| A new glycopeptide(Meretrix meretrix glycopeptide, MGP0501) possessing antitumor activity was isolated from Meretrix meretrix. It's moleculer weight was measured as 15 878Da by SDS-PAGE. MGP0501 consists of 55.18% of saccharide and 44.82% of protein.The antitumor activity of MGP0501 was preliminary assayed in vitro by MTT method. The results revealed that MGP0501 can strongly inhibit the proliferation of human cancer cell strains A549, HO8910, HeLa, KB and SMMC-7721 in a dose-dependent manner, especially to mice cancer cell strain B16. MGP0501 presented good temperature tolerance and the best antitumor activity in neutral solution. It should be noticed that MGP0501 was innoxious to cultured mice spleen lymphocyte. Furthermore, MGP0501 could inhibit adhesion of tumor cells to extracellular martrix, with 50% inhibition rate in 9.5μg/mL. MGP0501 was thus presumed having inhibition to tumor cell migration and transferation.Antitumor effect of MGP0501 to the growth of S180, Heps and EAC in tumor-bearing mice were also assayed in this paper. At the dosage of 6mg/kg iv, MGP0501 had a distinct inhibition effect to the growth of S180 and Heps, with inhibition rate of 68.5% and 66.43%, respectively. Abnormal karyokinesis of tumor histocyte treated with MGP0501 was observed by microscope, which indicated the probable target of antitumor activity ofMGP0501。Mechanism in antitumor were also discussed in the paper. The damage effect of MGP0501 to tumor cell were observed in electronic scan microscope. Tumor cell treated with MGP0501 presented typical apoptosis characteristic in morphology including crenate membrane, condensed nuclear and margination of nuclear chromatin by cytoplasmic vacuolation. Nucleic DNA fractionized and profiled as ladders in agarose electrophoresis. Variation in cell cycle of treated tumor were measured by flow cytometer. Most of the... |