Synthesis and pharmacological screening of certain imidazoquinazolone derivatives

Certain imidazoquinazolin-5[4H]-one derivatives have been synthesized by replacement of the 4-amino group compound I with different moieties of expected biological activity. Representative example of the synthesized compounds were tested for their anti-inflammatory, analgesic, antipyretic and anticonvulsant activities. Certain derivatives showed activities higher than that of the reference drugs

Conventional Vs non invasive ventilation in acute respiratory failure

Treatment of patients with acute respiratory failure [ARF] often involves mechanical ventilation via endotracheal intubation. Non-invasive positive pressure ventilation [NIV] using Bi-level positive airway pressure [BiPAP] can be a safe and effective means of improving gas exchange. 1] Assess non-invasive positive pressure ventilation [BiPAP] as an alternative way for ventilation in ARF, and to 2] Determine factors that can predict the successful use of BiPAP. Thirty patients with acute respiratory failure [both type I and II] were enrolled in the study and divided into two groups. Group I included 10 patients who were subjected to invasive mechanical ventilation. Group II included 20 patients were subjected to NIV using BiPAP. Both groups were compared regarding the following parameters: Arterial blood gases [ABG] on admission, 30 minutes after beginning of mechanical ventilation, 1[1/2] hour then once daily. Complications namely ventilator associated pneumonia [VAP], skin necrosis and CO[2] narcosis; static compliance and resistance were measured at day one and day two. Compared to group I, group II patients were associated with similar improvement in ABGs data at 30 minutes and at discontinuation of ventilation [Table A]. Group II patients showed significantly lower incidence in VAP [20% Vs 80%], shorter duration of mechanical ventilation [3 +/- 3 Vs 6 +/- 5 days, p=0.006], with shorter length of hospital stay [5.8 +/- 3.6 Vs 8.9 +/- 2.7 days, p=0.011] when compared to group I. Skin necrosis [50%] and CO[2] narcosis [20%] occurred in group II only. Group II patients showed significant difference change in compliance and change in resistance from day I to day II when compared to group I Table [B]. On univariate basis, parameters were analyzed to choose those who were associated with outcome in concern [successful NIV]. The following parameters were identified: Level of consciousness, pH [7.3 +/- 0.03 Vs 7.26 +/- 0.1, p=0.009] PCO[2] [69.16 +/- 13.14Vs 100.97 +/- 12.04] on admission, 1[1/2] hour after NIV, pH [7.37 +/- 0.03 Vs 7.31 +/- 0.17, p=0.005], PCO[2] [53.98 +/- 8.95 Vs 77.47 +/- 5.22, p=0.0001] in whom NIV succeeded and failed respectively. Then multivariate analysis utilizing two different techniques namely [multivariate logistic regression and discriminate analysis] was used. The variable identified was PCO[2] after 1[1/2] hour in the two models with specificity 100%. In patients with acute respiratory failure, non-invasive ventilation was as effective as conventional ventilation in improving gas exchange, associated with fewer serious complications and shorter stay in intensive care. One and half hour trial with NIV can predict success with BiPAP, as shown by an improvement in pH and PCO[2] and overall clinical picture. PCO[2] after 1[1/2] hour could be the sole predictor of successful NIV with 100% specificity

Anterior ethmoidal artery, a surgical and radiological study

Anterior ethmoidal artery [AEA] has a great clinical and surgical importance. It is a particularly important landmark for the fovea ethmoidalis and the base of the anterior cranial fossa. It is a possible sight of traumatic or intraoperative bleeding. Accurate localization of the anterior ethmoidal canal [AEC] and anterior ethmoidal artery [AEA] both radiologically and surgically and their relation to nasal lamellas and skull base in order to avoid the serious complications that might happen after violation of the canal or the artery. 50 patients diagnosed to have chronic rhinosinusitis [CRS] with or without sinonasal polyposis were selected. All the cases were subjected to: a] preoperative computerized tomography. b] operative intervension in the form of endoscopic sinus surgery [ESS], with dissection of the roof of the ethmoid sinuses for indentification of the anterior ethmoidal canal [AEC]. Radiological evaluation was done by axial, helical thin cuts and reconstructed saggital views, while assessment during surgery was encountered after direct endoscopic visualisation, using palpation with a probe and simple ruler measurements. Twelve patients had ESS performed on one side and 38 patients ESS on both sides. Thereby, a total of 88 AEC identifications were performed. In all dissections the AEC and AEA were successfully identified surgically and radiologically. On comparing surgical and radiological localization of the AEC in relation to the lamellas, it was found that the location of the AEC was the same in 86 dissections, while not in 2 dissections. AEC was positioned inside the skull base without bony defects in 82 dissections, and in 6 dissections, 2mm below the skull base, connected to it by a mesentry. Endoscopic localization of the AEC during surgery and the results of CT imaging were comparable. It was found that the AEA, the anterior turbinate axilla and the superomedial edge of the nostril were in a straight line. This finding was extremely helpful in the endoscopic search for the AEA

Evaluation of oils from the plants mentha sativa,] ocimum basilicum and cinnamomum camphor on survival, hepatic enzymes activities and protein electrophoresis of biomphalaria Alexandrina snails

Three plant oils from the plants Spearmint, Basil and Camphor were tested for their molluscicidal activity against Biomaphalaria alexandrina snails. Spearmint oil was more toxic than the other two oils against B. alexandrina. Its Lc50 was 42 ppm; meanwhile the values were 500 and 560 ppm for Basil and Camphor, respectively. Spearmint oil, also, showed a more deleterious effect against both miracidia and cercariae of S. mansoni than the other two oils, all of them were killed after 15 min of exposure to 70 ppm. The present results indicated that the alterations in total protein concentrations in tissues of treated snails were not significantly different from that of control ones. It was noticed, also, that the increase in the activity of ALT enzyme and the decrease in that of AlkP enzyme in tissues of treated snails were not significantly different than that of control snails. However, Spearmint oil at 32 and 42 ppm significantly decreased the activities of AST and ACP activities in snail's tissues in comparison with control ones. The electrophoretic [SDS-PAGE] pattern of tissue soluble proteins extracted from treated and controls B. alexandrina snails showed different plant oils effects on the synthesis of protein within snails yielded a complex pattern of polypeptides ranging in molecular weight between 14.7 to 304.6 KDa. Some bands were present in treated snails especially at Camphor oil and at 500ppm of Basil oil. At least, three bands were absent from tissues of snails treated with 42ppm of Spearmint oil in comparison with control group. The molecular weights of these bands are 14.9, 15.7 and 17.0 KDa. It was, also observed that total number of bands in snails treated with Basil or Camphor oil was more [15-17 bands] than that of control group [13 bands]

Enhancement of surgically repigmented vitiligo by narrow-band ultraviolet B phototherapy

Various surgical techniques and modifications have been described to treat recalcitrant but stable vitiligo with satisfactory results in terms of degree of repigmentation and color match. The minigrafting technique is relatively simple and can be carried out as an outpatient clinic procedure. Although minigrafting can be an effective treatment in vitiligo, failure to achieve complete repigmentation in a high percentage of patients remains a major drawback. This study was designed to evaluate the efficacy of postoperative UV-B supplementation to surgically repigmented vitiligo patches. The study included 20 patients with localized non-progressive vitiligo not responding to medical treatment or phototherapy. Patients were subdivided randomly into two groups [I, II] each including 10 patients. Patients in group I were treated by minigrafting only, while group II patients were treated by minigrafting followed by narrow band- UVB phototherapy. The current study showed that the combination of the surgical treatment [minigrafting] with the phototherapy [NB-UVB] was more effective in repigmenting focal and segmental stable vitiligo than treating it only surgically. The study recommends the use of narrow-band UVB as an adjuvant therapy after surgical repigmentation of vitiligo

prevalence of extramucosal fungal elements in eosinophilic chronic rhinosinusitis with bilateral polyposis

