Metabolites of Medicarpin and Their Distributions in Rats

Abstract

Medicarpin is a bioactive pterocarpan that has been attracting increasing attention in recent years. However, its metabolic fate in vivo is still unknown. To clarify its metabolism and the distribution of its metabolites in rats after oral administration, the HPLC-ESI-IT-TOF-MSn technique was used. A total of 165 new metabolites (13 phase I and 152 phase II metabolites) were tentatively identified, and 104, 29, 38, 41, 74, 28, 24, 15, 42, 8, 10, 3, and 17 metabolites were identified in urine, feces, plasma, the colon, intestine, stomach, liver, spleen, kidney, lung, heart, brain, and thymus, respectively. Metabolic reactions included demethylation, hydrogenation, hydroxylation, glucuronidation, sulfation, methylation, glycosylation, and vitamin C conjugation. M1 (medicarpin glucuronide), M5 (vestitol-1’-O-glucuronide) were distributed to 10 organs, and M1 was the most abundant metabolite in seven organs. Moreover, we found that isomerization of medicarpin must occur in vivo. At least 93 metabolites were regarded as potential new compounds by retrieving information from the Scifinder database. This is the first detailed report on the metabolism of ptercarpans in animals, which will help to deepen the understanding of the metabolism characteristics of medicarpin in vivo and provide a solid basis for further studies on the metabolism of other pterocarpans in animals.

Active Antioxidant Phenolics from Brazilian Red Propolis: An Optimization Study for Their Recovery and Identification by LC-ESI-QTOF-MS/MS

“…Compound 25 was characterized as medicarpin according to the precursor ion at m / z 269.0827. In its MS 2 spectra, the following typical product ions were detected: 254.0594([M–H–CH3 • ] − ), 225.0540, 105.0191, 121.0300 (C 7 H 5 O 2 , 3,5 A − )and 133.0287 [ 49 ]. Compound 27 (with [M–H] − at m / z 283.0619) and compound 28 (with [M–H] − at m / z 283.0988) were tentatively identified as 5,1′-Dihydroxy-7-methoxyisoflavone and 3,9-Dimethoxypterocarpan, respectively.…”

Research on Effect and Mechanism of Xuefu Zhuyu Decoction on CHD Based on Meta-Analysis and Network Pharmacology

“…Luteolin can improve ventricular function and reduce coronary reperfusion [ 43 ] and thrombotic tendency [ 44 ]. Medicarpin and its metabolites were transported in most organs of the body [ 45 ] and can promote the publication of other ingredients. Formononetin substantially attenuates the generation of atherosclerosis [ 46 ].…”

Heterologous biosynthesis of medicarpin using engineered Saccharomyces cerevisiae

“…Pterocarpans are abundant in medicinal plants, such as Pueraria Lobata and Hedysari Radix . Pterocarpans have diverse bioactivities, including anti-tumor, anti-osteoporosis, anti-bacterial, anti-inflammation, antioxidant, anti-estrogenic, inhibition of acetylcholinesterase and neuraminidase, and immunosuppressive activities [ 1 ]. Therefore, pterocarpans are potential drugs for the treatment of various diseases.…”