- 1. NIR-FT-Raman spectroscopic analytical characterization of the fruits, seeds, and phytotherapeutic oils from rosehips.
In this study nondestructive Raman spectroscopic analysis of rosehips has been conducted by laser excitation at 1064 nm, with the objective of direct measurement of different parts of the fruit, including the inside and outside of the seeds, while preserving the integrity of the more representative chemicals. Carotenoid substances are responsible for the major Raman features in the spectra of the fruit parts; analysis of the nu(1) mode (1520 cm(-1)) strongly indicates the presence of a C(9) carotene, and analysis of the main characteristic carotene band set (C=C, C-C, and C-CH(3) stretching modes at 1520, 1157, and 1007 cm(-1), respectively) suggests the presence of beta-carotene as the main constituent. Raman spectra of the seed parts show the presence of unsaturated fatty acids, which are predominant inside the seed; these spectra also reveal the fatty products content comprises cis isomers. Analysis of the CH-stretching region bands and comparison with those in the spectra obtained from linoleic acid and commercial rosehip oil indicate that the relative band intensity of the CH-stretching mode is strongly affected by the chemical environment of the fatty acid esters present in both parts (inside and outside) of rosehips seeds....(more)
da Silva CE, et al. Anal Bioanal Chem 2008 Dec;392(7-8):1489-96.
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- 2. Multitargeted therapy of cancer by lycopene.
Lycopene (psi,psi-carotene) is the most abundant carotenoid in tomatoes and is the red pigment of not only tomatoes but also rosehips, watermelon, papaya, pink grapefruit, and guava. Unlike beta-carotene, lycopene lacks a beta-ionone ring and therefore has no pro-vitamin A activity. However, the 11 conjugated and two non-conjugated double bonds in lycopene make it highly reactive towards oxygen and free radicals, and this anti-oxidant activity probably contributes to its efficacy as a chemoprevention agent. The reactivity of lycopene also explains why it isomerizes rapidly in blood and tissues from the biosynthetic all-trans form to a mixture of cis-isomers. Prospective and retrospective epidemiological studies indicating an inverse relationship between lycopene intake and prostate cancer risk have been supported by in vitro and in vivo experiments showing that oral lycopene is bioavailable, accumulates in prostate tissue and is localized to the nucleus of prostate epithelial cells. In addition to antioxidant activity, in vitro experiments indicate other mechanisms of chemoprevention by lycopene including induction of apoptosis and antiproliferation in cancer cells, anti-metastatic activity, and the upregulation of the antioxidant response element leading to the synthesis of cytoprotective enzymes. Lycopene is a substrate for carotene-9',10'-monooxygenase (CMO2) and can be converted to apo-10'-carotenal. Although Phase I and II studies have been published that establish the safety of lycopene supplementation, carefully designed and adequately powered clinical studies of lycopene are still needed to confirm its efficacy as a chemoprevention agent....(more)
van Breemen RB, et al. Cancer Lett 2008 Oct 8;269(2):339-51.
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- 3. Effects of food ingredients and oxygen exposure on premature browning in cooked beef.
Premature browning (PMB) in the centre of cooked hamburgers and beef loin (M. longissimus dorsi) steaks was assessed visually and instrumentally. Rosemary extract, ascorbic acid, sodium lactate, polyphosphate or lingonberry juice were added to freshly ground beef with predominant oxymyoglobin, and hamburgers were cooked to 62°C. In general, the tested ingredients did not reduce the extent of PMB in hamburgers, but polyphosphate tended to reduce PMB due to increased pH. Control burgers made of vacuum packaged meat with deoxymyoglobin were cooked to 62, 69 and 75°C, and did not express PMB. Beef loins were injected with a solution of sodium lactate, polyphosphate and sodium chloride. Loin steaks were stored under 75% O(2)/25% CO(2) for 5 days and also cooked to 62°C. Injected steaks had less PMB than non-injected controls, but of a low magnitude unlikely to influence the perception of doneness. The study demonstrated that anaerobic packaging is the most efficient measure to avoid PMB in beef....(more)
Sørheim O, et al. Meat Sci 2013 Jan;93(1):105-10.
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- 4. Phytochemical profile of Rosmarinus officinalis and Salvia officinalis extracts and correlation to their antioxidant and anti-proliferative activity.
The goal of this study was to monitor the anti-proliferative activity of Rosmarinus officinalis and Salvia officinalis extracts against cancer cells and to correlate this activity with their phytochemical profiles using liquid chromatography/diode array detection/electrospray ion trap tandem mass spectrometry (LC/DAD/ESI-MS(n)). For the quantitative estimation of triterpenic acids in the crude extracts an NMR based methodology was used and compared with the HPLC measurements, both applied for the first time, for the case of betulinic acid. Both extracts exerted cytotoxic activity through dose-dependent impairment of viability and mitochondrial activity of rat insulinoma m5F (RINm5F) cells. Decrease of RINm5F viability was mediated by nitric oxide (NO)-induced apoptosis. Importantly, these extracts potentiated NO and TNF-α release from macrophages therefore enhancing their cytocidal action. The rosemary extract developed more pronounced antioxidant, cytotoxic and immunomodifying activities, probably due to the presence of betulinic acid and a higher concentration of carnosic acid in its phytochemical profile....(more)
Kontogianni VG, et al. Food Chem 2013 Jan 1;136(1):120-9.