Chronic rhinosinusitis [CRS] is an inflammatory disease of the nasal and paranasal mucosa persisting for more than 3 months. Mucosal inflammations may be in the form of granulation tissue, polyp formation or fibrosis. Allergic fungal sinusitis [AFS] is the most common non invasive form of fungal rhinosinusitis. The diagnostic criteria for AFS are: [1] CRS, [2] the presence of allergic mucin and [3] the presence of fungal organisms within that mucin confirmed by culture, histology or both. The aim of this work is to define the prevalence of fungal elements in the nasal and sinus mucus in cases of CRS with bilateral polyposis compared with normal controls via mycologic and histologic identification of the various fungal species colonizing the viscid allergic mucin. For the 100 studied patients, 300 cultured plates were done, 281 positive cultures were reported; yeilding 29 different fungal genera. Aspergillus species were more prevalent than any other fungal elements in both patients and controls. Alternaria species were the second most commonly encountered fungal species among patients versus controls. Histopathological examination by fungalase stain is 100% sensitive versus Periodic Acid Schiff stain [PAS] and Gomori Methenamine Silver stain [GMS], both are 60% sensitive. The average number of organisms was higher in the patient group than in the controls. So the disease may be related to the amount of the fungal burden present in the mucus and not the mere presence of fungi giving rise to the future role of the quantitative analysis of fungal DNA in CRS using PCR. Increased awareness towards the rising role of the fungal etiology, implementing an allergic immunologic reaction in all cases of CRS with bilateral polyposis, may lead to a totally different concept in the management of CRP; as it would guide the surgeon on the surgical approach, the extent of resection, and any perioperative adjuvant medical therapy including immunotherapy and local antifungal therapy

Influence of certain fertilizers on the activity of some molluscicide against Biomphalaria Alexandrina and lymnaea natalensis snails

Effect of the fertilizers [ammonium nitrate, potassium sul- phate and urea] on molluscicides [copper sulphate, niclosamide and mollutox] against B. alexand-rina and L. natalensis was investigated. The molluscicides were more potant than fertilizers. Snails were exposed for 24 hr to a fertilizers using LC0 [1/10 and LC50] than, to molluscicides. Per- exposure to potassium sulphate caused a synergistic action with copper sulphate, niclosamide and mollutox on L. natalen-sis. Pre-exposure to urea caused an additive effect with niclo-samide and mollutox against L. natalensis and B. alexandrina res- pectively. Pre-exposure to ammonium nitrate caused an additive action to niclosamide on L. natalensis. Snails exposed for 24hr to one molluscicide, then exposed to fertilizers, showed that pre-exposure to niclosamide or mollutox caused an additive effect with ammonium nitrate and potassium sulphate. Pre-expo-sure to mollutox caused an additive effect with urea on the two snails' sp. Juvenile or adult B. alexandrina were ex-posed to LC0 of molluscicde-fertilizer mixture, showed that urea when mixed with each molluscicides showed greatly reduced on the growth rate percent, survival rate and snail fecundity mollus-cicides and fertilizers mixed at ratios of LC [40:10,30:20, 25:25, 20:30 and 10:40], the toxicity of the mixtures cau-sed antagonistic effect on adult B. alexandrina, but a mixture of niclosamide-ammonium nitrate caused a potent effect [syner-gism or additive] except at ratio 20:30 which showed an antago-nism on L. natalensis. Mixtures of copper sulphatepotassium sulphate [10:40], niclosamide-potassium sulphate [20:30], moll-utox-ammonium nitrate [25:25] revealed an additive effect on L. natalensis.

Semifield trials to control biomphalaria Alexandrina by different modes of exposure to certain plant and chemical molluscicides

Semi-field trials were carried out in Snail Research Station under simulated natural conditions to evaluate different modes of exposure to Anagallis arvensis and Calendula micrantha as plant molluscicides and bayluscide and copper sulphate as chemical molluscicides. Firstly, B. alexandrina were exposed to the tested molluscicides alone and in addition to two densities of aquatic plants. No apparent effect of aquatic plants on the activity of both plant and chemical molluscicides, this may be due that the two densities of the aquatic plants used were insufficient to interfere with the molluscicides action. Secondly, snails were pre-exposed to three sub-lethal concentrations of the plant molluscicides for 24h then to three concentrations of the chemical molluscicides and vice versa. The results indicate that the pre-exposure increases the snail mortality significantly in all treatments of bayluscide and A. arvensis [except in the highest concentration when the snails firstly exposed to bayluscide then to A. arvensis, where the two compared treatment showed 100%] and in all treatments of bayluscide and C. micrantha. Also, in one treatment of copper sulphate and A. arvensis [in the highest concentration when the snails firstly exposed to A. arvensis then to copper sulphate] and in three treatments of copper sulphate and C. micrantha, [in least and moderate concentrations when snails firstly exposed to C. micrantha then to copper sulphate and in the highest concentration when snails firstly exposed to copper sulphate then to C. micrantha]. Thirdly, snails were exposed to mixtures of six different ratios of hayluscide and each of A. arvensiS and C. micrantha. The results indicated that the snail mortality increased significantly only in the first treatient of bayluscide and A. arvensis mixtures and in treatment number 6 of bayluscide and C. micrantha

