Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.

Product information

CAS Number: 27740-01-8

Molecular Weight: 462.36

Formula: C21H18O12

Chemical Name: (2S, 3S, 4S, 5R, 6S)-6-{[5, 6-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-chromen-7-yl]oxy}-3, 4, 5-trihydroxyoxane-2-carboxylic acid

Smiles: OC(=O)[C@H]1O[C@@H](OC2=CC3OC(=CC(=O)C=3C(O)=C2O)C2C=CC(O)=CC=2)[C@H](O)[C@@H](O)[C@@H]1O

InChiKey: DJSISFGPUUYILV-ZFORQUDYSA-N

InChi: InChI=1S/C21H18O12/c22-8-3-1-7(2-4-8)10-5-9(23)13-11(31-10)6-12(14(24)15(13)25)32-21-18(28)16(26)17(27)19(33-21)20(29)30/h1-6,16-19,21-22,24-28H,(H,29,30)/t16-,17-,18+,19-,21+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (216.28 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Scutellarin treatment significantly reduces HepG2 cell viability in a dose-dependent manner, and inhibits migration and invasion of HCC cells in vitro. Scutellarin treatment significantly reduces STAT3 and Girders of actin filaments (Girdin) expression, STAT3 and Akt phosphorylation in HCC cells. Introduction of STAT3 overexpression restores the scutellarin-downregulated Girdin expression, Akt activation, migration and invasion of HCC cells. Furthermore, induction of Girdin overexpression completely abrogates the inhibition of scutellarin on the Akt phosphorylation, migration and invasion of HCC cells. Scutellarin can inhibit HCC cell metastasis in vivo, and migration and invasion in vitro by down-regulating the STAT3/Girdin/Akt signaling. Scutellarin selectively enhances Akt phosphorylation. Scutellarin is a putative therapeutic agent as it has been found to not only suppress microglial activation thus ameliorating neuroinflammation, but also enhance astrocytic reaction. Acutellarin amplifies the astrocytic reaction by upregulating the expression of neurotrophic factors among others thus indicating its neuroprotective role. Remarkably, the effects of scutellarin on reactive astrocytes are mediated by activated microglia supporting a functional "cross-talk" between the two glial types. Scutellarin can suppress RANKL-mediated osteoclastogenesis, the function of osteoclast bone resorption, and the expression levels of osteoclast-specific genes (tartrate-resistant acid phosphatase (TRAP), cathepsin K, c-Fos, NFATc1). Further investigation indicates that Scutellarin can inhibit RANKL-mediated MAPK and NF-κB signaling pathway, including JNK1/2, p38, ERK1/2, and IκBα phosphorylation.

In Vivo:

Scutellarin (50 mg/kg/day) significantly mitigates the lung and intrahepatic metastasis of HCC tumors in vivo. The numbers of the lung and intrahepatic metastatic tumors in the scutellarin-treated group are significantly less than that in the controls. The rats treated with Scutellarin display a significant alleviation in neurobehavioral deficits compared to the SAH group. Scutellarin enhanced eNOS expression compared with SAH rats.

References:

1. Ke Y, et al. Scutellarin suppresses migration and invasion of human hepatocellular carcinoma by inhibiting the STAT3/Girdin/Akt activity. Biochem Biophys Res Commun. 2016 Dec 18. pii: S0006-291X(16)32174-X
2. Yang LL, et al. Differential regulation of baicalin and scutellarin on AMPK and Akt in promoting adipose cell glucose disposal. Biochim Biophys Acta. 2016 Nov 27;1863(2):598-606.
3. Wu CY, et al. Scutellarin attenuates microglia-mediated neuroinflammation and promotes astrogliosis in cerebral ischemia - a therapeutic consideration. Curr Med Chem. 2016 Nov 18. [Epub ahead of print]

Products are for research use only. Not for human use.