scholarly journals Synthesis, Characterization, and Evaluation of Nanoparticles Loading Adriamycin Based on 2-Hydroxypropyltrimethyl Ammonium Chloride Chitosan Grafting Folic Acid

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2229
Author(s):  
Yingqi Mi ◽  
Jingjing Zhang ◽  
Lulin Zhang ◽  
Qing Li ◽  
Yuanzheng Cheng ◽  
...  
Keyword(s):  
Folic Acid ◽  
Cancer Cells ◽  
Ammonium Chloride ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Hydrodynamic Diameter ◽  
The Novel

Chitosan nanoparticles have been considered as potential candidates for drug loading/release in drug delivery systems. In this paper, nanoparticles (HACAFNP) loading adriamycin based on 2-hydroxypropyltrimethyl ammonium chloride chitosan grafting folic acid (HACF) were synthesized. The surface morphology of the novel nanoparticles was spherical or oval, and the nanoparticles exhibited a relatively small hydrodynamic diameter (85.6 ± 2.04 nm) and positive zeta potential (+21.06 ± 0.96 mV). The drug release of nanoparticles was assayed and represented a burst effect followed by a long-term steady release. Afterward, the antioxidant efficiencies of nanoparticles were assayed. In particular, the target nanoparticles exhibited significant enhancement in radical scavenging activities. Cytotoxicities against cancer cells (MCF-7, BGC-823, and HEPG-2) were estimated in vitro, and results showed nanoparticles inhibited the growth of cancer cells. It’s worth noting that the inhibition index of HACAFNP against BGC-823 cells was 71.19% with the sample concentration of 25 μg/mL, which was much higher than the inhibitory effect of ADM. It was demonstrated that the novel nanoparticles with dramatically enhanced biological activity, reduced cytotoxicity, and steady release could be used as the practical candidates for drug loading/release in a delivery system.

scholarly journals Preparation and Characterization of Curcumin Loaded Dextrin Sulfate- Chitosan Nanoparticles for Promoting Curcumin Anticancer Activity

2019 ◽  
Vol 16 (1) ◽  
pp. 185-195
Author(s):  
Nihal S Elbialy
Keyword(s):  
Cancer Cells ◽  
Polymeric Nanoparticles ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Hydrodynamic Diameter ◽  
Transmission Electron ◽  
Hct 116 ◽  
Nano Formulation

Curcumin as a natural medicinal agent has been proved to kill cancer cells effectively. However, its biomedical applications have been hindered owing to its poor bioavailability. Many nanoparticulate systems have been introduced to overcome this problem. Among this types polymeric-based nanoparticles which exhibit unique properties allowing their use as a efficient drug carrier. Developing a polymeric- blend nanoparticles will offer a promising nanocarrier with excellent biocompatibility, biodegradability and low immunogencity. In this study, curcumin nano-vehicle has been made up by combining dextren sulfate and chitosan (DSCSNPs). DSCSNPs have been characterized using different techniques. Transmission electron microscopy (TEM) which revealed the spherical, smooth surface of the nano-formulation. Dynamic light scattering (DLS) for measuring DSCSNPs hydrodynamic- diameter. Zeta potential measurements showed nanoparticles high stability. Fourier transform infrared spectroscopy (FTIR) confirmed  successful combination between the two polymers and curcumin loading on naoparticles surface. Curcumin release profile out of DSCSNPs showed high drug release in tumor acidic microenvironment. In vitro cytotoxicity measurements demonstrated that curcumin loaded polymeric nanoparticles (DSCSNPs-Cur) have high therapeutic efficacy against colon (HCT-116) and breast  (MCF-7) cancer cells compared with free curcumin.  DSCSNPs as a combined biopolymers is an excellent candidate for improving curcumin bioavailability  allowing its use as anticancer  agent.

Sorafenib and 5-Fluorouracil Loaded Dual Drug Nanodelivery Systems for Hepatocellular Carcinoma and Colorectal Adenocarcinoma

2021 ◽  
Author(s):  
Umme Ruman ◽  
Kalaivani Buskaran ◽  
Saifullah Bullo ◽  
Georgia Pastorin ◽  
Mas Jaffri Masarudin ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cancer Cells ◽  
Cell Lines ◽  
Colorectal Adenocarcinoma ◽  
Dermal Fibroblast ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Normal Human Dermal Fibroblast ◽  
Cytotoxicity Studies

