Pomegranate (Punica granatum) seed linolenic acid isomers: concentration-dependent modulation of estrogen receptor activity.
Pomegranate (Punica granatum) seed linolenic acid isomers were evaluated as selective estrogen receptor modulators (SERMs) in vitro. Punicic acid (PA) inhibited (IC(50)) estrogen receptor (ER) alpha at 7.2 microM, ERbeta at 8.8 microM; alpha-eleostearic acid (AEA) inhibited ERalpha/ERbeta at 6.5/7.8 microM. PA (not AEA) agonized ERalpha/ERbeta (EC(50)) at 1.8/2 microM, antagonizing at 101/80 microM. AEA antagonized ERalpha/ERbeta at 150/140 microM. PA and AEA induced ERalpha and ERbeta mRNA expression in MCF-7, but not in MDA-MB-231. Overall, the results show PA and AEA are SERMs.
Department of Experimental Therapeutics, Kyungpook National University, Taegu, Republic of Korea.
Hoang Ngoc Ai
HN
Tran
Soo-Young
SY
Bae
Bang-Ho
BH
Song
Bang-Hyo
BH
Lee
Young-Seok
YS
Bae
Young-Ho
YH
Kim
Ephraim Philip
EP
Lansky
Robert A
RA
Newman
D001943:Breast Neoplasms; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D047628:Estrogen Receptor alpha / Q000235:genetics / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000235:genetics / Q000378:metabolism; D005227:Fatty Acids / Q000032:analysis; D006801:Humans; D007536:Isomerism; D008041:Linoleic Acids / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D044243:Linoleic Acids, Conjugated / Q000378:metabolism; D008042:Linolenic Acids / Q000378:metabolism; D029561:Lythraceae / Q000737:chemistry*; D048789:Phytoestrogens / Q000378:metabolism / Q000494:pharmacology*; D010938:Plant Oils / Q000737:chemistry; D012333:RNA, Messenger / Q000032:analysis; D011960:Receptors, Estrogen / Q000187:drug effects* / Q000502:physiology*; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012639:Seeds / Q000737:chemistry*; D020845:Selective Estrogen Receptor Modulators / Q000378:metabolism / Q000494:pharmacology
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005227:Fatty Acids; D008041:Linoleic Acids; D044243:Linoleic Acids, Conjugated; D008042:Linolenic Acids; D048789:Phytoestrogens; D010938:Plant Oils; D012333:RNA, Messenger; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators