In-vivo edema inhibition of Hyoscyamus albus antioxidant extracts rich in calystegines

Aim: Everyday studies prove the increasing need for newer and safer agents to control cellular inflammatory response, an underlying cause for the pathophysiology of many other clinical cases. Results: Two newly designed sets of schiff 5a-h and chlacone 6a-f substituted pyrazoles were synthesized and evaluated for their in vivo/vitro anti-inflammatory activities. Most potent representatives were chosen for investigation of ulcerogenic and molecular docking properties. Conclusion: The synthesized compounds showed considerable edema inhibition percentage range if compared with celecoxib (13–93% and 58–93%, respectively) at different time intervals. Compound 6e showed the best screening results if compared with celecoxib (inhibition % = 93.62 and 93.51% at 5 h, COX-1/COX-2 selectivity index SI = 215.44 and 308.16 and ulcer index = 7.25 and 8, respectively).

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Synthesis, antiinflammatory activity, and molecular docking studies of bisphosphonic esters as potential MMP-8 and MMP-9 inhibitors

Beilstein Journal of Organic Chemistry ◽

10.3762/bjoc.16.108 ◽

2020 ◽

Vol 16 ◽

pp. 1277-1287

Author(s):

Abimelek Cortes-Pacheco ◽

María Adelina Jiménez-Arellanes ◽

Francisco José Palacios-Can ◽

José Antonio Valcarcel-Gamiño ◽

Rodrigo Said Razo-Hernández ◽

...

Keyword(s):

Molecular Docking ◽

Antiinflammatory Activity ◽

Topical Administration ◽

Positive Control ◽

Oral Route ◽

Docking Studies ◽

Bone Diseases ◽

Bioisosteric Replacement ◽

Edema Inhibition

Bisphosphonic acids (or bisphosphonates) have been successfully used in the clinic treatment of bone diseases for over decades. Additionally, the antiinflammatory activity of these compounds has been gaining attention. In our previous work, we synthesized and in vivo evaluated the bisphosphonic esters 1 and 2, finding a moderate edema inhibition upon oral and topical administration on BALB/c mice. Thus, in this work, the bioisosteric replacement of an amide functional group for an ester afforded the new bisphosphonates 3–6, which had a moderate oral edema inhibition (25 mg/kg dose) and a significant topical antiinflammatory activity (2 mg/ear) on BALB/c mice, with 6 being the most active hit (55.9% edema inhibition), comparable to the positive control (55.5% edema inhibition) on a TPA topical model. Next, to assess the acute toxicity of the synthesized derivatives, test animals were administered with 50–100 mg/kg of 3–6, respectively, by an oral route, and after 14 days, neither lethality nor a significative weight loss were observed. Finally, a structure–activity relationship (SAR) and a molecular docking analysis of 3–6 helped us to explain the trend observed in biological tests. Considering all these aspects, we propose the inhibition of MMP-8 and MMP-9 as a possible action mechanism of the synthesized derivatives.

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Potential Nutraceutical Benefits of In Vivo Grown Saffron (Crocus sativus L.) As Analgesic, Anti-inflammatory, Anticoagulant, and Antidepressant in Mice

Plants ◽

10.3390/plants9111414 ◽

2020 ◽

Vol 9 (11) ◽

pp. 1414

Author(s):

Asif Khan ◽

Nur Airina Muhamad ◽

Hammad Ismail ◽

Abdul Nasir ◽

Atif Ali Khan Khalil ◽

...

Keyword(s):

