bluuebunny/crossref_metadata_2025_split huggingface dataset:
Diagnostic utility of p501s (prostein) in comparison to prostate specific antigen (PSA) for the detection of metastatic prostatic adenocarcinoma
Authors: Yin Ming , Dhir Rajiv , Parwani Anil V 
Published: October 2007

Abstract

Background
Immunohistochemical detection of prostate specific antigen (PSA) is widely used to identify metastatic prostatic adenocarcinoma. However, PSA may not be expressed in some poorly differentiated prostatic carcinomas and its immunoreactivity has been found in some non-prostatic tissues. P501s (prostein) is a prostate-specific marker that is expressed in the cytoplasm of benign and malignant prostatic glandular cells. It has not been detected in any other normal or malignant tissues. The purpose of this study was to evaluate the expression of P501s in metastatic prostatic adenocarcinoma and compare its expression with PSA.

Methods
Immunohistochemical stains with anti-P501s antibodies were performed on 5-micron sections of tissue microarray (TMA) specimens. The TMA is constructed with normal donor prostates (NDP), prostatic adenocarcinoma (PRCA), non-neoplastic prostatic tissues adjacent to malignant glands (NAT), benign prostatic hyperplasia (BPH), high-grade prostatic neoplasia (PIN), metastatic adenocarcinoma to lymph nodes (MLN), metastatic adenocarcinoma to other sites (MC), and samples of benign testis, colon, adrenal and kidney. The two groups of metastatic lesions were also subjected to stains with antibodies to PSA. A composite score (ranging from 0 to 3) was assigned to score intensity of staining.

Results
Granular staining pattern of p501s was seen in all benign glands (score = 1.77 – 2.1) and malignant acini (score = 1.52) at the apical aspect of cytoplasm, predominantly adjacent to the nuclei. No staining was observed in controls including testis, colon, adrenal and kidney. The MLN group received a score of 1.0, with 10% of cases negative for p501s. The MC cases had a score of 0.64, with 16.7% of case showing loss of p501s expression. Although the metastatic lesions demonstrated similar rate of negative expression with PSA antibody, only 2 MC cases (3.3%) showed simultaneous negative stains for both P501S and PSA.

Conclusion
P501s is an organ specific marker for benign and malignant prostatic epithelial cells. Its characteristic cytoplasmic stain pattern provides an additional valuable immunomarker for detection of metastatic prostatic malignancy, even though the intensity of its expression is reduced, as in the case with PSA. Simultaneous stains with P501S and PSA will greatly improve the detection rate and identify a significant majority of the metastases.
Differential expression of the FAK family kinases in rheumatoid arthritis and osteoarthritis synovial tissues
Authors: Shahrara Shiva , Castro-Rueda Hernan P , Haines G Kenneth , Koch Alisa E 
Published: October 2007

AbstractThe focal adhesion kinase (FAK) family kinases, including FAK and proline-rich kinase 2 (Pyk)2, are the predominant mediators of integrin αvβ3 signaling events that play an important role in cell adhesion, osteoclast pathology, and angiogenesis, all processes important in rheumatoid arthritis (RA). Using immunohistochemical and western blot analysis, we studied the distribution of phospho (p)FAK, pPyk2, pSrc, pPaxillin and pPLCγ in the synovial tissue (ST) from patients with RA, osteoarthritis (OA) and normal donors (NDs) as well as in RA ST fibroblasts and peripheral blood differentiated macrophages (PB MΦs) treated with tumor necrosis factor-α (TNFα) or interleukin-1β (IL1β). RA and OA STs showed a greater percentage of pFAK on lining cells and MΦs compared with ND ST. RA ST fibroblasts expressed pFAK at baseline, which increased with TNFα or IL1β stimulation. Pyk2 and Src were phosphorylated more on RA versus OA and ND lining cells and MΦs. pPyk2 was expressed on RA ST fibrobasts but not in MΦs at baseline, however it was upregulated upon TNFα or IL1β activation in both cell types. pSrc was expressed in RA ST fibroblasts and MΦs at baseline and was further increased by TNFα or IL1β stimulation. pPaxillin and pPLCγ were upregulated in RA versus OA and ND lining cells and sublining MΦs. Activation of the FAK family signaling cascade on RA and OA lining cells may be responsible for cell adhesion and migration into the diseased STs. Therapies targeting this novel signaling pathway may be beneficial in RA.
Quantification of antiretroviral drugs for HIV-1 in the male genital tract: current data, limitations and implications for laboratory analysis
Authors: Chan Derek J , Ray John E 
Published: October 2007

