Antithrombotic effects and related mechanisms of Salvia deserta Schang root EtOAc extracts.

Salvia deserta Schang (SDS) belongs to the same family as Salvia miltiorrhiza bunge, one of the antithrombotic Chinese herbal medicines. In our study, EtOAc root extracts were analyzed for their effects on adenosine diphosphate (ADP)-induced platelet aggregation in rabbits and FeCl3-induced rat common carotid artery thrombosis as well as on rat blood plasma concentrations of thromboxane B2 (TXB2), 6-keto-prostaglandin F1 alpha (6-keto-PGF1α), antithrombin-III (AT-III), protein C (PC), plasminogen (PLG), plasminogen activator inhibitor (PAI-1), von Willebrand factor (vWF) and tissue-type plasminogen activator (t-PA). EtOAc extracts from SDS roots had significant inhibitory effects on ADP-induced maximum platelet aggregation rate (10.2 ± 2.6 vs control 35.7 ± 5.2; P < 0.05), reduced the FeCl3-induced rat common carotid artery thrombus weight and thrombus area ratio (P < 0.05), significantly decreased plasma TXB2, vWF and PAI-1 levels and increased 6-keto-PGF1α and t-PA levels in a dose dependent manner (all P < 0.05). Thus, the ratio of TXB2/6-keto-PGF1α was significantly decreased (P < 0.05), while the ratio of t-PA/PAI-1 was significantly increased (P < 0.05). In addition, enhanced AT-III and PC activities indicated coagulation inactivation effects of EtOAc SDS root extracts. EtOAc extraction from SDS showed antithrombotic effects, which are likely due to platelet adhesion and aggregation inhibition as well as anticoagulant activities.

Effects of Periostracum Cicadae on Cytokines and Apoptosis Regulatory Proteins in an IgA Nephropathy Rat Model.

Periostracum cicadae, the cast-off shell of the cicada Cryptotympana pustulata Fabricius, is used in traditional Chinese medicine for its diaphoretic, anticonvulsive, sedative, antipyretic, and antiallergic effects. However, the exact pathogenesis of immunoglobulin A nephropathy (IgAN) remains unclear, thereby hindering investigations to identify novel therapeutic agents. A rat IgAN model was established by administration of bovine serum albumin, lipopolysaccharide, and carbon tetrachloride, which simultaneously established blood stasis and a heat syndrome model. The animals were sacrificed to detect changes in protein levels in urine and blood. Immunofluorescence was performed to assess IgA deposition in the glomeruli. Tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß), and interleukin 6 (IL-6) levels were measured in bronchoalveolar lavage fluid (BALF) by enzyme-linked immunosorbent assay. Hematology and eosin, periodic acid-Schiff, TUNEL (TdT-mediated dUTP Nick-End Labeling), and immunohistochemical staining were performed to evaluate histopathological changes in kidney tissues. Additionally, target-related proteins were measured by Western blotting. Periostracum cicadae resulted in a reduction in blood and urine protein levels. Serum TNF-α, IL-1ß, and IL-6 levels significantly decreased in the periostracum cicadae-treated groups compared to the IgAN group. Furthermore, a reduction in MCP-1 (Monocyte Chemotactic Protein-1), TLR4 ((Toll-Like Receptor 4)), and IgA expression levels and a dose-dependent increase in caspase 3 expression were observed in response to periostracum cicadae treatment. TGF-ß1(Transforming Growth Factor-ß) levels decreased, whereas that of Fas increased in the kidney tissues of the periostracum cicadae-treated groups. The findings of the present study indicate that periostracum cicadae induces apoptosis and improves kidney inflammation and fibrosis in IgA nephropathy rat models.

Water-soluble polysaccharide from Erythronium sibiricum bulb: Structural characterisation and immunomodulating activity.

