Article
Immunology
Melissa Mairet-Khedim, Rithea Leang, Camille Marmai, Nimol Khim, Saorin Kim, Sopheakvatey Ke, Chhayleang Kauy, Nimol Kloeung, Rotha Eam, Sophy Chy, Brigitte Izac, Denis Mey Bouth, Maria Dorina Bustos, Pascal Ringwald, Frederic Ariey, Benoit Witkowski
Summary: The efficacy of artesunate-amodiaquine for uncomplicated falciparum malaria in Cambodia was found to be inadequate due to amodiaquine-resistant P. falciparum. The study identified that amodiaquine resistance was not associated with previously identified molecular markers.
CLINICAL INFECTIOUS DISEASES
(2021)
Editorial Material
Biology
Colin Sutherland, Didier Menard
Summary: A tool that analyzes the genome of parasites in the blood of malaria patients can assist policymakers in making informed decisions on how to address the increase in drug-resistant infections.
Article
Chemistry, Medicinal
Wei Liu, Chuyi Yu, Miaomiao Wang, Youyou He, Zhongjie Guo, Jin He, Ru Jiang, Qin Xu, Jianming Liang, Shengzheng Wang
Summary: Recently, the antitumor activity of artemisinin and its derivatives has been discovered. This study constructed novel Pt-IV-artesunate complexes to combine the antitumor advantages of artesunate and platinum drugs. The derivatives, especially 10f, exhibited potent in vitro antitumor activities against various cancer cell lines. Compound 10f demonstrated remarkable in vivo antitumor efficacy in a xenograft model, and also showed potent in vivo antimalarial activity. This study highlights the therapeutic potential of Pt(IV)-artesunate complexes as antitumor and antimalarial agents.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Editorial Material
Multidisciplinary Sciences
Jui A. Shah
Summary: This commentary reviews the success factors for Thailand to achieve zero malaria, focusing on effective surveillance, and discusses other measures needed to reach the goal on time.
NATURE COMMUNICATIONS
(2022)
Article
Medicine, General & Internal
Wenn-Chyau Lee, Bruce Russell, Bernett Lee, Cindy S. Chu, Aung Pyae Phyo, Kanlaya Sriprawat, Yee-Ling Lau, Francois Nosten, Laurent Renia
Summary: Brief exposure to artesunate (AS) stimulates rosetting, with AS-resistant isolates forming more rosettes rapidly for protection. Deletions in genes associated with AS-mediated rosetting are significantly selected in the parasite population, along with the K13 mutations as a marker of ART resistance.
Article
Chemistry, Medicinal
Benjamin R. Taft, Fumiaki Yokokawa, Tom Kirrane, Anne-Catherine Mata, Richard Huang, Nicole Blaquiere, Grace Waldron, Bin Zou, Oliver Simon, Subramanyam Vankadara, Wai Ling Chan, Mei Ding, Sandra Sim, Judith Straimer, Armand Guiguemde, Suresh B. Lakshminarayana, Jay Prakash Jain, Christophe Bodenreider, Christopher Thompson, Christian Lanshoeft, Wei Shu, Eric Fang, Jafri Qumber, Katherine Chan, Luying Pei, Yen-Liang Chen, Hanna Schulz, Jessie Lim, Siti Nurdiana Abas, Xiaoman Ang, Yugang Liu, Inigo Angulo-Barturen, Maria Belen Jimenez-Diaz, Francisco Javier Gamo, Benigno Crespo-Fernandez, Philip J. Rosenthal, Roland A. Cooper, Patrick Tumwebaze, Anna Caroline Campos Aguiar, Brice Campo, Simon Campbell, Jurgen Wagner, Thierry T. Diagana, Christopher Sarko
Summary: A highly potent antimalarial compound, INE963 (1), with favorable pharmacological properties, has been identified through high-throughput screening and shows potential for curing uncomplicated malaria.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Medicine, General & Internal
Dancan M. Wakoli, Bartholomew N. Ondigo, Douglas O. Ochora, Joseph G. Amwoma, Winnie Okore, Edwin W. Mwakio, Gladys Chemwor, Jackeline Juma, Raphael Okoth, Charles Okudo, Redemptah Yeda, Benjamin H. Opot, Agnes C. Cheruiyot, Dennis Juma, Amanda Roth, Benhards R. Ogutu, Daniel Boudreaux, Ben Andagalu, Hoseah M. Akala
Summary: This study investigated the susceptibility of Kenyan parasites to various antimalarials and found that while the parasites remained sensitive to Dihydroartemisinin-piperaquine and other antimalarials, the response to artemether and lumefantrine was declining.
