3'-Hydroxypterostilbene

Catalog No.S3940 Batch:S394001

Technical Data

Formula	C₁₆H₁₆O₄
Molecular Weight	272.30	CAS No.	475231-21-1
Solubility (25°C)*	In vitro	DMSO	54 mg/mL (198.31 mM)
		Ethanol	54 mg/mL (198.31 mM)
		Water	Insoluble
* <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.)

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Biological Activity

Description

3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.

Targets

p70S6K ^[1]

p38MAPK ^[1]

In vitro

3'-Hydroxypterostilbene decreases cell growth in cultured human colon cancer cells (COLO 205, HCT-116, and HT-29) in a dose-dependent manner, with IC50 values of 9.0, 40.2, and 70.9 µM, respectively. 3'-Hydroxypterostilbene effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. Treatment with HPSB causes reduction of mitochondrial membrane potential and induction of caspase-3 and caspage-9, which is associated with the degradation of DFF-45 and PARP, precedes the onset of apoptosis. It significantly down-regulates phosphatidylinositol 3-kinase (PI3K)/Akt and mitogen-activated protein kinases (MAPKs) signalings including decreased the phosphorylation of mammalian target of rapamycin (mTOR)^[1].

In vivo

3'-Hydroxypterostilbene by i.p. injection has anti-tumor efficacy gainst colon cancer through the inhibition of inflammation, metastasis, and angiogenesis as well as through the induction of apoptosis^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines COLO 205 cells Concentrations 5-100 µM Incubation Time 24 h Method For sub-G1 cell population analysis, COLO 205 cells (2×10⁵ cells/mL) are cultured in 12 well and treatment with various concentrations of pterostilbene or 3′-hydroxypterostilbene for 24 h. The cells are then harvested, washed with PBS, resuspended in 200 µL of PBS, and fixed in 800 µL of iced 100% ethanol at -20°C. After being left to stand overnight, the cell pellets are collected by centrifugation, resuspended in 1 mL of hypotonic buffer (0.5% Triton X-100 in PBS and 0.5 µg/mL RNase) with PI (50 µg/mL) and incubated at 37°C in the dark for 30 min. Fluorescence emitted from the PI-DNA complex is quantitated after excitation of the fluorescent dye.
Animal Study:^{^[1]}	Animal Models nude mice bearing COLO 205 tumor xenografts Dosages 10 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
COLO 205 cells
Concentrations
5-100 µM
Incubation Time
24 h
Method
For sub-G1 cell population analysis, COLO 205 cells (2×10⁵ cells/mL) are cultured in 12 well and treatment with various concentrations of pterostilbene or 3′-hydroxypterostilbene for 24 h. The cells are then harvested, washed with PBS, resuspended in 200 µL of PBS, and fixed in 800 µL of iced 100% ethanol at -20°C. After being left to stand overnight, the cell pellets are collected by centrifugation, resuspended in 1 mL of hypotonic buffer (0.5% Triton X-100 in PBS and 0.5 µg/mL RNase) with PI (50 µg/mL) and incubated at 37°C in the dark for 30 min. Fluorescence emitted from the PI-DNA complex is quantitated after excitation of the fluorescent dye.

Animal Study:^{^[1]}

Animal Models
nude mice bearing COLO 205 tumor xenografts
Dosages
10 mg/kg
Administration
i.p.

References

[1] Cheng TC, et al. PLoS One. 2014, 9(11):e111814.

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