PHARMACODYNAMICS STUDY OF ETHANOL EXTRACT OF CYCLEA BARBATA (MIERS.) LEAVES ON SRF AND COX-2 GASTRIC MICE WITH NSAID GASTROPATHY

Cancer caused uncontrolled cell proliferation and triggered by changes on cell information that regulate growth function. Each cell has different potential so many cancer prevalence such as endometrial cancer, lymph node cancer, lung cancer, skin and mammary gland cancer. The aims of this study were to assess the potential of dragon fruit skin ethanolic extract on white rats (Rattus norvegicus) exposed 7,12- Dimethylbenz(á)antrasena (DMBA) on mammary gland based on histopathological features and cyclooxygenase-2 (Cox-2) intensity. This study were used 20 of rats randomly divided into five group and each groups consisted of four rats, i.e: K+ weren’t treated DMBA and extract; K- were treated with DMBA; P1 were treated with DMBA and extract 10 mg/kg BW; P2 were treated with DMBA and extract 15 mg/kg BW; P3 were treated with DMBA and extract 20 mg/kg BW. The DMBA was given by intra dermal injection during twice a week for five weeks and the extracts with gastric tube everyday till 14 days. The data was analyzed by Anova test and continued with Duncan test. The result showed that the histopathological features were decrease significantly on P3. The variables of Cox-2 intensity were decrease significantly on P1, P2 and P3. Conclusion of this study was ethanol extract of dragon fruit skin can decrease neoplastic indication of mammary gland on white rats (R. norvegicus) based on histopathological features and Cox-2 inhibitors.

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Anti-inflammatory Effects ofScoparia dulcisL. and Betulinic Acid

The American Journal of Chinese Medicine ◽

10.1142/s0192415x11009329 ◽

2011 ◽

Vol 39 (05) ◽

pp. 943-956 ◽

Cited By ~ 38

Author(s):

Jen-Chieh Tsai ◽

Wen-Huang Peng ◽

Tai-Hui Chiu ◽

Shang-Chih Lai ◽

Chao-Ying Lee

Keyword(s):

Betulinic Acid ◽

High Performance ◽

Ethanol Extract ◽

Paw Edema ◽

Scoparia Dulcis ◽

Inflammatory Mechanism ◽

Tnf Α ◽

Cox 2 ◽

Anti Inflammatory ◽

Analytical Result

The aims of this study intended to investigate the anti-inflammatory activity of the 70% ethanol extract from Scoparia dulcis (SDE) and betulinic acid on λ-carrageenan-induced paw edema in mice. The anti-inflammatory mechanism of SDE and betulinic acid was examined by detecting the levels of cyclooxygenase-2 (COX-2), nitric oxide (NO), tumor necrosis factor (TNF-α), interleukin-1β (IL-1β) and malondialdehyde (MDA) in the edema paw tissue and the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione reductase (GRd) in the liver. The betulinic acid content in SDE was detected by high performance liquid chromatography (HPLC). In the anti-inflammatory model, the results showed that SDE (0.5 and 1.0 g/kg) and betulinic acid (20 and 40 mg/kg) reduced the paw edema at 3, 4 and 5 h after λ-carrageenan administration. Moreover, SDE and betulinic acid affected the levels of COX-2, NO, TNF-α and IL1-β in the λ-carrageenan-induced edema paws. The activities of SOD, GPx and GRd in the liver tissue were increased and the MDA levels in the edema paws were decreased. It is suggested that SDE and betulinic acid possessed anti-inflammatory activities and the anti-inflammatory mechanisms appear to be related to the reduction of the levels of COX-2, NO, TNF-α and IL1-β in inflamed tissues, as well as the inhibition of MDA level via increasing the activities of SOD, GPx and GRd. The analytical result showed that the content of betulinic acid in SDE was 6.25 mg/g extract.

