Bavachinin

Catalog No.S3878 Batch:S387801

Technical Data

Formula	C₂₁H₂₂O₄
Molecular Weight	338.40	CAS No.	19879-30-2
Solubility (25°C)*	In vitro	DMSO	67 mg/mL (197.99 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Bavachinin (7-O-Methylbavachin) is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).

Targets

PPARγ ^[1] (Cell-free assay)	PPAR-β/δ ^[1] (Cell-free assay)	PPARα ^[1] (Cell-free assay)
223 nM(Ki)	5.275 μM(Ki)	7.881 μM(Ki)

In vitro

Bavachinin inhibits increases in HIF-1α activity in human KB carcinoma (HeLa cellderivative)and human HOS osteosarcoma cells under hypoxia in a concentration-dependent manner, probably by enhancing the interaction between von Hippel-Lindau (VHL) and HIF-1α. Furthermore, Bavachinin decreases transcription of genes associated with angiogenesis and energy metabolism that are regulated by HIF-1, such as vascular endothelial growth factors (VEGF), Glut1 and Hexokinase2. Bavachinin also inhibits tube formation in human umbilical vein endothelial cells (HUVECs) as well as in vitro migration of KB cells. Bavachinin inhibits nitricoxide production in macrophages activated by lipopolysaccharide^[2].

In vivo

In db/db and DIO mice, BVC treatment ameliorates diabetes, hyperlipidaemia and BVC improves hepatotoxicity. BVC enhances glucose transport and utilisation, hepatic lipid turnover and fatty acid metabolism through PPAR networks, thereby improving insulin sensitivity, dyslipidaemia and fatty liver^[1]. In vivo studies show that injecting Bavachinin thrice weekly for four weeks significantly reduces tumor volume and CD31 expression in nude mice with KB xenografts^[2]. Following IV administration of bavachinin at 25 mg/kg to naïve female BALB/c mice, clearance is high (mean CL = 299.72 mL/min/kg) and is approximately 3.33-fold of hepatic blood flow. The mean volume of distribution of bavachinin is 11881.67 mL/kg, it is 16.39 times of total body water volume (725 mL/kg), indicating high extravascular distribution. The mean terminal half-life following IV dosing is 0.70 h, this is reflected a tight correlation between the clearance and terminal half-life. The PK properties of bavachinin are characterized as rapid oral absorption, high clearance, and poor absolute bioavailability following single oral and intravenous administration to naïve female BALB/c mice^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines HOS and KB Cells Concentrations -- Incubation Time 24 h Method HOS and KB Cells(1×10⁴) are seeded onto a 96-well plate with medium supplemented with 10% FBS and incubated for 24 h. Cells are then exposed to various concentrations of Bavachinin for an additional 24 h in hypoxic conditions. Cells are washed twice with phosphate-buffered saline and cell survival is assayed by treating with 100 μg/ml of MTT for 2h at 37 ℃. After washing with phosphate buffered saline, the resulting purple formazan is dissolved in 200 ml of dimethylsulphoxide and its absorbance is read at 540 nm.
Animal Study:^{^[2]}	Animal Models Female athymic nude mice Dosages 5 mg/kg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
HOS and KB Cells
Concentrations
--
Incubation Time
24 h
Method
HOS and KB Cells(1×10⁴) are seeded onto a 96-well plate with medium supplemented with 10% FBS and incubated for 24 h. Cells are then exposed to various concentrations of Bavachinin for an additional 24 h in hypoxic conditions. Cells are washed twice with phosphate-buffered saline and cell survival is assayed by treating with 100 μg/ml of MTT for 2h at 37 ℃. After washing with phosphate buffered saline, the resulting purple formazan is dissolved in 200 ml of dimethylsulphoxide and its absorbance is read at 540 nm.

Animal Study:^{^[2]}

Animal Models
Female athymic nude mice
Dosages
5 mg/kg
Administration
i.p.

References

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