Two new bisamides from the leaves of Aglaia perviridis.

Two new bisamides, aglaiamides A (1) and B (2), along with three known ones (3-5), were isolated from the leaves of Aglaia perviridis. Their structures were established on the basis of detailed spectroscopic analyses.

[The swelling behavior of choline fenofibrate hydrogel matrix tablets using dynamic image analysis].

The purpose of this study is to investigate the effects of formulation on the swelling behavior of choline fenofibrate hydrogel matrix tablets and reveal the relation between swelling property and release profile using dynamic image analysis. The volume swelling ratio (SR) and height/width (k) could evaluate the swelling behavior of matrix tablets well. The mount of hydroxypropyl methylcellulose (HPMC) and the ratio between K15M and K4M affected the volume swelling ratio, while PVP didn't. The three factors all impacted k, which was an indicator of the strength of the gel formed by HPMC. The accumulative release ratio and SR, the rate of swelling and the rate of release were compared. The proper model equations were established for the results with an excellent correlation. The results prove that there is a strong relevance between the swelling behavior and release property. This study provides a guideline in the study design for hydrogel matrix tablets.

[Preparation and properties of thermosensitive in situ gel for ophthalmic formulation containing pearl hydrolyzate].

The study was designed to generate an ophthalmic thermosensitive in situ gel with improved mechanical and mucoadhesive properties that may prolong the retention time to enhance the bioavalability of pearl hydrolyzate. The gene was comprised of poloxamer 407, poloxamer188 and Carbopol 934, which were optimized by central composite design and response surface methodology. The rheological properties, transcorneal permeability, retention time and in vitro release behaviors of the optimal gel formulation were investigated. The gel was Newtonian liquid at 25 ℃ and performed as a semisolid gel with non-Newtonian liquid property with a gelation time of 13 s at 35 ℃. Compared with a conventional eye drops, the ophthalmic in situ gel exhibited a sevenfold increase in retention with a sustained release behavior, which was observed with suitable permeability coefficient at 5.58 cm·s-1. In conclusion, the new gel of pearl hydrolyzate prolonged the release duration of drug, which may decrease the frequency of administration of pearl hydrolyzate.

[Determination of contact angle of pharmaceutical excipients and regulating effect of surfactants on their wettability].

To study the effects of surfactants on wettability of excipients, the contact angles of six types of surfactants on the surface of two common excipients and mixture of three surfactants with excipients were measured using hypsometry method. The results demonstrated that contact angle of water on the surface of excipients was associated with hydrophilcity of excipients. Contact angle was lowered with increase in hydrophilic groups of excipient molecules. The sequence of contact angle from small to large was starch < sodium benzoate < polyvinylpyrrolidone < sodium carboxymethylcellulose < sodium alginate < chitosan < hydroxypropyl methyl cellulose

[Isoflavonoids from Caragana changduensis and their nitric oxideinhibitory activities].

Ten isoflavonoids were isolated from the heartwoods of Caragana changduensis Lion f. by means of various column chromatographic techniques. Based on the detailed spectral data analysis (MS and NMR), as well as comparison with the literatures, their chemical structures were determined as 7,2'-dihydroxy-8,4'-dimethoxyisoflavone (1), 4'-hydroxy-7,3'-dimethoxyisoflavone (2), 5, 7, 4'-trihydroxy-2',5'-dimethoxyisoflavone (3), prunetin (4), afrormosin (5), odoratin (6), genistein (7), texasin (8), pratensein (9), and 6,7,3'-trihydroxy-4'-methoxyisoflavone (10). Among them, compounds 1-3 and 9-10 were isolated from the Caragana genus for the first time. All the compounds were obtained from this species for the first time. In the preliminary assays, compounds 1, 2, 6, and 7 possessed significant inhibitory effects on NO production, with IC50 values of 48.12, 25.32, 62.71, 43.59 µmol x L(-1), respectively.

[The rheology properties of common hydrophilic gel excipients].

To investigate theological properties of common hydrophilic gel excipients such as Carbopol based on viscosity, the viscosity was determined by rotation method and falling-ball method. Linear regression was made between ln(eta) and concentration, the slope of which was used to explore the relation between viscosity and concentration of different excipients. The viscosity flow active energy (E(eta)) was calculated according to Arrhenius equation and was used to investigate the relation between viscosity and temperature of different excipients. The results showed that viscosities measured by two methods were consistent. Concentration of guargum (GG) and hydroxypropylmethyl cellulose (HPMC) solution had a great influence on the viscosity, k > 5; while concentration of polyvinylpyrrolidone-K30 (PVP-K30) and polyethylene glycol 6000 (PEG6000) exerted a less effect on viscosity, k < 0.2; viscosity flow active energy of different excipients were close, which ranged from 30 to 40 kJ x mol(-1). Therefore, theological properties study could provide the basis for application of excipients and establish a foundation for the research of relation between excipients structure, property and function.

