Rollinsdalby2855

The present study was done to uncover the possible beneficial and/or detrimental effect(s) of nano-micelle curcumin (NMC) on oocyte in-vitro maturation and pre-implantation embryo development. Forty-eight mature female Wistar rats were assigned to control, 7.5, 15, and 30 mg/kg-1 NMC-receiving (orally, for 48 days) groups. To assess the cumulus-oocyte complexes (COCs), the ovaries were stimulated by administrating (i.p.) a 25 IU of the pregnant mare's serum gonadotropin (PMSG) hormone. Following 48-h, 15 IU of hCG was injected (i.p.), and the COCs were taken after 16-18-h. To analyze the pre-implantation embryo development ratio, the sperms were collected from clinically healthy male Wistar rats, and 3.0-3.6 × 106 per mL was added into the fertilization drop. The animals in 7.5 mg/kg-1 NMC-receiving group exhibited a higher oocyte number versus control and other NMC-receiving groups. The NMC, in a dose-dependent manner, decreased the Zygote, 2-cell, blastocyst percentages, as well as hatched embryos, compared to the control group (P less then 0.05). The 15 and 30 mg/kg-1 NMC-receiving groups represented a remarkable enhancement in type I arrest. Meanwhile, a significant (P less then 0.05) reduction was revealed in type III embryo arrest in the same groups. The NMC, at 7.5 mg/kg-1 potentially enhances the oocyte number, while it fairly reduces the pre-implantation embryo development, even when it is administrated in dose levels of 7.5 mg/kg-1 and/or higher. Although more studies are needed, the NMC could be considered as a suppressor of fertility potential, when consumed chronically even in low doses.Since melanocytes are the origin of melanoma and some skin disorders such as melasma, they are important cells from the perspective of medicinal chemistry. Therefore, a medication that can simultaneously overcome these diseases will be a successful potential therapeutic agent. Arbutin with phenolic structure is a powerful natural anti-tyrosinase agent. Hence, the phenolic structure of this drug, prompted us to design its novel calix [4]arene-based cluster. Therefore, the present study reports the synthesis and in-vitro bio-activities of cyclic tetramer of arbutin in comparison to its simple drug unit as the reference medication. The in-vitro biological results showed amplified anti-tyrosinase (6-fold) and anti-melanoma (27-fold) activities, in addition to more aqueous solubility (8-fold) for this cluster in relation to arbutin. Therefore, compared to arbutin, more bioactive cluster can be considered as a novel water-soluble melanogenesis inhibitor with high anti-melanoma activity.A target of best dissolution improvement of poorly soluble drugs is a necessity for the success of formulation in industry. The present work describes the preparation, optimization, and evaluation of a new spherical agglomeration technique for glimepiride as a model of poorly soluble drugs. It involved the emulsification of a drug solution containing a dispersed carrier that tailors the crystal habit of the drug to a perfect spherical geometry, in a poor solvent containing a hydrophilic polymer which imparts sphericity and strength to the formed agglomerates. The FTIR peaks of optimized product did not show any sign of chemical interaction between the drug and adsorbed carrier. The DSC and X ray diffractogram showed a peak characteristic of spherical agglomerates with much less intensity than that of glimepiride. The dissolution t1/2 of the drug slightly decreased from 381 min to 334 min in plain agglomerates. Introducing polymers in the aqueous phase of emulsion led to an improvement in the dissolution, reflected in t1/2 ranging from 118 to 231 min. Agglomerates prepared with Starlac/PVP demonstrated the most optimum physicochemical characteristics being spherical, with the best flowability and packability parameters. The t1/2 was as short as 19 min. The new carrier/polymer system offered a synergistic combination that highly contributed in dissolution enhancement of glimepiride. The spheronization and amorphisation offered by the new technique could account for such improvement.This study aimed to evaluate the in-vitro and in-vivo biological activities of newly synthesized nanochelating based silver nanoparticles (AgNPs) in mouse model. Nanochelating technology was used to design and synthesize the AgNPs. The animals studies were including the lethal dose (LD50) determination by the intraperitoneal administration in mice, and determination of liver enzymes levels and hematological parameters. Flow cytometry analysis was used to quantitatively determine apoptosis and necrotic cells in-vitro. The NPs A and NPs B have LD50 = 250 mg/kg and LD50 = 350 mg/kg, respectively and classified as non-toxic. In general, minor alterations were observed in levels of liver enzymes as indicative of liver damage. For blood parameters several factors associated with significant changes in AgNPs treated animals. Regarding animals weight, combination therapy showed more effective to maintain animals weight losses after infection. Flow cytometry results showed that AgNPs induced cell apoptosis-necrosis depends on AgNP size, concentration and exposure time. Cells damage due to AgNPs (A) with lower size (20-25 nm) were relatively more than cells exposed to AgNPs (B) (30-35 nm). The findings support the potent antibacterial activities of nanochelating based AgNPs. Also, the present study showed that nanochelating based AgNPs induce a moderate level of apoptosis/necrosis in mice, and affected several clinical parameters like blood parameters, liver enzymes, and body weight with no definite signs of toxicity.Functional foods have emerged as a new approach to improve human health in term of nutraceutical to prevent people from illness rather than cure patients