Membrane-stabilizing Effect Research Articles

Comparative Anti-inflammatory Activity of a Nanocomposite-Based Herbal Oral Rinse and a Commercial Oral Rinse.

The present study aimed to evaluate and compare the anti-inflammatory effects of two oral rinse formulations, a commercial oral rinse and anOcimum tenuiflorum and Ocimum gratissimum(nanocomposites, NCs) oral rinse, using in vitro assays commonly employed to assess anti-inflammatory activity. The anti-inflammatory potential of the oral rinse formulations was assessed using bovine serum albumin (BSA) denaturation, egg albumin denaturation, and membrane stabilization assays. Diclofenac sodium was used as a reference standard in all assays. The inhibition percentages of BSA denaturationand egg albumin denaturation assays, as well as membrane stabilization effects, were measured at various concentrations of the oral rinse formulations. Both the commercial oral rinse and theOcimum tenuiflorum and Ocimum gratissimumoral rinse demonstrated significant inhibition of BSA denaturation, indicating their anti-inflammatory potential. TheOcimum tenuiflorum and Ocimum gratissimum (NCs) oral rinse consistently showed higher inhibition percentages than the commercial oral rinse, suggesting stronger anti-inflammatory effects in this assay. In the egg albumin denaturation assay, both formulations exhibited inhibition of protein denaturation, with theOcimum tenuiflorum and Ocimum gratissimum(NCs) oral rinse showing comparable or slightly higher inhibition percentages. The membrane stabilization assay further supported the anti-inflammatory properties of both formulations, with theOcimum tenuiflorum and Ocimum gratissimum (NCs) oral rinse demonstrating efficacy comparable to diclofenac sodium. The results suggest thatOcimum tenuiflorum and Ocimum gratissimum (NCs) oral rinse may possess stronger anti-inflammatory effects compared tocommercial oral rinse, as evidenced by higher inhibition percentages in the BSA denaturation assay. Both formulations showed promising anti-inflammatory activity in the egg albumin denaturation and membrane stabilization assays, indicating their potential for mitigating inflammation. TheOcimum tenuiflorum and Ocimum gratissimum (NCs) oral rinse exhibits significant anti-inflammatory effects in vitro, potentially surpassing the efficacy of the commercial oral rinse. Further studies are needed to explore the clinical implications of these findings and to validate the anti-inflammatory properties of theOcimum tenuiflorum and Ocimum gratissimum (NCs) oral rinse in vivo.

Multifaceted Chemico-Pharmacological Insights into Cynometra ramiflora L.: Unveiling its GC-MS, Cytotoxic, Thrombolytic, Anti-Inflammatory, Antioxidant, Anti-Diarrheal, Hypoglycemic, and Analgesic Potentials

Objective: This study aimed to comprehensively evaluate the chemico-pharmacological properties of methanolic extractives derived from Cyanometra ramiflora leaves, encompassing a spectrum of activities including cytotoxic, thrombolytic, membrane-stabilizing, antioxidant, antidiarrheal, hypoglycemic, and analgesic effects. Methods: Phytomolecules were identified using Gas Chromatography-Mass Spectrometry (GC-MS), while antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and total phenolic content tests. Cytotoxicity was determined through the brine shrimp bioassay, while thrombolytic activity was evaluated via clot lysis assays, and membrane-stabilizing effects were investigated for potential anti-inflammatory properties. In-vivo experiments using mice were conducted solely with the methanolic extract to assess central and peripheral analgesic, hypoglycemic, and antidiarrheal properties. Results: The presence of 47 compounds in the methanolic extract, with tetratriacontyl pentafluoropropionate (9.25%), pentatriacontane (8.75%), and 2-methylhexacosane (5.9%) being predominant. The dichloromethane-soluble fraction exhibited the highest cytotoxicity, with a 50% lethal concentration (LC50) of 11.05 µg/mL. Both petroleum-ether and methanol-soluble fractions demonstrated more than 50% lysis in thrombolytic activity assays. Under hypotonic and heat-induced conditions, the ethyl acetate and dichloromethane-soluble fractions of C. ramiflora significantly reduced erythrocyte hemolysis. Notably, the methanol-soluble fraction exhibited significant antioxidant potential with 50% inhibitory concentration (IC50) of 17.71 μg/mL compared to the standard EDTA (IC50 = 75.94 μg/mL). The hypoglycemic investigation revealed a 63.73% reduction at 90 min with a 600 mg/kg dose, while mild antidiarrheal activity was observed with a 37.5% reduction in diarrhea at 4 h intervals. Significant analgesic effects were demonstrated in both central and peripheral tests, with a 68.53% reduction in writhing during the peripheral test and an average tail immersion time of 5.38 s at 90 min. Conclusion: C. ramiflora leaves show promise as natural sources for various pharmacological activities, including cytotoxicity, thrombosis, inflammation, antioxidant, hypoglycemic, and analgesic effects. However, further comprehensive research is recommended to elucidate the precise mechanisms of action and analyze the phytochemical composition of C. ramiflora plants.

