Citrus flavonoids-loaded chitosan derivatives-route nanofilm as drug delivery systems for cutaneous wound healing.

This study focuses on creating new forms of biomimetic nanofiber composites by combining copolymerizing and electrospinning approaches in the field of nanomedicine. The process involved utilizing the melt polymerization of proline (Pr) and hydroxyl proline (Hyp) to synthesize polymers based on Pr (PPE) and Hyp (PHPE). These polymers were then used in a grafting copolymerization process with chitosan (CS) to produce PHPC (1560 ± 81.08 KDa). A novel electrospun nanofiber scaffold was then produced using PHPC and/or CS, hyaluronic acid, polyvinyl alcohol, and naringenin (NR) as a loading drug. Finally, Mouse Dermal Fibroblast (MDF) cells were introduced to the wound dressing and assessed their therapeutic potential for wound healing in rats. The scaffolds were characterized by FTIR, NMR, DSC, and SEM analysis, which confirmed the amino acid grafting, loading drug, and porous and nanofibrous structures (>225 nm). The results showed that the PHPC-based scaffolds were more effective for swelling/absorption of wound secretions, had more elasticity/elongation, faster drug release, more MDF-cytocompatibility, and antibacterial activity against multidrug-resistant S. aureus compared to CS-based scaffolds. The in vivo studies showed that NR in combination with MDF can accelerate cell migration/proliferation, and remodeling phases of wound healing in both PHPC/CS-based scaffolds. Moreover, PHPC-based scaffolds promote collagen content, and better wound contraction, epithelialization, and neovascularization than CS-based, showing potential as wound-dressing.

Synthesis and Characterization of Novel pH-Responsive Aminated Alginate Derivatives Hydrogels for Tissue Engineering and Drug Delivery.

AIMS: The aims of this study are to synthesize new derivatives of sodium alginate that improve the inherent properties, such as hydrogel strengthening, and create environmental sensitivity, such as pH sensitivity, for use in drug delivery. BACKGROUND: Today, hydrogels, due to outstanding properties such as biodegradability, biocompatibility, mechanical properties, and response to stimuli properties, are widely used as harmless biomaterials in various fields in drug delivery, wound dressing, and tissue engineering. Stimulus-sensitive polymers significantly respond to slight changes in their environment. Different types of stimuli are used to influence the properties of polymers, the most important of which are temperature and pH because these are two vital factors in the human body; hence, temperature-sensitive and pHsensitive hydrogels have been extensively studied. The ability to absorb water and swell the hydrogel is due to hydrophilic chains in the hydrogel network, and water absorption by hydrogel can be controlled by response to the stimuli. Since hydrogels mimic human tissue, the ability to retain water in them is essential. As a result, it is considered in many biomedical drug delivery systems. Stimulusresponsive swelling can control diffusion out of and into the hydrogel network, which allows temporal and spatial control of drug release. When a drug is loaded onto a biodegradable and stimulisensitive hydrogel, the drug delivery system has the added advantage of sustained release of the drug, which reduces side effects. METHODS: In this study, two different hydrocarbons, [1,3-diaminopropane (DAP)] as a short-chain hydrocarbon, and [1,7-diaminoheptane (DAH)] as a long-chain hydrocarbon were grafted onto three types ofsodium alginate (SA), through amide bond linkages. The hydrogel copolymer matrices were compared with sodium alginate (SA) beads. The graft copolymers were characterized using FTIR, 1HNMR, XRD spectroscopy, elemental analysis (CHNS) and thermal analysis (TGA, DTA and DSC). An environmental scanning electron microscope (ESEM) was used to investigate the surface morphology of hydrogels. RESULTS: Effects of variables such as the length of hydrocarbon chains cross-linked to alginate, temperature, pH, and cross-linkers on the properties of hydrogels investigated in the temperature range of 2-70 ˚C and two different pH values (4.4 and 7.4). The results showed that when the hydrocarbon chain length of diamines decreases, the extent of cross-linking and strength of the hydrogels are increased. Other results suggest that the hydrogels obtained from high-viscosity alginate derivatives had positive pH sensitivity. Hydrogels prepared in this study demonstrated good mechanical and swelling ratios that are necessary for wound dressing. CONCLUSION: DAP-g-SA and DAH-g-SA pH-sensitive hydrogels were successfully synthesized through amide bond linkages. The new synthesis derivatives showed lower swelling levels at low pH (4.4). In contrast, their swelling levels at higher pH (7.4) were significantly enhanced. Higher swelling degree could be obtained at high pH. pH-responsive hydrogels are especially useful for various biological applications due to their unique feature of controlled swelling, biodegradability, biocompatibility, and fluid retention in their network structures. pH-responsive hydrogels, as intelligent systems, can be used in controlled-release drug delivery systems such as insulin delivery.

