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The study investigated the difference of intestinal absorption characteristics of root tuber of Cynanchum auriculatum extract between normal and functional dyspepsia(FD) model rats with everted intestine sac model.The content of syringic acid, scopoletin, caudatin, baishouwu benzophenone, qingyangshengenin and deacyhmetaplexigenin in the C.auriculatum extract in different intestinal segments was detected by UPLC-MS/MS.The cumulative absorption amount(Q) and absorption rate constant(K_a) of the six chemical constituents were calculated.The results showed that the six components could be absorbed into the intestinal sac and were unsaturated, which indicated that the absorption mechanism of scopoletin was active transport in the intestine, while that of the other five components were passive diffusion.For normal group, the syringic acid and baishouwu benzophenone in ileum, qingyangshengenin and deacyhmetaplexigenin in ileum and duodenum, and caudatin in colon were well absorbed and scopoletin at low, medium and high concentrations was found excellent absorption in jejunum, ileum, and colon, respectively.Whereas the best absorption site of each component was ileum in model group.The absorption characteristics of each component between normal group and model group were complex at different concentrations, showing inconsistent tendency of absorption, which suggested that the components of root tuber of C.auriculatum extract were selectively absorbed in small intestine, and the absorption characteristics of the six components could be changed under FD status.This study provided theoretical basis for the clinical drug application and development of root tuber of C.auriculatum.

The study aimed to investigate the mechanism of hepatoprotective effect of C-21 steroidal glucosides from Cynanchum auriculatum( Baishouwu) on oxidative stress in mice with liver injury. Mice were randomly divided into normal group,model group,positive control group,Baishouwu high group and Baishouwu low group. The liver injury model was induced by intraperitoneal injection of CCl4 peanut oil solution. All mice were sacrificed to collect blood and liver specimens. The activities of serum levels of ALT and AST were detected. The content of MDA and the activity of SOD in liver homogenate were examined by colorimetry method. Tissues were stained with hematoxylin-eosin for histological examination. The hepatic protein expressions of NF-κB p65,p-IκBα,i NOS and COX-2 were detected by Western blot. The mRNA expressions of TNF-α and IL-6 were determined by RT-PCR. It was found that treatment with C-21 steroidal glucosides from Baishouwu successfully attenuated liver injury induced by CCl4,as shown by decreased levels of serum biochemical indicators( AST,ALT)( P<0. 01). Administration of total C-21 steroidal glucosides enhanced the activity of SOD( P<0. 01) and decreased the content of MDA( P<0. 01) in liver homogenate. Microscopic features suggested that treatment with C-21 steroidal glucosides from Baishouwu was effective in inhibiting CCl4-induced hepatocyte edema and degeneration. Further studies showed that NF-κB p65 overexpression induced by CCl4 was decreased by C-21 steroidal glucosides,leading to the markedly down-regulated protein expression levels of p-IκBα,i NOS and COX-2,as well as the depression of TNF-α and IL-6 mRNA expressions. In conclusion,total C-21 steroidal glucosides from Baishouwu exhibited potent effect on oxidative stress pathway in mice with liver injury induced by CCl4,with enhanced activity of SOD,decreased content of MDA,and down-regulated levels of NF-κB p65,p-IκBα,i NOS and COX-2.

