Anti-Cancer

Cecropin B is a 35 amino acid chain that functions as an antibacterial and anti-cancer peptide. It is characterized by two alpha helices and has been researched because of the low cytotoxicity produced. Cecropin B has been shown to produce in vivo cytotoxic effects against stomach carcinomas. It has also been used to synthesize derivatives with activity against other cancer cell lines.

Cecropin B has been shown to cause bacterial and cancerous cell death by insertion into the cellular membrane, which is due to amphiphilic N-terminal residues. In low lipid to peptide membrane component ratios, cecropin B will form ion channels that will disrupt metabolic gradients and lead to cell death. With high membrane peptide concentrations, cecropin B was observed to aggregate membrane peptides and break the membrane into fragments.

Cecropin P1, porcine is a 31 amino acid antibacterial protein that can be isolated from pigs. Cecropin P1 is used as an antibacterial, antifungal and anti-cancer compound. The wide ranging effects of cecropin P1 are properties of its amphipathic N-terminal, lipophilic C-terminal and alpha helical structure. With these structural characteristics, cecropin P1 can bind to the membranes of pathogens and cancerous cells. Cecropin P1 then is inserted into the membrane of the respective cell and disrupts lipid bilayer cohesion, causing rapid membrane degradation and cell lysis.

Cephalomannine is an alkaloid compound derived from the plant Cephalotaxus manii and is a precursor of paclitaxel. It is used for its antineoplastic capabilities, which allow it to stabilize and halt microtubule formation during mitosis. Stalling microtubule formation increases Raf-1 expression stimulating downstream apoptotic pathways.

Clofazimine is an active phenazine composed of an imino group and aromatic tricyclic heterocycles that is used as an antimycobacterial, anti-inflammatory and anti-cancer compound. It has been shown to be a potent in vivo antimycobacterial agent toward Mycobacterium leprae and in vitro to Mycobacterium avium.

As an anti-inflammatory, clofazimine inhibits reactive oxygen species (ROS) formation within neutrophils by inhibiting myeloperoxidase catalyzed reactions. The formed ROS are responsible for activating tumor necrosis factor alpha (TNFα) and interleukin 8 (IL8), which are inflammatory cytokines.

Colchicine is an alkaloid isolated from Colchicum autumnale and other Colchica species. It is an antimitotic agent useful against various cancer cell lines. Colchicine disrupts microtubules and can be used to induce tetraploidy in plant cells. It is an activator of the JNK/SAPK signaling pathway and used to select for cells containing MDCK (NBL-2) resistance. Colchicine’s antimitotic properties are more effective against cancer cells due to their increased mitotic rate compared to that of healthy cells. Colchicine is useful in cell division studies.

Cryptotanshinone is a quinoid diterpene extracted from Salvia miltiorrhiza Bunge and has been used as an antibacterial, anti-inflammatory and anti-cancer compound. As an antibacterial agent, cryptotanshinone exhibits a broad range of activity against gram positive bacteria. In vivo studies of bactericidal mechanisms have shown cryptotanshinone to form superoxides which damage bacterial proteins, lipids and DNA.

Cryptotanshinone has also been used as an anti-inflammatory by inhibiting both nuclear factor-κB (NF-κB) activation and phosphorylation of mitogen-activated protein kinases (MAPK). The anti-inflammatory actions occur in downstream pathways, inhibiting p38 MAPK, c-Jun N-terminal kinases (JNKs) and lipopolysaccharide induced inflammation. Inhibition of these pathways and molecules will decrease pro-inflammatory pathway responses as well as cytokine synthesis.

As an anti-cancer agent, cryptotanshinone was used to inhibit cancer cell proliferation through the decreased expression of cyclin D1 or increase in cyclin A1 and cyclin B1 expression. It was also used to impede cancer motility by inhibiting complement component 5a protein (C5a), an analphylatoxin. Cryptotanshinone has also been used to reduce cell motility by inhibiting basic fibroblast growth factor (bFGF), a promoter of angiogenesis. Apoptotic effects were also observed by cryptotanshinone when it was used to inhibit signal transducer and activator of transcription-3 expression, which upregulates cell survival pathways.

The cyclosporins are a group of macrolide immunosuppressants isolated from fungi. They are researched for their use in prevention of post-transplant graft rejection. Their mechanism of action involves suppression of cytotoxic T-cell maturation and activity by binding lymphocyte protein cyclophilin. Cyclophilin and cyclosporin form a complex targeting calcineurin, which is responsible for activating T-lymphocytes. Additionally, the cyclosporins are researched for their ability to prevent damage to normal functioning cells in autoimmune disorders.

Cyclosporin A is over 99% pure and soluble in DMSO and ethyl alcohol.

The cyclosporins are a group of macrolide immunosuppressants isolated from fungi. They are researched for their use in prevention of post-transplant graft rejection. Their mechanism of action involves suppression of cytotoxic T-cell maturation and activity by binding lymphocyte protein cyclophilin. Cyclophilin and cyclosporin form a complex targeting calcineurin, which is responsible for activating T-lymphocytes. Additionally, the cyclosporins are researched for their ability to prevent damage to normal functioning cells in autoimmune disorders.

Cyclosporin B is soluble in DMSO and ethyl alcohol.

The cyclosporins are a group of macrolide immunosuppressants isolated from fungi. They are researched for their use in prevention of post-transplant graft rejection. Their mechanism of action involves suppression of cytotoxic T-cell maturation and activity by binding lymphocyte protein cyclophilin. Cyclophilin and cyclosporin form a complex targeting calcineurin, which is responsible for activating T-lymphocytes. Additionally, the cyclosporins are researched for their ability to prevent damage to normal functioning cells in autoimmune disorders.

