机构：[1]Clinical Pharmacy Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.[2]NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.[3]TCM-Integrated Hospital, Southern Medical University, Guangzhou 510315, China.[4]State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Magnolol, the main active ingredient of Magnolia officinalis, has been reported to display anti-inflammatory activity. Sulfation plays an important role in the metabolism of magnolol. The magnolol sulfated metabolite was identified by the ultra-performance liquid chromatography to quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and a proton nuclear magnetic resonance (1H-NMR). The magnolol sulfation activity of seven major recombinant sulfotransferases (SULTs) isoforms (SULT1A1*1, SULT1A1*2, SULT1A2, SULT1A3, SULT1B1, SULT1E1, and SULT2A1) was analyzed. The metabolic profile of magnolol was investigated in liver S9 fractions from human (HLS9), rat (RLS9), and mouse (MLS9). The anti-inflammatory effects of magnolol and its sulfated metabolite were evaluated in RAW264.7 cells stimulated by lipopolysaccharide (LPS). Magnolol was metabolized into a mono-sulfated metabolite by SULTs. Of the seven recombinant SULT isoforms examined, SULT1B1 exhibited the highest magnolol sulfation activity. In liver S9 fractions from different species, the CLint value of magnolol sulfation in HLS9 (0.96 µL/min/mg) was similar to that in RLS9 (0.99 µL/min/mg) but significantly higher than that in MLS9 (0.30 µL/min/mg). Magnolol and its sulfated metabolite both significantly downregulated the production of inflammatory mediators (IL-1β, IL-6 and TNF-α) stimulated by LPS (p < 0.001). These results indicated that SULT1B1 was the major enzyme responsible for the sulfation of magnolol and that the magnolol sulfated metabolite exhibited potential anti-inflammatory effects.
基金：
This work was supported by the National Natural Science Foundation of China (grant
82074110, 81873080), the Open Project of State Key Laboratory of Natural Medicines (grant SKLNMKF202209),
Guangzhou Basic and Applied Basic Research Foundation (grant 202201011117), and
the Pharmacy Project of Guangdong Province Hospital Association (grant 2021YXQN01).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2021]版：
大类|3 区生物学
小类|3 区生化与分子生物学
最新[2025]版：
大类|3 区生物学
小类|3 区生化与分子生物学
第一作者：
第一作者机构：[1]Clinical Pharmacy Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
共同第一作者：
通讯作者：
通讯机构：[2]NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.[3]TCM-Integrated Hospital, Southern Medical University, Guangzhou 510315, China.[4]State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
推荐引用方式(GB/T 7714)：
Xie Cong,Hu Wanyu,Gan Lili,et al.Sulfation and Its Effect on the Bioactivity of Magnolol, the Main Active Ingredient of Magnolia Officinalis[J].Metabolites.2022,12(9):doi:10.3390/metabo12090870.
APA：
Xie Cong,Hu Wanyu,Gan Lili,Fu Bingxuan,Zhao Xiaojie...&Ye Ling.(2022).Sulfation and Its Effect on the Bioactivity of Magnolol, the Main Active Ingredient of Magnolia Officinalis.Metabolites,12,(9)
MLA：
Xie Cong,et al."Sulfation and Its Effect on the Bioactivity of Magnolol, the Main Active Ingredient of Magnolia Officinalis".Metabolites 12..9(2022)
