Desoxyrhaponticin是一种来自rhubarb的stilbene glycoside，是强效的BACE1抑制剂，IC50值为1.213µM。
Cas No.:30197-14-9
Sample solution is provided at 25 µL, 10mM.
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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.
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]。
| Cell experiment [1]: | |
Cell lines | H1299 cells |
Preparation Method | H1299 cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), 100U/ml penicillin and 100μg/ml streptomycin at 37°C in 5% CO2/atmosphere. H1299 cells (3×103 cells) were seeded on 96-well plates, incubated for 24h, and then treated with different concentrations of Desoxyrhaponticin (0, 10, 20, 40, 80, 160, 320 and 640µM) at 37°C. After 4 days, cell viability was measured. |
Reaction Conditions | 0, 10, 20, 40, 80, 160, 320 and 640µM; 4 days |
Applications | Desoxyrhaponticin treatment significantly reduced the cell viability of H1299 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Neonatal Wistar rats were injected with streptozotocin (STZ) i.p. (100mg/kg in 50mM citrate buffer, pH 4.5) on the first day of birth. Mice were weaned 21 days after birth, housed in stainless steel wire cages, and given standard laboratory chow and tap water ad libitum. After 2h of fasting of the 12-week-old diabetic rats, an oral glucose tolerance test (OGTT) was performed. Glucose (2g/kg) was orally administered to the diabetic rats as a 0.4g/ml glucose solution. Desoxyrhaponticin was administered to the mice (300mg/kg; p.o.) in a 50% PEG 400 solution just before the glucose loading. Mice in the untreated diabetic group were given the 50% PEG 400 solution as the solvent control. Blood samples were collected from the tip of the rats’ tails before the glucose administration and at different times afterwards up to 120min. The plasma glucose level was measured. |
Dosage form | 300mg/kg for once; p.o. |
Applications | Desoxyrhaponticin treatment significantly reduced postprandial hyperglycemia in diabetic rats. |
References: | |
| Cas No. | 30197-14-9 | SDF | |
| 别名 | 脱氧土大黄苷 | ||
| Canonical SMILES | COC(C=C1)=CC=C1/C=C/C2=CC(O)=CC(O[C@@H]3O[C@@H]([C@@H](O)[C@H](O)[C@H]3O)CO)=C2 | ||
| 分子式 | C21H24O8 | 分子量 | 404.41 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4727 mL | 12.3637 mL | 24.7274 mL |
| 5 mM | 494.5 μL | 2.4727 mL | 4.9455 mL |
| 10 mM | 247.3 μL | 1.2364 mL | 2.4727 mL |
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