Dibenzocyclooctadiene lignans from Kadsura coccinea.

In vitro anti-allergic screening of medicinal herbal extracts revealed that the EtOAc extract of the rhizoma of Kadsura coccinea inhibited nitric oxide (NO) production in a lipopolysaccharide and recombinant mouse interferon-γ activated murine macrophage-like cell line, RAW264.7. Further fractionation of the EtOAc extract led to the isolation of two new dibenzocyclooctadiene lignans kadsuralignan G (1) and kadsuralignan L (2), and three known analog compounds. The absolute stereostructures were established by circular dichroism spectra. Both 1 and 2 showed moderate NO production inhibitory activities.

A high-performance liquid chromatography with circular dichroism detector for determination of stereochemistry of 6, 9-oxygen bridge dibenzocyclooctadiene lignans from kadsura coccinea.

The stereochemistry of two 6, 9-oxygen bridge dibenzocyclooctadiene lignans from Kadsura coccinea, are difficult to separate and very unstable. The present study was designed to develop a high-performance liquid chromatography using circular dichroism detection for the analysis of the stereochemistry. A new 6, 9-oxygen bridge dibenzocyclooctadiene lignans named Kadsulignan Q was firstly found with an S-biphenyl configuration. The other compound was identified as Kadsulignan L with an R- biphenyl configuration. In order to obtain kinetic data on their reversible interconversion, the stability was measured at different deuterated solvents such as deuterated methanol, deuterated chloroform and deuterated dimethylsulfoxide. The lignans were more unstable and converted more easily in deuterated methanol than in deuterated chloroform and deuterated dimethylsulfoxide.

Effects of ultrahigh pressure extraction on yield and antioxidant activity of chlorogenic acid and cynaroside extracted from flower buds of Lonicera japonica.

The present study was designed to establish and optimize a new method for extracting chlorogenic acid and cynaroside from Lonicera japonica Thunb. through orthogonal experimental designl. A new ultrahigh pressure extraction (UPE) technology was applied to extract chlorogenic acid and cynaroside from L. japonica. The influential factors, including solvent type, ethanol concentration, extraction pressure, time, and temperature, and the solid/liquid ratio, have been studied to optimize the extraction process. The optimal conditions for the UPE were developed by quantitative analysis of the extraction products by HPLC-DAD in comparison with standard samples. In addition, the microstructures of the medicinal materials before and after extraction were studied by scanning electron microscopy (SEM). Furthermore, the extraction efficiency of different extraction methods and the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities of the extracts were investigated. The optimal conditions for extracting chlorogenic acid and cynaroside were as follows: ethanol concentration, 60%; extraction pressure, 400 MPa; extraction time, 2 min; extraction temperature, 30 °C; and the solid/liquid ratio, 1 : 50. Under these conditions, the yields of chlorogenic acid and cynaroside were raised to 4.863% and 0.080%, respectively. Compared with other extraction methods, such as heat reflux extraction (HRE), ultrasonic extraction (UE), and Sohxlet extraction (SE), the UPE method showed several advantages, including higher extraction yield, shorter extraction time, lower energy consumption, and higher purity of the extracts. This study could help better utilize L. japonica flower buds as a readily accessible source of natural antioxidants in food and pharmaceutical industries.

Triterpenes from Kadsura coccinea.

In vitro anti-allergic screening of medicinal herbal extracts revealed that the 80% acetone extract of the rhizome of Kadsura coccinea inhibited nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-γ (IFN-γ) activated murine macrophage like cell line, RAW264.7. Further fractionation of the EtOAc extract led to the isolation of one new 3,4-seco-lanostane type triterpene named kadsuracoccin acid A (1) together with two known triterpenes anwuweizonic acid (2) and neokadsuranic acid B (3). Compounds 1-3 did not exhibit any inhibitory activities for NO production and IFN-γ activation.

Eryngiolide A, a cytotoxic macrocyclic diterpenoid with an unusual cyclododecane core skeleton produced by the edible mushroom Pleurotus eryngii.

Eryngiolide A (1), the first member of C20 diterpenoids with the skeleton deriving from a cyclododecane core fused with two γ-lactone units, was isolated from the solid culture of the edible mushroom Pleurotus eryngii. The structure of 1 was elucidated by extensive analysis of NMR spectra. Compound 1 exhibited moderate cytotoxicity against two human cancer lines in vitro.

