Abstract
Scutellarein (SCU), a flavone found in the perennial herb Scutellaria baicalensis, is known for a wide range of biological activities. In the present study, we investigated the effects of treatment with SCU flavonoids on inducing apoptosis via the extrinsic pathway in Hep3B cells. SCU treatment significantly inhibited Hep3B cell proliferation and induced G2/M phase cell cycle arrest by inhibiting the expression level of the proteins Cdc25C, cdk1 and Cyclin B1. Allophycocyanin (APC)/Annexin V and propidium iodide (PI) double-staining showed upregulation of apoptotic cell death fraction. We further confirmed apoptosis by 4′-6-diamidino-2-phenylindole (DAPI) fluorescent staining and observed DNA fragmentation with agarose gel electrophoresis. Further, immunoblotting results showed that treatment with SCU showed no changes in Bax and Bcl-xL protein levels. In addition, SCU treatment did not affect the mitochondrial membrane potential (MMP) in Hep3B cells. On the contrary, treatment with SCU increased the expression of Fas and Fas ligand (FasL), which activated cleaved caspase-8, caspase-3, and polymeric adenosine diphosphate ribose (PARP), whereas the expression level of death receptor 4 (DR4) decreased. We confirmed that the proteins expressed upon treatment with SCU were involved in the Fas-mediated pathway of apoptosis in Hep3B cells. Thus, our findings in the current study strongly imply that SCU can be a basic natural source for developing potent anti-cancer agents for hepatocellular carcinoma (HCC) treatment.
Highlights
Hepatocellular carcinoma (HCC) is the most common form of primary liver cancer in adults, and it has high malignancy and poor prognosis [1]
Along with the results obtained from MTT assay, microscopic examination revealed morphological changes including cell shrinkage, floating of dead cells, and decreased cell numbers in SCU-treated cells (Figure 1B), which further confirms the indications of apoptosis
The present study showed that treatment with SCU increased the expression of Fas ligand (FasL); FasL belongs to the tumor necrosis factor family and binds
Summary
Hepatocellular carcinoma (HCC) is the most common form of primary liver cancer in adults, and it has high malignancy and poor prognosis [1]. Flavonoids are natural polyphenolic compounds that are known for their significant biological beneficial properties (including anti-cancer, anti-allergic, and anti-inflammatory activities), and it is reported that they have low toxicity. Scutellaria baicalensis is one of the fundamental herbs used in traditional Chinese medicine, and it has a wide range of biological activities, such as anti-inflammation and anti-diarrheal effects [5,6]. The leaves and flowers of Scutellaria baicalensis contain flavonoid glycosides such as scutellarein (5,6,7,40 -tetrahydroxyflavone; SCU), a flavone found in the perennial herb that has a range of biological activities. Previous studies demonstrated that the whole flavonoid extract of SCU along with the monomer compound, have a broad scale of biological activities such as anti-oxidant, anti-inflammatory, and anticancer effects through the induction of apoptosis [7]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
