1 Unlike traditional chemotherapeutic agents, ATRA results in high complete remission rates, but without adverse effects, such as bone marrow hypoplasia. Since the 1980s, the medical drug all- trans retinoic acid (ATRA) has been clinically utilised for the treatment of acute promyelocytic leukemia. Keywords: nano-drugs, self-assembly, retinoid, cancer therapy, melanoma

Importantly, RHA nanoparticles inhibited the growth of xenograft tumors without obvious impact on haematological indexes and hepatorenal function of these tumor-bearing mice.Ĭonclusion: Our findings demonstrate the promise of RHA nanoparticles in treating malignant melanoma tumors with high efficacy and low toxicity.

However, opposite to our initial hypothesis, pre-treating the melanoma cells with RAR antagonists showed no impact on inhibitory effect of RHA nanoparticles, which suggested that the target of the molecule on melanoma cells is not RAR and retinoid X receptor (RXR). Results: RHA could form nanoparticle formation by self-assembly and abrogates growth of several solid tumor cell lines even after RHA nanoparticles’ washout. The putative synergic anticancer mechanism of activating retinoic acid receptor (RAR) and inhibiting HDAC were investigated via receptor inhibitor rescue assay and in vitro enzyme activity assay, respectively. Both in vitro cell viability, colony formation assay, and in vivo xenograft mouse tumor model were employed here to study anticancer activity of RHA nanoparticles. Methods: RHA nanoparticles were observed under transmission electron microscope (TEM). Although RHA was synthesized in 2005, its nanoscale self-assembly property, anticancer activity, and possible related mechanism are still unclear.

Retinoic hydroxamic acid (RHA) is a “fusion drug” of all-trans retinoic acid (ATRA) and vorinostat, a histone deacetylase (HDAC) inhibitor showing synergic effect with ATRA on cancer therapy. These carrier-free self-assembly nanomaterials are helpful to co-deliver two synergic drugs to the same site regardless of pharmacokinetic properties of individual drugs. Scientific Research Center for Translational Medicine, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 457 Zhongshan Road, Dalian 116023, People’s Republic of Chinaīackground: Amphiphilic fusion drugs are covalent conjugates of a lipophilic drug and a hydrophilic drug or their active fragments. Han Liao, 1, 2 Shan Zhao, 1, 2 Huihui Wang, 1, 2 Yang Liu, 1 Ying Zhang, 1 Guangwei Sun 1ġScientific Research Center for Translational Medicine, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, People’s Republic of China 2University of Chinese Academy of Sciences, Beijing 100049, People’s Republic of China

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