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]
All Product Categories
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Leishmania Related Products (99)
Related Products (99)
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Antileishmanial agent-41
0 ImagesCat. No.: HY-183290CAS No.: 3126462-44-7Antileishmanial agent-41 (Compound 20k) is a selective Antileishmanial agent with a IC50 of 1.51 μg/mL against Leishmania donovani. Antileishmanial agent-41 increases ROS levels. Antileishmanial agent-41 can be used for the research of leishmaniasis.
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Sitamaquine tosylate
0 ImagesCat. No.: HY-19688BCAS No.: 1019640-33-5Synonyms: WR 6026 tosylateSitamaquine (WR6026) tosylate, an orally active 8-aminoquinoline analog, is an antileishmanial agent. Sitamaquine tosylate inhibits mitochondrial complex II (succinate dehydrogenase). Sitamaquine tosylate is a lipophilic weak base that rapidly accumulates in acidic compartments of Leishmania spp., mainly in acidocalcisomes.
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Bractein
0 ImagesCat. No.: HY-N19720CAS No.: 22684-08-8Bractein is a natural aurone flavonoid with potential antioxidant activity. Bractein shows in vitro antileishmanial activity and inhibits promastigotes and intracellular amastigotes of Leishmania donovani. Bractein exhibits no obvious cytotoxicity against mammalian macrophages with an EC50 value > 25.0 μg/mL. Bractein can be used for the research of Leishmania.
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8CN
0 ImagesCat. No.: HY-W159102CAS No.: 40106-14-78CN, a 2-amino-thiophene derivative, has anti-leishmanial activity. 8CN can be used in research of Leishmaniasis.
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Antileishmanial agent-44
0 ImagesCat. No.: HY-184214Antileishmanial agent-44 is a histone deacetylase inhibitor targeting Leishmania donovani Sir2, with an IC50 of 0.652 μM against amastigotes. Antileishmanial agent-44 elevates ROS levels to induce oxidative stress, which causes mitochondrial membrane potential depolarization, cytochrome c release, phosphatidylserine externalization and DNA fragmentation, triggers apoptosis-like cell death, and arrests the cell cycle. Antileishmanial agent-44 upregulates the expression of Th1-type cytokines and NO in macrophages, reshapes host immune responses to eliminate intracellular parasites. Antileishmanial agent-44 inhibits parasites in infected golden hamsters in vivo. Antileishmanial agent-44 can be used for the research of visceral leishmaniasis.
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Naloxonazine
0 ImagesCat. No.: HY-137180CAS No.: 82824-01-9Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.
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ACS03
0 ImagesCat. No.: HY-177958CAS No.: 2227022-64-0ACS03 is a hybrid thiophene-acridine compound. ACS03 induces an increase in lactate dehydrogenase, glutathione S-transferase, and AChE activities. ACS03 has antileishmanial activity. ACS03 exhibits selective anti-cancer effects against colon carcinoma.
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Trypanothione synthetase-IN-4
0 ImagesCat. No.: HY-151149CAS No.: 3033799-62-8Trypanothione synthetase-IN-4 is a L. infantum trypanothione synthetase (TryS) inhibitor, and the activity is dependent on the concentration of the polyamine substrate. Trypanothione synthetase-IN-4 has potent antileishmanicidal activity with an EC50 value of 0.6 μM and a selectivity index of 35. Trypanothione synthetase-IN-4 can be used for the research of leishmaniasis.
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Castalagin
0 ImagesCat. No.: HY-N20707CAS No.: 24312-00-3Castalagin is an orally active natural product with multiple biological activities including antibacterial activity against bacteria and anti-leishmanial activity against Leishmania aethiopica. Castalagin exhibits inhibitory activity against PARP1 and DNA topoisomerase II, with an IC50 of 0.86 μM for bovine PARP1. Castalagin reduces poly (ADP-ribosyl) ation modification in cells. Castalagin binds to the cell envelope of Ruminococcus bromii, increases the ratio of CD8+/FOXP3+CD4+ T cells in the tumor microenvironment, and acts as a prebiotic to enhance the activity of anti-PD-1 therapy. Castalagin induces morphological changes in Leishmania aethiopica promastigotes and inhibits their proliferation. Castalagin inhibits PBP2a-mediated peptidoglycan layer stabilization, disrupts bacterial peptidoglycan assembly, and inhibits and disintegrates bacterial biofilms. Castalagin can be used in research related to diseases such as cancer, leishmaniasis, and bacterial infections.
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Antiparasitic agent-14
0 ImagesCat. No.: HY-149078CAS No.: 3046451-98-0Antiparasitic agent-14 is a potent antiparasitic agent. Antiparasitic agent-14 shows cytotoxicity and antiparasitic activity. Antiparasitic agent-14 inhibits the growth of trypomastigote and amastigote.
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14-Norpseurotin A
0 ImagesCat. No.: HY-133101CAS No.: 1031727-34-0Synonyms: 14-Norpseurotin14-Norpseurotin A (14-Norpseurotin) is an Antibacterial, antimalarial, and anticancer agent. 14-Norpseurotin A is isolated from various fungi of the Aspergillus genus. 14-Norpseurotin A induces neurite outgrowth. 14-Norpseurotin A inhibits the growth of Escherichia coli, Bacillus subtilis, and Micrococcus lysoleikticus. 14-Norpseurotin A exhibits antileishmanial activity against L. donovani, antiplasmodial activity against P. falciparum, and shows no activity against T. cruzi. 14-Norpseurotin A exerts anticancer activity against breast cancer. 14-Norpseurotin A is used in research related to leishmaniasis, malaria, and breast cancer.
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Euphorbadienol
0 ImagesEuphorbadienol (alpha-Euphorbol), a triterpenic compound, isolated from the latex of Euphorbia resinifera. The derivatives of Euphorbadienol can be used as elicitors of disease resistance, and has antileishmanial and antitrypanosomal activity.
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Piperolactam A
0 ImagesCat. No.: HY-N2894CAS No.: 112501-42-5Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani.
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Antiparasitic agent-2
0 ImagesCat. No.: HY-146041CAS No.: 2494277-80-2Antiparasitic agent-2 (compound 8a) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC50s of 7.28 μM and 2.30 μM, respectively. Antiparasitic agent-2 also has certain cytotoxicity against HepG2 (CC50 = 26.79 μM).
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Antileishmanial agent-4
0 ImagesCat. No.: HY-146744CAS No.: 2922333-23-9Antileishmanial agent-4 is a ribonucleoside analogue and acts as an antileishmanial agent.
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Niranthin
0 ImagesCat. No.: HY-N6054CAS No.: 50656-77-4Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
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Antileishmanial agent-27
0 ImagesCat. No.: HY-163457Antileishmanial agent-27 (compound 7j) is a benzothiazolo-coumarin derivative. Antileishmanial agent-27 is a competitive inhibitor of arginyl-tRNA synthetases (ArgRSs). Antileishmanial agent-27 shows selectivity toward ArgRS of Leishmania donovani (LdArgRS) than its human counterpart (HsArgRS), with IC50 values of 1.2 and 19 μM, respectively. Antileishmanial agent-27 possesses high pharmacokinetic properties.
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Anti-infective agent 6
0 ImagesCat. No.: HY-151612CAS No.: 2839192-35-5Anti-infective agent 6 (compound 28) is a potent anti-infectious agent. Anti-infective agent 6 shows a good activity against P. falciparum F32-ART (IC50=1.4 μM) with a good selectivity index (SI>36). Anti-infective agent 6 also shows a potency against L. donovani (IC50=3.5 μM).
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Antileishmanial agent-2
0 ImagesCat. No.: HY-132905CAS No.: 2863687-18-5Antileishmanial agent-2 shows submicromolar antileishmanial activity (IC50 = 0.29 μM) and a very high selectivity index with respect to mammalian cells.
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LC-61
0 ImagesCat. No.: HY-180130CAS No.: 2195159-10-3LC-61 is a potent antileishmanial agent with an IC50 of 0.076 µM against intracellular L. infantum.
