Desoxyrhaponticin, a stilbene glycoside from rhubarb, is a potent BACE1 inhibitor with an IC50 value of 1.213µM.

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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.

Protocol

Chemical Properties

Complete Stock Solution Preparation Table