scholarly journals ВИВЧЕННЯ ПРОТИЗАПАЛЬНОЇ АКТИВНОСТІ ОПРАЦЬОВАНОГО КРЕМУ БЕТАКАРБОКЛОМЕТ

Author(s):  
Арам Дуллах ◽  
І. О. Власенко ◽  
Г. М. Войтенко ◽  
Л. Л. Давтян

<p><strong>STUDY OF ANTIINFLAMMATORY ACTIVITY OF FORMULTATED CREAM BETAKARBOKLOMET</strong></p><p><strong>Aram Dullah, </strong><strong>I</strong><strong>.</strong><strong>O</strong><strong>.Vlasenko, </strong><strong>G</strong><strong>.</strong><strong>M</strong><strong>. </strong><strong>Voytenko</strong><strong>,</strong> <strong>L.L. Davtyan </strong></p><p><em>Shupik</em><em> </em><em>National</em><em> </em><em>medical</em><em> </em><em>academy</em><em> </em><em>of</em><em> </em><em>postgraduate education </em><strong></strong></p><p><strong>Summary:</strong> The article presents the results of a study of antiexudative activity of complexed antifungal cream, based on clotrimazole, betamethasone dipropionate, metronidazole and urea, for treatment of dermatomycosis.  By in vivo method (model of acute aseptic (dextran) inflammation) it was found that the formulated cream has antiinflammatory activity typical for glucocorticoids, dynamics and the value of which correspond to the activity of referent-medicine.</p><p><strong>Keywords: </strong>dermatomycosis, betamethasone diptopionate, antiexudative activity.</p><pre><strong>Introduction.</strong> Last years are characterized by marked increase in the incidence of fungal diseases, foot fungal infections take one of the highest incidence of skin diseases. They are often characterized by thickening of the stratum corneum layer of the foot’s skin, cracks and inflammation, causing pain and itching. The long term of mycological process leads to profound disorders of the body, complicating other diseases and reduces the quality of life.</pre><pre>When dermatomycosis is accompanied by inflammatory reaction of the skin combined using of antifungal agents and corticosteroids of local action is recommended. </pre><pre>Based on pharmaco- technological, physical, chemical and biological research mild drug (MDL) for complex treatment of dermatomycoses based on clotrimazole, metronidazole, urea and betamethasone dipropionate named Betakarboklomet was developed. </pre><pre>The purpose of the study was to investigate the anti-inflammatory activity of developed MDL .</pre><pre><strong>Methods</strong><strong>.</strong> The study of  MDL’s antiexudative activity conducted on a model of acute aseptic ( dextrane) inflammation by oncometric method was conducted. Exudative inflammation was assessed by measuring the volume of paw dynamics.</pre><p><strong>Results</strong><strong> </strong><strong>and</strong><strong> </strong><strong>discussion</strong>.</p><pre>The maximum increase in the volume of inflamed foot was observed within 1 hour after introduction of dextran, averaging 0.78 ml. In the next 5 hours foot swelling gradually decreased, but the output volume is not returned.</pre><pre>The study found that processed cream has expressed antiexudative activity, which is not significantly different from the reference product. Increase the volume of the paw of animals applied by drug Betakarboklomet was at the peak of edema (1 hour) 0,52 ± 0,02 ml , 3 h paw’s growth of volume of the original volume was 0,36 ± 0,02 ml, 5 hours - 0,20 ± 0,01 ml. The average value of MDL action for 5 hours was about 50.98 %, and for the reference product - 47.47 %.</pre><pre>Ability of developed cream Betakarboklomet to inhibit inflammation in the early stages manifested by betamethasone dipropionate, which, according to the literature, is able to reduce the synthesis of prostaglandins , prostacyclin, and others. Thus, our study of impact of developed cream Betakarboklomet on inflammation, suggests that MDL has a strong anti-inflammatory effect ( inhibits the development of serotonin edema).</pre><pre><strong>Conclusions</strong><strong>.</strong> Based on pharmacological studies of experimental inflammation induced by dextran, developed drug Betakarboklomet shows anti-inflammatory effect at the prototype.</pre>

2021 ◽  
Author(s):  
Sorina Danescu ◽  
Gabriela Adriana Filip ◽  
Remus Moldovan ◽  
Diana Olteanu ◽  
Andras Nagy ◽  
...  