Kaempferol as an Alternative Cryosupplement for Bovine Spermatozoa: Cytoprotective and Membrane-Stabilizing Effects.

Kaempferol (KAE) is a natural flavonoid with powerful reactive oxygen species (ROS) scavenging properties and beneficial effects on ex vivo sperm functionality. In this paper, we studied the ability of KAE to prevent or ameliorate structural, functional or oxidative damage to frozen-thawed bovine spermatozoa. The analysis focused on conventional sperm quality characteristics prior to or following thermoresistance tests, namely the oxidative profile of semen alongside sperm capacitation patterns, and the levels of key proteins involved in capacitation signaling. Semen samples obtained from 30 stud bulls were frozen in the presence of 12.5, 25 or 50 μM KAE and compared to native ejaculates (negative control-CtrlN) as well as semen samples cryopreserved in the absence of KAE (positive control-CtrlC). A significant post-thermoresistance test maintenance of the sperm motility (p < 0.001), membrane (p < 0.001) and acrosome integrity (p < 0.001), mitochondrial activity (p < 0.001) and DNA integrity (p < 0.001) was observed following supplementation with all KAE doses in comparison to CtrlC. Experimental groups supplemented with all KAE doses presented a significantly lower proportion of prematurely capacitated spermatozoa (p < 0.001) when compared with CtrlC. A significant decrease in the levels of the superoxide radical was recorded following administration of 12.5 (p < 0.05) and 25 μM KAE (p < 0.01). At the same time, supplementation with 25 μM KAE in the cryopreservation medium led to a significant stabilization of the activity of Mg2+-ATPase (p < 0.05) and Na+/K+-ATPase (p < 0.0001) in comparison to CtrlC. Western blot analysis revealed that supplementation with 25 μM KAE in the cryopreservation medium prevented the loss of the protein kinase A (PKA) and protein kinase C (PKC), which are intricately involved in the process of sperm activation. In conclusion, we may speculate that KAE is particularly efficient in the protection of sperm metabolism during the cryopreservation process through its ability to promote energy synthesis while quenching excessive ROS and to protect enzymes involved in the process of sperm capacitation and hyperactivation. These properties may provide supplementary protection to spermatozoa undergoing the freeze-thaw process.

Chemico-pharmacological evaluation of the methanolic leaf extract of Catharanthus ovalis: GC-MS/MS, in vivo, in vitro, and in silico approaches.

Introduction: Natural plant-based medicines have gained popularity recently as a major source of inventive, risk-free, and more potent secondary bioactive compounds with medicinal potential. Catharanthus ovalis is a perennial shrub containing various indole alkaloids cultivated extensively for local medical purposes. Methods: This research is conducted to identify the phytocompounds present in the leaves of C. ovalis and its central and peripheral analgesic, thrombolytic, and membrane-stabilizing activities through tail immersion, acetic acid-induced writhing, human blood clot lysis, and erythrocyte lysis by heat and hypotonic solution methods, respectively. Results and discussion: A total of 39 compounds were identified using GC-MS/MS techniques, including hexadecanoic acid, methyl ester (56.749%), methyl stearate (29.782%), carvacrol and its TBDMS derivative (12.586%), and 9-octadecenoic acid, methyl ester, (E)-] (9.297%) presented in high quantity. The highest tail immersion latency was observed for the 600mg/kg extract of C. ovalis crude extract. Both 400 and 600mg/kg doses of C. ovalis crude extract exhibited prominent peripheral analgesic activity. The maximum thrombolytic effect was observed by DCM soluble fraction extract by inhibiting 54.87% of the clot. However, the aqueous-soluble fraction of this extract manifested an excellent membrane-stabilizing effect by showing 73.98% and 87.51% hemolysis against heat- and hypotonic-induced hemolysis, respectively. Some of the compounds were identified as active agents against different receptors related to these diseases, which supported the findings of in vitro and in vivo tests. Conclusion: Further investigation needs to be conducted to specify and identify the exact mechanism of action of these compounds.

Biomathematical approach determination of a rational formula of complex phytocompositions

Despite the huge achievements of pharmaceutical chemistry, herbal medicines based on medicinal plant raw materials (MPRMs) are still in demand for the treatment of both humans and animals diseases. Their main advantage is the small number of contraindications and side effects. In this case, not one but several phytocompositions are often used, which makes it possible to enhance the effectiveness of the drugs and expand the spectrum of action. The key point in creating multicomponent (galenic) preparations is the development of an accurate phytocomposition formula that best meets the set goals. This process is quite complex and timeconsuming. The purpose of this study was to determine the rational formula of complex phytocompositions based on a biomathematical approach. To reduce the number of performed experiments compared to blind enumeration and increase the reliability and efficiency of the quantitative formula of the phytocomposition, we tested a combination of the approach used in mathematics to search for the extremum of functions of many variables with a biological experiment on Parametium caudatum. In this case, the variables were the shares of each MPRM in the final recipe; function was understood as the pharmacological activity of a substance, determined through its membrane-stabilizing and antioxidant effect. This made it possible to determine the effective ratio of phytocomposition components faster and at lower costs. A comparison was made among more than 100 model samples. It has been established that all of them are non-toxic and have a good antioxidant and membranestabilizing effect. The final combination is by 10-20% more effective than other model samples and therefore it is advisable to use it in the future as the main ingredient for obtaining liposomal preparations for external use with a good pharmacological effect.

