Synthesis and in vitro α-glucosidase and cholinesterases inhibitory actions of water-soluble metallophthalocyanines bearing ({6-[3-(diethylamino)phenoxy]hexyl}oxy groups

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KELEŞ T., BIYIKLIOĞLU Z., AKKAYA D., ÖZEL A., BARUT B.

Turkish Journal of Chemistry, vol.46, no.3, pp.786-795, 2022 (SCI-Expanded) identifier identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 46 Issue: 3
  • Publication Date: 2022
  • Doi Number: 10.55730/1300-0527.3368
  • Journal Name: Turkish Journal of Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.786-795
  • Keywords: Phthalocyanine, water-soluble, cholinesterases, alpha-Glucosidase, enzyme kinetic, CHOLINERGIC HYPOTHESIS, PHTHALOCYANINES, NEUROPROTECTION, AGGREGATION, DERIVATIVES, ANTIOXIDANT, DISEASE
  • Karadeniz Technical University Affiliated: Yes

Abstract

© TÜBİTAKIn this paper, we have prepared peripherally tetra-({6-[3-(diethylamino)phenoxy]hexyl}oxy substituted cobalt(II), copper(II), manganese(III) phthalocyanines (3, 4, 5) and their water-soluble derivatives (3a, 4a, 5a). Then, in vitro α-glucosidase and cholinesterases inhibitory actions of the water-soluble 3a, 4a, 5a were examined using spectrophotometric methods. 4a had the highest inhibitory effects among the tested compounds against α-glucosidase due to IC50 values. 4a and 5a had 40 fold higher inhibitory effects than the positive control. For cholinesterases, the compounds showed significant inhibitory actions that of galantamine which was used as a positive control. According to the SI value, 3a inhibited acetylcholinesterase enzyme selectively. In kinetic studies, 4a was a mixed inhibitor for α-glucosidase, 3a was a competitive inhibitor for AChE, and 4a was a mixed inhibitor for BuChE. The therapeutic potential of these compounds has been demonstrated by in vitro studies, but these data should be supported by further studies.