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Sargassum fulvellumProtects HaCaT Cells and BALB/c Mice from UVB-Induced Proinflammatory Responses

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/747846 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 4

Author(s):

Chan Lee ◽

Gyu Hwan Park ◽

Eun Mi Ahn ◽

Chan-Ik Park ◽

Jung-Hee Jang

Keyword(s):

Nitric Oxide ◽

Ethanol Extract ◽

Prostaglandin E ◽

Hacat Cells ◽

Uvb Irradiation ◽

Proinflammatory Mediators ◽

Sargassum Fulvellum ◽

Cox 2 ◽

Anti Inflammatory ◽

Skin Damages

Ultraviolet (UV) radiation has been reported to induce cutaneous inflammation such as erythema and edema via induction of proinflammatory enzymes and mediators.Sargassum fulvellumis a brown alga of Sargassaceae family which has been demonstrated to exhibit antipyretic, analgesic, antiedema, antioxidant, antitumor, fibrinolytic, and hepatoprotective activities. The purpose of this study is to investigate anti-inflammatory effects of ethylacetate fraction of ethanol extract ofSargassum fulvellum(SFE-EtOAc) in HaCaT keratinocytes and BALB/c mice. In HaCaT cells, SFE-EtOAc effectively inhibited UVB-induced cytotoxicity (60 mJ/cm2) and the expression of proinflammatory proteins such as cyclooxygenase-2 (COX-2), tumor necrosis factor-α(TNF-α), and inducible nitric oxide synthase (iNOS). Furthermore, SFE-EtOAc significantly reduced UVB-induced production of proinflammatory mediators including prostaglandin E2(PGE2) and nitric oxide (NO). In BALB/c mice, topical application of SFE-EtOAc prior to UVB irradiation (200 mJ/cm2) effectively suppressed the UVB-induced protein expression of COX-2, iNOS, and TNF-αand subsequently attenuated generation of PGE2and NO as well. In another experiment, SFE-EtOAc pretreatment suppressed UVB-induced reactive oxygen species production and exhibited an antioxidant potential by upregulation of antioxidant enzymes such as catalase and Cu/Zn-superoxide dismutase in HaCaT cells. These results suggest that SFE-EtOAc could be an effective anti-inflammatory agent protecting against UVB irradiation-induced skin damages.

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The Inhibition of Ethanol Extract of Phaleria macrocarpa Stem Bark on COX-2 Expression of HCT116 Colorectal Cancer Cell Line

Research Journal of Pharmacy and Technology ◽

10.5958/0974-360x.2019.00489.x ◽

2019 ◽

Vol 12 (6) ◽

pp. 2902

Author(s):

Ratu Shafira Hanifah ◽

Nadia Aida Novitarani ◽

Fadhilah Harmen ◽

Aryo Tedjo ◽

Norma Nur Azizah ◽

...

Keyword(s):

Colorectal Cancer ◽

Cell Line ◽

Cancer Cell ◽

Cancer Cell Line ◽

Ethanol Extract ◽

Stem Bark ◽

Colorectal Cancer Cell ◽

Colorectal Cancer Cell Line ◽

Phaleria Macrocarpa ◽

Cox 2

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Anti-Periodontitis Effect of Ethanol Extracts of Alpinia Katsumadai Seeds

Nutrients ◽

10.3390/nu14010136 ◽

2021 ◽

Vol 14 (1) ◽

pp. 136

Author(s):

Seo Woo Shin ◽

Young Sun Hwang

Keyword(s):

