scholarly journals Investigation of Active Anti-Inflammatory Constituents of Essential Oil from Pinus koraiensis (Sieb. et Zucc.) Wood in LPS-Stimulated RBL-2H3 Cells

Biomolecules ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 817
Author(s):  
Ji-Yoon Yang ◽  
Won-Sil Choi ◽  
Ki-Joong Kim ◽  
Chang-Deuk Eom ◽  
Mi-Jin Park

In a previous study, we demonstrated the anti-inflammatory activity of the essential oil extracted from Korean pine (Pinus koraiensis, Sieb. et Zucc.) wood. This study aims to investigate the active anti-inflammatory constituents of P. koraiensis oil. The essential oil was extracted from P. koraiensis wood by hydrodistillation and was divided into six fractions (A–F) through fractional distillation. Then, the anti-inflammatory activities of the fractions (A–F) were determined. Fractions A and F markedly downregulated the production of pro-inflammatory cytokines as well as the secretion of β-hexosaminidase in lipopolysaccharide (LPS)-stimulated RBL-2H3 cells. The main constituents of the active anti-inflammatory A and F fractions were (+)-α-pinene, (−)-β-pinene, (+)-α-terpineol, 3-carene, (+)-limonene, and longifolene. These six single compounds decreased the expression of inflammatory-related genes (i.e., IL-4 and IL-13) as well as the secretion of β-hexosaminidase in LPS-stimulated RBL-2H3 cells. (+)-α-Pinene, (−)-β-pinene, (+)-α-terpineol, and longifolene exhibited the strongest effects; these effects were comparable to those of the positive control (i.e., dexamethasone). The findings indicate that the interactions between these components exhibit potential for the management and/or treatment of inflammatory conditions as well as base structures for the development of novel anti-inflammatory drugs.

Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 653
Author(s):  
Seth O. Asiedu ◽  
Samuel K. Kwofie ◽  
Emmanuel Broni ◽  
Michael D. Wilson

Severely ill coronavirus disease 2019 (COVID-19) patients show elevated concentrations of pro-inflammatory cytokines, a situation commonly known as a cytokine storm. The p38 MAPK receptor is considered a plausible therapeutic target because of its involvement in the platelet activation processes leading to inflammation. This study aimed to identify potential natural product-derived inhibitory molecules against the p38α MAPK receptor to mitigate the eliciting of pro-inflammatory cytokines using computational techniques. The 3D X-ray structure of the receptor with PDB ID 3ZS5 was energy minimized using GROMACS and used for molecular docking via AutoDock Vina. The molecular docking was validated with an acceptable area under the curve (AUC) of 0.704, which was computed from the receiver operating characteristic (ROC) curve. A compendium of 38,271 natural products originating from Africa and China together with eleven known p38 MAPK inhibitors were screened against the receptor. Four potential lead compounds ZINC1691180, ZINC5519433, ZINC4520996 and ZINC5733756 were identified. The compounds formed strong intermolecular bonds with critical residues Val38, Ala51, Lys53, Thr106, Leu108, Met109 and Phe169. Additionally, they exhibited appreciably low binding energies which were corroborated via molecular mechanics Poisson–Boltzmann surface area (MM-PBSA) calculations. The compounds were also predicted to have plausible pharmacological profiles with insignificant toxicity. The molecules were also predicted to be anti-inflammatory, kinase inhibitors, antiviral, platelet aggregation inhibitors, and immunosuppressive, with probable activity (Pa) greater than probable inactivity (Pi). ZINC5733756 is structurally similar to estradiol with a Tanimoto coefficient value of 0.73, which exhibits anti-inflammatory activity by targeting the activation of Nrf2. Similarly, ZINC1691180 has been reported to elicit anti-inflammatory activity in vitro. The compounds may serve as scaffolds for the design of potential biotherapeutic molecules against the cytokine storm associated with COVID-19.


2010 ◽  
Vol 13 (4) ◽  
pp. 425-432 ◽  
Author(s):  
Z. A. Zakaria ◽  
A. S. Mohamad ◽  
M. S. Ahmad ◽  
A. F. Mokhtar ◽  
D. A. Israf ◽  
...  