Two sulfated triterpenoidal saponins from the barks of Zygophyllum fabago L.

Two new sulfated triterpenoid saponins, zygophylosides Q (1) and R (2), have been isolated from the barks of Zygophyllum fabago L. Their structures were elucidated as 3beta,24,28,30-tetrahydro-urs-20-ene-24-O-sulphonyl-3-O-[beta-D-glucopyranosyl]-30-O-beta-D-glucopyranoside and 3beta,24,28,30-tetrahydro-urs-20-ene-24-O-sulphonyl-3-O-[beta-D-xylopyranosyl]-30-O-beta-D-glucopyranoside, respectively, by spectral and chemical evidence.

Two new alkaloids from Capparis himalayensis.

Two new alkaloids, Capparin A (1) and B (2), along with seven known compounds 6-methoxyindoline-2,3-dione (3), wogonin (4), oroxylin A (5), kaempferol (6), apigenin (7), quercetin (8) and luteolin (9), were isolated from the whole plant of Capparis himalayensis. Their structures have been established on the basis of spectral methods and the structure of 1 was confirmed by X-ray crystallographic analysis.

Triterpenoidal saponins from the barks of Zygophyllum fabago L.

Two new triterpenoid saponins, zygophylosides O (1) and P (2), have been isolated from the barks of Zygophyllum fabago L. Their structures were elucidated as 3beta-[(2-O-sulfo-beta-D-xylopyranosyl)oxy]urs-12-ene-27,28-dioic acid and 3beta-[(2-O-sulfo-beta-D-xylopyranosyl)oxy]urs-12-ene-27,28-dioic acid 28-beta-D-glucopyranoside, respectively, by spectral and chemical evidence. Compound 1 showed weaker Nitric Oxide (NO) inhibitory activity.

Gerardianin A, a new abietane diterpenoid from Isodon lophanthoides var. gerardianus.

A new abietane diterpenoid, gerardianin A (1), along with a known compound 6,7-dehydroroyleanone (2), has been isolated from the aerial parts of Isodon lophanthoides var. gerardianus [Bentham] H. Hara. The structure of 1 was determined on the basis of spectroscopic methods and X-ray single-crystal diffraction analysis.

27-nor-triterpenoid glycosides from the barks of Zygophyllum fabago L.

From the bark of Zygophyllum fabago L., a new 27-nor-triterpenoid glycoside, 3-O-beta-D-glucopyranosyl-pyrocincholate (1), together with five known compounds, 3-O-6-deoxy-beta-D-glucopyranosyl-pyrocincholate (2), quinovic acid (3), 3-O-6-deoxy-beta-D-glucopyranosyl-quinovic acid (4), 3-O-beta-D-glucopyranosyl- quinovic acid (5) and 3-O-6-deoxy-beta-D-glucopyranosyl-cincholic acid (6), were isolated and their structures elucidated on the basis of spectroscopic data. Compounds 1, 2 and 3 showed some anti-tumour activities by MTT assay.

Triterpenoids from Hippophae rhamnoides L. and their nitric oxide production-inhibitory and DPPH radical-scavenging activities.

In our investigation on the chemical constituents of Hippophae rhamnoides L., the chloroform-soluble fraction of the 80% acetone extract of branch bark was observed to inhibit nitric oxide (NO) production in a lipopolysaccharide and recombinant mouse interferon-gamma-activated murine macrophage-like cell line, RAW 264.7 cells. Two new triterpenoids, 2-O-trans-p-coumaroyl maslinic acid (1) and 2-O-caffeoyl maslinic acid (2), and three known triterpenoids, oleanolic acid (3), 3-O-trans-p-coumaroyl oleanolic acid (4), and 3-O-caffeoyl oleanolic acid (5), and 6-methoxy-2H-1-benzopyran (6) and beta-sitosterol (7) were isolated from the branch bark extract. Their inhibitory activities on the production of NO in RAW 264.7 cells and radical-scavenging activities were examined.

New lignans from Kadsura coccinea and their nitric oxide inhibitory activities.

In vitro anti-allergic screening of medicinal herbal extracts revealed that the chloroform extract of the rhizoma of Kadsura coccinea inhibited nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-gamma (IFN-gamma) activated murine macrophage like cell line RAW 264.7. Further fractionation of the chloroform extract led to the isolation of three new lignans, including two dibenzocyclooctadiene lignans and one arylnaphthalene lignan, together with other three known dibenzocyclooctadiene lignans. This is the first report of NO production inhibitory activity of Kadsura coccinea and first report about the isolation of arylnaphthalene lignan from K. coccinea.