Abstract
Antiretroviral therapy has reduced the morbidity and mortality associated with HIV-1/AIDS in developed countries. Viral replication in blood plasma is suppressed by antiretroviral drugs, whereas virus in the male genital tract is genetically and phenotypically unique and may not be suppressed. This viral compartmentalization affects antiretroviral drug penetration of the male genital tract and capacity for antiretroviral therapy to reduce sexual transmission. The problem of having two distinct viral populations within any given individual is compounded by the fact that antiretroviral drugs penetrate semen to varying degrees. Incomplete suppression of genital tract virus may yield drug-resistant virus and increase the risk of sexual transmission. This review critically appraises current studies of antiretroviral drug quantification in semen and suggests recommendations to address observed limitations.
Urea inclusion compounds of enalapril maleate for the improvement of pharmaceutical characteristics
Authors: Thakral Seema , Madan A K 
Published: October 2007

Abstract
Urea is a well known adductor for linear organic compounds. In the present study, enalapril maleate, a substituted cyclic organic compound, was successfully included in urea together with a suitable rapidly adductible endocyte (RAE). Formation of the urea inclusion compound was confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction. The modified Zimmerschied calorimetric method was used to estimate the minimum amount of RAE required for adduction of enalapril maleate in urea. Urea-enalapril maleate-RAE inclusion compounds containing varying proportions of guests were prepared and their thermal behaviour studied by differential scanning calorimetry. Regression analysis revealed an excellent r2 value with regard to the influence of the relative proportion of RAE on the heat of decomposition. The inclusion compounds were found to exhibit good content uniformity and improved dissolution profile as demonstrated by increased dissolution efficiency. Studies revealed that urea inclusion may be a promising alternative for the formulation of potent poorly soluble drugs into immediate release products.
Effect of absorption rate on pharmacokinetics of ibuprofen in relation to chiral inversion in humans
Authors: Ding Guohua , Liu Yang , Sun Jiewen , Takeuchi Yuriko , Toda Takaki , Hayakawa Toru , Fukushima Shoji , Kishimoto Shuichi , Lin Wenhui , Inotsume Nobuo 
Published: October 2007

Abstract
The effect of absorption rate on the pharmacokinetics of ibuprofen enantiomers was investigated in 12 healthy Han Chinese male volunteers following oral administration of immediate-release (IR) and sustained-release (SR) preparations containing racemic ibuprofen (rac-ibuprofen). The area under the curve of the plasma concentration-time curve (AUC; (mean ± s.d.) values for rac-ibuprofen were 192.90 ± 43.47 for the SR preparation and 195.90 ± 31.69 μg h mL−1 for the IR preparation. AUC values for the enantiomers after administration of the SR formulation were 55.38 ± 17.79 and 92.51 ± 30.68 μg h mL−1 for R- and S-ibuprofen, respectively, and were 65.94 ± 20.06 and 100.81 ± 32.28 μg h mL−1 for R- and S-ibuprofen after administration of the IR preparation. These values did not differ significantly. Cmax values were significantly decreased with the SR preparation: 25.11 ± 5.71, 12.24 ± 3.79 and 12.38 ± 3.55 μg mL−1 for rac-, R-, and S-ibuprofen, respectively, after administration of the SR preparation, vs 46.21 ± 8.20, 20.82 ± 5.90 and 23.46 ± 7.30 μg mL−1 for rac-, R-, and S-ibuprofen, respectively, after administration of the IR preparation. Mean residence time was significantly increased: 7.01 ± 1.29, 5.52 ± 1.25 and 7.04 ± 1.30 h for rac-, R-, and S-ibuprofen, respectively, after administration of the SR preparation vs 4.34 ± 0.89, 3.43 ± 0.64 and 4.51 ± 0.79 h for rac-, R-, and S-ibuprofen, respectively, after administration of the IR preparation. AUC values for S-ibuprofen were significantly larger than those for R-ibuprofen in both preparations, indicating unidirectional chiral inversion. The S/R ratio of serum concentrations of enantiomers was 1.78-fold higher at 6 h after administration of the SR preparation compared with the IR preparation (P &lt; 0.01).
These results indicate that ibuprofen undergoes pre-systemic chiral inversion in parallel with a systemic process and that the clinical effects of rac-ibuprofen in humans depend on the absorption rate.
Inhibition effect of flavonoids on monocarboxylate transporter 1 (MCT1) in Caco-2 cells
Authors: Shim Chang-Koo , Cheon Eun-Pa , Kang Keon Wook , Seo Ki-Soo , Han Hyo-Kyung 
Published: October 2007

