HDF Cells Research Articles

Bio-prospecting the Anti-oxidative and Radioprotective Role of Bioactive Pigment Isolated from Pontibacter indicus

Aim: To evaluate the anti-oxidative and radioprotective role of Pontibacter indicus SCG24 pigment during radiation exposure Background: Radiation-induced cytotoxicity is quite common during cancer therapy. There is a need for naturally derived therapeutic molecules that can scavenge free radicals. They may act as substitutes for synthetic molecules. Hence, there is a need for urgent evaluation of these potent compounds before therapeutic application. Objective: The objective of this study is to examine the anti-oxidative and radioprotective role of P. indicus SCG24 pigment, specifically to evaluate free radical scavenging X-ray irradiated HDF cells Method: A radiotoleraent pigment-producing P. indicus SCG24 was isolated from pharmaceutical effluent. Chloroform was used as a primary solvent for pigment extraction. GCMS/MS analysed initial pigment composition. Various In-vitro antioxidant assays were performed using ABTS, FRAP, and DPPH assay. Flow cytometry was used to determine the rate of scavenging activity of pigment in HDF cells. Results: The GCMS/MS profile of the chloroform extract revealed twenty-two compounds. Furthermore, based on the DPPH, ABTS, and FRAP assay, the pigment was found to have significant antioxidant properties. The flow cytometry results indicate that the pigment possesses radioprotectant activity by neutralizing ROS species in HDF cells when exposed to X-ray radiation. Conclusion: These observations on P. indicus SCG24 pigment suggested that the pigment may have potential therapeutic importance.

Assessment of the Antioxidant and Photoprotective Properties of Cornus mas L. Extracts on HDF, HaCaT and A375 Cells Exposed to UVA Radiation.

The influence of UV radiation on skin discoloration, skin aging and the development of skin cancer is widely known. As a part of this study, the effect of extracts from three varieties of Cornus mas L. (C. mas L.) on skin cells exposed to UVA radiation was assessed. The analyses were performed on both normal and cancer skin cells. For this purpose, the potential photoprotective effects of the obtained extracts (aqueous and ethanolic) was assessed by performing two cytotoxicity tests (Alamar blue and Neutral red). Additionally, the antioxidant capacity was compared using three different assays. The 2',7'-dichlorodihydrofluorescein diacetate (H2DCFDA) probe was used to evaluate the intracellular level of free radicals in cells exposed to the simultaneous action of UVA radiation and dogwood extracts. Additionally, the ability to inhibit excessive pigmentation was determined by assessing the inhibition of melanin formation and tyrosinase activity. The obtained results confirmed the strong antioxidant properties of dogwood extracts and their photoprotective effect on normal skin cells. The ability to inhibit the viability of melanoma cells was also observed. Additionally, a reduction in oxidative stress in skin cells exposed to UVA radiation and a strong inhibition of melanin formation and tyrosinase activity have been demonstrated. This study shows that dogwood extract could be a valuable cosmetic raw material that can play both a photoprotective and antihyperpigmentation role in cosmetic preparations.

Anti-ageing mechanism of topical bioactive ingredient composition on skin based on network pharmacology.

To elucidate the anti-ageing mechanism of the combination of eight ingredients on the skin from a multidimensional view of the skin. The target pathway mechanisms of composition to delay skin ageing were investigated by a network pharmacology approach and experimentally validated at three levels: epidermal, dermal, and tissue. We identified 24 statistically significant skin ageing-related pathways, encompassing crucial processes such as epidermal barrier repair, dermal collagen and elastin production, inhibition of reactive oxygen species (ROS), as well as modulation of acetylcholine and acetylcholine receptor binding. Furthermore, our invitro experimental findings exhibited the following outcomes: the composition promotes fibroblast proliferation and the expression of barrier-related genes in the epidermis; it also stimulated the expression of collagen I, collagen III, and elastic fibre while inhibiting ROS and β-Gal levels in HDF cells within the dermis. Additionally, Spilanthol in the Acmella oleracea extract contained in the composition demonstrated neuro-relaxing activity in Zebrafish embryo, suggesting its potential as an anti-wrinkle ingredient at the hypodermis level. In vitro experiments validated the anti-ageing mechanism of composition at multiple skin levels. This framework can be extended to unravel the functional mechanisms of other clinically validated compositions, including traditional folk recipes utilized in cosmeceuticals.

Synergistic cytotoxicity of olive leaf extract-loaded lipid nanocarriers combined with Newcastle disease virus against cervical cancer cells.

