In vitro and in vivo assessment of meadowsweet (Filipendula ulmaria) as anti-inflammatory agent

2016 ◽  
Vol 193 ◽  
pp. 627-636 ◽  
Author(s):  
Jelena Katanić ◽  
Tatjana Boroja ◽  
Vladimir Mihailović ◽  
Stefanie Nikles ◽  
San-Po Pan ◽  
...  
2017 ◽  
Vol 198 ◽  
pp. 608-609
Author(s):  
Jelena Katanić ◽  
Tatjana Boroja ◽  
Vladimir Mihailović ◽  
Stefanie Nikles ◽  
San-Po Pan ◽  
...  

2020 ◽  
Vol 21 (16) ◽  
pp. 5700 ◽  
Author(s):  
Rianthong Phumsuay ◽  
Chawanphat Muangnoi ◽  
Peththa Wadu Dasuni Wasana ◽  
Hasriadi Hasriadi ◽  
Opa Vajragupta ◽  
...  

Curcumin diglutaric acid (CurDG), an ester prodrug of curcumin, has the potential to be developed as an anti-inflammatory agent due to its improved solubility and stability. In this study, the anti-inflammatory effects of CurDG were evaluated. The effects of CurDG on inflammatory mediators were evaluated in LPS-stimulated RAW 264.7 macrophage cells. CurDG reduced the increased levels of NO, IL-6, and TNF- α, as well as iNOS and COX-2 expression in cells to a greater extent than those of curcumin, along with the potent inhibition of MAPK (ERK1/2, JNK, and p38) activity. The anti-inflammatory effects were assessed in vivo by employing a carrageenan-induced mouse paw edema model. Oral administration of CurDG demonstrated significant anti-inflammatory effects in a dose-dependent manner in mice. The effects were significantly higher compared to those of curcumin at the corresponding doses (p < 0.05). Moreover, 25 mg/kg curcumin did not exert a significant anti-inflammatory effect for the overall time course as indicated by the area under the curve data, while the equimolar dose of CurDG produced significant anti-inflammatory effects comparable with 50, 100, and 200 mg/kg curcumin (p < 0.05). Similarly, CurDG significantly reduced the proinflammatory cytokine expression in paw edema tissues compared to curcumin (p < 0.05). These results provide the first experimental evidence for CurDG as a promising anti-inflammatory agent.


2018 ◽  
Vol 164 ◽  
pp. 332-339 ◽  
Author(s):  
Sara Daneshmand ◽  
Mahmoud Reza Jaafari ◽  
Jebrail Movaffagh ◽  
Bizhan Malaekeh-Nikouei ◽  
Mehrdad Iranshahi ◽  
...  

2019 ◽  
Vol 49 (20) ◽  
pp. 2725-2759 ◽  
Author(s):  
Prateek Pathak ◽  
Parjanya Kumar Shukla ◽  
Vladislav Naumovich ◽  
Maria Grishina ◽  
Vladimir Potemkin ◽  
...  

A novel series of a hybrid class of hybrid thiazolidin-4-one derivatives were designed and synthesized through one-pot catalytic synthesis. The reaction was catalyzed in the presence of silica-H2SO4(+6). The derivatives computational ADMET profile was calculated. The study shows that most active derivatives have optimal logP, higher anti-inflammatory activity score, and poor metabolism at the sight of P450-3A4 and 2D6. The entire series of derivatives were further evaluated for anti-tubercular (against Mycobacterium tuberculosis H37Rv (Resistant strain)) and anti-inflammatory activity (in-vivo assay using Wistar rat). The result showed that derivatives 4c, 4h, and 4m have significant potency against tested M. tuberculosis. However, derivatives 4i and 4j found significantly active against inflammation. In vitro COX inhibition assay also supported the result in favor of selectivity and efficacy of derivatives.


1997 ◽  
Vol 328 (2) ◽  
pp. 363-369 ◽  
Author(s):  
M. Sheu YU ◽  
Jeng F. WU Tzong L. LIN ◽  
C. Sheng KUO

We studied the effect of PPM-18, a chemically synthesized naphthoquinone derivative and also an anti-inflammatory agent, on the lipopolysaccharide (LPS)-activated inducible NO synthase (iNOS) expression in rat alveolar macrophages. Pretreatment of macrophages with PPM-18 (0.1-10 μM) significantly inhibited nitrite production, iNOS protein expression and iNOS mRNA accumulation. PPM-18 did not directly affect the enzymic activities of iNOS and other constitutive NOS forms. The LPS-induced increase in nuclear transcription factor κB (NF-κB) p65 and p50 in nucleus was suppressed by PPM-18 (10 μM). Moreover electrophoretic mobility-shift assays demonstrated that PPM-18 inhibited DNA binding to NF-κB induced by LPS in whole cells but not when added in the nuclear extract, suggesting that PPM-18 did not interfere directly with the binding of NF-κB to DNA and that some events had to be processed before NF-κB could bind DNA. Examination of NF-κB showed that PPM-18 stabilized the NF-κB inhibitor, IκBα, by preventing its degradation from NF-κB. Therefore the stabilization of IκBα might have contributed to the inhibition of NF-κB activation. These results also indicate strongly that NF-κB is involved in the production of NO on stimulation by LPS. PPM-18 significantly decreased the production of tumour necrosis factor α in response to LPS. PPM-18 protects mice against LPS-induced lethal toxicity. These results also indicate that PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter and exerts a beneficial effect in the mouse model of sepsis.


PPAR Research ◽  
2007 ◽  
Vol 2007 ◽  
pp. 1-5 ◽  
Author(s):  
Asha Jacob ◽  
Rongqian Wu ◽  
Mian Zhou ◽  
Ping Wang

Curcumin, the phytochemical component in turmeric, is used as a dietary spice and a topical ointment for the treatment of inflammation in India for centuries. Curcumin (diferuloylmethane) is relatively insoluble in water, but dissolves in acetone, dimethylsulphoxide, and ethanol. Commercial grade curcumin contains 10–20% curcuminoids, desmethoxycurcumin, and bisdesmethoxycurcumin and they are as effective as pure curcumin. Based on a number of clinical studies in carcinogenesis, a daily oral dose of 3.6 g curcumin has been efficacious for colorectal cancer and advocates its advancement into Phase II clinical studies. In addition to the anticancer effects, curcumin has been effective against a variety of disease conditions in both in vitro and in vivo preclinical studies. The present review highlights the importance of curcumin as an anti-inflammatory agent and suggests that the beneficial effect of curcumin is mediated by the upregulation of peroxisome proliferator-activated receptor-γ(PPAR-γ) activation.


2018 ◽  
Vol 18 (1) ◽  
pp. 60
Author(s):  
Ismiarni Komala ◽  
Supandi Supandi ◽  
Nurhasni Nurhasni ◽  
Ofa Suzanti Betha ◽  
Eka Putri ◽  
...  

Ethyl p-methoxycinnamate (EPMC) (1) has been isolated as a major compound from the rhizome of Kaempferia galanga together with the other compound ethyl cinnamate (2). As reported in the literature, EPMC (1) exhibited a significant in vitro and in vivo anti-inflammatory activity. In this research, we investigated the anti-inflammatory activity of compounds 1 and 2 by using anti-denaturation of heat bovine serum albumin (BSA) method. In order to analyze active sites that are responsible for the anti-inflammatory activity, therefore, it is necessary to conduct structural modification of EPMC (1). The structural modification was performed through re-esterification reaction by using conventional and assistance of the unmodified microwave oven. Evaluation of the results of the bioassay indicated that the ester and methoxy functional groups of EPMC (1) play an important role for the anti-inflammatory activity.


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