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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

Effect of sulindac and NOSH-sulindac on plasma TNF-α. At the end of the gastrointestinal safety evaluations as described in Section 2.3, blood was drawn and processed as described in Section 2.7 for determination of plasma TNF-α. SUL caused a significant rise in plasma TNF-α, however, this rise was significantly less in the NOSH-SUL-treated rats. Results are mean±SEM for 5 rats in each group, *P<0.001 vs vehicle, §P<0.01 vs SUL.
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f0025: Effect of sulindac and NOSH-sulindac on plasma TNF-α. At the end of the gastrointestinal safety evaluations as described in Section 2.3, blood was drawn and processed as described in Section 2.7 for determination of plasma TNF-α. SUL caused a significant rise in plasma TNF-α, however, this rise was significantly less in the NOSH-SUL-treated rats. Results are mean±SEM for 5 rats in each group, *P<0.001 vs vehicle, §P<0.01 vs SUL.

Mentions: We determined the inhibitory effect of SUL and NOSH-SUL on the proinflammatory cytokine tumor necrosis factor-α in plasma obtained from control and drug-treated animals at the end of the gastrointestinal safety experiments, 6 h post-administration (Section 2.3). Administration of SUL (200 mg/kg, 0.56 mmol/kg) increased TNFα concentration by about 25-fold (9.5±0.3 control and 230±5 pg/mL SUL). However, this rise was considerably lower in the NOSH-SUL-treated (476 mk/g, 0.56 mmol/kg) animals, 50±3 pg/mL (Fig. 5).


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)

Effect of sulindac and NOSH-sulindac on plasma TNF-α. At the end of the gastrointestinal safety evaluations as described in Section 2.3, blood was drawn and processed as described in Section 2.7 for determination of plasma TNF-α. SUL caused a significant rise in plasma TNF-α, however, this rise was significantly less in the NOSH-SUL-treated rats. Results are mean±SEM for 5 rats in each group, *P<0.001 vs vehicle, §P<0.01 vs SUL.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0025: Effect of sulindac and NOSH-sulindac on plasma TNF-α. At the end of the gastrointestinal safety evaluations as described in Section 2.3, blood was drawn and processed as described in Section 2.7 for determination of plasma TNF-α. SUL caused a significant rise in plasma TNF-α, however, this rise was significantly less in the NOSH-SUL-treated rats. Results are mean±SEM for 5 rats in each group, *P<0.001 vs vehicle, §P<0.01 vs SUL.
Mentions: We determined the inhibitory effect of SUL and NOSH-SUL on the proinflammatory cytokine tumor necrosis factor-α in plasma obtained from control and drug-treated animals at the end of the gastrointestinal safety experiments, 6 h post-administration (Section 2.3). Administration of SUL (200 mg/kg, 0.56 mmol/kg) increased TNFα concentration by about 25-fold (9.5±0.3 control and 230±5 pg/mL SUL). However, this rise was considerably lower in the NOSH-SUL-treated (476 mk/g, 0.56 mmol/kg) animals, 50±3 pg/mL (Fig. 5).

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