Despite recent medical progress, cervical cancer remains a major global health concern for women. Current standard treatments have limitations such as non-specific toxicity that necessitate development of safer and more effective therapeutic strategies. This research evaluated the combinatorial effects of olive leaf extract (OLE), rich in anti-cancer polyphenols, and the oncolytic Newcastle disease virus (NDV) against human cervical cancer cells. OLE was efficiently encapsulated (>94% loading) within MF59 lipid nanoparticles and nanostructured lipid carriers (NLCs; contains Precirol as NLC-P, contains Lecithin as NLC-L) to enhance stability, bioavailability, and targeted delivery. Physicochemical analysis confirmed successful encapsulation of OLE within nanoparticles smaller than 150 nm. In vitro cytotoxicity assays demonstrated significantly higher toxicity of the OLE-loaded nanoparticle formulations on HeLa cancer cells versus HDF normal cells (P<0.05). MF59 achieved the highest encapsulation efficiency, while NLC-P had the best drug release profile. NDV selectively infected and killed HeLa cells versus HDF cells. Notably, combining NDV with OLE-loaded nanoparticles led to significantly enhanced synergistic cytotoxicity against cancer cells (P<0.05), with NLC-P (OLE) and NDV producing the strongest effects. Apoptosis and cell cycle analyses confirmed the increased anti-cancer activity of the combinatorial treatment, which induced cell cycle arrest. This study provides evidence that co-delivery of OLE-loaded lipid nanoparticles and NDV potentiates anti-cancer activity against cervical cancer cells in vitro through a synergistic mechanism, warranting further development as a promising alternative cervical cancer therapy.

γ-Mangosteen, an autophagy enhancer, prevents skin-aging via activating KEAP1/NRF2 signaling and downregulating MAPKs/AP-1/NF-κB-mediated MMPs

BackgroundMangosteens, a naturally occurring xanthones, found abundantly in mangosteen fruits. The anti-skin aging potential of γ-mangosteen (GM) remains unexplored; therefore, we investigated the UVB-induced anti-skin aging of GM via activation of autophagy. HypothesisWe hypothesized that GM exerts antioxidant and anti-aging capabilities both in vitro and in vivo through activation of autophagy as well as control of KEAP1/NRF2 signaling and MAPKs/AP-1/NF-κB-mediated MMPs pathways. MethodsThe anti-skin aging effects of GM were studied using HDF cells and a mice model. Various assays, such as DPPH, ABTS, CUPRAC, FRAP, and ROS generation, assessed antioxidant activities. Kits measured antioxidant enzymes, SA-β-gal staining, collagen, MDA content, si-RNA experiments, and promoter assays. Western blotting evaluated protein levels of c-Jun, c-Fos, p-IκBα/β, p-NF-κB, MAPK, MMPs, collagenase, elastin, KEAP1, NRF2, HO-1, and autophagy-related proteins. ResultsGM exhibited strong antioxidant, collagenase and elastase enzyme inhibition activity surpassing α- and β-mangosteen. GM competitively inhibited elastase with a Ki value of 29.04 µM. GM orchestrated the KEAP1-NRF2 pathway, enhancing HO-1 expression, and suppressed UVB-induced ROS in HDF cells. NRF2 knockdown compromised GM's antioxidant efficacy, leading to uncontrolled ROS post-UVB. GM bolstered endogenous antioxidants, curbing lipid peroxidation in UVB-exposed HDF cells and BALB/c mice. GM effectively halted UVB-induced cell senescence, and reduced MMP-1/-9, while elevated TIMP-1 levels, augmented COL1A1, ELN, and HAS-2 expression in vitro and in vivo. Additionally, it suppressed UVB-induced MAPKs, AP-1, NF-κB phosphorylation. Pharmacological inhibitors synergistically enhanced GM's anti-skin aging potential. Moreover, GM inhibited UVB-induced mTOR activation, upregulated LC3-II, Atg5, Beclin 1, and reduced p62 in both UVB induced HDF cells and BALB/c mice, while blocking of autophagy successfully halt the GM effects against the UVB-induced increase of cell senescence, degradation of collagen through upregulation of MMP-1, underscoring GM's substantial anti-skin aging impact via autophagy induction in vitro and in vivo. ConclusionTogether, GM has potent antioxidant and anti-skin aging ingredients that can be used to formulate skin care products for both the nutraceutical and cosmeceutical industries.

Investigating the Effects of Dorema hyrcanum Root Extracts on Selective Induction of Programmed Cell Death in Glioblastoma, Ovarian Cancer and Breast Cancer Cell Lines.

Despite remarkable advances, cancer has remained the second cause of death, which shows that more potent novel compounds should be found. Ethnobotanical compounds have a long history of treating diseases, and several approved chemotherapeutic compounds were isolated from plants. The research aimed to evaluate the cytotoxic effects of Dorema hyrcanum root extract on ovarian, breast, and glioblastoma cells while examining its selectivity towards normal cells. Additionally, the study is directed to investigate cell death mechanisms, delineate modes of cell death, and explore intracellular ROS production. Cytotoxic effects of alcoholic, dichloromethane, and petroleum ether fractions of Dorema hyrcanum were investigated on cancer and normal cells by using MTT assay, and the concentration around IC50 values was used for flow cytometric assessment of apoptosis, evaluation of the expression of selected genes via RT-qPCR and production of ROS. Methanolic extract exhibited the highest cytotoxicity, impacting A2780CP and MDA-MB-231. All fractions showed comparable effects on U251 cells. Notably, extracts displayed higher IC50 values in normal HDF cells, indicating cancer cell specificity. Flow cytometry revealed induction of apoptosis and non-apoptotic death in all three cancer cell lines. QPCR results showed upregulation of related genes, with RIP3K prominently increased in U251 glioblastoma. The DCFH-DA assay demonstrated ROS induction by the PE fraction exclusively in A2780CP cells after 30 minutes and up to 24 hours. Dorema hyrcanum root extracts exhibited potent anti-tumor effects against all studied cell lines. The methanolic extract demonstrated the highest cytotoxicity, particularly against A2780CP and MDA-MB-231 cells. Importantly, all fractions displayed selectivity for cancer cells over normal HDF cells. Unique modes of action were observed, with the petroleum ether fraction inducing significant non-apoptotic cell death. These findings suggest promising therapeutic potential for Dorema hyrcanum in cancer treatment with subject to further mechanistic studies.

Phytofabrication of biocompatible chitosan-based ZnO nanocomposite aided by Cissus quadrangularis extract enriched with antimicrobial and antioxidant potential

A dynamic chitosan-based ZnO nanocomposite (NC) was fabricated via a cost-effective formulation and an eco-friendly procedure utilizing Cissus quadrangularis (CQ) plant extract. This study investigates the antimicrobial and antioxidant properties, together with the cytocompatibility aspects of chitosan-incorporated ZnO nanocomposite (CS-ZnO/CQE). The formation and structural morphology of the nanocomposites were examined using FTIR, UV–Vis, XRD, XPS, BET, TGA, SEM, and TEM techniques. The antibacterial test results demonstrated the greatest inhibitory zone diameter against S. aureus (19 ± 1.00 mm) and E. coli (17 ± 1.05 mm), assessed through agar well diffusion method. Also, the composite exhibited a DPPH inhibition rate of 78.7 ± 0.34 %, indicating its high effectiveness in neutralizing free radicals. In addition, the nanocomposite exhibited less toxicity towards human erythrocytes, HDF and HEK-293 cells as a result of the biocompatibility exhibited by CS, ZnO, and CQ plant extract. Likewise, it has exceptional cell migratory capacity and possesses biodegradability factors. These observations strongly suggest the potential of CS-ZnO/CQE as a cutting-edge antibacterial and antioxidant agent to be implemented in the medical sector.

Synthesis, characterization and biological activities of nitrophenol-substituted phosphazene dendrimers

This study introduces the synthesis and characterization of two novel nitrophenol-substituted phosphazene dendrimers, [N3P3(OC6H5NO2)6] (III) and [N3P3(OC6H5(NO2)2)5O]ˉ.C6H16N+.H2O (IV), derived from hexachlorocyclotriphosphazene (HCCP). The structures of the compounds were determined using elemental analysis, infrared spectroscopy, and X-ray crystallography. The optical properties of the crystals were investigated by photophysical methods. The thermal properties of the compounds were measured by thermogravimetry-differential thermal analysis (TG-DTA). The antibacterial and anticancer properties of the compounds were tested based on the antibacterial tests against Gram-negative (Escherichia coli ATCC 8739 G(-)) and Gram-positive (Staphylococcus aureus ATCC 6538 G(+), Bacillus subtilis 2a ATCC 23,857 G(+)) bacteria, as well as the MTT assay test on K562 leukemia cells (ATCC: CCL-243) and MCF-7 breast cancer cells (ATCC: HTB-22). The presence of six homogeneous 2-nitrophenol substitutions in compound III reduces the fluorescence of the phosphazene ring. The results showed that compound IV has a higher fluorescence intensity and similar toxicity to MCF-7 and HDF cells. The structural differences and the number of nitro groups in the nitrophenol ligands account for these variations. Our results suggest that these cyclophosphazene derivatives have promising properties for biomedical applications and further studies are warranted to explore their mechanisms of action and therapeutic potential.

