Bornyl derivatives of p-(Benzyloxy)phenylpropionic acid: In vivo evaluation of antidiabetic activity

Bornyl derivatives of p-(Benzyloxy)phenylpropionic acid: In vivo evaluation of antidiabetic activity Full article

Journal

Pharmaceuticals
ISSN: 1424-8247

Output data

Year: 2020, Volume: 13, Number: 11, Article number : 404, Pages count : 22 DOI: 10.3390/ph13110404

Tags

Bornyl derivative; Glucose tolerance; Hypoglycemic activity; Hypoglycemic multitarget activity; In silico prediction; Natural product; Type 2 diabetes mellitus

Authors

Kuranov Sergey ¹ , Luzina Olga ¹ , Khvostov Mikhail ¹ , Baev Dmitry ¹ , Kuznetsova Darya ¹ , Zhukova Nataliya ¹ , Vassiliev Pavel ² , Kochetkov Andrey ² , Tolstikova Tatyana ¹ , Salakhutdinov Nariman ¹

Affiliations

1	N. N. Vorozhtsov Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences, Novosibirsk, 630090, Russian Federation
2	Reasearch Center of Innovative Medicines, Laboratory for Information Technology in Pharmacology and Computer Modeling of Drugs, Volgograd State Medical University, Ministry of Health of Russian Federation, Volgograd, 400131, Russian Federation

A series of bornyl derivatives of p-(benzyloxy)phenylpropionic acid were prepared, and their hypoglycemic activities were examined by an oral glucose tolerance test in mice. The results of this test revealed two compounds, 1 and 3, that can reduce the blood level of glucose similarly to reference compound vildagliptin. Both compounds were tested in an experiment on mice with metabolic disorders: the C57BL/6Ay strain. Along with hypoglycemic properties, the two compounds showed different abilities to correct lipid metabolism disorders. In silico prediction revealed that the studied substances are most likely bifunctional multitarget hypoglycemic compounds whose mechanism of action is based on a pronounced reduction in insulin resistance and a strong incretin-mimetic effect. The difference in the size of effects of these compounds on biochemical parameters of blood in the experiment on C57BL/6Ay mice was in good agreement with the computational prediction of the priority ranking of biological targets for these compounds. These results indicate that bornyl derivatives of p-(benzyloxy)phenylpropionic acid have a good potential as new agents for diabetes mellitus treatment due to their hypoglycemic and lipid-normalizing properties. © 2020 by the authors. Licensee MDPI, Basel, Switzerland.

Kuranov S. , Luzina O. , Khvostov M. , Baev D. , Kuznetsova D. , Zhukova N. , Vassiliev P. , Kochetkov A. , Tolstikova T. , Salakhutdinov N.
Bornyl derivatives of p-(Benzyloxy)phenylpropionic acid: In vivo evaluation of antidiabetic activity

Pharmaceuticals. 2020. V.13. N11. 404 :1-22. DOI: 10.3390/ph13110404 WOS Scopus РИНЦ OpenAlex

Full text from publisher

Published online:

Nov 19, 2020

Web of science:	WOS:000593842000001
Scopus:	2-s2.0-85096366629
Elibrary:	45136328
OpenAlex:	W3098594124

DB	Citing
Scopus	5
Web of science	7
Elibrary	10
OpenAlex	7