Abstract Purpose: Here, we reported the sysnthesis of two clinically used drugs, 5-fluorouracil (5FU) and Sorafenib (SF)-loaded in chitosan nanoparticles and their priliminary study of therapeutics effect on hepatocellular carcinoma and colorectal adenocarcinoma cell lines. We have formulated chitosan nanoparticles (CS NPs) loaded dual (SF and 5-FU) drugs nanodelivery system for SF/5FU-CS NPs and their coating version with folic acid (FA) for SF/5FU-CS-FA NPS. Human hepatocellular carcinoma (HepG2) and colorectal adenocarcinoma (HT29) cell lines were selected for in vitro cytotoxicity studies to evaluate the preliminary anticancer efficacy of both nanoparticles.Characterization: The physiochemical characterization of SF/5FU-CS NPs and SF/5FU-CS-FA NPs were investigated by DLS, FESEM, HRTEM, EDX, XRD, TGA, FTIR, and HPLC methods.Results: DLS study has shown the size of SF/5FU-CS and SF/5FU-CS-FA nanoparticles were about 78±14 nm and 142±25 nm, respectively. HRTEM and FESEM studies confirmed the spherical shape with size of 60-70nm for SF/5FU-CS and 90-150 nm for SF/5FU-CS-FA NPs. The XRD results indicated the drug loading and folate-coating comfirmation. FTIR peaks confirmed the presence of drugs in the nanoparticles, as well as folate-coating on the surface of the nanoparticles. TGA results demonstrated the thermostability of both nanoparticles. The release profiles of SF and 5FU from the two designed NPs were found to be in a sustained manner according to the pseudo-second-order kinetics model indicating a good delivery system for tumor cells. The cytotoxicity studies confirmed the better anti-cancer activity of the nanoparticles compared to the free 5-fluorouracil and sorafenib against liver cancer cells, HepG2 and colon cancer cells, HT29. Conversely, both NPs were found not toxic towards normal human dermal fibroblast cells (HDF) cells.

Papain mediated synthesized gold nanoparticles encore the potency of bioconjugated Flutamide

2020 ◽  
Vol 21 ◽  
Author(s):  
Xiao Xu ◽  
Libo Man
Keyword(s):  
Prostate Cancer ◽  
Gold Nanoparticles ◽  
Cancer Cells ◽  
Drug Loading ◽  
Inhibitory Effect ◽  
Therapeutic Drug ◽  
Ros Generation ◽  
High Concentration ◽  
Vis Spectroscopy

Background: Prostate cancer is the second most common cause of male cancer death after lung cancer in the US. Therefore, there is an urgent need for a highly effective therapeutic drug at substantially low doses. Objective: Anti-androgen drug flutamide was delivered to the prostate cancer cells using papain mediated synthesized gold nanoparticles (PGNPs) as the drug delivery system. PGNPs and flutamide worked synergistically against cancer cells. Method: Flutamide was used to bioconjugate with PGNPs to improve its efficacy against prostate cancer. The synthesis and bioconjugation of flutamide with PGNPs (F-PGNPs) were characterized by various characterization techniques such as UV–vis spectroscopy, Transmission Electron Microscopy (TEM), Dynamic Light Scattering (DLS), and zeta potential to ensure the synthesis, size, shape, size distribution, and stability. The drug loading efficiency of flutamide in F-PGNPs was confirmed and validated by UV–vis spectroscopy. Eventually, in vitro studies were performed to determine the potency of F-PGNPs, changes in nuclear morphology, and generation of Reactive Oxygen Species (ROS). Results: The efficacy of F-PGNPs (IC50 is 46.54 µg/mL) was found to be improved significantly over pure flutamide (IC50 is 64.63 µg/mL) against human prostate cancer PC–3 cell line whereas F-PGNPs did not show any significant toxicity up to a fairly high concentration toward normal mouse macrophage J774A.1 cells. The apoptotic effects and ROS generation of F-PGNPs were analyzed by increased permeability of the cell membrane and condensed chromatin with deep blue and green fluorescent nucleus, respectively. The results clearly showed that F-PGNPs significantly improved the potency of flutamide by delivering it directly into the nucleus of cancer cells through caveolae-dependent endocytosis. Conclusion: Thus, the greater inhibitory effect of F-PGNPs over the pure drug would be of great advantage during prostate cancer treatment.

scholarly journals Carboxymethyl chitosan nanoparticles coupled with CD59-specific ligand peptide for targeted delivery of C-phycocyanin to HeLa cells

