Biomolecules 2019, 9, 360
9 of 10
Figures S1–S57: full characterization of all the conjugates (1H, 13C, FTIR, and mass spectrometry).
Author Contributions: Methodology, S.C.-M., L.D.P.-H. and E.M.-K.; formal analysis, L.D.P.-H. and E.M.-K.;
investigation, S.C.-M., L.D.P.-H., E.M.-K., T.R.-Á. and M.M.-G.; writing—original draft preparation, E.M.-K. and
M.M.-G.; writing—review and editing, M.M.-G.; supervision, S.C.-M., L.D.P.-H., E.M.-K. and M.M.-G.
Funding: This research was funded by DGAPA, grant number IN101117 and EMK was supported by a postdoctoral
fellowship from CONACyT.
Acknowledgments: We would also like to thank Rios O. H., Velasco L., Huerta S. E., Patiño M. M. R. and Peña
Gonzalez M. A. for their technical assistance.
Conflicts of Interest: The authors declare no conflict of interest.
References
1.
2.
3.
4.
5.
6.
Baan, B.; Dihal, A.A.; Hoff, E.; Bos, C.L.; Voorneveld, P.W.; Koelink, P.J.; Wildenberg, M.E.; Muncan, V.;
Heijmans, J.; Verspaget, H.W.; et al. 5-Aminosalicylic acid inhibits cell cycle progression in a phospholipase
D dependent manner in colorectal cancer. Gut. 2012, 61, 1708–1715. [CrossRef] [PubMed]
Koelink, P.J.; Hawinkels, L.J.; Wiercinska, E.; Sier, C.F.; ten Dijke, P.; Lamers, C.B.; Hommes, D.W.;
Verspaget, H.W. 5-Aminosalicylic acid inhibits TGF-β1 signalling in colorectal cancer cells. Cancer Lett. 2010,
Velayos, F.S.; Terdiman, J.P.; Walsh, J.M. Effect of 5-aminosalicylate use on colorectal cancer and dysplasia risk:
a systematic review and metaanalysis of observational studies. Am. J. Gastroenterol. 2005, 100, 1345–1353.
Eaden, J. Review article: the data supporting a role for aminosalicylates in the chemoprevention of colorectal
cancer in patients with inflammatory bowel disease. Aliment. Pharmacol. Ther. 2003, 18, 15–21. [CrossRef]
Méndez-Lucio, O.; Tran, J.; Medina-Franco, J.L.; Meurice, N.; Muller, M. Toward Drug Repurposing in
Epigenetics: Olsalazine as a Hypomethylating Compound Active in a Cellular Context. ChemMedChem.
Herfarth, H. The Role of Chemoprevention of Colorectal Cancer with 5-Aminosalicylates in Ulcerative Colitis.
7.
8.
Campbell, D.E.S.; Berglindh, T. Pharmacology of Olsalazine. Scand. J. Gastroenterol. 1988, 23, 7–12. [CrossRef]
Courtney, M.; Nunes, D.; Bergin, C.; O’Driscoll, M.; Trimble, V.; Keeling, P.; Weir, D.; Nunes, D. Randomised
comparison of olsalazine and mesalazine in prevention of relapses in ulcerative colitis. Lancet 1992, 339,
9.
Dhaneshwar, S.S.; Gairola, N.; Kandpal, M.; Bhatt, L.; Vadnerkar, G.; Kadam, S. RETRACTED: Synthesis,
kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid with
D-phenylalanine for colon specific drug delivery in inflammatory bowel disease. Bioorganic Med. Chem. Lett.
10. Lesniak, W.G.; Oskolkov, N.; Song, X.; Lal, B.; Yang, X.; Pomper, M.; Laterra, J.; Nimmagadda, S.;
McMahon, M.T. Salicylic Acid Conjugated Dendrimers Are a Tunable, High Performance CEST MRI
NanoPlatform. Nano Lett. 2016, 16, 2248–2253. [CrossRef]
11. Namazi, H.; Adeli, M. Dendrimers of citric acid and poly (ethylene glycol) as the new drug-delivery agents.
12. Wiwattanapatapee, R.; Lomlim, L.; Saramunee, K. Dendrimers conjugates for colonic delivery of
5-aminosalicylic acid. J. Control Release 2003, 88, 1–9. [CrossRef]
13. Wu, X.; Yu, G.; Luo, C.; Maeda, A.; Zhang, N.; Sun, D.; Zhou, Z.; Puntel, A.; Palczewski, K.; Zheng-Rong, L.
Synthesis and evaluation of a nanoglobular dendrimer 5-aminosalicylic acid conjugate with a hydrolyzable
Schiff base spacer for treating retinal degeneration. ACS Nano. 2014, 28, 153–161. [CrossRef] [PubMed]
14. Cheng, Y.; Xu, Z.; Ma, M.; Xu, T. Dendrimers as Drug Carriers: Applications in Different Routes of Drug
15. Medina, S.H.; El-Sayed, M.E. Dendrimers as Carriers for Delivery of Chemotherapeutic Agents. Chem Rev.