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- 5. Suppression of LPS-induced inflammatory activities by Rosmarinus officinalis L.
Rosemary (Rosmarinus officinalis L.) has been used in folk medicine to treat headaches, epilepsy, poor circulation, and many other ailments. It was found that rosemary could act as a stimulant and mild analgesic and could reduce inflammation. However, the mechanisms underlying the anti-inflammatory effects of rosemary need more study to be established. Therefore, in this study, the effects of rosemary on the activation of nuclear factor kappa beta (NF-kB) and mitogen-activated protein kinases (MAPKs), the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and the production of nitric oxide (NO), prostaglandin E(2) (PGE(2)), and cytokine in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells were investigated. A methanol extract of rosemary and its hexane fraction reduced NO generation with an IC(50) of 2.75 and 2.83 μg/ml, respectively. Also, the methanol extract and the hexane fraction inhibited LPS-induced MAPKs and NF-kB activation associated with the inhibition of iNOS or COX-2 expression. LPS-induced production of PGE(2) and tumour necrosis factor-alpha (TNF-α) were blocked by rosemary. Rosemary extract and its hexane fraction are important for the prevention of phosphorylation of MAPKs, thereby blocking NF-kB activation, which in turn leads to decreased expression of iNOS and COX-2, thus preventing inflammation....(more)
Yu MH, et al. Food Chem 2013 Jan 15;136(2):1047-54.
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- 6. Effect of green tea or rosemary extract on protein oxidation in Bologna type sausages prepared from oxidatively stressed pork.
Bologna type sausages were prepared from oxidatively stressed pork (UV-irradiation, 48 h, 5 °C) using a traditional recipe (control) or the same recipe but added green tea extract (500 ppm total phenolic compounds) or rosemary extract (400 ppm total phenolic compounds). Green tea and rosemary extracts protected against formation of TBARS and protein carbonyls. On the contrary, increased thiol loss and a distinct loss of myosin heavy chain and actin due to polymerization by reducible bonds as determined by SDS-page were found by addition of green tea extract. The enhanced protein polymerization was ascribed to the reaction between quinone compounds from the plant extracts and protein thiol groups to yield phenol-mediated protein polymerization. Analysis by ESR spectroscopy revealed increased radical intensities in sausages added plant extracts, which was ascribed to originate from protein-bound phenoxyl radicals, which may protect against other oxidatively induced protein modifications....(more)
Jongberg S, et al. Meat Sci 2013 Mar;93(3):538-46.
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- 7. Rosemary (Rosmarinus officinalis L.) Extract Regulates Glucose and Lipid Metabolism by Activating AMPK and PPAR Pathways in HepG2 Cells.
An epidemic of metabolic disorders such as obesity and diabetes is rising dramatically. Using natural products as potential preventive and therapeutic interventions for these disorders has drawn worldwide attention. Rosemary has been shown to lower blood glucose and cholesterol levels and mitigate weight gain in several in vivo studies. However, the mechanisms are essentially unknown. We investigated the effects of rosemary extract on metabolism and demonstrated that rosemary extract significantly increased glucose consumption in HepG2 cells. The phosphorylation of AMP-activated protein kinase (AMPK) and its substrate, acetyl-CoA carboxylase (ACC), was increased by rosemary extract. Rosemary extract also transcriptionally regulated the genes involved in metabolism, including SIRT1, PPARγ coactivator 1α (PGC1α), glucose-6-phosphatase (G6Pase), ACC, and low-density lipoprotein receptor (LDLR). Furthermore, the PPARγ-specific antagonist GW9662 diminished rosemary's effects on glucose consumption. Overall, our study suggested that rosemary potentially increases liver glycolysis and fatty acid oxidation by activating AMPK and PPAR pathways....(more)
Tu Z, et al. J Agric Food Chem 2013 Mar 6.
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- 8. Rosmarinus officinalis Extract Suppresses Propionibacterium acnes-Induced Inflammatory Responses.
Abstract Propionibacterium acnes is a key pathogen involved in the progression of acne inflammation. The development of a new agent possessing antimicrobial and anti-inflammatory activity against P. acnes is therefore of interest. In this study, we investigated the inhibitory effect of rosemary (Rosmarinus officinalis) extract on P. acnes-induced inflammation in vitro and in vivo. The results showed that ethanolic rosemary extract (ERE) significantly suppressed the secretion and mRNA expression of proinflammatory cytokines, including interleukin (IL)-8, IL-1β, and tumor necrosis factor-α in P. acnes-stimulated monocytic THP-1 cells. In an in vivo mouse model, concomitant intradermal injection of ERE attenuated the P. acnes-induced ear swelling and granulomatous inflammation. Since ERE suppressed the P. acnes-induced nuclear factor kappa-B (NF-κB) activation and mRNA expression of Toll-like receptor (TLR) 2, the suppressive effect of ERE might be due, at least partially, to diminished NF-κB activation and TLR2-mediated signaling pathways. Furthermore, three major constituents of ERE, carnosol, carnosic acid, and rosmarinic acid, exerted different immumodulatory activities in vitro. In brief, rosmarinic acid significantly suppressed IL-8 production, while the other two compounds inhibited IL-1β production. Further study is needed to explore the role of bioactive compounds of rosemary in mitigation of P. acnes-induced inflammation....(more)
Tsai TH, et al. J Med Food 2013 Apr;16(4):324-33.
