Plasmodium
Plasmodium parasites invade erythrocytes to access nutrients and occupy a protected intracellular niche[1]. Mechanistically, P. falciparum merozoite invasion depends on ligand-receptor interactions and regulated microneme and rhoptry secretion[2]. The apicoplast supports blood-stage growth mainly through isoprenoid precursor biosynthesis, shown by chemical rescue of parasites lacking this organelle[3]. Apicoplast-derived isoprenoids also support GPI-anchor biosynthesis, egress, and invasion in P. falciparum[4]. Compared with related apicomplexan parasites, malaria parasites use conserved host-cell entry logic but species-specific ligand-receptor interactions[1]. For experimental applications, apicoplast translation inhibitors and aminoacyl-tRNA synthetase inhibitors provide tools to test delayed death, organelle maintenance, and parasite viability[5][6].
Références:
- [1]. Cowman AF, et al. Invasion of red blood cells by malaria parasites. Cell. 2006 Feb 24;124(4):755-66. [Content Brief]
- [2]. Singh S, et al. Distinct external signals trigger sequential release of apical organelles during erythrocyte invasion by malaria parasites. PLoS Pathog. 2010 Feb 5;6(2):e1000746. [Content Brief]
- [3]. Yeh E, et al. Chemical rescue of malaria parasites lacking an apicoplast defines organelle function in blood-stage Plasmodium falciparum. PLoS Biol. 2011 Aug;9(8):e1001138. [Content Brief]
- [4]. Bulloch MS, et al. Apicoplast-derived isoprenoids are essential for biosynthesis of GPI protein anchors, and consequently for egress and invasion in Plasmodium falciparum. PLoS Pathog. 2024 Sep 6;20(9):e1012484. [Content Brief]
- [5]. Pasaje CF, et al. Selective inhibition of apicoplast tryptophanyl-tRNA synthetase causes delayed death in Plasmodium falciparum. Sci Rep. 2016 Jun 9;6:27531. [Content Brief]
- [6]. Herman JD, et al. The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs. Sci Transl Med. 2015 May 20;7(288):288ra77. [Content Brief]
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Plasmodium Produits associés (265)
Produits associés (265)
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Aristolactam A II
0 ImagesCat. No.: HY-N2891CAS No.: 53948-07-5Synonyms: Aristololactam A IIAristolactam A II (Aristololactam A II) is a weak COX inhibitor with cytotoxic and anti-plasmodial activities. Aristolactam A II exhibits inhibitory activity against Chloroquine (HY-17589A)-sensitive strains, and exerts its inhibitory effect on Plasmodium falciparum growth by inducing cell membrane damage marked by LDH release. Aristolactam A II can be applied to the research of malaria-related mechanisms.
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Eriodictyol chalcone
0 ImagesCat. No.: HY-N9551CAS No.: 14917-41-0Eriodictyol chalcone is an antioxidant that inhibits multiple key enzymes including 5-LOX (IC50=0.043 μM), aromatase/CYP19A1 (IC50=2.8 μM), PTPase 1B (IC50=1.26 μM), and COX (IC50=34 μM). Eriodictyol chalcone exhibits excellent free radical scavenging activity. Eriodictyol chalcone not only inhibits the growth of plasmodia and enhances the efficacy of Artemisinin (HY-B0094), but also reduces depression-like behaviors in animal models. Eriodictyol chalcone serves as a biosynthetic precursor for Aureusidin (HY-N9834). Eriodictyol chalcone is a potential dietary supplement and herbicide, and it can be applied to research on malaria, depression, breast cancer and other related diseases.
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Eschweilenol C
0 ImagesCat. No.: HY-N12352CAS No.: 211371-02-7Eschweilenol C is a selective Plasmodium falciparum growth inhibitor. Eschweilenol C disrupts haemoglobin metabolism, reduces haemozoin production, kills Plasmodium falciparum ring and trophozoite stages. Eschweilenol C can be used for the research of inflammatory disorders and malaria.
