scholarly journals Safflower Seed Extract Attenuates the Development of Osteoarthritis by Blocking NF-κB Signaling

2021 ◽  
Vol 14 (3) ◽  
pp. 258
Author(s):  
Seong Jae Han ◽  
Min Ju Lim ◽  
Kwang Min Lee ◽  
Eunjeong Oh ◽  
Yu Su Shin ◽  
...  
Keyword(s):  
High Performance ◽  
Therapeutic Agent ◽  
Nuclear Factor Κb ◽  
Cartilage Destruction ◽  
Seed Extract ◽  
Safflower Seed ◽  
The Matrix ◽  
A Disintegrin And Metalloproteinase ◽  
Main Components

Although safflower seed extract exhibits pharmacological activity against various diseases, the effects of its individual compounds on osteoarthritis (OA) have not been elucidated. Here, we evaluated the effects of these extracts and their single compounds on OA. N-(p-Coumaroyl) serotonin and N-feruloyl serotonin, main components of safflower seed extract, were isolated by high-performance liquid chromatography. Under in vitro OA mimic conditions, the expression of the matrix metalloproteinases (MMPs) MMP3/13 and a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS) ADAMTS5 were reduced in mouse chondrocytes treated with safflower seed extract. Furthermore, the oral administration of safflower seed extract attenuated cartilage destruction in a mouse OA model induced by destabilization of the medial meniscus. N-(p-Coumaroyl) serotonin and N-feruloyl serotonin, but not serotonin, reduced MMP3, MMP13, and ADAMTS5 expression in IL-1β-treated chondrocytes. Additionally, they significantly blocked the nuclear factor-κB (NF-κB) pathway by inhibiting IκB degradation and p65 phosphorylation. Our results suggest that safflower seed extract and its single compounds can attenuate cartilage destruction by suppressing MMP and ADMATS5 expression. The anti-arthritic effects are mediated by NF-κB signaling and involve the inhibition of IκB degradation and p65 phosphorylation. These results indicate that safflower seed extract may serve as a novel therapeutic agent against OA.

scholarly journals Vasculoprotective and Neuroprotective Effects of Various Parts of Pomegranate: In Vitro, In Vivo, and Preclinical Studies

2021 ◽  
Author(s):  
Maria Trapali ◽  
Vasiliki Lagouri
Keyword(s):  
Ellagic Acid ◽  
Therapeutic Agent ◽  
Neuroprotective Effect ◽  
Pomegranate Juice ◽  
In Vivo Studies ◽  
Neuroprotective Effects ◽  
Hydrolysable Tannins ◽  
Main Components

Pomegranate (Punica granatum L.) is one of the oldest edible fruits in the Mediterranean area and has been used extensively in the folk medicine. Popularity of pomegranate has increased especially in the last decade because of the health effects of the fruit. Polyphenols, represent the predominant class of phytochemicals of pomegranate, mainly consisting of hydrolysable tannins and ellagic acid. Pomegranate is a rich source of the ellagitannin punicalagin, which has aroused considerable interest in pomegranate fruit as a new therapeutic agent in recent years. Most studies on the effects of pomegranate juice have focused on its ability to cure diabetes and atherosclerosis. The present review summarizes some recent studies on the vasculoprotective and neuroprotective effect of various parts of pomegranate and its main compounds especially hydrolysable tannins ellagitannins, ellagic acid and their metabolites. The in vitro and in vivo studies, showed that the whole parts of pomegranate as well as its main components had a positive influence on blood glucose, lipid levels, oxidation stress and neuro/inflammatory biomarkers. They could be used as a future therapeutic agent towards several vascular and neurodegenerative disorders such as hypertension, coronary heart disease and Alzheimer.

scholarly journals PHARMACOKINETIC STUDY OF MATRIX MEMBRANE MODERATED TRANSDERMAL SYSTEM OF BOSENTAN MONOHYDRATE

2017 ◽  
Vol 10 (9) ◽  
pp. 255
Author(s):  
Revathi Mannam ◽  
Indira Muzib Yallamalli
Keyword(s):  
Controlled Release ◽  
High Performance ◽  
Release Kinetics ◽  
Research Work ◽  
Fold Increase ◽  
Oral Route ◽  
Fickian Diffusion ◽  
Pharmacokinetic Studies ◽  
The Matrix

