scholarly journals Topical Anti-Inflammatory and Analgesic Activities of Citrullus colocynthis Extract Cream in Rats

Medicina ◽  
2018 ◽  
Vol 54 (4) ◽  
pp. 51 ◽  
Author(s):  
Marzieh Pashmforosh ◽  
Hossein Rajabi Vardanjani ◽  
Hassan Rajabi Vardanjani ◽  
Mahdi Pashmforosh ◽  
Mohammad Khodayar

Background and objectives:Citrullus colocynthis (CC), known as bitter apple, is used to treat diabetes in Iranian traditional medicine. The aim of this study is to evaluate the anti-inflammatory and analgesic activities of CC cream in rats. Materials and Methods: The carrageenan-induced edema in a rat hind paw was carried out to evaluate the topical anti-inflammatory effect of the CC fruit extract cream (2–8%) and the tissue levels of IL-6 and TNF-α were estimated by using a commercial ELISA kit. The topical antinociceptive activity of CC cream (2–8%) was evaluated in the rat formalin test. To determine the role of opioid receptors in the local antinociceptive effect of the CC cream, naloxone (20 μg/paw, i.pl.), a non-selective opioid antagonist, was used. Results: The results showed that the CC cream (2–8%) dose-dependently reduced the carrageenan-induced paw edema and reversed the changes in the level of TNF-α and IL-6 due to carrageenan-induced edema (p < 0.01). The anti-inflammatory effect of CC cream 8% was comparable to that of hydrocortisone ointment 1%. Furthermore, the application of CC cream (2–8%) dose-dependently inhibited both first and second phases of the formalin test (p < 0.05). The antinociceptive effect of the CC cream (8%) was comparable to that of methyl salicylate cream 30%. Moreover, the administration of naloxone significantly reversed the topical antinociceptive effect of the CC cream (p < 0.05). Conclusions: For the first time, this study indicated that the topical application of CC cream possesses significant anti-inflammatory and antinociceptive activities in animal models, which were probably mediated by opioid receptors and the suppression of pro-inflammatory cytokines (TNF-α and IL-6). Thus, the CC cream can be used to treat inflammatory pain and inflammatory diseases.

2014 ◽  
Vol 42 (01) ◽  
pp. 223-242 ◽  
Author(s):  
Jung-Chun Liao ◽  
Wen-Te Chang ◽  
Meng-Shiou Lee ◽  
Yung-Jia Chiu ◽  
Wei-Kai Chao ◽  
...  

The seeds of Cuscuta chinensis, Cuscutae Semen, are commonly used as a medicinal material for treating the aching and weakness of the loins and knees, tonifying the defects of the liver and the kidney, and treating the diarrhea due to hypofunction of the kidney and the spleen. Since aching and inflammation are highly correlated with such diseases, the aim of this study is to investigate the possible antinociceptive and anti-inflammatory mechanisms of the seeds of C. chinensis. The antinociceptive effect of the seeds of C. chinensis was evaluated via the acetic acid-induced writhing response and formalin-induced paw licking methods. The anti-inflammatory effect was evaluated via the λ-carrageenan induced mouse paw edema method. The results found that 100 and 500 mg/kg of the methanol extract of the seeds of C. chinensis( CCMeOH) significantly decreased (p < 0.01 and p < 0.001, respectively) the writhing response in the acetic acid assay. Additionally, 20–500 mg/kg of CCMeOHsignificantly decreased licking time at the early (20 and 100 mg/kg, p < 0.001) and late phases (100 mg/kg, p < 0.01; 500 mg/kg, p < 0.001) of the formalin test, respectively. Furthermore, CCMeOH(100 and 500 mg/kg) significantly decreased (p < 0.01 and p < 0.001, respectively) edema paw volume four hours after λ-carrageenan had been injected. The results in the following study also revealed that the anti-inflammatory mechanism of CCMeOHmay be due to declined levels of NO and MDA in the edema paw by increasing the activities of SOD, GPx and GRd in the liver. In addition, CCMeOHalso decreased IL-1β, IL-6, NF-κB, TNF-α, and COX-2 levels. This is the first study to demonstrate the possible mechanisms for the antinociceptive and anti-inflammatory effects of CCMeOHin vivo. Thus, it provides evidence for the treatment of Cuscutae Semen in inflammatory diseases.


