Article
Multidisciplinary Sciences
Celia Miguel-Blanco, James M. Murithi, Ernest Diez Benavente, Fiona Angrisano, Katarzyna A. Sala, Donelly A. van Schalkwyk, Manu Vanaerschot, Frank Schwach, Matthew J. Fuchter, Oliver Billker, Colin J. Sutherland, Susana G. Campino, Taane G. Clark, Andrew M. Blagborough, David A. Fidock, Esperanza Herreros, Francisco Javier Gamo, Jake Baum, Michael J. Delves
Summary: New antimalarial therapeutics are urgently needed to combat emerging parasite and mosquito resistance. Intense drug screening efforts have identified promising new antimalarial molecules with novel modes of action to combat existing drug resistance.
SCIENTIFIC REPORTS
(2021)
Review
Chemistry, Medicinal
Preeti Kushwaha, Vipin Kumar, Biswajit Saha
Summary: beta-Carboline alkaloids are important nitrogen-based natural alkaloids and therapeutic molecules that exhibit various pharmacological activities through diverse mechanisms. There has been increasing attention towards developing effective antimalarial drugs based on this compound. This article comprehensively reviews the clinical and preclinical antimalarial scaffolds containing beta-carboline structure. The study focuses on the natural and semi-synthetic analogues of beta-carbolines reported in the last decade (2011-2021), providing insights into their mechanisms of action and potential for future therapeutic development.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Nanoscience & Nanotechnology
Xinyi Wang, Yiwei Xie, Ning Jiang, Jingyi Wang, Hongrui Liang, Dingyuan Liu, Na Yang, Xiaoyu Sang, Ying Feng, Ran Chen, Qijun Chen
Summary: This study developed a targeted drug delivery system for malaria treatment by preparing ferrite nanoparticles with ferromagnetic properties and loading them with artemisinin and heparin. The nanoparticles effectively targeted parasite-infected erythrocytes and interfered with the release of merozoites, enhancing the inhibitory efficacy of the antimalarial drug. Furthermore, the heparin-coated nanoparticles showed stronger blocking capability against malaria compared to free heparin due to multivalent interactions with surface receptors on merozoites.
ACS APPLIED MATERIALS & INTERFACES
(2021)
Article
Multidisciplinary Sciences
Arne Alder, Cecilia P. Sanchez, Matthew R. G. Russell, Lucy M. Collinson, Michael Lanzer, Michael J. Blackman, Tim-Wolf Gilberger, Joachim M. Matz
Summary: Malaria parasites use a complex to acidify the digestive vacuole and degrade host erythrocyte hemoglobin, which is essential for their survival in the human bloodstream.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Microbiology
Heather J. Painter, Joanne M. Morrisey, Michael W. Mather, Lindsey M. Orchard, Cuyler Luck, Martin J. Smilkstein, Michael K. Riscoe, Akhil B. Vaidya, Manuel Llinas
Summary: The emergence of drug-resistant Plasmodium falciparum parasites poses a challenge to global malaria eradication efforts, highlighting the importance of identifying new antimalarial drugs. Studying the molecular mechanism of drug resistance has revealed a novel resistance mechanism that could potentially guide the development of future antimalarial combination therapies.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Microbiology
James S. McCarthy, Azrin N. Abd-Rahman, Katharine A. Collins, Louise Marquart, Paul Griffin, Anne Kummel, Aline Fuchs, Cornelis Winnips, Vishal Mishra, Katalin Csermak-Renner, J. Prakash Jain, Preetam Gandhi
Summary: The new antimalarial compound cipargamin showed antimalarial activity in healthy volunteers infected with blood-stage Plasmodium falciparum, although some subjects experienced serious liver function changes during treatment. Further evaluation of the compound's hepatic safety profile is needed despite the promising antimalarial activity observed.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Review
Chemistry, Medicinal
Lekkala Ravindar, Siti Aishah Hasbullah, K. P. Rakesh, Nurul Izzaty Hassan
Summary: Malaria is a deadly parasitic infection ranked as the fifth most lethal worldwide. Antimalarial medications are crucial for preventing and eradicating malaria. The 4-aminoquinoline moiety has diverse biological applications and has been favored in antimalarial drug discovery. This review focuses on its efficacy when hybridized with various heterocyclic scaffolds, aiding the development of more effective antimalarial agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Microbiology
Fidelia Ijeoma Uche, Xiaozhen Guo, Jude Okokon, Imran Ullah, Paul Horrocks, Joshua Boateng, Chenggang Huang, Wen-Wu Li
Summary: This study investigates the in vitro and in vivo antiplasmodial activities of BBIQ alkaloids and their analogues, showing promising results with significant anti-parasitic effects at low concentrations. Cycleanine and its semisynthetic analogues demonstrate improved potency and selectivity, with potential as leads for further drug development.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Plant Sciences
Hae Soo Yun, Sylvatrie-Danne Dinzouna-Boutamba, Sanghyun Lee, Zin Moon, Dongmi Kwak, Dong-Il Chung, Yeonchul Hong, Man Hee Rhee, Youn-Kyoung Goo
Summary: The extract of Petasites japonicus shows potential antimalarial effects by inhibiting the proliferation of Plasmodium parasites and improving hematological parameters. These effects may be attributed to the inhibition of platelet activation related to attenuated glycoprotein VI downstream signaling.
