Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i>
<i>Andrographis paniculata</i> (AP) has been widely used in China for centuries to treat various diseases, and especially to treat inflammation. Diterpenoid lactones are the main anti-inflammatory components of AP. However, systematic chemical composition and biological activities, as we...
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MDPI AG
2019-07-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/24/15/2726 |
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| author | Lin Gan Yuanru Zheng Lijuan Deng Pinghua Sun Jiaxi Ye Xiduan Wei Feifei Liu Linzhong Yu Wencai Ye Chunlin Fan Junshan Liu Wenqing Zhang |
| author_facet | Lin Gan Yuanru Zheng Lijuan Deng Pinghua Sun Jiaxi Ye Xiduan Wei Feifei Liu Linzhong Yu Wencai Ye Chunlin Fan Junshan Liu Wenqing Zhang |
| author_sort | Lin Gan |
| collection | DOAJ |
| description | <i>Andrographis paniculata</i> (AP) has been widely used in China for centuries to treat various diseases, and especially to treat inflammation. Diterpenoid lactones are the main anti-inflammatory components of AP. However, systematic chemical composition and biological activities, as well as key pharmacophores, of these diterpenoid lactones from AP have not yet been clearly understood. In this study, 17 diterpenoid lactones, including 2 new compounds, were identified by spectroscopic methods, and most of them attenuated the generation of TNF-α and IL-6 in LPS-induced RAW 274.7 cells examined by ELISA. Pharmacophores of diterpenoid lactones responsible for the anti-inflammatory activities were revealed based on the quantitative structure-activity relationship (QSAR) models. Moreover, new compounds (<b>AP-1</b> and <b>AP-4</b>) exerted anti-inflammatory activity in LPS microinjection-induced zebrafish, which might be correlated with the inhibition of the translocation of NF-κB p65 from cytoplasm to nucleus. Our study provides guidelines for future structure modification and rational drug design of diterpenoid lactones with anti-inflammatory properties in medical chemistry. |
| first_indexed | 2024-12-13T01:14:55Z |
| format | Article |
| id | doaj.art-31f527656808477ab644b729095e14aa |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T01:14:55Z |
| publishDate | 2019-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-31f527656808477ab644b729095e14aa2022-12-22T00:04:21ZengMDPI AGMolecules1420-30492019-07-012415272610.3390/molecules24152726molecules24152726Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i>Lin Gan0Yuanru Zheng1Lijuan Deng2Pinghua Sun3Jiaxi Ye4Xiduan Wei5Feifei Liu6Linzhong Yu7Wencai Ye8Chunlin Fan9Junshan Liu10Wenqing Zhang11Division of Cell, Developmental and Integrative Biology, School of Medicine, South China University of Technology, Guangzhou 510641, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaFormula-pattern Research Center, School of Traditional Chinese Medicine, Jinan University, Guangzhou 510632, ChinaGuangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaGuangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaSchool of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaGuangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaGuangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaSchool of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, ChinaDivision of Cell, Developmental and Integrative Biology, School of Medicine, South China University of Technology, Guangzhou 510641, China<i>Andrographis paniculata</i> (AP) has been widely used in China for centuries to treat various diseases, and especially to treat inflammation. Diterpenoid lactones are the main anti-inflammatory components of AP. However, systematic chemical composition and biological activities, as well as key pharmacophores, of these diterpenoid lactones from AP have not yet been clearly understood. In this study, 17 diterpenoid lactones, including 2 new compounds, were identified by spectroscopic methods, and most of them attenuated the generation of TNF-α and IL-6 in LPS-induced RAW 274.7 cells examined by ELISA. Pharmacophores of diterpenoid lactones responsible for the anti-inflammatory activities were revealed based on the quantitative structure-activity relationship (QSAR) models. Moreover, new compounds (<b>AP-1</b> and <b>AP-4</b>) exerted anti-inflammatory activity in LPS microinjection-induced zebrafish, which might be correlated with the inhibition of the translocation of NF-κB p65 from cytoplasm to nucleus. Our study provides guidelines for future structure modification and rational drug design of diterpenoid lactones with anti-inflammatory properties in medical chemistry.https://www.mdpi.com/1420-3049/24/15/2726<i>Andrographis paniculate</i>diterpenoid lactonesanti-inflammatory3D-QSAR |
| spellingShingle | Lin Gan Yuanru Zheng Lijuan Deng Pinghua Sun Jiaxi Ye Xiduan Wei Feifei Liu Linzhong Yu Wencai Ye Chunlin Fan Junshan Liu Wenqing Zhang Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> Molecules <i>Andrographis paniculate</i> diterpenoid lactones anti-inflammatory 3D-QSAR |
| title | Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> |
| title_full | Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> |
| title_fullStr | Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> |
| title_full_unstemmed | Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> |
| title_short | Diterpenoid Lactones with Anti-Inflammatory Effects from the Aerial Parts of <i>Andrographis paniculata</i> |
| title_sort | diterpenoid lactones with anti inflammatory effects from the aerial parts of i andrographis paniculata i |
| topic | <i>Andrographis paniculate</i> diterpenoid lactones anti-inflammatory 3D-QSAR |
| url | https://www.mdpi.com/1420-3049/24/15/2726 |
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