2018 ◽  
Vol 9 (02) ◽  
pp. 20181-20191 ◽  
Author(s):  
Dr Maghsoudi, Hossein ◽  
Samaneh Haj-allahyari

Due to the side effects of current therapies for osteoarthritis one of the alternative medicine is using herbal medicine such as Nigella sativa .L which in Iranian traditional medicine has been used as a treatment option. The purpose of this study is evaluating the effect of alcoholic extract of Nigella sativa (AENS) on pro-inflammatory cytokines in Bovine Fibroblast-like BFLs (BFLS) and THP-1. BFLS cells were isolated from Radiocarpal joint. After evaluating of LC50 (27 µg/mL), both cells (5x105 (cells\wel)) were incubated at 37 ° C and 5% CO2 and 90% humidity for 72 hours with AENS (6.13 μg\ml as a media LC50). One set of cells was activated for 1h with LPS for RT-PCR analysis of COX-2, INOS, IL-1β, TNF-α expression and another set of cells was activated for 24h, cells supernatant were analyzed for PGE-2 and nitrite content. The present study demonstrates that AENS reduced expression levels of COX-2, INOS, TNF-α in control group. Reduced expression of COX2 and INOS was significantly along with the reducing production of NO and PGE2.Also, AENS decreased the expression of TNF-α and iL-1β in control group. Our results showed that the anti-inflammatory effect of AENS not only has anti-inflammatory effect on the BFLS cells but also related to the THP-1 that are active in the synovial membrane.


Dose-Response ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 155932582096172
Author(s):  
Ilaria Floris ◽  
Thorsten Rose ◽  
Juan Antonio Collado Rojas ◽  
Kurt Appel ◽  
Camille Roesch ◽  
...  

Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) are pro-inflammatory cytokines involved in acute and chronic inflammatory diseases. Indeed, immunotherapy blocking these 2 cytokines has been developed. Micro-immunotherapy (MI) also uses ultra-low doses (ULD) of pro-inflammatory cytokines, impregnated on lactose-sucrose pillules, to counteract their overexpression. The study has been conducted with 2 objectives: examine the anti-inflammatory effect in vitro and the capacity of 2 unitary medicines, TNF-α (27 CH) and IL-1β (27 CH), to reduce the secretion of TNF-α in human primary monocytes and THP-1 cells differentiated with phorbol-12-myristate-13-acetate, after lipopolysaccharide (LPS) exposure; then, investigate the presence of particles possibly containing starting materials using tunable resistive pulse sensing technique. The results show that the unitary medicines, tested at 3 pillules concentrations (5.5, 11 and 22 mM), have reduced the secretion of TNF-α in both models by about 10−20% vs. vehicle control, depending on concentration. In this exploratory study, particles (150−1000 nm) have been detected in MI ULD-impregnated pillules and a hypothesis for MI medicines mode of action has been proposed. Conscious that more evaluations are necessary, authors are cautious in the conclusions because the findings described in the study are still limited, and future investigations may lead to different hypothesis.


2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Ching-Wen Chang ◽  
Wen-Te Chang ◽  
Jung-Chun Liao ◽  
Yung-Jia Chiu ◽  
Ming-Tsuen Hsieh ◽  
...  

The aim of this study was to investigate possible analgesic and anti-inflammatory mechanisms of theCRMeOH. Analgesic effect was evaluated in two models including acetic acid-induced writhing response and formalin-induced paw licking. The anti-inflammatory effect was evaluated byλ-carrageenan-induced mouse paw edema and histopathologic analyses. The results showed thatCRMeOH(500 mg/kg) decreased writhing response in the acetic acid assay and licking time in the formalin test.CRMeOH(100 and 500 mg/kg) significantly decreased edema paw volume at 4th to 5th hours afterλ-carrageenan had been injected. Histopathologically,CRMeOHabated the level of tissue destruction and swelling of the edema paws. These results were indicated that anti-inflammatory mechanism ofCRMeOHmay be due to declined levels of NO and MDA in the edema paw through increasing the activities of SOD, GPx, and GRd in the liver. Additionally,CRMeOHalso decreased IL-1β, IL-6, NFκB, TNF-α, COX-2, and iNOS levels. The contents of two active ingredients, ursolic acid and lupeol, were quantitatively determined. This paper demonstrated possible mechanisms for the analgesic and anti-inflammatory effects ofCRMeOHand provided evidence for the classical treatment ofCissus repensin inflammatory diseases.


2010 ◽  
Vol 38 (03) ◽  
pp. 529-546 ◽  
Author(s):  
Zhen-Rung Lai ◽  
Wen-Huang Peng ◽  
Yu-Ling Ho ◽  
Shun-Chieh Huang ◽  
Tai-Hung Huang ◽  
...  