Abstract Fungal infections are a growing global health problem. Therefore, our group has designed and characterized a novel cocrystal formulation starting from ketoconazole and para-amino benzoic acid, named KET-PABA aiming to improve the bioavailability, biocompatibility, and efficiency of the parent drug. The cocrystal showed improved physical properties, such as stability in suspension, solubility, as well as antimycotic efficiency as compared to ketoconazole. The current study investigated the local possible side effects induced on BALBc mice skin by the application of KET-PABA cocrystal. KET-PABA proved to be safe, without signs of skin sensitization as shown by the mouse ear sensitization test (MEST), or histopathology. KET-PABA induced a potent anti-inflammatory effect through the inhibition of proinflammatory cytokines such as IL1α, IL1β, IL6 and TNFα, and other inflammation promoters such as NRF2, compared to the vehicle. KET-PABA had no effect on the levels of the anti-inflammatory cytokine IL10, or proinflammatory enzyme COX2 and had minimal effects on the activation of the NFκB pathway. Overall, KET-PABA application induced no sensitization, moreover, it induced an anti-inflammatory response. Based on the improved antimycotic effect versus ketoconazole and the anti-inflammatory action, KET-PABA cocrystal has the potential to be an efficient drug in the treatment of cutaneous mycosis.


2021 ◽  
Vol 5 (1) ◽  
pp. 40
Author(s):  
Livia Kurniati Saputra ◽  
Dian Novita Chandra ◽  
Ninik Mudjihartini

Low grade inflammation has been recognized of being involved in the pathogenesis of chronic disease pandemic. Individual lifestyle plays a major role in the development of low grade inflammation. Sedentary workers are at risk of low grade inflammation due to the nature of their work. Dietary habit also contributes to inflammatory status in the body. Dietary fiber intake indirectly affects the immune system. It has been hypothesized that fiber has anti-inflammatory effects, both body weight-related and body weight-unrelated This review will focus more on body weight-unrelated anti-inflammatory effect of fiber, especially through fiber’s fermentation metabolites, the short chain fatty acid (SCFA). Its anti-inflammatory effect can be seen by monitoring a biomarker of inflammation in the body, the high sensitivity C-reactive protein (hsCRP). This review’s objective is to cover the mechanisms and role of dietary fiber intake on serum hsCRP level as a marker of low grade inflammation on sedentary workers. 


2018 ◽  
Vol 13 (5) ◽  
pp. 1934578X1801300
Author(s):  
You Chul Chung ◽  
Sung-Min Park ◽  
Jin Hwa Kim ◽  
Geun Soo Lee ◽  
Jung No Lee ◽  
...  

The Trifolium pratense L. (red clover), which blossoms, leaves and stems can be used as medicines for treatment of burns, skin diseases, diabetes and other diseases. Recently study shown that pratol (7-hydroxy-4-methoxyflavone), an O-methylated flavone in T. pratense has been evaluated to induce melanogenesis in B16F10 melanoma cells. However, the anti-inflammatory effect of pratol has not been reported. In this study, we investigated the effects of pratol on anti-inflammation. We also studied the mechanism of action of pratol in LPS-stimulated RAW 264.7 cells. The cells were treated with various concentration of pratol (25, 50, or 100 μM) and 25 μM ammonium pyrrolidinedithiocarbamate (APDC) was used as control. The results in LPS-stimulated RAW 264.7 cells showed that pratol significantly reduced nitric oxide (NO) and prostaglandin E2 (PGE2) production without any cytotoxic. In addition, pratol strongly decreased the expression of inducible nitric oxide synthase (iNOS) and cyclooygenase (COX-2). Furthermore, pratol reduced proinflammatory cytokines such as tumour necrosis factor (TNF)-α, interleukin (IL)-1β and IL-6. We also found that pratol strongly inhibited activation of nuclear factor kappa B (NF-κB) by reducing the p65 phosphorylation and protecting inhibitory factor kappa B alpha (IκBα) degradation. The results suggest that, pratol may be used to treat or prevent inflammatory diseases such as dermatitis, arthritis, cardiovascular and cancer.


