Membrane-stabilizing Activity Research Articles

Assessment of clot-lysing and membrane-stabilizing activity of gallic acid through cyclooxygenase-1 and plasminogen interaction pathways

Assessment of clot-lysing and membrane-stabilizing activity of gallic acid through cyclooxygenase-1 and plasminogen interaction pathways

Phytochemical content, antioxidant, and anti-inflammatory activities of Morrocan Cynara cardunculus L. var. ferocissima leaf methanolic extract.

Cyanra cardunclus L. var. ferocissima is widely used in Morocco as a food and in traditional medicine. Therefore, this study aimed to determine, for the first time, the phytochemical content and antioxidant and anti-inflammatory activities of this variety. Qualitative tests were used to screen for the phytochemical compounds present in the extract, and spectrophotometric methods were used for quantification. The sugar profiles were determined using HPLC. Antioxidant activity was determined in vitro using DPPH, FRAP, and total antioxidant activity assays, and anti-inflammatory activity was assessed using serum albumin denaturation and membrane stabilization assays. The extract contained a high amount of total polyphenols, hydrocinnamic acids, anthocyanins, chlorophyll, ortho-diphenols, terpenoids, and triterpenoids. In addition, five sugars were identified with high amounts of raffinose and sucrose. The extract exerted considerable antioxidant activity by scavenging radicals and reducing power. It exerts anti-inflammatory effects by inhibiting protein denaturation and heat-inducing hemolysis. From the correlation results, anthocyanin, polyphenol, and triterpenoid contents were strongly correlated with DPPH free radical scavenging activity. Orthodiphenols, flavonols, and chlorophyll α were strongly correlated with FRAP, whereas orthodiphenols, hydrocinnamic acids, and triterpenoids were strongly correlated with total antioxidant activity. In terms of anti-inflammatory activity, orthodiphenols, hydrocinnamic acids, and triterpenoids correlated strongly with inhibition of bovine serum albumin denaturation activity, whereas terpenoids, flavonols, and chlorophyll correlated strongly with red cell membrane-stabilizing activity. In conclusion, the Moroccan Cynara cardunclus var. ferocissima leaf methanolic extract constitutes a promising source of phytochemicals with considerable antioxidant and anti-inflammatory activity.

Membrane-stabilizing and clot lysis activities of (±) citronellal: In-vitro studies

Numerous plants and their phytochemicals have been identified as having potential medicinal values and are used to treat different ailments worldwide. (±) Citronellal (CTL) is a monoterpene phytochemical with potential therapeutic benefits including anti-inflammatory, antioxidant, antifungal, and antibacterial actions. AimThe present study aimed to evaluate the membrane-stabilizing and clot-lysis activities of CTL through in vitro studies. For this, we performed hypotonic solution-induced erythrocyte lysing and human blood clot lysis methods to check the membrane-stabilizing and clot lysis capacities of CTL using acetylsalicylic acid (ASA) and streptokinase (STK) as standards, respectively. CTL exhibited concentration-dependent membrane-stabilizing activity with an IC50 = 28.83 ± 1.19 µg/mL. In the clot lysis test, CTL also showed a concentration-dependent clot lysing capacity, where it exhibited 50.46 ± 3.81 % clot lysis at a concentration of 160 μg/mL. In the latter case, the IC50 value was I158.22 ± 2.21 µg/mL. CTL exhibit potent membrane-stabilizing and moderate clot-lysis activity. We suppose that CTL may exert these effects, possibly through its capacity to inhibit inflammatory mediators. Further in vivo and in silico studies are required to elucidate CTL’s exact molecular mechanisms behind these biological effects.

