scholarly journals Germacranolides from Carpesium divaricatum: Some New Data on Cytotoxic and Anti-Inflammatory Activity

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4644
Author(s):  
Natalia Kłeczek ◽  
Janusz Malarz ◽  
Barbara Gierlikowska ◽  
Łukasz Skalniak ◽  
Agnieszka Galanty ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Sesquiterpene Lactones ◽  
Inflammatory Activity ◽  
Human Neutrophils ◽  
Normal Prostate ◽  
Prostate Epithelial Cells ◽  
Tnf Α ◽  
P53 Status ◽  
Anti Inflammatory

Carpesium divaricatum Sieb. & Zucc., a traditional medicinal plant used as an inflammation-relieving remedy, is a rich source of terpenoids. At least 40 germacrane-type sesquiterpene lactones, representatives of four different structural groups, were isolated from the plant. Cytotoxicity against cancer cells in vitro is the most frequently described biological activity of the compounds. However, little is known about the selectivity of the cytotoxic effect. The anti-inflammatory activity of the germacranolides is also poorly documented. The objective of the present study was to assess the cytotoxic activity of selected C. divaricatum germacranolides-derivatives of 4,5,8,9-tetrahydroxy-3-oxo-germacran-6,12-olide towards cancer and normal cell lines (including cells of different p53 status). Moreover, to assess the anti-inflammatory effect of the compounds, the release of four proinflammatory cytokines/chemokines (IL-1β, IL-8, TNF-α and CCL2) by lipopolysaccharide-stimulated human neutrophils was measured by ELISA. The investigated sesquiterpene lactones demonstrated nonselective activity towards prostate cancer (Du145 and PC3) and normal prostate epithelial cells (PNT2) as well as against melanoma cells (A375 and HTB140) and keratinocytes (HaCaT). Cytotoxic activity against osteosarcoma cells was independent of their p53 status. In sub-cytotoxic concentrations (0.5–2.5 µM) the studied compounds significantly decreased cytokine/chemokine release by lipopolysaccharide-stimulated human leukocytes.

scholarly journals In Vitro Antioxidant Activity of Crude Extracts of Harpagophytum Zeyheri and Their Anti-Inflammatory and Cytotoxicity Activity Compared With Diclofenac.

2021 ◽  
Author(s):  
Sibonokuhle F. Ncube ◽  
Lyndy J. McGaw ◽  
Emmanuel Mfotie Njoya ◽  
Hilton G.T. Ndagurwa ◽  
Peter J. Mundy ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Inflammatory Activity ◽  
In Vitro Assays ◽  
Cytotoxicity Activity ◽  
Tnf Α ◽  
Low Toxicity ◽  
Anti Inflammatory ◽  
Ethyl Acetate Extracts

Abstract Background This study evaluated the in vitro antioxidant activity and comparison of anti-inflammatory and cytotoxic activity of Harpagopytum zeyheri with diclofenac. Methods In vitro assays were conducted using water, ethanol and ethyl acetate extracts of H.zeyheri. The antioxidant activity was evaluated using the 2,2'-diphenyl-1-picrylhydrazy (DPPH) and 2,2'- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS)assays. The anti-inflammatory activity was determined by measuring the inhibition of nitric oxide (NO) on lipopolysaccharide (LPS)-induced RAW 264.7 mouse macrophages as well as cytokine (TNF-α and IL-10) expression on LPS-induced U937 human macrophages. For cytotoxicity, cell viability was determined using the 3-(4, 5-dimethylthiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results The ethyl acetate extract had the lowest IC50 values in the DPPH (5.91µg/ml) and ABTS (20.5µg/ml) assay compared to other extracts. Furthermore, the ethyl acetate extracts effectively inhibited NO and TNF-α and proved to be comparable to diclofenac at some concentrations. All extracts of H. zeyheri displayed dose dependent activity and were associated with low levels of human-IL-10 expression compared to quercetin. Furthermore, all extracts displayed low toxicity relative to diclofenac. Conclusions These findings show that H. zeyheri has significant antioxidant activity. Additionally, similarities exist in inflammatory activity of H. zeyheri to diclofenac at some concentrations as well as low toxicity in comparison to diclofenac.

scholarly journals Anti-Inflammatory Activity of Four Triterpenoids Isolated from Poriae Cutis

Foods ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 3155
Author(s):  
Lijia Zhang ◽  
Mengzhou Yin ◽  
Xi Feng ◽  
Salam A. Ibrahim ◽  
Ying Liu ◽  
...  
Keyword(s):  
High Speed ◽  
High Performance ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Dose Dependent

