A new hasubanan alkaloid, hernsubanine E (1), as well as two known compounds p-hydroxybenzaldehyde (2) and (-)-syringaresinol (3) have been isolated from the whole plants of Stephania hernandifolia by various column chromatographic methods. Their structures were identified by physicochemical properties and spectral analyses. Compounds 2 and 3 were isolated from the genus of Stephania for the first time.
Alkaloids ; chemistry ; Heterocyclic Compounds, 4 or More Rings ; chemistry ; isolation & purification ; Stephania ; chemistry

This study of the clinical use of nalbuphine as a component of a balanced anesthesia technique was undertaken with the purpose of exploring the feasibility and safety of this drug as well as to establish possible guidelines for its use.
Human ; Child ; ANESTHESIA ; ANESTHESIA AND ANALGESIA ; NALBUPHINE ; HETEROCYCLIC COMPOUNDS ; ALKALOIDS ; OPIATE ALKALOIDS ; MORPHINANS ; HETEROCYCLIC COMPOUNDS WITH 4 OR MORE RINGS ; MORPHINANS ; HETEROCYCLIC COMPOUNDS, BRIDGED-RING ; MORPHINANS ; POLYCYCLIC COMPOUNDS ; POLYCYCLIC HYDROCARBONS, AROMATIC ; PHENANTHRENES

OBJECTIVETo develop a Quantitative Assay of Multi-components by Single - marker (QAMS) for simultaneous determination of three components in Fructus Evodiae, and examine the feasibility of using the relative correction factors between the different types of compounds.

METHODRutaecarpine was selected as the internal reference substance; the relative correction factors of evodin and evodiamine were calculated. The contents of three components in 11 batches of samples were determined by both external standard method and QAMS. The validity of the QAMS method was evaluated by comparison of their quantitative results.

RESULTNo obvious differences (RSD < 5%) were found in the quantitative results of evodin and evodiamine in 11 batches of Fructus Evodiae determined by the two methods.

CONCLUSIONIt is feasible and suitable to determine evodin and evodiamine in Fructus Evodiae by QAMS, and this method can be used for a certain different types of compounds.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Evodia ; chemistry ; Furans ; analysis ; Heterocyclic Compounds, 4 or More Rings ; analysis ; Indole Alkaloids ; analysis ; Plant Extracts ; analysis ; Quinazolines ; analysis

OBJECTIVETo study the chemical constituents of Pholidota cantonensis.

METHODThe compounds were isolated and purified on silica gel, Sephadex LH-20, Chromatorex ODS column chromatography and the structures were determined based on the spectral and chemical evidences.

RESULTFour compounds were obtained and characterized as pholidonone (1), ephemeranthoquinone (2), orchinol (3), batatasin III (4).

CONCLUSIONThey have been isolated from this plant for the first time and pholidonone (1) was a new compound.

Benzoquinones ; chemistry ; Chromatography ; Drugs, Chinese Herbal ; chemistry ; Heterocyclic Compounds, 4 or More Rings ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Orchidaceae ; chemistry ; Resorcinols ; chemistry ; Stilbenes ; chemistry

AIMTo search for more bioactive compounds from the roots of Aconitum coreanum (Lèvl.) Rapaics.

METHODSHigh speed countercurrent chromatography was successfully applied to the separation of alkaloids from Aconitum coreanum. The structures were elucidated by their physicochemical properties and spectroscopic analysis.

RESULTSTwo-phase solvent system composed of CHCl3-CH3OH-0.2 mol x L(-1) HCl (10:3:3, volume ratio) was used in this experiment, eight alkaloids were obtained from the roots of Aconitum coreanum, which were identified as: 2alpha-propionyl-11alpha,13beta-diacetyl-14-hydroxyhetisine (I), Guanfu base P (II), Guanfu base G (III), Guanfu base F (IV), Guanfu base Z (V), Guanfu base O (VI), Guanfu base A (VII), Guanfu base B (VIII).

CONCLUSIONCompound I is a new alkaloid, named Guanfu base R.

