Effect of thymol on kinetic properties of Ca and K currents in rat skeletal muscle

Szentandrássy, Norbert; Szentesi, Péter; Magyar, János; Nánási, Péter P.; Csernoch, László

doi:10.1186/1471-2210-3-9

Cited by 22 publications

(11 citation statements)

References 25 publications

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“…Blockade of voltage-operated sodium channels were attributed to confer the antinociceptive and anesthetic effects (Haeseler et al, 2002). In rat skeletal muscle fibers isolated enzymatically, thymol (30–600 μg) treatment suppressed both calcium (Ca 2+ ) and potassium (K + ) currents in a concentration-dependent manner with half-maximal effect (EC 50 ) values of 193 ± 26 and 93 ± 11 μM and Hill coefficients of 2.52 ± 0.29 and 1.51 ± 0.18 respectively (Szentandrassy et al, 2003). Thymol has been shown to accelerate K + -induced contracture in skeletal muscle and inhibit Ca 2+ -binding by the fragmented sarcoplasmic reticulum thus causing the suppression of relaxation (Ebashi, 1965).…”

Section: Introductionmentioning

confidence: 99%

Pharmacological Properties and Molecular Mechanisms of Thymol: Prospects for Its Therapeutic Potential and Pharmaceutical Development

et al. 2017

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Thymol, chemically known as 2-isopropyl-5-methylphenol is a colorless crystalline monoterpene phenol. It is one of the most important dietary constituents in thyme species. For centuries, it has been used in traditional medicine and has been shown to possess various pharmacological properties including antioxidant, free radical scavenging, anti-inflammatory, analgesic, antispasmodic, antibacterial, antifungal, antiseptic and antitumor activities. The present article presents a detailed review of the scientific literature which reveals the pharmacological properties of thymol and its multiple therapeutic actions against various cardiovascular, neurological, rheumatological, gastrointestinal, metabolic and malignant diseases at both biochemical and molecular levels. The noteworthy effects of thymol are largely attributed to its anti-inflammatory (via inhibiting recruitment of cytokines and chemokines), antioxidant (via scavenging of free radicals, enhancing the endogenous enzymatic and non-enzymatic antioxidants and chelation of metal ions), antihyperlipidemic (via increasing the levels of high density lipoprotein cholesterol and decreasing the levels of low density lipoprotein cholesterol and low density lipoprotein cholesterol in the circulation and membrane stabilization) (via maintaining ionic homeostasis) effects. This review presents an overview of the current in vitro and in vivo data supporting thymol’s therapeutic activity and the challenges concerning its use for prevention and its therapeutic value as a dietary supplement or as a pharmacological agent or as an adjuvant along with current therapeutic agents for the treatment of various diseases. It is one of the potential candidates of natural origin that has shown promising therapeutic potential, pharmacological properties and molecular mechanisms as well as pharmacokinetic properties for the pharmaceutical development of thymol.

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Section: Introductionmentioning

confidence: 99%

Pharmacological Properties and Molecular Mechanisms of Thymol: Prospects for Its Therapeutic Potential and Pharmaceutical Development

et al. 2017

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“…Nevertheless, eugenol, a terpenoid widely used as a local anesthetic in dental clinics, exhibited greater pharmacological efficacy; it inhibited approximately 80% of the IK total in trigemal ganglion neurons . In contrast, thymol fully blocked the K + current in skeletal muscle . Thymol also completely suppresses the transient outward current ( I to ), the rapid component of the delayed rectifier current ( I Kr ), and the slow component of the delayed rectifier current ( I Ks ) in ventricular cardiomyocytes…”

