Antitumor effect and mechanism of an ellagic acid derivative on the HepG2 human hepatocellular carcinoma cell line.

In the present study, to identify the effective components of Chinese traditional herbs, Euphorbia hylonoma Hand.-Mazz. (Euphorbiaceae), a folk herb that has been used among the Qinling mountain area for hundreds of years, was investigated. 3,3'-Di-O-methyl ellagic acid-4'-O-ß-d-xylopyranoside (JNE2), an ellagic acid derivative, was isolated from the acetone extract of the herb and its antitumor activity against human hepatoma HepG2 cells was detected in vitro. The results showed that JNE2 inhibited the proliferation of HepG2 cells in a dose- and time-dependent manner and blocked the cell cycle at the G1/S phase. A high dosage of JNE2 induced apoptosis of the tumor cells, but no significant differences were identified between the treatment groups. The invasiveness of HepG2 cells was also inhibited by JNE2. The mechanism of the antitumor effect of JNE2 at the molecular level was presumed to be due to the upregulation of the protein expression of Bax and caspase-3, and the downregulation of the protein expression of Bcl-2 and CCND1. The results suggested that JNE2 is a potential antitumor agent that merits further investigation.

New alkaloids from Aconitum taipaicum and their cytotoxic activities.

Three new aconitine-type C19-diterpenoid alkaloids, taipeinines A-C (1-3), were isolated from the roots of Aconitum taipaicum. The chemical structures of these three compounds were established as (1α,6α,8α,14α,16α)-20-ethyl-8,14-dihydroxy-1,6,16-trimethoxy-4-(methoxymethyl)-aconitane (1), (1α,6α,8α,14α,16ß)-20-ethyl-8,14-dihydroxy-1,6,16-trimethoxy-4-(methoxymethyl)-aconitane (2) and (1α,6α,8α,14α,16α)-20-ethyl-1,8,14-trihydroxy-6,16-dimethoxy-4-(methoxymethyl)-aconitane (3), respectively, on the basis of spectroscopic analyses, mainly MS, 1D and 2D NMR. The cytotoxic activities of these compounds were also assayed, and the results were quite impressive.

[Analysis of petroleum fraction from flower, stem and leaf of Aconitum taipeicum by GC-MS].

OBJECTIVE: To analyze the chemical constituents of petroleum fraction of Aconitum taipeicum. METHODS: The methanol extract of Aconitum taipeicum were extracted by petroleum and then analyzed by GC-MS. The compounds were quantitatively determined by normalization method. RESULTS: Twenty eight compounds were separated and identified. Most of them were alkane, fat acids and their esters and alkenes. The Nonacosane covered 13.057% of the total peaks, while 19-methyl-18,21-Hexatriacontanediether 8.180%, Ethylen eglycol monooctadecy ether 7.851%, 3,7,11,15-Tetramethyl-2-hexadecen-1-ol 7.805%, Metahyl Palmitate 6.676% and so on. CONCLUSION: This is the first report of constituents from the flower, stem and leaf of Aconitum taipeicum. The results will provide foundation for further exploitation and use of Aconitum taipeicum.

Two new amide alkaloids with anti-leukaemia activities from Aconitum taipeicum.

Two new amide alkaloids, named 3-isopropyl-tetrahydropyrrolo [1,2-a] pyrimidine-2,4(1H,3H)-dione (1) and 1-acetyl-2,3,6-triisopropyl-tetrahydropyrimidin-4(1H)-one (2), were isolated from the roots of Aconitum taipeicum. Their chemical structures were characterized on the basis of MS, 1D- and 2D NMR. The anti-leukaemia activities of the compounds were also tested. The results indicated that the compounds exhibited more significant cell growth inhibitory activities against HL-60 cells than adriamycin, with the IC(50) of 1.1 ± 0.03 µg/mL and 1.6 ± 0.07 µg/mL respectively. In addition, two compounds showed anti-tumor activities against K562 cells as well.

[Study on in vitro release and transdermal behaviors of mumps cataplasm of complex prescription].

OBJECTIVE: To investigate the in vitro release and transdermal behaviors of mumps cataplasm of complex prescription. METHODS: The improved Franz difficusion was used and the concentration of drugs was detected. DCS was determined by HPLC and flavanoid contents were determined by UV. RESULTS: The accumulation skin permeation percentage of DCS and flavanoid was 32% and 21%, respectively, the in vitro release percentage of DCS and flavanoid was 47% and 42%, respectively. CONCLUSION: The transdermal behavior of mumps cataplasm of complex prescription is an zero-order kinetics progress. The in vitro release behavior is in accordance with the Higuchi equation.

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.

[Analysis of petroleum fraction of Aconitum taipeicum by GC-MS].

OBJECTIVE: To analyze the chemical constituents of petroleum fraction of Aconitum taipeicum. METHODS: The methanol extracts of Aconitum taipeicum were extracted by petroleum and then analyzed by GC-MS. The compounds were quantiatively determined by normalization method. RESULTS: Thirty-eight compounds were separated and thirty-three compounds that covered 97.28% of the total peaks were identified. Most of them were fat acids and their esters, steroids and alkenes. The n-Hexadecanoic acid covered 12.083% of the total peaks, while Stigmast-4-en-3-one 10.183%, Linolein, 1-mono-8.96%, 9, 12-Octadecadienoic acid (Z,Z)-8.054% and so on. CONCLUSION: This is the first report of constituents of Aconitum taipeicum except alkaloids. The results will provide foundation for further exploitation and use of Aconitum taipeicum.

[Preliminary study on purification technics of total flavonoids in Rhodiola dumulosa by macroporous resin].

OBJECTIVE: To choose the best macroporous resin for purifying total flavonoids in Rhodiola dumulosa and study various factors affecting purification of resin in order to optimize the technics. METHODS: Using methods combining static adsorption with desorption and dynamic adsorption with desorption, evaluating the technics by determination of total flavonoids in Rhodiola dumulosa using ultraviolet and visible spectrophotometry. RESULTS: The best macroporous resin was D101. The optimized technics were as follows: sample total flavonoids concentration was 3.625 mg/ml, adsorption velocity was 2 BV/h, desorption ethanol concentration was 95%, desorption velocity was 2 BV/h, eluant volume was 5 BV, the purity of total flavonoids could reach 48.5%. CONCLUSIONS: Purification performance of D101 macroporous resin is the best, and it is fit for the preliminary purification of total flavonoids in Rhodiola dumulosa.

[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.