Capillary Tube ◽

Forced Swim Test ◽

Ethanolic Extract ◽

Crocus Sativus ◽

Herbaceous Plant ◽

Standard Drug ◽

Immobility Time ◽

Anti Inflammatory ◽

Edema Inhibition

Crocus sativus, a medicinally important herbaceous plant, has been traditionally used to cure coughs, colds, insomnia, cramps, asthma, and pain. Moreover, the therapeutic applications of saffron include its immunomodulatory and anticancer properties. The current experimental analysis was performed to explore the potential nutraceutical efficacy of corm, leaf, petal, and stigma of saffron ethanolic extracts as analgesic, anti-inflammatory, anticoagulant, and antidepressant using hot plate, carrageenan-induced paw edema, capillary tube and forced swim test, respectively in mice. The results indicated that among all the extracts, stigma ethanolic extract (SEE) represented maximum latency activity (72.85%) and edema inhibition (77.33%) followed by petal ethanolic extract (PEE) with latency activity and edema inhibition of 64.06 and 70.50%, respectively. Corm ethanolic extract (CEE) and leaf ethanolic extract (LEE) displayed mild analgesic activity of 22.40% and 29.07%, respectively. Additionally, LEE (53.29%) and CEE (47.47%) exhibited mild to moderate response against inflammation. The coagulation time of SEE (101.66 s) was almost equivalent to the standard drug, aspirin (101.66 s), suggesting a strong anticoagulant effect followed by PEE (86.5 s). LEE (66.83 s) represented moderate inhibitory effect on coagulation activity while CEE (42.83 s) showed neutral effect. Additionally, PEE and SEE also expressed itself as potential antidepressants with immobility time ≤76.66 s, while CEE (96.50 s) and LEE (106.83 s) indicated moderate to mild antidepressant efficacy. Based on the in vivo activities, saffron extract, particularly SEE and PEE, can be used as a potential nutraceutical and therapeutic agent due to its significant pharmacological activities.

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Effect of Gooseberry (Physalis angulata) Ethanol Extract in Wistar Rats Carrageenan-Induced Paw Oedema

Global Medical & Health Communication (GMHC) ◽

10.29313/gmhc.v9i1.6336 ◽

2021 ◽

Vol 9 (1) ◽

Author(s):

Ami Nurlatifah ◽

Eka Hendryanny ◽

Yuniarti Yuniarti

Keyword(s):

Test Group ◽

Ethanol Extract ◽

Positive Control ◽

Negative Control ◽

Control Group ◽

Sample Test ◽

Anti Inflammatory ◽

One Way Anova ◽

Edema Inhibition

Gooseberry is an herbaceous plant that contains flavonoids. Flavonoid is one of the secondary metabolites that have an anti-inflammatory effect. This study aims to determine the effect of using ethanol extract of gooseberry as an anti-inflammatory in carrageenan-induced paw edema. This study was in vivo experimental laboratory using a completely randomized design of 25 Wistar rats and divided into five groups. The negative control group was given carboxymethylcellulose. The positive control group has given diclofenac sodium 27 mg/200 gBW. The sample test group has given ethanol extract of gooseberry with 3.6 mg/200 gBW, 5.4 mg/200 gBW, and 7.2 mg/200 gBW dosage. Paw rat’s inflammation induced by injecting carrageenan and measured from 1st to 6th hour using a pletismometer. This study has conducted at Pharmacology Laboratory, Universitas Islam Bandung, and the Laboratory of Therapy and Pharmacology, Universitas Padjajaran, from June to September 2019. The result of average edema volume paw rats using the Kruskal-Wallis test on the 6th hour was p=0.02 (p<0.05). The Mann-Whitney test was p<0.05, showing differences between negative control and positive control and sample test groups. One-way ANOVA test on the percentage of edema inhibition between positive control and sample test group had p=0.107. It shows no significant difference. An effect of ethanol of extract of gooseberries as an anti-inflammatory with the highest percentage of edema inhibition is 5.4 mg/200 gBW dosage. The flavonoid content in gooseberries is thought to inhibit the formation of prostaglandins by inhibiting the cyclooxygenase enzyme. In conclusion, the ethanol extract of gooseberry can be anti-inflammatory. EFEK EKSTRAK ETANOL CIPLUKAN (PHYSALIS ANGULATA) TERHADAP EDEMA TELAPAK KAKI TIKUS GALUR WISTAR YANG DIINDUKSI KARAGENANCiplukan adalah tanaman herbal yang mengandung flavonoid. Flavonoid merupakan salah satu metabolit sekunder yang dapat memberikan efek antiinflamasi. Penelitian ini bertujuan mengetahui pengaruh penggunaan ekstrak etanol ciplukan sebagai antiinflamasi pada tikus yang diinduksi karagenan. Penelitian ini merupakan penelitian laboratorium eksperimental in vivo menggunakan desain rancangan acak lengkap pada 25 ekor tikus galur Wistar yang terbagi ke dalam lima kelompok. Kelompok kontrol negatif diberi carboxymethilcellulose. Kontrol positif diberi sodium diklofenak 27 mg/200 gBB. Kelompok uji diberi ekstrak etanol ciplukan dengan dosis 3,6 mg/200 gBB; 5,4 mg/200 gBB; dan 7,2 mg/200 gBB. Induksi inflamasi dilakukan dengan menginjeksikan karagenan pada telapak kaki tikus, lalu diukur menggunakan pletismometer dari jam ke-1 hingga jam ke-6. Penelitian ini dilakukan di Laboratorium Farmasi, Universitas Islam Bandung dan Laboratorium Farmasi dan Terapi, Universitas Padjajaran dari bulan Juni hingga September 2019. Volume rerata telapak kaki tikus pada jam ke-6 menggunakan Uji Kruskal-Wallis adalah p=0,02 (p<0,05). Hasil Uji Mann-Whitney diperoleh p<0,05 yang menunjukkan terdapat perbedaan bermakna antara kontrol negatif dan kontrol positif serta kelompok uji. Uji one-way ANOVA pada persentase penghambatan edema antara kontrol positif dan kelompok uji diperoleh p=0,107 yang menunjukkan tidak terdapat perbedaan yang bermakna. Terdapat pengaruh ekstrak etanol ciplukan sebagai antiinflamasi dengan persentase penghambatan edema tertinggi pada dosis 5,4 mg/200 gBB. Kandungan flavonoid pada ciplukan diduga mampu menghambat pembentukan prostaglandin dengan menginhibisi enzim siklooksigenase. Simpulan penelitian ini adalah ekstrak etanol ciplukan dapat digunakan sebagai antiinflamasi.