Anti-Arthritic, Anti-Inflammatory, Thrombolytic, Membrane Stabilizing, Antifungal and Cytotoxic Activity of Polyscias scutellaria Leaf Extract: An In-vitro Analysis

The objective of this investigations was to evaluate in Vitro anti-arthritic, anti-inflammatory, thrombolytic, membrane stabilizing, antifungal and cytotoxic activities from the methanolic leaf extract of Polyscias scutellaria. Primary evaluation of methanolic extract of Polyscias scutellaria leaf (MEPSL) was performed via phytochemical screening. Presence of Alkaloids, flavonoids, saponins, glycosides, carbohydrates and reducing sugars were observed by phytochemical screening, among other secondary compounds. Using in vitro methods of protein denaturation, the anti-arthritic and anti-inflammatory properties of MEPSL was investigated. The results showed that the extracts significantly slowed down arthritis and inflammation with the percent inhibition of 94.59% and 86.33% at the conc. of 1000 µg/mL compared to the standard diclofenac sodium (98.19%) and acetyle salicylic acid (98.56%) at same concentration respectively. The thrombolytic activity of the extracts was additionally examined by clotlysis method, and the results showed that the ability to break up blood clots increased with the amount of extract used with the value of 97.32% which is very significant compared to the standard streptokinase which showed clotlysis of 91.304%. MEPSL was also showed action that stabilized membranes by using heat induced hemolysis method, which could be helpful in treating conditions like bleeding and swelling with the percent of protection value of 58.87% when compared to standard diclofenac sodium with the percent of protection value 73.63%. Antifungal action was also seen, which shows that it could be used to treat diseases caused by fungi with the zone of inhibition 7-36 mm varying on the type of fungi. Lastly, in vitro method was used to investigate the extracts' damaging effect on Artemia salina by using shrimp lethality assay. The results showed significant cytotoxicity with the LC50 value of 1.057 µg/mL compared to the standard vincristine sulphate (LC50 value of 0.608 µg/mL). To sum up, it is clear that the phytochemical found in this plant can be used for wide range of drug discovery field due to its potent pharmacological actions.

The role of beta-adrenoreceptors in postoperative ileus in rats

The aim of the research was to evaluate the influence of antagonists of specific beta-adrenergic receptor subtypes on bowel motility following abdominal surgery in rat model of postoperative ileus. Bowel motility was measured by the intestinal transit of Evans blue introduced via orogastric tube after surgical procedures of skin incision, laparotomy and laparotomy with gut manipulation. Male rats were given individual adrenergic receptor subtypes antagonists intraperitoneally, and the influence of administered agents on intestinal transit of Evans blue was then evaluated. No statistically significant differences in the length of intestine in tested rats were observed. Propranolol administered prior to surgical procedure has shown protective effect on Evans blue migration in rats undergoing laparotomy and gut manipulation. Intestinal dye transit for propranolol doses of 10, 30 and 45 mg/kg was 18.00 ± 1.88c m, 23.75 ± 1.71 cm and 22.5 ± 2.43 cm, respectively, and for last two doses, statistically significant increase of dye passage was noted, compared to Evans blue transit of 11.00 ± 2.43 cm in the control group. No acceleration of dye migration was seen following administration of beta1-, beta2- and beta3-selective adrenergic receptor antagonist metoprolol, ICI 118.551 and SR58894A, respectively. Our research confirmed that propranolol at high doses, as seen by other researchers, improved bowel motility in early phase of postoperative ileus. That slight acceleration of intestinal dye transit after surgery with gut manipulation is rather connected with membrane-stabilizing action, than the receptor blocking effect, as this effect was not observed after the application of selective antagonists of respective subtypes of beta-adrenergic receptor.

Development of industrial technology of plant substance of viburnum opulus fruit liquid extract