Bone Resorption ◽

Dental Plaque ◽

Cathepsin D ◽

Health Effect ◽

Osteoclast Differentiation ◽

Ethanol Extract ◽

Antibody Array ◽

Oral Keratinocytes ◽

Ongoing Research ◽

Cox 2

Oral microbes are intimately associated with many oral and systemic diseases. Ongoing research is seeking to elucidate drugs that prevent and treat microbial diseases. Various functions of Alpinia Katsumadai seed extracts have been reported such as their anti-viral, anti-oxidant, anti-inflammatory, anti-puritic, anti-emetic, and cytoprotective effects. Here, we investigated the anti-periodontitis effect of an ethanol extract of Alpinia Katsumadai seeds (EEAKSs) on dental plaque bacteria (DPB)-induced inflammation and bone resorption. DPB and Porphyromonas gingivalis (P. gingivalis) were cultured and lipopolysaccharide (LPS) was extracted. Prostaglandin E2 (PGE2) and cyclooxygenase 2 (COX-2) levels were estimated using ELISA. Cytotoxicity was also verified. Proteases were screened using a protease antibody array method. Osteoclastic bone resorption was also investigated. EEAKSs suppressed P. gingivalis growth on agar plates. LPS prepared from dental plaque bacteria (DPB-LPS) and P. gingivalis (PG-LPS) significantly increased PGE2 and COX2 levels in immortalized gingival fibroblasts (IGFs), immortalized human oral keratinocytes (IHOKs), and RAW264.7 macrophage cells. However, DPB-LPS and PG-LPS-induced PGE2 and COX-2 increases were effectively abolished by EEAKS treatment at non-cytotoxic concentrations. In the protease antibody array, matrix metalloproteinase (MMP)-2, MMP-3, MMP-7, kallikrein 10, cathepsin D, and cathepsin V levels were increased by PG-LPS stimulation. However, increases in protease levels except for cathepsin D were suppressed by EEAKS treatment. In addition, RANKL-induced osteoclast differentiation was significantly inhibited by EEAKS treatment, leading to reductions in resorption pit formation. These results suggest that EEAKSs exerted a beneficial oral health effect to help prevent DPB-mediated periodontal disease.

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The Medicinal Timber Canarium patentinervium Miq. (Burseraceae Kunth.) Is an Anti-Inflammatory Bioresource of Dual Inhibitors of Cyclooxygenase (COX) and 5-Lipoxygenase (5-LOX)

ISRN Biotechnology ◽

10.5402/2013/986361 ◽

2013 ◽

Vol 2013 ◽

pp. 1-8 ◽

Cited By ~ 5

Author(s):

R. Mogana ◽

K. Teng-Jin ◽

C. Wiart

Keyword(s):

Inflammatory Diseases ◽

Ethanolic Extract ◽

Ethanol Extract ◽

Frap Assay ◽

Dual Inhibitor ◽

Lead Compounds ◽

Dual Inhibitors ◽

Cox 2 ◽

Cox 1

The barks and leaves extracts of Canarium patentinervium Miq. (Burseraceae Kunth.) were investigated for cyclooxygenase (COX) and 5-lipoxygenase (LOX) inhibition via in vitro models. The corresponding antioxidative power of the plant extract was also tested via nonenzyme and enzyme in vitro assays. The ethanolic extract of leaves inhibited the enzymatic activity of 5-LOX, COX-1, and COX-2 with IC50 equal to 49.66±0.02 μg/mL, 0.60±0.01 μg/mL, and 1.07±0.01 μg/mL, respectively, with selective COX-2 activity noted in ethanolic extract of barks with COX-1/COX-2 ratio of 1.22. The ethanol extract of barks confronted oxidation in the ABTS, DPPH, and FRAP assay with EC50 values equal to 0.93±0.01 μg/mL, 2.33±0.02 μg/mL, and 67.00±0.32 μg/mL, respectively, while the ethanol extract of leaves confronted oxidation in β-carotene bleaching assay and superoxide dismutase (SOD) assay with EC50 value of 6.04±0.02 μg/mL and IC50 value of 3.05±0.01 μg/mL. The ethanol extract acts as a dual inhibitor of LOX and COX enzymes with potent antioxidant capacity. The clinical significance of these data is quite clear that they support a role for Canarium patentinervium Miq. (Burseraceae Kunth.) as a source of lead compounds in the management of inflammatory diseases.

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Anti–Inflammatory and Antioxidant Properties of the Ethanol Extract of Clerodendrum Cyrtophyllum Turcz in Copper Sulfate-Induced Inflammation in Zebrafish

Antioxidants ◽

10.3390/antiox9030192 ◽

2020 ◽

Vol 9 (3) ◽

pp. 192 ◽

Cited By ~ 4

Author(s):

Thu Hang Nguyen ◽

Hong Diep Le ◽

Thanh Nguyen Thi Kim ◽

Hai Pham The ◽

Thi Mai Nguyen ◽

...

