Anti-tumor activities and mechanism study of α-pinene derivative in vivo and in vitro

  • Lianbao Ye
  • Xiaoshun Zhang
  • Qiuxiang Xu
  • Yongming Cai
  • Wei Gao
  • Weiqiang ChenEmail author
Original Article


In previous study, we designed novel α-pinene derivatives based on theories of bioalkylating agents using α-pinene as lead compound and patented these compounds, in which compound α-pinene derivative GY-1 (6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methyl-4-methylbenzenesulfonat) showed strongest inhibition on hepatoma carcinoma cell BEL-7402. In this study, we investigated effect of GY-1 on hepatocellular carcinoma in vitro and in vivo, and explored its mechanism of anti-hepatoma. The results showed that GY-1 showed good anti-liver cancer activity with the IC50 of 84.7 μmol/L in vitro, inhibited tumor growth in vivo with dose-dependent, and GY-1 could arrest the growth of hepatoma cells in the S phase and induced apoptosis in hepatoma cells, down-regulated the expression of C-myc, CDK2 and CyclinE, and up-regulate p53.


α-Pinene derivative Anti-hepatoma activity Anti-hepatoma mechanism Apoptosis Cell cycle 



The work was supported by Special Innovation Project of Guangdong Education Department (Natural Science) (2017KTSCX107), Guangdong Natural Science Foundation (2015A03031356, 2015A030310176), Science and Technology Planning Project of Guangdong Province (2016A020215159,2017ZC0199), Medical Scientific Research Foundation of Guangdong province (B2019004), Key laboratory of new drug discovery and evaluation of ordinary universities of Guangdong province(2017KSYS002), Guangzhou key laboratory of construction and application of new drug screening model systems(201805010006), Guangdong province precise medicine and big data engineering technology research center for traditional Chinese medicine, the open project foundation of the Fujian Provincial Key Laboratory of Theoretical and Computational Chemistry (201502), Guangdong province engineering technology center for molecular probes and biomedical imaging.

Author contributions

WC and LY contributed to the conception and design of the experiments, analysis of the data and revised the paper. WG selected and analyzed the data. QX, XZ, YC, performed the biological studies.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

Ethics approval and consent to participate

The current study was not required to complete an ethical assessment.

Supplementary material

280_2019_3997_MOESM1_ESM.docx (232 kb)
Supplementary material 1 (DOCX 232 kb)


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Copyright information

© Springer-Verlag GmbH Germany, part of Springer Nature 2019

Authors and Affiliations

  1. 1.School of PharmacyGuangdong Pharmaceutical UniversityGuangzhouChina
  2. 2.Undergraduate Nursing SchoolGuangdong Pharmaceutical UniversityGuangzhouChina
  3. 3.Anhui Haikang Pharmaceutical CO., LTDAnqingChina
  4. 4.Guangdong Province Precise Medicine and Big Data Engineering Technology Research Center for Traditional Chinese MedicineGuangdong Pharmaceutical UniversityGuangzhouChina
  5. 5.Guangdong Key Laboratory of Pharmaceutical Bioactive SubstancesGuangdong Pharmaceutical UniversityGuangzhouChina

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