A water-soluble polysaccharide named ESBP2-1 was isolated from Erythronium sibiricum bulb through anion-exchange and size-exclusion chromatography. ESBP2-1 is a neutral polysaccharide fraction with an average molecular weight of 9.4×105Da and is composed of glucose, galactose and arabinose in a ratio of 24.3:1.1:1. Methylation analysis, partial hydrolysis and NMR studies revealed that the backbone of ESBP2-1 primarily consists of repeating →1)-α-d-Glcp-(4→ units where the disaccharide side chains of Arap-(1→6)-α-d-Galp-(1→ residue are attached to the O-6 position of Glc. An in vitro assay showed that ESBP2-1 significantly promoted the proliferation and neutral red phagocytosis of RAW 264.7 macrophage cells. In addition, ESBP2-1 stimulated the production of secretory molecules (nitric oxide, TNF-α and IL-1ß) of RAW264.7 cells in a dose-dependent manner. These results suggest that ESBP2-1 is a potential immunostimulator.

Microscopic identification and in vitro activity of Agastache rugosa (Fisch. et Mey) from Xinjiang, China.

BACKGROUND: Agastache rugosa is well-known as a common traditional Chinese medicine, which have relieving summer-heat, analgesic and antipyretic effects, have long been used as folkloristic remedy in the treatment of several infectious diseases, anti-inflammatory, and for its antibacterial properties. Considering the lack of available data on the morphology, anatomy and in vitro activity of A. rugosa, the goal of the present study was to carry out the microscopic identification of its aerial parts and in vitro activity research as a contribution to the quality control and reasonable utilization involving A. rugosa. METHODS: The present study was (a) to describe the microscopic identification with usual light and scanning electron microtechniques of A. rugosa, collected from Xinjiang Region; (b) based on previous research on the essential oil constituents among different parts of A. rugosa from Xinjiang by GC-MS method, to evaluate its antibacterial effect and cell viabilitity assay. RESULTS: The microscopic identification of botanical material showed some typical structure. The essential oils from the dried flower (EOF) and leaves (EOL) of A. rugosa were 0.29% and 0.57% (w/w), respectively. The in vitro antibacterial activities showed strong inhibition against S.aureus, E. coli of EOF; strong inhibition against E. coli of EOL. Based GC-MS analysis, the MTT assay showed a dose and time-dependent increase in damage for gastric cancer cell line SGC-7901. CONCLUSIONS: The results of this work, based on an extensive analytical characterization of the EOF and EOL chemical composition, compared with other origins, showed A. rugosa possessed antibacterial and cytotoxicity properties activities, which need much additional work to open up new biomedical application of these components.

Genome-wide analysis suggests divergent evolution of lipid phosphotases/phosphotransferase genes in plants.

Genes of the LPPT (lipid phosphatase/phosphotransferase) family play important roles in lipid phosphorous transfer and triacylglycerol accumulation in plants. To provide overviews of the plant LPPT family and their overall relationships, here we carried out genome-wide identifications and analyses of plant LPPT family members. A total of 643 putative LPPT genes were identified from 48 sequenced plant genomes, among which 205 genes from 14 plants were chosen for further analyses. Plant LPPT genes belonged to three distinctive groups, namely the LPT (lipid phosphotransfease), LPP (lipid phosphatase), and pLPP (plastidic lipid phosphotransfease) groups. Genes of the LPT group could be further partitioned into three groups, two of which were only identified in terrestrial plants. Genes in the LPP and pLPP groups experienced duplications in early stages of plant evolution. Among 17 Zea mays LPPT genes, divergence of temporal-spatial expression patterns was revealed based on microarray data analysis. Peptide sequences of plant LPPT genes harbored different conserved motifs. A test of Branch Model versus One-ratio Model did not support significant selective pressures acting on different groups of LPPT genes, although quite different nonsynonymous evolutionary rates and selective pressures were observed. The complete picture of the plant LPPT family provided here should facilitate further investigations of plant LPPT genes and offer a better understanding of lipid biosynthesis in plants.

Optimised extraction of Erythronium sibiricum bulb polysaccharides and evaluation of their bioactivities.

In this study, the extraction of Erythronium sibiricum bulb polysaccharides (ESBP) through hot water decoction was optimised using response surface methodology (RSM) and a three-level, four-factor Box-Behnken design. The optimum extraction conditions were as follows: extraction time of 4.28h, extraction temperature of 90°C, ratio of liquid to raw material of 37 mL/g and extraction cycle number of three. The experimental yield (37.25%±0.17%) agreed with the predicted value of the RSM model (37.465%). Preliminary ESBP characterisation was conducted through physicochemical analysis. Biological activity test results showed that ESBP exhibited antioxidant activities and excellent anti-inflammatory and analgesic activities, indicating its potential as an anti-inflammatory and analgesic agent.