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Cheilanthifoline
0 ImagesCheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively.
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Alstonine
0 ImagesAlstonine is a major indole alkaloid compound of a plant-based remedy. Alstonine has antipsychotic, anxiolytic, anticancer and antimalarial properties.
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Norcaesalpinin E
0 ImagesCat. No.: HY-N7583CAS No.: 854038-96-3Norcaesalpinin E, a C-17-norcassane-type diterpene found in Caesalpinia crista, is a Plasmodium falciparum growth inhibitor with an IC50 of 90 nM. Norcaesalpinin E induces dose-dependent growth inhibition of Plasmodium falciparum. Norcaesalpinin E can be used for the research of malaria.
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4-Propylcatechol
0 Images4-Propylcatechol is an Allylpyrocatechol (HY-124127) analog. 4-Propylcatechol shows anti-malarial activity against Plasmodium falciparum CDC-1 with an IC50 of 32 µM.
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(S)-Hydroxychloroquine
0 ImagesCat. No.: HY-B1370ACAS No.: 137433-24-0Synonyms: (S)-HCQ(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine. Hydroxychloroquine, a synthetic antimalarial agent, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro.
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(R)-Hydroxychloroquine
0 ImagesCat. No.: HY-B1370BCAS No.: 137433-23-9Synonyms: (R)-HCQ(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
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FNDR-20123 free base
0 ImagesCat. No.: HY-131708CAS No.: 1267502-34-0FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations.
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Quinine hemisulfate
0 ImagesQuinine hemisulfate is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine hemisulfate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
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Naphthoquine
0 ImagesCat. No.: HY-17036ACAS No.: 173531-57-2Naphthoquine is an orally active antimalarial and antiviral agent. Naphthoquine exhibits ex vivo activity against multidrug-resistant Plasmodium falciparum and Plasmodium vivax, preferentially targeting ring-stage rather than trophozoite-stage parasites. Naphthoquine inhibits coronavirus (SARS-CoV-2, HCoV-OC43, HCoV-229E) replication by affecting viral entry and post-entry replication. Naphthoquine is used for research on malaria and Covid-19.
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Desethyl chloroquine-d4
0 ImagesCat. No.: HY-135811SCAS No.: 1189971-72-9Desethyl chloroquine-d4 is the deuterium labeled Desethyl chloroquine. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.
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Cycloguanil-d4 (hydrochloride)
0 ImagesCat. No.: HY-12784ASCAS No.: 1189427-23-3Synonyms: Chlorguanide triazine-d4 hydrochlorideCycloguanil-d4 (Chlorguanide triazine-d4) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil hydrochloride inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
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Atovaquone-d5
0 ImagesCat. No.: HY-13832S2CAS No.: 1329792-63-3Synonyms: Atavaquone-d5Atovaquone-d5 is the deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome?bc1?complex. Atovaquone is against human and ?P. falciparum?cytochrome?bc1?activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia.
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Halofantrine
0 ImagesCat. No.: HY-A0148CAS No.: 69756-53-2Synonyms: SKF-102886 free base; WR-171669Halofantrine (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.
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Pulixin
0 ImagesCat. No.: HY-N10197CAS No.: 2826264-81-5Pulixin prevents FREP1 from binding to P. falciparum-infected cell lysate. Pulixin blocks the transmission of the parasite to mosquitoes with an EC50 of 11 µM. Pulixin also inhibits the proliferation of asexual-stage P. falciparum with an EC50 of 47 nM.
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(S)-GSK1379725A
0 ImagesCat. No.: HY-145431CAS No.: 2359618-49-6(S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity.
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SJ000025081
0 ImagesCat. No.: HY-136448CAS No.: 421571-66-6SJ000025081 is a dihydropyridine and acts as a potent antimalarial agent. SJ000025081 results in an obvious suppression of the parasitemia in a murine malaria model infected with P. yoelii.
