Veratramine, a steroidal alkaloid originating from Veratrum nigrum L. CYP2D6 and SULT2A1 mediating hydroxylation and sulfation were identified as the major biotransformation for veratramine. Veratramine significantly inhibits the hedgehog pathway in NIH/3T3 cells. Veratramine is both a release and uptake inhibitor of serotonin. Veratramine exhibits cytotoxic activity against human tumor cell lines A549, PANC-1, SW1990 and NCI-H249. Veratramine has demonstrated distinct anti-hypertension effects in spontaneously hypertensive rats.

S-fluoxetine is an enantiomer of fluoxetine, a potent and selective inhibitor of the neuronal serotonin-uptake carrier and a clinically effective antidepressant. R-fluoxetine and S-fluoxetine enantiomers are nearly equipotent at blocking serotonin reuptake. In all biochemical and pharmacological studies, the eudismic ratio for the fluoxetine enantiomers is also near unity. A study examining the relative contributions of CYP enzymes to the metabolism of S-fluoxetine, and R-fluoxetine found dramatic differences. These data led to discovery programs between Lilly and Sepracor for the individual enantiomers. S-fluoxetine was studied in a phase 2 clinical trial for the prophylaxis of migraine, however, development was discontinued.

Naftopidil,(R)- is an enantiomer of Naftopidil (NAF), a specific subtype selective α1-adrenoceptor blocker. Racemic Naftopidil is frequently used for the treatment of lower urinary tract symptoms/benign prostatic hyperplasia. No significant differences in pharmacokinetic parameters were observed between R(+)- and S(−)-NAF after intravenous administration. However, mean plasma concentrations of R(+)-NAF were lower than those of S(-)-NAF after intragastric administration. R(+)-NAF bioavailability in rats was consistently about two-fold lower than that of S(-)-NAF. The fractions of R(+)- NAF reaching the prostate and metabolized in the liver were higher than those of S(−)-NAF. The major pathways of R(+)- NAF metabolism in vitro were demethylation and hydroxylation. CYP2C9 played the most important role in the demethylation and hydroxylation of both NAF enantiomers. CYP2C19 was another CYP isoform that played a major role in R(+)-NAF metabolism.

Dihydromethysticin is one of the six major kavalactones found in the roots of kava plant. Dihydromethysticin was found to be very effective in producing analgesia in the tail immersion test. Dihydromethysticin kavalactone induces apoptosis in osteosarcoma cells through modulation of PI3K/Akt pathway, disruption of mitochondrial membrane potential and inducing cell cycle arrest. Dihydromethysticin was identified as a promising lung cancer chemopreventive agent. Low concentrations of the kavalactone (+)-dihydromethysticin enhanced the binding of ligands to the GABAA receptors on freeze-dried rat cortex preparations.

Sesamolin from Sesamun indicum seeds plays important role in plant defense, such as antifeedant as well as potent antioxidants and insecticides. Sesaminol has potent inhibition of cytochrome P450 (CYPs). The neuroprotective effect of sesamolin was also observed in vivo using gerbils subjected to a focal cerebral ischemia induced by occlusion of the right common carotid artery and the right middle cerebral artery. Lipid peroxidation activity, measured as 2-thiobarbituric acid reactive substances, was significantly lower in the kidneys and liver of the sesamolin-fed rats than in the controls.

Palmatine is a protoberberine alkaloid. Palmatine is major component of herbal preparations mainly used in traditional medicine Chinese, Korean and Indian. Palmatine can be found in various medicinal plants such as Coptis chinensis, Rhizoma coptidis, Corydalis yanhusuo, Radix tinosporae, among others. It exerts diverse pharmacological and biological properties. Palmatine has been proposed as a promising DNA phototherapy drug, notably due to its ability to produce in situ singlet oxygen only when interacting with DNA.