In vitro evaluation of estrogenic, antiestrogenic and antitumor effects of amentoflavone.

Apigenin, a flavonoid, is reported to act as an estrogen receptor (ER) agonist and inhibit aromatase enzyme. However, amentoflavone, a biflavonoid bearing two apigenin molecules, has not been evaluated for its endocrine modulatory effects. Besides, it is highly consumed by young people to build muscles, enhance mood and lose weight. In the present study, apigenin was used as a reference molecule and ER mediated as well as ER-independent estrogenic/antiestrogenic activity of amentoflavone was investigated. Antitumor activity of amentoflavone was also investigated in both ER positive (MCF-7 BUS) and triple-negative (MDA-MB-231) breast cancer cells and its cytotoxicity was evaluated in human breast epithelial cells (MCF-10A). Our data confirmed ER agonist, aromatase inhibitory and cytotoxic effects of apigenin in breast cancer cells, where no ER mediated estrogenic effect and physiologically irrelevant, slight, aromatase inhibition was found for amentoflavone. Although selective cytotoxicity of amentoflavone was found in MCF-7 BUS cells, it does not seem to be an alternative to the present cytotoxic drugs. Therefore, neither an adverse effect, mediated by an estrogenic/antiestrogenic effect of amentoflavone nor a therapeutical benefit would be expected from amentoflavone. Further studies could be performed to investigate its in vivo effects.

Investigation of the effects of using single-wall carbon nanotubes (SWCNTs) in ozone measurement with passive samplers.

UNLABELLED: Passive samplers are used in air quality monitoring for many years to compete in terms of being economical with continuous measurement systems. In this study, different amounts of single-wall carbon nanotubes (SWCNTs) were added in the impregnation solution of the filters of passive samplers and the effect on the absorption of ozone studied. The results of the measurement of ozone with varying amounts of SWCNTs added to the impregnation solution of the filters of the passive samplers were compared with the results of the continuous ozone measurement system (CS). Measurements were performed for 7 days and 14 days at two different exposure times. The increase of the amount of SWCNTs on the filters of the passive samplers, however, did not have an effect on the measurement of ozone. The measurement results of the passive samplers of the 14-day exposure periods, alternating with the 7-day exposure periods, were lower considerably than the results of the 7-day exposure. IMPLICATIONS: The accuracy and the use of passive samplers in SWCNTs are expected to provide high measurement results. Observing the effect of the change in the amount of diffusion of pollutants held in the SWCNT is also one of the expected implications.

A Divalent PAMAM-Based Matrix Metalloproteinase/Carbonic Anhydrase Inhibitor for the Treatment of Dry Eye Syndrome.

Synthetic sulfonamide derivatives are a class of potent matrix metalloproteinase inhibitors (MMPI) that have potential for the treatment of diseases related to uncontrolled expression of these enzymes. The lack of selectivity of the large majority of such inhibitors, leading to the inhibition of MMPs in tissues other than the targeted one, has dramatically reduced the therapeutic interest in MMPIs. The recent development of efficient drug delivery systems that allow the transportation of a selected drug to its site of action has opened the way to new perspectives in the use of MMPIs. Here, a PAMAM-based divalent dendron with two sulfonamidic residues was synthesized. This nanomolar inhibitor binds to the catalytic domain of two MMPs as well as to the transmembrane human carbonic anhydrases (hCAs) XII, which is present in the eye and considered an antiglaucoma target. In the animal model of an experimental dry eye, no occurrence of dotted staining in eyes treated with our inhibitor was observed, indicating no symptoms of corneal desiccation.

Montelukast prevents ischaemia/reperfusion-induced ovarian damage in rats.

