首页 > 最新文献

Al-Azhar Journal of Pharmaceutical Sciences最新文献

英文 中文
REVIEW ON THE SIGNIFICANCE OF QUINAZOLINONE DERIVATIVES AS POTENT ANTIHYPERGLYCEMIC AGENTS 喹唑啉酮衍生物作为强效降糖药的意义综述
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223768
Helmy M. Sakr
Diabetes mellitus is a chronic metabolic disease which is characterized by high blood sugar levels over a prolonged period of time. Uncontrolled hyperglycemia can lead to serious damage to many vital organs in the body, including kidney damage, heart disease, and nerve damage. The goal of treatment of diabetes mellitus is reduction of blood glucose levels and controlling subsequent complications. Different mechanisms are involved in diabetes mellitus treatment. Quinazolinone and its derivatives have been found as effective and versatile pharmacophoric units in medicinal chemistry to design and develop a wide range of bioactive compounds. The present review summarizes the advances in lead compounds of quinazolinone hybrids and their related heterocycles in treatment of diabetes mellitus. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting the hypoglycemic effect.
糖尿病是一种以长期高血糖为特征的慢性代谢性疾病。不受控制的高血糖会导致身体许多重要器官的严重损害,包括肾脏损害、心脏病和神经损伤。糖尿病的治疗目标是降低血糖水平和控制并发症。糖尿病的治疗涉及多种机制。喹唑啉酮及其衍生物在药物化学中被发现是一种有效和通用的药效单位,可用于设计和开发广泛的生物活性化合物。本文综述了喹唑啉酮类杂环化合物及其相关杂环化合物在糖尿病治疗中的研究进展。此外,该综述还有助于加强药物开发过程,了解这些杂交药效特征在显示降糖作用中的潜在作用。
{"title":"REVIEW ON THE SIGNIFICANCE OF QUINAZOLINONE DERIVATIVES AS POTENT ANTIHYPERGLYCEMIC AGENTS","authors":"Helmy M. Sakr","doi":"10.21608/ajps.2022.223768","DOIUrl":"https://doi.org/10.21608/ajps.2022.223768","url":null,"abstract":"Diabetes mellitus is a chronic metabolic disease which is characterized by high blood sugar levels over a prolonged period of time. Uncontrolled hyperglycemia can lead to serious damage to many vital organs in the body, including kidney damage, heart disease, and nerve damage. The goal of treatment of diabetes mellitus is reduction of blood glucose levels and controlling subsequent complications. Different mechanisms are involved in diabetes mellitus treatment. Quinazolinone and its derivatives have been found as effective and versatile pharmacophoric units in medicinal chemistry to design and develop a wide range of bioactive compounds. The present review summarizes the advances in lead compounds of quinazolinone hybrids and their related heterocycles in treatment of diabetes mellitus. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting the hypoglycemic effect.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85650066","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
EVALUATION OF ANTIDIABETIC AND ANTI-OBESITY POTENTIAL AND SAFETY OF A POLYHERBAL REMEDY 一种复方中药的抗糖尿病和抗肥胖潜力及安全性评价
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223776
Amal H. Ahmed
Objective: To evaluate the antidiabetic and anti-obesity potentials and the safety of a polyherbal remedy. Method: A mixture of polyherbal remedy containing Gymnema sylvestre, Garcinia cambogia, Cleome droserifolia, and Nigella sativa (100 or 200 mg/Kg, p.o.) was subjected to qualitative chemical identification for marker compounds on individual plant extracts using Q-TOF-LC-MS. In addition, the antidiabetic and antiobesity potential were evaluated in streptozotocin-induced diabetic rats using metformin (100 mg/Kg, p.o.) and insulin (10 U/Kg, IP) as standards. The evaluation based on fasting blood glucose level (FBG), insulin level, and change in body weight gain of different treatment groups. Furthermore, the safety profile was assessed by the measurement of certain biochemical, hematological, and histopathological parameters. Results: A total of thirteen marker compounds, (Gymnemoside ND1, Myricetin, Hydroxycitric acid lactone, Garcinol, Garcimangosone D, 5,3`-Dihydroxy-3,6,7,4`,5`pentamethoxyflavone, 5-Hydroxy-3,6,7,3`,4`,5`-hexamethoxyflavone, Magnoflorine, Kaempferol glycoside, Sapindoside B, Alpha-hedrin, Tauroside H2, and Thymoquinone) were identified in the four plant extracts individually. The administration of polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated diabetic rats resulted in a significant decrease in the FBG by 62, 67, 44 and 73 % respectively, and significant increase in insulin level by 2161, 3433, 2400 and 5658 %, respectively, as compared to vehicle-treated control. Regarding the body weight change, polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated animals demonstrated a significant decrease by 45, 54, 72 and 65%, respectively, as compared to their initial weight. The results of polyherbal remedy (100 or 200 mg/Kg, p.o.)-treated groups showed a dose-independent potency between that obtained from insulinand metformin-treated groups. Concerning the safety profile; treatment with remedy extracts markedly improved the streptozotocin-induced alteration in the hepatic biochemical, and hematological indices (liver enzymes, total protein, albumin, TC, TG, HDL, LDL, RBCs count, WBCs count, Hb concentration and platelet count) besides preservation of the normal histopathological features of liver, kidney, and pancreas. Conclusion: The polyherbal remedy can be used as an effective and safe treatment of obesity, diabetes, and its complications.
