Lobetyol

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Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Lobetyol Chemical Structure

CAS No. : 136171-87-4

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Description

Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity^[1]^[2]. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

Bax

Bcl-2

In Vitro

Lobetyol (0-100 μg/mL, 0-48 h) leads to a dose-and time-dependent proliferation inhibition in MKN45 cells^[1].
Lobetyol (0-100 μg/mL, 48 h) induces apoptosis and cell cycle arrest in a time- and dose-dependent manner in MKN45 cells^[1].
Lobetyol (0-100 μg/mL, 48 h) increases the expression level of Bax, P53, and decreased the expression level of Bcl-2^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MKN45 cells
Concentration:	0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time:	12 h, 24 h, 48 h
Result:	Showed a dose-and time-dependent proliferation inhibition in MKN45 cells, with an IC₅₀ of 71.47 ± 4.29 μg/mL at 48 h. Exhibited more safety on L02 and HEK293 human normal cell lines.

Apoptosis Analysis^[1]

Cell Line:	MKN45 cells
Concentration:	0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time:	48 h
Result:	Increased the apoptotic population in MKN45 cells in a dose-dependent manner. Flow cytometic assay of Annexin-V/PI revealed apoptotic populations under increasing dose of lobetyol ranging from 0 μg/mL, 50 μg/mL, 75 μg/mL, to 100 μg/mL are 5.5%, 13.74%, 27.32% to 31.57%, respectively.

Western Blot Analysis^[1]

Cell Line:	MKN45 cells
Concentration:	0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time:	12 h, 24 h, 48 h
Result:	Increased the expression level of Bax, P53, and decreased the expression level of Bcl-2. The release of cytochrome c was detected, followed by caspase-9 and -3 activations.

In Vivo

Lobetyol (0-10 mg/kg, Once per 3 days) suppresses tumor growth in MKN45 nude models^[1].

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

Animal Model:	BALB/C nude mice (6 weeks-old, injected intraperitoneally with MKN45 cells)^[1]
Dosage:	0, 2, 5, 10 mg/kg
Administration:	Once per 3 days
Result:	Suppressed tumor growth in MKN45 nude models. The protein levels of Ki67 in MKN45 cells were significantly decreased. Meanwhile, cleaved-caspase-3 positive MKN45 cells were found increased with the tendency of lobetyol concentrations in the study in vivo.

Molecular Weight

234.29

Formula

C₁₄H₁₈O₃

CAS No.

136171-87-4

SMILES

C/C=C/C#CC#CC(O)C(O)/C=C/CCCO

Structure Classification

Others

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shen J, et al. Lobetyol activate MAPK pathways associated with G1/S cell cycle arrest and apoptosis in MKN45 cells in vitro and in vivo. Biomed Pharmacother. 2016 Jul;81:120-127. [Content Brief]

[2]. Xie Q, et al. The in vitro/in vivo metabolic pathways analysis of lobetyol, lobetyolin, and lobetyolinin, three polyacetylenes from Codonopsis Radix, by UHPLC-Q/TOF-MS and UHPLC-MS/MS. J Pharm Biomed Anal. 2023 Jan 20;223:115140. [Content Brief]

Lobetyol Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lobetyol136171-87-4ApoptosisBcl-2 FamilyMDM-2/p53MKN45Cell cycle arrestMAPKInhibitorinhibitorinhibit

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