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https://www.readbyqxmd.com/read/28087910/-progress-on-anti-tumor-molecular-mechanisms-of-dihydroartemisinin
#1
Peng Cao, Dongjin Leng, Ying Li, Ziwei Zhang, Lei Liu, Xiaoyan Li
Artemisinin is an anti-malarial drug with poor water solubility and oral absorption; so a variety of derivatives based on the parent nucleus have been developed. Compared with artemisinin, dihydroartemisinin (DHA) has a stronger anti-malaria activity, and has the advantages of high metabolic rate and better water solubility. Recent studies have discovered that DHA has a good inhibitory effect on tumor cells, which is closely related to the peroxide bridge in its molecular structure. Since tumor cells need more Fe(3+) than normal cells, there are a large number of transferrin receptors on the tumor cell membrane...
May 25, 2016: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28086874/new-developments-in-anti-malarial-target-candidate-and-product-profiles
#2
REVIEW
Jeremy N Burrows, Stephan Duparc, Winston E Gutteridge, Rob Hooft van Huijsduijnen, Wiweka Kaszubska, Fiona Macintyre, Sébastien Mazzuri, Jörg J Möhrle, Timothy N C Wells
A decade of discovery and development of new anti-malarial medicines has led to a renewed focus on malaria elimination and eradication. Changes in the way new anti-malarial drugs are discovered and developed have led to a dramatic increase in the number and diversity of new molecules presently in pre-clinical and early clinical development. The twin challenges faced can be summarized by multi-drug resistant malaria from the Greater Mekong Sub-region, and the need to provide simplified medicines. This review lists changes in anti-malarial target candidate and target product profiles over the last 4 years...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28086840/evidence-of-multiple-insecticide-resistance-mechanisms-in-anopheles-gambiae-populations-in-bangui-central-african-republic
#3
Marina Lidwine Olé Sangba, Aboubakar Sidick, Renaud Govoetchan, Christian Dide-Agossou, Razaki A Ossè, Martin Akogbeto, Mamadou Ousmane Ndiath
BACKGROUND: Knowledge of insecticide resistance status in the main malaria vectors is an essential component of effective malaria vector control. This study presents the first evaluation of the status of insecticide resistance in Anopheles gambiae populations from Bangui, the Central African Republic. METHODS: Anopheles mosquitoes were reared from larvae collected in seven districts of Bangui between September to November 2014. The World Health Organisation's bioassay susceptibility tests to lambda-cyhalothrin (0...
January 13, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28086782/in-vivo-antiplasmodial-activity-and-toxicological-assessment-of-hydroethanolic-crude-extract-of-ajuga-remota
#4
Aschalew Nardos, Eyasu Makonnen
BACKGROUND: Malaria is one of the most life-threatening health problems worldwide and treatment has been compromised by drug resistance. Identifying lead molecules from natural products might help to find better anti-malarial drugs, since those obtained from natural sources are still effective against malarial parasites. This study aimed at investigating the in vivo antiplasmodial activity of crude extract of the leaves of Ajuga remota together with its safety in mice models. METHODS: In vivo parasite growth inhibitory effect of crude extract was assessed in mice inoculated with Plasmodium berghei (ANKA strain)...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28086777/profile-of-molecular-mutations-in-pfdhfr-pfdhps-pfmdr1-and-pfcrt-genes-of-plasmodium-falciparum-related-to-resistance-to-different-anti-malarial-drugs-in-the-bata-district-equatorial-guinea
#5
Pedro Berzosa, Andrés Esteban-Cantos, Luz García, Vicenta González, Marisa Navarro, Taiomara Fernández, María Romay-Barja, Zaida Herrador, José Miguel Rubio, Policarpo Ncogo, María Santana-Morales, Basilio Valladares, Matilde Riloha, Agustín Benito
