- 1. Rutaecarpine effects on expression of hepatic phase-1, phase-2 metabolism and transporter genes as a basis of herb-drug interactions.
ETHNOPHARMACOLOGICAL RELEVANCE:
Rutaecarpine is an alkaloid of Evodia rutaecarpa which is traditionally used to treat human diseases. Rutaecarpine has been used in combination with other drugs in the treatment of disorders and found to produce herb-drug interactions. The basis of these herb-drug interactions is not completely understood.
AIM OF STUDY:
To examine the effects of rutaecarpine on the expression of drug processing genes, including Phase-1 (P450 enzyme genes), Phase-2 (glucuronidation and sulfation genes) and Phase-3 (drug transporters) in liver of mice.
MATERIALS AND METHODS:
Mice were orally administered rutaecarpine at the doses of 10, 20, and 30mg/kg for consecutive 7 days. Twenty-four hours after the last dose, blood and liver were collected. Total RNA was isolated, purified, and subjected to real-time RT-PCR analysis of genes of interest.
RESULTS:
Rutaecarpine administration induced Cyp1a2, 2b10 and 2e1 as previously reported. Cyp3a11 and Cyp4a10 were also induced. For phase-2 enzyme genes, rutaecarpine increased glucuronyltransferases (Ugt1a1 and Ugt1a6), but had no effects on sulfotransferase (Sult1a1 and Sult1b1). Most interestingly, rutaecarpine increased hepatic uptake of organic anion transporting peptides (Oatp1a1, Oayp1a4, Oatp1b2, and Oatp2b1) and induced efflux transporter such as multidrug resistance-associated proteins (Mrp1, Mrp2, Mrp3, and Mrp4), especially at the doses of 20mg/kg and above.
CONCLUSION:
The interactions of rutaecarpine with drugs involve not only the induction of cytochrome P450 enzyme genes, but also the induction of hepatic transporters and phase-2 enzyme genes. The effects of rutaecarpine on these drug processing genes could play integrated roles in producing herb-drug interactions.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Zhu QN, et al. J Ethnopharmacol 2013 May 2;147(1):215-9.
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- 2. Simultaneous determination of three alkaloids, four ginsenosides and limonin in the plasma of normal and headache rats after oral administration of Wu-Zhu-Yu decoction by a novel ultra fast liquid chromatography-tandem mass spectrometry method: applicatio
A novel, sensitive and reliable ultra fast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) method has been developed and validated for simultaneous quantitation of eight main active ingredients (evodiamine, rutaecarpine, dehydroevodiamine, limonin, ginsenoside Rb1 , Rd, Re and Rg1 ) in rat plasma after oral administration of Wu-Zhu-Yu (WZY) decoction, which is a celebrated and widely used Traditional Chinese Medicine formula for the treatment of headache. The analytes and internal standard (IS) were separated on a SHIM-PACK XR-ODS II column, and the detection was performed on a UFLC-MS/MS system with turbo ion spray source. The lower limits of quantification were 1.5, 0.5, 1.0, 2.0, 2.0, 1.0, 0.5 and 0.2 ng ml(-1) for evodiamine, rutaecarpine, dehydroevodiamine, limonin, gensenoside Rb1 , Rd, Re and Rg1 , respectively. Linearity, accuracy, precision and absolute recoveries of the eight analytes were all within satisfaction. The IS-normalized matrix factor was adopted for assessing the matrix effect and accompanied with a satisfactory result. The validated method has been successfully applied to compare pharmacokinetic profiles of the eight active ingredients in rat plasma between normal and headache rats after administration. Exact pharmaceutical effect of WZY decoction on headache was demonstrated by the ethological response of headache rats induced by nitric oxide donor after administration. The results indicated that the absorption of evodiamine, rutaecarpine, gensenoside Rb1 , Re and Rg1 in headache group were significantly higher than those in normal group with similar concentration-time curves while no significant differences existed in limonin and ginsenoside Rd between the two groups. Copyright © 2013 John Wiley & Sons, Ltd....(more)
Xu H, et al. J Mass Spectrom 2013 Apr;48(4):519-32.
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- 3. Pharmacokinetic comparisons of rutaecarpine and evodiamine after oral administration of Wu-Chu-Yu extracts with different purities to rats.
ETHNOPHARMACOLOGICAL RELEVANCE:
Wu-Chu-Yu is a well-known herbal drug used for hypertension. Rutaecarpine and evodiamine are main bioactive components of the medicine.
MATERIALS AND METHODS:
A sensitive and specific HPLC method was developed to analyze rutaecarpine (Rut) and evodiamine (Evo) in rat whole blood. The pharmacokinetics of Rut and Evo after oral administration of Wu-Chu-Yu extracts with different purities to rats was compared to evaluate the effect of purity of Wu-Chu-Yu extracts on the absorption of Rut and Evo. Male Sprague-Dawley rats were given Wu-Chu-Yu extracts with different purities (high, medium and low) approximately the same doses of equivalent to Rut (40 mg/kg) and Evo (31 mg/kg). The contents of Rut and Evo were 45 and 35%, 28 and 21%, 9 and 7% in high, medium and low purity extracts, respectively. At different time points (0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3 and 4h) after administration, the concentrations of Rut and Evo in rat whole blood were determined by HPLC, and main pharmacokinetic parameters were calculated.
RESULTS:
The results indicated that the absorption of Rut and Evo in Wu-Chu-Yu extracts was improved when compared with the pure Rut and Evo and there were significant differences among different groups.
CONCLUSIONS:
The bioavailability of Rut and Evo was increased along with the increasing of purity (16%-80%) in Wu-Chu-Yu extracts.
Copyright © 2011 Elsevier Ireland Ltd. All rights reserved....(more)
Xu S, et al. J Ethnopharmacol 2012 Jan 31;139(2):395-400.
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- 4. Efficient syntheses of 2,3-disubstituted natural quinazolinones via iridium catalysis.
Related Products: Rutaecarpine
- 5. Simultaneous determination and pharmacokinetic analysis of seven alkaloids and two flavonoids from rat plasma by HPLC-DAD after oral administration of Wuzhuyu decoction.
A simple and sensitive high-performance liquid chromatographic method was developed for the simultaneous determination and pharmacokinetic analysis of seven alkaloids dehydroevodiamine (DHED), 10-hydroxyrutaecarpine (HDR), evodiamine (EDM), rutaecarpine (RCP), 1-methyl-2-n-nonyl-4(1H)quinolone (MNQ), evocarpine (ECP), and dihydroevocarpine (DHE), and two flavonoids isorhamnetin-7-O-rutinoside (RIM) and diosmetin-7-O-β-d-glucopyranoside (GRD) in rat plasma after oral administration of Wuzhuyu decoction. The flow rate was kept at 1.0 ml/min and the detection wavelength was set at 300 nm. The calibration curves were linear in the range of 0.5013-30.076 μg/ml for DHED, 0.2161-21.608 μg/ml for RIM, 0.161-12.876 μg/ml for HDR, 0.2146-21.457 μg/ml for GRD, 2.0464-40.928 μg/ml for EDM, 1.0398-31.194 μg/ml for RCP, 0.5970-35.818 μg/ml for MNQ, 0.8371-20.928 μg/ml for ECP, and 0.5167-31.003 μg/ml for DHE. The precision (relative standard deviation (RSD), %) for all was less than 10% and the accuracy (relative error (RE), %) was within ± 10%. The results demonstrated that the assay had remarkable reproducibility with acceptable accuracy and precision. The lower limit of quantifications for the compounds in plasma ranged from 0.12 to 0.23 μg/ml and the lower limit of detections ranged from 0.024 to 0.076 μg/ml. This validated method has been successfully applied in the pharmacokinetics study of seven alkaloids and two flavonoids after orally administrating the Wuzhuyu decoction to rats....(more)
Hu CQ, et al. J Asian Nat Prod Res 2012;14(4):370-81.
