scholarly journals Antioxidant, Anti-Inflammatory, and Analgesic Activities ofAgrimonia eupatoriaL. Infusion

2017 ◽  
Vol 2017 ◽  
pp. 1-13 ◽  
Author(s):  
Telmo N. Santos ◽  
Gustavo Costa ◽  
J. Pinto Ferreira ◽  
Joana Liberal ◽  
Vera Francisco ◽  
...  

Agrimony (Agrimonia eupatoriaL.) (Ae) is used in traditional medicine to treat inflammatory and oxidative related diseases. Therefore, this study focuses on the anti-inflammatory and analgesic potential of Ae infusion (AeI). Phenolic compounds characterization was achieved by HPLC-PDA-ESI/MSn. To evaluate antioxidant potential, 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion, hydroxyl radical, and SNAP assays were used. In vitro anti-inflammatory activity of AeI was investigated in LPS-stimulated macrophages by measuring the NO production. In vivo anti-inflammatory activity was validated using the mouse carrageenan-induced paw edema model. Peripheral and central analgesic potential was evaluated using the acetic acid-induced writhing and hot-plate tests, respectively, as well as the formalin assay to assess both activities. The safety profile was disclosed in vitro and in vivo, using MTT and hematoxylin assays, respectively. Vitexin, quercetinO-galloyl-hexoside, and kaempferolO-acetyl-hexosyl-rhamnoside were referred to in this species for the first time. AeI and mainly AePF (Ae polyphenolic fraction) showed a significant antiradical activity against all tested radicals. Both AeI and AePF decreased NO levels in vitro, AePF being more active than AeI. In vivo anti-inflammatory and analgesic activities were verified for both samples at concentrations devoid of toxicity. Agrimony infusion and, mainly, AePF are potential sources of antiradical and anti-inflammatory polyphenols.

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.


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.


2014 ◽  
Vol 42 (04) ◽  
pp. 949-965 ◽  
Author(s):  
Haoyu Ye ◽  
Caifeng Xie ◽  
Wenshuang Wu ◽  
Minli Xiang ◽  
Zhuowei Liu ◽  
...  

The present study was designed to investigate the in vitro and in vivo anti-inflammatory activity of flavonoids isolated from Millettia pachycarpa Benth. The seeds of M. pachycarpa Benth were extracted with ethanol and subjected to chromatographic separation for the isolation of bioactive compounds. Their structures were elucidated by spectroscopic methods. The anti-inflammatory activity of the compounds was investigated by evaluating the inhibition ability of NO production, iNOS activity and iNOS protein expression induced by LPS-stimulated RAW264.7 macrophages in vitro and the carrageenan-induced hind paw edema model in vivo. Molecular docking simulation was also employed to obtain the binding parameters in the binding pocket of iNOS. Thirteen compounds (1–13) were isolated from Chinese herbal medicine M. pachycarpa Benth. Among them, 4-hydroxylonchocarpin (6) and deguelin (7) exhibited remarkable inhibitory rates of 66.5% and 57.7%, respectively, compared with that of 52.5% of indomethacin in LPS-induced macrophages cells. 4-hydroxylonchocarpin (6) with low toxicity (IC50 > 100 μm) exhibited better inhibitory effects to positive control of 1400W on iNOS activity at the concentration of 10 μm. Western blot assay revealed that 4-hydroxylonchocarpin (6) inhibited iNOS protein expression in RAW264.7 cells and molecular docking simulation showed that 4-hydroxylonchocarpin (6) fit well into the binding pocket of iNOS. In the carrageenan-induced paw edema model, our data revealed that the anti-inflammatory potential of 4-hydroxylonchocarpin (6) at 10 mg/kg showed comparable inhibitory ability to indomethacin at 5 h while a higher concentration of 4-hydroxylonchocarpin (6) at 50 mg/kg showed higher inhibitory activity than indomethacin, which was further confirmed by plasma levels of nitrite. The overall results suggest that 4-hydroxylonchocarpin (6) might be used as a potential therapeutic agent for inflammation-associated disorders.


2021 ◽  
Author(s):  
Ravindra Jagannath Waghole ◽  
Ashwini Vivek Misar ◽  
Neha Shashikant Kulkarni ◽  
Feroz Khan ◽  
Dattatraya Gopal Naik ◽  
...  

Abstract The severity and perseverance of the inflammation have been demonstrated in many health conditions. The limitations of existing medications, propose the need for newer alternative anti-inflammatory medications. In our earlier studies, we demonstrated the topical anti-inflammatory potential of crude ethanolic extract of Tetrastigma sulcatum leaves and its fractions. In the present study, we further explored anti-inflammatory activity of T. sulcatum extract, fractions, pure compound and its derivatives using in vitro and in vivo bioassay techniques. We attempted to isolate a pure compound from leaf extract and was identified as Friedelan-3β-ol (CI) and its derivatives Friedelinol acetate (C II) and Friedelinol methyl ether (C III) were synthesized. Treatment with crude extract and its fractions demonstrated a significant reduction in the mRNA expression levels of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) and nitric oxide (NO) production in LPS-stimulated inflammation in RAW 264.7 cells. Likewise, compounds CI, CII and CIII showed a similar pattern of significant inhibition of proinflammatory cytokines and NO production. In vivo study in Carrageenan induced paw-inflammatory mice model demonstrated reduced paw oedema and proinflammatory cytokines levels in a dose-dependent manner upon treatment of extract, its fractions, pure compound (CI), and their derivatives (CII and CIII.). The docking study showed all the compounds (CI, CII and CIII) share common residues with Dexamethasone. TNF- α exhibited the most interacting residues with the compounds. The present study confirmed the T. sulcatum ’s anti-inflammatory activity, suggesting Friedelan-3β-ol as an active component in a crude extract.


2018 ◽  
Vol 2018 ◽  
pp. 1-17 ◽  
Author(s):  
Han Gyung Kim ◽  
Subin Choi ◽  
Jongsung Lee ◽  
Yo Han Hong ◽  
Deok Jeong ◽  
...  

Celtis choseniana is the traditional plant used at Korea as a herbal medicine to ameliorate inflammatory responses. Although Celtis choseniana has been traditionally used as a herbal medicine at Korea, no systemic research has been conducted on its anti-inflammatory activity. Therefore, the present study explored an anti-inflammatory effect and its underlying molecular mechanism using Celtis choseniana methanol extract (Cc-ME) in macrophage-mediated inflammatory responses. In vitro anti-inflammatory activity of Cc-ME was evaluated using RAW264.7 cells and peritoneal macrophages stimulated by lipopolysaccharide (LPS), pam3CSK4 (Pam3), or poly(I:C). In vivo anti-inflammatory activity of Cc-ME was investigated using acute inflammatory disease mouse models, such as LPS-induced peritonitis and HCl/EtOH-induced gastritis. The molecular mechanism of Cc-ME-mediated anti-inflammatory activity was examined by Western blot analysis and immunoprecipitation using whole cell and nuclear fraction prepared from the LPS-stimulated RAW264.7 cells and HEK293 cells. Cc-ME inhibited NO production and mRNA expression of inducible nitric oxide synthase (iNOS), cyclooxygenase (COX-2), and tumor necrosis factor-alpha (TNF-α) in the RAW264.7 cells and peritoneal macrophages induced by LPS, pam3, or poly(I:C) without cytotoxicity. High-performance liquid chromatography (HPLC) analysis showed that Cc-ME contained anti-inflammatory flavonoids quercetin, luteolin, and kaempferol. Among those, the content of luteolin, which showed an inhibitory effect on NO production, was highest. Cc-ME suppressed the NF-κB signaling pathway by targeting Src and interrupting molecular interactions between Src and p85, its downstream kinase. Moreover, Cc-ME ameliorated the morphological finding of peritonitis and gastritis in the mouse disease models. Therefore, these results suggest that Cc-ME exerted in vitro and in vivo anti-inflammatory activity in LPS-stimulated macrophages and mouse models of acute inflammatory diseases. This anti-inflammatory activity of Cc-ME was dominantly mediated by targeting Src in NF-κB signaling pathway during macrophage-mediated inflammatory responses.


2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400 ◽  
Author(s):  
Karoline Costa Lima ◽  
Domingos Tabajara de Oliveira Martins ◽  
Antonio Macho ◽  
Ruberlei Godinho de Oliveira ◽  
Eduarda Pavan ◽  
...  

Phytochemical investigation of the hydroethanolic extract of the inner stem bark of Dilodendron bipinnatum (HEDb) by column chromatography led to the separation of three major fractions: a) a mixture of phytosterols (ST mixture), including β-sitosterol (1), stigmasterol (2) and campesterol (3); b) a mixture of 3- O-β-glucopyranosyl-β-sitosterol (4) and 3- O-β-glucopyranosyl-stigmasterol (5) (SGP mixture); and c) epicatechin (6), as a single isolate. Their structures were determined by spectrometric analysis using 1H- and 13C-NMR spectroscopy, and GC-MS. The safety profile of the SGP mixture, when evaluated on RAW 264.7 cells, using the alamar blue® assay, exhibited no cytotoxic effects. The anti-inflammatory activity was comparatively analyzed in vivo using the lipopolysaccharide (LPS)-induced peritonitis model in mice, showing a strong reduction of leukocyte migration to the peritoneal cavity using both the SGP mixture and the HEDb. In vitro assessment of nitric oxide (NO) in the macrophagic RAW 264.7 cell line showed an inhibition of NO by the SGP mixture when cells were stimulated with LPS. Taken together, the results show an important contribution of the sterol glucoside mixture on the anti-inflammatory activity of HEDb. Also, one of the mechanisms for such inhibition seems to be a direct inhibition of NO production in stimulated macrophages.


