Neuraminidase Inhibitor of Garcinia atroviridis L. Fruits and Leaves Using Partial Purification and Molecular Characterization.

Muchtaridi Muchtaridi,Aisyah Saad Abdul Rahim,Rina Fajri Nuwarda,Emmy Hainida Khairul Ikram,Habibah A Wahab,Amirah Mohd Gazzali

doi:10.3390/molecules27030949

Muchtaridi Muchtaridi, Aisyah Saad Abdul Rahim + Show 4 more

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https://doi.org/10.3390/molecules27030949

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Abstract

Neuraminidase (NA) is an enzyme that prevents virions from aggregating within the host cell and promotes cell-to-cell spread by cleaving glycosidic linkages to sialic acid. The best-known neuraminidase is the viral neuraminidase, which present in the influenza virus. Thus, the development of anti-influenza drugs that inhibit NA has emerged as an important and intriguing approach in the treatment of influenza. Garcinia atroviridis L. (GA) dried fruits (GAF) are used commercially as seasoning and in beverages. The main objective of this study was to identify a new potential neuraminidase inhibitor from GA. A bioassay-guided fractionation method was applied to obtain the bioactive compounds leading to the identification of garcinia acid and naringenin. In an enzyme inhibition study, garcinia acid demonstrated the highest activity when compared to naringenin. Garcinia acid had the highest activity, with an IC50 of 17.34–17.53 µg/mL or 91.22–92.21 µM against Clostridium perfringens-NA, and 56.71–57.85 µg/mL or 298.32–304.31 µM against H1N1-NA. Based on molecular docking results, garcinia acid interacted with the triad arginine residues (Arg118, Arg292, and Arg371) of the viral neuraminidase, implying that this compound has the potential to act as a NA enzyme inhibitor.

Highlights

Influenza continues to be a significant public health concern since it causes annual epidemics, and has the potential to spark a global pandemic
The current study aims to investigate the inhibitory activity of isolated compounds from G. atroviridis L. against
The MeOH extract was evaluated against C. perfringens-NA, which resulted in an IC50 value of 9.43 g/mL as shown in Figure 1. n-Hexane extracts were found to be less active against C. perfringens-NA, whereas EtOAc extracts were observed to be the most active against both C. perfringens-NA and H1N1-NA

Summary

Introduction

Influenza continues to be a significant public health concern since it causes annual epidemics, and has the potential to spark a global pandemic. Annual seasonal influenza epidemics are predicted to result in approximately 3 to 5 million cases of severe illness, and 290,000 to 650,000 respiratory-related deaths [1]. Among the four genera of influenza viruses (influenza types A, B, C, and D), type A is the most pathogenic group of viruses capable of causing severe respiratory illnesses or death [2]. The 2009 swine flu H1N1 and the highly pathogenic avian flu H5N1 are among influenza A viruses that have posed significant health risks in many parts of the world. The World Health Organization determined swine flu (H1N1) to be a pandemic. There were 94,512 confirmed cases in 123 countries, including 112 cases in Malaysia [3]

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