Antimicrobial,anti-inflammatory,anti-ulcer and antioxidant activities of Carlina acanthifolia root essential oil

The root of Carlina acanthifolia All. (Asteraceae) has been traditionally used in the treatment of various disorders including stomach and skin diseases. We studied antimicrobial, anti-inflammatory, anti-ulcer and antioxidant activities of Carlina acanthifolia root essential oil, in order to validate some of the ethnopharmacological claims. Antimicrobial activity was tested on 15 bacteria and three strains of fungi using the agar diffusion and broth microdilution methods. In assessing anti-inflammatory activity the carrageenan-induced rat paw oedema test was used, while ethanol-induced stress gastric ulcer test in rats was used in testing anti-ulcer activity. Antioxidant properties were evaluated trough the effect of the essential oil on lipid peroxidation (TBA assay) and its capability of quenching 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH radicals. The oil expressed significant antimicrobial activity, being the most active against Gram (+) bacteria: Streptococcus pyogenes, Enterococcus faecalis, Bacillus subtilis and against Candida albicans. In all applied concentrations, Carlina acanthifolia root essential oil reduced carrageenan-induced rat paw oedema in dose-dependent manner, achieving high degree of anti-inflammatory activity. The effect was comparable with that of indomethacin used as a reference drug. In the ethanol-induced stress gastric ulcer test in rats, it was shown that the tested essential oil produced significant dose-dependent gastroprotective activity. The results also pointed out substantial and dose-dependent antioxidant activity of the investigated essential oil, with carlina oxide as the main antioxidant component.     

Clinical evaluation of immunosuppressive factors (IAP-immunosuppressive acidic protein, IS-immunosuppressive substance) in head and neck cancer

It is reported that the levels of serum IAP and IS are useful parameters to evaluate the prognosis along with the clinical course of tumor bearing patients. Serum IAP and IS were examined in 149 patients with head and neck cancer. The level of serum IAP and IS increased in patients with not only advanced stages, but also poor prognosis. In general, the patients with death or recurrence had higher levels of serum IAP and IS than those with good prognosis. It is concluded that serum IAP and IS well reflect the immunological condition and clinical course of patients with cancer and may be one of the useful parameter for them.     

Usefulness of 123I-iomazenil SPECT in pediatric patients with neurological disease

This study examined the usefulness of 123I-iomazenil SPECT (IMZ-SPECT), a type of brain scintigram that focuses on the central benzodiazepine receptor in order to determine its distribution and the function of inhibitory neurons. IMZ-SPECT has been used for the detection of epileptogenic foci, especially when surgical intervention is considered. Interictal study by IMZ-SPECT is widely available at numerous institutions and its usefulness has been confirmed in patients with not only focal cortical dysplasia and hippocampal sclerosis, but also tuberous sclerosis and neuronal migration disorders, even when magnetic resonance image fails to demonstrate any abnormal findings. When interpreting scintigrams, the developmental dynamic change of the central benzodiazepine receptor in childhood and the duration of the benzodiazepine exposure period should be taken into consideration. It is expected that IMZ-SPECT will be used in various neurological disorders other than epilepsy in the future allow medical services to be provided based on findings in the inhibitory synaptic system obtained with IMZ-SPECT.     

Clinical study of patients undergoing paperless electroencephalography in emergency room

Fifty-eight patients who visited the emergency room of our center with febrile convulsions and impaired consciousness, and underwent paperless electroencephalography soon after arrival. They consisted of 25 male and 33 female children, ranging in age from 5 months to 15 years and 4 months, with a mean age of 4 years and 10 months. The final diagnoses were poor responsiveness associated with fever and febrile delirium in 5 patients, febrile convulsions in 26, encephalitis/encephalopathy in 24, convulsions associated with mild gastroenteritis in 2, and aseptic meningitis in 1. The appearance of spindle wave within 24 hours after admission was considered to be a favorable prognostic factor, whereas generalized high-amplitude delta waves without fast-wave components and dysrhythmic flat basic waves were considered poor prognostic factors. We conclude that bed-side paperless electroencephalography is useful for the evaluation of changes in the brain function and course of treatment.     

Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors

HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the synthesis of orally bioavailable azaindole hydroxamic acids that were potent inhibitors of the HIV-1 IN enzyme. Here we disclose the design and synthesis of novel tricyclic N-hydroxy-dihydronaphthyridinones as potent, orally bioavailable HIV-1 integrase inhibitors displaying excellent ligand and lipophilic efficiencies.     