2019 ◽  
pp. 82-87
Author(s):  
B. V. Pristupa ◽  
I. O. Shyshkin ◽  
Ya. V. Rozhkovsky ◽  
V. O. Gelmboldt

In the last decade, high cariesprophylactic efficacy of ammonium hexafluorosilicates, including salts with substituted biologically active ammonium cations, has been demonstrated. Among the promising anti-caries agents are recently synthesized 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates, for whose cations anti-inflammatory activity is expected. The aim of the work is to assess the presence of anti-inflammatory activity in the series of 2-, 3-, 4-carboxymethylpyridinium hexafluorosilicates in the experiment. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates (I–III, respectively) were synthesized according to the previously proposed technique, carrageenan is a commercial preparation, reference drug is a indomethacin. Experiments on the anti-inflammatory activity of hexafluorosilicates were performed on 77 white Wistar male rats weighing 174–190 g using the carrageenan model of inflammation. The inflammatory reaction was reproduced by subplantary administration of 0.1 ml of a 0.2% solution of carrageenan, the studied compounds were administered orally in doses 1/10, 1/20, 1/50 from LD50 for the compound III. It was established that after administration of carrageenan, animals of the control group showed marked paw edema, which gradually increased and was maximal after 24 hours of observation. According to the data obtained, the indices for compounds I-III practically do not differ from those of the control group. This indicates that, despite the results of the PASS forecast and the presence of acetic acid residue, an anti-inflammatory pharmacofor, in compounds I-III, the compounds under study do not have an anti-inflammatory effect in the carrageenan model. 2-, 3-, 4-Carboxymethylpyridinium hexafluorosilicates do not show the expected anti-inflammatory activity in the carrageenan model of inflammation.


Biomedika ◽  
2012 ◽  
Vol 4 (2) ◽  
Author(s):  
Tanti Azizah Sujono ◽  
Raudatul Patimah ◽  
Ratna Yuliani

In-flammation is the body’s reaction to foreign substances that enter the body with signs of redness, heat, swelling, pain, and impaired organ functions. Curcuma rhizome including medicinal plants that have properties relieve the pain and inflammation of the skin. The purpose of this research was to examine the anti-iflammation effect of Curcuma zedoaria (Berg) Roscoe Rhizome infusion on carrageenan induced paw edema in rats. This research used experimental method with completely randomized design. Twenty five healthy Wistar male rats, 2-3 months old and 150-250 g divided into five groups and each group consist of 5 rats. Rats in group I that served as negative control were given 2.5 mL/200gbw of aquadest. Rats in group II as positive control were given sodium diclofenac with dose of 6.75 mg/kgbw. Group III, IV, and V were given Curcuma zedoaria (Berg) Roscoe Rhizome infusion with dose of 0.625, 1.250 and 2.500 g/kgbw, respectively. Treatments were given per oral 1 hour before injection of 0.1 ml carrageenan 1% subplantar. Rat paw edema volume was measured before and after carrageenan injection. The measurement was done every 0.5 hour for 6 hours observation. Area Under the Curve (AUC) that is calculated from paw edema volume data, was use to calculate percentage of anti-inflammatory effect. Data were analyzed with one way Anova and Least Signifi cant Difference with confi dence level 95%. Infusion of Curcuma zedoaria Rhizome with doses of 0,625, 1,250, and 2,500 g/kgbw had anti-inflammatory effect in Wistar male rats which were induced by Carrageenan 1%. Percentage of anti-inflammation effect (44,16+5,11)%, (48,70+7,05)%, (59,09+9,61)% respectively and the effects were equivalent with positive control.Key words: Anti-inflammation, Curcuma zedoaria (Berg) Roscoe, infusion, Carrageenan.


2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Indah Puti Rahmayani Sabirin ◽  
Euis Reni Yuslianti

