Citation: Xiaolin Zhang, Xiuli Liu, Luhui Qin, Chao Tang, Yu Huo, Jinbin Wei, Ming Chen, Yutong Gao, Xiaoping Zhang, Yani Wu, Yongxiang Zhao, Renbin Huang, Liping Zhong, Bing Wang. Averrhoa carambola extractive inhibits breast cancer via regulating CEPT1 and LYPLA1[J]. Chinese Chemical Letters, ;2023, 34(3): 107618. doi: 10.1016/j.cclet.2022.06.041 shu

Averrhoa carambola extractive inhibits breast cancer via regulating CEPT1 and LYPLA1

Xiaolin Zhang ^{a, 1} ,
Xiuli Liu ^{b, 1} ,
Luhui Qin ^{a, 1} ,
Chao Tang ^{b, 1} ,
Yu Huo ^b ,
Jinbin Wei ^a ,
Ming Chen ^a ,
Yutong Gao ^a ,
Xiaoping Zhang ^a ,
Yani Wu ^a ,
Yongxiang Zhao ^b ,
Renbin Huang ^{a, *,} ,
Liping Zhong ^{b, *,} ,
Bing Wang ^{c, *,}

a.
Pharmaceutical College, Guangxi Medical University, Nanning 530021, China
b.
National Center for International Biotargeting Theranostics, Guangxi Key Laboratory of Biotargeting Theranostics, Collaborative Innovation Center for Targeting Tumor Theranostics, Guangxi Medical University, Nanning 530021, China
c.
Department of Spine Surgery, The Second Xiangya Hospital of Central South University, Changsha 410011, China

huangrenbin518@163.com

zhong_liping@163.com

wbxyeyy@csu.edu.cn

Received Date: 3 March 2022
Revised Date: 14 June 2022
Accepted Date: 15 June 2022
Available Online: 19 June 2022

Figures(4)

Liposomes have been widely exploited as a drug delivery system in treating tumors because of their advantage to enhance anti-tumor efficacy and reduce side effects. In this study, the tumor-targeted 2-dodecyl-6-methoxycyclohexa-2, 5-diene-1, 4-dione (DMDD, i.e., Averrhoa carambola extractive) liposomes (HA/TN-DLP) were conducted and assessed. HA/TN-DLP showed controllable drug loading (up to 83%) with high stability. In vitro and in vivo studies showed good cell uptake behavior and high inhibition rate of breast cancer compared to free DMDD. HA/TN-DLP might be the suitable for DMDD due to its better advantages in delivery, penetrability, and targeting-tumor capability. For in vivo mouse model tests, HA/TN-DLP effectively inhibited tumor growth compared to free DMDD. Further analyses indicated that HA/TN-DLP inhibited the glycerophospholipid metabolism pathway by reducing the biosynthesis of phosphatidylcholine and 1-acyl-sn-glycero-3-phosphocholine through regulating the expressions of CEPT1 and LYPLA1, and inhibited tumor cell growth by regulating the PI3K/Akt and NF-κB signaling pathways. In conclusion, the obviously enhanced antitumor effect further demonstrated that HA/TN-DLP may be a promising tumor-targeting agent.
- DMDD,
- Breast cancer,
- Transcriptomics,
- Metabolomics,
- PI3K/Akt pathway,
- Glycerophospholipid metabolism pathway
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