Nowadays, the development of domestic herbal medicines for the treatment of diseases of the cardiovascular system remains one of the current problems in the health care system of Ukraine. Some types of plant raw materials that can be successfully used in the complex therapy of cardiovascular diseases include viburnum fruits (Viburnum opulus L.). Pharmacological activity, the antimicrobial, antioxidant and cardioprotective properties of the extract developed on their basis from the fruits of the viburnum opulus fruit liquid extract (VOFLE) have studied by preclinical in vitro researches.
 The aim of the work was the development of industrial technology of the domestic plant substance Viburnum opulus fruit liquid extract (VOFLE) for the purpose of it further introduction into the tablet dosage form.
 Experimental samples of viburnum opulus fruits of domestic origin were used as object of research, harvested in the experimental fields of the Institute of Vegetable and Melon growing of the National Academy of Agrarian Sciences of Ukraine (Kharkiv region) to obtain the plant substance VOFLE. Physicochemical and pharmacotechnological methods of research have been used in our work.
 As a result of physical, chemical and pharmacotechnological researches, a domestic plant substance – Viburnum opulus fruit liquid extract (VOFLE) has been developed and standardized by extracting viburnum fruits (Viburni opuli fructus) by water-ethanol mixture 50% at the general ratio of raw material: extractant – 1:10, the analysis of each production stage of the technological process was carried out in order to establish the main technological parameters that are subjected to monitoring during the introduction of plant substances in industrial production and during the validation of the technological process.
 The technology of the domestic herbal substance viburnum opulus fruit liquid extract (VOFLE) obtaining was theoretically justified and experimentally developed with the aim of its further introduction into a tablet medicinal form of cardioprotective and membrane-stabilizing activity. A technological block diagram was developed with the definition of its main critical stages of the production process of the herbal substance, as well as a production equipment scheme, which was tested in industrial conditions of the LLC «Pharmaceutical Company "Zdorovya"», Kharkiv.

The Systematic Assessment of the Membrane-Stabilizing and Antioxidant Activities of Several Kazakhstani Plants in the Asteraceae Family.

The objective of our research was to examine the antioxidant and membrane-protective characteristics of a few medicinal plant extracts belonging to the Asteracea family, along with their flavonoid and polyphenolic content, in order to identify strategies for enhancing beverage composition and boosting the antioxidant capacity of green and black tea. The activity of aqueous-ethanolic extracts from the dried parts of plants, such as Arictum tomentosum Mill., Ghnapilum kasachstanicum Kirp. & Kuprian. ex Kirp., Artemisia schrenkiana Ledeb., A. rutifolia Steph. ex Spreng., A. cina O.Berg, and A. vulgaris L., were examined using a model of Wistar rats. Thiobarbituric acid-reacting substances (TBARS), a marker of malondialdehyde concentration, were used to measure the amount of lipid peroxidation (LPO) in liver microsomes. Considering the outcomes, the extracts from A. tomentosum, G. kasachstanicum, and A. vulgaris exhibit the strongest membrane-stabilizing action among those examined. At a concentration of 5 g/mL, the extracts of these plants demonstrated a significant anti-hemolitic impact, whereas the remaining extracts displayed a similar effect at doses above 10 g/mL. Accordingly, among the extracts studied, the A. tomentosum, G. kasachstanicum, A. schrenkiana, A. rutifolia, A. cina, and A. vulgaris extracts have significant antioxidant properties. The integrated antioxidant and antihemolytic qualities of A. tomentosum and green tea extracts were comparable to those of the individual plant extracts. When the extracts of A. schrenkiana and green tea were combined, similar outcomes were seen, suggesting that there was no appreciable synergistic interaction.

Phytochemical screening and evaluation of antioxidant, anti-inflammatory, antimicrobial, and membrane-stabilizing activities of different fractional extracts of Grewia nervosa (Lour.) Panigrahi

