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1. Assessing risks of Plasmodium falciparum resistance to select next-generation antimalarials

Author:
Maëlle Duffey; Benjamin Blasco; Jeremy N. Burrows; Timothy N.C. Wells; David A. Fidock; Didier Leroy
Source:
Trends in parasitology 2021 v.37 no.8 pp. 709-721
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; Plasmodium falciparum; antibiotic resistance genes; drug design; drug resistance; parasitology; therapeutics;     Show all 7 Subjects
Abstract:
... Strategies to counteract or prevent emerging drug resistance are crucial for the design of next-generation antimalarials. In the past, resistant parasites were generally identified following treatment failures in patients, and compounds would have to be abandoned late in development. An early understanding of how candidate therapeutics lose efficacy as parasites evolve resistance is important ...
DOI:
10.1016/j.pt.2021.04.006

2. Repurposing Antimalarials to Tackle the COVID-19 Pandemic

Author:
Sanjeev Krishna; Yolanda Augustin; Jigang Wang; Chengchao Xu; Henry M. Staines; Hans Platteeuw; Adeeba Kamarulzaman; Amadou Sall; Peter Kremsner
Source:
Trends in parasitology 2021 v.37 no.1 pp. 8-11
ISSN:
1471-4922
Subject:
Coronavirus infections; Severe acute respiratory syndrome coronavirus; anti-inflammatory activity; clinical trials; interleukin-6; pandemic; parasitology; pyronaridine
Abstract:
... Artemisinin-based combination therapies (ACTs) have demonstrated in vitro inhibition of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Artemisinins have also shown anti-inflammatory effects, including inhibition of interleukin-6 (IL-6) that plays a key role in the development of severe coronavirus disease 2019 (COVID-19). There is now sufficient evidence for the effectiveness of ACT ...
DOI:
10.1016/j.pt.2020.10.003

3. In silico evaluation of the compounds of the ayurvedic drug, AYUSH-64, for the action against the SARS-CoV-2 main protease

Author:
Thrigulla Saketh Ram; Manne Munikumar; Vankudavath Naik Raju; Parasannanavar Devaraj; Naveen Kumar Boiroju; Rajkumar Hemalatha; P.V.V. Prasad; Manohar Gundeti; Brijesh S. Sisodia; Sharad Pawar; G.P. Prasad; Mukesh Chincholikar; Sumeet Goel; Anupam Mangal; Sudesh Gaidhani; N. Srikanth; K.S. Dhiman
Source:
Journal of Ayurveda and integrative medicine 2022 v.13 no.1 pp. 100413
ISSN:
0975-9476
Subject:
antimalarials,   etc   ; Alstonia scholaris; Ayurvedic medicine; COVID-19 infection; Severe acute respiratory syndrome coronavirus 2; antiviral agents; computer simulation; computer software; energy; lead; ligands; molecular dynamics; pandemic; proteinases; public health; vaccines; viruses; India;     Show all 18 Subjects
Abstract:
... Outbreak of Corona Virus Disease in late 2019 (COVID-19) has become a pandemic global Public health emergency. Since there is no approved anti-viral drug or vaccine declared for the disease and investigating existing drugs against the COVID-19.AYUSH-64 is an Ayurvedic formulation, developed and patented by Central Council of Research in Ayurvedic Sciences, India, has been in clinical use as anti-m ...
DOI:
10.1016/j.jaim.2021.02.004

4. Plants used traditionally as antimalarials in Latin America: Mining the tree of life for potential new medicines

Author:
William Milliken; Barnaby E. Walker; Melanie-Jayne R. Howes; Félix Forest; Eimear Nic Lughadha
Source:
Journal of ethnopharmacology 2021 v.279 pp. 114221
ISSN:
0378-8741
Subject:
Aristolochia; Aspidosperma; Cinchona; Croton; Liliopsida; Momordica; Piper; Plasmodium; Solanum; Stachytarpheta; artemisinin; drug resistance; ethnobotany; flora; geographical distribution; health services; herbaria; indigenous species; malaria; people; phylogeny; therapeutics; traditional medicine; trees; Latin America
Abstract:
... Malaria remains a serious and challenging disease. Traditional antimalarial medicines are largely based on plants, and ethnopharmacological research has inspired the development of antimalarial pharmaceuticals such as artemisinin. Antimalarial drug resistance is an increasing problem in Plasmodium species, and new therapeutic strategies to combat malaria are needed. Although the number of malaria ...
DOI:
10.1016/j.jep.2021.114221

5. Plasmodium stage-selective antimalarials from Lophira lanceolata stem bark

Author:
Harouna Soré; Annalisa Lopatriello; Yehenew A. Ebstie; Alain R. Tenoh Guedoung; Adama Hilou; José A. Pereira; Anake Kijjoa; Annette Habluetzel; Orazio Taglialatela-Scafati
Source:
Phytochemistry 2020 v.174 pp. 112336
ISSN:
0031-9422
Subject:
antimalarials,   etc   ; Culicidae; Lophira lanceolata; Plasmodium; bark; glycosylation; humans; malaria; mass spectrometry; medicinal plants; moieties; nuclear magnetic resonance spectroscopy; parasites; phytochemicals;     Show all 14 Subjects
Abstract:
... Targeting the transmissible stages of the Plasmodium parasite that develop in the human and mosquito host is a crucial strategy for malaria control and elimination. Medicinal plants offer a prolific source for the discovery of new antimalarial compounds. The recent identification of the gametocytocidal activity of lophirone E, obtained from the African plant Lophira lanceolata (Ochnaceae ...
DOI:
10.1016/j.phytochem.2020.112336

6. MalDA, Accelerating Malaria Drug Discovery

Author:
Tuo Yang; Sabine Ottilie; Eva S. Istvan; Karla P. Godinez-Macias; Amanda K. Lukens; Beatriz Baragaña; Brice Campo; Chris Walpole; Jacquin C. Niles; Kelly Chibale; Koen J. Dechering; Manuel Llinás; Marcus C.S. Lee; Nobutaka Kato; Susan Wyllie; Case W. McNamara; Francisco Javier Gamo; Jeremy Burrows; David A. Fidock; Daniel E. Goldberg; Ian H. Gilbert; Dyann F. Wirth; Elizabeth A. Winzeler; the Malaria Drug Accelerator Consortium
Source:
Trends in parasitology 2021 v.37 no.6 pp. 493-507
ISSN:
1471-4922
Subject:
antimalarials,   etc   ; lead; malaria; parasitology;     Show all 4 Subjects
Abstract:
... The Malaria Drug Accelerator (MalDA) is a consortium of 15 leading scientific laboratories. The aim of MalDA is to improve and accelerate the early antimalarial drug discovery process by identifying new, essential, druggable targets. In addition, it seeks to produce early lead inhibitors that may be advanced into drug candidates suitable for preclinical development and subsequent clinical testing ...
DOI:
10.1016/j.pt.2021.01.009

7. Structure Elucidation and Confirmation of Phloroglucinols from the Roots of Garcinia dauphinensis by Comparison of Experimental and Calculated ECD Spectra and Specific Rotations

Author:
Kirk C. Pearce; Rolly G. Fuentes; Susana Calderon; Rageshwari Marolikar; David G. I. Kingston; T. Daniel Crawford
Source:
Journal of natural products 2021 v.84 no.4 pp. 1163-1174
ISSN:
1520-6025
Subject:
antimalarials,   etc   ; Garcinia; stereochemistry; stereoisomers;     Show all 4 Subjects
Abstract:
... Eight phloroglucinols from Garcinia dauphinensis were recently reported to have good to moderate antiplasmodial and anticancer activities, consistent with other phloroglucinol derivatives isolated from natural sources. Chiroptical properties were previously calculated and compared to experimental data for compound 2 as a means to deduce its absolute configuration. Tentative assignments for the rem ...
DOI:
10.1021/acs.jnatprod.0c01208

