OF DRUG DESIGN AND MECHANISM
OF DRUG ACTION
EFFECT OF N-[IMINO(1-PIPERIDINYL)METHYL]GUANIDINE
ON FREE-RADICAL PROCESSES AND ANTIOXIDANT-ENZYME
ACTIVITY IN KIDNEYS OF RATS WITH EXPERIMENTAL
TYPE 2 DIABETES MELLITUS
E. I. Sklyarova,
T. N. Popova,
K. K. Shul’gin,
V. V. Spitsina,
D. V. Kryl’skii,
and A. V. Semenikhina
Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 52, No. 3, pp.3–6,March, 2018.
Original article submitted October 28, 2015.
The effect of the synthetic biguanide derivative N-[imino(1-piperidinyl)methyl]guanidine on free-radical pro-
cesses, diene conjugate levels, and superoxide-dismutase and catalase activity in kidneys of rats with experi-
mental type 2 diabetes mellitus (DM2) was studied. It was established that administration of this compound to
rats with DM2 helped to normalize the studied parameters, which may have been due to its positive regulating
effect on free-radical homeostasis.
Keywords: type 2 diabetes mellitus, free-radical processes, antioxidant enzymes, biguanides.
Development of new therapeutic approaches to type 2 di
abetes mellitus (DM2), including use of antioxidant drugs, is
currently a crucial task. The present work studied the syn
thetic biguanide derivative N-[imino(1-piperidinyl)methyl]-
guanidine (NIPMG) (Fig. 1), which was chosen for the tar
geted biological activity using the structure—property pre
diction program PASS (Prediction of Activity Spectra for
Substances), available on-line at http://www.ibmh.msk.su/
pass [http://www.pharmaexpert.ru/PASSOnline/] [1, 2].
NIPMG was synthesized from piperidine (I) and dicyan
diamide (II) in EtOH with HCl (Scheme 1). The obtained
biguanide hydrochloride III was converted to the free base
using sodium methoxide (Scheme 2, Tables 1 and 2).
The goal of the present work was to study the effect of
NIPMG on free-radical processes (FRPs), diene conjugate
(DC) levels, and superoxide-dismutase (SOD, EC 188.8.131.52)
and catalase (EC 184.108.40.206) activities in kidneys of rats with
Pharmaceutical Chemistry Journal, Vol. 52, No. 3, June, 2018 (Russian Original Vol. 52, No. 3, March, 2018)
0091-150X/18/5203-0191 © 2018 Springer Science+Business Media, LLC
Voronezh State University, 1 Universitetskaya Sq., Voronezh, 394018
Center for High Technology, Scientific Research Institute of Applied
Acoustics, 7A 9th of May St., Dubna-1, Moscow Oblast, 141981 Russia.