Schisantherin A is a dibenzocyclooctadiene originally found in Schisandra that exhibits anti-tussive, sedative, anti-inflammatory, anti-osteoporotic, neuroprotective, cognition enhancing, and cardioprotective activities. In macrophages, schisantherin A decreases LPS-induced expression and activity of iNOS, COX-2, NO, IL-6, and TNF-α. Schisantherin A also decreases RANKL-induced NF-κB signaling by inhibiting IκBα degradation and suppressing JNK and ERK1/2 activation in vitro; it also inhibits osteoclast function and bone erosion in vivo. In animal models of Alzheimer’s disease, schisantherin A inhibits amyloid-β (Aβ)-induced learning and memory impairments in Y maze, shuttle box, and Morris water maze assays. Additionally, this compound lowers left ventricular systolic and end diastolic pressures, decreases infarct size and maldionaldehyde release, and increases superoxide dismutase activity, preventing myocardial apoptosis in animal models of cardiac ischemia/reperfusion. Schisantherin A conferred significant protection against MPTP-induced loss of TH-positive dopaminergic neurons in a Parkinson's disease (PD) mice model. Western blotting analysis demonstrated that Schisantherin A exhibited neuroprotection against MPP(+) through the regulation of two distinct pathways including increasing CREB-mediated Bcl-2 expression and activating PI3K/Akt survival signaling suggesting that StA might be a promising neuroprotective agent for the prevention of PD.

Hydroxyitraconazole is the antifungally active metabolite of itraconazole formed in the liver by Ω-1-oxidation of itraconazole's 1-methylpropyl substituent. Hydroxyitraconazole has being shown to inhibit ATP-binding cassette yransporters P-Glycoprotein, BCRP, and BSEP..

Ergocristine is an alkoloid originally isolated from Iberian ergot. In the rat, ergocristine acts as an alpha 2-adrenoceptors agonist, and an alpha 1-adrenoceptors antagonist. It is able to regulate glutamate uptake and dopamine release. Ergocristine is controlled as a list I chemical of because it is considered as a chemical precursor used in the illicit manufacture of lysergic acid diethylamide,

Pitavastatin lactone is the major metabolite of pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase, which is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. Uridine 5’ -diphosphate (UDP) glucuronosyl transferase (UGT) is critically involved in the lactonization of pitavastatin in man and animals. The metabolic and transporter profiles of pitavastatin in man are complex, involving acid/lactone interconversion. Both forms of pitavastatin are observed in-vivo following oral administration. Lactone form and pitavastatin differ in substrate activity towards uptake and efflux transporters.

Gambogic acid (GA), a naturally occurring xanthone-based moiety, reported from Garcinia hanburyi tree, is known to perform numerous intracellular and extracellular actions, including programmed cell death, autophagy, cell cycle arrest, antiangiogenesis, antimetastatic, and anti-inflammatory activities. In addition, GA-based synergistic approaches have been proven to enhance the healing strength of existing chemotherapeutic agents along with lesser side effects. Among cellular targets of gambogic acid topoisomerase, multidrug-resistant protein ATP-binding cassette transporter B1 (ABCB1) and Transferrin receptor.