Article
Infectious Diseases
Navaporn Posayapisit, Jutharat Pengon, Philip J. Shaw, Chairat Uthaipibull, Darin Kongkasuriyachai, Aung Pyae Phyo, Francois Nosten, Yongyuth Yuthavong, Sumalee Kamchonwongpaisan
Summary: The effectiveness of antimalarial drug P218 against artemisinin-resistant Plasmodium falciparum is still uncertain, despite its efficacy against other drug-resistant parasites.
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2023)
Article
Infectious Diseases
Najia Karim Ghanchi, Bushra Qurashi, Hadiqa Raees, Mohammad Asim Beg
Summary: The study describes single nucleotide polymorphisms in the Kelch protein propeller domain of Plasmodium falciparum associated with artemisinin resistance in Southern Pakistan. All isolates analyzed for k13 propeller allele were observed as wild-type post implementation of ACT in Pakistan. Known variants associated with reduced susceptibility to artemisinin-based combination therapy (ACT) were not found, indicating favorable conditions for anti-malarial efficacy in the region.
Article
Microbiology
Nguyen Duc Manh, Nguyen Van Thanh, Huynh Hong Quang, Nguyen Thi Thanh Van, Nguyen Ngoc San, Nguyen Chinh Phong, Geoffrey W. Birrell, Michael D. Edstein, Kimberly A. Edgel, Nicholas J. Martin, Marina Chavchich
Summary: The rise in Plasmodium falciparum resistance to dihydroartemisinin-piperaquine in Vietnam has led to the evaluation of alternative artemisinin-based combination therapies. A trial of pyronaridine-artesunate in Dak Nong province, Vietnam showed high efficacy in treating falciparum malaria, despite a high prevalence of parasites with resistance mutations to both artemisinins and piperaquine among the patients.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Review
Pharmacology & Pharmacy
Jiayun Chen, Peng Gao, Wei Xiao, Guangqing Cheng, Sanjeev Krishna, Jianyou Wang, Yin Kwan Wong, Chen Wang, Liwei Gu, Dong Hua Yang, Jigang Wang
Summary: In this study, we investigated the stage-specific mechanisms of partial resistance to artemisinin in Plasmodium falciparum carrying the Kelch13 C580Y mutation. Our findings revealed the activation and expression patterns of artemisinin targets varied at different stages and periods of parasite development, with the late trophozoite stage harboring the largest number of targets. We also identified 36 overlapping targets and demonstrated the artemisinin-insensitivity of fatty acid-associated activities in the resistant strain.
DRUG RESISTANCE UPDATES
(2023)
Article
Infectious Diseases
Sompob Saralamba, Julie A. Simpson, Noppon Choosri, Lisa White, Wirichada Pan-Ngum, Arjen M. Dondorp, Nicholas J. White
Summary: A new pharmacodynamic model of antimalarial drugs is proposed, which includes reversible parasite injury and temporary drug refractoriness, to explain the failure of frequent dosing to improve therapeutic efficacy in malaria. The model predicts and supports observed therapeutic responses.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Review
Infectious Diseases
Wan-Yu Chu, Thomas P. C. Dorlo
Summary: Pyronaridine-artesunate has been strongly recommended in the recently updated WHO Guidelines for the Treatment of Malaria in 2022 as the newest artemisinin-based combination therapy for uncomplicated Plasmodium falciparum and Plasmodium vivax malaria. It is being adopted in areas with increasing chloroquine resistance. Pyronaridine is an old antimalarial agent that inhibits the synthesis of the haemozoin pigment in the Plasmodium digestive vacuole. Its pharmacokinetic properties are influenced by its tendency to accumulate in blood cells.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Review
Pharmacology & Pharmacy
Borimas Hanboonkunupakarn, Joel Tarning, Sasithon Pukrittayakamee, Kesinee Chotivanich
Summary: The emergence of artemisinin resistance poses a major obstacle to global malaria eradication programs. However, resistant infections can still be effectively treated by modifying treatment regimens and combining with other antimalarial drugs.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Manel Ouji, Michel Nguyen, Romain Mustiere, Tony Jimenez, Jean-Michel Augereau, Francoise Benoit-Vical, Celine Deraeve
Summary: Relying on the identification of relevant malaria targets in the context of artemisinin resistance, novel drug combinations and hybrids demonstrated remarkable antimalarial activity against both artemisinin-sensitive and artemisinin-resistant Plasmodium falciparum parasites, highlighting their therapeutic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)