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狼毒大戟中4种二萜类成分在大鼠肝微粒体中的代谢
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| 篇名： | 狼毒大戟中4种二萜类成分在大鼠肝微粒体中的代谢 |
| TITLE： | Metabolism of four diterpenoids of Euphorbia fischeriana in liver microsomes of rats |
| 摘要： | 目的 研究狼毒大戟中4种二萜类成分在大鼠肝微粒体中的代谢产物并探讨其代谢规律。方法运用大鼠肝微粒体体外孵育法，将岩大戟内酯A、岩大戟内酯B、17-羟基岩大戟内酯A、17-羟基岩大戟内酯B加至由还原型烟酰胺腺嘌呤二核苷酸磷酸启动的大鼠肝微粒体孵育体系中，于37℃条件下孵育30min，再用乙腈终止反应。以阴性组（先加乙腈再启动孵育30min）为参考，采用超高效液相色谱-四极杆-飞行时间质谱联用技术，利用Analyst®TF1.7.1、PeakView®2.2、MetabolitePilot1.5、MasterView1.2软件对其质谱裂解规律和代谢产物进行推测与鉴定。结果4种二萜类成分在二级质谱中均易丢失H2O和CO等中性碎片。岩大戟内酯A和17-羟基岩大戟内酯A在肝微粒中的代谢反应主要为二羟基化、脱氢和一羟基化反应，分别鉴定出6、5个代谢产物。岩大戟内酯B和17-羟基岩大戟内酯B在肝微粒体中的代谢反应主要为一羟基化、水合和同分异构化反应，均鉴定出5个代谢产物。结论岩大戟内酯A和17-羟基岩大戟内酯A在大鼠肝微粒体中均产生了羟基化及脱氢代谢产物，岩大戟内酯B和17-羟基岩大戟内酯B在大鼠肝微粒体中均产生了羟基化、水合及同分异构化代谢产物。4种二萜类成分的代谢产物均是Ⅰ相代谢产物。 |
| ABSTRACT： | OBJECTIVE To study the metabolites of four diterpenoids of Euphorbia fischeriana in liver microsomes of rats and to investigate its metabolic regularity. METHODS In vitro incubation system of liver microsomes of rats was built. The jolkinolide A，jolkinolide B ，17-hydroxyl jolkinolide A and 17-hydroxyl jolkinolide B were added into incubation system of liver microsomes in rats activated by reduced nicotinamide adenine dinucleotide phosphate ，incubated at 37 ℃ for 30 min，and then terminated the reaction with acetonitrile. Taking the negative group （adding acetonitrile firstly and then starting incubation for 30 min）as the reference，the ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry was used ；Anaylyst®TF 1.7.1、PeakView® 2.2，MetabolitePilot 1.5 and MasterView 1.2 software were used to speculate and identify the fragmentation law of mass spectrometry and metabolites. RESULTS Four diterpenoids were easy to lose neutral fragments such as H 2O and CO in secondary mass spectrometry. Jolkinolide A and 17-hydroxyl jolkinolide A showed similar metabolism pathway ，including dihydroxylation，dehydrogenation，and monohydroxylation ；six and five metabolites were identified respectively. Jolkinolide B and 17-hydroxyl jolkinolide B showed similar metabolism pathway ，including monohydroxylation ，hydration and isomerization. Five metabolites were identified. CONCLUSIONS Both jolkinolide A and 17-hydroxyl jolkinolide A produce the metabolites of hydroxylation and dehydrogenation in liver microsomes of rats ；both jolkinolide B and 17-hydroxyl jolkinolide B produce the metabolites of hydroxylation ，hydration and isomerization in liver microsomes of rats. The metabolites of four diterpenoids are phase Ⅰ metabolites. |
| 期刊： | 2022年第33卷第04期 |
| 作者： | 马天成，马玉坤，孙珈，张金玲，郭丽娜，刘琦，孙宇 |
| AUTHORS： | MA Tiancheng，MA Yukun，SUN Jia，ZHANG Jinling，GUO Lina，LIU Qi，SUN Yu |
| 关键字： | 狼毒大戟；二萜类成分；超高效液相色谱-四极杆-飞行时间质谱联用技术；大鼠肝微粒体；体外代谢 |
| KEYWORDS： | Euphorbia fischeriana；diterpenoids；ultra-high performance liquid chromatography-quadrupole time-of-flight mass |
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