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| Targets |
Salvigenin targets multiple pathways: it inhibits acetylcholinesterase (AChE) activity, which may enhance cholinergic neurotransmission. It also modulates NF-κB and MAPK signaling, reducing pro-inflammatory cytokines. Salvigenin activates Nrf2, increasing antioxidant enzymes. In cancer, it induces apoptosis via mitochondrial pathways and inhibits cell proliferation by arresting cell cycle at G1 phase. Additionally, it inhibits α-glucosidase and pancreatic lipase, suggesting antidiabetic and anti-obesity potential.
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| ln Vitro |
H2O2-induced cell death is prevented in SH-SY5Y cells by salvigenin (0-100 μM, 3 hours) [1]. In H2O2-exposed SH-SY5Y cells, salvigenin (0-100 μM, 2 hours) dramatically lowers ROS generation, raises glutathione levels, lowers the degree of apoptosis, and enhances autophagy [1].
In vitro, salvigenin exhibits significant antioxidant activity by scavenging DPPH and ABTS radicals with IC50 values in the micromolar range. It inhibits AChE with an IC50 of approximately 50 μM. Salvigenin reduces LPS-induced NO and PGE2 production in macrophages, and decreases TNF-α and IL-6 levels. It induces apoptosis in various cancer cell lines (e.g., breast, colon, liver) with IC50 values of 10-50 μM. It also inhibits α-glucosidase activity, reducing glucose absorption. |
| ln Vivo |
In tumor-bearing mice, salvigenin (0-9.68 μg/mouse/day; intraperitoneal injection; 4 or 12 days) demonstrates immunomodulatory and anti-tumor properties [2].
In vivo, salvigenin has shown neuroprotective effects in scopolamine-induced memory impairment in rodents, improving cognitive performance and reducing oxidative stress in the brain. It also exhibits anti-inflammatory effects in carrageenan-induced paw edema models. In diabetic mice, salvigenin lowers blood glucose levels by inhibiting α-glucosidase. Anticancer efficacy has been demonstrated in xenograft models, where salvigenin reduces tumor volume. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for salvigenin include AChE inhibition assays using Ellman's method, where the enzyme reacts with acetylthiocholine and the product is measured spectrophotometrically. α-Glucosidase inhibition is assessed using p-nitrophenyl-α-D-glucopyranoside as substrate. COX-2 inhibition can be tested using a colorimetric COX assay. Antioxidant assays (DPPH, ABTS) are conducted to determine radical scavenging activity. No specific receptor binding assays are performed.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SY5Y cells exposed to H2O2 (300 μM) Tested Concentrations: 10, 25, 50 and 100 μM Incubation Duration: 3 hrs (hours) Experimental Results: SH-SY5Y cells (25 and 50μM optimal) protected from H2O2 Protection - Induces cell death. Apoptosis analysis [1] Cell Types: SY5Y cells were exposed to H2O2 (300 μM) Tested Concentrations: 10, 25, 50 and 100 μM Incubation Duration: 2 h Experimental Results: The degree of apoptosis induced by H2O2 was Dramatically diminished. Western Blot Analysis[1] Cell Types: SY5Y cells exposed to H2O2 (300 μM) Tested Concentrations: 10, 25, 50 and 100 μM Incubation Duration: 2 hrs (hours) Experimental Results: diminished cleaved caspase-3 and Bax/Bcl-2 ratio. Reduces caspase-12 and calpain levels. diminished levels of Atg7, Atg12 and LC3-II/LC3-I. In vitro cellular assays for salvigenin are performed using macrophages (RAW 264.7) for anti-inflammatory studies: cells are treated with salvigenin and stimulated with LPS, and NO, PGE2, and cytokines are measured. Neuroblastoma cells (e.g., SH-SY5Y) are used to assess neuroprotection against oxidative stress. Cancer cells are used for viability (MTT), apoptosis (annexin V), and cell cycle analysis by flow cytometry. Western blotting detects changes in signaling proteins such as NF-κB and Nrf2. |
| Animal Protocol |
Animal/Disease Models: Inbred female balb/c (Bagg ALBino) mouse, 6 to 8 weeks old, containing MCF-7 cells [2]
Doses: 3.65, 5.85, and 9.68 μg/mouse/day for 4 or 12 days Route of Administration: intraperitoneal (ip) injection Experimental Results: demonstrated a significant increase in DTH response in a dose-dependent manner. Dramatically diminished tumor growth rate, increased lymphocyte proliferation index, increased IFN-γ levels and diminished IL-4 production. Spleen CD4+CD25+Foxp3+ T lymphocytes were Dramatically diminished. In vivo animal experiments for salvigenin are conducted in rodent models. For memory impairment, mice are given salvigenin orally before scopolamine, and cognitive tests (Morris water maze, Y-maze) are performed. Inflammatory models: rats are treated with salvigenin and paw edema is induced by carrageenan. For antidiabetic, mice are fed a high-sugar diet and blood glucose is measured. In xenograft models, tumor-bearing mice receive salvigenin intraperitoneally, and tumor growth is monitored. |
| ADME/Pharmacokinetics |
Salvigenin has a molecular weight of 328.32 g/mol and a molecular formula of C18H16O6. It is a yellow crystalline solid, soluble in DMSO, ethanol, and methanol, but poorly soluble in water. Its logP suggests moderate lipophilicity. Pharmacokinetic studies in rats show oral bioavailability of about 20-30%, with a half-life of 3-5 hours. It is metabolized by glucuronidation and sulfation and excreted in urine and bile. The compound is stable under normal storage conditions.
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| Toxicity/Toxicokinetics |
Salvigenin has been evaluated for safety in preclinical studies. In acute toxicity tests in mice, oral doses up to 1000 mg/kg showed no mortality or significant adverse effects. Subacute toxicity studies are limited, but no major organ damage has been reported. The compound has low cytotoxicity in normal cell lines, indicating a good selectivity index. However, long-term safety and genotoxicity have not been fully assessed. It is considered safe for research use.
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| References | |
| Additional Infomation |
Salvigenin is a trimethoxyflavonoid, a derivative of baicalin, with its 4', 6, and 7-hydroxyl groups replaced by methoxy groups. It possesses various functions, including inducing autophagy, inhibiting apoptosis, lowering blood lipids, immunomodulation, antitumor activity, neuroprotection, hypoglycemia, and as a plant metabolite. It is a trimethoxyflavonoid and monohydroxyflavonoid, functionally related to baicalin. Salvigenin has been found in Salvigenin, nettle, and other organisms with relevant data. See also: Orange peel (partial).
Salvigenin is a natural flavonoid with promising pharmacological activities, including neuroprotective, anti-inflammatory, antidiabetic, and anticancer effects. It is found in sage and other medicinal plants. Salvigenin's mechanism involves inhibition of AChE, modulation of NF-κB and Nrf2, and induction of apoptosis. It has attracted research interest for its potential in treating Alzheimer's disease, diabetes, and cancer. However, it is not an approved drug and requires further development. Its natural abundance makes it a candidate for phytopharmaceutical applications. |
| Molecular Formula |
C18H16O6
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| Molecular Weight |
328.3160
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| Exact Mass |
328.094
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| CAS # |
19103-54-9
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| Related CAS # |
Salvigenin-d9
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| PubChem CID |
161271
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
535.9±50.0 °C at 760 mmHg
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| Flash Point |
196.9±23.6 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
3.01
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QCDYOIZVELGOLZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16O6/c1-21-11-6-4-10(5-7-11)13-8-12(19)16-14(24-13)9-15(22-2)18(23-3)17(16)20/h4-9,20H,1-3H3
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| Chemical Name |
5-hydroxy-6,7-dimethoxy-2-(4-methoxyphenyl)chromen-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~20 mg/mL (~60.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (6.09 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0458 mL | 15.2290 mL | 30.4581 mL | |
| 5 mM | 0.6092 mL | 3.0458 mL | 6.0916 mL | |
| 10 mM | 0.3046 mL | 1.5229 mL | 3.0458 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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