| Porphyrins and metalloporphyrins are significant function-substances, which exist in nature widely. They have been applied in analytical chemistry, medicine, bionics, protecting environment widely. Many novel porphyrin-based photosensitizers have been developed for the photodynamic therapy (PDT) of tumor and other illness. Low damage, small side-effect and therapy repeatly are the advantages of PDT. In bionics, metalloporphyrins can be model compounds of some big functiona-molecules and substitute for them to realize some physiological functions.Hematoporphyrin compound is one kind of the porphyrins, prepared from hemachrome (heme), can selectively stay in cancer cells and has special affinity to them. Metronidazole has sensitizing effect to radiation and chemotherapy. Because metronidazole distributes all of the tissues when it is injected into the body and unable to control the drug concentration in tumor, so it has sensitizing effect to normal tissues more or less. We synthesized hematoporphyrin-metronidazole compounds by connecting hematoporphyrin and metronidazole. It is expected that porphyrin makes the biological guide effect and the new compounds have better therapy effect.In this paper, we have developed two new techniques of high purity heme preparation. The purity of heme could be more than 99% and the production of heme could be 73.3% by these methods. The cost ofproduction is reduced to Y35/g. The method is quick and easy, could be applied in industrial production.Hematoporphyrin dimethyl ether metronidazole (HDMEM) was synthesized from heme. Their structures have been characterized by IR, UV-VIS, NMR and MS. The researches of fluorescent properties of new compounds have been done through fluorescent scanning spectrum. The results indicate that the new compounds still have the same fluorescent properties as the porphyrin compounds. The in vitro antitumor activities of HDMEM have been initially tested by trypan blue infiltration, It is investigated that the new compounds have good in vitro antitumor activities. In addition, we have synthesized Cu, Zn, Mn, Co four metalloporphyrins, the structures of them have been confirmed by IR and UV-VIS. An assay of their superoxide dismutase (SOD) activity was performed by means of riboflavin-methionine photoreduction method. Their catalase (CAT) activity have been demonstrated by means of spectrophotometry. It has been found that Cu, Mn, Co metalloporphyrins possess excellent scavenging O·2- and decomposing H2O2 functions in the range of 10-5-10-6mol/L.
|
PDF Full Text Request