-mitigate-prolonged-neurological-manifestations-after-eradication-of-severe-plasmodium-falciparum-parasitemia
#7
Chihiro Hasegawa, Akiko Inagaki, Gohei Yamada, Koji Morita, Isamu Kitamura, Koya Ariyoshi
A 58-year-old Japanese man with a high parasitemia of Plasmodium falciparum, returning from Uganda, was admitted to our hospital since his consciousness level rapidly deteriorated after the initial dose of mefloquine. Despite the parasitemia was cleared by quinine by day 7, the coma remained unchanged and diffuse leukoencephalopathy was detected on magnetic resonance image. Steroid pulse therapy was initiated on day 8. Subsequently, the neurological manifestations improved and he was discharged on day 73 without any sequelae...
2016: Internal Medicine
https://www.readbyqxmd.com/read/27831748/therapeutic-effects-of-antibiotic-drug-mefloquine-against-cervical-cancer-through-impairing-mitochondrial-function-and-inhibiting-mtor-pathway
#8
Hui Li, Shun Jiao, Xin Li, Hasina Banu, Shreejana Hamal, Xianrong Wang
Targeting mitochondria is an attractive strategy for cancer therapy due to the essential roles of mitochondria in cancer cell energy metabolism. In this study, we show that mefloquine, an antibiotic drug, effectively targets cervical cancer cells through impairing mitochondrial function. Mefloquine dose-dependently induces apoptosis and inhibits proliferation and anchorage-independent colony formation of multiple cervical cancer cell lines. Mefloquine alone inhibits cervical tumor growth in vivo and its combination with paclitaxel is synergistic in inhibiting tumor growth...
August 11, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/27825353/analysis-of-anti-malarial-resistance-markers-in-pfmdr1-and-pfcrt-across-southeast-asia-in-the-tracking-resistance-to-artemisinin-collaboration
#9
Krongkan Srimuang, Olivo Miotto, Pharath Lim, Rick M Fairhurst, Dominic P Kwiatkowski, Charles J Woodrow, Mallika Imwong
BACKGROUND: Declining anti-malarial efficacy of artemisinin-based combination therapy, and reduced Plasmodium falciparum susceptibility to individual anti-malarials are being documented across an expanding area of Southeast Asia (SEA). Genotypic markers complement phenotypic studies in assessing the efficacy of individual anti-malarials. METHODS: The markers pfmdr1 and pfcrt were genotyped in parasite samples obtained in 2011-2014 at 14 TRAC (Tracking Resistance to Artemisinin Collaboration) sites in mainland Southeast Asia using a combination of PCR and next-generation sequencing methods...
November 8, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27799060/mefloquine-associated-dizziness-diplopia-and-central-serous-chorioretinopathy-a-case-report
#10
Manish Jain, Remington L Nevin, Iajaz Ahmed
BACKGROUND: Many acute and chronic neurological sequelae from the quinoline derivative antimalarial drug mefloquine, including dizziness and effects on the visual system such as diplopia and blurred vision, may be attributable to focal central nervous system toxicity. Maculopathy has also been reported with use of mefloquine, although the mechanism of this effect has remained unclear. Identification of a common mechanism of toxicity plausibly underlying these visual and non-visual effects may provide broader insights into the acute and chronic neuropsychiatric effects of this and other quinoline antimalarial drugs...
October 31, 2016: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/27793910/highly-halaven-resistant-kbv20c-cancer-cells-can-be-sensitized-by-co-treatment-with-fluphenazine
#11
Ji Hyun Cheon, Byung Mu Lee, Hyung Sik Kim, Sungpil Yoon
AIM: To identify conditions that induce an increase in the sensitivity of highly Halaven (HAL)-resistant cancer cells compared to sensitive cells. MATERIALS AND METHODS: We observed that drug-resistant KBV20C cells are highly resistant to HAL compared to other antimitotic drugs. The concentration required to treat KBV20C cells was almost 500-fold higher than that used to treat sensitive parent KB cells. In order to increase sensitization, HAL-treated KBV20C cells were co-treated with the repositioned drug, fluphenazine (FLU)...
