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Rapamycin functionalized carbon Dots: Target-oriented synthesis and suppression of vascular cell senescence
Jiaxin Dong1, Qi Wang2, Tingting Gu1
1Institute for Advanced Ceramics, State Key Laboratory of Urban Water Resource and Environment, Harbin Institute of Technology, Harbin 150001, PR China.
Abstract:
Suppression of vascular cell senescence is of great significance in preventing cardiovascular diseases such as hypertension and atherosclerosis. The oxidative stress damage caused by reactive oxygen species (ROS) can lead to cellular senescence. Rapamycin (Rapa) is well known to suppress cell senescence via mammalian target of rapamycin (mTOR) pathway. However, poor water solubility and lack of ROS scavenging ability limit the further development of Rapa. To improve the solubility of Rapa and endow with ROS scavenging ability, Rapa functionalized carbon dots (Rapa-CDs) are target-oriented synthesized via free radical polymerization combination with hydrothermal carbonization. Rapa-CDs improve the solubility of Rapa and show ROS scavenging abilities. The solubility of Rapa-CDs with 9.41 g is improved 3.6 × 104 times higher than that of Rapa (2.6 × 10-4 g). The half maximal inhibitory concentration (IC50) of Rapa-CDs toward hydroxyl radical (•OH) and 2,2-Diphenyl-1-picrylhydrazyl free radical (DPPH•) are 0.18 and 0.17 mg/mL, respectively. Rapa-CDs show anti-oxidative stress effect in HEVECs (Human Umbilical Vein Endothelial Cells) via reducing ROS levels by 87 %. Rapa-CDs alleviate HUVECs senescence by suppressing mTOR overactivation, attenuate the expression of P53, P21 and P16. The study demonstrates the target-oriented synthesis of drugs functionalized CDs with anti-senescence via dual-pathway of anti-oxidative stress and mTOR.
Insights
This study developed Rapamycin-functionalized carbon dots (Rapa-CDs) to combat vascular cell senescence and cardiovascular diseases. Rapa-CDs enhance Rapamycin
Area of Science:
- Biomaterials Science
- Nanotechnology
- Cardiovascular Research
- Cellular Senescence
Background:
- Vascular cell senescence contributes to cardiovascular diseases like hypertension and atherosclerosis.
- Oxidative stress from reactive oxygen species (ROS) induces cellular senescence.
- Rapamycin (Rapa) suppresses senescence via the mTOR pathway but suffers from poor solubility and lack of ROS scavenging.
Purpose of the Study:
- To enhance Rapamycin's solubility and introduce ROS scavenging capabilities.
- To develop Rapamycin-functionalized carbon dots (Rapa-CDs) for improved anti-senescence properties.
- To investigate the anti-senescence mechanisms of Rapa-CDs in endothelial cells.
Main Methods:
- Synthesized Rapa-CDs using free radical polymerization and hydrothermal carbonization.
- Quantified Rapa-CDs solubility and ROS scavenging efficacy (IC50 for hydroxyl and DPPH radicals).
- Assessed anti-oxidative stress effects in Human Umbilical Vein Endothelial Cells (HEVECs) by measuring ROS levels.
- Evaluated Rapa-CDs' impact on senescence markers (mTOR, P53, P21, P16) in Human Umbilical Vein Endothelial Cells (HUVECs).
Main Results:
- Rapa-CDs exhibited a 3.6 × 10^4 times increase in solubility compared to Rapamycin.
- Rapa-CDs demonstrated significant ROS scavenging abilities with low IC50 values for hydroxyl and DPPH radicals.
- Rapa-CDs reduced ROS levels in HEVECs by 87% and alleviated HUVEC senescence by suppressing mTOR overactivation.
- Rapa-CDs attenuated the expression of senescence-associated proteins P53, P21, and P16.
Conclusions:
- Target-oriented synthesis of drug-functionalized carbon dots (CDs) is feasible for anti-senescence applications.
- Rapa-CDs offer improved solubility and ROS scavenging, overcoming limitations of free Rapamycin.
- Rapa-CDs exert anti-senescence effects through dual pathways: anti-oxidative stress and mTOR inhibition.
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