Design and synthesis of novel organometallic complexes using boronated phenylalanine derivatives as potential anticancer agents

Drug design and discovery studies are important because of the prevalence of diseases without available medical cures. New anticancer agents are particularly urgent because of the high mortality rate associated with cancer. A series of mononuclear gold (III) and platinum (II) complexes based on boronated phenylalanine (BPA) were designed and synthesized using 4,4’-dimethyl-2,2’-dipyridyl (L1) or 1,10-phenanthroline-5,6-dion (L2) ligands to obtain promising anticancer drug candidates. Proton nuclear magnetic resonance, infrared, mass spectrometry, and elemental analyses were utilized for chemical characterizations. Cell viability, cancer cell colony formation, endothelial tube formation, and cytoskeleton staining assays were performed using A549 lung adenocarcinoma and human umbilical vein endothelial cells (HUVECs) to investigate preliminary pharmacological activities. L1-based platinum (II) complex (BPA-L1-Pt) was the most promising complex, and has similar activity with the approved chemotherapy drug cis-platinum. Half maximal inhibitory concentration values for BPA-L1-Pt were 9.15 µM on A549s and 16.61 µM on HUVECs; the values for cis-platinum were 5.24 µM on A549s and 23.14 µM on HUVECs. Consequently, further synthesis studies should be performed to boost the cancer cell selectivity feature of BPA by varying metal and ligand types.     

The problems and advantages of one lung ventilation during surgical intervention in pulmonary hydatid cyst disease

Background Hydatid disease is the most severe helminthic zoonosis, with an important public health problem especially in rural areas in Turkey. The aim of this study was to review the problems and advantages encountered in surgical treatment of 43 patients who were ventilated with one-lung ventilation during last four years. Methods Patients, operated with one-lung ventilation, constitute the study group. Data related to symptoms, radiographic findings, performed surgical procedures, perioperative and postoperative morbidity, hospitalization time, and cyst recurrence were collected from each individual's records. Results Cystotomy and capitonnage were performed in all cases. Perioperative complications were seen in 5 patients. Four of these 5 patients had double-lumen endotracheal tube malpositioning. In one patient hypoxemia developed. The most common postoperative complication was atelectasis. One patient had recurrent cysts. There was no perioperative or postoperative death. Conclusions We prefer cystotomy and capitonnage because it is a fast and effective technique with limited postoperative complications. One-lung ventilation prevents the exposure of lower lung areas from massive aspiration, which may cause acute obstruction of airways, and contamination by cyst contents from the operative part of the lung that causes recurrent disease. One-lung ventilation in pulmonary hydatid cyst surgery may be preferred owing to lower mortality and morbidity rates.     

Effects of intranasal 17beta-estradiol and raloxifene on lipid profile and fibrinogen in hypercholesterolemic postmenopausal women: a randomized, placebo-controlled clinical trial.

AIM: To compare the effects of 17beta-estradiol given intranasally (intranasal E2) and raloxifene on serum lipid profile and fibrinogen in hypercholesterolemic postmenopausal women. METHODS: The study population consisted of 46 women after menopause. The placebo group (n = 11) was given calcium, while the intervention groups were given intranasal E2 (Aerodiol; Servier, Chambray-les-Tours, France) (n = 16) or raloxifene (Evista; Lilly SA, Madrid, Spain) (n = 19). Blood lipids and fibrinogen were compared between groups at baseline and after 3 months of treatment. RESULTS: The group receiving intranasal E2 showed a significant decrease in triglyceride levels (p<0.05) and a marked increase in high-density lipoprotein cholesterol levels (p<0.05). No changes in lipid profile were observed in the raloxifene and placebo groups. Raloxifene caused a significant decrease in fibrinogen levels (p<0.05). CONCLUSION: Intranasal E2 exerts significant effects on lipid profile in hypercholesterolemic postmenopausal women. Raloxifene has a greater impact on fibrinogen than intranasal E2 application.     

Electron inelastic mean free path formula and CSDA-range calculation in biological compounds for low and intermediate energies.

