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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
Author(s)
Sudto, Kanokorn
Saparpakorn, Patchreenart
Tancharoen, Chompoonuch
Techasakul, Supanna
Khunnawutmanotham, Nisachon
Vajrodaya, Srunya
Ge, Hui Ming
Tan, Ren Xiang
Hannongbua, Supa
Date Issued
November 1, 2019
Type
Article
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.
Citation
Chiang Mai Journal of Science, 46(6), 1161-1175, 2019