Wild Bitter Melon Leaf Extract Inhibits Porphyromonas gingivalis-Induced Inflammation: Identification of Active Compounds through Bioassay-Guided Isolation

Abstract

Porphyromonas gingivalis has been identified as one of the major periodontal pathogens. Activity-directed fractionation and purification processes were employed to identify the anti-inflammatory active compounds using heat-killed P. gingivalis-stimulated human monocytic THP-1 cells in vitro. Five major fractions were collected from the ethanol/ethyl acetate extract of wild bitter melon (Momordica charantia Linn. var. abbreviata Ser.) leaves and evaluated for their anti-inflammatory activity against P. gingivalis. Among the test fractions, Fraction 5 effectively decreased heat-killed P. gingivalis-induced interleukin (IL)-8 and was subjected to separation and purification by using chromatographic techniques. Two cucurbitane triterpenoids were isolated from the active fraction and identified as 5β,19-epoxycucurbita-6,23-diene-3β,19,25-triol (1) and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al (2) by comparing spectral data. Treatments of both compounds in vitro potently suppressed P. gingivalis-induced IL-8, IL-6, and IL-1β levels and the activation of mitogen-activated protein kinase (MAPK) in THP-1 cells. Both compounds effectively inhibited the mRNA levels of IL-6, tumor necrosis factor (TNF)-α, and cyclooxygenase (COX)-2 in P. gingivalis-stimulated gingival tissue of mice. These findings imply that 5β, 19-epoxycucurbita-6,23-diene-3β,19,25-triol and 3β,7β,25-trihydroxycucurbita-5,23-dien-19-al could be used for the development of novel therapeutic approaches against P. gingivalis infections.

Momordica charantia, a Nutraceutical Approach for Inflammatory Related Diseases

“…This activity was attributed to the anti-inflammatory effects of phenolic compounds present in the extract (Huang et al, 2015). Cucurbitane triterpenods isolated from MC leaves strongly suppressed Porphyromonas gingivalis -induced IL-8, IL-6, and IL-1β levels (Tsai et al, 2016).…”

Bitter melon (Momordica charantia) attenuates atherosclerosis in apo-E knock-out mice possibly through reducing triglyceride and anti-inflammation

“…Abundant evidences showed that Traditional Chinese Medicine (TCM) can present the progression of atherosclerosis via anti-oxidation and anti-inflammation [ 3 – 5 ]. The bioactive components of bitter melon, one of the most common TCMs, have been reported to improve the glucose and lipids metabolism, important risk factors of atherosclerosis, via anti-oxidation and anti-inflammation [ 6 – 9 ]. Furthermore, studies show that BM can regulate metabolism through the activation of peroxisome proliferator-activated receptor (PPAR) and AMP-activated protein kinase (AMPK) [ 10 – 16 ], which may represent protective mechanisms against atherosclerosis via potential anti-inflammation in endothelial cells [ 17 , 18 ].…”

Bioactive properties and phenolic profile of Momordica charantia L. medicinal plant growing wild in Trinidad and Tobago

“…Cucurbitane triterpenods previously isolated from leaves of wild M. charantia potently suppressed Porphyromonas gingivalisinduced IL-8, IL-6, and IL-1␤ levels (Tsai et al, 2016). Methanolic extract of M. charantia leaves inhibited the carrageenan-induced edema in vivo with results comparable to indomethacin (Ganesan et al, 2008).…”