Enhanced purification protocol for the angiotensin-converting enzyme from bovine systems and investigation of the in vitro effect of some active substances

2021 ◽  
pp. 109604
Author(s):  
Fatih Karahan ◽  
Vedat Turkoglu
Peptides ◽  
2011 ◽  
Vol 32 (5) ◽  
pp. 1013-1019 ◽  
Author(s):  
Tânia Tavares ◽  
Maria del Mar Contreras ◽  
Manuela Amorim ◽  
Manuela Pintado ◽  
Isidra Recio ◽  
...  

Author(s):  
A.Z. Dautova ◽  
E.A. Khazhieva ◽  
V.G. Shamratova ◽  
L.Z. Sadykova

The aim of the paper was to study the association of polymorphic variants of rs4646994 (I/D) of the angiotensin converting enzyme gene (ACE) and rs5810761 (+9/-9) of the bradykinin B2 receptor gene (BDKRB2) with erythrocyte adrenoreactivity (ARE) in athletes and untrained young men. Materials and Methods. The study involved 61 young men (aged 21–23) with different levels of motor activity (MA). ARE was evaluated according to the erythrocyte sedimentation rate (ESR) change under adrenaline in vitro at final concentrations 10-5, 10-6, 10-7, 10-9, 10-11, 10-13 g/ml of venous blood. According to the effect observed and ESR shifts under adrenaline, we distinguished 3 ARE types: antiaggregative (AnAg), areactive (Ar) and aggregative (Ar). Results. The results of comparative and correlation analyses demonstrated that young athletes with +9/-9 (BDKRB2) genotype were characterized by a higher aggregative resistance of erythrocytes to the effects of both physiological (<10-9 g/ml) (physiological adrenaline concentration, PAC) and stressful doses (>10-9 g/ml) of adrenaline (stress adrenaline concentration, SAC), as well as by predominance of AnAg and Ar ARE types. In athletes, among the representatives of different genotypes of АСЕ gene I/D polymorphism, the erythrocyte response to adrenaline did not have any statistically significant differences. In physically inactive students, namely individuals with the D/D genotype, maximal ESR deviation under PAC was less than in those with I/D genotype. Conclusion. Athletes with *-9 allele (+9/-9 genotype) in their genotype can be considered more stress-resistant, which is provided by optimal adaptive and compensatory body mechanisms. Apparently, resistance of cells to the adrenaline contributes much to the work of these mechanisms. As for the ACE gene polymorphism, its effect on the suspension characteristics of erythrocytes is less pronounced not only in physically inactive young men, but in athletes as well. Keywords: erythrocyte adrenoreactivity (ARE), stress tolerance, β2 bradykinin receptor gene (BDKRB2), angiotensin converting enzyme (ACE) gene, motor activity. Цель работы – изучить ассоциацию полиморфных вариантов rs4646994 (I/D) гена ангиотензинпревращающего фермента (АСЕ) и rs5810761 (+9/-9) гена рецептора брадикинина 2 типа (BDKRB2) с адренореактивностью эритроцитов (АРЭ) у спортсменов и юношей, ведущих физически малоактивный образ жизни. Материалы и методы. В исследовании принял участие 61 юноша с разным уровнем двигательной активности (ДА) в возрасте 21–23 лет. Оценку АРЭ проводили по изменению скорости оседания эритроцитов (СОЭ) под действием адреналина in vitro в конечных концентрациях 10-5, 10-6, 10-7, 10-8, 10-9, 10-11, 10-13 г/мл венозной крови. По характеру наблюдаемого эффекта в соответствии с направленностью сдвигов СОЭ в присутствии адреналина мы выделили 3 типа АРЭ: антиагрегационный (АнАг), ареактивный (Ар) и агрегационный (Аг). Результаты. По результатам сравнительного и корреляционного анализа установлено, что юноши-спортсмены с генотипом +9/-9 (BDKRB2) характеризуются более высокой агрегативной устойчивостью эритроцитов к воздействию как физиологических (10-9 г/мл и ниже), так и повышенных (стрессовых) доз (выше 10-8 г/мл крови) адреналина, а также преобладанием АнАг- и Ар-типов АРЭ. У представителей разных генотипов полиморфизма I/D гена АСЕ реакция эритроцитов на адреналин не имела статистически значимых различий в группе спортсменов, тогда как в группе малоактивных студентов у лиц с генотипом D/D максимальное отклонение СОЭ при ФКА было меньше, чем при генотипе I/D. Выводы. Спортсменов, имеющих в своём генотипе аллель *-9 (+9/-9 генотип), можно считать более стрессоустойчивыми, что обеспечивается оптимальными адаптивно-компенсаторными механизмами организма, существенная роль в обеспечении которых, по-видимому, принадлежит устойчивости клеток к действию адреналина. Что касается полиморфизма гена АСЕ, то его влияние на суспензионные характеристики эритроцитов выражено слабее не только у физически малоактивных юношей, но и у спортсменов. Ключевые слова: адренореактивность эритроцитов (АРЭ), стрессоустойчивость, ген рецептора брадикинина β2 (BDKRB2), ген ангиотензинпревращающего фермента (АСЕ), двигательная активность.