Keyword(s):

Oxidative Stress ◽

Antioxidant Properties ◽

Ethanol Extract ◽

Copper Accumulation ◽

Protective Activity ◽

Rheumatic Arthritis ◽

Fluorescent Intensity ◽

Zebrafish Larvae ◽

Cox 2 ◽

Anti Inflammatory

Oxidative stress and inflammation are commonly present in many chronic diseases. These responses are closely related to pathophysiological processes. The inflammatory process can induce oxidative stress and vice versa through the activation of multiple pathways. Therefore, agents with antioxidant and/or anti-inflammatory activities are very useful in the treatment of many pathologies. Clerodendrum cyrthophyllum Turcz, a plant belonging to the Verbenaceae family, is used in Vietnamese traditional medicine for treating migraine, hypertension, inflammation of the throat, and rheumatic arthritis. Despite its usefulness, studies on its biological properties are still scarce. In this study, ethanol extract (EE) of leaves of C. cyrtophyllum showed protective activity against CuSO4 toxicity. The protective activity was proven to relate to antioxidant and anti-inflammatory properties. EE exhibited relatively high antioxidant activity (IC50 of 16.45 µg/mL) as measured by DPPH assay. In an in vivo anti-antioxidant test, three days post fertilization (dpf) zebrafish larvae were treated with different concentrations of EE for 1 h and then exposed to 10 µM CuSO4 for 20 min to induce oxidative stress. Fluorescent probes were used to detect and quantify oxidative stress by measuring the fluorescent intensity (FI) in larvae. FI significantly decreased in the presence of EE at 5 and 20 µg/mL, demonstrating EE’s profound antioxidant effects, reducing or preventing oxidative stress from CuSO4. Moreover, the co-administration of EE also protected zebrafish larvae against oxidative damage from CuSO4 through down-regulation of hsp70 and gadd45bb expression and upregulation of sod. Due to copper accumulation in zebrafish tissues, the damage and oxidative stress were exacerbated overtime, resulting in the upregulation of genes related to inflammatory processes such as cox-2, pla2, c3a, mpo, and pro- and anti-inflammatory cytokines (il-1ß, il-8, tnf-α, and il-10, respectively). However, the association of CuSO4 with EE significantly decreased the expression of cox-2, pla2, c3a, mpo, il-8, and il-1ß. Taken together, the results suggest that EE has potent antioxidant and anti-inflammatory activities and may be useful in the treatment of various inflammatory diseases.

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Boehmeria niveaAttenuates the Development of Dextran Sulfate Sodium-Induced Experimental Colitis

Mediators of Inflammation ◽

10.1155/2014/231942 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 7

Author(s):

Eun Ju Shin ◽

Mi Jeong Sung ◽

Hye Jeong Yang ◽

Myung Sunny Kim ◽

Jin-Taek Hwang

Keyword(s):

Activity Index ◽

Disease Activity Index ◽

Ethanol Extract ◽

Experimental Colitis ◽

Control Group ◽

Untreated Control Group ◽

Colon Tissue ◽

Chemotactic Protein ◽

Cox 2 ◽

Histopathological Score

We examined the therapeutic effect of an ethanol extract derived fromBoehmeria nivea(Linn.) Gaudich in a mouse model of experimental colitis. Treatment with 70% ethanol extract derived fromB. nivea(EBN) at a dose of 100, 200, or 500 mg/(kg·d) improved colon shortening, body weight, the disease activity index (DAI), and histopathological score of DSS-induced colitis mice. DSS significantly increased the levels of cyclooxygenase-(COX-) 2 in colon tissue relative to that of the untreated control group. EBN administered at 100, 200, or 500 mg/(kg·d) reduced COX-2 levels in the DSS-treated mice. In addition, EBN decreased the DSS-induced secretion of the inflammatory cytokine interleukin-6 (IL-6) and chemokine monocyte chemotactic protein-1 (MCP-1). Taken together, these data suggest thatB. niveaextract is effective in preventing colitis.

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Antibacterial, Immunomodulatory, and Lung Protective Effects of Boswelliadalzielii Oleoresin Ethanol Extract in Pulmonary Diseases: In Vitro and In Vivo Studies

Antibiotics ◽

10.3390/antibiotics10121444 ◽

2021 ◽

Vol 10 (12) ◽

pp. 1444

Author(s):

Badriyah Alotaibi ◽

Walaa A. Negm ◽

Engy Elekhnawy ◽

Thanaa A. El-Masry ◽

Walaa S. Elseady ◽

...

