Background: A global death toll of 608,000 in 2022 and emerging parasite resistance to artemisinin, the mainstay of antimalarial chemotherapy derived from the Chinese herb Artemisia annua, urge the development of novel antimalarials. A clinical trial has found high antimalarial potency for aqueous extracts of A. annua as well as its African counterpart Artemisia afra, which contains only trace amounts of artemisinin. The artemisinin-independent antimalarial activity of A. afra points to the existence of other antimalarials present in the plant. However, the publication was retracted due to ethical and methodological concerns in the trial, so the only evidence for antimalarial activity of A. afra is built on in vitro studies reporting efficacy only in the microgram per milliliter range.
Hypothesis: Our study aims to shed more light on the controversy around the antimalarial activity of A. afra by assessing its efficacy in mice. In particular, we are testing the hypothesis that A. afra contains a pro-drug that is inactive in vitro but active in vivo after metabolization by the mammalian host.
Methods: Plasmodium berghei-infected mice were treated once or thrice (on three consecutive days) with various doses of A. afra, A. annua, or pure artemisinin.
Results: Aqueous powder suspensions of A. annua but not A. afra showed antimalarial activity in mice.
Conclusion: Our experiments conducted in mice do not support the pro-drug hypothesis.
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http://dx.doi.org/10.1016/j.phymed.2024.155644 | DOI Listing |
Sci Rep
January 2025
Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-University of Barcelona), Rosselló 149-153, Barcelona, 08036, Spain.
We recently characterized the potent antiplasmodial activity of the aggregated protein dye YAT2150, whose presumed mode of action is the inhibition of protein aggregation in the malaria parasite. Using single-dose and ramping methods, assays were done to select Plasmodium falciparum parasites resistant to YAT2150 concentrations ranging from 3× to 0.25× the in vitro IC of the compound (in the two-digit nM range) and performed a cross-resistance assessment in P.
View Article and Find Full Text PDFInt J Pharm
January 2025
Faculty of Pharmacy, Almarisah Madani University, Makassar, Indonesia; Department of Pharmacy and Pharmaceutical Technology, Almarisah Madani University, Makassar, Indonesia. Electronic address:
The combination of the active compounds curcumin and piperine (CP) is effective as an antimalarial; however, the solubility and bioavailability of CP are very low. This study aims to formulate CP in nanoparticles (NP), which are then fabricated into dissolving microneedles (DMN). The NPs were prepared with a concentration ratio of CP-Chitosan-So.
View Article and Find Full Text PDFLupus
January 2025
Department of Medical Education, INCMNSZ, Ciudad de Mexico, Mexico.
Background: Glucocorticoids are frequently employed in systemic lupus erythematosus (SLE) patients and play a critical role in the induction therapy of lupus nephritis (LN), despite their many side effects, including steroid-induced diabetes (SID). Information regarding SID in SLE patients is quite scant.
Purpose: The aim of this study was to determine risk factors associated with the development of SID in patients with LN.
Lupus Sci Med
January 2025
Division of Rheumatology, Department of Internal Medicine, Seoul St. Mary's Hospital, College of Medicine, The Catholic University of Korea, Seoul, Republic of Korea
Objective: Osteoporosis is a common comorbidity in patients with SLE, and bone loss in patients with SLE has a multifactorial aetiology. This study aimed to evaluate the therapeutic efficacy of denosumab in patients with SLE with osteoporosis and to analyse the factors influencing therapeutic efficacy.
Methods: A total of 166 patients with SLE with osteoporosis who initiated denosumab between January 2016 and December 2023 were included.
Eur J Med Chem
January 2025
Department of Immunology, College of Basic Medical Sciences, China Medical University, Shenyang, 110122, China. Electronic address:
Artesunate, a semisynthetic derivative of artemisinin, is not only recommended as the first-line drug for treating severe malaria but is also a significant member of Artemisinin-based Combination Therapies (ACTs), used in combination with other artemisinin derivatives for treating uncomplicated malaria. Beyond its potent anti-malarial activity, artesunate has garnered considerable attention for its pharmacological effects, which encompass broad-spectrum anti-tumor, anti-viral, and anti-inflammatory properties. It has collectively demonstrated superior drug tolerance, low toxicity, and mild side effects in cell line experiments in vitro, experimental animal models, and clinical drug researches, as a monotherapy or in combination with other agents.
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