November 2016: Anticancer Research
https://www.readbyqxmd.com/read/27793909/attenuation-of-colchicine-toxicity-in-drug-resistant-cancer-cells-by-co-treatment-with-anti-malarial-drugs
#12
Ae-Ran Choi, Ju-Hwa Kim, Ji Hyun Cheon, Hyung Sik Kim, Sungpil Yoon
BACKGROUND/AIM: Colchicine (COL) is a well-known and potent microtubule targeting anticancer agent. The purpose of our study was to identify conditions that increase sensitization of COL-resistant cancer cells that overexpress P-glycoprotein (P-gp). MATERIALS AND METHODS: The anti-malarial drugs chloroquine (CHL), mefloquine (MEF) and primaquine (PRI) have been shown to increase sensitization in drug-resistant KBV20C cells via P-gp inhibition. Therefore, we tested whether co-treatment of COL with PRI, CHL or MEF increases sensitivity in COL-resistant KBV20C cells over that of cells treated with COL alone and whether these effects are attributable to P-gp activity...
November 2016: Anticancer Research
https://www.readbyqxmd.com/read/27788228/prevalence-of-plasmodium-falciparum-molecular-markers-of-antimalarial-drug-resistance-in-a-residual-malaria-focus-area-in-sabah-malaysia
#13
Nor Azrina Norahmad, Mohd Ridzuan Mohd Abd Razak, Noor Rain Abdullah, Umi Rubiah Sastu, Mallika Imwong, Prem Kumar Muniandy, Muhammad Nor Farhan Saat, Amirrudin Muhammad, Jenarun Jelip, Moizin Tikuson, Norsalleh Yusof, Christina Rundi, Rose Nani Mudin, Ami Fazlin Syed Mohamed
Chloroquine (CQ) and fansidar (sulphadoxine-pyrimethamine, SP) were widely used for treatment of Plasmodium falciparum for several decades in Malaysia prior to the introduction of Artemisinin-based Combination Therapy (ACT) in 2008. Our previous study in Kalabakan, located in south-east coast of Sabah showed a high prevalence of resistance to CQ and SP, suggesting the use of the treatment may no longer be effective in the area. This study aimed to provide a baseline data of antimalarial drug resistant markers on P...
2016: PloS One
https://www.readbyqxmd.com/read/27777838/elucidation-of-the-enantiodiscrimination-properties-of-a-nonracemic-chiral-alignment-medium-through-gel-based-capillary-electrochromatography-separation-of-the-mefloquine-stereoisomers
#14
Ayat Allah Al-Massaedh, Manuel Schmidt, Ute Pyell, Uwe M Reinscheid
Enantiodiscrimination and enantioseparation are two highly important processes in chemistry, often performed by using NMR spectroscopy and chromatography. For a better understanding of the mechanistic details, the same system should be studied by both methods. In addition, isotropic and anisotropic NMR parameters should be obtained, the latter using alignment media so that residual dipolar couplings and chemical-shift anisotropies can be measured. Consequently, a chiral alignment medium was used for the first time in chiral gel-based capillary electrochromatography with the four stereoisomers of the antimalaria drug mefloquine as test compounds...
October 2016: ChemistryOpen
https://www.readbyqxmd.com/read/27769299/ex-vivo-piperaquine-resistance-developed-rapidly-in-plasmodium-falciparum-isolates-in-northern-cambodia-compared-to-thailand
#15
Suwanna Chaorattanakawee, Chanthap Lon, Krisada Jongsakul, Jariyanart Gawee, Somethy Sok, Siratchana Sundrakes, Nareth Kong, Chatchadaporn Thamnurak, Soklyda Chann, Sorayut Chattrakarn, Chantida Praditpol, Nillawan Buathong, Nichapat Uthaimongkol, Philip Smith, Narongrid Sirisopana, Rekol Huy, Satharath Prom, Mark M Fukuda, Delia Bethell, Douglas S Walsh, Charlotte Lanteri, David Saunders
BACKGROUND: The recent dramatic decline in dihydroartemisinin-piperaquine (DHA-PPQ) efficacy in northwestern Cambodia has raised concerns about the rapid spread of piperaquine resistance just as DHA-PPQ is being introduced as first-line therapy in neighbouring countries. METHODS: Ex vivo parasite susceptibilities were tracked to determine the rate of progression of DHA, PPQ and mefloquine (MQ) resistance from sentinel sites on the Thai-Cambodian and Thai-Myanmar borders from 2010 to 2015...
