104,822 research outputs found
Effects of differential extraction of Verbena officinalis on rat models of inflammation, cicatrization and gastric damage
Planta Med. 2007 Mar;73(3):227-35. Epub 2007 Mar 12.
Effects of differential extraction of Verbena officinalis on rat models of inflammation, cicatrization and gastric damage.
Speroni E, Cervellati R, Costa S, Guerra MC, Utan A, Govoni P, Berger A, Müller A, Stuppner H.
Source
Dipartimento di Farmacologia, Università di Bologna, Bologna, Italy. [email protected]
Abstract
Verbena officinalis L. is used in folk medicine for the treatment of inflammatory disorders, skin burns, abrasions, and gastric diseases. Extracts obtained with different solvents (methanol, VoME; enriched flavonoids, VoEF; supercritical CO2, VoCO2) were evaluated for anti-inflammatory, gastroprotective and cicatrizing activities. Additionally, the antioxidant capacity was determined in vitro. In order to confirm the activities investigated, histological observations were performed. All extracts induce a remarkable anti-inflammatory activity. The gastric damage is significantly reduced by all extracts administered, whereby the most pronounced protection is observed for the VoCO2 and VoEF extracts. Finally, a wound healing effect is obtained particularly by the CO2 extract, suggesting the presence of some lipophilic active principles. Histological evidence confirms the results evaluated with the animal procedures. The results obtained after oral administration of V. officinalis extracts are also in agreement with the antioxidant capacity evaluated in vitro, confirming the relationship between pharmacological activities and antiradical efficacy
Effect of Non-Volatile Constituents of Elsholtzia ciliata (Thunb.) Hyl. from Southern Vietnam on Reactive Oxygen Species and Nitric Oxide Release in Macrophages
The extract of Elsholtzia ciliata aerial parts was subjected to bio-guided isolation using the intercellular ROS reduction in J774A.1 macrophages to monitor the anti-oxidative activity. Fifteen compounds were isolated from the active fractions including eleven flavonoids (vitexin, pedalin, luteolin-7-O-β-d-glucopyranoside, apigenin-5-O-β-d-glucopyranoside, apigenin-7-O-β-d-glucopyranoside, chrysoeriol-7-O-β-d-glucopyranoside, 7,3′-dimethoxyluteolin-6-O-β-d-glucopyranoside, luteolin, 5,6,4′-trihydroxy-7,3′-dimethoxyflavone, 5-hydroxy-6,7-dimethoxyflavone (compound 13), 5-hydroxy-7,8-dimethoxyflavone); three hydroxycinnamic acid derivatives (caffeic acid, 4-(E)-caffeoyl-l-threonic acid, 4-O-(E)-p-coumaroyl-l-threonic acid) and one fatty acid (α-linolenic acid). The biological evaluation of these compounds (10–2.5 μm) indicated that all of them exerted good antioxidant and anti-inflammatory activities, in particular compound 13
Unusual secondary metabolites of the aerial parts of dionysia diapensifolia bioss. (primulaceae) and their anti-inflammatory activity
The genus Dionysia, belonging to the Primulaceae family, encompasses more than 50 species worldwide with a center of diversity located in the arid Irano-Turanian mountains. In this study, a phytochemical investigation of the aerial parts of D. diapensifolia Bioss. led to the isolation of 24 phenolic compounds 1–7 and 9–25, and one sesquiterpenoid 8. Compound 1 was identified as new natural product, while isolation of 2 and 3, already known as synthetic products, from a natural source is reported for the first time in the present study. Isolation of compound 8 from a Dionysia species and indeed the whole Primulaceae family is reported for the first time too. Structure elucidation was performed by extensive spectroscopic analyses (1D-, 2D-NMR, and MS), and by comparison with reported literature data. Furthermore, DP4+ chemical shift probability calculations were performed to establish the relative configuration of compound 1. Additionally, subfractions obtained by liquid-liquid extraction of the methanolic extract of the plant, and subsequently the isolated new and selected known compounds 1–4, 6, 8–11 obtained from the diethyl ether subfraction were investigated for their inhibitory effect on NO release and iNOS and COX-2 expression in J774A.1 murine macrophages. The results showed a potential anti-inflammatory activity of the obtained subfractions, of which the diethyl ether subfraction was the most active one in inhibiting NO release and COX-2 expression (p < 0.001). Among the investigated isolated compounds, compound 4 significantly (p < 0.001) inhibited NO release and iNOS and COX-2 expression in a comparable manner like the used positive controls (L-NAME and indomethacin, respectively). Moreover, other isolated substances displayed moderate to high inhibitory activities, illustrating the potential anti-inflammatory activity of Dionysia diapensifolia