Swimming training combined with chitosan supplementation reduces the development of obesity and oxidative stress in high-fat diet-fed mice.

Obesity is often introduced as one of the metabolic disorders caused by imbalance between energy consumption and metabolisable energy intake. Experts in the field considered obesity as one of the robust risk factors for the lifestyle-associated diseases. The present research examined interventional effects of marine chitosan (CS), swimming training (ST) and combination of CS and ST (CS + ST) in the mice fed with high-fat diets (HFD). In this study, sample size was considered more than three in groups. Forty mice were randomly divided into five groups (n 8 per group) including control group (received the standard diet), HFD group (received high-fat food with 20 % fat), HFD + CS group (treated with high-fat food with 5 % CS), HFD + ST group (treated with HFD and ST) and HFD + CS + ST group (treated with high-fat food with 5 % CS and ST). After 8 weeks, the blood glucose, oxidative stress (OS) and lipid profile were measured. The results showed that CS + ST group has more effects in the control of body weight with the increased concentration of HDL-cholesterol, OS inhibition via enhancing the body antioxidant capacity in comparison with the ST or CS alone in HFD-fed mice. Moreover, lipid profile was improved in CS + ST-treated mice compared with HFD-treated mice, and OS inhibition correlated with the greater activities of the antioxidant enzyme enhances the lipid oxidation, cholesterol and fatty acid homoeostasis. The results suggested that a dietary intervention with a combined ST and CS can be a feasible supplementary for human prevention of obesity.

Phytochemical analysis of Holothuria leucospilota, a sea cucumber from Persian Gulf.

Sea cucumbers are widely consumed in traditional medicine and food. These animals have a considerable secondary metabolite and also several potential biological activities. This study investigated the phytochemical and cytotoxic evaluation of Holothuria leucospilota (H. leucospilota), a sea cucumber from Persian Gulf. The saponin composition of H. leucospilota was studied by different partitioning and chromatography methods such as thin layer chromatography (TLC), medium pressure liquid chromatography (MPLC) and high performance LC (HPLC). The marine sea cucumber Holostane-type triterpenoids (1-3) were characterized by physical and spectroscopic examination (1 and 2 dimensional neuclear magnetic resonance and mass experiments) with data analysis. The structure of compounds 1-3 identified as echinoside A, holothurine A, and 24-dehydroechinoside A, showed moderate cytotoxic activity with IC50 values of 1.9 ± 0.07, 6.8 ± 0.23, and 2.57 ± 0.18 µg/mL against HeLa and 10.4 ± 0.32, 8.9 ± 0.24, and 4.4 ± 0.13 on HUVEC cell line, respectively. In conclusion, the holostane-type triterpenoids showed moderate cytotoxic activity against HeLa cell line and have a prosperous future to be introduced as a lead structure.

Quantitative evaluation of n-alkanes, PAHs, and petroleum biomarker accumulation in beach-stranded tar balls and coastal surface sediments in the Bushehr Province, Persian Gulf (Iran).

Coastal areas within the Bushehr Province (BP), Persian Gulf, Iran, face great challenges due to the heavy organic contamination caused by rapid industrialization, and the presence of numerous oil fields. In addition, in 2014, a significant number of tar balls are found along the coasts of BP. A total of 96 samples (48 coastal sediments and 48 tar balls) were taken from eight sampling points at the BP coast during the summer of 2014. These samples were analyzed to identify the sources and characteristics of their organic matter using diagnostic ratios and fingerprint analysis based on the distribution of the source-specific biomarkers of n-alkanes, PAHs,1 hopanes and steranes. Mean concentration of n-alkanes (µg g-1 dw) and PAHs (ng g-1 dw) varied respectively from 405 to 220,626, and 267 to 23,568 in coastal sediments, while ranged respectively from 664 to 145,285 and 390 to 46,426 in tar balls. In addition, mean concentration of hopanes and steranes (ng g-1 dw) were between 18.17 and 3349 and 184.66 to 1578 in coastal sediments, whereas in tar balls were 235-1899 and 520-1504, respectively. Pri/Phy2 ratio was 0.25 to 1.51 (0.65) and 0.36 to 1 (0.63) in coastal sediment and tar ball samples, respectively, and the occurrence of UCM3 in both matrices, reflecting the petrogenic OM4 inputs and chronic oil contamination, respectively. The C30 and C29 homologues followed Gammacerane were detected in both matrices, in particular those collected from intensive industrial activities, suggesting petrogenic sources of OM. The coastal sediment PAHs profiles were significantly dominated by HMW5-PAHs in the Bahregan Beach (BAB) (78% of total PAHs), Bandare-Genaveh (GP) (66%), and Bandare-Bushehr (BUB) (61%) stations, while the Bashi Beach (BSB) (40%), Bandare-Kangan (KP) (57%), and Bandare-Asaluyeh (AP) (51%) stations exhibited higher proportion of LMW6-PAHs. PCA7 indicated that the tar ball and coastal sediment samples deposited along the Southwest of the BP beaches are most likely originated from the Abuzar oil. Based on the intensity of the anthropogenic activities, NPMDS8 analysis revealed that the GP, BAB, NNP, AP, and KP sampling sites had a high concentration of detected organic pollutants. To the best of our knowledge, this is the first study that investigates oil pollution in costal sediments and tar balls in the BP, providing insights in to the fate of oil in the coastal areas of the Persian Gulf, Iran.