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- 6. Mosquito larvicidal activity of alkaloids and limonoids derived from Evodia rutaecarpa unripe fruits against Aedes albopictus (Diptera: Culicidae).
In recent years, uses of environment friendly and biodegradable natural insecticides of plant origin have received renewed attention as agents for vector control. During a screening program for new agrochemicals from Chinese medicinal herbs and local wild plants, the ethanol extract of Evodia rutaecarpa Hook f. et Thomas (Rutaceae) unripe fruits was found to possess larvicidal activity against the mosquitoes. The aim of this research was to determine larvicidal activity of the ethanol extract of E. rutaecarpa unripe fruits and the isolated constituents against the larvae of the Culicidae mosquito Aedes albopictus. The powder, 5 kg of the fruit material, was extracted with 30 l of 95 % ethanol, filtered, and evaporated to dryness in a rotary vacuum evaporator. The crude extract was then partitioned between methanol-water and n-hexane. The n-hexane fraction was evaporated off to given n-hexane extract. The aqueous layer was repartitioned with chloroform to provide chloroform extract after evaporation of the solvent. Further partitioning with ethyl acetate gave a residue after evaporation of the solvent. Bioactivity-directed chromatographic separation of chloroform extract on repeated silica gel columns led to the isolation of three alkaloids (evodiamine, rutaecarpine, and wuchuyuamide I) and two limonoids (evodol and limonin). The structures of the constituent compounds were elucidated based on high-resolution electron impact mass spectrometry and nuclear magnetic resonance. Evodiamine, rutaecarpine, and wuchuyuamide I exhibited strong larvicidal activity against the early fourth instar larvae of A. albopictus with LC(50) values of 12.51, 17.02, and 26.16 μg/ml, respectively. Limonin and evodol also possessed larvicidal activity against the Asian tiger mosquitoes with LC(50) values of 32.43 and 52.22 μg/ml, respectively, while the ethanol extract had a LC(50) value of 43.21 μg/ml. The results indicated that the ethanol extract of E. rutaecarpa and the five isolated constituents have a good potential as a source for natural larvicides....(more)
Liu ZL, et al. Parasitol Res 2012 Sep;111(3):991-6.
Related Products: Rutaecarpine
- 7. Evaluation of the microbial community in industrial rye sourdough upon continuous back-slopping propagation revealed Lactobacillus helveticus as the dominant species.
AIMS:
To assess the structure and stability of a dominant lactic acid bacteria (LAB) population during the propagation of rye sourdough in an industrial semi-fluid production over a period of 7 months.
METHODS AND RESULTS:
The sourdough was started from a 6-year-old freeze-dried sourdough originating from the same bakery. A unique microbial consortium consisting mainly of bacteria belonging to species Lactobacillus helveticus, Lactobacillus panis and Lactobacillus pontis was identified based on culture-dependent (Rep-PCR) and culture-independent [denaturing gradient gel electrophoresis (DGGE)] methods. Three of the isolated Lact. helveticus strains showed remarkable adaptation to the sourdough conditions. They differed from the type strain by the ability to ferment compounds specific to plant material, like salicin, cellobiose and sucrose, but did not ferment lactose.
CONCLUSION:
We showed remarkable stability of a LAB consortium in rye sourdough started from lyophilized sourdough and propagated in a large bakery for 7 months. Lactobacillus helveticus was detected as the dominant species in the consortium and was shown to be metabolically adapted to the sourdough environment.
SIGNIFICANCE AND IMPACT OF THE STUDY:
The use of an established and adapted microbial consortium as a starter is a good alternative to commercial starter strains.
© 2012 The Society for Applied Microbiology....(more)
Viiard E, et al. J Appl Microbiol 2013 Feb;114(2):404-12.
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- 8. Neuroprotective compounds from Salix pseudo-lasiogyne twigs and their anti-amnesic effects on scopolamine-induced memory deficit in mice.
Bioassay-guided fractionation of an 80% methanolic extract of Salix pseudo-lasiogyne twigs has resulted in the isolation of two new compounds (1-2) along with ten known ones (3-12). The new compounds were determined to be 3'-O-acetylsalicin (1) and 2',6'-O-acetylsalicortin (2) by using spectroscopic analyses. Compounds (3-12) were identified as salicin (3), 2'-O-acetylsalicin (4), salicortin (5), 2'-O-acetylsalicortin (6), 3'-O-acetylsalicortin (7), 6'-O-acetylsalicortin (8), 2'-O-(E)-ρ-coumaroylsalicortin (9), grandidentatin (10), isograndidentatin (11), and saligenin (12). Among the isolated compounds, compounds 2, 5, 6, 7, and 8 bearing 1-hydroxy-6-oxo-2-cyclohexenecarboxylate moiety significantly inhibited lipopolysaccharide-induced nitric oxide production in BV2 microglial cells in vitro. Further, we studied anti-amnesic activities of the 80% methanolic extract, the EtOAc fraction, and compound 6 from S. pseudo-lasiogyne. They exerted a significant cognitive-enhancing effect on scopolamine-induced memory deficit in mice. In addition, they also significantly increased the reduced activities of glutathione reductase and superoxide dismutase and the glutathione content in the hippocampus and cortex of scopolamine-induced amnesic mice....(more)
Yang H, et al. Planta Med 2013 Jan;79(1):78-82.
Related Products: Salicin
- 9. Activation of a casB gene encoding β-glucosidase of Pectobacterium carotovorum subsp. carotovorum LY34.
Two cas genes were isolated from Pectobacterium carotovorum subsp. carotovorum LY34 (Pcc LY34). Sequence analysis of the 4873 bp cloned DNA fragment (accession number AY866383) revealed two open reading frames (casF and casB) that are predicted to encode 658 and 467 amino acid proteins, respectively. The CasF protein is similar to other PTS enzyme II components. casB encodes β-glucosidase, a member of the glycosyl hydrolase family 1. An inverted repeat sequence was identified in the casB promoter region, and was hypothesized to have a negative effect on casB transcription. Replacement of the casB promoter of Pcc LY34 with the bglB promoter activated the casB gene, consistent with the repeats inhibiting expression of casB. Purified CasB enzyme was estimated to be 53,000 Da by SDS-PAGE, and hydrolyzed salicin, arbutin, pNPG, and MUG. CasB exhibited maximal activity toward pNPG at pH 7.0 and 40 °C, and Mg(2+) is essential for its activity. Two conserved glutamate residues (Glu(177) and Glu(366)) were shown to be important for CasB activity....(more)
Kim MK, et al. Microbiol Res 2013 Mar 30;168(3):138-46.
Related Products: Salicin
- 10. Biochemical properties of a novel glycoside hydrolase family 1 β-glucosidase (PtBglu1) from Paecilomyces thermophila expressed in Pichia pastoris.
A novel β-glucosidase gene (PtBglu1) from the thermophilic fungus, Paecilomyces thermophila, was cloned and expressed in Pichia pastoris. PtBglu1 contained an open reading frame of 1440-bp nucleotides and encoded a protein of 479 amino acids which showed significant similarity to other fungal β-glucosidases from glycoside hydrolase (GH) family 1. The recombinant β-glucosidase (PtBglu1) was secreted at high level of 190.2 U mL(-1) in high cell density fermentor (5L). PtBglu1 was purified to homogeneity, and was found to be a glycoprotein with molecular mass of 56.7 kDa. The purified PtBglu1 showed optimum catalytic activity at pH 6.0 and 55 °C. The enzyme exhibited broad substrate specificity with highest activity toward pNP-β-D-glucopyranoside, followed by pNP-β-D-galactopyranoside and cellobiose. The K(m) values for pNP-β-D-glucopyranoside, cellobiose, gentiobiose and salicin were 0.55 mM, 1.0 mM, 1.74 mM and 6.85 mM, respectively. These properties make PtBglu1 a potential candidate for various industrial applications....(more)
Yang S, et al. Carbohydr Polym 2013 Jan 30;92(1):784-91.
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- 11. Chryseobacterium frigidisoli sp. nov., a psychrotolerant species of the family Flavobacteriaceae isolated from a glacier forefield of the Larsemann Hills, East Antarctica.
In the scope of diversity studies in glacier forefields on the Larsemann Hills, East Antarctica, a novel psychrotolerant, non-motile Gram-negative, shiny yellow, rod-shaped, aerobic bacterium PB4T was isolated from a soil sample. Strain PB4T produces indole from tryptophan and hydrolyses casein. It grows between 0°C and 25°C with an optimum growth temperature at 20°C. A wide range of substrates are used as sole carbon source and acid is produced from from esculin ferric citrate, D-cellobiose, D-maltose, D-lactose, D-saccharose, D-trehalose, D-melizitose, glycogen, amidon (starch) and gentibiose and weak from D-glucose, amygdalin, salicin and D-turanose. The major menaquinone is MK-6. Identified major fatty acids (>10%) are iso-C15:0 (13.0%) and iso-2OH-C15:0 (51.2%). G+C content is 33.7 mol%. For strain PB4T, highest 16S rRNA gene sequence similarity was found to the type strains of Chryseobacterium humi (97.0%) and Chryseobacterium marinum (96.5%). Considering phenotypic and genotypic characterisation, strain PB4T represents a novel species in the genus Chryseobacterium (Flavobacteriaceae), for which the name Chryseobacterium frigidisoli is proposed. The type strain is PB4T (LMG 27025)....(more)
Bajerski F, et al. Int J Syst Evol Microbiol 2013 Jan 4.
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- 12. Chemical constituents of Caesalpinia decapetala (Roth) Alston.
The current study targets the chemical constituents of Caesalpinia decapetala (Roth) Alston and investigates the bioactivities of the isolated compounds. Fourteen known compounds were isolated using column chromatography, and structural identification was performed by physical and spectral analyses. The biological activities of the compounds were also evaluated by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and 2,2-diphenlyl-1-picrylhydrazyl (DPPH) assays. Emodin (6), baicalein (9), and apigenin (12) displayed antitumor activities against the MGC-803 cell line, while quercetin (2), rutin (5), baicalein (9), and epicatechin (13) showed stronger DPPH scavenging activities compared with ascorbic acid. Andrographolide (1), quercetin (2), bergenin (4), rutin (5), emodin (6), betulin (7), baicalein (9), polydatin (10), salicin (11), and apigenin (12), were obtained from C. decapetala (Roth) Alston for the first time....(more)
Wei XH, et al. Molecules 2013 Jan 22;18(1):1325-36.
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- 13. Predicting in silico which mixtures of the natural products of plants might most effectively kill human leukemia cells?
The aim of the analysis of just 13 natural products of plants was to predict the most likely effective artificial mixtures of 2-3 most effective natural products on leukemia cells from over 364 possible mixtures. The natural product selected included resveratrol, honokiol, chrysin, limonene, cholecalciferol, cerulenin, aloe emodin, and salicin and had over 600 potential protein targets. Target profiling used the Ontomine set of tools for literature searches of potential binding proteins, binding constant predictions, binding site predictions, and pathway network pattern analysis. The analyses indicated that 6 of the 13 natural products predicted binding proteins which were important targets for established cancer treatments. Improvements in effectiveness were predicted for artificial combinations of 2 or 3 natural products. That effect might be attributed to drug synergism rather than increased numbers of binding proteins bound (dose effects). Among natural products, the combinations of aloe emodin with mevinolin and honokiol were predicted to be the most effective combination for AML-related predicted binding proteins. Therefore, plant extracts may in future provide more effective medicines than the single purified natural products of modern medicine, in some cases....(more)
El-Shemy HA, et al. Evid Based Complement Alternat Med 2013;2013:801501.
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- 14. Dynamic Localization of a Transcription Factor in Bacillus subtilis: the LicT Antiterminator Relocalizes in Response to Inducer Availability.
Bacillus subtilis transports β-glucosides such as salicin by a dedicated phosphotransferase system (PTS). The expression of the β-glucoside permease BglP is induced in the presence of the substrate salicin, and this induction requires the binding of the antiterminator protein LicT to a specific RNA target in the 5' region of the bglP mRNA to prevent the formation of a transcription terminator. LicT is composed of an N-terminal RNA-binding domain and two consecutive PTS regulation domains, PRD1 and PRD2. In the absence of salicin, LicT is phosphorylated on PRD1 by BglP and thereby inactivated. In the presence of the inducer, the phosphate group from PRD1 is transferred back to BglP and consequently to the incoming substrate, resulting in the activation of LicT. In this study, we have investigated the intracellular localization of LicT. While the protein was evenly distributed in the cell in the absence of the inducer, we observed a subpolar localization of LicT if salicin was present in the medium. Upon addition or removal of the inducer, LicT rapidly relocalized in the cells. This dynamic relocalization did not depend on the binding of LicT to its RNA target sites, since the localization pattern was not affected by deletion of all LicT binding sites. In contrast, experiments with mutants affected in the PTS components as well as mutations of the LicT phosphorylation sites revealed that phosphorylation of LicT by the PTS components plays a major role in the control of the subcellular localization of this RNA-binding transcription factor....(more)
Rothe FM, et al. J Bacteriol 2013 May;195(10):2146-54.
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- 15. Bartonella bovis isolated from a cow with endocarditis.
A 7-year-old pregnant Angus cow was found dead in the field. At necropsy, the aortic valve was expanded by moderate fibrous connective tissue and acidophilic coagulum containing multifocal marked bacteria, mineral, neutrophils, and red blood cells. Numerous tiny grayish, opaque bacterial colonies were detected on blood agar plates at 7 days after inoculation with a swab of the heart valve of the cow. The bacterium was a Gram-negative, very small coccobacillus that was catalase, oxidase, and urease negative, and did not change litmus milk, triple sugar iron agar, and sulfide-indole-motility medium. The bacterium was negative for esculin hydrolysis, phenylalanine deaminase, nitrate reduction, and gelatin hydrolysis. The isolate did not produce acid from glycerol, inulin, lactose, maltose, mannose, raffinose, salicin, sorbitol, sucrose, trehalose, glycogen, ribose, or starch. Polymerase chain reaction tests for the gltA, ssrA, ftsZ, ribC, rpoB, and 16S ribosomal RNA genes of Bartonella species were positive for the isolate. Amplicons were sequenced, and the gltA, ribC, ssrA, and 16S ribosomal RNA gene sequences were found to have 100% homology to the type strain of Bartonella bovis, whereas the fts and rpoB sequences showed 99.9% and 99.6% homology, respectively, to the type strain of Bartonella bovis. Diagnosticians should be aware of slow-growing microorganisms, and culture media should be incubated beyond the standard period to enhance the recovery of Bartonella species....(more)
Erol E, et al. J Vet Diagn Invest 2013 Mar;25(2):288-90.
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- 16. GH1-family 6-P-β-glucosidases from human microbiome lactic acid bacteria.
In lactic acid bacteria and other bacteria, carbohydrate uptake is mostly governed by phosphoenolpyruvate-dependent phosphotransferase systems (PTSs). PTS-dependent translocation through the cell membrane is coupled with phosphorylation of the incoming sugar. After translocation through the bacterial membrane, the β-glycosidic bond in 6'-P-β-glucoside is cleaved, releasing 6-P-β-glucose and the respective aglycon. This reaction is catalyzed by 6-P-β-glucosidases, which belong to two glycoside hydrolase (GH) families: GH1 and GH4. Here, the high-resolution crystal structures of GH1 6-P-β-glucosidases from Lactobacillus plantarum (LpPbg1) and Streptococcus mutans (SmBgl) and their complexes with ligands are reported. Both enzymes show hydrolytic activity towards 6'-P-β-glucosides. The LpPbg1 structure has been determined in an apo form as well as in a complex with phosphate and a glucose molecule corresponding to the aglycon molecule. The S. mutans homolog contains a sulfate ion in the phosphate-dedicated subcavity. SmBgl was also crystallized in the presence of the reaction product 6-P-β-glucose. For a mutated variant of the S. mutans enzyme (E375Q), the structure of a 6'-P-salicin complex has also been determined. The presence of natural ligands enabled the definition of the structural elements that are responsible for substrate recognition during catalysis....(more)
Michalska K, et al. Acta Crystallogr D Biol Crystallogr 2013 Mar;69(Pt 3):451-63.
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- 17. <sup>13</sup>C Tracer Reveals Phenolic Acids Biosynthesis in Hairy Root Cultures of Salvia miltiorrhiza.
Rosmarinic acid (RA) and lithospermic acid B (LAB) are two typical phenolic acids with significant bioactivities that may contribute to the therapeutic effects of Salvia miltiorrhiza. Precise knowledge of the biosynthetic pathway leading to RA and LAB is a necessary prerequisite to optimize the production of important phenolic compounds in S. miltiorrhiza. In vivo isotopic labeling experiments using [ring-<sup>13</sup>C]-phenylalanine, combined with dynamic measurements of metabolite levels by UPLC/Q-TOF, were used to investigate the metabolic origin of phenolic acids in S. miltiorrhiza. These data indicate the in vivo phenolic biosynthetic pathway: two intermediates from the general phenylpropanoid pathway and the tyrosine-derived pathway, 4-coumaroyl-CoA and 3,4-dihydroxyphenyllactic acid (DHPL), are coupled by the ester-forming enzyme rosmarinic acid synthase (SmRAS) to form 4-coumaroyl-3',4'-dihydroxyphenyllactic acid (4C-DHPL). The 3-hydroxyl group is introduced late in the pathway by a cytochrome P450-dependent monooxygenase (SmCYP98A14) to form RA. Subsequently, RA is transformed to a phenoxyl radical by oxidation, and two phenoxyl radicals unite spontaneously to form LAB. The results indicate aspects of the complexity of phenolic acid biosynthesis in S. miltiorrhiza and expand an understanding of phenylpropanoid-derived metabolic pathways. The candidate genes for the key enzymes that were revealed provide a substantial foundation for follow-up research on improving the production of important phenolic acids through metabolic engineering in the future....(more)
Di P, et al. ACS Chem Biol 2013 May 7.
Related Products: Salvia Root Extract
- 18. Composition of volatile in micropropagated and field grown aromatic plants from Tuscany Islands.
Aromatic plant species present in the natural Park of Tuscany Archipelago are used as flavoring agents and spices, as dietary supplements and in cosmetics and aromatherapy. The plants are usually collected from wild stands, inducing a depletion of the natural habitat. Therefore, micropropagation of these aromatic plants can play a role in the protection of the natural ecosystem, can guarantee a massive sustainable production and can provide standardized plant materials for diverse economical purposes. The aim of this study is to compare the volatile organic compounds produced by the wild plants with those from in vitro plantlets using headspace solid phase micro-extraction (HS-SPME) followed by capillary gas-chromatography coupled to mass spectrometry (GC-MS). Typical plants of this natural area selected for this work were Calamintha nepeta L., Crithmum maritimum L., Lavandula angustifolia L., Myrtus communis L., Rosmarinus officinalis L., Salvia officinalis L. and Satureja hortensis L. Different explants were used: microcuttings with vegetative apical parts, axillary buds and internodes. Sterilization percentage, multiplication rate and shoot length, as well as root formation were measured. The volatile aromatic profiles produced from in vitro plantlets were compared with those of the wild plants, in particular for C. maritimum, R. officinalis, S. officinalis and S. hortensis. This study indicated that the micropropagation technique can represent a valid alternative to produce massive and sterile plant material characterised by the same aromatic flavour as in the wild grown plants....(more)
Pistelli L, et al. Acta Biochim Pol 2013;60(1):43-50.
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- 19. Traditional uses of some medicinal plants in Malatya (Turkey).
ETHNOPHARMACOLOGICAL RELEVANCE:
This study has identified not only the wild plants collected for medical purposes by local people of Malatya Province in the Eastern Anatolia Region, but also the uses and local names of these plants. It tried to provide a source for researchers studying in ethnobotany, pharmacology and chemistry by comparing the information obtained from traditionally used herbs with previous laboratory studies.
AIM OF THE STUDY:
In Turkey, use of plants for medical purposes has been a tradition. This study aims to identify wild plants collected for medical purposes by the local people of Malatya Province, located in the Eastern Anatolia Region of Turkey, and to establish the uses and local names of these plants.
MATERIALS AND METHODS:
A field study had been carried out for a period of approximately 2 years (2010-2011). A questionnaire was administered to the local people, through face-to-face interviews. During this period, 330 vascular plant specimens were collected. Demographic characteristics of participants, names of the local plants, their utilized parts and preparation methods were investigated and recorded. The plant species were collected within the scope of the study; herbarium materials were prepared; and the specimens were entitled. In addition, the relative importance value of the species was determined and informant consensus factor (FIC) was calculated for the medicinal plants included in the study.
