Parasite

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline has antibacterial activity and antitumor activity.

SQ109 (NSC-722041) is an effective inhibitor of the trypomastigote form of the parasite (IC50 = 50 nM). SQ109 is an antitubercular agent and targets MmpL3.

Hypocrellin A is a natural PKC inhibitor with light-induced antitumor, antifungal and antiviral activities and also exerts immunomodulatory effects on MHC-restricted antigen presentation.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

Lotilaner is a parasiticide. It is used as a potent non-competitive antagonist of insects GABACl receptors (IC50 of 23.84 nM for Drosophila melanogaster GABA receptor). It also has no effect on a dog GABAA receptor.

RRx-001 is a potent inhibitor ofglucose 6-phosphate dehydrogenase(G6PD) and with potent antimalarial activity

(-)-Anonaine can be extracted from several species of Magnoliaceae and Annelidae and has antimalarial, antibacterial, antifungal, antioxidant, anticancer, antidepressant and vasodilatory activities. (-)-Anonaine induces apoptosis in human cervical cancer (HeLa) cells, induces DNA damage and inhibits the growth and migration of human lung cancer h1299 cells through Bax and caspase-dependent pathways.

Obatoclax Mesylate (GX15-070) is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3.

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

Santonin (alpha-Santonin) is a potent antiparasitic agent.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg kg, i.v., 50-200 J cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg m2, IV, 100 J cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

Andropanolide is a dipterocarbon from Andrographis paniculata with anti-HIV, antimalarial and anticancer activities and inhibits Lipopolysaccharides (LPS)-stimulated overproduction of nitric oxide (NO) in RAW264.7 macrophages.

Kukoamine A possesses anticancer, cytoprotective, antioxidant, and anti-inflammatory activities, it also has neuroprotective effects through inhibiting oxidative stress and apoptosis after whole-brain irradiation (WBI) in rats.

Licoflavone B has schistosomicidal activity, it showed high S. mansoni ATPase (IC50 of 23.78 μM) and ADPase (IC50 of 31.50 μM) inhibitory activities.

RR-11a analog (aza-peptide Michael acceptor, 7a) is an inhibitor of asparaginyl endopeptidase with IC50s of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.

N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent and the major biologically active amodiaquine metabolite. Its IC50 values against strains V1 S and 3D7 were 97 nM and 25 nM, respectively.

Dehydroemetine is an effective antigenic insecticide, which is a synthetic analogue of Emetine dihydrochloride. It can be used to prevent and treat amoeba infections and diseases. It has the effect of treating leishmania infection with skin damage and resistance to metronidazole amoebiosis.

Modoflaner is an antiparasitic (veterinary use).

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Sarolaner (PF-6450567) is an orally active, broad-spectrum ectoparasiticide with an LC80 of 0.3 μg mL against C. felis and an LC100 of 0.003 μg mL against O. turicata.

ZY-19489 is an antimalarial compound that is a potential single-dose cure for Plasmodium falciparum and Plasmodium vivax malaria. It has received orphan drug designation from the FDA.

CRK12-IN-2 is a potent inhibitor of CRK12.CRK12-IN-2 inhibits the parasite, with EC50 values of 3.2 and 0.08 nM for Trypanosoma congolense and Trypanosoma vivax, respectively.CRK12-IN-2 can be used for the prevention and treatment of trypanosomiasis in animals.

LeuRS-IN-1 hydrochloride is an orally active and highly potent inhibitor of Mycobacterium tuberculosis leucyl-tRNA synthetase with anti-leukemic activity and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in the study of leukemia.

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Dihydroartemisinin (Artenimol) is a metabolite of artemisinin.

Bruceine A (NSC-31616)(NSC-310616; Dihydrobrusatol) is a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.); are potential candidates for the treatment of canine babesiosis.

Afoxolaner is an isoxazoline insecticide acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect GABA and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

Asiatic acid (Dammarolic acid) is the aglycone of asiaticoside used in wound healing with antioxidant, anti-inflammatory, and neuroprotective properties.

Avermectin B1a is a macrocyclic lactone disaccharide anthelmintic agent .

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM).

Strictosamide possesses antibacterial and antiviral activities, it also may have important effects on inflammation and inflammatory pain.

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.

Ivermectin (MK-933) is an activator of glutamate-gated chloride channels (GluCls) with antiparasitic activity.

Beta-mangostin (β-Mangostin) is a xanthone compound with antibacterial and antimalarial activities. Beta-mangostin present in Cratoxylum arborescens and exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg mL. Beta-mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg mL. Beta-mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

UCT943 is an inhibitor of Plasmodium falciparum PI4K (IC50 = 23 nM).

UCB7362 (GLXC-26743) is an orally available and potent plasmepsin X (PMX) inhibitor with anti-malarial activity.UCB7362 inhibits parasite reproduction.

1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the growth of three pancreatic cancer cell lines, i.e., PANC-1, SW199 and CAPAN-1; induces cytotoxicity in Capan-2 cells via the induction of cellular apoptosis involving the mitochondrial pathway.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

Lupenone is a natural product isolated from Rhizoma Musae and has good anti-diabetic activity,and has anti-inflammatory activity.lupenone were potent PTP1B inhibitors with IC50 values of 15.11±1.23μM.

Artemisone (BAY 44-9585) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains (IC50: 0.83 nM). It also is a potent inhibitor of human CMV.