A new suberin from roots of Ephedra sinica Stapf / 药学学报

Six compounds were isolated from the roots of Ephedra sinica Stapf using various chromatographic techniques such as silica gel column chromatography, thin layer chromatography and semi-preparative HPLC. Their chemical structures were identified by analysis of physicochemical properties and spectral data, and determined as (Z)-docosanylferulate (1), (E)-docosanylferulate (2), bis (2-ethylheptyl) phythalate (3), 2,2′-oxybis (1,4-di-tert-butylbenzene) (4), diisobutyl phthalate (5), bis (2-ethylhexyl) phthalate (6). Among them, compound 1 is a new compound, compounds 2-4 were first isolated from Ephedra. A corticosterone-induced PC-12 cell injury model was used for compound activity screening. The results showed that compounds 1 and 5 significantly improved corticosterone-induced PC-12 cell injury and significantly increased 5-HT7 receptor protein expression in the cells, indicating potential antidepressant activity.

Pharmacokinetic study of the complication of Ephedra sinica and Prunus armeniaca in bronchial asthma model rats / 中国药房

OBJECTIVE To study the pharmacokinetic changes in the plasma and cerebrospinal fluid of bronchial asthma model rats after the complication of Ephedra sinica and Prunus armeniaca. METHODS SD male rats were randomly divided into blank group， model group， E. sinica group （12 g/kg， calculated by raw drug， similarly hereinafter）， P. armeniaca group （6 g/kg） and E. sinica-P. armeniaca drug-pair group （12 g/kg of E. sinica+6 g/kg of P. armeniaca）， with 6 rats in each group. Except for the blank group， the bronchial asthma model was induced by spraying rats in each group with an equal volume mixture of 2% acetylcholine chloride and 0.4% histamine phosphate， once a day， for 7 d. One hour before modeling every time， rats in each group were gavaged with the corresponding drug/normal saline， once a day， for 7 d. After the final administration and provocation of asthma， blood and cerebrospinal fluid collection were performed at different time points. The plasma and cerebrospinal fluid samples were pre-treated （with geranylgeranyl as the internal standard）， and the mass concentrations of ephedrine/pseudoephedrine， methyl ephedrine and amygdalin in both samples were determined by liquid chromatography-tandem mass spectrometry. DAS 2.0 pharmacokinetic software was used to determine the main pharmacokinetic parameters through the non-atrial chamber model and to compare the changes of the pharmacokinetic parameters before and after the combination of the two drugs. RESULTS Compared with E. sinica group， cmax and AUC0-21.33 h （or AUC0-10.67 h） of ephedrine/pseudoephedrine and methyl ephedrine in the plasma and cerebrospinal fluid of rats were significantly reduced in E. sinica-P. armeniaca drug-pair group， while CLZ/F and VZ/F were significantly increased （P＜0.05 or P＜0.01）； tmax of methyl ephedrine in the cerebrospinal fluid was significantly shortened （P＜ 0.05）.Compared with P. armeniaca group， the t1/2 of amygdalin in the plasma of rats in E. sinica-P. armeniaca drug-pair group was significantly shortened， and CLZ/F was significantly increased （P＜0.01）； the tmax of bitter amygdalin in the cerebrospinal fluid was significantly shortened， and the AUC0-10.67 h， CLZ/F， and VZ/F were significantly increased （P＜0.01）. CONCLUSIONS The combination of E. sinica and P. armeniaca accelerates the absorption and elimination of ephedra alkaloids， thus reducing the accumulation of ephedra alkaloids in the bronchial asthma model rats.

Effect of ephedra water extract on liver injury induced by cisplatin / 国际中医中药杂志

Objective To study the effect of water extract of ephedra on hepatic injury induced by cisplatin in rats. Methods Forty rats were randomly divided into the blank group, model group, and ephedra water extract was divided into the low dose group, medium and high dose group. Ephedra water extract in the low, medium dose group, high dose group were 100, 200, 400 mg/kg. The normal saline of equal volume was used in the blank group and model group, once a day for 10 days. In addition to the blank group, the other groups were given cisplatin (8 mg/kg) on the 6th day to establish the model of liver injury in rats. The changes of body weight, serum ALT, AST and liver MDA, NO, SOD, GSH were detected by biochemical method. The pathological changes of liver tissue were observed by the staining. Results On the 3rd day and 5th day after administration of cisplatin, the body weight of the rats in the low, medium and high dose group were significantly higher than that in the model group (P<0.05 or P<0.01). Compared with the model group, the serum AST (328.00 ± 168.00 U/L, 297.00 ± 139.00 U/L vs. 409.00 ± 364.00 U/L), ALT (122.00 ± 76.00 U/L, 97.00 ± 64.00 U/L vs. 198.00 ± 156.00 U/L) in the medium-, high- dose group significantly decreased (P<0.05 or P<0.01). The content of SOD (34.98 ± 7.40 U/mg, 41.80 ± 8.10 U/mg vs. 12.70 ± 3.10 U/mg), GSH (16.90 ± 1.70 mg/g, 22.70 ± 3.70 mg/g vs. 9.90 ± 1.30 mg/g) in the medium-, high- dose group significantly increased,while the content of MDA (3.20 ± 0.60 nmol/ml, 2.20 ± 0.30 nmol/ml vs. 4.30 ± 0.70 nmol/ml), NO (0.90 ± 0.10 μmol/L, 0.80 ± 0.20 μmol/L vs. 1.20 ± 0.30 μmol/L) significantly decreased (P<0.05 or P<0.01). Conclusion The ephedra water extract can protect the liver injury induced by cisplatin in rats.

Study of brain distribution of Ephedra alkaloids based on UHPLC-QTOF-MSE and UHPLC-MS/MS method / 药学学报

Using ultra high performance liquid chromatography (UHPLC) coupled with mass spectrum (MS) technology, a method has been established for separation and analysis of alkaloid isomers. Alkaloids in Ephedra sinica transitionally crossed blood brain barrier (BBB) and the distribution were investigated. The concentrations of Ephedra alkaloids in rat central nervous system (CNS) were determined to acquire the distribution characteristics and differences in cerebral cortex, cerebellum, hippocampus, striatum, medulla oblongata and hypothalamus. It was founded that pseudoephedrine, norephedrine, norpseudoephedrine, methylephedrine (methylpseudoephedrine) were able to cross BBB fast via gastro-intestinal tract after administrated with Ephedra sinica. Cortex and hippocampus was the main distribution region, followed by hypothalamus, striatum and cerebellum, in which medulla oblongata had the least. The distribution of various alkaloids, as AUC0-t, brain/AUC0-t, blood was ephedrine > methylephedrine > demethyl ephedrine. Alkaloids in Ephedra sinica crossed BBB rapidly, showing the regional distribution tendency in central nervous system, and the distribution was diversity. This group of data provides distribution of bioactive constituents of Ephedra in CNS.

Transcriptome characterization of Ephedra sinica with 454 ESTs / 中国中药杂志

Using the latest 454 GS FLX platform and Titanium regent, a substantial expressed sequence tag (ESTs) dataset of Ephedra sinica was produced, and the profile of gene expression and function gene of which were investigated. A total of 48 389 reads with an average length of 373 bp were generated. These 454 reads were assembled into 18 801 unigenes, which were all 454 sequencing identified. A total number of 10 531 unigenes(56.0%) were annotated using BLAST searches (E-value≤1×10⁻⁵) against the Nr, Nt, TAIR, SwissProt and KEGG databases. With respect to genes related to ephedrine biosynthesis, 19 unigenes(encoding 9 enzymes) were found. A total of 97 putative genes encoding cytochrome P450s were also discovered. Data presented in this study will provide an important resource for the scientific community that is interested in the functional genomics and secondary metabolism of E. sinica.

Comparison on celluar anti-inflammatory and immunoregulatory activities of seven derivative combinations of Yaotongning with alkaloid as main part and in vivo pharmacodynamic evaluation on optimized candidate combination / 中草药

Objective: To investigate which kind of Chinese medicinal effective fractions will produce good comprehensive cellular pharmacological activities when they were combined with alkaloids from Strychnos nux-vomica and Ephedra sinica, and to evaluate in vivo pharmacological activities of the effective fraction combination screened by cellular experiments. Methods: The equal proportion mixture of alkaloids from S. nux-vomica and E. sinica was set as a sample (sample 1, A); Two samples (samples 2 and 3) were designed by respectively adding the equal ratio mixture of five flavonoids (F) at 50% into alkaloids from S. nux-vomica or E. sinica; Four samples (samples 4-7) were designed by respectively adding F, equal proportion mixture of four saponins (S), equal ratio mixture of six volatile oils/aqueous (V), and equal proportion mixture of six polysaccharides (P) at 50% into A. Murine macrophage cells and chondrocytes were exposed to the new recipes, and then the half inhibitory concentration (IC50) of recipes for inhibiting (PGE2) in macrophages and the half effective concentration (EC50) for promotion of the secretion of IL-6, IL-1β, and TNF-α in macrophages were detected and compared. The interactions among the active fractions were evaluated by comparing the experimental EC50/IC50 values to their corresponding additive EC50/IC50 values calculated by the least square optimum method. The in vivo pharmacodynamics of the best combination was evaluated by the ear swelling model and delayed type hypersensitivity (DTH) model in mice. Results: Sample 4 has good comprehensive activities of cellular anti-inflammation and immunoregulation. Moreover, strong synergistic effect among the effective fractions in this sample was observed; Cellular anti-inflammatory activities of samples 5, 6, and 7 were equivalent with sample 4; Samples 5 and 7 had good comprehensive cellular immunoregulation activity; But the alkaloids mixture (A) and the combinations of S. nux-vomica or E. sinica alkaloids with F (samples 2 and 3) were significantly weaker than sample 4 in cellular anti-inflammation, immunoregulation, and chondrocyte-proliferation. Sample 4 also exhibits a certain effect on in vivo anti-inflammation and immunity in mice when A was decreased at 25% or 5%. Conclusion: It is not suitable to design a combination just by alkaloids from S. nux-vomica and alkaloids of E. sinica; Alkaloids from S. nux-vomica or alkaloids of E. sinica are also not appropriate to solely combine with the mixture of flavonoids (F). When A is combined with F, S, V, and P, respectively, synergistic or additive effects among the active fractions are usually observed. These active fractions help to strengthen comprehensive cellular pharmacological activities of A. Sample 4 not only has good cellular activities of anti-inflammation and immunoregulation but also has better in vivo effect on anti-inflammation and immunity, suggesting that it is feasible to screen the optimized Chinese medicine formula based on cellular pharmacological experiments.

Comparative analysis of volatile oils in the stems and roots of Ephedra sinica via GC-MS-based plant metabolomics / 中国天然药物

With a great difference in therapeutic effects of Mahuang (MH, the stems of Ephedra sinica) and Mahuanggen (MHG, the roots of Ephedra sinica), chemical differences between MH and MHG should be investigated. In the present study, gas chromatography-mass spectrometry (GC-MS)-based plant metabolomics was employed to compare volatile oil profiles of MH and MHG. The antioxidant activities of volatile oils from MH and MHG were also compared. 32 differential chemical markers were identified according to the variable importance in the projection (VIP) value of orthogonal partial least squares discriminant analysis (OPLS-DA) and P value of Mann-Whitney test. Among them, chemical markers of tetramethylpyrazine (TMP) and α-terpineol were quantified. Their contents were much higher in most MH samples compared with MHG. The antioxidant assay demonstrated that MH had significantly higher free radical-scavenging activity than MHG. Although MH and MHG derived from the same medicinal plant, there was much difference in their volatile oil profiles. MH samples had significantly higher content of two reported pharmacologically important chemical markers of TMP and α-terpineol, which may account for their different antioxidant activities.

