Reagents and instruments for immunology, cell biology and molecular biology.

Bruceantin [41451-75-6]

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Cat# HY-N0840-1mg

Size : 1mg

Brand : MedChemExpress

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Description

Bruceantin ((-)-Bruceantin) is a quassinoid found in B. javanica. Bruceantin activates caspase signaling pathway, causes the mitochondrial dysfunction, inhibits cell proliferation, induces cell differentiation and apoptosis. Bruceantin exhibits anti-leukemia and antiprotozoal activities^[1]^[2]^[3].

Cellular Effect

Cell Line	Type	Value	Description	References
BV-173	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human BV173 cells by trypan blue exclusion method Cytotoxicity against human BV173 cells by trypan blue exclusion method	[PMID: 14987068]
Daudi	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human Daudi cells by trypan blue exclusion method Cytotoxicity against human Daudi cells by trypan blue exclusion method	[PMID: 14987068]
HeLa	IC₅₀	0.051 μM Compound: 7	Inhibition of protein synthesis in human HeLa cells assessed as [35S]methionine incorporation into protein treated for 45 mins before [35S]methionine addition by Whatman paper analysis Inhibition of protein synthesis in human HeLa cells assessed as [35S]methionine incorporation into protein treated for 45 mins before [35S]methionine addition by Whatman paper analysis	[PMID: 19199792]
HL-60	EC₅₀	0.02 μM Compound: 2	Induction of cell differentiation in human HL60 cells assessed as superoxide anion production after 4 days by NBT reduction assay Induction of cell differentiation in human HL60 cells assessed as superoxide anion production after 4 days by NBT reduction assay	[PMID: 11754601]
HL-60	IC₅₀	0.04 μM Compound: 2	Cytotoxicity against human HL60 cells assessed as loss of membrane integrity after 4 days by trypan blue exclusion assay Cytotoxicity against human HL60 cells assessed as loss of membrane integrity after 4 days by trypan blue exclusion assay	[PMID: 11754601]
HL-60	IC₅₀	0.04 μM Compound: 2	Antiproliferative activity against human HL60 cells assessed as inhibition of [3H]thymidine incorporation after 4 days by liquid scintillation counter Antiproliferative activity against human HL60 cells assessed as inhibition of [3H]thymidine incorporation after 4 days by liquid scintillation counter	[PMID: 11754601]
HL-60	IC₅₀	12.2 nM Compound: Bruceantin	Induction of apoptosis in human HL60 cells after 24 hrs by DAPI staining Induction of apoptosis in human HL60 cells after 24 hrs by DAPI staining	[PMID: 14987068]
HL-60	IC₅₀	20 ng/mL Compound: Bruceantin	Cytotoxicity against human HL60 cells by trypan blue exclusion method Cytotoxicity against human HL60 cells by trypan blue exclusion method	[PMID: 14987068]
Kasumi 1	IC₅₀	20 ng/mL Compound: Bruceantin	Cytotoxicity against human Kasumi-1 cells by trypan blue exclusion method Cytotoxicity against human Kasumi-1 cells by trypan blue exclusion method	[PMID: 14987068]
LNCaP	ED₅₀	11 nM Compound: 6	Cytotoxicity against hormone-dependent human LNCAP cells after 2 days by sulforhodamine B assay Cytotoxicity against hormone-dependent human LNCAP cells after 2 days by sulforhodamine B assay	[PMID: 19026551]
Lu1	ED₅₀	12 nM Compound: 6	Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay Cytotoxicity against human Lu1 cells after 2 days by sulforhodamine B assay	[PMID: 19026551]
MCF7	ED₅₀	0.27 nM Compound: 6	Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay in presence of 43 uM (-)-hydnocarpin Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay in presence of 43 uM (-)-hydnocarpin	[PMID: 19026551]
MCF7	ED₅₀	2 nM Compound: 6	Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay Cytotoxicity against human MCF7 cells after 2 days by sulforhodamine B assay	[PMID: 19026551]
NB-4	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human NB4 cells by trypan blue exclusion method Cytotoxicity against human NB4 cells by trypan blue exclusion method	[PMID: 14987068]
NCI-H929	IC₅₀	115 nM Compound: Bruceantin	Induction of apoptosis in human NCI-H929 cells after 24 hrs by DAPI staining Induction of apoptosis in human NCI-H929 cells after 24 hrs by DAPI staining	[PMID: 14987068]
REH	IC₅₀	20 ng/mL Compound: Bruceantin	Cytotoxicity against human REH cells by trypan blue exclusion method Cytotoxicity against human REH cells by trypan blue exclusion method	[PMID: 14987068]
RPMI-8226	IC₅₀	12.8 nM Compound: Bruceantin	Induction of apoptosis in human RPMI8226 cells after 24 hrs by DAPI staining Induction of apoptosis in human RPMI8226 cells after 24 hrs by DAPI staining	[PMID: 14987068]
RS4-11	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human RS4:11 cells by trypan blue exclusion method Cytotoxicity against human RS4:11 cells by trypan blue exclusion method	[PMID: 14987068]
SU-DHL-6	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human DHL6 cells by trypan blue exclusion method Cytotoxicity against human DHL6 cells by trypan blue exclusion method	[PMID: 14987068]
U-266	IC₅₀	49 nM Compound: Bruceantin	Induction of apoptosis in human U266 cells after 24 hrs by DAPI staining Induction of apoptosis in human U266 cells after 24 hrs by DAPI staining	[PMID: 14987068]
U-937	IC₅₀	< 15 ng/mL Compound: Bruceantin	Cytotoxicity against human U937 cells by trypan blue exclusion method Cytotoxicity against human U937 cells by trypan blue exclusion method	[PMID: 14987068]

