Anticancer activity and mechanism of Scutellaria barbata extract on human lung cancer cell line A549

Life Sci. 2004 Sep 17;75(18):2233-44. doi: 10.1016/j.lfs.2004.05.015.

Abstract

Scutellaria barbata (S. barbata), a traditional Chinese herbal medicine native to southern China, is widely used as an anti-inflammatory and a diuretic in China. Several studies have indicated that extracts of S. barbata have growth inhibitory effects on a number of human cancers. Treatment of lung cancer, digestive system cancers, hepatoma, breast cancer, and chorioepithelioma by S. barbata extracts was reported. However, the mechanism underlying the antitumor activity was unclear. In this study, we studied the growth inhibitory effect of S. barbata and determined its mechanism of antitumor activity using human lung cancer cell line A549. Our results showed that ethanol extracts of S. barbata greatly inhibited A549 cell growth, with IC50 of 0.21 mg/ml. The major mechanisms of inhibition included cell apoptosis and cytotoxic effects. cDNA microarray analysis showed that 16 genes, involved in DNA damage, cell cycle control, nucleic acid binding and protein phosphorylation, underwent more than 5-fold change. These data indicated that these processes are involved in S. barbata-mediated killing of cancer cells. A surprising finding is that CD209, related to dendritic cell (DC) function, was dramatically downregulated by 102-fold. Further functional studies are needed to assess the role of the array-identified genes in S. barbata mediated anticancer activity.

MeSH terms

  • Annexin A5 / metabolism
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Apoptosis / drug effects
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Caspase 3
  • Caspase 7
  • Caspases / metabolism
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Coloring Agents
  • DNA, Complementary / biosynthesis
  • DNA, Complementary / genetics
  • Humans
  • L-Lactate Dehydrogenase / metabolism
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Microscopy, Fluorescence
  • Oligonucleotide Array Sequence Analysis
  • Plant Extracts / pharmacology
  • Scutellaria / chemistry*
  • Tetrazolium Salts
  • Thiazoles

Substances

  • Annexin A5
  • Antineoplastic Agents, Phytogenic
  • Coloring Agents
  • DNA, Complementary
  • Plant Extracts
  • Tetrazolium Salts
  • Thiazoles
  • L-Lactate Dehydrogenase
  • CASP3 protein, human
  • CASP7 protein, human
  • Caspase 3
  • Caspase 7
  • Caspases
  • thiazolyl blue