scholarly journals Berberine-Loaded Carboxylmethyl Chitosan Nanoparticles Ameliorate DSS-Induced Colitis and Remodel Gut Microbiota in Mice

2021 ◽  
Vol 12 ◽  
Author(s):  
Luqing Zhao ◽  
Xueying Du ◽  
Jiaxin Tian ◽  
Xiuhong Kang ◽  
Yuxin Li ◽  
...  
Keyword(s):  
Gut Microbiota ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Triggered Release ◽  
Release Studies ◽  
Anti Inflammatory ◽  
High Concentrations ◽  
Recurrent Inflammation

Inflammatory bowel disease (IBD) is a refractory disorder characterized by chronic and recurrent inflammation. The progression and pathogenesis of IBD is closely related to oxidative stress and irregularly high concentrations of reactive oxygen species (ROS). A new oxidation-responsive nano prodrug was constructed from a phenylboronic esters-modified carboxylmethyl chitosan (OC-B) conjugated with berberine (BBR) that degrades selectively in response to ROS. The optimized micelles exhibited well-controlled physiochemical properties and stability in a physiological environment. OC-B-BBR micelles could effectively encapsulate the anti-inflammatory drug berberine and exhibit ideal H2O2-triggered release behavior as confirmed by in vitro drug loading and release studies. The in vivo anti-inflammatory effect and regulation of gut microbiota caused by it were explored in mice with colitis induced by dextran sodium sulfate (DSS). The results showed that OC-B-BBR significantly ameliorated colitis symptoms and colon damage by regulating the expression levels of IL-6 and remodeling gut microbiota. In summary, this study exhibited a novel BBR-loaded Carboxylmethyl Chitosan nano delivery system which may represent a promising approach for improving IBD treatment.

Ellagitannins, Gallotannins and their Metabolites- The Contribution to the Anti-Inflammatory Effect of Food Products and Medicinal Plants

2019 ◽  
Vol 25 (37) ◽  
pp. 4946-4967 ◽  
Author(s):  
Anna K. Kiss ◽  
Jakub P. Piwowarski
Keyword(s):  
Immune Response ◽  
Gastrointestinal Tract ◽  
Gut Microbiota ◽  
Health Effects ◽  
Biological Effects ◽  
Food Products ◽  
Anti Inflammatory ◽  
The Impact

The popularity of food products and medicinal plant materials containing hydrolysable tannins (HT) is nowadays rapidly increasing. Among various health effects attributable to the products of plant origin rich in gallotannins and/or ellagitannins the most often underlined is the beneficial influence on diseases possessing inflammatory background. Results of clinical, interventional and animal in vivo studies clearly indicate the antiinflammatory potential of HT-containing products, as well as pure ellagitannins and gallotannins. In recent years a great emphasis has been put on the consideration of metabolism and bioavailability of natural products during examination of their biological effects. Conducted in vivo and in vitro studies of polyphenols metabolism put a new light on this issue and indicate the gut microbiota to play a crucial role in the health effects following their oral administration. The aim of the review is to summarize the knowledge about HT-containing products’ phytochemistry and their anti-inflammatory effects together with discussion of the data about observed biological activities with regards to the current concepts on the HTs’ bioavailability and metabolism. Orally administered HT-containing products due to the limited bioavailability of ellagitannins and gallotannins can influence immune response at the level of gastrointestinal tract as well as express modulating effects on the gut microbiota composition. However, due to the chemical changes being a result of their transit through gastrointestinal tract, comprising of hydrolysis and gut microbiota metabolism, the activity of produced metabolites has to be taken into consideration. Studies regarding biological effects of the HTs’ metabolites, in particular urolithins, indicate their strong and structure-dependent anti-inflammatory activities, being observed at the concentrations, which fit the range of their established bioavailability. The impact of HTs on inflammatory processes has been well established on various in vivo and in vitro models, while influence of microbiota metabolites on silencing the immune response gives a new perspective on understanding anti-inflammatory effects attributed to HT containing products, especially their postulated effectiveness in inflammatory bowel diseases (IBD) and cardiovascular diseases.

scholarly journals Interaction between Gut Microbiota and Curcumin: A New Key of Understanding for the Health Effects of Curcumin