Illuminating new possibilities: Effects of copper oxide nanoparticles on gastrointestinal adenocarcinoma cells in hypoxic condition

Cancer remains a major global health concern, necessitating the development of novel therapeutic approaches. Hypoxia is a common characteristic of solid tumors that plays a critical role in tumor progression, making it a prime target for anticancer therapies. This study aimed to determine the effects of copper oxide nanoparticles (CuONPs) on human gastrointestinal cancer cells in hypoxic condition for the first time. Toxicity of CuONPs was evaluated on human colon and gastric adenocarcinoma cells and normal fibroblasts by alamarBlue assay. Real-time polymerase chain reaction (PCR) was performed to study the effects of CuONPs on genes involved in cell apoptosis. To elucidate the molecular mechanisms underlying the effects of CuONPs in hypoxic condition, molecular docking was conducted on HIF-1α. Results revealed dose- and cell-type-dependent toxic effects of CuONPs, as a more significant (p < 0.0001) decrease in viability of LoVo cells (23 %) was observed compared to MKN-45 and HDF cells. In addition, CuONPs significantly (p < 0.0001) reduced LoVo cell viability down to 30.2 % in hypoxic condition. Gene expression analysis revealed significant (p < 0.0001) overexpression of P53 and BAX but downregulation of BCL-2 and CCND1 after treatment with CuONPs. Molecular docking indicated the preferable binding of CuONPs to the HIF-1α PAS-B domain through interaction with 15 residues with −4.8 kcal/mol binding energy. Our findings open up new possibilities for modulating HIF-1 activity and inhibiting hypoxia-induced tumor progression.

Statistical modeling, optimization and characterization of andrographolide loaded emulgel for its therapeutic application on skin cancer through enhancing its skin permeability

Andrographolide is a natural diterpene lactone with multiple biological effects. In the present study, a total of 11 andrographolide-loaded emulgels (ANG 1- ANG 11) were prepared by emulsification and solvent evaporation method using flaxseed oil and xanthan gum in different ratios, as suggested by the Design-Expert software. A 2-factor-5-level design was employed with different responses including spreadability, extrudability, viscosity, and drug release after 1 h (h) and 24 h. Based on the Design-Expert software response, the optimized emulgel ANG 12 was formulated and evaluated. The 24 h In-vitro drug release was found to be 95.7 % following Higuchi kinetics. Ex-vivo skin retention of 784.78 ug/cm2 was observed during the study. MTT assay performed on Human epidermoid carcinoma (A-431) cells demonstrated cell growth arrest at G0/G1 and G2/M phase after 24 h of ANG 12 treatment (IC50: 11.5 µg/ml). The cellular permeability of ANG-12 was assessed by Fluorescein isothiocyanate (FITC) assay. Compared to untreated cells (0.54 % uptake) the ANG-12 treated cells had shown 87.17 % FITC permeation. The biocompatibility study performed on non-cancerous human dermal fibroblast cells (HDF cells) shows 91.54 % viability after 24 h of the treatment showing the non-toxic nature of ANG-12. Confocal imaging had shown a significant time-dependent increase in in-vivo cellular uptake with enhanced, progressive penetration of the emulgel into the skin. An in-vivo skin irritation study conducted on Swiss albino mice confirmed the safety aspects of the ANG 12. Hence, it can be concluded that nanoemulgel of andrographolide (ANG 12) could be a novel approach to treating skin cancer.