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- 9. Antitumor effect of 5-fluorouracil is enhanced by rosemary extract in both drug sensitive and resistant colon cancer cells.
5-Fluorouracil (5-FU) is the most used chemotherapeutic agent in colorectal cancer. However, resistance to this drug is relatively frequent, and new strategies to overcome it are urgently needed. The aim of this work was to determine the antitumor properties of a supercritical fluid rosemary extract (SFRE), alone and in combination with 5-FU, as a potential adjuvant therapy useful for colon cancer patients. This extract has been recognized as a healthy component by the European Food Safety Authority (EFSA). The effects of SFRE both alone and in combination with 5-FU were evaluated in different human colon cancer cells in terms of cell viability, cytotoxicity, and cell transformation. Additionally, colon cancer cells resistant to 5-FU were used to assay the effects of SFRE on drug resistance. Finally, qRT-PCR was performed to ascertain the mechanism by which SFRE potentiates the effect of 5-FU. Our results show that SFRE displays dose-dependent antitumor activities and exerts a synergistic effect in combination with 5-FU on colon cancer cells. Furthermore, SFRE sensitizes 5-FU-resistant cells to the therapeutic activity of this drug, constituting a beneficial agent against both 5-FU sensitive and resistant tumor cells. Gene expression analysis indicates that the enhancement of the effect of 5-FU by SFRE might be explained by the downregulation of TYMS and TK1, enzymes related to 5-FU resistance....(more)
González-Vallinas M, et al. Pharmacol Res 2013 Jun;72:61-8.
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- 10. Bioavailability of the major bioactive diterpenoids in a rosemary extract: Metabolic profile in the intestine, liver, plasma, and brain of Zucker rats.
SCOPE:
Carnosic acid (CA) and derived diterpenes abundant in rosemary extracts (REs) exert anti-obesity effects. The aim of this study was to investigate the bioavailability of these compounds in a rat model of obesity.
METHODS AND RESULTS:
A total of 26 compounds were tentatively identified based on accurate mass information and the isotopic pattern provided by TOF-MS analyzer. The main metabolites detected in the gut content, liver, and plasma were the glucuronide conjugates of CA, carnosol, and rosmanol. Two other metabolites were also identified: CA 12-methyl ether and 5,6,7,10-tetrahydro-7-hydroxyrosmariquinone. All the metabolites were detected as early as 25 min following oral administration. Most of the compounds remained in the intestine, liver, and (or) plasma at substantial concentrations for several hours supporting their potential health benefits in these tissues. We also corroborated the presence of small quantities of CA and detected trace quantities of the main CA metabolites in the brain. Notably, we did not find significant differences in the metabolic profile between lean and obese rats.
CONCLUSION:
We report for the first time a comprehensive profile of metabolites in various organs following the oral consumption of an RE enriched in CA and contribute to establish the potential bioactive molecules.
© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Romo Vaquero M, et al. Mol Nutr Food Res 2013 Apr 27.
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- 11. Effects of dietary rosemary extract on lamb spoilage under retail display conditions.
A dietary rosemary extract (RE) was tested to extend the shelf life of raw lamb meat. Lambs were supplemented with 0.6mgkg(-1) RE during fattening (from 13 to 25kg live weight). Meat spoilage (total viable counts, psycrophilic bacteria, Enterobacteriaceae, molds and yeasts), TBARS, CIE L*a*b* color and the sensory traits of lamb cuts were analyzed on days 0, 7, 14 or 21 under retail display conditions (70/30 O(2)/CO(2) atmosphere, 2°C temperature and 1600lx lighting). Supplementation of the lamb diet with RE was effective (P<0.05) in prolonging the time chilled-packed lamb cuts could be kept under retail display conditions. Dietary rosemary clearly inhibited lipid oxidation and rancidity, and was moderately efficient in preventing sensory deterioration and microbial spoilage. Although the results concerning meat preservation were limited, the dietary use of rosemary extracts in lambs seems to be promising as a nutritional strategy for improving meat quality....(more)
Bañón S, et al. Meat Sci 2012 Mar;90(3):579-83.
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- 12. Studies of reaction variables for lipase-catalyzed production of alpha-linolenic acid enriched structured lipid and oxidative stability with antioxidants.