BackgroundGrewia nervosa (Lour.) Panigrahi, a medicinal herb native to the steep forested region of Bangladesh, is utilized as a treatment for a variety of diseases or conditions, including dysmenorrhea, paratyphoid, bone fractures, jaundice, kidney stones, dyspepsia, heat stroke, cold, fever, diarrhea, hepatitis B, ingestion, and anthelmintic medication. This research aims to investigate the phyto-pharmacological qualities of this herb. MethodsThe herb was extracted using absolute ethanol followed by fractionation with n-hexane and chloroform. Following an initial investigation of phytochemicals, antioxidant, anti-inflammatory, antimicrobial, and membrane stabilization activities were assessed using the DPPH, egg albumin model, disc diffusion method, and erythrocyte hemolysis model, respectively. ResultsA preliminary phytochemical report suggests that G. nervosa contains reducing sugars, gums, amides, alkaloids, glycosides, flavonoids, steroids, tannins, flavonoids, and saponins. In a concentration-dependent approach, its fractional extracts displayed promising antioxidant, anti-inflammatory, antimicrobial, and membrane-stabilizing activity. It was seen that all fractions had a statistically significant capacity to prevent RBCs from hemolyzing, which suggests a potent membrane stabilizing function in-vitro. ConclusionTaken together, G. nervosa possesses important secondary metabolites and exhibits in-vitro antioxidant, anti-inflammatory, antimicrobial, and membrane stabilizing capacities. This endorses the conventional usage of G. nervosa, although additional study is needed on this potentially beneficial plant.

Synthesis and Evaluation of 1,2,4-Triazole Derivatives for Antioxidant, Anti-inflammatory, Cytotoxicity and QSAR Analysis

A series of novel 4-amino-5-substituted-1,2,4-triazole-3-thiol derivatives (B1-B18) were synthesized and characterized by spectral analysis. Equimolar portions of thiocarbohydrazide and different acids (substituted aryl/heteroaryl/aliphatic) were fused to synthesize the title compounds. The compounds were evaluated for cytotoxicity, in vitro anti-inflammatory activity and antioxidant activities. Cytotoxicity studies highlighted B4 (2,4-dichloro analog) as the potent cytotoxic molecule with IC50 value of 20.35 μM against MCF-7 cell line compared to cisplatin (IC50 = 12.06 μM). B4 (2,4-dichloro), B18 (oleayl) and B14 (2-hydroxy) showed significant membrane-stabilizing activity with IC50 values < 35 μM, whereas B11 (3,4-dimethoxy), B4 (2,4-dichloro) and B14 (2-hydroxy) displayed moderate proteinase inhibitory activity with IC50 values < 72 μM. Compounds possessing phenolic hydroxyl group (B12−B14) demonstrated an appreciable antioxidant activity in the studied antioxidant models. QSAR analysis revealed the important contribution of molecular connectivity, ionization potential and mass of the compounds for optimum cytotoxicity. Present results suggested compound B4 as a potential lead molecule to design novel and potent cytotoxic and anti-inflammatory agents.

A review on the ethnopharmacology, phytochemistry and pharmacology of Polygonum hydropiper Linn.

Polygonum hydropiper is a herb with worldwide distribution, having tremendous value as traditional medicine among different communities. It is used to cure many kinds of ailments such as gynaecological disorders, ulcer, anxiety, pain, cancer, etc. The present review gives emphasis on a thorough and updated study of the botanical description and taxonomy, distribution, habitat, ethnopharmacology, phytochemical constituents, pharmacological activities and toxicological aspects of P. hydropiper. The information included in this review was collected from different scientific databases like PubMed, ScienceDirect, Google Scholar, etc. In addition to the botanical description and taxonomy, lots of ethnomedicinal use of the water-pepper plant could be found. A good number of compounds belonging to the categories like alkaloids, carbohydrates, flavonoids, etc. were confirmed to be present in the plant. Moreover, in different studies, this plant was found to possess activities like anti-Alzheimer, antibacterial, antidementia, antifertility, neuropharmacological, sedative, anxiolytic, thrombolytic and membrane-stabilizing activity, etc. with minimal toxicity. These properties may be directly related to its possession of a large number of bioactive molecules of different categories. Based on these properties, isolation of responsible compound(s), evaluation of molecular mechanisms of their action and clinical trials are recommended.

