gondii

13,21-Dihydroeurycomanone (Pasakbumin C) is a natural product isolated from the root of Eurycoma longifolia with antiparasitic activity such as Plasmodium falciparum and Toxoplasma gondii.

Fluphenazine decanoate is dopamine D2 receptor blocke,and is a long-acting phenothiazine neuroleptic that used to treat schizophrenia.

Diclazuril (R-64433) is a coccidiostat.

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor, suppressing the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM, a hDHFR IC50 of 308 ± 71 nM, and a hDHFR to TgDHFR selectivity ratio of 196.

CpCDPK1/TgCDPK1-IN-2 is a dual inhibitor of CpCDPK1 and TgCDPK1 with IC50 values of 12 and 5 nM for CpCDPK1 and TgCDPK1, respectively.CpCDPK1/TgCDPK1-IN-2 can be used in the study of diseases associated with infection of toxoplasmas such as Toxoplasma gondii, Cryptosporidium parvum and C. hominus. CpCDPK1/TgCDPK1-IN-2 can be used to study diseases associated with infections of toxoplasma gondii (T. gondii), Cryptosporidium parvum (C. parvum), and Cryptosporidium hominus (C. hominus).

Spiramycin (Rovamycin) is a macrolide antibiotic produced by Streptomyces ambofaciens, effective against gram-positive aerobic pathogens, N. gonorrhoeae, and staphylococci, and is used to treat infections caused by bacteria and Toxoplasma gondii.

2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and exhibits anti-infective activity against Leishmania and Toxoplasma gondii RH.

LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion. LHVS is a potent, non-selective cysteine protease inhibitor.

Antibacterial agent 242, a potent inhibitor of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR), demonstrates an IC50 of 5.46 μM against Toxoplasma gondii. It effectively inhibits the enzymatic activity of TgDXR in vitro as well as the proliferation of T. gondii.

Antiparasitic agent-25 (Compounds 11) is an orally active antiparasitic compound. It inhibits the invasion and replication capabilities of parasites and has an irreversible effect on Toxoplasma gondii. The agent significantly reduces the replication rate of Toxoplasma gondii, with an IC50 value of 6.33 μM, and exhibits low cytotoxicity, having a CC50 value of 285 μM.

ELQ-121 is a potent inhibitor of the ubiquinol oxidation (QO) site in parasites. It exhibits an in vitro IC50 of 0.05 nM against both chloroquine-sensitive and multi-drug resistant Plasmodium falciparum. ELQ-121 also inhibits Toxoplasma gondii and Neospora caninum with an in vitro IC50 of less than 1 nM. It hinders the proliferation of Bacteroides fragilis tachyzoites with an IC50 of 0.49 nM and induces mitochondrial disruption. Furthermore, ELQ-121 can be formulated into a polyethylene glycol carbonate prodrug, which shows efficacy against P. yoelii in mice. ELQ-121 is applicable for antimalarial research.

Antitoxoplasmal agent-1 (Compound 4) is an antiparasitic agent with significant activity and selectivity against T. gondii, exhibiting an IC50 of 3.1 μM. It also demonstrates activity against L. major promastigotes with an EC50 of 23.3 μM. This compound is applicable for research into parasitic diseases.

Conoidin A is a cell-permeable inhibitor of the T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. It covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 μM. It also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for research on ischaemic heart disease.

TRC-19 is a potent and selective inhibitor of Toxoplasma gondii dihydrofolate reductase. TRC-19 shows an IC50 of 9 nM and 89-fold selectivity in favor of Toxoplasma gondii dihydrofolate reductase.

Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Antiprotozoal antibiotics. II. Isolation and characterization of trypacidin, a new antibiotic, active against Trypanosoma cruzi and Toxoplasma gondiiJ. Antibiot. (Tokyo)16157-160(1963) 2.Song, Z., Liu, Y., Gao, J., et al.Antitubercular metabolites from the marine-derived fungus strain Aspergillus fumigatus MF029Nat. Prod. Res.1-8(2019) 3.Gauthier, T., Wang, X., Dos Santos, J.S., et al.Trypacidin, a spore-borne toxin from Aspergillus fumigatus, is cytotoxic to lung cellsPLoS One7(2)e29906(2012)

MC1742 is a broad-spectrum HDAC inhibitor, inhibiting HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10, and HDAC11. MC1742 inhibits the growth of parasites in vitro, blocking the growth of Toxoplasma gondii tachyzoites and severely disrupting the expression of parasitic genes. MC1742 has potential anticancer activity, inhibiting the growth arrest, apoptosis, and growth of cancer cells. MC1742 has potential anticancer activity, inhibiting growth arrest, apoptosis and differentiation of cancer cells.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

17-GMB-APA-GA, a potent HSP90 inhibitor, is an ADC cytotoxin commonly employed for studying latent T. gondii infection.

Anti-Trypanosoma cruzi agent-1 (Compd 3b), a selective compound against NINOA trypomastigote (IC 50 = 0.51 μM) and INC-5 epimastigote (IC 50 = 3.06 μM), also possesses anti-T. gondii activity [1].

MMV687807 is a potent anthelmintic compound exhibiting strong efficacy against Toxoplasma gondii (T. gondii). It demonstrates an IC50 value of 0.15 μM and a CC50 value of 1.69 μM [1].

GW300657X is a small molecule inhibitor that blocks toxoplasma gondii rhoptry kinase 18 and maintains moderate CDK2-cyclin A inhibitory activity.

Phosphoglucomutase promotes cyst development in Toxoplasma gondii. Deficiency of Phosphoglucomutase causes metabolic disorders.

4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties. It effectively reduces the population of Vero cells infected by T. gondii promastigotes and amastigotes, with EC50 values of 0.8 and 0.37 µM, respectively. Furthermore, at concentrations of 4 and 8 µM, CDF enhances the efficacy of 5-fluorouracil and oxaliplatin in inhibiting the formation of both primary and secondary colonospheres in chemoresistant HCT116 cells.

4-Thiouracil is a photoactivatable probe designated for site-specific applications in detecting RNA structures and nucleic acid-nucleic acid contacts. Upon illumination with ultraviolet light exceeding 300 nm and in the presence of oxygen, it serves as an energy donor, facilitating the generation of singlet oxygen through triplet-triplet energy transfer. This process enables the highly reactive oxygen species to interact with 4-thiouracil, leading to the formation of uracil and uracil-6-sulfonate; the latter exhibits fluorescence around a wavelength of approximately 390 nm. Additionally, 4-Thiouracil functions as a substrate for T. gondii uracil phosphoribosyltransferase, allowing the synthesis of 4-thiouridine monophosphate for subsequent integration into RNA.