8. Two new bisindole alkaloids from Tabernaemontana macrocarpa Jack

Author:
Puteri Amelia; Alfarius Eko Nugroho; Yusuke Hirasawa; Toshio Kaneda; Takahiro Tougan; Toshihiro Horii; Hiroshi Morita
Source:
Natural medicines 2021 v.75 no.3 pp. 633-642
ISSN:
1340-3443
Subject:
antimalarials,   etc   ; Plasmodium falciparum; Tabernaemontana; bark; spectroscopy;     Show all 5 Subjects
Abstract:
... . Bisnaecarpamine A exhibited potent antimalarial activity against Plasmodium falciparum 3D7 strain with IC₅₀ value of 28.8 µM. ...
DOI:
10.1007/s11418-021-01510-4

9. Asymmetric Total Synthesis and Biosynthetic Implications of Perovskones, Hydrangenone, and Hydrangenone B

Author:
Baochao Yang; Guoen Wen; Quan Zhang; Min Hou; Haibing He; Shuanhu Gao
Source:
Journal of the American Chemical Society 2021 v.143 no.17 pp. 6370-6375
ISSN:
1520-5126
Subject:
antimalarials,   etc   ; Salvia; biosynthesis; cycloaddition reactions; triterpenoids;     Show all 5 Subjects
Abstract:
... Perovskones and hydrangenones are a family of structurally complex triterpenoids that were mainly isolated from the genus Salvia medicinal plants. These isoprenoids exhibit a broad range of biological activities, such as antitumor and antiplasmodial activities. Here, we report the collective total synthesis of perovskone, perovskones C, D, F, hydrangenone, and hydrangenone B. The key strategies in ...
DOI:
10.1021/jacs.1c02674

10. Antiplasmodial Compounds from Deep-Water Marine Invertebrates

Author:
Amy E. Wright; Jennifer E. Collins; Bracken Roberts; Jill C. Roberts; Priscilla L. Winder; John K. Reed; Maria Cristina Diaz; Shirley A. Pomponi; Debopam Chakrabarti
Source:
Marine drugs 2021 v.19 no.4 pp. -
ISSN:
1660-3397
Subject:
antimalarials,   etc   ; Plasmodium falciparum; diterpenoids; fractionation; malaria; parasites; schizogony; therapeutics;     Show all 8 Subjects
Abstract:
... at the schizont stage if added any time prior to late schizogony at 42 hours post invasion, (HPI). In contrast, early life cycle exposure to nitenin (prior to 18 HPI) was identified as crucial to parasite inhibition, suggesting nitenin may target the maturation of the parasite during the transition from ring to early trophozoite (6–18 HPI), a novel property among known antimalarials. ...
DOI:
10.3390/md19040179

11. My 60-Year Love Affair with Natural Products

Author:
David G. I. Kingston
Source:
Journal of natural products 2021 v.84 no.3 pp. 932-948
ISSN:
1520-6025
Subject:
antimalarials,   etc   ; antineoplastic agents; biosynthesis; chemistry; insects; paclitaxel;     Show all 6 Subjects
Abstract:
... The author describes his 60-year career in studying the chemistry of natural products, which includes structural, synthetic, and biosynthetic studies of natural products ranging from insect pigments, antibiotics, and fecal mutagens to taxol and other anticancer natural products as well as antimalarial natural products. One of the compounds discussed, napabucasin, is now an anticancer drug ...
DOI:
10.1021/acs.jnatprod.0c01237

12. Total Synthesis and Computational Investigations of Sesquiterpene-Tropolones Ameliorate Stereochemical Inconsistencies and Resolve an Ambiguous Biosynthetic Relationship

Author:
Christopher Y. Bemis; Chad N. Ungarean; Alexander S. Shved; Cooper S. Jamieson; Taehwan Hwang; Ken S. Lee; K. N. Houk; David Sarlah
Source:
Journal of the American Chemical Society 2021 v.143 no.15 pp. 6006-6017
ISSN:
1520-5126
Subject:
antimalarials,   etc   ; biosynthesis; diastereoselectivity; meroterpenoids; metabolites; sesquiterpenoids; stereochemistry;     Show all 7 Subjects
Abstract:
... The sesquiterpene-tropolones belong to a distinctive structural class of meroterpene natural products with impressive biological activities, including anticancer, antifungal, antimalarial, and antibacterial. In this article, we describe a concise, modular, and cycloaddition-based approach to a series of sesquiterpene mono- and bistropolones, including (−)-epolone B, (+)-isoepolone B ...
DOI:
10.1021/jacs.1c02150

