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

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Showing 1 - 10 of 24 results

Imipenem is a beta-lactam antibiotic belongings to the subgroup of carbapenems. Imipenem has a broad spectrum of activity against aerobic and anaerobic Gram positive as well as Gram negative bacteria. It is particularly important for its activity against Pseudomonas aeruginosa and the Enterococcus species. Imipenem is rapidly degraded by the renal enzyme dehydropeptidase when administered alone, and is always co-administered with cilastatin to prevent this inactivation. The bactericidal activity of imipenem results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B. Imipenem is marketed under the brand name Primaxin. PRIMAXIN I.M. (Imipenem and Cilastatin for Injectable Suspension) is a formulation of imipenem (a thienamycin antibiotic) and cilastatin sodium (the inhibitor of the renal dipeptidase, dehydropeptidase I). PRIMAXIN I.M. is a potent broad spectrum antibacterial agent for intramuscular administration.
Lincomycin (LINCOCIN®) is an antibiotic produced by Streptomyces lincolnensis (Streptomycetaceae family). It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. Lincomycin (LINCOCIN®) inhibits protein synthesis in susceptible bacteria by binding to the 50S subunits of bacterial ribosomes and preventing peptide bond formation upon transcription. It is usually considered bacteriostatic, but may be bactericidal in high concentrations or when used against highly susceptible microorganisms.
Penicillin V is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Penicillin V has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Penicillin V results from the inhibition of cell wall synthesis and is mediated through Penicillin V binding to penicillin binding proteins (PBPs). Penicillin V is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Penicillin V inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Penicillin V interferes with an autolysin inhibitor. Used for the treatment of mild to moderately severe infections (e.g. dental infection, infections in the heart, middle ear infections, rheumatic fever, scarlet fever, skin infections, upper and lower respiratory tract infections) due to microorganisms.
Aporeine (Roemerine) is an aporphine alkaloid that can be isolated from many plants such as Annona senegalensis, Turkish Papaver and Rollinialeptopetala. Aporeine has been reported to exhibit antibacterial activity. It has also been demonstrated to have certain antifungal activity. Aporeine showed selective inhibitory effect on Cox-2.
Isopimaric acid is a widely available tricyclic diterpenoid well represented in the resin of conifers of the genera Pinus, Larix, and Picea. It exhibits interesting biological and pharmaceutical properties such as antimicrobial, antiviral, antiallergenic, and anti‐inflammatory activities. It acts as a large conductance Ca2+activated K+ channel (BK channel) opener. BK channel openers have emerged as potentially useful agents in the therapy of various diseases associated with both the central nervous system and smooth muscle system.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zaluzanin D is a sesquiterpene lactone that has been isolated from the aerial parts of Vernonia arborea as a major constituent (0.04%). Zaluzanin D isolated from laurel (Laurus nobilis L.) has being shown to induce cell death and morphological change indicative of apoptotic chromatin condensation in leukemia HL-60 cells. Zaluzanin D demonstrated antibacterial activity against Bacillus subtilis and Staphylococcus aureus.
Vulpinic Acid is a lichen metabolite with anti-inflammatory properties. Vulpinic Acid acts as photoprotective agent and antifungal agent. Vulpinic acid mainly affects cell cycle, glycogen metabolism, transcription and translation to fungi. Vulpinic acid showed very strong inhibition effect on TrxR (mitochondrial thioredoxin reductase), so it may be used as a potential drug for cancer therapy. Vulpinic acid possesses diverse biological activities, and lichens containing Vulpinic acid have a strong history of medicinal use. For example, Eskimos and people of Northern Europe have used lichens containing Vulpinic acid to poison the wolf and fox.Lichens containing Vulpinic acid are used as fodder for reindeer and emergency food by Arctic and Subarctic peoples. In central Europe, members of the genus Cetraria, which is known to produce Vulpinic acid, have been used as laxatives and have been taken for coughing, including that associated with tuberculosis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimethylhydroquinone (2,3,5-Trimethylhydroquinone, TMHQ) is a compound with a wide range of important practical applications. As shown by data from the patent literature, this compound can be used in the synthesis of dyes, pigments, antioxidants, polymerization inhibitors, and other important chemicals. However, the main use of this compound is as an intermediate in the industrial synthesis of vitamin E. Because of the importance of vitamin E in medicine, food manufacturing, and cattle breeding, there is continuing interest in the methods for the preparation of 2,3,5-trimethylhydroquinone. Trimethylhydroquinone presented obvious in vitro anti-MRSA activity.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Hypocrellin B (HB), a natural perylenequinone pigment, has been successfully employed in the photodynamic therapy (PDT) in a variety of human cancer cells due to its high singlet oxygen yield. Hypocrellin B exhibits antibacterial, anti-metastatic, and anticancer chemotherapeutic activities. Hypocrellin B inhibits proliferation of Staphylococcus by increasing ROS levels and damaging cell walls. In ovarian cancer cells, this compound induces apoptosis and inhibits cell migration and adhesion under photodynamic stimulation; it also induces tumor regression in animal models of lymphoma. In vitro, hypocrellin B induces DNA strand breakage.
Sclareolide is a sesquiterpene lactone natural product derived from various plant sources including Salvia sclarea, Salvia yosgadensis, and cigar tobacco. Sclareolide demonstrated good antibacterial activity against common human pathogens, including Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Enterococcus faecalis. Sclareolide is not generally known for its bioactive properties. Instead, it is mostly used as a fixative or base in the perfume industry. It is also used in cosmetics, because it is thought to contribute to tanning of skin and/or darkening of hair.