[Fingerprint comparison of mountain cultivated ginseng and wild ginseng by HPLC].

OBJECTIVE: To establish the fingerprint of mountain cultivated ginseng by HPLC and compare the fingerprint with that of wild ginseng for the quality control. METHODS: The analysis was carried out on a ZORBAX Eclipse XDB-C18 column (150 mm x 4.6 mm, 5 microm) with a mobile phase consisting of water-acetonitrile with gradient elution, and the flow rate was 1 mL/min. The column temperature was set at (30 +/- 0.15) degrees C and UV detection wavelength was set at 203 nm. RESULTS: There were 15 common peaks in the fingerprint of mountain cultivated ginseng. The similarities of 10 batches ginseng were between 0.90 and 1.00. CONCLUSION: This method has good characteristics and specificity, and could be used for quality control of mountain cultivated ginseng. The type and content of components in wild ginseng were slightly higher than those in mountain cultivation ones.

Identification of the metabolites of baicalein in human plasma.

The metabolites of baicalein in human plasma were investigated after taking baicalein, which is one of the main bioactive flavones in Scutellaria baicalensis Georgi. Five metabolites (M1-M5) together with the parent drug baicalein (P) were detected and identified by the HPLC-diode-array detector (DAD) and LC-MS/MS methods. Among them, 7-methoxybaicalein 6-O-glucuronide (M5) is a new metabolite. Based on the results, the proposed metabolic pathway of baicalein in humans was inferred.

Two acylated flavonoid glycosides from the leaves of Quercus dentata.

Two new acylated flavonoid glycosides have been isolated from the leaves of Quercus dentata Thunb. On the basis of chemical and spectral data, the structures of the compounds have been elucidated as kaempferol 3-O-(2", 4"-diacetyl-3"-cis-p-coumaroyl-6"-trans-p-coumaroyl)-beta-D-glucopyranoside (1), and kaempferol 3-O-(2"-trans-p-coumaroyl-3", 4"-diacetyl-6"-cisp-coumaroyl)-beta-D-glucopyranoside (2).

RGD-based strategies for improving antitumor activity of paclitaxel-loaded liposomes in nude mice xenografted with human ovarian cancer.

Tumor-targeting drug delivery systems are being the ideal carrier for systemic administration of antiproliferative drugs. RGD peptide (arginine-glycine-aspartic acid) modified liposomes containing paclitaxel (RGD-SSL-PTX). The arginine-glycine-aspartic acid tripeptide (RGD) modified sterically stabilized liposomes (SSL) containing paclitaxel (PTX) (RGD-SSL-PTX), which could increase targeting to tumor by binding with the integrin receptors overexpressed on tumor cells. The encapsulation efficiency was more than 90% and the mean particle size was of 120 nm with a narrow size distribution. It was indicated that significant cytotoxicity (3.5 times lower IC(50)) was found in the SKOV-3 human ovarian cancer cells treated with RGD-SSL-PTX preparation, as well as the intracellular uptake of liposomes (a 6.21-fold increase in fluorescence intensity), when compared to those of non-targeted liposomes (SSL). For in vivo antitumor activity, it was shown in the present study that RGD-SSL-PTX preparation had the strongest tumor growth inhibition among the test formulations (P < 0.05) in BALB/c nude mice xenografted with SKOV-3 solid tumor. Meanwhile, there was no significant change in the body weight of the animals treated with RGD-SSL-PTX for intravenous injection at a dose of 12.5 mg/kg. It was suggested that the RGD-SSL-PTX preparation might have a great advantage over present-day chemotherapy with Taxol in curing those tumors overexpressing integrin receptors.

Inhibitors of bone resorption from Halenia corniculata.

Eleven xanthones (1-11), three flavonoids (12-14) and three secoiridoids (15-17) were isolated from the aerial parts of Halenia corniculata. Among those compounds, 1-hydroxy-2,3,4,5-tetramethoxyxanthone (1), 1-hydroxy-2,3,4,7-tetramethoxyxanthone (2), 1-hydroxy-2,3,4,5,7-pentamethoxyxanthone (3), 1-hydroxy-2,3,5-trimethoxyxanthone (4), 1,8-dihydroxy-3,5-dimethoxyxanthone (7), and luteolin (12), at the concentration of 1 microg/mL, effectively inhibited the osteoclast differentiation in a co-culture system with mouse osteoblastic calvarial cells and bone marrow cells. Notably, compounds 1, 3, and 4 exhibited, in a dose-dependent manner, significant inhibition of osteoclast differentiation even at a low concentration (0.01 microg/mL). All the inhibitory compounds, except for compound 7, significantly reduced the pit formation on the dentine slice compared with the control group. For the survival of the mature osteoclasts, compounds 1-4 and 12 (1 microg/mL), significantly decreased the survival number through induction of cell apoptosis, and compound 4 exhibited a significant inhibitory effect on osteoclast survival even at the low concentration of 0.1 microg/mL.