Nonsteroidal anti-inflammatory drugs (NSAIDs) have been widely used for the treatment of inflammation. However, despite their effectiveness, most NSAIDs cause various side effects that negatively affect the management of inflammation and, in part, pain. Thus, there is a need to search for new anti-inflammatory agents with few, or no, side effects. Natural products of plant, animal, or microorganism origin have been good sources of new bioactive compounds. The present study was carried out to evaluate the acute and chronic anti-inflammatory activities of the essential oil of the rhizomes of Zingiber zerumbet (Zingiberaceae) using the carrageenan-induced paw edema and cotton pellet-induced granuloma tests, respectively. The effect of the essential oil on inflammatory- and noninflammatory-mediated pain was also assessed using the formalin test. Essential oil of Z. zerumbet, at doses of 30, 100, and 300 mg/kg, was administered intraperitoneally to rats. The substance exhibited significant anti-inflammatory activity both in acute and chronic animal models. The essential oil also inhibited inflammatory- and noninflammatory-mediated pain when assessed using the formalin test. In conclusion, the essential oil of Z. zerumbet possessed anti-inflammatory activity, in addition to its antinociceptive activity, which may explain its traditional uses to treat inflammatory-related ailments.


2018 ◽  
Vol 11 (4) ◽  
pp. 1755-1761
Author(s):  
Eun-Jin Yang ◽  
Sungchan Jang ◽  
Kwang Hee Hyun ◽  
Eun-Young Jung ◽  
Seung-Young Kim ◽  
...  

The anti-inflammatory activity and non-toxicity of Sonchus oleraceus extract (J6) were tested by measuring its effect on the levels of nitric oxide (NO), prostaglandin E2 (PGE2), and the pro-inflammatory cytokines, interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α), in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. We treated the RAW264.7 cells with various concentrations (50, 100, or 200 μg/mL) of J6. Our results showed that J6 inhibited the production of NO, PGE2, and pro-inflammatory cytokines in a concentration-dependent manner, without compromising cell viability. In addition, we provided supporting evidence that the inhibitory activity of J6 on the production of NO and PGE2 occurred via the downregulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively. Our findings suggest that J6 is a new source for anti-inflammatory drugs and ingredients for healthcare products that include functional cosmetics.


2017 ◽  
Vol 15 (3) ◽  
pp. 143-151 ◽  
Author(s):  
Rui Fei ◽  
Huan Zhang ◽  
Sheng Zhong ◽  
Baigong Xue ◽  
Yuanqi Gao ◽  
...  

Serine protease inhibitors (serpins) are a superfamily of proteins involved in many important biological processes, including inflammation. Serpins dysfunction-related diseases are mainly treated by augmentation therapy using serpins purified from human plasma. Pnserpin from hyperthermophilic archaeon Pyrobaculum neutrophilum showed protease inhibition activity and high stability. In this study, we examined the anti-inflammatory activity of Pnserpin using xylene-induced acute inflammatory model of mouse ear swelling and lipopolysaccharide (LPS)-induced murine RAW 264.7 macrophages cellular model. The inhibition of mouse ear swelling and the production of pro-inflammatory cytokines in mouse serum or in macrophages cell were used to evaluate the anti-inflammatory effect of Pnserpin. Our results showed that Pnserpin could inhibit the xylene-induced mouse ear swelling and suppress the production of pro-inflammatory cytokines in mouse serum and in LPS-induced RAW264.7 cells. This study indicated that Pnserpin might have anti-inflammatory effect in vivo and in vitro.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Edina Pandur ◽  
Alex Balatinácz ◽  
Giuseppe Micalizzi ◽  
Luigi Mondello ◽  
Adrienn Horváth ◽  
...  

Abstract Background Pseudomonas aeruginosa is the most common Gram-negative bacterium associated with nosocomial respiratory infections. Lavender essential oil is mainly used in aromatherapy, but it has several pharmacological and therapeutic properties. Furthermore, it possesses antifungal and antibacterial activities. The anti-inflammatory activity of essential oils may depend on the composition and the ratio of the compounds. The constitution of the essential oils extracted from the different stages of flowering period varies, which makes it plausible that the collection time of the flowers influences the anti-inflammatory effects. Different types of essential oils reduce inflammation acting similarly by modulating the activity and action of the NFκB signalling pathway, which is the major regulator of the transcription of pro-inflammatory cytokines. Methods Lavender essential oils were distilled from lavender plant cultivated in Hungary and the flowers were harvested at the beginning and at the end of flowering period. The experiments were carried out on THP-1 human monocyte/macrophage cell line as in vitro cell culture model for monitoring the effects of lavender essential oils and the main compound linalool on P. aeruginosa LPS stimulated inflammation. The mRNA and protein levels of four pro-inflammatory cytokines, IL-6, IL-1β, IL-8 and TNFα were determined by Real Time PCR and ELISA measurements. The effects of essential oils were compared to the response to two NFκB inhibitors, luteolin and ACHP. Results Linalool and lavender essential oil extracted from plants at the beginning of flowering period were successful in decreasing pro-inflammatory cytokine production following LPS pretreatment. In case of IL-8 and IL-1β lavender oil showed stronger effect compared to linalool and both of them acted similarly to NFκB inhibitors. Pretreatments with linalool and lavender essential oil/beginning of flowering period prevented pro-inflammatory cytokine production compared to LPS treatment alone. Although lavender essential oil/end of flowering period decreased IL-6, IL-1β and IL-8 mRNA expression in case of LPS pretreatment, it was not capable to reduce cytokine secretion. Conclusion Based on our results it has been proven that lavender essential oil extracted at the beginning of flowering period is a potent inhibitor of the synthesis of four pro-inflammatory cytokines IL-6, IL-8, IL-β and TNFα of THP-1 cells. This supports the relevance of the collection of the lavender flowers from early blooming period for essential oil production and for the utilization as an anti-inflammatory treatment.


