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肉苁蓉总苷在人工胃、肠液中的代谢转化研究 Δ

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王昕蕾 ，刘博男，张蒙蒙，刘贵玉，胡 扬，孙向明，李文兰（哈尔滨商业大学药学院，哈尔滨 150076）
中图分类号 R917 文献标志码 A 文章编号 1001-0408（2020）01-0053-09
DOI 10.6039/j.issn.1001-0408.2020.01.10

摘 要 目的：研究肉苁蓉总苷在人工胃、肠液中的代谢转化，推测其在体内的代谢转化途径。方法：采用超高效液相色谱串联飞
行时间质谱法。色谱柱为ACQUITY UPLC BEH，柱温为25 ℃，流动相为0.2％甲酸水-乙腈溶液（梯度洗脱），流速为0.2 mL/min，
检测波长为330 nm；离子源为电喷雾离子源，质荷比（m/z）为50→1 000；在正、负离子模式下，对肉苁蓉总苷在人工胃、肠液中的代
谢成分进行鉴定分析，并结合文献推测肉苁蓉总苷在人工胃、肠液中代谢途径。结果：肉苁蓉总苷经人工胃液代谢后，共推测出
69个成分，其中14个原型成分（如芥子醛葡萄糖苷、胡萝卜苷等）、55个代谢成分（如Methyl-O-Kankanoside J、Methyl-O-Kankano-
side E等），推测其代谢途径有甲基化、去甲基化、羟基化、甲氧基化、乙酰化、硫酸化、葡萄糖醛酸化。肉苁蓉总苷经人工肠液代谢
后，共推测出 90 个成分，其中 4 个原型成分（如 Kankanoside M、Kankanoside L 等）、86 个代谢成分（如 Methyl-O-Kankanoside、
Methyl-O-Kankanoside E等），推测其代谢途径有甲基化、去甲基化、羟基化、去羟基化、甲氧基化、乙酰化、硫酸化、葡萄糖醛酸化。
结论：本研究初步推测肉苁蓉总苷在人工胃、肠液中可能通过甲基化、去甲基化、羟基化等多种途径进行代谢转化，可为肉苁蓉总
苷的体内代谢转化研究提供参考依据。
关键词 肉苁蓉总苷；代谢；人工胃液；人工肠液；超高效液相色谱串联飞行时间质谱法；成分分析

Study on Metabolic Transformation of Total Glycosides of Cistanche deserticola in Artificial Gastric and
Intestinal Juice
WANG Xinlei，LIU Bonan，ZHANG Mengmeng，LIU Guiyu，HU Yang，SUN Xiangming，LI Wenlan（College of
Pharmacy，Harbin University of Commerce，Harbin 150076，China）
ABSTRACT OBJECTIVE：To study the metabolic transformation of total glycosides of Cistanche deserticola in artificial gastric
and intestinal juice，and to speculate its metabolic transformation pathway in vivo. METHODS：UPLC/Q-TOF-MS was adopted.
The determination was performed on ACQUITY UPLC BEH column with mobile phase consisted of 0.2％ formic acid
water-acetonitrile（gradient elution）at the flow rate of 0.2 mL/min. The detection wavelength was set at 330 nm，and column
temperature was 25 ℃. The ion source was electrospray ion source，and mass to charge ratio（m/z）was 50→1 000. In the positive
and negative ion mode，the metabolic components of the total glycosides of C. deserticola in artificial gastric and intestinal juice
were identified analysis，and combined with the literature，the metabolic pathway of total glycosides of C. deserticola in artificial
gastric and intestinal juice was speculated. RESULTS：After the total glycosides of C. deserticola were metabolized by artificial
gastric juice，and a total of 69 components were estimated，including 14 prototype components （such as Mustard aldehyde
glucoside，daucosstorol） and 55 metabolic components （such as Methyl-O-Kankanoside J，Methyl-O-Kankanoside E），it is
speculated that its metabolic pathways were methylation，demethylation，hydroxylation，methoxylation，acetylation，sulfation，and
glucuronidation. After the total glycosides of C. deserticola were metabolized by artificial intestinal juice，a total of 90 components
were estimated，including 4 prototype components（such as Kankanoside M，Kankanoside L）and 86 metabolic components（such
as Methyl-O-Kankanoside， Methyl-O-Kankanoside E）. It was speculated that its metabolic pathways were methylation，
demethylation，hydroxylation，dehydroxylation，methoxylation，acetylation，sulfation and glucuronidation. CONCLUSIONS：This
study preliminarily speculates that the total glycosides of C. deserticola may be metabolized by methylation，demethylation，
hydroxylation and other metabolic pathway in artificial gastrointestinal juice，which may provide reference for the in vivo metabolic
transformation of total glycosides of C. deserticola.
KEYWORDS Total glycosides of Cistanche deserticola；Metabolism；Artificial gastric juice；Artificial intestinal juice；UPLC/
Q-TOF-MS；Component analysis

肉苁蓉为列当科植物肉灰蓉（Cistanche desertico Wight]的干燥带鳞叶的肉质茎 。始载于《神农本草
[1]
La Y.C.Ma）或 花 肉 灰 蓉 [Cistanche tubulosa（Schenk） 经》，列为上品，性甘、咸、温，归肾、大肠经 。传统药理
[2]
学研究表明，肉苁蓉具有补肾阳、益精血、润肠通便等作
Δ 基金项目：黑龙江省科学基金项目（No.ZD2017014）；哈尔滨商
[3]
用 。现代药理学表明，其具有抗疲劳、抗衰老、增强机
业大学校科学基金项目（No.18XN083）
体免疫力及显著的拟雌激素作用 [4-7] 。目前，从肉苁蓉中
＊硕士研究生。研究方向：中药药效物质基础及质量标准化研
已分离并鉴定出多种化学成分，主要有苯乙醇苷类、环
究。E-mail：2715543753@qq.com
# 通信作者：教授，博士生导师。研究方向：中药药效物质基础及 烯醚萜苷类、木脂素类等，其中苯乙醇苷类是肉苁蓉中
质量标准化研究。E-mail：lwldzd@163.com 主要的活性成分 [8-12] 。为进一步追踪肉苁蓉总苷的代谢
中国药房 2020年第31卷第1期 China Pharmacy 2020 Vol. 31 No. 1 ·53 ·