Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor
<i>Cistanche</i> species, the ginseng of the desert, has been recorded to possess many biological activities in traditional Chinese pharmacopoeia and has been used as an anti-aging medicine. Three phenylethanoid glycosides—echinacoside, tubuloside A, and acteoside—wer...
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MDPI AG
2019-02-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/24/4/720 |
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| author | Chieh-Ju Wu Mei-Yin Chien Nan-Hei Lin Yi-Chiao Lin Wen-Ying Chen Chao-Hsiang Chen Jason T. C. Tzen |
| author_facet | Chieh-Ju Wu Mei-Yin Chien Nan-Hei Lin Yi-Chiao Lin Wen-Ying Chen Chao-Hsiang Chen Jason T. C. Tzen |
| author_sort | Chieh-Ju Wu |
| collection | DOAJ |
| description | <i>Cistanche</i> species, the ginseng of the desert, has been recorded to possess many biological activities in traditional Chinese pharmacopoeia and has been used as an anti-aging medicine. Three phenylethanoid glycosides—echinacoside, tubuloside A, and acteoside—were detected in the water extract of <i>Cistanche tubulosa</i> (Schenk) R. Wight and the major constituent, echinacoside, was further purified. Echinacoside of a concentration higher than 10<sup>−6</sup> M displayed significant activity to stimulate growth hormone secretion of rat pituitary cells. Similar to growth hormone-releasing hormone-6, a synthetic analog of ghrelin, the stimulation of growth hormone secretion by echinacoside was inhibited by [D-Arg<sup>1</sup>, D-Phe<sup>5</sup>, D-Trp<sup>7,9</sup>, Leu<sup>11</sup>]-substance P, an inverse agonist of the ghrelin receptor. Molecular modeling showed that all the three phenylethanoid glycosides adequately interacted with the binding pocket of the ghrelin receptor, and echinacoside displayed a slightly better interaction with the receptor than tubuloside A and acteoside. The results suggest that phenylethanoid glycosides, particularly echinacoside, are active constituents putatively responsible for the anti-aging effects of <i>C. tubulosa</i> and may be considered to develop as non-peptidyl analogues of ghrelin. |
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| last_indexed | 2024-12-24T05:08:37Z |
| publishDate | 2019-02-01 |
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| spelling | doaj.art-62fd990d4e004204ba017a883f5a7f082022-12-21T17:13:45ZengMDPI AGMolecules1420-30492019-02-0124472010.3390/molecules24040720molecules24040720Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin ReceptorChieh-Ju Wu0Mei-Yin Chien1Nan-Hei Lin2Yi-Chiao Lin3Wen-Ying Chen4Chao-Hsiang Chen5Jason T. C. Tzen6Graduate Institute of Biotechnology, National Chung-Hsing University, Taichung 402, TaiwanKo Da Pharmaceutical Co. Ltd., Taoyuan 324, TaiwanGraduate Institute of Biotechnology, National Chung-Hsing University, Taichung 402, TaiwanGraduate Institute of Biotechnology, National Chung-Hsing University, Taichung 402, TaiwanDepartment of Veterinary Medicine, National Chung-Hsing University, Taichung 402, TaiwanKo Da Pharmaceutical Co. Ltd., Taoyuan 324, TaiwanGraduate Institute of Biotechnology, National Chung-Hsing University, Taichung 402, Taiwan<i>Cistanche</i> species, the ginseng of the desert, has been recorded to possess many biological activities in traditional Chinese pharmacopoeia and has been used as an anti-aging medicine. Three phenylethanoid glycosides—echinacoside, tubuloside A, and acteoside—were detected in the water extract of <i>Cistanche tubulosa</i> (Schenk) R. Wight and the major constituent, echinacoside, was further purified. Echinacoside of a concentration higher than 10<sup>−6</sup> M displayed significant activity to stimulate growth hormone secretion of rat pituitary cells. Similar to growth hormone-releasing hormone-6, a synthetic analog of ghrelin, the stimulation of growth hormone secretion by echinacoside was inhibited by [D-Arg<sup>1</sup>, D-Phe<sup>5</sup>, D-Trp<sup>7,9</sup>, Leu<sup>11</sup>]-substance P, an inverse agonist of the ghrelin receptor. Molecular modeling showed that all the three phenylethanoid glycosides adequately interacted with the binding pocket of the ghrelin receptor, and echinacoside displayed a slightly better interaction with the receptor than tubuloside A and acteoside. The results suggest that phenylethanoid glycosides, particularly echinacoside, are active constituents putatively responsible for the anti-aging effects of <i>C. tubulosa</i> and may be considered to develop as non-peptidyl analogues of ghrelin.https://www.mdpi.com/1420-3049/24/4/720cistanche tubulosaechinacosideghrelingrowth hormone secretionphenylethanoid glycosides |
| spellingShingle | Chieh-Ju Wu Mei-Yin Chien Nan-Hei Lin Yi-Chiao Lin Wen-Ying Chen Chao-Hsiang Chen Jason T. C. Tzen Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor Molecules cistanche tubulosa echinacoside ghrelin growth hormone secretion phenylethanoid glycosides |
| title | Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor |
| title_full | Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor |
| title_fullStr | Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor |
| title_full_unstemmed | Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor |
| title_short | Echinacoside Isolated from <i>Cistanche tubulosa</i> Putatively Stimulates Growth Hormone Secretion via Activation of the Ghrelin Receptor |
| title_sort | echinacoside isolated from i cistanche tubulosa i putatively stimulates growth hormone secretion via activation of the ghrelin receptor |
| topic | cistanche tubulosa echinacoside ghrelin growth hormone secretion phenylethanoid glycosides |
| url | https://www.mdpi.com/1420-3049/24/4/720 |
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