In this study, triterpenoid compounds from Poriae Cutis were separated by high-speed countercurrent chromatography (HSCCC) and identified using ultra-high performance liquid chromatography quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) and nuclear magnetic resonance (NMR). The in vitro anti-inflammatory activities of the purified triterpenoids on RAW 264.7 cells were also investigated. Triterpenoids, poricoic acid B, poricoic acid A, dehydrotrametenolic acid, and dehydroeburicoic acid were obtained; their levels of purity were 90%, 92%, 93%, and 96%, respectively. The results indicated that poricoic acid B had higher anti-inflammatory activity than those of poricoic acid A by inhibiting the generation of NO in lipopolysaccharide (LPS)-induced RAW 264.7 cells. However, dehydrotrametenolic acid and dehydroeburicoic acid had no anti-inflammatory activity. In addition, the production of cytokines (TNF-α, IL-1β, and IL-6) in cells treated with poricoic acid B decreased in a dose-dependent manner in the concentration range from 10 to 40 μg/mL. The results provide evidence for the use of Poriae Cutis as a natural anti-inflammatory agent in medicines and functional foods.

scholarly journals Small molecule therapeutics for COVID-19: repurposing of inhaled furosemide

PeerJ ◽  
2020 ◽  
Vol 8 ◽  
pp. e9533 ◽  
Author(s):  
Zhiyu Wang ◽  
Yanfei Wang ◽  
Prachi Vilekar ◽  
Seung-Pil Yang ◽  
Mayuri Gupta ◽  
...  
Keyword(s):  
Inflammatory Cytokines ◽  
Small Molecule ◽  
Inflammatory Activity ◽  
Health Concern ◽  
Docking Simulations ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Novel Coronavirus ◽  
Pro Inflammatory Cytokines

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.

scholarly journals In Vitro and In Vivo Anti-Inflammatory Activity of Tetrastigma Sulcatum Leaf Extract, Pure Compound and Its Derivatives

2021 ◽  
Author(s):  
Ravindra Jagannath Waghole ◽  
Ashwini Vivek Misar ◽  
Neha Shashikant Kulkarni ◽  
Feroz Khan ◽  
Dattatraya Gopal Naik ◽  
...  
Keyword(s):  
Proinflammatory Cytokines ◽  
Crude Extract ◽  
Leaf Extract ◽  
Inflammatory Activity ◽  
No Production ◽  
Pure Compound ◽  
Tnf Α ◽  
Anti Inflammatory

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.

scholarly journals In vitro antioxidant activity of crude extracts of Harpagophytum zeyheri and their anti-inflammatory and cytotoxicity activity compared with diclofenac

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Sibonokuhle F. Ncube ◽  
Lyndy J. McGaw ◽  
Emmanuel Mfotie Njoya ◽  
Hilton G. T. Ndagurwa ◽  
Peter J. Mundy ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Inflammatory Activity ◽  
In Vitro Assays ◽  
Tnf Α ◽  
Low Toxicity ◽  
Anti Inflammatory ◽  
Ethyl Acetate Extracts ◽  
In Vitro Antioxidant Activity

Abstract Background This study evaluated the in vitro antioxidant activity and comparison of anti-inflammatory and cytotoxic activity of Harpagopytum zeyheri with diclofenac. Methods In vitro assays were conducted using water, ethanol, and ethyl acetate extracts of H.zeyheri. The antioxidant activity was evaluated using the 2,2′-diphenyl-1-picrylhydrazy (DPPH) and 2,2′- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. The anti-inflammatory activity was determined by measuring the inhibition of nitric oxide (NO) on lipopolysaccharide (LPS)-induced RAW 264.7 mouse macrophages as well as cytokine (TNF-α and IL-10) expression on LPS-induced U937 human macrophages. For cytotoxicity, cell viability was determined using the 3-(4, 5-dimethylthiazol- 2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results The ethyl acetate extract had the lowest IC50 values in the DPPH (5.91 μg/ml) and ABTS (20.5 μg/ml) assay compared to other extracts. Furthermore, the ethyl acetate extracts effectively inhibited NO and TNF-α and proved to be comparable to diclofenac at some concentrations. All extracts of H. zeyheri displayed dose-dependent activity and were associated with low levels of human-IL-10 expression compared to quercetin. Furthermore, all extracts displayed low toxicity relative to diclofenac. Conclusions These findings show that H. zeyheri has significant antioxidant activity. Additionally, similarities exist in the inflammatory activity of H. zeyheri to diclofenac at some concentrations as well as low toxicity in comparison to diclofenac.

