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Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors
Sinomenine (SIN) is widely used in China to treat a variety of rheumatic diseases (RA), and has various pharmacological effects such as anti-inflammatory, analgesic, and anti-tumor effects. However, due to the histamine release characteristics of SIN, its adverse reactions such as allergic reactions...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6337707/ https://www.ncbi.nlm.nih.gov/pubmed/30586944 http://dx.doi.org/10.3390/ijms20010070 |
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author | Zhang, Yu-Shi Han, Jia-Yin Iqbal, Omer Liang, Ai-Hua |
author_facet | Zhang, Yu-Shi Han, Jia-Yin Iqbal, Omer Liang, Ai-Hua |
author_sort | Zhang, Yu-Shi |
collection | PubMed |
description | Sinomenine (SIN) is widely used in China to treat a variety of rheumatic diseases (RA), and has various pharmacological effects such as anti-inflammatory, analgesic, and anti-tumor effects. However, due to the histamine release characteristics of SIN, its adverse reactions such as allergic reactions, gastrointestinal reactions, and circulatory systemic reactions have been drawing increasing attention. We present here a systematic review of the chemical structure, pharmacological effects, clinical application, and adverse reactions of SIN, a detailed discussion on the relationship between histamine/histamine receptor and mechanism of action of SIN. In addition, we simulated the binding of SIN to four histamine receptors by using a virtual molecular docking method and found that the bonding intensity between SIN and receptors varied in the order shown as follows: H1R > H2R ~ H3R > H4R. The docking results suggested that SIN might exhibit dual regulatory effects in many processes such as cyclooxygenase-2 (COX-2) expression, NF-κB pathway activation, and degranulation of mast cells to release histamine, thereby exhibiting pro-inflammatory (adverse reactions)/anti-inflammatory effects. This study provides a theoretical basis for the clinical treatment of inflammations seen such as in RA using SIN, and also suggests that SIN has great potential in the field of cancer treatment and will have very important social and economic significance. |
format | Online Article Text |
id | pubmed-6337707 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-63377072019-01-22 Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors Zhang, Yu-Shi Han, Jia-Yin Iqbal, Omer Liang, Ai-Hua Int J Mol Sci Review Sinomenine (SIN) is widely used in China to treat a variety of rheumatic diseases (RA), and has various pharmacological effects such as anti-inflammatory, analgesic, and anti-tumor effects. However, due to the histamine release characteristics of SIN, its adverse reactions such as allergic reactions, gastrointestinal reactions, and circulatory systemic reactions have been drawing increasing attention. We present here a systematic review of the chemical structure, pharmacological effects, clinical application, and adverse reactions of SIN, a detailed discussion on the relationship between histamine/histamine receptor and mechanism of action of SIN. In addition, we simulated the binding of SIN to four histamine receptors by using a virtual molecular docking method and found that the bonding intensity between SIN and receptors varied in the order shown as follows: H1R > H2R ~ H3R > H4R. The docking results suggested that SIN might exhibit dual regulatory effects in many processes such as cyclooxygenase-2 (COX-2) expression, NF-κB pathway activation, and degranulation of mast cells to release histamine, thereby exhibiting pro-inflammatory (adverse reactions)/anti-inflammatory effects. This study provides a theoretical basis for the clinical treatment of inflammations seen such as in RA using SIN, and also suggests that SIN has great potential in the field of cancer treatment and will have very important social and economic significance. MDPI 2018-12-24 /pmc/articles/PMC6337707/ /pubmed/30586944 http://dx.doi.org/10.3390/ijms20010070 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Zhang, Yu-Shi Han, Jia-Yin Iqbal, Omer Liang, Ai-Hua Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title | Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title_full | Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title_fullStr | Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title_full_unstemmed | Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title_short | Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors |
title_sort | research advances and prospects on mechanism of sinomenin on histamine release and the binding to histamine receptors |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6337707/ https://www.ncbi.nlm.nih.gov/pubmed/30586944 http://dx.doi.org/10.3390/ijms20010070 |
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