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. 2014 Dec:99:159-65.
doi: 10.1016/j.fitote.2014.09.018. Epub 2014 Oct 2.

In vitro human fecal microbial metabolism of Forsythoside A and biological activities of its metabolites

Shihua Xing  1 , Ying Peng  1 , Mengyue Wang  1 , Daofeng Chen  2 , Xiaobo Li  3
Affiliations

In vitro human fecal microbial metabolism of Forsythoside A and biological activities of its metabolites

Shihua Xing et al. Fitoterapia. 2014 Dec.

Abstract

The present study aimed to investigate the metabolism of Forsythoside A (FTA) by human fecal bacteria to clarify the relationship between its intestinal metabolism and its pharmacological activities. FTA was incubated with human fecal microflora in vitro to investigate its metabolic process, and highly sensitive and specific ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was performed using MetaboLynx software for metabolite analysis. Caffeic acid (CA) and hydroxytyrosol (HT) were obtained by hydrolysis of FTA, and CA was further hydrogenated to form 3,4-dihydroxybenzenepropionic acid (DCA). The anticomplementary, antimicrobial and antiendotoxin activities of FTA and its metabolites by human fecal microflora were evaluated in vitro with a hemolysis assay, the agar disc-diffusion method, the MIC value and the gel clot LAL assay, respectively. The metabolites showed higher biological activity than FTA, especially HT and DCA. Orally administered FTA may be metabolized to HT and DCA, and the pharmacological effects of FTA may be dependent on intestinal bacterial metabolism.

Keywords: 3,4-Dihydroxybenzenepropionic acid (PubChem CID: 348154); Anticomplement; Antiendotoxin; Antimicrobial; Caffeic acid (PubChem CID: 689043); Forsythoside A; Forsythoside A (PubChem CID: 45358127); Hydroxytyrosol (PubChem CID: 82755); Intestinal bacteria; Metabolite.

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Figures

None
Graphical abstract
Fig. 1
Fig. 1
TIC chromatograms of FTA incubated with human intestinal bacteria.
Fig. 2
Fig. 2
Time courses of FTA production over 24 h after incubation with human intestinal bacteria. The data are presented as the mean ± SD.
Fig. 3
Fig. 3
The possible metabolic pathway of FTA incubated with human intestinal bacteria.
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