Antianoxic action and active constituents of evodiae fructus

In order to develop new drugs from natural products, constituents of natural medicines were examined for their effectiveness in the KCN-induced anoxia model in mice. Methanol extract from a Chinese medicine, evodia (fruits of Evodia rutaecarpa Benth. or E. officinalis Dode), had a significant effect in the KCN-induced anoxia model in mice and therefore the active constituents were further examined. The results indicated that the antianoxic action of evodia was found in the fraction containing evodiamine. Further analysis of the active constituent indicated that evodiamine and rutaecarpine, indole-alkaloids found in large amounts in the Chinese medicine evodia, were mainly responsible for the antianoxic action.     

The sennoside constituents of rhei rhizoma and sennae folium as inhibitors of serum monoamine oxidase

Four (in total) compounds with inhibitory effects on the activity of bovine serum monoamine oxidase were isolated from the methanol-water extracts of Rhei Rhizoma (Daiou) and Sennae Folium (Senna), and identified as sennosides A, B, E and F. Among them, sennosides A and B were obtained from both Rhei Rhizoma and Sennae Folium, while sennosides E and F were detected only in the former. The 50% inhibitory concentrations of the four sennosides were 17, 9, 24 and 13 microM, respectively, and the type of inhibition by seenosides A and B with respect to allylamine as the substrate was non-competitive.     

Biologically active constituents of Aglaia erythrosperma

From the fruits and leaves of Aglaia erythrosperma (Meliaceae), 10 chemical constituents were isolated and identified, i.e. the dammarane triterpenoids cabraleadiol (1), cabraleahydroxylactone (2), ethyl eichlerianoate (3), eichlerialactone (4), aglinin A (5), cabralealactone (6), the aglaialactone 5,6-desmethylenedioxy-5-methoxy-aglalactone (7), the flavagline 4'-demethoxy-3',4'-methylenedioxy-methyl rocaglate (8) and two coumarins: scoparone and scopoletin. Flavagline 8 exhibited antimalarial activity with an IC(50) value of 7.30 μg mL(-1) and was strongly cytotoxic against small cell lung cancer (NCI-H187), epidermoid carcinoma (KB) and breast cancer (BC) cell lines, with IC(50) values of 2.17, 2.10 and 0.11 μg mL(-1), respectively. Aglinin A (5) displayed moderate cytotoxicity against all the three cancer cell lines, whereas ethyl eichlerianoate (3), cabralealactone (6) and the aglaialactone 7 were exclusively cytotoxic to NCI-H187 cell line. Cabraleahydroxylactone (2) showed antiviral activity against herpes simplex virus type-1 with an IC(50) value of 3.20 μg mL(-1), in comparison with the standard acyclovir (IC(50)?= 1.90 μg mL(-1)). When tested for antimycobacterial activity against Mycobacterium tuberculosis H(37)Ra, compounds 1-4 and 6-8 displayed minimum inhibitory concentration in the range of 25-50 μg mL(-1).     

野生与栽培羌活药材挥发油含量及组分的比较分析

分析野生和栽培羌活药材挥发油含量及其组分的变化,为羌活药材的引种栽培及进一步的开发利用提供了依据。采用水蒸气蒸馏法提取羌活药材中的挥发油,通过GC-MS对挥发油成分进行分析鉴定;利用聚类分析对测定结果进行分类;通过相关分析研究海拔对羌活药材挥发油含量的影响。6份药材样品挥发油含量范围为1.60～7.98 mL/100g,6份羌活药材挥发油成分经GC-MS分析,共鉴定出57个化合物,共有成分12个;基于挥发油成分种类及相对含量的聚类分析显示了羌活药材挥发性成分种类及含量的种间差异;相关分析结果表明,海拔高度与挥发油含量存在显著正相关。野生和栽培羌活药材挥发油含量存在差异,总体上野生羌活药材的挥发油含量高于栽培种;羌活药材挥发油含量随海拔升高而增加。     

Exploratory analysis of chromatographic fingerprints to distinguish rhizoma Chuanxiong and rhizoma Ligustici

Identification and quality control of products of natural origin, used for preventive and therapeutical goals, is required by regulating authorities, as the World Health Organization. This study focuses on the identification and distinction of the rhizomes from two Chinese herbs, rhizoma Chuanxiong (from Ligusticum chuanxiong Hort.) and rhizoma Ligustici (from Ligusticum jeholense Nakai et Kitag), by chromatographic fingerprints. A second goal is using the fingerprints to assay ferulic acid, as its concentration provides an additional differentiation feature. Several extraction methods were tested, to obtain the highest number of peaks in the fingerprints. The best results were found using 76:19:5 (v/v/v) methanol/water/formic acid as solvent and extracting the pulverized material on a shaking bath for 15 min. Then fingerprint optimization was done. Most information about the herbs, i.e. the highest number of peaks, was observed on a Hypersil ODS column (250 mm × 4.6 mm ID, 5 μm), 1.0% acetic acid in the mobile phase and employing within 50 min linear gradient elution from 5:95 (v/v) to 95:5 (v/v) acetonitrile/water. The final fingerprints were able to distinguish rhizoma Chuanxiong and Ligustici, based on correlation coefficients combined with exploratory data analysis. The distinction was visualized using Principal Component Analysis, Projection Pursuit and Hierarchical Clustering Analysis techniques. Quantification of ferulic acid was possible in the fingerprints of both rhizomes. The time-different intermediate precisions of the fingerprints and of the ferulic acid quantification were shown to be acceptable.     

Determination of the active ingredients in Gastrodia rhizoma by capillary electrophoresis with electrochemical detection

A simple, reliable and reproducible method, based on capillary electrophoresis (CE) with electrochemical detection (ED), for the determination of five active ingredients and three carbohydrates in extracts of Gastrodia rhizoma is described in this work. The main active ingredients are gastrodin, 4-hydroxybenzyl alcohol, vanillyl alcohol, 4-hydroxybenzylaldehyde and vanillin. Operated in a wall-jet configuration, a 300 microm diameter carbon disc electrode was used as a working electrode, with a good response at +1000 mV (vs. SCE) for 4-hydroxybenzyl alcohol, vanillyl alcohol, 4-hydroxybenzylaldehyde and vanillin; a 300 microm diameter copper disc electrode exhibits a good response at +650 mV (vs. SCE) for gastrodin, sucrose, glucose and fructose. Under optimum conditions, 4-hydroxybenzyl alcohol, vanillyl alcohol, 4-hydroxybenzylaldehyde and vanillin in 100 mmol l(-1) borate buffer (pH 9.2) and gastrodin, sucrose, glucose and fructose in 50 mmol l(-1) sodium hydroxide buffer were baseline separated within 18 min. The response was linear over two orders of magnitude with a detection limit (S/N = 3) in the range 3 x 10(-7)-1.8 x 10(-6) mol l(-1) for all eight analytes. This method was successfully used in the analysis of traditional Chinese medicine, and the assay results were satisfactory.     

Gastrointestinal motility enhancing effect of ginger and its active constituents

The effect of ginger root (Zingiberis Rhizoma) on gastrointestinal motility was examined based on its ability to enhance charcoal meal transport in mice. Oral administrations of the acetone extract of ginger (which contains volatile oils and bitter substances) at 75 mg/kg, [6]-shogaol at 2.5 mg/kg, or a [6]-, [8]- or [10]-gingerol at 5 mg/kg enhanced the transport of a charcoal meal. The effects of these substances were similar to or slightly weaker than those of metoclopramide and donperidone.     

Isolation of biologically active plant constituents by liquid chromatography

Strategies are outlined for the separation of biologically active products of plant origin. The techniques involved include low-pressure liquid chromatography, semi-preparative high-performance liquid chromatography, flash chromatography and droplet counter-current chromatography. Their application to the isolation of compounds from Sesamum angolense (Pedaliaceae), Psorospermum febrifugum (Guttiferae) and Cordia goetzei (Boraginaceae) is described.     