目的:评价一种复方中药的抗糖尿病和抗肥胖作用及安全性。方法:采用Q-TOF-LC-MS方法,分别以100或200 mg/Kg (p.o)的复方金缕藤、藤黄、白花、黑草(Nigella sativa)为对照品,对各植物提取物的标记物进行定性化学鉴定。此外,以二甲双胍(100 mg/Kg, p.o)和胰岛素(10 U/Kg, IP)为标准,评价链脲佐菌素诱导的糖尿病大鼠的抗糖尿病和抗肥胖潜能。不同治疗组空腹血糖水平(FBG)、胰岛素水平及体重增加变化的评价。此外,通过测量某些生化、血液学和组织病理学参数来评估安全性。结果:从四种植物提取物中分别鉴定出13个标记化合物,分别为裸子皂苷ND1、杨梅素、羟基柠檬酸内酯、Garcinol、garcimangoone D、5,3 ' -二羟基3,6,7,4 ',5 ' -五甲基甲氧基黄酮、5-羟基3,6,7,3 ',4 ',5 ' -六甲基甲氧基黄酮、木兰碱、山奈酚糖苷、皂苷B、α -hedrin、牛皮苷H2和百里醌。多药提取物(100或200 mg/Kg, p.o)、二甲双胍和胰岛素治疗的糖尿病大鼠,与对照相比,空腹血糖分别显著降低62%、67%、44%和73%,胰岛素水平分别显著升高2161、3433、2400和5658 %。在体重变化方面,多药提取物(100或200 mg/Kg, p.o.)、二甲双胍和胰岛素治疗的动物与初始体重相比,分别显著减少了45%、54%、72%和65%。复方(100或200 mg/Kg, p.o.)处理组的效力与胰岛素组和二甲双胍处理组之间呈剂量无关。关于安全概况;药物提取物治疗显著改善了链脲佐菌素引起的肝脏生化和血液学指标(肝酶、总蛋白、白蛋白、TC、TG、HDL、LDL、红细胞计数、白细胞计数、Hb浓度和血小板计数)的改变,同时保持了肝脏、肾脏和胰腺的正常组织病理学特征。结论:复方中药可作为一种安全有效的治疗肥胖、糖尿病及其并发症的方法。
{"title":"EVALUATION OF ANTIDIABETIC AND ANTI-OBESITY POTENTIAL AND SAFETY OF A POLYHERBAL REMEDY","authors":"Amal H. Ahmed","doi":"10.21608/ajps.2022.223776","DOIUrl":"https://doi.org/10.21608/ajps.2022.223776","url":null,"abstract":"Objective: To evaluate the antidiabetic and anti-obesity potentials and the safety of a polyherbal remedy. Method: A mixture of polyherbal remedy containing Gymnema sylvestre, Garcinia cambogia, Cleome droserifolia, and Nigella sativa (100 or 200 mg/Kg, p.o.) was subjected to qualitative chemical identification for marker compounds on individual plant extracts using Q-TOF-LC-MS. In addition, the antidiabetic and antiobesity potential were evaluated in streptozotocin-induced diabetic rats using metformin (100 mg/Kg, p.o.) and insulin (10 U/Kg, IP) as standards. The evaluation based on fasting blood glucose level (FBG), insulin level, and change in body weight gain of different treatment groups. Furthermore, the safety profile was assessed by the measurement of certain biochemical, hematological, and histopathological parameters. Results: A total of thirteen marker compounds, (Gymnemoside ND1, Myricetin, Hydroxycitric acid lactone, Garcinol, Garcimangosone D, 5,3`-Dihydroxy-3,6,7,4`,5`pentamethoxyflavone, 5-Hydroxy-3,6,7,3`,4`,5`-hexamethoxyflavone, Magnoflorine, Kaempferol glycoside, Sapindoside B, Alpha-hedrin, Tauroside H2, and Thymoquinone) were identified in the four plant extracts individually. The administration of polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated diabetic rats resulted in a significant decrease in the FBG by 62, 67, 44 and 73 % respectively, and significant increase in insulin level by 2161, 3433, 2400 and 5658 %, respectively, as compared to vehicle-treated control. Regarding the body weight change, polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated animals demonstrated a significant decrease by 45, 54, 72 and 65%, respectively, as compared to their initial weight. The results of polyherbal remedy (100 or 200 mg/Kg, p.o.)-treated groups showed a dose-independent potency between that obtained from insulinand metformin-treated groups. Concerning the safety profile; treatment with remedy extracts markedly improved the streptozotocin-induced alteration in the hepatic biochemical, and hematological indices (liver enzymes, total protein, albumin, TC, TG, HDL, LDL, RBCs count, WBCs count, Hb concentration and platelet count) besides preservation of the normal histopathological features of liver, kidney, and pancreas. Conclusion: The polyherbal remedy can be used as an effective and safe treatment of obesity, diabetes, and its complications.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88039795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
PRODUCTION OF FATTY ACIDS BY YARROWIA LIPOLYTICA USING AGRO-INDUSTRIAL WASTE AT LOW TEMPERATURE 低温下利用农工废弃物生产脂肪酸的多脂耶氏菌
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223772
Mohamed Al-Hewaily
Single-cell oil has long been considered an alternative to conventional oil sources. The oil produced can also be used as a feedstock for biodiesel production. In this research, Morphological, microscopical, Biochemical tests and VITEK 2 YST ID card are used to identify most lipid screening yeast isolate named Y4. Many parameters (different Carbone sources, different nitrogen sources, PH, Incubation days, shaking, and statistic incubation) were studied using the optimization of one variable at time (OVAT). On YED agar media, the isolated yeast Yarrowia lipolyticaY4 gave the maximum biomass of 4.15±0.04 g/l, lipid yield of 0.86±0.03 g/l and lipid content of 20.67±0.62 %, respectively. Molasses was utilized as a carbon source and it was supporting both yeast growth and lipid production with two-fold increase biomass of 9.36±0.06 g/l, lipid yield of 1.80±0.18 g/l and lipid content of 19.31±1.81 %. Also, the oil profile by gas chromatography was contain 36.17%, 56.54% and 7.26% of saturated, monounsaturated and polyunsaturated fatty acids after 7 days’ incubation period at refrigerator and, contain 64.21%, 28.40%, and 7.33% of saturated, monounsaturated and polyunsaturated fatty acids after 30 days’ incubation at refrigerator. Consequently, this work study new insights for the economical oil production with valuable profile using cheap agro-industrial waste molasses as a substrate for growth of marine Yarrowia lipolyticaY4 yeast at low temperature 4°C for one week and one month.