BACKGROUND: The emergence of drug resistance in Plasmodium falciparum has been a major contributor to the global burden of malaria. Drug resistance complicates treatment, and it is one of the most important problems in malaria control. This study assessed the level of mutations in P. falciparum genes, pfdhfr, pfdhps, pfmdr1, and pfcrt, related to resistance to different anti-malarial drugs, in the Continental Region of Equatorial Guinea, after 8 years of implementing artesunate combination therapies as the first-line treatment...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28086775/rapid-decline-in-the-susceptibility-of-plasmodium-falciparum-to-dihydroartemisinin-piperaquine-in-the-south-of-vietnam
#6
Ngo Viet Thanh, Nguyen Thuy-Nhien, Nguyen Thi Kim Tuyen, Nguyen Thanh Tong, Nguyen Thuy Nha-Ca, Le Thanh Dong, Huynh Hong Quang, Jeremy Farrar, Guy Thwaites, Nicholas J White, Marcel Wolbers, Tran Tinh Hien
BACKGROUND: Artemisinin resistant Plasmodium falciparum has emerged in the countries of the Greater Mekong sub-region posing a serious threat to global malaria elimination efforts. The relationship of artemisinin resistance to treatment failure has been unclear. METHODS: In annual studies conducted in three malaria endemic provinces in the south of Vietnam (Binh Phuoc, Ninh Thuan and Gia Lai) between 2011 and 2015, 489 patients with uncomplicated P. falciparum malaria were enrolled in detailed clinical, parasitological and molecular therapeutic response assessments with 42 days follow up...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#7
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Sabroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasites lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites equivalent to the known antimalarials, chloroquine and mefloquine...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28077167/role-of-anopheles-cellia-rufipes-gough-1910-and-other-local-anophelines-in-human-malaria-transmission-in-the-northern-savannah-of-cameroon-a-cross-sectional-survey
#8
Raymond N Tabue, Parfait Awono-Ambene, Josiane Etang, Jean Atangana, Antonio-Nkondjio C, Jean C Toto, Salomon Patchoke, Rose G F Leke, Etienne Fondjo, Abraham P Mnzava, Tessa B Knox, Alexis Tougordi, Martin J Donnelly, Jude D Bigoga
BACKGROUND: As part of a study to determine the impact of insecticide resistance on the effectiveness of long-lasting insecticide treated nets (LLINs) in the north of Cameroon, the unexpectedly high density and anthropophilic behaviour of Anopheles rufipes lead us to investigate this species bionomics and role in human malaria parasite transmission. METHODS: For four consecutive years (2011-2014), annual cross-sectional sampling of adult mosquitoes was conducted during the peak malaria season (September-October) in three health districts in northern Cameroon...
January 11, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28076467/the-search-for-novel-insecticide-targets-in-the-post-genomics-era-with-a-specific-focus-on-g-protein-coupled-receptors
#9
Michelle Ngai, Mary Ann McDowell
Insects are considered pests globally, implicated in the destruction of agricultural fields and transmission of pathogens that cause deadly human diseases, such as dengue, Zika and malaria. The diversity of the insecticide arsenal has remained stagnant for decades, but the recent rise of insecticide resistance fueled the discovery of novel modes of action, and the power of genomics has reinvigorated this search. This review discusses the importance of comparative and functional insect genomics in the identification of potential gene targets for an insecticidal mode of action with low off-target toxicity...
January 1, 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28073732/insecticide-resistance-in-anopheles-mosquitoes%C3%A2-additional-obstacles-in-the-battle-against-malaria
#10
A Rubert, L Guillon-Grammatico, J Chandenier, I Dimier-Poisson, G Desoubeaux
Mosquitoes of the genus Anopheles are malaria vectors in tropical areas and were of course designated as primary targets by programs for malaria control. Repellent sprays, indoor use of insecticides, and massive delivery of mosquito nets are standard examples of the means widely used to combat malaria. This synthetic review supplies an overview of all of the modes of resistance developed by Anopheles mosquitoes against these human actions. The misuse of each available tool has gradually led to a decrease in its global effectiveness...