The influence of the aqueous extract of ephedra sinica treating in brain damage after subarachnoid hemorrhage in rats / 重庆医学

Objective To observe the therapeutic effect and mechanism of the aqueous extract of ephedra sinica on brain damage after subarachnoid hemorrhage(SAH)in rats.Methods Totally 50 rats of Sprague-Dawley were randomly divided into control group,model group and three groups treated with different concentrations(4,12,36 mg/kg).The changes of the cerebral water content,malondialdehyde(MDA),glutathione peroxidase(GSH-Px)and hydroxy radical of brain tissue were recorded,and he-matoxylin-eosin(HE)staining was used to test the subarachnoid haemorrhagia and oedema,and immunohistochemistry and western blot were carried out to assay the expression of complement C3 in brains of different animal in different group 3d after operation. Results On the postoperative 3 days,compared with the model group,the content of MDA、GSH-Px activity and hydroxyl radical of 12、36 mg/kg treatment groups significantly reduced(P 0.05),but GSH-Px activity and inhibition of hydroxyl radical significantly reduced(P <0.01),and the cerebral water content of 12,36 mg/kg groups were obviously lower compared with model group.The expression of complement C3 was significantly lower on 36 mg/kg treatment group and edema reduced.Conclusion The aqueous extract of ephedra could significantly inhibit the activity of complement C3,prevent the production of MDA、GSH-Px and hydroxyl radical,reduce the severity of cerebral edema and the in-flammatory response,which has a better therapeutic effect SAH animals.

Flavonoids from roots of Ephedra sinica / 中草药

Objective: To study the flavonoids from the roots of Ephedra sinica in Ephedra Tourn. ex L. Methods: The roots of E. sinica were extracted with 90% ethanol, and isolated and purified by silica gel, Sephadex LH-20, and RP-18 gel column chromatography. All the compounds were identified based on spectral analyses (including MS, 1H-NMR, and 13C-NMR). Results: Thirteen flavonoids were isolated from the roots of E. sinica and were characterized as ephedrannin A (1), mahuannin A (2), mahuannin B (3), mahuannin D (4), apigenin (5), kaempferol (6), quercetin (7), dihydroquercetin (8), 3′, 4′, 5, 7-tetrahydroxy flavanone (9), (+)-catechin (10), (-)-epi-catechin (11), afzelechin (12), and (-)-epi-afzelechin (13), respectively. Conclusion: Compounds 7-13 are obtained from this plant for the first time.

A Case of Ischemic Colitis Associated with the Herbal Food Supplement Ma Huang

Ischemic colitis is a condition that usually occurs in the elderly, as a form of vascular disease. However, ischemic colitis also occurs, though rarely, in healthy young adults. Moreover, food supplements containing Ephedra sinica or ma huang have been linked to adverse central nervous and cardiovascular events. A 40-year-old man was admitted to our emergency department after 2 episodes of abdominal pain and bloody diarrhea that lasted 24 hours. His medical history was unremarkable for risk factors of bowel ischemia, except for well-controlled hypertension. However, a weight-loss supplement, Ephedra sinica, had been prescribed for daily use during the previous month. Both abdominal/pelvic computed tomography and colonoscopy revealed findings compatible with ischemic colitis. His conditions spontaneously improved without any serious complications, and he was advised to discontinue the use of herbal medications containing ephedrine. In this paper, we describe a case of ischemic colitis that was potentially linked to the use of ma huang with a review of the relevant literature.

A Clinical Study on the Efficacy of Cosmetics Containing the Root of Ephedra sinica and the Bark of Betula platyphylla var. japonica Related to Skin Furrows / 대한피부과학회지

BACKGROUND: Skin smoothness in aging skin, in combination of intrinsic aging and photoaging, is of ever-increasing interest which leads to the development of various wrinkle diminuation products including those containing herbal medicines. OBJECTIVES: The purpose of this study was to assess the efficacy of cosmetics containing roots of Ephedra sinica and Betula platyphylla var. japonica on reducing skin furrows. METHOD: Creams containing Ephedra sinica's root and Betula platyphylla var. japonica were applied to forearms of 30 healthy subjects in 2 age groups for 8 weeks and 4 weeks, respectively while silicone skin replicas were taken from medial and lateral sides of the forearm every 4 weeks of the study starting from the week 0. Then the changes of the skin furrows were analyzed with skin visiometer. RESULTS: 1. At week 8, a significant reduction of average roughness and maximum roughness were observed in volunteers younger than age 50 on their Ephedra sinica's root-treated side compared with the placebo-treated side (p<0.05). 2. No statistically significant changes were observed with both Ephedra sinica's root and Betula platyphylla var. japonica in the group of age over 50. 3. Comparison of the changes between treatment groups of both Ephedra sinica's root and Betula platyphylla var. japonica at any assessment time did not show statistically significant differences between the medial and lateral side of forearm, while the treatment group of Ephedra sinica's root showed statistically significant differences between the young and old at week 8 (p<0.05). CONCLUSIONS: The treatment of Ephedra sinica's root seems to be partially effective in improving skin furrows in youth. To our knowledge, this study is the first trial to evaluate the efficacy of both Ephedra sinica's root and Betula platyphylla var. japonica on decreasing wrinkle in the world.

