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| 5mg |
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| 10mg |
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| Targets |
Chrysosplenol D targets multiple cellular pathways. It induces ERK1/2-mediated apoptosis in triple-negative breast cancer cells. The compound also has anti-inflammatory effects by suppressing LPS-induced release of IL-1 beta, IL-6, and MCP-1 in Raw264.7 cells. It exerts its anti-proliferative effect through inhibiting cell cycle and inducing apoptosis. The compound has moderate antitrypanosomal activity.
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| ln Vitro |
Chrysosplenol D has an IC50 of 63.48 μM, which inhibits the viability of CaCo2 cells[1]. The viability of TNBC cell lines MDA-MB-231, CAL-51, CAL-148, as well as MCF7, A549, MIA PaCa-2, and PC-3, is selectively inhibited by chyrosplenol D (1-100 μM; 48 h) [2]. Chrysosplenol D (1–10 μM; 48 h) causes aberrant cell cycle behaviors, such as cells aggregating in the S phase and a portion of the G2/M phase [2]. Breast cancer cells undergo apoptosis when exposed to chyrosplenol D (1–10 μM; 48 h) [2]. With an IC50 of 47.27 μM against Tb brucei, chysosplenol D exhibits moderate antitrypanosome activity [3].
In vitro studies demonstrate that chrysosplenol D induces ERK1/2-mediated apoptosis in triple-negative human breast cancer cells. It suppresses LPS-induced release of IL-1 beta, IL-6, and MCP-1 in Raw264.7 cells, inhibiting inflammation in vitro. The compound exerts its anti-proliferative effect on tsFT210 cells through inhibiting cell cycle and inducing apoptosis. It has anti-inflammatory, antimalarial, antibacterial, and antifungal activities. |
| ln Vivo |
On chicken chorioallantoic membrane, chyrosplenol D (30 μM; 3 d) inhibits the growth of MDA-MB-231 tumors [2]. In mice, LPS-induced systemic inflammatory response syndrome (SIRS) is prevented by chyrosplenol D (0.07-0.28 mmol/kg) [4]. Croton oil-induced ear edema in mice is inhibited by chyrosplenol D (1-1.5 μMol/cm2) [4].
In vivo, chrysosplenol D inhibits inflammation. The compound has been shown to suppress LPS-induced release of inflammatory cytokines, indicating anti-inflammatory activity in vivo. It also has moderate antitrypanosomal activity. Further studies would be needed to evaluate its efficacy in other disease models. The compound's anti-inflammatory, antimalarial, antibacterial, and antifungal activities suggest potential for various therapeutic applications. |
| Enzyme Assay |
The anti-inflammatory activity of chrysosplenol D can be assessed using LPS-stimulated Raw264.7 macrophages. Cells are treated with varying concentrations of chrysosplenol D and stimulated with LPS. The release of pro-inflammatory cytokines (IL-1 beta, IL-6, MCP-1) is measured by ELISA. The anti-proliferative effect is assessed using tsFT210 cells. Apoptosis is measured by annexin V/propidium iodide staining or caspase activation assays. Cell cycle analysis is performed using flow cytometry.
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| Cell Assay |
The cellular activity of chrysosplenol D is assessed using various cell lines including triple-negative breast cancer cells, Raw264.7 macrophages, and tsFT210 cells. Cells are treated with varying concentrations of chrysosplenol D. Cell viability is measured using MTT assays. Apoptosis is assessed by annexin V/propidium iodide staining or caspase activation assays. ERK1/2 phosphorylation is assessed by Western blotting. Cytokine release is measured by ELISA.
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| Animal Protocol |
Chrysosplenol D has been evaluated in animal models of inflammation. In these studies, the compound is administered at various doses. Inflammatory markers are measured. The compound inhibits LPS-induced inflammation in vivo. Its anti-inflammatory, antimalarial, antibacterial, and antifungal activities suggest potential for various in vivo applications. Further studies would be needed to evaluate its efficacy in other disease models.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for chrysosplenol D. The compound has a molecular weight of 360.3 g/mol and a molecular formula of C18H16O8. It has a melting point of 236-238 °C and a boiling point of 645.0±55.0 °C. It is soluble in chloroform, dichloromethane, ethyl acetate, DMSO, and acetone. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for chrysosplenol D. As a natural flavonoid, it may have a favorable safety profile. The compound is intended for research use only. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. Its anti-inflammatory and anti-proliferative activities suggest that it may have beneficial effects, but off-target effects would need to be assessed.
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| References |
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| Additional Infomation |
3',4',5-Trihydroxy-3,6,7-Trimethoxyflavonoid is a trimethoxyflavonoid, a 3,6,7-trimethyl ether derivative of quercetin. It possesses antitumor activity and is also a metabolite. It is a trihydroxyflavonoid and a trimethoxyflavonoid, functionally related to quercetin. Hypericin D has been reported in Acanthospermum australe, Chrysosplenium grayanum, and other organisms with relevant data. See also: Vitex negundo fruit (partial).
Chrysosplenol D (CAS# 14965-20-9) is a methoxyflavonoid that induces ERK1/2-mediated apoptosis in triple-negative breast cancer cells. It suppresses LPS-induced release of IL-1 beta, IL-6, and MCP-1, inhibiting inflammation in vitro and in vivo. The compound exerts anti-proliferative effects through cell cycle inhibition and apoptosis induction. It has anti-inflammatory, antimalarial, antibacterial, antifungal, and moderate antitrypanosomal activities. The molecular formula is C18H16O8. The compound is also known as 5,3',4'-trihydroxy-3,6,7-trimethoxyflavone. |
| Molecular Formula |
C18H16O8
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| Molecular Weight |
360.31
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| Exact Mass |
360.084
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| CAS # |
14965-20-9
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| PubChem CID |
5280699
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
645.0±55.0 °C at 760 mmHg
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| Flash Point |
237.3±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.680
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| LogP |
2.29
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BYWLLSQTJBXAPV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16O8/c1-23-12-7-11-13(14(21)17(12)24-2)15(22)18(25-3)16(26-11)8-4-5-9(19)10(20)6-8/h4-7,19-21H,1-3H3
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| Chemical Name |
2-(3,4-dihydroxyphenyl)-5-hydroxy-3,6,7-trimethoxychromen-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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : 50 mg/mL (138.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.94 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 25.0 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 | 2.7754 mL | 13.8769 mL | 27.7539 mL | |
| 5 mM | 0.5551 mL | 2.7754 mL | 5.5508 mL | |
| 10 mM | 0.2775 mL | 1.3877 mL | 2.7754 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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