2. Academic Validation
  3. Diosbulbin C, a novel active ingredient in Dioscorea bulbifera L. extract, inhibits lung cancer cell proliferation by inducing G0/G1 phase cell cycle arrest

Diosbulbin C, a novel active ingredient in Dioscorea bulbifera L. extract, inhibits lung cancer cell proliferation by inducing G0/G1 phase cell cycle arrest

  • BMC Complement Med Ther. 2023 Dec 4;23(1):436. doi: 10.1186/s12906-023-04245-9.
Zhiyu Zhu 1,  Yanfen Liu 1,  Jiangping Zeng 1,  Shuyi Ren 1,  Lu Wei 1,  Fei Wang 1,  Xiaoyu Sun 1,  Yufei Huang 1,  Haiyang Jiang 1,  Xinbing Sui 1 2,  Weiwei Jin 3,  Lijun Jin 4,  Xueni Sun 5 6
Affiliations

Affiliations

  • 1 School of Pharmacy, Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, 311121, Zhejiang, China.
  • 2 Department of Gastrointestinal and Pancreatic Surgery, Key Laboratory of Gastroenterology of Zhejiang Province, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou, 310014, Zhejiang, China.
  • 3 Department of Gastrointestinal and Pancreatic Surgery, Key Laboratory of Gastroenterology of Zhejiang Province, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou, 310014, Zhejiang, China. jinww@zju.edu.cn.
  • 4 Department of Traditional Chinese Medicine, Hangzhou Shangcheng District People's Hospital, Hangzhou, China. 58646061@qq.com.
  • 5 School of Pharmacy, Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines, Engineering Laboratory of Development and Application of Traditional Chinese Medicines, Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou, 311121, Zhejiang, China. xnsun@hznu.edu.cn.
  • 6 Department of Gastrointestinal and Pancreatic Surgery, Key Laboratory of Gastroenterology of Zhejiang Province, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou, 310014, Zhejiang, China. xnsun@hznu.edu.cn.
PMID: 38049779 DOI: 10.1186/s12906-023-04245-9
Abstract

Background: Despite the critical progress of non-small cell lung Cancer (NSCLC) therapeutic approaches, the clinical outcomes remain considerably poor. The requirement of developing novel therapeutic interventions is still urgent. In this study, we showed for the first time that diosbulbin C, a natural diterpene lactone component extracted from traditional Chinese medicine Dioscorea bulbifera L., possesses high Anticancer activity in NSCLC.

Methods: A549 and NCI-H1299 cells were used. The inhibitory effects of the diosbulbin C on NSCLC cell proliferation were evaluated using cytotoxicity, clone formation, EdU assay, and flow cytometry. Network pharmacology methods were used to explore the targets through which the diosbulbin C inhibited NSCLC cell proliferation. Molecular docking, qRT-PCR, and western blotting were used to validate the molecular targets and regulated molecules of diosbulbin C in NSCLC.

Results: Diosbulbin C treatment in NSCLC cells results in a remarkable reduction in cell proliferation and induces significant G0/G1 phase cell cycle arrest. Akt1, DHFR, and TYMS were identified as the potential targets of diosbulbin C. Diosbulbin C may inhibit NSCLC cell proliferation by downregulating the expression/activation of Akt, DHFR, and TYMS. In addition, diosbulbin C was predicted to exhibit high drug-likeness properties with good water solubility and intestinal absorption, highlighting its potential value in the discovery and development of anti-lung Cancer drugs.

Conclusions: Diosbulbin C induces cell cycle arrest and inhibits the proliferation of NSCLC cells, possibly by downregulating the expression/activation of Akt, DHFR, and TYMS.

Keywords

Anticancer activity; Bioactive ingredient; Diosbulbin C; Non-small cell lung cancer; Traditional Chinese medicine.

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