Nutrients ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 2499 ◽  
Author(s):  
Beatrice Scazzocchio ◽  
Luisa Minghetti ◽  
Massimo D’Archivio
Keyword(s):  
Gut Microbiota ◽  
Neurological Diseases ◽  
Curcuma Longa ◽  
Pharmacological Activities ◽  
Systemic Bioavailability ◽  
Microbiome Profile ◽  
Regulatory Effects ◽  
High Concentrations

Curcumin, a lipophilic polyphenol contained in the rhizome of Curcuma longa (turmeric), has been used for centuries in traditional Asian medicine, and nowadays it is widely used in food as dietary spice worldwide. It has received considerable attention for its pharmacological activities, which appear to act primarily through anti-inflammatory and antioxidant mechanisms. For this reason, it has been proposed as a tool for the management of many diseases, among which are gastrointestinal and neurological diseases, diabetes, and several types of cancer. However, the pharmacology of curcumin remains to be elucidated; indeed, a discrepancy exists between the well-documented in vitro and in vivo activities of curcumin and its poor bioavailability and chemical instability that should limit any therapeutic effect. Recently, it has been hypothesized that curcumin could exert direct regulative effects primarily in the gastrointestinal tract, where high concentrations of this polyphenol have been detected after oral administration. Consequently, it might be hypothesized that curcumin directly exerts its regulatory effects on the gut microbiota, thus explaining the paradox between its low systemic bioavailability and its wide pharmacological activities. It is well known that the microbiota has several important roles in human physiology, and its composition can be influenced by a multitude of environmental and lifestyle factors. Accordingly, any perturbations in gut microbiome profile or dysbiosis can have a key role in human disease progression. Interestingly, curcumin and its metabolites have been shown to influence the microbiota. It is worth noting that from the interaction between curcumin and microbiota two different phenomena arise: the regulation of intestinal microflora by curcumin and the biotransformation of curcumin by gut microbiota, both of them potentially crucial for curcumin activity. This review summarizes the most recent studies on this topic, highlighting the strong connection between curcumin and gut microbiota, with the final aim of adding new insight into the potential mechanisms by which curcumin exerts its effects.

scholarly journals Anti-Inflammatory Activities of Pentaherbs formula and Its Influence on Gut Microbiota in Allergic Asthma

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2776 ◽  
Author(s):  
Miranda Tsang ◽  
Sau-Wan Cheng ◽  
Jing Zhu ◽  
Karam Atli ◽  
Ben Chan ◽  
...  
Keyword(s):  
Gut Microbiota ◽  
Allergic Asthma ◽  
Herbal Medicines ◽  
Oral Intake ◽  
Allergic Diseases ◽  
Short Chain Fatty Acids ◽  
Mice Model ◽  
Anti Inflammatory

Allergic asthma is a highly prevalent airway inflammatory disease, which involves the interaction between the immune system, environmental and genetic factors. Co-relation between allergic asthma and gut microbiota upon the change of diet have been widely reported, implicating that oral intake of alternative medicines possess a potential in the management of allergic asthma. Previous clinical, in vivo, and in vitro studies have shown that the Pentaherbs formula (PHF) comprising five traditional Chinese herbal medicines Lonicerae Flos, Menthae Herba, Phellodendri Cortex, Moutan Cortex, and Atractylodis Rhizoma possesses an anti-allergic and anti-inflammatory potential through suppressing various immune effector cells. In the present study, to further investigate the anti-inflammatory activities of PHF in allergic asthma, intragastrical administration of PHF was found to reduce airway hyperresponsiveness, airway wall remodeling and goblet cells hyperplasia in an ovalbumin (OVA)-induced allergic asthma mice model. PHF also significantly suppressed pulmonary eosinophilia and asthma-related cytokines IL-4 and IL-33 in bronchoalveolar lavage (BAL) fluid. In addition, PHF modulated the splenic regulatory T cells population, up-regulated regulatory interleukin (IL)-10 in serum, altered the microbial community structure and the short chain fatty acids content in the gut of the asthmatic mice. This study sheds light on the anti-inflammatory activities of PHF on allergic asthma. It also provides novel in vivo evidence that herbal medicines can ameliorate symptoms of allergic diseases may potentially prevent the development of subsequent atopic disorder such as allergic asthma through the influence of the gut microbiota.

scholarly journals Polylactide Nanocapsules Attenuate Adverse Cardiac Cellular Effects of Lyso-7, a Pan-PPAR Agonist/Anti-Inflammatory New Thiazolidinedione

