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- Magnolol Causes Alterations in the Cell Cycle in Androgen Insensitive Human Prostate Cancer Cells In Vitro by Affecting Expression of Key Cell Cycle Regulatory Proteins. [JOURNAL ARTICLE]
- Nutr Cancer 2014 Sep 29.:1-11.
Prostate cancer, one of the most common cancers in the Western world, affects many men worldwide. This study investigated the effects of magnolol, a compound found in the roots and bark of the magnolia tree Magnolia officinalis, on the behavior of 2 androgen insensitive human prostate cancer cell lines, DU145 and PC3, in vitro. Magnolol, in a 24-h exposure at 40 and 80 μM, was found to be cytotoxic to cells. Magnolol also affected cell cycle progression of DU145 and PC3 cells, resulting in alterations to the cell cycle and subsequently decreasing the proportion of cells entering the G2/M-phase of the cell cycle. Magnolol inhibited the expression of cell cycle regulatory proteins including cyclins A, B1, D1, and E, as well as CDK2 and CDK4. Protein expression levels of pRBp107 decreased and pRBp130 protein expression levels increased in response to magnolol exposure, whereas p16(INK4a), p21, and p27 protein expression levels were apparently unchanged post 24-h exposure. Magnolol exposure at 6 h did increase p27 protein expression levels. This study has demonstrated that magnolol can alter the behavior of androgen insensitive human prostate cancer cells in vitro and suggests that magnolol may have potential as a novel anti-prostate cancer agent.
- A literature review and case series of accelerating fracture healing in postmenopausal osteoporotic working women. [Journal Article, Review]
- J Orthop 2014 Sep; 11(3):150-2.
Majority of fractures do not cause significant long-term morbidity and mortality. A 10% of these fractures result in impaired fracture healing, drastically affecting quality of life in affected patients. Satisfactory healing of these osteoporotic fractures are critically important to functional recovery, morbidity, and quality of life. Some therapies for osteoporosis may affect the processes associated with bone repair. For example, bisphosphonates in experimental models are associated with increased callus size and mineralization, reduced callus remodeling, and improved mechanical strength. Local and systemic bisphosphonate treatment may improve implant fixation. No negative impact on fracture healing has been observed, even after major surgery or when administered immediately after fracture. For the osteoanabolic agent teriparatide, case reports and a randomized trial have produced mixed results, but they are consistent with a positive impact of teriparatide on fracture healing. At this point, therefore, there is no evidence that osteoporosis therapies are detrimental to fracture healing with some promising experimental evidence for positive effects on healing, notably for those agents whose actions are primarily anabolic.
- Recent advances in chronic granulomatous disease. [JOURNAL ARTICLE]
- J Infect 2014 Sep 25.
Chronic Granulomatous Disease (CGD) is a primary immunodeficiency caused by abnormities in the NADPH Oxidase that is involved in the respiratory burst responsible for initiating the killing of microbes ingested by phagocytic cells. The hallmark of CGD is recurrent infection but the inflammatory complications can prove difficult to treat. New insights into the mechanisms responsible for the inflammatory complications have led to new therapies. The treatment of CGD colitis with an anti-tumour necrosis alpha agent has been shown to be successful but associated with significant infectious complications. Haematopoietic stem cell transplants offer the possibility of cure for those with ether a matched or unrelated donor transplant, with results of the latter improving significantly over recent years. Gene Therapy offers the promise of cure without the need for a transplant but better vectors are required.
- Discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis biofilms using a scaffold hopping strategy. [JOURNAL ARTICLE]
- Bioorg Med Chem Lett 2014 Sep 15.
Staphylococcus aureus and Staphylococcus epidermidis are recognized as the most frequent cause of biofilm-associated nosocomial and indwelling medical device infections. Biofilm-associated infections are known to be highly resistant to our current arsenal of clinically used antibiotics and antibacterial agents. To exacerbate this problem, no therapeutic option exists that targets biofilm-dependent machinery critical to Staphylococcal biofilm formation and maintenance. Here, we describe the discovery of a series of quinoline small molecules that demonstrate potent biofilm dispersal activity against methicillin-resistant S. aureus and S. epidermidis using a scaffold hopping strategy. This interesting class of quinolines also has select synthetic analogues that demonstrate potent antibacterial activity and biofilm inhibition against S. aureus and S. epidermidis.
- Evaluation of hypoglycemic and hypolipidemic activity of methanol extract of Brassica oleracea. [Journal Article]
- Chin J Nat Med 2014 Sep; 12(9):648-53.
The hypoglycemic and hypolipidemic effects of the methanol extract of Brassica oleracea var. capitata (MEB) was evaluated in alloxan-induced diabetic rabbits.The study was conducted on twenty-eight healthy white rabbits of either sex. All animals were equally divided into four groups. After confirmation of hyperglycemia, the animals of the treated and standard groups were administered MEB (500 mg·kg(-1)) and glibenclamide (10 mg·kg(-1)), respectively for 15 and 30 days. The animals of the normal and diabetic controls received normal saline 1 mL/day equivalent to the volume of doses given to the test and standard animals. Biochemical tests were performed at the end of dosing, i.e. the 16(th) and 31(st) days.The MEB revealed a decrease of 106.6 mg·dL(-1) in fasting blood glucose as compared to diabetic control, which was almost comparable to glibenclamide; both of these changes were highly significant. The decrease in total cholesterol and low density lipoprotein was 94.3 and 96.5 mg·dL(-1), respectively, whereas the high-density lipoprotein was increased by 26.7 mg·dL(-1), as compared to diabetic control. All of the changes in lipid profile were statistically significant.These results suggest the potential of MEB as a hypoglycemic and hypolipidemic agent.