单细胞油一直被认为是传统石油的替代品。所生产的油也可以用作生物柴油生产的原料。本研究采用形态学、显微、生化检测和VITEK 2 YST ID卡对大部分脂质筛选酵母分离物进行鉴定,命名为Y4。研究了多个参数(不同碳源、不同氮源、PH、孵育天数、摇摇和统计孵育),每次优化一个变量(OVAT)。在YED琼脂培养基上,分离得到的酵母解脂耶氏酵母(yrowia lipolyticaY4)最大生物量为4.15±0.04 g/l,脂质产量为0.86±0.03 g/l,脂质含量为20.67±0.62%。以糖蜜为碳源,同时支持酵母生长和脂质生产,生物量提高2倍(9.36±0.06 g/l),脂质产量提高1倍(1.80±0.18 g/l),脂质含量提高19.31±1.81%。经气相色谱分析,经7 d冷藏后的油剖面饱和、单不饱和和多不饱和脂肪酸含量分别为36.17%、56.54%和7.26%,经30 d冷藏后的油剖面饱和、单不饱和和多不饱和脂肪酸含量分别为64.21%、28.40%和7.33%。因此,本研究为利用廉价的农工废糖作为底物,在低温4℃条件下培养海洋耶氏酵母1周和1个月的经济产油提供了有价值的新见解。
{"title":"PRODUCTION OF FATTY ACIDS BY YARROWIA LIPOLYTICA USING AGRO-INDUSTRIAL WASTE AT LOW TEMPERATURE","authors":"Mohamed Al-Hewaily","doi":"10.21608/ajps.2022.223772","DOIUrl":"https://doi.org/10.21608/ajps.2022.223772","url":null,"abstract":"Single-cell oil has long been considered an alternative to conventional oil sources. The oil produced can also be used as a feedstock for biodiesel production. In this research, Morphological, microscopical, Biochemical tests and VITEK 2 YST ID card are used to identify most lipid screening yeast isolate named Y4. Many parameters (different Carbone sources, different nitrogen sources, PH, Incubation days, shaking, and statistic incubation) were studied using the optimization of one variable at time (OVAT). On YED agar media, the isolated yeast Yarrowia lipolyticaY4 gave the maximum biomass of 4.15±0.04 g/l, lipid yield of 0.86±0.03 g/l and lipid content of 20.67±0.62 %, respectively. Molasses was utilized as a carbon source and it was supporting both yeast growth and lipid production with two-fold increase biomass of 9.36±0.06 g/l, lipid yield of 1.80±0.18 g/l and lipid content of 19.31±1.81 %. Also, the oil profile by gas chromatography was contain 36.17%, 56.54% and 7.26% of saturated, monounsaturated and polyunsaturated fatty acids after 7 days’ incubation period at refrigerator and, contain 64.21%, 28.40%, and 7.33% of saturated, monounsaturated and polyunsaturated fatty acids after 30 days’ incubation at refrigerator. Consequently, this work study new insights for the economical oil production with valuable profile using cheap agro-industrial waste molasses as a substrate for growth of marine Yarrowia lipolyticaY4 yeast at low temperature 4°C for one week and one month.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87937444","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
ISOLATION AND CHARACTERIZATION OF CRUDE OIL-DEGRADING BACTERIA FROM PETROLEUM OIL CONTAMINATED EGYPTIAN SOILS 石油污染埃及土壤中原油降解细菌的分离与鉴定
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223771
Sara El-Shennawy
Eleven bacterial strains were isolated from two different oil contaminated Egyptian soils. They were characterized according to their phenotypic examination as species of the genus Bacillus. These bacterial populations showed counts ranging between 8 and 10 log CFU/g soil on the agar plates. An experimental study was undertaken to assess the efficiency of these bacterial isolates in degradation of the petroleum oil in their culture medium amended with 1% v/v petroleum oil. Results revealed that both CS1.1 and CS1.7 are the most effective isolates to degrade two crude oils from Suez and Agiba Company for the first time by growing the individual isolates separately on oil agar media. In addition, CS1.1and CS1.7 exhibited 55.6% and 53.5%, respectively emulsification activity after 48 hrs. incubation time. Also, isolates CS1.1 and CS1.7 could reduce the surface tension to 36.5 ± 0.25mN/m and 37.5 ± 0.45mN/m, respectively in less than 12 hrs. in glucose based media. The gravimetric analysis revealed that both CS1.1 and CS1.7 isolates were able to degrade the petroleum oil and utilize it as a sole carbon source for growth, energy and reproduction. These isolates, CS1.1 and CS1.7 degraded 65% and 64 % of added petroleum oil respectively, over 15 days incubation time. Also, the change in absorbance values of the tested samples from 0.936 O.D. to 1.832 O.D. compared with the control sample 0.815 O.D. indicates the breakdown of the molecular structure of oil and confirms the degradation of crude oil by bacterial isolates. Physiological and biochemical parameters for those the most potent degrading isolates were determined. They were identified as Bacillus subtilis and Bacillus licheniformis.
从两种不同的石油污染埃及土壤中分离出11株细菌。根据表型鉴定,它们属于芽孢杆菌属。这些细菌种群在琼脂板上显示的数量在8到10 log CFU/g土壤之间。我们进行了一项实验研究,以评估这些细菌分离物在添加1% v/v石油的培养基中降解石油的效率。结果表明,CS1.1和CS1.7分别在油脂琼脂培养基上培养,对苏伊士和Agiba公司两种原油的降解效果最佳。cs1.1和CS1.7在48 h后的乳化活性分别为55.6%和53.5%。培养时间。分离物CS1.1和CS1.7在12 h内可将表面张力分别降低至36.5±0.25mN/m和37.5±0.45mN/m。在葡萄糖基培养基中。重量分析表明,CS1.1和CS1.7分离物均能降解石油,并将石油作为唯一的碳源进行生长、能源和繁殖。在15天的培养时间内,CS1.1和CS1.7对添加的石油分别降解了65%和64%。与对照样品0.815 O.D.相比,检测样品的吸光度值从0.936 O.D.变化到1.832 O.D.,表明原油的分子结构被破坏,证实了分离菌对原油的降解作用。测定了最有效降解菌株的生理生化参数。鉴定为枯草芽孢杆菌和地衣芽孢杆菌。
{"title":"ISOLATION AND CHARACTERIZATION OF CRUDE OIL-DEGRADING BACTERIA FROM PETROLEUM OIL CONTAMINATED EGYPTIAN SOILS","authors":"Sara El-Shennawy","doi":"10.21608/ajps.2022.223771","DOIUrl":"https://doi.org/10.21608/ajps.2022.223771","url":null,"abstract":"Eleven bacterial strains were isolated from two different oil contaminated Egyptian soils. They were characterized according to their phenotypic examination as species of the genus Bacillus. These bacterial populations showed counts ranging between 8 and 10 log CFU/g soil on the agar plates. An experimental study was undertaken to assess the efficiency of these bacterial isolates in degradation of the petroleum oil in their culture medium amended with 1% v/v petroleum oil. Results revealed that both CS1.1 and CS1.7 are the most effective isolates to degrade two crude oils from Suez and Agiba Company for the first time by growing the individual isolates separately on oil agar media. In addition, CS1.1and CS1.7 exhibited 55.6% and 53.5%, respectively emulsification activity after 48 hrs. incubation time. Also, isolates CS1.1 and CS1.7 could reduce the surface tension to 36.5 ± 0.25mN/m and 37.5 ± 0.45mN/m, respectively in less than 12 hrs. in glucose based media. The gravimetric analysis revealed that both CS1.1 and CS1.7 isolates were able to degrade the petroleum oil and utilize it as a sole carbon source for growth, energy and reproduction. These isolates, CS1.1 and CS1.7 degraded 65% and 64 % of added petroleum oil respectively, over 15 days incubation time. Also, the change in absorbance values of the tested samples from 0.936 O.D. to 1.832 O.D. compared with the control sample 0.815 O.D. indicates the breakdown of the molecular structure of oil and confirms the degradation of crude oil by bacterial isolates. Physiological and biochemical parameters for those the most potent degrading isolates were determined. They were identified as Bacillus subtilis and Bacillus licheniformis.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73100871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
SPECTROPHOTOMETRIC METHODS FOR DETREMINATION OF TOLTRAZURIL IN PRESENCE OF ITS ALKALI-INDUCED DEGRADATION PRODUCT 用分光光度法测定妥曲祖利碱致降解产物的含量
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223769
Amr M. Abdelfatah
Toltrazuril is a veterinary antiprotozoal drug. In this work, four different simple, accurate, and sensitive spectrophotometric methods have been developed to determine toltrazuril in the presence of its alkali-induced degradation product. Two of these methods depend on selection of two wavelengths at zero order spectrum these methods include (A) dual wavelength method at 239.60 and 257.40 nm, (B) simultaneous equation method at 242.4 nm (λmax of toltrazuril) and 249.8 nm (λmax of toltrazuril degradation product),while the another two methods are (C) area under the curve method at (235245)nm and ( 247-257) nm of toltrazuril and its degradation product and (D) ratio derivative method the absorption spectra of toltrazuril were divided by a suitable absorption spectrum of its degradation product (divisor) and the amplitudes of the first derivative of the ratio spectra at 219 nm were recorded. These methods have been validated for linearity, accuracy and precision and found to be rapid, precise to applied for determination of toltrazuril in Yoserzoril ® suspension.
托曲祖利是一种兽药。本研究建立了四种不同的简单、准确、灵敏的分光光度法来测定碱诱导降解产物中托曲祖利的含量。其中两种方法依赖于零阶光谱中两个波长的选择,这些方法包括(A) 239.60和257.40 nm的双波长法;(B)在242.4 nm处(托曲祖利的λmax)和249.8 nm处(托曲祖利降解产物的λmax)的联立方程法,另外两种方法分别是(C)在托曲祖利及其降解产物的(235245)nm和(247-257)nm处的曲线下面积法和(D)比值导数法,将托曲祖利的吸收光谱除以其降解产物的合适吸收光谱(除数),比值光谱在219 nm处的一阶导数振幅为记录下来。这些方法具有良好的线性度、准确度和精密度,可快速、准确地用于约塞佐利®混悬液中托曲祖里的测定。
{"title":"SPECTROPHOTOMETRIC METHODS FOR DETREMINATION OF TOLTRAZURIL IN PRESENCE OF ITS ALKALI-INDUCED DEGRADATION PRODUCT","authors":"Amr M. Abdelfatah","doi":"10.21608/ajps.2022.223769","DOIUrl":"https://doi.org/10.21608/ajps.2022.223769","url":null,"abstract":"Toltrazuril is a veterinary antiprotozoal drug. In this work, four different simple, accurate, and sensitive spectrophotometric methods have been developed to determine toltrazuril in the presence of its alkali-induced degradation product. Two of these methods depend on selection of two wavelengths at zero order spectrum these methods include (A) dual wavelength method at 239.60 and 257.40 nm, (B) simultaneous equation method at 242.4 nm (λmax of toltrazuril) and 249.8 nm (λmax of toltrazuril degradation product),while the another two methods are (C) area under the curve method at (235245)nm and ( 247-257) nm of toltrazuril and its degradation product and (D) ratio derivative method the absorption spectra of toltrazuril were divided by a suitable absorption spectrum of its degradation product (divisor) and the amplitudes of the first derivative of the ratio spectra at 219 nm were recorded. These methods have been validated for linearity, accuracy and precision and found to be rapid, precise to applied for determination of toltrazuril in Yoserzoril ® suspension.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84730258","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
