Leishmania Inhibitor

PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC₅₀s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.

Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.

Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC₅₀ of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC₅₀ of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

25-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).

Naringenin 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).

DNDI-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.

Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC₅₀ of 12.2 μM in HeLa cells. Retro-2 induces cell autophagy.

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC₅₀ of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC₅₀s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica.

Isopimpinellin, an orally active compound isolated from Glomerella cingulata. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect.

Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity.

Dehydroemetine is an orally active antiparasitic agent. Dehydroemetine can inhibit parasites such as Entamoeba histolytica, and it can also be used in the research of parasitic diseases like visceral leishmaniasis.

Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC₅₀=0.27 μg/ml).

BpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC₅₀s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. BpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). BpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

Harpagide is a class of iridoid glycoside isolated from Scrophularia ningpoensis and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes (T.b. rhodesiense) with an IC₅₀ of 21 μg/mL. Harpagide exerts significant antileishmanial activity against L. donovani with an IC₅₀ value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities.

Defensin HNP-1 human is a type of human neutrophil peptide (HNPs). Defensin HNP-1 human possesses immunomodulatory functions and can delay the apoptosis of neutrophils. Defensin HNP-1 human inhibits DNA/RNA/protein synthesis and interferes with metabolic pathways, thus exhibiting broad antibacterial activity. Defensin HNP-1 human has direct inactivation effects on HIV, HSV-1, HSV-2, CMV, influenza virus, etc. Defensin HNP-1 human has antileishmanial activity. Defensin HNP-1 human is involved in endothelial cell dysfunction during the early development of atherosclerosis.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC₅₀s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.

Hypocrellin B, a pigment isolated from the fungi Hypocrella bambusae and Shiraia bambusicola, is an apoptosis inducer. Hypocrellin B can be used as a photosensitizer for photodynamic therapy of cancer. Hypocrellin B also has antimicrobial and antileishmanial activities.

Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.