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Synthesis and characterization of oxidovanadium complexes as enzyme inhibitors targeting dipeptidyl peptidase IV
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Xie, Ming-jin, Zhu, Ming-rong, Lu, Chun-Mei, Jin, Yi, Gao, Li-Hui, Li, Ling, Zhou, Jie, Li, Fan-fang, Zhao, Qi Hua, Liu, Hong-Ke, Sadler, P. J. and Sanchez-Cano, Carlos (2017) Synthesis and characterization of oxidovanadium complexes as enzyme inhibitors targeting dipeptidyl peptidase IV. Journal of Inorganic Biochemistry, 175 . pp. 29-35. doi:10.1016/j.jinorgbio.2017.06.014 ISSN 0162-0134.
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Official URL: https://doi.org/10.1016/j.jinorgbio.2017.06.014
Abstract
Two oxidovanadium(IV) complexes carrying Schiff base ligands obtained from the condensation of 4,5-dichlorobenzene-1,2-diamine and salicylaldehyde derivatives were synthesised and characterised, including their X-ray crystallographic structures. They were evaluated as dipeptidyl peptidase IV (DPP-IV) inhibitors for the treatment of type 2 diabetes. These compounds were moderate inhibitors of DPP-IV, with IC50 values of ca. 40 μM. In vivo tests showed that complexes 1 and 2 could lower significantly the level of glucose in the blood of alloxan-diabetic mice at doses of 22.5 mg V·kg− 1 and 29.6 mg V·kg− 1, respectively. Moreover, molecular modeling studies suggested that the oxidovanadium complexes 1 and 2 could fit well into the active-site cleft of the kinase domain of DPP-IV. To the best of our knowledge, this is the first report of vanadium complexes capable of inhibiting DPP-IV.
| Item Type: | Journal Article | ||||||||
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| Subjects: | Q Science > QD Chemistry Q Science > QP Physiology |
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| Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry | ||||||||
| SWORD Depositor: | Library Publications Router | ||||||||
| Library of Congress Subject Headings (LCSH): | Enzyme inhibitors, Schiff bases, Vanadium, Non-insulin-dependent diabetes -- Treatment | ||||||||
| Journal or Publication Title: | Journal of Inorganic Biochemistry | ||||||||
| Publisher: | Elsevier Science Inc | ||||||||
| ISSN: | 0162-0134 | ||||||||
| Official Date: | October 2017 | ||||||||
| Dates: |
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| Volume: | 175 | ||||||||
| Page Range: | pp. 29-35 | ||||||||
| DOI: | 10.1016/j.jinorgbio.2017.06.014 | ||||||||
| Status: | Peer Reviewed | ||||||||
| Publication Status: | Published | ||||||||
| Reuse Statement (publisher, data, author rights): | ** Embargo End Date: 14-07-2017 ** From Crossref via Jisc Publications Router. ** Licence for this article starting on 14-07-2017: http://creativecommons.org/licenses/by/4.0/ | ||||||||
| Access rights to Published version: | Restricted or Subscription Access | ||||||||
| Date of first compliant deposit: | 27 July 2017 | ||||||||
| Date of first compliant Open Access: | 27 July 2017 | ||||||||
| Funder: | Guo jia zi ran ke xue ji jin wei yuan hui (China) [National Natural Science Foundation of China] (NSFC), Yunnan Sheng (China), European Research Council (ERC), Engineering and Physical Sciences Research Council (EPSRC) | ||||||||
| Grant number: | 21161022, 21061016, 81260502, 21420102002 (NSFC), 2001CI002 (Yunnan Sheng (China)), 247450 (ERC), EP/F034210/1 (EPSRC) |
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