This study is aimed to provide the source for clinical medication by clarifing the common base of Mongolia medicinal materials "Du Ge Mo Nong". In this paper literature research and plant taxonomy method were adopted combined with investigation of the markets and clinical use status to clarify the origin of common traditional Mongolian medicine "Du Ge Mo Nong". The results showed that the Mongolian medicine "Du Ge Mo Nong" and Tibetan medicine "Du Mu Niu" were the same crude drug and originated from the seeds of Holarrhena antidysenteriaca of family Apocynaceae in earliest time. In Mongolian medicine clinic, the seed of Cynanchum thesioides of family Asclepiadaceae and the fruit of Forsythia suspense of family Oleaceae was used respectively about 18 century and recent time, as the substitutes of H. antidysenteriaca. In present standards on Mongolian material medicine, C. thesioides is including only, and H. antidysenterica is not used almost. In Tibetan medicine clinic, H. antidysenterica is being used so far. But there are various substitutes including the seeds, fruits or grass of many species classified to family Apocynaceae, Asclepiadaceae and Onagraceae from ancient time to the present, and C. forrestii and C. komarovii may be used at present. It's necessary to strengthen the arrangement on Mongolian medicine's varieties by the multidisciplinary methods including literature research, investigation of resources and the use state, and comparison of active substances and biological activities between the different substitutes,and so on., Competing Interests: The authors of this article and the planning committee members and staff have no relevant financial relationships with commercial interests to disclose., (Copyright© by the Chinese Pharmaceutical Association.)

In order to isolate and purify the reference compounds and improve the quality standard of ethnic medicine of Radix of Cynanchum otophyllum, the ethanol extracts were isolated by column chromatography onsilica gel, C₁₈ reverse-phase silica gel, and semi-preparative HPLC. Twelve compounds were isolated and their structures were elucidated as 2,4-dihydroxy-6-methoxyphenylethanone(1), 4,6-dihydroxy-2-methoxyphenylethanone(2), p-hydroxyacetophenone(3), baishouwubenzophenone(4), 2,4-dihydroxyacetophenone(5), 2,5-dihydroxyacetophenone(6), otophylloside A(7),otophylloside B(8), caudatin-3-O-β-D-cymaropyranosyl-(1→4)-β-D-digitoxopyranoside(9),caudatin-3-O-β-D-glucopyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-digitoxopyranoside(10),qingyangshengenin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranoside(11),caudatin-3-O-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside(12) on the basis of spectral analysis. Compounds 1 and 2 were isolated from the genus Cynanchum for the first time, and compounds 3-4, 9-12 were obtained from this plant for the first time.These compounds are main active components of Radix of C.otophyllum and can be used as reference substances for the quality control of this ethnic medicine., Competing Interests: The authors of this article and the planning committee members and staff have no relevant financial relationships with commercial interests to disclose., (Copyright© by the Chinese Pharmaceutical Association.)

Eleven C21 steroids were isolated from chloroform extract of roots of Cynanchum otophyllumby silica gel, MCI, ODS columns, and semi-preparative HPLC. Their structures were determined by spectroscopic data analysis as otophylloside B(1), caudatin-3-O-beta-D-cymaropyranosyl-(1-->4)-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (2), caudatin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (3), caudatin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-digitoxopyranosyl-(1-->4)-beta-D-cymaropyranoside (4), otophylloside O (5), gagamine-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (6), sinomarinoside B (7), mucronatosides C (8), wallicoside J (9), stephanoside H (10), and qinyangshengenin-3-O-beta-D-oleandropyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-digitoxopyranoside (11). Among them, compounds 2-3, and 6-11 were separated from the roots of this plant for the first time.

Objective: To study anti-HIV activity and mechanism of Cynanchum otophyllum glucan sulfate in vitro., Method: Anti-HIV-1 activity was detected with syncytial formation assay and quantitative P24 enzyme-linked immunosorbent assay (ELISA); cytotoxicity was tested with MTT colorimetric assay. Antiviral mechanism was investigated by fusion inhibition, time of addition and pre-treatment experiments., Result: The 50% inhibition concentrations (IC50) of PS20 for HIV-1(IIIB), HIV-1(Ada-M), and HIV-1(Bal), were 0.26, 0.46, 0.90 micromol x L(-1), respectively. Studies on antiviral mechanism of PS20 showed that target molecule may be viral envelope protein., Conclusion: The results suggested that PS20 had high anti-HIV activity and was worth to be studied further.