In Vitro

Bruceantin (2.5-40 ng/mL, 24 h) downregulates the expression of c-Myc in cell RPMI 8226, induces a decrease in mitochondrial membrane potential, leads to the release of cytochrome c, activates caspase-3/7, and induces apoptosis in cells RPMI 8226, U266 and H929 with IC₅₀s of 13, 49 and 115 nM, respectively^[1].
Bruceantin (0.1-1 μg/mL, 4-5 days) exhibits anti-amoebic activity, inhibits Entamoeba histolytica with an IC₅₀ of 0.018 μg/mL^[3].

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

Apoptosis Analysis^[1]

Cell Line:	RPMI 8226, U266 and H929
Concentration:	2.5-40 ng/mL
Incubation Time:	24 h
Result:	Induced apoptosis.

Western Blot Analysis^[1]

Cell Line:	RPMI 8226
Concentration:	2.5-40 ng/mL
Incubation Time:	24 h
Result:	Inhibited the expression of c-Myc in RPMI 8226.

In Vivo

Bruceantin (1.25-12 mg/kg, ip, every 3 days for 40 days) exhibits antitumor effect in mouse RPMI 8226 xenograft models^[1].

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

Animal Model:	Mouse RPMI 8226 xenograft models^[1]
Dosage:	1.25-12 mg/kg
Administration:	ip, every 3 days for 40 days
Result:	Inhibited tumor growth.

Molecular Weight

548.58

Formula

C₂₈H₃₆O₁₁

CAS No.

41451-75-6

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1([C@H]([C@H](O)[C@]2(07)[C@]3(C4)C)O)[C@@]([C@H](C5=O)OC(/C=C(C)/C(C)C)=O)(07)[C@@]2([C@@](O5)(07)C[C@@]3(07)C(C)=C(O)C4=O)CO1)OC

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (182.29 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	1.8229 mL	9.1144 mL	18.2289 mL
5 mM	0.3646 mL	1.8229 mL	3.6458 mL
10 mM	0.1823 mL	0.9114 mL	1.8229 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (4.56 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.56 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.94%

Data Sheet (280 KB) SDS (393 KB)

COA (253 KB) LCMS (115 KB)

Handling Instructions (2659 KB)

References

[1]. Cuendet M, et al. Multiple myeloma regression mediated by bruceantin. Clin Cancer Res. 2004 Feb 1;10(3):1170-9. [Content Brief]

[2]. Cuendet M, et al. Antitumor activity of bruceantin: an old drug with new promise. J Nat Prod. 2004 Feb;67(2):269-72. [Content Brief]

[3]. Gillin FD, et al., Bruceantin, a potent amoebicide from a plant, Brucea antidysenterica. Antimicrob Agents Chemother. 1982 Aug;22(2):342-5. [Content Brief]

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