bluuebunny/crossref_metadata_2025_split huggingface dataset:
Strontium fructose 1,6-diphosphate alleviates early diabetic testopathy by suppressing abnormal testicular matrix metalloproteinase system in streptozocin-treated rats
Authors: Zhang Qi , Liu Hao-Ran , Ying Han-Jie , Dai De-Zai , Tang Xiao-Yun , Dai Yin 
Published: October 2010

Abstract

Objectives
Male hypogonadism is frequently associated with testopathy in patients with type 2 diabetes and in middle-aged males. We hypothesized that abnormal matrix metalloproteinases (MMPs) and their tissue inhibitors (TIMPs) in testis have large roles to play in male hypogonadism. It has been found in diabetic rats that a novel compound, strontium fructose 1,6-diphosphate (FDP-Sr), with extra high energy supply, could reverse male hypogonadism by normalizing MMP-9 and TIMPs in the testis. We investigated whether FDP-Sr could be promising in treating diabetic testopathy.

Methods
Adult male Sprague-Dawley rats were administered a single dose of streptozocin (65 mg/kg, i.p.) to induce diabetes. The diabetic rats were treated with FDP-Sr in three doses or testosterone propionate in the final four weeks during the eight-week study.

Key findings
Serum testosterone, activity of marker enzymes, and mRNA of MMPs and TIMPs and protein of MMP-9 in the testis were detected. After eight weeks, the activity of acid phosphatase, lactate dehydrogenase, succinate dehydrogenase and γ-glutamyl transpeptidase in testis were significantly decreased (P &lt; 0.01), accompanied by down-regulated mRNA and activity of MMP-2 and MMP-9 (P &lt; 0.01) and upregulated mRNA of TIMP-1 and TIMP-2. Downregulated MMP-9 protein and degenerative changes in histology were predominant in diabetic testis.

Conclusions
FDP-Sr or testosterone propionate significantly normalized expression and activity of the MMPs–TIMPs system to attenuate changes in serum testosterone, marker enzymes and histology in testis. Effects of FDP-S-r were dose-dependent and comparable with those of testosterone propionate. By supplying extra energy, FDP-Sr could be promising in treating diabetic testopathy by normalizing abnormal MMP-9 and its endogenous inhibitors in testes.
Antiulcerogenic and anti-inflammatory activities of the essential oil from Pterodon emarginatus seeds
Authors: Dutra Rafael C , Fava Marcelo B , Alves Caio C S , Ferreira Ana P , Barbosa Nádia R 
Published: October 2010

Abstract

Objectives
The objective of this work was to investigate the antiulcerogenic and anti-inflammatory activities of the essential oil from Pterodon emarginatus seeds.

Methods
The following tests were used: ulcers induced by ethanol, indometacin and HCl/ethanol, and pleurisy induced by carrageenan in Swiss albino rats. The rats were treated by the oral route with essential oil of P. emarginatus seeds.

Key findings
The essential oil at 100, 300 and 500 mg/kg exhibited significant protection against ulcers induced by ethanol, indometacin and HCl/ethanol (P &lt; 0.001). The essential oil caused a marked reduction in the exudate volume and inhibited leucocyte and neutrophil influx (P &lt; 0.05) in carrageenan-induced pleurisy. Moreover, the essential oil significantly decreased nitric oxide (NO) and interleukin-1 (IL-1) levels, without affecting tumour necrosis factor-α production.

Conclusions
The results demonstrated the marked antiulcerogenic and anti-inflammatory effects of the essential oil from P. emarginatus, which are, at least in part, a consequence of NO and IL-1 modulation. P. emarginatus or its constituents might represent new therapeutic options to treat gastric ulcers and inflammatory diseases.
Relaxing effects of Valeriana officinalis extracts on isolated human non-pregnant uterine muscle
Authors: Occhiuto Francesco , Pino Annalisa , Palumbo Dora Rita , Samperi Stefania , De Pasquale Rita , Sturlese Emanuele , Circosta Clara 
Published: October 2010

Abstract

Objectives
This study investigated the relaxing effects of Valeriana officinalis L. (Valerianaceae) on human uterine muscle. The major uses of this species in Europe are as a sedative and an anxiolytic; it is also used as a spasmolytic to treat gastrointestinal spasm.

