Study On Synthesis And Biological Activity Of Ascorbic Acid Sesquioxide Ge(Ⅳ) Compound

OBJECTIVE Studying route of synthesis of the ascorbic acid sesquioxide Ge(â…£). Identifying the structure of this coordination compound, researching the biological activity of the compound, which containing three aspects : toxicity, activity of anti- tumor, inhibition of new blood vessel on chick embryo chorioallantoic membrane (CAM).METHODS Germanium dioxide as raw material , a new ascorbic acid sesquioxideGe(â…£) compound was first synthesized by the reaction of germanium chloroforme (GeHCl3)with double bond of ascorbic acid. The structure of this compound was characterized by elemental analysis, IR and UV. In the process of studying toxicity, confined by concentration and volume of the medicine, LD₅₀ could not be measured. Rat's maximum tolerated dose (MTD) was 9 g/kg. In order to know the inhibitory effect on S₁₈₀and H₂₂, Rat's maximum tolerated dose(MTD) as high concentration, selecting middle, and lowconcentration, the different dose of the medicine were poured into the stomach of mouse, to count restraining tumor rates after experiment, which responsing inhibitory effect on S180 and H₂₂ . And the relationship between inhibitory effect and dose was determined. The ascorbic acid Sesquioxide Ge(â…£) loaded with methylcellulose membranes was put on chick CAM surface of 7-day-old eggs and continued incubating for 48 hours . Local vessel density was measured under dissection microscope. The inhibitory effects on CAM angiogenesis were demonstrated.RESULTS Ascorbic acid Sesquioxide Ge(â…£)was synthesized by by the reaction of germanium chloroforme (GeHCl₃)with double bond of ascorbicacid, which has the structure of (?) in its molecule. The chemical formula is (GeC₆H₉O₆)₂O₃. During studying toxicity, confined by medicine concentration or volume, LD₅₀ could not be measured. Rat's maximum tolerated dose (MTD) was 9 g/kg. Ascorbic Acid SesquioxyGe(â…£) had significant restraining function to the tumors of S₁₈₀ and H₂₂ Average inhbiting tumor rate were 61.8%, 68.2%, respectively, which outstrip control group. The Ge(â…£) complex has inhibitory effects on formation of chick CAM. The three different doses, 2.5mg/egg, 1.5mg/egg and 0.5mg/egg, dose-dependently decreased the density of local blood vessels.CONCLUSION Ascorbic acid Sesquioxide Ge(â…£) is new compound with very low toxicity. The copound has inhibitory effects on S₁₈₀ and H₂₂, inhibitory effects on angiogenesis of chick CAM angiogenesis.