HPLC-based cytotoxicity profiling and LC-ESIQTOF-MS/MS analysis of Helichrysum leucocephalum

IntroductionHelichrysum leucocephalum Boiss. (Asteraceae) is an endemic plant to Iran. No reports have studied the cytotoxicity of the plant. The current study aimed to evaluate the cytotoxicity of H. leucocephalum collected from Fars province (Iran) against MCF-7 and HDF cell lines using HPLC-based activity profiling and to annotate the active constituents by LC-ESIQTOF-MS/MS. MethodsH. leucocephalum was collected from three locations in Fars province. The dried flowers and leaves were separately extracted by percolation using methanol. The crude extracts were fractionated by liquid-liquid partitioning with dichloromethane (DCM) and aqueous methanol. The cytotoxicity of the fractions was evaluated against MCF-7 and HDF cells by Alamarblue assay. HPLC-based activity profiling was used to track the active constituents. LC-MS dereplication strategy was used for the annotation of the compounds in the active time window. LC-MS data were preprocessed by MZmine 3.3.0 and submitted to multivariate analysis to compare the differences and similarities in the metabolites of the samples. ResultsThe DCM fractions showed a dose-dependent cytotoxicity against the cancerous cells (IC50s, 9.8–105.1 μg/ml). In general, the metabolites of the flowers and their cytotoxicity were higher than the leaves. LCESIMS/MS analyses revealed that prenylated and geranylated α,β-unsaturated spiroketal phloroglucinols were among the active constituents. ConclusionIt can be concluded that H. leucocephalum is a rich source of phloroglucinol derivatives with cytotoxic activities. Further phytochemical analysis is needed to characterize the bioactive components.

Characterizing Nanoparticle Isolated by Yam Bean (Pachyrhizus erosus) as a Potential Agent for Nanocosmetics: An in vitro and in vivo Approaches.

This study investigated the potential of Plant-Derived Exosome-Like Nanoparticles (PDENs) as cosmeceutical nanocarriers for treating skin problems, such as scar removal, face rejuvenation, anti-aging, and anti-pigmentation. Researchers isolated PDENs from Yam Bean (Pachyrhizus erosus) using PEG-based precipitation, gradual filtration, and various centrifugations at low temperatures. Followed by in vitro and in vivo studies using HDF cells and Zebrafish. The morphology of the YB-PDENs was determined using TEM analysis, they had a spherical shape with diameters of 236,83 ± 9,27nm according to PSA. The study found that YB-PDENs were stable in aquabidest at 4°C for one month of storage and had ~-26,5 mV of Zeta Potential. The concentration of YB-PDENs was measured using the BCA Assay, and internalization of YB-PDENs to HDF cells was observed using a Confocal Laser Scanning Microscope labelled with PKH67. As for cytotoxicity, after 24 and 72 hours of incubation with YB-PDENs, the viability of HDF cells remained more than 80%. The study also examined cell migration using the Scratch Assay and found that at 2,5 μg/mL, YB-PDENs had better migration results than other concentrations. Immunocytochemistry showed that collagen expression was higher after 14 days of incubation with YB-PDENs, and melanocytes in zebrafish decreased at each concentration compared with controls. In conclusion, this study is the first to extract and describe PDENs from Yam Bean (Pachyrhizus erosus), with YB-PDENs having a promising anti-melanogenic effect in skin treatment. This study highlights the potential of YB-PDENs as a promising alternative to depigmentation and skin whitening treatments.

Potential of Plant-derived Exosome-like Nanoparticles from Physalis peruviana Fruit for Human Dermal Fibroblast Regeneration and Remodeling.

This research aimed to study the potential of PDEN from P. peruviana fruits (PENC) for regenerating and remodeling HDF. Large wounds are dangerous and require prompt and effective healing. Various efforts have been undertaken, but have been somewhat ineffective. Plant-derived exosome-like nanoparticles (PDEN) are easily sampled, relatively cost-effective, exhibit high yields, and are nonimmunogenic. The objective of the study was to isolate and characterize PDEN from Physalis peruviana (PENC), and determine PENC's internalization and toxicity on HDF cells, PENC's ability to regenerate HDF (proliferation and migration), and PENC ability's to remodel HDF (collagen I and MMP- 1 production). PENC was isolated using gradual filtration and centrifugation, followed by sedimentation using PEG6000. Characterization was done using a particle size analyzer, zeta potential analyzer, TEM, and BCA assay. Internalization was done using PKH67 staining. Toxicity and proliferation assays were conducted using MTT assay; meanwhile, migration assay was carried out by employing the scratch assay. Collagen I production was performed using immunocytochemistry and MMP-1 production was conducted using ELISA. MTT assay showed a PENC concentration of 2.5 until 500 μg/mL and being non-toxic to cells. PENC has been found to induce cell proliferation in 1, 3, 5, and 7 days. PENC at a concentration of 2.5, 5, and 7.5 μg/mL, also accelerated HDF migration using the scratch assay in two days. In remodeling, PENC upregulated collagen-1 expression from day 7 to 14 compared to control. MMP-1 declined from day 2 to 7 in every PENC concentration and increased on day 14. Meanwhile, ROS declined from day 2 to 7 and 14, with PENC inducing a rise in the ROS level compared to control. Overall, PENC at concentrations of 2.5, 5, and 7.5 μg/mL induced HDF proliferation and migration, upregulated collagen I production, and decreased MMP-1 levels. Isolated PENC was 190-220 nm in size, circular, covered with membrane, and its zeta potential was -6.7 mV; it could also be stored at 4°C for up to 2 weeks in aqua bidest. Protein concentration ranged between 170-1,395 μg/mL. Using PKH67, PENC could enter HDF within 6 hours. PENC was non-toxic up to a concentration of 500 μg/mL. Using MTT and scratch assay, PENC was found to elevate HDF proliferation and migration, and reorganize actin. Using immunocytochemistry, collagen I was upregulated by PENC, whereas MMP-1 concentration was reduced.

