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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Ethylhydrocupreine hydrochloride
0 ImagesSynonyms: Optochin hydrochlorideEthylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
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L-Canaline
0 ImagesL-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects.
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Tuberostemonine
0 ImagesTuberostemonine is a stenine alkaloid that can be isolated from Stemona tuberosa and Stemona sessifolia. Tuberostemonine is an antimalarial agent that has inhibitory activity against Ferredoxin-NADP+ reductases (FNRs) from Plasmodium falciparum (PfFNR). Tuberostemonine can reduce the number of citric acid-induced coughs in guinea pigs. Tuberostemonine decreases bronchoalveolar lavage fluid (BALF), neutrophil and macrophage infiltration and reduces peribronchial and perivascular inflammatory cell infiltration in mouse model of acute lung inflammation. Tuberostemonine has a level of activity as a feeding deterrent .
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Quinacrine hydrochloride hydrate
0 ImagesSynonyms: Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrateQuinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
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Pafuramidine
0 ImagesSynonyms: DB289Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.
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5,7,3',4'-Tetramethoxyflavone
0 Images5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
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KDU691
0 ImagesKDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.
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Manzamine A hydrochloride
0 ImagesSynonyms: Keramamine A hydrochlorideManzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
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Artelinic acid
0 ImagesArtelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes.
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Ganaplacide hydrochloride
0 ImagesSynonyms: KAF156 hydrochloride; GNF156 hydrochlorideGanaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
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MMV390048
0 ImagesMMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
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Artemether-d3
0 ImagesSynonyms: Dihydroqinghaosu methyl ether-d3; Dihydroartemisinin methyl ether-d3; SM224-d3Artemether-d3 is the deuterium labeled Artemether. Artemether is an antimalarial for the treatment of resistant strains of falciparum malaria.
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SIBA
0 ImagesSynonyms: 5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosineSIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies.
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Ursolic acid acetate
0 ImagesSynonyms: Acetylursolic acid; 3-Acetylursolic acidUrsolic acid acetate (Acetylursolic acid) is a triterpenoid compound and an inhibitor of Plasmodium falciparum heat shock protein 90 (PfHsp90) with a KD of 8.16 μM. Ursolic acid acetate is cytotoxic to KB cells, with an IC50 value of 8.4 μM. Ursolic acid acetate can be used in tumor and antimalarial research.
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Naphthoquine phosphate
0 ImagesNaphthoquine phosphate is an orally active antimalarial and antiviral agent. Naphthoquine phosphate exhibits ex vivo activity against multidrug-resistant Plasmodium falciparum and Plasmodium vivax, preferentially targeting ring-stage rather than trophozoite-stage parasites. Naphthoquine phosphate inhibits coronavirus (SARS-CoV-2, HCoV-OC43, HCoV-229E) replication by affecting viral entry and post-entry replication. Naphthoquine phosphate is used for research on malaria and Covid-19.
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8-Deoxygartanin
0 Images8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE). 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM.
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Halofuginone lactate
0 ImagesSynonyms: RU-19110 lactateHalofuginone lactate (RU-19110 lactate), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
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(2S)-2'-Methoxykurarinone
0 ImagesSynonyms: 2'-O-Methylkurarinone(2S)-2'-Methoxykurarinone (2'-O-Methylkurarinone) is a flavanone natural product found in the roots of Sophora flavescens, possessing anti-sepsis, inhibitory effects on osteoclast differentiation and bone resorption, anti-inflammatory, and anti-Plasmodium activities. (2S)-2'-Methoxykurarinone exhibits an EC50 = 2.4 μM against the FCR-3 strain of Plasmodium falciparum. In sepsis models, (2S)-2'-Methoxykurarinone modulates immune cell function and inhibits inflammation and oxidative stress. In bone-related models, (2S)-2'-Methoxykurarinone blocks osteoclast differentiation and bone resorption, and inhibits RANKL-mediated Akt, p38, and JNK signaling pathways. In skin inflammation models, (2S)-2'-Methoxykurarinone inhibits NF-κB pathway activation, upregulates HO-1 expression, and suppresses CCL27 chemokine production in HaCaT cells. (2S)-2'-Methoxykurarinone is useful for research on osteoporosis, sepsis, inflammatory skin diseases (such as atopic dermatitis and allergic contact dermatitis), and malaria.
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Febrifugine dihydrochloride
0 ImagesFebrifugine dihydrochloride is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine dihydrochloride inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids.