In this study, we evaluated the analgesic effect of the methanol extract of Kalanchoe gracilis (MKGS) stem in animal models by inducing writhing response with acetic acid and conducting formalin test. The anti-inflammatory effect of MKGS was also estimated on mice with λ-carrageenan induced paw edema model. In order to investigate the anti-inflammatory mechanism of MKGS, we analyzed the activities of glutathione peroxidase (GPx) and glutathione reductase (GRx) in the liver, and the levels of interleukin-1β (IL-1β), tumor necrosis factor (TNF-α), malondialdehyde (MDA) and nitric oxide (NO) in the edema paw tissue. In the analgesic tests, MKGS (0.5 and 1.0 g/kg) decreased both the acetic acid-induced writhing response and the licking time in the late phase of the formalin test. In the anti-inflammatory test, MKGS (0.1, 0.5 and 1.0 g/kg) decreased paw edema at the third, fourth, fifth and sixth hours after λ-carrageenan had been administrated. Furthermore, MKGS increased the activities of SOD and GRx in liver tissues and decreased MDA level in the edema paws three hours after λ-carrageenan was injected. MKGS also affected the levels of IL-1β, TNF-α and NO induced by λ-carrageenan. All these results suggested that MKGS possessed analgesic and anti-inflammatory effects. The anti-inflammatory mechanism of MKGS might be related to the lowering of MDA level in the edema paw via increasing the activities of superoxide dismutase (SOD) and GRx in the liver, as well as the decreases in the levels of TNF-α and NO, and the production of IL-1β in inflamed tissues.


2019 ◽  
Vol 16 (10) ◽  
pp. 1157-1166
Author(s):  
Rodrigo César da Silva ◽  
Fabiano Veiga ◽  
Fabiana Cardoso Vilela ◽  
André Victor Pereira ◽  
Thayssa Tavares da Silva Cunha ◽  
...  

Background: : A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: : The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- bromobenzyloxime (8d) and (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- (methylsulfonyl)benzyloxime (8f) as promising bioactive prototypes. Results:: These compounds have significant analgesic and anti-inflammatory effects, as evidenced by formalin-induced mice paw edema and carrageenan-induced mice paw edema tests. In the formalin test, compounds 8b and 8f evidenced both anti-inflammatory and direct analgesic activities and in the carrageenan-induced paw edema, with compounds 8c, 8d, and 8f showing the best inhibitory effects, exceeding the standard drugs indomethacin and celecoxib. Conclusion: : Molecular docking studies have provided additional evidence that the pharmacological profile of these compounds may be related to inhibition of COX enzymes, with slight preference for COX-1. These results led us to identify the new O-benzyloxime ethers 8b, 8d and 8f as orally bioactive prototypes, with a novel structural pattern capable of being explored in further studies aiming at their optimization and development as drug candidates.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2529
Author(s):  
Haeyeop Kim ◽  
Woo Seok Yang ◽  
Khin Myo Htwe ◽  
Mi-Nam Lee ◽  
Young-Dong Kim ◽  
...  

Dipterocarpus tuberculatus Roxb. has been used traditionally as a remedy for many diseases, especially inflammation. Therefore, we analyzed and explored the mechanism of the anti-inflammatory effect of a Dipterocarpus tuberculatus Roxb. ethanol extract (Dt-EE). Dt-EE clearly and dose-dependently inhibited the expression of pro-inflammatory cytokines such as IL-6, TNF-α, and IL-1β in lipopolysaccharide (LPS)-treated RAW264.7 cells. Also, Dt-EE suppressed the activation of the MyD88/TRIF-mediated AP-1 pathway and the AP-1 pathway related proteins JNK2, MKK4/7, and TAK1, which occurred as a result of inhibiting the kinase activity of IRAK1 and IRAK4, the most upstream factors of the AP-1 pathway. Finally, Dt-EE displayed hepatoprotective activity in a mouse model of hepatitis induced with LPS/D-galactosamine (D-GalN) through decreasing the serum levels of alanine aminotransferase and suppressing the activation of JNK and IRAK1. Therefore, our results strongly suggest that Dt-EE could be a candidate anti-inflammatory herbal medicine with IRAK1/AP-1 inhibitory and hepatoprotective properties.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Rosangela Montanaro ◽  
Alessio D’Addona ◽  
Andrea Izzo ◽  
Carlo Ruosi ◽  
Vincenzo Brancaleone