Membrane-stabilizing properties of Viburnum opulus fruit liquid extract and cardioprotective effect of tablets based on it

Aim. To study the membrane-stabilizing properties of Viburnum opulus fruit liquid extract (VOFLE) and the cardioprotective activity of “Viburnikor” tablets developed on the basis of VOFLE. Materials and methods. Membrane-stabilizing properties of VOFLE were studied according to the Jager F.C. method in rats with determination of the spontaneous hemolysis degree caused by peroxide oxidation of erythrocyte membranes lipids. VOFLE (50, 100, 150 mg/kg), reference drugs Quercetin (200 mg/kg) and vitamin E (50 mg/kg) were administered to animals intragastrically (i/g) for 7 days. Adrenaline myocardiodystrophy was reproduced in rats by a single subcutaneous injection of adrenaline hydrochloride (0.18 % solution) in the dose of 0.5 mg/kg (0.28 ml/kg) of the body weight. Thirty (30) white male rats with an initial weight of 230-270 g, aged 6-6.5 months were used in the experiment. “Viburnikor” tablets (100 and 150 mg/kg of the VOFLE content) and Quercetin (200 mg/kg) were administered i/g for 7 days, the last time 1 hour before the cardiotoxin administration. The activity of the drugs was evaluated by the survival of animals, the functional state of the myocardium (ECG studies), the effect on the heart mass ratio, the activity of aspartate aminotransferase (AST), the level of active products interacting with thiobarbituric acid (TBA-AP), the content of reduced glutathione (RG) and catalase activity in the heart homogenate. Results and discussion. The VOFLE studied showed the most pronounced membrane-stabilizing effect in the doses of 100 and 150 mg/kg, respectively, 22 and 34 %, the intensity of which was not inferior to the reference drugs Quercetin (26 %) and vitamin E (28 %). On the model of catecholamine myocardiodystrophy, “Viburnikor” tablets (100 and 150 mg/kg) contributed to the improvement of the heart function, as evidenced by the normalization of electrocardiographic parameters and heart mass ratio to the level of intact animals. It has been shown that the cardioprotective properties of “Viburnikor” tablets are exhibited by detecting anticytolic (decrease in the AST activity to the level of intact control) and antioxidant action (decrease in the level of TBA-AP in the myocardium of animals by 31 % (p&lt;0.05) and 33 % (p&lt;0.05), respectively, and a 1.6- and 1.7-fold increase in RG (p&lt;0.05) and catalase (p&lt;0.05) versus the control pathology). Conclusions. It has been proven that the most pronounced membrane-stabilizing effect of the VOFLE studied is in the doses of 100 and 150 mg/kg. Cardioprotective properties of “Viburnikor” tablets have been determined on the model of catecholamine myocardiodystrophy by revealing anticytolic and antioxidant effects. By the intensity of the membrane-stabilizing and cardioprotective activity of the drugs studied, VOFLE and “Viburnikor” tablets are not inferior to the reference drugs.

Taurine Protects Doxorubicin-Induced Hepatotoxicity via Its Membrane-Stabilizing Effect in Rats.

Doxorubicin (dox) is a chemotherapeutic agent widely used against various tumors. However, the clinical use of this agent is limited due to various organ toxicities. Taurine is an intracellular free β-amino acid with antioxidant properties. The present study investigated the protective mechanism of taurine on dox-induced hepatotoxicity. In total, 31 male Sprague-Dawley rats were used in the study. The control group received intraperitoneal (i.p.) 0.9% NaCl alone for 14 days; the taurine (Tau) group received i.p. taurine 150 mg/kg body weight/day for 14 days; the dox group received dox on days 12, 13, and 14 at a cumulative dose of 25 mg/kg body weight/3 days; and the tau+dox group received taurine and dox together at the same dose and through the same route. On day 15, biochemical evaluations were performed on blood samples taken from the left ventricle followed by histological examinations on liver samples. Dox was found to increase liver function enzymes and tissue protein carbonyl levels, causing congestion and tissue damage, thereby leading to dysfunction. Tau was found to histologically preserve the liver morphology without showing any corrective effect on oxidative stress parameters. These findings suggest that the membrane-stabilizing effect of taurine may be more effective than its radical scavenging activity in preventing dox-induced toxicity. Taurine can prevent doxorubicin-induced hepatotoxicity through non-antioxidant pathways.

