Evaluation, in vitro, of the radioprotection of DNA from γ-rays by naphazoline

Prouillac, Caroline; Célariès, Benoît; Vicendo, Patricia; Rima, G.

doi:10.1016/j.crvi.2006.01.002

Cited by 10 publications

(7 citation statements)

References 9 publications

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“…According to Kulinskii et al [ 25 ], the radioprotective effectiveness of epinephrine and norepinephrine is realized through their binding to α 1 -adrenergic receptors. Later, highly protective properties were observed in the α 1 -adrenergic agonists methoxamine, phenylephrine, naphazoline and indralin [ 26 – 33 ].…”

Section: Introductionmentioning

confidence: 99%

Comparative efficacy and the window of radioprotection for adrenergic and serotoninergic agents and aminothiols in experiments with small and large animals

Ушаков

2014

Journal of Radiation Research

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This review gives a comparative evaluation of the radioprotective properties and the therapeutic index (TI) of radioprotectors from various pharmacological group in experiments on both small and large animals. It presents a hypothesis explaining the decrease in the TI of cystamine and 5-methoxytryptamine (mexamine), and the retention of that of α1-adrenomimetic indralin, and also compares the effects on large and small animals. The considerable differences in the therapeutic indices of catecholamines, serotonin and cystamine are a consequence of specific features of their mechanisms of radioprotective action. Radioprotectors acting via receptor mediation tend to provide a more expanded window of protection. The reduction in the TI of cystamine in larger animals, such as dogs, may be caused by the greater increase in toxicity of aminothiols in relation to the decrease in their optimal doses for radioprotective effect in going from mice to dogs, which is a consequence of the slower metabolic processes in larger animals. The somatogenic phase of intoxication by cystamine is significantly longer than the duration of its radioprotective effect, and increases with irradiation. The decrease in the radioprotective effect and the TI of mexamine in experiments with dogs may be caused by their lower sensitivity to the acute hypoxia induced by the mexamine. This is because of lower gradient in oxygen tension between tissue cells and blood capillaries under acute hypoxia that is determined by lower initial oxygen consumption in a large animal as compared with a small animal. Indralin likely provides optimal radioprotective effects and a higher TI for large animals via the increased specificity of its adrenergic effect on tissue respiration, which supports the development of acute hypoxia in the radiosensitive tissues of large animals. The stimulatory effect of indralin on early post-irradiation haematopoietic recovery cannot provide a high level of radioprotective action for large animals, but it may promote recovery.

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Section: Introductionmentioning

confidence: 99%

Comparative efficacy and the window of radioprotection for adrenergic and serotoninergic agents and aminothiols in experiments with small and large animals

Ушаков

2014

Journal of Radiation Research

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“…These free radicals will then attack nucleic acids, lipid membranes and proteins to produce secondary radical, hydrogen peroxide (H 2 O 2 ). Hydrogen peroxide can be converted into hydroxyl ion through Fenton reaction [ 8 , 9 , 10 ]. High level of free radicals existence causes toxicity to the cells and induces mutation and carcinogenesis, while low level of free radicals leads to cell proliferation inhibition and apoptosis induction [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

Gelam Honey Protects against Gamma-Irradiation Damage to Antioxidant Enzymes in Human Diploid Fibroblasts

et al. 2013

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The present study was designed to determine the radioprotective effects of Malaysian Gelam honey on gene expression and enzyme activity of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) of human diploid fibroblasts (HDFs) subjected to gamma-irradiation. Six groups of HDFs were studied: untreated control, irradiated HDFs, Gelam honey-treated HDFs and HDF treated with Gelam honey pre-, during- and post-irradiation. HDFs were treated with 6 mg/mL of sterilized Gelam honey (w/v) for 24 h and exposed to 1 Gray (Gy) of gamma rays at the dose rate of 0.25 Gy/min. Gamma-irradiation was shown to down-regulate SOD1, SOD2, CAT and GPx1 gene expressions (p < 0.05). Conversely, HDFs treated with Gelam honey alone showed up-regulation of all genes studied. Similarly, SOD, CAT and GPx enzyme activities in HDFs decreased with gamma-irradiation and increased when cells were treated with Gelam honey (p < 0.05). Furthermore, of the three different stages of study treatment, pre-treatment with Gelam honey caused up-regulation of SOD1, SOD2 and CAT genes expression and increased the activity of SOD and CAT. As a conclusion, Gelam honey modulates the expression of antioxidant enzymes at gene and protein levels in irradiated HDFs indicating its potential as a radioprotectant agent.

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“…При этом периферические α-адренорецепторы оказывают значительное влияние на регуляцию системы кровообращения. Рецепторы данного типа были открыты в почках, и было [32]. На основе полученных in silico данных можно предположить, что радиозащитный эффект нафазолина дополнительно к установленным может быть обусловлен в том числе и активацией антиоксидантных ферментов, в частности супероксиддисмутазы (Р а =0,621).…”

Section: организация здравоохраненияunclassified

Predictability study of the pharmacodynamic properties of drugs <i>in silico</i> by the example of comparing data on the naphazoline clinical use and the results of computer modeling

Иванов

Seleznev

Ivchenko³

et al. 2020

Bulletin of the Russian Military Medical Academy

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The forecast of naphazoline pharmacological properties has been made using the PASS computer program and the ADVER-Pred web resource of the Way2Drug information and computing platform. Biological activity, mechanisms of action, toxic and side effects, as well as other types of activity of the studied drug associated with interaction with antitargets, metabolism and gene expression regulation have been determined. The results of the naphazoline pharmacological properties forecast obtained in silico have been compared with the information available in the literature about its systemic effects in clinical use and poisoning.It has been established that the studied chemical compound has a very wide spectrum of action, which is primarily associated with the stimulation of adrenoreceptors and imidazoline receptors located in many organs and tissues of the body. At the same time, other mechanisms of naphazoline action forecasted in silico allow us to determine possible directions for further research of its clinical use. Among the toxic and side effects, along with such known adverse events as effect on the central nervous system and arterial hypertension, in the clinical use of naphazoline special attention should be paid to the cardio-, hepato- and nephrotoxic effects forecasted with a high degree of probability. The prominent toxic effect of naphazoline can cause the occurrence of life- threatening conditions - acute cerebrovascular disorder, myocardial infarction, cardiac rhythm disorders, acute left ventricular failure. The obtained data confirm that the use of modern computer methods that provide an assessment of biological activity based on the drug-like compound graphic formula allows us to obtain a forecast with a high degree of confidence for both new pharmacological substances and for drugs approved for clinical use in order to clarify their pharmacological properties.

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Evaluation, in vitro, of the radioprotection of DNA from γ-rays by naphazoline

Cited by 10 publications

References 9 publications

Comparative efficacy and the window of radioprotection for adrenergic and serotoninergic agents and aminothiols in experiments with small and large animals

Comparative efficacy and the window of radioprotection for adrenergic and serotoninergic agents and aminothiols in experiments with small and large animals

Gelam Honey Protects against Gamma-Irradiation Damage to Antioxidant Enzymes in Human Diploid Fibroblasts

Predictability study of the pharmacodynamic properties of drugs <i>in silico</i> by the example of comparing data on the naphazoline clinical use and the results of computer modeling

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