PeerJ ◽  
2020 ◽  
Vol 8 ◽  
pp. e9533 ◽  
Author(s):  
Zhiyu Wang ◽  
Yanfei Wang ◽  
Prachi Vilekar ◽  
Seung-Pil Yang ◽  
Mayuri Gupta ◽  
...  

The novel coronavirus SARS-CoV-2 has become a global health concern. The morbidity and mortality of the potentially lethal infection caused by this virus arise from the initial viral infection and the subsequent host inflammatory response. The latter may lead to excessive release of pro-inflammatory cytokines, IL-6 and IL-8, as well as TNF-α ultimately culminating in hypercytokinemia (“cytokine storm”). To address this immuno-inflammatory pathogenesis, multiple clinical trials have been proposed to evaluate anti-inflammatory biologic therapies targeting specific cytokines. However, despite the obvious clinical utility of such biologics, their specific applicability to COVID-19 has multiple drawbacks, including they target only one of the multiple cytokines involved in COVID-19’s immunopathy. Therefore, we set out to identify a small molecule with broad-spectrum anti-inflammatory mechanism of action targeting multiple cytokines of innate immunity. In this study, a library of small molecules endogenous to the human body was assembled, subjected to in silico molecular docking simulations and a focused in vitro screen to identify anti-pro-inflammatory activity via interleukin inhibition. This has enabled us to identify the loop diuretic furosemide as a candidate molecule. To pre-clinically evaluate furosemide as a putative COVID-19 therapeutic, we studied its anti-inflammatory activity on RAW264.7, THP-1 and SIM-A9 cell lines stimulated by lipopolysaccharide (LPS). Upon treatment with furosemide, LPS-induced production of pro-inflammatory cytokines was reduced, indicating that furosemide suppresses the M1 polarization, including IL-6 and TNF-α release. In addition, we found that furosemide promotes the production of anti-inflammatory cytokine products (IL-1RA, arginase), indicating M2 polarization. Accordingly, we conclude that furosemide is a reasonably potent inhibitor of IL-6 and TNF-α that is also safe, inexpensive and well-studied. Our pre-clinical data suggest that it may be a candidate for repurposing as an inhaled therapy against COVID-19.


Author(s):  
Opeyemi N. Avoseh ◽  
Isiaka A. Ogunwande ◽  
Yahaya Yakubu ◽  
Peter O. Afolabi

Aims: Considering the lack of scientific studies focused on the pharmacological activity of Cordia millenii essential oil, this work was designed to evaluate the anti-inflammatory and anti-nociceptive activities of essential oil from the root bark. Study Design: The design of the study include collection of root bark of Cordia millenii, hydrodistillation of essential oil from the plant and evaluation of its anti-inflammatory and anti-nociceptive potentials. Place and Duration of Study: Department of Chemistry, Lagos State University, Nigeria between May 2017 and April 2018. Methodology: The root bark of C. millenii were collected from Ayetoro, Ilesha (7°37¢0N 4°43¢0E), Osun State, Nigeria in June 2017. Essential oils were obtained from the air-dry sample by hydrodistillation procedure in an all glass Clevenger-apparatus. The anti-inflammatory activity was evaluated by carrageenan-induced rat paw edema. The anti-nociceptive action was established from the hot-plate analysis. Statistical analysis was performed using GraphPad Prism (version 7.02). Results: The anti-inflammatory activity of the essential oil was statistically significant (p < 0.001) at 1st and 3rd h for the 100 mg/kg p.o., at 1st-3rd h for the 200/kg mg p.o. and at 3rd and 4th h for the 400 mg/kg p.o. In addition, the 100 mg/kg p.o. showed significant activity (p < 0.01) at 2nd h. Also, the anti-inflammatory activity was significant (p < 0.05) for 100 mg/kg p.o. (4th h), 200 mg/kg p.o. (4th h) and 400 mg/kg p.o (1st h). The essential oil of C. millenii displayed high activity (p <0.001) for all doses in the hot plate anti-nociceptive assay which was time and dose independent. Conclusion: Results demonstrate that the essential oil of C. millenii was effective in the treatment of inflammatory conditions, thereby supporting the traditional use of this herb.


