Anti-Parasite

Albendazole is a benzimidazole derivative typically used as a comprehensive antiparasitic belonging to the anthelminthic group and works by disrupting microtubule formation. Microtubule disruption diminishes glucose transport which increases glycogen catabolism. Eventually, this net loss of energy results in tissue death.

The resulting tissue death caused by microtubule formation is a sought after mechanism in oncology research. In vitro research of albendazole on HNSCC (head and neck squamous cancer cells) had shown cell cycle arrest in G2/M stage, resulting in apoptosis. Disruption of microtubule formation also prevented malignant cell migration.

Artesunate is a synthetic compound that is highly employed for its anti-malarial capabilities and is currently studied for its applications in oncology research and surgical procedures. In anti-malarial studies, it has been shown to disrupt EXP1 activity, which is a glutathione transferase responsible for cell detoxification in Plasmodium falciparum. Artesunate activity has been shown to be enhanced when co-administered with amodiaquine HCl.

In oncology research, Artesunate is used to arrest cancer growth in the G2/M phase and upregulate proteins p21 and Beclin1. These proteins are mainly related to apoptosis with p21 being a regulator of the process and Beclin1 playing a role in cell death by autophagy. Artesunate has also been shown to form an endoperoxide bridge which generates carbon radicals that dismantle the cell. However, the observed radical formation is dose and time dependent.

Artesunate has been shown to provide organ damage reduction in rats exposed to hemorrhagic shock. Administration of ART occurred after resuscitation and did not function as a preventative. Artesunate operates by decreasing cell apoptosis through protein kinase B (PKB) stimulation and glycogen synthase kinase inhibition. Cell survival is also enhanced by nuclear factor kappa B (NfkB) suppression, diminishing proinflammatory cytokine synthesis.

Dimethylcarbamazine citrate salt (DEC) is an antiparasitic piperazine derivative that has been used against Wuchereria bancrofti. It is a stable compound in salt form and has been used to research antimalarial resistances in W. bancrofti. DEC inhibits arachidonic acid synthesis, which is a key component for a protective sheath formed by pre-larval W. bancrofti called microfilaria.

Flubendazole is a benzimidazole compound that is used as an antiparasitic and anti-cancer agent. It has been shown to be an effective anthelminthic chemical by inhibiting tubulin synthesis and disrupting cytoskeleton formation. Flubendazole has also been shown in vivo to be a strong anti-cancer compound by the same mechanism and is potent toward vinblastine resistant cell lines.

Tubulin is vital protein component that provides the structural shape of cells as well as being integral to replication. Halting tubulin formation ruins the structural integrity and dysregulates cytosolic equilibrium. Tubulin inhibition also effects the subfamilies α-tubulin and β-tubulin which facilitate chromosomal migration during cellular replication.

Formononetin is an isoflavonoid phytoestrogen that is used in microbiology and oncology research as a vasodilator, anti-viral, anti-inflammatory and anti-cancer agent. It has also been used as an anti-parasitic compound against Giardia lamblia trophozoites however, the mechanism of action is not well understood.

Praziquantel is an anthelmintic drug used against schistosomes and cestodes. It functions by increasing the tegmentum permeability to calcium ions. This induces paralytic muscle contraction and death. Praziquantel is more effective on adult parasites than young parasites. It suppresses glucose uptake and stimulates lactate release.

Praziquantel is used to study voltage-gated calcium channels.