Ephedra sinica in preventing hyperacute rejection in guinea pig-to-rat cardiac xenotransplantation / 第三军医大学学报

Objective To study Ephedra sinica in preventing hyperacute rejection in guinea pig-to-rat cardiac xenotransplantation. Methods The recipient rats were divided into two groups: control group and experiment group, according to whether administrated complement inhibiting component (CIC) from Ephedra sinica. In 15 min after operation, 4 rats from control group and 4 from experiment group were sacrificed to detect the pathologic changes in cardiac tissues. The complement parameters including CH_(50), APH_(50), and C_(3) were determined during the period of 0, 10, 15, 30, 45 min in serial serum. Results The survival time was significantly prolonged and pathological changes were less in experiment group than that in control group. Conclusion The study reveals that both classical pathway and alternative pathway of complement activation can be induced by xenotransplantation and Ephedra sinica can prolong the xenograft time by inhibiting complement activities and postposing hyperacute rejection.

Comparison on constituents from different parts between wild growing and cultivated planting of Ephedra sinica / 中草药

Objective To compare the difference in constituents from different parts of wild and cultivated Ephedra sinica. Methods Using the solvent of 50% methyl alcohol to extract from the stems and roots of wild and cultivated E. sinica under heating reflux, respectively and then determine the content of ephedrine in each extractions by HPLC. The volatile oil was extracted by stream-distillation and analyzed by GC-MS method. Results The content of the ephedrine in extraction of stems and roots of wild E. sinica was 0.55% and 0.000 57% while the content of the cultivated was 0.26% and 0.001 7%. Forty-five compounds in the volatile oil were identified by GC-MS method, among them 13 compounds existed in both wild and cultivated E. sinica. Conclusion The content of the ephedrine is about two times of the cultivated in wild E. sinica′s stems, while it is very low in the roots of two kinds of herbs. And ephedrine is not found in the volatile oil.

Determination of ephedrine alkaloids in Ephedra sinica by nonaqueous capillary electrophoresis / 中草药

Object To develop a rapid method for the determination of ephedrine alkaloids in Ephedra sinica Stapf by nonaqueous capillary electrophoresis (NACE) and evaluate the extracting method by determining the amount of alkaloids Methods The buffer contained 50 mmol/L ammonium acetate in methanol without any additives was used And the detection wavelength was 210 nm Results The best separation result was achieved within 8 min Linearity was obtained in range of 9 8-147 0 ?g/mL pseudoephedrine, 6 8-102 0 ?g/mL for norephedrin, 9 4-141 0 ?g/mL for ephedrine, 4 8-72 0 ?g/mL for norpseudoephdrine, 6 8-102 0 ?g/mL for methylephedrine respectively The recovery range of these five alkaloids was 95 0%-100 4% Conclusion This method is rapid and accurate for the quantitative analysis of ephedrin alkaloids in E sinica

Analysis of essential oil in cultivated Ephedra Sinica Stapf in Gansu Province / 中成药

AIM: To analyze the chemical constituents of essential oil in Ephedra Sinica Stapf from Gansu Province. METHODS: The essential oil in Ephedra Sinica Stapf was extracted by steam distillation and analyzed by gas chromatography-mass spectrometry(GC-MS). RESULTS: 71 Compounds were identified from Ephedra Sinica Stapf of 3 different sources(Minqin,Zhenyuan and Gulang County),and contained 28 same components such as tetramethylpyrazine、linalool、?-terpineol、4-terpineol、d-?-terpineol、hexadecanoic acid and so on.The contents of d-?terpineol and hexadecanoic acid in Ephedra Sinica Stapf were the highest. CONCLUSION: Essential oils in Ephedra Sinica Stapf from Gansu Province do not contain 1-?-terpineol.