Cryptotanshinone is one of the major tanshinones isolated from the roots of the plant Salvia miltiorrhiza Bunge (Danshen). Danshen has been widely used in traditional Chinese medicine for treatment of a variety of diseases, including coronary artery disease, acute ischemic stroke, hyperlipidemia, chronic renal failure, chronic hepatitis, and Alzheimer's disease, showing no serious adverse effects. Recent studies have shown that cryptotanshinone not only possesses the potential for treatment and prevention of the above-mentioned diseases, but also is a potent anticancer agent. In vitro studies have demonstrated that cryptotanshinone inhibits cell proliferation in a variety of cancer cell lines, including rhabdomyosarcoma, melanoma, cervical, colon, breast and prostate cancer cells. It has been described that cryptotanshinone induced a G1/G0 cell cycle arrest in rhabdomyosarcoma (Rh30) and prostate cancer (DU145) cells by downregulating expression of cyclin D1 and phosphorylation of retinoblastoma protein (Rb), but induced a G2/ M cell cycle arrest in melanoma (B16) cells via upregulating expression of Cdc25c, cyclin A1 and cyclin B1. Cryptotanshinone inhibiting expression of Aurora A kinase led to significant suppression of prostate cancer cells in vitro and in mice. Cryptotanshinone also induces cell death in cancer cells.

Schisandrin is a bioactive compound found in Schisandra chinensis. Schisandrin exhibits antioxidant properties and ameliorates ovariectomy-induced memory impairment in rats, and Aβ1-42-induced memory impairment in mice. Schisandrin has an anti-asthmatic effect on OVA-induced airway inflammation in a murine asthma model. The compound inhibits proliferation of breast cancer cell lines at concentrations of 20-100 uM.

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.

S-Adenosyl-L-homocysteine (SAH), a potent methyltransferase inhibitor and a substrate of the s-adenosylhomocysteine hydrolase, is an amino acid derivative and an intermediator or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis. It was shown, that the plasma SAH might be a novel biomarker for the early clinical identification of cardiovascular disease. In addition, the elevated SAH in Alzheimer's brain was related to markers of disease progression and cognitive impairment.

GW-9508 is a small-molecule agonist of the fatty acid receptors GPR40 and GPR120. GW-9508 exerts wide-range activity in animal models: anti-depressant, anti-inflammatory, anti-diabetic and analgetic actions.

E-2012 is a gamma secretase modulator that is being evaluated as a potential new treatment for Alzheimer's disease. E-2012, a new chemical entity discovered by Eisai, has shown some potential in non-clinical studies to reduce the production of beta-amyloid Abeta 40/42 by modulating the function of gamma-secretase without interfering with the Notch-processing.

Pseudopelletierine is the main alkaloid derived from the root-bark of the pomegranate tree (Punica granatum). Pseudopelletierine is used as an enzyme substrate.

Isovitexin (apigenin-6-C-glucoside), an isomer of vitexin, is found in plants such as pigeon pea, Passiflora, bamboo, mimosa, wheat leaves, rice hull of Oryza sativa and others. Isovitexin is poorly absorbed in the gastrointestinal tract. The highest level of intravenously administrated isovitexin was examined in kidney, liver, lung, and lowest in the brain. Isovitexin helps to stimulate apoptotic cell death and autophagy of various cancer cells through the upstream regulation of Bax, PARP, p-JNK, and MAPK and the downstream regulation of the caspases Bcl-2 and ERK1/2. Isovitexin has been proved to have various activities, such as anti-oxidant, anti-inflammatory, anti-Alzheimer's disease and others.

Pifithrin-alpha is a small molecule p53 functional inhibitor reported to behave like an antiapoptotic agent in neurodegenerative models. Pifithrin-alpha is a prodrug that under physiological conditions spontaneously undergoes ring closure to yield pifithrin-beta. Pifithrin-beta demonstrated antiproliferative and neuroprotective effects in vitro. Pifithrin-beta is able to activate the aryl hydrocarbon receptor (AhR) in a complete independent way of the p53 inhibition.

ABT-239 is a selective, nonimidazole H3 receptor antagonist/inverse agonist, which was investigated by Abbott laboratory as a potential drug for treatment of a variety of cognitive disorders including attention deficit/hyperactivity disorder, Alzheimer's disease, and schizophrenia.