scholarly journals An Experimental Study of the Cryopreserved Placenta Extract Effect On the Sodium Diclofenac Anti-Inflammatory Activity

2021 ◽  
Vol 5 (3) ◽  
pp. 144-152
Author(s):  
Fedir Hladkykh

Background. As a means of correcting the ulcerogenic effect of nonsteroidal anti-inflammatory drugs, our attention was attracted by a cryopreserved extract of the human placenta, which has a multivector spectrum of biological activity. To date, there is no information about its effect on the specific activity of this class of medicines (anti-inflammatory, analgesic, etc.) in published sources. Objective. We are aimed to characterize the effect of cryopreserved placenta extract on the anti-inflammatory activity of diclofenac sodium when administered separately in a model of acute exudative inflammation. Methods. Experimental studies in vivo were conducted on 28 nonlinear male laboratory rats. The model of acute exudative inflammation was reproduced by subplantar injection of 0.1 ml of 1.0% aqueous solution of λ-karagenin into the right hind limb of rats. Cryopreserved placenta extract was administered intramuscularly at a dose of 0.16 ml/kg 60 minutes before diclofenac sodium (8 mg/kg). Results. Preventive administration of diclofenac sodium caused an antiexudative effect as early as 30 minutes after administration of λ-karagenin – its anti-inflammatory activity was 11.0%, which is 4.6 times higher than similar indicators at the same time in rats injected with placental cryoextract. At 60 minutes of observation, diclofenac sodium was comparable in anti-inflammatory activity with cryopreserved placenta extract: 28.6% and 22.2%, respectively, but at 120 and 180 minutes, diclofenac sodium exceeded the studied cryoextract in antiphlogistic effect by 1.6 times in both periods of observation. The anti-inflammatory effect of the combined separate administration of placenta cryoextract and diclofenac sodium before λ-karagenin for 30 and 60 minutes was 12.7% and 32.3%, respectively, which is comparable with analogous indicators against the background of diclofenac sodium monotherapy. However, at 120 minutes of observation, the group of combined use of placenta cryoextract and diclofenac sodium showed the greatest anti-inflammatory effect among rats of all the studied groups – 52.6%, which was 2.2 times higher than the indicators of the placenta cryoextract monotherapy group and 1.4 times lower than the indicators of the rats of the diclofenac sodium monotherapy group. Conclusions. 4 hours after administration, placental cryoextract had a suppressive effect on kinins like diclofenac sodium, and in the prostaglandin period of caragenin-induced inflammation against the background of combined use of the studied cryoextract and diclofenac sodium, the anti-inflammatory activity was 46.4 %. This suggests a suppressive effect on the production of prostaglandins as a possible mechanism of anti-exudative action of cryopreserved placenta extract.

Author(s):  
Thriveni Vasanth Kumar ◽  
Manjunatha H. ◽  
Rajesh Kp

Objective: Dietary curcumin and capsaicin are well known for their health beneficial potencies. The current study was done to assess the anti-inflammatory activity of curcumin, capsaicin and their combination by employing in vitro and in vivo models.Methods: We investigated the protective effect of curcumin, capsaicin and their combination using in vitro heat induced human red blood cell (HRBC) membrane stabilisation, in vivo 3% agar induced leukocyte mobilisation and acetic acid induced vascular permeability assay.Results: Curcumin, capsaicin and their combination exhibited concentration dependent protective effect against heat-induced HRBC membrane destabilisation, while combined curcumin and capsaicin restored 87.0±0.64 % membrane stability and it is found to be better than curcumin, capsaicin and diclofenac sodium (75.0±0.25. 72±0.9 and 80.0±0.31 %) protective effect. In agar suspension induced leukocyte mobilization assay, the combined curcumin and capsaicin had shown 39.5±1.58 % of inhibition compared to individual curcumin and capsaicin, which showed moderate inhibition of 16.0±3.14 and 21.6±2.17 % respectively. Besides, the combined curcumin and capsaicin had shown highly significant inhibition of acetic acid-induced vascular permeability in rats (62.0±3.14 %), whereas individual curcumin and capsaicin showed moderate inhibition of vascular permeability with 36.0±2.41 and 43.0±1.92 % respectively.Conclusion: This study demonstrates the significant anti-inflammatory property of combined curcumin and capsaicin at half of the individual concentration of curcumin and capsaicin.


