Fisetin decreases the duration of ictal-like discharges in mouse hippocampal slices

ÖZTÜRK, Hilal; Başoğlu, Harun; Yorulmaz, Nuri; Aydın-Abidin, Selcen; Abidin, İsmail

doi:10.1007/s10867-022-09612-0

Cited by 6 publications

(5 citation statements)

References 41 publications

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“…In accordance with our previous study [16b,45] molecular docking investigations were conducted. Briefly, receptor protein structure obtained from protein data bank (PDB) which are NMDA (5B3J), GABA‐A (6D6T), AMPA (7LEP) and fmpemboron docked to these receptors by using Autodock 4.2.6 software.…”

Section: Experimental Sectionsmentioning

confidence: 77%

Title: A Boron‐Chelating Piperazine‐Tethered Schiff Base Can Modulate Excitability in Brain Slices in a Specific Frequency Range

Basoglu,

Degirmencioglu,

Ozturk

et al. 2023

ChemistrySelect

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The ability of boron‐containing compounds to make various bonds with biological targets draws attention in their use as new therapeutic agents. In this study, the effect of a newly synthesized molecule with the short name fmpemboron, “Difluoro [2‐[([2‐[4‐(2,3,4‐trimethoxybenzyl)piperazin‐1‐yl]ethyl] imino‐κN)methyl]phenolato‐κO]boron (5)”on the excitability of neurons in the brain was investigated for the first time. First of all, fmpemboron was synthesized and characterized. Secondly, virtual scanning of the molecule was performed using ADME and molecular docking methods. Then, epileptiform activities were induced in mouse brain slices using Mg‐free or 4AP methods, and the effect of fmpemboron (5) at different concentrations was examined. The absorbance peak wavelength of fmpemboron (5) is between 330–340 nm and the fluorescence emission peak is 435 nm. According to ADME and molecular docking results, fmpemboron (5) can cross the blood‐brain barrier (BBB) and has affinity for the NMDA receptor. It also significantly reduces the power of oscillations between 8–12 Hz and 13–29 Hz in epileptiform activities generated by the Mg‐free method. Administration of 10 μM fmpemboron (5) had a modulatory effect on epileptiform activities, indicating that fmpemboron (5) can affect various neurological functions through NMDA channels. However, in‐vivo dose‐dependent studies are required to further investigate the effects of this novel molecule.

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Section: Experimental Sectionsmentioning

confidence: 77%

Title: A Boron‐Chelating Piperazine‐Tethered Schiff Base Can Modulate Excitability in Brain Slices in a Specific Frequency Range

Basoglu,

Degirmencioglu,

Ozturk

et al. 2023

ChemistrySelect

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“…Finally, beta (13-30 Hz) and gamma (30-50 Hz) band activities with higher frequency range were matched with attention and other cognitive activities (26)(27)(28). Studies have found that fisetin, which is known to bind to HCN2 channels with high affinity, significantly reduces ictal discharge duration, especially in mice with epilepsy models (29). In addition, there are studies providing evidence that fisetin is neuroprotective in animal models of different disease models and cell culture studies.…”

Section: Discussionmentioning

confidence: 94%

Flavonoidlerin Beyin Fonksiyonu Üzerindeki Potansiyellerini Keşfetmek: Üç Fenolik Bileşiğin Beyin Elektriksel Aktivitesi Üzerindeki Etkileri

ÖZTÜRK,

BAŞOĞLU,

ABİDİN

et al. 2023

Harran Üniversitesi Tıp Fakültesi Dergisi

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Background: The most common polyphenolic compounds taken up by the organism through the food chain are flavonoids. Known to cross the blood-brain barrier, 7,8-DHF, L-theanine and Fisetin are re-ported to have neuronal effects as well as therapeutic potential for neurodegenerative diseases. How-ever, little is known on their acute effects of neuronal function. This study aims to describe the effects of the mentioned flavonoids on the total ECoG activities and band analyzes of healthy mice. Materials and Methods: For this purpose, 3 different groups consisting of 7 subjects were created for each flavonoid administration. After the baseline electrophysiological recordings, flavonoid administra-tion was performed and acute effects were determined. Results: 7.8-DHF increased the theta, alpha and beta band activities while decreasing the total ECoG power. L-theanine and Fisetin did not significantly alter the total ECoG activity. However, L-theanine statistically increased theta, alpha and beta band activities. Conclusions: In conclusion, our data showed that flavonoids could acutely modulate the ECoG respons-es in a band specific manner. They can be considered as candidate molecules for drug discovery studies for central nervous system disorders.

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“…Molecular Docking studies were performed as described elsewhere. 2 Briefly the molecular structure of 5H7P4C4O was obtained from PubChem database (ID: 5877945) and protein structure obtained from protein data bank (PDB), which are NMDA (5B3J), GABA-A (6D6T), AMPA (7LEP) and 5H7P4C4O docked to these receptors by using Autodock 4.2.6 software. For detection of active binding sites, ifenprodil, bicuculline and perampanel were used as references for NMDA, GABA-A and AMPA receptors, respectively.…”

Section: Molecular Docking and Adme Studiesmentioning

confidence: 99%

“…4-aminopyridine (4AP) induced epilepsy method in brain slices were performed as described elsewhere. 2,12,13,15 Briefly ACSF containing 100 μM 4AP were perfused to the chamber to initiate epileptiform activities. Electrophysiological recordings were taken from the CA3 region for 30 minutes after mature epileptiform activity was obtained.…”

Section: Electrophysiological Recordingsmentioning

confidence: 99%

“…Epilepsy is a neurological disorder characterized by recurrent seizures caused by abnormal and excessive neuronal activity in the brain. 1,2 Seizures occur when there is an imbalance between neuronal excitation and inhibition in the central nervous system (CNS). 3 Only the basic chemical properties of the 5H7P4C4O molecule are known, and best of our knowledge, there is no study in the literature on its biological effects.…”

Section: Introductionmentioning

confidence: 99%

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Investigation of In Silico Properties of [5-Hydroxy-7-(Pentyloxy)-2-Phenyl-4h-Chromen-4-One] molecule and its Effects on In-Vitro Epileptiform Activation in Brain Slices

BAŞOĞLU,

ÖZTÜRK,

YORULMAZ

et al. 2023

Acta Medica Nicomedia

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Amaç: Epilepsi tam tedavisi olmayan bir hastalıktır ve yeni ilaç adaylarının araştırılmasını gerektirir. 5-hidroksi-7-(pentiloksi)-2-fenil-4h-kromen-4-one (5H7P4C4O) molekülü ticari olarak mevcuttur, ancak çözünürlüğü, spektroskopik özellikleri ve biyolojik aktivitesi bilinmemektedir. Bu makale, epilepsi tedavisi için 5H7P4C4O adlı bir molekülün ve bunun merkezi sinir sistemindeki (MSS) potansiyel biyolojik etkilerinin araştırılmasına odaklanmaktadır. Yöntem: İlk olarak 5H7P4C4O'nun çözünürlüğü ve spektroskopik özellikleri belirlendi. Fizikokimyasal, farmakokinetik ve ilaca benzerlik özellikleri ADME programı ile in silico olarak değerlendirildi. Ayrıca molekülün nörolojik aktivite üzerindeki potansiyeline odaklanılarak, 5H7P4C4O molekülünün NMDA, AMPA ve GABA-A reseptörleri üzerindeki etkileşim potansiyelleri moleküler yerleştirme yöntemiyle incelenmiştir. Bağlanma enerjileri, NMDA ve GABA-A reseptörleri için potansiyel afinite gösterdi. Daha sonra 5H7P4C4O molekülünün akut etkisi, 30-35 günlük C57BL/6 farelerinin beyin kesitlerinde hipokampusun CA3 bölgesinde elektrofizyolojik olarak incelendi. Epileptiform aktivite, Mg+2 içermeyen ortamda veya 4-aminopiridin (4AP, 100 uM) ile indüklendi. Bulgular: 5H7P4C4O, tek başına uygulandığında 5, 10 ve 20 μM dozlarda hiçbir uyarıcı etki göstermedi. Bununla birlikte, Mg+2 içermeyen modelde iktal sinyalleri söndürdü ve 0-47 Hz frekans aralığındaki sinyallerin toplam gücü üzerinde dikkate değer bir modülatör etki gösterdi. Sonuç: Elde edilen sonuçlara göre 5H7P4C4O'nun nöronal stimülasyon üzerinde modülatör etki göstermektedir. Bu etkiyi sadece Mg+2 içermeyen modelde göstermesi NMDA reseptörleri üzerinden etkinlik gösterdiğini düşündürmektedir. Ayrıca, güç sinyallerini belirli bir frekans aralığında toplama yeteneği, bilişsel ve/veya diğer beyin işlevlerinde potansiyel etkilerinin olduğunu gösterir.

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Fisetin decreases the duration of ictal-like discharges in mouse hippocampal slices

Cited by 6 publications

References 41 publications

Title: A Boron‐Chelating Piperazine‐Tethered Schiff Base Can Modulate Excitability in Brain Slices in a Specific Frequency Range

Title: A Boron‐Chelating Piperazine‐Tethered Schiff Base Can Modulate Excitability in Brain Slices in a Specific Frequency Range

Flavonoidlerin Beyin Fonksiyonu Üzerindeki Potansiyellerini Keşfetmek: Üç Fenolik Bileşiğin Beyin Elektriksel Aktivitesi Üzerindeki Etkileri

Investigation of In Silico Properties of [5-Hydroxy-7-(Pentyloxy)-2-Phenyl-4h-Chromen-4-One] molecule and its Effects on In-Vitro Epileptiform Activation in Brain Slices

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