Citation: Zhihua Guo, Liuqi Shi, Huayang Feng, Fan Yang, Zhanrong Li, Junjie Zhang, Lin Jin, Jingguo Li. Reduction-sensitive nanomicelles: Delivery celastrol for retinoblastoma cells effective apoptosis[J]. Chinese Chemical Letters, ;2021, 32(3): 1046-1050. doi: 10.1016/j.cclet.2020.03.066 shu

Reduction-sensitive nanomicelles: Delivery celastrol for retinoblastoma cells effective apoptosis

Zhihua Guo ^{a, 1} ,
Liuqi Shi ^{a, b, 1} ,
Huayang Feng ^{a, b} ,
Fan Yang ^a ,
Zhanrong Li ^{a, **,} ,
Junjie Zhang ^a ,
Lin Jin ^a ,
Jingguo Li ^{a, b, **,}

a.
Henan Eye Hospital, Henan Provincial People's Hospital, Zhengzhou University People's Hospital, Zhengzhou 450003, China
b.
School of Materials Science and Engineering, Zhengzhou University, Zhengzhou 450001, China

^**

lizhanrong@zzu.edu.cn

lijingguo@zzu.edu.cn

Received Date: 20 January 2020
Revised Date: 23 March 2020
Accepted Date: 24 March 2020
Available Online: 4 April 2020

Figures(4)

Celastrol, a Chinese herbal medicine, has exhibited anticancer activity in many types of cancer cells. However, the further clinical application of celastrol is restricted by its poor water solubility and serious side effects. Furthermore, the apoptosis mechanism of tumor cells induced by celastrol has not been exhausted yet. In this study, we developed a reduction sensitive polymeric vector for tumor-targeted celastrol delivery. And our researches indicated that the celastrol could be delivered by reduction-sensitive nanomedicine (RSNMs) with a controlled release strategy. Meanwhile, the cell uptake results indicated that excellent reduction-sensitive behavior of RSNMs could effectively accelerate celastrol into the human retinoblastoma (RB) cell. The cell cytotoxicity assay demonstrated that celastrol inhibited proliferation of human RB Y79 cells growth in a dose-dependent manner. Furthermore, the results of flow cytometry and terminal dUTP nick-end labeling (TUNEL) staining showed that celastrol induced apoptosis of the RB Y79 cells, and revealed a time-dependent increase in apoptosis induction of RB Y79 cells. The results of western blotting showed that celastrol induced the apoptosis of human RB Y79 cells involving the activation of caspase-3 and caspase-9. In conclusion, our results revealed that RSNMs may be utilized as a novel therapy for retinoblastoma.
- Reduction-sensitive,
- Nanomicelles,
- Retinoblastoma,
- Celastrol,
- Cell apoptosis
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