Cyclosporin D is soluble in DMSO and ethyl alcohol.

Dabrafenib is a compound used as a serine/threonine-protein kinase B-Raf inhibitor for oncology research. It competitively inhibits V600E BRAF gene mutations which are characteristic in melanoma cancers. Inhibition of B-Raf proteins, by dabrafenib, interrupts mitogen-activated protein kinase/extracellular signal regulated kinase (MAPK/ERK) pathways, which regulate cell growth.This action halts cell proliferative activity and engages apoptosis.

Dacarbazine (DTIC) is an anti-cancer prodrug that has been used as a standard for comparing the efficacy of new antineoplastic compounds. It is used with other anti-cancer compounds to both increase potency and disrupt side-effects generated by DTIC. While being a strong antineoplastic agent, DTIC has also been shown to stimulate interleukin 8 (IL8) and vascular endothelial growth factor (VEGF) expression in cancer cells.

DTIC is transformed by liver enzymes into its active methyl diazonium cation form. The active form of DTIC has displayed anti-tumor activity following light exposure. It has been shown that the light exposure catalyzes methyl diazonium cation to form a carbine and aryl radical. These radicals damage DNA of malignant cancer cells, producing cytotoxic effects and eventual cell death.

Dexamethasone 21-phosphate disodium salt is a system glucocorticoid with anti-inflammatory properties. Dexamethasone 21-phosphate disodium salt is the pro-drug, which is converted to dexamethasone. It stimulates uptake of glutamine in the cerebral cortex and induces apoptosis. Additionally, it is an inhibitor of the sodium phosphate symporter and GR activator.

Dihydrotanshinone I is a compound extracted from the plant Salvie miltorrhiza Bunge. It is used as a gram positive antibacterial and anti-cancer compound. In both in vivo and in vitro research, dihydrotanshinone I generated reactive oxygen species which trigger apoptosis in bacteria and cancer cells.

Dihydrotanshinone I triggers apoptosis by directly damaging DNA and preventing further replication or by activating p38 mitogen-activated protein kinases (p38 MAPK). This class of protein kinase engages apoptosis by activating caspases which are proteases that induce cell death. Dihydrotanshinone I has also been shown to inhibit cell growth past the G1 stage and prevent blood vessel formation by inhibiting hypoxia-inducible factor (HIF-1) activity.

Doxorubicin HCl is an anthracycline antibiotic that inhibits cancer progression by suppressing DNA replication. It is the 12-hydroxylated form of daunorubicin and causes DNA intercalation. It also inhibits topoisomerase II. Doxorubicin is researched for its efficacy against non-Hodgkin’s lymphoma, multiple myeloma, acute leukemias, Kaposi sarcoma, Wilm tumor, Ewing sarcoma, and cancers of the breast, lung, ovary, endometrium, and adrenal cortex. Doxorubicin is an MRP-1 substrate and has been used in drug-resistance studies.

Embelin is a benzoquinone derivative found in Ardisia japonica which is a plant native to eastern Asia. It is used as an anti-cancer compound as well as an anti-inflammatory. Embelin has also been exhibited anthelminthic properties against cestode parasites.

In oncology research, embelin has been used to disrupt X-linked inhibitor of apoptosis (XIAP) activity. Embelin binds the Baculovirus IAP Repeat 3 (BIR3) domain on XIAP and subsequently disrupts apoptosis regulation. Inactivation of BIR3 allows proteins caspase-9 and Diablo homologs/Smac proteins to freely promote apoptotic pathways.

Embelin has also been used to quell inflammatory responses by inhibiting eicosanoid synthesis.It has been shown that embelin targets eicosanoid synthesizing proteins 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase (MPGES). Embelin has also been shown to disrupt eicosanoid synthesis through XIAP suppression.

Emodin is a compound used as an anti-inflammatory and anti-cancer agent. It has been shown that emodin suppresses inflammatory responses in vitro by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) protein complexes. This effect occurs from emodin binding and preserving an inhibitory subunit on NF-κB.

Emodin has also been shown to induce apoptosis in mouse neuroectodermal tumors both in vivo and in vitro. Cell death is induced by inhibiting protein tyrosine kinase (PTK), a regulator of cell growth. Constraining PTK activity prevents further cell development which signals an apoptotic cascade.

Epibrassinolide is a plant steroid hormone of the brassinosteroid family. Its functions include protection from environmental stressors and altering the metabolism under a variety of conditions. Epibrassinolide has been shown to decrease toxicity and stimulate healthy plant growth in plants under stress.

EGCG has been shown to have a broad spectrum of antibacterial activity against gram positive and some gram negative bacteria. It is used synergistically with penicillin binding protein inhibitors because both target peptidoglycan on the cell wall. While the exact mechanism is not known, research on EGCG activity indicates bacterial cell wall damage by direct peptidoglycan binding.

Erlotinib HCl is an anti-cancer agent targeting epidermal growth factor receptor (EGFR) tyrosine kinase ATP binding sites, which are commonly overexpressed and sometimes mutated in a variety of cancers. Erlotinib prevents the formation of EGFR homodimers leading to suppression of signal transmittance and tumor growth inhibition. Additionally, erlotinib suppresses cyclin-dependent kinase 2 (Cdk2). It has been shown to be effective against non-small cell lung cancer and pancreatic cancer.

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.