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KMID : 1161420120150040369
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Journal of Medicinal Food
2012 Volume.15 No. 4 p.369 ~ p.377
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Inhibition of Nuclear Transcription Factor-κB and Activation of Peroxisome Proliferator-Activated Receptors in HepG2 Cells by Cucurbitane-Type Triterpene Glycosides from Momordica charantia
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Nhiem Nguyen Xuan
Yen Pham Hai
Ngan Nguyen Thi Thanh
Quang Tran Hong
Kiem Phan Van
Minh Chau Van
Tai Bui Huu
Cuong Nguyen Xuan
Song Seok-Bean
Kim Young-Ho
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Abstract
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Momordica charantia is used to treat various diseases, including inflammatory conditions. Previous reports indicated that the extract of this plant inhibits activation of nuclear transcription factor-κB (NF-κB) but activates peroxisome proliferator-activated receptor (PPAR). Additionally, cucurbitane-type triterpene glycosides are the main bioactive components of the fruit of M. charantia. Therefore, we investigated the anti-inflammatory activity of 17 cucurbitane-type triterpene glycosides (1?17) isolated from this plant. Their inhibition of NF-κB and activation of PPAR activities in HepG2 cells were measured using luciferase reporter and PPAR subtype transactivation assays. Compounds 6 and 8 were found to inhibit NF-κB activation stimulated by tumor necrosis factor-α (TNFα) in a dose-dependent manner. With 50% inhibition concentration (IC50) values of 0.4?μM, compounds 6 and 8 were more potent inhibitors than the positive control, sulfasalazine (IC50=0.9?μM). Compounds 4, 6, and 8 also inhibited TNFα-induced expressions of inducible nitric oxide synthase and cyclooxygenase-2 mRNA. However, only compound 13 significantly increased PPARγ transactivation.
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KEYWORD
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Cucurbitaceae, cucurbitane-type triterpene glycoside, Momordica charantia, nuclear transcription factor-κB, peroxisome proliferator-activated receptor γ
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