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].
Références:
- [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 Produits associés (94)
Produits associés (94)
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Allopurinol riboside
0 ImagesAllopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.
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(S)-4-Thiazolidinecarboxylic acid
0 ImagesCat. No.: HY-W039443CAS No.: 45521-09-3(S)-4-Thiazolidinecarboxylic acid (L-4-thioproline) is a glutamate 5-kinase inhibitor with an IC50 of 1.8 mM against LdG5K. (S)-4-Thiazolidinecarboxylic acid can be used in the research of leishmaniasis and Escherichia coli infections.
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ABMA
0 ImagesABMA is a broad-spectrum inhibitor of intracellular toxins and pathogens. ABMA efficiently protects cells against various toxins and pathogens including viruses, intracellular bacteria and parasite. ABMA selectively acts at host cell late endosomes rather than targeting toxin or pathogen itself. ABMA has broad-spectrum anti-infection activity.
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Pentadecane
0 ImagesPentadecane is an orally active natural plant volatile alkane with anti-inflammatory, analgesic, antipyretic and anti-leishmanial activities. Pentadecane presents IC50 values of 65.3 μM, 60.5 μM and 194.8 μM against Leishmania infantum promastigotes, amastigotes and intracellular amastigotes, respectively. Pentadecane downregulates the mRNA expression of TNF-α and IL-12 and inhibits the release of inflammatory mediators. Pentadecane arrests the cell cycle of Leishmania infantum and induces apoptosis. Pentadecane can be applied to the research of inflammation and leishmaniasis.
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Mahanine
0 ImagesCat. No.: HY-121368CAS No.: 28360-49-8Mahanine is a carbazole alkaloid with various biological properties. Mahanine is a potent anticancer agent against different types of cancer cells. Mahanine exhibits antileishmanial activity and can be used for Leishmania infection research research.
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Bacopasaponin C
0 ImagesBacopasaponin C is an orally active natural glycoside. Bacopasaponin C can be isolated from Bacopa monniera. Bacopasaponin C inhibits Verapamil (HY-14275)-stimulated P-gp ATPase activity with an IC50 of 57.83 μg/mL. Bacopasaponin C has antitumor activity against sarcomas. Bacopasaponin C has antiparasitic activity against Leishmania donovani.
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Defensin HNP-1 human TFA
0 ImagesCat. No.: HY-P2310APureté: 99.08%Defensin HNP-1 human TFA is a type of human neutrophil peptide (HNPs). Defensin HNP-1 human TFA possesses immunomodulatory functions and can delay the apoptosis of neutrophils. Defensin HNP-1 human TFA inhibits DNA/RNA/protein synthesis and interferes with metabolic pathways, thus exhibiting broad antibacterial activity. Defensin HNP-1 human TFA has direct inactivation effects on HIV, HSV-1, HSV-2, CMV, influenza virus, etc. Defensin HNP-1 human TFA has antileishmanial activity. Defensin HNP-1 human TFA is involved in endothelial cell dysfunction during the early development of atherosclerosis.
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Myricetin 3-O-glucoside
0 ImagesSynonyms: Myricetin 3-β-D-glucopyranosideMyricetin 3-O-glucoside (Myricetin 3-β-D-glucopyranoside) is a flavonol from Tibouchina paratropica and Hakmeitau beans. Myricetin 3-O-glucoside exhibits anti-Leishmanial, anti-inflammatory and antimicrobial activities.
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GNF6702
0 ImagesGNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis.
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NR-7h
0 ImagesNR-7h is a selective p38α/p38β MAPK PROTAC degrader with multiple activities including anti-leishmanial, anti-malarial, and anti-Mayaro virus properties. NR-7h induces specific degradation of p38α/p38β isoforms and p38-MAPK via the ubiquitin-proteasome system. NR-7h reduces the load of Leishmania donovani, modulates the cytokine profile toward a pro-inflammatory phenotype, and enhances the oxidative burst of macrophages. NR-7h inhibits the growth of Plasmodium falciparum in human red blood cells and merozoite invasion. NR-7h reduces the replication of Mayaro virus and the expression of E1 protein in primary human dermal fibroblasts. NR-7h can be used in studies related to parasitic infections, viral infections, and breast cancer.