Solvent-free preparation of novel 2-[phenyl (pyridine-2-ylamino) methyl] phenols as pseudo-betti processor for natural products.

BACKGROUND: 2-Aminopyridine and benzaldehydes mixture readily reacted with phenols at 80°C without any solvents to produce novel 2-[phenyl (pyridine-2-yl amino (methyl] phenol derivatives as pseudo-Betti products in good to high yields. These compounds are efficient processor for synthesis of the natural products. OBJECTIVES: We decided to report the synthesis of a series of novel N-heteroaryl-arylmethyl phenols via a simple three-component, one-pot method, using aromatic aldehydes, heteroaryl amines, and phenols in the absence of any acid catalysts and under solvent-free conditions. MATERIALS AND METHODS: All starting materials were purchased from Merck and Aldrich companies. The IR spectra were recorded on a Perkin-Elmer RXI infrared spectrometer. RESULTS: The reaction is convenient, operationally simple, proceeds quickly, and does not need solvents or expensive starting materials. The structures of the products were characterized by their spectral (1H NMR and IR) data. CONCLUSIONS: We have developed a new, simple, and efficient method for one-pot aminoalkylation of active phenol compounds with various imines prepared from 2-aminopyrimidine and benzaldehydes in good to high yields (40%-97%).

Marine Sponge/H3PO4: As a Naturally Occurring Chiral Catalyst for Solvent-free Fischer-Indole Synthesis.

BACKGROUND: A new and efficient method have been developed for the synthesis of different indole derivatives from various ketones, having at least one hydrogen atom attached to each of their α-carbon atoms, and hydrazines in solvent-free conditions, using marine sponge/H3PO4 as a naturally occurring chiral catalyst. OBJECTIVES: This study recommended the use of marine sponge/H3PO4 as a naturally occurring chiral catalyst for preparation of phenylhydrazones from ketones having one α-hydrogen and subsequent cyclisation of the products to indoles. MATERIALS AND METHODS: The reaction was carried out by mixing the phenylhydrazine, ketone, and marine sponge/H3PO4 powder in mortar and pestle; the mixture was ground at room temperature in an appropriate time until TLC show the completion of the reaction. The product extracted by CH2Cl2 and evaporation of solvent yields the products. RESULTS: In this research work, several indoles are synthesized using phenylhydrazine and aliphatic or aromatic ketone as starting materials, in the presence of marine sponge/H3PO4 powder as a natural catalyst under solvent-free condition. CONCLUSIONS: We found marine sponge/H3PO4 to be an effective catalyst for indolisation of phenylhydrazones from ketones having α-hydrogens in solvent-free conditions.

SiO2/H2SO4: An Efficient Catalytic System for Solvent-free 1, 5-benzodiazepines Synthesis.

BACKGROUND: 1, 5-Benzodiazepines have been investigated extensively by organic chemists due to their medicinal and pharmacological properties. These compounds are synthesized by condensation of o-phenylenediamines with carbonyl compounds in the presence of acid catalysts. OBJECTIVES: During our studies on the application of silica resin with acid functional moieties, we found that SiO2/H2SO4 mixture is a simple and efficient catalyst for this method under microwave irradiation. MATERIALS AND METHODS: The reaction was carried out simply by grinding SiO2/H2SO4 mixture with o-phenylenediamine, and ketone in the mortar; then the mixture was poured out into a sealed flask. Subsequently, it was irradiated in a microwave oven. RESULTS: In this method a series of cyclic and acyclic ketones underwent above conversion to form corresponding 1, 5-benzodiazepines. CONCLUSIONS: In conclusion, this method is a simple, rapid, and high yielding reaction (78-95%).