AbstractClodronate is a bisphosphonate agent commonly used as anti-osteoporotic drug. Throughout its use, additional anti-inflammatory and analgesic properties have been reported, although the benefits described in the literature could not solely relate to their inhibition of bone resorption. Thus, the purpose of our in vitro study is to investigate whether there are underlying mechanisms explaining the anti-inflammatory effect of clodronate and possibly involving hydrogen sulphide (H2S). Immortalised fibroblast-like synoviocyte cells (K4IM) were cultured and treated with clodronate in presence of TNF-α. Clodronate significantly modulated iNOS expression elicited by TNF-α. Inflammatory markers induced by TNF-α, including IL-1, IL-6, MCP-1 and RANTES, were also suppressed following administration of clodronate. Furthermore, the reduction in enzymatic biosynthesis of CSE-derived H2S, together with the reduction in CSE expression associated with TNF-α treatment, was reverted by clodronate, thus rescuing endogenous H2S pathway activity. Clodronate displays antinflammatory properties through the modulation of H2S pathway and cytokines levels, thus assuring the control of the inflammatory state. Although further investigation is needed to stress out how clodronate exerts its control on H2S pathway, here we showed for the first the involvement of H2S in the additive beneficial effects observed following clodronate therapy.


2008 ◽  
Vol 294 (6) ◽  
pp. L1043-L1048 ◽  
Author(s):  
Wolfram Burkhardt ◽  
Petra Koehne ◽  
Heide Wissel ◽  
Susanne Graf ◽  
Hans Proquitté ◽  
...  

Perfluorocarbons (PFC) reduce the production of various inflammatory cytokines, including TNF-α. The anti-inflammatory effect is not entirely understood. If anti-inflammatory properties are caused by a mechanical barrier, PFC in the alveoli should have no effect on the inflammatory response to intravenous LPS administration. To test that hypothesis, rats ( n = 31) were administered LPS intravenously and were either spontaneously breathing (Spont), conventionally ventilated (CMV), or receiving partial liquid ventilation (PLV). Serum concentration of TNF-α was measured. The pulmonary expressions of TNF-α and TNF-α receptor 1 protein and of TNF-α and ICAM-1 mRNA were determined. LPS caused a significant ( P < 0.001) increase in serum TNF-α. Serum TNF-α concentration was similar in LPS/Spont (525 ± 180 pg/ml) and LPS/CMV (504 ± 154 pg/ml) but was significantly ( P < 0.001) lower in animals of the LPS/PLV group (274 ± 101 pg/ml). Immunohistochemical data on TNF-α protein expression showed a LPS-induced increase in TNF-α and TNF-α receptor 1 expression that was diminished by partial liquid ventilation. PCR measurements revealed a lower expression of TNF-α and ICAM-1 mRNA in LPS/PLV than in LPS/CMV or LPS/Spont animals. Semiquantitative histological evaluation revealed only minor alveolar inflammation with no significant differences between the groups. Low serum TNF-α concentration in PFC-treated animals is most likely explained by a decreased production of TNF-α in the lung.


Author(s):  
Mario I Ortiz ◽  
Raquel Cariño-Cortés ◽  
Victor Manuel Muñoz Pérez ◽  
Andres Salas Casas ◽  
Gilberto Castañeda-Hernández

The aim of this study was to examine if the peripheral antinociception of α-bisabolol involve the participation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) synthesis followed by K+ channel opening in the formalin test. Wistar rats were injected in the dorsal surface of the right hind paw with formalin (1%). Rats received a subcutaneous injection into the dorsal surface of the paw of vehicles or increasing doses of α-bisabolol (100-300 µg/paw). To determine whether the peripheral antinociception induced by α-bisabolol was mediated by either the opioid receptors or the NO-cGMP-K+ channels pathway, the effect of pretreatment (10 min before formalin injection) with the appropriate vehicles, naloxone, naltrexone, L-NAME, ODQ, glibenclamide, glipizide, apamin, charybdotoxin, tetraethylammonium or 4-aminopyridine on the antinociceptive effects induced by local peripheral α-bisabolol (300 µg/paw) were assessed. α-bisabolol produced antinociception during both phases of the formalin test. α-bisabolol antinociception was blocked by L-NAME, ODQ, and all the K+ channels blockers. The peripheral antinociceptive effect produced by α-bisabolol was not blocked by the opioid receptor inhibitors. α-bisabolol was able to active the NO-cGMP-K+ channels pathway in order to produce its antinoceptive effect. The participation of opioid receptors in the peripheral local antinociception induced by α-bisabolol is excluded.


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