Tumor Biology ◽  
2017 ◽  
Vol 39 (3) ◽  
pp. 101042831769226 ◽  
Author(s):  
Peng Yang ◽  
Bing Li ◽  
Qi-Feng Yin ◽  
Yu-Juan Wang
Keyword(s):  
Hela Cells ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Inhibitory Effect ◽  
Carboxymethyl Chitosan ◽  
Synthesis Conditions ◽  
Novel Approach ◽  
Specific Ligand

The combination of nanotechnology and medicine will be the next generation of vehicles for targeted drug delivery. Carboxymethyl chitosan loaded with the anticancer drug C-phycocyanin and the CD59-specific ligand peptide for cancer cell targeting were used to create C-phycocyanin/carboxymethyl chitosan–CD59-specific ligand peptide nanoparticles using the ionic-gelation method. Optimal synthesis conditions, selected by response surface methodology, comprised the ratio carboxymethyl chitosan:C-phycocyanin = 3:1, and carboxymethyl chitosan and CaCl2 concentrations of 2.0 and 1.0 mg/mL, respectively. The resulting nanoparticles were spherical, with diameters of approximately 200 nm; the entrapment efficient was about 65%; and the drug loading was about 20%. The release of C-phycocyanin from C-phycocyanin/carboxymethyl chitosan nanoparticles was pH sensitive and had a sustainable effect in vitro. Guided by the CD59-specific ligand peptide, the nanoparticles efficiently targeted the surface of HeLa cells and had an obvious inhibitory effect on HeLa cell proliferation as determined by methyl thiazolyl tetrazolium assays. The nanoparticles were hemocompatible and induced apoptosis by upregulation of cleaved caspase-3 and cleaved polyADP-ribose polymerase proteins, and downregulation of Bcl-2 proteins. Our study provides a novel approach to the research and development of marine drugs, and support for targeted therapy using anticancer drugs.

Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Enzyme Inhibitor ◽  
Radical Scavenging Activity ◽  
Curcuma Longa ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Inhibitory Effect ◽  
Curcumin Derivatives ◽  
Reducing Power Assay

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

scholarly journals Chemical Composition, In Vitro and In Silico Antioxidant Potential of Melissa officinalis subsp. officinalis Essential Oil

Antioxidants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1081
Author(s):  
Matilda Rădulescu ◽  
Călin Jianu ◽  
Alexandra Teodora Lukinich-Gruia ◽  
Marius Mioc ◽  
Alexandra Mioc ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
In Silico ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Melissa Officinalis ◽  
Β Carotene

The investigation aimed to study the in vitro and in silico antioxidant properties of Melissa officinalis subsp. officinalis essential oil (MOEO). The chemical composition of MOEO was determined using GC–MS analysis. Among 36 compounds identified in MOEO, the main were beta-cubebene (27.66%), beta-caryophyllene (27.41%), alpha-cadinene (4.72%), caryophyllene oxide (4.09%), and alpha-cadinol (4.07%), respectively. In vitro antioxidant properties of MOEO have been studied in 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging, and inhibition of β-carotene bleaching assays. The half-maximal inhibitory concentration (IC50) for the radical scavenging abilities of ABTS and DPPH were 1.225 ± 0.011 μg/mL and 14.015 ± 0.027 μg/mL, respectively, demonstrating good antioxidant activity. Moreover, MOEO exhibited a strong inhibitory effect (94.031 ± 0.082%) in the β-carotene bleaching assay by neutralizing hydroperoxides, responsible for the oxidation of highly unsaturated β-carotene. Furthermore, molecular docking showed that the MOEO components could exert an in vitro antioxidant activity through xanthine oxidoreductase inhibition. The most active structures are minor MOEO components (approximately 6%), among which the highest affinity for the target protein belongs to carvacrol.

scholarly journals GC-MS Based Identification of the Volatile Components of Six Astragalus Species from Uzbekistan and Their Biological Activity

Plants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 124
Author(s):  
Haidy A. Gad ◽  
Nilufar Z. Mamadalieva ◽  
Stefan Böhmdorfer ◽  
Thomas Rosenau ◽  
Gokhan Zengin ◽  
...  
Keyword(s):  
Radical Scavenging ◽  
Reducing Power ◽  
Principal Component ◽  
Inhibitory Effect ◽  
Maximum Activity ◽  
Volatile Components ◽  
Drug Candidates ◽  
Predominant Component ◽  
Clear Differentiation