Objective: The objective of the present research work is to carry out the pharmacokinetic studies of optimized matrix membrane moderatedtransdermal patch of bosentan monohydrate.Materials and Methods: The matrix membrane moderated transdermal system was formulated using HPMC, HPMC K4M and E RLPO. In vitrodiffusion studies were carried out using modified Franz diffusion cell and for the optimized transdermal patch, pharmacokinetic studies were carriedout using New Zealand male rabbits. Plasma samples were quantified using high-performance liquid chromatography.Results: The in vitro diffusion studies revealed that formulation F3 with HPMC K4M and E RLPO had controlled release up to 28 hrs, and a maximumof 95.02±2.68% drug was released. The release kinetics followed mixed order non-Fickian diffusion. The pharmacokinetic studies of the optimizedpatch revealed controlled release up to 45 hrs where a 2.2-fold increase in area under curve (AUC) and 3.8 times increase in mean residence time(MRT) were observed compared to oral route. The results were appeared to be significant at p≤0.05. The variation in half-life was found to be notstatistically significant when compared between oral and transdermal routes.Conclusion: The pharmacokinetic results concluded that the matrix membrane moderated transdermal system with extended AUC and MRT canenhance the bioavailability of bosentan monohydrate by minimizing the drug-related side effects in oral route.

scholarly journals Schisandrol A Suppresses Catabolic Factor Expression by Blocking NF-κB Signaling in Osteoarthritis

2021 ◽  
Vol 14 (3) ◽  
pp. 241
Author(s):  
Seong Jae Han ◽  
Jimoon Jun ◽  
Seong-il Eyun ◽  
Choong-Gu Lee ◽  
Jimin Jeon ◽  
...  
Keyword(s):  
Therapeutic Agent ◽  
Cartilage Destruction ◽  
Dependent Manner ◽  
Oral Gavage ◽  
Osteoarthritic Cartilage ◽  
Surgical Model ◽  
Dose Dependent ◽  
Cox2 Expression

Schisandrol A possesses pharmacological properties and is used to treat various diseases; however, its effects on osteoarthritis (OA) progression remain unclear. Here, we investigated Schisandrol A as a potential therapeutic agent for OA. In vitro, Schisandrol A effects were confirmed based on the levels of expression of catabolic factors (MMPs, ADAMTS5, and Cox2) induced by IL-1β or Schisandrol A treatment in chondrocytes. In vivo, experimental OA in mice was induced using a destabilized medial meniscus (DMM) surgical model or oral gavage of Schisandrol A in a dose-dependent manner, and demonstrated using histological analysis. In vitro and in vivo analyses demonstrated that Schisandrol A inhibition attenuated osteoarthritic cartilage destruction via the regulation of Mmp3, Mmp13, Adamts5, and Cox2 expression. In the NF-κB signaling pathway, Schisandrol A suppressed the degradation of IκB and the phosphorylation of p65 induced by IL-1β. Overall, and Schisandrol A reduced the expression of catabolic factors by blocking NF-κB signaling and prevented cartilage destruction. Therefore, Schisandrol A attenuated OA progression, and can be used to develop novel OA drug therapies.

scholarly journals In Vitro Antiacne and Antidandruff activity of extracted stigmasterol from seed waste of safflower (Carthamus tinctorius L.)

2019 ◽  
Vol 6 (sp1) ◽  
pp. 568-574 ◽  
Author(s):  
Monika Chaudhary ◽  
Vartika Verma ◽  
Nidhi Srivastava
Keyword(s):  
High Performance ◽  
Carthamus Tinctorius ◽  
Diffusion Method ◽  
Safflower Seed ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Preliminary Study ◽  
Waste Extract ◽  
Layer Chromatography