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Anti-Inflammatory Derivatives with Dual Mechanism of Action from the Metabolomic Screening of Poincianella pluviosa

Molecules ◽

10.3390/molecules24234375 ◽

2019 ◽

Vol 24 (23) ◽

pp. 4375 ◽

Cited By ~ 2

Author(s):

Olívia da S. Domingos ◽

Bianca G. V. Alcântara ◽

Mário F. C. Santos ◽

Tatiane C. S. Maiolini ◽

Danielle F. Dias ◽

...

Keyword(s):

Mechanisms Of Action ◽

Complex Mixtures ◽

Pharmacological Properties ◽

In Vivo Experiments ◽

Chromatographic Process ◽

Anti Inflammatory ◽

Dual Mechanism ◽

Edema Inhibition ◽

Metabolomics Analysis

Metabolomics approaches have become fundamental strategies for the analysis of complex mixtures, guiding the isolation of target compounds by focusing on unpublished or promising pharmacological properties. The discovery of novel anti-inflammatory agents is important due to several limitations regarding their potency, efficacy, and adverse effects. Thus, novel anti-inflammatory candidates are essential, aiming to find agents with better mechanisms of action. In this context, extracts from Poincianella pluviosa var. peltophoroides demonstrated significant in vivo anti-inflammatory potential. Thus, metabolomics analysis based on UHPLC-UV-HRFTMS data was performed for the identification of biomarkers with anti-inflammatory properties. Metabolomics-guided chromatographic process led to the isolation of novel compounds 4‴-methoxycaesalpinioflavone and 7-methoxycaesalpinioflavone, as well as known derivatives rhuschalcone VI and caesalpinioflavone. Isolated compounds caused edema inhibition and neutrophil recruitment. Two of them showed better efficacy than reference drugs (indomethacin and dexamethasone). Results of in vivo experiments corroborated those obtained through metabolomics and statistical analyses guiding the isolation of substances of interest.

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Fine Structural Changes in the Microvasculature of the Mouse Pinna: Aging and Radiation Injury

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100050287 ◽

1974 ◽

Vol 32 ◽

pp. 54-55

Author(s):

S. Phyllis Steamer ◽

Rosemarie L. Devine

Keyword(s):

Structural Changes ◽

Radiation Treatment ◽

Arterial Stenosis ◽

Ultrastructural Changes ◽

Vascular Effects ◽

Microvascular Changes ◽

Surrounding Connective Tissue ◽

Fission Neutrons ◽

Total Body

The importance of radiation damage to the skin and its vasculature was recognized by the early radiologists. In more recent studies, vascular effects were shown to involve the endothelium as well as the surrounding connective tissue. Microvascular changes in the mouse pinna were studied in vivo and recorded photographically over a period of 12-18 months. Radiation treatment at 110 days of age was total body exposure to either 240 rad fission neutrons or 855 rad 60Co gamma rays. After in vivo observations in control and irradiated mice, animals were sacrificed for examination of changes in vascular fine structure. Vessels were selected from regions of specific interest that had been identified on photomicrographs. Prominent ultrastructural changes can be attributed to aging as well as to radiation treatment. Of principal concern were determinations of ultrastructural changes associated with venous dilatations, segmental arterial stenosis and tortuosities of both veins and arteries, effects that had been identified on the basis of light microscopic observations. Tortuosities and irregularly dilated vein segments were related to both aging and radiation changes but arterial stenosis was observed only in irradiated animals.

