In silico approach for identification of potential tetracyclic triterpenoids from mushroom as HMG-CoA reductase inhibitor

Cardiovascular disease is estimated to be responsible for one-third of all global deaths annually. It occurs mostly due to hyperlipidemia, a condition where excessive cholesterol deposits in blood vessels. A favorable target for treating hyperlipidemia involves the crucial role of inhibition of a specific enzyme known as 3-Hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase). The primary goal of this present study is to identify potential HMG-CoA reductase inhibitors containing tetracyclic triterpene nucleus derived from mushrooms. A library of 86 myco-constituents bearing a tetracyclic triterpene scaffold was prepared and screened to identify potential HMG-CoA reductase inhibitors targeting proteins 1HW8 and 1HW9. For this purpose, molecular docking, ADME prediction, and molecular dynamics (MD) simulation studies were performed on this in-house prepared database. The virtual screening results exhibited M_02(c) as the best hit with promising SP Glide scores compared to standard statin drugs. In order to assess the stability and interactions, a 100 ns MD simulation was performed. Further, M_02(c) was also analysed for MMGBSA binding energy to access and validate the thermodynamic stability of the protein-ligand complex. The results of this study revealed that M_02(c) is a promising hit molecule and may emerge as a potent HMG-CoA reductase inhibitor in preventing and treating hyperlipidemia.

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Publication Details

Journal
Aspects of Molecular Medicine
Published
2024-09-05
DOI
https://doi.org/10.1016/j.amolm.2024.100053
Citations
8
Primary Topic
Fungal Biology and Applications
Type
article
Field-Weighted Citation Impact
3.58
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article

In silico approach for identification of potential tetracyclic triterpenoids from mushroom as HMG-CoA reductase inhibitor

Rishav Mazumder, Bimal Debnath, Sudhan Debnath, Deijy Choudhury et al.
8 citations
Aspects of Molecular Medicine
Fungal Biology and Applications
3.58
article

In silico approach for identification of potential tetracyclic triterpenoids from mushroom as HMG-CoA reductase inhibitor

Rishav Mazumder, Bimal Debnath, Sudhan Debnath, Deijy Choudhury, Rajat Ghosh, Alekhya Sarkar, Ashmita Ghosh
article en
8 citations

Abstract

Cardiovascular disease is estimated to be responsible for one-third of all global deaths annually. It occurs mostly due to hyperlipidemia, a condition where excessive cholesterol deposits in blood vessels. A favorable target for treating hyperlipidemia involves the crucial role of inhibition of a specific enzyme known as 3-Hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase). The primary goal of this present study is to identify potential HMG-CoA reductase inhibitors containing tetracyclic triterpene nucleus derived from mushrooms. A library of 86 myco-constituents bearing a tetracyclic triterpene scaffold was prepared and screened to identify potential HMG-CoA reductase inhibitors targeting proteins 1HW8 and 1HW9. For this purpose, molecular docking, ADME prediction, and molecular dynamics (MD) simulation studies were performed on this in-house prepared database. The virtual screening results exhibited M_02(c) as the best hit with promising SP Glide scores compared to standard statin drugs. In order to assess the stability and interactions, a 100 ns MD simulation was performed. Further, M_02(c) was also analysed for MMGBSA binding energy to access and validate the thermodynamic stability of the protein-ligand complex. The results of this study revealed that M_02(c) is a promising hit molecule and may emerge as a potent HMG-CoA reductase inhibitor in preventing and treating hyperlipidemia.

Aspects of Molecular MedicineVol. 4
Tripura University (IN)
Openalex Percentile: Top 7%
Fungal Biology and Applications
3.58
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