. 2020 Nov 20;25(22):5431. doi: 10.3390/molecules25225431

Table 1.

Flavonoids with gastroprotective and/or anti-ulcer activity.

Compound	Natural and/or Food Source	Experimental Protocol/Dose	Route Administration/Organism Test	Effect or Mechanism	Reference
Flavonols
Quercetin	Food source: onions, broccoli, apple, cherry and grape	in vivo Ethanol—2.5 mg/kg	(p.o.)/Rat	↓ MMP-9, iNOS, MPO ↑GSH	[53]
		in vivo NSAIDs (indomethacin)—50 and 100 mg/kg	(p.o.)/Rat	↑ Nrf2, SOD, GPx ↓ ICAM-1, MPO, P-selectin	[55]
		in vitro NSAIDs (indomethacin)—0.0331 mMol/L	Caco-2 cell	↓ NF-κB, IL-8	[55]
		in vitro anti-H. pylori—0.000212–0.423 mMol/L	Cell culture	Inhibition	[56]
		in vivo anti-H. pylori—25 mg/kg	(p.o.)/Mice	↓ TNF-α, IL-1β	[56]
Kaempferol	Food source: broccoli, cabbage, beans, leeks, tomatoes, strawberries, grapes and propolis	in vivo Ethanol—40, 80 and 160 mg/kg	(p.o.)/Mice	↓ MPO, TNF-α, IL-1β, IL-6 ↑ NO	[46]
Kaempferol		in vitro anti-H. pylori—0.0015625 to 0.2 mMol/L	AGS cells	↓ CagA, VacA, TNF-α, IL-1β, IL-8	[47]
Kaempferide	Propolis	in vivo Pylorus ligature—3 mg/kg	(i.g)/Mice	↓ pH, H⁺ concentration, secretion of volume, pepsin activity	[48]
Kaempferide	Propolis	in vivo HCl/Ethanol—3 mg/kg	(i.p)/Mice	↑ SOD, CAT, GST, mucus ↓ MPO	[48]
Morin	Species of Moraceae family	in vivo NSAIDs (indomethacin)—50 mg/kg	(p.o.)/Rat	↓ MPO, NF-κB, TNF-α, iNOS, ICAM-1, IL-6, caspase-3 ↑ PGE₂, SOD	[60]
Quercitrin	Solidago chilensis	in vivo HCl/Ethanol—1, 38 mg/kg	(p.o.)/Mice	↑ GSH ↓ MPO	[68]
Quercitrin	Solidago chilensis	in vitro Proton pump activity—0.00223 to 0.223 mMol/L	Cell culture	Inhibition	[68]
Afzelin	Solidago chilensis	in vivo HCl/Ethanol—0.026 and 0.078 mg/kg	(p.o.)/Mice	↓ MPO	[68]
Afzelin	Solidago chilensis	in vitro Proton pump activity—0.00231 to 0.231 mMol/L	Cell culture	Inhibition	[68]
Rutin	Food source: tomatoes, orange, carrots, sweet potatoes, black tea, and apple peels	in vivo NSAIDs (indomethacin)—200 mg/kg	(p.o)/Rat	↑ GSH, SOD ↓ MPO	[63]
		in vivo-Ischemia and reperfusion—50, 100, and 200 mg/kg	(p.o)/Rat	↓ iNOS, MPO, MDA	[64]
		in vivo Ethanol—20, 40 and 80 mg/kg	(p.o)/Rat	↓ MDA ↑ GPx	[65]
		in vivo Acetic Acid—20, 40 and 80 mg/kg	(p.o)/Rat	↓ MDA ↑ GPx	[65]
		in vitro Proton pump activity—IC₅₀ of 0.0590 mMol/L	Cell culture	Inhibition	[66]
Flavanols
Catechin	Green tea	in vivo NSAIDs (ketoprofen)—25 mg/kg	(p.o)/Rat	↑ GPx, GR, Nrf2	[73]
Epicatechin	Green tea	in vivo Pylorus ligature—25 and 50 mg/kg	(p.o)/Rat	↓ H⁺ secretion	[72]
Epicatechin	Green tea	in vivo Ethanol—25 and 50 mg/kg	(p.o)/Rat	↑ Mucus, SHs, NO, SOD, HSP-7	[72]
Epigallocatechin gallate	Green tea	in vivo NSAIDs (indomethacin)—0,5, 1, 2, 3 and 5 mg/kg	(p.o)/Rat	↓ iNOS, MPO ↑ Mucin, PGE₂	[70,71]
Flavones
Isoorientin	Gentiana triflora and Eremurus spectabilis	in vivo NSAIDs (indomethacin)—25, 50, 100 mg/kg	(p.o)/Rat	↓ MDA ↑ GSH, SOD	[98]
Chrysin	Passiflora incarnate, Oroxylum indicum, Matricaria chamomilla, propolis	in vivo NSAIDs (indomethacin)—50 and 100 mg/kg	(p.o)/Rat	↑ Mucus, GSH, CAT, VEGF ↓ MDA	[89]
Chrysin		in vivo Acetic Acid—10 mg/kg	(p.o)/Mice	↓ COX-2, MMP-9, caspase-3 ↑ EGF, COX-1	[90]
Nobiletin	Citrus fruits	in vivo Ethanol—5, 10 or 20 mg/kg	(p.o)/Mice	↑ PGE₂, SOD ↓ TNF-α, IL-6	[103]
