1470302-79-4

Upstream product

• 24697-74-3 Leonurine 
• 2616-64-0 UDP-glucuronic acid 
• 530-57-4 3,5-dimethoxy-4-hydroxybenzoic acid 
• 208465-10-5 N²,N³-bis(tert-butoxycarbonyl)-N¹-(4-hydroxybutyl)guanidine 
• 6318-20-3 O-acetylsyringic acid 
• 1260119-23-0 3,5-dimethoxy-4-acetoxybenzoic acid 4-(N,N′-tert-butylcarbonylguanidino)butyl ester 

Relevant academic research and scientific papers

Identification of UDP-glucuronosyltransferase isoforms responsible for leonurine glucuronidation in human liver and intestinal microsomes

1. Leonurine is a potent component of herbal medicine Herba leonuri. The detail information on leonurine metabolism in human has not been revealed so far. 2. Two primary metabolites, leonurine O-glucuronide and demethylated leonurine, were observed and identified in pooled human liver microsomes (HLMs) and O-glucuronide is the predominant one. 3. Among 12 recombinant human UDP-glucuronosyltransferases (UGTs), UGT1A1, UGT1A8, UGT1A9, and UGT1A10 showed catalyzing activity toward leonurine glucuronidation. The intrinsic clearance (CLint) of UGT1A1 was approximately 15-to 20-fold higher than that of UGT1A8, UGT1A9, and UGT1A10, respectively. Both chemical inhibition study and correlation study demonstrated that leonurine glucuronidation activities in HLMs had significant relationship with UGT1A1 activities. 4. Leonurine glucuronide was the major metabolite in human liver microsomes. UGT1A1 was principal enzyme that responsible for leonurine glucuronidation in human liver and intestine microsomes.

Leonurine metabolite and preparation method thereof

The invention belongs to the field of medicine synthesis, and particularly relates to a leonurine main metabolite and a preparation method thereof. The main metabolite which has a structure shown in the formula (I) (please see the formula in the descripti