New triterpenoids from the latex of Euphorbia resinifera Berg.

Nine novel compounds, six euphane triterpenes, Euphorol A-D (1-4), H (8) and I (9), and three tirucallane triterpenes, Euphorol E-G (5-7) including four nortriterpenes, together with seven known compounds (10-16) have been isolated from the methanol extraction of Euphorbium. Their structures were established on the basis of extensive analyses of their HR-ESI-MS, UV, IR, 1D and 2D NMR methods. A putative biogenetic relationship to these compounds was proposed. The cytotoxicity of all these isolates against MCF-7, U937 and C6 cancer cell lines was evaluated. Compounds 1-3, 10, 11 and 13-16 exhibited moderate cytotoxic activities.

Anti-platelet aggregation activities of different fractions in leaves of Apocynum venetum L.

UNLABELLED: Ethnopharmacological relevance Apocynum venetum: is widely used in Uygur and traditional Chinese medicine. Modern pharmaceutical studies have shown that leaves of A. venetum have effects of liver protection, antidepressant and regulation of blood pressure. However, it is unclear that which components have pharmacological activities. AIM OF THE STUDY: The aim was to study chemical constituents of A. venetum and its anti-platelet aggregation activity. MATERIALS AND METHODS: Nephelometery was applied to evaluate anti-platelet aggregation activity of multi-components of A. venetum. Systematic separation components were characterized by HPLC analysis method, and in vitro screening active components by anti-platelet aggregation study. RESULTS: Ethyl acetate fraction (L-III) and L-III-4 have better anti-platelet aggregation activity than other fractions. The results indicated that isoquercitrin, hyperoside and other flavonoids have anti-platelet aggregation activity in A. venetum. CONCLUSION: Our studies provide basis on the endeavors of screening chemicals with that anti-platelet aggregation activity in leaves of A. venetum.

A novel method HPLC-DAD analysis of the Contentsof Moutan Cortexand Paeoniae Radix Alba with similar constituents-monoterpene glycosides in Guizhi Fuling Wan.

A variety of traditional Chinese medical formulations contain two or more herbs from the same genus or family. Although these herbs may have a similar appearance and constituents, they usually have different pharmacodynamic actions. A series of qualitative and quantitative analysis methods are developed to determine one or more compounds for quality control of medicine. As far as we know, no method has been found to determine the real ratio of the two herbs along with the prescription. In this study, we used HPLC-DAD as a way to determine the content of Moutan cortex (M) and Paeoniae radix alba (P) in GuizhiFuling Wan (GZFLW). An effective, accurate and reliable HPLC-DAD method was developed for detecting the content of M and P in GZFLW through the analysis of four monoterpeneglycosides, namely, galloylpaeoniflorin (1), paeoniflorin (2), mudanpioside C (3) and benzoylpaeoniflorin (4). Due to the different UV characteristics of the compounds, the detection wavelength was 270 nm for 1 and 2, while 3 and 4 were monitored at 254 nm and 230 nm, respectively. Four equations were put forward to describe the relationship between content of M as well as P and the four monoterpene glycosides in GZFLW. After validation, all the accuracies of the M and P contents in GZFLW were within 10%. The result showed that the method could be successfully applied to analyze the contents of M and P in GZFLW. Moreover, our method may be more widely used to control the quality of proprietary Chinese medicines, especially for those containing the same genus or family herbs, in industrial GMP production.

Poly[[[[1-ethyl-6,8-difluoro-7-(3-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxyl-ato]cadmium]-µ-benzene-1,4-dicarboxyl-ato] trihydrate].

In the title layered coordination polymer, {[Cd(C(17)H(18)F(2)N(3)O(3))(C(8)H(4)O(4))]·3H(2)O}(n), the Cd(II) atom exhibits a very distorted CdO(6) octa-hedral geometry defined by one O(3),O(4)-bidentate 1-ethyl-6,8-difluoro-7-(3-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxyl-ate (lome) ligand, one O,O'-bidentate benzene-1,4-dicarboxyl-ate (bdc) dianion and two O-monodentate bdc dianions. Both the bdc species in the asymmetric unit are completed by crystallographic inversion symmetry. The bridging bdc dianions link the cadmium nodes into a recta-ngular grid lying parallel to (01). A network of N-H⋯O and O-H⋯O hydrogen bonds helps to establish the packing.

[Effects of jingtian tongmai recipe on atherosclerotic plaque in rabbits].

OBJECTIVE: To evaluate the inhibiting effects of Jingtian Tongmai Recipe (JTTMR) in different dosages on atherosclerotic plaque using the arteriosclerosis rabbit model induced by high cholesterol diet supplemented with immunological injury. METHODS: Fifty-four healthy New Zealand rabbits were randomly divided into six groups: the normal control group, the model group, the Xuezhikang (XZK) treated group and the three JTTMR treated groups treated respectively with low (1.29 g/kg/day), medium (2.57 g/kg/day) and high (5.14 g/kg/day) dosage of JTTMR. Indexes including serum lipids, C-reactive protein (CRP), and area ratio of aortic plaque/intima (PIR), and intima-media thickness ratio (IMT) were examined. RESULTS: Comparison of blood lipids showed that serum levels of total cholesterol (TC), triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) were higher significantly in the model group than in the normal group (P<0.05); TC and LDL-C were lower in the XZK group and the JTTMR groups than in the model group (P<0.05); and these indexes were significantly lower in the medium dose JTTMR group than those in the low and high dose JTTMR groups (P<0.05); while no significant difference of TG between the model group, the JTTMR groups and the XZK group were observed (P>0.05). As for level of high-density lipoprotein cholesterol (HDL-C), that in the XZK group and high dose JTTMR group was higher than that in the other 4 groups (P<0.05). Comparison of CRP showed that it was higher in the model group than in the normal group (P<0.05), while the difference among the other 4 groups was insignificant (P>0.05). No plaque and increase of intima/media thickness was found in the normal group; either PIR or IMT were lesser in the JTTMR groups than those in the model group (P<0.05), and comparison among the three JTTMR groups showed those in the medium dose group was the least (P<0.05). CONCLUSION: JTTMR has arteriosclerosis inhibiting effect, which might be realized through its anti-inflammatory and lipids regulating actions, but the effects are not dose-dependent. The optimal effect is showed by using medium dose of JTTMR, equivalent to the dose used for human adult.

Studies on chemical constituents from EtOAc fraction of Sorbus tianschanica / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Sorbus tianschanica.</p><p><b>METHOD</b>The compounds were isolated and purified by recrystallization and chromatography with silica gel and resin. Their structures were identified by physicochemical properties and spectral analysis.</p><p><b>RESULT</b>Seven compounds were isolated from the EtOH extraction and six structures were identified as benzoic acid (1), benzyl-O-beta-D-glucopyranoside (2), ursolic acid (3), 2alpha-hydroxyursolic acid (4), hyperoside (5), quercetin-3-O-glucoside (6).</p><p><b>CONCLUSION</b>Compounds 1-5 were isolated from S. tianschanica for the first time.</p>

[Synthesis and in vitro antioxidant activity of homo- and heterocyclic diene derivatives of glycyrrhetol].

Chemical modification was performed for improving the antioxidant activity of lead compound glycyrrhetinic acid (Ib). Two conjugated diene derivatives were prepared by reduction and dehydration reactions. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA probe, while evaluating the capacity to inhibit reactive oxygen species (ROS) formation. The initial result showed that the two homo- and heterocyclic diene derivatives--18beta-olean-11,13(18)-diene-3beta, 30-diol (IV) and 18beta-olean-9 (11), 12-diene-3beta, 30-diol (V) exhibited strong antioxidant activities, at a concentration of 1.0 mg x mL(-1), they inhibited free radical (ROS) formation by 45% and 41%, respectively. In the same conditions, the lead compound (Ib) and the reference vitamin E inhibited ROS activity by 31% and 32%. Our results suggest that the elimination of the 11-keto group and the chemical reduction of 30-carboxylic group into hydroxyl function can increase the antioxidant activity of Ib significantly.