MICROBIOLOGICAL AND MOLECULAR STUDIES OF SOME GRAM NEGATIVE PATHOGENS CAUSING BLOOD STREAM INFECTIONS IN INTENSIVE CARE UNITS 一些引起重症监护病房血流感染的革兰氏阴性病原体的微生物学和分子研究
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223773
Mohab Sayed
Bloodstream infections (BSIs) and especially central line associated bloodstream infections (CLABSIs), are increasing globally as an important cause of morbidity and mortality. The condition can be life threatening in critically ill patients in the intensive care units (ICUs) of the hospitals. There are serious concerns about the rapid increase of multidrug resistant Gram negative bacteria (MDR-GNB) such as Escherichia coli, Klebsiella pneumonia and Acinetobacter baumannii as the major causes of bloodstream infections. The aim of the study was to emphasize on the significance of MDR-GNB, determine their antibiotic susceptibility pattern, genotypic identification as well as the detection of some virulence genes. Blood specimens were collected from 231 bacteremic patients admitted to different ICUs at three tertiary care hospitals in Egypt. Recovered bacterial isolates were subjected to biochemical identification using conventional methods. Antimicrobial susceptibility testing was performed on Gram negative isolates using both Kirby-Bauer disc diffusion method and Vitek-2 system. Thirty MDR-GNB isolates were selected and screened for the presence of 16S-23S rRNA, UIDA and OMPA genes using PCR assays to confirm their identification. Also, the thirty isolates were screened for the presence of East-1, Cnf-1, IutA and FyuA genes. A total of 185 clinical isolates were recovered from 185 positive blood specimens. Laboratory examination of the positive blood culture specimens revealed that 120 (64.4%), 56 (30.2 %) and 9 (4.8%) were Gram negative, Gram positive and Candida spp., respectively. Thirty MDR-GNB were selected and their antimicrobial susceptibility was compared using the conventional and the Vitek-2 system. For the K. pneumoniae isolates 100% Categorical agreement (CA) was detected for Ceftriaxone, Cefepime, Gentamicin, Amikacin and Tetracycline. For the E. coli CA of (100%) was seen for Ampicillin+Sulbactam, Cefepime, Amikacin, Ciprofloxacin and Tigecycline. categorical agreement (100%) was seen with the tested antibiotics for A. baumannii. Genotypic confirmation of the selected MDR isolates indicated the presence of genes used for identification in all of them. As for the harboring of virulence genes, EAST-1 gene has only been found in 13.3% of the isolates. CNF-1 gene has been identified in 66.6% of the isolates, IutA gene has been found in 96.6% of the isolates and FyuA has been found in 90% of the isolates. Gram negative pathogens were found to be the major bacteria causing bloodstream infection. Vitek-2 system provide accurate antimicrobial susceptibility testing results. CNF-1 toxin production related gene was found to be Az. J. Pharm Sci. Vol. 65, March, 2022. 149 prevalent in most of the isolates. IutA and FyuA siderophore formation related genes were found to be prevalent in most of the isolates.
血液感染(bsi),特别是中央静脉相关性血液感染(CLABSIs),作为发病率和死亡率的重要原因,在全球范围内正在增加。在医院重症监护病房(icu)的重症患者中,这种情况可能危及生命。大肠杆菌、肺炎克雷伯菌和鲍曼不动杆菌等多重耐药革兰氏阴性菌(MDR-GNB)作为血流感染的主要原因迅速增加,令人严重关切。本研究的目的是强调耐多药gnb的重要性,确定其药敏模式、基因型鉴定以及部分毒力基因的检测。采集了埃及三所三级医院不同icu收治的231例菌血症患者的血样。回收的细菌分离株采用常规方法进行生化鉴定。采用Kirby-Bauer圆盘扩散法和Vitek-2系统对革兰氏阴性菌株进行药敏试验。选择30株耐多药gnb分离株,采用PCR方法对其16S-23S rRNA、UIDA和OMPA基因进行筛选,以确认其鉴定。同时,对30株分离株进行了East-1、Cnf-1、IutA和FyuA基因的筛选。从185份阳性血样中共分离出185株临床分离株。实验室检测阳性血培养标本革兰氏阴性120例(64.4%),革兰氏阳性56例(30.2%),假丝酵母菌9例(4.8%)。选择30株MDR-GNB,采用常规与Vitek-2系统进行药敏比较。肺炎克雷伯菌分离株头孢曲松、头孢吡肟、庆大霉素、阿米卡星和四环素的分类一致性为100%。对于大肠杆菌,氨苄西林+舒巴坦、头孢吡肟、阿米卡星、环丙沙星和替加环素的CA均为100%。与所检测的鲍曼不动杆菌抗生素完全一致(100%)。对所选耐多药菌株的基因型确认表明,所有菌株都存在用于鉴定的基因。至于携带毒力基因,仅在13.3%的分离株中发现了EAST-1基因。66.6%的分离株中检出CNF-1基因,96.6%的分离株中检出IutA基因,90%的分离株中检出FyuA基因。革兰氏阴性致病菌是引起血流感染的主要细菌。Vitek-2系统提供准确的抗菌药物敏感性测试结果。CNF-1毒素产生相关基因为Az. J.药学杂志。第65卷,2022年3月。149在大多数分离株中流行。大多数菌株中普遍存在IutA和FyuA铁载体形成相关基因。
{"title":"MICROBIOLOGICAL AND MOLECULAR STUDIES OF SOME GRAM NEGATIVE PATHOGENS CAUSING BLOOD STREAM INFECTIONS IN INTENSIVE CARE UNITS","authors":"Mohab Sayed","doi":"10.21608/ajps.2022.223773","DOIUrl":"https://doi.org/10.21608/ajps.2022.223773","url":null,"abstract":"Bloodstream infections (BSIs) and especially central line associated bloodstream infections (CLABSIs), are increasing globally as an important cause of morbidity and mortality. The condition can be life threatening in critically ill patients in the intensive care units (ICUs) of the hospitals. There are serious concerns about the rapid increase of multidrug resistant Gram negative bacteria (MDR-GNB) such as Escherichia coli, Klebsiella pneumonia and Acinetobacter baumannii as the major causes of bloodstream infections. The aim