Preparation Of 3MH-EGCG-nanoparticles And Its Antitumor Activities

(-)-Epigallocatechin gallate (EGCG) from green tea polyphenols has been widely recognized as a food active component which has strong biological activity and highly medicinal function. In addition, compare with other plant polyphenol, EGCG has the same drawbacks, namely, its application encounter is a bottleneck because of its low stability in gastrointestinal tract. 3-Mercapto hexanol (3MH), an artificial flavoring additive possesses high acitivity of antioxidation, it can properly enhance the antioxidantive capacity of EGCG, subject to certain conditions. In this paper,nanoparticles self-assembled with 3-Mercapto hexanol (3MH), beta-lactoglobulin (?-Lg) and EGCG by heat-induced technology was studied, the property of 3MH-EGCG-nanoparticles (MEN)and antitumor activity in vitro and in vivo were investigated.(1) The condition to prepare MEN was optimized. MEN was obtained with size of 46.81 nm,zeta potential -34.4mV and PDI 0.059, by using a molar ratio of P-Lg/EGCG at 1:32, and 3MH/EGCG at 1.2:1. The EGCG entrapment efficiency of the nanoparticles was 60.12%, and the EGCG loading amount was 1045.37 nmol · mg-1. Image from transmission electron microscope showed the nanoparticles have good dispersion homogeneity.(2) Experiments in vitro showed MEN with good appearance when stored at 4? or room temperature, and with good release properties, after 36h, its release rate of EGCG was 58.4%, at 37?, pH7.2. DPPH test showed that 3MH could significantly increase the scavenging capacities of the MEN on DPPH radicals, contrast with EGCG group. The experiment of acute toxicity showed a maximum dose of 100 mg EGCG/kg in MEN is safe for mice, and no side effects were observed from the various organs of animals.(3) The proliferation inhibition of cancer cells lines showed MEN have a high inhibition rate against human melanin tumor cell and human stomach cancer cells HGC-27. The IC50 for A-3 75 and HGC-27 was 32.44 ?g/mL and 38.44 ?g/mL (equivalence to EGCG). The experiment in vivo using nude mice of A-375 tumor-bearing showed that the tumor suppressing effect of MEN significantly improve compared to native EGCG. The inhibition rate of tumor reached 49.47 %,meanwhile, no injure from MEN was observed on the basis of the body weight, liver and spleen.