Yangwen Luo, Jing Wen, I. Kanfer, Pei Yu, S. Patnala
Sceletium tortuosum is a well-known medicinal plant in South Africa with potential applications. Its raw material, extracts and isolated alkaloids are used as dietary supplements, natural medicines and health food. In this paper, methods of planting, extraction, isolation and identification of Sceletium tortuosum , as well as its chemical structure of main extracted alkaloids, their related pharmacological effects and mechanisms for treating the disease are reviewed. In general, Sceletium tortuosum is active to central nervous system (CNS) by inhibiting phosphodiesterase isozyme 4 (PDE4), serotonin (5-HT) uptake and acetylcholinesterase (AChE). It also acts as a monoamine releasing agent for antidepressant effects. Therefore, it is a useful therapeutic agent in clinical use.
{"title":"Sceletium Tortuosum: Effects on Central Nervous System and Related Disease","authors":"Yangwen Luo, Jing Wen, I. Kanfer, Pei Yu, S. Patnala","doi":"10.5281/ZENODO.4015978","DOIUrl":"https://doi.org/10.5281/ZENODO.4015978","url":null,"abstract":"Sceletium tortuosum is a well-known medicinal plant in South Africa with potential applications. Its raw material, extracts and isolated alkaloids are used as dietary supplements, natural medicines and health food. In this paper, methods of planting, extraction, isolation and identification of Sceletium tortuosum , as well as its chemical structure of main extracted alkaloids, their related pharmacological effects and mechanisms for treating the disease are reviewed. In general, Sceletium tortuosum is active to central nervous system (CNS) by inhibiting phosphodiesterase isozyme 4 (PDE4), serotonin (5-HT) uptake and acetylcholinesterase (AChE). It also acts as a monoamine releasing agent for antidepressant effects. Therefore, it is a useful therapeutic agent in clinical use.","PeriodicalId":16721,"journal":{"name":"Journal of pharmaceutical and biomedical sciences","volume":"29 9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77270197","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}
Background Tinibs were a kind of important epidermal growth factor receptor (EGFR) inhibitors used as potential therapeutic agents in treating non-small cell lung cancer (NSCLC) in clinic. The drug resistance of clinical used tinibs made the development of more active tinib analogues an attractive field in research. Quinazoline ring was regarded as the key fragment in tinibs and quinazolinone was indispensible intermediate in the synthesis of quinazoline. Thus, synthesis of quinazolinone intermediates was a key step which would further limit the overall yield of final product of tinib analogues. However, the commonly used synthetic scheme was somewhat complicated and time consuming with relatively low yield in heterocylization of quinazolinone and its derivatives. Aim In this work, we intended to explore an effective way to improve synthesis of heterocyclization of 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one (compound 5), the key fragment of erlotinib analogues, in both reaction procedure and yield, thus to provide reference to synthesis of other quinazolinone derivatives. Methods A simple microwave-assisted one-pot reaction was employed to improve the synthesis of heterocyclization of quinazolinone ring. The reaction conditions, including microwave power, temperature and time of reaction, were screened to achieve high yield under simple operation. Results 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one (compound 5) was successfully synthesized from starting material of 4,5-bis(2-methoxyethoxy)-2-nitrobenzonitrile by microwave reaction, which was finished in 1 hour just by one step. The yield of heterocyclization was increased from 29.8% of commonly used three-step scheme to 50% herein. Conclusion Microwave reaction efficiently improved synthesis of heterocyclization of 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one into "quinazolinone in both synthetic procedure and yield. The results may provide valuable reference to synthesis of other quinazolinone derivatives.
{"title":"Microwave Reaction Improved Heterocyclization of Quinazolinone Ring in Synthesis of Erlotinib Analogues","authors":"J. Man, J. Qi, Jie Jiang, Sha Li","doi":"10.5281/ZENODO.3903346","DOIUrl":"https://doi.org/10.5281/ZENODO.3903346","url":null,"abstract":"Background Tinibs were a kind of important epidermal growth factor receptor (EGFR) inhibitors used as potential therapeutic agents in treating non-small cell lung cancer (NSCLC) in clinic. The drug resistance of clinical used tinibs made the development of more active tinib analogues an attractive field in research. Quinazoline ring was regarded as the key fragment in tinibs and quinazolinone was indispensible intermediate in the synthesis of quinazoline. Thus, synthesis of quinazolinone intermediates was a key step which would further limit the overall yield of final product of tinib analogues. However, the commonly used synthetic scheme was somewhat complicated and time consuming with relatively low yield in heterocylization of quinazolinone and its derivatives. Aim In this work, we intended to explore an effective way to improve synthesis of heterocyclization of 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one (compound 5), the key fragment of erlotinib analogues, in both reaction procedure and yield, thus to provide reference to synthesis of other quinazolinone derivatives. Methods A simple microwave-assisted one-pot reaction was employed to improve the synthesis of heterocyclization of quinazolinone ring. The reaction conditions, including microwave power, temperature and time of reaction, were screened to achieve high yield under simple operation. Results 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one (compound 5) was successfully synthesized from starting material of 4,5-bis(2-methoxyethoxy)-2-nitrobenzonitrile by microwave reaction, which was finished in 1 hour just by one step. The yield of heterocyclization was increased from 29.8% of commonly used three-step scheme to 50% herein. Conclusion Microwave reaction efficiently improved synthesis of heterocyclization of 6,7-bis(2-methoxyethoxy)quinazolin-4(3H)-one into \"quinazolinone in both synthetic procedure and yield. The results may provide valuable reference to synthesis of other quinazolinone derivatives.","PeriodicalId":16721,"journal":{"name":"Journal of pharmaceutical and biomedical sciences","volume":"98 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85795364","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}
Objective To investigate the clinical effect of levosimendan in perioperative aortic and/or mitral valve replacement. Methods Patients undergoing open heart aortic and/or mitral valve replacement in our hospital from January 2018 to December 2019 were enrolled. 45 patients in the control group received routine perioperative treatment based on dopamine, while 45 patients in the research group received continuous perioperative administration of levosimendan injection for 24h on the basis of routine treatment. The left ventricular ejection fraction (LVEF), left ventricular end-diastolic diameter (LVDd) and left ventricular end-systolic diameter (LVDs) were evaluated by color doppler echocardiography before and one week after surgery. Postoperative mechanical ventilation weaning time, length of ICU stays, number of vasoactive drugs used and withdrawal time; indexes of liver and kidney function before and on the day after surgery to 10 days after surgery; use of in vitro support techniques such as aortic balloon pulsation (IABP), continuous renal replacement therapy (CRRT) and extracorporeal membrane oxygenation (ECMO) within 5 days of perioperative period. Results The improvement of LVDs and LVEF in the study group using levosimendan one week after the operation was significantly better than that in the control group (P value was 0.013 and 0.001, respectively), and fewer kinds of vasoactive drugs were needed (P<0.001), and the risk of postoperative AKI in the study group was significantly lower than that in the control group ( P=0.047 ). Conclusion The perioperative use of levosimendan can effectively promote the recovery of cardiac systolic function and reduce the risk of postoperative AKI.
{"title":"Clinical study of Perioperative Use of Levosimendan in Patients Undergoing Heart Valve Replacement","authors":"Jiawen Huang, Chengfeng Huang, Zhao-fen Lin, Zhidong Zhang","doi":"10.5281/ZENODO.3923653","DOIUrl":"https://doi.org/10.5281/ZENODO.3923653","url":null,"abstract":"Objective To investigate the clinical effect of levosimendan in perioperative aortic and/or mitral valve replacement. Methods Patients undergoing open heart aortic and/or mitral valve replacement in our hospital from January 2018 to December 2019 were enrolled. 