Effects of 1.8-cineole (eucalyptol) on the spontaneous contractile activity of smooth muscles fibre

Plamen, Sagorchev; Lukanov, Julian; e-Michael, Beer Andr

doi:10.5897/jmpr2014.5717

Cited by 7 publications

(3 citation statements)

References 13 publications

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“…It also has the advantage of bringing the effects of the drugs under research closer to how they would act in the body by allowing for the calculation of important pharmacological variables while retaining tissue function [ 122 ]. Previously [ 123 , 124 , 125 , 126 , 127 ], we applied the isolated tissue bath for ex vivo SM activity investigation of different compounds. Thus, we applied the same technique to the exogenous administration of 5 × 10 −5 mol/L PID-loaded Ag NPs (n = 7), compared to Ag NPs (n = 6) and PID only (n = 6).…”

Section: Resultsmentioning

confidence: 99%

Drug-Delivery Silver Nanoparticles: A New Perspective for Phenindione as an Anticoagulant

Nikolova,

Milusheva,

Gledacheva

et al. 2023

Biomedicines

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Anticoagulants prevent the blood from developing the coagulation process, which is the primary cause of death in thromboembolic illnesses. Phenindione (PID) is a well-known anticoagulant that is rarely employed because it totally prevents coagulation, which can be a life-threatening complication. The goal of the current study is to synthesize drug-loaded Ag NPs to slow down the coagulation process. Methods: A rapid synthesis and stabilization of silver nanoparticles as drug-delivery systems for phenindione (PID) were applied for the first time. Results: Several methods are used to determine the size of the resulting Ag NPs. Additionally, the drug-release capabilities of Ag NPs were established. Density functional theory (DFT) calculations were performed for the first time to indicate the nature of the interaction between PID and nanostructures. DFT findings supported that galactose-loaded nanostructure could be a proper delivery system for phenindione. The drug-loaded Ag NPs were characterized in vitro for their antimicrobial, cytotoxic, and anticoagulant activities, and ex vivo for spasmolytic activity. The obtained data confirmed the drug-release experiments. Drug-loaded Ag NPs showed that prothrombin time (PT, sec) and activated partial thromboplastin time (APTT, sec) are approximately 1.5 times longer than the normal values, while PID itself stopped coagulation at all. This can make the PID-loaded Ag NPs better therapeutic anticoagulants. PID was compared to PID-loaded Ag NPs in antimicrobial, spasmolytic activity, and cytotoxicity. All the experiments confirmed the drug-release results.

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Section: Resultsmentioning

confidence: 99%

Drug-Delivery Silver Nanoparticles: A New Perspective for Phenindione as an Anticoagulant

Nikolova,

Milusheva,

Gledacheva

et al. 2023

Biomedicines

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“…Another advantage is that retaining tissue function permits calculation of important pharmacological variables that are more meaningful in a tissue vs. a cellular setting; it comes closer to how the drugs examined would work in the body as a whole [21]. Previously [22][23][24][25][26], the isolated tissue bath was applied for ex vivo SM activity investigation of different compounds, including isoquinoline derivatives. Thus, we applied the same technique to the technique reported in this article with N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides.…”

Section: Resultsmentioning

confidence: 99%

Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

et al. 2022

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This article concerns the synthesis and biological activities of some N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides as isoquinoline precursors and compounds with smooth muscle (SM) relaxant activity. Aim: find the biological activity of N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides and compare it with papaverine, an isoquinoline alkaloid that has been known as a brain and coronary vasodilator and SM relaxant. Materials and methods: In silico simulation with the PASS online program predicts SM relaxant activity for the compounds. The amides were tested on the isolated gastric SM preparations (SMPs) from rats to determine their effects on spontaneous contractile activity (CA) compared with papaverine. The in vivo effect on the learning and memory processes of rats was also assessed. Results: the data from the isometric measurements showed that one of the compounds caused ex vivo relaxation in circular SM tissues isolated from the stomach (corpus) of male Wistar rats. Conclusion: We found that the compound’s SM relaxation uses the papaverine pathway. It also has an improving effect on the cognitive functions of learning and memory processes in rats.

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“…Given the interest in the field of drug discovery, examining the biological activity of recently synthesized compounds is an important scientific topic. Various substances, including 1,2,3,4-tetrahydroisoquinolines [ 26 ], isoquinoline precursors [ 20 ], and eucalyptol [ 27 ], among others, have been the subject of our prior publications on the synthesis and SM activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Molecular Docking, and Biological Evaluation of Novel Anthranilic Acid Hybrid and Its Diamides as Antispasmodics

Milusheva,

Gledacheva,

Stefanova

et al. 2023

IJMS

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The present article focuses on the synthesis and biological evaluation of a novel anthranilic acid hybrid and its diamides as antispasmodics. Methods: Due to the predicted in silico methods spasmolytic activity, we synthesized a hybrid molecule of anthranilic acid and 2-(3-chlorophenyl)ethylamine. The obtained hybrid was then applied in acylation with different acyl chlorides. Using in silico analysis, pharmacodynamic profiles of the compounds were predicted. A thorough biological evaluation of the compounds was conducted assessing their in vitro antimicrobial, cytotoxic, anti-inflammatory activity, and ex vivo spasmolytic activity. Density functional theory (DFT) calculation, including geometry optimization, molecular electrostatic potential (MEP) surface, and HOMO-LUMO analysis for the synthesized compounds was conducted using the B3LYP/6–311G(d,p) method to explore the electronic behavior, reactive regions, and stability and chemical reactivity of the compounds. Furthermore, molecular docking simulation along with viscosity measurement indicated that the newly synthesized compounds interact with DNA via groove binding mode. The obtained results from all the experiments demonstrate that the hybrid molecule and its diamides inherit spasmolytic, antimicrobial, and anti-inflammatory capabilities, making them excellent candidates for future medications.

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Effects of 1.8-cineole (eucalyptol) on the spontaneous contractile activity of smooth muscles fibre

Cited by 7 publications

References 13 publications

Drug-Delivery Silver Nanoparticles: A New Perspective for Phenindione as an Anticoagulant

Drug-Delivery Silver Nanoparticles: A New Perspective for Phenindione as an Anticoagulant

Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

Synthesis, Molecular Docking, and Biological Evaluation of Novel Anthranilic Acid Hybrid and Its Diamides as Antispasmodics

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