2021 ◽  
Author(s):  
Reinier Gesto-Borroto ◽  
Gabriela Meneses ◽  
Alejandro Espinosa-Cerón ◽  
Guillermo Granados ◽  
Jacquelynne Cervantes-Torres ◽  
...  

Abstract The genus Galphimia is widely distributed in Mexico, and is represented by 22 species, including medicinal species. The sedative and anti-inflammatory effects of galphimines produced by the species Galphimia glauca have been documented. Formerly, molecular studies using DNA barcodes demonstrated that nine populations botanically classified as Galphimia glauca belong to four different species of the genus Galphimia, and that only one exhibited the sedative properties; however, all the collected species showed anti-inflammatory activity. Other bioactive compounds like quercetin, galphins, galphimidins and glaucacetalins have been identified from methanolic extracts of plants botanically classified as Galphimia glauca. The aim of this work was to determine the anti-inflammatory activity of methanolic extracts of nine collected Galphimia spp. populations grown in Mexico. The possible modes of action were analyzed by evaluating the inhibition of LPS-induced inflammation processes both in vitro and in vivo. The nine populations were evaluated by an in vitro model using RAW 264.7 murine macrophage cells, and two populations (a galphimine-producing and a non-galphimine-producing population) were selected for the in vivo experiments of systemic inflammation and neuroinflammation in mice. Results suggest that an anti-inflammatory in vitro effect was present in all the studied populations, evidenced by the inhibition of nitrite production. An inhibitory systemic inflammation in mice was exerted by the two analyzed populations. In the neuroinflammation model, the anti-inflammatory effect was demonstrated in methanolic extract of the non-galphimine-producing population. For the populations of Galphimia spp. studied herein, the anti-inflammatory effect could not be correlated to the presence of galphimines.


2021 ◽  
Vol 16 (10) ◽  
pp. 1934578X2110559
Author(s):  
Le Minh Ha ◽  
Ngo Thi Phuong ◽  
Nguyen Thi Thu Hien ◽  
Pham Thi Tam ◽  
Do Thi Thao ◽  
...  

In this study, we aimed at evaluating in vitro and in vivo anti-inflammatory activity of various extracts of the rhizomes of Globba pendula Roxb. Three extracts ( n-hexane, ethyl acetate, and water) were screened for their inhibitory effect on NO production by lipopolysaccharide-stimulated RAW 264.7 macrophages. The ethyl acetate extract of G. pendula rhizomes (EGP) showed a potential effect with an IC50 value of 32.45 µg/mL. For in vivo study, the ethyl acetate extract was further investigated for its anti-inflammatory effect using collagen antibody-induced arthritic mice (CAIA). The level of arthritis in experimental mice significantly reduced ( P < .05) after treatment with EGP at a dose of 500 mg/kg body weight (b.w.). This study also revealed that EGP is orally non-toxic. Ethyl p-methoxy cinamate was identified as the main constituent of EGP, which may result in its anti-inflammatory effect.


Author(s):  
Mansi L. Patil ◽  
Swati S. Gaikwad ◽  
Naresh J. Gaikwad

Introduction: Pain is an immunological response to any infection or inflammation and long term use of pain management therapy includes use of Nonsteroidal anti-inflammatory drugs which is associated with occurrence of toxicity as well as gastrointestinal bleeding. Therefore, the investigation of new analgesic and anti-inflammatory agents remains a major challenge. Aims: The objective of this research study is to undergo the pharmacological evaluation of newly synthesized benzoxazole derivatives. These novel derivatives were evaluated for anti-nociceptive, anti-inflammatory and cytotoxic activity using various in-vivo and ex-vivo methods. Methods: The study was carried out using swiss mice (adult male) weighing between 20gm to 30gm and were divided into groups containing (n=6) six animals in each group for treatment. The anti-nociceptive activity was performed by using 0.1ml of 0.6% v/v acetic acid as nociception inducer and evaluated by the diminished number of abdominal writhes. The anti-inflammatory activity was done using 0.1 ml of 2% w/v Carrageenan induced paw edema method was observed which was evaluated by calculating the percent maximum possible effect. Histopathological evaluation and cytotoxic activity of the compounds was carried out. Results: The results of this research study revealed that synthesized derivatives (a, b, c, d and e) showed promising anti-nociceptive and anti-inflammatory effect along significantly higher cytotoxic activity in MCF-7 cell lines. Conclusion: It can be concluded that synthesized derivatives (a, b, c, d and e) have potential anti-nociceptive and anti-inflammatory effect along with cytotoxic activity and certain modification in structure may result in potent activity.


