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]

Leishmania Inhibitors (74)

Leishmania Produits associés (84):

By Type:	Pan (16) Selective (7)

Cat. No.	Nom du produit	Effet	Pureté

HY-N9194

5-Methoxycanthin-6-one
5-Methoxycanthin-6-one is an orally active inhibitor of Leishmania strains. 5-Methoxycanthin-6-one shows cytotoxicity with an IC₅₀ of 5.44 μg/mL against Ailanthus altissima cells.

HY-146042

Antiparasitic agent-4	Inhibitor
Antiparasitic agent-4 (compound 4q) has highly antiparasitic activity against Leishmania infantum (L. infantum) and Trypanosoma cruzi (T. cruzi) with IC₅₀s of 8.51 μM and 2.20 μM, respectively. Antiparasitic agent-4 also has certain cytotoxicity against HepG2 (CC₅₀ = 18.97 μM).

HY-130993

Isatropolone A	Inhibitor
Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against *Leishmania donovani* with an IC₅₀ of 0.5 μM.

HY-127087

Isogarcinol	Inhibitor
Isogarcinol (Cambogin) is a potent AChE and BChE inhibitor, with IC₅₀ values of 1.13 and 8.30 μM, respectively. Isogarcinol also shows leishmanicidal activity, with an IC₅₀ of 0.33 μM against L. donovani.

HY-146745

Antileishmanial agent-5	Inhibitor
Antileishmanial agent-4 is a ribonucleoside analogue and acts as an antileishmanial agent. Antileishmanial agent-4 is against L.infantum and T.cruzi with EC₅₀ values of 0.68 μM and 0.83 μM, respectively.

HY-120154

Palitantin	Inhibitor
Palitantin ((±)-Palitantin), a metabolite of Penicillium frequentans on Leishmania brasiliensis, has antiprotozoal effect against Leishmania brasiliensis.

HY-184205

LASSBio-1736	Inhibitor
LASSBio-1736 is a Cysteine protease inhibitor and antimalarial agent. LASSBio-1736 targets the promastigote form of Leishmania major. LASSBio-1736 can be used in the research of leishmaniasis.

HY-B0221A

Amphotericin B trihydrate
Amphotericin B trihydrate, a polyene antibiotic, is first isolated from fermenter cultures of Streptomyces nodosus. Amphotericin B trihydrate also possesses antileishmanial activity.

HY-183262

Antileishmanial agent-40	Inhibitor
Antileishmanial agent-40 is an orally active and selective antileishmanial agent. Antileishmanial agent-40 elevates intracellular reactive oxygen species (ROS) levels in Leishmania donovani promastigotes. Antileishmanial agent-40 induces cell cycle arrest at the sub-G₀/G₁ phase in Leishmania donovani promastigotes, indicative of programmed-like parasite death. Antileishmanial agent-40 can be used for the research of leishmaniasis.

HY-151148

Trypanothione synthetase-IN-1
Trypanothione synthetase-IN-1 (Compound 1) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC₅₀ of 14.8 μM when triamine spermidine is as polyamine S.

HY-N10441

3β-Hydroxy-hop-22(29)-ene	Inhibitor
3β-Hydroxy-hop-22(29)-ene (compound 3) is a potent antiparasitic agent. 3β-Hydroxy-hop-22(29)-ene shows moderate activity against Trypanosoma cruzi and Leishmania mexicana.

HY-178784

Antileishmanial agent-37	Inhibitor
Antileishmanial agent-37 (Compound 1b) is an antileishmanial agent, TbPTR1 (an IC₅₀ value of 17.1 μM) and LmPTR1 inhibitor. Anti-leishmaniasis agent-37 has a moderate effect against Leishmania infantum.

HY-151935

Antileishmanial agent-13	Inhibitor
Antileishmanial agent-13 is a quinoline-isatin hybrid, acts as an antileishmanial agent against L. Major Leishmania strain. Antileishmanial agent-13 acquires the antileishmanial activity via the anti-folate mechanism. Antileishmanial agent-13 has potent inhibition against both promastigote and amastigote forms with IC₅₀s of 0.604 μM and 0.508 μM, respectively.

HY-183290

Antileishmanial agent-41	Inhibitor
Antileishmanial 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.

HY-19688B

Sitamaquine tosylate	Inhibitor
Sitamaquine (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.

HY-N19720

Bractein	Inhibitor
Bractein 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.

HY-W159102

8CN	Inhibitor
8CN, a 2-amino-thiophene derivative, has anti-leishmanial activity. 8CN can be used in research of Leishmaniasis.

HY-184214

Antileishmanial agent-44	Inhibitor
Antileishmanial 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.

HY-137180

Naloxonazine
Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.

HY-177958

ACS03	Inhibitor
ACS03 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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