Ferrocene-containing tetrahydropyrazolopyrazolones: Antioxidant and antimicrobial activity.

A series of ferrocenes which contain dinitrogen-fused pyrazolidinone ring were synthesized from acryloylferrocene (4) and N,N'­cyclic azomethine imines (3). Novel 5­aryl­6­ferrocenoyltetrahydropyrazolo[1,2­a]pyrazol­1(5H)-ones were obtained as mixtures of two diastereoisomers (trans and cis) which were separated and isolated as pure substances. Ortho-substituted N,N'­cyclic azomethine imines 5-oxo-2-(2,4,6-trimethylbenzylidene)pyrazolidin-2-ium-1-ide (3e) and 2-(2-methoxybenzylidene)-5-oxopyrazolidin-2-ium-1-ide (3f) reacted stereoselectively affording only trans-6-ferrocenoyl-5-mesityltetrahydropyrazolo[1,2-a]pyrazol-1(5H)-one (5e) and 6-ferrocenoyl-5-(2-methoxyphenyl)tetrahydropyrazolo[1,2-a]pyrazol-1(5H)-one (5f). Ferrocenyl derivatives were screened for in vitro antioxidant and antifungal activities and excellent DPPH and ABTS radicals scavenging activity was observed with majority of tested 5­aryl­6­ferrocenoyltetrahydropyrazolo[1,2­a]pyrazol­1(5H)-ones. Several tested compounds showed selective scavenging properties neutralizing ABTS•+ radical cations in contrast to inactivity toward DPPH radicals. Trans-5-aryl-6-ferrocenoyltetrahydropyrazolo[1,2-a]pyrazol-1(5H)-ones 5b, 5c, 5d, 5j as well as cis-6-ferrocenoyl-5-(p-tolyl)tetrahydropyrazolo[1,2-a]pyrazol-1(5H)-one (6d) displayed fungal growth inhibition at low concentration against C. albicans and/or A. brasiliensis. Molecular docking studies revealed that the cis-6-ferrocenoyl-5-(4-nitrophenyl)tetrahydropyrazolo[1,2-a]pyrazol-1(5H)-one (6l) and cis-6-ferrocenoyl-5-(naphthalen-2-yl)tetrahydropyrazolo[1,2-a]pyrazol-1(5H)-one (6n) have potential to become lead molecules in drug discovery process.

Towards the re-introduction of grass pea (Lathyrus sativus) in the West Balkan Countries: the case of Serbia and Srpska (Bosnia and Herzegovina).

Vetchlings (Lathyrus spp.) are widely distributed in both Serbia and Srpska, and represent a valuable component of local floras all over the Balkan Peninsula. Despite this and the existence of a traditional Serbian name for grass pea (Lathyrus sativus L.), sastrica, and a pan-Slavic name for all vetchlings, grahor, today they are almost forgotten crops. The joint action of the Institute of Field and Vegetable Crops and the Faculty of Agriculture is aimed at re-introducing grass pea and other vetchlings as multifunctional crops. Within the legume collection in the Institute of Field and Vegetable Crops, a small Lathyrus spp. collection, including about 100 accessions of 16 species, most of them being grass pea, was established in 2002. The landraces of grass pea were collected in several regions of Serbia and Srpska, where they are used for human consumption. Grass pea is commonly used boiled and along with other pulses, with no reports on lathyrism among the local people. The first Serbian breeding programme in Novi Sad produced already two grass pea lines that were registered in November 2009 under the names of Studenica and Sitnica, developed from the crosses of Polish cultivars and local Serbian landraces.

[Blood replacement in severely injured patients].

Haemorrhage remains a leading cause of early death in injured and application of concentrated RBC transfusion in the treatment of multiple injuries is the basis and potential component of saving lives. The aim of this study was to analyze the received amount reimbursed blood in patients with severe trauma, depending on the outcome, severity and mechanism of injury. Collected data on gender, age and age as the mechanism of injury, amount of blood recovered intraoperatively and during the first six days of hospitalization, which were analyzed according to outcome of treatment, ISS, AIS, and APACHE II score. Results showed that patients with lethal outcome received a larger amount of blood, there is a statistically significant correlation with ISS and AIS score for extremity injuries, and that larger amount of blood received patients injured in the traffic accidents, as pedestrians and motorcycle riders/bike, and there is no correlation with APACHE II score. Based on the importance of this topic for further research are necessary in this area in order to more accurately define indications and dosage and method of reimbursement of blood in patient with severe trauma.