Evaluation of Dose-dependent Interactions of Antibiotics using RBC Membrane Model Systems

Background: The present study aims to understand the membrane interactions of three different antibiotics widely used for non-specific viral diseases. Methods: The dose-dependent membrane interactions of the selected antibiotics were elucidated using octanol: water partition coefficient and hemolysis assay. Results: Our octanol: water partition coefficient experiments indicated that among the three antibiotics (Azithromycin, Erythromycin, and Amoxicillin), azithromycin and erythromycin were more hydrophobic compared to amoxicillin. This finding also correlated with hypotonic hemolysis assay experiments where the membrane stabilization effects of both azithromycin and erythromycin were reduced in a dose-dependent manner compared to amoxicillin. Conclusion: This may be attributed to the hydrophobic nature of azithromycin, and erythromycin penetrates deeper into the RBC membrane to the extent of the hydrophobic core compared to amoxicillin. The result is also concurrent with the observations from the hemolysis assay in the isotonic conditions. To conclude, among the three antibiotics, azithromycin, erythromycin localized on the hydrophobic core of the lipid membrane, and amoxicillin localized on the outer surface and slight penetration to the outer leaflet of the membrane.

Membrane-stabilizing and protective effects of curcumin in a rotenone-induced rat model of Parkinson disease.

Parkinson disease (PD) is a chronic progressive neurodegenerative disease characterized by both motor and non-motor features. Numerous risk factors (oxidative stress, free radical formation, and several environmental toxins) have been associated with PD. The experimental studies were carried out under in vivo conditions. Biochemical data analysis indicated that compared with the parameters of control (C) rats, rotenone-induced PD rats showed a significant decrease in the specific content of the total fraction of isoforms of O2--producing, heat-stable, NADPH-containing associates (NLP-Nox) from membrane formations of tissues (brain, liver, lung, and small intestine). Compared with the C group indices, in the PD and PD + curcumin (PD + CU) groups there is some change in the shape of the optical absorption spectra of isoforms associated with a change in the amount of Nox in the isoform composition of the total fraction of the NLP-Nox associate. Thus, daily administration of CU (200mg/kg, i.p.) to PD rats for 63days had a regulatory effect, bringing the specific content and O2--producing activity of the total fraction of NLP-Nox isoforms closer to the norm. CU has membrane-stabilizing effects in rotenone-induced PD.

Anti-inflammatory mechanisms of eucalyptol rich Eucalyptus globulus essential oil alone and in combination with flurbiprofen.

Inflammation is the core contributor in the pathogenesis of various acute and chronic illness including appendicitis, bronchitis, arthritis, cancer and neurological diseases. NSAIDs, commonly used medications for inflammatory diseases, on prolonged use cause GI bleeding, ulcers and many more issues. Plant-based therapeutic agents including essential oils in combination with low-dose synthetic drugs have been shown to produce synergistic effects and reduce complications of synthetic drugs. This study was designed to evaluate the anti-inflammatory, analgesic and anti-pyretic properties of Eucalyptus globulus essential oil alone and in combination with flurbiprofen. GC-MS analysis was performed to screen chemical composition of oil. In vitro anti-inflammatory assay (membrane stabilization assay) and in vivo inflammatory acute(carrageenan and histamine-induced paw oedema)and chronic (cotton pellet-induced granuloma and Complete Freund's adjuvant-induced arthritis)modelswere performed to check anti-inflammatoryproperties. Acetic acid-induced algesia and yeast-induced pyrexia models were performed to check analgesic and anti-pyretic properties. qRT-PCR was performed to study the effect of treatments on the expression of inflammatory biomarkers. GC-MS analysis of E. globulus essential oil showed the presence of eucalyptol along with other active biomolecules. 500 + 10mg/kg of oil-drug combination showed significantly (p < 0.05) better in vitro membrane stabilization effects as compared with groups treated with 500mg/kg of E. globulus oil and10mg/kg of Flurbiprofenalone. 500 + 10mg/kg of oil-drug combination showed significantly (p < 0.05) better anti-inflammatory, analgesic and antipyretic effects as compared to 500mg/kg of E. globulus oil alone in all in vivo models. When comparison wasdone between 500 + 10mg/kg of oil-drug combination-treated and 10mg/kg Flurbiprofen-treated group, the former group showed significantly (p < 0.05) better anti-inflammatory and anti-pyretic effects, but there were non-significant differences in the analgesic model. Animal grouptreated with10mg/kg of Flurbiprofen showed significantly (p < 0.05) better anti-inflammatory and analgesic effects than group treated with500mg/kg of oil alone while, there were non-significant differences in anti-pyretic effects. qRT-PCR analysis showed significant (p < 0.05)down-regulation in the expressionof IL-4 and TNF-α in serum samples of animals treated with 500 + 10mg/kg of oil-drug combination as compared to thediseased control (arthritic)group. Overall, the current research demonstrates that Eucalyptus globulus essential oil in combination with flurbiprofen showed better anti-inflammatory, analgesic and anti-pyretic effects than oil and flurbiprofen alone which is attributed to the down-regulation of pro-inflammatory biomarkers (IL-4 and TNF-α). Further studies are required to formulate a stable dosage form and to check the anti-inflammatory efficacy in different inflammatory disorders.