Sampling of gaseous trace constituents from air on active carbon

Next to the collection of particulate matter from air by micropore filtration, gaseous trace constituents may be sampled by an additional or separate active carbon cartridge. Either reversible or irreversible adsorption results. Important respective applications are the assay ²²²Rn (emanation) and the collection of mercury vapor. Formulation of both cases and their consequences for routine application are given here. This revised version was published online in August 2006 with corrections to the Cover Date.     

A new butenolide cinnamate and other biological active chemical constituents from Polygonum glabrum

Phytochemical investigation of the methanol extract of the aerial parts of Polygonum glabrum afforded one new natural product ( ? )-2-methoxy-2-butenolide-3-cinnamate (1) along with six known compounds, β-hydroxyfriedalanol (2), 3-hydroxy-5-methoxystilbene (3), ( ? ) pinocembrin (4), sitosterol-(6′-O-palmitoyl)-3-O-β-d-glucopyranoside (5), ( ? ) pinocembrin-5-methyl ether (6) and sitosterol-3-O-β-d-glucopyranoside (7). Compound 1 showed promising in vitro anti-HIV-1 activity against primary isolates HIV-1_UG070 (X4, subtype D) and HIV-1_VB59 (R5, subtype C) assayed using TZM-bl cell line with IC₅₀ in the range of 15.68–22.43 μg/mL. The extract showed TI in the range of 19.19–27.37 with IC₅₀ in the range of 10.90–15.55 μg/mL. Compounds 1, 3 and 4 exhibited in vitro anti-mycobacterium activity against Mycobacterium tuberculosis H37Ra with IC₅₀ values of 1.43, 3.33 and 1.11 μg/mL in dormant phase and 2.27, 3.33 and 1.21 μg/mL in active phase, respectively. Compound 4 was found to be the most active antiproliferative with IC₅₀ values of 1.88–11.00 μg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines.     

Neurite outgrowth-promoting active constituents of the Japanese cypress (Chamaecyparis obtusa)

In the screening of biologically active constituents from woody plants, the methanol extract of leaves of Chamaecyparis obtusa showed potent neurite outgrowth-promoting activity in neuronal PC12 cells. The ethyl acetate-soluble fraction of the methanol extract showed potent activity and was separated by means of various chromatographic methods to give the two new compounds 1 and 2, as well as 11 known lignan and sesquiterpene derivatives. The structures of the new compounds were determined to be 9-O-acetyldihydrosesamin (1) and 9-O-(11-hydroxyeudesman-4-yl)dihydrosesamin (2), respectively, in NMR studies including 2D-NMR experiments. Of the 13 compounds, the known compound hinokinin (5) and the new compound 2 showed potent neurite outgrowth-promoting activity in PC 12 cells.     

知母药材高效液相指纹图谱研究

用高效液相色谱法建立了知母药材的指纹图谱分析方法。采用ZorbaxEclipseXDB C18色谱柱(5μm,4.6×250mm,Agilent),流动相为乙腈和25mmol/LKH2PO4缓冲液,梯度洗脱;流速:1.0mL/min;柱温为25℃;检测波长257nm。确定了8批不同产地知母药材甲醇提取部分6个共有峰,各产地药材指纹图谱与对照指纹图谱相似度良好(>0.9),可以用来作定性研究。方法准确可靠,为提高知母药材质量控制标准提供参考。     

Biologically active constituents of Centipeda minima: sesquiterpenes of potential anti-allergy activity.

Ether, methanol and aqueous extracts of Centipeda minima (Compositae) herbs were found to have significant anti-allergy activities in passive cutaneous anaphylaxis (PCA) test. Three flavonoids, two sesquiterpene lactones and an amide were isolated from this plant material as inhibitors to induced histamine release from mast cells. The sesquiterpenes were identified as isobutyroylplenolin and senecioylplenolin by spectral investigations. The flavonoids and sesquiterpenes exhibited significant anti-allergy activity in PCA test with p.o. administration.     