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1521
Author(s):  
Giani M. Garcia ◽  
Jérôme Roy ◽  
Ivan R. Pitta ◽  
Dulcinéia S. P. Abdalla ◽  
Andrea Grabe-Guimarães ◽  
...  
Keyword(s):  
Drug Effects ◽  
Repeated Administration ◽  
Repeated Treatment ◽  
Decay Kinetics ◽  
Cell Contraction ◽  
Cellular Effects ◽  
Anti Inflammatory ◽  
High Concentrations

Lyso-7 is a novel synthetic thiazolidinedione, which is a receptor (pan) agonist of PPAR α,β/δ,γ with anti-inflammatory activity. We investigated the cardiotoxicity of free Lyso-7 in vitro (4.5–450 nM), and Lyso-7 loaded in polylactic acid nanocapsules (NC) in vivo (Lyso-7-NC, 1.6 mg/kg). In previous work, we characterized Lyso-7-NC. We administered intravenously Lyso-7, Lyso-7-NC, control, and blank-NC once a day for seven days in mice. We assessed cell contraction and intracellular Ca2+ transients on single mice cardiomyocytes enzymatically isolated. Lyso-7 reduced cell contraction and accelerated relaxation while lowering diastolic Ca2+ and reducing Ca2+ transient amplitude. Lyso-7 also promoted abnormal ectopic diastolic Ca2+ events, which isoproterenol dramatically enhanced. Incorporation of Lyso-7 in NC attenuated drug effects on cell contraction and prevented its impact on relaxation, diastolic Ca2+, Ca2+ transient amplitude, Ca2+ transient decay kinetics, and promotion of diastolic Ca2+ events. Acute effects of Lyso-7 on cardiomyocytes in vitro at high concentrations (450 nM) were globally similar to those observed after repeated administration in vivo. In conclusion, we show evidence for off-target effects of Lyso-7, seen during acute exposure of cardiomyocytes to high concentrations and after repeated treatment in mice. Nano-encapsulation of Lyso-7 in polymeric NC attenuated the unwanted effects, particularly ectopic Ca2+ events known to support life-threatening arrhythmias favored by stress or exercise.

scholarly journals Formulation, Optimization and In Vivo Evaluation of Fucoidan-Based Cream with Anti-Inflammatory Properties

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 643
Author(s):  
Ekaterina D. Obluchinskaya ◽  
Olga N. Pozharitskaya ◽  
Elena V. Flisyuk ◽  
Alexander N. Shikov
Keyword(s):  
Topical Application ◽  
Colloidal Stability ◽  
High Dose ◽  
In Vivo Evaluation ◽  
Release Studies ◽  
Anti Inflammatory ◽  
Kinetics Of ◽  
Best Fit

Fucoidan is a polysaccharide found in brown alga with glorious potential for pharmacological activities, among which its anti-inflammatory properties have gained meaningful attention. Due to several advantages of formulations for topical application, this study aimed to develop and optimize a fucoidan-based cream formulation and to investigate its anti-inflammatory potential after topical application in vivo. Fucoidan from Fucus vesiculosus L. was used. The cream base consisting of olive oil and Kolliphor RH40 was optimized followed by in vitro agar diffusion and drug release studies. The fucoidan-based cream with 13% Kolliphor P 407, 1% Transcutol P, and 5% PEG400 showed good spreadability, washability, and colloidal stability, and it did not irritate the skin. The kinetics of fucoidan release from the optimized cream exhibited the best fit to the Korsmeyer–Peppas and Higuchi models with R2 > 0.99. Fucoidan release was controlled by drug diffusion and anomalous transport provided by the optimized cream base. The formulation was stable and provided high fucoidan release after storage for 1 year. Topical application of the fucoidan-based cream dose-dependently inhibited carrageenan-induced edema and ameliorated mechanical allodynia in rats. The efficacy of the fucoidan-based cream at a high dose was comparable with the efficacy of diclofenac gel. The fucoidan-based cream could be considered a promising anti-inflammatory formulation.

scholarly journals Enhancement of Osteogenic Induction by LL37 Modified With Collagen Binding Domain in Vitro and in Vivo