Quinidine therapy for West syndrome with KCNTI mutation: A case report

The KCNT1 gene encodes the sodium-dependent potassium channel, with quinidine being a partial antagonist of the KCNT1 channel. Gain-of-function KCNT1 mutations cause early onset epileptic encephalopathies including migrating partial seizures of infancy (MPSI). At 5 months of age, our patient presented with epileptic spasms and hypsarrhythmia by electroencephalogram. Psychomotor retardation was observed from early infancy. The patient was diagnosed with West syndrome. Consequently, various anti-epileptic drugs, adrenocorticotropic hormone therapy (twice), and ketogenic diet therapy were tried. However, the epileptic spasms were intractable. Whole exome sequencing identified a KCNT1 mutation (c.1955G>T; p.G652V). At 2 years and 6 months, the patient had daily epileptic spasms despite valproate and lamotrigine treatment, and was therefore admitted for quinidine therapy. With quinidine therapy, decreased epileptic spasms and decreased epileptiform paroxysmal activity were observed by interictal EEG. Regarding development, babbling, responsiveness, oral feeding and muscle tone were ameliorated. Only transient diarrhea was observed as an adverse effect. Thus, quinidine therapy should be attempted in patients with West syndrome caused by KCNT1 mutations, as reported for MPSI.     

Sodium-23 MR imaging of the kidney in guinea pig at 2.1 T, following arterial, venous, and ureteral ligation

In vivo 23Na magnetic resonance images of guinea pig kidney were obtained at 2.1 T using a spin-echo sequence with an echo time of 19 ms. The intact kidney showed a very strong signal intensity in the sodium image. The signal intensity of the kidney decreased to 55% after ligation of the renal artery together with the vein and the ureter. The total sodium content in the excised kidney after arterial occlusion, measured by flame photometry, was 24% higher than that in the intact kidney. The transverse relaxation time (T2) of the extracellular sodium in the isolated kidney decreased to one-third of that in the intact kidney. This shortening of T2 may be partly responsible for the decrease in the 23Na signal intensity from the kidney after arterial occlusion.     

Potassium-39 nuclear magnetic resonance observation of intracellular potassium without chemical shift reagents during metabolic inhibition in the isolated perfused rat heart

The intracellular potassium content of perfused rat heart was measured by potassium-39 nuclear magnetic resonance (NMR) spectroscopy at 33 degrees C with an inversion recovery technique based on the fact that the spin-lattice relaxation time (T1) of the intracellular potassium (8.3 msec at 8.45 T) is much faster than that of the extracellular potassium (68 msec). Intracellular potassium decreased to 60.2 +/- 4.3% of the control level (mean +/- SEM, n = 6) at 40 minutes from the start of metabolic inhibition (2 mM cyanide, 0 mM glucose). Removal of cyanide restored intracellular potassium to 94.2 +/- 3.9% at 30 minutes from the restart of oxidative metabolism. The cumulative potassium loss was determined from the flow rate and potassium concentration of the coronary effluent, which reached 139 +/- 12 mumol/g dry wt during 40 minutes of metabolic inhibition. This value was calculated as 41.8% of intracellular potassium in the control heart and agreed with the decrement of intracellular potassium measured by NMR. During the metabolic inhibition and recovery period, a linear correlation was observed between the changes in 39K NMR-observed intracellular potassium and the cumulative potassium loss. The present results evaluate the inversion recovery technique as a method to successfully monitor the myocardial intracellular potassium.     

Evaluation of prostacyclin analogue OP-41483 as an adjunct to crystalloid cardioplegia in infants and children

A chemically stable prostacyclin analogue (PGI2-A, carbacyclin, OP-41483) was evaluated as an adjunct to potassium cardioplegia in infants (n = 13) and children (n = 32), in whom the current potassium cardioplegia may be limited in its effects. PGI2-A was added in a dose of 300 micrograms/L to the potassium cardioplegic solution. Postoperatively, peak levels of the myocardial-specific isoenzyme of creatine kinase (MB-CK) were compared for the PGI2 group and a control group (n = 65). In patients 1 year of age or older (n = 32 and 49 for the PGI2 and control groups, respectively), the MB-CK level was significantly lower in the PGI2 group only when compared between the subgroups with an aortic cross-clamp time of 120 minutes or more (n = 9 and 10; MB-CK level, 35.2 +/- 15.6 vs 68.3 +/- 32.4 IU/L;p less than 0.05). In patients less than 1 year of age, in whom aortic cross-clamp times were generally less than 120 minutes, the MB-CK level was also lower in the PGI2-A group than in the control group (n = 13 and 16; MB-CK level, 33.6 +/- 14.3 vs 61.6 +/- 36.3 IU/L;p less than 0.05). Infants less than 6 months of age (n = 18) underwent ultrastructural assessment of left ventricular myocardial biopsy specimens, and the PGI2-A group showed better results in mitochondrial and intracellular edema scores. This clinical trial showed beneficial effects of PGI2-A used with crystalloid potassium cardioplegia in infants and children.