Design, efficient synthesis, docking studies, and anticancer evaluation of new quinoxalines as potential intercalative Topo II inhibitors and apoptosis inducers.

As an extension for our earlier effort in the field of discovery of anticancer agents acting on DNA and Topo II, eighteen quinoxaline derivatives were designed and synthesized. Such members were designed to possess the main essential pharmacophoric features of DNA intercalators. The cytotoxic potential of the synthesized compounds was assessed against a group of human cancer cell lines (HCT-116, HepG2, and MCF-7). Doxorubicin as potential intercalative Topo II inhibitor, was used as a positive reference. In general, compounds 12, 15, 19, 21, and 22 showed promising anti-proliferative activities against the three cell lines with IC50 values ranging from 2.81 to 10.23 µM. The cytotoxicities of the most active compounds against normal human cells (WI-38) were evaluated, and the results revealed that these compounds have low toxicity. Further examination for the most active anti-proliferative members as Topo II inhibitors was also performed, showing a narrow range of the inhibitory activities (from 0.45 to 1.06 µM). In addition, DNA/methyl green assay was carried out to evaluate DNA-binding potential of such compounds. The results indicated that these compounds have strong to moderate DNA-binding affinities ranging from 33.48 to 51.23 µM. Further studies exhibited the capability of compound 22 to induce apoptosis in HepG2 cells and can arrest growth of such cells at G2/M phase. Also, compound 22 produced a significant increase in the level of caspase- 3 (10 folds) and caspase-9 (7 folds) compared to the control cells. Molecular docking studies were also conducted to investigate possible binding interactions between the target compounds and the DNA-Topo II complex.

Osteoid Osteoma at the Proximal Diaphysis of the Fifth Metatarsal.

The foot is rarely the focus of osteoid osteoma, and only a few of those cases are related to the fifth metatarsal. The present case demonstrates that atypical symptoms with suspicious findings on plain radiographs that are not associated with trauma must be analyzed carefully to determine the nature of the lesion and perform the precise treatment to obtain and sustain the cure. A 29-year-old man presented to the outpatient clinic with a 2-year history of chronic pain in the lateral aspect of his left forefoot. The onset was not related to trauma, surgery, local infection, osteomyelitis, or another entity regarding the proximal fifth metatarsal. The patient noted that the pain was aggravated at night and typically subsided with the use of salicylates or other nonsteroidal anti-inflammatory drugs. Initial plain radiographs demonstrated cortical thickening and a lytic lesion at the proximal diaphysis of the fifth metatarsal. Because the pain relief was transient, we suspected an osteoid osteoma lesion, and subsequent magnetic resonance imaging manifested pathognomonic signs of subperiosteal osteoid osteoma. Diagnosis was followed by planning of the surgery that ended the patient's symptoms.

The laboratory inventory handling with poliovirus and potential infectious materials in Mongolia / Монголын Анагаах Ухаан

BackgroundIn 1988, the Forty-first World Health Assembly adopted a resolution for the Global Polio Eradication.Since the initiative was launched, number of polio cases has fallen by over 99%. Today, only threecountries in the world, Afghanistan, Pakistan and Nigeria - remain polio-endemic. The Polio Eradicationand Endgame Strategic Plan of 2013-2018 calls for the gradual eradication of wild virus strain and thevaccine virus strain at the same time. In order to prevent the border transmission of wild type poliovirus,virus leakage from laboratories, it is required to conduct inventory of laboratories handling poliovirus andpotential infectious materials every 2 year.GoalTo identify laboratories handling poliovirus and potential infectious materialsMethodsSurvey of laboratories handling poliovirus and potential infectious materials was conducted amongstate, private, clinical, biomedical and environmental testing in total of 127 laboratories operating in21 provinces and 9 districts of Ulaanbaatar city by questionnaire. Survey questionnaire consists of 6sections (general, sample storage, laboratory biosafety, staff knowledge, information source, trainingand etc.). Study results were processed using SPSS-19 statistical programme.Results34.7% of 96 biomedical laboratories were analyzed stool samples. These laboratories were analyzedrotavirus (17.0%), intestinal bacteria (67.0%), Helicobacter (14.3%), parasite and other indicators (1.7%)in stool samples. 43.8% of laboratories were stored stool samples for one day and 3.1% up to oneyear. From 31 environmental testing laboratories 73.3% were bacterialdetection test on environmentalsamples. 60% of wastewater samples were collected from rivers, 16% on entrance to wastewatertreatment plant and after biological treatment combined, and 24% from other sources. Soil sampleswere collected near waste disposal and other sources (46.4%), and from unknown sources (53.6%).24.1% of all laboratories were stored environmental samples for 3 days, 3.4% for 45 days. Accordingto results, surveyed laboratories did not store samples for more than 1 year. Also, none of surveyedlaboratories (100%) were not stored poliovirus and potential infectious materials.Conclusion· The investigated laboratories were not stored poliovirus and potential infectious materials.· The biosafety and biosecurity status of laboratories should be improved in near future throughenhancing knowledge of laboratory workers and organizing training related to biosafetyandbiosecurity.