2020 ◽  
Author(s):  
Xiaoxuan Lin ◽  
Sipeng Chen ◽  
Jingjing Quan ◽  
Qi Zhang ◽  
Muzi Liao ◽  
...  
Keyword(s):  
Biological Activities ◽  
Drug Loading ◽  
Bone Diseases ◽  
Binding Domain ◽  
Collagen Binding ◽  
Promising Alternative ◽  
Osteogenic Induction ◽  
Anti Inflammatory

Abstract Bone defect diseases, particularly induced by inflammation, render a challenge for designing ideal drug-loading scaffold that could facilitate bone repairing and eliminate inflammatory pathogens. LL37 is considered as promising alternative loading drug due to its broad-spectrum antimicrobial effect and various bio-functions including osteogenic induction. In this study, we synthesized modified LL37 by adding collagen binding domain (CBD), which aim to provide a specific binding onto collagen and slow-releasing pattern. The modified peptide was proved to exhibit similar biological activities to nature LL37 on rat BMSCs including promoting migration activity, anti-inflammatory activity and osteogenic induction in vitro. Ectopic bone formation experiment further confirmed the angiogenesis and osteoinduction activities in vivo. Collectively, LL37-CBD may be a potential loaded drug for preventative and curative applications in Inflammation-induced bone diseases, exerting dual strategies including anti-inflammatory and osteogenic effects.

Liposomes as colloidal nanovehicles: on the road to success in intravenous drug delivery

2018 ◽  
Vol 34 (3) ◽  
pp. 365-383 ◽  
Author(s):  
Sumaira Naeem ◽  
Geetha Viswanathan ◽  
Misni Bin Misran
Keyword(s):  
Drug Delivery ◽  
Drug Loading ◽  
Delivery Systems ◽  
Stimuli Responsive ◽  
Colloidal Systems ◽  
Triggered Release ◽  
The Road ◽  
On The Road

AbstractThe advancement of research in colloidal systems has led to the increased application of this technology in more effective and targeted drug delivery. Nanotechnology enables control over functionality parameters and allows innovations in biodegradable, biocompatible, and stimuli-responsive delivery systems. The first closed bilayer phospholipid system, the liposome system, has been making steady progress over five decades of extensive research and has been efficient in achieving many desirable parameters such as remote drug loading, size-controlling measures, longer circulation half-lives, and triggered release. Liposome-mediated drug delivery has been successful in overcoming obstacles to cellular and tissue uptake of drugs with improved biodistributionin vitroandin vivo. These colloidal nanovehicles have moved on from a mere concept to clinical applications in various drug delivery systems for antifungal, antibiotic, and anticancer drugs.

scholarly journals NF-κB-dependent anti-inflammatory activity of urolithins, gut microbiota ellagic acid-derived metabolites, in human colonic fibroblasts

2010 ◽  
Vol 104 (4) ◽  
pp. 503-512 ◽  
Author(s):  
Antonio González-Sarrías ◽  
Mar Larrosa ◽  
Francisco Abraham Tomás-Barberán ◽  
Piero Dolara ◽  
Juan Carlos Espín
Keyword(s):  
Gut Microbiota ◽  
Ellagic Acid ◽  
Mitogen Activated Protein Kinase ◽  
Protein Levels ◽  
Mitogen Activated Protein ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
The Individual

Previous studies have reported the anti-inflammatory properties of pomegranate extracts, suggesting that ellagitannins (ET) and ellagic acid (EA) are the main anti-inflammatory compounds. However, both ET and EA are metabolised in vivo by the gut microbiota to yield urolithins (Uro) which can be found in the gut and in systemic bloodstream. The present study was carried out to evaluate the individual effect of EA and their microbiota-derived metabolites Uro on colon fibroblasts upon IL-1β treatment as an in vitro inflammation model. Uro-A and Uro-B (10 μm) inhibited PGE2 production (85 and 40 %, respectively) after IL-1β stimulation, whereas EA did not show any effect. Uro-A, but not Uro-B, down-regulated cyclo-oxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1) mRNA expression and protein levels. Both Uro inhibited NF-κB translocation to nucleus. Slight but significant effects were found in the activation of mitogen-activated protein kinase (MAPK) pathways. Uro-A lowered c-Jun N-terminal kinase phosphorylation state, and both Uro inhibited p38 activation. No metabolites derived from Uro or EA were found in the cell media upon incubation of EA or Uro with the cells, and only traces of the compounds were found inside the cells. The present results suggest that Uro, mainly Uro-A, are the main compounds that are responsible for the pomegranate anti-inflammatory properties. The mechanism of action implicated seems to be via the inhibition of activation of NF-κB and MAPK, down-regulation of COX-2 and mPGES-1 expressions, and consequently,via the reduction of PGE2 production. Taking into account that Uro did not enter the cells, a competitive binding for IL-1β membrane receptor cannot be discarded.