Baicalein	Scutellaria baicalensis	in vivo HCl/Ethanol—10, 30 and 100 mg/kg	(p.o)/Mice	↑ SHs, NO, GSH, mucus ↓ MPO	[81]
		in vitro Proton pump activity—0.0370 and 0.111 mMol/L	Culture cell	Inhibition	[81]
		in vitro anti-H. pylori—IC₅₀ 0.331 mMol/L	AGS cells	↓ IL-8, Vac A, capacity of adhesion	[82]
Baicalin	Scutellaria baicalensis	in vivo Pylorus ligature—5, 10 and 15 mg/kg	(p.o)/Rat	↓ H⁺ secretion	[83]
		in vivo Acetic Acid—6.5 and 13 mg/kg	(p.o)/Rat	↑ SOD, GSH, GPx ↓ MDA, IL-8, TNF-α	[85]
		in vitro anti-H. pylori—IC₅₀ 0.431 mMol/L	GES-1 cells	↓ IL-8, IL-1β, Vac A, urease, adhesion, hefA	[82,84]
Diosmin	Citrus fruits (lemon)	in vivo Ethanol—100 mg/kg	(p.o)/Mice	↓ TNF-α, NF-kB, MPO, caspase-3, Cit C, Bcl2 ↑ IL-10, GSH, GPx, PGE₂, NO	[92]
Diosmin	Citrus fruits (lemon)	in vitro anti-H. pylori—CIM 0.822 mMol/L	Culture cell	Inhibition	[93]
Flavanones
Naringin	Citrus fruits (orange, lemon)	in vivo Ethanol—100 and 200 mg/kg	(p.o)/Rat	↓ MDA, IL-6, TNF-α, caspase-3 ↑ GSH, SOD	[107]
Pinostrobin	Boesenbergia rotunda	in vivo Ethanol—20 and 40 mg/kg	(p.o)/Rat	↓ COX-2	[109]
Flavanones
Hesperidin	Citrus fruits (orange, lemon)	in vivo NSAIDs (indomethacin)—150, 300 and 450 mg/kg	(p.o)/Rat	↑ GSH, SOD, CAT	[117]
		in vivo Ethanol—50 mg/kg	(p.o)/Rat	↓ COX-2, TNF-α, MDA ↑ SOD, CAT, GPx	[119]
		in vivo Stress—100 mg/kg	(p.o)/Rat	↑ GSH, SOD, CAT, mucin ↓ MDA	[120]
		in vivo Acetic Acid—3 and 10 mg/kg	(p.o)/Rat	↑ Mucin, GSH, SOD, CAT ↓ MPO	[121]
		in vitro anti-H. pylori—0.05–0.5 mMol/L	Culture cell	Inhibition	[122]
Neohesperidine	Citrus fruits (orange, lemon)	in vivo NSAIDs (indomethacin)—100 mg/kg	(p.o)/Rat	↓ COX-2, TNF-α, MDA ↑ GSH	[116]
Isoflavonoids
Genistein	Soy-based foods (Glycine max or Soy hispida)	in vivo NSAIDs (indomethacin)—10 mg/kg	(p.o)/Rat	↓ TNF-α, MDA, iNOS ↑ SOD, PGE₂	[125]
Genistein	Soy-based foods (Glycine max or Soy hispida)	in vivo NSAIDs (indomethacin)—10 mg/kg for 7 days	(p.o)/Rat	↑ NO, PGE₂, SOD ↓ MDA, TNF-α, MPO	[126]
Biochanin A	Soy-based foods	in vivo Ethanol—25 and 50 mg/kg	(p.o)/Rat	↑ NO, SOD ↓ MDA	[129]
Furanoflavonoids
Karanjin	Pongamia pinnata	in vivo Ethanol—10 and 20 mg/kg	(p.o)/Rat	↑ CAT, GPx, SOD ↓ MDA	[133]
Karanjin	Pongamia pinnata	in vitro Proton pump activity-0.0273–0.192 mMol/L	Culture cell	Inhibition	[133]
Biflavonoids
Kolaviron	Garcinia kola	in vivo Ethanol—100 and 200 mg/kg	(p.o)/Rat	↑ NO, mucus ↓ MDA	[138]
Kolaviron	Garcinia kola	in vitro Proton pump activity—IC₅₀ of 0.0744 mMol/L	Culture cell	Inhibition	[139]
Other flavonoids
Silymarin	Silybum marianum	in vivo Ethanol—50 mg/kg	(p.o)/Rat	↓ MPO, TNF-α, IL-6, NF-kB ↑ GPx, SOD, Nfr2	[149,150]

Legend: Bcl2-B-cell lymphoma-2; CagA-Cytotoxin associated gene A; CAT–Catalase; COX–Cyclooxygenase; GPx - Glutathione peroxidase; GSH-Glutathione; GST-Glutathione transferase; HSP-7-Heat shock protein-7; IL-10-Interleukin 10; IL-1β-interleukin 1 β; IL-6–Interleukin 6; IL-8–Interleukin 8; iNOS-Inducible nitric oxide synthase; MDA–Malondialdehyde; MMP-9-Matrix metalloproteinase; MPO-Myeloperoxidase; NF-κB-Nuclear factor-kappa B; NO–nitric oxide; Nrf2-Nuclear factor related to erythroid 2; NSAIDs-Non-steroidal anti-inflammatory; PGE₂-Prostaglandin E₂, SHs-Sulfhydryl compounds; SOD-Superoxide dismutase; TNF-α-Tumor necroses factor-α; VacA-Vacuolating cytotoxin; VEGF-Vascular endothelial growth fator.