The role of taurine in male reproduction: Physiology, pathology and toxicology.

Taurine, a sulfur-containing amino acid, has a wide range of biological effects, such as bile salt formation, osmotic regulation, oxidative stress inhibition, immunomodulation and neuromodulation. Taurine has been proved to be synthesized and abundant in male reproductive organs. Recently, accumulating data showed that taurine has a potential protective effect on reproductive function of male animals. In physiology, taurine can promote the endocrine function of the hypothalamus-pituitary-testis (HPT) axis, testicular tissue development, spermatogenesis and maturation, delay the aging of testicular structure and function, maintain the homeostasis of the testicular environment, and enhance sexual ability. In pathology, taurine supplement may be beneficial to alleviate pathological damage of male reproductive system, including oxidative damage of sperm preservation in vitro, testicular reperfusion injury and diabetes -induced reproductive complications. In addition, taurine acts as a protective agent against toxic damage to the male reproductive system by exogenous substances (e.g., therapeutic drugs, environmental pollutants, radiation). Related mechanisms include reduced oxidative stress, increased antioxidant capacity, inhibited inflammation and apoptosis, restored the secretory activity of the HPT axis, reduced chromosomal variation, enhanced sperm mitochondrial energy metabolism, cell membrane stabilization effect, etc. Therefore, this article reviewed the protective effect of taurine on male reproductive function and its detailed mechanism, in order to provide reference for further research and clinical application.

Effects of Carbamazepine on Cardiovascular System: Literature Review

Carbamazepine is an anticonvulsant that is commonly used in neurological and psychiatric patients to treat epileptic seizures, neuropathic pain, or bipolar disorder. Carbamazepine side effects, as well as side effects of many antiepileptic drugs, include cardiotoxic effects such as atrioventricular block, bradycardia, and cardiac rhythm disorders. However, carbamazepine has also been reported to have antiarrhythmic, normotimic, and membrane-stabilizing effects. This results in its administration to treat arrhythmias in children. Based on literature, carbamazepine administration as anti-arrhythmic drug is known in cases where the basic therapy was ineffective. The medication is not registered anywhere in the world for this purpose. Thus, it can be administered only off-label. The aim of our literature review is to analyze and summarize the existing data on carbamazepine effects on cardiovascular system, to determine its safety as anti-arrhythmic drug, and to describe various factors fostering its side effects.

Influence of Placenta Cryoextract on the Liver Metabolic and Functional State in Case of D-Galactosamine Hepatitis

Background. Viral hepatitis is one of the most common and dangerous diseases in the world and is the third most common infectious disease. The development of new, more effective and safer hepatoprotective drugs is an urgent task of biomedicine. A wide range of proven biological properties in cryoextract of human placenta, in particular the presence of antioxidant, immunomodulating and anti-inflammatory effects, suggests that it has a hepatoprotective effect. A model of D-galactosamine toxic hepatitis, which is similar to human viral hepatitis in terms of morphological and biochemical changes in the liver, was chosen for the study. Objective. We are aimed to study the effect of the therapeutic and preventive administration of cryopreserved placenta extract on the metabolic and functional state of the liver in the model of D-galactosamine hepatitis in rats. Methods. The study was conducted on 28 male rats weighing 200–220 g. Hepatitis was simulated by a single intraperitoneal injection of a 20% aqueous solution of D-galactosamine at a dose of 400 mg/kg. The cryoextract was administered in the treatment-prophylactic mode – 1 time per day for 3 days before the administration of D-galactosamine and another 2 days after the administration of the aminosugar (5 administrations in total). Results. The development of experimental D-galactosamine hepatitis in rats leads to the formation of functional and metabolic disorders in the form of the activation of lipid peroxidation processes, a violation of pigment metabolism, a decrease in the protein-synthesizing function and the development of cytolytic syndrome, which were indicated by an increase (p &lt; 0.001) in the level of reactants with thiobarbituric acid in liver homogenates by 2.2 times, an increase (p &lt; 0.001) in the level of total bilirubin by 2.5 times, a decrease (p &lt; 0.001) in the albumin-globulin ratio by 46.8% and an increase (p &lt; 0.001) in the level of alanine-aminotransferases by 2.2 times and the level of aspartate-aminotransferases by 70.3% compared to the values ​​of intact animals. Against the background of the administration of placenta cryoextract in experimental hepatitis, the level of reactants with thiobarbituric acid decreased (p &lt; 0.001) by 43.8%, the level of alanine-aminotransferases decreased (p &lt; 0.001) by 2.4 times, and the level of aspartate-aminotransferases decreased (p &lt; 0.001) by 45.3%; the level of total protein increased (p &lt; 0.01) by 17.4%, and the level of total bilirubin decreased (p &lt; 0.001) by 53.5% compared to the indicators of untreated animals. Conclusions. Administration of cryopreserved placenta extract normalized metabolic processes in the liver and restored its functional state due to antioxidant and membrane-stabilizing effects, which weakened the cytolytic syndrome caused by the administration of D-galactosamine and restored the protein-synthesizing function of the liver. In addition, administration of the specified cryoextract neutralized D-galactosamine-induced hyperbilirubinemia.

