Uses of Oxaevodiamine Derivatives
A technology of heteroevodiamine and derivatives, which is applied in the field of oxaevodiamine derivatives, can solve the problems that have not been reported in the literature, and achieve the effect of reducing cytotoxicity
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Embodiment 1
[0033] Example 1: Four oxa-evodiamine derivatives have reduced cytotoxicity than evodiamine
[0034] Human neuroblastoma cells shy5y and human liver cancer cells hepG2 were seeded in 96-well plates respectively, with 10,000 cells per well. Cells were cultured overnight. The oxa-evodiamine derivatives of formulas I~IV were added to the cells cultured overnight, with a final concentration of 5 μg / ml. The addition of vehicle DMSO was used as a negative control, and the same concentration of evodiamine was used as a positive control (6 for each drug). repeat). The cells continued to be cultured for 48 hours, and the number of living cells was analyzed with CCK-8kit, and the results were as follows: figure 1 . The results showed that: compared with evodiamine, the cytotoxicity of the compounds of formulas I~IV to shy5y was respectively reduced by 77%, 67%, 87% and 110%; the cytotoxicity to hepG2 was respectively reduced by 250%, 210%, 170% and 260%, p<0.05.
Embodiment 2
[0035] Example 2: 4 kinds of oxa-evodiamine derivatives have enhanced antioxidant activity than evodiamine
[0036] Human neuroblastoma cells shy5y were seeded in 96-well plates at 10,000 cells per well. Cells were grown overnight. Add 4 kinds of oxa-evodiamine derivatives to the cells cultured overnight, the final concentration is 0.05 μg / ml, the addition of vehicle DMSO is used as negative control, and the same concentration of evodiamine is used as positive control (6 replicates for each drug) . After the cells were further cultured for 3 hours, hydrogen peroxide was added to each well to 200um / ml, and PBS was used as H 2 o 2 For the negative control, continue to cultivate for 24 hours, CCK-8kit analyzes the number of viable cells ( figure 2 ). The results showed that the four derivatives all had a good protective effect on the cell activity under the action of hydrogen peroxide, indicating that the four derivatives all had good antioxidant activity. Compared with ev...
Embodiment 3
[0037] Example 3: Therapeutic Effects of Four Oxaevodiamine Derivatives on Transgenic Dementia Mice
[0038] 4-month-old female APP / PS1 double transgenic dementia model mice and wild-type mice of the same age and sex were divided into 7 groups, 7 mice in each group, respectively wild control group, model control group, evodiamine treatment group, derivatives 49 treatment group, derivative 51 treatment group, derivative 58 treatment group, derivative 60 treatment group. Evodiamine and four oxa-evodiamine derivatives were respectively dissolved in 20% PEG / PBS solution, and injected intraperitoneally at a dose of 1.6 mg / kg body weight / day, 5 times a week for 4 consecutive weeks. The wild and model controls were given equal volumes of vehicle. One week after drug withdrawal, the water maze experiment was carried out in a conventional manner, trained for 5 days, and the spatial memory ability of the mice was detected on the 6th day ( image 3 ). The results showed that the resid...
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