Abstract
α-Mangostin (αM), a traditional natural product with promising application of treating a series of diseases, was limited use in clinical due to its hydrophobicity. Herein, MPEG-PCL nanomicelles were used to embed the αM for resolving hydrophobicity and improving the anti-melanoma effect of the αM. The anti-melanoma activity and potential mechanisms of biodegradable αM/MPEG-PCL nanomicelles were investigated. The αM/MPEG-PCL nanomicelles possessed a stronger effect on anti-melanoma compared to the free αM both in vitro and in vivo with a low cytotoxicity in non-tumor cell lines. In the research of mechanisms, the αM/MPEG-PCL nanomicelles inhibited the proliferation of melanoma cell, induced apoptosis via both apoptosis pathways of intrinsic and exogenous in vitro, as well as suppressed tumor growth and restrained angiogenesis in vivo, which implied that the αM/MPEG-PCL nanomicelles have potential application as a novel chemotherapeutic agent in melanoma therapy.
Highlights
Nanotechnology, an international gold rush, is a revolutionizing and rapidly evolving technology inspiring many areas in this word[1,2]
The mixture was dissolved in normal saline solution, which allowed the αM self-assembled into the MPEG-PCL nanomicelles
The MPEG-PCL nanomicelles were successfully applied in resolving the poor aqueous solubility of the αM and enhancing the activity of anti-melanoma
Summary
Nanotechnology, an international gold rush, is a revolutionizing and rapidly evolving technology inspiring many areas in this word[1,2]. The progress and exploitation of nanotechnology in medicine have conquered tremendous breakthrough in human health career[3,4]. The effective nanotechnology is of great significance in the improvement of nanomedicine which has received extensive attention in application of gene therapy, personalized treatments, and precision medicine for oncotherapy[5,6,7], notably the development of new drug delivery. Yang et al Cell Death and Disease (2019)10:146. One of the more promising ways to treat melanoma is the application of nanomedicine. Africa and its peel had used for centuries as a traditional medicine to cure inflammation, ulcer, skin infection, wound healing, and other diseases. Α-Mangostin (αM) (Fig. 1a), the major xanthone derivative, is the most important secondary metabolite extracted from the pericarp of mangosteen[19,20,21]. The αM is a strong oleophilic compound with poor aqueous solubility[25], which limits its clinical applications
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