Difference in the susceptibilty to certain molluscicides and Schistosoma mansoni infection of three forms Egyptian Biomphalaria glabrata

The first generation of three morphologically different forms of B. glabrata collected from Giza was compared for LC50 values susceptibility to bayluscide and copper sulfate [chemical molluscicides], Anagallis arvensis and Calendula micrantha [plant molluscicides] as well as to Schistosoma mansoni infection. Form 2 as juvenile and adult was less sensitive to C. Micrantha and A. arvensis. Form 3 as juvenile and form 1 as adult were least sensitive to CuSO4. Approximately, the same susceptibility to bayluscide was observed in the three forms, either as juvenile or adult. The sublethal concentrations of the molluscicides on the three forms of B. glabrata showed no significant difference in the growth or survival rate in-between. Form 2 was significantly higher in the egg-laying capacity. The total protein concentration was not affected, except in certain cases, where the increase was primarily due to the increase in the globulin concentrations which was observed with the marked increase observed in the urea concentration and the marked increase or inhibition in the activity of either aspartate aminotransferase [AST] or alanine aminotransferase [ALT]. The digestive gland of the three forms of B. glabrata showed a low susceptibility to infection with the local strain of S. mansoni

Erthrocyte adhesion markers [CD36] in pediatric sickle cell anemia: relation to clinical syndrome, HbF and hydroxyurea therapy

To investigate the possible role of erythrocyte adhesion marker [CD36] in modulating adhesion of sickle erythrocytes to vascular endothelium, 28 children with homozygous sickle cell anemia [SS disease] were studied using this physiologically crucial period to evaluate the relationships between a major erythrocyte adhesion marker [CD36] and HbF. CD36+ erythrocytes were assessed using the flow cytometry and expressed as% of positive cells. The mean level of CD36+ erythrocytes was 1.67% +/- 0.55% with an inverse relationship between CD36 positivity and HbF. In univariate analysis, significant correlations with various hematologic parameters and CD36 positivity were noted. Hydroxyurea therapy lowered CD36 positivity even before the peak level of HbF, it also improved all hematologic parameters. There was a strong positive correlation between CD36 positivity and the increased duration of HU therapy; this could be a from of tolerance to the drug over-time. Patients with painful crisis had lower% of CD36+ erythrocytes than stable patients but still statistically significantly higher than the controls. CD36% was strongly positively correlated to the reticulocyte count, being two faces of the same coin, implicated in the process of vasoocclusion. More therapeutic modalities are needed that tackle more effectively the primepathogenetic mechanisms of vasoocclusion; namely, adhesion molecules

Influence of some natural and synthetic substances on certain fresh water organsisms and the snail vectors of Schistosomiasis and Fascioliasis

The effect of plants Anagallis arvensis, Calendula micrantha and Ambrosia maritima and the synthetic chemical molluscicides bayluscide and copper sulphate on survivorship, egg production of the snail vectors of schistosomiasis [Biomphalaria alexandrina] and fascioliasis [Lymnaea natalensis] and on some fresh water organisms were studied. Anagallis arvensis and Calendula micrantha showed good molluscicidal action against B. alexandrina and L. natalensis where LC90 values were 88 and 93 ppm, respectively, for A. arvensis and 135 and 100 ppm, respectively, for Calendula micrantha. The cumulative mortality of B. alexandrina [70%] was considerably high after 4 weeks of continuous exposure to A. arvensis. Complete inhibition of egg production was obtained for B. alexandrina after 2 weeks of exposure to low concentration of C. micrantha, bayluscide and copper sulphate. A. arvensis increased the maximum standing crops of algal biomass of Sirogyra [1.1358 g] and daily specific growth rate [0.0586 g.], while the control was 1.0106 g. and 0.0503 g., respectively. A low toxic effect on Daphnia pula was obtained under the effect of Anagul1is arvensis [5% mortality] and calendula micrantha [25% mortality] compared with synthetic molluscicides suggesting the use of the tested plants as molluscicides

