A novel melittin nano-liposome exerted excellent anti-hepatocellular carcinoma efficacy with better biological safety.
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.
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.
Jie
J
Mao
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.
Shujun
S
Liu
The Second Hospital of Nanjing, Nanjing, 320100, China.
Min
M
Ai
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Zhuo
Z
Wang
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.
Duowei
D
Wang
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.
Xianjing
X
Li
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.
Kaiyong
K
Hu
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. 1620154324@cpu.edu.cn.|Institute of Pharmaceutical Science, China Pharmaceutical University, No 639, Longmian Rd., Nanjing, 211198, China. 1620154324@cpu.edu.cn.
Xinghua
X
Gao
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. valianty@hotmail.com.|Institute of Pharmaceutical Science, China Pharmaceutical University, No 639, Longmian Rd., Nanjing, 211198, China. valianty@hotmail.com.
Yong
Y
Yang
D000818:Animals; D001516:Bees; D002214:Capsules / Q000737:chemistry; D006528:Carcinoma, Hepatocellular / Q000150:complications / Q000188:drug therapy*; D064593:Heterografts; D006801:Humans; D006967:Hypersensitivity / Q000517:prevention & control; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D008081:Liposomes; D008113:Liver Neoplasms / Q000150:complications / Q000188:drug therapy*; D008555:Melitten / Q000008:administration & dosage* / Q000009:adverse effects / Q000633:toxicity; D051379:Mice; D053758:Nanoparticles; D020442:Poloxamer / Q000627:therapeutic use*
D002214:Capsules; D008081:Liposomes; D020442:Poloxamer; D008555:Melitten
Anti-tumor activity; Bee venom; Biological safety; Melittin nano-liposomes