Anti-melanoma activity of Bupleurum chinense, Bupleurum kaoi and nanoparticle formulation of their major bioactive compound saikosaponin-d

Stephen Chu Sung Hu, I-Ta Lee, Ming Hong Yen, Chun Ching Lin, Chiang Wen Lee, Feng Lin Yen

研究成果: 雜誌貢獻文章同行評審

17 引文 斯高帕斯(Scopus)

摘要

Ethnopharmacological relevance Bupleurum chinense is a traditional Chinese medicinal herb which has been used to treat various inflammatory and infectious diseases, while Bupleurum kaoi is an endemic plant in Taiwan. We determined whether B. chinense and B. kaoi and their biologically active saikosaponin compounds possess anti-melanoma activity. In addition, we developed a novel saikosaponin-d nanoparticle system to improve its solubility, and evaluated its antiproliferative effects and molecular mechanisms in melanoma cells. Materials and methods Ethanolic extracts from B. chinense and B. kaoi were prepared, and their saikosaponin contents were determined by high performance liquid chromatography analysis. Saikosaponin-d nanoparticles were synthesized, and their physicochemical properties were evaluated by particle size analyzer, transmission electron microscopy, differential scanning calorimetry, X-ray diffractometry, and Fourier transform infrared spectroscopy. Human A375.S2 melanoma cells were cultured, and cell viability determined by the MTT assay. Apoptosis was evaluated by determination of mitochondrial membrane potential, and signal transduction pathways investigated by Western blotting. Results Ethanolic extracts from B. kaoi showed more potent antiproliferative effect on human A375.S2 melanoma cells compared to B. chinense. The saikosaponin-a, -c and -d contents were higher in B. kaoi compared to B. chinense. Saikosaponin-d was the most potent compound in terms of anti-melanoma activity, and saikosaponin-d nanoparticles exhibited increased water solubility due to lowered particle size, amorphous transformation and intermolecular hydrogen bond formation with the excipient. Furthermore, saikosaponin-d nanoparticles showed enhanced antiproliferative activity against melanoma cells, and induced apoptosis through the mitochondrial pathway. The anti-melanoma activity was mediated by phosphorylation of JNK and p38, phosphorylation of p53, increased level of cytochrome c, and activation of caspase 9. Conclusions B. kaoi contains higher saikosaponin content and shows greater anti-melanoma activity than B. chinense. Saikosaponin-d nanoparticles have improved solubility, and may have potential use in the future as a form of treatment for melanoma.
原文英語
頁(從 - 到)432-442
頁數11
期刊Journal of Ethnopharmacology
179
DOIs
出版狀態已發佈 - 二月 17 2016
對外發佈

ASJC Scopus subject areas

  • 藥理
  • 藥物發現

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