BIOMAT Database Logo BIOMAT Database Logo

Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice. 2013

Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Center for Tuberculosis Research, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.

Mycobactin biosynthesis in Mycobacterium tuberculosis facilitates iron acquisition, which is required for growth and virulence. The mycobactin biosynthesis inhibitor salicyl-AMS [5'-O-(N-salicylsulfamoyl)adenosine] inhibits M. tuberculosis growth in vitro under iron-limited conditions. Here, we conducted a single-dose pharmacokinetic study and a monotherapy study of salicyl-AMS with mice. Intraperitoneal injection yielded much better pharmacokinetic parameter values than oral administration did. Monotherapy of salicyl-AMS at 5.6 or 16.7 mg/kg significantly inhibited M. tuberculosis growth in the mouse lung, providing the first in vivo proof of concept for this novel antibacterial strategy.

UI MeSH Term Description Entries
D008168 Lung Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood. Lungs
D008807 Mice, Inbred BALB C An inbred strain of mouse that is widely used in IMMUNOLOGY studies and cancer research. BALB C Mice, Inbred,BALB C Mouse, Inbred,Inbred BALB C Mice,Inbred BALB C Mouse,Mice, BALB C,Mouse, BALB C,Mouse, Inbred BALB C,BALB C Mice,BALB C Mouse
D009169 Mycobacterium tuberculosis A species of gram-positive, aerobic bacteria that produces TUBERCULOSIS in humans, other primates, CATTLE; DOGS; and some other animals which have contact with humans. Growth tends to be in serpentine, cordlike masses in which the bacilli show a parallel orientation. Mycobacterium tuberculosis H37Rv
D010080 Oxazoles Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions. Oxazole,1,3-Oxazolium-5-Oxides,Munchnones,1,3 Oxazolium 5 Oxides
D011897 Random Allocation A process involving chance used in therapeutic trials or other research endeavor for allocating experimental subjects, human or animal, between treatment and control groups, or among treatment groups. It may also apply to experiments on inanimate objects. Randomization,Allocation, Random
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

Related Publications

Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Kinetic Analyses of the Siderophore Biosynthesis Inhibitor Salicyl-AMS and Analogues as MbtA Inhibitors and Antimycobacterial Agents.
February 2019, Biochemistry,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Polymer micelle formulation for the proteasome inhibitor drug carfilzomib: Anticancer efficacy and pharmacokinetic studies in mice.
January 2017, PloS one,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Gram-scale preparation of the antibiotic lead compound salicyl-AMS, a potent inhibitor of bacterial salicylate adenylation enzymes.
January 2020, Methods in enzymology,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Phase I trial and pharmacokinetic studies of alpha-difluoromethylornithine--an inhibitor of polyamine biosynthesis.
February 1984, Journal of clinical oncology : official journal of the American Society of Clinical Oncology,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Stealth Liposomes Encapsulating a Potent ACAT1/SOAT1 Inhibitor F12511: Pharmacokinetic, Biodistribution, and Toxicity Studies in Wild-Type Mice and Efficacy Studies in Triple Transgenic Alzheimer's Disease Mice.
July 2023, International journal of molecular sciences,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
AMS method validation for quantitation in pharmacokinetic studies with concomitant extravascular and intravenous administration.
February 2011, Bioanalysis,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
In vitro and in vivo studies of the properties and effects of antimacrophage sers (AMS).
September 1971, Clinical and experimental immunology,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
The biosynthesis of fibrinogen: in vivo studies.
June 1983, Annals of the New York Academy of Sciences,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Synthesis of deuterium-labelled 5'-O-[N-(Salicyl)sulfamoyl]adenosine (Sal-AMS-d(4)) as an internal standard for quantitation of Sal-AMS.
February 2008, Journal of labelled compounds & radiopharmaceuticals,
Shichun Lun, and Haidan Guo, and John Adamson, and Justin S Cisar, and Tony D Davis, and Sivagami Sundaram Chavadi, and J David Warren, and Luis E N Quadri, and Derek S Tan, and William R Bishai
Methionine biosynthesis in lemna: inhibitor studies.
May 1982, Plant physiology,
Copied contents to your clipboard!