November 1, 2016: Médecine et Santé Tropicales
https://www.readbyqxmd.com/read/28072872/population-pharmacokinetic-properties-of-piperaquine-in-falciparum-malaria-an-individual-participant-data-meta-analysis
#11
Richard M Hoglund, Lesley Workman, Michael D Edstein, Nguyen Xuan Thanh, Nguyen Ngoc Quang, Issaka Zongo, Jean Bosco Ouedraogo, Steffen Borrmann, Leah Mwai, Christian Nsanzabana, Ric N Price, Prabin Dahal, Nancy C Sambol, Sunil Parikh, Francois Nosten, Elizabeth A Ashley, Aung Pyae Phyo, Khin Maung Lwin, Rose McGready, Nicholas P J Day, Philippe J Guerin, Nicholas J White, Karen I Barnes, Joel Tarning
BACKGROUND: Artemisinin-based combination therapies (ACTs) are the mainstay of the current treatment of uncomplicated Plasmodium falciparum malaria, but ACT resistance is spreading across Southeast Asia. Dihydroartemisinin-piperaquine is one of the five ACTs currently recommended by the World Health Organization. Previous studies suggest that young children (<5 y) with malaria are under-dosed. This study utilised a population-based pharmacokinetic approach to optimise the antimalarial treatment regimen for piperaquine...
January 2017: PLoS Medicine
https://www.readbyqxmd.com/read/28069653/the-molecular-epidemiology-of-pf-k13-mutations-in-senegal-using-targeted-amplicon-deep-sequencing
#12
Eldin Talundzic, Yaye D Ndiaye, Awa B Deme, Christian Olsen, Dhruviben S Patel, Shweta Biliya, Rachel Daniels, Fredrik O Vannberg, Sarah K Volkman, Venkatachalam Udhayakumar, Daouda Ndiaye
The emergence of Plasmodium falciparum (Pf) resistance to artemisinin in Southeast Asia threatens malaria control and elimination activities worldwide. Multiple polymorphisms in the Pf kelch gene found in chromosome 13 (Pfk13) have been associated with artemisinin resistance. Surveillance of potential drug resistance loci within a population that may emerge under increasing drug pressure is an important public health activity. In this context, P. falciparum infections from an observational surveillance study in Senegal were genotyped using targeted amplicon deep sequencing (TADS) for Pfk13 polymorphisms...
January 9, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28069075/domestic-trends-in-malaria-research-and-development-in-china-and-its-global-influence
#13
Yang-Mu Huang, Lu-Wen Shi, Rui She, Jing Bai, Shi-Yong Jiao, Yan Guo
BACKGROUND: Though many countries, including China, are moving towards malaria elimination, malaria remains a major global health threat. Due to the spread of antimalarial drug resistance and the need for innovative medical products during the elimination phase, further research and development (R&D) of innovative tools in both epidemic and elimination areas is needed. This study aims to identify the trends and gaps in malaria R&D in China, and aims to offer suggestions on how China can be more effectively involved in global malaria R&D...
January 10, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/28069024/efficient-method-for-establishing-f1-progeny-from-wild-populations-of-anopheles-mosquitoes
#14
Thiery N Nepomichene, Lala Andrianaivolambo, Sébastien Boyer, Catherine Bourgouin
BACKGROUND: The changing malaria situation in Madagascar requires additional knowledge on the physiology and behaviour of local mosquito vectors. However, the absence of established colonies for several anopheline species present in Madagascar constitutes a limiting factor. To avoid labour intensive work and uncertainty for success of establishing Anopheles colonies from Malagasy species, field collections of blood-fed females and in-tube forced oviposition were combined to reliably produce large numbers of F1 progeny...
January 9, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28067439/the-anopheles-gambiae-transcriptome-a-turning-point-for-malaria-control
#15
REVIEW
A Domingos, R Pinheiro-Silva, J Couto, V do Rosário, J de la Fuente
Mosquitoes are important vectors of several pathogens and thereby contribute to the spread of diseases, with social, economic and public health impacts. Amongst the approximately 450 species of Anopheles, about 60 are recognized as vectors of human malaria, the most important parasitic disease. In Africa, Anopheles gambiae is the main malaria vector mosquito. Current malaria control strategies are largely focused on drugs and vector control measures such as insecticides and bed-nets. Improvement of current, and the development of new, mosquito-targeted malaria control methods rely on a better understanding of mosquito vector biology...