The present study deals with extraction of saponins and their characterization from the seed wastes of safflower. The presence of stigmasterol in the extracted safflower seed waste (S.W.S) was confirmed by Thin Layer Chromatography (TLC), followed by Fourier-Transform Infrared Spectroscopy (FTIR) and High Performance Liquid Chromatography (HPLC) on the basis of its peak compared with stigmasterol standard. FTIR showed the identical functional groups of butanolic extract of SSW with standard while TLC and HPLC showed their notable peak and retention time with the same. Further in-vitro antiacne and antidandruff microbial activity of extracted stigmasterol was confirmed by disc diffusion method. This preliminary study has exhibited anti-acne and anti dandruff potential of Safflower seed waste extract, in future which could be used in therapies and cosmetic applications.

scholarly journals Lycorine Suppresses Endplate-Chondrocyte Degeneration and Prevents Intervertebral Disc Degeneration by Inhibiting NF-κB Signalling Pathway

2018 ◽  
Vol 45 (3) ◽  
pp. 1252-1269 ◽  
Author(s):  
Gangliang Wang ◽  
Kangmao Huang ◽  
Yangxin Dong ◽  
Shuai Chen ◽  
Jianfeng Zhang ◽  
...  
Keyword(s):  
Intervertebral Disc ◽  
Disc Degeneration ◽  
High Performance ◽  
Underlying Mechanism ◽  
Nuclear Factor Κb ◽  
Inhibitory Effect ◽  
Cell Degeneration ◽  
Ivd Degeneration ◽  
Protease Expression

Background/Aims: Cartilaginous endplate (CEP) degeneration is an important cause for intervertebral disc (IVD) degeneration that leads to low-back pain. The identification of compounds that may prevent CEP degeneration is of interest for the prevention of IVD degeneration. Methods: Catabolic protease expression in the CEP of disc degeneration patients was first assessed. The toxicity, function and underlying mechanism of lycorine (LY) on CEP-derived chondrocytes degeneration were assessed in vitro by flow cytometry analysis and western blotting. The concentration and function of LY in rat-tail disc-degeneration models were also assessed by HPLC (High Performance Liquid Chromatography) quantification and histological analysis. Results: In CEP cells, Interleukin (IL)-1β upregulated the expression of matrix metalloproteinase (MMP)-3, MMP-13, a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS)-4 and ADAMTS-5 that is critical for the degradation of cartilage extracellular matrix. Interestingly, LY suppressed the expression of these enzymes via the inhibition of nuclear factor-κB (NFκB) signalling and thus prevented IL-1β-induced endplate cell degeneration in vitro. More importantly, LY also reduced the expression of MMP-3, MMP-13, ADAMTS-4 and ADAMTS-5 in CEP and exerted a protective effect on both CEP and nucleus pulposus (NP) degeneration. In addition to its inhibitory effect on matrix-degrading protease expression, LY treatment also reduced positive regulators of proinflammatory cytokines, such as MIF, which can be secreted by CEP cells and subsequently target NP cells. Conclusion: LY could serve as a potential drug for treating IVD disease.

Biocompatible Delivery System for Metformin: Characterization, Radiolabeling and In Vitro Studies

2020 ◽  
Vol 20 (13) ◽  
pp. 1626-1634 ◽  
Author(s):  
Burcu Aydın ◽  
Eser Uçar ◽  
Volkan Tekin ◽  
Çiğdem İçhedef ◽  
Serap Teksöz
Keyword(s):  
Breast Cancer ◽  
Liver Cancer ◽  
Cancer Cell ◽  
High Performance ◽  
Cancer Cell Line ◽  
In Vitro Studies ◽  
Biological Behavior ◽  
Size And Morphology ◽  
Main Components