Objective: To study the optimizal hydrolysis process for C21 steroidal glycoside of Bai Shou Wu by acetic acid., Method: The effects of acetic acid concentration, reaction temperature and reaction time had been investigated using orthogonal design and the contents of kidjoranin 3-O-beta-digitoxopyranoside, caudatin, kidjoranin 3-O-alpha-L-diginopyranosyl-(1 --> 4)-beta-cymaropyranoside and caudatin 3-O-beta-cymaropyranoside as response indexs were determined by the high performance liquid chromatography., Result: The factors influencing acetic extraction efficiency were as follows: A > B > C (A. reaction temperature; B. reaction time; C. acetic acid concentration). The optimal hydrolysis condition obtained was: refluxing for 6 hours with 5.0% dilute CH3COOH solution at 100 degrees C., Conclusion: The content of antitumor active ingredients under the optimum hydrolysis condition is raised obviously and has a great part in studying this antitumor drug.

Objective: To investigate the effect of general glycosides from Cynanchun auriculatum of Jiangsu on liver fibrosis of rats., Method: Seventy-two Wistar rats were randomly divided into normal group, model group, BSW three doses treated group and hydrocortisone treated group. CCl4 (50%, 2 mL x kg(-1)) was orally administraeated twice a week for 8 weeks. The liver and spleen indices were observed. The level of serum GPT, GOT, and HA, PCIII and the level of SOD, HyP, MDA in liver homogenates was also measured. The histopathologic change in hepatic of rats was examined., Result: The elevation of serum GPT, GOT, HA, PCIll, MDA and HyP and the content of liver homogenates were attanuated remarkably by BSW treatment. BSW groups also increased the level of SOD of liver homogenates, and make the fibrotic liver better., Conclusion: The general glycosides in C. auriculatum of jiangsu province have an anti-hepatic fibrosis ettect on CCl4-induced fibrosis rats, the mechanisms might be associated with its anti-oxidative action.

Objective: To investigate the inhibition of three C2 steroidal saponins from Cynanchum auriculatum on the cell growth and cell cycle of human lung cancer A549 cells., Method: A549 cells were exposed to three C21 steroidal saponins of different concentrations (5, 10, 20, 40, 60, 80, 100 micromol L(-1)) for 48 hours. After 48 h, MTT assay was used to evaluate the inhibiting effects of three C21 steroidal saponins on the proliferation of the A549 cells. Exponential growth phase A549 cells were treated with 47, 34, 60 micromol x L(-1) of three C21 steroidal saponins respectively for 12, 24, 48 h, then the changes of cell cycle were analyzed by flow cytometry., Result: The three C21 steroidal saponins could inhibit the growth of A549 cells in dose-dependent manner and IC50 is 46. 07 mol x L(-1), 33.02 mol x L(-1), 59.92 mol x L(-1) respectively. The cell cycle analysis showed that wilfoside C1N and wilfoside C3N increased the percentage of G0/G1 phase cells and decreased G2/M and S-phase cells while the proportion of cells in S-phase was lower and in G2/M phase the proportion was higher than control when the cells were cultivated with wilfoside K1N (P < 0.05, P < 0.01)., Conclusion: Three C21 steroidal saponins could inhibit the proliferation of A549 cells in dose-dependent manner and the mechanism may be related to its arresting the cell cycle.

High performance liquid chromatography coupled with on-line electrospray tandem mass spectrometry (HPLC/ESI-MS/MS) was used to identify C21 steroidal glycosides in the roots of Cynanchum atratum. The structures of C21 steroidal glycosides were deduced from mass fragments features in positive and negative mode. The constituents of C. atratum were separated and detected. 7 compounds were identified by comparing their ESI-MS/MS data with the reference compounds and 2 compounds were inferred solely by the ESI-MS/MS data. The method is sensitive, and provides good separation and rapid qualitative characterization of C21 steroidal glycosides in the roots of C. atratum.

