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 (β-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 μg/mL and 38.44 μg/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.