Betulin

Synonyms: betulinol, betuline, betulinic alcohol

Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.

Betulin Chemical Structure

Betulin Chemical Structure

CAS: 473-98-3

Selleck's Betulin has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.51%
99.51

Betulin Related Products

Choose Selective Fatty Acid Synthase Inhibitors

Biological Activity

Description Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
In vitro
In vitro Betulin significantly inhibits cell viability in cervix carcinoma HeLa cells, hepatoma HepG2 cells, lung adenocarcinoma A549 cells, and breast cancer MCF-7 cells with IC50 values ranging from 10 to 15 mg/mL. While betulin exhibits only moderate anticancer activity in other human cancer cells such as hepatoma SK-HEP-1 cells, prostate carcinoma PC-3, and lung carcinoma NCI-H460, with IC50 values ranging from 20 to 60 mg/mL, it shows minor growth inhibition in human erythroleukemia K562 cells (IC50>100 mg/mL). Betulin does not directly trigger mitochondrial cytochrome c release in isolated mitochondria. Bax and Bak are rapidly translocated to the mitochondria 30 min after betulin treatment[1]. In vitro, Betulin inhibits LPS-induced tumor necrosis factor α (TNF-α) and (interleukin) IL-6 levels and up-regulates the level of IL-10. Also Betulin suppresses the phosphorylation of nuclear factor-kB (NF-kB) p65 protein in LPS-stimulated RAW 264.7 cells[2].
In Vivo
In vivo In vivo, Betulin alleviates LPS-induced acute lung injury. Treatment with Betulin diminishes pro-inflammatory cytokines, myeloperoxidase activity and bacterial loads in lung tissue during gramnegative pneumonia. In HFD-fed apoE−/− mice, betulin administration significantly reduces lesions in en face aortas and aortic sinuses. Furthermore, betulin administration significantly increases ABCA1 expression and suppresses macrophage positive areas in the aortic sinuses. Moreover, betulin administration improves plasma lipid profiles and enhances fecal cholesterol excretion in the mice[3].
Animal Research Animal Models C57BL/6J male mice aged 8 weeks
Dosages 4 or 8 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01657292 Completed
Burns
Birken AG|Amryt Pharma
August 2012 Phase 3

Chemical Information & Solubility

Molecular Weight 442.72 Formula

C30H50O2

CAS No. 473-98-3 SDF Download Betulin SDF
Smiles CC(=C)C1CCC2(C1C3CCC4C5(CCC(C(C5CCC4(C3(CC2)C)C)(C)C)O)C)CO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 7 mg/mL ( (15.81 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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