OBJECTIVE: To investigate the efficacy of montelukast for prevention of ischaemia/reperfusion (I/R) injury in rat ovary. STUDY DESIGN: Twenty-four female adult rats were included in the study. I/R injury was induced by CO2 pneumoperitoneum in a laparoscopic rat model. The rats were divided at random into three groups: the sham group was subjected to catheter insertion but was not subjected to pneumoperitoneum; the saline group was subjected to 60 min of pneumoperitoneum and 30 min of reperfusion, with 1 mg/kg physiological saline administered 10 min before pneumoperitoneum; and the montelukast group was subjected to 60 min of pneumoperitoneum and 30 min of reperfusion, with 20mg/kg montelukast administered 10 min before pneumoperitoneum. Damage to ovarian tissue was scored by histopathological evaluation. Caspase-3 expression was determined immunohistochemically. Ovarian tissue levels of malondialdehyde and glutathione, and plasma total antioxidant capacity were measured biochemically. RESULTS: In comparison with the sham group, ovarian sections in the montelukast group had higher scores for follicular degeneration and oedema (p<0.001). Montelukast treatment prevented tissue damage in ovaries, and this result was significant. Caspase-3 expression was only observed in ovarian surface epithelium in the saline and montelukast groups. However, the mean caspase-3 expression score was higher in the saline group than the montelukast group (p<0.001). Tissue levels of malondialdehyde were higher in the montelukast group than the sham group, but plasma total antioxidant capacity and tissue levels of glutathione were significantly lower. Pretreatment with montelukast reduced lipid peroxidation (p<0.005) and improved antioxidant status in rats (p<0.001). CONCLUSION: Montelukast is effective for the prevention of I/R-induced damage in rat ovary.

Analysis of pomegranate juice components in rat corpora cavernosal relaxation.

This study evaluated the action of pomegranate juice (PJ) and its five principal phenolic constituents on rat corpus cavernosum smooth muscle (CCSM). Isometric tension studies were performed after precontraction with phenylephrine in CCSM from rats. Relaxant responses to PJ and its constituents ellagic acid (EA), chlorogenic acid, caffeic acid, cumaric acid and rutin were investigated. PJ and EA caused CCSM relaxations (94.1 ± 3.7 and 51.3 ± 9.9%), while others induced limited relaxant responses. EA response was not inhibited by L-N(G)-nitroarginine methyl ester (100 µM) and 1H-[1,2,4]-oxadiazolo[4,3-a]quinoxalin-1-one (1 µM). Tetraethylammonium (100 µM) and apamin (10 µM) and nifedipine (10 µM) inhibited EA-induced relaxations at 10(-3) M by 84%, 82% and 78%, respectively. Glibenclamide (10 µM) inhibited EA response (97%, 100 µM). PJ-induced relaxation was not altered by several inhibitors. EA was estimated to be responsible for 13.3% of relaxation caused by PJ. Our study demonstrated that PJ and EA-induced marked relaxations in CCSM. The opening of Ca(2+)-activated K+ channels and the inhibition of Ca(2+)-channels regulate the relaxation by EA, but not PJ. EA has a minor contribution to the marked relaxation obtained by PJ, suggesting the presence of other PJ constituents, which induce nitric oxide-independent corporal relaxation. Further studies are needed to examine the potential of PJ in combination with a PDE5 inhibitor in ED.

Cortical Blindness due to Bilateral Occipital Infarcts in a Renal Failure Patient with Prostate Cancer: A Rare Complication of Hemodialysis.

Loss of vision is a rare complication seen in hemodialysis patients. It is thought to develop because of the hypotension that can be observed during dialysis. This paper involves a patient with acute loss of vision during hemodialysis due to bilateral occipital infarcts.

Relation between Doppler findings and perinatal outcomes in fetuses with intrauterine growth restriction.

PURPOSE OF INVESTIGATION: To find the relationship between fetal Doppler findings and perinatal outcomes in intrauterine growth restriction. METHODS: Eighty-two cases with a prenatal diagnosis of intrauterine growth restriction between November 2008 and July 2009 were included in this prospective study at Ege University School of Medicine. Fetuses were grouped according to Doppler parameters: those with normal Doppler findings (n = 43), and those with impaired arterial (n = 27) and venous systems (n = 12). RESULTS: Out of 82 growth restricted cases, 43 (52.4%) had normal Doppler findings, while 27 (32.9%) displayed impaired arterial parameters and 12 (14.6%) had impaired venous parameters. The mean first minute Apgar scores were 7.57 +/- 1.53 for the group with normal Doppler flows, 6.8 +/- 2 for the group with an impaired arterial system, and 4 +/- 1.94 for the group with an impaired venous system. Two cases from the normal Doppler flow group (n = 42), four cases from the impaired arterial flow group (n = 27), and 11 cases from the impaired venous flow group (n = 11) had fifth minute Apgar scores under 6. Evaluation of the umbilical artery blood gas revealed acidosis in two cases from the normal Doppler flow group (n = 42), three cases from the impaired arterial system group (n = 27), and five cases from the impaired venous system group (n = 11). CONCLUSION: A Doppler spectrum from normal to venous system impairment correlated with poor fetal outcomes including fetal acidosis, fetal mortality and morbidity, decreased Apgar scores at 1 and 5 min, and neonatal morbidity.

Removal of volatile organic compounds by natural materials during composting of poultry litter.

The objective of this study was to reduce volatile organic compounds (VOCs) produced during composting of poultry litter. The natural zeolite, expanded perlite, pumice and expanded vermiculite as the natural materials were used for the reducing of VOCs. Composting was performed in a laboratory scale in-vessel composting plant. Poultry litter was composted for 100 d with volumetric ratio of natural materials:poultry litter of 1:10. The VOCs were tested using the FT-IR method by VOCs analyzer. Studies showed that VOCs generation was the greatest in the control treatment without any natural materials. The natural materials significantly reduced VOCs. At the end of the processes, removal efficiency was 79.73% for NZ treatment, 54.59% for EP treatment, 88.22% for P treatment and 61.53% for EV treatment. Potential of removal for VOCs on poultry litter matrix using natural materials was in order of: P>NZ>EV>EP.

Reliability and validity of the Turkish version of the Hamilton Depression Rating Scale.

The aim of the study was to examine the reliability and validity of the Turkish version of the Hamilton Depression Rating Scale (HDRS). Ninety-four patients with major depression/depressive mood disorders and 40 healthy controls participated in the study. The severity of depression was assessed with the HDRS, Beck Depression Inventory (BDI), and Clinical Global Impression score (CGI). The test-retest reliability coefficient of the HDRS was based on a 5-day interval was.85, with a Cronbach alpha coefficient of.75 and a split-half reliability coefficient of.76. Interrater reliability coefficients based on the independent ratings of four assessors were between.87 and.98. The correlation between the HDRS and BDI scores was.48, and between the HDRS and CGI it was.56. Principal Components Analysis yielded six factors. The correlation (-.13) between the control and patient groups indicates that the HDRS assesses depression very well.

The validity of diagnosis of melancholic depression according to different diagnostic systems.

BACKGROUND: Melancholic versus nonmelancholic depression dichotomy is perhaps the most widely accepted distinction in categorization of depression. This research aims to compare RDC, DSM-III, DSM-III-R, DSM-IV and ICD-10 melancholic/endogenous/somatic and nomelancholic/nonendogenous/nonsomatic depressive patients with regards to biological variables thyroid stimulating hormone (TSH), basal and post dexamethasone cortisol levels, age, age of onset of depression, psychosocial stressors, and severity of depression. METHODS: Sixty-five patients who had been diagnosed as having major depression according to DSM III-R, using SCID were included in this study. Patients were divided into melancholic and nonmelancholic subtypes using RDC, DSM-III, DSM III-R, DSM-IV and ICD-10 criteria and groups were compared on the basis of biological variables, as well as age, psychosocial stressors and the severity of depression. RESULTS: RDC endogenous depressives were older, more severely depressed and had higher cortisol levels then RDC nonendogenous depressives. DSM III-R melancholics were older, more severely depressed, reported fewer numbers of psychosocial stressors and had lower levels of TSH than nonmelancholics. DSM-IV melancholics were more severely depressed, had higher basal and post dexamethasone cortisol levels and lower TSH levels. The ICD 10 somatic depression group contained more severe, older depressives with lower TSH levels. CONCLUSION: The results of this research show that different criteria may identify different groups of patients as having melancholic depression. They also partly support the hypothesis that endogenous or melancholic depression have a biological basis. LIMITATIONS OF STUDY: The study involved a relatively small sample size from a single centre and the results are based on this relatively small sample.

Moclobemide and sertraline in the treatment of depressive disorders: a comparative study.

The efficacy and tolerability of moclobemide and sertraline were compared in a 13 week trial on 55 depressive patients. Patients were diagnosed according to DSM-III-R criteria using SCID (Structured Clinical Interview for DSM-III-R). The study group was composed of 48 patients with major depression and 7 with minor depression. Patients were randomized in two drug groups and raters were blind to the drugs patients used. HDRS and CGI were used to assess the change in depressive symptoms. Twenty seven patients received moclobemide and 28 patients received sertraline. The dose of moclobemide used was 300-600 mg/day and that of sertraline was 50-200 mg/day. At the end of 13 weeks mean drop in HDRS for the overall group was 14.78 and the response rate calculated as percentage of patients showing a 50% drop in HDRS score was 77.8. The response rate was 76.5% for moclobemide and 78.5% for sertraline. The difference was not significant. The side effects were assessed by using UKU Side Effects Rating Scale. The most three observed side effects were dry mouth, headache and insomnia.