Alpha-linolenic acid (ALA) enriched structured lipid (SL) was produced by lipase-catalyzed interesterification from perilla oil (PO) and corn oil (CO). The effects of different reaction conditions (substrate molar ratio [PO/CO 1:1 to 1:3], reaction time [0 to 24 h], and reaction temperature [55 to 65 °C]) were studied. Lipozyme RM IM from Rhizomucor miehei was used as biocatalyst. We obtained 32.39% of ALA in SL obtained under the optimized conditions (molar ratio-1:1 [PO:CO], temperature-60 °C, reaction time-15 h). In SL, the major triacylglycerol (TAG) species (linolenoyl-linolenoyl-linolenoyl glycerol [LnLnLn], linolenoyl-linolenoyl-linoleoyl glycerol [LnLnL]) mainly from PO and linoleoyl-linoleoyl-oleoyl glycerol (LLO), linoleoyl-oleoyl-oleoyl glycerol (LOO), palmitoyl-linoleoyl-oleoyl glycerol (PLO) from CO decreased while linolenoyl-linolenoyl-oleoyl glycerol (LnLnO) (18.41%), trilinolein (LLL) (9.06%), LLO (16.66%), palmitoyl-linoleoyl-linoleoyl glycerol (PLL) (9.69%) were increased compared to that of physical blend. Total tocopherol content (28.01 mg/100 g), saponification value (SV) (192.2), and iodine value (IV) (161.9) were obtained. Furthermore, oxidative stability of the SL was also investigated by addition of 3 different antioxidants (each 200 ppm of rosemary extract [SL-ROS], BHT [SL-BHT], catechin [SL-CAT]) was added into SL and stored in 60 °C oven for 30 d. 2-Thiobabituric acid-reactive substances (TBARS) value was 0.16 mg/kg in SL-CAT and 0.18 mg/kg in SL-ROS as compared with 0.22 mg/kg in control (SL) after oxidation. The lowest peroxide value (POV, 200.9 meq/kg) and longest induction time (29.88 h) was also observed in SL-CAT....(more)
Mitra K, et al. J Food Sci 2012 Jan;77(1):C39-45.
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- 13. Identification of 1,8-Cineole, Borneol, Camphor, and Thujone as Anti-inflammatory Compounds in a Salvia officinalis L. Infusion Using Human Gingival Fibroblasts.
Drinking or gargling Salvia officinalis L. infusion (sage infusion) is thought to soothe a sore throat, tonsillitis, and inflamed, red gums, although structure-based scientific evidence for the key anti-inflammatory compounds in sage infusion is scarce. Human gingival fibroblasts (HGF-1) were treated with sage infusion (SI) or SI fractions containing either its volatile components and water (aqueous distillate, AD) or its dry matter (DM) for six hours. SI, AD, and DM reduced a mean phorbol-12-myristate-13-acetate/ionomycin (PMA/I)-stimulated release of the pro-inflammatory interleukins IL-6 and IL-8 by more than 50% (p < 0.05). Cellular uptake experiments and subsequent GC-MS analysis using stable-isotope-labeled internal standards revealed the presence of 1,8-cineole, borneol, camphor, and α-/β-thujone in SI-treated cells; LC-MS analysis demonstrated the presence of rosmarinic acid. A significant, more than 50% mean inhibition of PMA/I-induced IL-6 and IL-8 release was demonstrated for the volatile compounds 1,8-cineole, borneol, camphor, and thujone, but not for the nonvolatile rosmarinic acid when applied in concentrations representative of sage infusion. Therefore, the volatile compounds were found to be more effective than rosmarinic acid. 1,8-Cineole, borneol, camphor, and α-/β-thujone chiefly contribute to the anti-inflammatory activity of sage infusion in human gingival fibroblasts....(more)
Ehrnhöfer-Ressler MM, et al. J Agric Food Chem 2013 Apr 10;61(14):3451-9.
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- 14. Direct Determination of Rosmarinic Acid in Lamiaceae Herbs Using Diffuse Reflectance Infrared Fourier Transform Spectroscopy (DRIFTS) and Chemometrics.
For the determination of rosmarinic acid (RA) directly in pulverized plant material, a method is developed using diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS) without any physicochemical pretreatment of samples. The RA content of 11 samples of eight different Lamiaceae herbs, as determined by high performance liquid chromatography (HPLC), varied between 86 ± 1 mg/g (in lemon balm) and 12.0 ± 0.8 mg/g (in hyssop) of dried plant material. The 11 samples and 50 other additional samples, which were prepared by mixing initial samples with KBr, were measured using DRIFTS. The second derivative of the spectral region 1344-806 cm(-1) was used and the corresponding data were analyzed using partial least squares (PLS) regression. The correlation between infrared spectral analysis and HPLC measurements shows that the DRIFTS method is sufficiently accurate, simple, and rapid. The RA content of the 11 Lamiaceae samples determined by DRIFTS ranged from 81 ± 4 mg/g (in lemon balm) to 12 ± 3 mg/g (in hyssop) of dried plant material....(more)
Saltas D, et al. J Agric Food Chem 2013 Apr 3;61(13):3235-41.
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- 15. Characterization of phenolics of Sarcandra glabra by non-targeted high-performance liquid chromatography fingerprinting and following targeted electrospray ionisation tandem mass spectrometry/time-of-flight mass spectrometry analyses.