Effect of copper sulphate, certain plants and adjuvants on the snails Biomphalaria alexandrina and Lymnae natalensis and on the zooplankton [Daphnia pulex]

The snails Biomphalaria alexandrina and Lymnaea natalensis were exposed to 1/10 LC50 of copper sulphate or of the plants Anagallis arvensis, Calendula micrantha and Ambrosia maritima. The snails were exposed firstly to copper sulphate then to each of the tested plants and vice-versa. The results showed that the pre-exposure of snails to A. arvensis and C. micrantha plants increased the molluscicidal action of copper sulphate against B. alexandrina and L. natalensis where it caused an additive effect. The pre-exposure to A. maritima caused different effects with copper sulphate, where it showed antagonistic effect on B. alexandrina and additive effect on L. natalensis snails. The pre-exposure of snails to copper sulphate increased the molluscicidal action of the tested plants against B. alexandrina and L. natalensis where it caused synergistic effect in case of Anagallis arvensis and Calendula micrantha against L. natalensis and additive effect in the rest of the treatments. Mixing of copper sulphate with each of the tested plants at different ratios caused antagonism in the molluscicidal activity of copper sulphate against B. alexandrina and L. natalensis snails. The addition of each of the following adjuvants; mono-ethylene glycol mono-oleate, mono-ethylene glycol di-oleate, potassium di-hydrogen phosphate and KZ mineral oil to copper sulphate increased the molluscicidal activity of copper sulphate against B. alexandrina, where it caused synergistic effect. In case of L. natalensis, mono-ethylene glycol mono-oleate and mono-ethylene glycol di-oleate caused an additive effect; while, potassium di-hydrogen phosphate and KZ mineral oil induced antagonistic effect. The result of examination of the toxic effect of copper sulphate in combination with each of the tested adjuvant against Daphnia pulex indicated that the treatment of copper sulphate and mono-ethylene glycol di-oleate increases the molluscicidal activity of copper sulphate and at the same time reduces its toxic effect against non-target organisms [Daphnia] and is the best for application

Impact of desiccation on biology of Biomphalaria alexandrina and Bulinus truncatus snails

Biomphalaria alexandrina and Bulinus truncates snails were exposed to either complete or partial desiccation. Complete desiccation was carried out in dried plastic jars, while in partial one, the snails were exposed on filter paper saturated with dechlorinated and chlorinated water. Desiccation periods were 1 or 3 days, followed by recovery [1, 4, 6 and 8 days]. This technique was continued throughout 6 weeks for B. truncates and 18 weeks for B. alexandrina. Also, the hatchability of eggs laid by desiccated B. alexandrina eggs was evaluated. All treatments of both partial and complete desiccation decreased the survival and net reproductive rates of B. alexandrina and B. truncates snails. The net reproductive rates for snails partially desiccated for 24hr, followed by 6 days of recovery were reduced by 72.3% and 57.9% for B. alexandrina and B. truncates, respectively. Moreover, elongation of partial desiccation to 3 days, followed by 4 days of recovery highly suppressed this parameter for B. truncates to be 1.68 compared to 13.29 for control groups as well the life span of desiccated snails was shortened. In addition, B. truncates could not survive after 3 days of complete desiccation followed by 4 days of recovery, while only 7% of B. alexandrina survived at the 6th week of the test. Data also indicated that hatchability of B. alexandrina eggs obtained from snails exposed to both types of desiccation was not approximately affected, but the hatchability period was elongated in some treatments

Molluscicidal activities of certain pesticide and their mixtures against Biomphalaria alexandrina

