Mao Jie, Liu Shujun, Ai Min, Wang Zhuo, Wang Duowei, Li Xianjing, Hu Kaiyong, Gao Xinghua, Yang Yong
State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, Center for New Drug Safety Evaluation and Research, China Pharmaceutical University, Nanjing, 211198, China.
The Second Hospital of Nanjing, Nanjing, 320100, China.
J Hematol Oncol. 2017 Mar 20;10(1):71. doi: 10.1186/s13045-017-0442-y.
Melittin is the main effective component of bee venom and has extensive biological functions; however, serious side effects have restricted its clinical application. Preclinical and clinical studies showed that the main adverse events were allergic reaction and pain at the administration site. To decrease the toxicity, we prepared melittin nano-liposomes by encapsulating melittin with poloxamer 188 and explored the inhibitory activities on liver cancer together with biological safety. Here, we showed that melittin nano-liposomes significantly inhibited the survival of hepatocellular carcinoma (HCC) cells in vitro and prominently suppressed the growth of subcutaneous and orthotopic HCC transplantation tumors in vivo. It was important that it induced less inflammation and allergy in mice compared with melittin. Overall, melittin nano-liposomes would have a better application in HCC therapy due to its significant anti-tumor activity and better biological safety.
蜂毒肽是蜂毒的主要有效成分,具有广泛的生物学功能;然而,严重的副作用限制了其临床应用。临床前和临床研究表明,主要不良事件是过敏反应和给药部位疼痛。为降低毒性,我们用泊洛沙姆188包裹蜂毒肽制备了蜂毒肽纳米脂质体,并探讨了其对肝癌的抑制活性及生物安全性。在此,我们发现蜂毒肽纳米脂质体在体外显著抑制肝癌(HCC)细胞的存活,在体内明显抑制皮下和原位HCC移植瘤的生长。重要的是,与蜂毒肽相比,它在小鼠体内引起的炎症和过敏较少。总体而言,蜂毒肽纳米脂质体因其显著的抗肿瘤活性和更好的生物安全性,在HCC治疗中具有更好的应用前景。