Neurotrophic Action of Comenic Acid and Its Derivatives Potassium Comenate and Calcium Comenate

2018 ◽  
Vol 165 (4) ◽  
pp. 465-469 ◽  
Author(s):  
L. V. Shurygina ◽  
E. I. Zlishcheva ◽  
A. A. Kravtsov
2015 ◽  
Vol 159 (4) ◽  
pp. 466-468 ◽  
Author(s):  
L. V. Shurygina ◽  
E. I. Zlishcheva ◽  
V. V. Khablyuk ◽  
A. N. Kravtsova ◽  
N. O. Abramova ◽  
...  

2019 ◽  
Vol 89 (3) ◽  
pp. 465
Author(s):  
О.Е. Дик

AbstractA bifurcation analysis of a nociceptive neuron model was performed to study how the firing activity pattern changes when an antinociceptive response to damaging pain stimulation arises in rat dorsal ganglia. Ectopic train activity was found to arise in the model. Suppression of train activity was demonstrated to proceed solely through modification of the activation gating structure of the Na _ V 1.8 slow sodium channel in response to comenic acid, which exerts an analgesic effect and is an active ingredient of the new nonopioid analgesic Anoceptin.


1978 ◽  
Vol 12 (2) ◽  
pp. 230-233
Author(s):  
G. A. Khutornenko ◽  
I. G. Gubareva ◽  
V. V. Parin ◽  
A. E. Vasil'ev

Author(s):  
Ilya V. Rogachevskii ◽  
Vera B. Plakhova ◽  
Valentina A. Penniyaynen ◽  
Stanislav G. Terekhin ◽  
Svetlana A. Podzorova ◽  
...  

A gamma-pyrone derivative, comenic acid, activates the opioid-like receptor-mediated signaling pathway that modulates the NaV1.8 channels in the primary sensory neuron membrane. These channels are responsible for generation of the nociceptive signal; gamma-pyrones can therefore have a great therapeutic potential as analgesics, and this effect deserves a deeper understanding. The novelty of our approach to the design of a medicinal substance is based on a combination of the data obtained on living neurons using very sensitive physiological methods and the results of quantum-chemical calculations. This approach allows to correlate the molecular structure of gamma-pyrones with their ability to evoke a physiological response of the neuron. Comenic acid can bind two calcium cations. One of them is chelated by the carbonyl and the hydroxyl functional groups, while another one forms the salt bond with the carboxylate anion. Calcium-bound gamma-pyrones are fundamentally different in electrostatic properties from the free gamma-pyrone molecules. These two calcium ions are the key elements involved in ligand-receptor binding. It is very likely ion-ionic interactions between these cations and anionic functional groups of the opioid-like receptor that activate the latter. The calculated intercationic distance of 9.5 Å is a structural criterion for effective ligand-receptor binding of calcium-bound gamma-pyrones.


2018 ◽  
Vol 13 (11) ◽  
pp. 1934578X1801301 ◽  
Author(s):  
Alexey V. Kletskov ◽  
Vladimir I. Potkin ◽  
Irina A. Kolesnik ◽  
Sergey K. Petkevich ◽  
Anastasia V. Kvachonak ◽  
...  

Methyl 5-hydroxy-4-oxo-4 H-pyran-2-carboxylate was synthesized by esterification of methanol with comenic acid under acidic catalysis. The obtained ester was alkylated with 3-(chloromethyl)-5-phenylisoxazole and 4,5-dichloro-3-(chloromethyl)isothiazole to afford corresponding conjugates containing isoxazole and isothiazole moieties which then were transformed into water-soluble Li-salts. During the bioassays of synthesized isoxazole and isothiazole derivatives of comenic acid in mixtures with first-line antitumor drug Temobel (Temozolomid) used in brain tumors chemotherapy, a synergetic effect was observed.


2020 ◽  
Vol 21 (22) ◽  
pp. 8717
Author(s):  
Hitoshi Tonomura ◽  
Masateru Nagae ◽  
Ryota Takatori ◽  
Hidenobu Ishibashi ◽  
Tomonori Itsuji ◽  
...  

This paper aims to provide a comprehensive review of the changing role of hepatocyte growth factor (HGF) signaling in the healthy and diseased synovial joint and spine. HGF is a multifunctional growth factor that, like its specific receptor c-Met, is widely expressed in several bone and joint tissues. HGF has profound effects on cell survival and proliferation, matrix metabolism, inflammatory response, and neurotrophic action. HGF plays an important role in normal bone and cartilage turnover. Changes in HGF/c-Met have also been linked to pathophysiological changes in degenerative joint diseases, such as osteoarthritis (OA) and intervertebral disc degeneration (IDD). A therapeutic role of HGF has been proposed in the regeneration of osteoarticular tissues. HGF also influences bone remodeling and peripheral nerve activity. Studies aimed at elucidating the changing role of HGF/c-Met signaling in OA and IDD at different pathophysiological stages, and their specific molecular mechanisms are needed. Such studies will contribute to safe and effective HGF/c-Met signaling-based treatments for OA and IDD.


1853 ◽  
Vol 20 (3) ◽  
pp. 401-416
Author(s):  
Henry How

In a paper on Comenic Acid, read before this Society in April of last year, and since honoured with a place in its Transactions, I mentioned my being engaged in an investigation on Meconic Acid; the details of the experiments referred to form the matter of the present communication.My object in undertaking this subject was to ascertain if products corresponding to those described as derived from comenic acid were formed under similar circumstances in the case of meconic acid. I also thought it probable, that as the former is itself a derivative of the latter, the changes undergone by meconic acid in some reactions, would be found to result in substances apparently the immediate derivatives of comenic acid. This remark refers to the action of heat on meconate of ammonia; and it will be seen that the expectation was realised. A similar result was found in other instances, where it had not been anticipated.


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