toxoplasma gondii

Diclazuril (R-64433) 是一种具有口服活性的抗球虫剂，是苯乙腈衍生物。它可用于某些传染病和寄生虫病的相关研究。

CpCDPK1 TgCDPK1-IN-2 是 CpCDPK1 和 TgCDPK1 双重抑制剂，对 CpCDPK1 和 TgCDPK1 有抑制这样，IC50 值分别为 12 和 5 nM。CpCDPK1 TgCDPK1-IN-2 可用于研究弓形虫 (T. gondii)、细小隐孢子虫 (C. parvum) 和隐孢子虫 (C. hominus) 等顶复门原生动物感染相关疾病。

Spiramycin (Rovamycin) 是一种由安博链霉菌产生的大环内酯类抗生素，具有抗细菌和弓形虫活性，并具有抗寄生虫作用。它由 16 个内酯环组成，其上附着 mycaminose，forosamine 和 mycarose 三种糖。

Antibacterial agent 242 作为一种有效的1-去氧-D-木糖醇 5-磷酸还异构酶 (DXR) 抑制剂，针对Toxoplasmagondii显示出显著的抗性，其IC50值达到5.46 μM。此外，该化合物还能抑制体外TgDXR酶活性，并阻止T. gondii的增殖。

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 是一种广谱的 HDAC 抑制剂，抑制 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8、HDAC10 和 HDAC11。MC1742 在体外抑制寄生虫的生长，可阻断刚地弓形虫速殖子的生长并严重破坏寄生虫基因表达。MC1742 具有潜在的抗癌活性，抑制癌细胞生长停滞、凋亡和分化。

Fanotaprim 是二氢叶酸还原酶的有效抑制剂，抑制 tgDHFR (Toxoplasma gondiiDHFR) 和 hDHFR (human DHFR)的 IC50分别为 1.57 和 308 nM。Fanotaprim 在研究弓形虫病方面具有价值。

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. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

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可促进弓形虫的囊肿发育。缺乏 Phosphoglucomutase 会引发代谢疾病。

TgENR-IN-1 (Compound 5a) 作为弓形虫烯酰还原酶 (TgENR) 抑制剂, 在1 μM 浓度时可降低25%的TgENR活性。其在寄生虫组织中显示出的毒性较高，IC50 值超过 10 μM。

13,21-Dihydroeurycomanone (Pasakbumin C) 是从 Eurycoma longifolia 根部分离得到的一种天然产物，有抗寄生虫活性。

2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol能够抑制THP-1 cell line增殖，对Leishmania 和Toxoplasma gondii RH具有抗感染的作用。