Parasite Inhibitor

Isoquinoline is an analog of pyridine. Isoquinoline-based alkaloids, such as p-tolyl bisisoquinoline, phthaloyl isoquinoline, and naphthyl isoquinoline, exhibit anticancer activity. Berberine, an isoquinoline alkaloid, exerts anti-inflammatory effects in diabetic mice by downregulating the gene expression ratios of pro-/anti-inflammatory and Th1/Th2 cytokines. Additionally, some isoquinoline-based compounds also possess antidepressant, antibacterial, antimalarial, and anti-HIV activities.

Caryophyllene oxide ((-)-Caryophyllene oxide) is a bicyclic sesquiterpene with anticancer effects. Caryophyllene oxide induces apoptosis of PC-3 cells. Caryophyllene oxide shows analgesic and anti-inflammatory activities. Caryophyllene oxide has insecticidal, antioxidant, antimicrobial, antifungal, and antiparasitic properties.

Buparvaquone is a hydroxynaphthoquinone antiprotozoal agent related to parvaquone and atovaquone.

Santonin is an active principle of the plant Artemisia cina, which is formely used to treat worms.

Sodium metavanadate, 99% (Sodium vanadate (V), 99%) is an orally active phosphate structural analog and protein tyrosine phosphatase (PTPases) inhibitor. Sodium metavanadate, 99% mimics phosphate to interfere with phosphoprotein reactions, inhibits GAPDH, Na⁺/K⁺-ATPase and microbial membrane ATPase, and acts as a terminal electron acceptor for anaerobic respiration. Sodium metavanadate, 99% induces ROS production, G2/M phase arrest, mitochondrial membrane potential loss and apoptosis in breast cancer cells, and reduces tumor volume in tumor-bearing mice. Sodium metavanadate, 99% also exhibits oral insulin-sensitizing and metabolic regulatory activities, and reduces plasmodium parasitemia levels. Sodium metavanadate, 99% can be used in studies related to cadmium exposure-induced metabolic syndrome, plasmodium infection, breast cancer and type 1 diabetes.

Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors (nAChRs). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran binds to [³H]epibatidine in the neural cord membrane of American cockroach with an IC₅₀ of 890 nM and to [³H]α-bungarotoxin with an IC₅₀ of 36.1 μM. Dinotefuran exhibits knockdown activity (KD₅₀=0.351 nmol/g) and lethal activity (LD₅₀=0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks.

Cladosporin is an antibiotic and an an antifungal metabolite that can be produced in good yield in the mycelium of Cladosporium cladosporioid. Cladosporin exhibits inhibitory activity against various dermatophytes, plant pathogens, and bacteria. Cladosporin also exhibits antimalarial activity through inhibition of cytoplasmic lysine-tRNA synthetase of Plasmodium (PfKrs1).

bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC₅₀s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease.

Hycanthone is an apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor, DNA intercalator and Antischistosomal agent, with an IC₅₀ of 80 nM against APE1. Hycanthone irreversibly inhibits thymidine incorporation into DNA in adult sensitive *Schistosoma mansoni*, while exerts weak inhibitory effects on uridine and leucine incorporation. Hycanthone reduces influenza virus-induced interferon production. Hycanthone exhibits mutagenic effects in various organisms, shows teratogenicity in mice and rabbits, and induces neoplastic liver lesions in partially hepatectomized mice. Hycanthone can be used in research related to schistosomiasis and cancer.

10-Deacetylbaccatin-III is an intermediate in the preparation process of paclitaxel. 10-Deacetylbaccatin III can be isolated from the dried needles and small branches of the European yew tree (Taxus baccata). 10-Deacetylbaccatin III exhibits antileishmanial activity.

Lactupicrin (Lactucopicrin) exhibits analgesic, sedative, antimalarial activities and atheroprotective effect. Lactupicrin inhibits acetylcholinesterase (AChE) with an IC₅₀ of 150.3 μM. Lactupicrin is an orally active characteristic bitter sesquiterpene lactone.

Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic. Doramectin is an active compound against S.mansoni in an NMRI mouse infection model.

Risedronic acid (Risedronate) sodium, a bisphosphonate, is a potent anti-resorption agent that inhibits osteoclast-mediated bone resorption and changes the bone metabolism. Risedronic acid sodium suppresses osteoblast differentiation and induced caspase- and isoprenoid depletion-dependent apoptosis. Risedronic acid sodium inhibits blood stages of Plasmodium falciparum (IC₅₀ of 20.3 μM). Risedronic acid sodium inhibits the transfer of the farnesyl pyrophosphate group to parasite proteins.

Broxyquinoline (Dibromohydroxyquinoline) is an effective inhibitor of severe fever with thrombocytopenia syndrome virus (SFTSV) with an IC₅₀ of 5.8 µM. Additionally, Broxyquinoline is an inhibitor of CpACBP₁ with an IC₅₀ of 64.9 μM. CpACBP₁ is a fatty acyl-CoA binding protein of Cryptosporidium parvum, thus Broxyquinoline has the potential to inhibit parasite growth. Broxyquinoline shows promise for research in the field of infectious diseases.

Benzimidazole is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

Oxantel pamoate (Oxantel embonate) is an anthelmintic agent that potently against Trichuris muris. Oxantel pamoate inhibits fumarate reductase (Frd) activity in some pathogenic bacteria and inhibits P. gingivalis homotypic biofilm formation (IC₅₀ of 2.2 μM).

(R)-(-)-2-Phenylglycinol (D-Phenylglycinol; (-)-Phenylglycinol) is a chiral β-amino alcohol, a starting material for chiral synthesis, and a potential nematicide. (R)-(-)-2-Phenylglycinol exhibits nematicidal and egg hatching inhibitory activity against the southern root-knot nematode (Meloidogyne incognita), and is also an upregulated metabolite in the fermentation broth of Streptomyces aquilus JXGZ01. (R)-(-)-2-Phenylglycinol can be used as a framework for constructing zwitterionic bicyclic lactams and multi-substituted piperidine/piperidine acid drugs. (R)-(-)-2-Phenylglycinol can be used in drug synthesis and nematode infection-related research.

Tioconazole (UK-20349) is a broad-spectrum antifungal imidazole derivative. Tioconazole inhibits several dermatophytes and yeasts, with MIC₅₀ values of less than 3.12 mg/L and 9 mg/L, respectively. Additionally, Tioconazole exhibits anti-parasitic activity. Tioconazole exerts anticancer activity by inhibiting the PI3K/AKT/mTOR signaling pathway and blocking autophagy. Tioconazole is applicable for research in the fields of anti-infection and anticancer therapy.

Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes.