Human Dermal Fibroblast Cell Line Research Articles

Application of Kenaf Seed Oil‐Nanostructured Lipid Carrier to Palm‐Based α‐Tocopherol Cream for Photoprotection

AbstractThe application of a nanostructured lipid carrier (NLC) to ultraviolet (UV) filter encapsulation was found to enhance its safe use. In this work, a kenaf seed oil‐NLC (KSO‐NLC) coloaded with 1% diethylamino hydroxybenzoyl hexyl benzoate and 1% ethylhexyl triazone was used as an active ingredient in α‐tocopherol cream to develop a photoprotective prototype. It was then subjected to further analysis to determine its physical properties, storage stability, and cytotoxicity. The ratio of KSO‐NLC to α‐tocopherol cream was optimized based on the sun protection factor (SPF) value using a UV transmittance analyzer. The physical properties of the samples were analyzed, and the amount of α‐tocopherol was quantified by ultra‐high‐performance liquid chromatography. The optimized sample was then evaluated for in vitro antioxidant activities using 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid assays. Meanwhile, in vitro cytotoxicity was studied on a normal human dermal fibroblast cell line using thiazolyl blue tetrazolium bromide and cell counting kit‐8 assays. The sample of KSO‐NLC to α‐tocopherol cream in a ratio of 1:2 (N3) showed SPF value >50. Besides, the samples showed microbial stability and sustainable α‐tocopherol content upon 12 weeks of storage. The cytotoxicity evaluation of N3 and α‐tocopherol cream (N5) showed >100% cell proliferation, which indicated that there is no side effect on the cell growth, while triggering the cell proliferation with the presence of bioactive compounds. Overall, the findings of the study are promising for the development of new sunscreen formulation with the utilization of KSO‐NLC and palm‐based α‐tocopherol cream.

An Anti-Inflammatory 2,4-Cyclized-3,4-Secospongian Diterpenoid and Furanoterpene-Related Metabolites of a Marine Sponge Spongia sp. from the Red Sea.

Chemical investigation of a Red Sea Spongia sp. led to the isolation of four new compounds, i.e., 17-dehydroxysponalactone (1), a carboxylic acid, spongiafuranic acid A (2), one hydroxamic acid, spongiafuranohydroxamic acid A (3), and a furanyl trinorsesterpenoid 16-epi-irciformonin G (4), along with three known metabolites (−)-sponalisolide B (5), 18-nor- 3,17-dihydroxy-spongia-3,13(16),14-trien-2-one (6), and cholesta-7-ene-3β,5α-diol-6-one (7). The biosynthetic pathway for the molecular skeleton of 1 and related compounds was postulated for the first time. Anti-inflammatory activity of these metabolites to inhibit superoxide anion generation and elastase release in N-formyl-methionyl-leucyl phenylalanine/cytochalasin B (fMLF/CB)-induced human neutrophil cells and cytotoxicity of these compounds toward three cancer cell lines and one human dermal fibroblast cell line were assayed. Compound 1 was found to significantly reduce the superoxide anion generation and elastase release at a concentration of 10 μM, and compound 5 was also found to display strong inhibitory activity against superoxide anion generation at the same concentration. Due to the noncytotoxic activity and the potent inhibitory effect toward the superoxide anion generation and elastase release, 1 and 5 can be considered to be promising anti-inflammatory agents.

Chemical analysis, antioxidant, cytotoxic and antimicrobial properties of propolis from different geographic regions

Propolis is a resinous beehive product containing functional compounds and differs based on geographical region. Physicochemical properties of each propolis effectuate their uses within modern applications. Therefore, this study was aimed to evaluate the chemical composition, antioxidant, antimicrobial, and cytotoxic activity of propolis ethanol extracts (PEE) sourced from six geographical regions. Antioxidant potency was determined using four assays: DPPH, ABTS, reducing power, and malondialdehyde inhibition (MDA). The phenolic (TPC) and flavonoid content (TFC) was calculated as gallic acid and catechol equivalents, respectively. Antimicrobial properties of propolis against pathogens and toxigenic fungi were determined using agar well diffusion assay. The cytotoxicity effect was estimated against the human dermal fibroblast (HDF) cell line using MTT assay. The results manifested propolis variations of samples, specifically for the chemical composition (p < 0.05). Omanis' propolis recorded by the highest moisture content, while the Egyptian propolis featured by high protein content. Brazilians' propolis was distinguished among samples by the highest ash content (p < 0.05). Propolis from Saudi, Omani, China, and Bulgaria represented by higher fiber content. Egyptians' propolis showed a promising antioxidant and antimicrobial potency, reflecting a high activity against food pathogen and toxigenic fungi. The IC50 values of propolis samples following 24 h exposure to the normal human dermal fibroblast (HDF) cells did not show any cytotoxic effect. This study demonstrated the distinguishes between propolis sourced from different regions regarding their bioactive contents. The Egyptian's propolis can be recommended as a preservative additive that can be applied to solve numerous food safety issues.

3D Propolis-Sodium Alginate Scaffolds: Influence on Structural Parameters, Release Mechanisms, Cell Cytotoxicity and Antibacterial Activity.

In this study, the main aim was to fabricate propolis (Ps)-containing wound dressing patches using 3D printing technology. Different combinations and structures of propolis (Ps)-incorporated sodium alginate (SA) scaffolds were developed. The morphological studies showed that the porosity of developed scaffolds was optimized when 20% (v/v) of Ps was added to the solution. The pore sizes decreased by increasing Ps concentration up to a certain level due to its adhesive properties. The mechanical, swelling-degradation (weight loss) behaviors, and Ps release kinetics were highlighted for the scaffold stability. An antimicrobial assay was employed to test and screen antimicrobial behavior of Ps against Escherichia coli and Staphylococcus aureus strains. The results show that the Ps-added scaffolds have an excellent antibacterial activity because of Ps compounds. An in vitro cytotoxicity test was also applied on the scaffold by using the extract method on the human dermal fibroblasts (HFFF2) cell line. The 3D-printed SA–Ps scaffolds are very useful structures for wound dressing applications.

Development of Moringa oleifera Standardized Leaf Extract Nanofibers Impregnated onto Hydrocolloid Film as A Potential Chronic Wound Dressing

This research focuses on the development of a hybrid dressing, i.e. Moringa oleifera (MOL) leave extract nanofibers impregnated onto an alginate-pectin hydrocolloid film for chronic wound healing. The MOL nanofibers impregnated hydrocolloid films were characterised and optimised by physicomechanical properties, moisture transmission, swelling ratio, microscopy analysis, Franz diffusion drug release and cell viability assays. From the preformulation studies, PEO 6 % solution with viscosity above 1.3 Pa·s was found suitable to be electrospun into uniform nanofibers (diameter 322.7±78.02 nm). The moisture transmission rate and swelling ratio studies revealed that the MOL nanofiber-film was useful for the application of light to medium suppurating wounds. The Franz diffusion cell study showed that the electrospun duration could influence the amount of MOL released from the nanofibers-film. Finally, cell viability assays revealed that the MOL nanofibers-films hybrid dressing did not cause cytotoxicity to human dermal fibroblast and human epithelial keratinocytes cell lines. In conclusion, a hybrid MOL nanofibers impregnated hydrocolloid films dressing was successfully formulated and this study has implied that MOL nanofibers-film could be an alternative treatment option for treating chronic wounds.

In vitro toxicity assessment of crosslinking agents used in hyaluronic acid dermal filler

Hyaluronic acid (HA) dermal fillers are produced by crosslinking HA with agents, such as 1,4-butanediol diglycidyl ether (BDDE) and poly (ethylene glycol) diglycidyl ether (PEGDE) to acquire desired properties. Thus, the safety evaluation of these crosslinkers is needed at the cellular level. In the present study, cell viability, cytotoxicity, membrane integrity, reactive oxygen species (ROS), mitochondrial membrane potential (MMP), and inflammatory responses were evaluated in the human keratinocyte cell line, HaCaT and human dermal fibroblast cell line, HDF in response to treatment with the crosslinkers. In both the cell lines, BDDE significantly decreased cell viability at 100–1000 ppm, while PEGDE showed a decrease at 500–1000 ppm. In HaCaT cells, BDDE markedly increased cytotoxicity (lactate dehydrogenase release) at 100–1000 ppm, but PEGDE showed an increase at 500–1000 ppm. Cells treated with BDDE (100 ppm) caused alteration in the integrity of cell membrane and shape. In both the cell lines, BDDE-treated cells showed significantly higher ROS levels and MMP loss than PEGDE-treated cells. Also, BDDE-treated cells exhibited higher COX-2 expression at 100 ppm. Expression of inflammatory cytokines (TNF-α, and IL-1 β) was higher in BDDE-treated cells. Taken together, PEGDE-treated cells showed markedly lower cytotoxicity, ROS production, and inflammatory responses than BDDE-treated cells. Our data suggest that PEGDE is safer than BDDE as a crosslinker in HA dermal fillers.

Hydrostatic pressure can induce apoptosis of the skin

We previously showed that high hydrostatic pressure (HHP) treatment at 200 MPa for 10 min induced complete cell death in skin and skin tumors via necrosis. We used this technique to treat a giant congenital melanocytic nevus and reused the inactivated nevus tissue as a dermis autograft. However, skin inactivated by HHP promoted inflammation in a preclinical study using a porcine model. Therefore, in the present study, we explored the pressurization conditions that induce apoptosis of the skin, as apoptotic cells are not believed to promote inflammation, so the engraftment of inactivated skin should be improved. Using a human dermal fibroblast cell line in suspension culture, we found that HHP at 50 MPa for ≥ 36 h completely induced fibroblast cell death via apoptosis based on the morphological changes in transmission electron microscopy, reactive oxygen species elevation, caspase activation and phosphatidylserine membrane translocation. Furthermore, immunohistochemistry with terminal deoxynucleotidyl transferase dUTP nick-end labeling and cleaved caspase-3 showed most cells in the skin inactivated by pressurization to be apoptotic. Consequently, in vivo grafting of apoptosis-induced inactivated skin resulted in successful engraftment and greater dermal cellular density and macrophage infiltration than our existing method. Our finding supports an alternative approach to hydrostatic pressure application.

Evaluation of Gene Expression and In Vitro Enzyme Study for Antiaging Effect of Crocin and Lutein

Background: Tubular calyx of flowers of Nyctanthes arbour-tristis contains an apocarotenoid crocin, a major constituent present in saffron stigma. The flowers of N. arbortristis are readily available, hence can be an economic substitute for saffron. Lutein from flowers of Tagetes patula, is another carotenoid which is a popular antioxidant. Objective: Oxidative stress is a major contributor to the process of aging. Carotenoids are powerful antioxidants. Hence, the study was carried out to evaluate anticollagenase activity and antielastase activity using gene expression study in Human dermal fibroblasts. Methods: Crocin was isolated from the tubular calyx of Nyctanthes arbortristis using flash chromatographic technique and lutein was isolated using column chromatography. Anticollagenase and antielastase activity of crocin and lutein were carried out using collagenase from Clostridium histolyticum as enzyme and porcine pancreatic elastase. Cytotoxicity of crocin and lutein was determined in Human Dermal Fibroblast cell line (HDF) through MTT assay. In gene expression study, the HDF Cell line was inoculated with Crocin (450 and 250 ppm) and lutein (100 and 50 ppm) separately for 24 hrs and the m-RNA expression levels of COL Type-1 and elastin were determined using RT-PCR. The results were compared with standards. Result: Crocin and lutein both showed inhibition of collagenase and elastase enzyme which are responsible for aging process. The cytotoxic concentration CTC 50 (ppm) for Crocin and lutein was found to be 790.2 ppm and 137.14 ppm. Gene expression study on crocin rich extract of Nyctanthes arbortristis showed upregulation of both collagen and elastin gene whereas lutein rich extract having concentration100 μg/ml showed up regulation by 0.02 fold and concentration 50 μg/ml showed down regulation. Conclusion: In vitro collagenase and elastase enzyme study and Gene expression study showed that these carotenoids are potential antiageing agents which can be substituted to synthetic cosmeceuticals as well as saffron.

Urtica dioica Extract Inhibits Cell Proliferation and Induces Apoptosis in HepG2 and HTC116 as Gastrointestinal Cancer Cell Lines.

Nowadays the use of plant-derived products has been extensively examined in the treatment of many types of gastrointestinal cancers such as hepatocarcinoma and colon cancer. Urtica dioica is a traditional herb that has many pharmacological effects and wildly used as a therapeutic agent in cancer. Herein, we have evaluated the effects of the different concentrations of Methanolic Extract of Urtica dioica (MEUD) on viability, death pattern, and expression of the apoptosis-related gene in normal Human Dermal Fibroblast (HDF), hepatocarcinoma cell lines (HepG2) and colon-cancer cell line (HCT116). A high-performance liquid chromatography method was developed to simultaneously separate 3 phenolic acids in MEUD. HepG2 and HCT116 cell lines as well as HDF normal cell line were cultured in suitable media. After 24 and 48h, in the cultured cell with different concentrations of MEUD, cells viability was assessed by MTT assay, and apoptosis was also evaluated at the cellular level by Annexin V/PI flow cytometry analyzing and AO/EB staining. BCL2 and BAX gene expressions were assessed by TaqMan real-time PCR assay. MEUD showed antiproliferative effects on HepG2 and HTC116 cells after 48h with an IC50 value of about 410 and 420μg/ml, respectively (P < 0.001). Apoptotic cells were observed in HepG2 and HTC116 cells but not in HDF. Furthermore, the increased level of BAX/BCL-2 ratio was observed in HepG2 and HTC116 cells under the treatment of different concentrations of MEUD. The MEUD may influence hepatocarcinoma and colon-cancer cell lines at specific doses and change their proliferation rate by changing the expression of BAX and BCL2.

Efficient synthesis of amino acids capped gold nanoparticles from easily reducible aryldiazonium tetrachloroaurate(III) salts for cellular uptake study.

Biomimetic synthesis of gold nanoparticles (GNPs) is critical in biomedical applications. Gold bioconjugates were fabricated by capping the water-dispersible gold-carbon nanoparticles with tyrosine, tryptophan and cysteine amino acids. Incubation of the water-soluble and easily reducible aryldiazonium gold(III) salt [HOOC-4-C6H4N≡N]AuCl4 with amino acids at room temperature formed a purple color over a few minutes with tryptophan and tyrosine and over two hours with cysteine. Rarely that cysteine is capable of reducing gold(III) precursors; however, a cysteine capped gold bioconjugate was synthesized and characterized in this study. Capping GNPs with amino acids was confirmed by high resolution transmission electron microscopy (TEM) and agarose gel electrophoresis. Depending on the amino acid, synthesized particles size was 27.2 ± 5.4nm, 14.6 ± 7.7nm and 8.6 ± 2.6nm for tyrosine, tryptophan and cysteine, respectively. The amino acids capped GNPs showed negligible cytotoxicity to human dermal normal fibroblast cell lines. The highly water dispersible bioconjugates were studied for in vitro cellular uptake by HeLa cancer cells using confocal laser scan microscopy (CLSM) after being labelled with FITC (GNPs-COOH-FITC) and the nuclei were counter stained with DAPI fluorescent dyes. The biomimetic route for the synthesis of the amino acids reduced gold-carbon nanoparticles will benefit the applications in biomedical devices and biosensors.

Synthesis and in vitro biological evaluations of novel tetrapeptide as therapeutic agent for wound treatment

We report a new small peptide containing four amino acid residues (glycine-aspartic acid-proline-histidine) conjugated with palmitic acid (Palmitoyl-GDPH) that was synthesized, characterized and evaluated for its biological activities. The Palmitoyl-GDPH was prepared by solid phase peptide synthesis (SPPS) with high percentage purity of 98.6%. The results of circular dichroism (CD) demonstrated the feasibility and stability of Palmitoyl-GDPH secondary structure at many temperatures up to 60 °C. Palmitoyl-GDPH showed its greatest collagenase inhibition activity and nitric oxide (NO) scavenging effect of 80.00 ± 2.22% at 1.0 mg/ml and 83.40 ± 8.08% at 2.5 mg/ml, respectively. In addition, in-vitro cell based study revealed that Palmitoyl-GDPH was not toxic and possessed strong proliferative activity towards normal human dermal fibroblast (NHDF) cell line. Wound scratch assay method showed that Palmitoyl-GDPH significantly promoted the cell migration which progressed faster compared to tetracycline-treated group (positive control) by about 98.39 ± 2.79% and 95.79 ± 3.83%, respectively. Collectively, these results suggested that newly synthesized Palmitoyl-GDPH possessed a strong candidate for use as therapeutic agent and can be a novel approach in the treatment of cutaneous wounds.

In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer.