Background: In recent years, the uses of nanotechnology in medicine have an increasing potential as an effective nanocarrier system. These systems are improved with the purpose of maximizing therapeutic activity and minimizing undesirable side-effects. Moreover, radiolabeled nanoparticles can be used as agents for diagnosis and therapeutic purposes in clinical applications. They have three main components: the core, the targeting biomolecule, and the radionuclide. Objective: It is aimed to synthesize Metformin (MET) loaded Solid Lipid Nanoparticles (MET-SLN) and radiolabeled with technetium-99m tricarbonyl core. Methods: The structure of synthesized nanoparticles was characterized by Fourier Transform Infrared Spectroscopy (FTIR). The particle size and morphology of nanoparticles were examined by Dynamic Light Scattering (DLS), and Scanning Electron Microscope (SEM). Quality control studies of radiolabeled MET-SLN [99mTc(CO)3-MET-SLN] were performed by High-Performance Liquid Radiochromatography (HPLRC) and Thin Layer Radiochromatography (TLRC). Results: The radiolabeling yield of [99mTc(CO)3-MET-SLN] was found to be 88%. In vitro studies have been performed on cancer lines(MCF7, MDA-MD-231 breast, and HEPG2 liver cancer cells) to determine the biological behavior of 99mTc(CO)3-MET-SLNs. Conclusion: The results showed that higher uptake values were observed on estrogen-positive MCF7 breast cancer cell line according to estrogen negative MDA-MB-231 breast cancer and HEPG2 liver cancer cell lines.

scholarly journals In vitro and in vivo anti-inflammatory properties of Mayan propolis

2020 ◽  
Vol 18 ◽  
pp. 205873922093528
Author(s):  
Jorge Xool-Tamayo ◽  
Ivan Chan-Zapata ◽  
Víctor Ermilo Arana-Argaez ◽  
Fabiola Villa-de la Torre ◽  
Julio César Torres-Romero ◽  
...  
Keyword(s):  
Inflammatory Cytokines ◽  
High Performance ◽  
Enzyme Linked Immunosorbent Assay ◽  
Thiazolyl Blue Tetrazolium Bromide ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Main Components ◽  
Macrophage Viability

Introduction Propolis has been used traditionally for different human diseases and even recently as dental biomaterials because of its antibacterial, antimycotic, and anti-inflammatory properties. However, a proper correlation between in vitro and in vivo anti-inflammatory properties has not been clearly established. Methods The composition of propolis was determined by high-performance liquid chromatography–ultraviolet mass spectrometry (HPLC-UV-MS). Viability of ethanolic propolis solution was evaluated by thiazolyl blue tetrazolium bromide (MTT) assay on murine macrophages. The anti-inflammatory properties were assessed both in vitro through the enzyme-linked immunosorbent assay (ELISA) quantification of various cytokines and in vivo by induced edemas. Results Chemical analysis showed pinocembrin, pinobanksin-3-O-acetate, and pinobanksin-3-O-propionate as the main components of propolis. Macrophage viability was high (106%) when propolis was used up to 50 µg/mL. ELISA studies showed a reduction in the expression of pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α) up to 145 pg/mL, 350 pg/mL, and 210 pg/mL, respectively, while the anti-inflammatory cytokines (IL-10 and IL-4) were increased up to 833 pg/mL and 446 pg/mL. Finally, edema was reduced on paw and ear mice by 9% and 22%, respectively. Conclusion Mayan propolis has strong in vitro anti-inflammatory properties without compromising macrophage viability, resulting in a low-to-mild in vivo anti-inflammatory response.

scholarly journals In Vitro Study of the Bioavailability and Bioaccessibility of the Main Compounds Present in Ayahuasca Beverages

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5555
Author(s):  
Joana Gonçalves ◽  
Miguel Castilho ◽  
Tiago Rosado ◽  
Ângelo Luís ◽  
José Restolho ◽  
...  
Keyword(s):  
High Performance ◽  
Cell Monolayer ◽  
In Vitro Study ◽  
In Vitro Digestion ◽  
Array Detector ◽  
Digestion Process ◽  
Commercial Mixture ◽  
The Matrix ◽  
Cell Incubation

Ayahuasca is a psychoactive beverage that contains the psychoactive compound N,N-dimethyltryptamine and β-carboline alkaloids. This study aims at determining in vitro the bioavailability and bioaccessibility of the main compounds present in decoctions of four individual plants, in a commercial mixture and in four mixtures of two individual plants used in the preparation of Ayahuasca. The samples were subjected to an in vitro digestion process, and the Caco-2 cell line was used as an absorption model. The integrity and permeability of the cell monolayer were evaluated, as well as the cytotoxicity of the extracts. After digestion and cell incubation, the compounds absorbed by the cell monolayer were quantified by high-performance liquid chromatography coupled to a diode array detector. The results showed that compounds such as N,N-dimethyltryptamine, Harmine, Harmaline, Harmol, Harmalol and Tetrahydroharmine were released from the matrix during the in vitro digestion process, becoming bioaccessible. Similarly, some of these compounds, after being incubated with the cell monolayer, were absorbed, becoming bioavailable. The extracts did not show cytotoxicity after cell incubation, and the integrity and permeability of the cell monolayer were not compromised.