of the study was to emphasize on the significance of MDR-GNB, determine their antibiotic susceptibility pattern, genotypic identification as well as the detection of some virulence genes. Blood specimens were collected from 231 bacteremic patients admitted to different ICUs at three tertiary care hospitals in Egypt. Recovered bacterial isolates were subjected to biochemical identification using conventional methods. Antimicrobial susceptibility testing was performed on Gram negative isolates using both Kirby-Bauer disc diffusion method and Vitek-2 system. Thirty MDR-GNB isolates were selected and screened for the presence of 16S-23S rRNA, UIDA and OMPA genes using PCR assays to confirm their identification. Also, the thirty isolates were screened for the presence of East-1, Cnf-1, IutA and FyuA genes. A total of 185 clinical isolates were recovered from 185 positive blood specimens. Laboratory examination of the positive blood culture specimens revealed that 120 (64.4%), 56 (30.2 %) and 9 (4.8%) were Gram negative, Gram positive and Candida spp., respectively. Thirty MDR-GNB were selected and their antimicrobial susceptibility was compared using the conventional and the Vitek-2 system. For the K. pneumoniae isolates 100% Categorical agreement (CA) was detected for Ceftriaxone, Cefepime, Gentamicin, Amikacin and Tetracycline. For the E. coli CA of (100%) was seen for Ampicillin+Sulbactam, Cefepime, Amikacin, Ciprofloxacin and Tigecycline. categorical agreement (100%) was seen with the tested antibiotics for A. baumannii. Genotypic confirmation of the selected MDR isolates indicated the presence of genes used for identification in all of them. As for the harboring of virulence genes, EAST-1 gene has only been found in 13.3% of the isolates. CNF-1 gene has been identified in 66.6% of the isolates, IutA gene has been found in 96.6% of the isolates and FyuA has been found in 90% of the isolates. Gram negative pathogens were found to be the major bacteria causing bloodstream infection. Vitek-2 system provide accurate antimicrobial susceptibility testing results. CNF-1 toxin production related gene was found to be Az. J. Pharm Sci. Vol. 65, March, 2022. 149 prevalent in most of the isolates. IutA and FyuA siderophore formation related genes were found to be prevalent in most of the isolates.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"12 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80404692","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
EFFECT OF DIFFERENT PLANT GROWTH REGULATORS ON PLANT REGENERATION AND CALLUS INDUCTION OF PLUMBAGO AURICULATA AND SOME SECONDARY METABOLITES CONTENT 不同植物生长调节剂对木丹植株再生和愈伤组织诱导及次生代谢产物含量的影响
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223767
Abdelrahman Nabil
Plumbago becomes one of the essential medicinal, and decorative plants belonging to the family plumbaginaceae due to the present of plumbagin a secondary metabolite. In this study, the nodal segments of shoots of Plumbago auriculata were used as an explant in establishing in vitro cultures. In vitro callus initiation and shoot regeneration was studied using mixtures of auxins, antiauxins (pChlorophenoxyisobutyric acid and 2,3,5-triiodobenzoic acid), and cytokinins. The medium comprising one mg/l PCIB and 0.5 mg/l BA produced the most significant outcomes in the case of callus induction. However, the best shooting number was given (11.18) with the same combination after eight weeks. According to the data, the leaves extract had the highest level of polyphenols (742.6 mg/100g.d. w) and flavonoids (563.9 mg/100g.d. w).
由于其次生代谢产物铅白金苷的存在,铅白金成为铅白金科重要的药用和装饰植物之一。本研究以木耳垂枝节段为外植体建立离体培养。利用生长素、抗生长素(pchlorphenoxyisobutyric acid和2,3,5-三碘苯甲酸)和细胞分裂素的混合物,研究了离体愈伤组织的形成和芽的再生。1 mg/l PCIB和0.5 mg/l BA的培养基对愈伤组织的诱导效果最为显著。8周后,相同组合的最佳射击次数为11.18次。根据数据,叶提取物的多酚含量最高(742.6 mg/100g.d)。W)和类黄酮(563.9 mg/100g.d)。w)。
{"title":"EFFECT OF DIFFERENT PLANT GROWTH REGULATORS ON PLANT REGENERATION AND CALLUS INDUCTION OF PLUMBAGO AURICULATA AND SOME SECONDARY METABOLITES CONTENT","authors":"Abdelrahman Nabil","doi":"10.21608/ajps.2022.223767","DOIUrl":"https://doi.org/10.21608/ajps.2022.223767","url":null,"abstract":"Plumbago becomes one of the essential medicinal, and decorative plants belonging to the family plumbaginaceae due to the present of plumbagin a secondary metabolite. In this study, the nodal segments of shoots of Plumbago auriculata were used as an explant in establishing in vitro cultures. In vitro callus initiation and shoot regeneration was studied using mixtures of auxins, antiauxins (pChlorophenoxyisobutyric acid and 2,3,5-triiodobenzoic acid), and cytokinins. The medium comprising one mg/l PCIB and 0.5 mg/l BA produced the most significant outcomes in the case of callus induction. However, the best shooting number was given (11.18) with the same combination after eight weeks. According to the data, the leaves extract had the highest level of polyphenols (742.6 mg/100g.d. w) and flavonoids (563.9 mg/100g.d. w).","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75305595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A DIHYDROCHALCONE AND SGLT2 INHIBITOR ABATE METHOTREXATE HEPATOTOXICITY IN MALE RATS; A COMPARATIVE STUDY 二氢查尔酮和sglt2抑制剂对甲氨蝶呤肝毒性的影响比较研究
