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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Pentamidine dimesylate
0 ImagesPentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
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Trypaflavin
0 ImagesTrypaflavin is an acridine compound and antimalarial agent. Trypaflavin invades germ cells. Trypaflavin induces aberrations in unfertilized oocytes. Trypaflavin increases the frequency of chromosomal aberrations. Trypaflavin shows weak mutagenicity. Trypaflavin is highly toxic to Leishmania, causing immediate lysis of the leptomonads.
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5-Methoxycanthin-6-one
0 ImagesCat. No.: HY-N9194CAS No.: 15071-56-45-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.
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N-Desmethyl clomipramine hydrochloride (Standard)
0 ImagesSynonyms: Desmethylclomipramine hydrochloride (Standard); Norclomipramine hydrochloride (Standard)N-Desmethyl clomipramine hydrochloride (Standard) (Desmethylclomipramine hydrochloride (Standard); Norclomipramine hydrochloride (Standard)) is the analytical standard of N-Desmethyl clomipramine hydrochloride (HY-12388A). This product is intended for research and analytical applications. N-Desmethyl clomipramine hydrochloride is the orally active major active metabolite of the tricyclic antidepressant Clomipramine (HY-B0457A), possessing multiple activities including anti-inflammatory, antioxidant, antibacterial, and antiparasitic effects. N-Desmethyl clomipramine hydrochloride blocks autophagosome-lysosome fusion, leading to the accumulation of LC3-II, p62, ATG7, WIPI2, and ATG5-12, reactivates the p53/p21 pathway, induces apoptosis through C-PARP and C-CAS3, and inhibits the proliferation, migration, and invasion of renal cancer cells. N-Desmethyl clomipramine hydrochloride inhibits LdTOPIA, inducing R-loop accumulation in the nucleus of Leishmania, ultimately causing parasite death. N-Desmethyl clomipramine hydrochloride can be used for research on depression, metastatic renal cell carcinoma, and leishmaniasis.
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25-Hydroperoxycycloart-23-en-3β-ol
0 ImagesCat. No.: HY-N17550CAS No.: 173740-54-025-Hydroperoxycycloart-23-en-3β-ol is an anticancer, antibacterial, and antimalarial agent. 25-Hydroperoxycycloart-23-en-3β-ol can be isolated from Blepharodon nitidum. 25-Hydroperoxycycloart-23-en-3β-ol exhibits anti-Mycobacterium tuberculosis and antileishmanial activities. 25-Hydroperoxycycloart-23-en-3β-ol shows significant cytotoxic activity against a panel of tumor cell lines (large cell lung cancer, melanoma, colon adenocarcinoma, chronic myelogenous leukemia).
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Antiparasitic agent-4
0 ImagesCat. No.: HY-146042CAS No.: 2253996-66-4Antiparasitic 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).
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Naringenin 4',7-dimethyl ether
0 ImagesSynonyms: NRG-DMNaringenin 4',7-dimethyl ether, Naringenin (HY-N0100) derivative is an anti-seizure agent. Naringenin 4',7-dimethyl ether attenuates pentylenetetrazole-induced seizures in larval zebrafish and reduces seizures in the mouse 6-Hz psychomotor seizure model. Naringenin 4',7-dimethyl ether can be used for the research of epilepsy. Naringenin 4',7-dimethyl ether is an active agent against Leishmania mexicana (17.8 µM) and Trypanosoma brucei (17.5 µM).
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Isatropolone A
0 ImagesCat. No.: HY-130993CAS No.: 2097813-40-4Isatropolone 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.
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Isogarcinol
0 ImagesCat. No.: HY-127087CAS No.: 71117-97-0Synonyms: Cambogin
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Antileishmanial agent-5
0 ImagesCat. No.: HY-146745CAS No.: 2922333-29-5Antileishmanial 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.
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DNDI-VL-2098
0 ImagesCat. No.: HY-W663179CAS No.: 681492-17-1DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis.
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Palitantin
0 ImagesCat. No.: HY-120154CAS No.: 15265-28-8Synonyms: (±)-PalitantinPalitantin ((±)-Palitantin), a metabolite of Penicillium frequentans on Leishmania brasiliensis, has antiprotozoal effect against Leishmania brasiliensis.
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LASSBio-1736
0 ImagesCat. No.: HY-184205CAS No.: 1554691-37-0LASSBio-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.
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Amphotericin B trihydrate
0 ImagesCat. No.: HY-B0221ACAS No.: 1202017-46-6Amphotericin B trihydrate, a polyene antibiotic, is first isolated from fermenter cultures of Streptomyces nodosus. Amphotericin B trihydrate also possesses antileishmanial activity.
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Antileishmanial agent-40
0 ImagesCat. No.: HY-183262CAS No.: 3126462-40-3Antileishmanial 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.
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N-Desmethyl clomipramine
0 ImagesN-Desmethyl clomipramine (Desmethylclomipramine; Norclomipramine) is the orally active major active metabolite of the tricyclic antidepressant Clomipramine (HY-B0457A), possessing multiple activities including anti-inflammatory, antioxidant, antibacterial, and antiparasitic effects. N-Desmethyl clomipramine blocks autophagosome-lysosome fusion, leading to the accumulation of LC3-II, p62, ATG7, WIPI2, and ATG5-12, reactivates the p53/p21 pathway, induces apoptosis through C-PARP and C-CAS3, and inhibits the proliferation, migration, and invasion of renal cancer cells. N-Desmethyl clomipramine inhibits LdTOPIA, inducing R-loop accumulation in the nucleus of Leishmania, ultimately causing parasite death. N-Desmethyl clomipramine can be used for research on depression, metastatic renal cell carcinoma, and leishmaniasis.
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Trypanothione synthetase-IN-1
0 ImagesCat. No.: HY-151148CAS No.: 2355349-41-4Trypanothione 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.
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3β-Hydroxy-hop-22(29)-ene
0 ImagesCat. No.: HY-N10441CAS No.: 58801-23-33β-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.
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Antileishmanial agent-37
0 ImagesCat. No.: HY-178784Antileishmanial 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.
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Antileishmanial agent-13
0 ImagesCat. No.: HY-151935CAS No.: 853725-86-7Antileishmanial 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.