Pharmacokinetic interaction between tanshinones and polyphenolic extracts of salvia miltinorrhiza BUNGE after intravenous administration in rats.

The objective of this study was to investigate the interaction between tanshinones and polyphenolic extracts of Salvia miltiorrhiza BUNGE in rats. The rats in the medium dose groups were given an intravenous administration of 10 mg/kg tanshinones extract-loaded emulsion (equivalent to 4.0 mg/kg tanshinone IIA (TSIIA)), 100 mg/kg polyphenolic extract solution (equivalent to 61.2 mg/kg salvianolic acid B (Sal B)) or mixed extracts-loaded emulsion (equivalent to 4.0 mg/kg TSIIA and 61.2 mg/kg Sal B). The dosage given to the low dose groups was half that of the medium dose groups, while the high dose groups received twice the dosage of the medium dose groups. The areas under the plasma concentration-time curve (AUC) of TSIIA and Sal B were considerably increased (about 2-14 fold) after intravenous administration of mixed extracts-loaded emulsion in comparison with the equivalent dose of the corresponding extract administration. An increase of about 2-fold was observed in both the low and medium dose groups for TSIIA and Sal B, while there was at least a 14- and 5-fold significant increase (p<0.01) for TSIIA and Sal B in the high dose groups, respectively which was due to a significant (p<0.01) reduction in total plasma clearance (CL(t)). The peak plasma concentrations (C(0.083 h)) of TSIIA and Sal B were also both significantly increased (p<0.01). However, no significant differences in the terminal elimination half-life (t(1/2)) of TSIIA and Sal B in the mixed extracts-loaded emulsion groups were found compared with that of the corresponding extract groups except for the high dose groups of TSIIA (p<0.05). Therefore, a pharmacokinetic interaction occurs between tanshinones and polyphenolic extracts of Salvia miltinorrhiza BUNGE after intravenous administration in rats, which affects the pharmacokinetic process of TSIIA and Sal B in vivo.

[RP-HPLC determination of betulinic acid in Callicarpa macrophylla].

OBJECTIVE: To establish an RP-HPLC method for determination of betulinic acid in Callicarpa macrophylla, a commonly used herbal in Yunnan. METHOD: A Kromasil-C18 column (4.6 mm x 200 mm, 5 microm) and a mobile phase consisted of acetonitrile-0.1% phosphoric acid (63: 37) were used. The flow rate was 1.0 mL x min(-1) and the UV detector wavelength was 205 nm. RESULT: Betulinic acid was well separated from other compounds in C. macrophylla. The content of betulinic acid in C. macrophylla from different origins showed apparent differences, the content of betulinic acid in C. macrophylla from Yunnan was the highest. The calibration curve was linear in the range of 0.016 6-0.332 mg x mL(-1) of betulinic acid with correlation coefficient 0.999 8. The average recovery of betulinic acid was 98.5%. CONCLUSION: The method is simple, accurate and reproducible, and is suitable for the quality control of C. macrophylla.

Metabolites of scutellarein in rat plasma.

The metabolism of scutellarein was investigated in rats. Four metabolites (M1-M4) together with scutellarein were detected and identified as scutellarein-glucuronides in rat plasma by HPLC-DAD, HPLC-MS, and HPLC-MS/MS.

[Study on chemical constituents of Euphorbia hylonoma hand. -Mazz].

OBJECTIVE: To study the constituents of the roots of Euphorbia hylonoma Hand. -Mazz. METHODS: The chemical constituents were isolated and purified by solvent extraction together with various chromatographic techniques, the structures were elucidated on the basis of chemical properties and spectral data. RESULTS: Eight compounds were isolated from the acetone extracts of the roots of Euphorbia hylonoma Hand-Mazz., which were euphol(I), 5-hydroxymethylfuraldehyde(II), beta-sitosterol(III), beta-sitosterol glucoside (IV),3,3',4-tri-o-methylellagic acid(V), 3, 3' tdi-o-methylellagic acid (VI),3,3'-di-o-methylellagic acid-4'-o-beta-dxylopyranosid (VII), gallic acid(VIII). CONCLUSION: The compounds II, VI, VII, VIII were isolated from Euphorbia hylonoma Hand-Mazz. for the first time.

[Studies on the methods of extract and determination of total tannins and gallic acids of the root of Euphorbia hylonoma].

