Flavonoids identified from Korean Scutellaria baicalensis induce apoptosis by ROS generation and caspase activation on human fibrosarcoma cells

• Published in: The American journal of Chinese medicine (1979) Vol. 42; no. 2; p. 465
• Main Authors: Zhang, Jue, Park, Hyeon-Soo, Kim, Jin-A, Hong, Gyeong-Eun, Nagappan, Arulkumar, Park, Kwang-Il, Kim, Gon-Sup
• Format: Journal Article
• Language: English
• Published: Singapore 2014
• Subjects: Apoptosis - drug effects; Basic Helix-Loop-Helix Leucine Zipper Transcription Factors - metabolism; bcl-2-Associated X Protein - metabolism; bcl-X Protein - metabolism; Caspases - metabolism; Cell Survival - drug effects; Cell Transformation, Neoplastic - drug effects; Cells, Cultured; DNA-Binding Proteins - metabolism; Dose-Response Relationship, Drug; Fibrosarcoma - genetics; Fibrosarcoma - metabolism; Fibrosarcoma - pathology; Flavonoids - isolation & purification; Flavonoids - pharmacology; Gene Expression - drug effects; Heterogeneous-Nuclear Ribonucleoprotein K - metabolism; Humans; Korea; Plant Extracts - chemistry; Reactive Oxygen Species - adverse effects; Reactive Oxygen Species - metabolism; Scutellaria baicalensis - chemistry; Transcription Factors - metabolism; Tumor Cells, Cultured; Up-Regulation - drug effects; Korea
• ISSN: 0192-415X
• DOI: 10.1142/s0192415x14500311

The effects of flavonoids from Korean Scutellaria baicalensis on fibrosarcoma HT1080 cells and their underlying molecular mechanism were investigated in this study. Flavonoids affected HT1080 cell proliferation by interrupting cell cycle progress, obviously augmenting the proportion of sub-G1 and diminishing that of G1 phase, and undergoing apoptosis at the tested dosage (100-400 μg/mL). In addition, the mediated apoptosis was mainly caused by total reactive oxygen species (ROS) generation and by up-regulating the ratio of Bax/Bcl-xL, triggering caspase cascades (caspase-3, -9 and -8), and inactivating PARP, dose-dependently. The proteomics results showed that AP-4, ARID 5B, HNRNP K, PLOG, Prdx6, and myosin-1, associated with cell growth, differentiation and development, and overexpressed in gastric cancer, colorectal cancer, pancreatic cancer, etc., were statistically down-regulated after the flavonoids treatment. Taken together, our data demonstrated that flavonoids from Korean S. baicalensis induced apoptosis in HT1080 cells, which involved a hierarchy of cellular pathways and multiple signal proteins, and might be a potential anticancer therapeutic agent.