Evaluation of recent methods versus conventional methods for diagnosis of early-onset neonatal sepsis.

INTRODUCTION: Hospital-acquired infections continue to be a major public health problem, especially among neonates. Large proportions of infants are admitted to neonatal intensive care units (NICUs) and receive potent systemic antibiotics while the diagnostic work-up is still in progress. This study aimed to evaluate the recent methods for diagnosing neonatal sepsis (NS) and compare them to conventional diagnostic work-up. METHODOLOGY: The study included 100 neonates divided into three groups: proven early-onset NS, clinical early-onset NS, and negative infectious status. Bacterial DNA was detected in the blood by broad-range 16S rDNA polymerase chain reaction (PCR). Markers for diagnosis of bacterial infection, which includedprocalcitonin (PCT), interleukin-6 (IL-6), and highly sensitive C-reactive protein (hs-CRP), were measured by enzyme-linked immunosorbent assay (ELISA). RESULTS: Blood culture was positive in 25 cases, while PCR for 16S rDNA was positive in 32 cases. Hs-CRP was significantly elevated in 30 patients in group 1, 35 patients in group 2, and 8 patients in group 3. IL-6 was significantly elevated in 28 patients in group 1, 24 patients in group 2, and 9 patients in group 3. PCT was found to be significantly elevated in 29 patients in group 1, 31 patients in group 2, and 2 patients in group 3. CONCLUSIONS: The16S rDNA PCR assay was more sensitive than blood culture. The combination of markers (hs-CRP, PCT, and IL-6) is better than single markers to diagnose sepsis. PCT had greater diagnostic value than did hs-CRP and IL-6, while IL-6 was better for diagnosis of neonatal infection.

Insufficiency femoral fractures in patients undergoing prolonged alendronate therapy.

A 76-year-old woman complaining of pain and swelling in her right thigh was admitted to our clinic. She had been undergoing alendronate therapy for more than 10 years. Physical examination revealed a mild swelling, pathologic motion and pain in her right thigh. Radiograms showed a transverse fracture with a medial spike in the area of thickened cortices of femoral diaphysis. She received surgical stabilization. The patient is now pain-free and she has walked with full weight bearing without any complications since the first postoperative day. Dual-energy X-ray absorptiometry revealed a T-score for the lumbal spine of -2.89 and for the hip of -3.55. We stopped alendronate treatment. However the patient is receiving only calcium and vitamin D.

Reactions of 1,3-Diphenyl-2-pyrazolin-5-one and 4-Amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one. Synthesis of Some New Pyrazoles and Pyrazolones.

1,3-Diphenyl-2-pyrazolin-5-one 1 was converted to 5-azido-4-formylpyrazolone 3 which is used as the key starting compounds of some new pyrazole derivatives 4-9. Also, 4-amino-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one 10 is coupled with some diazonium salts to give coloured products 11, and reacted with isocyanates and isothiocyanates to give pyrazolylurea and thiourea derivatives which are then reacted with organohalogen compounds under PTC conditions to give 13,14 while with some active methylene compounds yielded 15 via Michael 1,4-addition reaction.

[Diagnosis and treatment of perforated pulmonary echinococcosis]. / Diagnoza i lechenie na perforiraliia belodroben ekhinokok.

UNLABELLED: Pulmonar hydatidosis is widespread disease. It is presented with different complications one of which is the perforation of the cyst into the pleural cavity. The aim of our research is to share our experience in diagnosis and operative treatment of the complications with perforated pulmonary echinococcus. MATERIALS AND METHODS: In the study the we have examined 278 patients with pulmonary echinococcus, 14 of which have perforation of the cyst into the pleural cavity.

[Pancreatic blood flow function in patients with duodenal peptic ulcer]. / Sostoianie krovotoka podzheludochnoi zhelezy u bol'nykh iazvennoi bolezn'iu dvenadtsatiperstnoi kishki.

The condition was studied of bloodflow in 29 patients with duodenal ulcer, operated on because conservative therapy proved to be ineffective. In patients with uncomplicated duodenal ulcer, disorders of the pancreas bloodflow are at their greatest in the area of the head of the gland at the level of arterioles, with arteriolospasm phenomena being most noticeable. The secured data are to be taken account of in selection of therapeutic measures to be instituted in the patients.

[Rupture of posterior wall of the left ventricle after mitral valve prosthesis]. / Razryv zadnei stenki levogo zheludochka posle protezirovaniia mitralnogo klapana.

Rupture of the posterior wall of the left ventricle is a comparatively rare complication occurring after prosthesis of the mitral valve, but resulting in high mortality. There is a great diverse of opinions regarding the causes of this complication. The likely causes are surgical injury and the used method for prosthesis. The authors studied 9 patients with rupture of the posterior wall of the left ventricle following mitral prosthesis. In all patients the prosthesis was carried out by the routine procedure by dissecting the two mitral cusps with subvalvular structures. Two (22%) patients survived after defect plasty. The above surgical policy is the most effective to control bleeding and achieve a favourable result of correction of this complication.