13. Bisindole alkaloids from Voacanga grandifolia leaves

Author:
Alfarius Eko Nugroho; Yurika Ono; Eunji Jin; Yusuke Hirasawa; Toshio Kaneda; Abdul Rahman; Idha Kusumawati; Takahiro Tougan; Toshihiro Horii; Noor Cholies Zaini; Hiroshi Morita
Source:
Natural medicines 2021 v.75 no.2 pp. 408-414
ISSN:
1340-3443
Subject:
antimalarials,   etc   ; Plasmodium falciparum; Voacanga; cytotoxicity; human cell lines;     Show all 5 Subjects
Abstract:
... Two new bisindole alkaloids, 12′-O-demethyl-vobtusine-5-lactam and isovobtusine-N-oxide (1 and 2), were isolated from the leaves of Voacanga grandifolia, together with two known bisindole alkaloids. Their structures were elucidated on the basis of 1D and 2D NMR data. 1 and 2 showed potent antimalarial activity against Plasmodium falciparum 3D7 and very low cytotoxic activity against a human cell ...
DOI:
10.1007/s11418-020-01475-w

14. Current methods for the detection of antimalarial drug resistance in Plasmodium parasites infecting humans

Author:
Lucinda Slater; Martha Betson; Shoaib Ashraf; Neil Sargison; Umer Chaudhry
Source:
Acta tropica 2021 v.216 pp. 105828
ISSN:
0001-706X
Subject:
antimalarials,   etc   ; Plasmodium; blood; disease surveillance; drug resistance; epidemiology; malaria;     Show all 7 Subjects
Abstract:
... Malaria is the world's deadliest parasitic disease. Great progress has been made in the fight against malaria over the past two decades, but this has recently begun to plateau, in part due to the global development of antimalarial drug resistance. The ability to track drug resistance is necessary to achieve progress in treatment, disease surveillance and epidemiology, which has prompted ...
DOI:
10.1016/j.actatropica.2021.105828

15. The Amaryllidaceae alkaloids haemanthamine, haemanthidine and their semisynthetic derivatives as potential drugs

Author:
Lucie Cahlíková; Ippei Kawano; Martina Řezáčová; Gerald Blunden; Daniela Hulcová; Radim Havelek
Source:
Phytochemistry reviews 2021 v.20 no.1 pp. 303-323
ISSN:
1568-7767
Subject:
antimalarials,   etc   ; Amaryllidaceae; anticonvulsants; antioxidants; enzymes; medicine; metabolites; plant biochemistry;     Show all 8 Subjects
Abstract:
... Plants of the Amaryllidaceae family, have a wide distribution through both tropical and sub-tropical regions of the world. They have also a long and notable place in the history of traditional and Western medicine. Amaryllidaceae alkaloids are a structurally diverse group of plant metabolites with a wide range of biological properties including antimalarial, antitumor, antimicrobial, antiviral ...
DOI:
10.1007/s11101-020-09675-8

16. Antimicrobial, antimalarial, and cytotoxic substances from the insect pathogenic fungus Beauveria asiatica BCC 16812

Author:
Jittra Kornsakulkarn; Thapanee Pruksatrakul; Panida Surawatanawong; Chattawat Thangsrikeattigun; Somjit Komwijit; Nattawut Boonyuen; Chawanee Thongpanchang
Source:
Phytochemistry letters 2021 v.43 pp. 8-15
ISSN:
1874-3900
Subject:
antimalarials,   etc   ; Beauveria; cytotoxicity; entomopathogenic fungi; picolinic acid; plant biochemistry; spectroscopy;     Show all 7 Subjects
Abstract:
... by the application of modified Mosher’s method and ECD calculation. Compounds 9–11 exhibited antimalarial (IC₅₀ 0.47–1.79 u g/mL), antimicrobial (MIC 3.13–50.0 u g/mL), and cytotoxic (IC₅₀ 0.26–1.23 u g/mL) activities, while compounds 1, 2, 8, and 14 showed only cytotoxicity against Vero cell lines, with IC₅₀ values range 12.96–47.03 u g/mL. ...
DOI:
10.1016/j.phytol.2021.03.003