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Oleocanthal
0 ImagesCat. No.: HY-124481CAS No.: 289030-99-5Oleocanthal is an orally active phenolic seciridoid compound. Oleocanthal can be extracted from olive oil. Oleocanthal inhibits COX-1 and COX-2, reduces ROS and NO, and upregulates Nrf-2 and HO-1. Oleocanthal reduces Aβ deposition. Oleocanthal exhibits anti-Leishmania activity against promastigotes and amastigotes of L. major, with IC50 values of 18.7 and 87 μg/mL, respectively. Oleocanthal exhibits anticancer activity against colon, breast, liver, and melanoma cancers. Oleocanthal also exhibits anti-inflammatory and neuroprotective properties. Oleocanthal can be used in Alzheimer's disease research.
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2-Benzoxazolinone
0 ImagesSynonyms: 2-Benzoxazolone; 1,3-Benzoxazol-2(3H)-one; 2-Hydroxybenzoxazole2-Benzoxazolinone is an anti-leishmanial agent with an LC50 of 40 μg/mL against L. donovani. A building block in chemical synthesis. 1,3-Benzoxazol-2(3H)-one derivatives have antimicrobial activity against a selection of Gram-positive, Gram-negative bacteria and yeasts. Derivatives as anti-quorum sensing agent.
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Zolunicant
0 ImagesSynonyms: MM-110; (±)-18-MethoxycoronaridineZolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.
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PPA-904
0 ImagesPPA-904 is a specific phenothiazine photosensitizer in photodynamic research (PDT) research, especially topical application for cutaneous leishmaniasis in vivo.
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GSK3186899
0 ImagesSynonyms: DDD-853651GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.
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Galeflaprit
0 ImagesSynonyms: LXE408Galeflaprit (LXE408) is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. Galeflaprit has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Galeflaprit has a low propensity to cross the blood brain barrier. Galeflaprit has the potential for visceral leishmaniasis (VL) research.
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Anemonin
0 ImagesSynonyms: Pulsatilla camphor; Anemonine; trans-AnemoninAnemonin (Pulsatilla camphor; Anemonine; trans-Anemonin) is a naturally occurring bislactone small molecule derived from Ranunculaceae with blood-brain barrier permeability, possessing a variety of activities including anti-inflammatory, antioxidant, neuroprotective, melanogenesis-inhibiting, and antiparasitic effects. Anemonin inhibits iNOS to reduce NO release; it inhibits PKC-θ protein expression and downregulates the pro-inflammatory factors TNF-α, IL-1β, and IL-6; it enhances the activities of the antioxidant enzymes SOD, CAT, and GSH-Px, and reduces MDA and ROS levels. Anemonin modulates the Bcl-2 / Bax / caspase-3 pathway to inhibit apoptosis; it downregulates melanogenesis-related molecules including MITF, TYR, TRP1, and TRP2, thereby inhibiting melanin synthesis in human melanocytes. Anemonin inhibits Leishmania and Schistosoma mansoni. Anemonin is used in research related to diseases such as hyperpigmentation, cerebral ischemia/reperfusion injury, inflammation, sepsis-induced acute lung injury, acute ulcerative colitis, leishmaniasis, and schistosomiasis.
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DNDI-6148
0 ImagesDNDI-6148 is a novel preclinical candidate for the research of visceral leishmaniasis.
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Pentadecane-d32
0 ImagesPentadecane-d32 is the deuterium labeled Pentadecane (HY-N7926). Pentadecane is an orally active natural plant volatile alkane with anti-inflammatory, analgesic, antipyretic and anti-leishmanial activities. Pentadecane presents IC50 values of 65.3 μM, 60.5 μM and 194.8 μM against Leishmania infantum promastigotes, amastigotes and intracellular amastigotes, respectively. Pentadecane downregulates the mRNA expression of TNF-α and IL-12 and inhibits the release of inflammatory mediators. Pentadecane arrests the cell cycle of Leishmania infantum and induces apoptosis. Pentadecane can be applied to the research of inflammation and leishmaniasis.