Methods
We evaluated two valerian extracts (ethanolic and aqueous) in comparison with a natural mixture of valepotriates and nifedipine on spontaneous and agonist-induced contractions in non-pregnant human myometrium in vitro. Qualitative and quantitative chemical analysis was used to correlate the chemical composition of extracts with their spasmolytic effects. Myometrial strips were obtained from hysterectomy specimens of premenopausal women. Longitudinal muscle strips were mounted vertically in tissue baths under physiological conditions to record their isometric contraction. The responses of cumulative concentrations of valerian extracts on spontaneous contractions in the presence and absence of the β-adrenoceptor blocker atenolol or the cyclooxygenase inhibitor indometacin, and on agonist-induced contractions, were investigated.

Key findings
Valerian extracts and valepotriates inhibited uterine contra***ctility in a concentration-dependent manner. Pretreatment with either atenolol or indometacin did not affect the uterine responses to valerian extracts. Valerian extract reduced the maximal contractile response induced by acetylcholine, phenylephrine and histamine independent of the stimulus.

Conclusions
Valerian extracts may have direct inhibitory effects on the contractility of the human uterus and this justifies the traditional use of this plant in the treatment of uterine cramping associated with dysmenorrhoea.
Novel formulation of solid lipid microparticles of curcumin for anti-angiogenic and anti-inflammatory activity for optimization of therapy of inflammatory bowel disease
Authors: Yadav Vivek Ramshankar , Suresh Sarasija , Devi Kshama , Yadav Seema 
Published: October 2010

AbstractObjectivesThis project was undertaken with a view to optimize the treatment of inflammatory bowel disease through a novel drug delivery approach for localized treatment in the colon. Curcumin has poor aqueous solubility, poor stability in the gastrointestinal tract and poor bioavailability. The purpose of the study was to prepare and evaluate the anti-inflammatory activity of solid lipid microparticles (SLMs) of curcumin for the treatment of inflammatory bowel disease in a colitis-induced rat model by a colon-specific delivery approach.MethodsWe have developed a novel formulation approach for treating experimental colitis in the rat model. SLMs of curcumin were prepared with various lipids, such as palmitic acid, stearic acid and soya lecithin, with an optimized percentage of poloxamer 188. The SLMs of curcumin were characterized for particle size, drug content, drug entrapment, in-vitro release, surface morphology and infrared, differential scanning calorimetry and X-ray studies. The colonic delivery system of SLM formulations of curcumin were further investigated for their anti-angiogenic and anti-inflammatory activity using chick embryo and rat colitis models.Key findingsParticle size, drug content, drug entrapment and in-vitro release studies showed that formulation F4 containing one part stearic acid and 0.5% surfactant had the smallest diameter of 108 μm, 79.24% entrapment and exhibited excellent in-vitro release characteristics when compared with other formulations and pure curcumin. SLMs of curcumin (F4) proved to be a potent angio-inhibitory compound, as demonstrated by inhibition of angiogenesis in the chorioallantoic membrane assay. Rats treated with curcumin and its SLM complex showed a faster weight gain compared with dextran sulfate solution (DSS) control rats. The increase in whole colon length appeared to be significantly greater in SLM-treated rats when compared with pure curcumin and DSS control rats. An additional finding in the DSS-treated rats was chronic cell infiltration with predominance of eosinophils. Decreased mast cell numbers in the mucosa of the colon of SLMs of curcumin and pure curcumin-treated rats was observed.ConclusionsThe degree of colitis caused by administration of DSS was significantly attenuated by colonic delivery of SLMs of curcumin. Being a nontoxic natural dietary product, curcumin could be useful in the therapeutic strategy for inflammatory bowel disease patients.
Novel oral fast-disintegrating drug delivery devices with predefined inner structure fabricated by Three-Dimensional Printing
Authors: Yu Deng-Guang , Shen Xia-Xia , Branford-White Chris , Zhu Li-Min , White Kenneth , Yang Xiang Liang 
Published: October 2010

Abstract

Objectives
Novel fast-disintegrating drug delivery devices with special inner structure characteristics were designed and fabricated using Three-Dimensional Printing.

Methods
Based on computer-aided design models, fast-disintegrating drug delivery devices containing loose powders were prepared automatically using the Three-Dimensional Printing system. The inner powder regions were prepared by depositing the binder solutions onto selected regions during the layer-printing process.