RESULTS:
In the area of research, 132 individuals who had knowledge about plants were interviewed. Mean age of the respondents was 44 years (in 35-73 years range). 108 plants were found to be used for medical purposes before in the literature analysis of the plants used in our study, while 15 plants were found to have no literature records. The most common families are: Asteraceae (21 plants), Lamiaceae (14 plants), and Rosaceae (12 plants). Local people were recorded to use the aerial parts, branches, flowers, fruits, latex, leaves, matured fruits, peduncle, resin, rhizomes, root bark, roots, seeds and style of the plants. Besides, it was observed that they dried and stored plants in unfavorable seasons in order to use them later. The medicinal uses of Heracleum antasiaticum Manden., Pimpinella olivieroides Boiss. & Hausskn., Scandix iberica Bieb., Taraxacum hybernum Stev., Tripleurospermum transcaucasicum (Manden.) Pobed., Cerastium chlorifolium Fisch. & Mey., Andrachne telephioides L., Euphorbia denticulata Lam., Astragalus cephalotes Banks. & Sol. var. brevicalyx Eig., Geranium ibericum Cav., Cyclotrichium nivenum (Boiss.) Manden. & Scheng., Salvia syriaca L., Papaver arenarium Bieb., Dactylis glomerata L., Polygonum arenarium Waldst. & Kit. that we found were used in our study area and recorded for the first time. No information could be obtained regarding the names of eight wild plants that are being used in Malatya. In Turkey, local plant names display differences especially due to ethnographic reasons. The plants used in Malatya are known by the same or different local names in various parts of Anatolia. Our research area also includes people with Kurdish and Zaza ethnic origins. The respondents of the questionnaire are Turkish citizens.
CONCLUSION:
These plants are used in the treatment of many diseases. Comparison of the data obtained in this study from derived the plants growing in Malatya with the experimental data obtained in previous laboratory studies proved ethnobotanical usages to a great extent. Literature review indicated that curative plants that grow in Malatya are used in different parts of the world for the treatment of the same or similar diseases. These plants, used for the treatment of many varying diseases, are abundantly found in this region. Drying enabled local people to use medicinal plants in every seasons of the year. The plant flora of Malatya is threatened by such factors as g...(more)
Tetik F, et al. J Ethnopharmacol 2013 Mar 7;146(1):331-46.
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- 20. Application of quality by design to the process development of botanical drug products: a case study.
This paper was designed to assess the value of quality by design (QbD) to improve the manufacturing process understanding of botanical drug products. Ethanol precipitation, a widely used unit operation in the manufacture of botanical drug products was employed to illustrate the use of QbD, taking the process of danshen (the dry root of Salvia miltiorrhiza Bunge) as an example. The recovery of four active pharmaceutical ingredients (APIs) and the removal of saccharides were used to represent the performance of ethanol precipitation. Potentially critical variables, including density of concentrate, ethanol consumption, and settling temperature were identified through risk assessment methods. Design of experiments (DOE) was used to evaluate the effects of the potentially critical factors on the performance of ethanol precipitation. It was observed that higher density of concentrate leads to higher removal of saccharides, but results in lower recovery of APIs. With the rise of ethanol consumption, the recovery of different APIs behaves in different ways. A potential design space of ethanol precipitation operation was established through DOE studies. The results in this work facilitate the enhanced understanding of the relationships between multiple factors (material attributes and process parameters) and the performance of ethanol precipitation. This case study demonstrated that QbD is a powerful tool to develop manufacturing process of botanical drug products....(more)
Zhang L, et al. AAPS PharmSciTech 2013 Mar;14(1):277-86.
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- 21. A novel Danshensu derivative confers cardioprotection via PI3K/Akt and Nrf2 pathways.
BACKGROUND:
Danshensu (3-(3,4-dihydroxyphenyl) lactic acid, DSS) is one of the most promising cardioprotective components in the root of Salvia miltiorrhiza but its poor chemical stability poses hurdles in its therapeutic development. It is therefore desirable to enhance the stability of DSS by chemical modification to improve its activities. In the present study, a novel DSS derivative named ADTM was synthesized and characterized for its cardioprotective properties.
METHODS:
Oxidative stress was induced in H9c2 cardiomyoblast cells by tert-butylhydroperoxide (t-BHP) and the protective effects of ADTM were evaluated. For in vivo study, adult rats were treated with vehicle, DSS, ADTM or amlodipine (n=6-8/group) for 24h before the induction of acute myocardial ischemia. At the end of each experiment, infarct size was measured. Underlying the mechanisms of the cardioprotective effects of ADTM were further investigated in H9c2 cells and rat myocardium by evaluating the effects of Nrf2 (NF-E2-related factor 2) and Akt/PI3K pathways.
RESULTS:
ADTM was approximately 10 times more effective than DSS against t-BHP-induced cell injury in H9c2 cells. In rat myocardial ischemia model, ADTM treatment significantly alleviated myocardial infarction. Akt/PI3K and Nrf2 pathways were demonstrated to be involved in both in vitro and in vivo experiments.
CONCLUSIONS:
These results demonstrated that ADTM displayed much better cardioprotective effects than its parent compounds both in vitro and in vivo. This cardioprotection is mediated, at least in part, through Akt/PI3K and Nrf2 pathways. This novel compound represents a promising candidate for the treatment of cardiovascular diseases (CVDs), particularly myocardial infarction.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Cui G, et al. Int J Cardiol 2013 Jan 3.
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- 22. Modulation of esterified drug metabolism by tanshinones from Salvia miltiorrhiza ("Danshen").
The roots of Salvia miltiorrhiza ("Danshen") are used in traditional Chinese medicine for the treatment of numerous ailments including cardiovascular disease, hypertension, and ischemic stroke. Extracts of S. miltiorrhiza roots in the formulation "Compound Danshen Dripping Pill" are undergoing clinical trials in the United States. To date, the active components of this material have not been conclusively identified. We have determined that S. miltiorrhiza roots contain potent human carboxylesterase (CE) inhibitors, due to the presence of tanshinones. K(i) values in the nM range were determined for inhibition of both the liver and intestinal CEs. As CEs hydrolyze clinically used drugs, the ability of tanshinones and S. miltiorrhiza root extracts to modulate the metabolism of the anticancer prodrug irinotecan (CPT-11) was assessed. Our results indicate that marked inhibition of human CEs occurs following incubation with both pure compounds and crude material and that drug hydrolysis is significantly reduced. Consequently, a reduction in the cytotoxicity of irinotecan is observed following dosing with either purified tanshinones or S. miltiorrhiza root extracts. It is concluded that remedies containing tanshinones should be avoided when individuals are taking esterified agents and that patients should be warned of the potential drug-drug interaction that may occur with this material....(more)
Hatfield MJ, et al. J Nat Prod 2013 Jan 25;76(1):36-44.
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- 23. [Clinical observation of treating 62 patients with severe aplastic anemia failing in immunosuppressive therapy by integrative medicine].
OBJECTIVE:
To explore treatment methods for patients with severe aplastic anemia (SAA) failing in immunosuppressive therapy (IST).
METHODS:
Totally 62 SAA patients failing in IST were treated by integrative medicine (IM). The treatment course was divided into three stages: the critical emergency stage, the improvement stage, and the recovery stage. In the critical emergency stage, patients were treated with Lingyang Yigui Decoction (LYD, consisting of 1.2 g antelope horn, 6 g coptis chinensis, 12 g stir-baked Fructus Gardeniae, 30 g rehmannia rhizoma, 50 g lalang grass rhizome, 9 g amur corktree bark, 12 g Cortex Moutan, 9 g ass-hide gelatin, 30 g red date, 6 g prepared licorice root, etc.) and Erzhi Busui Decoction (EBD, consisting of 120 g glossy privet fruit, 100 g eclipta prostrata, 24 g prepared Gold Theragran, 12 g fructus lycii, 90 g rehmannia rhizoma, 60 g astragalus, 9 g Angelica sinensis, 9 g ass-hide gelatin, 30 g honeysuckle flower, 12 g lotus plumule, and so on) alternatively, one dose daily, decocted twice, taken in two portions. Meanwhile, 50 mg Testosterone Propionate was intramuscularly injected every other day to the improvement stage. Those with fever were treated with LYD by adding 60 g gypsum, 60 g common anemarrhena, 30 g dandelion, 30 g bittersweet herb, 30 g blackend swallowwort root and rhizome, 15 g hemsley rockvine root tuber, and so on. In the improvement stage patients were treated with Jixueteng Compound (Jixueteng Zhengyang Decoction was administered to those of Shen-yang deficiency syndrome: consisting of 100 g spatholobus suberectus, 60 g astragalus, 3 g red ginseng, 12 g psoralea corylifolia, 18 g dodder seed, 12 g angelica, 18 g Herba Epimedii, 6 g common fenugreek seed, 24 g Gold Theragran, 30 g glossy privet fruit, 30 g eclipta prostrata, 6 g dried human placenta, and so on). Meanwhile, 50 mg Testosterone Propionate was intramuscularly injected every other day. Jixueteng Yijing Decoction was administered to those of Shen-yin deficiency syndrome: consisting of 100 g glossy privet fruit, 100 g eclipta prostrata, 90 g rehmannia rhizoma, 30 g spatholobus suberectus, 12 g dodder seed, 6 g psoralea corylifolia, 30 g prepared Gold Theragran, 9 g ass-hide gelatin, 9 g fructus lycii, 24 g Salvia miltiorrhiza, 30 g astragalus, 6 g angelica, and so on), one dose daily, decocted twice, taken in two portions. The treatment lasted to the recovery stage. The medication was gradually reduced to the follow-ups of drug discontinuance. Results After 6 -57 months of treatment, 12 patients (accounting for 19.4%) were basically cured, 14 (22.6%) relieved, 8 (12. 9%) markedly improved, 28 (45.2%) ineffectively, with the total effective rate of 54. 8%. Totally 23 patients had the body temperature ranging 37.6-38.5 degrees C at the first visit to our hospital. They took 2 h- 6 days to have pyretolysis ( <37.5 degrees C) after treatment. Twenty patients with body temperature higher than 38.5 degrees C took 4 h - 5 days to have pyretolysis after treatment. Totally 26 patients suffering from IST induced abnormalities of liver and renal functions (ALT, AST, BUN, and Cr) at the first visit were treated by IM for 2 months. They were restored to the normal levels in 25 cases.
CONCLUSIONS:
The treatment of SAA failing in IST had its specificity. The staging targeted treatment is in line with its pathophysiology. The key points for its treatment might be lie in the improvement and protection of hematopoietic microenvironment of bone marrows. The antisepsis and anti-inflammation of Chinese herbs hindered its aggravating tendency....(more)
Su EY, et al. Zhongguo Zhong Xi Yi Jie He Za Zhi 2012 Dec;32(12):1616-20. Chinese.
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- 24. Involvement of the different extracts from roots of Salvia miltiorrhiza Bunge on acute hypobaric hypoxia-induced cardiovascular effects in rats--preliminary report.
The present study was carried out to investigate the protective effects of roots of Salvia miltiorrhiza Bunge on hypobaric hypoxia. Two extracts of S. miltiorrhiza (extract 1: ethanol : water - 50 : 50; extract 2: 96% ethanol) were used. The experiments were performed after 7 consecutive days of administration of the extracts (200 mg/kg b.w., intragastrically) to male Wistar rats. Next, after placing animals for 60 min in the controlled acute hypobaric hypoxia (500 mm Hg) the systolic arterial blood pressure (SAP) in conscious rats, bioelectric heart activity in unconscious rats and analysis of oxidative stress parameters in the blood of rats: malonyldialdehyde (MDA) and lipid peroxidase (LPO) concentration, activity of superoxide dismutase (SOD) or glutathione peroxidase (GPX) were assayed. It was found out that the extract 1 augmented the lowering of SAP shown in hypoxia affected control rats. On the contrary the extract 2 reversed SAP to values obtained in control animals. Moreover, both extracts led to the normalization of hypoxia-induced tachycardia and levels of MDA, LPO and SOD. It seems that the above-mentioned effects are coupled with different active compounds content in the extracts, however more studies are needed to confirm this hypothesis....(more)
Buchwald W, et al. Pol J Vet Sci 2012;15(4):693-701.
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- 25. [Cloning and bioinformatics analysis of 2-c-methyl-D-erythritol 2,4-cyclodiphosphate synthase gene in Salvia miltiorrhiza].
OBJECTIVE:
To clone and analysis a 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase (SmMCS) full-length eDNA from Salvia miltiorrhiza hairy roots.
METHOD:
A full-length eDNA of SmMCS has been cloned by designing specific primers according to the transcriptome database and using the RACE strategy. ORF Finder was used to find the open reading frame of SmMCS cDNA and ClustalW has been performed to analysis the multiple amino acid sequence alignment. Phylogenetic tree has been constructed using MEGA 5. 1. Real-time quantitative PCR have been applied to detect the transcription level of SmMCS from hairy roots after elicitor Ag+ supplied.
RESULT:
The SmMCS cDNA sequence was obtained. The full length of SmMCS (DNA was 988 bp encoding 234 amino acids. The deduced protein had isoelectric point (pI) of 8.53 and a calculated molecular weight about 24. 6 kDa. Results of real time PCR indicated that elicitor of Ag+ stimulated the increase of mRNA expression of SmMCS in hairy roots, and were increased dramatically at 12 h.
CONCLUSION:
The full-length cDNA of SmMCS was cloned from S. miltiorrhiza hairy root,which can provide a gene target for further studies of tanshinones biosynthesis and terpenoid secondary metabolites....(more)
Gao W, et al. Zhongguo Zhong Yao Za Zhi 2012 Nov;37(22):3365-70. Chinese.
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- 26. [Seedling index of Salvia miltiorrhiza and its simulation model].