THE EFFECT OF QUERCETIN ON MORPHOLOGICAL AND BIOCHEMICAL CHANGES IN RAT LIVER UNDER 270TH DAY CENTRAL DEPRIVATION OF LUTEINIZING HORMONE SYNTHESIS

The development of the inflammatory process in the liver, including under the influence of hepatitis B and C viruses, is controlled by cells of the immune system, namely, sinusoidal endothelial cells, Ito cells and Kupffer cells. Macrophages play one of the key roles in creating the line of defense. The way in which specific populations of macrophages contribute to liver disease and regeneration is a matter of constant debate. Therefore, identifying the characteristics of these populations of human macrophages is of undeniable value in studying their role in the development of liver pathology. The flavonoid quercetin has capillary-stabilizing properties due to its antioxidant and membrane-stabilizing action. The aim of our study was to determine the changes in immunocompetent liver cells, both qualitative and quantitative, caused by inhibition of central testosterone synthesis in male rats due to the introduction of triptorelin acetate on the 270th day, and the potential effect of quercetin on morphology and liver antigen-presenting cells count against the background of previous administration of triptorelin acetate solution. The experiments were performed on 30 adult male white rats. Rats were divided into 3 groups: control (10), experimental I (10), and experimental II (10). Animals from experimental group I were injected triptorelin acetate subcutaneously at a dose of 0.3 mg of active substance per kg of body weight. In experimental group II, animals received triptorelin acetate in the same dosage and quercetin 100 mg per kg body weight 3 times a week, whereas the control group was administered saline. We conducted biochemical studies in 10% liver tissue homogenate. The main production of superoxide anionic radical (SAR) and superoxide dismutase activity were determined. Peroxynitrite and superoxide anion radical are powerful oxidants that can damage biological polymers (DNA, proteins and biological membranes) and lead to the development of oxidative-nitrosative stress.

Experimental study of the pharmacological activity of new azaheterocycles derivatives: A literature review

Diseases associated with the pathology of the cardiovascular system are one of the key causes of death all over the world. In particular, arrhythmia may entail the most severe complications, including unexpected death. With high-tech advances, antiarrhythmic drugs remain an integral part of both therapy and prevention. However, the existing arsenal of drugs often does not provide the necessary clinical effect, and therapy is associated with a high risk of severe adverse events. Another significant problem today is the administration of low-toxic drugs that provide effective anesthesia with a sufficient depth and duration of action. Currently, there is also the problem of the limited effectiveness of many drugs with antitumor, antimicrobial, antiviral, antifungal, anti-inflammatory activity and action on the central nervous system. One of the solutions to address the existing problems in these areas is the search and study of compounds that may serve as a basis for the development of new drugs. Given the membrane-stabilizing action by influencing ion channels, new derivatives of azaheterocycles- compounds of piperidine and piperazine are of particular interest in these areas of medicine. According to domestic studies, new piperidine derivatives during screening and in-depth studies showed pronounced local anesthetic activity during infiltration and conduction anesthesia. The results of a number of studies confirm the presence of antiarrhythmic activity in piperidine derivatives. Experimental data on the synthesis and study of the pharmacological activity of new derivatives of piperidine and piperazine in world practice prove their promise for the creation of drugs in various fields of medicine in the future.

OPTIMIZATION OF DIAGNOSIS OF SECONDARY METABOLIC DISORDERS AND TREATMENT TACTICS IN PATIENTS WITH ANEMIA IN NEOPLASTIC DISEASE IN COLORECTAL CANCER

