新型金属卟啉光敏剂的合成及其抗菌活性

Synthesis and antibacterial activities of novel metalloporphyrins as photosensitizers

利用电中性的对苯二酚与2-硝基-5,10,15,20-四芳基卟啉反应,制备了一系列新型用于光动力治疗光敏剂研究的2-氢醌-5,10,15,20-四（4-2]羟基苯基）卟啉L和其配合物ML（M=Cu（Ⅱ）,Ni（Ⅱ）,Zn（Ⅱ））,产率达90%以上.以青霉素钠作对照,研究了该光敏剂对金黄色葡萄球菌（Staphylococcus aureus ATCC 25923）和大肠杆菌（Escherichia coli ATCC 25922）的抑菌活性.实验结果表明：光敏剂为NiL,浓度为80 μmol/L时,就能完全抑制金黄色葡萄球菌的生长,而相应的青霉素钠的浓度为320 μmol/L,但对大肠杆菌的作用不明显.因此,2-氢醌-5,10,15,20-四（4-羟基苯基）卟啉光敏剂在杀菌、消毒等方面具有很好的应用前景.

A series of 2 - hydroquinone - 5,10,15,20 - tetra（4 - hydroxylphenyl）- porphyrins and their complexes as new photosensitizers for photodynamic therapy were synthesized by direct reaction of 2 - nitro - 5,10,15,20 - tetra （4 - hydroxyl phenyl）- porphyrin and neutral hydroquinone with above 90% yields obtaining, and the antibacterial activities of 2 - hydroquinone - 5,10,15,20 - tetra （4 - hydroxylphenyl）- porphyrin and their complexes on Staphylococcus aureus （ATCC 25923 ） and Escherichia coli （ATCC 25922） were tested. The results show that Staphylococcus aureus （ATCC 25923） can be inhibited completely when the concentration is 0.08 mmol/L,and that of Na ampicillin is 0. 32 mmol/L. But it was not so effective on Escherichia coli （ATCC 25922）. Therefore, 2 - （hydroquinon - 2 - yl）- 5,10, 15,20 - tetra （4 - hydroxylphenyl）- porphyrin and its Ni （ Ⅱ ） complexes are potent and promising anti - Staphylococcus aureus agents.