2018 ◽  
Vol 16 (S1) ◽  
pp. S143-S148
Author(s):  
M. Touaibia

This study was designed to evaluate the chemical composition and anti-inflammatory activity of the common myrtle (Myrtus communisL.) essential oil. The composition ofMyrtus communisL. essential oil, extracted by steam distillation, was characterized by a high fraction (80.9%) of oxygenated monoterpenes. The major components were myrtenyl acetate (38.7%), eucalyptol (12.7%), α-pinene (13.7%), and linalool (7.00%). The chemical profile of this essential oil allows us to classify it as myrtényle acétate/α- pinène chemotype, but with atypical proportions, related to the harvesting area. In the carrageenan-induced paw edema, five different groups were established and the essential oil was administered orally in three different doses. The common myrtle essential oil (100 mg/kg) was able to reduce the paw edema, with a comparable effect to that observed with diclofenac (positive control). This is the first report to demonstrate a significant anti-inflammatory activity of Algerian common myrtle essential oil.


Author(s):  
Mahmood Ahmad Khan ◽  
Rafat Sultana Ahmed ◽  
Nilesh Chandra ◽  
Vinod Kumar Arora ◽  
Athar Ali

Background: Rheumatoid Arthritis (RA) is a devastating disease characterized by continual addition of leukocytes and T cells within the articular cavity causing inflammation and cartilage destruction. Withania somnifera is one of the most precious medicinal herbs, reported to have antioxidant, anti‐inflammatory, and immunomodulatory properties. </P><P> Objective: The purpose of this study was to evaluate anti-inflammatory activity of aqueous extract of Withania somnifera roots (WSAq) in Collagen Induced Arthritic (CIA) rats. </P><P> Methods: To achieve this, we assessed the level of inflammatory cytokines such as Tumor Necrosis Factor (TNF)-&#945;, IL-1&#946;, IL-6 and IL-10 in CIA rats. Further, transcription factor, oxidative stress parameters and CD+8 expressions were also analyzed in CIA rats. </P><P> Results: Arthritic rats showed a greater increase in the levels of pro inflammatory cytokines such as TNF-&#945;, IL-1&#946;, IL-6, transcription factor NF-&#954;B and a decrease in IL-10 concentration than controls rats. Oral administration of WSAq at a dose of 300mg/kg.wt. (WSAq300) appreciably attenuated the production of these pro inflammatory cytokines. This anti-inflammatory activity of WSAq300 might be partly mediated through an increase in the secretion of IL-10 and inhibition of NF-&#954;B activity. Further, arthritic rats also show increased oxidative stress as compared to control rats. This increased oxidative stress in the arthritic rats appears to be the outcome of both an activated pro-oxidant and a poor antioxidant defense system. Treatment with WSAq300 strongly ameliorates all these ROS parameters significantly to near normal. Additional, metalloproteinase MMP-8 levels were also measured and found to be increased in CIA rats, which after treatment with WSAq300 came down to near normal. </P><P> Conclusion: From the above results, it can be concluded that the use of WSAq300 may be a valuable supplement which can improve human arthritis.


Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 275 ◽  
Author(s):  
Fanhui Kong ◽  
Bae Lee ◽  
Kun Wei

5-Hydroxymethylfurfural (5-HMF) is found in many food products including honey, dried fruits, coffee and black garlic extracts. Here, we investigated the anti-inflammatory activity of 5-HMF and its underlying mechanisms in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. 5-HMF pretreatment ranging from 31.5 to 126.0 μg/mL reduced the production of nitric oxide (NO), prostaglandin E2 (PGE2) and pro-inflammatory cytokines (TNF-α, IL-1β and IL-6) in a concentration-dependent manner in LPS-stimulated cells. Moreover, 5-HMF-pretreated cells significantly down-regulated the mRNA expression of two major inflammatory mediators, nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and suppressed the production of pro-inflammatory cytokines, as compared with the only LPS-stimulated cells. 5-HMF suppressed the phosphorylation of extracellular regulated protein kinases (ERK1/2), c-Jun N-terminal kinase (JNK), IκBα, NF-κB p65, the mammalian target of rapamycin (mTOR) and protein kinase B (Akt). Besides, 5-HMF was proved to inhibit NF-κB p65 translocation into nucleus to activate inflammatory gene transcription. These results suggest that 5-HMF could exert the anti-inflammatory activity in the LPS-induced inflammatory response by inhibiting the MAPK, NF-κB and Akt/mTOR pathways. Thus, 5-HMF could be considered as a therapeutic ingredient in functional foods.


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