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Bioactivity evaluations of betulin identified from the bark of Betula platyphylla var. japonica for cancer therapy

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Abstract

Identification of bioactive natural products with anticancer activity as well as alleviating effects on chemotherapy-induced side effects has significant implications for cancer treatment. Betula platyphylla var. japonica, commonly known as Asian white birch, has been used in Chinese traditional medicine for a variety of purposes. In this study, the medicinal properties of betulin from B. platyphylla var. japonica useful for cancer management were investigated. LC/MS analysis revealed that betulin is a main chemical component of the EtOH extract of B. platyphylla var. japonica bark, and betulin was isolated from EtOH extract using an LC/MS-guided isolation method. Its structure was identified with 1H and 13C NMR spectroscopic data and LC/MS analysis and then compared to the previously reported spectroscopic and physical data. We first verified the cytotoxicity of betulin against three human lung adenocarcinoma cell lines, A549, H1264, and Calu-6, with IC50 values ranging from 18.7 to 39.6 μM. Regarding alleviation of side effects associated with anticancer chemotherapy, betulin ameliorated cisplatin-induced renal cell damage to 80% of the control value from the concentration of 5 μM. In addition, betulin showed anti-gastritis activity against ethanol-induced gastric damage in rats and notably reduced the gastric damage index compared to control in a concentration-dependent manner. These findings provide the first experimental evidence for potential use of B. platyphylla var. japonica as a functional food for cancer treatment that simultaneously alleviates the side effects of chemotherapy.

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Acknowledgements

This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (2015R1C1A1A02037383) and by the Ministry of Education (NRF-2012R1A5A2A28671860).

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Authors and Affiliations

  1. School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea

    Hae Min So, Hee Jeong Eom, Dahae Lee, Sil Kim & Ki Hyun Kim

  2. College of Korean Medicine, Gachon University, Seongnam, 461-701, Republic of Korea

    Ki Sung Kang

  3. Research Center, Natural Medicine Research Team, Richwood Trading Company, LTD, Seoul, 08826, Republic of Korea

    Il Kyun Lee

  4. Department of Molecular and Cellular Biology, Samsung Medical Center, Sungkyunkwan University School of Medicine, Suwon, 16419, Republic of Korea

    Kwan-Hyuck Baek

  5. Department of Food Science and Biotechnology, Kyonggi University, Suwon, 443-760, Republic of Korea

    Jun Yeon Park

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So, H.M., Eom, H.J., Lee, D. et al. Bioactivity evaluations of betulin identified from the bark of Betula platyphylla var. japonica for cancer therapy. Arch. Pharm. Res. 41, 815–822 (2018). https://doi.org/10.1007/s12272-018-1064-9

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