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Therapeutic potential of liposome@azoramide in cancer by suppressing oxidative phosphorylation
Xin Wang1,2, Zihan Xu1,2, Yiyao Zeng1
1Division of Breast Surgery, Department of General Surgery, West China Hospital, Sichuan University, Chengdu, China.
Objective:
Targeting cancer cell metabolism represents a promising therapeutic strategy; however, metabolic reprogramming in tumor cells complicates the effectiveness of therapies aimed at disrupting these pathways.
Methods:
This study explored the potential of Azoramide, a compound previously associated with enhanced insulin sensitivity, to modulate cancer metabolism. Azoramide-loaded nano-liposomes (Lip@Azo) were prepared via the thin-film hydration method, chosen for its simplicity and efficiency. We evaluated the anti-tumor efficacy of Lip@Azo and investigated the underlying mechanisms.
Results:
We showed that azoramide effectively inhibits tumor growth by suppressing oxidative phosphorylation (OXPHOS) both in vitro and in vivo. Azoramide downregulated OXPHOS proteins, reduced mitochondrial respiration, and induced reactive oxygen species (ROS), leading to decreased mitochondrial ATP generation. Additionally, azoramide downregulated PGC-1α, a key regulator of mitochondrial function, disrupting mitochondrial homeostasis and further impairing tumor cell metabolism, which induced apoptosis and ferroptosis in cancer cells. To enhance the solubility and delivery of azoramide, we encapsulated the compound in liposomes (Lip@Azo), which significantly improved its therapeutic efficacy in vivo.
Conclusion:
Overall, our findings suggest that Lip@Azo is a promising strategy for targeting mitochondrial metabolism in cancer, offering a new avenue for therapeutic development in oncology.
Insights
Azoramide, delivered via liposomes (Lip@Azo), effectively inhibits cancer growth by targeting mitochondrial metabolism. This novel approach suppresses oxidative phosphorylation and induces cancer cell death, offering a promising new cancer therapy.
Area of Science:
- Oncology
- Metabolic Pathways
- Drug Delivery Systems
Background:
- Cancer cell metabolism is a key therapeutic target.
- Metabolic reprogramming in tumors presents challenges for existing therapies.
- Azoramide, known for insulin sensitivity, is explored for cancer treatment.
Purpose of the Study:
- To investigate Azoramide's potential to modulate cancer metabolism.
- To evaluate the anti-tumor efficacy and mechanisms of Azoramide-loaded liposomes (Lip@Azo).
Main Methods:
- Azoramide was encapsulated in liposomes (Lip@Azo) using thin-film hydration.
- In vitro and in vivo studies assessed anti-tumor efficacy.
- Mechanisms involving oxidative phosphorylation, ROS, PGC-1α, apoptosis, and ferroptosis were investigated.
Main Results:
- Azoramide suppressed tumor growth by inhibiting oxidative phosphorylation (OXPHOS) in vitro and in vivo.
- It reduced mitochondrial respiration, decreased ATP generation, and induced reactive oxygen species (ROS).
- Azoramide downregulated PGC-1α, leading to apoptosis and ferroptosis, with Lip@Azo enhancing therapeutic efficacy.
Conclusions:
- Lip@Azo demonstrates significant anti-tumor activity by targeting mitochondrial metabolism.
- This approach offers a novel therapeutic strategy for cancer treatment.
- Further development of Lip@Azo holds promise for oncology applications.
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