Lupenone Isolated from Adenophora triphylla var. japonica Extract Inhibits Adipogenic Differentiation through the Downregulation of PPARγ in 3T3‐L1 Cells

Abstract

Adenophora triphylla var. japonica (Campanulaceae) is known to have anti-inflammatory and anti-tussive effects. Dysfunction of adipocytes and adipose tissue in obesity is related to various inflammatory cytokines or adipokines. In this study, we investigated whether lupenone isolated from A. triphylla var. japonica extract inhibits adipocyte differentiation and expression of adipogenic marker genes in 3T3-L1 preadipocytes. We demonstrated that lupenone resulted in a significant reduction in lipid accumulation and expression of adipogenic marker genes in a dose-dependent manner. In addition, lupenone decreased the transcriptional activity of peroxisome proliferator-activated receptor γ (PPARγ) induced by troglitazone, and we also demonstrated that lupenone suppressed the PPARγ and CCAAT-enhancer-binding protein α (C/EBPα) protein levels. These findings demonstrated that lupenone isolated from A. triphylla var. japonica extract effectively inhibited adipocyte differentiation through downregulation of related transcription factor, particularly the PPARγ gene.

RP-HPLC Characterization of Lupenone and β-Sitosterol in Rhizoma Musae and Evaluation of the Anti-Diabetic Activity of Lupenone in Diabetic Sprague-Dawley Rats

“…Ba-jiao is a perennial herb, and when we measured the largest part of fresh Rhizoma Musae using a standard ruler, the obtained size (diameter) was used to represent the growth stage. The different growth stages (5,7,10,13,15, and 20 cm) of Rhizoma Musae collected at the same harvest time and origin displayed a range of lupenone and β-sitosterol levels. When the diameter of Rhizoma Musae was approximately 7-13 cm, lupenone content was higher.…”

“…Current studies have shown that lupenone and β-sitosterol possess multiple pharmacological activities. For example, in vitro studies have found that lupenone stimulates melanogenesis in B 16 murine melanoma cells [10], as well as inhibits α-glucosidase (α-Glu) and protein tyrosine phosphatase 1B (PTP1B) activities [11,12], Furthermore, lupenone inhibits adipogenic differentiation via downregulation of peroxisome proliferator-activated receptor PPARγ expression in 3T3-L1 cells [13]. Additionally, previous studies have reported that β-sitosterol inhibits the growth of HT-29 human colon cancer cells and induces apoptosis of LNCaP human prostate cancer cells in vitro [14,15].…”

Chemical Constituents of Hoya cagayanensis C. M. Burton

“…Lupenone (3) inhibits adipocyte differentiation by suppressing PPARγ and C/EBPα protein levels (Ahn and Oh, 2013). It also increases the tyrosinase enzyme expression via mitogen-activated protein kinase phosphorylated extracellular signal regulated kinases 1 and 2 phosphorylation inhibition which results to stimulation of melanogenesis.…”

Ethnobotany, Phytochemistry, Pharmacology of the Korean Campanulaceae: A Comprehensive Review

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