Evolution of anti-parkinsonian activity of monoterpenoid (1 R ,2 R ,6 S )-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in various in vivo models

Sukhorukova, N. A.; Kapitsa, I. G.; Ivanova, E. A.; Воронина, Т. А.; Ardashov, Oleg V.; Волчо, К. П.; Хазанов, В. А.; Salakhutdinov, N. F.

doi:10.1016/j.ejphar.2017.09.022

Cited by 9 publications

(11 citation statements)

References 28 publications

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“…Place the animal on an arena and assess four indicators of movement: mobile counts and mobile time (two beam breaks in less than 1 s and duration of this activity),and static counts and active time (two beam breaks that took longer than 1 s and the duration of this activity) 1 (Hille et al, 2001) Uninformed 6 (Neustadt et al, 2007;Zhang et al, 2008;Neustadt et al, 2009;Panarese et al, 2019;Manikandaselvi et al, 2012;Valdman et al, 2017) T A B L E 2 (Continued)…”

Section: Inclined Plane Testmentioning

confidence: 99%

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Waku

Magalhães

Alves

et al. 2021

Eur J of Neuroscience

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Several useful animal models for parkinsonism have been developed so far. Haloperidol‐induced catalepsy is often used as a rodent model for the study of motor impairments observed in Parkinson's disease and related disorders and for the screening of potential antiparkinsonian compounds. The objective of this systematic review is to identify publications that used the haloperidol‐induced catalepsy model for parkinsonism and to explore the methodological characteristics and the main questions addressed in these studies. A careful systematic search of the literature was carried out by accessing articles in three different databases: Web of Science, PubMed and SCOPUS. The selection and inclusion of studies were performed based on the abstract and, subsequently, on full‐text analysis. Data extraction included the objective of the study, study design and outcome of interest. Two hundred and fifty‐five articles were included in the review. Publication years ranged from 1981 to 2020. Most studies used the model to explore the effects of potential treatments for parkinsonism. Although the methodological characteristics used are quite varied, most studies used Wistar rats as experimental subjects. The most frequent dose of haloperidol used was 1.0 mg/kg, and the horizontal bar test was the most used to assess catalepsy. The data presented here provide a framework for an evidence‐based approach to the design of preclinical research on parkinsonism using the haloperidol‐induced catalepsy model. This model has been used routinely and successfully and is likely to continue to play a critical role in the ongoing search for the next generation of therapeutic interventions for parkinsonism.

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Section: Inclined Plane Testmentioning

confidence: 99%

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Waku

Magalhães

Alves

et al. 2021

Eur J of Neuroscience

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“…Parkinson’s disease (PD) is a neurodegenerative disease that is characterized by a gradual loss of dopaminergic neurons in the midbrain substantia nigra pars compacta (SNc) and consequently degeneration of striatal dopaminergic nerve terminal fibers, 1 which can eventually deplete striatal dopamine levels. 2 PD is characterized by special clinical signs including rigidity, slow movement, resting tremor, postural instability, and gait weakness, attributable to loss of dopaminergic neurons. 3,4 These symptoms are progressive and become notable probably because of the spread of pathology in the basal ganglia, 5 with the involvement of oxidative stress resulting from the elevated reactive oxygen species (ROS) produced by many sources, including mitochondrial dysfunction, dopamine metabolism, neuroinflammation of dopaminergic neurons, and aging.…”

Section: Introductionmentioning

confidence: 99%

Neuroprotective effect of agmatine (decarboxylated l-arginine) against oxidative stress and neuroinflammation in rotenone model of Parkinson’s disease

et al. 2018

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Parkinson’s disease (PD) is the second most common age-related neurodegenerative disease after Alzheimer’s disease, characterized by loss of dopaminergic neurons in substantia nigra pars compacta, accompanied by motor and nonmotor symptoms. The neuropathological hallmarks of PD are well reported, but the etiology of the disease is still undefined; several studies assume that oxidative stress, mitochondrial defects, and neuroinflammation play vital roles in the progress of the disease. The current study was established to investigate the neuroprotective effect of agmatine on a rotenone (ROT)-induced experimental model of PD. Adult male Sprague Dawley rats were subcutaneously injected with ROT at a dose of 2 mg/kg body weight for 35 days. Agmatine was injected intraperitoneally at 50 and 100 mg/kg body weight, 1 h prior to ROT administration. ROT-treated rats that received agmatine showed better performance on beam walking and an elevated number of rears within the cylinder test. In addition, agmatine reduced midbrain malondialdehyde as an indication of lipid peroxidation, pro-inflammatory cytokines including tumor necrosis factor alpha and interleukin-1β, and glial fibrillary acidic protein. Moreover, agmatine was responsible for preventing loss of tyrosine hydroxylase-positive neurons. In conclusion, our study showed that agmatine possesses a dose-dependent neuroprotective effect through its antioxidant and anti-inflammatory activities. These findings need further clinical investigations of agmatine as a promising neuroprotective agent for the future treatment of PD.

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“…Previously we identified BBB-penetrating monoterpenoid (1 R ,2 R ,6 S )-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (Prottremin), demonstrating anti-PD activity in animal MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine), rotenone, 6-hydroxydopamine (6-OHDA), and haloperidol models of PD [ 8 , 9 , 10 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

A Newly Identified Monoterpenoid-Based Small Molecule Able to Support the Survival of Primary Cultured Dopamine Neurons and Alleviate MPTP-Induced Toxicity In Vivo

et al. 2022

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Parkinson’s disease (PD) is the most common age-related movement disorder characterized by the progressive loss of nigrostriatal dopaminergic neurons. To date, PD treatment strategies are mostly based on dopamine replacement medicines, which can alleviate motor symptoms but do not slow down the progression of neurodegeneration. Thus, there is a need for disease-modifying PD therapies. The aim of this work was to evaluate the neuroprotective effects of the novel compound PA96 on dopamine neurons in vivo and in vitro, assess its ability to alleviate motor deficits in MPTP- and haloperidol-based PD models, as well as PK profile and BBB penetration. PA96 was synthesized from (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl) cyclohex-3-ene-1,2-diol (Prottremin) using the original three-step stereoselective procedure. We found that PA96: (1) supported the survival of cultured näive dopamine neurons; (2) supported the survival of MPP+-challenged dopamine neurons in vitro and in vivo; (3) had chemically appropriate properties (synthesis, solubility, etc.); (4) alleviated motor deficits in MPTP- and haloperidol-based models of PD; (5) penetrated the blood–brain barrier in vivo; and (6) was eliminated from the bloodstream relative rapidly. In conclusion, the present article demonstrates the identification of PA96 as a lead compound for the future development of this compound into a clinically used drug.

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Evolution of anti-parkinsonian activity of monoterpenoid (1 R ,2 R ,6 S )-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in various in vivo models

Cited by 9 publications

References 28 publications

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Neuroprotective effect of agmatine (decarboxylated l-arginine) against oxidative stress and neuroinflammation in rotenone model of Parkinson’s disease

A Newly Identified Monoterpenoid-Based Small Molecule Able to Support the Survival of Primary Cultured Dopamine Neurons and Alleviate MPTP-Induced Toxicity In Vivo

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