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223775
Adel T Osman
1 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt. 2 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt. 3 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Nahda University, Beni-Suef 62514, Egypt. 4 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Deraya University, Minya 61519, Egypt. Corresponding author E-mail: adelosman.45@azhar.edu.eg ABSTRACT
1爱资哈尔大学药学院药理学与毒理学教研室,埃及阿西乌特71524 . 2贝尼苏夫大学药学院药理学与毒理学教研室,埃及贝尼苏夫62514 . 3那赫达大学药学院药理学与毒理学教研室,埃及贝尼苏夫62514 . 4德拉亚大学药学院药理学与毒理学教研室,埃及明亚61519。通讯作者E-mail: adelosman.45@azhar.edu.eg
{"title":"A DIHYDROCHALCONE AND SGLT2 INHIBITOR ABATE METHOTREXATE HEPATOTOXICITY IN MALE RATS; A COMPARATIVE STUDY","authors":"Adel T Osman","doi":"10.21608/ajps.2022.223775","DOIUrl":"https://doi.org/10.21608/ajps.2022.223775","url":null,"abstract":"1 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt. 2 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt. 3 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Nahda University, Beni-Suef 62514, Egypt. 4 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Deraya University, Minya 61519, Egypt. Corresponding author E-mail: adelosman.45@azhar.edu.eg ABSTRACT","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88153914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
TWO DIFFERENT CHROMATOGRAPHIC METHODS FOR SIMULTANEOUS DETERMINATION OF COMMON COLD DRUGS AMBROXOL HYDROCHLORIDE, PSEUDOEPHEDRINE HYDROCHLORIDE, LEVOCETERIZINE DIHYDROCHLORIDE AND DESLORATADINE, IN PURE FORMS, AND IN PHARMACEUTICAL DOSAGE FORMS. 常用感冒药盐酸氨溴索、盐酸伪麻黄碱、盐酸左西替嗪和地氯雷他定纯剂型和制剂剂型的两种不同色谱法同时测定。
Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223770
Amany Morsi
Two chromatographic methods were developed for simultaneous determination of some drugs used in common cold. First method is TLC-Densitometric method for the simultaneous estimation of Ambroxol hydrochloride (AMB), Pseudoephedrine hydrochloride (PSE) and Desloratadine (DES) in pure form and in pharmaceutical dosage form, the best resolution was obtained by the use of mobile phase (Ethyl acetate: methanol: ammonia), (14: 0.8: 0.5, v/v/v), the scanning of spots was performed at 254 nm in concentration range (1-40 ug/spot), (5-35 ug/spot),(0.2-2) ug/spot for AMB, PSE and DES, respectively. With LOD 0.262, 0.358 and 0.006 ug/ml. And LOQ 0.793, 1.09 and 0.018 ug /ml for AMB, PSE and DES, respectively. Second method is HPLC-UV Method for the Simultaneous determination of Ambroxol hydrochloride(AMB),Pseudoephedrine hydrochloride(PSE), Desloratadine (DES) and levoceterizine dihydrochloride (LVC) in quaternary mixture by using mobile phase consisted of acetonitrile: 0.01 M phosphate buffer (PH 5.5) (50:50, v/v) in an isocratic mode through inertsil C8 (250mm x 4.6mm, 5 μ) column at a flow rate of 1.3 ml/min. UV detection was carried out at 215 nm in concentration range (1.6-40), (3.2-40) , (0.69), (2.4-8.4 ) ug/ml for AMB, PSE , DES and LVC, respectively .With LOD 0.428, 0.180, 0.125 and 0.124, ug/ml And LOQ 1.299 , 0.550, 0.379, and 0.375ug/ml for AMB, PSE , DES and LVC, respectively The validation of the proposed methods was done according to ICH guidelines.
建立了两种色谱法同时测定感冒用药物的方法。第一种方法采用tlc -密度法同时测定盐酸氨溴索(AMB)、盐酸伪麻黄碱(PSE)和地氯雷他定(DES)的纯剂型和制剂剂型,采用流动相(乙酸乙酯:甲醇:氨)、(14:0.8:0.5,v/v/v)获得最佳分辨率,在254 nm处进行斑点扫描,分别在浓度范围(1-40 ug/spot)、(5-35 ug/spot)、(0.2-2)ug/spot下对AMB、PSE和DES进行斑点扫描。检出限分别为0.262、0.358和0.006 ug/ml。AMB、PSE和DES的检出限分别为0.793、1.09和0.018 ug /ml。第二种方法是HPLC-UV法,采用乙腈:0.01 M磷酸盐缓冲液(PH 5.5) (50:50, v/v)为流动相,流速为1.3 ml/min, inertsil C8 (250mm × 4.6mm, 5 μ)柱,流速为1.3 ml/min,同时测定季铵盐混合物中盐酸氨溴索(AMB)、盐酸伪麻黄碱(PSE)、地氯雷他定(DES)和盐酸左旋西嗪(LVC)的含量。在215nm波长下,在浓度范围(1.6 ~ 40)、(3.2 ~ 40)、(0.69)、(2.4 ~ 8.4)ug/ml范围内对AMB、PSE、DES和LVC进行紫外检测,检出限分别为0.428、0.180、0.125、0.124 ug/ml,检出限分别为1.299、0.550、0.379、0.375ug/ml。
{"title":"TWO DIFFERENT CHROMATOGRAPHIC METHODS FOR SIMULTANEOUS DETERMINATION OF COMMON COLD DRUGS AMBROXOL HYDROCHLORIDE, PSEUDOEPHEDRINE HYDROCHLORIDE, LEVOCETERIZINE DIHYDROCHLORIDE AND DESLORATADINE, IN PURE FORMS, AND IN PHARMACEUTICAL DOSAGE FORMS.","authors":"Amany Morsi","doi":"10.21608/ajps.2022.223770","DOIUrl":"https://doi.org/10.21608/ajps.2022.223770","url":null,"abstract":"Two chromatographic methods were developed for simultaneous determination of some drugs used in common cold. First method is TLC-Densitometric method for the simultaneous estimation of Ambroxol hydrochloride (AMB), Pseudoephedrine hydrochloride (PSE) and Desloratadine (DES) in pure form and in pharmaceutical dosage form, the best resolution was obtained by the use of mobile phase (Ethyl acetate: methanol: ammonia), (14: 0.8: 0.5, v/v/v), the scanning of spots was performed at 254 nm in concentration range (1-40 ug/spot), (5-35 ug/spot),(0.2-2) ug/spot for AMB, PSE and DES, respectively. With LOD 0.262, 0.358 and 0.006 ug/ml. And LOQ 0.793, 1.09 and 0.018 ug /ml for AMB, PSE and DES, respectively. Second method is HPLC-UV Method for the Simultaneous determination of Ambroxol hydrochloride(AMB),Pseudoephedrine hydrochloride(PSE), Desloratadine (DES) and levoceterizine dihydrochloride (LVC) in quaternary mixture by using mobile phase consisted of acetonitrile: 0.01 M phosphate buffer (PH 5.5) (50:50, v/v) in an isocratic mode through inertsil C8 (250mm x 4.6mm, 5 μ) column at a flow rate of 1.3 ml/min. UV detection was carried out at 215 nm in concentration range (1.6-40), (3.2-40) , (0.69), (2.4-8.4 ) ug/ml for AMB, PSE , DES and LVC, respectively .With LOD 0.428, 0.180, 0.125 and 0.124, ug/ml And LOQ 1.299 , 0.550, 0.379, and 0.375ug/ml for AMB, PSE , DES and LVC, respectively The validation of the proposed methods was done according to ICH guidelines.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82584799","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY 具有抗癌活性的新型吡唑[3,4- d]嘧啶衍生物的合成及生物学评价