The urolithin B nanomicellar delivery system as an efficient selective anticancer compound.

Urolithin B (UB), the antioxidant polyphenol has a protective impact on several organs against oxidative stress. However, its bioactivity is limited by its hydrophobic structure. In the current study, UB was encapsulated into a liposomal structure to improve its bioactivities anticancer, and antimicrobial potential. The UB nano-emulsions (UB-NE) were synthesized and characterized utilizing FESEM, DLS, FTIR, and Zeta-potential analysis. The UB-NMs' selective toxicity was studied by conducting an MTT assay on MCF-7, PANC, AGS, and ASPC1 cells. The AO/PI analysis verified the UB-NMs' cytotoxicity on ASPC1 cell lines and approved the MTT results. Finally, the antibacterial activity of the UB-NMs was studied on both gram-positive (B. subtilis, S. aureus) and gram-negative (E. Coli, P. aeruginosa) bacteria by conducting MIC and MBC analysis. The 68.15nm UB-NMs did not reduce the normal HDF cells' survival. However, they reduced the cancer cells' (PANC and AGS cell lines) survival at high treatment concentrations (> 250µg/mL) compared with normal HDF and cancer MCF-7 cells. Moreover, the IC50 doses of UB-NMs for the ASPC1 and PANC cancer cells were measured at 44.87, and 221.02µg/mL, respectively. The UB-NMs selectively exhibited apoptotic-mediated cytotoxicity on the human pancreatic tumor cell line (ASPC1) by down-regulating BCL2 and NFKB gene expression. Also, the BAX gene expression was up-regulated in the ASPC1-treated cells. Moreover, they exhibited significant anti-bactericidal activity against the E. coli (MIC = 50µg/mL, MBC = 150µg/mL), P. aeruginosa (MIC = 75µg/mL, MBC = 275µg/mL), B. subtilis (MIC = 125µg/mL, MBC = 450µg/mL), and S. aureus (MIC = 50µg/mL, MBC = 200µg/mL) strains. The significant selective cytotoxic impact of the UB-NMs on the human pancreatic tumor cell line makes it an applicable anti-pancreatic cancer compound. Moreover, the antibacterial activity of UB-NMs has the potential to decrease bacterial-mediated pancreatic cancer. However, several bacterial strains and further cancer cell lines are required to verify the UB-NMs' anticancer potential.

Efficient and Traceable Tamoxifen Delivery to Breast Cancer Cells Using Folic Acid‐Decorated and PEGylated Graphene Quantum Dots

AbstractGraphene quantum dots (GQDs) possess potential properties for the targeted transport and tracking of anticancer medication to tumor cells. For this purpose, the synthesized GQDs were decorated with folic acid (FA) and methoxy polyethylene glycol (mPEG2000), and finally loaded with tamoxifen (TMX) drug. The synthesized nano‐drug was characterized using FTIR, XRD, UV‐Vis, PL, HRTEM, FESEM, and DLS analytical devices. Based on the obtained data, the average hydrodynamic diameter of particles dissolved in water was 294.7 nm and the size of dehydrated particles was between 53 and 210 nm. PL data showed that prepared nanoparticles have an emission wavelength of 438 nm, which is in the blue fluorescent wavelength range, thus making these nanoparticles suitable for cell imaging. The encapsulation efficiency and loading percentage of tamoxifen in nanoparticles were calculated at about 52.5 % and 30 %, respectively, and cumulative drug release reached 89 % within 42 hours. The cytotoxicity effects of nanoparticles were investigated. According to IC50 results, the targeted mPEG‐GQDs‐FA/TMX (TMX‐FPGs) nano‐drug was more toxic than free TMX on MCF‐7 cells and had reduced side effects on healthy HDF cells. TMX‐FPGs induced apoptosis cell death, significantly. The confocal imaging experiments showed that TMX‐FPGs are appropriate for monitoring and targeting MCF‐7 cells.