Through the correlation analysis on the quantitative traits and their ratios of Salvia miltiorrhiza seedlings and seedling quality, a series of representative indices reflecting the seedling quality of the plant species were determined, and the seedling index suitable to the S. miltiorrhiza seedlings was ascertained by correlation degree analysis. Meanwhile, based on the relationships between the seedling index and the air temperature, solar radiation and air humidity, a simulation model for the seedling index of S. miltiorrhiza was established. The experimental data of different test plots and planting dates were used to validate the model. The results showed that the root diameter, stem diameter, crown dry mass, root dry mass, and plant dry mass had significant positive relationships with the other traits, and could be used as the indicators of the seedling's health. The seedling index of S. miltiorrhiza could be calculated by (stem diameter/root diameter + root dry mass/crown dry mass) x plant dry mass. The stem diameter, root dry mass, crown dry mass and plant dry mass had higher correlations with the seedling index, and thus, the seedling index determined by these indicators could better reflect the seedling's quality. The coefficient of determination (R2) between the predicted and measured values based on 1:1 line was 0.95, and the root mean squared error (RMSE) was 0.15, indicating that the model established in this study could precisely reflect the quantitative relationships between the seedling index of S. miltiorrhiza and the environmental factors....(more)
Huang SH, et al. Ying Yong Sheng Tai Xue Bao 2012 Oct;23(10):2779-85. Chinese.
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- 27. Salvianolic acid B inhibits the amyloid formation of human islet amyloid polypeptideand protects pancreatic beta-cells against cytotoxicity.
The misfolding of human islet amyloid polypeptide (hIAPP) is regarded as one of the causative factors of type 2 diabetes mellitus (T2DM). Salvia miltiorrhiza (Danshen), one of the most commonly used of traditional Chinese medicines, is often used in Compound Recipes for treating diabetes, however with unclear mechanisms. Since salvianolic acid B (SalB) is the most abundant bioactive ingredient of salvia miltiorrhiza water-extract. In this study, we tested whether SalB has any effect on the amyloidogenicity of hIAPP. Our results clearly suggest that SalB can significantly inhibit the formation of hIAPP amyloid and disaggregate hIAPP fibrils. Furthermore, photo-crosslinking based oligomerization studies suggest SalB significantly suppresses the toxic oligomerization of hIAPP monomers. Cytotoxicity protection effects on pancreatic INS-1 cells by SalB were also observed using MTT-based assays, potentially due to the inhibition on the membrane disruption effects and attenuated mitochondria impairment induced by hIAPP. These results provide evidence that SalB may further be studied on the possible pharmacological treatment for T2DM....(more)
Cheng B, et al. Proteins 2013 Apr;81(4):613-21.
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- 28. Cardioprotective effect of salvianolic acid B against arsenic trioxide-induced injury in cardiac H9c2 cells via the PI3K/Akt signal pathway.
The clinical use of arsenic trioxide (ATO), a potent anti-neoplastic agent, is often limited because of its severe cardiotoxicity. Salviae miltiorrhiza is widely used for the treatment of cardiovascular diseases. One of the most abundant ingredients of S. miltiorrhiza is salvianolic acid B (Sal B). The present study was designed to evaluate whether Sal B protects against ATO-induced cardiac cell injury in vitro. With MTT cell viability assay, LDH release, ROS generation, caspase-3 activity assay and Hoechst 33342/PI staining, we found that Sal B pretreatment provided significantly protection against ATO-induced cell death. The effect was correlated with the activation of the PI3K/Akt signal pathway. Conversely, blocking Akt activation with the PI3K inhibitor LY294002 effectively suppressed the protective effect of Sal B against ATO-induced cell apoptosis. In addition, the PI3K inhibitor partially blocked the effects of Sal B on the upregulation of Bcl-2 and Bcl-xl protein expression, and downregulation of Bax protein expression. Collectively, the results showed that Sal B decreased the apoptosis and necrosis of H9c2 cardiomyocytes caused by ATO treatment, and PI3K played a crucial role in enhancing cell survival during this process. These observations indicate that Sal B has the potential to exert cardioprotective effects against ATO toxicity....(more)
Wang M, et al. Toxicol Lett 2013 Feb 4;216(2-3):100-7.
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- 29. Efficacy of salvianolic acid B combined with triamcinolone acetonide in the treatment of oral submucous fibrosis.
OBJECTIVE:
The aim of this study was to investigate the effectiveness of triamcinolone acetonide (TA) and salvianolic acid B (SA-B) intralesional combined injection in the treatment of oral submucous fibrosis (OSF).
MATERIAL AND METHODS:
A randomized clinical trial was performed. TA, SA-B, and TA combined with SA-B were consecutively applied intralesionally weekly for 20 weeks. Mouth opening and burning sensation improvement as determined by a 100-mm visual analog scale were evaluated at weeks 10, 20, and 44.
RESULTS:
Forty-two subjects fulfilled the study without obvious adverse reactions. The net gain in mouth opening was 2.00 ± 1.21 mm in the TA group, 3.48 ± 2.23 mm in the SA-B group, and 5.50 ± 1.80 mm in the TA + SA-B group at week 44. The burning sensation improved by 3.05 ± 0.76 in the TA group, 4.96 ± 0.97 in the SA-B group, and 6.11 ± 0.93 in the TA + SA-B group by the end of the study.
CONCLUSIONS:
TA + SA-B intralesional injections improved mouth open and burning sensation in these OSF patients.
Copyright © 2013 Elsevier Inc. All rights reserved....(more)
Jiang XW, et al. Oral Surg Oral Med Oral Pathol Oral Radiol 2013 Mar;115(3):339-44.
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- 30. Simultaneous determination of six hydrophilic components in rat plasma after oral administration of Jitai tablet by liquid chromatography-electrospray ionization-tandem mass spectrometry: application to a pharmacokinetic study.
A liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method was developed and validated for the simultaneous determination of amygdalin (ADL), danshensu (DSS), ferulic acid (FA), hydroxysafflor yellow A (HSYA), salvianolic acid A (SAA) and salvianolic acid B (SAB) in rat plasma. Plasma samples were pretreated by protein precipitation with acetonitrile. LC separation was performed on a Zorbax Eclipse Plus C18 column (3.0mm×100mm I.D, 1.8μm) with gradient elution using a mobile phase consisting of acetonitrile-0.1% formic acid in water at a flow rate of 0.3mL/min. ESI-MS spectra was acquired in negative ion multiple reaction monitoring mode. The mass transition ion-pair was followed as m/z 456.0→323.1, m/z 197.3→178.8, m/z 193.0→133.9, m/z 611.1→325.2, m/z 493.0→295.0, and m/z 717.0→519.0 for ADL, DSS, FA, HSYA, SAA and SAB, respectively. All analytes showed good linearity over a wide concentration range (r>0.99). The lower limit of quantification was 7ng/mL, 2ng/mL, 4ng/mL, 1ng/mL, 2ng/mL, and 4ng/mL for ADL, DSS, FA, HSYA, SAA and SAB, respectively. The mean recovery of the analytes ranged from 86.29% to 93.16%. The intra- and inter-day precisions were in the range of 1.50-9.98% and the accuracies were between 91.17% and 99.46%. The validated method was successfully applied to a pharmacokinetic study of the six hydrophilic components in rat plasma after oral administration of Jitai tablet....(more)
Wang SP, et al. J Chromatogr B Analyt Technol Biomed Life Sci 2013 Jan 1;912:75-84.
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- 31. SMND-309 promotes angiogenesis in human umbilical vein endothelial cells through activating erythropoietin receptor/STAT3/VEGF pathways.
