Synthesis and broad-spectrum antiproliferative activity of diarylamides and diarylureas possessing 1,3,4-oxadiazole derivatives

Gamal El-Din, M.M.,El-Gamal, M.I.,Abdel-Maksoud, M.S.,Yoo, K.H.,Oh, C.H. Pergamon Press 2015 Bioorganic & medicinal chemistry letters Vol.25 No.8

A series of diarylamides and diarylureas possessing 1,3,4-oxadiazole scaffold was designed and synthesized. Their in vitro antiproliferative activities were tested against a panel of 58 cell lines of nine different cancer types at the NCI, and compared with Sorafenib as a reference compound. Most of the compounds showed strong and broad-spectrum antiproliferative activities. The diarylurea compound 2g possessing 4-chloro-3-(trifluoromethyl)phenyl terminal moiety showed the highest mean % inhibition value of about 100% over the 58-cell line panel at 10μM concentration. Also compounds 2h, 2l, 2m exhibited mean % inhibition over 90% at 10μM concentration. The IC<SUB>50</SUB> value of compound 2b over SNB-75 CNS cancer cell line was 0.65μM. Compound 2h also exerted submicromolar IC<SUB>50</SUB> values of 0.67, 0.80, and 0.87μM against PC-3 prostate cancer cell line, HCT-116 colon cancer cell line, and ACHN renal cancer cell line, respectively. Compound 2h showed comparable efficacy to Sorafenib.

이슬람에서 본 인간자원에 관한 사상과 실제

가말알카진다르 한국이슬람학회 1990 한국이슬람학회논총 Vol.1 No.1

Does anaesthesia in mothers during delivery affect bilirubin levels in their neonates?

El-Kabbany, Zeinab A,Toaima, Nadin N,Toaima, Tamer N,EL-Din, Mona Y Gamal The Korean Pediatric Society 2017 Clinical and Experimental Pediatrics (CEP) Vol.60 No.12

Purpose: This study aimed to assess whether different anesthetic techniques and oxytocin use applied during delivery affect transcutaneous bilirubin levels during the first 24 hours in neonates. Methods: A total of 1,044 neonates delivered by either caesarian section (C/S) or normal vaginal delivery (NVD) were included in the study. They were classified into 5 groups as follows: group 1: born by C/S using general anesthesia, group 2: C/S using spinal anaesthesia, group 3: C/S using general anesthesia after failed spinal block, group 4: by NVD without anesthesia, and group 5: oxytocin-induced vaginal delivery without anesthesia. Transcutaneous total bilirubin levels (TBLs) were measured during the first 24 hours and on the fifth and eighth days of life and the levels in different groups were compared. Results: The TBLs were significantly higher in neonates delivered by C/S using general anesthesia rather than spinal anesthesia (P<0.001), and both groups had higher levels than those born by NVD without anesthesia ($P{\leq}0.001$). However, the group receiving general anesthesia after failed spinal block was found to have the highest bilirubin level. Moreover, TBLs were significantly higher with the use of oxytocin ($P{\leq}0.001$). Conclusions: C/S and general anesthesia adversely affect the bilirubin levels in neonates, and the use of oxytocin during vaginal delivery also increases TBLs in neonates.

Does anaesthesia in mothers during delivery affect bilirubin levels in their neonates?

Zeinab A El-Kabbany,Nadin N Toaima,Tamer N Toaima,Mona Y Gamal EL-Din 대한소아청소년과학회 2017 Clinical and Experimental Pediatrics (CEP) Vol.60 No.12

Purpose: This study aimed to assess whether different anesthetic techniques and oxytocin use applied during delivery affect transcutaneous bilirubin levels during the first 24 hours in neonates. Methods: A total of 1,044 neonates delivered by either caesarian section (C/S) or normal vaginal delivery (NVD) were included in the study. They were classified into 5 groups as follows: group 1: born by C/S using general anesthesia, group 2: C/S using spinal anaesthesia, group 3: C/S using general anesthesia after failed spinal block, group 4: by NVD without anesthesia, and group 5: oxytocin-induced vaginal delivery without anesthesia. Transcutaneous total bilirubin levels (TBLs) were measured during the first 24 hours and on the fifth and eighth days of life and the levels in different groups were compared. Results: The TBLs were significantly higher in neonates delivered by C/S using general anesthesia rather than spinal anesthesia (P<0.001), and both groups had higher levels than those born by NVD without anesthesia (P≤0.001). However, the group receiving general anesthesia after failed spinal block was found to have the highest bilirubin level. Moreover, TBLs were significantly higher with the use of oxytocin (P≤0.001). Conclusions: C/S and general anesthesia adversely affect the bilirubin levels in neonates, and the use of oxytocin during vaginal delivery also increases TBLs in neonates.