Results
The devices showed acceptable pharmacotechnical properties and fine hardness (63.4 N/cm2) due to the synergistic action of several binding mechanisms, but unsatisfactory friability, with 3.55% total mass loss during the friability tests. Scanning electron microscope images clearly showed that the printed regions were well bound, and that the drug particle size was reduced or individual particles could no longer be distinguished. In contrast, the unprinted regions were uncompacted, with cracks and fissures among the loose mixed powder. All the drug delivery devices disintegrated and wetted rapidly in in-vitro tests. The average disintegration and wetting times were 23.4 s and 67.6 s, respectively. Dissolution tests showed that 98.5% of the drug was released within 2 min.

Conclusions
Three-Dimensional Printing offers strategies for the development of novel oral fast-disintegrating drug delivery devices.
Comparison of WHO and US FDA biowaiver dissolution test conditions using bioequivalent doxycycline hyclate drug products
Authors: Strauch Stefanie , Jantratid Ekarat , Dressman Jennifer B 
Published: October 2010

Abstract

Objectives
The dissolution characteristics of immediate-release doxycycline hyclate products with certified in-vivo bioequivalence to the innovator product were tested with a view to possible application of biowaiver-based approval.

Methods
Five products were tested using US Pharmacopeia Apparatus 2: Antodox 100 mg hard gelatin capsules, Doxycyclin AL 100 T tablets, Doxycyclin-ratiopharm 100 soft gelatin capsules, Doxycyclin STADA 100 mg tablets and Doxy-Wolff 100 mg tablets. Three compendial buffers were used as dissolution media: simulated gastric fluid without pepsin, pH 1.2, acetate buffer, pH 4.5, and simulated intestinal fluid without pancreatin, pH 6.8. Results were obtained at two paddle speeds recommended for biowaiver applications: 75 rpm (World Health Organization; WHO) and 50 rpm (US Food and Drug Administration; US FDA).

Key findings
The results for the tablets and hard gelatin capsules indicate that a paddle speed of 75 rpm is more representative than 50 rpm, since 75 rpm generates dissolution profiles corresponding more closely to the in-vivo profiles than those at 50 rpm. For evaluating soft gelatin capsule formulations with lipid fill, both US FDA and WHO methods were found to be over-discriminating.

Conclusions
Bioequivalence of immediate-release doxycycline hyclate tablets and hard gelatin capsules, but not soft gelatin capsules, can be evaluated in vitro using the biowaiver dissolution test conditions specified by the WHO.
Active absorption of ginsenoside Rg1 in vitro and in vivo: the role of sodium-dependent glucose co-transporter 1
Authors: Xiong Jing , Sun Minjie , Guo Jianxin , Huang Luosheng , Wang Shujing , Meng Boyu , Ping Qineng 
Published: October 2010

Abstract

Objectives
Our previous study suggested that adrenaline (epinephrine) could be an effective absorption enhancer for ginsenoside Rg1 (Rg1). This study focused on the transport mechanism of Rg1 and the role of sodium-dependent glucose co-transporter 1 in the regulation of Rg1 uptake after exposure to adrenaline.

Methods
Caco-2 cells were used as an in-vitro model to assess the absorption mechanism of Rg1. Also the effect of D-glucose on adrenaline-induced absorption of Rg1 was investigated in vivo in rats.

Key findings
Results showed that the uptake of Rg1 was temperature-dependent. The transport from the basolateral side to the apical side was significantly lower compared with that from the apical to the basolateral side (P &lt; 0.01). The transport of Rg1 was concentration dependent (Km was 41.60 mM, Vmax was 353.75 mol/cm2/min). Cells incubated with D-glucose-free medium exhibited significantly greater Rg1 uptake (+ 62.6%) compared with cells in D-glucose-containing medium. The data indicated that sodium-dependent glucose co-transporter 1 was involved in the transport of Rg1. Adrenaline-induced uptake of Rg1 was significantly inhibited in the presence of phlorizin and the absence of Na+. In the in-vivo study in rats, it was found that after co-administration with D-glucose, the adrenaline-induced absorption of Rg1 was inhibited. The area under the concentration-time curve (AUC0→∞) value was significantly decreased from 64.57 ± 27.08 to 1.37 ± 0.42 μg/ml h (P &lt; 0.001).