January 9, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28056979/malaria-epidemiology-in-central-myanmar-identification-of-a-multi-species-asymptomatic-reservoir-of-infection
#16
Isaac Ghinai, Jackie Cook, Teddy Tun Win Hla, Hein Myat Thu Htet, Tom Hall, Inke Nd Lubis, Rosanna Ghinai, Therese Hesketh, Ye Naung, Mya Mya Lwin, Tint Swe Latt, David L Heymann, Colin J Sutherland, Chris Drakeley, Nigel Field
BACKGROUND: The spread of artemisinin-resistant Plasmodium falciparum is a global health concern. Myanmar stands at the frontier of artemisinin-resistant P. falciparum. Myanmar also has the highest reported malaria burden in Southeast Asia; it is integral in the World Health Organization's plan to eliminate malaria in Southeast Asia, yet few epidemiological data exist for the general population in Myanmar. METHODS: This cross-sectional, probability household survey was conducted in Phyu township, Bago Region (central Myanmar), during the wet season of 2013...
January 5, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28056932/in-vivo-antimalarial-activity-of-crude-extracts-and-solvent-fractions-of-leaves-of-strychnos-mitis-in-plasmodium-berghei-infected-mice
#17
Selamawit Fentahun, Eyasu Makonnen, Tesfaye Awas, Mirutse Giday
BACKGROUND: Malaria is a major public health problem in the world which is responsible for death of millions particularly in sub-Saharan Africa. Today, the control of malaria has become gradually more complex due to the spread of drug-resistant parasites. Medicinal plants are the unquestionable source of effective antimalarials. The present study aimed to evaluate antiplasmodial activity and acute toxicity of the plant Strychnos mitis in Plasmodium berghei infected mice. METHODS: Standard procedures were employed to investigate acute toxicity and 4-day suppressive effect of crude aqueous and hydro-methanolic extracts of the leaves of Strychnos mitis against P...
January 5, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28043395/artesunate-tafenoquine-combination-therapy-promotes-clearance-and-abrogates-transmission-of-the-avian-malaria-parasite-plasmodium-gallinaceum
#18
Suchada Tasai, Tawee Saiwichai, Morakot Kaewthamasorn, Sonthaya Tiawsirisup, Prayute Buddhirakkul, Sirintip Chaichalotornkul, Sittiporn Pattaradilokrat
Clinical manifestations of malaria infection in vertebrate hosts arise from the multiplication of the asexual stage parasites in the blood, while the gametocytes are responsible for the transmission of the disease. Antimalarial drugs that target the blood stage parasites and transmissible gametocytes are rare, but are essentially needed for the effective control of malaria and for limiting the spread of resistance. Artemisinin and its derivatives are the current first-line antimalarials that are effective against the blood stage parasites and gametocytes, but resistance to artemisinin has now emerged and spread in various malaria endemic areas...
January 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28042865/the-role-of-natural-products-in-drug-discovery-and-development-against-neglected-tropical-diseases
#19
REVIEW
Peter Mubanga Cheuka, Godfrey Mayoka, Peggoty Mutai, Kelly Chibale
Endemic in 149 tropical and subtropical countries, neglected tropical diseases (NTDs) affect more than 1 billion people annually, including 875 million children in developing economies. These diseases are also responsible for over 500,000 deaths per year and are characterized by long-term disability and severe pain. The impact of the combined NTDs closely rivals that of malaria and tuberculosis. Current treatment options are associated with various limitations including widespread drug resistance, severe adverse effects, lengthy treatment duration, unfavorable toxicity profiles, and complicated drug administration procedures...
December 31, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28040597/marine-actinobacteria-as-a-drug-treasure-house
#20
REVIEW
Syed Shams Ul Hassan, Abdul Lateef Shaikh
Marine actinobacteria have been considered as a gold mine with respect to great potential regarding their secondary metabolites. Most of the researches have been conducted on actinobacteria's derived secondary metabolites to examine its pharmacological properties. Actinobacteria have a potential to provide future drugs against crucial diseases, such as drug-resistance bacteria, cancer, a range of viral illnesses, malaria, several infections and inflammations. Although, the mode of action of many bio molecules are still untapped, for a tangible number of compounds by which they interfere with human pathogenesis are reported here with detailed diagrammed illustrations...
December 29, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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