scholarly journals Study of resveratrol against bone loss by using in-silico and in-vitro methods

2023 ◽  
Vol 83 ◽  
Author(s):  
S. R. Abbas ◽  
R. T. Khan ◽  
S. Shafique ◽  
S. Mumtaz ◽  
A. A. Khan ◽  
...  
Keyword(s):  
Bone Loss ◽  
In Silico ◽  
Bioactive Compound ◽  
Drug Preparation ◽  
Glass Coverslip ◽  
Rhodamine Phalloidin ◽  
Trimethyl Ether ◽  
Macrophage Colony ◽  
Triton X

Abstract By applying the in-silico method, resveratrol was docked on those proteins which are responsible for bone loss. The Molecular docking data between the resveratrol and Receptor activator of nuclear factor-kappa-Β ligand [RANKL] receptors proved that resveratrol binds tightly to the receptors, showed the highest binding affinities of −6.9, −7.6, −7.1, −6.9, −6.7, and −7.1 kcal/mol. According to in-vitro data, Resveratrol reduced the osteoclasts after treating Marrow-Derived Macrophages [BMM] with Macrophage colony-stimulating factor [MCSF] 20ng / ml and RANKL 50ng / ml, with different concentrations of resveratrol (2.5, 10 μg / ml) For 7 days, the cells were treated with MCSF (20 ng / ml) and RANKL (40 ng / ml) together with concentrated trimethyl ether and resveratrol (2.5, 10 μg / ml) within 12 hours. Which, not affect cell survival. After fixing osteoclast cells with formaldehyde fixative on glass coverslip followed by incubation with 0.1% Triton X-100 in PBS for 5 min and after that stain with rhodamine phalloidin staining for actin and Hoechst for nuclei. Fluorescence microscopy was performed to see the distribution of filaments actin [F.actin]. Finally, resveratrol reduced the actin ring formation. Resveratrol is the best bioactive compound for drug preparation against bone loss.

Elevation of fibrinogen due to loss of ovarian function enhances actin ring formation and leads to increased bone resorption

2012 ◽  
Vol 303 (11) ◽  
pp. E1296-E1303 ◽  
Author(s):  
Ke Ke ◽  
Woon-Ki Kim ◽  
Ok-Joo Sul ◽  
Van Tien Phan ◽  
Mi-Hyun Lee ◽  
...  
Keyword(s):  
Bone Resorption ◽  
Bone Loss ◽  
Ovarian Function ◽  
Annexin V ◽  
Ring Formation ◽  
Tartrate Resistant Acid Phosphatase ◽  
Actin Ring ◽  
Macrophage Colony ◽  
And Function

The aim of the present study was to evaluate the effect of fibrinogen on number and function of osteoclasts (OC) consequently resulting in bone loss. It was hypothesized that the enhanced level of released fibrinogen due to loss of ovarian function caused bone loss by acting on OCs. Bone loss was induced by ovariectomy (OVX) in mice and analyzed by micro-CT. The effect of fibrinogen on OCs was evaluated by tartrate-resistant acid phosphatase, annexin V, actin staining, pit formation observed on dentine slices, and Western blotting. Exogenous fibrinogen increased OC survival, actin ring formation, and bone resorption in vitro. The effect of fibrinogen was dependent on β3-integrin, which is a marker for mature OCs. Fibrinogen induced the activation of transforming oncogene from Ak strain (Akt), Ras-related C3 botulinum toxin substrate 1 (Rac1), and Rho family of GTPase (Rho) and the degradation of the Bcl-2 interacting mediator of cell death (Bim) in a manner similar to macrophage colony-stimulating factor (M-CSF). OVX increased plasma fibrinogen and serum M-CSF together with elevated actin ring formation and bone loss. The increased fibrinogen level due to loss of ovarian function may contribute, at least partly, to bone loss through the enhanced number and activity of OCs.

scholarly journals Engineering of L-Plastin Peptide-Loaded Biodegradable Nanoparticles for Sustained Delivery and Suppression of Osteoclast Function In Vitro

2019 ◽  
Vol 2019 ◽  
pp. 1-13 ◽  
Author(s):  
Sunipa Majumdar ◽  
Aniket S. Wadajkar ◽  
Hanan Aljohani ◽  
Mark A. Reynolds ◽  
Anthony J. Kim ◽  
...  
Keyword(s):  
Bone Resorption ◽  
Bone Loss ◽  
Sustained Release ◽  
Double Emulsion ◽  
Small Molecular Weight ◽  
Rhodamine Phalloidin ◽  
Amino Terminal ◽  
Osteoclast Function

We have recently demonstrated that a small molecular weight amino-terminal peptide of L-plastin (10 amino acids; “MARGSVSDEE”) suppressed the phosphorylation of endogenous L-plastin. Therefore, the formation of nascent sealing zones (NSZs) and bone resorption are reduced. The aim of this study was to develop a biodegradable and biocompatible PLGA nanocarrier that could be loaded with the L-plastin peptide of interest and determine the efficacy in vitro in osteoclast cultures. L-plastin MARGSVSDEE (P1) and scrambled control (P3) peptide-loaded PLGA-PEG nanoparticles (NP1 and NP3, respectively) were synthesized by double emulsion technique. The biological effect of nanoparticles on osteoclasts was evaluated by immunoprecipitation, immunoblotting, rhodamine-phalloidin staining of actin filaments, and pit forming assays. Physical characterization of well-dispersed NP1 and NP3 demonstrated ~130-150 nm size, < 0.07 polydispersity index, ~-3 mV ζ-potential, and a sustained release of the peptide for three weeks. Biological characterization in osteoclast cultures demonstrated the following: NP1 significantly reduced (a) endogenous L-plastin phosphorylation; (b) formation of NSZs and sealing rings; (c) resorption. However, the assembly of podosomes which are critical for cell adhesion was not affected. L-plastin peptide-loaded PLGA-PEG nanocarriers have promising potential for the treatment of diseases associated with bone loss. Future studies will use this sustained release of peptide strategy to systematically suppress osteoclast bone resorption activity in vivo in mouse models demonstrating bone loss.

