Cover Image

Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid

Inflammatory bowel disease (IBD) is the main risk factor for developing colorectal cancer which is common in patients of all ages. 5-Aminosalicylic acid (5-ASA), structurally relat ed to the salicylates, is highly active in the treatment of IBD with minor side effects. In this study, the synthesis of...

Full description

Saved in:
Bibliographic Details
Main Authors: Yousefi, Samira, Bayat, Saadi, Rahman, Mohd Basyaruddin Abdul, Ibrahim, Zalikha, Abdulmalek, Emilia
Format: Article
Language:English
Published: Wiley 2017
Online Access:http://psasir.upm.edu.my/id/eprint/63359/1/Synthesis%20and%20in%20vitro%20bioactivity%20evaluation%20of%20new%20galactose%20and%20fructose%20ester%20derivatives%20of%205-aminosalicylic%20acid.pdf
http://psasir.upm.edu.my/id/eprint/63359/
https://onlinelibrary.wiley.com/doi/epdf/10.1002/cbdv.201600362
Tags: Add Tag
No Tags, Be the first to tag this record!
id my.upm.eprints.63359
record_format eprints
spelling my.upm.eprints.633592018-10-16T00:31:31Z http://psasir.upm.edu.my/id/eprint/63359/ Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid Yousefi, Samira Bayat, Saadi Rahman, Mohd Basyaruddin Abdul Ibrahim, Zalikha Abdulmalek, Emilia Inflammatory bowel disease (IBD) is the main risk factor for developing colorectal cancer which is common in patients of all ages. 5-Aminosalicylic acid (5-ASA), structurally relat ed to the salicylates, is highly active in the treatment of IBD with minor side effects. In this study, the synthesis of galactose and fructose esters of 5-ASA was planned to evaluate the role of glycoconjugation on the bioactivity of the parent drug. The antibacterial activity of the new compounds were evaluated against two Gram-negative and two Gram-positive species of bacteria, with a notable effect observed against Staphylococcus aureus and Escherichia coli in comparisons with the 5-ASA. Cytotoxicity testing over HT-29 and 3T3 cell lines indicated that the toxicity of the new products against normal cells was significantly reduced compared with the original drug, whereas their activity against cancerous cells was slightly decreased. The anti-inflammatory activity test in RAW264.7 macrophage cells indicated that the inhibition of nitric oxide by both of the monosaccharide conjugated derivatives was slight ly improved in comparison with the non-conjugated drug. Wiley 2017 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/63359/1/Synthesis%20and%20in%20vitro%20bioactivity%20evaluation%20of%20new%20galactose%20and%20fructose%20ester%20derivatives%20of%205-aminosalicylic%20acid.pdf Yousefi, Samira and Bayat, Saadi and Rahman, Mohd Basyaruddin Abdul and Ibrahim, Zalikha and Abdulmalek, Emilia (2017) Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid. Chemistry & Biodiversity, 14 (4). art. no. e1600362. pp. 1-11. ISSN 1612-1872; ESSN: 1612-1880 https://onlinelibrary.wiley.com/doi/epdf/10.1002/cbdv.201600362 10.1002/cbdv.201600362
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description Inflammatory bowel disease (IBD) is the main risk factor for developing colorectal cancer which is common in patients of all ages. 5-Aminosalicylic acid (5-ASA), structurally relat ed to the salicylates, is highly active in the treatment of IBD with minor side effects. In this study, the synthesis of galactose and fructose esters of 5-ASA was planned to evaluate the role of glycoconjugation on the bioactivity of the parent drug. The antibacterial activity of the new compounds were evaluated against two Gram-negative and two Gram-positive species of bacteria, with a notable effect observed against Staphylococcus aureus and Escherichia coli in comparisons with the 5-ASA. Cytotoxicity testing over HT-29 and 3T3 cell lines indicated that the toxicity of the new products against normal cells was significantly reduced compared with the original drug, whereas their activity against cancerous cells was slightly decreased. The anti-inflammatory activity test in RAW264.7 macrophage cells indicated that the inhibition of nitric oxide by both of the monosaccharide conjugated derivatives was slight ly improved in comparison with the non-conjugated drug.
format Article
author Yousefi, Samira
Bayat, Saadi
Rahman, Mohd Basyaruddin Abdul
Ibrahim, Zalikha
Abdulmalek, Emilia
spellingShingle Yousefi, Samira
Bayat, Saadi
Rahman, Mohd Basyaruddin Abdul
Ibrahim, Zalikha
Abdulmalek, Emilia
Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
author_facet Yousefi, Samira
Bayat, Saadi
Rahman, Mohd Basyaruddin Abdul
Ibrahim, Zalikha
Abdulmalek, Emilia
author_sort Yousefi, Samira
title Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
title_short Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
title_full Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
title_fullStr Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
title_full_unstemmed Synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
title_sort synthesis and in vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid
publisher Wiley
publishDate 2017
url http://psasir.upm.edu.my/id/eprint/63359/1/Synthesis%20and%20in%20vitro%20bioactivity%20evaluation%20of%20new%20galactose%20and%20fructose%20ester%20derivatives%20of%205-aminosalicylic%20acid.pdf
http://psasir.upm.edu.my/id/eprint/63359/
https://onlinelibrary.wiley.com/doi/epdf/10.1002/cbdv.201600362
_version_ 1643837781298905088
score 13.211869

Similar Items