Article
Chemistry, Multidisciplinary
Usama Ramadan Abdelmohsen, Soad A. L. Bayoumi, Nesma M. Mohamed, Yaser A. Mostafa, Che J. Ngwa, Gabriele Pradel, Salwa F. Farag
Summary: Malaria is a dangerous parasitic disease, and new antimalarial drugs are urgently needed. Natural products, particularly phenylpropanoids, have shown potential as antimalarial agents. In this study, in silico analysis and in vitro assays were conducted to assess the antimalarial activity of naturally-occurring phenylpropanoids.
Article
Immunology
Bridget E. Barber, Azrin N. Abd-Rahman, Rebecca Webster, Adam J. Potter, Stacey Llewellyn, Louise Marquart, Nischal Sahai, Indika Leelasena, Geoffrey W. Birrell, Michael D. Edstein, G. Dennis Shanks, David Wesche, Joerg J. Moehrle, James S. McCarthy
Summary: A single oral dose of tafenoquine is effective against blood-stage Plasmodium falciparum infection, but prior screening for glucose 6-phosphate dehydrogenase deficiency is necessary due to the estimated dose required to clear asexual parasitaemia being >= 460 mg (in adults).
CLINICAL INFECTIOUS DISEASES
(2023)
Article
Microbiology
Hae-Soo Yun, Sylvatrie-Danne Dinzouna-Boutamba, Sanghyun Lee, Zin Moon, Dongmi Kwak, Man-Hee Rhee, Dong-Il Chung, Yeonchul Hong, Youn-Kyoung Goo
Summary: The study evaluated the antimalarial activity of Ranunculus japonicus extract against different strains of malaria parasites, showing significant inhibition of both chloroquine-sensitive and resistant strains. In infected mice, the extract demonstrated potent antimalarial activity with improved hepatic, renal, and hematologic parameters, indicating no apparent toxicity.
Article
Infectious Diseases
Sangdao Somsri, Mathirut Mungthin, Natthaporn Klubthawee, Poom Adisakwattana, Warunee Hanpithakpong, Ratchaneewan Aunpad
Summary: Mitochondria are considered a novel drug target due to their key role in energy production and programmed cell death. A mitochondria-penetrating peptide, (F(x)r)(3), showed potent and selective antimalarial activity by entering malaria-infected red cells and targeting the parasite mitochondria without significant toxicity to mammalian cells. This study provides a first report on the antimalarial activity of (F(x)r)(3) and its rapid killing activity compared to the known drug atovaquone.
Article
Medicine, General & Internal
Rachel Weitzman, Ortal Calfon-Peretz, Trishna Saha, Naamah Bloch, Karin Ben Zaken, Avi Rosenfeld, Moshe Amitay, Abraham O. Samson
Summary: Malaria is a prevalent parasitic disease that kills between one and two million people, mostly children, every year. Most antimalarial drugs exhibit cyclic resistance patterns, supporting the use of combination therapy with multiple antimalarial drugs.
JOURNAL OF CLINICAL MEDICINE
(2022)
Article
Infectious Diseases
Hanna Y. Ehrlich, Fabrice Some, Thomas Bazie, Catherine Neya Ebou, Estelle Lotio Dembele, Richard Balma, Justin Goodwin, Martina Wade, Amy K. Bei, Jean-Bosco Ouedraogo, Brian Foy, Roch K. Dabire, Sunil Parikh
Summary: This study aimed to assess the feasibility of using blood fed mosquitos for surveillance of antimalarial drug resistance in southwest Burkina Faso. The study found that molecular markers in both human blood samples and mosquito blood meals exhibited similar temporal trends, but the frequencies were not statistically equivalent in all scenarios. Further research is needed to determine empirical and pragmatic thresholds of difference. Xenomonitoring could be an efficient tool for rapid surveillance of emerging antimalarial resistance in regions with insufficient surveillance.
Article
Microbiology
Gowtham Subramanian, Meenakshi A. Belekar, Anurag Shukla, Jie Xin Tong, Ameya Sinha, Trang T. T. Chu, Akshay S. Kulkarni, Peter R. Preiser, D. Srinivasa Reddy, Kevin S. W. Tan, Dhanasekaran Shanmugam, Rajesh Chandramohanadas
Article
Chemistry, Organic
Akshay S. Kulkarni, Rahul D. Shingare, Rambabu Dandela, D. Srinivasa Reddy
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2018)
Article
Chemistry, Multidisciplinary
Gaetan Bayiha Ba Njock, Trixie Ann Bartholomeusz, Dominique Ngono Bikobo, Mohammadali Foroozandeh, Rupali Shivapurkar, Philippe Christen, Dieudonne Emmanuel Pegnyemb, Damien Jeannerat
HELVETICA CHIMICA ACTA
(2013)
Article
Biochemistry & Molecular Biology
Rupali Shivapurkar, Cleiton M. Souza, Damien Jeannerat, Howard Riezman
JOURNAL OF LIPID RESEARCH
(2011)
Article
Chemistry, Multidisciplinary
Akshay S. Kulkarni, Remya Ramesh, Safal Walia, Shahebaz Sayyad, Ganesh B. Gathalkar, Seetharamsing Balamkundu, Manali Joshi, Avalokiteswar Sen, D. Srinivasa Reddy
Summary: Personal protection to control mosquitoes is an effective way to prevent deadly diseases, but the gold standard mosquito repellent DEET is facing resistance from mosquitoes. Researchers have synthesized a novel series of silicon-containing acyl piperidines and found some compounds with good mosquito-repellent properties.
Article
Chemistry, Multidisciplinary
Rahul D. Shingare, Akshay S. Kulkarni, Revannath L. Sutar, D. Srinivasa Reddy