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| Targets |
The targets of Oroxin A include insulin signaling-related proteins (e.g., p-AKT, GLUT4) and pro-inflammatory factors (e.g., TNF-α, IL-6) [1]
The targets of Oroxin A include endoplasmic reticulum (ER) stress-related proteins (e.g., GRP78, CHOP) and senescence-related proteins (e.g., p16, p21) [2] |
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| ln Vitro |
In HEK-293t cells, oroxin A (0.5-100 μM; 24 hours) dramatically raises PPARγ transcription levels, with a dose of 50 μM showing the greatest activation effect [1].
1. Improvement of insulin resistance in HepG2 cells (Reference [1]): Insulin-resistant HepG2 cells (induced by 100 nM insulin for 24 hours) were treated with Oroxin A (5, 10, 20 μM) for 12 hours. 2-NBDG fluorescence assay showed Oroxin A dose-dependently increased glucose uptake: 20 μM increased it by 45% compared to the insulin-resistant control. Western blot showed 20 μM Oroxin A upregulated p-AKT (Ser473) by 2.2-fold and GLUT4 by 1.8-fold, and downregulated TNF-α and IL-6 mRNA by 50% and 55% (qPCR) [1] 2. Antiproliferative activity in breast cancer cells (Reference [2]): Oroxin A (10, 20, 30, 40 μM) was treated with MCF-7 (ER-positive) and MDA-MB-231 (triple-negative) breast cancer cells for 48 hours. MTT assay showed IC50 values of 25 μM (MCF-7) and 30 μM (MDA-MB-231). Clone formation assay showed 30 μM Oroxin A reduced colony numbers by 65% (MCF-7) and 60% (MDA-MB-231) [2] 3. Induction of ER stress and senescence in breast cancer cells (Reference [2]): Western blot showed 30 μM Oroxin A upregulated ER stress markers (GRP78 by 2.5-fold, CHOP by 3.0-fold) and senescence markers (p16 by 2.3-fold, p21 by 2.0-fold) in MCF-7 cells. β-Galactosidase staining showed 30 μM Oroxin A increased senescent cell ratio from 5% to 45% [2] |
| ln Vivo |
1. Prevention of prediabetes progression to diabetes in mice (Reference [1]): C57BL/6 mice were induced to prediabetes by streptozotocin (STZ, 40 mg/kg, intraperitoneal, 5 days) + high-fat diet (HFD, 60% fat calories) for 4 weeks. Mice were divided into 3 groups (n=8): (1) Model control (0.5% CMC); (2) Oroxin A 10 mg/kg; (3) Oroxin A 20 mg/kg (oral gavage, once daily, 8 weeks). The 20 mg/kg group showed: (1) Fasting blood glucose reduced from 8.5 mmol/L to 6.2 mmol/L; (2) Insulin tolerance test (ITT) AUC reduced by 35%; (3) Hepatic TNF-α and IL-6 protein levels reduced by 45% and 50%; (4) Hepatic p-AKT and GLUT4 increased by 1.9-fold and 1.7-fold (Western blot) [1]
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| Enzyme Assay |
1. Glucose uptake assay (Reference [1]): Insulin-resistant HepG2 cells were seeded in 96-well plates. After treating with Oroxin A (5-20 μM) for 12 hours, 100 μL of 2-NBDG (100 μM) was added and incubated at 37°C for 30 minutes. Cells were washed with PBS 3 times, and fluorescence intensity (excitation 485 nm, emission 535 nm) was measured to quantify glucose uptake [1]
2. ER stress-related protein detection (Reference [2]): MCF-7 cells treated with Oroxin A (10-40 μM) for 24 hours were lysed with RIPA buffer. 30 μg of protein was separated by SDS-PAGE, transferred to PVDF membrane, and incubated with primary antibodies (GRP78, CHOP, β-actin) overnight at 4°C. After secondary antibody incubation, ECL reagent was used for chemiluminescence, and band density was quantified by ImageJ [2] |
| Cell Assay |
1. Insulin-resistant HepG2 cell assay (Reference [1]): HepG2 cells were cultured in DMEM + 10% FBS at 37°C, 5% CO₂. To induce insulin resistance, cells were treated with 100 nM insulin for 24 hours. Then Oroxin A (5-20 μM) was added and cultured for 12 hours. Glucose uptake was detected by 2-NBDG assay, and protein/mRNA expression was detected by Western blot/qPCR [1]
2. Breast cancer cell proliferation and senescence assay (Reference [2]): MCF-7/MDA-MB-231 cells were cultured in RPMI 1640 + 10% FBS. For MTT assay: cells were seeded in 96-well plates, treated with Oroxin A (10-40 μM) for 48 hours, added with MTT (5 mg/mL) and incubated for 4 hours, then dissolved in DMSO and measured at 570 nm. For senescence assay: cells were treated with 30 μM Oroxin A for 72 hours, fixed with 4% paraformaldehyde, stained with β-galactosidase staining solution at 37°C overnight, and senescent cells (blue) were counted [2] |
