Abstract
Cistanche 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 Cistanche tubulosa (Schenk) R. Wight and the major constituent, echinacoside, was further purified. Echinacoside of a concentration higher than 10−6 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-Arg1, D-Phe5, D-Trp7,9, Leu11]-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 C. tubulosa and may be considered to develop as non-peptidyl analogues of ghrelin.
Highlights
Cistanche species (Orobanchaceae), the so-called ginseng of the desert, is a holoparasitic plant found in the desert region of northwestern China
Ghrelin and echinacoside found as a major phenylethanoid glycoside in Cistanche species were documented to possess several equivalent physiological activities, including anti-aging effects presumably through hypothalamuspituitary-gonadal axis
We showed that echinacoside isolated from C. tubulosa might stimulate growth hormone secretion from rat primary anterior pituitary cells putatively via growth hormone secretagogue receptor (GHSR) activation in a manner similar to ghrelin
Summary
Cistanche species (Orobanchaceae), the so-called ginseng of the desert, is a holoparasitic plant found in the desert region of northwestern China. This herbal medicine has been recorded to possess several biological activities such as constipation relief, longevity, and aphrodisiac properties in traditional Chinese pharmacopoeia [1]. Different species of Cistanche are commonly named according to their hosts and growing environments, such as Cistanche deserticola Y.C. Ma and Cistanche tubulosa (Schenk) R. C. deserticola, hosted by Haloxylon ammodendron mainly found in Inner Mongolia, was originally regarded as the standard Cistanche source in Chinese Pharmacopoeia, but has been listed as an endangered plant species in China since 1984. C. tubulosa, hosted by Tamarix ramosissima grown in Xinjiang Hetian, tends to possess a fast growth rate, and agricultural cultivation of this
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