OBJECTIVETo evaluate the effect of Radix euphorbiae pekinensis extract on the permeability and bioavailability of paclitaxel co-administered orally.

METHODSBased on Ussing Chamber and in vivo experiment, the permeability and bioavailability of paclitaxel were evaluated after oral co-administration with radix euphorbiae pekinensis in rats. The contents of paclitaxel in the permeates and the blood samples were determined using HPLC and LC-MS/MS method, respectively.

RESULTSIn Radix euphorbiae pekinensis co-administration group, the Papp of the mucosal-to-serosal (M-S) transport or serosal-to-mucosal transport (S-M) of paclitaxel in the jejunum or ileum segment differed significantly from those in verapamil co-administration group and blank control group (P<0.05), but the Papp of S-M transport in the colon showed no significant difference from that in the blank control group. In the blank group, the average absolute bioavailability (AB%) of orally administered paclitaxel was only 2.81%, compared to that of 7.63% in radix euphorbiae pekinensis group. The average AB% in verapamil group was about 1.5 times that of the blank group.

CONCLUSIONCo-administration of Radix euphorbiae pekinensis extract can increase the bioavailability of orally administered paclitaxel.

Administration, Oral ; Animals ; Biological Availability ; Biological Transport ; Chromatography, High Pressure Liquid ; Euphorbiaceae ; chemistry ; Paclitaxel ; pharmacokinetics ; Permeability ; Plant Extracts ; pharmacology ; Plant Roots ; chemistry ; Rats ; Tandem Mass Spectrometry ; Verapamil

Fourteen compounds were isolated from 95% ethanol extract by silica gel, MCI, and ODS column chromatography. These compounds were respectively identified as quercetin (1), kaempferol (2), (+)-catechin (3), fraxin (4), protocatechuic acid (5), gallic acid (6), methyl gallate (7), ethyl gallate (8), apocynol A (9), baccatin (10), cerevisterol (11), ellagic acid (12), 3, 3',4'-tri-0-methylellagic acid(13) and N-benzoyl-L-phenylalaninyl-N-benzoyl-L-phenylalaninate(14) by analyzing their spectral data and comparing with the previously reported literatures. Except for gallic acid (6), all other compounds were isolated from this plant for the first time. Compounds 1, 2 and 6 showed moderate anti-proliferation activities on tumor cells.
Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cell Survival ; drug effects ; Drugs, Chinese Herbal ; chemistry ; toxicity ; Euphorbiaceae ; chemistry ; Humans ; Plants, Medicinal ; chemistry ; Spectrometry, Mass, Electrospray Ionization

We investigated the anti-nociceptive effect of Excoecaria agallocha (E.agallocha) against chemically and thermally induced nociception, Albino mice received a dose of 10, 15, 20, or 25 mg/kg of alkaline chloroform fraction (Alk-CF) of E.agallocha by oral administration. Compared with controls, Alk-CF decreased the writhing numbers (P<0.01) in a dose dependent manner. Further we determined that, Alk-CF contained, a potent compared to control, also potent anti-nociceptive agent that acted via opioid receptors and using HPLC, identified this compound as Rutin. Docking simulation demonstrated that Rutin interacted strongly with cyclooxygenase, forming a number of specific hydrogen bonds. In conclusion we have identified peripheral and central anti-nociceptive activities of E.agallocha that involve opioid receptor, and in which the active compound is Rutin.
Analgesics ; isolation & purification ; therapeutic use ; Animals ; Drug Evaluation, Preclinical ; Euphorbiaceae ; chemistry ; Female ; Male ; Mice ; Pain ; drug therapy ; Phytotherapy ; Plant Extracts ; chemistry ; therapeutic use ; Rutin ; isolation & purification ; therapeutic use

AIM: To investigate the chemical constituents in the stems of Trigonostemon heterophyllus. METHOD: The chemical constituents were isolated by column chromatography on silica gel, Rp-18, and Sephadex LH-20, and their structures were elucidated on the basis of spectroscopic analysis. RESULTS: Three compounds were isolated and identified as a new diterpene, trigonoheterene B (1), together with two known compounds, trigonostemone (2) and trigonochinene B (3). CONCLUSION Compound 1 is new. Compounds 2 and 3 showed antibacterial activities.
Diterpenes ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Euphorbiaceae ; chemistry ; Molecular Structure ; Plant Stems ; chemistry