2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Elisa Colombo ◽  
Enrico Sangiovanni ◽  
Mario Dell'Agli

Several biological activities of pomegranate have been widely described in the literature, but the anti-inflammatory effect in the gastrointestinal tract has not been reviewed till now. The aim of the present paper is to summarize the evidence for or against the efficacy of pomegranate for coping with inflammatory conditions of the gastro-intestinal tract. The paper has been organized in three parts: (1) the first one is devoted to the modifications of pomegranate active compounds in the gastro-intestinal tract; (2) the second one considering the literature regarding the anti-inflammatory effect of pomegranate at gastric level; (3) the third part considers the anti-inflammatory effect of pomegranate in the gut.In vivostudies performed on the whole fruit or juice, peel, and flowers demonstrate antiulcer effect in a variety of animal models. Ellagic acid was the main responsible for this effect, although other individual ellagitannins could contribute to the biological activity of the mixture. Different preparations of pomegranate, including extracts from peels, flowers, seeds, and juice, show a significant anti-inflammatory activity in the gut. No clinical studies have been found, thus suggesting that future clinical studies are necessary to clarify the beneficial effects of pomegranate in the gastrointestinal tract.


2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Sameh Ben Khedir ◽  
Masarra Mzid ◽  
Sana Bardaa ◽  
Dorsaf Moalla ◽  
Zouheir Sahnoun ◽  
...  

In order to find new topical anti-inflammatory agents, we had recourse to a medicinal plant. This work was designed to determine the topical anti-inflammatory effect ofPistacia lentiscusfruit oil (PLFO), using carrageenan-induced paw edema rat model, and to evaluate its effects on oxidative stress. The topical anti-inflammatory activity of PLFO was compared to Inflocine® and estimated by measuring the diameter of paw edema, for 5 hours at a 1-hour interval. After that the rats were scarified and the inflamed paw tissue was removed for the exploration of some parameters of oxidative stress and histopathology. PLFO showed a significant anti-inflammatory activity in comparison with the Inflocine. The percentages of edema inhibition were 70% and % 51.5% (p<0.01), respectively, after five hours. The treatment with PLFO and Inflocine led to significant increases (p≤0.05) in the activities of CAT, SOD, and GPX and significant decreases in the MDA level and AOPP activity in the paw tissue after Carr injection, in comparison with the Carr group. Therefore, our findings demonstrate that PLFO might accelerate the development of new drugs which could be used scientifically as a source for natural health products in the treatment of topical inflammation.


Author(s):  
E.N. Kurmanova ◽  
E.V. Ferubko ◽  
L.B. Strelkova ◽  
R.K. Kurmanov ◽  
O.P. Sheichenko