Nω-Nitro-L-Arginine Methylester Ameliorates Myocardial Toxicity Induced by Doxorubicin

( Mahmoud Ahmed Mansour ),( Ayman Gamal El Din ),( Mahmoud N. Nagi ),( Othman A. Al Shabanah ),( Abdullah M. Al Bekairi ) 생화학분자생물학회 2003 BMB Reports Vol.36 No.6

The effects of No-nitro-L-arginine methylester (L-NAME) and L-arginine on cardiotoxicity that is induced by doxorubicin (Dox) were investigated. A single dose of Dox 15mgkg i.p. induced cardiotoxicity, manifested biochemically by a significant elevation of serum creatine phosphokinase (CPK) activity [EC 2.7,3.2]. Moreover, cardiotoxicity was further confirmed by a significant increase in lipid peroxides, measured as malon-di-aldehyde (MDA) in cardiac tissue homogenates. The administration of L-NAME 4 mg/kg/d p.o. in drinking water 5 days before and 3 days after the Dox injection significantly ameliorated the cardiotoxic effects of Dox, judged by the improvement in both serum CPK activity and lipid peroxides in the cardiac tissue homogenates. On the other hand, the administration of L-arginine 70mg/kg/d p.o. did not protect the cardiac tissues against the toxicity that was induced by the Dox treatment. The findings of this study suggest that L-NAME can attenuate the cardiac dysfunction that is produced by the Dox treatment via the mechanism(s), which may involve the inhibition of the nitric oxide (NO) formation. L-NAME may, therefore, be a beneficial remedy for cardiotoxicity that is induced by Dox and can then be used to improve the therapeutic index of Dox.

Nω-Nitro-L-Arginine Methylester Ameliorates Myocardial Toxicity Induced by Doxorubicin

Mansour, Mahmoud Ahmed,El-Din, Ayman Gamal,Nagi, Mahmoud N.,Al-Shabanah, Othman A.,Al-Bekairi, Abdullah M. Korean Society for Biochemistry and Molecular Biol 2003 Journal of biochemistry and molecular biology Vol.36 No.6

The effects of $N{\omega}$-nitro-L-arginine methylester (L-NAME) and L-arginine on cardiotoxicity that is induced by doxorubicin (Dox) were investigated. A single dose of Dox 15 mg/kg i.p. induced cardiotoxicity, manifested biochemically by a significant elevation of serum creatine phosphokinase (CPK) activity [EC 2.7.3.2]. Moreover, cardiotoxicity was further confirmed by a significant increase in lipid peroxides, measured as malon-di-aldehyde (MDA) in cardiac tissue homogenates. The administration of L-NAME 4 mg/kg/d p.o. in drinking water 5 days before and 3 days after the Dox injection significantly ameliorated the cardiotoxic effects of Dox, judged by the improvement in both serum CPK activity and lipid peroxides in the cardiac tissue homogenates. On the other hand, the administration of L-arginine 70 mg/kg/d p.o. did not protect the cardiac tissues against the toxicity that was induced by the Dox treatment. The findings of this study suggest that L-NAME can attenuate the cardiac dysfunction that is produced by the Dox treatment via the mechanism(s), which may involve the inhibition of the nitric oxide (NO) formation. L-NAME may, therefore, be a beneficial remedy for cardiotoxicity that is induced by Dox and can then be used to improve the therapeutic index of Dox.

Desalination of Basal Water by Mesoporous Carbons Nanocomposite Membrane

Choi, Jeongdong,Ahn, Youngho,El-Din, Mohamed Gamal,Kim, Eun-Sik American Scientific Publishers 2016 Journal of Nanoscience and Nanotechnology Vol.16 No.2

<P>The hydro-transportation process used to obtain bitumen from the Alberta oil sands produces large volume of basal depressurization water (BDW), which contains high salt concentrations. In this research, thin-film nanocomposite (TFN) membrane technology applied to treat BDW in lab-scale, and evaluated water properties before and after the treatment. The average rejection ratios of ionic species were 95.2% and 92.8% by TFN membrane (with ordered mesoporous carbons (OMCs)) and thin-film composite (TFC) (without OMCs) membrane, respectively. The turbidity and total dissolved solids (TDS) were completely rejected in all treatment conditions. Interestingly, the water flux of TFN membrane was dramatically increased compared to TFC membrane. The increase of water flux was believed to be caused by the increased membrane surface hydrophilicity and nano-pore effects by the OMCs.</P>

MDM2 Expression in Serous and Mucinous Epithelial Tumours of the Ovary

Abdelaal, Shereen E,Habib, Fahima M,el Din, Amina A Gamal,Gabal, Samia M,Hassan, Nabila S,Ibrahim, Nihad A Asian Pacific Journal of Cancer Prevention 2016 Asian Pacific journal of cancer prevention Vol.17 No.7