The anti-malarial potential of different parts of Allophylus africanus P. Beauv and Tragia benthamii Baker were determined in vivo for suppressive, curative and cytotoxic activities in mice receiving 0.2 mL of a standard inoculum size of 1 × 10(7) infected erythrocytes of Plasmodium berghei (NK-65) intraperitoneally. The A. africanus extracts suppressed parasitaemia following administration to infected mice by 92.82%-97.81% on day 7 post-infection against 96.81% for chloroquine. The infected extract-treated animals had significantly moderate (P < 0.05) packed cell volume (PCV) compared with the infected, untreated animals. Phytochemical screening revealed a predominance of tannins, saponins, flavonoids and carbohydrates in all parts of A. africanus, and alkaloids instead of flavonoids in the extract of T. benthamii. The results suggest that the extract possesses considerable antimalarial activity. These results support further studies on A. africanus.
Animals ; Antimalarials ; administration & dosage ; chemistry ; Drug Evaluation, Preclinical ; Euphorbiaceae ; chemistry ; Female ; Humans ; Malaria ; drug therapy ; parasitology ; Male ; Mice ; Plant Extracts ; administration & dosage ; chemistry ; Plasmodium berghei ; drug effects ; Sapindaceae ; chemistry

To study the chemical constituents of Alchornea trewioides, silica gel column chromatography, Sephadex LH-20, reverse phase ODS column chromatography, MCI and semi-preparative HPLC were used to separate the 95% EtOH extract of the root of Alchornea trewioides. The structures were elucidated on the basis of spectroscopic studies including ESI-TOF-MS, 1H NMR, 13C NMR, HSQC and HMBC. Eight phenolic acids were obtained and identified as 1-O-galloyl-6-O-vanilloyl-beta-glucose (1), gallic acid (2), ethyl gallate (3), syringic acid (4), glucosyringic acid (5), erigeside C (6), 3, 4-dimethoxyphenyl-(6'-O-alpha-L-rhamnosyl)-beta-D-glucopyranoside (7) and 3, 4, 5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside (8). Among them, compound 1 is a new compound, compounds 4-8 are isolated from the genus Alchornea for the first time, and the others are isolated from the plant for the first time.
Benzoates ; chemistry ; isolation & purification ; Euphorbiaceae ; chemistry ; Gallic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Glucose ; analogs & derivatives ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Hydroxybenzoates ; chemistry ; isolation & purification ; Molecular Structure ; Phenols ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry

OBJECTIVETo study the chemical constituents of Excoecaria acerifclia.

METHODColumn chromatography on Silica gel and Sephadex LH-20 were applied for isolation and purification of the constituents. The structures were elucidated on the basis of spectrascopic analysis, chemical evidences and by comparison with the data reported in the literature.

RESULTFrom the crude EtOAc fraction of Excoecaria acerifclia F. Didr, 14 compounds were isolated and identified as 7,8-trans-4,5,9-trihydroxy-3,3',9'-trimethoxy-7-O-5',8-O-4'-neolignan (1), 7,8-trans 4,5,9,9'-tetrahydroxy-3,3'-dimethoxy-7-O-5',8-O-4'-neolignan (2), malloapelin C (3), sy-ringaresinol (4), 2alpha,3beta,24-trihydroxy-12-ursen-28-oic acid (5), 11-hydroxy-3-oxo-12-ursen-28-oic acid (6), 6-hydroxy-20 (29)-lupen-3-one (7), isolupenyl acetate (8), kaempferol (9), quercetin (10), apigenin (11), catechin (12), kamepferol-3-O-beta-D-galactopyranoside (13), and catechin (6-->8) catechin (14).

CONCLUSIONSCompound 1 was new, the remained compounds were isolated and identified from E. acerifclia for the first time. Among them, compounds 5-8 are triterpenoids, while the other compounds are phenylpropanoids.

Chromatography ; Drugs, Chinese Herbal ; chemistry ; Euphorbiaceae ; chemistry ; Organic Chemicals ; analysis

OBJECTIVETo establish a method for analyzing the content of total polyphenols in leaves of Jatropha curcas. L.