17. Unintentional artenimol/piperaquine overdose in two children occurring without evidence of subsequent cardiotoxicity

Author:
Alexandra Tielli; Vincent Jullien; Lauren Pull; Olivier Bouchaud; Jean-Yves Siriez
Source:
International journal of antimicrobial agents 2021 v.57 no.5 pp. 106347
ISSN:
0924-8579
Subject:
antimalarials,   etc   ; blood serum; cardiotoxicity; electrophysiology; hospitals; overdose; patients; piperaquine; France;     Show all 9 Subjects
Abstract:
... At the emergency department of the Robert-Debré children's hospital in Paris, France, artenimol/piperaquine (AP) has been the first-line antimalarial treatment since September 2012. Most children receive the first dose at the hospital and return home if, after 1 hour's observation, there have been no episodes of vomiting. Here we report the case of two children, aged 11 years and 5 years ...
DOI:
10.1016/j.ijantimicag.2021.106347

18. Fast ¹⁹F Magic Angle Spinning NMR Crystallography for Structural Characterization of Fluorine-Containing Pharmaceutical Compounds

Author:
Changmiao Guo; Matthew P. Fritz; Jochem Struppe; Sebastian Wegner; John Stringer; Ivan V. Sergeyev; Caitlin M. Quinn; Angela M. Gronenborn; Tatyana Polenova
Source:
Analytical chemistry 2021 v.93 no.23 pp. 8210-8218
ISSN:
1520-6882
Subject:
antimalarials,   etc   ; analytical chemistry; crystallography; fluorine; nuclear magnetic resonance spectroscopy; spectral analysis;     Show all 6 Subjects
Abstract:
... for structural characterization of fluorine-containing crystalline pharmaceutical compounds at natural abundance, using the antimalarial fluorine-containing drug mefloquine as an example. We demonstrate the utility of 2D ¹⁹F–¹³C and ¹⁹F–¹⁹F dipolar-coupling-based correlation experiments for ¹⁹F and ¹³C resonance frequency assignment, which permit identification of crystallographically inequivalent sites ...
DOI:
10.1021/acs.analchem.1c00784

19. Computational and experimental studies on the inhibitory mechanism of hydroxychloroquine on hERG

Author:
Ran Yu; Peng Li
Source:
Toxicology 2021 v.458 pp. 152822
ISSN:
0300-483X
Subject:
antimalarials,   etc   ; adverse effects; arrhythmia; fluoroquinolones; genes; humans; potassium; potassium channels; quinoline;     Show all 9 Subjects
Abstract:
... Hydroxychloroquine (HCQ) was noted to produce severe cardiac arrhythmia, an adverse effect as its use against severe acute respiratory syndrome caused by coronavirus 2 (SAES-CoV-2). HCQ is an antimalarial drug with quinoline structure. Some other quinoline compounds, such as fluoroquinolone antibiotics (FQs), also lead to arrhythmias characterized by QT prolongation. QT prolongation is usually ...
DOI:
10.1016/j.tox.2021.152822

20. Oxidative stress mediated apoptotic potential of mefloquine on experimental trichinellosis

Author:
Dalia A. Elmehy; Howaida I.H. Ismail; Nema A. Soliman; Basma S. Amer; Heba H. Elkaliny; Ahmad A. El-Ebiary; Ghada A. Gamea
Source:
Acta tropica 2021 v.213 pp. 105760
ISSN:
0001-706X
Subject:
antimalarials,   etc   ; albendazole; antioxidants; apoptosis; biomarkers; immunohistochemistry; jejunum; muscles; oxidants; oxidative stress; trichinosis;     Show all 11 Subjects
Abstract:
... Conventional anthelmintics such as albendazole could not achieve complete cure of trichinellosis till now. The antimalarial mefloquine mediates oxidative stress and disrupts lysosomal functions leading to cell death. Therefore, the aim of this work was to investigate the effect of mefloquine on experimental acute and chronic trichinellosis and to clarify the possible mechanisms of such effects ...
DOI:
10.1016/j.actatropica.2020.105760