Controlled Drug Releasing Intravitreal Implant Using Biodegradable PLGA

2003 ◽  
Author(s):  
Juyoung Park ◽  
Murad Melhem ◽  
Desai Pankaj ◽  
Ronald W. Millard ◽  
Rupak K. Banerjee
Keyword(s):  
High Performance Liquid Chromatography ◽  
Release Rate ◽  
High Performance ◽  
Mixed Type ◽  
Intravitreal Implant ◽  
Solvent Cast ◽  
Different Types ◽  
The Matrix ◽  
Phosphate Buffered Saline

The goal of this work is to compare the in vitro drug (Nimodipine) release rate from three different types (matrix, reservoir, and combination types) of intravitreal implants using a biodegradable polymer (PLGA). The matrix implants were prepared by a solvent cast method and the reservoir implants were fabricated by using a pellet press. The combination implants were a mixed type of matrix and reservoir implants. Each implant was placed in a vial with 7mL of Phosphate Buffered Saline (PBS) containing 0.4 g/L of Bovine Serum Albumin (BSA) and 0.5 mL aliquots were removed for the drug assay for 25 days. The sample was analyzed to determine the concentration using High Performance Liquid Chromatography (HPLC). Over 20 days, the average steady state release rate in vitro is 13.05±6.17, 2.66±1.98, 8.85±6.36 μg/day for matrix, reservoir, and combination implants, respectively.

Morphology of High-Performance Rigid-Rod Polymer Fibers and Molecular Composites

1989 ◽  
Vol 47 ◽  
pp. 338-339
Author(s):  
W.W. Adams ◽  
S. J. Krause
Keyword(s):  
Tensile Strength ◽  
High Performance ◽  
Liquid Crystalline ◽  
Molecular Level ◽  
Synergistic Effects ◽  
Tensile Modulus ◽  
Commercial Development ◽  
The Matrix ◽  
Molecular Composites ◽  
Rigid Rod

Rigid-rod polymers such as PBO, poly(paraphenylene benzobisoxazole), Figure 1a, are now in commercial development for use as high-performance fibers and for reinforcement at the molecular level in molecular composites. Spinning of liquid crystalline polyphosphoric acid solutions of PBO, followed by washing, drying, and tension heat treatment produces fibers which have the following properties: density of 1.59 g/cm3; tensile strength of 820 kpsi; tensile modulus of 52 Mpsi; compressive strength of 50 kpsi; they are electrically insulating; they do not absorb moisture; and they are insensitive to radiation, including ultraviolet. Since the chain modulus of PBO is estimated to be 730 GPa, the high stiffness also affords the opportunity to reinforce a flexible coil polymer at the molecular level, in analogy to a chopped fiber reinforced composite. The objectives of the molecular composite concept are to eliminate the thermal expansion coefficient mismatch between the fiber and the matrix, as occurs in conventional composites, to eliminate the interface between the fiber and the matrix, and, hopefully, to obtain synergistic effects from the exceptional stiffness of the rigid-rod molecule. These expectations have been confirmed in the case of blending rigid-rod PBZT, poly(paraphenylene benzobisthiazole), Figure 1b, with stiff-chain ABPBI, poly 2,5(6) benzimidazole, Fig. 1c A film with 30% PBZT/70% ABPBI had tensile strength 190 kpsi and tensile modulus of 13 Mpsi when solution spun from a 3% methane sulfonic acid solution into a film. The modulus, as predicted by rule of mixtures, for a film with this composition and with planar isotropic orientation, should be 16 Mpsi. The experimental value is 80% of the theoretical value indicating that the concept of a molecular composite is valid.

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