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Artemisinin resistance

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https://www.readbyqxmd.com/read/28319807/targeting-nf-kappa-b-signaling-by-artesunate-restores-sensitivity-of-castrate-resistant-prostate-cancer-cells-to-antiandrogens
#1
Jessica J Nunes, Swaroop K Pandey, Anjali Yadav, Sakshi Goel, Bushra Ateeq
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC). Here, we assessed artesunate (AS), an artemisinin derivative, for its anticancer properties and ability to alleviate resistance to androgen receptor (AR) antagonists. We have shown AS in combination with bicalutamide (Bic) attenuates the oncogenic properties of the castrate-resistant (PC3, 22RV1) and androgen-responsive (LNCaP) PCa cells...
March 16, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28319782/synthesis-and-antiplasmodial-activity-of-novel-indoleamide-derivatives-bearing-sulfonamide-and-triazole-pharmacophores
#2
N Devender, Sarika Gunjan, Renu Tripathi, Rama Pati Tripathi
Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28318947/docking-synthesis-and-antimalarial-activity-of-novel-4-anilinoquinoline-derivatives
#3
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/28302108/confirmation-of-plasmodium-falciparum-in-vitro-resistance-to-monodesethylamodiaquine-and-chloroquine-in-dakar-senegal-in-2015
#4
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/28289248/antimalarial-drug-resistance-a-threat-to-malaria-elimination
#5
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/28289193/host-immunity-to-plasmodium-falciparum-and-the-assessment-of-emerging-artemisinin-resistance-in-a-multinational-cohort
#6
Ricardo Ataide, Elizabeth A Ashley, Rosanna Powell, Jo-Anne Chan, Michael J Malloy, Katherine O'Flaherty, Eizo Takashima, Christine Langer, Takafumi Tsuboi, Arjen M Dondorp, Nicholas P Day, Mehul Dhorda, Rick M Fairhurst, Pharath Lim, Chanaki Amaratunga, Sasithon Pukrittayakamee, Tran Tinh Hien, Ye Htut, Mayfong Mayxay, M Abul Faiz, James G Beeson, Francois Nosten, Julie A Simpson, Nicholas J White, Freya J I Fowkes
Artemisinin-resistant falciparum malaria, defined by a slow-clearance phenotype and the presence of kelch13 mutants, has emerged in the Greater Mekong Subregion. Naturally acquired immunity to malaria clears parasites independent of antimalarial drugs. We hypothesized that between- and within-population variations in host immunity influence parasite clearance after artemisinin treatment and the interpretation of emerging artemisinin resistance. Antibodies specific to 12 Plasmodium falciparum sporozoite and blood-stage antigens were determined in 959 patients (from 11 sites in Southeast Asia) participating in a multinational cohort study assessing parasite clearance half-life (PCt1/2) after artesunate treatment and kelch13 mutations...
March 13, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28289029/antimalarial-hybrid-molecules-a-close-reality-or-a-distant-dream
#7
Drishti Agarwal, Rinkoo D Gupta, Satish K Awasthi
Emergence of drug resistant Plasmodium falciparum strains has led to a situation of haste in the scientific and pharmaceutical communities. Hence, all their efforts are redirected towards finding alternate chemotherapeutic agents that are capable of combating multi-drug resistant parasite strains. In the above light, scientists have come up with the concept of hybridisation of two or more active pharmacophores into a single chemical entity, resulting in 'antimalarial hybrids.' The approach has been applied widely for lead generation against deadly diseases such as cancer and AIDS, with proven potential to be used as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery...
March 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28289025/age-weight-and-cyp2d6-genotype-are-major-determinants-of-primaquine-pharmacokinetics-in-african-children
#8
Bronner P Gonçalves, Helmi Pett, Alfred B Tiono, Daryl Murry, Sodiomon Sirima, Mikko Niemi, Teun Bousema, Chris Drakeley, Rob Ter Heine
Low dose primaquine is recommended to prevent Plasmodium falciparum malaria transmission in areas threatened by artemisinin resistance and areas aiming for malaria elimination. Community treatment campaigns with artemisinin-based combination therapy in combination with the gametocytocidal primaquine dose target all age groups but no studies thus far have assessed the pharmacokinetics of this gametocytocidal drug in African children. We recruited forty children participating in a primaquine efficacy trial in Burkina Faso to study primaquine pharmacokinetics...