| Animal Protocol |
1. Prediabetic mouse model and drug administration (Reference [1]): 6-week-old male C57BL/6 mice were fed HFD for 1 week, then injected with STZ (40 mg/kg, intraperitoneal) once daily for 5 days. After 4 weeks, mice with fasting blood glucose 6.1-7.0 mmol/L were defined as prediabetic. Oroxin A was dissolved in 0.5% carboxymethyl cellulose (CMC) to concentrations of 1 mg/mL and 2 mg/mL. Mice were given oral gavage of 10 mg/kg or 20 mg/kg Oroxin A once daily for 8 weeks; the model group received 0.5% CMC [1]
2. Sample collection and detection (Reference [1]): After 8 weeks of administration, mice were fasted for 12 hours, blood was collected via orbital venous plexus to detect fasting blood glucose and insulin. Livers were excised, part was fixed in 4% paraformaldehyde for histological analysis, and part was homogenized for Western blot/qPCR to detect insulin signaling proteins and inflammatory factors [1] |
| Toxicity/Toxicokinetics |
1. In vivo safety (Reference [1]): No mouse deaths were observed during the 8-week oral treatment with Oroxin A (10, 20 mg/kg). The body weight (28.5 ± 1.2 g) of the 20 mg/kg group was not significantly different from that of the model group (27.8 ± 1.0 g). Serum ALT (26 ± 4 U/L), AST (70 ± 6 U/L), and creatinine (42 ± 5 μmol/L) of the 20 mg/kg group were all within the normal range [1]. 2. In vitro safety (Reference [2]): Oroxin A (at concentrations up to 40 μM) had no significant cytotoxicity to normal human mammary epithelial cells (MCF-10A), with cell viability >85% (MTT assay) [2].
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| References |
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| Additional Infomation |
According to reports, Oroxin A is found in Scutellaria comosa, Scutellaria immaculata, and other organisms with relevant data.
1. Source and structure (References [1][2]): Oroxin A is a flavonoid compound isolated from the seeds of Oroxylum indicum, a traditional Chinese medicine plant, commonly known as "wood butterfly" [1][2] 2. Mechanism of action: (1) In prediabetes: Oroxin A improves insulin sensitivity by activating the AKT-GLUT4 signaling pathway and inhibiting systemic inflammation [1]; (2) In breast cancer: it inhibits cell proliferation by inducing strong endoplasmic reticulum stress (upregulating GRP78/CHOP) and cellular senescence (upregulating p16/p21) [2] 3. Therapeutic potential: Oroxin A shows potential in preventing the progression of prediabetes to type 2 diabetes and in treating ER-positive/triple-negative breast cancer [1][2] |
| Molecular Formula |
C21H20O10
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|---|---|
| Molecular Weight |
432.3775
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| Exact Mass |
432.105
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| CAS # |
57396-78-8
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| PubChem CID |
5320313
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
784.0±60.0 °C at 760 mmHg
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| Flash Point |
279.0±26.4 °C
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| Vapour Pressure |
0.0±2.9 mmHg at 25°C
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| Index of Refraction |
1.717
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| LogP |
0.47
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
677
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC=C(C=C1)C2=CC(=O)C3=C(C(=C(C=C3O2)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O
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| InChi Key |
IPQKDIRUZHOIOM-IAAKTDFRSA-N
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| InChi Code |
InChI=1S/C21H20O10/c22-8-14-17(25)19(27)20(28)21(31-14)30-13-7-12-15(18(26)16(13)24)10(23)6-11(29-12)9-4-2-1-3-5-9/h1-7,14,17,19-22,24-28H,8H2/t14-,17-,19+,20-,21-/m1/s1
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| Chemical Name |
5,6-dihydroxy-2-phenyl-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~289.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3128 mL | 11.5639 mL | 23.1278 mL | |
| 5 mM | 0.4626 mL | 2.3128 mL | 4.6256 mL | |
| 10 mM | 0.2313 mL | 1.1564 mL | 2.3128 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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