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Potential neurotrophic activity and cytotoxicity of selected C21 steroidal glycosides from Cynanchum otophyllum

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Cynanchum otophyllum was traditionally used for treating muscle and skeletal pain, epilepsy, abdominal pain, and tightness. Four known C21 steroidal glycosides, namely caudatin 3-O-β-cymaropyranoside (1), caudatin 3-O-β-D-cymaropyranosyl-(1 → 4)-β-D-cymaropyranoside (2), otophylloside B (3), and otophylloside A (4) were isolated from the roots of this plant and their neurotrophic activities were examined in rat neuronal PC12 cell model, while their cytotoxicities were evaluated in human cancer cells and normal fibroblasts. Differential promoting effects on neurite-bearing cells were found among testing compounds, with 2 the most potent. On the other hand, selective cytotoxicity against human colon cancer cells HCT-116 of 2 was firstly demonstrated here. Besides, 2 induced inhibitory activities on cancer cell proliferation, sphere formation and interfered the cell cycle. The new potential pharmacological activities of 2 on colon cancer cells were revealed in the present study.

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The authors would like to thank Mr. Hin-Fai Kwok and Ms. Si Gao of Institute of Chinese Medicine, The Chinese University of Hong Kong (CUHK), for their technical support. Also thanks to Prof. Sheng-Ji Pei of Kunming Institute of Botany, Chinese Academy of Sciences for his help in the authentication of the plant material. This study was partly supported by grants of the State Key Laboratory of Research on Bioactivities and Clinical Applications of Medicinal Plants (CUHK) [formerly known as Partner State Key Laboratory of Phytochemistry and Plant Resources in West China] from HKSAR and CUHK. The study was also supported by Foundational Project of Yunnan Key Laboratory of Tobacco Chemistry, R&D Center of China Tobacco Yunnan Industrial Co., Ltd (KCFZ-2017-1096) and Autonomous Deployment Project (KIB2017010) of Kunming Institute of Botany, Chinese Academy of Sciences.

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Correspondence to Clara Bik-San Lau or Minghua Qiu.

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Dong, J., Yue, G.G., Lee, J.K. et al. Potential neurotrophic activity and cytotoxicity of selected C21 steroidal glycosides from Cynanchum otophyllum. Med Chem Res 29, 549–555 (2020). https://doi.org/10.1007/s00044-020-02506-7

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  • Cynanchum otophyllum
  • Neurotrophic activity
  • Cytotoxicity
  • Colon cancer cells