The inflammatory response is one of natural process in the body to protect itself following tissue injury, but it can cause discomfort. Noni (Morinda citrifolia L.) leaf known as a traditional medicament to help reduce the inflammatory effect. The leaves empirically applied as a wrapping on fever or wound. The purpose of this study was to identify the anti-inflammatory effect of topical noni leaf extract paste in 5% and 10% concentration by examination of Wistar rat paw edema induced by λ-carrageenan. Twenty-four Wistar rats divided into four groups, which were negative control, positive control with diclofenac sodium 1% gel, 5% noni leaf, and 10% noni leaf paste groups. Paw edema was induced by intraplantar injection of 1% λ-carrageenan to every rat. Every treatment subsequently applied in the plantar area before injection, and the changed paw volume measured with plethysmometer at minutes 0, 30, 60, and 90. This study was at the Animal Laboratory, Faculty of Medicine, Universitas Jenderal Achmad Yani, Cimahi city in October–December 2017. The result displayed that the minimum volume after 90 minutes was on 5% and 10% noni leaf paste group, which is 1.00 mL. Kruskal-Wallis test result of inflammatory percentage was significantly different among every group in each examination time (p<0.05). Post-hoc test showed that inflammatory reduction on paw edema with noni leaf paste application on both concentrations were significantly different compared to the negative control. However, it was not different from the positive control group. This study showed that application of noni leaf paste in 5% and 10% concentration could help reduce inflammatory response on skin possibly by the active anti-inflammatory ingredients of noni leaf. EFEK PASTA EKSTRAK DAUN MENGKUDU (MORINDA CITRIFOLIA L.) TOPIKAL TERHADAP EDEMA KAKI TIKUS GALUR WISTAR YANG DIINDUKSI KARAGENANInflamasi adalah proses alami tubuh untuk melindunginya setelah cedera, namun hal tersebut dapat menyebabkan ketidaknyamanan. Daun mengkudu (Morinda citrifolia L.) dikenal sebagai obat tradisional untuk menurunkan efek inflamasi yang secara empiris digunakan untuk mengobati demam dan luka. Tujuan penelitian ini adalah mengetahui efek anti-inflamasi pasta ekstrak daun mengkudu melalui pemeriksaan edema kaki tikus yang diinduksi karagenan-λ. Dua puluh empat tikus galur Wistar dibagi menjadi 4 kelompok, yaitu kontrol negatif dengan akuades, kontrol positif (aplikasi gel Na diklofenak 1%), serta perlakuan pasta daun mengkudu 5% dan 10%. Edema dibuat dengan menginjeksi intraplantar tikus dengan 1% karagenan-λ pada tiap kelompok. Tiap-tiap perlakuan diaplikasikan sebelum tikus diinjeksi dan perubahan volume kaki tikus diukur dengan pletismometer di menit ke-0, 30, 60, dan 90. Penelitian ini dilakukan di Laboratorium Hewan, Fakultas Kedokteran, Universitas Jenderal Achmad Yani, Kota Cimahi pada Oktober–Desember 2017. Hasil pengukuran memperlihatkan penurunan volume edema kaki terkecil setelah 90 menit pada kelompok pasta daun mengkudu 10%, yaitu 1,00 mL. Hasil Uji Kruskal-Wallis terhadap persentase inflamasi berbeda nyata pada tiap kelompok dan tiap waktu pengamatan (p<0,05). Hasil uji beda menunjukkan bahwa penurunan inflamasi kaki tikus pada perlakuan pasta daun mengkudu kedua konsentrasi berbeda nyata dibanding dengan kontrol negatif, tetapi tidak berbeda dengan kontrol positif. Penelitian ini menunjukkan bahwa pasta daun mengkudu 5% dan 10% dapat membantu menurunkan reaksi inflamasi kulit dan efeknya sejalan dengan Na diklofenak karena zat aktif yang bersifat anti-inflamasi dalam daun mengkudu.


Author(s):  
Olga Fedorovna Belaia ◽  
D. C. Gutkin ◽  
E. V. Volchkova ◽  
A. N. Sundukova ◽  
E. N. Kareva ◽  
...  

Local inflammation in H. pylori infection is characterized by infiltration of the gastric mucosa by neutrophils and specific lymphocytes, an increase in the production of immunoregulatory, pro- and anti-inflammatory cytokines. IL-4 is the most important regulatory cytokine that plays a role in a huge number of immune and non-immune functions. IL-8 is a potent angiogenic factor and chemoattractant, its presence in the circulation can have a systemic pro-inflammatory effect on the body. IL-4 and IL-8 in H. pylori infection has been studied insufficiently. The goal is to establish serum levels of IL-4 and IL-8 in patients with chronic gastritis and peptic ulcer and duodenal ulcer. Materials and methods. 95 patients of the gastroenterological department were examined, of them 37 men and 58 women (mean age 59 years): 53 patients diagnosed with chronic active gastritis (CAG, including erosive gastroduodenitis) and 42 patients diagnosed with peptic ulcer (PU). Patients were conditionally divided into 4 subgroups: PU (without confirming the presence in patients with Hp according to generally accepted methods), PU + Hp (patients with the presence of Hp), CAG and CAG + Hp. Results. An increase in serum IL-4 levels (above 10 pg / ml) was observed in only 50.7% of patients, with approximately the same frequency in patients with CAG and PU, and an increase in serum IL-8 levels (above 0.062 ng / ml) - in most patients (90%), and the highest levels of IL8 were detected in patients with PU + Hp. In the first analysis, 31% of patients had elevated levels of IL-8 in the absence of IL-4, while in the second analysis - already 62% of patients (p ≤ 0.01). This indicated a sharp twofold decrease in the production of IL-4 in just a few days between the two analyzes. Conclusion. Considering that an increase in serum levels of IL-8 is found in a larger number of patients than IL-4, which, moreover, ceases to be detected in serum, it can be assumed that the production and anti-inflammatory effect of IL-4 are insufficient in some patients with gastritis and peptic ulcer disease. Against this background, elevated levels of IL-8 can help maintain inflammation in a significant number of patients, as well as reduce the effectiveness of eradication therapy.


Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4294 ◽  
Author(s):  
Jianmei Zhang ◽  
Stephanie Triseptya Hunto ◽  
Yoonyong Yang ◽  
Jongsung Lee ◽  
Jae Youl Cho

Tabebuia impetiginosa, a plant native to the Amazon rainforest and other parts of Latin America, is traditionally used for treating fever, malaria, bacterial and fungal infections, and skin diseases. Additionally, several categories of phytochemicals and extracts isolated from T. impetiginosa have been studied via various models and displayed pharmacological activities. This review aims to uncover and summarize the research concerning T. impetiginosa, particularly its traditional uses, phytochemistry, and immunopharmacological activity, as well as to provide guidance for future research. A comprehensive search of the published literature was conducted to locate original publications pertaining to T. impetiginosa up to June 2020. The main inquiry used the following keywords in various combinations in titles and abstracts: T. impetiginosa, Taheebo, traditional uses, phytochemistry, immunopharmacological, anti-inflammatory activity. Immunopharmacological activity described in this paper includes its anti-inflammatory, anti-allergic, anti-autoimmune, and anti-cancer properties. Particularly, T. impetiginosa has a strong effect on anti-inflammatory activity. This paper also describes the target pathway underlying how T. impetiginosa inhibits the inflammatory response. The need for further investigation to identify other pharmacological activities as well as the exact target proteins of T. impetiginosa was also highlighted. T. impetiginosa may provide a new strategy for prevention and treatment of many immunological disorders that foster extensive research to identify potential anti-inflammatory and immunomodulatory compounds and fractions as well as to explore the underlying mechanisms of this herb. Further scientific evidence is required for clinical trials on its immunopharmacological effects and safety.


2020 ◽  
Vol 1 (2) ◽  
pp. 68-73
Author(s):  
Aufar Zimamuz Zaman Al Hajiri ◽  
Diaz Syafrie Abdillah ◽  
Mohammad Qoimam Bilqisthi Zulfikar

Osteoarthritis (OA) is the most common type of arthritis (inflammation of the joints). OA can affect all cartilage throughout the body, including the spine, but mainly attacks the legs from the pelvis, especially the knee to the ankle which affects about 10% of men and 18% of women over 60 years old. Pharmacotherapy, surgery, and complementary therapy are the currently managements of OA. Nigella sativa (NS) is one of the herbal plants which is part of the prophet's medicines in the Islamic world which still used. Thymoquinone (TQ) is one of NS compound, has an anti-inflammatory effect by inhibit the formation of eicosanoids in leukocytes and lipid peroxidation, or inhibit the expression of PF NF-κB subunits and p50 subunits with TNF-a promoters, and reduce levels of C-reactive protein (CRP). TQ also has a chondroprotective effects mechanism by decreases prostaglandin E2 (PGE) mediated by IL-1β and inhibits MMP synthesis in chondrocytes. Through its anti-inflammatory and chondroprotective effect, NS is a potential therapeutic agent which beneficial use for OA management without toxicological effects when given.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1454
Author(s):  
Kézia Cristine Barbosa Ferreira ◽  
Ana Beatriz Caribé dos Santos Valle ◽  
Camila Quinetti Paes ◽  
Guilherme Diniz Tavares ◽  
Frederico Pittella

The main function of the skin is to protect the body from the external environment. However, the skin can undergo inflammatory processes, due to genetic, hormonal, or environmental factors. When the defense system is overloaded, there is an increase in pro-inflammatory mediators and reactive oxygen species (ROS), which results in skin disorders. Among the substances used to treat these inflammatory processes, many natural substances with anti-inflammatory and antioxidant properties are being studied: nature is yet an abundant source to obtain diverse pharmacological actives. The treatment of skin diseases is usually focused on topical application, as it reduces the risk of systemic side effects and prevents drug degradation by first-pass metabolism. Thus, the properties of drug delivery vehicles can facilitate or inhibit its permeation. Due to the hydrophobic nature of the skin, a promising strategy to improve dermal drug penetration is the use of lipid-based nanoparticles, such as nanostructured lipid carriers (NLC). Therefore, in this review, we present NLC as a tool to improve dermal administration of natural substances with anti-inflammatory properties.


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