(Z)-Guggulsterone is a natural product that lowers cholesterol due to its function as an antagonist ligand for the bile acid receptor. (Z)-Guggulsterone is a nuclear hormone receptor that regulates the transcription of several genes involved in cholesterol metabolism and plays a role in cholesterol level regulation. (Z)-Guggulsterone is also a selective farnesoid X receptor (FXR) modulator. Both Guggulsterone isomers were demonstrated to suppress lipopolysaccharide-induced inflammation by inhibiting IκB-α degradation and NF-κB activation. GS has medicinal properties such as anti-inflammatory, hepatoprotective, muscle relaxing, hypocholesterolemic and anti-obesity, antimycobacterial, antischistomal, larvicidal, and molluscicida.

Auraptene (7-Geranyloxycoumarin) is the best known and most abundant prenyloxycoumarin present in nature. It is synthesized by various plant species, mainly those of the Rutaceae and Umbelliferae (Apiaceae) families, comprising many edible fruits and vegetables such as lemons, grapefruit, and orange. Auraptene has shown a remarkable effect in the prevention of degenerative diseases, in particular, it has been reported to be one the most promising known natural chemopreventive agents against several types of cancer. The effect in humans is not yet known.

LY-255283 is a tetrazole derivative that acts as the competitive antagonist of the Leukotriene B4 (LTB4) receptor 2 (BLT2). LY255283 shows potent inhibition of LTB4 binding to human neutrophils and of LTB4-induced aggregation of guinea-pig neutrophils. In guinea-pigs, this compound also suppressed both specific binding of LTB4 to lung membrane and LTB4-induced contraction of lung parenchyma. Intravenous and oral administration of LY255283 dose-dependently reduced airway obstruction in guinea-pigs induced by LTB4, but not by histamine and U- 46619. Antigen-induced lung eosinophilia in rats was inhibited by orally administered LY255283. LY255283 exhibited the ability to suppress the shock induced by endotoxin and splanchnic artery occlusion in rats. LY255283 (bolus i.v. and subsequent infusion) attenuated endotoxin-induced adult respira¬tory distress syndrome in the pig model. LY255283 is used in leukotriene receptor research along with other selective leukotriene receptor agonists and antagonist to identify and differentiate the physiological and cell signaling effects of the leukotriene B4 receptor on processes such as paclitaxel resistance in MCF-7/DOX breast cancer cells, monocyte-derived dendritic cell chemotaxis, and 5-lipoxygenase activity and interleukin-8 production in human neutrophils.

Farnesol, (2E,6E)- is an isoprenoid found in many aromatic plants and is also produced in humans, where it acts on numerous nuclear receptors and has received considerable attention due to its apparent anticancer properties. Farnesol is present in many essential oils such as citronella, neroli, cyclamen, lemon grass, tuberose, rose, musk, balsam, and tolu. It is used in perfumery to emphasize the odors of sweet floral perfumes. Its method of action for enhancing perfume scent is as a co-solvent that regulates the volatility of the odorants. It is especially used in lilac perfumes. Farnesol is a natural pesticide for mites and is a pheromone for several other insects. In a 1994 report released by five top cigarette companies, farnesol was listed as one of 599 additives to cigarettes. Farnesol has been suggested to function as a chemopreventative and anti-tumor agent. Farnesol is subject to restrictions on its use in perfumery as some people may become sensitized to it, however, the evidence that farnesol can cause an allergic reaction in humans is disputed.

Oleanolic acid or oleanic acid is a naturally occurring pentacyclic triterpenoid. It is widely distributed in food and plants where it exists as a free acid or as an aglycone of triterpenoid saponins. Oleanolic acid protects the liver from acute chemically induced liver injury, fibrosis and cirrhosis caused by chronic liver diseases. Its possess cytotoxic activity against tumor cell lines

Flutrimazole (trade names Flusporan, Funcenal, Micetal, Topiderm) is an imidazole derivative, a wide-spectrum antifungal drug used for the topical treatment of superficial mycoses of the skin. Flutrimazole interferes with the synthesis of ergosterol by inhibiting the activity of the enzyme lanosterol 14 α-demethylase. Flutrimazole’s antifungal activity has been demonstrated in in vivo and in vitro studies to be comparable to that of clotrimazole and higher than bifonazole. During clinical trials the incidence of adverse reactions in relation to the use of Flutrimazole skin cream was 8%, being the most frequent those described as slight burning, irritation, itching, and erythema in the area of application.

Cholic acid is a primary bile acid synthesized from cholesterol in the liver. Endogenous bile acids including cholic acid enhance bile flow and provide the physiologic feedback inhibition of bile acid synthesis. The mechanism of action of cholic acid has not been fully established; however, it is known that cholic acid and its conjugates are endogenous ligands of the nuclear receptor, farnesoid X receptor (FXR). FXR regulates enzymes and transporters that are involved in bile acid synthesis and in the enterohepatic circulation to maintain bile acid homeostasis under normal physiologic conditions. U.S. Food and Drug Administration approved Cholbam (cholic acid) capsules, the first FDA approved treatment for pediatric and adult patients with bile acid synthesis disorders due to single enzyme defects, and for patients with peroxisomal disorders (including Zellweger spectrum disorders).

Ursodiol tablets, USP are bile acids indicated for the treatment of patients with primary biliary cirrhosis. Ursodiol (Ursodeoxycholic acid), a naturally occurring hydrophilic bile acid, derived from cholesterol, is present as a minor fraction of the total human bile acid pool. Ursodeoxycholic acid reduces elevated liver enzyme levels by facilitating bile flow through the liver and protecting liver cells. The main mechanism if anticholelithic. Although the exact process of ursodiol's anticholelithic action is not completely understood, it is thought that the drug is concentrated in bile and decreases biliary cholesterol by suppressing hepatic synthesis and secretion of cholesterol and by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution. In addition to the replacement and displacement of toxic bile acids, other mechanisms of action include cytoprotection of the injured bile duct epithelial cells (cholangiocytes) against toxic effects of bile acids, inhibition of apotosis of hepatocytes, immunomodulatory effects, and stimulation of bile secretion by hepatocytes and cholangiocytes. Neither accidental nor intentional overdosing with ursodeoxycholic acid has been reported. Doses of ursodeoxycholic acid in the range of 16-20 mg/kg/day have been tolerated for 6-37 months without symptoms by 7 patients. The LD50 for ursodeoxycholic acid in rats is over 5000 mg/kg given over 7-10 days and over 7500 mg/kg for mice. The most likely manifestation of severe overdose with ursodeoxycholic acid would probably be diarrhea, which should be treated symptomatically.