METHODSGallic acid was used as reference substance, the content of total polyphenols was analyzed Folin-Ciocalteu chromatometry.

RESULTSThere was a good linearity for gallic acid in the range of 0.002-0.010 g.L(-1). The content of total polyphenols in the leaves of Jatropha curcas. L was approximately 6.74% with RSD 0.75%. The sample solution was stable during 10-90 min with RSD 0.28%. The precision RSD was 0.23% and the average recovery 99.85% (n=5).

CONCLUSIONThis method is simple, fast and reproducible.

Euphorbiaceae ; chemistry ; Plant Leaves ; chemistry ; Polyphenols ; analysis ; isolation & purification

OBJECTIVETo investigate the chemical constituents of Excoecaria acerifclia and their antitumor activities.

METHODThe constituents were isolated and purified by column chromatography. Their structures were identified by their physicochemical properties and spectral features. Cytotoxicities of the purified compounds were evaluated by MTI method against human cancer cell lines HepG2.

RESULTEight compounds were isolated and identified as: 7-hydroxy-6-methoxy-coumarin (1), 8-hydroxy-6,7-methoxy-coumarin (2), kaempferol (3), kaempferol-3-O-beta-D-glucoside (4), quercetin-3-O-beta-D galactoside (5), kaempferol-3-O-beta-D-glucoside-2"-gallate (6), beta-sitosterol (7), daucosterol (8).

CONCLUSIONAll compounds were isolated from this plant for the first time. Compounds 5 showed inhibitory activity towards HepG2 with IC50 values of 7.13 mol x L(-1).

Cell Proliferation ; drug effects ; Euphorbiaceae ; chemistry ; Hep G2 Cells ; Humans ; Plant Extracts ; analysis ; isolation & purification ; pharmacology

OBJECTIVETo evaluate the antimicrobial activity of the methanol extract from the stem bark of Drypetes tessmanniana, fractions (DTB1-5) as well as compounds [friedelin (2), 3,7-dioxofriedelane (3), 3,15-dioxofriedelane (4), 3beta- O-(E)-3,5-dihydroxycinnamoyl-11-oxo-olean-12-ene (6), and 3beta,6alpha-dihydroxylup-20(29)-ene (7).

METHODSAgar disc diffusion was used to determine the sensitivity of the above samples, whilst the microdilution method was used for the determination of the minimal inhibitory concentration (MIC) and the minimal microbicidal concentrations (MMC).

RESULTSThe diffusion test showed that the crude extract was able to prevent the growth of all tested organisms. All other samples showed selective activity. The inhibitory effect of the fraction DTB2 was noted on 63.7%, that of DTB1 and DBT3 on 54.6%, whilst DTB4 and DTB5 were active on 9.1% of the 11 tested organisms. The tested compounds prevented the growth of 81.8% of the tested microbial species for compounds 3 and 4, 36.7% for compound 6, and 18.2% for compound 7. The results of the MIC determinations indicated perceptible values for DTB and compound 4 on 81.8% of the tested organisms. For other samples, MICs were detected on 0-63.7%. The lowest MIC value (78.12 microg/mL) for the crude extract and fractions (DTB2) was observed on M. audouinii. The corresponding value for isolated compounds (156.25 microg/mL) was noted with compounds 3 on S. faecalis and 4 on M. audouinii audouinii. The results of the MMC determination suggested that the microbicidal effect of most of the tested samples on the studied microorganisms could be expected.

CONCLUSIONThe methanol extract from the stem bark of Drypetes. tessmanniana (Euphorbiaceae) as well as some of the isolated compounds might be potential sources of new antimicrobial drugs.

Anti-Infective Agents ; chemistry ; isolation & purification ; pharmacology ; Bacteria ; drug effects ; Disk Diffusion Antimicrobial Tests ; Euphorbiaceae ; chemistry ; Fungi ; drug effects ; Methanol ; chemistry ; Microbial Sensitivity Tests ; Plant Bark ; chemistry ; Plant Extracts ; pharmacology ; Plant Stems ; chemistry ; Reference Standards