Design and Evaluation of a Novel Anti-microbial Peptide from Cathelicidin-2: Selectively Active Against Acinetobacter baumannii.

Infections caused by pathogenic microorganisms have increased the need for hospital care and have thus represented a public health problem and a significant financial burden. Classical treatments consisting of traditional antibiotics face several challenges today. Anti-microbial peptides (AMPs) are a conserved characteristic of the innate immune response among different animal species to defend against pathogenic microorganisms. In this study, a new peptide sequence (mCHTL131-140) was designed using the in silico approach. Cathelicidin-2 (UniprotID: Q2IAL7) was used as a potential antimicrobial protein, and a novel 10 - 12 amino acids sequence AMP was designed using bioinformatics tools and the AMP databases. Then, the anti-bacterial, anti-biofilm, and anti-fungal properties of the peptide, as well as its hemolytic activity and cytotoxicity towards human fibroblast (HDF) cells, were investigated in vitro. Online bioinformatics tools indicated that the peptide sequence could have anti-bacterial, anti-viral, anti-fungal, and anti-biofilm properties with little hemolytic properties. The experimental tests confirmed that mCHTL131-140 exhibited the best anti-bacterial properties against Acinetobacter baumannii and had fair anti-fungal properties. Besides, it did not cause red blood cell lysis and showed no cytotoxicity towards HDF cells. In general, the designed peptide can be considered a promising AMP to control hospital-acquired infections by A. baumannii.

Fucoidan isolated from the edible seaweed Sargassum fusiforme suppresses skin damage stimulated by airborne particulate matter

Particulate matter (PM) pollution is a major environmental factor to global health problems. It exposes to the skin of human body, induces skin diseases and aging. Sargassum fusiforme is rich in a variety of bioactive substances and possesses the potential to protect skin against PM-stimulated damage. The purpose of this study is to investigate the effect of the fucoidan (SF-F4) isolated from S. fusiforme on PM-stimulated skin damage in human keratinocytes (HaCaT cells) and human dermal fibroblasts (HDF cells). The results show that PM significantly increased ROS level and promoted the cell death in both HaCaT cells and HDF cells. However, SF-F4 effectively increased the viability of PM-treated HaCaT cells by inhibiting apoptosis via scavenging intracellular ROS. In addition, SF-F4 regulated the expressions of MMPs and pro-inflammatory molecules in PM-stimulated HDF cells in a concentration-dependent manner, thus, it increasing pro-collagen content of PM-stimulated HDF cells. In conclusion, the current findings indicate that SF-F4 can effective inhibit PM-induced oxidative stress and reduce the secretion of pro-inflammatory factors and MMPs in cells, thereby slowing down the triggering of skin damage, suggesting that SF-F4 may be a potential pharmaceutical or cosmetic ingredient.

Yttrium Oxide nanoparticles induce cytotoxicity, genotoxicity, apoptosis, and ferroptosis in the human triple-negative breast cancer MDA-MB-231 cells

