U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1 - 10 of 23 results

Doxycycline is an antibacterial drug synthetically derived from oxytetracycline and used to treat a wide variety of bacterial infections, including those that cause acne. Doxycycline is used for bacterial pneumonia, acne, chlamydia infections, early Lyme disease, cholera, and syphilis. It is also useful for the treatment of malaria when used with quinine and for the prevention of malaria. Common side effects include diarrhea, nausea, vomiting, a red rash, and an increased risk of a sunburn. If used during pregnancy or in young children may result in permanent problems with the teeth including changes in their color. Its use during breastfeeding is probably safe. Like other tetracycline antibiotics, Doxycycline is protein synthesis inhibitors, inhibiting the binding of aminoacyl-tRNA to the mRNA-ribosome complex by binding to the 30S ribosomal subunit in the mRNA translation complex.
HU-308 ([(1R,2R,5R)-2-[2,6-dimethoxy-4-(2-methyloctan-2-yl)phenyl]-7,7-dimethyl-4-bicyclo[3.1.1]hept-3-enyl]methanol) is a potent, selective agonist for the CB2 receptor. The synthesis and characterization took place in the laboratory of Prof. Mechoulam at the Hebrew University of Jerusalem in the late 1990s. It has analgesic effects, promotes proliferation of neural stem cells,[3] and protects both liver and blood vessel tissues against oxidative stress via inhibition of TNF-α. In vivo, HU-308 has hypotensive, analgesic, and anti-inflammatory activities in mice that can be reversed by the CB2 receptor antagonist SR 144528 but not the CB1 receptor antagonist rimonabant. Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration, tissue, and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation, and apoptosis. HU-308 increases proliferation of HT29 colon cancer cells and growth of tumors in an HT29 mouse xenograft model. The physiological and toxicological properties of this compound have not been evaluated in humans.
Sanguinarine is an extract of the bloodroot plant Sanguinaria canadensis, a member of the poppy family. It is an inhibitor of protein phosphatases PP1, PP2C and PP2B in vitro. Also inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and other enzymes. Sanguinarine exerts a protective effect in cerebral ischemia, and this effect is associated with its anti-inflammatory and anti-apoptotic properties. It was clinically tested as an agent against gingivitis and tooth plaques.
β-Amyrin, a pentacyclic triterpenoid compound, that was found in many medicinal plants, including Protium heptaphyllum (Aubl.) Marchand, Catharanthus roseus (L.) G. Don, and Camellia tenuifolia (Hayata) Coh. Stuart. Several studies have reported that β-amyrin shows multiple pharmacological activities, such as the induction of angiogenesis in vascular endothelial cells and anti-inflammatory, antifibrotic, anti-apoptotic, anti-diabetic, anti-hyperlipidemic, and anti-nociceptive activities.
Sanguinarine is a toxic polycyclic quaternary ammonium salt. It is extracted from some plants, including bloodroot (Sanguinaria canadensis), Mexican prickly poppy Argemone mexicana, Chelidonium majus and Macleaya cordata. Sanguinarine is a toxin that kills animal cells through its action on the Na+-K+-ATPase transmembrane protein. If applied to the skin, sanguinarine may cause a massive scab of dead flesh, called an eschar. For this reason, sanguinarine is termed an escharotic. Preliminary pre-clinical in vitro and in vivo studies have demonstrated that sanguinarine causes apoptosis in human cancer cells, and recommend study of sanguinarine as a potential cancer treatment. Sanguinarine has been the subject of other medical fields as well. For instance, it has garnered interest as a chemical defense against microorganisms and viruses. Notably, experiments on human plaque accumulation in the presence of sanguinarine suggest the toxin may be effective against oral microbial isolates. However, no products containing sanguinarine are currently approved by the FDA for the treatment of cancer; the FDA warns that unapproved bloodroot preparations are ineffective and dangerous.
Status:
US Previously Marketed
Source:
Zinc Stearate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Zinc Stearate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Zinc stearate is a mild antiseptic and astringent, and it has been used as a local soothing application for inflammatory and irritating skin diseases. Zinc stearate is primarily used in pharmacuetical formulations as a lubricant in tablet and capsule manufacture at concentrations up to 1.5% w/w. It is a protective agent used in powders and ointments in the treatment of eczema, acne, and other skin diseases. GRAS - Zinc stearate complies with FDA Standard CFR 21 sections 177.2600, 182.8994 and 178.2010.

Class (Stereo):
CHEMICAL (ACHIRAL)


Crystalline solid. Decomposes at 120°C. Contact may cause slight irritation to skin, eyes, and mucous membranes. May be slightly toxic by ingestion. Used to make other chemicals. Magnesium Hexafluorosilicate is used for mothproofing of textile fabrics. It has being used in the treatment of experimental caries of rats.
Status:
Possibly Marketed Outside US
Source:
DECAPINOL by Ferrosan
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Delmopinol, a surface-active cationic agent. It was approved by FDA under the name Decapinol for the treatment of gingivitis and prevention of periodontitis. The drug interacts with the early acquired pellicle, the thin layer of saliva polymers and proteins covering teeth and gums, and forms a barrier over teeth and gums. This barrier prevents the microbial adhesion and colonisation on the tooth and gum surface. Delmopinol itself has no bactericidal activity.
Status:
Possibly Marketed Outside US
Source:
Japan:Epidihydrocholesterin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Epidihydrocholesterin (Cholestanol) is a sterol that differs from cholesterol by the absence of a double bond in the B ring and, in humans, is present in far lower concentrations than cholesterol. Epidihydrocholesterin is reported as an ingredient of Presteron. Presteron is an anti-inflammatory drug. It was reported that Presteron had no side effects like steroids on oral administration and intramuscular injection in human. Presteron partly inhibited ovine COX-1 by 10.4%, but it did not inhibit human recombinant COX-2 at all. Presteron inhibits the action of bradykinin, a potent inflammatory mediator, by suppressing Ca2+ dependent cellular PLA2 (cPLA2) and/or secretory PLA2 (sPLA2), and COX-1, resulting in alleviation of inflammation.
Oxantel is a narrow-spectrum anthelmintic effective against whipworms in dogs and cats. It is ineffective against other roundworms, flukes, tapeworms or external parasites. Oxantel acts on the nervous system of the worms as inhibitors of acetylcholinesterase. Oxantel, a cholinergic anthelmintic and fumarate reductase inhibitor, significantly inhibited biofilm formation by P. gingivalis and disrupted established biofilms at concentrations below its MIC against planktonic cells. Oxantel was more effective against P. gingivalis in biofilm than metronidazole, a commonly used antibiotic for periodontitis. When oxantel was administrated to human beings for the treatment of trichuriasis, no drug reaction or side effects were reported, and the results of hematologic, biochemical and urinary examinations didn’t reveal any significant drug-related changes.