Conclusions
The data suggested that adrenaline enhanced the absorption of Rg1 by regulating sodium-dependent glucose co-transporter 1.
Phycocyanin liposomes for topical anti-inflammatory activity: in-vitro in-vivo studies
Authors: Manconia Maria , Pendás Jehzabel , Ledón Nurys , Moreira Tomás , Sinico Chiara , Saso Luciano , Fadda Anna Maria 
Published: October 2010

Abstract

Objectives
The aim of this work was to investigate the anti-inflammatory activity of C-phycocyanin (C-PC) on skin inflammation after topical administration and the influence of liposomal delivery on its pharmacokinetic properties.

Methods
Liposomes of different size and structure were prepared with different techniques using soy phosphatidylcholine and cholesterol. Vesicular dispersions were characterised by transmission electron microscopy, optical and fluorescence microscopy for vesicle formation and morphology, dynamic laser light scattering for size distribution, and Zetasizer for zeta-potential. C-PC skin penetration and permeation experiments were performed in vitro using vertical diffusion Franz cells and human skin treated with either free or liposomal drug dispersed in a Carbopol gel.

Key findings
The protein was mainly localised in the stratum corneum, while no permeation of C-PC through the whole skin thickness was detected. Two percent C-PC-encapsulating liposomes showed the best drug accumulation in the stratum corneum and the whole skin, higher than that of the corresponding free 2% C-PC gel. Moreover, skin deposition of liposomal C-PC was dose dependent since skin accumulation values increased as the C-PC concentration in liposomes increased. The topical anti-inflammatory activity of samples was evaluated in vivo as inhibition of croton oil-induced or arachidonic acid-induced ear oedema in rats.

Conclusions
The results showed that C-PC can be successfully used as an anti-inflammatory drug and that liposomal encapsulation is effective in improving its anti-inflammatory activity.
Oral bioavailability enhancement of a hydrophilic drug delivered via folic acid-coupled liposomes in rats
Authors: Ling Sharon Sheue Nee , Yuen Kah Hay , Magosso Enrico , Barker Susan Anne 
Published: October 2010

Abstract

Objectives
A liposome preparation that is amenable to receptor-mediated endocytosis has been developed to enhance the oral bioavailability of poorly absorbable peptidomi-metic drugs by use of folic acid as the mediator of liposomal uptake.

Methods
Folic acid was physically coupled to the surface of the liposomes and cefotaxime was used as the model drug. In-vivo evaluation was carried out on eight Sprague-Dawley rats in a two-way crossover study to compare the oral bioavailability of cefotaxime loaded in folic acid-free liposomes and folic acid-coupled liposomes. Blood samples were collected from the tail vein and plasma cefotaxime levels were determined using an HPLC method.

Key findings
Enhanced oral bioavailability (AUC0-∞) of cefotaxime was observed when administered via folic acid-coupled liposomes. The peak plasma concentration (Cmax) of cefotaxime was increased when administered via folic acid-coupled liposomes as compared with folic acid-free liposomes. At 90% confidence interval, the value for AUC0-∞ was 1.4–2-times higher and the value for Cmax was 1.2–1.8-times higher for the folic acid-coupled liposomes compared with folic acid-free liposomes.

Conclusions
Folic acid could enhance the uptake of liposomally entrapped drug. It could be a useful candidate to supplement liposome delivery systems.
Protective effects of coffee-derived compounds on lipopolysaccharide/d-galactosamine induced acute liver injury in rats
Authors: Akashi Iwao , Kagami Keisuke , Hirano Toshihiko , Oka Kitaro 
Published: October 2010

Abstract

Objectives
The protective effects of coffee-derived compounds on lipopolysaccharide/d-galactosamine (LPS/d-GalN) induced acute liver injury in rats were investigated.

Methods
Wistar rats were orally administered saline (control) or one of the test compounds (caffeine, chlorogenic acid, trigonelline, nicotinic acid or eight ***pyrazinoic acids) at a dose of 100 mg/kg, respectively. This was followed by intraperitoneal injection with LPS (100 μg/kg)/d-GalN (250 mg/kg) 1 h after administration of the test compounds. Blood samples were collected up to 12 h after LPS/d-GalN injection, followed by determination of plasma aspartate aminotransferase, alanine aminotransferase, tumour necrosis factor α (TNF-α) and interleukin 10 (IL-10) levels.

