1. Academic Validation
  2. (-)-Asarinin from the Roots of Asarum sieboldii Induces Apoptotic Cell Death via Caspase Activation in Human Ovarian Cancer Cells

(-)-Asarinin from the Roots of Asarum sieboldii Induces Apoptotic Cell Death via Caspase Activation in Human Ovarian Cancer Cells

  • Molecules. 2018 Jul 25;23(8):1849. doi: 10.3390/molecules23081849.
Miran Jeong 1 Hye Mi Kim 2 Jin Su Lee 3 4 Jung-Hye Choi 5 6 Dae Sik Jang 7 8
Affiliations

Affiliations

  • 1 College of Pharmacy, Kyung Hee University, Seoul 02447, Korea. jeongmiran@hanmail.net.
  • 2 College of Pharmacy, Kyung Hee University, Seoul 02447, Korea. hyemi586@gmail.com.
  • 3 College of Pharmacy, Kyung Hee University, Seoul 02447, Korea. lee2649318@naver.com.
  • 4 Department of Life & Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Korea. lee2649318@naver.com.
  • 5 College of Pharmacy, Kyung Hee University, Seoul 02447, Korea. jchoi@khu.ac.kr.
  • 6 Department of Life & Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Korea. jchoi@khu.ac.kr.
  • 7 College of Pharmacy, Kyung Hee University, Seoul 02447, Korea. dsjang@khu.ac.kr.
  • 8 Department of Life & Nanopharmaceutical Sciences, Kyung Hee University, Seoul 02447, Korea. dsjang@khu.ac.kr.
Abstract

Two tetrahydrofurofurano Lignans (1 and 2), four Phenylpropanoids (36), and two alkamides (7 and 8) were isolated from the EtOAc-soluble fraction of the roots of Asarum sieboldii. The chemical structures of the isolates were identified by analysis of spectroscopic data measurements, and by a comparison of their data with published values. The isolates (1, 2, 48) were evaluated for their cytotoxicity against human ovarian Cancer cells (A2780 and SKOV3) and immortalized ovarian surface epithelial cells (IOSE80PC) using a MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide) assay. Of the isolates, (-)-asarinin (1) exhibited the most potent cytotoxicity to both A2780 and SKOV3 cells. A propidium iodide/annexin V-fluorescein isothiocyanate (V-FITC) double staining assay showed that (-)-asarinin (1) induces apoptotic cell death in ovarian Cancer cells. In addition, (-)-asarinin (1) increased the activation of Caspase-3, Caspase-8, and caspase-9 in ovarian Cancer cells. Pretreatment with Caspase inhibitors attenuated the cell death induced by (-)-asarinin (1). In conclusion, our findings show that (-)-asarinin (1) from the roots of A. sieboldii may induce caspase-dependent apoptotic cell death in human Cancer cells.

Keywords

(−)-asarinin; Asarum sieboldii; apoptosis; caspase; cytotoxicity; ovarian cancer cells.

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