Colorectal cancer is one of the most common oncological diseases, therefore, the study of this problem is an important issue in clinical practice. This problem becomes especially urgent in case of the formation of anemic syndrome in patients, which causes the emergence of a mutual burden syndrome and increases the risks for a patient. The progressive nature of anemia in colorectal cancer is accompanied by secondary metabolic disorders. The material for the study was the blood plasma of 445 patients (228 men and 217 women). Among them, 53 patients (31 women and 22 men) with iron deficiency anemia were examined and included in the first observation group (І) and 392 patients (206 men (52,55 %) and 186 women (47.45 %)) with colorectal cancer whose course of the underlying disease was burdened with anemia in neoplastic disease were included in the second observation group (II). Among the patients in the second (II) observation group, there were 222 individuals (119 men and 103 women) with malignant neoplasms of the colon (ICD-10 code: С.18), 29 individuals (16 men and 13 women) with malignant neoplasms of the rectosigmoid junction (ICD-10 code: C.19), 138 individuals (82 men and 56 women) with malignant neoplasms of the rectum (code ICD-10 C.20) and 3 patients (2 men and 1 woman) with malignant neoplasms of the anus (ICD-10 code: C.21). The age of the examined patients was from 22 to 79 years. It was found that prior to the initiation of treatment in patients with anemia in neoplastic disease, regardless of the course of colorectal cancer, there was a significant increase in the plasma level of free fractions of heparin, histamine and serotonin (p < 0,001); the ratio of histamine: serotonin was also changed in comparison with the values in the control group (p < 0,05), which indicated both an increased release of heparin, histamine and serotonin from the depot, and an impaired inactivation processes of these biologically active substances. It was correctly concluded that in addition to the baseline therapy the administration of arginine glutamate which causes both antihypoxic and membrane-stabilizing action, reliably contributes to the normalization of secondary metabolic disorders of histamine, serotonin and heparin metabolism in anemia in neoplastic disease in patients with colorectal cancer.

Evaluation of anti-arthritic activity of Spathodea Campanulata of root bark extract on freund’s adjuvant induced arthritis in rats models

Rheumatoid arthritis is a chronic systemic inflammation of the synovial joint and progressive destruction of cartilage and bone that may affect many tissues and organs-skin, blood vessels, heart, lungs and muscles but principally attacks the joints, producing a non-suppurative proliferative andinflammatory synovitis that often progresses to destruction of the articular cartilage and ankylosis of the joints. Angiogenesis and microvascular lesions are common features of RA inflammation, which leads to abnormal serum protein infiltration into the synovium. The objective of the study was to determine the preliminary phytochemical constituents, to evaluate acute toxicity studies, In-vitroanti-oxidant studies, In vitroand In-vivoanti-arthritic activity of theroot bark of Spathodea campanulata.. Paw edema was induced in rats by intra plantar injection of 0.1ml of Complete Freund’s Adjuvant (CFA) in left hind paw. The ethanolic extract of Spathodea campanulata (150mg/Kg & 300mg/Kg) and Diclofenac Sodium were orally administered for 28 consecutive days.Percentage inhibition was determined by Protein denaturation method and Membrane Stabilizing Activity Hematological, Histopathology, Radiological Analysis of CFA-induced arthritis in rat was performed. Statisticalsignificant was analyzed by one-way ANOVA followed by Tukey test. Our study concluded that ethanolic extract at the dose of 300 mg/kg showed significant anti-arthritic activity when compared to Diclofenac sodium

Оптимізація діагностики вторинних метаболічних порушень та лікувальної тактики у пацієнтів із анемією злоякісного новоутворення при колоректальному раку

