Research output: Contribution to journal › Article › peer-review
Evolution of anti-parkinsonian activity of monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in various in vivo models. / Valdman, Elena; Kapitsa, Inga; Ivanova, Еlena et al.
In: European Journal of Pharmacology, Vol. 815, 15.11.2017, p. 351-363.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - Evolution of anti-parkinsonian activity of monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in various in vivo models
AU - Valdman, Elena
AU - Kapitsa, Inga
AU - Ivanova, Еlena
AU - Voronina, Tat`iana
AU - Ardashov, Oleg
AU - Volcho, Konstantin
AU - Khazanov, Veniamin
AU - Salakhutdinov, Nariman
N1 - Publisher Copyright: © 2017 Elsevier B.V.
PY - 2017/11/15
Y1 - 2017/11/15
N2 - It has been found recently that monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (Diol) demonstrates high antiparkinsonian activity in some animal models. We carried out an extended study of the antiparkinsonian activity of Diol in a set of relevant animal models. Diol (20 mg/kg) exhibited an anticataleptogenic effect in the haloperidol-induced catalepsy model and restored motor activity in animals in the reserpine-induced model of oligokinesia. The ability of Diol singly administered before MPTP injection to reduce rigidity comparable to that of activity of L-DOPA (100 mg/kg) was found using the model of Parkinsonian syndrome (PS) induced by single injection of MPTP (30 mg/kg) to C57BL/6 mice. In the model of PS induced by subchronic administration of MPTP (4 × 20 mg/kg), Diol at a dose of 20 mg/kg reduced rigidity with effectiveness comparable to that of L-DOPA, while being superior to L-DOPA in terms of its effect on motor activity. It was found using the model of PS induced by systemic administration of rotenone that subchronic daily oral administration of Diol prior to rotenone injection reduced severity of PS in rats. Assessment of the effects of chronic administration of Diol (20 mg/kg) and L-DOPA to animals with 6-OHDA-induced PS showed that administration of Diol alleviated the symptoms of sensorimotor deficit in right limbs in rats. Thus, the potent antiparkinsonian activity of Diol was demonstrated in all the used rodent models experiments. Diol (20 mg/kg) is as effective as the comparator agent L-DOPA administered at doses of 50–100 mg/kg.
AB - It has been found recently that monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (Diol) demonstrates high antiparkinsonian activity in some animal models. We carried out an extended study of the antiparkinsonian activity of Diol in a set of relevant animal models. Diol (20 mg/kg) exhibited an anticataleptogenic effect in the haloperidol-induced catalepsy model and restored motor activity in animals in the reserpine-induced model of oligokinesia. The ability of Diol singly administered before MPTP injection to reduce rigidity comparable to that of activity of L-DOPA (100 mg/kg) was found using the model of Parkinsonian syndrome (PS) induced by single injection of MPTP (30 mg/kg) to C57BL/6 mice. In the model of PS induced by subchronic administration of MPTP (4 × 20 mg/kg), Diol at a dose of 20 mg/kg reduced rigidity with effectiveness comparable to that of L-DOPA, while being superior to L-DOPA in terms of its effect on motor activity. It was found using the model of PS induced by systemic administration of rotenone that subchronic daily oral administration of Diol prior to rotenone injection reduced severity of PS in rats. Assessment of the effects of chronic administration of Diol (20 mg/kg) and L-DOPA to animals with 6-OHDA-induced PS showed that administration of Diol alleviated the symptoms of sensorimotor deficit in right limbs in rats. Thus, the potent antiparkinsonian activity of Diol was demonstrated in all the used rodent models experiments. Diol (20 mg/kg) is as effective as the comparator agent L-DOPA administered at doses of 50–100 mg/kg.
KW - 6-OHDA
KW - Levodopa
KW - MPTP
KW - Parkinson disease
KW - Rotenone
KW - Terpene
KW - SERIES
KW - RATS
KW - MOUSE MODEL
KW - DISEASE
KW - ANIMAL-MODELS
KW - MICE
KW - BRAIN
KW - Antiparkinson Agents/pharmacology
KW - Oxotremorine/pharmacology
KW - Mice, Inbred C57BL
KW - Reserpine/pharmacology
KW - Parkinsonian Disorders/drug therapy
KW - Male
KW - Cyclohexanols/pharmacology
KW - Catalepsy/drug therapy
KW - Animals
KW - Mice
KW - Disease Models, Animal
UR - http://www.scopus.com/inward/record.url?scp=85030244099&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2017.09.022
DO - 10.1016/j.ejphar.2017.09.022
M3 - Article
C2 - 28939292
AN - SCOPUS:85030244099
VL - 815
SP - 351
EP - 363
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
ER -
ID: 8968373