Preservation of human spermatozoa in a simple medium

AbstractThe objective of this study was to estimate the best conditions for sperm preservation in a simple medium and to examine the changes in sperm morphology and vitality due to preservation.Swim-up technique was carried out using KSOMaa medium (potassium simplex optimized medium with amino acid) then, such sperms were preserved without/with supplementation of BSA to the medium in two different osmolarities (271 and 800mOsmal). Sperms were preserved for 2weeks in three different temperatures (37°C, 4°C and −20°C). Our results demonstrated that: (1) KSOMaa medium is a good medium to obtain progressive motile sperms with a good morphology. (2) The best conditions for preserving human spermatozoa were 800mOsmol KSOM-BSA and a holding temperature of −20°C. (3) Light and electron microscopy showed that cryodamage has been induced in some human spermatozoa due to preservation. Collectively, our data indicate that this new simple procedure could be the method of choice for selecting motile and morphologically normal spermatozoa. This new preservation method may help in vitro fertilization centers but should be tested to check the embryonic development after intracytoplasmic sperm injection

INTRANASAL MICROEMULGEL AS SURROGATE CARRIER TO ENHANCE LOW ORAL BIOAVAILABILITY OF SULPIRIDE

Objective: The purpose of this study is to evaluate microemulsion based gel (MBG) of sulpiride "a poorly water soluble antipsychotic with low oral bioavailability."Methods: Gelling polymers such as sodium carboxymethylcellulose (CMC-Na), hydroxyl propyl methyl cellulose (HPMC K4m), carbopol 940 and Na alginate were evaluated for their potential to gel sulpiride microemulsions (MEs) without affecting the MEs structure. Also, sulpiride solution (SS) and conventional gel (without ME) were prepared and compared with MBG. Gel formulations were checked for their viscosity, pH, spreadability (S), mucoadhesive force (MF), and nasal ciliotoxicity studies. The in vitro release of sulpiride across a cellophane membrane and its permeation through the nasal mucosa in phosphate buffered saline pH 6.8 (PBS) were also performed. In addition, a pharmacodynamic study of optimized formulae compared to SS and microemulsion (ME) was evaluated in rats.Results: CMC-Na and HPMC K4m were not able to gel sulpiride loaded MEs while Na alginate gave an unclear gel with a sticky texture. Results revealed that the viscosity, mucoadhesion force, and spreadability of the MBG increased with increasing carbopol 940 concentrations. The flux was arranged as the following, MBG>conventional gel>sulpiride solution (SS). According to histopathological study, safe and non-irritant MBGs suitable for nasal administration were successfully prepared. Finally, the pharmacodynamic study indicated that intranasal sulpiride MBG had a significant effect (*P<0.001) than SS and ME administered either intravenous or intranasal.Conclusion: MBG provides signiï¬cant enhancement in nasal bioavailability not only by absorption enhancing effect of ME but also, by increasing nasal residence tim

Exocyclic enaminones as building blocks for synthesis of bioactive polyheterocyclic compounds

The reaction of exocyclic enaminones namely, 2-(dimethylaminomethylene)-3,4-dihydro-2H-naphthalen-1-one,  3-(dimethylaminomethylene)-thiochroman-4-one and 2-(dimethyl-aminomethylene)-indane-1,3-dione, each with heterocyclic diazonium salts afforded the respective hydrazones which undergo either in situ dehydrative cyclization or cyclized by heating with acetic acid to give polycyclic compounds. The structure of all the newly synthesized products were confirmed by elemental and spectral (IR, IH NMR, Mass) data. Also, the biological activity of some of the prepared compounds was tested against some microorganisms and promising results were obtained

Azo-Hydrazone Tautomerism and Antimicrobial activity of New substituted Imidazolines and Perimidines

Two new series of 2-{1-[(substitutedphenyl)-hydrazono]-2-oxo-2-phenyl-ethyl}-5,5-diphenyl-3,5-dihydro-imidazol-4-one  and  (1H-Perimidin-2-yl)-[(substitutedphenyl)-hydrazono]-acetic acid ethyl ester were prepared by coupling the diazonium salt of aniline and its derivatives with 2-(2-oxo-2-phenyl-ethylidene)-5,5-diphenyl-imidazolidin-4-one or ethyl 3-dimethylamino-2-(1H-perimidin-2-yl)-propenoate in ethanolic sodium hydroxide solution. The structures of all the newly synthesized compounds were confirmed by spectral (IR, 1H NMR, mass) spectra , and X-ray crystallographic and elemental analyses. Also, the azo-hydrazone tautomerism of these compounds was discussed. In addition, all the newly synthesized compounds were screened for their antibacterial and antifungal activity and the results obtained indicated that some of these compounds exhibited excellent activity

Low cost options of carbon sources, gelling agents and supporting materials used for micropropagation of shoot tips of banana cultivar Grand Nain