The aim of the study is to investigate the direct angiogenic activities of SMND-309, a novel metabolite of salvianolic acid B, on human umbilical vein endothelial cells (HUVEC) in vitro and its potential molecular mechanisms. Effects of SMND-309 on proliferation and adhesion of HUVEC were measured using sulforhodamine B assay and cell adhesion assay kit, respectively. Effects of SMND-309 on migration and differentiation of HUVEC were examined through wound-healing assay and tube formation on matrigel method, respectively. Expressions of erythropoietin (EPO), EPO receptor, phosphorylated EPO receptor, signal transducer and activator of transcription 3 (STAT3), phosphorylated STAT3 and vascular endothelial growth factor (VEGF) were detected by Western blot. Knocking down EPO receptor gene and blocking the epidermal growth factor (EGF) receptor/Janus kinase 2 (JAK2) pathways were used to explore the potential mechanisms in SMND-309 induced angiogenesis. SMND-309 strongly induced the proliferation of HUVEC in a concentration-dependent manner within the concentrations of 1-30 μg/ml and significantly promoted the adhesion of HUVEC to different extracellular matrix at 30μg/ml. SMND-309 at doses of 3, 10, 30 μg/ml significantly enhanced the migration, capillary-like structure formation, and the levels of VEGF, phosphorylated EPO receptor and phosphorylated STAT3. Results from further experiments using HUVEC(EPO receptor-) and AG-490 showed that SMND-309 activated EPO receptor first, and then stimulated JAK2/STAT3, which up-regulated the expression of VEGF, and resulted in the angiogenesis. These results clearly show that SMND-309 has powerful angiogenic activity on HUVEC, which is mostly correlated with the up-regulation of VEGF through EPO receptor/STAT3 signal pathways....(more)
Du G, et al. Eur J Pharmacol 2013 Jan 30;700(1-3):173-80.
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- 32. Novel multiple agents loaded PLGA nanoparticles for brain delivery via inner ear administration: in vitro and in vivo evaluation.
The aim of this study was to develop novel multiple agents loaded poly (D,L-lactide-co-glycolide acid) (PLGA) nanoparticles (NPs) and evaluate their potential for brain delivery via inner ear administration. PLGA NPs loaded with salvianolic acid B (Sal B), tanshinone IIA (TS IIA) and panax notoginsenoside (PNS) were prepared by double emulsion/solvent evaporation method. It was observed that optimized NPs displayed satisfactory encapsulation efficiency and desired sustained-release characteristics. NPs following intratympanic administration (IT) in guinea pigs greatly improved drug distribution within the inner ear, cerebrospinal fluid (CSF) and brain tissues compared with intravenous administration (IV). Pharmacodynamic studies demonstrated that NPs following IT markedly inhibited oxidizing reactions and protected the brain from cerebral ischemia reperfusion (I/R) injury by upregulating superoxide dismutase (SOD) activity both in serum and brain tissues, simultaneously significantly reducing the levels of malondialdehyde (MDA) and nitric oxide synthase (NOS). Moreover intratympanic delivery did not cause injury of cochlear function by preliminary study on the toxicity. These findings suggested that PLGA NPs-based delivery system via inner ear administration was a promising candidate to brain delivery for the treatment of brain diseases....(more)
Zhang X, et al. Eur J Pharm Sci 2013 Mar 12;48(4-5):595-603.
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- 33. Near infrared spectroscopy in combination with chemometrics as a process analytical technology (PAT) tool for on-line quantitative monitoring of alcohol precipitation.
The application of near infrared (NIR) spectroscopy for on-line quantitative monitoring of alcohol precipitation of the Danhong injection was investigated. For the NIR measurements, two fiber optic probes designed to transmit NIR radiation through a 2mm path length flow cell were applied to collect spectra in real-time. Particle swarm optimization- (PSO-) based least square support vector machines (LS-SVM) and partial least squares (PLS) models were developed for quantitative analysis of the critical intermediate quality attributes: the soluble solid content (SSC) and concentrations of danshensu (DSS), protocatechuic aldehyde (PA), hydroxysafflor yellow A (HSYA) and salvianolic acid B (SAB). The optimal models were then used for on-line quantitative monitoring of alcohol precipitation. The results showed that the PSO-based LS-SVM with a radial basis function (RBF) kernel was slightly better than the conventional PLS method, even though both methods exhibited satisfactory fitting results and predictive abilities. In this study, successful models were built and applied on-line; these models proffer real-time data and instant feedback about alcohol precipitation....(more)
Jin Y, et al. J Pharm Biomed Anal 2013 Apr 15;77:32-9.
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- 34. Salvianolic acid B protects from pulmonary microcirculation disturbance induced by lipopolysaccharide in rat.
The aim of the present study was to examine the effect and possible mechanism of salvianolic acid B (SalB) on pulmonary microcirculation disturbance induced by lipopolysaccharide (LPS) in rat. Male Sprague-Dawley rats were subjected to thoracotomy under continuous anesthesia and mechanical ventilation. Albumin leakage from pulmonary capillary and the numbers of leukocytes adherent to the pulmonary capillary wall were determined for 60 min by an upright microscope upon LPS (2 mg · kg(-1) · h(-1)) infusion with or without administration of SalB (5 mg · kg(-1) · h(-1)). Pulmonary tissue wet-to-dry weight ratio, tumor necrosis factor α, and interleukin 8 in plasma and bronchoalveolar lavage fluid were measured. In addition, the expressions of E-selectin, intercellular adhesion molecule 1, and myeloperoxidase in pulmonary tissue were assessed by immunohistochemistry. The expressions of aquaporin 1 (AQP-1), AQP-5, metalloproteinase 2 (MMP-2), and MMP-9 were assessed by Western blot assay. Pretreatment with SalB significantly attenuated LPS-induced pulmonary microcirculatory disturbance, including the increase in leukocyte adhesion and albumin leakage. In addition, LPS increased pulmonary tissue wet-to-dry weight ratio and tumor necrosis factor α and interleukin 8 levels in plasma and bronchoalveolar lavage fluid enhanced the expression of E-selectin, intercellular adhesion molecule 1, myeloperoxidase, MMP-2, and MMP-9, whereas it decreased the expression of AQP-1 and AQP-5 in pulmonary tissue, all of which were attenuated by SalB pretreatment. Salvianolic acid B pretreatment improves pulmonary microcirculation disturbance and lung injury on LPS exposure. More studies are required to evaluate the potential of SalB as an option for protecting lung from endotoxemia....(more)
Lin F, et al. Shock 2013 Mar;39(3):317-25.
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- 35. Multivariate data analysis of UV spectra in monitoring elution and determining endpoint of chromatography using polyamide column.
Chromatography using polyamide column is one of the most critical purification operations that affect the safety and efficacy of traditional Chinese medicine (TCM) products. To ensure successful operation and reduce time and solvent consumption, UV spectroscopy combined with multivariate data analysis as an online analytical tool was developed for monitoring the polyamide column chromatography of the TCM Danshen. The process trajectories were established by principal component analysis of the UV spectra and used to determine the endpoint of the washing stage and investigate the impacts of the process conditions. The online analysis method developed determined the concentration of salvianolic acid B (an important compound in Danshen) in the effluent rapidly and precisely with a coefficient of determination of 0.9963 and helped to collect salvianolic acid B quantitatively for determining the endpoint of elution. The methodology proposed is an effective approach applicable in guiding successful operations in the chromatographic separation....(more)
Yan B, et al. J Sep Sci 2013 Apr;36(7):1231-7.
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