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Induction and Differentiation of Dental Epithelium in Vivo and in Vitro

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100053425 ◽

1982 ◽

Vol 40 ◽

pp. 142-145

Author(s):

E. J. Kollar

Keyword(s):

Connective Tissue ◽

Oral Mucosa ◽

Basal Lamina ◽

Functional Derivatives ◽

Specific Source ◽

Dental Epithelium ◽

Connective Tissue Stroma

The differentiation and maintenance of many specialized epithelial structures are dependent on the underlying connective tissue stroma and on an intact basal lamina. These requirements are especially stringent in the development and maintenance of the skin and oral mucosa. The keratinization patterns of thin or thick cornified layers as well as the appearance of specialized functional derivatives such as hair and teeth can be correlated with the specific source of stroma which supports these differentiated expressions.

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Ultrastructural Correlations between Clonal Human Tumor Colonies and in Vivo Neoplasms

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100053711 ◽

1982 ◽

Vol 40 ◽

pp. 210-211

Author(s):

M.J. Murphy ◽

R.R. Price ◽

J.C. Sloman

Keyword(s):

Cultured Cells ◽

Human Tumor ◽

Cell Type ◽

Tumor Mass ◽

Initial Cell ◽

Cloning Assay ◽

Human Tumor Cloning ◽

The Relationship

The in vitro human tumor cloning assay originally described by Salmon and Hamburger has been applied recently to the investigation of differential anti-tumor drug sensitivities over a broad range of human neoplasms. A major problem in the acceptance of this technique has been the question of the relationship between the cultured cells and the original patient tumor, i.e., whether the colonies that develop derive from the neoplasm or from some other cell type within the initial cell population. A study of the ultrastructural morphology of the cultured cells vs. patient tumor has therefore been undertaken to resolve this question. Direct correlation was assured by division of a common tumor mass at surgical resection, one biopsy being fixed for TEM studies, the second being rapidly transported to the laboratory for culture.

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Structural analysis of the photosynthetic membrane from Ectothiorhodospira halochloris

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s042482010007727x ◽

1983 ◽

Vol 41 ◽

pp. 740-741

Author(s):

H. Engelhardt ◽

R. Guckenberger ◽

W. Baumeister

Keyword(s):

Lattice Structure ◽

Bacterial Species ◽

Hexagonal Lattice ◽

Reaction Centre ◽

Photosynthetic Membrane ◽

Rhodopseudomonas Viridis ◽

Photosynthetic Membranes ◽

Ectothiorhodospira Halochloris ◽

Main Components

Bacterial photosynthetic membranes contain, apart from lipids and electron transport components, reaction centre (RC) and light harvesting (LH) polypeptides as the main components. The RC-LH complexes in Rhodopseudomonas viridis membranes are known since quite seme time to form a hexagonal lattice structure in vivo; hence this membrane attracted the particular attention of electron microscopists. Contrary to previous claims in the literature we found, however, that 2-D periodically organized photosynthetic membranes are not a unique feature of Rhodopseudomonas viridis. At least five bacterial species, all bacteriophyll b - containing, possess membranes with the RC-LH complexes regularly arrayed. All these membranes appear to have a similar lattice structure and fine-morphology. The lattice spacings of the Ectothiorhodospira haloohloris, Ectothiorhodospira abdelmalekii and Rhodopseudomonas viridis membranes are close to 13 nm, those of Thiocapsa pfennigii and Rhodopseudomonas sulfoviridis are slightly smaller (∼12.5 nm).

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The Infection of Cells by Bullet-Shaped Viruses

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100063779 ◽

1969 ◽

Vol 27 ◽

pp. 372-373

Author(s):

Frederick A. Murphy ◽

Alyne K. Harrison ◽

Sylvia G. Whitfield

Keyword(s):

Electron Microscopy ◽

Physical Properties ◽

Host Cell ◽

Thin Section ◽

Cultured Cells ◽

Cell Infection ◽

Thin Section Electron Microscopy ◽

Section Electron ◽

Section Electron Microscopy

The bullet-shaped viruses are currently classified together on the basis of similarities in virion morphology and physical properties. Biologically and ecologically the member viruses are extremely diverse. In searching for further bases for making comparisons of these agents, the nature of host cell infection, both in vivo and in cultured cells, has been explored by thin-section electron microscopy.

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