through medical treatment. In Asian society, particularly in Thailand, the utilizations of functional ingredients have been integrated in every parts of ordinary life. In this study, the tyrosine kinase activity of epidermal growth factor receptor (EGFR) inhibiting properties of 23 Thai's herbs-ethanol extracts have been examined. The crude extracts of only four species that inhibit the activity of EGFR-tyrosine kinase, Azadirachta indica (neem, Sa-dao), Brucea javanica (L.) Merr. (Rajadad), Hibiscus sabdariffa L. (Roselle, Krachiap daeng), and Saccharum chinensis Roxb. selleckchem (Red sugar cane). Moreover, only ethanol extractions from A. indica and B. javanica were also showed antitumor effect to non-small cell lung cancer, A549 cells.Recently Nutrition and Food Chemistry researches have been focused on plants and their products or their secondary metabolites having anti-alzheimer, anti-cancer, anti-aging, and antioxidant properties. Among these plants Salvia L. (Lamiaceae) species come into prominence with their booster effects due to high antioxidant contents, which have over 900 species in the world and 98 in Turkey. Some Salvia species are already in use as herbal treatment of vessel stiffness, Dementia like problems and cancer. Recently some species of Salvia are of extensive research topic. In this study, inhibitory potentials of secondary metabolites, rosmarinic acid, salvigenin, salvianolic acid A and B, tanshinone I and IIA, cyrtotanshinone, dihydrotanshinone I, carnosic acid, carnosol, and danshensu sodium salt were investigated against acetylcholinesterase, butyrylcholinesterase, urease and tyrosinase enzymes both in-vitro and in slico in detail. Elevated inhibitory effects on acetyl- and butyryl-cholinesterase of dihydrotanshinone I (IC50 1.50 ± 0.02 and 0.50 ± 0.01 µg/mL, respectively), carnasol (IC50 11.15 ± 0.05 ve 3.92 ± 0.03 µg/mL) and carnosic acid (IC50 31.83 ± 0.65 ve 4.12±0.04 µg/mL) were observed. Furthermore, all other secondary metabolites were active against butyrylcholinesterase. Anti-urease (42.41 ± 0.85%) and anti-tyrosinase (39.82 ± 1.16%) activities of tanshinone I were also observed. Potential inhibitory effects of these molecules on target proteins were investigated using DOCK and molecular dynamics calculations. Dock score analysis and Lipinski parameters were demonstrated that these ligands are potential inhibitors against relevant enzymes. Our findings suggest that Salvia species can be utilized as a ptential source of anti-alzheimer active compounds for designing novel products.A new phthalide, namely 7-methoxy-3-propylidenephthalide (1), along with two known compounds (2, 3) were isolated from the roots of the edible herb Levisticum officinale W.D.J. Koch, commonly known as lovage and well known in traditional medicine for its spasmolytic and diuretic effects. The structure of the new compound was established by HRMS and 1D & 2D NMR (1H 1H COSY, HMQC, and HMBC) spectroscopic analysis. All compounds are reported for the first time from L. officinale. Compounds 1-3 were tested against two Gram negative (Escherichia coli, Pseudomonas aeruginosa) and two Gram positive (Staphylococcus aureus and vancomycin-resistant Enterococcus [VRE] faecium) bacteria strains. Compound 3 was active against S. aureus, E. coli and vancomycin-resistant E. faecium with MIC values of 16, 64, and 128 μg/mL, respectively.Recent studies suggest that reducing the induction temperature would improve the quality of some recombinant inclusion bodies (IB) by providing a native-like secondary structure and leading to an improvement in protein recovery. This study focused on optimizing the solubilization condition of Reteplase, a recombinant protein with 9 disulfide bonds. The influence of lowering induction temperature and urea concentration was investigated on the secondary structure of the recombinant protein through FTIR analysis. Induction temperature reduction decreased the percentage of helixes and loops from 49 to 8. In addition, FTIR spectroscopy corroborates the drastic impact of this parameter on Reteplase secondary structure. Even though lowering urea concentration tripled the solubility of IBs expressed at lower induction temperature, the final yield is still quite low to be considered as optimum. On the other hand, the percentage of beta strands and turns in secondary structure of dissolved proteins were proportional to urea concentration. Therefore, in case of Reteplase, protein expression at low temperature (25 °C) was not efficient to improve the protein recovery yield. Future studies need to focus on using other methods of solubilizing IBs to improve protein recovery.Wnts are the major ligands responsible for activating Wnt signaling pathway through binding to Frizzled proteins (Fzd) as the receptors. Among these ligands, Wnt2 plays the main role in the tumorigenesis of several human cancers especially colorectal cancer (CRC). Therefore, it can be considered as a potential drug target. The aim of this study was to identify potential drug candidates against two binding sites of Wnt2. Structure-based virtual screening approaches were applied to identify compounds against binding sites of Wnt2 for inhibiting the interaction Wnt2 and Fzd receptors. The best hit compounds from molecular docking of National Cancer Institute diversity set II database were used for structural similarity search on ZINC database, obtaining large hit compounds query to perform a virtual screening and retrieving potential lead compounds. Eight lead compounds were selected while their binding affinity, binding modes interactions, and molecular dynamics simulations studies were assessed. Molecular docking studies showed that eight selected lead compounds can bind to the desired binding sites of Wnt2 in a high affinity manner.