March 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28288121/a-genetic-system-to-study-plasmodium-falciparum-protein-function
#9
Jakob Birnbaum, Sven Flemming, Nick Reichard, Alexandra Blancke Soares, Paolo Mesén-Ramírez, Ernst Jonscher, Bärbel Bergmann, Tobias Spielmann
Current systems to study essential genes in the human malaria parasite Plasmodium falciparum are often inefficient and time intensive, and they depend on the genetic modification of the target locus, a process hindered by the low frequency of integration of episomal DNA into the genome. Here, we introduce a method, termed selection-linked integration (SLI), to rapidly select for genomic integration. SLI allowed us to functionally analyze targets at the gene and protein levels, thus permitting mislocalization of native proteins, a strategy known as knock sideways, floxing to induce diCre-based excision of genes and knocking in altered gene copies...
March 13, 2017: Nature Methods
https://www.readbyqxmd.com/read/28273638/antimalarial-activity-and-safety-assessment-of-flueggea-virosa-leaves-and-its-major-constituent-with-special-emphasis-on-their-mode-of-action
#10
Shiv Vardan Singh, Ashan Manhas, Yogesh Kumar, Sonali Mishra, Karuna Shanker, Feroz Khan, Kumkum Srivastava, Anirban Pal
A clinical emergency stands due to the appearance of drug resistant Plasmodium strains necessitate novel and effective antimalarial chemotypes, where plants seem as the prime option, especially after the discovery of quinine and artemisinin. The present study was aimed towards bioprospecting leaves of Flueggea virosa for its antimalarial efficacy and active principles. Crude hydro-ethanolic extract along with solvent derived fractions were tested in vitro against Plasmodium falciparum CQ sensitive (3D7) and resistant (K1) strains, where all the fractions exhibited potential activity (IC50 values <10μg/mL) against both the strains...
March 5, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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
#11
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/28259160/in-vivo-efficacy-of-top-five-surveyed-ghanaian-herbal-anti-malarial-products
#12
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/28257497/investigating-antimalarial-drug-interactions-of-emetine-dihydrochloride-hydrate-using-calcusyn-based-interactivity-calculations
#13
Holly Matthews, Jon Deakin, May Rajab, Maryam Idris-Usman, Niroshini J Nirmalan
The widespread introduction of artemisinin-based combination therapy has contributed to recent reductions in malaria mortality. Combination therapies have a range of advantages, including synergism, toxicity reduction, and delaying the onset of resistance acquisition. Unfortunately, antimalarial combination therapy is limited by the depleting repertoire of effective drugs with distinct target pathways. To fast-track antimalarial drug discovery, we have previously employed drug-repositioning to identify the anti-amoebic drug, emetine dihydrochloride hydrate, as a potential candidate for repositioned use against malaria...
2017: PloS One
https://www.readbyqxmd.com/read/28249591/controlled-release-of-artemisone-for-the-treatment-of-experimental-cerebral-malaria
#14
Jacob Golenser, Viola Buchholz, Amir Bagheri, Abed Nasereddin, Ron Dzikowski, Jintao Guo, Nicholas H Hunt, Sara Eyal, Natalia Vakruk, Andreas Greiner
BACKGROUND: Cerebral malaria (CM) is a leading cause of malarial mortality resulting from infection by Plasmodium falciparum. Treatment commonly involves adjunctive care and injections or transfusion of artemisinins. All artemisinins that are in current use are metabolized to dihydroxyartemisinin (DHA), to which there is already some parasite resistance. We used artemisone, a derivative that does not convert to DHA, has improved pharmacokinetics and anti-plasmodial activity and is also anti-inflammatory (an advantage given the immunopathological nature of CM)...