OBJECTIVE: To determine total tannins and gallic acid of the root of Euphorbia hyloomla. METHODS: With the gallic acid as reference, tannins and gallic acid of the root of Euphorbia hylonoma were determined by ultraviolet spectrophtometer and high performance liquid chromatography, respectively. RESULTS: The content of tannins of the root of Euphorbia hylonoma were determined by different extract methods, including extracted by water, 70% alcohol, acetone on supersound, the determination data were 4.375%, 7.240%, 3.958%, respectively. When used recirculation method by water, 70% alcohol, acetone, the determination data were the determination data are 3.773%, 2.503%, 1.59%, respectively. The content of gallic acid of the root was 0.047%. CONCLUSION: Content of total tannins by alcohol super sound is the highest comparing with other extract methods, this method can used in extract of total Tannins of the root of Euphorbia hylonoma.

[Advances in studies on pharmacokinetics of aristolochic acid I].

Aristolochic acid I (AA-I) was absorbed and distributed quickly in vivo, the plasma concentration-time curve were fit with the open two-compartment model and one-compartment model, respectively. The elimination of AA-I has relationship with the dosage, the low dose group eliminates more quickly than the high dose group. The characters of pharmacokinetics of AA-I induce the cumulation of AA-I in vivo and the nephrotoxin to the kidney and other viscera.

Effects of magnolol and honokiol derived from traditional Chinese herbal remedies on gastrointestinal movement.

AIM: To study the effects of magnolol and honokiol on isolated smooth muscle of gastrointestinal tract and their relationship with Ca2+, and on the gastric emptying and the intestinal propulsive activity in mice. METHODS: Routine experimental methods using isolated gastric fundus strips of rats and isolated ileum segments of guinea pigs were adopted to measure the smooth muscle tension. The effects of magnolol 10(-3), 10(-4), 10(-5) mol/L, and honokiol 10(-4), 10(-5), 10(-6) mol/L on the contractility of gastric fundus strips of rats and ileum of guinea pigs induced by acetylcholine (Ach) and 5-hydroxytryptamine (5-HT) was assessed respectively. The method using nuclein and pigment methylene blue was adopted to measure the gastric retention rate of nuclein and the intestinal propulsive ratio of a nutritional semi-solid meal for assessing the effect of magnolol and honokiol (0.5, 2, 20 mg/kg) on gastric emptying and intestinal propulsion. RESULTS: Magnolol and honokiol significantly inhibited the contractility of isolated gastric fundus strips of rats treated with Ach or 5-HT and isolated ileum guinea pigs treated with Ach or CaCl2, and both of them behaved as non-competitive muscarinic antagonists. Magnolol and honokiol inhibited the contraction induced by Ach in Ca2+-free medium and extracellular Ca2+-dependent contraction induced by Ach. Each group of magnolol and honokiol experiments significantly decreased the residual rate of nuclein in the stomach and increased the intestinal propulsive ratio in mice. CONCLUSION: The inhibitory effect of magnolol and honokiol on contractility of the smooth muscles of isolated gastric fundus strips of rats and isolated ileum of guinea pigs is associated with a calcium-antagonistic effect. Magnolol and honokiol can improve the gastric emptying of a semi-solid meal and intestinal propulsive activity in mice.

Sesquiterpenes and alkaloids from Lindera chunii and their inhibitory activities against HIV-1 integrase.

Three new eudesmane type sesquiterpenoid lindenanolides E (1), F (2) and G (3), and two new aporphine alkaloid lindechunines A (18) and B (20) were isolated from roots of Lindera chunii MERR., together with seven known sesquiterpenes including a new naturally-occurring lindenanolide H (4) and eight known aporphine alkaloids. The structures of these compounds were determined by spectroscopic means. Of the isolated compounds, hernandonine (14), laurolistine (16), 7-oxohernangerine (17) and lindechunine A (18) showed significant anti-human immunodeficiency virus type 1 (HIV-1) integrase activity with IC(50) values of 16.3, 7.7, 18.2 and 21.1 microM, respectively. The major alkaloids presented in the roots of L. chunii were quantitatively analyzed by an HPLC method.

[Study on chemical constituents of rhizome of Anemone raddeana].

AIM: To investigate the chemical constituents of the rhizome of Anemone raddeana Regel, so as to find new active compounds. METHODS: The ethanol extracts of the rhizome of Anemone raddeana were obtained by silica column, HPLC. The structures of the compounds were elucidated by means of physico-chemical method and spectral analysis (IR, FAB-MS, 1HNMR, 13CNMR, DEPT, 1H-1H COSY, HMQC, HMBC). RESULTS: Nine compounds were isolated and identified as 27-hydroxyolean-12(13)-en-28-oic acid-3-0-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside (1), eleutheroside K (2), Oleanolic acid-3-O-alpha-L-rhamnopyranosyl-(1-->2)-[beta-D- glucopyranosyl-(1-->4)]-alpha-L-arabinopyranoside (3), betulin (4), betulic acid (5), acetyloleamolic acid (6), evonymitol (7), oleamolic acid (8) and diosgenin (9). CONCLUSION: Compound 1 is a new compound, named raddeanoside 12. Compounds 3-7 were isolated from this plant for the first time.