Kinetics and Mechanism Study of Competitive Inhibition of Jack-Bean Urease by Baicalin
المؤلفون المشاركون
Tan, Lirong
Su, Jiyan
Wu, Dianwei
Yu, Xiaodan
Su, Zuqing
He, Jingjin
Kong, Songzhi
Lin, Ji
Lai, Xiao-Ping
Wu, Xiao-Li
Su, Zi-Ren
المصدر
العدد
المجلد 2013، العدد 2013 (31 ديسمبر/كانون الأول 2013)، ص ص. 1-9، 9ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2013-10-01
دولة النشر
مصر
عدد الصفحات
9
التخصصات الرئيسية
الطب البشري
تكنولوجيا المعلومات وعلم الحاسوب
الملخص EN
Baicalin (BA) is the principal component of Radix Scutellariae responsible for its pharmacological activity.
In this study, kinetics and mechanism of inhibition by BA against jack-bean urease were investigated for its therapeutic potential.
It was revealed that the IC50 of BA against jack-bean urease was 2.74 ± 0.51 mM, which was proved to be a competitive and concentration-dependent inhibition with slow-binding progress curves.
The rapid formation of initial BA-urease complex with an inhibition constant of Ki=3.89 × 10−3 mM was followed by a slow isomerization into the final complex with an overall inhibition constant of Ki*=1.47×10-4 mM.
High effectiveness of thiol protectors against BA inhibition indicated that the strategic role of the active-site sulfhydryl group of the urease was involved in the blocking process.
Moreover, the inhibition of BA was proved to be reversible due to the fact that urease could be reactivated by dithiothreitol but not reactant dilution.
Molecular docking assay suggested that BA made contacts with the important activating sulfhydryl group Cys-592 residues and restricted the mobility of the active-site flap.
Taken together, it could be deduced that BA was a competitive inhibitor targeting thiol groups of urease in a slow-binding manner both reversibly and concentration-dependently, serving as a promising urease inhibitor for treatments on urease-related diseases.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Tan, Lirong& Su, Jiyan& Wu, Dianwei& Yu, Xiaodan& Su, Zuqing& He, Jingjin…[et al.]. 2013. Kinetics and Mechanism Study of Competitive Inhibition of Jack-Bean Urease by Baicalin. The Scientific World Journal،Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-1033402
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Tan, Lirong…[et al.]. Kinetics and Mechanism Study of Competitive Inhibition of Jack-Bean Urease by Baicalin. The Scientific World Journal No. 2013 (2013), pp.1-9.
https://search.emarefa.net/detail/BIM-1033402
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Tan, Lirong& Su, Jiyan& Wu, Dianwei& Yu, Xiaodan& Su, Zuqing& He, Jingjin…[et al.]. Kinetics and Mechanism Study of Competitive Inhibition of Jack-Bean Urease by Baicalin. The Scientific World Journal. 2013. Vol. 2013, no. 2013, pp.1-9.
https://search.emarefa.net/detail/BIM-1033402
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1033402
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر