Leishmania
Leishmania is an obligate intracellular protozoan parasite transmitted by sand flies, and mammalian infection centers on macrophages as both host cells and immune effector cells[1]. Mechanistically, the parasite regulates phagosome maturation to support intracellular growth and avoid destruction after uptake into macrophages[1]. Lipophosphoglycan (LPG) is a surface glycoconjugate virulence factor that supports metacyclic establishment in host cells but declines during amastigote development[2]. Compared with related glycoconjugates, LPG showed a distinct virulence role in Leishmania major, because lpg mutants were attenuated in macrophage and mouse infection models[3]. GP63, or leishmanolysin, represents a separate virulence factor; targeted deletion in L. major identified GP63 as required for full parasite virulence[4]. In macrophage biology, GP63 influences antimicrobial functions and alters signaling pathways that regulate microbicidal responses[5]. For experimental applications, intracellular amastigote assays provide a clinically relevant drug-screening model, whereas promastigote screens are easier to automate but can miss active compounds[6].
References:
- [1]. Podinovskaia M, et al. Leishmania and the macrophage: a multifaceted interaction. Future Microbiol. 2015;10(1):111-29. [Content Brief]
- [2]. Mandell MA, et al. Quantitative single-cell analysis of Leishmania major amastigote differentiation demonstrates variably extended expression of the lipophosphoglycan (LPG) virulence factor in different host cell types. PLoS Negl Trop Dis. 2022 Oct 27;16(10):e0010893. [Content Brief]
- [3]. Späth GF, et al. Lipophosphoglycan is a virulence factor distinct from related glycoconjugates in the protozoan parasite Leishmania major. Proc Natl Acad Sci U S A. 2000 Aug 1;97(16):9258-63. [Content Brief]
- [4]. Joshi PB, et al. Targeted gene deletion in Leishmania major identifies leishmanolysin (GP63) as a virulence factor. Mol Biochem Parasitol. 2002 Mar;120(1):33-40. [Content Brief]
- [5]. Olivier M, et al. Leishmania virulence factors: focus on the metalloprotease GP63. Microbes Infect. 2012 Dec;14(15):1377-89. [Content Brief]
- [6]. De Muylder G, et al. A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit. PLoS Negl Trop Dis. 2011 Jul;5(7):e1253. [Content Brief]
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Leishmania Related Products (94)
Related Products (94)
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Antileishmanial agent-38
0 ImagesCat. No.: HY-179584Antileishmanial agent-38 (compound 197) is a host-directed small molecule antileishmanial agent exhibiting potent broad-spectrum activity against Leishmania spp. Antileishmanial agent-38 inhibits intracellular parasites primarily by targeting the host protein lysozyme, while also displaying direct activity against extracellular L. donovani promastigotes. Antileishmanial agent-38 can be used for leishmaniasis research.
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Pentamidine dihydrochloride
0 ImagesCat. No.: HY-B0537ACAS No.: 50357-45-4Synonyms: MP-601205 dihydrochloridePentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
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Julocrotine
0 ImagesJulocrotine is a naturally derived, orally active glutarimide alkaloid. Julocrotine alleviates rotenone-induced climbing impairment in Drosophila melanogaster and elevation of malondialdehyde levels in brain tissues, and restores the elevated mRNA levels of superoxide dismutase and catalase to normal. Julocrotine inhibits the growth of Leishmania amazonensis, induces its ultrastructural changes and reduces the number of amastigotes. Julocrotine can be used in research related to Parkinson's disease and cutaneous leishmaniasis.
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Didesmethylpromazine
0 ImagesDidesmethylpromazine (Compound 18) is a trypanothione reductase inhibitor with an I50of 1412 μM against T. cruzi trypanothione reductase. Didesmethylpromazine can be used in the research of trypanosome and leishmania infections.
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18-Methoxycoronaridine
0 ImagesCat. No.: HY-106980CAS No.: 308123-60-6Synonyms: (-)-18-Methoxycoronaridine18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC50 values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine also exhibits potent antiparasitic activity. 18-Methoxycoronaridine can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis.
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Colchicoside
0 ImagesColchicoside is a monoglycosylated colchicine alkaloid glycoside with anti-leishmanial activity. Colchicoside can be obtained by specific glycosylation of Colchicine (HY-16569) by Astragalus vesicarius plant suspension cells, and is also found in Gloriosa superba seeds. Colchicoside can serve as a precursor for the synthesis of Thiocolchicoside (HY-N0301). Colchicoside can be used in research related to anti-leishmanial infection.
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Antileishmanial agent-35
0 ImagesCat. No.: HY-178033CAS No.: 100611-91-4Antileishmanial agent-35 (Compound 6) is an antileishmanial agent with an IC50 of 0.29μM for promastigotes of Leishmania amazonensis. Antileishmanial agent-35 significantly decreases the mitochondrial membrane potential and ATP levels, and further increases the production of ROS by a blockage in the electron transport chain, where ubiquinone intervenes. Antileishmanial agent-35 can be used for cutaneous leishmaniases research.
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Antiparasitic agent-40
0 ImagesCat. No.: HY-181437CAS No.: 65655-84-7Antiparasitic agent-40 (compound 4.3) is a 4-thiazolidinone-based antileishmaniasis inhibitor. Antiparasitic agent-40 exhibits significant inhibitory activity against methionine aminopeptidase.
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E5700
0 ImagesCat. No.: HY-123746CAS No.: 332132-39-5E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.
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Antileishmanial agent-43
0 ImagesCat. No.: HY-183621Antileishmanial agent-43 is a 3,4,5‑trisubstituted isoxazole with selective antileishmanial activity. Antileishmanial agent-43 shows IC50 values of 12.7 μM against Leishmania amazonensis promastigotes and 0.96 μM against intracellular amastigotes. Antileishmanial agent-43 induces ROS elevation, oxidative stress and mitochondrial dysfunction, resulting in lipid peroxidation, mitochondrial depolarization and ATP imbalance. Antileishmanial agent-43 causes cell shrinkage, phosphatidylserine externalization, plasma membrane permeabilization, and promotes autophagy. Antileishmanial agent-43 can be used for the research of leishmaniasis.
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Antileishmanial agent-39
0 ImagesCat. No.: HY-180833Antileishmanial agent-39 (Compound 4h) is an antileishmanial agent. Antileishmanial agent-39 shows antileishmanial activity against the axenic amastigote form of Leishmania infantum with an IC50 of 0.42 μM.
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Antiparasitic agent-39
0 ImagesCat. No.: HY-180943CAS No.: 2568585-37-3Antiparasitic agent-39 (Compound 14) is a selective antiparasitic agent and Deferasirox (HY-17359) derivative. Antiparasitic agent-39 reduces the mitochondrial membrane potential. Antiparasitic agent-39 shows antiparasitic activity against T. brucei, T. gambiense, L. Mexicana, T. gondii, B. divergens, P. falciparum with EC50s of 4.2 nM, 10.4 nM, 52.0 nM, 17.0 nM, 41.2 nM, 54.8 nM, respectively.
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Trypanothione synthetase-IN-2
0 ImagesCat. No.: HY-151150CAS No.: 3033799-60-6Trypanothione synthetase-IN-2 (Compound 3) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 5.4 μM when triamine spermidine is as polyamine S.
