Non-digestible stachyose promotes bioavailability of genistein through inhibiting intestinal degradation and first-pass metabolism of genistein in mice

Abstract

This study was designed to explore the molecular mechanism of stachyose in enhancing the gastrointestinal stability and absorption of soybean genistein in mice. Male Kunming mice in each group (n = 8) were administered by intragastric gavage with saline, stachyose (250 mg/kg·bw), genistein (100 mg/kg·bw), and stachyose (50, 250, and 500 mg/kg·bw) together with genistein (100 mg/kg·bw) for 4 consecutive weeks, respectively, and then their urine, feces, blood, gut, and liver were collected. UPLC-qTOF/MS analysis showed that levels of genistein and its metabolites (dihydrogenistein, genistein 7-sulfate sodium salt, genistein 4’-β-D-glucuronide, and genistein 7-β-D-glucuronide) in serum and urine were increased with an increase in stachyose dosages in mice. Furthermore, the feces level of genistein aglycone was also elevated by co-treatment of stachyose with genistein. However, the feces concentration of dihydrogenistein, a characteristic metabolite of genistein by gut microorganism, was decreased by stachyose administration in a dose-dependent manner. Additionally, the simultaneous administration with stachyose and genistein in mice could decrease intestinal SULT, UGT, P-gp, and MRP1 expression, relative to the treatment with individual stachyose or genistein. These results demonstrate that stachyose-mediated inhibition against the intestinal degradation of genistein and expression of phase II enzymes and efflux transporters can largely contribute to the elevated bioavailability of soybean genistein.

Antioxidant, antimicrobial, and antiproliferative activity-based comparative study of peel and flesh polyphenols from Actinidia chinensis

“…Vaporization heater and capillary heater were maintained at 100°C and 300°C, respectively. The analysis was carried out by following the methoof Lu et al (25) with slight modifications. Briefly, analysis was conducted in the scan mode (m/z) from 100 to 1,000 in selected ion monitoring mode of negative (m/z) 464 for isoquercetin, (m/z) 306 for epigallocatechin, (m/z) 168 for dihydroxyphenylacetic acid, (m/z) 290 for catechin, (m/z) 194 for ferulic acid, (m/z) 288 for epicatechin, (m/z) 169 for gallic acid, (m/z) 286 for kaempferol, (m/z) 301 for quercetin and (m/z) 609 for rutin.…”

Stachyose Improves the Effects of Berberine on Glucose Metabolism by Regulating Intestinal Microbiota and Short-Chain Fatty Acids in Spontaneous Type 2 Diabetic KKAy Mice

“…As a classic prebiotic, Sta has been proven to promote the growth of beneficial intestinal bacteria, inhibit pathogenic bacteria, and improve glucose metabolism (Liu et al, 2019;Liang et al, 2020). Moreover, Sta enhances the absorption of soybean genistein and tea polyphenols in mice (Li et al, 2016;Lu et al, 2017). Therefore, we hypothesized that Sta improves the actions of BBR on glucose homeostasis by regulating intestinal microbiota.…”

Genistein inhibits human papillary thyroid cancer cell detachment, invasion and metastasis

“…Owing to its structural similarity to endogenous estrogen 17 estradiol, Genistein is also called phytoestrogens and could bind with estrogen receptor and activate its downstream signaling pathway 14, 15. Lu et al found when the mice were administrated with genistein at 100 mg/kg, the serum concentrations of genistein was at an average of approximately 60 ng/ml, and stachyose could enhance the absorption of genistein in mice 16. Genistein was shown to be a potent inhibitor of the tyrosine-specific protein kinase RET , and has been used for clinical treatment of prostate carcinoma and non-small cell lung cancer 17-22.…”