Protective effect of Plumericin in inflammatory bowel disease: regulation of inflammatory and oxidative stress response in vitro and in vivo
Inflammatory bowel diseases (IBDs) are characterized by chronic relapsing intestinal inflammation. Although IBDs etiology remains unknown, the mechanisms of inflammation and oxidative stress as well as dysbiotic conditions and aberrations in the epithelial barrier are recognized as involved in the pathogenesis of these diseases [1]. Conventional therapy in IBDs uses anti-inflammatory and immunosuppressive corticosteroids, as well as biological drugs, however, the low remission rate and the severe side effects of these therapies are not satisfactory for IBDs pharmacological treatment. Thus, there is a great need for new drugs with anti-inflammatory and anti-oxidant activities. In this study we evaluated the effect of Plumericin, one of the main bioactive components extracted from the bark of Himatanthus sucuuba (Woodson) on intestinal inflammation, both in vitro, on rat intestinal epithelial cells (IEC-6), and in vivo, in an experimental model of DNBS-induced colitis. Our results indicated that Plumericin significantly reduces pro-inflammatory factors with a pivotal role in IBDs, such as tumor necrosis factor-α (TNF-α) levels, cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) expression and nitrotyrosine formation. Plumericin was also able to inhibit nuclear factor-kB (NF-kB) activation and to reduce reactive oxygen species (ROS) release. Moreover, Plumericin activates the nuclear factor erythroidderived 2 (Nrf2) anti-oxidant pathway and inhibited inflammasomeactivation in IEC-6. The anti-inflammatory and antioxidant effects observed in vitro, associated with a reduced intestinal macroscopic damage, were confirmed in vivo in DNBS-induced colitis in rat. Plumericin shows anti-inflammatory and antioxidant activities at intestinal level and therefore, could be a promising agent the treatment of IBDs. References [1] Naga K.R. Ghattamanenia S K. Panchal LB. Nutraceuticals in rodent models as potential treatments for human Inflammatory Bowel Disease. Pharmacol Res June 2018; 132: 99–107
In vivo efficacy of different extracts of Edelweiss (Leontopodium alpinum Cass.) in animal models
Going Beyond Counting First Authors in Author Co-citation Analysis
The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Wulfenia carinthiaca Jacq., Antioxidant and Pharmacological Activities
Abstract
Relative antioxidant activities of a methanolic extract of three phenylpropanoid glycosides and three iridoid glycosides from Wulfenia carinthiaca were evaluated using the Briggs-Rauscher (BR) reaction method. This method is based on the inhibitory effects by antioxidants on oscillations of the BR reaction. The total extract showed a certain antioxidant activity with respect to resorcinol chosen as standard. The three phenylpropanoid glycosides showed a very high relative antioxidant activity while iridoid glycosides had practically no activity. These experimental results were confirmed by empirical calculations based on the BDE (Bond Dissociation Enthalpy) theory. The total phenolic content was also measured for the phenylpropanoid glycosides using the Folin-Ciocalteu reagent. The obtained values as gallic acid equivalents were in perfect agreement with the relative antioxidant activities. From a pharmacological point of view the results obtained demonstrate that the methanolic extract of W. carinthiaca have antinociceptive and antiedematogenic effects in the different models adopted. The plant extract produced a significant inhibition, dose related, of the rat paw edema induced by carrageenin. The anti-inflammatory activity is probably due to the phenylpropanoid compounds present in the plant. The histological sections of paw tissue in animals treated with Wulfenia carinthiaca extract confirmed the anti-inflammatory effects. The results of the antinociceptive assay indicated a significant reduction on the number of abdominal writhes of mice, induced by acetic acid