March 1, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28249583/molecular-surveillance-of-artemisinin-resistance-falciparum-malaria-among-migrant-goldmine-workers-in-myanmar
#15
Myat Htut Nyunt, Bo Wang, Khin Myo Aye, Kyin Hla Aye, Jin-Hee Han, Seong-Kyun Lee, Kay Thwe Han, Ye Htut, Eun-Taek Han
BACKGROUND: Artemisinin resistance has been reported in Greater Mekong Sub-region countries, including Myanmar. After discovery of artemisinin resistance marker (K13), molecular surveillance on artemisinin resistance in endemic regions have been conducted. As the migrant population represents a high percentage of malaria cases, molecular surveillance of artemisinin resistance among migrant workers is of great concern. METHODS: A cross-sectional survey was conducted in Shwegyin Township, where migrants work in the goldmines...
March 1, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28242661/prediction-of-improved-antimalarial-chemoprevention-with-weekly-dosing-of-dihydroartemisinin-piperaquine
#16
Jesmin Permala, Joel Tarning, François Nosten, Nicholas J White, Mats O Karlsson, Martin Bergstrand
Intermittent preventive treatment (IPT) is used to reduce malaria morbidity and mortality, especially in vulnerable groups such as children and pregnant women. IPT with the fixed dose combination of piperaquine (PQ) and dihydroartemisinin (DHA) is being evaluated as a potential mass treatment to control and eliminate artemisinin resistant falciparum malaria. This study explored alternative DHA-PQ adult dosing regimens compared to the monthly adult dosing regimen currently being studied in clinical trials. A time-to-event model describing the concentration-effect relationship of preventive DHA-PQ administration was used to explore the potential clinical efficacy of once weekly adult dosing regimens...
February 27, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28241761/antimalarial-activity-of-garcinia-mangostana-l-rind-and-its-synergistic-effect-with-artemisinin-in-vitro
#17
Susy Tjahjani
BACKGROUND: Malaria especially falciparum malaria still causes high morbidity and mortality in tropical countries. Several factors have been linked to this situation and the most important one is the rapid spread of parasite resistance to the currently available antimalarials, including artemisinin. Artemisinin is the main component of the currently recommended antimalarial, artemisinin based combination therapy (ACT), and it is a free radical generating antimalarial. Garcinia mangostana L (mangosteen) rind contain a lot of xanthone compounds acting as an antioxidant and exhibited antimalarial activity...
February 28, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28230749/design-of-drug-delivery-systems-containing-artemisinin-and-its-derivatives
#18
REVIEW
Blessing Atim Aderibigbe
Artemisinin and its derivatives have been reported to be experimentally effective for the treatment of highly aggressive cancers without developing drug resistance, they are useful for the treatment of malaria, other protozoal infections and they exhibit antiviral activity. However, they are limited pharmacologically by their poor bioavailability, short half-life in vivo, poor water solubility and long term usage results in toxicity. They are also expensive for the treatment of malaria when compared to other antimalarials...
February 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28225668/emergence-of-indigenous-artemisinin-resistant-plasmodium-falciparum-in-africa
#19
LETTER
Feng Lu, Richard Culleton, Meihua Zhang, Abhinay Ramaprasad, Lorenz von Seidlein, Huayun Zhou, Guoding Zhu, Jianxia Tang, Yaobao Liu, Weiming Wang, Yuanyuan Cao, Sui Xu, Yaping Gu, Julin Li, Chao Zhang, Qi Gao, Didier Menard, Arnab Pain, Haitao Yang, Qingfeng Zhang, Jun Cao
No abstract text is available yet for this article.
March 9, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28221121/molecular-evidence-of-drug-resistance-in-asymptomatic-malaria-infections-myanmar-2015
#20
Myat Htut Nyunt, Thinzar Shein, Ni Ni Zaw, Soe Soe Han, Fauzi Muh, Seong-Kyun Lee, Jin-Hee Han, Kyaw Zin Thant, Eun-Taek Han, Myat Phone Kyaw
Artemisinin resistance containment in Myanmar was initiated in 2011 after artemisinin-resistant Plasmodium falciparum malaria was reported. Molecular evidence suggests that asymptomatic malaria infections harboring drug resistance genes are present among residents of the Myanmar artemisinin resistance containment zone. This evidence supports efforts to eliminate these hidden infections.
March 2017: Emerging Infectious Diseases
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