Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i>
The vines and leaves of <i>Momordica charantia</i> L. are used as herbal medicines to treat inflammation-related disorders. However, their safety profile remains uncharacterized, and the constituents in their extracts that exert anti-inflammatory and adverse effects remain unclear. This...
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MDPI AG
2022-01-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/23/3/1071 |
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| author | Mei-Chia Chou Yuan-Jia Lee Yao-Ting Wang Shi-Yie Cheng Hsueh-Ling Cheng |
| author_facet | Mei-Chia Chou Yuan-Jia Lee Yao-Ting Wang Shi-Yie Cheng Hsueh-Ling Cheng |
| author_sort | Mei-Chia Chou |
| collection | DOAJ |
| description | The vines and leaves of <i>Momordica charantia</i> L. are used as herbal medicines to treat inflammation-related disorders. However, their safety profile remains uncharacterized, and the constituents in their extracts that exert anti-inflammatory and adverse effects remain unclear. This study isolated the characteristic cucurbitane-type triterpenoid species in the vines and leaves of <i>M. charantia</i> L. and analyzed their cytotoxicity, anti-inflammatory effects, and underlying mechanisms. Four structurally related triterpenoids—momordicines I, II, IV, and (23E) 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD)—were isolated from the triterpenoid-rich fractions of extracts from the vines and leaves of <i>M. charantia</i>. Momordicine I was cytotoxic on normal cells, momordicine II exerted milder cytotoxicity, and momordicine IV and TCD had no obvious adverse effects on cell growth. TCD had anti-inflammatory activity both in vivo and in vitro. In lipopolysaccharide-stimulated RAW 264.7 cells, TCD inhibited the inhibitor kappa B kinase/nuclear factor-κB pathway and enhanced the expression of nuclear factor erythroid 2-related factor 2, heme oxygenase-1, and glutamate-cysteine ligase modifier subunit through the extracellular signal-regulated kinase1/2 and p38. Thus, the vines and leaves of <i>M. charantia</i> should be used with caution. An extraction protocol that can enrich TCD but remove momordicine I would likely enhance the safety of the extract. |
| first_indexed | 2024-03-09T23:50:28Z |
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| language | English |
| last_indexed | 2024-03-09T23:50:28Z |
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| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-3ee15ba2699e40b58ce7f4b5757ccdb52023-11-23T16:34:35ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-01-01233107110.3390/ijms23031071Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i>Mei-Chia Chou0Yuan-Jia Lee1Yao-Ting Wang2Shi-Yie Cheng3Hsueh-Ling Cheng4Graduate Institute of Bioresources, National Pingtung University of Science and Technology, Neipu, Pingtung County 912301, TaiwanDepartment of Biological Science and Technology, National Pingtung University of Science and Technology, Neipu, Pingtung County 912301, TaiwanDepartment of Life Sciences, National University of Kaohsiung, Kaohsiung 811726, TaiwanDepartment of Life Sciences, National University of Kaohsiung, Kaohsiung 811726, TaiwanDepartment of Biological Science and Technology, National Pingtung University of Science and Technology, Neipu, Pingtung County 912301, TaiwanThe vines and leaves of <i>Momordica charantia</i> L. are used as herbal medicines to treat inflammation-related disorders. However, their safety profile remains uncharacterized, and the constituents in their extracts that exert anti-inflammatory and adverse effects remain unclear. This study isolated the characteristic cucurbitane-type triterpenoid species in the vines and leaves of <i>M. charantia</i> L. and analyzed their cytotoxicity, anti-inflammatory effects, and underlying mechanisms. Four structurally related triterpenoids—momordicines I, II, IV, and (23E) 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (TCD)—were isolated from the triterpenoid-rich fractions of extracts from the vines and leaves of <i>M. charantia</i>. Momordicine I was cytotoxic on normal cells, momordicine II exerted milder cytotoxicity, and momordicine IV and TCD had no obvious adverse effects on cell growth. TCD had anti-inflammatory activity both in vivo and in vitro. In lipopolysaccharide-stimulated RAW 264.7 cells, TCD inhibited the inhibitor kappa B kinase/nuclear factor-κB pathway and enhanced the expression of nuclear factor erythroid 2-related factor 2, heme oxygenase-1, and glutamate-cysteine ligase modifier subunit through the extracellular signal-regulated kinase1/2 and p38. Thus, the vines and leaves of <i>M. charantia</i> should be used with caution. An extraction protocol that can enrich TCD but remove momordicine I would likely enhance the safety of the extract.https://www.mdpi.com/1422-0067/23/3/1071<i>Momordica charantia</i>triterpenoidanti-inflammationantioxidant enzymesNrf2heme oxygenase-1 |
| spellingShingle | Mei-Chia Chou Yuan-Jia Lee Yao-Ting Wang Shi-Yie Cheng Hsueh-Ling Cheng Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> International Journal of Molecular Sciences <i>Momordica charantia</i> triterpenoid anti-inflammation antioxidant enzymes Nrf2 heme oxygenase-1 |
| title | Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> |
| title_full | Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> |
| title_fullStr | Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> |
| title_full_unstemmed | Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> |
| title_short | Cytotoxic and Anti-Inflammatory Triterpenoids in the Vines and Leaves of <i>Momordica charantia</i> |
| title_sort | cytotoxic and anti inflammatory triterpenoids in the vines and leaves of i momordica charantia i |
| topic | <i>Momordica charantia</i> triterpenoid anti-inflammation antioxidant enzymes Nrf2 heme oxygenase-1 |
| url | https://www.mdpi.com/1422-0067/23/3/1071 |
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