In this study, we successfully characterised the phenolic profiles of Sarcandra glabra (Thunb.) Nakai by high-performance liquid chromatography (HPLC) fingerprinting analyses and mass spectrometry (MS) identification. We first established a specific and valid HPLC approach for fingerprint analysis of S. glabra based on HPLC-UV detection. Using several chemometric methods such as similarity evaluation and principal components analysis, we determined herb-markers peaks from many HPLC peaks. The structures of these herb-markers were further identified targetedly by electrospray ionisation tandem mass spectrometry (ESI-MS/MS)/time-of-flight mass spectrometry (TOF-MS) analyses. As results, four phenolics, including chlorogenic acid, caffeic acid, 4-O-glucopyranosyl rosmarinic acid and rosmarinic acid, were characterised as major herb-markers for the stems of S. glabra, while another three phenolics, including kaempferol-3-O-β-d-glucuronic acid, chlorogenic acid and rosmarinic acid, were characteristic components for the leaves. The compounds may be very useful for further phenolome analysis....(more)
Zhou H, et al. Food Chem 2013 Jun 15;138(4):2390-8.
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- 16. Antioxidant capacity and the correlation with major phenolic compounds, anthocyanin, and tocopherol content in various extracts from the wild edible Boletus edulis mushroom.
Boletus edulis is a wild edible mushroom habitually consumed by rural populations. Ethanolic and methanolic extracts was obtained in cold and hot water from dried fruit bodies. The antioxidant activity of freeze-dried extracts from B. edulis were investigated using free radicals scavenging activity, reducing power, metal chelating effect, inhibition of lipid peroxidation, and the identification of antioxidant compounds. The levels of different compounds with antioxidant properties were higher in alcoholic extracts compared with aqueous extracts. Rosmarinic acid was the major phenolic compound, it being identified in a concentration between 7 ± 0.23 and 56 ± 0.15 mg/100 g extract. A positive correlation between the content of total phenols, flavonoids, anthocyanins, and tocopherols, and the antioxidant capacity of the extracts was determined. The results showed that the ethanolic extract of Romanian wild mushroom B. edulis represents a natural source of functional compounds....(more)
Vamanu E, et al. Biomed Res Int 2013;2013:313905.
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- 17. Rosmarinus officinalis Extract Suppresses Propionibacterium acnes-Induced Inflammatory Responses.
Abstract Propionibacterium acnes is a key pathogen involved in the progression of acne inflammation. The development of a new agent possessing antimicrobial and anti-inflammatory activity against P. acnes is therefore of interest. In this study, we investigated the inhibitory effect of rosemary (Rosmarinus officinalis) extract on P. acnes-induced inflammation in vitro and in vivo. The results showed that ethanolic rosemary extract (ERE) significantly suppressed the secretion and mRNA expression of proinflammatory cytokines, including interleukin (IL)-8, IL-1β, and tumor necrosis factor-α in P. acnes-stimulated monocytic THP-1 cells. In an in vivo mouse model, concomitant intradermal injection of ERE attenuated the P. acnes-induced ear swelling and granulomatous inflammation. Since ERE suppressed the P. acnes-induced nuclear factor kappa-B (NF-κB) activation and mRNA expression of Toll-like receptor (TLR) 2, the suppressive effect of ERE might be due, at least partially, to diminished NF-κB activation and TLR2-mediated signaling pathways. Furthermore, three major constituents of ERE, carnosol, carnosic acid, and rosmarinic acid, exerted different immumodulatory activities in vitro. In brief, rosmarinic acid significantly suppressed IL-8 production, while the other two compounds inhibited IL-1β production. Further study is needed to explore the role of bioactive compounds of rosemary in mitigation of P. acnes-induced inflammation....(more)
Tsai TH, et al. J Med Food 2013 Apr;16(4):324-33.
Related Products: Rosmarinic Acid
- 18. Qualitative and quantitative analysis of the major constituents in Chinese medicinal preparation Dan-Lou tablet by ultra high performance liquid chromatography/diode-array detector/quadrupole time-of-flight tandem mass spectrometry.
A rapid ultra high performance liquid chromatography/diode-array detector/quadrupole time-of-flight tandem mass spectrometry (UPLC-DAD-QTOF) method and a ultra high performance liquid chromatography coupled with diode-array detector (UPLC-DAD) method were developed for qualitative and quantitative analyses of the major chemical constituents in Dan-Lou tablet. Sixty-eight compounds including flavonoids, phenolic acids, tanshinones, protostane triterpenoids, lactones, and paeoniflorins were unambiguously or tentatively identified by comparing their retention times and accurate mass measurement in 40min with references or literature data. Among them, 19 compounds: gallic acid, danshensu, 5-hydroxymethyl-2-furaldehyde, 3'-hydroxy puerarin, puerarin, 3'-methoxy puerarin, mirificin, daidzin, paeoniflorin, calycosin-7-O-β-D-glucoside, naringin, genistin, rosmarinic acid, salvianolic acid B, salvianolic acid A, formononetin, calycosin, cryptotanshinone and tanshinone IIA were further quantified in 30min as marker substances. It was found that the calibration curves for all analytes showed good linearity (R(2)>0.9997) within the test ranges. The overall limits of detection (LODs) and limits of quantification (LOQs) were 0.0073-0.34μg/mL and 0.022-1.04μg/mL, respectively. The relative standard deviations (RSDs) for intra- and inter-day precisions were below 1.90% and 2.85%, respectively. The results of repeatability were less than 2.74%. The sample was stable for at least 48h. The mean recovery rates ranged from 95.5% to 105% with the relative standard deviations (RSDs) less than 2.96%. The results showed that the developed quantitative method was linear, sensitive, and precise for quality control of Dan-Lou tablet....(more)
Dong J, et al. J Pharm Biomed Anal 2013 Jun;80:50-62.