scholarly journals In silico and in vitro assessment on antidiabetic efficacy of secondary metabolites from Syzygium cumini (L.) Skeels

2016 ◽  
Vol 3 (4) ◽  
pp. 360
Author(s):  
Twinkle Sunder Bansode ◽  
Amit Gupta ◽  
B K Salalkar
Keyword(s):  
Secondary Metabolites ◽  
Ellagic Acid ◽  
In Silico ◽  
Ethanol Extract ◽  
Bioactive Compound ◽  
Alpha Amylase ◽  
Herbal Remedies ◽  
Syzygium Cumini ◽  
Standard Drug

India ranks high for prevalence of diabetes and the treatment of diabetes without any side effects is still challenging. Though herbal remedies help reduce the side effect, proper standardization of phytochemical which prove as a bioactive compound, its proper dose and clinical trials are lacking. In our investigation, we studied the binding mechanism of the secondary metabolites of Syzygium cumini, their in vitro antidiabetic activity and the number of phytochemicals present. In silico study revealed that ellagic acid has a potential to modulate the carbohydrate metabolizing enzyme activity showing higher affinity for the enzymes with much lesser binding energy, -4.73 kcal/mol for alpha amylase, -4.87 kcal/mol for beta-glucosidase, -4.79 kcal/mol for glycogen synthase kinase, -4.18 kcal/mol for glucokinase and -4.49 kcal/mol for alpha-glucosidase. In vitro-Alpha amylase inhibitory activity assay showed that ethanol extract has the highest value of percent inhibition (73.33%) as compared to standard drug Acarbose (65.99%). Finally, TLC analysis cleared that ethanol extract contains five compounds one of which may be a bioactive compound, ellagic acid. Further purification and characterization of the ellagic acid is needed.

scholarly journals Inhibition of human thrombin by the constituents of licorice: inhibition kinetics and mechanistic insights through in vitro and in silico studies

RSC Advances ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 3626-3635 ◽  
Author(s):  
Cheng-Cheng Shi ◽  
Tian-Ran Chen ◽  
Qi-Hua Zhang ◽  
Ling-Hua Wei ◽  
Chao Huang ◽  
...  
Keyword(s):  
In Silico ◽  
Bioactive Compound ◽  
Inhibition Kinetics ◽  
Strong Inhibition ◽  
Licochalcone A ◽  
In Silico Studies ◽  
Human Thrombin ◽  
Inhibition Of Thrombin

Licochalcone A, a bioactive compound from licorice, displayed strong inhibition of thrombin.

IN VITRO/IN SILICO CHARACTERIZATION OF ACTIVE AND PASSIVE STRESSES IN CARDIAC MUSCLE

2012 ◽  
Vol 10 (2) ◽  
pp. 171-188 ◽  
Author(s):  
Markus Boel ◽  
Oscar J. Abilez ◽  
Ahmed N Assar ◽  
Christopher K. Zarins ◽  
Ellen Kuhl
Keyword(s):  
Cardiac Muscle ◽  
In Silico ◽  
In Silico Characterization

Role of 4-O Galloylchlorogenic Acid in Lung Cancer- An Insilico Approach

2017 ◽  
Vol 9 (5) ◽  
Author(s):  
Jaynthy C. ◽  
N. Premjanu ◽  
Abhinav Srivastava
Keyword(s):  
Lung Cancer ◽  
Cell Proliferation ◽  
In Silico ◽  
Computational Study ◽  
Regulation Mechanism ◽  
Down Regulation ◽  
Fruit Extract ◽  
In Vitro Techniques ◽  
Discovery Studio

Cancer is a major disease with millions of patients diagnosed each year with high mortality around the world. Various studies are still going on to study the further mechanisms and pathways of the cancer cell proliferation. Fucosylation is one of the most important oligosaccharide modifications involved in cancer and inflammation. In cancer development increased core fucosylation by FUT8 play an important role in cell proliferation. Down regulation of FUT8 expression may help cure lung cancer. Therefore the computational study based on the down regulation mechanism of FUT8 was mechanised. Sapota fruit extract, containing 4-Ogalloylchlorogenic acid was used as the inhibitor against FUT-8 as target and docking was performed using in-silico tool, Accelrys Discovery Studio. There were several conformations of the docked result, and conformation 1 showed 80% dock score between the ligand and the target. Further the amino acids of the inhibitor involved in docking were studied using another tool, Ligplot. Thus, in-silico analysis based on drug designing parameters shows that the fruit extract can be studied further using in-vitro techniques to know its pharmacokinetics.

Sign in / Sign up

Export Citation Format

Share Document