Chrysosplenetin

Name: Chrysosplenetin
Brand: MedChemExpress
SKU: HY-N1457
Rating: 5.0 (3 reviews)

Cat. No.: HY-N1457 Purity: 99.84%: Data Sheet
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Chrysosplenetin is an orally active polymethoxyflavone. Chrysosplenetin exerts anticancer effects by inhibiting topoisomerase, protecting DNA and inducing apoptosis. Chrysosplenetin acts as an antimalarial sensitizer, reverses Artemisinin (HY-B0094) resistance by inhibiting and downregulating P-glycoprotein, and enhances the efficacy of Artemisinin. Chrysosplenetin promotes bone formation by activating the Wnt/β-catenin pathway and exerts anti-osteoporotic effects.

For research use only. We do not sell to patients.

Chrysosplenetin Chemical Structure

CAS No. : 603-56-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
20 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE Chrysosplenetin

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CYP3A

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against epidermoid carcinoma cell line In vitro cytotoxicity against epidermoid carcinoma cell line	[PMID: 8182705]
A-431	ED₅₀	0.33 μM Compound: 70	Antiproliferative activity against human A431 cells assessed as reduction in cell viability Antiproliferative activity against human A431 cells assessed as reduction in cell viability	[PMID: 30830783]
Col2	IC₅₀	> 10 μM Compound: 70	Antiproliferative activity against human Col2 cells assessed as reduction in cell viability Antiproliferative activity against human Col2 cells assessed as reduction in cell viability	[PMID: 30830783]
Colon carcinoma cell	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against colon cancer cell line In vitro cytotoxicity against colon cancer cell line	[PMID: 8182705]
Fibrosarcoma cell line	EC₅₀	4.2 μg/mL Compound: 4	In vitro cytotoxicity against fibrosarcoma cell line In vitro cytotoxicity against fibrosarcoma cell line	[PMID: 8182705]
HT	ED₅₀	0.33 μM Compound: 70	Antiproliferative activity against human HT cells assessed as reduction in cell viability Antiproliferative activity against human HT cells assessed as reduction in cell viability	[PMID: 30830783]
HT-29	IC₅₀	14.2 μM Compound: 4	Compound was tested for cytotoxicity against colon adenocarcinoma Compound was tested for cytotoxicity against colon adenocarcinoma	[PMID: 8182705]
HT-29	IC₅₀	> 10 μM Compound: 70	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability	[PMID: 30830783]
KB	EC₅₀	0.8 μg/mL Compound: 4	In vitro cytotoxicity against vinblastine resistant KB cell line In vitro cytotoxicity against vinblastine resistant KB cell line	[PMID: 8182705]
KB	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against oral epidermoid carcinoma cell line In vitro cytotoxicity against oral epidermoid carcinoma cell line	[PMID: 8182705]
KB	ED₅₀	0.33 μM Compound: 70	Antiproliferative activity against human KB/HeLa cells assessed as reduction in cell viability Antiproliferative activity against human KB/HeLa cells assessed as reduction in cell viability	[PMID: 30830783]
KB	ED₅₀	7.42 μg/mL Compound: chrysosplenol B	Cytotoxicity against human KB cells after 72 hrs Cytotoxicity against human KB cells after 72 hrs	[PMID: 1955888]
KB	IC₅₀	> 47.8 μM Compound: 11	Cytotoxicity against human KB cells by sulforhodamine B assay Cytotoxicity against human KB cells by sulforhodamine B assay	[PMID: 26928423]
KB-V1	ED₅₀	2.14 μM Compound: 70	Antiproliferative activity against human KBV1 cells assessed as reduction in cell viability Antiproliferative activity against human KBV1 cells assessed as reduction in cell viability	[PMID: 30830783]
Lung cancer cell line	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against lung cancer cell line In vitro cytotoxicity against lung cancer cell line	[PMID: 8182705]
P388	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against murine lymphoid neoplasm cell line In vitro cytotoxicity against murine lymphoid neoplasm cell line	[PMID: 8182705]
P388	ED₅₀	0.33 μM Compound: 70	Antiproliferative activity against mouse P388 cells assessed as reduction in cell viability Antiproliferative activity against mouse P388 cells assessed as reduction in cell viability	[PMID: 30830783]
SK-OV-3	IC₅₀	79 μM Compound: 4	Compound was tested for cytotoxicity against ovarian adenocarcinoma, multidrug resistant Compound was tested for cytotoxicity against ovarian adenocarcinoma, multidrug resistant	[PMID: 8182705]
SK-VLB	IC₅₀	> 133 μM Compound: 4	Compound was tested for cytotoxicity against colon adenocarcinoma Compound was tested for cytotoxicity against colon adenocarcinoma	[PMID: 8182705]
U-373MG ATCC	EC₅₀	> 20 μg/mL Compound: 4	In vitro cytotoxicity against glioblastoma cell line In vitro cytotoxicity against glioblastoma cell line	[PMID: 8182705]
U-373MG ATCC	ED₅₀	0.33 μM Compound: 70	Antiproliferative activity against human U373 cells assessed as reduction in cell viability Antiproliferative activity against human U373 cells assessed as reduction in cell viability	[PMID: 30830783]
Vero	IC₅₀	> 47.8 μM Compound: 11	Cytotoxicity against African green monkey Vero cells by sulforhodamine B assay Cytotoxicity against African green monkey Vero cells by sulforhodamine B assay	[PMID: 26928423]

In Vitro

Chrysosplenetin (6.06 μM) slightly enhances the transcriptional activities of PXR and CAR in human colorectal cancer LS174T cells^[1].
Chrysosplenetin (72 h) potently inhibits the proliferation of MCF-7 breast cancer cells, with an IC₅₀ of 0.3 μM after 72 h of incubation^[2].
Chrysosplenetin (12.5-100 μM; 1 h) protects supercoiled pBR322 plasmid DNA against Fenton reagent-induced oxidative damage in a concentration-dependent manner^[2].
Chrysosplenetin (20 μM; 6 h) inhibits P-gp-mediated artemisinin efflux in P-gp-overexpressing Caco-2 cells, increases the apical-to-basolateral permeability of artemisinin and reduces its efflux ratio^[3].
Chrysosplenetin (5-20 μM; 1-14 days) promotes the proliferation of hBMSCs in a time-dependent manner^[4].
Chrysosplenetin (5-20 μM; 14 days) promotes mineral deposition in hBMSCs^[4].
Chrysosplenetin (5-20 μM; 14 days) upregulates the expression of osteoblast marker genes (RUNX2, BGLAP, CTNNB1, BMP2) in hBMSCs after 14 days of treatment^[4].
Chrysosplenetin (10 μM; 3-14 days) activates the expression of Wnt/β-catenin pathway target genes (CTNNB1, TCF7, LEF1, CCND1, JUN, c-MYC) in hBMSCs^[4].
Chrysosplenetin (10 μM; 3-14 days) upregulates the expression of osteogenic downstream genes (RUNX2, DLX5, SPP1, COL1, BGLAP, BMP2) in human bone marrow mesenchymal stem cells (hBMSCs)^[4].
Chrysosplenetin (10 μM; 3-14 days) upregulates the expression level of total β-catenin protein and downregulates the expression of p-β-catenin protein in hBMSCs at a concentration of 10 μM^[4].
Chrysosplenetin (10 μM) promotes the nuclear translocation of β-catenin in hBMSCs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:	human bone marrow stromal cells (hBMSCs)
Concentration:	5, 10 and 20 μM
Incubation Time:	1, 2, 3, 7, 14 days
Result:	Promoted hBMSC proliferation in a time-dependent manner, with the maximal positive effect achieved at 10 μM.

Real Time qPCR^[4]

Cell Line:	hBMSCs
Concentration:	5, 10 and 20 μM
Incubation Time:	14 days
Result:	Significantly increased mRNA expression levels of RUNX2, BGLAP (Osteocalcin), CTNNB1 (β-catenin), and BMP2 in a non-dose-dependent manner, with maximal increases observed at 10 μM.

Real Time qPCR^[4]

Cell Line:	hBMSCs
Concentration:	10 μM
Incubation Time:	3, 7, 14 days
Result:	Significantly elevated mRNA levels of CTNNB1, TCF7, LEF1, CCND1 (cyclin D), JUN (c-JUN), and c-MYC relative to untreated controls at 3, 7, and 14 days.\nSignificantly increased mRNA expression levels of RUNX2, DLX5, SPP1 (Osteopontin), COL1 (Collagen type I), BGLAP, and BMP2 relative to untreated controls at 3, 7, and 14 days. Upregulated BMP2 expression that was not reversed by DKK1 pretreatment.

Western Blot Analysis^[4]

Cell Line:	hBMSCs
Concentration:	10 μM
Incubation Time:	3, 7, 14 days
Result:	Increased total β-catenin protein expression relative to untreated controls, with peak expression at 7 days. Significantly suppressed p-β-catenin protein expression relative to untreated controls across 3, 7, and 14 days.

In Vivo

Chrysosplenetin (80 mg/kg, p.o., once daily for 7 consecutive days) exhibits direct antimalarial activity against artemisinin-resistant Plasmodium berghei K173; when administered in combination with artemisinin at a 1:2 ratio, it sensitizes artemisinin-resistant malaria parasites to artemisinin; it also exerts effects by regulating host P-glycoprotein homeostasis, hemozoin/heme metabolism and related signaling pathways^[1].
Chrysosplenetin (4-160 mg/kg, p.o., once daily for 7 consecutive days) reverses the artemisinin-induced upregulation of MDR1 mRNA and P-gp protein expression in the small intestine of mice, and exerts weak stimulatory effects on the ATPase activity associated with ABC transporters^[3].
Chrysosplenetin (3 mg/kg; i.p.; once every 2 days; for 6 consecutive weeks) significantly alleviates estrogen deficiency-induced bone loss in ovariectomized mice by improving bone microstructural parameters and increasing the number and activity of osteoblasts^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	ICR (male, 4 weeks old, 18.0-22.0 g, malaria model); FVB background Abcb1a (P-gp)-deficient knockout (KO) (male, 4 weeks old, 18.0-22.0 g, malaria model)^[1]
Dosage:	80 mg/kg (single agent); 80 mg/kg + 40 mg/kg artemisinin (1:2 combination)
Administration:	p.o.; once daily; 7 consecutive days
Result:	Reduced parasitaemia and achieved significant inhibition percentage against artemisinin-resistant P. berghei K173.

Animal Model:	ICR mice (male, 18-22 g body weight)^[3]
Dosage:	4 mg/kg (co-administered with artemisinin); 40 mg/kg (co-administered with artemisinin); 80 mg/kg (alone or co-administered with artemisinin); 160 mg/kg (co-administered with artemisinin)
Administration:	i.g.; daily; 7 consecutive days
Result:	Reversed artemisinin-induced up-regulation of MDR1 mRNA in mouse small intestine to levels matching the negative contro. Reversed artemisinin-induced up-regulation of P-gp protein expression in mouse small intestine to levels matching the negative control. Caused a slight, statistically significant increase in ABC transporter-related ATPase activity in mouse small intestine compared to artemisinin alone.

Animal Model:	C57BL/6 J (female, 7 weeks old, ovariectomized)^[4]
Dosage:	3 mg/kg
Administration:	i.p.; every 2 days; 6 weeks
Result:	Significantly increased bone volume/total volume (BV/TV), trabecular number (Tb.N), and trabecular thickness (Tb.Th), while significantly reducing trabecular separation (Tb.Sp) relative to untreated OVX mice. Confirmed increased BV/TV, plus significant increases in osteoblast number per bone perimeter (N.Ob/B.Pm) and osteoblast surface per bone surface (Ob.S/BS), along with elevated relative osteocalcin expression in femurs. Reduced Osteocalcin/Bone Gla Protein (Ot/Bgp) levels, increased Bone Alkaline Phosphatase (Balp) levels, and altered Calcitonin (Ct) levels relative to untreated OVX mice.

Molecular Weight

374.34

Formula

C₁₉H₁₈O₈

CAS No.

603-56-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(OC)=C(C2=CC=C(O)C(OC)=C2)OC3=CC(OC)=C(OC)C(O)=C13

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (267.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6714 mL	13.3568 mL	26.7137 mL
5 mM	0.5343 mL	2.6714 mL	5.3427 mL
10 mM	0.2671 mL	1.3357 mL	2.6714 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (288 KB) SDS (394 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. Wang L, et al. Antimalarial activity and sensitization of chrysosplenetin against artemisinin-resistant genotype Plasmodium berghei K173 potentially via dual-mechanism of maintaining host P-glycoprotein homeostasis mediated by NF-κB p52 or PXR/CAR signaling pathways and regulating heme/haemozoin metabolism. Phytother Res. 2023;37(7):2939-2956. [Content Brief]

[2]. Şöhretoğlu D, et al. In vitro and in silico assessment of DNA interaction, topoisomerase I and II inhibition properties of chrysosplenetin. Int J Biol Macromol. 2020;163:1053-1059. [Content Brief]

[3]. Ma L, et al. Chrysosplenetin inhibits artemisinin efflux in P-gp-over-expressing Caco-2 cells and reverses P-gp/MDR1 mRNA up-regulated expression induced by artemisinin in mouse small intestine. Pharmaceutical Biology. 2017 Jan 1;55(1):374-80.

[4]. Hong G, et al. Chrysosplenetin promotes osteoblastogenesis of bone marrow stromal cells via Wnt/β-catenin pathway and enhances osteogenesis in estrogen deficiency-induced bone loss. Stem Cell Res Ther. 2019;10(1):277. Published 2019 Aug 29. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6714 mL	13.3568 mL	26.7137 mL	66.7842 mL
	5 mM	0.5343 mL	2.6714 mL	5.3427 mL	13.3568 mL
	10 mM	0.2671 mL	1.3357 mL	2.6714 mL	6.6784 mL
	15 mM	0.1781 mL	0.8905 mL	1.7809 mL	4.4523 mL
	20 mM	0.1336 mL	0.6678 mL	1.3357 mL	3.3392 mL
	25 mM	0.1069 mL	0.5343 mL	1.0685 mL	2.6714 mL
	30 mM	0.0890 mL	0.4452 mL	0.8905 mL	2.2261 mL
	40 mM	0.0668 mL	0.3339 mL	0.6678 mL	1.6696 mL
	50 mM	0.0534 mL	0.2671 mL	0.5343 mL	1.3357 mL
	60 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1131 mL
	80 mM	0.0334 mL	0.1670 mL	0.3339 mL	0.8348 mL
	100 mM	0.0267 mL	0.1336 mL	0.2671 mL	0.6678 mL