Aconitum ; chemistry ; Countercurrent Distribution ; Heterocyclic Compounds, 4 or More Rings ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry

The membrane proximal α helix of integrin β subunit cytoplasmic tails plays an important functional role by interacting with various intracellular proteins, namely talin, α-actinin or skelemin. This study was designed to investigate the functional role of 5 highly conserved charged amino acids (R(724), K(725), E(726), E(731), E(733)) within this α helix by site-directed mutagenesis. The result showed that CHO cells expressing the αIIbβ3E726Q mutant had the most prominent phenotype and characterized by defective cell spreading on immobilized fibrinogen. In addition, this E726Q mutation induced membrane blebbing in cells adherent on fibrinogen, and this blebbing could be inhibited by the myosin light chain ATPase inhibitor blebbistatin. It is concluded that the membrane proximal α-helix of integrin β3 subunit is important in linking the phospholipid membrane to the submembraneous actin cortex.
Animals ; CHO Cells ; Cell Surface Extensions ; Cricetinae ; Cricetulus ; Heterocyclic Compounds, 4 or More Rings ; chemistry ; Integrin beta3 ; genetics ; Mutagenesis, Site-Directed ; Mutation ; Protein Structure, Tertiary

OBJECTIVETo study the chemical constituents in the heartwood of Taxus cuspidata.

METHODSilica gel column chromatography, preparative HPLC and preparative TLC were used to isolate and purify the chemical constituents; 1H- and 13C-NMR spectroscopic methods were used for structural identification.

RESULTTen compounds, taxinine (1), taxusin (2), beta-sitosterol (3), 1 beta-hydroxybaccatin I (4), 2alpha, 5alpha, 10beta-triacetoxy-14beta-(2'-methyl) butanoyloxy-4 (20), 11-taxadiene (5), 2alpha, 5alpha, 10beta-triacetoxy-14beta-(2'-methyl-3'-hydroxy-butanoyloxyl-4 (20), 11-taxadiene (yunnanxane) (6), 9alpha, 10beta, 13alpha-triacetoxy-5alpha-cinnamoyltaxa-4 (20), 11-diene (7), 2-deacetoxytaxinine J (8), taxezopidine G (9), 2alpha, 7beta, 9alpha, 10beta, 13alpha-pentaacetoxyl-taxa-4 (20), 11-dien-5-ol (5-decinnamoyltaxinine J) (10), were isolated and identified from the heartwood of T. cuspidata.

CONCLUSIONThree taxanes, 1 beta-hydroxybaccatin I (4), 2alpha, 5alpha, 10beta-triacetoxy-14beta-(2'-methyl-3'-hydroxy-butanoyloxy)-4 (20), 11-taxadiene (yunnanxane) (6), and 2alpha, 7beta, 9alpha, 10beta, 13alpha-pentaacetoxyltaxa-4 (20) , 11-dien-5-ol (10), were obtained from this plant for the first time.

Diterpenes ; chemistry ; isolation & purification ; Heterocyclic Compounds, 4 or More Rings ; Plant Stems ; chemistry ; Plants, Medicinal ; chemistry ; Taxoids ; chemistry ; isolation & purification ; Taxus ; chemistry

AIMTo investigate the chemical composition of the root of Salvia przewalskii Maxim.

METHODSCompounds were isolated by silica gel column chromatography. Structures of these compounds were elucidated by spectral analysis (EI-MS, FAB-MS, 1HNMR, 13CNMR, 1H-1H COSY, 1H-13C COSY, HMBC, NOESY) and phytochemical properties.

RESULTSEight compounds were isolated and identified as: tanshinone II-A (I), crypotanshinone (II), przewaquinone A (III), sugiol (IV), ursolic acid (V), 2 alpha, 3 alpha-dihydroxy urs-12-ene-28-acid (VI), oleanolic acid (VII), and neo-przewaquinone A (VIII).

CONCLUSIONCompound VIII is a new compound, and compound II, IV, V, VI and VII are isolated from this plant for the first time.

