Toyocamycin is a nucleoside- type antibiotic analogue of adenosine, isolated from Streptomyces species. Toyocamycin is an antibiotic first isolated by Nishimura et al. from a new species of Streptomyces (St. toyocaensis), with a rather specific antibiotic spectrum. It strongly inhibits Candida albicans and Mycobacterium tuberculosis, without notable action on other microorganisms, such as many gram-positive and gramnegative bacteria, fungi, and yeast. Toyocamycin is an anti-tumor antibiotic with various target activities. Toyocamycin is a potent inhibitor of RNA self-cleavage in mammalian cells. It also inhibits phosphatidylinositol kinase, a cell proliferation regulator. Toyocamycin can suppress thapsigargin-, tunicamycin- and 2-deoxyglucose-induced XBP1 mRNA splicing in HeLa cells. This suppression doesn’t affect the activating of transcription factor 6 (ATF6) and PKR-like ER kinase (PERK)’s activation. Toyocamycin prevents IRE1a-induced XBP1 mRNA cleavage in vitro. In mammalian cells, toyocamycin inhibits RNA synthesis. Toyocamycin induces apoptosis of MM cells including bortezomib-resistant cells at nanomolar levels in a dose-dependent manner. It also inhibited growth of xenografts in an in vivo model of human multiple myeloma. It is also a lead compound for developing anti-MM therapy and XBP1 as an appropriate molecular target for anti-multiple myeloma therapy. Toyocamycin was the first identified small-molecule inhibitor of Rio1, showing mixed inhibition. This mode of action of toyocamycin results from its dual activity towards the Rio1 kinase. On the one hand, toyocamycin acts as an ATP-competitive inhibitor, and on the other hand, it stabilizes the less catalytically active oligomeric isoform of the Rio1 kinase.

Cystine is the oxidized dimer form of the amino acid cysteine. Cystine serves two biological functions, a site of redox reactions and a mechanical linkage that allows proteins to retain their 3-dimensional structure. It is common in many foods such as eggs, meat, dairy products, and whole grains as well as skin, horns and hair. Human hair and skin contain approximately 10–14% cystine by mass. Cysteine supplements are sometimes marketed as anti-aging products with claims of improved skin elasticity. Cysteine is more easily absorbed by the body than cystine, so most supplements contain cysteine rather than cystine. N-acetyl-cysteine (NAC) is better absorbed than other cysteine or cystine supplements.

Mangafodipir (sold under the brand name Teslascan as mangafodipir trisodium) is a contrast agent delivered intravenously to enhance contrast in magnetic resonance imaging (MRI) of the liver. Mangafodipir is a manganese (Mn2+) chelate with the ligand fodipir (dipyridoxyl diphosphate or DPDP). Mangafodipir trisodium is metabolised (dephosphorylated) and partially transmetallated (manganese exchanged for zinc) after intravenous administration. Manganese that is released from mangafodipir is taken up by hepatocytes thereby increasing the SI of normal liver tissue. This may result in an improvement of the detection of liver metastases, which usually have no hepatocytes. The metabolites of fodipir are renally excreted, whilst the biliary route mainly excretes manganese. Mangafodipir was withdrawn from the US market in 2003 and the European market in 2012.

Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.

Tangeretin is an O-polymethoxylated flavone that is found in tangerine and other citrus peels. Its natural role is to strengthen the cell wall and act as a plant's defensive mechanism against disease-causing pathogens. Animal studies have shown the potential fo tangeretin as a therapeutic in a number of conditions including cancers, asthma, CKD, hypercholesterolemia, and Parkinson's disease.

Hederagenin is a triterpenoid saponin. It can inhibit LPS-stimulated expression of iNOS, COX-2, and NF-κB. Hederagenin exhibits multiple pharmacological activities in the treatment of hyperlipidemia, antilipid peroxidation, antiplatelet aggregation, liver protection, antidepression, anti-inflammation.

Lanosterol represents the first step in sterol formation and can be converted by lanosterol 14 α-demethylase (CYP51, a member of the cytochrome P450 family), to follicular fluid meiosis activating factor (FF-MAF), a sterol intermediate that has been extensively studied and shown to activate meiosis in gametes. Lanosterol modulates TLR4-mediated innate immune responses in macrophages. Lanosterol accumulation increases membrane fluidity and ROS production, thus potentiating phagocytosis and the ability to kill bacteria. Preliminary studies in dogs and rabbits have shown that lanosterol can prevent and even reverse cataract formation. However, Lanosterol 25 mM solution did not reverse opacification of human age-related cataractous nuclei. Lanosterol induces mitochondrial uncoupling and protects dopaminergic neurons from cell death in a model for Parkinson's disease.

Madecassic acid is a naturally produced terpene from Centella asiatica. It has demonstrated anti-inflammatory and anti-diabetic effects by blocking NF-kB activation and altering lipid metabolism in mice. Madecassic acid has also shown anti-tumor effects in a mouse model of colon cancer; and, was demonstrated in vitro to stimulate the growth of neurofilaments from rat PC1 cells.

Osthol is an O-methylated coumarin found in plants such as Cnidium monnieri, Angelica archangelica and Angelica pubescens which are often used in traditional eastern medicine. It is known to be a calcium channel blocker and is reported to have neuroprotective, osteogenic, immunomodulatory, anticancer, hepatoprotective, cardiovascular protective, and antimicrobial activities.

Zingerone is one of the active phenolic components isolated from Zingiber officinale. Zingerone is primarily present in dry ginger, but cooking or drying also converts gingerol into zingerone by a retroaldol reaction. Chemically synthesized zingerone is vanillyl acetone, which is a member of the phenolic alkanone group, and its varied pharmacological properties include antioxidant, anti-inflammatory, and anticancer activities. Thus, zingeroneshowed strong anti-angiogenic activity via the inhibition of MMP-2 and MMP-9 during tumor progression. Zingerone was likely to be broad-spectrum anti-inflammatory agents in most organs that suppressed the activation of NF-κB, the production of IL-1β, and the infiltration of inflammatory cells in mice. Zingerone effectively inhibits 1,2-dimethylhydrazine-induced colon carcinogenesis in male Wistar rats. Zingerone possess radioprotective effects in laboratory animals and in cultured cells in vitro. Zingerone produced marked improvement in stress induced irritable bowel disorder, which could be attributed to the powerful antioxidant nature, direct effect on the intestinal smooth muscle and adaptogenic nature. Analysis of the qualities that constituted zingerone irritation found that the sensations produced are predominantly burning and warmth, making it qualitatively similar to capsaicin.