Estrogenic and antiestrogenic activities of phloridzin.
Phloridzin, a phloretin 2'-beta-D-glucoside, belongs to dihydrochalcones and mainly exists in the fruits of Malus pumila Mill., Lithocarpus polystachyus REHD and the root skins, stems, tender leaves and fruits of Malus hupehensis. It has many pharmacological activities, such as regulating blood sugar level and blood pressure, protecting heart, scavenging of oxygen free radicals and antioxidant injuries. Thus, market demand of products containing phloridzin is increasing year by year. Our research results demonstrated that phloridzin is provided with a double directional adjusting function of estrogenic and antiestrogenic activities. It showed significant effects on the proliferation of estrogen sensitive estrogen receptor (ER) (+)MCF-7 cells in the absence of estrogen. When added with 17beta-estradiol, phloridzin showed antagonism on estradiol-induced MCF-7 cell proliferation, but it did not significantly affect proliferation of estrogen insensitive ER (-)MDA-MB-231 cells. Phloridzin induced beta-galactosidase activity in a yeast two-hybrid assay. Light increase of the uterine weight and serum estradiol content of mouse was observed when the glucoside was administered orally for 7 d. After oral administration, phloridzin was found mainly in the blood and a small part was metabolized to phloretin. Our investigation proved that phloridzin was distributed at the target organ and played the role of phytoestrogen.
Wang
Junzhi
J
Hubei Key Laboratory of Natural Products Research and Development (China Three Gorges University), College of Chemistry and Life Science, China Three Gorges University, China.
Chung
Mi Hwa
MH
Xue
Bingjie
B
Ma
Hong
H
Ma
Chaomei
C
Hattori
Masao
M
D000230:Adenocarcinoma / Q000188:drug therapy; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004958:Estradiol / Q000378:metabolism; D020847:Estrogen Receptor Modulators / Q000494:pharmacology*; D004967:Estrogens / Q000494:pharmacology / Q000627:therapeutic use; D029962:Fagaceae / Q000737:chemistry; D005260:Female; D005960:Glucosides / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D027845:Malus / Q000737:chemistry*; D051379:Mice; D008815:Mice, Inbred Strains; D009929:Organ Size; D010695:Phlorhizin / Q000493:pharmacokinetics / Q000494:pharmacology*; D048789:Phytoestrogens / Q000494:pharmacology* / Q000627:therapeutic use; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use; D011960:Receptors, Estrogen / Q000378:metabolism*; D014018:Tissue Distribution; D014599:Uterus / Q000378:metabolism; D015003:Yeasts; D001616:beta-Galactosidase / Q000378:metabolism
D000972:Antineoplastic Agents, Phytogenic; D020847:Estrogen Receptor Modulators; D004967:Estrogens; D005960:Glucosides; D048789:Phytoestrogens; D010936:Plant Extracts; D011960:Receptors, Estrogen; D004958:Estradiol; D010695:Phlorhizin; D001616:beta-Galactosidase