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- 19. PAK1-deficiency/down-regulation reduces brood size, activates HSP16.2 gene and extends lifespan in Caenorhabditis elegans.
There is an increasing evidence that the oncogenic kinase PAK1 is responsible not only for malignant transformation, but also for several other diseases such as inflammatory diseases (asthma and arthritis), infectious diseases including malaria, AIDS, and flu, as well as a series of neuronal diseases/disorders (neurofibromatosis, tuberous sclerosis, Alzheimer's diseases, Huntington's disease, epilepsy, depression, learning deficit, etc.) which often cause premature death. Interestingly, a few natural PAK1-blockers such as curcumin, caffeic acid (CA) and rosmarinic acid (RA) extend the lifespan of the nematode Caenorhabditis elegans or fruit flies. Here, to explore the possibility that C. elegans could provide us with a quick and inexpensive in vivo screening system for a series of more potent but safe (non-toxic) PAK1-blocking therapeutics, we examined the effects of PAK1-deficiency or down-regulation on a few selected functions of this worm, including reproduction, expression of HSP16.2 gene, and lifespan. In short, we found that PAK1 promotes reproduction, whereas it inactivates HSP16.2 gene and shortens lifespan, as do PI-3 kinase (AGE-1), TOR, and insulin-like signalling /ILS (Daf-2) in this worm. These findings not only support the "trade-off" theory on reproduction versus lifespan, but also suggest the possibility that the reduced reproduction (or HSP16.2 gene activation) of this worm could be used as the first indicator of extended lifespan for a quick in vivo screening for PAK1-blockers....(more)
Yanase S, et al. Drug Discov Ther 2013 Feb;7(1):29-35.
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- 20. Enrichment of antioxidant compounds from lemon balm (Melissa officinalis) by pressurized liquid extraction and enzyme-assisted extraction.
In this work enzyme-assisted extraction (EAE) and pressurized liquid extraction (PLE) are applied for extraction of natural compounds from lemon balm (Melissa officinalis). Cellulase, endo-β-1,4 xylanase and pectinase were studied in order to degrade cell wall of lemon balm leaves and to release phenolic compounds. On the other hand, in order to compare the performance obtained with EAE, PLE using water and ethanol was employed maintaining 150°C as extraction temperature. The obtained extracts were characterized in terms of antioxidant capacity by using DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging and trolox equivalent antioxidant capacity (TEAC) in vitro assays, whereas the Folin-Ciocalteu procedure was employed to estimate the total phenols content. On the other hand, extracts were chemically characterized by liquid chromatography tandem mass spectrometry (LC-MS/MS). The results showed that EAE enhanced the total phenolic content and the antioxidant capacity compared to a non-enzymatic control. PLE extracts presented higher amount of phenols and antioxidant capacity than enzyme-assisted extracts, reaching the highest values on water extracts (193.18mggallicacid/gextract and EC50=6.81μg/mL). Among the bioactive phenolic compounds identified in lemon balm, rosmarinic acid was the main component, although other important compounds were also identified, such as caffeic acid derivatives (salvianolic acids, lithospermic acid) and rosmarinic acid derivatives (rosmarinic acid hexoside, sagerinic acid, sulfated rosmarinic acid). The present study confirms that EAE and PLE can be considered alternative methods for the extraction of natural compounds with biological activity from natural sources....(more)
Miron TL, et al. J Chromatogr A 2013 May 3;1288:1-9.
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- 21. Antioxidant activities and phenolics of Passiflora edulis seed recovered from juice production residue.
Passion fruit seed was refluxed in methanolic water and further liquid - liquid extracted yielding n-Hexane, Ethyl acetate (EtOAc) and aqueous (Aq.) extracts. The EtOAc part was the most potent antioxidant (IC 50DPPH = 2.7 ± 0.2 and IC 50ABTS = 9.0 ± 0.0 µg/mL) that significantly (p < 0.05) better than Aq. extract (IC 50DPPH = 177.8 ± 1.3 and IC 50ABTS = 15.4 ± 0.0 µg/mL). The antioxidant EtOAc exhibited ferric reducing powder (EC1mM FeSO4 = 2,813.9 ± 11.6) and tyrosinase inhibitory effect (39.9 ± 0.0 % at 1 mg/mL). The more potent active extract had significant higher total phenolic content than the Aq. one (p < 0.05). Sun protection factor of the EtOAc extract was comparable to ferulic acid. Chlorogenic acid, rosmarinic acid and quercetin were highly found in EtOAc extract, whereas kojic acid and gallic acid were largely determined in the Aq. part. The most potent biologically active fraction was non cytotoxic in vero cells at the highest test concentration (50 µg/mL). A process to minimize the waste from the fruit juice production is offered. Passion fruit value and profitability in agribusinesses will be increased by the biochemical transformation of the seed into active extracts appraisal for natural cosmetic as a multifunction ingredient....(more)
Lourith N, et al. J Oleo Sci 2013;62(4):235-40.
