Sulindac sulfide

Sulindac sulfide is an active metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor sulindac (Item No, 10004386).^1,2 It inhibits both COX-1 and COX-2 (IC₅₀s = 1.9 and 1.21 µM, respectively), whereas the parent compound, sulindac, is much less effective (IC₅₀ = 58 µM for COX-2 and > 100 µM for COX-1).³ Sulindac sulfide also inhibits aldose reductase (IC₅₀ = 279 nM), blocking NADPH-dependent reduction of glucose to sorbitol, and reducing type 2 diabetic complications.⁴ It increases the expression and activity of NAD(P)H quinone oxidoreductase 1.⁵ Sulindac sulfide inhibits colorectal cancer growth both in vitro and in vivo.⁶

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1. Kitamura, S., and Tatsumi, K. In vitro metabolism of sulindac and sulindac sulfide: Enzymatic formation of sulfoxide and sulfone. Jpn. J. Pharmacol. 32(5), 833-838 (1982).

2. Brunell, D., Sagher, D., Kesaraju, S., et al. Studies on the metabolism and biological activity of the epimers of sulindac. Drug Metab. Dispos. 39(6), 1014-1021 (2011).

3. Warner, T.D., Giuliano, F., Vojnovic, I., et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: A full in vitro analysis. Proc. Natl. Acad. Sci. USA 96(13), 7563-7568 (1999).

4. Zheng, X., Zhang, L., Zhai, J., et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Lett. 586(1), 55-59 (2012).

5. Kung, H.N., Weng, T.Y., Liu, Y.L., et al. Sulindac compounds facilitate the cytotoxicity of β-lapachone by up-regulation of NAD(P)H quinone oxidoreductase in human lung cancer cells. PLoS One 9(2), 1-15 (2014).

6. Williams, C.S., Goldman, A.P., Sheng, H., et al. Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth. Neoplasia 1(2), 170-176 (1999).