As a famous health food in China, Cistanche deserticola (C. deserticola) suggested an estrogenic activity according to our previous study. However, no one clarifies its active material basis to date. To find more potentially active constituents and elucidate metabolic pathways of metabolites, a method to simultaneously analyze multiple absorbed constituents and metabolites from C. deserticola in rat serum and urine was established using high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (HPLC/Q-TOF-MS). Based on HPLC/Q-TOF-MS method, a total of 24 components, involving 9 prototype constituents and 15 metabolites in rat serum and urine samples, were tentatively identified based on retention time, ultraviolet spectrum, MS data, compound fragmentation laws, published literatures, and reference substances. Most of the compounds existed in the form of metabolites. The proposed metabolic pathways of main metabolites were discussed, including methylation, demethylation, hydrolysis, hydroxylation, acetoxylation, glucuronidation, dehydrogenation, sulfation, esterification, and so on. Phenylethanoid glycosides were extensively metabolized and mutually transformed in vivo. This investigation provided valuable information for further study of the active ingredients and action mechanism of C. deserticola.

High-performance liquid chromatography (HPLC) is an efficient method that is widely used to assess the quality of traditional Chinese medicine (TCM). It is well known that the quality of TCM has a direct effect on its efficacy; therefore, in order to thoroughly explain how TCM exerts its efficacy, it is necessary to characterize its active ingredients and assess their quality. The application of the spectrum-effect method is crucial for determining the pharmacological basis of materials. The aim of the present study was to examine the correlation between chemical spectra and estrogenic activity of Cuscuta chinensis Lam., in order to reveal active compounds with potential therapeutic effects. The spectra of Cuscuta chinensis Lam. were recorded using HPLC, and estrogenic activity was determined using a uterus growth test and MTT assay. Combination of the results of bivariate analysis, principal component analysis and Gray relational analysis identified 19 active compounds, as follows: Querceglucopyranoside, kaempferol-7-rhamnosy, kaempferol-3-β-D-glucuronide, apigenin, 4-caffeoyl-5-coumaroylquinic acid, kaempferol-3-arabofuranoside, quercetin-3-O -β-D-apiofuranosyl-(1→2)-β-D-galactoside, dicaffeoylquinic acid, hyperin, quercitin, isorhamnetin, chlorogenic acid, quercetin, quercltrin-2''-gallate, quercetin-3, 7-α-L-dirhamnoside and stigmasterol, as well as one unknown compound. The present study laid a foundation for in vivo metabolic studies regarding Cuscuta chinensis Lam. and for the development of its clinical application.

LC technology is a recognized method used worldwide to evaluate the quality of traditional Chinese medicines (TCM). The quality of TCM has a direct impact on its efficacy. Therefore, in order to thoroughly reveal how TCM exerts its efficacy, first of all, it is necessary to understand the material basis for its efficacy, and then to control the quality of active compounds. The application of the spectrum-effect relationship method is crucial for determining the pharmacological material basis. The goal of this paper was to investigate the underlying correlations between the chemical profiles and oestrogenic activity of Cistanche, to reveal the active compounds. The chemical profiles of Cistanche were recorded using HPLC/Q-TOF-MS/MS, and oestrogenic activity was determined by the Uterus growth test and the MTT assay. Then combining the results of bivariate analysis, principal component analysis and gray correlation analysis method, fifteen active compounds were identified. They are 8-epiloganic acid, salidroside, syringalide A 3’-α-l-rhamnopyranoside, cistanoside A, echinacoside, cistanoside F, cistanoside B, cistanoside C, osmanthuside B, acteoside, isoacteoside, tubuloside B, 2’-acetylacteoside, and two unknown compounds. This study lays a foundation for in vivo studies of Cistanche and for the development of its clinical application.

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