Parasite

Aramite is an insecticide that may have carcinogenic effects on mammals.

Abierixin 具备显著的抗球虫特性，同时具弱抗菌作用及离子载体活性。

Cycloguanil is an antimalarial.

Ivermectin B1b is the minor component . It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.

Aspyrone is a polyketide fungal metabolite that has been found inAspergillusand has diverse biological activities.1,2It is active against a panel of 13 fungi when used at a concentration of 20 μg/ml and a panel of 21 bacteria in a disc assay when used at a concentration of 100 μg per disc.1Aspyrone (10-1,000 mg/L) is nematocidal againstP. penetrans.2 1.Torres, M., Balcells, M., Sala, N., et al.Bactericidal and fungicidal activity of Aspergillus ochraceus metabolites and some derivativesPestic. Sci.53(1)9-14(1999) 2.Kimura, Y., Nakahara, S., and Fujioka, S.Aspyrone, a nematicidal compound isolated from the fungus, Aspergillus melleusBiosci. Biotech. Biochem.60(8)1375-1376(1996)

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.

Norbatzelladine L 是一种 Pdr5p 转运蛋白催化活性和功能活性的抑制剂。Norbatzelladine L 抑制 Pdr5p ATPase 活性，IC50值为 3.8 µM。Norbatzelladine L 具有抗真菌 (antifungal)、抗寄生虫 (antiparasitic)、抗病毒 (antiviral)、抗细菌 (antibacterial) 和抗肿瘤活性。

Antiparasitic agent-18 (compound 3a) 对T. brucei (EC50=0.4 μM)、T. cruzi (EC50=0.21 μM) 和 L. donovani (EC50=0.26 μM) 表现出高度的活性和选择性，证明其为一种有效的抗原虫化合物。

Cycloaspeptide A 是从内生真菌Penicillium janczewskii 中分离出来的，具有抗寄生虫活性。

Leucinostatin B is a peptide antibiotic from Paecilomyces lilacinus A-267.

NPD-1335 (Benzyl alkynamide 37) 一种有效的布氏锥虫磷酸二酯酶 B1 (TbrPDEB1) 抑制剂，具有针对布氏锥虫寄生虫的亚微摩尔活性。 NPD-1335 (Benzyl alkynamide 37) 显示出改善的细胞毒性谱。 NPD-1335 (Benzyl alkynamide 37) 会增加细胞内 cAMP 水平，导致细胞周期和细胞死亡的改变。

α-Cadinol 是一种抗真菌剂，可以抑制彩绒革盖菌 (Coriolus versicolor) 和硫磺多孔菌 (Laetiporus sulfureus) 的生长，并具有抗螨活性。

DXR inhibitor 11a是一种针对P. falciparum 1-脱氧-D-木糖-5-磷酸还原异构酶(DXR; IC50 = 0.11 µM)的抑制剂。它能够抑制在分离的人类红细胞中P. falciparum的生长(IC50 = 0.37 µM)。

Puberulic acid 对 Plasmodium falciparum K1 (chloroquine-resistant) 的 IC50 为 0.050 µM，显示抗疟疾活性。该化合物可从 Penicillium viticola 中分离。

RyRs activator 1 是兰尼碱受体 (RyRs) 的有效激活剂。RyRs activator 1 在 0.5 mg/L 时，杀幼虫活性为100%，在 0.01 mg/L 时，杀幼虫活性为90%。

MMV665852, an antischistosomal agent, has been shown to inhibit worm viability in vitro and reduce worm burden in S. mansoni-infected mice.

NPD-001 is an effective inhibitor of TbrPDEB1. NPD-001 is 10-fold more potent on hPDE4 (hPDE4B1 IC50 = 0.6 nM) than on TbrPDEB1 (IC50 = 4 nM).

Chlorempenthrin is a synthetic pyrethroid insecticide.

Oxamniquine is an effective compound for the treatment of schistosomiasis.

Ambelline 具有抗肿瘤活性。

Melarsomine, a trivalent arsenical compound, is employed as an adulticide for canine heartworm disease and other helminth infections. It has significant utility in the research of these conditions.

Antitrypanosomal agent 8 (compound 3b) 对布氏锥虫 (Trypanosoma brucei) 表现出较强的抗锥虫体作用 (IC50: 0.79 μM)。Antitrypanosomal agent 8 对 L6 细胞具有一定的细胞毒性，其 IC50 值为 80.95 μM。

Anti-infective agent 4 (compound 73) 是一种口服具有活力的 Trypanosoma cruzi 抑制剂 (IC50: 0.016 μM)。Anti-infective agent 4 能够有效降低体内寄生虫负担，能够用于研究感染。

Amphotalide is an anthelminthic agent.

Antimalarial agent 26是一种1,4-萘醌衍生物，作为口服抗疟药物，对恶性疟原虫(P. falciparum)表现出细胞毒性，并具有优于哺乳动物细胞系的选择性。该化合物能够有效抑制体内P. berghei引起的寄生虫血症。

Uredofos 是一种广谱驱虫药，它犬绦虫、蛔虫、钩虫和鞭虫都非常有效。

Liroldine is a new synthetic agent with antiamoebic activity.

Destomycin A 是一种具备多重生物活性的氨基糖苷类抗生素，能有效对抗革兰氏阳性菌及革兰氏阴性菌，同时具有抗真菌和驱虫的特性。此外，Destomycin A 可抑制 Escherichia coli 细胞中的多肽合成，并能激活动物组织内的腺苷酸环化酶。

CWHM-1008 is an effective oral antimalarial drug. The EC50 values of the drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains are 46 and 21 nM, respectively.

Soporidine 是由寄生植物 Striga hermonthica 萌发的拮抗剂。它能够特异性抑制 S. hermonthica 独脚金内酯受体，阻碍寄生虫的萌发。

Z-LLY-FMK (Calpain Inhibitor IV) 为一种钙蛋白酶抑制剂，涉及调控多个细胞系统的凋亡过程。该化合物能够抑制胆总管结扎所引起的肠细胞凋亡(apoptosis)。

Quinine hemisulfate是一种抗心律失常剂。Quinine hemisulfate 是一种口服有效的、选择性的细胞色素 P450db (cytochrome P450db) 抑制剂。Quinine hemisulfate 是 K+通道 (K+channel) 的有效阻断剂，IC50值为 19.9 μM。Quinine hemisulfate 同时具有抗疟疾的研究潜力。

Ebsulfur 是苯并异噻唑酮类的寄生虫抑制剂，靶向布氏锥虫 (Trypanosoma brucei) 的锥虫硫酮还原酶 (TryR)，其对布氏锥虫的IC50值为61-293 nM。Ebsulfur 可应用于非洲锥虫病的研究。

Tripynadine 是一种口服活性的抗疟药。

Anti-Trypanosoma cruzi agent-7（compound 1）是一种有效的Trypanosoma cruzi抑制剂，EC50为1.26 µM，适用于查加斯病的研究。

SARS-CoV-IN-3 is an effective SARS-CoV replication inhibitor.