Trypanosoma Inhibitor

Dehydrobruceine A is a low potent antitrypanosomal agent, with an IC₅₀ of 88.5 nM for Plasmodium falciparum.

Alazopeptin is a non-ribosomal tripeptide azoamino acid antibiotic isolated from various Streptomyces species, with significant anti-tumor, antibacterial and trypanocidal activities. Alazopeptin exhibits cytotoxicity against mouse leukemia cells and S-180 tumor cells, inhibits the growth of Bacillus subtilis, and shows activity against Trypanosoma brucei. Alazopeptin can be widely used in studies related to mouse leukemia, S-180 tumor, human African trypanosomiasis and nagana.

Antiparasitic 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).

MDL 73811 is a potent AdoMetDC inhibitor and anti-trypanosomal compound. MDL 73811 has curative efficacy in a hemolymphatic model of HAT.

Antitrypanosomal agent 6 (compound 18a) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 6 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC₅₀ value of 0.47 μM. Antitrypanosomal agent 6 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA.

Antiparasitic agent-16, a pyridine-thiazolidinone, has anti-Trypanosoma cruzi and leishmanicidal activities. Antiparasitic agent-16 has IC₅₀s of 1.0 μM and 0.6 μM against trypomastigote and amastigote forms of T. cruzi. Antiparasitic agent-16 has IC₅₀s of 150.2 μM and 16.75 μM against trypomastigote and amastigote forms of L. amazonensis. Antiparasitic agent-16 induces parasite cell death through necrosis induction. Antiparasitic agent-16 induces morphological changes such as shortening, retraction and curvature of the parasite body and leakage of internal content with T. cruzi trypomastigotes.

Anti-Trypanosoma cruzi agent-8 is an anti-Trypanosoma agent and also a Trypanosoma cruzi trypanothione reductase (TcTR) inhibitor, with an IC₅₀ of 3.9 μM against TcTR. Anti-Trypanosoma cruzi agent-8 functionally inhibits the enzymatic activity of TcTR. Anti-Trypanosoma cruzi agent-8 exhibits trypanocidal activity against intracellular Trypanosoma cruzi amastigotes.

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

FTI-2628 is an antimalarial agent and a farnesyl transferase inhibitor, with an IC₅₀ of 41.7 nM against TbPET. FTI-2628 attenuates glucose-stimulated insulin secretion. FTI-2628 exhibits antimalarial activity against Trypanosoma brucei.

Antitrypanosomal agent 31 is an antitrypanosoma agent with a pEC50 of 6.4. Antitrypanosomal agent 31 inhibits GSK-3β, CDK-2, and CDK-4 with pIC₅₀s of 5.8, 6.9, and 7.1, respectively. Antitrypanosomal agent 31 can be used for the research of human african trypanosomiasis.

NEU-4438 is an antimalarial agent. NEU-4438 inhibits DNA synthesis, reduces AMPK-γ, and increases Clathrin heavy chain. NEU-4438 exhibits antiparasitic activity against Trypanosoma brucei. NEU-4438 reduces trypanosome tissue burden in a chronic HAT mouse model.

E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC₅₀ of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.

Antiparasitic agent-39 (Compound 14) is a selective antiparasitic agent and Deferasirox (HY-17359) derivative. Antiparasitic agent-39 reduces the mitochondrial membrane potential. Antiparasitic agent-39 shows antiparasitic activity against T. brucei, T. gambiense, L. Mexicana, T. gondii, B. divergens, P. falciparum with EC₅₀s of 4.2 nM, 10.4 nM, 52.0 nM, 17.0 nM, 41.2 nM, 54.8 nM, respectively.

Ambigol C is an ambigol, Antibacterial agent and Antimalarial agent. Ambigol C is isolated from Fischerella ambigua 108b. Ambigol C exhibits selective antibacterial activity against Gram-positive Staphylococcus aureus strains (including MRSA) with MIC values of 0.98-3.91 μg/mL. Ambigol C also shows potent antibacterial activity against B. megaterium, and possesses weak antimalarial and trypanocidal effects. Ambigol C can be used in the research of bacterial infections, plasmodial infections and trypanosomal infections.

Erioflorin is a sesquiterpene lactone compound originally isolated from plants of the Asteraceae family (such as Eriophyllum confertiflorum and species of the Podanthus genus). Erioflorin acts as a selective β-TrCP1 modulator. Erioflorin induces cell apoptosis by increasing intracellular reactive oxygen species (ROS) production and decreasing mitochondrial membrane potential, inhibits the NF-κB signaling pathway by blocking the phosphorylation of IκBα, and prevents the ubiquitination and degradation of the tumor suppressor Pdcd4 by inhibiting the interaction between Pdcd4 and the E3 ubiquitin ligase β-TrCP1. Erioflorin can be used in research related to breast cancer, colon cancer, advanced prostate cancer, and Chagas disease.