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Diptoindonesin D, a Potent Antibacterial Activity Against Gram-positive Bacteria, an Inhibitor of Penicillin-binding Protein 2a from the Stem Bark of Shorea roxburghii G.Don


Paper Type 
Contributed Paper
Title 
Diptoindonesin D, a Potent Antibacterial Activity Against Gram-positive Bacteria, an Inhibitor of Penicillin-binding Protein 2a from the Stem Bark of Shorea roxburghii G.Don
Author 
Kanokorn Sudto, Patchreenart Saparpakorn, Chompoonuch Tancharoen, Darinee Phromyothin, Supanna Techasakul, Nisachon Khunnawutmanotham, Srunya Vajrodaya, Hui-Ming Ge, Ren Xiang Tan, and Supa Hannongbua*
Email 
fscisph@ku.ac.th
Abstract:
 The emergence and spread of antimicrobial resistance (AMR) is a serious threat to public
human health. The challenge now is an urgent need to new potent antibiotics combating AMR which
can be an effective way to solve the crisis. A new potent antibacterial activity of diptoindonesin D,
together with four known compounds as hopeafuran, α-viniferan, hopeahainol A and hopeahainol
C were isolated from the stem bark of Shorea roxburghii G. Don in Khon Kaen province, Thailand.
Diptoindonesin D were screened for antimicrobial activity and possesses significant activity minimum
inhibitory concentrations (MIC) values of 4.68 and 9.37 μg/mL against Staphylococcus epidermidis and
Staphylococcus aureus, respectively. The absolute configuration of diptoindonesin D were evaluated by
circular dichroism (ECD) calculations. The ECD results indicated that the possible configuration of
diptoindonesin D should be R-configuration. Furthermore, reverse docking was performed to identify
the protein target of diptoindonesin D based on four scoring functions using GOLD program. This
investigation is the first time that reveals interaction between diptoindonesin D and its binding with
cell wall synthesis protein targets. The results highlighted that, penicillin-binding protein 2a (PBP2a), an
antibacterial cell wall, might be the potential target for the binding of diptoindonesin D. The obtained
results can be useful as a guideline for the development of effective diptoindonesin D as a PBP2a
inhibitor.
Start & End Page 
1161 - 1175
Received Date 
2019-06-23
Revised Date 
Accepted Date 
2019-08-02
Full Text 
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Keyword 
antimicrobial resistance, Shorea roxburghii G. Don, target identification, cell wall target, molecular docking, ECD calculations
Volume 
Vol.46 No.6 (November 2019)
DOI 
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