Objective: To develop an approach to the determination of saponins in Radix Cynanchi Atrati, and to optimize the parameters for purified the preparation of total saponins by macroporous resin column chromatography., Method: Using cynanversicoside A as a reference, the determination of saponins was performed; according to the elution rate and the purity of the products, the preparation performance of total saponins by macroporous resin was investigated, and its parameters were optimized., Result: The saponins in Radix Cynanchi Atrati were successfully determined at 518 nm by vanillin-perchloric acid as spray reagent. The macroporous resin HP-20 showed static absorption ratio of 59. 3 mg x g(-1); the 70% ethanol extraction of Radix Cynanchi Atrati was eluted from column of macroporous resin HP-20 by water and 30% ethanol, and the saponins were concentrated in 90% ethanol solution. The content of saponin part eluted from HP-20 column was 77.62%., Conclusion: The proposed approach allows convenient and efficient preparation and purification of saponin in Radix Cynanchi Atrati.

Objective: To study the effect of C21 steroidal glycoside (CSG) from the root of Cynanchum auriculatum from Jiangsu on D-galactose (D-gal) induced aging model mice., Method: D-gal aging mouse model was established by cervicodorsal region subcutaneous injection with D-gal once a day for eight successive weeks. The mice in the normal control group (NCG, non-modeled) and the model control group (MCG, modeled but untreated) were treated with 1% CMC-Na. The model mice in the low, middle and high-dose CSG and Vitamin E treated groups were treated with a dose of (10, 20, 40, 100 mg x kg(-1) per day, respectively. The SOD activity, MDA content and telomerase activity in serum, heart, liver and brain tissues of mice were measured., Result: CSG could obviously increase the SOD activity and decrease the MDA level in serum, heart, liver and brain tissues in D-gal aging mice (P < 0.01). There was no significant difference between three CSG treated groups and Vitamin E treated groups. In comparison of telomerase activity between MCG and the treated groups, it was shown that there was a significant increase in serum in middle and high dose group, and in heart tissues in CSG and Vit E treated groups, but was not in liver and brain tissue., Conclusion: This study demonstrates that CSG can antagonize free radical injury, increase the SOD activity and decrease the MDA content of serum, heart, liver and brain in D-gal aging mice, and increase the telomerase activity in serum and heart tissues but not in liver and brain tissue.

Objective: To study the chemical constituents from the roots and rhizome of Cynanchum atratum., Method: The chemical constituents were isolated and repeatedly purified by silica gel chromatography and the structures were elucidated by the NMR spectra and physicochemical properties., Result: Twelve compounds were obtained and nine of them were identified as 2, 4-dihyroxyacetophe none (1), 2, 6-dihyroxyacetophenone (2), 4-hydroxybenzenemethanol (3), benzoic acid (4), beta-amyrin acetate (5), palmitic acid (6), beta-sitosterol (7), beta-daucosterol (8), glaucogenin C-3-O-alpha-D-oleandropyranosyl-(1 --> 4)-beta-D-digitoxopyranosyl-(1 -->4)-alpha-D-oleandropyranoside (9)., Conclusion: Seven compounds were obtained from C. atratum for the first time.

Objective: To study the central pharmacological effect of the water and chloroform-extract compounds from C. chinese in mice., Method: The independent activity test and the hypnotic synergism test by sub-threshold hypnotic dosage of pentobarbital were employed to evaluate the central pharmacological effect of the extract-compounds, and the minimal neurotoxicity was evaluated by the rotorod test., Result: the extract-compounds exhibited significant dose-related inhibition effect of the spontaneous motor activity in mice after intraperitoneal administration. And the two extract-compounds promoted the hypnotic effect by sub-threshold hypnotic dosage administration of pentobarbital, and produced ED50 value of 2.36 g kg (-1) and 0.75 g kg(-1), respectively. Also, both extract-compounds showed no neurotoxicity in the experiment., Conclusion: The extract compounds from C. chinese showed inhibitional effect on CNS.