scholarly journals A Comparative Review of Autologous Conditioned Serum and Autologous Protein Solution for Treatment of Osteoarthritis in Horses

2021 ◽  
Vol 8 ◽  
Author(s):  
Livia Camargo Garbin ◽  
Michael J. Morris
Keyword(s):  
Interleukin 1 ◽  
Joint Inflammation ◽  
Clinical Results ◽  
Protein Solution ◽  
Autologous Conditioned Serum ◽  
Comparative Review ◽  
Anti Inflammatory ◽  
High Concentrations

Many alternative treatments aimed at modulating osteoarthritis (OA) progression have been developed in the past decades, including the use of cytokine inhibitors. IL-1β is considered one of the most impactful cytokines in OA disease and therefore, its blockage offers a promising approach for the modulation of OA. Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory protein belonging to the IL-1 family that competes with IL-1β for occupancy of its receptors, without triggering the same downstream inflammatory response. Because of its natural anti-inflammatory properties, different methods have been proposed to use IL-1Ra therapeutically in OA. Autologous conditioned serum (ACS) and autologous protein solution (APS) are blood-derived products produced with the use of specialized commercial kits. These processes result in hemoderivatives with high concentrations of IL-1Ra and other cytokines and growth factors with potential modulatory effects on OA progression. Several studies have demonstrated potential anti-inflammatory effect of these therapies with promising clinical results. However, as with any hemoderivatives, clinical outcomes may vary. For optimal therapeutic use, further research is warranted for a more comprehensive understanding of the product's composition and interaction of its components in joint inflammation. Additionally, differences between ACS and APS treatments may not be clear for many clients and clinicians. Thus, the objective of this narrative review is to guide the reader in important aspects of ACS and APS therapies, in vitro and in vivo applications and to compare the use of both treatments in OA.

scholarly journals Green Synthesis of Gold and Iron Nanoparticles for Targeted Delivery: An In Vitro and In Vivo Study

2021 ◽  
Vol 2021 ◽  
pp. 1-16
Author(s):  
Beenish Khanzada ◽  
Nosheen Akthar ◽  
Muhammad Zeeshan Bhatti ◽  
Hammad Ismail ◽  
Mohammed Alqarni ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Medicinal Plants ◽  
Targeted Delivery ◽  
Iron Nanoparticles ◽  
Drug Loading ◽  
Research Work ◽  
Ficus Microcarpa ◽  
Anti Inflammatory

Nanotechnology has vast applications in almost all fields of science and technology. The use of medicinal plants for the synthesis of metallic nanoparticles has gained much attention nowadays. In the current research work, six medicinal plants were used for the synthesis of gold nanoparticles (AuNPs) and iron nanoparticles (FeNPs). The synthesized nanoparticles were characterized by different techniques including UV-visible spectrophotometry, scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR). Furthermore, the activities of green synthesized nanoparticles were screened in vitro using, for example, antibacterial, antioxidant, cytotoxic, and DNA protection assays. Both FeNPs and AuNPs had spherical shapes with an average size less than 50 nm and were found to have good antimicrobial and nontoxic effects. Furthermore, FeNPs from Ficus microcarpa demonstrated high drug loading efficiency (65%) as compared to an anti-inflammatory drug (diclofenac potassium, DFP). We also evaluated the drug delivery potential, as well as anti-inflammatory and anticoagulant properties, of nanoparticles in vivo. Interestingly, AuNPs of Syzygium cumini exhibited strong anti-inflammatory potential as compared to DFP and diclofenac-loaded FeNPs of Ficus microcarpa. The results suggest potential pharmacological applications of biogenic synthesized AuNPs and FeNPs which can be explored further. The study revealed that the green synthesized AuNPs and FeNPs provide a promising approach for the synthesis of drug-loaded nanoparticles and consequently in the field of targeted drug delivery.

Sign in / Sign up

Export Citation Format

Share Document