October 21, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27747687/prolonged-neuropsychiatric-symptoms-in-a-military-service-member-exposed-to-mefloquine
#16
Jeffrey Livezey, Thomas Oliver, Louis Cantilena
A 32-year-old male developed neuropsychiatric symptoms 2 weeks after starting mefloquine 250 mg/week for malaria prophylaxis. He continued to take the medication for the next 4 months. Initial symptoms included vivid dreams and anxiety, as well as balance problems. These symptoms persisted and progressed over the next 4 years to include vertigo, emotional lability, and poor short-term memory, which have greatly affected his personal and professional life. An extensive evaluation revealed objective evidence supporting a central vestibulopathy...
December 2016: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/27667552/conjugation-of-n-acylhydrazone-and-1-2-4-oxadiazole-leads-to-the-identification-of-active-antimalarial-agents
#17
José Maurício Dos Santos Filho, Diogo Manoel Alves de Queiroz E Silva, Taís Soares Macedo, Helena Mariana Pitangueira Teixeira, Diogo Rodrigo Magalhaes Moreira, Soura Challal, Jean-Luc Wolfender, Emerson Ferreira Queiroz, Milena Botelho Pereira Soares
Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, synthesis and antiparasitic evaluation of two novel series of 1,2,4-oxadiazoles in conjugation to N-acylhydrazones, both groups recognized as privileged structures, as well as the studies on the antimalarial activity of 16 previous described analogues. By varying substituents attached to the phenyl ring, it was possible to retain, enhance or increase the antiparasitic activity in comparison to the nonsubstituted derivatives...
September 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27645758/a-case-of-progressive-multifocal-leukoencephalopathy-with-chronic-renal-failure-whose-jc-virus-in-cerebrospinal-fluid-disappeared-after-mefloquine-mirtazapine-dual-therapy
#18
Eiichi Ohnuki, Shinya Asayama, Tomoko Asayama, Kazuo Nakamichi, Masayuki Saijo, Satoru Kosaka
An 83-year-old man with chronic renal failure was referred to our hospital because of subacute progressive right hemiparesis. A brain MRI showed high-intensity lesions in bilateral middle cerebellar peduncles and white matter of the left frontal lobe on T2-weighted images. The lesions increased gradually, so we suspected a brain tumor because (1)H-MRS images showed elevated Cho and decreased NAA, and also pathologic findings of the brain biopsy suggested glioblastoma. However, JC virus (JCV) in cerebrospinal fluid was revealed highly positive by PCR...
September 16, 2016: Rinshō Shinkeigaku, Clinical Neurology
https://www.readbyqxmd.com/read/27638865/uk-troops-to-continue-to-receive-mefloquine-despite-concern-over-adverse-events
#19
Caroline White
No abstract text is available yet for this article.
2016: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/27625401/effectiveness-of-twice-a-week-prophylaxis-with-atovaquone-proguanil-malarone%C3%A2-in-long-term-travellers-to-west-africa
#20
Tamar Lachish, Maskit Bar-Meir, Neta Eisenberg, Eli Schwartz
BACKGROUND: Current guidelines recommend daily dosing of atovaquone-proguanil (AP), beginning a day before travel to endemic areas and continuing for 7 days after departure. Adherence of long-term travellers to daily malaria chemoprophylaxis tends to be poor, even when residing in highly endemic malaria regions. Evidence from a volunteer challenging study suggests that non-daily, longer intervals dosing of AP provides effective protection against Plasmodium falciparum This study examines the effectiveness of twice weekly AP prophylaxis in long-term travellers to highly endemic P...
June 2016: Journal of Travel Medicine
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