Desoxyrhaponticin, a stilbene glycoside from rhubarb, is a potent BACE1 inhibitor with an IC50 value of 1.213µM [1]. Desoxyrhaponticin improves insulin resistance (IR) and reduces lipid accumulation through the PI3K/AKT/mTOR signaling pathway[2]. Desoxyrhaponticin is widely used as an internal standard to develop high-speed counter-current chromatography (HSCCC) methods for the large-scale separation and identification of related compounds[3].
In vitro, Desoxyrhaponticin treatment for 4 days significantly inhibited the proliferation of H1299 cells and HBE cells, with IC50 values of 86.68µM and 58.83µM, respectively[4]. Treatment with 400µM Desoxyrhaponticin for 24 hours strongly inhibited the expression of Fatty acid synthase (FAS) in MCF-7 cells and the activity of FAS within the cells, and promoted cell apoptosis[5]. Treatment with 10µM Desoxyrhaponticin for 48 hours significantly inhibited the accumulation of triglycerides (TG) in 3T3-L1 preadipocytes and increased the level of PPARγ[6].
In vivo, Desoxyrhaponticin treatment via a single oral administration at a dose of 300mg/kg for 2 hours significantly reduced postprandial hyperglycemia in diabetic rats[7].
References:
[1] Oh J M, Kim S H, Pandey B P, et al. A stilbenoid, rhapontigenin, isolated from the root of Rheum palmatum L. acts as a potent BACE1 inhibitor[J]. Fitoterapia, 2025, 182: 106484.
[2] Gao Y, Wu Y, Tie F, et al. Stilbenoids from fenugreek seeds alleviate insulin resistance by regulating the PI3K/AKT/mTOR signaling pathway in a type 2 diabetes zebrafish model[J]. Heliyon, 2024, 10(13).
[3] Wang X, Wang H, Ding C, et al. One‐step preparative separation of two polyhydroxystilbenes from Rheum likiangense sam. by high‐speed counter‐current chromatography[J]. Phytochemical Analysis, 2012, 23(6): 684-688.
[4] Fan M, Liu Q, Ma X, et al. ZNF131-BACH1 transcriptionally accelerates RAD51-dependent homologous recombination repair and therapy-resistance of non-small-lung cancer cells by preventing their degradation from CUL3[J]. Theranostics, 2024, 14(18): 7241.
[5] Li P, Tian W, Wang X, et al. Inhibitory effect of desoxyrhaponticin and rhaponticin, two natural stilbene glycosides from the Tibetan nutritional food Rheum tanguticum Maxim. ex Balf., on fatty acid synthase and human breast cancer cells[J]. Food & function, 2014, 5(2): 251-256.
[6] Li G, Luan G, He Y, et al. Polyphenol Stilbenes from Fenugreek (Trigonella foenum-graecum L.) Seeds Improve Insulin Sensitivity and Mitochondrial Function in 3T3‐L1 Adipocytes[J]. Oxidative Medicine and Cellular Longevity, 2018, 2018(1): 7634362.
[7] Li J M, Che C T, Lau C B S, et al. Desoxyrhaponticin (3, 5-dihydroxy-4′-methoxystilbene 3-O-β-d-glucoside) inhibits glucose uptake in the intestine and kidney: In vitro and in vivo studies[J]. The Journal of pharmacology and experimental therapeutics, 2007, 320(1): 38-46.
Desoxyrhaponticin是一种来自rhubarb的stilbene glycoside，是强效的BACE1抑制剂，IC50值为1.213µM[1]。Desoxyrhaponticin通过PI3K/AKT/mTOR信号通路改善胰岛素抵抗并减少脂质积累[2]。Desoxyrhaponticin被广泛用作内标，用于开发高速逆流色谱(HSCCC)方法，以大规模分离和鉴定相关化合物[3]。
在体外，Desoxyrhaponticin处理4天显著抑制了H1299细胞和HBE细胞的增殖，IC50值分别为86.68µM和58.83µM[4]。400µM的Desoxyrhaponticin处理MCF-7细胞24小时，强烈抑制了脂肪酸合酶(FAS)的表达和细胞内FAS的活性，并促进了细胞凋亡[5]。10µM的Desoxyrhaponticin处理3T3-L1前脂肪细胞48小时，显著抑制了甘油三酯(TG)的积累并提高了PPARγ的水平[6]。
在体内，单次口服300mg/kg剂量的Desoxyrhaponticin 2小时，显著降低了糖尿病大鼠的餐后高血糖[7]。