scholarly journals Preparation of Herbal Formulation for Inflammatory Bowel Disease Based on In Vitro Screening and In Vivo Evaluation in a Mouse Model of Experimental Colitis

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 464 ◽  
Author(s):  
Jaemin Lee ◽  
Han-Seok Choi ◽  
Jinkyung Lee ◽  
Jimin Park ◽  
Sang-Back Kim ◽  
...  
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Inflammatory Activity ◽  
In Vitro Screening ◽  
Screening Experiments ◽  
Tnf Α ◽  
Inflammatory Bowel ◽  
Anti Inflammatory ◽  
Colitis Model

Many medicinal plants have been used traditionally in East Asia for the treatment of gastrointestinal disease and inflammation. The aim of this study was to evaluate the anti-inflammatory activity of 350 extracts (175 water extracts and 175 ethanol extracts) from 71 single plants, 97 mixtures of two plants, and seven formulations based on traditional medicine, to find herbal formulations to treat inflammatory bowel disease (IBD). In the in vitro screening, nitric oxide (NO), tumor necrosis factor (TNF)-α, and interleukin (IL)-6 levels were determined in LPS-treated RAW264.7 cells and the TNF-α induced monocyte-epithelial cell adhesion assay was used for the evaluation of the anti-inflammatory activity of the compounds. Dextran sulfate sodium (DSS)-induced colitis model and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis model were used to evaluate the therapeutic effect against IBD of the samples selected from the in vitro screening. KM1608, composed of Zingiber officinale, Terminalia chebula and Aucklandia lappa, was prepared based on the screening experiments. The oral administration of KM1608 significantly attenuated the severity of colitis symptoms, such as weight loss, diarrhea, and rectal bleeding, in TNBS-induced colitis. In addition, inflammatory mediators, such as myeloperoxidase, TNF-α, and IL-6 levels decreased in the lysate of colon tissues treated with KM1608. Collectively, KM1608 ameliorated colitis through the regulation of inflammatory responses within the colon, which indicated that KM1608 had potential for the treatment of IBD.

scholarly journals Macrophages from Mice Administered Rhus verniciflua Stokes Extract Show Selective Anti-Inflammatory Activity

Nutrients ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 1926 ◽  
Author(s):  
Bo-Geun Kim ◽  
Youngju Song ◽  
Mi-Gi Lee ◽  
Jin-Mo Ku ◽  
So-Jung Jin ◽  
...  
Keyword(s):  
Inflammatory Response ◽  
Intraperitoneal Injection ◽  
Surface Expression ◽  
Inflammatory Activity ◽  
Monocyte Differentiation ◽  
Rhus Verniciflua Stokes ◽  
Rhus Verniciflua ◽  
Tnf Α ◽  
Anti Inflammatory

The bark of Rhus verniciflua Stokes (RVS) is used as a food additive and herbal medicine for various inflammatory disorders and cancer in Eastern Asia. RVS has been shown to exert anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated macrophages in vitro, but whether oral administration of RVS affects the inflammatory response of macrophage needs to be verified. RVS was given orally to mice for ten days. For isolation of macrophages, intraperitoneal injection of thioglycollate was performed. For determination of serum inflammatory response, intraperitoneal injection of LPS was applied. RVS stimulated monocyte differentiation in thioglycollate-induced peritonitis by increasing the population of cells expressing CD11b and class A scavenger receptors. These monocyte-derived macrophages showed an increased uptake of acetylated low-density lipoprotein. When peritoneal macrophages from the RVS group were stimulated with LPS, the levels of tumor necrosis factor (TNF)-α and interleukin (IL)-6 in the supernatant decreased, but the level of IL-12 increased. The surface expression of CD86 was reduced, but surface expression of class II major histocompatibility complex molecules was increased. RVS suppressed the serum levels of LPS-induced TNF-α and IL-6. Collectively, RVS promoted monocyte differentiation upon inflammatory insults and conferred selective anti-inflammatory activity without causing overall inhibitory effects on immune cells.

scholarly journals Anti-Inflammatory Properties, Bioaccessibility and Intestinal Absorption of Sea Fennel (Crithmum maritimum) Extract Encapsulated in Soy Phosphatidylcholine Liposomes