Key findings
Plasma aspartate aminotransferase and alanine aminotransferase levels were significantly increased after LPS/d-GalN-treatment, but were suppressed by pretreatment with caffeine (n = 5), nicotinic acid, non-substituted pyrazinoic acid or 5-methylpyrazinoic acid (n = 6, respectively) 12 h after LPS/d-GalN-treatment (P &lt; 0.01, respectively). Moreover, the animals pretreated with these test compounds showed significantly higher survival rates (83–100%) compared with the control (23%). Only pretreatment with caffeine significantly suppressed the LPS/d-GalN induced elevation of plasma TNF-α levels 1 and 2 h after LPS/d-GalN-treatment (P &lt; 0.01, respectively). Pretreatment with caffeine, nicotinic acid or non-substituted pyrazinoic acid activated the LPS/d-GalN induced elevation of plasma IL-10 levels at 1 and 2 h, although there were no statistically significant differences in IL-10 levels between control and nicotinic acid or non-substituted pyrazinoic acid treated rats.

Conclusions
The results suggest that caffeine, nicotinic acid, non-substituted pyrazinoic acid and 5-methylpyrazinoic acid can protect against LPS/d-GalN induced acute liver injury, which may be mediated by the reduction of TNF-α production and/or increasing IL-10 production.
Bis-(3-hydroxyphenyl) diselenide inhibits LPS-stimulated iNOS and COX-2 expression in RAW 264.7 macrophage cells through the NF-kB inactivation
Authors: Shin Kyung-Min , Shen Liulan , Park Seung Jae , Jeong Jin-Hyun , Lee Kyung-Tae 
Published: October 2010

Abstract

Objectives
Previously, we reported that diaryl diselenide compounds have strong inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophages. In this study, we investigated the molecular mechanisms underlying NO suppression and prostaglandin E2 (PGE2) production by diaryl diselenide compounds, bis-(2-hydroxyphenyl) diselenide (DSE-A), bis-(3-hydroxyphenyl) diselenide (DSE-B), bis-(4-hydroxyphenyl) diselenide (DSE-C), dipyridyl diselenide (DSE-D) and diphenyl diselenide (DSE-E).

Methods
The effect of these compounds on NO suppression and PGE2 production was investigated in RAW 264.7 macrophages.

Key findings
Our data indicate that of the above, DSE-B most potently inhibits NO and PGE2 production, and that it also significantly reduces the releases of tumour necrosis factor (TNF)-α, interleukin(IL)-1β and IL-6. Consistent with these observations, DSE-B also reduced the protein levels of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), and the mRNA levels of iNOS, COX-2, TNF-α, IL-1β and IL-6. Furthermore, DSE-B inhibited LPS-induced nuclear factor-κB (NF-κB) activation, which was associated with the prevention of the inhibitor κB-α (IκB-α) degradation and a subsequent reduction in nuclear p65 protein levels.

Conclusions
Taken together, our data suggest that the anti-inflammatory properties of DSE-B are due to reduction in the expression of iNOS, COX-2, TNF-α, IL-1β and IL-6 through the down-regulation of NF-κB binding activity.
Morphine or its withdrawal affects plasma malondialdehyde, vitamin E levels and absence or presence of abstinence signs in rats
Authors: Pinelli Arnaldo , Cighetti Giuliana , Trivulzio Silvio , Accinni Roberto 
Published: October 2010

Abstract

Objectives
Various experimental observations show that morphine treatment generates reactive oxygen species, and that its discontinuation leads to signs of withdrawal. We therefore investigated plasma malondialdehyde and vitamin E levels under both conditions to verify the occurrence of any alterations in oxidative metabolism, and whether these are associated with behavioural changes.

Methods
We investigated the effects of morphine or morphine plus naloxone on plasma malondialdehyde, vitamin E levels and withdrawal signs such as jumping, wet dog shakes and faecal excretion in rats. Furthermore, isopropylnoradrenaline was injected in rabbits to verify its effects on plasma malondialdehyde levels.

Key findings
Morphine treatment increased free malondialdehyde and decreased vitamin E levels. The elevation in malondialdehyde levels were exacerbated by the abrupt removal of morphine by naloxone, which also led to the appearance of withdrawal signs. The increased malondialdehyde values can be attributed to the interactions of reactive oxygen species with unsaturated fatty acids, and the lowered levels of vitamin E to its interactions with reactive oxygen species.

Conclusions
A connection seems to exist between altered peroxide status and withdrawal signs in abstinent animals.