The Bag-1 inhibitor, Thio-2, reverses an atypical 3D morphology driven by Bag-1L overexpression in a MCF-10A model of ductal carcinoma in situ
Mammary MCF-10A cells seeded on reconstituted basement membrane form spherical structures with a hollow central lumen termed acini which are a physiologically-relevant model of mammary morphogenesis. Bcl-2 associated athanogene 1 (Bag-1) is a multifunctional protein overexpressed in breast cancer and ductal carcinoma in situ (DCIS). When present in the nucleus Bag-1 is predictive of clinical outcome in breast cancer. Bag-1 exists as three main isoforms, which are produced by alternative translation initiation from a single mRNA. The long isoform of Bag-1, Bag-1L, contains a nuclear localisation sequence not present in the other isoforms. When present in the nucleus Bag-1L, but not the other Bag-1 isoforms, can interact with and modulate the activities of oestrogen, androgen, and vitamin D receptors, Overexpression of Bag-1 mRNA in MCF-10A, is known to produce acini with luminal filling reminiscent of DCIS. As this mRNA predominantly overexpresses the short isoform of Bag-1, Bag-1S, we set out to examine whether the nuclear Bag-1 isoform is sufficient to drive premalignant change by developing a Bag-1L overexpressing MCF-10A model. Two clones differentially overexpressing Bag-1L were grown in 2D and 3D cultures and compared to an established model of HER2-driven transformation. In 2D cultures, Bag-1L overexpression reduced proliferation but did not affect insulin responsiveness or clonogenicity. Acini formed by Bag-1L-overexpressing cells exhibited reduced luminal clearing when compared to controls. An abnormal branching morphology was also observed which correlated with the level of Bag-1L overexpression suggesting further malignant change. Treatment with Thio-2, a small-molecule inhibitor of Bag-1 reduced the level of branching. In summary, 3D cultures of MCF-10A mammary epithelial cells overexpressing Bag-1L demonstrate a premalignant phenotype with features of DCIS. Using this model to test the small molecule Bag-1 inhibitor, Thio-2, reveals its potential to reverse the atypical branched morphology of acini which characterises this premalignant change
Quantitative determination of alkannins and shikonins in endemic Mediterranean Alkanna species
The optical antipodes alkannin/shikonin (A/S) and their esters are potent pharmaceutical substances found in the roots of 150 Boraginaceous species. This study estimated and compared total and free A/S content and A/S enantiomeric ratio in roots of 11 Alkanna species (A. corcyrensis, A. tinctoria, A. pindicola, A. orientalis, A. methanaea, A. calliensis, A. graeca, A. primuliflora, A. stribrnyi, A. sieberi and A. noneiformis) growing wild in various Greek regions, to compare with cultivated species. It also re-characterized the chirality of A/S commercial samples, since most of them were misnamed by the providers. Several Alkanna species were collected (groups 1 and 3) and botanically identified, whereas some Alkanna species were cultivated from collected seeds (group 2). Free A/S and derivatives were extracted from the dried roots of Alkanna species and analyzed by high performance liquid chromatography-diode array detection (HPLC-DAD). For total A/S content the hexane extracts of Alkanna roots were hydrolyzed and analyzed by HPLC-DAD. Chirality determination and A/S enantiomeric ratio estimation was performed for several commercial samples by polarimetry,chiral LC-DAD and circular dichroism studies. Quantitative analysis revealed that A/S content varied from one region to another even within the same species. Most of the cultivated samples contained greater amounts of free and total A/S compared with the wild ones, wheras no difference was observed in A/S enantiomeric ratio. All the Alkanna samples tested contain mainly alkannin derivatives. Some of the examined Alkanna species of the Greek flora that are endemic to the Mediterranean area could serve as alternative sources for medicinally valuable A/S derivatives. Most of the commercial A/S samples tested were misnamed in terms of chirality and re-characterized
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