Enzyme active sites: bioinformatics,architecture, and mechanisms of action

A comparative analysis of the amino acid sequences of some enzymes which comprise superfamilies of enzymes belonging to different classes was carried out. Based on the amino acid sequence alignment for enzymes belonging to different classes with the use of the information entropy as a criterion, the amino acid residues involved in the catalytic portion of the active site are demonstrated to be most conservative. The rating scale for conservativeness of amino acids in enzymes is created. Glycine and aspartic acid are the most commonly occurring conservative amino acids essential for the catalysis. The role of aspartic acid and histidine in the mechanism of molecule activation in the catalytic site is considered using hydrolases as examples. The role of glycine, proline, and cysteine in the structural organization of the active sites is discussed.     

The antiulcer action of sophora and the active constituent in Sophora. II. The antiulcer action of vexibinol

The inhibitory effect of vexibinol, one of the flavanols found in Sophora, on gastric ulcers induced by HCl-ethanol has been reported previously. In the present study, the effect of vexibinol was examined in various experimental ulcer models in order to determine the mechanism of its antiulcer action. The results indicated that the oral administration of vexibinol at 25-50 mg/kg significantly inhibited the development of ulcers induced by HCl-ethanol, 0.6 N HCl 0.2 N NaOH, absolute ethanol and 1% NH3. In addition, an intraduodenal administration of vexibinol at 300 mg/kg significantly inhibited Shay's ulcer. Further, intraduodenal administration at 300 mg/kg significantly inhibited acid secretion caused by 2-deoxy-D-glucose. These results suggest that vexibinol has not only gastric mucosal protective action but also an inhibitory effect on the secretion of gastric acids.     

Biologically active constituents of Arnebia euchroma: structures of new monoterpenylbenzoquinones: arnebinone and arnebifuranone.

Two quinonic compounds, arnebinone and arnebifuranone, were isolated from the roots of Arnebia euchroma and their structures were elucidated on the basis of spectral evidence. Arnebionone is a monoterpenyl-benzoquinone in which the monoterpene moiety forms a fused ring to the benzoquinone. Arnebifuranone is another monoterpenylbenzoquinone with a furan ring containing side chain which is bonded to the benzoquinone at the head carbon of C10 moiety originating from the geranyl moiety of geranylhydroquinone.     

Simultaneous determination of four active constituents in the roots of Scrophularia buergeriana by HPLC-DAD and LC-ESI-MS

The chemical profile of four main bioactive constituents including harpagoside (HS), 8-O-(E-p-methoxycinnamoyl)harpagide (HG), E-cinnamic acid (CA), and E-p-methoxycinnamic acid (MCA), in the extract of Scrophularia buergeriana was studied using HPLC-diode array detector-electrospray-MS (HPLC-DAD-ESI-MS). The HPLC-DAD conditions were optimized for the simultaneous analysis of these four compounds. This method was validated in terms of specificity, linearity (r(2) >0.9998), precision (< 2.0% RSD), and recoveries (94.4-115.1%). The LOD of these compounds were ranged from 5.9 to 37.8 ng. In addition, the main compounds in S. buergeriana and S. ningpoensis were quantified using this validated method, which resulted in significant difference in the contents of these compounds between the species.     

HPLC法同时测定忍冬叶中9种活性成分的研究

为了有效利用忍冬植株,建立了同时检测忍冬叶中新绿原酸、绿原酸、咖啡酸、芦丁、木犀草苷、金丝桃苷、异绿原酸C、木犀草素和槲皮素9种活性成分含量的HPLC分析方法,并用于忍冬叶中活性成分的定量测定,为忍冬叶多指标质量评价标准提供理论依据和方法参考.