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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INE963
0 ImagesINE963 is a potent and fast-acting blood-stage antimalarial agent, with an EC50s of 3-6 nM. INE963 is potential for single-dose cures in uncomplicated malaria.
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Lapachol
0 ImagesLapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity.
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beta-Mangostin
0 ImagesSynonyms: β-Mangostinbeta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).
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DSM265
0 ImagesDSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM.
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Dehydrocorydaline chloride
0 ImagesSynonyms: 13-Methylpalmatine chlorideDehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
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Cipargamin
0 ImagesSynonyms: NITD609; KAE609Cipargamin (NITD609) is an potent antimalarial compound, with an IC50 of appr 1 nM against P. falciparum.
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Febrifugine
0 ImagesFebrifugine is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids.
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Cycloguanil hydrochloride
0 ImagesCycloguanil (Chlorguanide triazine) 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 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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Piperaquine tetraphosphate tetrahydrate
0 ImagesPiperaquine tetraphosphate tetrahydrate is a bisquinoline antimalarial agent. Piperaquine tetraphosphate tetrahydrate can be used in antimalarial research in combination with Artemisinin.
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Azlocillin sodium salt
0 ImagesSynonyms: Sodium azlocillinAzlocillin sodium salt (Sodium azlocillin), a semisynthetic penicillin, is a broad spectrum β-lactam antibiotic. Azlocillin sodium salt shows antipseudomonal activity, and also potent against the malarial parasite Plasmodium falciparum.
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Cabamiquine
0 ImagesSynonyms: DDD107498; DDD-498; M5717Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.
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Halofantrine hydrochloride
0 ImagesSynonyms: SKF-102886; WR-171669 hydrochlorideHalofantrine hydrochloride (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 hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.
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Hydroxychloroquine sulfate (Standard)
0 ImagesHydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
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DL-threo-PDMP hydrochloride
0 ImagesDL-threo-PDMP hydrochloride is a competitive glucosylceramide synthase (GCS) inhibitor and antimalarial agent. DL-threo-PDMP hydrochloride competitively inhibits the activity of GCS. DL-threo-PDMP hydrochloride restores cisplatin sensitivity in cisplatin-resistant testicular germ cell tumor cells. DL-threo-PDMP hydrochloride blocks the growth of ring-stage Plasmodium falciparum parasites.
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AN3661
0 ImagesAN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
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Artemotil
0 ImagesSynonyms: β-Arteether; (+)-Arteether; ArteetherArtemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
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Cinchonidine
0 ImagesCinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