In this study, Biomphalaria alexandrina snails were collected from irrigation canals at Giza Governorate and maintained on fresh lettuce leaves under suitable laboratory conditions. Niclosamide and uccmaluscide proved to be the most effective compounds, followed by copper sulfate. This was followed by anilofos, isoprothiolane and fluazifop-P-butyl. Moreover, butachlor herbicide was the least potent compound. In general, the specific molluscicides showed more efficiency than the conventional tested herbicides and fungicides on the treated snails. Pre-exposure to 1/10 LC50 of anilofos, butachlor and isoprothiolane showed synergistic effects to uccmaluscide. However, the same treatment with 1/10 LC50 of fluazifop-P-butyl, isoprothiolane and butachlor gave an additive effect to copper sulfate and niclosamide on the treated snails. Data indicated that when butachlor, anilofos, fluazifop-P-butyl or isoprothiolane added to copper sulfate at ratios of 10:40 and 20:30 of LC50 as well as anilofos when added to copper sulfate at 30:20 showed synergism in activity against snails. On the contrary, the tested mixtures with niclosamide resulted in an antagonistic action, while they showed synergistic effect. Isoprothiolane-uccmaluscide mixture at a ratio of 40:10 of LC50 showed an additive effect on the snails. The determination of niclosamide by gas chromatography indicated that niclosamide showed relatively slower degradation either in case of niclosamide or its mixture with butachlor. Meanwhile, its mixture with anilofos or fluazifop-p-butyl or isoprothiolane showed a rapid degradation

molluscicidal efficacy of three products against Biomphalaria alexandrina and Lymnaea natalensis

The toxicity of three local formulated products [Sol EC [mineral oil], Sisi-6 [surfactant] and castor bean oil EC [plant oil]] was tested against Biomphalaria alexandrina and Lymnaea natalensis in two water sources. The results indicated that in dechlorinated water after 24-hour exposure, castor bean oil was the most toxic product against the snails, followed by Sisi-6 and Sol [EC] with LC90 of 250 ppm and 8 ppm against B. alexandrina and L. natalensis, respectively. When Nile water was used after 6-hour exposure, a high concentration of castor bean oil [4 LC90] did not cause 100% mortality of the snails; it was achieved by 2 LC90 of Sisi-6 with Nile water. On the other hand, castor bean oil was more fatal to eggs of the snails [LC90 = 660 ppm] than the other two products. In general, L. natalensis was more susceptible to the experimental products than B. alexandrina

Ocular changes in insulin-dependent diabetic patients: risk factors

This work aimed at finding out the frequency of different ocular changes in insulin dependent diabetic patients and the relation - if any- between the present abnormalities and some of the suggested risk factors. The study was carried out on 40 insulin dependent diabetic patients ranging in age between 6.5 and 2 4 years and 10- age and sex- matched non-diabetic persons taken as control. Fifty percent of the studied eyes of diabetic patients had at least one abnormality. The presence of non-leaking microaneurysms was the most frequently observed one [52.5%], followed by conjunctival microvascular abnormalities [25%], then premature detachment of vitreous [22.5%] and leaking microaneurysms [22.5%]. Ocular changes were significantly more frequent among older diabetic patients [>/= 15 years of age], diabetics with longer duration of the disease [>4 years], and those with uncontrolled diabetic state [HbA1c >/= 8.75%]. Diabetic children less than 15 years of age who developed ocular abnormalities had significantly higher serum levels of triglyceride [TG] and very low density lipoproteins [VLDL] than those with no ocular changes. Diabetic patients aged more than 15 years, with ocular abnormalities, had significantly higher glycosylated hemoglobin [HbA[1c]] concentrations and longer duration of diabetes mellitus. It was concluded that the long-term glycemic control and the duration of diabetes mellitus were the major risk factors for the development of ocular changes among diabetics

Anatomical study of the caprine mammary gland and its correspondence to ultrasonographic findings

The present work aimed to provide a guide for the anatomical and systemic evaluation of caprine mammary gland by radiographical and ultrasound mammography which may be a useful technique in the assessment of the anatomical morphology [teat, gland cistern, the duct system, glandular parenchyma and suspensory ligaments]. For this purpose a sum of twenty udder were dissected and six alive goats in different age of lactation were examined by brightness mode [B. mode] ultrasonography with 5 MHZ [sector] and 6 MHZ [Linear] transducer. The dimensions of another 30 teats were also given. The caprine mammary gland acquired a globular pendulous glandular body. From the middle of the base of each body a peg-like teat was erected. By the use of a magnifying lens the teat showed three different layers, an external, middle and an internal one. These layers appeared sonographically as two hyperechoic bands separated by a central hypoechoic one. The cavity system of the mammary gland could be distinguished into a teat canal and lactiferous sinus. The latter comprises a Pars papillaris and Pars glandularis. In addition the glandular portion of the gland depends on the stage of lactation. This could be necessary for further understanding of some surgical and pathological problems that may be beneficial for further studies