Ca2+ Signaling Is the Basis for Pacemaker Activity and Neurotransduction in Interstitial Cells of the GI Tract.

Years ago gastrointestinal motility was thought to be due to interactions between enteric nerves and smooth muscle cells (SMCs) in the tunica muscularis. Thus, regulatory mechanisms controlling motility were either myogenic or neurogenic. Now we know that populations of interstitial cells, c-Kit+ (interstitial cells of Cajal or ICC), and PDGFRα+ cells (formerly "fibroblast-like" cells) are electrically coupled to SMCs, forming the SIP syncytium. Pacemaker and neurotransduction functions are provided by interstitial cells through Ca2+ release from the endoplasmic reticulum (ER) and activation of Ca2+-activated ion channels in the plasma membrane (PM). ICC express Ca2+-activated Cl- channels encoded by Ano1. When activated, Ano1 channels produce inward current and, therefore, depolarizing or excitatory effects in the SIP syncytium. PDGFRα+ cells express Ca2+-activated K+ channels encoded by Kcnn3. These channels generate outward current when activated and hyperpolarizing or membrane-stabilizing effects in the SIP syncytium. Inputs from enteric and sympathetic neurons regulate Ca2+ transients in ICC and PDGFRα+ cells, and currents activated in these cells conduct to SMCs and regulate contractile behaviors. ICC also serve as pacemakers, generating slow waves that are the electrophysiological basis for gastric peristalsis and intestinal segmentation. Pacemaker types of ICC express voltage-dependent Ca2+ conductances that organize Ca2+ transients, and therefore Ano1 channel openings, into clusters that define the amplitude and duration of slow waves. Ca2+ handling mechanisms are at the heart of interstitial cell function, yet little is known about what happens to Ca2+ dynamics in these cells in GI motility disorders.

The variants of enteral distress syndrome correction with peritonitis

To determine the effectiveness of a new treatment regimen for patients with widespread peritonitis with an accent on enteroprotection based on the use of a drug of the metabolic type of action of remaxol and physiotherapy. Clinical and laboratory studies of 82 patients with widespread peritonitis, mainly with grade 2 severity according to the Mannheim peritonitis Index, severe form - according to the ARASNE II scale. In the 1st group (28) patients underwent intraoperative intestinal intubation in the traditional way; in the 2nd (22) - intestinal intubation according to the original method; in the 3rd (32) - intestinal intubation according to the original method and combined use of remaxol (parenterally, enterally and intraperitoneally). An intestinal tube of an original design was used, which allows electrical stimulation of the duodenum in the postoperative period. The study evaluates clinical data, the results of instrumental and laboratory studies: ultrasound examination of the abdominal cavity, assessment of the functional state of the small intestine, a number of indicators of homeostasis. It was shown that in patients with acute widespread peritonitis who underwent intestinal intubation according to the original method (group 2), as well as in combination with remaxol (group 3), the postoperative period was relatively more favorable. One of the factors optimizing the course of the disease was the relatively rapid restoration of the structural and functional state of the small intestine due to its electrical stimulation. The clinical and laboratory positive effect was especially significant in the 3rd group of patients, in which the use of remaxol, which has a membrane-stabilizing effect, played a special role in the enteroprotective effect. Timely correction of enteral distress syndrome resulted in a significant decrease in the severity of the syndrome of endogenous intoxication and oxidative stress, which was important in significantly improving the results of treatment of patients. The use of technical innovations in the form of an original nasointestinal tube, which allows to quickly restore intestinal motility due to electrical stimulation, as well as the use of remaxol (parenterally, enterally and intraperitoneally) significantly optimize the course of the early postoperative period of patients with acute widespread peritonitis.

CHARACTERISTICS OF THE INTERACTION BETWEEN LOW-INTENSITY LASER RADIATION AND ERYTHROCYTES

The results of the effect of low-intensity laser radiation on lipid peroxidation and the sorption capacity of erythrocyte membranes under stress are presented. The membrane-stabilizing effect of low-intensity laser radiation and a decrease in the rate of free radical processes are noted, which indicates the prospects of using laser radiation as an activator of the body's natural antioxidant systems. An increase in the sorption capacity of erythrocyte membranes proves the advisability of using low-intensity laser radiation to increase the adaptive capacity and to protect the body from stress.

