PMID- 22248180
OWN - NLM
STAT- MEDLINE
DCOM- 20120716
LR  - 20211021
IS  - 1557-7600 (Electronic)
IS  - 1096-620X (Print)
IS  - 1096-620X (Linking)
VI  - 15
IP  - 4
DP  - 2012 Apr
TI  - Inhibition of nuclear transcription factor-kappaB and activation of peroxisome 
      proliferator-activated receptors in HepG2 cells by cucurbitane-type triterpene 
      glycosides from Momordica charantia.
PG  - 369-77
LID - 10.1089/jmf.2011.1766 [doi]
AB  - 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-kappaB (NF-kappaB) 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-kappaB 
      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-kappaB activation stimulated by tumor necrosis factor-alpha (TNFalpha) in a 
      dose-dependent manner. With 50% inhibition concentration (IC(50)) values of 
      0.4 muM, compounds 6 and 8 were more potent inhibitors than the positive control, 
      sulfasalazine (IC(50)=0.9 muM). Compounds 4, 6, and 8 also inhibited TNFalpha-induced 
      expressions of inducible nitric oxide synthase and cyclooxygenase-2 mRNA. 
      However, only compound 13 significantly increased PPARgamma transactivation.
FAU - Nhiem, Nguyen Xuan
AU  - Nhiem NX
AD  - College of Pharmacy, Chungnam National University, Daejeon, Korea.
FAU - Yen, Pham Hai
AU  - Yen PH
FAU - Ngan, Nguyen Thi Thanh
AU  - Ngan NT
FAU - Quang, Tran Hong
AU  - Quang TH
FAU - Kiem, Phan Van
AU  - Kiem PV
FAU - Minh, Chau Van
AU  - Minh CV
FAU - Tai, Bui Huu
AU  - Tai BH
FAU - Cuong, Nguyen Xuan
AU  - Cuong NX
FAU - Song, Seok Bean
AU  - Song SB
FAU - Kim, Young Ho
AU  - Kim YH
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20120116
PL  - United States
TA  - J Med Food
JT  - Journal of medicinal food
JID - 9812512
RN  - 0 (Anti-Inflammatory Agents)
RN  - 0 (Glycosides)
RN  - 0 (NF-kappa B)
RN  - 0 (PPAR gamma)
RN  - 0 (Peroxisome Proliferator-Activated Receptors)
RN  - 0 (Plant Extracts)
RN  - 0 (RNA, Messenger)
RN  - 0 (Triterpenes)
RN  - 0 (Tumor Necrosis Factor-alpha)
RN  - 0 (cucurbitane)
RN  - EC 1.13.12.- (Luciferases)
RN  - EC 1.14.13.39 (Nitric Oxide Synthase Type II)
RN  - EC 1.14.99.1 (Cyclooxygenase 2)
RN  - EC 1.14.99.1 (PTGS2 protein, human)
SB  - IM
MH  - Anti-Inflammatory Agents/*pharmacology
MH  - Cyclooxygenase 2/genetics/metabolism
MH  - Gene Expression Regulation/drug effects
MH  - Glycosides/*pharmacology
MH  - Hep G2 Cells
MH  - Humans
MH  - Inhibitory Concentration 50
MH  - Luciferases/metabolism
MH  - Momordica charantia/*chemistry
MH  - NF-kappa B/*antagonists & inhibitors/metabolism
MH  - Nitric Oxide Synthase Type II/genetics/metabolism
MH  - PPAR gamma/metabolism
MH  - Peroxisome Proliferator-Activated Receptors/*metabolism
MH  - Plant Extracts/*pharmacology
MH  - RNA, Messenger/metabolism
MH  - Triterpenes/*pharmacology
MH  - Tumor Necrosis Factor-alpha/antagonists & inhibitors/metabolism
PMC - PMC3308713
EDAT- 2012/01/18 06:00
MHDA- 2012/07/17 06:00
PMCR- 2013/04/01
CRDT- 2012/01/18 06:00
PHST- 2012/01/18 06:00 [entrez]
PHST- 2012/01/18 06:00 [pubmed]
PHST- 2012/07/17 06:00 [medline]
PHST- 2013/04/01 00:00 [pmc-release]
AID - 10.1089/jmf.2011.1766 [pii]
AID - 10.1089/jmf.2011.1766 [doi]
PST - ppublish
SO  - J Med Food. 2012 Apr;15(4):369-77. doi: 10.1089/jmf.2011.1766. Epub 2012 Jan 16.