Sevanol and its analogues: chemical synthesis, biological effects and molecular docking

Belozerova, Olga A.; Osmakov, Dmitry I.; Vladimirov, Andrey; Koshelev, Sergey G.; Chugunov, Anton O.; Andreev, Yaroslav A.; Паликов, В. А.; Palikova, Yu. A.; Shaykhutdinova, E. R.; Gvozd, Artem; Dyachenko, Igor A.; Efremov, Roman G.; Kublitski, Vadim S.; Козлов, С. А.

doi:10.22541/au.158880257.72351495

Cited by 6 publications

(2 citation statements)

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“…Sevanol is a natural lignan isolated from thyme Armenia that has anti-inflammatory and analgesic effects, with specific targets not yet defined. However, chemically synthesized sevanol and its analogs have been demonstrated to affect ASIC1a and ASIC3 (Belozerova et al, 2020). Further studies have shown that sevanol has a binding site that can be occupied by FRRF-amide peptides, which are located in the central vestibule of the ASIC1a channel (Belozerova et al, 2020).…”

Section: Natural Organic Mattermentioning

confidence: 99%

“…However, chemically synthesized sevanol and its analogs have been demonstrated to affect ASIC1a and ASIC3 (Belozerova et al, 2020). Further studies have shown that sevanol has a binding site that can be occupied by FRRF-amide peptides, which are located in the central vestibule of the ASIC1a channel (Belozerova et al, 2020). This observation suggests a possible mechanism by which sevanol inhibits ASIC1a, but further studies are needed to verify this possibility.…”

Section: Natural Organic Mattermentioning

confidence: 99%

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ASIC1a channel in Age-Related Diseases: Therapeutic Implications

Zhou

Liang

et al. 2022

Preprint

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Age-related diseases have become more common with the advancing age of the worldwide population. Such diseases involve multiple organs, with tissue degeneration and cellular apoptosis. To date, there is a general lack of effective drugs for treatment of most age-related diseases and there is therefore an urgent need to identify novel drug targets for improved treatment. Acid-sensing ion channel 1a (ASIC1a) is a degenerin/epithelial sodium channel family member, which is activated in an acidic environment to regulate pathophysiological processes such as acidosis, inflammation, hypoxia, and ischemia. A large body of evidence suggests that ASIC1a plays an important role in the development of age-related diseases (e.g., stroke, rheumatoid arthritis, Huntington’s disease, and Parkinson’s disease.). Herein we present: 1) a review of ASIC1a channel properties, distribution, and physiological function; 2) a summary of the pharmacological properties of ASIC1a; 3) and a consideration of ASIC1a as a potential therapeutic target for treatment of age-related disease.

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Section: Natural Organic Mattermentioning

confidence: 99%

Section: Natural Organic Mattermentioning

confidence: 99%

ASIC1a channel in Age-Related Diseases: Therapeutic Implications

Zhou

Liang

et al. 2022

Preprint

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Retinoic Acid-Differentiated Neuroblastoma SH-SY5Y Is an Accessible In Vitro Model to Study Native Human Acid-Sensing Ion Channels 1a (ASIC1a)

Kalinovskii

Osmakov

Koshelev

et al. 2022

Biology

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Human neuroblastoma SH-SY5Y is a prominent neurobiological tool used for studying neuropathophysiological processes. We investigated acid-sensing (ASIC) and transient receptor potential vanilloid-1 (TRPV1) and ankyrin-1 (TRPA1) ion channels present in untreated and differentiated neuroblastoma SH-SY5Y to propose a new means for their study in neuronal-like cells. Using a quantitative real-time PCR and a whole-cell patch-clamp technique, ion channel expression profiles, functionality, and the pharmacological actions of their ligands were characterized. A low-level expression of ASIC1a and ASIC2 was detected in untreated cells. The treatment with 10 μM of retinoic acid (RA) for 6 days resulted in neuronal differentiation that was accompanied by a remarkable increase in ASIC1a expression, while ASIC2 expression remained almost unaltered. In response to acid stimuli, differentiated cells showed prominent ASIC-like currents. Detailed kinetic and pharmacological characterization suggests that homomeric ASIC1a is a dominant isoform among the present ASIC channels. RA-treatment also reduced the expression of TRPV1 and TRPA1, and minor electrophysiological responses to their agonists were found in untreated cells. Neuroblastoma SH-SY5Y treated with RA can serve as a model system to study the effects of different ligands on native human ASIC1a in neuronal-like cells. This approach can improve the characterization of modulators for the development of new neuroprotective and analgesic drugs.

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Recent Developments in Protein Lactylation in PTSD and CVD: Novel Strategies and Targets

Kozlakidis,

Shi,

Abarbanel

et al. 2023

BioTech

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In 1938, Corneille Heymans received the Nobel Prize in physiology for discovering that oxygen sensing in the aortic arch and carotid sinus was mediated by the nervous system. The genetics of this process remained unclear until 1991 when Gregg Semenza while studying erythropoietin, came upon hypoxia-inducible factor 1, for which he obtained the Nobel Prize in 2019. The same year, Yingming Zhao found protein lactylation, a posttranslational modification that can alter the function of hypoxia-inducible factor 1, the master regulator of cellular senescence, a pathology implicated in both post-traumatic stress disorder (PTSD) and cardiovascular disease (CVD). The genetic correlation between PTSD and CVD has been demonstrated by many studies, of which the most recent one utilizes large-scale genetics to estimate the risk factors for these conditions. This study focuses on the role of hypertension and dysfunctional interleukin 7 in PTSD and CVD, the former caused by stress-induced sympathetic arousal and elevated angiotensin II, while the latter links stress to premature endothelial cell senescence and early vascular aging. This review summarizes the recent developments and highlights several novel PTSD and CVD pharmacological targets. They include lactylation of histone and non-histone proteins, along with the related biomolecular actors such as hypoxia-inducible factor 1α, erythropoietin, acid-sensing ion channels, basigin, and Interleukin 7, as well as strategies to delay premature cellular senescence by telomere lengthening and resetting the epigenetic clock.

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Sevanol and its analogues: chemical synthesis, biological effects and molecular docking

Cited by 6 publications

References 0 publications

ASIC1a channel in Age-Related Diseases: Therapeutic Implications

ASIC1a channel in Age-Related Diseases: Therapeutic Implications

Retinoic Acid-Differentiated Neuroblastoma SH-SY5Y Is an Accessible In Vitro Model to Study Native Human Acid-Sensing Ion Channels 1a (ASIC1a)

Recent Developments in Protein Lactylation in PTSD and CVD: Novel Strategies and Targets

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