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目的:研究从大风子科箣柊属植物南岭柞木(Xylosma controversumClos)与箣柊[Scolopiachinensis(Lour.)Clos]中分离得到的27个化合物对磷酸二酯酶是否具有抑制活性。方法:将化合物与蛇毒磷酸二酯酶在37℃孵育30 min后,检测磷酸二酯酶底物双(4-硝基苯基)磷酸酯的产物4-硝基酚在405 nm的吸收度值的变化来检测酶活性的变化。结果:从27个化合物中筛选到3个化合物儿茶素-5-O-β-D-吡喃葡萄糖苷、(±)-儿茶素和xylosmin对蛇毒磷酸二酯酶有较强抑制作用,且均具有良好的浓度抑制曲线,与阳性对照化合物EDTA-2Na和L-半胱氨酸相比较,它们对蛇毒磷酸二酯酶均具有中等的抑制作用,其中(±)-儿茶素的酶抑制作用最强。结论:南岭柞木化学成分儿茶素-5-O-β-D-吡喃葡萄糖苷和(±)-儿茶素及箣柊的化学成分xylosmin对蛇毒磷酸二酯酶有酶抑制活性。
Objective: To study whether 27 compounds isolated from Xylosma controversum Clos and Scolopiachinensis (Lour.) Clos have inhibitory activity against phosphodiesterase. METHODS: After the compound was incubated with venom phosphodiesterase at 37 °C for 30 min, the absorbance of 4-nitrophenol, the product of phosphodiesterase substrate bis (4-nitrophenyl) phosphate, was measured at 405 nm. The changes to detect changes in enzyme activity. RESULTS: Three compounds, catechin-5-O-β-D-glucopyranoside, (±)-catechin and xylosmin, were screened out from 27 compounds and had a strong inhibitory effect on venom phosphodiesterase. Both have a good concentration inhibition curve, and they have a moderate inhibitory effect on the venom phosphodiesterase compared to the positive control compounds EDTA-2Na and L-cysteine, of which (±)-catechins The strongest inhibitory effect. CONCLUSION: Xylosmin, the chemical constituent of catechin-5-O-β-D-glucopyranoside and (±)-catechin and saponin from Nanling eucalyptus, has enzyme inhibitory activity against venom phosphodiesterase.