The purpose of the study was to study the content of free fraction of heparin, histamine and serotonin in plasma of peripheral venous blood of patients with malignant neoplasm anemia in colorectal cancer, depending on the severity of anemia. Materials and methods. The material for the study was the blood plasma of 445 patients (228 men and 217 women). Among them, 53 patients (31 women and 22 men) with iron deficiency anemia were examined and included in the first observation group (І) and 392 patients (206 men (52.55 %) and 186 women (47.45 %)) with colorectal cancer whose course of the underlying disease was burdened with malignant neoplasm anemia (ICD-10 code: D63.0) were included in the second observation group (II). Among the patients in the second (II) observation group, there were 222 individuals (119 men and 103 women) with malignant neoplasms of the colon (ICD-10 code: С.18), 29 individuals (16 men and 13 women) with malignant neoplasms of the rectosigmoid junction (ICD-10 code: C.19), 138 individuals (82 men and 56 women) with malignant neoplasms of the rectum (code ICD-10 C.20) and 3 patients (2 men and 1 woman) with malignant neoplasms of the anus (ICD-10 code: C.21). The mean age of the patients was 63.3 ± 1.2 years old. The plasma level of free fraction of heparin of the examined patients was determined using the photocolorimetric method on photoelectric colorimeter 56-M after its preliminary isolation by electrophoretic method according to the appropriate procedure (B. V. Mykhailychenko, S. V. Vydyborets (2000)). The plasma level of free histamine and serotonin of the examined patients was studied using the method of fluorometric analysis on the analyzer “BIAN-130”-“BIAN-100” according to the procedure of B. V. Mykhailychenko, S. V. Vydyborets (1999). Results and discussion. It was found that prior to the initiation of treatment in patients with malignant neoplasm anemia, regardless of the course of colorectal cancer, there was a significant increase in the plasma level of free fraction of heparin, histamine, serotonin (p < 0.001); the ratio of free histamine to free serotonin was also changed in comparison with the values in the control group (p < 0.05), which indicated both an increased release of heparin, histamine and serotonin from the depot, and an impaired inactivation processes of these biologically active substances. Considering all of the above and the quite obvious reasons, namely, the secondary metabolic disorders of serotonin, histamine, heparin which manifested by a significant increase in their plasma level of patients with malignant neoplasm anemia in colorectal cancer, we suggested the need to use a medicinal product in a complex of therapeutic measures which can cause antihypoxic, membrane stabilizing and anti-edema action. Conclusion. Malignant neoplasm anemia in colorectal cancer is accompanied by significant changes in the metabolism of biologically active substances – free fraction of heparin, histamine, serotonin, and the ratio of free histamine to serotonin. It was correctly concluded that in addition to the baseline therapy the administration of arginine glutamate which causes both antihypoxic and membrane-stabilizing action, reliably contributes to the normalization of secondary metabolic disorders of histamine, serotonin and heparin metabolism in malignant neoplasm anemia in patients with colorectal cancer

Особенности ведения больных негоспитальной пневмонией с сопутствующей патологией: обоснование целесообразности использования антигипоксантов на примере этилметилгидроксипиридина сукцината

Внебольничная пневмония относится к наиболее распространенным инфекционным заболеваниям ХХI века и остается важной медико-социальной проблемой из-за достаточно высоких показателей инвалидизации и смертности, а также значительных экономических потерь. Сопутствующие хронические заболевания и состояния, количество которых увеличивается с возрастом, способствуют усилению тяжести и неблагоприятному прогнозу пневмонии. Сочетание патологий, патогенез которых включает гипоксический компонент, у одного больного определяет исключительную важность и необходимость понимания механизмов гипоксии (в том числе на клеточном уровне), а также социальную значимость проблемы защиты организма от кислородной недостаточности и сопутствующего энергодефицита, в том числе с помощью антигипоксантов с антиоксидантным и мембраностабилизирующим действием. В многочисленных экспериментальных и клинических исследованиях получены данные о плейотропных эффектах сукцината и сукцинатсодержащих антигипоксантов у больных с заболеваниями и состояниями, которые сопровождаются гипоксическими расстройствами. Создана достаточная доказательная база клинических исследований, в которых установлена целесообразность использования этилметилгидроксипиридина сукцината в составе комплексной терапии у больных с острыми и хроническими нарушениями мозгового кровообращения, тревожными расстройствами, у пациентов со стабильной стенокардией, острым коронарным синдромом, сердечной недостаточностью, артериальной гипертензией. Раннее добавление препарата в состав комбинированной терапии на догоспитальном этапе лечения пневмонии будет способствовать уменьшению возникновения острых осложнений или декомпенсации течения сопутствующих хронических состояний, ускорению регресса проявлений постинфекционной астении, вегетативной лабильности, когнитивного дефицита.

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.