The compositions of volatile components in the aerial parts of six Astragalus species, namely A. campylotrichus (Aca), A. chiwensis (Ach), A. lehmannianus (Ale), A. macronyx (Ama), A. mucidus (Amu) and A. sieversianus (Asi), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of Aca, Ach, Ale, Ama, Amu and Asi whole oils, respectively. Sylvestrene was the most predominant component in Asi, Amu and Ama, with highest concentration in Asi (64.64%). In addition, (E)-2-hexenal was present in a high percentage in both Ale and Ach (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all Astragalus species and a high correlation between the Amu and Ama species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), α- amylase, α-glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, Ama exhibited the maximum activity (24.12 ± 2.24 mg TE/g sample), and the volatiles from Amu exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both Ale and Ama showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). Asi demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for Ale (138.42 mg KAE/g). Accordingly, Astragalus species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer’s disease, diabetes mellitus and oxidative stress-related diseases.

scholarly journals Combined Luteolin and Indole-3-Carbinol Synergistically Constrains ERα-Positive Breast Cancer by Dual Inhibiting Estrogen Receptor Alpha and Cyclin-Dependent Kinase 4/6 Pathway in Cultured Cells and Xenograft Mice

Cancers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 2116
Author(s):  
Xiaoyong Wang ◽  
Lijuan Zhang ◽  
Qi Dai ◽  
Hongzong Si ◽  
Longyun Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cell ◽  
Breast Cancer Cells ◽  
Cultured Cells ◽  
Inhibitory Effect ◽  
Cyclin Dependent Kinase ◽  
Xenograft Mice ◽  
The Individual

The high concentrations of individual phytochemicals in vitro studies cannot be physiologically achieved in humans. Our solution for this concentration gap between in vitro and human studies is to combine two or more phytochemicals. We screened 12 phytochemicals by pairwise combining two compounds at a low level to select combinations exerting the synergistic inhibitory effect of breast cancer cell proliferation. A novel combination of luteolin at 30 μM (LUT30) and indole-3-carbinol 40 μM (I3C40) identified that this combination (L30I40) synergistically constrains ERα+ breast cancer cell (MCF7 and T47D) proliferation only, but not triple-negative breast cancer cells. At the same time, the individual LUT30 and I3C40 do not have this anti-proliferative effect in ERα+ breast cancer cells. Moreover, this combination L30I40 does not have toxicity on endothelial cells compared to the current commercial drugs. Similarly, the combination of LUT and I3C (LUT10 mg + I3C10 mg/kg/day) (IP injection) synergistically suppresses tumor growth in MCF7 cells-derived xenograft mice, but the individual LUT (10 mg/kg/day) and I3C (20 mg/kg/day) do not show an inhibitory effect. This combination synergistically downregulates two major therapeutic targets ERα and cyclin dependent kinase (CDK) 4/6/retinoblastoma (Rb) pathway, both in cultured cells and xenograft tumors. These results provide a solid foundation that a combination of LUT and I3C may be a practical approach to treat ERα+ breast cancer cells after clinical trials.

scholarly journals MicroRNA-124 Regulates the Proliferation of Colorectal Cancer Cells by TargetingiASPP

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Kuijie Liu ◽  
Hua Zhao ◽  
Hongliang Yao ◽  
Sanlin Lei ◽  
Zhendong Lei ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Target Prediction ◽  
Inhibitory Effect ◽  
Luciferase Reporter ◽  
Luciferase Reporter Gene ◽  
Small Noncoding Rnas ◽  
Colorectal Cancer Cells ◽  
Microrna 124

MicroRNAs are a class of small, noncoding RNAs that function as critical regulators of gene expression by targeting mRNAs for translational repression or degradation. In this study, we demonstrate that expression of microRNA-124 (miR-124) is significantly downregulated in colorectal cancer tissues and cell lines, compared to the matched adjacent tissues. We identified and confirmed inhibitor of apoptosis-stimulating protein of p53 (iASPP) as a novel, direct target of miR-124 using target prediction algorithms and luciferase reporter gene assays. Overexpression of miR-124 suppressed iASPP protein expression, upregulated expression of the downstream signaling molecule nuclear factor-kappa B (NF-κB), and attenuated cell viability, proliferation, and colony formation in SW480 and HT-29 colorectal cancer cells in vitro. Forced overexpression ofiASPPpartly rescued the inhibitory effect of miR-124 on SW480 and HT29 cell proliferation. Taken together, these findings shed light on the role and mechanism of action of miR-124, indicate that the miR-124/iASPP axis can regulate the proliferation of colorectal cancer cells, and suggest that miR-124 may serve as a potential therapeutic target for colorectal cancer.

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