Taurine as a Natural Antioxidant: From Direct Antioxidant Effects to Protective Action in Various Toxicological Models.

Natural antioxidants have received tremendous attention over the last 3 decades. At the same time, the attitude to free radicals is slowly changing, and their signalling role in adaptation to stress has recently received a lot of attention. Among many different antioxidants in the body, taurine (Tau), a sulphur-containing non-proteinogenic β-amino acid, is shown to have a special place as an important natural modulator of the antioxidant defence networks. Indeed, Tau is synthesised in most mammals and birds, and the Tau requirement is met by both synthesis and food/feed supply. From the analysis of recent data, it could be concluded that the direct antioxidant effect of Tau due to scavenging free radicals is limited and could be expected only in a few mammalian/avian tissues (e.g., heart and eye) with comparatively high (>15–20 mM) Tau concentrations. The stabilising effects of Tau on mitochondria, a prime site of free radical formation, are characterised and deserve more attention. Tau deficiency has been shown to compromise the electron transport chain in mitochondria and significantly increase free radical production. It seems likely that by maintaining the optimal Tau status of mitochondria, it is possible to control free radical production. Tau’s antioxidant protective action is of great importance in various stress conditions in human life, and is related to commercial animal and poultry production. In various in vitro and in vivo toxicological models, Tau showed AO protective effects. The membrane-stabilizing effects, inhibiting effects on ROS-producing enzymes, as well as the indirect AO effects of Tau via redox balance maintenance associated with the modulation of various transcription factors (e.g., Nrf2 and NF-κB) and vitagenes could also contribute to its protective action in stress conditions, and thus deserve more attention.

Comparative chromato-mass spectrometric study of tinctures based on Echinacea purpurea (L.) Moench

An urgent problem today is the spread of secondary immunodeficiencies associated with increased stress, urbanization, and negative changes in the environment that lead to impaired immune function. Herbal remedies are milder, less likely to become addictive and have side effects, and are long-lasting. A promising plant with immunomodulatory action is Echinacea purpurea (L.) Moench, a member of the family Asteraceae. The main active ingredients of echinacea are phenolic compounds, carbohydrates, and alkylamides. The chemical composition of echinacea is also represented by flavonoids, tannins, saponins, higher fatty acids, amino acids, betaine, essential oil, macro- and microelements (Se, Co, Ag, Mo, Zn, Mg, K, Na, Fe, etc.). Drugs have immunostimulatory, antioxidant, membrane-stabilizing effect, promote healing of wounds, burns, ulcers, are used in infectious and viral diseases, especially HF. They are traditionally used for furunculosis, septicemia (infection of the blood), pyorrhea, tonsillitis, especially for the treatment of boils, carbuncles, and abscesses. It is also important that in modern pharmaceutical science the leading place is occupied by research related to the introduction into medical practice of herbal medicines, the study of their chemical composition, standardization, development of optimal technologies for the manufacture of phytopreparations. That is why the objects of our research were tinctures based on Echinacea purpurea. The aim of the work is to study and compare the component composition of tinctures based on Echinacea purpurea (L.) Moench using gas chromatography (GC). Materials and methods. Tinctures of rhizomes with roots of Echinacea purpurea were used for the study: experimental – made according to industrial technological recipe (1:5, extractant – ethanol 70 %) from raw materials harvested in July 2019 at the research site of Zaporizhzhia State Medical University and control – finished products LLC “Zhytomyr Pharmaceutical Factory”, series 20319. Tinctures were investigated on a gas chromatograph Agilent 7890B with mass spectrometric detector 5977B. The NIST14 mass spectrum library was used to identify the components. Results. 31 (experimental) and 23 (control) components were identified by GC in rhizomes with rhizomes of Echinacea purpurea. The results of the study indicate that the qualitative and quantitative chemical composition of rhizomes with roots of Echinacea purpurea was characterized by complexity and variability. This fact complicates the process of standardization of phytopreparations and can affect their effectiveness and safety. Therefore, members of the genus Echinacea should be the subject of further in-depth chemical study. Conclusions. A comparative analysis of the component composition of tinctures based on Echinacea purpurea (L.) Moench was studied and performed with the help of GC. The GC method is suitable for the determination of natural BAS in the composition of phytopreparations from echinacea and can be used in the development of methods for their standardization. The results of the study were of value for further development and improvement of analytical regulations for raw materials and phytopreparations from Echinacea purpurea. They can also be the basis for the creation of new substances with immunomodulatory activity based on the underground organs of echinacea.