Modern Medicines (Assortment) and Trends in the Improvement of Dosage Forms of Hepatoprotective Agents (Review)

Introduction. Liver diseases with all the variety of clinical manifestations have common pathogenetic links at the cellular level. The group of hepatoprotective agents is represented by drugs that exhibit versatile mechanisms for protecting liver cells from the effects of damaging factors, the main of which are membrane-stabilizing, antioxidant, regenerative, detoxifying, choleretic and anti-inflammatory effects. The high therapeutic and hepatoprotective effectiveness of modern drugs is largely due to their metabolic effects, as well as their ability to bind free radicals and reactive oxygen species in the cell.Text. The purpose of this work is to form an analytical review of the literature on the assortment and concepts of improving the dosage forms of hepatoprotective agents. According to the analysis and systematization of modern publications devoted to the use of hepatoprotectors in the treatment of liver diseases, it is shown that it is necessary to develop new formulations and combinations of biologically active substances with the manifestation of versatile mechanisms of hepatoprotection, as well as to improve the composition and manufacturing technologies of existing traditional therapies. One of the current trends is the use of new substances in the development of traditional and innovative dosage forms. The search for biologically active molecules with antioxidant, antiradical and membrane-stabilizing activity that can be considered as effective hepatoprotectors continues. An integral task of pharmaceutical development is the creation of bioavailable drugs that have a prolonged effect and minimal side effects. A promising direction in pharmaceutical technology is the development of innovative drugs for the directed transport of biologically active molecules to the affected organ.Conclusion. As a result of the analysis of modern data, priority directions for the development and improvement of existing formulations based on modern approaches to the production of innovative dosage forms are identified. The relevance of improving the dosage forms of hepatoprotectors presented on the pharmaceutical market is shown. Of particular interest is the development of innovative targeted delivery systems with effective and safe hepatoprotectors in various combinations, including those based on cinnamic acid derivatives.

Systematic Analysis of Combined Antioxidant and Membrane-Stabilizing Properties of Several Lamiaceae Family Kazakhstani Plants for Potential Production of Tea Beverages.

One of the most important compounds that exhibit a wide range of biological activities with especially strong antioxidant action are plant polyphenols. In the course of the experiment, the dose-dependent effects of polyphenols-rich extracts isolated from the Lamiaceae family Kazakhstani plants were studied on the processes of lipid peroxidation and on the degree of erythrocytes hemolysis. The activity of aqueous-ethanolic extracts from dried parts of plants, such as Origanum vulgare, Ziziphora bungeana, Dracocephalum integrifolium, Mentha piperita, Leonurus turkestanicus, Thymus serpyllum, and Salvia officinalis, was studied in a Wistar rat model. Lipid peroxidation (LPO) in liver microsomes was assessed by measuring malondialdehyde content in the form of thiobarbituric acid-reacting substances (TBARS). Estimation of osmotic resistance of isolated erythrocytes was evaluated based on hemoglobin absorbance. The amount of total phenolics in the extracts was measured using the Folin-Ciocalteu reagent method. Based on the results, Thymus serpyllum extract exhibited a significantly higher antioxidant activity (IC50 = 3.3 ± 0.7) compared to other plant extracts. Accordingly, among the extracts studied, those from Salvia officinalis, Thymus serpyllum, and Origanum vulgare show the most pronounced membrane-stabilizing activity. Antioxidant and antihemolytic properties of green tea and Origanum vulgare extract mixtures were similar to that of each individual plant extract. Similar results were obtained when the green tea extract was mixed with Mentha piperita, Ziziphora bungeana, and Dracocephalum integrifolium extracts, indicating no discernible synergistic interaction.

Betaxolol: A comprehensive profile.

Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing (local anesthetic) activity. Betaxolol selectively and competitively binds to and blocks beta-1 (β1) adrenergic receptors in the heart, thereby decreasing cardiac contractility and rate. This leads to a reduction in cardiac output and lowers blood pressure. When applied topically in the eye, this agent reduces aqueous humor secretion and lowers the intraocular pressure (IOP). In addition, betaxolol prevents the release of renin, a hormone secreted by the kidneys that causes constriction of blood vessels. Betaxolol (S)-(-)-enantiomer shows higher pharmacological activity. This chapter provides a complete review of nomenclature, physiochemical properties, methods of preparation, identification techniques and various qualitative and quantitative analytical techniques as well as pharmacology of betaxolol. In addition, the chapter also includes review of several methods for enantiomeric separation betaxolol using chromatographic techniques.