Microencapsulation and targeted delivery of cytotoxic and antibacterial agents of photodynamic therapy (PDT) improve the treatment outcomes for infectious diseases and cancer. In many cases, the loss of activity, poor encapsulation efficiency, and inadequate drug dosing hamper the success of this strategy. Therefore, the development of novel and reliable microencapsulated drug formulations granting high efficacy is of paramount importance. Here we report the in vitro delivery of a water-soluble cationic PDT drug, zinc phthalocyanine choline derivative (Cholosens), by biodegradable microcapsules assembled from dextran sulfate (DS) and poly-l-arginine (PArg). A photosensitizer was loaded in pre-formed [DS/PArg]4 hollow microcapsules with or without exposure to heat. Loading efficacy and drug release were quantitatively studied depending on the capsule concentration to emphasize the interactions between the DS/PArg multilayer network and Cholosens. The loading data were used to determine the dosage for heated and intact capsules to measure their PDT activity in vitro. The capsules were tested using human cervical adenocarcinoma (HeLa) and normal human dermal fibroblast (NHDF) cell lines, and two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. Our results provide compelling evidence that encapsulated forms of Cholosens are efficient as PDT drugs for both eukaryotic cells and bacteria at specified capsule-to-cell ratios.

Antiviral, Antibacterial, Antifungal, and Cytotoxic Silver(I) BioMOF Assembled from 1,3,5-Triaza-7-Phoshaadamantane and Pyromellitic Acid.

The present study reports the synthesis, characterization, and crystal structure of a novel bioactive metal-organic framework, [Ag4(µ-PTA)2(µ3-PTA)2(µ4-pma)(H2O)2]n·6nH2O (bioMOF 1), which was assembled from silver(I) oxide, 1,3,5-triaza-7-phosphaadamantane (PTA), and pyromellitic acid (H4pma). This product was isolated as a stable microcrystalline solid and characterized by standard methods, including elemental analysis, 1H and 31P{1H} NMR and FTIR spectroscopy, and single crystal X-ray diffraction. The crystal structure of 1 disclosed a very complex ribbon-pillared 3D metal-organic framework driven by three different types of bridging ligands (µ-PTA, µ3-PTA, and µ4-pma4−). Various bioactivity characteristics of bioMOF 1 were investigated, revealing that this compound acts as a potent antimicrobial against pathogenic strains of standard Gram-negative (Escherichia coli, Pseudomonas aeruginosa) and Gram-positive (Staphylococcus aureus) bacteria, as well as a yeast (Candida albicans). Further, 1 showed significant antiviral activity against human adenovirus 36 (HAdV-36). Finally, bioMOF 1 revealed high cytotoxicity toward an abnormal epithelioid cervix carcinoma (HeLa) cell line with low toxicity toward a normal human dermal fibroblast (NHDF) cell line. This study not only broadens the family of PTA-based coordination polymers but also highlights their promising multifaceted bioactivity.

Design, Synthesis, and Antimicrobial Evaluation of a New Series of N-Sulfonamide 2-Pyridones as Dual Inhibitors of DHPS and DHFR Enzymes.

Sulfonamides and trimethoprim (TMP) drugs are normally used to inhibit the action of dihydropteroate synthase (DHPS) and dihydrofolate reductase (DHFR) enzymes, respectively. In this work, a new series of N-sulfonamide 2-pyridone derivatives that combine the inhibitory activities of DHPS and DHFR into one molecule were synthesized and evaluated for its in vitro antimicrobial activity and the ability to inhibit the action of both enzymes simultaneously. The synthesis was carried out via the reaction of novel benzothiazol sulfonylhydrazide with ketene dithioacetal derivatives, and the structures of the resultant compounds were confirmed using spectral and elemental techniques. Among the synthesized compounds, five compounds 3b, 5a, 5b, 11a, and 11b were found to possess significant antimicrobial activities against tested bacterial and fungi strains. The compounds were also examined for their cytotoxicity on HFB4 human dermal fibroblast cell line using MTT assay. The in vitro enzyme assay study of these compounds against DHPS and DHFR enzymes showed that compound 11a was the most potent inhibitor against both enzymes with IC50 values of 2.76 and 0.20 μg/mL, respectively. Docking studies showed that this compound has occupied both the p-aminobenzoic acid and pterin binding pockets of DHPS as well as the pterin binding pocket of DHFR. The results of these investigations confirmed that compound 11a is the most potent dual DHPS/DHFR inhibitor.