Section: Resultsmentioning

confidence: 99%

Inhibitory Effect of Terpinen-4-ol on Voltage-Dependent Potassium Currents in Rat Small Sensory Neurons

et al. 2015

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The biological and pharmacological activities of the terpenoid terpinen-4-ol (1), which include depressant effects in the central nervous system, are of potential therapeutic interest. In the present study, the effects of 1 on neuronal excitability and voltage-dependent K(+) currents in the somatic sensory system were investigated. Intact and dissociated neurons of rat dorsal root ganglia (DRG) were used for intracellular and patch-clamp recordings, respectively. In neurons of intact DRG, 1 caused concentration-dependent depolarization of the resting membrane potential and increased input resistance. 1 also inhibited action potentials (AP) and decreased AP parameters, with the exception of AP duration, which was increased. In dissociated DRG neurons, 1 partially blocked the total K(+) current in a concentration-dependent manner. 1 inhibited I(A), I(D), and I(K) with IC50 values of 3.2 ± 03, 0.7 ± 0.1, and 1.6 ± 0.7 mM, respectively. 1 did not shift either the steady-state activation or inactivation curves of I(A), I(D), and I(K) but reduced the decay time course of I(A). The alterations in DRG reported here are consistent with the inhibition of K(+) currents and might partially explain the effect of 1 on excitable tissues.

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“…by epoxides or formaldehydes) or noncovalently, interfering with transcription or damaging the DNA; protein denaturation or coagulation through changes in polarity or hydrogen bonding of the local environment (e.g., by alcohols); and disruption of redox homeostasis (e.g., by metals such as silver, or derivatized phenol compounds). − Disrupting redox homeostasis produces many outcomes, including overstimulation of oxygen uptake, disrupting ATP synthesis by interfering with electron transport chains, and uncoupling oxidative phosphorylation or active transport of protons from other processes. ,, The fine balance of redox homeostasis in cells can be disrupted by introducing or modulating the metabolism of free radicals . For example, phenol compounds are potent redox cyclers in cells, which can destabilize cellular redox homeostasis and/or antioxidant systems, inhibiting the growth of microbial pathogens. ,, In particular, inhibition of glutathione reductase or superoxide dismutase enzymes or defense pathways such as the mitogen-activated protein kinase (MAPK) pathway may effectively prevent fungal growth by redox-active compounds …”

Section: Introductionmentioning

confidence: 99%

Design and Testing of Safer, More Effective Preservatives for Consumer Products

Buckley

Hart‐Cooper

Kim

et al. 2017

ACS Sustainable Chem. Eng.

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Preservatives deter microbial growth, providing crucial functions of safety and durability in composite materials, formulated products, and food packaging. Concern for human health and the environmental impact of some preservatives has led to regulatory restrictions and public pressure to remove individual classes of compounds, such as parabens and chromated copper arsenate, from consumer products. Bans do not address the need for safe, effective alternative preservatives, which are critical for both product performance (including lifespan and therefore life cycle metrics) and consumer safety. In this work, we studied both the safety and efficacy of a series of phenolic preservatives and compared them to common preservatives found in personal care products and building materials. We quantified antimicrobial activity against Aspergillus brasiliensis (mold) and Pseudomonas aeruginosa (Gram negative bacteria), and we conducted a hazard assessment, complemented by computational modeling, to evaluate the human and environmental health impacts of these chemicals. We found that octyl gallate demonstrates better antimicrobial activity and comparable or lower hazards, compared to current-use preservatives. Therefore, octyl gallate may serve as a viable small-molecule preservative, particularly in conjunction with low concentrations of other preservatives that act through complementary mechanisms.

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Effect of thymol on kinetic properties of Ca and K currents in rat skeletal muscle

Cited by 22 publications

References 25 publications

Pharmacological Properties and Molecular Mechanisms of Thymol: Prospects for Its Therapeutic Potential and Pharmaceutical Development

Pharmacological Properties and Molecular Mechanisms of Thymol: Prospects for Its Therapeutic Potential and Pharmaceutical Development

Inhibitory Effect of Terpinen-4-ol on Voltage-Dependent Potassium Currents in Rat Small Sensory Neurons

Design and Testing of Safer, More Effective Preservatives for Consumer Products

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