Змееголовник молдавский (Dracocephalum moldavica L.) в народной медицине используется в качестве противовоспалительного, ранозаживляющего, отхаркивающего и седативного средства. В ФГБНУ ВИЛАР разработан змееголовника молдавского травы экстракт сухой под условным названием «Люкатил» (сумма фенольных соединений 64,12% в пересчёте на цинарозид). Цель работы - изучение острой токсичности и противовоспалительной активности экстракта змееголовника для разработки на его основе лекарственного препарата. Методика. Проведено определение параметров острой токсичности и противовоспалительной активности экстракта. При изучении острой токсичности экстракта по методу Кербера использованы белые нелинейные мыши-самцы в количестве 30 особей. «Люкатил» вводили животным внутрижелудочно в дозах 500, 1000, 1500 и 2000 мг/кг. Для выявления противовоспалительной активности экстракта змееголовника молдавского использована in vitro ферментная биотест-система на основе индуцибельной NO-синтазы. Для выявления противовоспалительной активности экстракта in vivo использованы нелинейные мыши-самцы. Оценку влияния экстракта в дозе 200 мг/кг на экссудативную стадию воспаления проводили на модели 1% формалинового отёка. В качества препарата сравнения использовали индометацин (5 мг/кг). Формалиновый отёк вызывали однократным субплантарным введением под апоневроз задней правой лапки мыши 0,05 мл 1% формалина в качестве флогогенного агента. Величину отёка определяли по разнице в массе лапок контрольных и опытных животных и рассчитывали процент снижения степени отёка. Результаты. При однократном введении экстракт «Люкатил» не приводил к гибели животных, изменения внешнего вида и поведенческих реакций мышей не наблюдалось. В соответствии с классификацией токсичности химических веществ по ГОСТ 12.1.007-76 «Люкатил» является малотоксичным веществом. In vitro установлена высокая противовоспалительная активность экстракта, при этом остаточная активность iNOS снижалась до 25%. Экстракт в дозе 200 мг/кг in vivo обладал статистически значимым противовоспалительным эффектом. Он подавлял развитие экссудативной фазы воспаления на 33,7%, по сравнению с контрольной группой животных, уступая противовоспалительному эффекту индометацина. Заключение. Змееголовника молдавского травы экстракт сухой под условным названием «Люкатил» является малотоксичным веществом, обладает выраженным противовоспалительным эффектом в опытах in vitro, in vivo и является перспективным объектом для дальнейшего фармакологического изучения в качестве противовоспалительного лекарственного средства.Moldavian dragonhead (Dracocephalum moldavica L.) is used in traditional medicine as an anti-inflammatory, wound-healing, expectorant, and sedative means. In our Institute, a Moldavian dragonhead herb dry extract (total phenolic content, 64.12% in cynaroside equivalent) was developed and conventionally named Lyukatil. Objective. To study acute toxicity and anti-inflammatory activity of the dragonhead extract for developing a drug based on this extract. Method. Parameters of acute toxicity and anti-inflammatory activity of the extract were assessed. The study of acute toxicity of the extract was performed using the Kerber method on male white mongrel mice (n=30). Lyukatil was administered to the animals intragastrically at doses of 500 mg/kg, 1000 mg/kg, 1500 mg/kg, and 2000 mg/kg. Anti-inflammatory activity of the Moldavian dragonhead extract was determined in vitro using an enzyme Biotest system based on inducible NO synthase. Mongrel male mice were used to study the anti-inflammatory activity of the extract in vivo. The effect of the extract at a dose of 200 mg/kg on the exudative phase of inflammation was evaluated on a model of 1% formalin-induced edema. Indomethacin 5 mg/kg was used as a reference drug. Formalin edema was induced by a single subplantar injection of 0.05 ml of 1% formalin as a phlogogenic agent under the aponeurosis of the right hind leg. The degree of edema was determined by the difference in leg weights in control and experimental animals; then the decrease in edema was calculated in per cent. Results. A single administration of the extract Lyukatil did not cause death of animals, changes in the appearance or in behavioral responses, shortness of breath, or drowsiness. In accordance with the toxicity classification for chemical substances as per GOST Standard 12.1.007-76, Lyukatil is a low-toxic substance. The extract at a dose of 200 mg/kg exerted a significant anti-inflammatory effect as shown by suppression of the exudative phase of formalin-induced inflammation by 33.7% compared to the control group. However, this effect was inferior to the anti-inflammatory effect of indomethacin. Conclusions. The Moldavian dragonhead herb dry extract under the conventional name of Lyukatil is a low-toxic substance that has a significant anti-inflammatory effect both in vitro and in vivo and is a promising target for further pharmacological studies as an anti-inflammatory drug.