The high cost of materials used for media preparation is chiefly constituted by gelling agents and sucrose. The objective of this study was to develop efficient micropropagation techniques for the newly released banana cultivar Grand Nain at a low cost by testing different alternatives of carbon sources (sucrose),gelling agents and supporting materials. Three experiments were conducted to test different carbon sources, gelling agents and support matrices.  In the first experiment, different carbon sources were tested. These included the refined imported sugar special for tissue culture from Sigma Company, Kenana (refined local sugar), Alguneid (brown local sugar) and beet crystal imported sugar from the local market. Results showed that all sources of sucrose resulted in the highest number of explants with shoots, however, Alguneid sugar induced significantly higher number of shoots per explants. There was 99.4% reduction in the medium cost compared to the standard medium of Sigma sugar. The second experiment was conducted to test different gelling agents such as corn starch at 50.0g/l plus agar at 3.0 and 4.0 g/l, corn starch at 50.0g/l plus phytagel at 1.25 and 1.5 g/l, respectively. Phytagel at 2.5 g/l and agar at 9 g/l were used as control. Gelling agents did not differ in the percentage of explants with shoots. However, corn starch at 50.0g/l and phytagel at 1.5 g/l resulted in the highest number of shoots which reduced the medium cost by 30.7%. In the third experiment, different supporting materials were used as low cost options including stone matrices, glass beads, cotton fiber and filter paper. Rock stones were the best supporting material in liquid medium for propagation of banana cv. Grand Nain. It resulted in significantly higher percentage of explants with shoots, number of shoots per explant and plant height.   ارتفاع كلفة الزراعة النسيجية النباتية هو السبب في عدم تطبيقها علي نطاق واسع. إن تكلفة المواد الجيلاتينية (الآجار والفايتاجل) والسكر تمثل أكبر تكلفة بين العناصر المكونة للوسط الغذائي. الهدف من هذه الدراسة هو تطوير خيارات اقتصادية لتقنية زراعة الأنسجة للإكثار الدقيق للموز الصنف قراند نين المجاز حديثاً وذلك باختبار بدائل للسكر والمواد الجلاتينية وايجاد مواد داعمة للزراعات النسيجية في الأوساط الغذائية السائلة. أجريت الاختبارات في هذه الدراسة بإستخدام النظام العشوائي الكامل في خمس مكررات وأربع قمم نامية في كل مكرر. تم تنفيذ ثلاث تجارب بهدف خفض تكلفة الاكثار الدقيق للموز الصنف قراندنين. فى التجربة الأولى تم اختبار أربعة مصادر الكربون وهى: سيقما (سكر نقى مستورد خاص بزراعة الأنسجة من شركة سيقما), كنانة (سكر نقى منتج محلياً من شركة سكر كنانة), الجنيد   ( سكر بنى منتج محلياً من مصنع الجنيد) والبنجر( سكر بلورى مستورد). لا توجد فروقات معنوية بين أنواع السكر التي تم اختبارها في النسبة المئوية للقمم النامية للموز التي تم تحفيز نموات جديدة منها وعدد النموات الجديدة (السيقان)، لكن عدد السيقان النامية من كل قمة نامية علي سكر الجنيد أعلي معنويا من أنواع السكر الأخرى. باستخدام هذه البدائل تم تخفيض 99.4% من تكلفة السكر في الوسط الغذائي. أجريت التجربة الثانية لاختبار مواد جلاتينية مختلفة وهى: 50.0 جرام/لتر من نشا الذرة الشامية مع3.0  جرام/لتر و4.0 جرام/لتر اجار,50.0 جرام/لتر من النشأ مع1.25  جرام/لتر و1.5 جرام/لتر فايتاجل, 2.5 جرام/لتر فايتاجل و9 جرام/لتر اجار كشواهد. أوضحت النتائج أن الاحلال الجزئي للمواد الجلاتينية (الفايتاجل والاجار) بمقدار 50.0 جرام/لتر من نشا الذرة الشامية يمكن استخدامه للإكثار الدقيق للموز صنف قراندنين، حيث لا توجد فروقات معنوية بين كل المعاملات في النسبة المئوية لأجزاء الموز التي تم تحفيز نموات جديدة منها وعدد السيقان مع تخفيض 40.7-30.7 %و65.8-54.7 % في كلفة الآجار والفايتاجل علي التوالي. فى التجربة الثالثة تمت زراعة القمم النامية فى وسط غذائي سائل باستخدام دعامات مختلفة وهى: مصفوفات من الحصى, البلى, ألياف قطنية و أوراق الترشيح. أثبتت النتائج أن مصفوفات الحصى هى أفضل الدعامات المختبرة فى الوسط الغذائي السائل.   &nbsp

Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFR\u3csup\u3eWT\u3c/sup\u3e and EGFR\u3csup\u3eT790M\u3c/sup\u3e

New 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their in vitro anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds 8, 10, 12a, and 12b showed potent anti-proliferative activities. Compound 12b was the most promising member with IC50 values of 8.21 and 19.56 µM against A549 and HCT-116, respectively. Compounds 8, 10, 12a, and 12b were evaluated for their kinase inhibitory activities against wild EGFR (EGFRWT). Compound 12b was the most potent member showing an IC50 value of 0.016 µM. In addition, compound 12b showed noticeable activity against mutant EGFR (EGFRT790M) (IC50 = 0.236 µM). Flow cytometric analyses revealed that compound 12b is a good apoptotic inducer and can arrest the cell cycle at S and G2/M phases. Furthermore, it produced an 8.8-fold increase in BAX/Bcl-2 ratio. Molecular docking studies were carried out against EGFRWT and EGFRT790M