BackgroundTriple-negative breast cancer (TNBC) is a lethal mammary carcinoma subtype that affects females and is associated with a worse prognosis. Chemotherapy is the only conventional therapy available for patients with TNBC due to the lack of therapeutic targets. Yttrium oxide (Y2O3) is a rare earth metal oxide, whose nanoparticle (NPs) formulations are used in various applications, including biological imaging, the material sciences, and the chemical synthesis of inorganic chemicals. However, the biological activity of Y2O3-NPs against TNBC cells has not been fully explored. The current study was conducted to assess Y2O3-NPs’ anticancer activity against the human TNBC MDA-MB-231 cell line.MethodsTransmission electron microscopy (TEM), X-ray diffraction, Zeta potential, and dynamic light scattering (DLS) were used to characterize the Y2O3-NPs. SRB cell viability, reactive oxygen species (ROS) measurement, single-cell gel electrophoresis (comet assay), qPCR, flow cytometry, and Western blot were employed to assess the anticancer activity of the Y2O3-NPs.ResultsOur results indicate favorable physiochemical properties of Y2O3-NPs (with approximately average size 14 nm, Zeta Potential about − 53.2 mV, and polydispersity index = 0.630). Y2O3-NPs showed a potent cytotoxic effect against MDA-MB-231 cells, with IC50 values of 74.4 µg/mL, without cytotoxic effect on the normal retina REP1 and human dermal fibroblast HDF cell lines. Further, treatment of MDA-MB-231 cells with IC50 Y2O3-NPs resulted in increased oxidative stress, accumulation of intracellular ROS levels, and induced DNA damage assessed by Comet assay. Upon Y2O3-NPs treatment, a significant increase in the early and late phases of apoptosis was revealed in MDA-MB-231 cells. qPCR results showed that Y2O3-NPs significantly upregulated the pro-apoptotic genes CASP3 and CASP8 as well as ferroptosis-related gene heme oxygenase-1 (HO-1), whereas the anti-apoptotic gene BCL2 was significantly downregulated.ConclusionThis study suggests that Y2O3-NPs are safe on normal REP1 and HDF cells and exhibited a potent selective cytotoxic effect against the TNBC MDA-MB-231 cells through increasing levels of ROS generation with subsequent DNA damage, and induction of apoptosis and ferroptosis.

Uncovering chemical profiles, biological potentials, and protection effect against ECM destruction in H2 O2 -treated HDF cells of the extracts of Stachys tundjeliensis.

The genus Stachys L., one of the largest genera of the Lamiaceae family, is highly represented in Turkey. This study was conducted to determine the bio-pharmaceutical potential and phenolic contents of six different extracts from aerial parts of Stachys tundjeliensis. The obtained results showed that the ethanol extract exhibited the highest antioxidant activity in the antioxidant assays. Meanwhile, the ethanol extract displayed strong inhibitory activity against α-tyrosinase, the dichloromethane extract exhibited potent inhibition against butyrylcholinesterase, and the n-hexane extract against α-amylase. Based on ultra-high performance liquid chromatography coupled to high-resolution mass spectrometryanalysis, more than 90 secondary metabolites, including hydroxybenzoic acid, hydroxycinnamic acid, and their glycosides, acylquinic acids, phenylethanoid glycosides, and various flavonoids were identified or tentatively annotated in the studied S. tundjeliensis extracts. It was observed that the application of S. tundjeliensis eliminated H2 O2 -induced oxidative stress. It was determined that protein levels of phospho-nuclear factor kappa B (NF-κB), receptor for advanced glycation endproducts, and activator protein-1, which are activated in the nucleus, decreased, and the synthesis of matrix metalloproteinase (MMP)-2 and MMP-9 also decreased to basal levels. Overall, these findings suggest that S. tundjeliensis contains diverse bioactive compounds for the development of nutraceuticals or functional foods with potent biological properties.

Poly(vinyl alcohol)/chitosan hydrogel incorporating chitooligosaccharide-gentisic acid conjugate with antioxidant and antibacterial properties as a potential wound dressing

The design and development of wound dressing with antioxidant and antibacterial properties to accelerate wound healing remain challenging. In this study, we synthesize a chitooligosaccharide-gentisic acid (COS-GSA) conjugate using the free-radical grafting method, and fabricate a poly(vinyl alcohol) (PVA)/chitosan (CH)/COS-GSA (PVA/CH/CG) hydrogel using a freeze-thaw method. We characterize the synthesized COS-GSA conjugates using through polyphenol assay, absorbance, and 1H NMR spectroscopy and evaluate their antioxidant properties. The COS-GSA conjugates are successfully synthesized and exhibit better antioxidant properties than pristine COSs. Subsequently, the fabricated hydrogel is characterized based on its morphological analysis, rheological properties, water contact angle, swelling, degradation, water retention properties, and COS-GSA release profiles. Finally, the biocompatibility of the fabricated hydrogel is evaluated on HDF and HaCaT cells through indirect and direct cytotoxicity. The PVA/CH/CG hydrogel exhibited significantly higher antioxidant properties (DPPH, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and hydrogen peroxide (H2O2) scavenging activities) and antibacterial activities (Staphylococcus aureus and Pseudomonas aeruginosa) compared to other fabricated hydrogels such as PVA, PVA/CH, and PVA/CH/COS (PVA/CH/C). These results provide evidence that PVA/CH/CG hydrogels with antioxidant, antibacterial, and non-cytotoxic properties have great potential for wound-dressing applications.