Cargando…
Accelerated identification of serine racemase inhibitor from Centella asiatica
Serine racemase (SR) converts the free form of L-serine into D-serine (DS) in the mammalian brain. The DS functions as a co-agonist of N-methyl D-aspartate (NMDA) receptor. The over- activation of NMDA receptor leads to many neurological disorders like stroke, amyotrophic lateral sclerosis, Alzheime...
Autores principales: | , , , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2020
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7070078/ https://www.ncbi.nlm.nih.gov/pubmed/32170206 http://dx.doi.org/10.1038/s41598-020-61494-1 |
_version_ | 1783505903404711936 |
---|---|
author | Rani, Komal Tyagi, Mitali Mazumder, Mohit Singh, Akanksha Shanmugam, Annaian Dalal, Krishna Pillai, Manoj Samudrala, Gourinath Kumar, Saroj Srinivasan, Alagiri |
author_facet | Rani, Komal Tyagi, Mitali Mazumder, Mohit Singh, Akanksha Shanmugam, Annaian Dalal, Krishna Pillai, Manoj Samudrala, Gourinath Kumar, Saroj Srinivasan, Alagiri |
author_sort | Rani, Komal |
collection | PubMed |
description | Serine racemase (SR) converts the free form of L-serine into D-serine (DS) in the mammalian brain. The DS functions as a co-agonist of N-methyl D-aspartate (NMDA) receptor. The over- activation of NMDA receptor leads to many neurological disorders like stroke, amyotrophic lateral sclerosis, Alzheimer’s disease and an effective inhibitor of SR could be a corrective method for the receptor over-activation. We report for the first time here a rapid way of purifying and identifying an inhibitor from medicinal plants known to have the neuro-protective effect. We have purified SR inhibitor from the methanolic extract of Centella asiatica by affinity method. High resolution mass spectrometry and infrared spectroscopy were used to identify the ligand to be madecassoside. We have shown the madecassoside binding in silico and its inhibition of recombinant human serine racemase in vitro and ex vivo. |
format | Online Article Text |
id | pubmed-7070078 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
spelling | pubmed-70700782020-03-22 Accelerated identification of serine racemase inhibitor from Centella asiatica Rani, Komal Tyagi, Mitali Mazumder, Mohit Singh, Akanksha Shanmugam, Annaian Dalal, Krishna Pillai, Manoj Samudrala, Gourinath Kumar, Saroj Srinivasan, Alagiri Sci Rep Article Serine racemase (SR) converts the free form of L-serine into D-serine (DS) in the mammalian brain. The DS functions as a co-agonist of N-methyl D-aspartate (NMDA) receptor. The over- activation of NMDA receptor leads to many neurological disorders like stroke, amyotrophic lateral sclerosis, Alzheimer’s disease and an effective inhibitor of SR could be a corrective method for the receptor over-activation. We report for the first time here a rapid way of purifying and identifying an inhibitor from medicinal plants known to have the neuro-protective effect. We have purified SR inhibitor from the methanolic extract of Centella asiatica by affinity method. High resolution mass spectrometry and infrared spectroscopy were used to identify the ligand to be madecassoside. We have shown the madecassoside binding in silico and its inhibition of recombinant human serine racemase in vitro and ex vivo. Nature Publishing Group UK 2020-03-13 /pmc/articles/PMC7070078/ /pubmed/32170206 http://dx.doi.org/10.1038/s41598-020-61494-1 Text en © The Author(s) 2020 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/. |
spellingShingle | Article Rani, Komal Tyagi, Mitali Mazumder, Mohit Singh, Akanksha Shanmugam, Annaian Dalal, Krishna Pillai, Manoj Samudrala, Gourinath Kumar, Saroj Srinivasan, Alagiri Accelerated identification of serine racemase inhibitor from Centella asiatica |
title | Accelerated identification of serine racemase inhibitor from Centella asiatica |
title_full | Accelerated identification of serine racemase inhibitor from Centella asiatica |
title_fullStr | Accelerated identification of serine racemase inhibitor from Centella asiatica |
title_full_unstemmed | Accelerated identification of serine racemase inhibitor from Centella asiatica |
title_short | Accelerated identification of serine racemase inhibitor from Centella asiatica |
title_sort | accelerated identification of serine racemase inhibitor from centella asiatica |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7070078/ https://www.ncbi.nlm.nih.gov/pubmed/32170206 http://dx.doi.org/10.1038/s41598-020-61494-1 |
work_keys_str_mv | AT ranikomal acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT tyagimitali acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT mazumdermohit acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT singhakanksha acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT shanmugamannaian acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT dalalkrishna acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT pillaimanoj acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT samudralagourinath acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT kumarsaroj acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica AT srinivasanalagiri acceleratedidentificationofserineracemaseinhibitorfromcentellaasiatica |