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].
References:
- [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 Related Products (266)
Related Products (266)
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Nitidine chloride
0 ImagesNitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
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Mefloquine hydrochloride
0 ImagesSynonyms: Mefloquin hydrochlorideMefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine hydrochloride is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research.
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Daphnetin
0 ImagesDaphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
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Prodigiosin
0 ImagesProdigiosin (Prodigiosine) is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin is a potent inhibitor of the Wnt/β-catenin pathway. Prodigiosin has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties.
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Nanaomycin A
0 ImagesNanaomycin A is a selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A inhibits the in vitro growth of human Plasmodium falciparum with an IC80 of 33.1 nM.
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Amodiaquine dihydrochloride dihydrate
0 ImagesAmodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
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Ascomycin
0 ImagesSynonyms: Immunomycin; FR-900520; FK520Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research.
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Betulonic acid
0 ImagesSynonyms: Betunolic acid; Liquidambaric acid; (+)-Betulonic acid
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Radicicol
0 ImagesSynonyms: MonordenRadicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation. Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM.
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Methylene blue trihydrate
0 ImagesMethylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment.
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SID 26681509
0 ImagesSID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
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Amodiaquine dihydrochloride
0 ImagesAmodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
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Borrelidin
0 ImagesBorrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells. Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively.
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Chloroquine dihydrochloride
0 ImagesChloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
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Quinine hydrochloride dihydrate
0 ImagesQuinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate 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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Proguanil
0 ImagesProguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
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Lumefantrine
0 ImagesSynonyms: BenflumetolLumefantrine is an active antimalarial molecule used in combination with Artemether as a first- and second-line antimalarial drug with oral activity.
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Mefloquine
0 ImagesSynonyms: MefloquinMefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.
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Tafenoquine Succinate
0 ImagesSynonyms: WR 238605 SuccinateTafenoquine Succinate (WR 238605 Succinate) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent.