AbstractThis study aimed to investigate the inhibition effect of flavonoids on monocarboxylate transporter 1 (MCT1) in Caco-2 cells. The cellular uptake of benzoic acid was examined in the presence and the absence of naringin, naringenin, morin, silybin and quercetin in Caco-2 cells. All the tested flavonoids except naringin significantly inhibited (P &lt; 0.05) the cellular uptake of [14C]-benzoic acid. Particularly, naringenin and silybin exhibited strong inhibition effects with IC50 values of 23.4 and 30.2 μm, respectively. Kinetic analysis indicated that the inhibition mode of naringenin and silybin on MCT1 activity was competitive with a Ki of 15∼20 μm. The effect of flavonoids on the gene expression of MCT1 was also examined by using RT-PCR and western blot analysis. Results indicated that the expression level of MCT1 was not affected by the treatment with naringenin or silybin. The cellular accumulation of naringenin in Caco-2 cells was not changed in the presence of benzoic acid or l-lactic acid, implying that naringenin might not be a substrate of MCT1. In conclusion, some flavonoids appeared to be competitive inhibitors of MCT1, suggesting the potential for diet-drug interactions between flavonoids and MCT1 substrates.
Effects of quinine on the intracellular calcium level and membrane potential of PC 12 cultures
Authors: Akiyoshi Takeshi , Tanaka Naoko , Nakamura Tomoko , Matzno Sumio , Shinozuka Kazumasa , Uchida Takahiro 
Published: October 2007

Abstract
The mechanism for the perception of bitterness appears to be quite complicated, even for quinine, which is a model bitter substance, and thus has yet to be completely elucidated. To investigate the possibility of being able to predict the bitterness of quinine solutions, we examined the effects of quinine on intracellular calcium ion concentration ([Ca2+]i) and membrane potentials in PC 12 cultures. [Ca2+]i and membrane potentials were analysed by fluorescence confocal microscopic imaging using the Ca2+-sensitive probe Calcium Green 1/AM and the membrane potential-sensitive probe bis-(1,3-dibutylbarbituric acid) trimethine oxonol (DiBAC4(3)). Quinine elicited an increase in the membrane potential along with a concentration-dependent increase in [Ca2+]i. These increases were inhibited by extracellular Ca2+-free conditions, thapsigargin, which is a Ca2+-pump inhibitor, and U73122, which is a phospholipase C inhibitor. The quinine-induced increase in [Ca2+]i levels was inhibited by nifedipine, an L-type Ca2+-channel blocker, ω-conotoxin, a T-type Ca2+-channel blocker, and BMI-40, which is a bitterness-masking substance. These results suggest that responses in PC 12 cultures may be used as a simple model of bitterness perception.
The gastric emptying of food as measured by gamma-scintigraphy and electrical impedance tomography (EIT) and its influence on the gastric emptying of tablets of different dimensions
Authors: Podczeck Fridrun , Mitchell Catherine L , Newton J Michael , Evans David , Short Michael B 
Published: October 2007