- Effects of age on the pharmacokinetics of tramadol and its active metabolite, O-desmethyltramadol following intravenous administration to foals. [JOURNAL ARTICLE]
- Equine Vet J 2014 Sep 29.
Tramadol is an analgesic agent used in humans and a number of veterinary species. The pharmacokinetics and behavioural effects of tramadol and its active metabolite have been described in adult horses, but not in young foals.To characterise the pharmacokinetics, metabolism and some induced behavioural and physiologic responses following i.v. tramadol administration in the same group of foals on 4 different occasions, from a few days after birth to 43 days of age.Experimental.Tramadol was administered intravenously (3 mg/kg bwt) to a group of 8 foals on 4 separate occasions at 6-8, 13-15, 20-22 and 40-43 days of age. Blood samples were collected prior to administration and at multiple times until 48 h post administration. Blood samples were analysed for tramadol and metabolite concentrations and pharmacokinetics determined at each age. Behavioural and physiologic effects were also assessed.The average volume of distribution was 5.10, 4.63, 4.02 and 3.84 L/kg and clearance 3.44, 3.08 and 3.14 and 2.69 L/h/kg when foals were 6-8, 13-15, 20-22 and 40-43 days of age, respectively. There was not a significant difference in the elimination half-life between age groups (1.52, 1.73, 113 and 1.51 for 6-8, 13-15, 20-22 and 40-43 days of age, respectively). The metabolites produced were the same as in adult horses, however, glucuronidation capabilities, appeared to increase with increasing age. Tramadol administration was well tolerated at all ages studied with sedation noted in the older 3 age groups.Tramadol appears to be consistently well-tolerated following intravenous administration of 3 mg/kg bwt to foals ranging in age from 1-6 weeks. Although analgesic concentrations in foals have yet to be established, the results of this study support further study of tramadol for clinical use in foals.
- Properties and characterization of agar/CuNP bionanocomposite films prepared with different copper salts and reducing agents. [JOURNAL ARTICLE]
- Carbohydr Polym 2014 Dec 19.:484-492.
Various types of agar-based bio-nanocomposite (BNC) films were prepared by blending agar and six different copper nanoparticles (CuNPs) with different shapes and sizes obtained from three different sources of copper salts and two different reducing agents. The BNC films were characterized by UV-visible, FE-SEM, FT-IR, and XRD. The thermogravimetric study showed that the melting point of BNC films was increased when ascorbic acid was used as a reducing agent for CuNPs synthesis. Apparent surface color and transmittance of agar film was greatly influenced by the reinforcement of CuNPs. However, mechanical and water vapor barrier properties did not change significantly (p>0.05) by blending with CuNPs. Tensile modulus and tensile strength decreased slightly for all types of CuNPs reinforced while elongation at break slightly increased when CuNPs produced by ascorbic acid were blended. The agar bio-nanocomposite films showed profound antibacterial activity against both Gram-positive and Gram-negative food-borne pathogenic bacteria.
- Selective extraction of polysaccharide affects the adsorption of proanthocyanidin by grape cell walls. [JOURNAL ARTICLE]
- Carbohydr Polym 2014 Dec 19.:102-114.
Cell wall material was isolated from two Vitis vinifera grape varieties, Cabernet Sauvignon and Shiraz, following a buffered phenol extraction method. Using sequential fractionation in chelating agent, then increasing the molarity of aqueous potassium hydroxide, polysaccharide classes were selectively extracted from cell walls to produce fractions of defined polysaccharide composition. Following the application of phloroglucinolysis and a modified HCl-butanol colourimetric assay to cell wall fractions, more than 54% of cell wall-bound proanthocyanidin was localised within the chelator-soluble (pectic) fraction. Model adsorption experiments with a purified skin proanthocyanidin confirmed that the removal of pectic polysaccharides by chelator most significantly reduced the adsorption of proanthocyanidin by cell walls. Nevertheless, cell wall hemicellulosic fractions retained a high binding capacity for proanthocyanidin, although lower than that observed when pectin was present. Following removal of hemicelluloses by fractionation, the primarily lignocellulosic residue had a significantly reduced affinity for proanthocyanidin. With the exception of lignocellulose, a greater selectivity of adsorption for higher molecular mass proanthocyanidins was observed by the respective cell wall fractions.
- Oxidation and pH responsive nanoparticles based on ferrocene-modified chitosan oligosaccharide for 5-fluorouracil delivery. [JOURNAL ARTICLE]
- Carbohydr Polym 2014 Dec 19.:27-35.
Stimuli-responsive nanoparticles based on biodegradable and biocompatible saccharides are potentially superior carriers under different physical conditions. In this study, we present a detailed investigation on the oxidation and pH responses of ferrocene-modified chitosan oligosaccharide (FcCOS) nanoparticles for 5-Fluorouracil (5-FU) Delivery. The dispersion of FcCOS nanoparticles depends strongly on pH change. NaClO, H2O2 and oxygen, as oxidant models, in a weak acid solution displayed varying accelerations as the disassembly progressed. 5-FU, as a drug model, is efficiently uploaded in FcCOS nanoparticle (approximately 238nm). The in vitro release of 5-FU from FcCOS nanoparticles studies show that the accumulative release increased with the decrease of pH under bubbled N2. Interestingly, the sample under bubbled air has a higher accumulative release up to 59.64% at pH 3.8, compared with samples under bubbled N2 just 49.02%. The results suggested that FcCOS nanoparticles disassembled faster and the release of drug molecules was accelerated because of the synergistic effect of oxidative agent and low pH. Thus, FcCOS can be developed as an effective pH and oxidation dual-responsive carrier to enhance drug efficacy for cancer treatment.