(1,2,6,7-3H)-Testosterone is a radiolabeled form of the corresponding steroid hormone. It can be used to study testosterone metabolism and androgen receptor binding in tissues.

Benzoylmesaconine (BMA) is the main Aconitum alkaloid in Radix Aconiti Lateralis Preparata. Notably, the high levels of toxicity of Radix Aconiti are derived from diester aconitum alkaloids, including aconitine, mesaconitine and hypaconitine, which can be hydrolyzed to benzoylaconine, benzoylmesaconine and benzoylhypaconine, respectively. Benzoylmesaconine exhibits biological effects, including analgesic, antiviral and antifungal activities.

Allocryptopine is isoquinoline alkaloid found primarily in the plant families Fumariaceae, Papaveraceae, Berberidaceae, Ranunculaceae, Rutaceae, and Sapindaceae. It have been reported to possess strong antibacterial, anti-inflammatoty, antiparasitic, antineoplastic and anti-addictive activities. Allocryptopine inhibits human acetylcholinesterase and butyrylcholinesterase. It blocks hERG current in HEK293 cells. Allocryptopine strongly enhanced the I(peak) of the T353I channel by enhancing the plasma membrane (PM) expression of Nav1.5 and rescued defective trafficking after co-incubation with HEK293 cells that carry mutation channel 24 h. A possible preparation for the treatment of HIV-1 and HIV-2 viruses containing pharmaceutically effective amounts of allocryptopine has been patented.

Methylcytisine (Caulophylline) is a nicotinic alkaloid found in Caulophyllum thalictroides, also known as blue cohosh. Methylcytisine is a second potentially hazardous compound identified from blue cohosh. In cultured rat embryos, N-methylcytisine from blue cohosh caused major malformations. At a concentration of 20 ppm the effects included open anterior neural tube, poor or absent eye development, and twisted tail. Higher concentrations of Methylcytisine inhibited overall growth and morphogenesis, in addition to producing similar malformations. In a separate study, Methylcytisine was also found to stimulate the ganglion cells of the cardiac vagus in frogs, paralyze the ganglia of the cardiac vagus in dogs, and produce hyperglycemia in rabbits. Some of the actions of Methylcytisine are similar to nicotine. N-Methylcytisine in blue cohosh-containing dietary supplements has been measured at concentrations ranging from 5-850 ppm. No research has been conducted on the pharmacokinetics or pharmacodynamics of blue cohosh or its constituents; therefore, the clinical significance of the experiments discussed above remains unknown. However, women anticipating a pregnancy may want to avoid using blue cohosh-containing dietary supplements until the potential in vivo teratogenic effects of this botanical are understood.

Roquefortine C, a cyclopeptide derived from the diketopiperazine cyclo(Trp-dehydroHis), is a secondary metabolite produced by several Penicillium species, especially by Penicillium roqueforti, which is used as starter culture for blue cheese production. Although roquefortine C is frequently detected in the products, it obviously has an insignificant toxicity to humans after ingestion. However, intoxications in dogs and cattle have been reported. Its bacteriostatic activities against Gram-positive bacteria lead to Roquefortine C potential use in antibiotics, but its development as a drug has been stopped due to its neurotoxic effects in mice. Roquefortine C activates P-gp and inhibits P450-3A and other haemoproteins. Roquefortine C can serve as a sensitive biomarker for penitrem A intoxication.

Enniatin B is a cyclic hexadepsipeptide it contains three N-methyl-Lvaline and three a-hydroxy-D-isovaleric molecules. It is generated by multiple Fusarium strains. It has ionophoric, antibiotic and insecticidal activity. A mixture of Enniatins A, A1, B and B1 (called fusafungine) was originally patented as local antibiotic for the topically treatment of nose and throat infections. Enniatin B is a mycotoxin contaminant found in vegetables, cereals and coffee. Enniatin B did not show genotoxic activity but demonstrated cytotoxicity at low micromolar concentrations. The observed activities included the specific inhibition of acyl-CoA cholesterol acyltransferase, depolarization of mitochondria, inhibition of osteoclastic bone resorption, and induction of apoptosis in cancer cells as well as the interaction with ATP-binding cassette transporters such as P-glycoprotein. Enniatin B demonstrated synergistic activity against cervical cancer in vitro and in vivo.

Carnosic acid [CA, (4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7- propan-2-yl-2,3,4,9,10,10a-hexahydrophenanthrene-4a-carboxylic acid] is a phenolic diterpene found in the leaves of the rosemary plant (Rosmarinus officinalis) and is used routinely as a food and cosmetic additive due to its antioxidant and antimicrobial properties. Carnosic acid as a food additive has a good safety profile and does not pose a health concern. Carnosic acid has demonstrated anti-inflammatory, anticancer, photoprotective, and antiadipogenic activities in vitro. Carnosic acid was shown to induce significant weight loss and reduced visceral adiposity in ob/ob mice fed a diet supplemented with carnosic acid. Carnosic acid is used as a preservative or antioxidant in food and nonfood products (e.g. toothpaste, mouthwash and chewing gum) -in which it has an antimicrobial effect on the microbes responsible for bad breath- or in skin care products.

Retrorsine (RTS) is a naturally occurring pyrrolizidine alkaloid (PA), isolated from Senecio retrorsus of South African origin. Retrorsine is a hepatotoxic Pyrrolizidine alkaloid which specifically inhibits the proliferation of hepatocytes and subsequently induces liver injury. The toxic effect of PAs has received plentiful clinical attention, yet the understanding of the mechanism of Retrorsine-induced hepatotoxicity is still limited. It has been reported that the CYPs mediated bioactivation is necessary for the toxicity of PAs and that CYP3A4 is the major isoform involved in the metabolism of Retrorsine. Together withCYP3A4, Organic cation transporter 1 mediates the liver-specific uptake of Retrorsine and plays an important role in RTS-induced hepatotoxicity. Retrorsine impairs liver regeneration after partial hepatectomy, not only by an S or G2/M phase block but also by a block located before the G1/S transition of the cell cycle. Treatment of rats with retrorsine, a pyrrolizidine alkaloid, results in a series of chronic and progressive hepatic lesions, including a long-lasting block in the cell cycle.

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.