Author(s):  
Nehad J. Ahmed

Aims: This study aims to review the efficacy of chloroquine and hydroxychloroquine to treat coronavirus disease 2019 (COVID-19) associated pneumonia. Methodology: This review includes searching Google scholar for publications about the use of hydroxychloroquinein the treatment of COVID-19 using the words of (Covid-19) AND hydroxychloroquine. Results: Chloroquine and hydroxychloroquine have proven effective in treating coronavirus in China in vitro, but till now only few clinical trials are available and these trials were conducted on a small sample size of the patients. The efficacy of chloroquine and hydroxychloroquine is mainly due to its effect on angiotensin-converting enzyme II (ACE2). Conclusion: The use of chloroquine and hydroxychloroquine could be very promising but more trials are needed that include larger sample size and more data are required about the comparison between chloroquine and hydroxychloroquine with other antivirals.


2021 ◽  
Vol 2 (1) ◽  
pp. 16-27
Author(s):  
Zahra Sharifinia ◽  
◽  
Samira Asadi ◽  
Mahyar Irani ◽  
Abdollah Allahverdi ◽  
...  

Objective: The receptor-binding domain (RBD) of the S1 domain of the SARS-CoV- 2 Spike protein performs a key role in the interaction with Angiotensin-converting enzyme 2 (ACE2), leading to both subsequent S2 domain-mediated membrane fusion and incorporation of viral RNA in host cells. Methods: In this study, we investigated the inhibitor’s targeted compounds through existing human ACE2 drugs to use as a future viral invasion. 54 FDA approved drugs were selected to assess their binding affinity to the ACE2 receptor. The structurebased methods via computational ones have been used for virtual screening of the best drugs from the drug database. Key Findings: The ligands “Cinacalcet” and “Levomefolic acid” highaffinity scores can be a potential drug preventing Spike protein of SARS-CoV-2 and human ACE2 interaction. Levomefolic acid from vitamin B family was proved to be a potential drug as a spike protein inhibitor in previous clinical and computational studies. Besides that, in this study, the capability of Levomefolic acid to avoid ACE2 and Spike protein of SARS-CoV-2 interaction is indicated. Therefore, it is worth to consider this drug for more in vitro investigations as ACE2 and Spike protein inhibition candidate. Conclusion: The two Cinacalcet and Levomefolic acid are the two ligands that have highest energy binding for human ACE2 blocking among 54 FDA approved drugs.


1994 ◽  
Vol 6 (8) ◽  
pp. 1153-1160 ◽  
Author(s):  
Sergei Danilov ◽  
Elena Atochina ◽  
Holger Hiemisch ◽  
Tatiana Churak-ova ◽  
Aygul Moldobayeva ◽  
...  

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 16-24
Author(s):  
Mohammed Oday Ezzat ◽  
Basma M. Abd Razik ◽  
Kutayba F. Dawood

The prevalence of a novel coronavirus (2019-nCoV) in the last few months represents a serious threat as a world health emergency concern. Angiotensin-converting enzyme 2 (ACE2) is the host cellular receptor for the respiratory syndrome of coronavirus epidemic in 2019 (2019-nCoV). In this work, the active site of ACE2 is successfully located by Sitmap prediction tool and validated by different marketed drugs. To design and discover new medical countermeasure drugs, we evaluate a total of 184 molecules of 7-chloro-N-methylquinolin-4-amine derivatives for binding affinity inside the crystal structure of ACE2 located active site. A novel series of N-substituted 2,5-bis[(7-chloroquinolin-4-yl)amino]pentanoic acid derivatives is generated and evaluated for a prospect as a lead compound for (2019-nCoV) medication with a docking score range of (-10.60 to -8.99) kcal/mol for the highest twenty derivatives. Moreover, the ADME pharmaceutical properties were evaluated for further proposed experimental evaluation in vitro or in vivo


Sign in / Sign up

Export Citation Format

Share Document