Curcuma longa extract protects against gastric ulcers by blocking H2 histamine receptors.
Curcuma longa has been commonly used as a traditional remedy for a variety of symptoms such as inflammation, gastritis and gastric ulcer. When C. longa extract was administered per os to pylori-ligated rat stomachs, it reduced gastric acid secretion and protected against the formation of gastric mucosal lesions. We therefore tested whether C. longa extract inhibits gastric ulcers by blocking the H(2) histamine receptor. Dimaprit, a H(2) histamine receptor agonist, induced intracellular cAMP production in U937 and HL-60 promyelocytes. Pretreatment with C. longa extract significantly blocked dimaprit-induced cAMP production in a concentration dependent manner, but had no effect on the elevation of cAMP levels triggered by isoproterenol-induced beta(2)-adrenoceptor activation in U937 cells. To identify the active component(s) of C. longa extract, we sequentially fractionated it by extraction with ethyl acetate, n-butanol and water. We found that the ethyl acetate extract showed the most potent H(2)R antagonistic effect against dimaprit-induced cAMP production. However, curcumin, a major component of C. longa extract, showed no H(2)R blocking effect. C. longa ethanol extract and ethylacetate extract also blocked the binding of [(3)H]-tiotidine to membrane receptors on HL-60 cells. These findings suggest that the extract from C. longa specifically inhibits gastric acid secretion by blocking H(2) histamine receptors in a competitive manner.
Kim
Dong-Chan
DC
Division of Molecular and Life Science, SBD-NCRC, Pohang University of Science and Technology, South Korea.
Kim
Sun-Hee
SH
Choi
Bo-Hwa
BH
Baek
Nam-In
NI
Kim
Daeho
D
Kim
Mahn-Joo
MJ
Kim
Kyong-Tai
KT
D000085:Acetates / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D030024:Curcuma; D000242:Cyclic AMP / Q000037:antagonists & inhibitors / Q000378:metabolism; D017259:Dimaprit / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000293:injuries / Q000378:metabolism; D042381:Granulocyte Precursor Cells / Q000187:drug effects / Q000473:pathology; D018922:HL-60 Cells; D006635:Histamine H2 Antagonists / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008297:Male; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011899:Ranitidine / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011970:Receptors, Histamine H2 / Q000187:drug effects*; D013276:Stomach Ulcer / Q000188:drug therapy / Q000517:prevention & control*; D020298:U937 Cells
D000085:Acetates; D000897:Anti-Ulcer Agents; D006635:Histamine H2 Antagonists; D010936:Plant Extracts; D011970:Receptors, Histamine H2; C007650:ethyl acetate; D011899:Ranitidine; D000242:Cyclic AMP; D017259:Dimaprit