Abstract
The vines and leaves of Momordica charantia 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 M. charantia 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 M. charantia. 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 M. charantia should be used with caution. An extraction protocol that can enrich TCD but remove momordicine I would likely enhance the safety of the extract.
Highlights
Momordica charantia L. belongs to the Cucurbitaceae family, and its fruit is commonly known as bitter melon or bitter gourd
Aside from the fruits, the vines and leaves of M. charantia L. are used as herbal medicines in treating inflammation-related disorders [1,2]
The results indicate that TCD and LPS both activated mitogen-activated protein kinases (MAPKs) and that TCD did not suppress LP9So-f 18 induced MAPK activation
Summary
Momordica charantia L. belongs to the Cucurbitaceae family, and its fruit is commonly known as bitter melon or bitter gourd Each part of this plant, including the vines, leaves, fruits, roots, and seeds, has been used in folk medicine to treat various diseases, including diabetes, worm infection, and inflammation [1,2]. Aside from the fruits, the vines and leaves of M. charantia L. are used as herbal medicines in treating inflammation-related disorders [1,2]. Momordicine II produced a milder under 0.1–100 μM, cell survival exceeded 70% These data suggest that momordicin4eoIf 1is the most toxic to normal cells among the four compounds, exerting deleterious effects on both cell lines in concentrations higher than 10 or 20 μM. Momordicine II produced a mdeitldriemr ednettarlimefefencttaloenffIeEcCt -o1n8 IcEelCls-.18Mcoemllso.rMdiocimneorIdVicainde ITVCaDnwd eTrCeDnowt heraermnofut lhtaormnofurml taol nceolrlms ianl tcheellsinidnitchaeteidndcoicnactendtrcaotniocenns.trations
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