Medicinal compositions based on natural vegetal raw materials and individual substances for prevention and treatment of urolithiasis: substantiation of composition and biological screening

Kidney and urinary tract diseases are an urgent problem of our time. An increase in the level of kidney and urinary tract diseases occurs with a decrease in the quality of life and ecology. Recently, due to changes in nutrition, sedentary lifestyle, and the impact of various adverse environmental factors, the formation of kidney stones has become increasingly common. Numerous metabolic disorders in urolithiasis require the use of various drugs. At the same time, despite the constant expansion of the range of synthetic drugs, herbal drugs occupy a significant place in the treatment and prevention of kidney pathology. Therefore, the creation of combinations of medicinal plant raw materials and individual chemical substances that are effective in urolithiasis is an urgent issue of modern medicine and pharmacy. Purpose. Establishing optimal ratios within constructed combinations for membrane-stabilizing and antioxidant activity as an indirect measure of specific activity The scientific novelty of the study is the design of compositions effective for dissolving urinary calculus. Materials and methods. We used technological methods for designing compositions based on natural plant raw materials and individual chemical substances — indapamide, ketoprofen, and mexidol. Biological methods: the effect of the developed combinations on daphnia was studied. Biological screening characterizes the presence of membrane-stabilizing and antioxidant effects in the developed formulations and can be a preliminary indicator for determining specific activity. Results. It was found that the most effective compositions for the vital activities of daphnia were: Composition 1: Sum of individual dry extracts + Indapamide Composition 2: Sum of individual dry extracts + Ketoprofen Composition 3: Sum of individual dry extracts + Mexidol Conclusion. We have developed the following compositions: 1. Sum of individual phytoextracts (dyer’s madder rhizomes with roots (extractant — 70 % ethanol), Orthosiphon stamineus leaves (extractant — 40 % ethanol), knot grass (extractant — 70 % ethanol), birch buds (extractant — 70 % ethanol), peppermint leaves (extractant — 96 % ethanol), bay laurel leaves (extractant — 40 % ethanol), common licorice rhizomes with roots (extractant — 0.25 % ammonia solution) + indapamide. 2. Sum of individual phytoextracts (dyer’s madder rhizomes with roots (extractant — 70 % ethanol), Orthosiphon stamineus leaves (extractant — 40 % ethanol), knot grass (extractant — 70 % ethanol), birch buds (extractant — 70 % ethanol), peppermint leaves (extractant — 96 % ethanol), bay laurel leaves (extractant — 40 % ethanol), common licorice rhizomes with roots (extractant — 0.25 % ammonia solution) + ketoprofen. 3. Sum of individual phytoextracts (dyer’s madder rhizomes with roots (extractant — 70 % ethanol), Orthosiphon stamineus leaves (extractant — 40 % ethanol), knot grass (extractant — 70 % ethanol), birch buds (extractant — 70 % ethanol), peppermint leaves (extractant — 96 % ethanol), bay laurel leaves (extractant — 40 % ethanol), common licorice rhizomes with roots (extractant — 0.25 % ammonia solution) + mexidol. They have membrane-stabilizing and antioxidant activity, which has been tested by biological screening on daphnia. The presence of these two types of activity is the initial screening for a subsequent pharmacological study — the determination of specific activity.

Theoretical study of the possibility of decamethoxin complexes with thiotriazolinе to be formed

Over the last decade, much attention has been paid to the prevention and treatment of chronic diseases of the oral mucosa.&#x0D; This is primarily due to the increase in the number of patients who seek dental care for diseases of the oral mucosa (DOM).&#x0D; Currently, due to the lack of special epidemiological studies, information on the pathology of the oral mucosa in the literature is almost non-existent. The etiology and pathogenesis have not been definitively elucidated. It is established that a significant role in the pathogenesis of chronic inflammatory processes belongs to the state of the microbiocenosis of the oral mucosa.&#x0D; One of the most striking examples of domestic drugs of the antioxidant group is thiotriazoline, developed by the staff of the NGO “Pharmatron”, as well as specialists of the Department of Pharmaceutical Chemistry of Zaporozhye State Medical University under the leadership of professor Mazur I. A. This drug has an antioxidant and membrane-stabilizing effect.&#x0D; The aim. The combined use of several drugs can be complicated by the formation of their supramolecular complexes. Therefore, before the introduction of several substances in it is necessary to model the possibility of intermolecular interactions between them. For this purpose, methods of quantum chemistry are used.&#x0D; Material and methods. We examined the structures and energy characteristics of the complexes, formed thiotriazoline and decamethoxin, also carried out analysis and established at what temperature the formation of a substance from two active components was possible.&#x0D; Results. As a result, the probability of the formation of intermolecular hydrogen bonds is reduced, which is very well seen in the trend of interactions between acid and morpholine.&#x0D; Conclusions. Quantum chemical study of a two-component system consisting of thiotriazoline and decamethoxine showed that the most energetically advantageous three-component complexes have a sufficiently low interaction energy of thiotriazoline and decamethoxine. In addition, the data that are provided in the analysis of the tree diagram suggest that in the technological process in the manufacture of dosage forms, it is advisable to use a temperature not higher than 115℃.