Abstract
A study in human volunteers has been designed to evaluate the influence of different food regimes on the gastric emptying of 3 mm and 10 mm diameter tablets. Dextrose and beef drinks were used as liquid food; a mixture of minced beef and mashed potato (shepherd's pie) was used as a solid meal. The gastric emptying of these foods was monitored simultaneously with electrical impedance tomography (EIT) and gamma-scintigraphy (GS), and was quantified in terms of the time before gastric emptying started, the lag time, the mean gastric residence time (MGRT) and its variance (VGRT), and the time for complete emptying. The gastric emptying time of the tablets was established by monitoring the position of the tablets, which had been labelled with suitable radio isotopes, by GS. The two systems for monitoring gastric emptying of the foods did not provide equivalent results: times obtained with EIT were generally shorter than those obtained with GS for the liquid foods, but were longer for the solid meal. There was only a slight difference in the emptying times of the two liquid foods, whereas values for MGRT, VGRT and the time for complete emptying were considerably longer for the solid meal. In nearly all instances the tablets emptied after the foods had emptied completely from the stomach. Gastric emptying times were longer for the 3 mm tablets than the 10 mm tablets, whatever food they were taken with. The difference between the median emptying times was significant when the meal was either a dextrose solution or a beef drink, but not when the meal was shepherd's pie. The increase in gastric emptying time of tablets induced by solid food was greater than that associated with the differences in tablet size. By providing a protocol that did not allow the administration of further food until after the tablets had emptied from the stomach, no tablet emptying times exceeded 6 h.
Effect of 2-hydroxy 4-methoxy benzoic acid on an experimental model of hyperlipidaemia, induced by chronic ethanol treatment
Authors: Saravanan Nadana , Nalini Namasivayam 
Published: October 2007

Abstract
The aim of the present study was to determine the effect of 2-hydroxy 4-methoxy benzoic acid (HMBA), the active principle of Hemidesmus indicus, an indigenous Ayurvedic medicinal plant in India. We investigated the effect of HMBA on hyperlipidaemia induced by ethanol, exploring food intake, body weight, and hepatic and plasma lipids and lipoproteins. Male Wistar rats weighing 130–180 g were given ethanol (5 g kg−1 p.o.) daily for 30 days. Subsequently, ethanol-fed rats were given HMBA intragastrically at a dose of 200 μg kg−1 per day for 30 days. At the end of the total experimental period of 60 days, plasma concentrations of total cholesterol (CHO), triglycerides (TG), lipoproteins (LP), phospholipids (PL), free fatty acids (FFA) and lipoprotein lipase (LPL), and hepatic CHO, TG and PL were measured. Treatment of ethanol-fed rats with HMBA significantly decreased plasma CHO, TG, LP, PL and FFA and hepatic CHO, TG and PL, and increased plasma LPL concentrations compared with values in untreated ethanol-fed rats (all P &lt; 0.05). Food intake and average body weight at the end of the experimental period were significantly increased by HMBA administration. In conclusion, administration of HMBA decreased lipids and lipoprotein concentrations significantly in an animal model of ethanol-induced hyperlipidaemia.
Apigenin (4‘,5,7-trihydroxyflavone) regulates hyperglycaemia, thyroid dysfunction and lipid peroxidation in alloxan-induced diabetic mice
Authors: Panda Sunanda , Kar Anand 
Published: October 2007

Abstract
The potential of apigenin (4′,5,7-trihydroxyflavone) in regulating hyperglycaemia, thyroid dysfunction and lipid peroxidation (LPO) has been revealed. While in alloxan-treated diabetic animals, a significant decrease in the concentrations of serum insulin, thyroxine (T4) and triiodothyronine (T3), with a parallel increase in serum glucose and hepatic glucose-6-phospatase (G-6-Pase) activity, was observed, administration of 0.78 mg kg−1 of apigenin for 10 consecutive days increased the levels of serum insulin and thyroid hormones with a parallel decrease in glucose concentration and hepatic G-6-Pase activity. Alloxan-induced elevation in serum cholesterol was also reduced by the compound. With respect to LPO, while in alloxan-treated animals an increase in hepatic LPO and a decrease in the activity of cellular antioxidants, such as catalase (CAT) and superoxide dismutase (SOD), and in glutathione (GSH) content was observed, administration of apigenin to alloxan-treated mice reversed all these changes, suggesting its hepatoprotective potential. Similar effects of apigenin were also observed in most of the parameters in normoglycaemic animals. It appears that apigenin has a potential to regulate diabetes mellitus, as well as disease-induced thyroid dysfunction and lipid peroxidation.
Gastroprotective properties of Myristica malabarica against indometacin-induced stomach ulceration: a mechanistic exploration
Authors: Banerjee Debashish , Maity Biswanath , Bauri Ajay K , Bandyopadhyay Sandip K , Chattopadhyay Subrata 
Published: October 2007