Author(s):  
GARIGE BABA SHANKAR RAO ◽  
SRISAILAM K ◽  
V UMA MAHESHWARA RAO ◽  
VASUDHA B

Objective: This current investigation assesses in vivo central and peripheral analgesic effects and anti-inflammatory properties of fractions obtained from Galphimia glauca (GG) stem methanol extract. Methods: The laboratory models such as Swiss albino mice and Wistar albino rats were employed in the studies. The GG stem methanol extract was subjected to fractionation with solvents such as hexane, chloroform, ethyl acetate, and methanol. Orally, the dose range of 100, 200, and 400 mg/kg was given for 1 day for evaluating analgesic (hotplate test, tail clip test, writhing test, and formalin test) and weekdays for assessing anti-inflammatory activity (carrageenan and cotton pellet test methods), respectively. The experimental studies were further conducted for determining the involvement of central and peripheral receptor actions in the analgesic activity of the extract by prechallenging it with naloxone and acetic acid, respectively. The in vivo anti-inflammatory studies were conducted using carrageenan-induced rat paw edema model and cotton pellet granuloma test. Results: The LD50 of the extract was found to be >2000 mg/kg b.w. The methanol fraction of 400 mg/kg dose exhibited significant (p≤0.001) and dose-dependent analgesic and anti-inflammatory activity. It also exhibited central and peripheral analgesic actions when treated with naloxone and acetic acid, respectively. Conclusion: The results revealed that the stem methanol fraction has more potential in terms of analgesic and anti-inflammatory properties.


Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 741 ◽  
Author(s):  
Jiwon Jang ◽  
Jong Sub Lee ◽  
Young-Jin Jang ◽  
Eui Su Choung ◽  
Wan Yi Li ◽  
...  

Inflammation is a fundamental process for defending against foreign antigens that involves various transcriptional regulatory processes as well as molecular signaling pathways. Despite its protective roles in the human body, the activation of inflammation may also convey various diseases including autoimmune disease and cancer. Sorbaria kirilowii is a plant originating from Asia, with no anti-inflammatory activity reported. In this paper, we discovered an anti-inflammatory effect of S. kirilowii ethanol extract (Sk-EE) both in vivo and in vitro. In vitro effects of Sk-EE were determined with lipopolysaccharide (LPS)-stimulated RAW264.7 cells, while ex vivo analysis was performed using peritoneal macrophages of thioglycollate (TG)-induced mice. Sk-EE significantly reduced the nitric oxide (NO) production of induced macrophages and inhibited the expression of inflammation-related cytokines and the activation of transcription factors. Moreover, treatment with Sk-EE also decreased the activation of proteins involved in nuclear factor (NF)-κB signaling cascade; among them, Src was a prime target of Sk-EE. For in vivo assessment of the anti-inflammatory effect of Sk-EE, HCl/EtOH was given by the oral route to mice for gastritis induction. Sk-EE injection dose-dependently reduced the inflammatory lesion area of the stomach in gastritis-induced mice. Taking these results together, Sk-EE exerts its anti-inflammatory activity by regulating intracellular NF-κB signaling pathways and also shows an authentic effect on reducing gastric inflammation.


2020 ◽  
Vol 16 (5) ◽  
pp. 593-605
Author(s):  
André F. Vilvert ◽  
Marcus Vinícius P.S. Nascimento ◽  
Rosivaldo dos S. Borges ◽  
Eduardo M. Dalmarco

Background: Paracetamol (p-aminophenol) and salicylates are nonsteroidal antiinflammatory drugs that are widely used in the general population. The adverse effects of both drugs continue to be a focus of the pharmaceutical industry in the development of new molecules that will increase treatment safety. In this context, we tested nine compounds derived from paracetamol and salicylates, synthesized in our laboratory, for their safety and ex vivo and in vivo anti-inflammatory activity. Methods: We analyzed the cytotoxicity of the compounds in ex vivo mice neutrophils, and their ability to inhibit the production of pro-inflammatory mediators (nitric oxide and interleukin-6) after stimulating with LPS. Next, in the selected molecules, we evaluated the anti-inflammatory effect on an in vivo inflammatory model of acute lung injury in mice. All nine compounds were also submitted to the cytotoxicity assay, like the original compounds. Results: None of the compounds showed cytotoxicity under the cells used. However, of the initial compounds, only five demonstrated anti-inflammatory effect, inhibiting Nitric Oxide (NO) and interleukin 6 (IL-6) production by neutrophils stimulated with Lipopolysaccharide (LPS). After this initial trial, four modified compounds were able to reduce leukocyte migration and fluid leakage in the bronchoalveolar lavage of mice. However, only the compound 5a1, derived from the esterification of gentisic acid, was able to significantly inhibit the levels of all pro-inflammatory cytokines and increase the levels of antiinflammatory cytokines evaluated. Conclusion: In conclusion, all compounds showed a good safety profile, and many of them had an antiinflammatory effect. However, the compound derived from gentisic acid is highlighted for its significant effects ex vivo and in vivo and in this context, we believe that this compound is a potential candidate for the development of a new anti-inflammatory drug.


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