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. 2022 Jan 25;27(3):777. doi: 10.3390/molecules27030777

Table 1.

Recent advances in bioavailability and metabolism studies carried out in animal models.

Matrix Bioactive Compounds Model
(Nº Animals/Volunteers)
Biological Samples Collection
Times
Technique
(Column)
Relevant Results (Metabolites, Reactions, etc.) Reference
Rosemary extract Flavonoids, diterpenes and triterpenes Mice model (in situ perfusion assay) (n = 7) Gastrointestinal liquid 5, 10, 15, 20, 25, 30 min HPLC–ESI–QTOF-MS
(RP-C18)
Several diterpenes and four new metabolites detected in plasma.
Sulfation and glucuronidation reactions.
[37]
Plasma End of the assay
Ginsenoside Rb1 Ginsenoside Rb1, Impact of 3 different fibers Male Sprague Dawley rats
(n = 32)
Plasma 0, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, and 48 h UHPLC–ESI–QQQ-MS (RP-C18) Secondary ginsenosides, especially ginsenoside CK, are the major active metabolites.
Prebiotics promote the proliferation of certain bacterial strains that improve the biotransformation and bioavailability of ginsenosides.
[76]
Feces -14 d, 0 h and 48 h
Quercetin glucoside mixture supplement Quercetin glucoside (Quercetin-3-O-glucoside) and its glucose adducts Male Wistar/ST rats
(n = 35)
Plasma Once in weeks 2, 4, 6, 8 HPLC–ESI–QQQ-MS (RP-C18) Three phases of quercetin metabolism, including cumulative, transient, and stable phases revealed.
Water-soluble dietary fibers, especially soybean fiber, enhanced quercetin bioavailability.
[69]
Urine Two times in weeks 2, 4, 6, 8
Feces Three times in weeks 2, 4, 6, 8
Tomato juice Lycopene, naringenin and chlorogenic acid Sprague Dawley rats
(n = 16)
Plasma End of experiment HPLC–ESI–IT-MS (RP-C18) Total cholesterol was lower after the intervention.
Low bioavailability of chlorogenic acid and naringenin.
[30]
Urine Daily for 5 weeks
Feces Daily for 5 weeks
Liver End of experiment
Arbequina table olives Hydroxytyrosol, tyrosol, verbascoside, luteolin, salidroside and p-coumaric acid Male Sprague-Dawley rats
(n = 7)
Plasma 0, 30 min HPLC–ESI-
QIT-MS
(RP-C18)
The possible metabolism suffered in the enterocytes cannot be underestimated.
Importance of different mechanisms of absorption depending on the
hydrophilic or lipophilic nature of the analyte.
[90]
Red raspberry Raspberry Ketone (4-(4-hydroxyphenyl)-2-butanone)) Mice
(Non-specified)
Plasma End of experiment UHPLC–ESI– QQQ-MS (RP-C18) 25 analytes identified as
RK-derived metabolites.
[31]
Brain End of experiment
Extra virgin olive oil (EVOO) Oleocanthal (OLC) Sprague-Dawley rats (n = 4) Intestinal fluid Every 5 min for 60 min UHPLC–ESI-QQQ-MS (RP-C18) Metabolism of phase I and II.
Higher levels of OLC are expected to reach human plasma vs. rat plasma.
[36]
Plasma and intestinal lumen End of experiment
Red grape polyphenols Flavanols, phenolic acids, cinnamic acids, valerolactone and valeric acid Wistar rats
(n = 12)
Serum 0, 2, 4, 7, 24, 48 h HPLC–ESI–QTOF-MS (RP-C18) Organic cultivation system influences the bioavailability and metabolism of polyphenols.
Phase II metabolites.
[80]
Red grape polyphenols Cinnamic acid, benzoic acid, flavonoid, phenylpropionic and phenylacetic acid Male Fischer-344 rats
(n = 54)
Serum End of experiment HPLC–ESI–QTOF-MS (RP-C18) Flavonoid phase II metabolites.
6 h of light per day improves bioavailability of phenolic compounds.
[81]
Calafate berry extract Anthocyanins and hydroxycinnamic acids Gerbils
(n = 18)
Plasma 0, 1, 2, 4, 8, 12 h GC–EI-
QQQ-MS (HP-5MS)
ß-oxidation products were detected. Hydroxycinnamic, benzoic, and phenylacetic acids derivatives.
No parental anthocyanins were detected.
[74]
Red wine extract. Flavan-3-ols, proanthocyanidins Male Sprague-Dawley rats
(n = 3)
Plasma 24 h UHPLC–ESI–Q-Orbitrap-MS (RP-C18) Phase II metabolism. Importance of the colonic microbiota in the transformation of proanthocyanidins. [60]
Urine 24 h
Feces 24 h
Corylin extract supplement Corylin metabolites Male SPF grade KM mice
(n = 18)
Plasma 0.5, 6 h UHPLC–ESI–QTOF-MS (RP-C18) Phase I metabolism of corylin.
Oxidation, hydration, glucuronidation and sulfation reactions.
[34]
Urine End of experiment
Feces End of experiment
Bile End of experiment
Grape pomace Phenolic acids and anthocyanins Male rats
(n = 30)
Urine 0, 6 and 14 months UHPLC–ESI–QTOF-MS
(RP-C18)
Methylated, sulfated and glucuronidated metabolites.
Growth inhibition of Clostridium.
[98]
Malaxinic acid and its aglycone Malaxinic acid (MA) and its aglycone (MAA) Male Sprague-Dawley rats
(n = 50)
Plasma 0, 15, 30, 60, 120, 240, 480 min HPLC–ESI–Q-IT-MS
(RP-C18)
Absence of intact forms of MA and MAA.
Glucuronide metabolites were detected.
[73]
Rice bran enzymatic extract Ferulic acid Male Wistar rats
(n = 50)
Plasma 0, 15, 30, 60 min
3, 6, 12, 18, 24 h
UHPLC–ESI–QQQ-MS (RP-C18) Sulfated metabolites and unconjugated simple aromatic acids.
Phase II metabolites.
[61]
Urine 0, 1, 2, 3, 4, 5, 6, 9, 24, 48 h
Feces 0, 24, 36, 48 h
Specific phenolic compounds Hydroxytyrosol, hydroxytyrosol acetate, DOPAC Sprague-Dawley rats
(n = 120)
Plasma 0, 0.5, 1, 2, 4, 8, 24 h UHPLC–ESI–QQQ-MS (RP-C18) Influence of the sex-linked metabolism on the excretion pattern.
The amounts of bioactive compounds did not result in a proportional increase in their plasma concentrations.
[83]

CK, compound K; DOPAC, dihydroxyphenyl acetic acid; EI, electronic impact; ESI, electrospray ionization; EVOO, extra virgin olive oil; GC, gas chromatography; HPLC, high-performance liquid chromatography; IT, ion trap; KM: Kunming mice; MA, malaxinic acid; MAA, malaxinic acid aglycone; MS, mass spectrometry; OLC, oleocanthal; Q, quadrupole; QQQ, triple quadrupole; QTOF, quadrupole time of flight; RP, reversed phase; RK, raspberry ketone (4-(4-hydroxyphenyl)-2-butanone)); SPF, specific pathogen-free; UHPLC, ultrahigh-performance liquid chromatography.