45 patients in the control group received routine perioperative treatment based on dopamine, while 45 patients in the research group received continuous perioperative administration of levosimendan injection for 24h on the basis of routine treatment. The left ventricular ejection fraction (LVEF), left ventricular end-diastolic diameter (LVDd) and left ventricular end-systolic diameter (LVDs) were evaluated by color doppler echocardiography before and one week after surgery. Postoperative mechanical ventilation weaning time, length of ICU stays, number of vasoactive drugs used and withdrawal time; indexes of liver and kidney function before and on the day after surgery to 10 days after surgery; use of in vitro support techniques such as aortic balloon pulsation (IABP), continuous renal replacement therapy (CRRT) and extracorporeal membrane oxygenation (ECMO) within 5 days of perioperative period. Results The improvement of LVDs and LVEF in the study group using levosimendan one week after the operation was significantly better than that in the control group (P value was 0.013 and 0.001, respectively), and fewer kinds of vasoactive drugs were needed (P<0.001), and the risk of postoperative AKI in the study group was significantly lower than that in the control group ( P=0.047 ). Conclusion The perioperative use of levosimendan can effectively promote the recovery of cardiac systolic function and reduce the risk of postoperative AKI.","PeriodicalId":16721,"journal":{"name":"Journal of pharmaceutical and biomedical sciences","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84633451","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}
Pub Date : 2018-09-10DOI: 10.23888/pavlovj201826121-35
Dovganiuk Ap, Tarasova Ap, Pokrovskiy Mv
We are glad to introduce several variants of pharmacological correction of ischemic hepatic injury by three different types of medicines—incretinomimetics, imidazoline receptor’s agonists and biguanides. The study was conducted at the center for preclinical studies, Belgorod National Research University. The experiment was performed on both sex rats, divided into seven groups (n = 10): An intact group, pseudo-operated animals (autopsy of the abdominal wall without ligation of the liver vessels), ischemia/reperfusion group without drug correction, animals undergoing ischemia/liver reperfusion + metformin (50 mg/kg), animals undergoing ischemia/liver reperfusion + moxonidine (1 ?g/kg), animals undergoing ischemia/liver reperfusion + C7070 (10 mg/kg). For the evaluation, the coefficients calculated from the level of hepatic transaminases (ALT, AST), as well as morphometric ratios of the area of necrosis and deep ischemia of the liver, were used for evaluation according to the histological examination. The experiment was performed on 50 rats of both sexes, divided into the next groups (n = 10): An intact group; pseudo-operated animals (autopsy of the abdominal wall without ligation of the liver vessels), ischemia/reperfusion group without drug correction, animals undergoing ischemia/liver reperfusion + metformin (50 mg/kg), animals undergoing ischemia/liver reperfusion + moxonidine (1 ?g/kg), animals undergoing ischemia/liver reperfusion + C7070 (10 mg/kg), animals undergoing ischemia/liver reperfusion + vildagliptine (0.2 mg/kg), animals undergoing ischemia/liver reperfusion + exenatide (10 ?g/kg). For the evaluation, the coefficients calculated from the level of hepatic transaminases (ALT, AST), as well as morphometric ratios of the area of necrosis and deep ischemia of the liver, were used for the evaluation according to the histological examination. Conclusion The imidazoline receptor agonists significantly and significantly reduce the functional and morphological manifestations of liver ischemia/reperfusion.
{"title":"Possible Ways of Pharmacological Correction of Ischemic Liver Damage","authors":"Dovganiuk Ap, Tarasova Ap, Pokrovskiy Mv","doi":"10.23888/pavlovj201826121-35","DOIUrl":"https://doi.org/10.23888/pavlovj201826121-35","url":null,"abstract":"We are glad to introduce several variants of pharmacological correction of ischemic hepatic injury by three different types of medicines—incretinomimetics, imidazoline receptor’s agonists and biguanides. The study was conducted at the center for preclinical studies, Belgorod National Research University. The experiment was performed on both sex rats, divided into seven groups (n = 10): An intact group, pseudo-operated animals (autopsy of the abdominal wall without ligation of the liver vessels), ischemia/reperfusion group without drug correction, animals undergoing ischemia/liver reperfusion + metformin (50 mg/kg), animals undergoing ischemia/liver reperfusion + moxonidine (1 ?g/kg), animals undergoing ischemia/liver reperfusion + C7070 (10 mg/kg). For the evaluation, the coefficients calculated from the level of hepatic transaminases (ALT, AST), as well as morphometric ratios of the area of necrosis and deep ischemia of the liver, were used for evaluation according to the histological examination. The experiment was performed on 50 rats of both sexes, divided into the next groups (n = 10): An intact group; pseudo-operated animals (autopsy of the abdominal wall without ligation of the liver vessels), ischemia/reperfusion group without drug correction, animals undergoing ischemia/liver reperfusion + metformin (50 mg/kg), animals undergoing ischemia/liver reperfusion + moxonidine (1 ?g/kg), animals undergoing ischemia/liver reperfusion + C7070 (10 mg/kg), animals undergoing ischemia/liver reperfusion + vildagliptine (0.2 mg/kg), animals undergoing ischemia/liver reperfusion + exenatide (10 ?g/kg). For the evaluation, the coefficients calculated from the level of hepatic transaminases (ALT, AST), as well as morphometric ratios of the area of necrosis and deep ischemia of the liver, were used for the evaluation according to the histological examination. Conclusion The imidazoline receptor agonists significantly and significantly reduce the functional and morphological manifestations of liver ischemia/reperfusion.","PeriodicalId":16721,"journal":{"name":"Journal of pharmaceutical and biomedical sciences","volume":"52 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77751128","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：