Objective: To study the chemical constituents of Cynanchum forrestii., Method: Chromatographic techniques were applied to isolated chemical constituents. The structures were identified on the basis of physico-chemical constants and spectroscopic data., Result: Eight compounds were isolated from the 95% ethanol extract of the roots of C. forrestii and elucidated as ( + ) -5'-methoxyisolariciresinol 3a-O-beta-D-glucopyranoside (1), hexahydroxycholest-7-en-6-one (2), tylophorinidine (3), sucrose (4), palmitic acid (5), beta-sitosterol (6), daucosterol (7), nonanedioic acid (8)., Conclusion: Compounds 1-3 from this genus, and compounds 4-8 from the plant were obtained for the first time.

Objective: To study chemical constituents from Cynanchum auriculatum., Method: The chemical components were isolated and purified by silca gel, sephedex-LH-20 and ODS column chromatography. The chemical structures were elucidated on the basis of physicochemical properties and spectral data., Result: Thirteen compounds were isolated and identified as: caudatin (1), metaplexigenin (2), cynauricuoside A (3), succinic acid (4), azelaic acid (5), wilforibiose (6), sucrose (7), 1-O-hexadecanolenin (8), beta-amyrin acetate (9), cynanchone A (10), acetylquinol (11), beta-sitosterol (12), daucosterol (13)., Conclusion: Compounds 4-9 were obtained from this plant for the first time.

Objective: To study the effects of PRCB1a (one component of polysaccharides from Radix Cynanchi Bungei) on transformation of T lymphocytes of rabbit in vitro and immune function in mice., Method: Three doses of PRCB1a (2,4,6 g x L(-1)) were respectively put in bottle with PHA and blood of rabbit. The effect of PRCB1a on immunity in vitro was studied by observing transformation of T lymphocytes; The dosage of PRCB1a (50,100,150 mg x kg(-1) x d(-1)) was given orally for seven days. The effects on immune function were investigated in mice., Result: Three doses of PRCB1a could significantly promote (P < 0.01) the ability of T lymphocytes proliferation; PRCB1a could improve the mouse thymus and spleen index, the celiac macrophage ability of engulfing CRBC, the delayed type hypersensitivity ability and the macrophage engulfing carbon granula ability., Conclusion: The results indicate PRCB1a can enhance nonspectific and specific cellular immune function.

Objective: To study the chemical features of CPB-4, a heteropolysaccharide obtained from Cynanchum paniculatum., Method: Sugar composition analysis, methylation analysis, partial hydrolysis and carbon-13 nuclear magnetic resonance were used to determine the sugar composition, linkages, main chain, branch chains and branching points., Result: CPB-4 is composed of L-arabinose, L-xylose, L-rhamnose and D-galactose in closely molar ratios of 0.8:0.2:0.2:1.0. Its main chain is comprised of 1, 5 linked galactose and side chains are comprised of terminal xylose, terminal arabinose, oligosaccharide of arabinose and oligosaccharide of arabinose, rhamnose and galactose. The branching points are located at C-6 and C-2 of galactose., Conclusion: CPB-4 is a new heteropolysaccharide from C. paniculatum.

Objective: To investigate the chemical constituents in the aerial part of Cynanchum chinense., Method: The chemical constituents were extracted with solvent and separated by column chromatography. The structures were identified by spectral methods:, Result: The structures were identified as 7-O-alpha-L-rhamnopy-ranosyl-kaempferol-3-O-alpha-L-rhamnopyranoside, 7-O-alpha-L-rhamnopy-ranosyl-kaempferol-3-O-beta-D-glucopyranoside and 7-O-alpha-L-rhamnopyr-anosylkaempferol-3-O-beta-D-glucopyranosyl(1-->2)- beta-D-glucopyranoside., Conclusion: All the three compounds were separated from C. chinense for the first time.