In this study, for low atomic number targets and biological compounds, an inelastic mean free path (IMFP) formula and energy straggling parameter formula are presented, being valid for low and high electron energies. In addition, calculation of the continuous slowing down approximation-range (CSDA-range) from the stopping power is also made. The IMFP and the energy straggling parameter formulae are evaluated using the generalized oscillator strength (GOS) model and the exchange correction to the inelastic differential cross section (IDCS) given by Inokuti, M., [1978. Inelastic collisions of fast charged particles with atoms and molecules--the Bethe theory revisited. Rev. Mod. Phys. 50, 23-35]. The IMFP and CSDA-range for the biological compounds C5H5N5 (adenine), C5H5N5O (guanine), C4H5N3O (cytosine), C5H6N2O2 (thymine), C20H27N7O13P2 (cytosine-guanine) and C19H26N8O13P2 (thymine-adenine) have been introduced for incident electrons in the energy range 20 eV-1 MeV. The calculated results are compared with semi-empirical results and other theoretical results, good agreement being found with experimental data and Monte Carlo (PENELOPE code) predictions. All the IMFP versus energy curves exhibit minima around 80 eV.     

Delayed Reduction of Irreducible Chronic Posterolateral Dislocation of the Knee with Buttonholing of the Medial Femoral Condyle

Abstract Traumatic knee dislocations are relatively rare and almost always respond to closed reduction; however, a small percentage of knee dislocations are irreducible and in these cases open reduction is frequently required. A 65-year-old man with an unreduced posterolateral knee dislocation with laterally dislocated patella was seen 3 weeks after a motor vehicle accident. Medial femoral condyle was found buttonholed through the medial capsule together with the medial collateral ligament and lying in the medial joint space that allowed posterior rotary dislocation of the joint. Both cruciate ligaments and medial meniscus were torn. There was no evidence of any vascular or nerve injury. Reduction was accomplished by removal of the capsuloligamentous structures which were incarcerated in the trochlea and intercondylar notch and by excision of meniscal tear. Following posterior cruciate ligament reconstruction with patellar tendon autograft, lateral patellar release, vastus medialis advancement, and gracilis transfer were done.     

Comparison of indium-111 octreotide and thallium-201 scintigraphy in patients mammographically suspected of having breast cancer: Preliminary results

Indium-111 octreotide and thallium-201 scintigraphic studies were compared in 21 patients (16 with palpable and five with non-palpable lesions) suspected of having breast malignancies on the basis of mammography. Early (15 min) and late (3 h)²⁰¹Tl (111 MBq) and 4-h and 24-h¹¹¹In-octreotide (111–148 MBq) static planar anterior images (matrix 256×256) were obtained on separate days. Images were evaluated both visually and quantitatively. Biopsy was performed following the imaging studies. Histopathology revealed 17 breast carcinomas (15 cases of invasive ductal carcinoma, one mucinous adenocarcinoma and one intraductal carcinoma) and four benign breast lesions (two fibroadenomas, one abscess and one case of fat necrosis). The means histopathologcial tumour size (mean largest diameter) was 3.38±1.9 cm.¹¹¹In-octreotide detected 16 of the 17 breast cancers (94%) while²⁰¹Tl detected 13 of them (76%). Both¹¹¹In-octreotide and²⁰¹Tl missed one nonpalpable carcinoma showing only an isolated cluster of microcalcifications on mammography. The smallest tumour size detected by both agents 1.5×1.5 cm. Of the four benign lesions, only the breast abscess revealed both²⁰¹Tl and¹¹¹In-octreotide uptake.¹¹¹In-octreotide scan also showed tracer uptake in five of the six patients with histologically proven axillary metastases, while four of these six patients showed²⁰¹Tl uptake. The tumour/background (T/B) ratios of late¹¹¹In-octreotide and²⁰¹Tl images were 1.71±0.38 and 1.46±0.30 respectively (P=0.039). In this preliminary study,¹¹¹In-octreotide yielded more favourable results than²⁰¹Tl in the detection of breast carcinomas. However, the diagnostic efficacy of¹¹¹In-octreotide imaging needs to be investigated in larger patient series.