2021 ◽  
Vol 18 ◽  
Author(s):  
G. Ganga Reddy ◽  
Ch Venkata Ramana Reddy ◽  
B. Srinivasa Reddy

Aim: The reactions were carried out by one pot three-component synthesis, 3-cyanoacetylindole (1) on reaction with aromatic aldehydes (2) and β-naphthol (3) in an aqueous medium in presence of L-proline as a catalyst under reflux for 30 min, resulted (3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl)methanone (4). The method has many advantages like short reaction times, good yields and simple workup procedure besides being green in nature. Pharmacological evaluation of title compounds was done for anti-inflammatory and analgesic activities. Anti-inflammatory activity was carried carrageenan-induced paw edema model in which indomethacin was used as standard and analgesic activity was evaluated by eddy's hot plate method using diclofenac as standard drug. Background: Benzopyrans or chromenes are an important class of heterocyclic compounds due to their broad spectrum of biological activity and a wide range of applications in medicinal chemistry. The chromene moiety is found in various natural products with interesting biological properties. Chromenes constitute the basic backbone of various types of polyphenols and are widely found in alkaloids, tocopherols, flavonoids and anthocyanins. Indoles are omnipresent in various bioactive compounds like alkaloids, agrochemicals and pharmaceuticals. Objective: To synthesize one-pot stepwise Green synthesis, anti-inflammatory and analgesic activities of 3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl)methanones Methods: The acute anti-inflammatory effect was evaluated by carrageenan-induced mice paw edema (Ma Rachchh et al., 2011). Edema was induced by injecting carrageenan (1% w/v, 0.1 ml) in the right hind paw of mice. The test compounds 1-12, indomethacin (10 mg/kg) and the vehicle were administered orally one hour before injection of carrageenan. Paw volume was measured with digital plethysmometer at 0, 30, 60, 90, 120 min after injection. Percentage increase =A-B/ A *100 Results: Carrageenan Induced paw edema model was used for Anti-inflammatory activity in which animals treated with standard (indomethacin) and test compounds showed a significant decrease in the paw edema. Analgesic activity was estimated by using Eddy’s hot plate method; animals were treated with standard (diclofenac) and test compounds showed a significant increase in the reaction time. Conclusion: A green, One-pot, step-wise and three-component synthesis of 3-amino-1-phenyl-1H-benzo[f]chromen-2-yl) (1H-indol-3-yl) methanone was achieved by using water as a solvent, L-proline as catalyst under reflux conditions. The reactions were carried out in eco-friendly conditions with shorter reaction times, easier workup and high yields. Anti-inflammatory activity was evaluated by carrageenan-induced paw edema model where significant anti-inflammatory activity is shown by all the test compounds (4a-l) when compared to standard drug. Analgesic activity was studied by Eddy’s Hot plate method and Test compounds 4e, 4f, 4h, 4i, 4j, 4k, 4l showed significant activities when compared to the reference drug.


2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Pranporn Kuropakornpong ◽  
Arunporn Itharat ◽  
Sumalee Panthong ◽  
Seewaboon Sireeratawong ◽  
Buncha Ooraikul

Benjakul (BJK) is a Thai traditional remedy consisting of five plants: Piper chaba Hunt., Piper sarmentosum Roxb., Piper interruptum Opiz., Plumbago indica Linn., and Zingiber officinale Roscoe. It is used as a first-line drug to balance patient’s symptoms before other treatments. BJK ethanolic extract has been reported to show anti-inflammatory activity through various mediators, e.g., nitric oxide, TNF-α, IL-1β, and IL-6. Therefore, BJK could serve as a potential novel anti-inflammatory herbal medicine. However, studies on prostaglandin E2 (PGE2), one of the key mediators in acute inflammation, and anti-inflammation in animal models (in vivo) have not been done. This study investigated the anti-inflammatory activity of BJK extract and some of its chemical compounds against PGE2 production in murine macrophage (RAW 264.7) cell line and two in vivo models of anti-inflammatory studies. Ethanolic extract of BJK (BJK[E]) showed high inhibitory activity against PGE2 production with an IC50 value of 5.82 ± 0.10 μg/mL but its water extract (BJK[W]) was inactive. Two chemicals from BJK[E], i.e., plumbagin and myristicin, which served as biological markers, showed strong activity with IC50 values of 0.08 ± 0.01 and 1.80 ± 0.06 μg/mL, respectively. BJK[E] was administered both topically and orally to rats inhibited with inflammation induced by ethyl phenylpropiolate (rat ear edema model) and carrageenan (hind paw edema model). Moreover, the biological activity of BJK extract did not reduce after six-month storage under accelerated condition (40°C, 75% RH). This indicated its stability and a 24-month shelf-life under normal condition. These results supported not only the use of BJK in Thai traditional medicine but also the possibility of further development of phytopharmaceutical products from BJK.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 743
Author(s):  
Geovana F. G. Silvestre ◽  
Renally P. Lucena ◽  
Genil D. Oliveira ◽  
Helimarcos N. Pereira ◽  
Jhonatta A. B. Dias ◽  
...  

This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg−1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich’s carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg−1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.


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