Synthesis and Cytotoxic Analysis of Novel Myrtenyl Grafted Pseudo-Peptides Revealed Potential Candidates for Anticancer Therapy.

Myrtenal is a natural monoterpene isolated from essential oils of several plants and their derivates have shown to have several biological properties including cytotoxicity. The cytotoxic activity of these derivates are being investigated for their antitumor effect leading to the development of potential anticancer agents. In this study, novels Myrtenyl grafted pseudo-peptides were designed, synthesized and functionally characterized as possible therapeutic agents for cancer treatment. Thirteen novel Myrtenyl grafted pseudo-peptides were prepared in high atom economy and efficiency by a classic Ugi-4CR and sequential post-modification. Their structures were confirmed by NMR, and ESI-MS, and its cytotoxic activity was evaluated in three cancer cell lines and primary CD4+ T cells at different proliferative cycles. Our results revealed that some of these compounds showed significant cytotoxicity against human gastric, breast and colon adenocarcinoma cells lines, but not against human dermal fibroblast cell line. Moreover, from the thirteen novel myrtenyl synthesized the compound (1R,5S)-N-{[1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl]methyl}-N-[2-(cyclohexylamino)-2–oxoethyl]-6,6-dimethylbicyclo[3.1.1]hept-2-ene-2-carboxamide (3b) proved to be the best candidate in terms of acceptable EC50, and Emax values in cancer cell lines and at inducing cytotoxicity in CD4+ T cells undergoing active proliferation, without affecting non-proliferating T cells. Overall, the synthesis and characterization of our Myrtenyl derivates revealed novel potential anticancer candidates with selective cytotoxic activity.

Synthesis, Structural, and Cytotoxic Properties of New Water-Soluble Copper(II) Complexes based on 2,9-Dimethyl-1,10-Phenanthroline and Their One Derivative Containing 1,3,5-Triaza-7-Phosphaadamantane-7-Oxide.

A series of water-soluble copper(II) complexes based on 2,9-dimethyl-1,10-phenanthroline (dmphen) and mixed-ligands, containing PTA=O (1,3,5-triaza-7-phosphaadamantane-7-oxide) have been synthesized and fully characterized. Two types of complexes have been obtained, monocationic [Cu(NO3)(O-PTA=O)(dmphen)][PF6] (1), [Cu(Cl)(dmphen)2][PF6] (2), and neutral [Cu(NO3)2(dmphen)] (3). The solid-state structures of all complexes have been determined by single-crystal X-ray diffraction. Magnetic studies for the complex 1–3 indicated a very weak antiferromagnetic interaction between copper(II) ions in crystal lattice. Complexes were successfully evaluated for their cytotoxic activities on the normal human dermal fibroblast (NHDF) cell line and the antitumor activity using the human lung carcinoma (A549), epithelioid cervix carcinoma (HeLa), colon (LoVo), and breast adenocarcinoma (MCF-7) cell lines. Complexes 1 and 3 revealed lower toxicity to NHDF than A549 and HeLa cells, meanwhile compound 2 appeared to be more toxic to NHDF cell line in comparison to all cancer lines. Additionally, interactions between the complexes and human apo-transferrin (apo-Tf) using fluorescence and circular dichroism (CD) spectroscopy were also investigated. All compounds interacted with apo-transferrin, causing same changes of the protein conformation. Electrostatic interactions dominate in the 1/2 – apo- Tf systems and hydrophobic and ionic interactions in the case of 3.

Synthesis and biological evaluation of some 4-aminoquinoline derivatives as potential antitubercular agents

BackgroundBased on bioisosteric similarities with thiacetazone, a series of 7-chloro-4-aminoquinoline derivatives have been designed and synthesized. The target compounds were elucidated by NMR, mass, and FTIR spectral data. All synthesized compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv (MTB), and human dermal fibroblast cell lines were used to assess toxicity of selected ligands.ResultsAll of the designed compounds showed inhibition of MTB with MIC of 1.56–50 μM. Among the tested compounds, 7c and 7g proved to be most potent MTB inhibitors (MIC = 1.56 μM).ConclusionsThe outcome of present study suggests that most of the synthesized compounds are sensitive to Mycobacterium tuberculosis and showed acceptable range for molecular parameters. Thus, 7-chloro-4-aminoquinolines could be a useful lead for the development of new MTB inhibitory agents.