Pub Date : 2021-03-01 DOI: 10.21608/AJPS.2021.153563
Farag F. Sherbiny
A series of novel pyrazolo[3,4-d]pyrimidine derivatives have been designed based on chemical modifications on the general features of the reported and clinically used EGFR-TKIs such as repalcing of quinazoline moiety of reported EGFR-TKIs as erlotinib by pyrazolo[3,4-d]pyrimidine nucleus,introducing different hydrophobic moieties including phenyl, aromatic heterocyclic, fused aromatic or aliphatic structures , introducing different linkers which may be one atom , two atoms, three atoms, four atoms and five atoms and introducing of phenyl ring at position-3 of 1H-pyrazolo[3,4d]pyrimidine nucleus to occupy the hydrophobic region II of ATP binding site. All the new synthesized compounds were biologically screened in vitro for their cytotoxic activities against four cancer cell lines namely, HepG-2, MCF-7, HCT-116, and Hela. The results of cytotoxic evaluation indicated that compound VI was found to be the most prominent broad-spectrum cytotoxic activity and significantly more potent than doxorubicin with IC50 values of 6.18, 6.48, 4.03, and 5.82μM against tested cell lines. In addition, compounds IXa,b displayed promising cytotoxic effect against all tested cell lines with IC50 values less than 30 μM compared with doxorubicin as a control drug. Besides, compound X possessed excellent anti-proliferative activities against the four cell lines with IC50 values ranging from 18 μM to 39.5 μM. Structural pharmacophoric features indicated that pyrazolo[3,4-d]pyrimidine scaffold having a four atoms linker as thiosemicarbazide moiety as compounds IXa,b which substituted with aliphatic moiety at the 4-position was more potent than those possessing one atom, two atoms, three atoms and five atoms linkers which lead to significant decrease in cytotoxic
根据已报道和临床使用的EGFR-TKIs的一般特征,设计了一系列新的吡唑[3,4-d]嘧啶衍生物,如用吡唑[3,4-d]嘧啶核取代已报道的EGFR-TKIs的喹唑啉部分作为埃洛替尼,引入不同的疏水部分,包括苯基、芳香杂环、融合芳香或脂肪结构,引入不同的连接物,可以是一个原子、两个原子、三个原子,4个原子和5个原子,并在1h -吡唑[3,4d]嘧啶核的-3位引入苯基环,占据ATP结合位点的疏水区II。所有新合成的化合物在体外进行了生物筛选,以测定其对HepG-2、MCF-7、HCT-116和Hela四种癌细胞的细胞毒活性。细胞毒性评价结果表明,化合物VI具有最显著的广谱细胞毒活性,其IC50值分别为6.18、6.48、4.03和5.82μM,显著高于阿霉素。此外,与对照药物阿霉素相比,化合物IXa、b对所有被试细胞系均表现出良好的细胞毒作用,IC50值小于30 μM。此外,化合物X对4种细胞系均具有良好的抗增殖活性,IC50值在18 ~ 39.5 μM之间。结构药效特征表明,吡唑啉[3,4-d]嘧啶支架具有4原子连接体作为硫代氨基脲基团,如化合物IXa,b在4位取代脂肪基团,比具有1原子、2原子、3原子和5原子连接体的支架更有效,导致细胞毒性显著降低
{"title":"SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY","authors":"Farag F. Sherbiny","doi":"10.21608/AJPS.2021.153563","DOIUrl":"https://doi.org/10.21608/AJPS.2021.153563","url":null,"abstract":"A series of novel pyrazolo[3,4-d]pyrimidine derivatives have been designed based on chemical modifications on the general features of the reported and clinically used EGFR-TKIs such as repalcing of quinazoline moiety of reported EGFR-TKIs as erlotinib by pyrazolo[3,4-d]pyrimidine nucleus,introducing different hydrophobic moieties including phenyl, aromatic heterocyclic, fused aromatic or aliphatic structures , introducing different linkers which may be one atom , two atoms, three atoms, four atoms and five atoms and introducing of phenyl ring at position-3 of 1H-pyrazolo[3,4d]pyrimidine nucleus to occupy the hydrophobic region II of ATP binding site. All the new synthesized compounds were biologically screened in vitro for their cytotoxic activities against four cancer cell lines namely, HepG-2, MCF-7, HCT-116, and Hela. The results of cytotoxic evaluation indicated that compound VI was found to be the most prominent broad-spectrum cytotoxic activity and significantly more potent than doxorubicin with IC50 values of 6.18, 6.48, 4.03, and 5.82μM against tested cell lines. In addition, compounds IXa,b displayed promising cytotoxic effect against all tested cell lines with IC50 values less than 30 μM compared with doxorubicin as a control drug. Besides, compound X possessed excellent anti-proliferative activities against the four cell lines with IC50 values ranging from 18 μM to 39.5 μM. Structural pharmacophoric features indicated that pyrazolo[3,4-d]pyrimidine scaffold having a four atoms linker as thiosemicarbazide moiety as compounds IXa,b which substituted with aliphatic moiety at the 4-position was more potent than those possessing one atom, two atoms, three atoms and five atoms linkers which lead to significant decrease in cytotoxic","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76170698","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
期刊
Al-Azhar Journal of Pharmaceutical Sciences
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1