Heterocyclic Compounds, 4 or More Rings ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Oleanolic Acid ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Quinones ; chemistry ; isolation & purification ; Salvia ; chemistry ; Triterpenes ; chemistry ; isolation & purification

AIMTo establish an analytical method for determination of guanfu base A (GFA) concentration in plasma and to study its pharmacokinetic profile in dogs.

METHODSSix dogs were given a 7.56 mg.kg-1 dose intravenously. Blood samples were collected at various time-points after drug administration. Analytical method based on liquid chromatography-mass spectrometry (LC-MS) was established to determine the plasma concentration of GFA. Pharmacokinetic evaluation was carried out using the 3P87 program.

RESULTSThe calibration curves were linear over the concentration range from 0.42 microgram.mL-1 to 21.2 micrograms.mL-1 (gamma = 0.9994). The intra-day and inter-day precisions were generally good (< 15%) at low, medium and high concentrations. The overall recovery of the analytes was more than 80%. Six dogs were given an i.v. dose of 7.56 mg.kg-1 of GFA hydrochloride, an open three compartment model best described the concentration-time profiles for GFA. The half-lives for the rapid and slow distribution phase and terminal elimination phase (T1/2 pi, T1/2 alpha and T1/2 beta) were 0.07 h, 1.5 h, and 13.5 h, respectively. The total area under the plasma concentration-time curve (AUC), the volume of the central compartment (Vc), and plasma clearance (CLs) were 61.43 micrograms.h.mL-1, 0.37 L.kg-1 and 0.14 L.kg-1.h-1, respectively.

CONCLUSIONThe analytical method was shown to be sensitive, specific, rapid and reproducible, and was suitable for pharmacokinetic studies of GFA.

Aconitum ; chemistry ; Alkaloids ; blood ; isolation & purification ; pharmacokinetics ; Animals ; Area Under Curve ; Chromatography, Liquid ; methods ; Dogs ; Female ; Gas Chromatography-Mass Spectrometry ; methods ; Heterocyclic Compounds, 4 or More Rings ; Male ; Metabolic Clearance Rate ; Plants, Medicinal ; chemistry

OBJECTIVETo investigate the effect and safety of intravenous Guanfu Base A hydrochloride (GFA) in the treatment of ventricular arrhythmias.

METHODSPatients without severe structural heart disease presenting with equal or more than 150 premature ventricular contractions per hour and/or non sustained ventricular tachycardia in drug-free holter monitoring were recruited in this double blind randomized active-controlled study. Eligible patients were randomly assigned to receive GFA or propafenone intravenously by a proportion of 1:1 in a double-blind manner. Intravenous bolus of the study medicine was given, followed by maintenance infusion for 6 hours. 24 hours continuous electrocardiographic recordings were performed to evaluate the efficacy. Vital signs, electrocardiograms and adverse events were documented before, during and after drug administration.

RESULTSA total of 201 patients came from eight centres were randomized to GFA or propafenone group. The demographic characteristics, the extent of ventricular arrhythmias and baseline clinical findings were comparable between the two groups. There were no significant differences in the percentage of reducing premature ventricular contractions and the accumulated efficacy between two groups. GFA had tendency to be more effective than propafenone in reducing the number of ventricular ectopy (P = 0.0609). There were no significant differences in the onset of action after drug administration between two drugs. The tolerance of GFA was better than propafenone. The adverse events in GFA group were less severe than those in propafenone group.

CONCLUSIONSIntravenous GFA in controlling the premature ventricular contraction has comparable effect to IV propafenone. Tolerance of GFA was better than propafenone.

Adolescent ; Adult ; Anti-Arrhythmia Agents ; therapeutic use ; Double-Blind Method ; Female ; Heterocyclic Compounds, 4 or More Rings ; therapeutic use ; Humans ; Male ; Middle Aged ; Phytotherapy ; Tachycardia, Ventricular ; drug therapy ; Ventricular Premature Complexes ; drug therapy ; Young Adult