Keyword(s):

Gene Expression ◽

Cell Line ◽

Ethanol Extract ◽

Lung Damage ◽

Pulmonary Diseases ◽

Human Skin Fibroblast ◽

Tnf Α ◽

Cox 2

Lung diseases such as asthma, chronic obstructive pulmonary diseases, and pneumonia are causing many global health problems. The COVID-19 pandemic has directed the scientific community’s attention toward performing more research to explore novel therapeutic drugs for pulmonary diseases. Herein, gas chromatography coupled with mass spectrometry tentatively identified 44 compounds in frankincense ethanol extract (FEE). We investigated the antibacterial and antibiofilm effects of FEE against Pseudomonas aeruginosa bacteria, isolated from patients with respiratory infections. In addition, its in vitro immunomodulatory activity was explored by the detection of the gene expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), nitric oxide synthase (iNOS), cycloxygenase-2 (COX-2), and nuclear factor kappa-B (NF-κB) in lipopolysaccharide (LPS)-induced peripheral blood mononuclear cells (PBMC). In addition, its anticancer activity against the A549 lung cancer cell line and human skin fibroblast (HSF) normal cell line was studied. Moreover, the in vivo lung protective potential of FEE was explored histologically and immunohistochemically in mice using a benzo(a)pyrene induced lung damage model. FEE exhibited antibacterial and antibiofilm activities besides the significant inhibition of gene expression of TNFα, IL-6, and NF-κB. FEE also exerted a cytotoxic effect against A549 cell line. Histological and immunohistochemical investigations with morphometric analysis of the mean area percentage and color intensity of positive TNF-α, COX-2, and NF-κB and Bcl-2 reactions revealed the lung protective activity of FEE. This study outlined the promising therapeutic activity of oleoresin obtained from B. dalzielii in the treatment of different pulmonary diseases.

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Hepatoprotective Activity of Pirdot Leaves (Saurauia vulcani Korth) Ethanol Extract in Laboratory Rats (Rattus norvegicus) and Characterization of Bioactive Compounds Using a Molecular Docking Approach

Open Access Macedonian Journal of Medical Sciences ◽

10.3889/oamjms.2021.7624 ◽

2021 ◽

Vol 9 (A) ◽

pp. 1265-1270

Author(s):

Erlintan Sinaga ◽

Syafruddin Ilyas ◽

Salomo Hutahaean ◽

Panal Sitorus

Keyword(s):

Molecular Docking ◽

Binding Affinity ◽

Bioactive Compounds ◽

Ethanol Extract ◽

Treated Group ◽

Hepatoprotective Activity ◽

Tnf Α ◽

Pomolic Acid ◽

Docking Approach ◽

Cox 2

AIM: The hepatoprotective activities of bioactive compounds Pirdot were investigated in vivo and in silico. METHODS: In this study, the completely randomized design non-factorial was experimentally to assess the value of SGPT and SGOT and twenty four adult male rats were divided into four groups : group G0, control group; group G1, a treated group received 0.1 ml sheep red blood cell; group G2, a treated group received 500 mg ethanol extract Pirdot; group G3, a group treated received 500 mg ethanol extract Pirdot and 0,1 ml sheep red blood cell. On thirty one days of treatment, the blood of all rats group were taken to value SGPT and SGOT using DiaLab kit. Furthermore, the molecular docking study was done to analyse molecular interaction that COX-2 and TNF-α were the primary target protein of bioactive compounds of Pirdot associated with hepatoprotective activities. In addition, it tends to be the target of non-steroidal anti-inflammatory drugs such as Ibuprofen. RESULTS: The results show SGOT and SGPT value significantly [p<0.05] decreased on Group G2 and G3. Moreover, the bioactive compounds of Pirdot, such as Pomolic acid and Ursolic acid tend to be the potential compound on liver protection. Moreover, Pomolic acid has a good binding affinity -14.6 kcal mol-1 with COX-2 Protein and the binding affinity of cis-3-O-p-hydroxycinnamoyl Ursolic acid was -15.1 kcal mol-1 associated with TNF-α Protein. CONLUSION: Pirdot Leaves (Saurauia vulcani Korth.) Ethanol Extract showed Hepatoprotective activity in rats (Rattus norvegicus). Molecular docking approach showed that pomolic acid has a good binding affinity with COX-2 Protein and TNF-α Protein.

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