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NOSH-sulindac (AVT-18A) is a novel nitric oxide- and hydrogen sulfide-releasing hybrid that is gastrointestinal safe and has potent anti-inflammatory, analgesic, antipyretic, anti-platelet, and anti-cancer properties.

Kashfi K, Chattopadhyay M, Kodela R - Redox Biol (2015)

Bottom Line: Gastrointestinal safety: 6h post-administration, number/size of hemorrhagic lesions in stomachs were counted.Both agents reduced PGE2 levels in stomach tissue; however, NOSH-sulindac did not cause any stomach ulcers, whereas sulindac caused significant bleeding.These results demonstrate that NOSH-sulindac is gastrointestinal safe, and maintains the anti-inflammatory, analgesic, antipyretic, and antiplatelet properties of its parent compound sulinsac, with anti-growth activity against a wide variety of human cancer cells.

View Article: PubMed Central - PubMed

Affiliation: Department of Physiology, Pharmacology and Neuroscience, Sophie Davis School of Biomedical Education, City University of New York Medical School, New York, United States; Avicenna Pharmaceuticals Inc., New York, NY, United States. Electronic address: kashfi@med.cuny.edu.

No MeSH data available.


Related in: MedlinePlus

Structural components of NOSH-sulindac. The parent compound sulindac is shown in the shaded box. The parts of the molecule that releases NO and H2S are shown in the dotted ellipses.
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f0005: Structural components of NOSH-sulindac. The parent compound sulindac is shown in the shaded box. The parts of the molecule that releases NO and H2S are shown in the dotted ellipses.

Mentions: NOSH-SUL (AVT-18A), (Z)-4-(3-thioxo-3H-1,2-dithiol-5-yl) phenyl 5-(2-(5-fluoro-2-methyl-1-(4-(methylsulfinyl) benzylidene)-1H-inden-3-yl) acetoxy)-2-((4-(nitrooxy) butanoyl)oxy) benzoate was synthesized as described previously [29] and was a gift from Avicenna Pharmaceuticals Inc, (New York, NY). The structural components of the NOSH-SUL are shown in Fig. 1. Lipopolysaccharide (LPS) from Escherichia coli, SUL, and carrageenan were purchased from Sigma (St. Louis, MO, USA). Kits used for determination of PGE2, lipid peroxidation, and superoxide dismutase, were from Cayman Chemical (Ann Arbor, MI).


NOSH-sulindac (AVT-18A) is a novel nitric oxide- and hydrogen sulfide-releasing hybrid that is gastrointestinal safe and has potent anti-inflammatory, analgesic, antipyretic, anti-platelet, and anti-cancer properties.

Kashfi K, Chattopadhyay M, Kodela R - Redox Biol (2015)

Structural components of NOSH-sulindac. The parent compound sulindac is shown in the shaded box. The parts of the molecule that releases NO and H2S are shown in the dotted ellipses.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4556776&req=5

f0005: Structural components of NOSH-sulindac. The parent compound sulindac is shown in the shaded box. The parts of the molecule that releases NO and H2S are shown in the dotted ellipses.
Mentions: NOSH-SUL (AVT-18A), (Z)-4-(3-thioxo-3H-1,2-dithiol-5-yl) phenyl 5-(2-(5-fluoro-2-methyl-1-(4-(methylsulfinyl) benzylidene)-1H-inden-3-yl) acetoxy)-2-((4-(nitrooxy) butanoyl)oxy) benzoate was synthesized as described previously [29] and was a gift from Avicenna Pharmaceuticals Inc, (New York, NY). The structural components of the NOSH-SUL are shown in Fig. 1. Lipopolysaccharide (LPS) from Escherichia coli, SUL, and carrageenan were purchased from Sigma (St. Louis, MO, USA). Kits used for determination of PGE2, lipid peroxidation, and superoxide dismutase, were from Cayman Chemical (Ann Arbor, MI).

Bottom Line: Gastrointestinal safety: 6h post-administration, number/size of hemorrhagic lesions in stomachs were counted.Both agents reduced PGE2 levels in stomach tissue; however, NOSH-sulindac did not cause any stomach ulcers, whereas sulindac caused significant bleeding.These results demonstrate that NOSH-sulindac is gastrointestinal safe, and maintains the anti-inflammatory, analgesic, antipyretic, and antiplatelet properties of its parent compound sulinsac, with anti-growth activity against a wide variety of human cancer cells.

View Article: PubMed Central - PubMed

Affiliation: Department of Physiology, Pharmacology and Neuroscience, Sophie Davis School of Biomedical Education, City University of New York Medical School, New York, United States; Avicenna Pharmaceuticals Inc., New York, NY, United States. Electronic address: kashfi@med.cuny.edu.

No MeSH data available.


Related in: MedlinePlus