Nutrients ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 210
Author(s):  
Ailén Alemán ◽  
Daniel Marín-Peñalver ◽  
Pilar Fernández de Palencia ◽  
María del Carmen Gómez-Guillén ◽  
Pilar Montero
Keyword(s):  
Chlorogenic Acid ◽  
Cell Monolayer ◽  
Inflammatory Activity ◽  
Polyphenolic Compound ◽  
Gastrointestinal Digestion ◽  
Phosphatidylcholine Liposomes ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Inflammatory Effect

A sea fennel (Crithmum maritimum) aqueous extract was prepared and loaded into soybean phosphatidylcholine liposomes. Both the free extract (FE), and the empty (L) and loaded (L-FE) liposomes were shown to be non-cytotoxic to THP-1 and Caco-2 cells. The anti-inflammatory effect was tested on THP-1 cells differentiated into macrophages. FE showed anti-inflammatory activity, revealed by the induced secretion of IL-10 cytokines in macrophages that were subsequently stimulated with LPS. Also, a decrease in TNF-α production by L was observed, evidencing that liposomes reduced the pro-inflammatory mediators’ secretion. The liposomes (L) showed protective anti-inflammatory activity and also were able to downregulate the inflammation. Furthermore, L-FE were also found to downregulate the inflammation response, as they were able to decrease TNF-α secretion in macrophages previously exposed to LPS. The simulated in vitro gastrointestinal digestion (GID) of FE diminished the chlorogenic acid content (the main polyphenolic compound of the extract) by 40%, while in L-FE, the amount of this phenolic compound increased with respect to the undigested liposomes. The amount of bioaccessible chlorogenic, however, was similar for FE and L-FE. The percentage of chlorogenic acid absorbed through a Caco-2 cell monolayer after 3 h of incubation, was significantly similar for the extract and the liposomes (~1.5%), without finding significant differences once the extract and liposomes were digested.

Synthesis and In Vitro Anti-inflammatory Activity of C20 Epimeric Ocotillol-Type Triterpenes and Protopanaxadiol

Planta Medica ◽  
2018 ◽  
Vol 85 (04) ◽  
pp. 292-301 ◽  
Author(s):  
Jianqiang Zhang ◽  
Qian Zhang ◽  
Yangrong Xu ◽  
Huixiang Li ◽  
Fenglan Zhao ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Prostaglandin E2 ◽  
Interleukin 6 ◽  
Inflammatory Mediator ◽  
Interleukin 10 ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Tnf Α ◽  
Anti Inflammatory

AbstractGinseng is a perennial herb that contains various medicinal substances. The major active constituents of ginseng are ginsenosides, which have multifarious biological activities. Some pharmacological activities are closely dependent on the stereoisomers derived from the configuration at C20. In this study, the in vitro anti-inflammatory activity of C20 epimeric ocotillol-type triterpenes (2, 3, 9, and 10) and protopanaxadiol [20(S/R)-protopanaxadiol] were investigated. Epimers 2 and 3 were prepared starting from 20(S)-protopanaxadiol. Epimers 9 and 10 were synthesized from 20(R)-3-acetylprotopanaxadiol (7). The anti-inflammatory activity of 2, 3, 9, 10, 20(S)-protopanaxadiol, and 20(R)-protopanaxadiol was evaluated in cultured mouse macrophage RAW 264.7 cells. The MTT assay was used to measure the cytotoxicity. RAW 264.7 cells were stimulated by lipopolysaccharide to release the inflammatory mediators nitric oxide, prostaglandin E2, TNF-α, and interleukin-6 and anti-inflammatory mediator interleukin-10. The effect of the compounds on the overproduction of nitric oxide, prostaglandin E2, TNF-α, interleukin-6, and interleukin-10 was determined using Griess and ELISA methods. The results demonstrated that the in vitro anti-inflammatory activities of C20 epimeric ocotillol-type triterpenes and protopanaxadiol were different. Both the 20S-epimers (2 and 3) and 20R-epimers (9 and 10) inhibited the release of inflammatory mediator nitric oxide, while mainly the 20S-epimers inhibited the release of inflammatory mediator prostaglandin E2, and the 20R-epimers inhibited the release of inflammatory cytokine TNF-α. Both the 20S-epimers [2, 3, and 20(S)-protopanaxadiol] and 20R-epimers [9, 10, and 20(R)-protopanaxadiol] inhibited the release of inflammatory cytokine interleukin-6, but mainly the 20S-epimers [2, 3, and 20(S)-protopanaxadiol] increased the release of anti-inflammatory mediator interleukin-10.

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