Abstract
The healing activity of the methanol extract of the spice rampatri, Myristica malabarica, (RM) and omeprazole against indometacin-induced stomach ulceration has been studied in a mouse model. Treatment with RM (40 mg kg−1 per day) and omeprazole (3 mg kg−1 per day) for 3 days could effectively heal the stomach ulceration, as revealed from the ulcer indices and histopathological studies. Compared with the ulcerated group, treatment with RM and omeprazole for 3 days reduced the macroscopic damage score by approximately 72% and 76%, respectively (P &lt; 0.001), establishing the efficacy of RM. The extent of ulcer healing offered by 3 days' treatment with RM or omeprazole was better than that observed with natural recovery over 5 and 7 days (P &lt; 0.05). The healing capacities of RM and omeprazole could be attributed to their antioxidant activity as well as the ability to enhance the mucin content of the gastric tissues. Both drugs reduced lipid peroxidation (by 42–44%) and protein carbonyl content (by 34%), and augmented non-protein thiol levels beyond normal values. Furthermore, RM improved the mucin level beyond the normal value, while omeprazole restored it to near normalcy.
Scutellaria baicalensis and a constituent flavonoid, baicalein, attenuate ritonavir-induced gastrointestinal side-effects
Authors: Mehendale Sangeeta , Aung Han , Wang Chong-Zhi , Tong Robin , Foo Adela , Xie Jing-Tian , Yuan Chun-Su 
Published: October 2007

Abstract
Ritonavir, a protease inhibitor drug, is commonly used in AIDS therapy. As with other chemotherapeutic drugs that cause gastrointestinal adverse effects, ritonavir treatment is associated with significant nausea and vomiting. This study investigated whether Scutellaria baicalensis, and its active flavonoid constituent, baicalein, attenuate the gastrointestinal effects of ritonavir. The effects of herb administration were evaluated in ritonavir-treated rats using a rat pica model, which simulates nausea and vomiting in humans. The effects of herb administration on gastric emptying in rats were also measured. Ritonavir treatment resulted in increased kaolin intake or severe pica, the intensity of which was reduced significantly with S. baicalensis administration (1 mg kg−1; P &lt; 0.05). High-performance liquid chromatography analysis of S. baicalensis showed the presence of an extremely potent flavonoid constituent, baicalein. The study aimed to determine if baicalein contributed to the anti-pica effect of the extract. It was observed that baicalein dose-dependently decreased pica in ritonavir-treated rats (P &lt; 0.001). In addition to inducing pica, ritonavir also significantly delayed gastric emptying, which could contribute to ritonavir-induced gastrointestinal dysfunction. When S. baicalensis extract was administered to ritonavir-treated rats the delayed gastric emptying was significantly attenuated (P &lt; 0.05). The results suggest that S. baicalensis and the constituent baicalein reduce the gastrointestinal dysfunction caused by ritonavir. It is concluded that S. baicalensis may potentially have a role to play in reducing drug-induced adverse effects.
Antinociceptive action of limonexic acid obtained fromRaulinoa echinata
Authors: Biavatti Maique W , Westerlon Rosângela , Burger Cristiani , Mora Ticiana Camila , De Souza Márcia Maria 
Published: October 2007

AbstractThe antinociceptive effect of the limonexic acid isolate of Raulinoa echinata Cowan in four models of pain in mice is described. When evaluated against acetic acid-induced abdominal constrictions, limonexic acid (10, 30 and 60 mg kg−1, i.p.) produced dose-related inhibition of the number of constrictions, with a mean ID50 value of 43 (2.3–79) μmol kg−1, and was more potent than some standard drugs. In the formalin test, limonexic acid inhibited both the first and second phases of formalin-induced pain. Furthermore, the effect was more pronounced in the second phase, with a mean ID50 value of 13.66 (9.35–19.61) μmol kg−1, and had a pharmacological profile that was similar to standard drugs such as acetaminophen and acetyl salicylic acid. Limonexic acid also produced dose-related inhibition of glutamate- and capsaicin-induced pain, with mean ID50 values of 11.67 (8.51–16.0) μmol kg−1 and 47.17 (36.51–60.93) μmol kg−1, respectively. The mechanism of action is not completely understood, but seems to involve direct interaction with the GABAergic and nitroxidergic pathways.