Anti-cancer effect of gallic acid in presence of low level laser irradiation: ROS production and induction of apoptosis and ferroptosis

BackgroundThere are different treatments for breast cancer and melanoma that mostly have some side effects. One of the therapeutic strategies is the use of natural components. Phenol components are a class of antioxidants in plants that have many biological functions like anticancer effects. Gallic acid (GA) is a natural polyhydroxy phenolic compound and commonly found in various foods. In the present study, GA effects alone and in combination with low-level laser irradiation on human dermal fibroblast cell line (HDF), human non-tumorigenic breast epithelial cell line (MCF10A), breast cancer cell line (MDA-MB-231) and melanoma cancer cell line (A375) was under the investigation.MethodsThe normal and cancerous cell lines were exposed to 660 nm low-level laser with 3 J/cm2 for 90 s. Then, the cells were treated with different concentrations of GA for 24 h. In another study, the cell lines firstly were treated with GA and then exposed to low-level laser irradiation. The effects of GA and low-level laser on cell survival and apoptosis were examined using MTT assay, light microscopy, ROS production assay, fluorescence microscopy (AO/EB double staining) and flow cytometry.ResultsThe results showed that pre-treatment with low-level laser and then GA reduced the survival of breast cancer cells and melanoma more than the first treatment with GA and then low-level laser irradiation. Our findings showed that ROS production in cells treated with both low-level laser and GA was more than the cells treated with GA alone. The apoptosis and ferroptosis assays confirmed the MTT results which combination treatment with low-level laser and then GA increase the cell death probably via apoptosis and ferroptosis cell death mechanisms compared to GA alone.ConclusionsThis study suggests that low-level laser irradiation alone is not able to cause death in human normal and cancerous cells. Preirradiation followed by GA treatment did not change the cell viability in human normal significantly but reduces the cell survival of cancer cells more than GA alone.

Electrospinning 3D bioactive glasses for wound healing

An electrospinning technique was used to produce three-dimensional (3D) bioactive glass fibrous scaffolds, in the SiO2–CaO sol-gel system, for wound healing applications. Previously, it was thought that 3D cotton wool-like structures could only be produced from sol-gel when the sol contained calcium nitrate, implying that the Ca2+ and its electronic charge had a significant effect on the structure produced. Here, fibres with a 3D appearance were also electrospun from compositions containing only silica. A polymer binding agent was added to inorganic sol-gel solutions, enabling electrospinning prior to bioactive glass network formation and the polymer was removed by calcination. While the addition of Ca2+ contributes to the 3D morphology, here we show that other factors, such as relative humidity, play an important role in producing the 3D cotton-wool-like macrostructure of the fibres. A human dermal fibroblast cell line (CD-18CO) was exposed to dissolution products of the samples. Cell proliferation and metabolic activity tests were carried out and a VEGF ELISA showed a significant increase in VEGF production in cells exposed to the bioactive glass samples compared to control in DMEM. A novel SiO2–CaO nanofibrous scaffold was created that showed tailorable physical and dissolution properties, the control and composition of these release products are important for directing desirable wound healing interactions.

Aluminium and calcium lake pigments of Lac natural dye

This work presents the physicochemical properties of the prepared lac lakes. The study revealed the stability, cytotoxicity and use of lac lake pigment as a cosmetic colorant. SEM, XRD and DSC were used to study the characteristics of the lac lakes.. The color stability of lac dye and its lakes was investigated at ambient temperature and at 45 °C, in sunlight,fluorescent light and darkness, for 3 months. Cytotoxicity on human dermal skin fibroblast cell lines was tested using MTT assay and the use of the lakes as a colorant in lip color product was studied. Different metal salts resulted in lac lakes of different shades and appearance. SEM, XRD and DSC results indicated that the morphology and structure of lac dye were changed after reacting with metal salts which support the coordination of metal ion with lac dye. The lac lakes were not cytotoxic to human dermal skin fibroblast cells (0.78-100 µg/mL). Lac lakes exhibited less alteration of color shade over acidic and basic conditions when compared with the lac dye itself. Additionally, the lake pigments displayed better color stability than lac dye and produced an orange-brown shade of lip color product. The results suggest that lac lake pigments have good potential for use as cosmetic colorant.