Background: Different types of cancer exhibit abnormalities in cell cycle regulators. The murine double minute-2(MDM2) cell cycle regulator is a proto-oncogene that negatively regulates the P53 tumour suppressor gene. Surface epithelial tumours constitute approximately two thirds of ovarian neoplasms. Each histologic type can be classified as benign, borderline and malignant. This study aimed to examine immunohistochemical expression of the MDM2 protein in ovarian serous and mucinous epithelial tumours (benign, borderline and malignant). Materials and Methods: This study included forty five ovarian tumours, subdivided into fifteen cystadenomas (5 serous and 10 mucinous), fifteen borderline tumours (11 serous and 4 mucinous) and fifteen cystadenocarcinomas (9 serous and 6 mucinous). Paraffin sections were stained with haematoxylin and eosin for histopathologic study, and with mouse monoclonal anti-MDM2 antibody for immunohistochemistry. Results: MDM2 positivity was detected in 28.9% of the studied ovarian tumours. All benign tumours were negative and positivity was significantly higher in malignant than borderline tumours (P value of chi-square test =0.000). Significantly, all MDM2 positive mucinous tumours were malignant with no positive mucinous borderline tumours. Malignant tumours showed positive MDM2 expression in 83.3% of mucinous type and in 55.6% of serous type. Borderline serous tumours showed negative MDM2 in 72.7% of cases (P value of Z test =0.04). Conclusions: Alterations in the expression of the cell cycle regulator (MDM2) occur early in the process of tumourigenesis in serous and mucinous ovarian tumours. We suggest that MDM2 may be used in those tumours as a marker for risk stratification and identification of cases with cancer development and progression. We recommend further studies on MDM2 immunohistochemistry, in conjunction with adjuvant methods as DNA ploidy and FISH gene amplification, focusing on the mucinous tumours and differentiating between the three tumour categories, benign, borderline and malignant.

Biochemically Altered Human Erythrocytes as a Carrier for Targeted Delivery of Primaquine: an In Vitro Study

Fars K. Alanazi,Ibrahim A. Alsarra,Gamal El-Din I. Harisa,Ahmad Maqboul,Magdi Abdel-Hamid,Steven H. Neau 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.4

The aim of this study was to investigate human erythrocytes as a carrier for targeted drug delivery of primaquine (PQ). The process of PQ loading in human erythrocytes, as well as the effect of PQ loading on the oxidative status of erythrocytes, was also studied. At PQ concentrations of 2, 4, 6, and 8 mg/mL and an incubation time of 2 h, the ratios of the concentrations of PQ entrapped in erythrocytes to that in the incubation medium were 0.515, 0.688, 0.697 and 0.788, respectively. The maximal decline of erythrocyte reduced glutathione content was observed at 8 mg/mL of PQ compared with native erythrocytes p < 0.001. In contrast, malondialdehyde and protein carbonyl were significantly increased in cells loaded with PQ (p < 0.001). Furthermore, osmotic fragility of PQ carrier erythrocytes was increased in comparison with unloaded cells. Electron microscopy revealed spherocyte formation with PQ carrier erythrocytes. PQ-loaded cells showed sustained drug release over a 48 h period. Erythrocytes were loaded with PQ successfully, but there were some biochemical as well as physiological changes that resulted from the effect of PQ on the oxidative status of drugloaded erythrocytes. These changes may result in favorable targeting of PQ-loaded cells to reticulo-endothelial organs. The relative impact of these changes remains to be explored in ongoing animal studies.

바이오차의 원료, 온도, 스팀 활성화가 바이오차 성질과 납 흡착능에 미치는 영향

곽진협,( Md Shahinoor Islam ),( Siyuan Wang ),( Selamawit Ashagre Messele ),( M. Anne Naeth ),( Mohamed Gamal El-din ),( Scott X. Chang ) 한국농공학회 2019 한국농공학회 학술대회초록집 Vol.2019 No.-

바이오차(biochar)는 폐수 내 중금속 및 유기 오염물질을 제거할 수 있는 물질로 각광을 받고 있다. 하지만 바이오차 생성 조건에 따른 성질 변화와 그에 따른 폐수 내 중금속 제거능에 대한 연구는 미비하였다. 본 연구는 바이오차의 원료, 열분해 온도, 그리고 스팀 활성화가 바이오차의 물리적, 화학적 성질과 납 흡착능에 미치는 영향을 알아보기 위해 수행하였다. 톱밥, 카놀라 짚, 밀짚, 그리고 축산 분뇨 펠렛을 이용하여 300, 500, 700 ℃에서 스팀 활성화가 있거나 없는 조건에서 바이오차를 제조하였다. 열분해 온도가 증가함에 따라 바이오차 pH, 표면적, 그리고 탄소 함량이 증가하였으며, 산소 및 수소 함량 그리고 작용기가 감소하였다. 스팀 활성화는 바이오차의 표면적은 증가시켰지만 다른 성질에는 영향을 미치지 않았다. 스팀 활성화를 시키지 않은 바이오차 중 카놀라와 밀짚을 700 ℃에서 생성하였을 때 납 흡착능이 최대였다. 또한 열분해 온도가 증가함에 따라 납 흡착능이 증가하였는데, 이는 바이오차 pH, 에쉬함량 및 표면적이 증가하면서 침전, 이온 교환, 내권복합화가 증가하였기 때문으로 판단된다. 스팀 활성화에 의해 납 흡착능이 증가하였는데, 이는 바이오차의 표면적이 증가하였기 때문이다. 납 흡착은 2차 동역학 모델을 따랐다. 연구 결과 폐수 정화를 위해 지역 농업과 임업에서 발생하는 부산물을 이용하여 바이오차를 제조할 수 있으며 생성 조건에 따라 최적의 바이오차를 생성할 수 있을 것으로 판단된다.