Antioxidant activity of selected plant species; potential new sources of natural antioxidants.

The aim of this study was to examine six plants from Serbia for their potential antioxidant activity. Therefore, six antioxidant activity assays were carried out, including: total antioxidant capacity, DPPH free-radical scavenging, the inhibitory activity toward lipid peroxidation, Fe(3+)- reducing power, Fe(2+)- chelating ability and hydroxyl radical scavenging activity. Total phenolic and flavonoid contents were also determined for each alcoholic extract. Cotinus coggygria extract contained the highest amount of total phenols (413mg GAE /g dry extract), while the highest proportion of flavonoids was found in the Echium vulgare methanol extract (105 mg RU/g). Cotinus coggygria and Halacsya sendtneri alcoholic extracts showed the highest total antioxidant capacity (313 and 231 mg AA/g dry extract), as well as DPPH free-radical scavenging (IC(50)=9 and 99 µg/ml), inhibitory activity toward lipid peroxidation (IC(50)=3 and 17 µg/ml) and reducing power. Whereas, the greatest hydroxyl radical scavenging activity, as well as ferrous ion chelating ability showed Echium vulgare, Echium rubrum and Halacsya sendtneri.

Nuclear volume in type I gastric intestinal metaplasia.

OBJECTIVE: To retrospectively compare nuclear size of epithelial cells in type I intestinal metaplasia (IM) from various pathologic lesions of gastric mucosa. STUDY DESIGN: Endoscopic mucosal biopsies with type I IM from intestinal type gastric carcinoma (n = 25), chronic gastritis (n = 40) and benign ulcer (n = 32) cases were analyzed. After standard fixation, embedding, sectioning, routine hematoxylin and eosin and alcian blue--periodic acid--Schiff reaction (pH 1.0 and 2.5) staining were used for identification of IM. The mean point sampled nuclear intercept was estimated by the original test system and 100x objective at a total magnification of 1,200x. To obtain the mean nuclear volume, the cubed nuclear intercept was multiplied by pi/3. In each case 100 epithelial cell nuclei were analyzed. RESULTS: In type I IM in gastric carcinoma cases there was significantly greater nuclear volume (118.34 +/- 10.32 micron 3) than in type I IM in other pathologic states of gastric mucosa (77.72 +/- 8.58 micron 3). CONCLUSION: The karyometric findings of the present study suggest a difference between type I IM found in benign pathologic states and type I IM found in gastric mucosa surrounding carcinoma, despite morphologic and histochemical similarities. Nuclear volume may be used in early detection of precancerous states of gastric mucosa.

Improvement in ratings of tension after TRH administration in healthy women.

Administration of thyrotropin releasing hormone (TRH), 400 micrograms i.v., to healthy premenopausal women resulted in improvement in ratings of tension on the 100 mm line test. The max. mean improvement in tension ratings was significantly greater after TRH than after saline (t = 2.27, df = 9, p less than 0.05); after TRH administration, eight of 10 subjects showed greater than 30% improvement in tension ratings, while only three of 10 subjects receiving saline reported a comparable degree of improvement. No significant improvement in ratings of mood state were noted after administration of either TRH or saline. These findings extend previous reports of behavioral effects of TRH in normal subjects. The possibility that the behavioral effects of TRH may be influenced by the state of activity of the CNS is discussed.

Hyperthyroidism due to excess thyrotropin secretion: follow-up studies.

Follow-up studies of a woman with hyperthyroidism due to excessive TSH secretion, previously reported (1), are described. For most of the ensuing years, she has been treated with methimazole. On several occasions, methimazole was discontinued; each time elevations of serum TSH, T4, and T3 concentrations, similar in magnitude to those originally present, occurred. Initially, her serum TSH concentrations fell substantially after dexamethasone administration and did not change after TRH. The same responses have occurred on several occasions during the follow-up period. Serum glycoprotein alpha-subunit and TSH-beta concentrations were normal and did not change after TRH administration, but serum alpha-subunit declined during dexamethasone and increased slightly after gonadotropin-releasing hormone. No increase in serum TSH occurred after TRH administration when TSH secretion was decreased by dexamethasone administration. No evidence of pituitary enlargement has developed during the 7-yr follow-up period. The cause of this patient's excessive TSH secretion remains unknown, but her TSH secretory dynamics are most consistent with those found in patients who had TSH-secreting pituitary adenomas reported in recent years.