Development And Application Of Dengue Virus Ns2b/Ns3 Protease Inhibition Assay Using Alphascreen® Technology.

Penyakit denggi yang disebabkan oleh virus denggi merupakan suatu masalah kesihatan di peringkat global. Protease NS2B/NS3 merupakan protein bukan struktur yang memainkan peranan penting dalam replikasi dan kematangan virus denggi. Dengue is an infectious disease caused by the dengue virus and is a global health problem. NS2B/NS3 protease is a non-structural protein which plays a pivotal role in viral replication and maturation of the dengue virus

Data on the construction of a recombinant HEK293 cell line overexpressing hERG potassium channel and examining the presence of hERG mRNA and protein expression

The data presented in this article are related to the research article entitled “The effects of deoxyelephantopin on the cardiac delayed rectifier potassium channel current (IKr) and human ether-a-go-go-related gene (hERG) expression” (Y.F. Teah, M.A. Abduraman, A. Amanah, M.I. Adenan, S.F. Sulaiman, M.L. Tan) [1], which the possible hERG blocking properties of deoxyelephantopin were investigated. This article describes the construction of human embryonic kidney 293 (HEK293) cells overexpressing HERG potassium channel and verification of the presence of hERG mRNA and protein expression in this recombinant cell line

Anti-tumor Activity of NuvastaticTM (C5OSEW5050ESA) of Orthosiphon stamineus and Rosmarinic Acid in An Athymic Nude Mice Model of Breast Cancer

The current treatment strategies for metastatic breast cancer depend on the cancer subtype by palliating symptoms and prolonging life. However, triple-negative breast cancers have no targeted treatment available. Orthosiphon stamineus (O.s) is a traditional folk medicine plant used in South East Asia to treat many diseases. The aim of this study is to evaluate the anti-tumor activity of O.s extract formulation (ID: C5EOSEW5050ESA trademarked as NuvastaticTM) and its major component, rosmarinic acid in a breast in vivo tumor xenograft model. Human triple-negative breast cancer cells were transplanted into the mammary fat pad of 20 athymic nude mice. Fourteen days post-injection, mice were randomly assigned to four groups. C5EOSEW5050ESA (200 and 400 mg/kg/day) and rosmarinic acid (32 mg/kg/day) were administered orally. The body weight and tumor size were measured twice a week. Histopathological analyses of tumor tissues were conducted. Tumor necrosis and tumor growth were determined by hematoxylin and eosin staining. A significant reduction in tumor size and growth was found in all treatment groups. No significant difference between C5EOSEW5050ESA at 200 mg/kg and rosmarinic acid in the reduction of tumor size and necrosis. However, a more significant reduction was found in tumor growth and necrosis with 400 mg/kg of C5EOSEW5050ESA treatment as compared to other treatments. These results highlighted the anti-tumor activity of C5EOSEW5050ESA in reducing breast tumor growth in mice compared to the lower dose of C5EOSEW5050ESA and rosmarinic acid. This study provides valuable insights into using C5EOSEW5050ESA as a treatment to target triple-negative breast cancers in vivo

The Effects Of Mitragynine On P-Glycoprotein Regulations And Its Neurotoxicity Mechanisms In Brain Cell Lines

The main objective is to determine the effects of mitragynine on P-gp regulations and neurotoxicity effects of drug-herb interactions between mitragynine and P-gp substrates in the PC12 cells using both in silico and in vitro approaches

Development of a NS2B/NS3 protease inhibition assay using AlphaScreen® beads for screening of anti-dengue activities

Background: Dengue infection is an endemic infectious disease and it can lead to dengue fever, dengue hemorrhagic fever, and/or dengue shock syndromes. Dengue NS2B/NS3 protease complex is essential for viral replication and is a primary target for anti-dengue drug development. In this study, a NS2B/NS3 protease inhibition assay was developed using AlphaScreen® beads and was used to screen compounds for their protease inhibition activities. Methods: The assay system utilized a known NS2B/NS3 peptide substrate, a recombinant of NS2B/NS3 protease with proprietary StrepTactin® donor and nickel chelate acceptor beads in 384-well format. Results: The optimized assay to screen for NS2B/NS3 protease inhibitors was demonstrated to be potentially useful with reasonable zʹ factor, coefficient variance and signal to background ratio. However, screening of synthesized thioguanine derivatives using the optimized AlphaScreen® assay revealed weak NS2B/NS3 inhibition activities. Conclusion: The AlphaScreen® assay to screen for NS2B/NS3 protease inhibitors is potentially applicable for high throughput screening