Related Products: Rosmarinic Acid
- 22. Molecular Recognition of Rosmarinic Acid from Salvia?sclareoides Extracts by Acetylcholinesterase: A New Binding Site Detected by NMR Spectroscopy.
Acetylcholinesterase (AChE) inhibition is one of the most currently available therapies for the management of Alzheimer's disease (AD) symptoms. In this context, NMR spectroscopy binding studies were accomplished to explain the inhibition of AChE activity by Salvia sclareoides extracts. HPLC-MS analyses of the acetone, butanol and water extracts eluted with methanol and acidified water showed that rosmarinic acid is present in all the studied samples and is a major constituent of butanol and water extracts. Moreover, luteolin 4'-O-glucoside, luteolin 3',7-di-O-glucoside and luteolin 7-O-(6''-O-acetylglucoside) were identified by MS<sup>2</sup> and MS<sup>3</sup> data acquired during the LC-MS<sup>n</sup> runs. Quantification of rosmarinic acid by HPLC with diode-array detection (DAD) showed that the butanol extract is the richest one in this component (134μg mg<sup>-1</sup> extract). Saturation transfer difference (STD) NMR spectroscopy binding experiments of S. sclareoides crude extracts in the presence of AChE in buffer solution determined rosmarinic acid as the only explicit binder for AChE. Furthermore, the binding epitope and the AChE-bound conformation of rosmarinic acid were further elucidated by STD and transferred NOE effect (trNOESY) experiments. As a control, NMR spectroscopy binding experiments were also carried out with pure rosmarinic acid, thus confirming the specific interaction and inhibition of this compound against AChE. The binding site of AChE for rosmarinic acid was also investigated by STD-based competition binding experiments using Donepezil, a drug currently used to treat AD, as a reference. These competition experiments demonstrated that rosmarinic acid does not compete with Donepezil for the same binding site. A 3D model of the molecular complex has been proposed. Therefore, the combination of the NMR spectroscopy based data with molecular modelling has permitted us to detect a new binding site in AChE, which could be used for future drug development....(more)
Marcelo F, et al. Chemistry 2013 Mar 27.
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- 23. A randomized, double-blind, placebo-controlled study of ten-cha (Rubus suavissimus) on house dust mite allergic rhinitis.
OBJECTIVE:
Self-care with ten-cha is the most common complementary alternative medicine for allergic rhinitis in Japan, but evidence for an actual therapeutic effect is lacking. The purpose of the study was to investigate the effect of ten-cha (Rubus suavissimus) on house dust mite allergic rhinitis.
METHODS:
The study was performed in the otolaryngology departments of 5 facilities (Chiba University, Kagoshima University, Fukui University, Okayama University, and Nippon Medical School) from July to December 2009. A randomized double-blind study was performed with central enrollment and allocation. The subjects ingested 400mg of ten-cha extract or placebo (3 capsules/day) daily for 4 weeks as a food intervention. The number of subjects was chosen with anticipation of an effect equivalent to that of mast cell-stabilizing drugs. A nasal allergy diary-based symptom score and a QOL score were used for evaluation.
RESULTS:
The ten-cha and placebo groups included 47 and 42 subjects, respectively. The improvement rates for sneeze, nasal discharge, nasal obstruction, and symptom scores were greater in the ten-cha group than in the placebo group throughout the intervention period, and the effect tended to increase with time in the ten-cha group. However, the differences between the groups were not significant. QOL was not significantly improved in either group.
CONCLUSION:
Ingestion of ten-cha had an effect on allergic rhinitis, but the effect of Ten-Cha was limited and did not differ significantly from placebo. These results suggest that ten-cha does not exhibit an effect equivalent to mast cell-stabilizing drugs at the dose used in this study.
Crown Copyright © 2010. Published by Elsevier Ireland Ltd. All rights reserved....(more)
Yonekura S, et al. Auris Nasus Larynx 2011 Oct;38(5):600-7.
Related Products: Rubus Suavissimus Extract
- 24. Improvement of obesity phenotype by Chinese sweet leaf tea (Rubus suavissimus) components in high-fat diet-induced obese rats.
Drinking an herbal tea to lose weight is a well-liked concept. This study was designed to examine the possible improvement of obesity phenotype by a new tea represented by its purified components, gallic acid, ellagic acid, and rubusoside (GER). Male obese-prone SD rats were given low-fat diet, high-fat diet, or high-fat diet plus GER at the dose of 0.22 g/kg of body weight for 9 weeks. GER significantly reduced body weight gain by 22% compared to the high-fat diet control group with 48% less abdominal fat gain. Food intake was not affected. Blood glucose was lowered in the GER-treated group, whereas serum triglycerides and cholesterol were significantly reduced by 50%. This improved obesity phenotype may be associated with the attenuated expression of vascular endothelial growth factor in preadipocyte 3T3-L1 cells. Although other underlying, possibly multiple, mechanisms behind the improved phenotype are largely unknown, the observed improvement of multiple obesity-related parameters by the new tea warrants further investigations....(more)
Koh GY, et al. J Agric Food Chem 2011 Jan 12;59(1):98-104.
Related Products: Rubus Suavissimus Extract
- 25. Rubus suavissimus S. Lee extract increases early adipogenesis in 3T3-L1 preadipocytes.
Leaves of Rubus suavissimus S. Lee (Rosaceae) are used to prepare tiencha or sweet tea, which is helpful for body weight control by restricting calorie intake in obese patients. Obesity is a risk factor for metabolic syndrome, and a possible approach to treatment is to promote early adipogenesis in adipose tissue, thereby leading to replacement of enlarged adipocytes that secrete inflammatory factors with small adipocytes.We therefore investigated the effect of extract of tiencha leaves on early adipogenesis by using 3T3-L1 preadipocytes as a model. Tiencha extract significantly and concentration-dependently increased adipogenesis measured in terms of lipid accumulation by means of Oil Red O assay and increased the expression of adiponectin and leptin. In the early phase of adipogenesis, tiencha extract increased the mRNA expression of adipogenic transcription factors CCAAT/enhancer binding protein α (C/EBPα) and proliferator-activated receptor γ (PPARγ). In contrast, mRNA expression of other adipogenic transcription factors, C/EBPδ and C/EBPβ, was unaffected. The mRNA expression levels of adipocyte-specific genes encoding adipocyte protein 2 (aP2), lipoprotein lipase (LPL), and glucose transporter 4 (Glut4), which are regulated by C/EBPα and PPARγ, were also increased. A PPARγ inhibitor, GW9662, partially inhibited the enhancing effect of tiencha extract on lipogenesis. These results suggest that tiencha extract enhances early adipogenesis by increasing the expression of adipogenic transcription factors C/EBPα and PPARγ....(more)
Ezure T, et al. J Nat Med 2011 Apr;65(2):247-53.
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- 26. Purification of a water extract of Chinese sweet tea plant (Rubus suavissimus S. Lee) by alcohol precipitation.
The aqueous extraction process of the leaves of Rubus suavissimus often brings in a large amount of nonactive polysaccharides as part of the constituents. To purify this water extract for potential elevated bioactivity, an alcohol precipitation (AP) consisting of gradient regimens was applied, and its resultants were examined through colorimetric and HPLC analyses. AP was effective in partitioning the aqueous crude extract into a soluble supernatant and an insoluble precipitant, and its effect varied significantly with alcohol regimens. Generally, the higher the alcohol concentration, the purer was the resultant extract. At its maximum, approximately 36% (w/w) of the crude extract, of which 23% was polysaccharides, was precipitated and removed, resulting in a purified extract consisting of over 20% bioactive marker compounds (gallic acid, ellagic acid, rutin, rubusoside, and steviol monoside). The removal of 11% polysaccharides from the crude water extract by using alcohol precipitation was complete at 70% alcohol regimen. Higher alcohol levels resulted in even purer extracts, possibly by removing some compounds of uncertain bioactivity. Alcohol precipitation is an effective way of removing polysaccharides from the water extract of the sweet tea plant and could be used as an initial simple purification tool for many water plant extracts that contain large amounts of polysaccharides....(more)
Koh GY, et al. J Agric Food Chem 2009 Jun 10;57(11):5000-6.
Related Products: Rubus Suavissimus Extract
- 27. Quantitative and fingerprint analyses of Chinese sweet tea plant ( Rubus suavissimus S. Lee).
The quality of botanical food is increasingly assessed by the content of multiple bioactive compounds. This study reports, for the first time, an HPLC fingerprinting method for the quality evaluation of Rubus suavissimus leaves possessing multiple bioactivities. Five constituents, gallic acid, rutin, ellagic acid, rubusoside, and steviol monoside, were quantified and used in developing qualitative chromatographic fingerprints. The limits of detection and quantification ranged from 0.29 to 37.86 mug/mL. The relative standard deviations (RSDs) of intra- and interday precisions were no more than 3.14 and 3.01%, respectively. The average recoveries were between 93.1 and 97.5%. The developed method was validated in the analysis 14 leaf samples with satisfactory results. The contents of the five marker compounds accounted for an average of about 6% w/w with a variability of 16% among the 14 samples collected from a single site and year. Gallic acid was the least, whereas steviol monoside the most, variable compound among the 14 leaf samples. The characteristic compound rubusoside that is responsible for the sweet taste accounted for 5% of leaf weight. The validated method can now be used to quantitatively and qualitatively assess the quality of R. suavissimus leaves as traditional beverage or potential medicines....(more)
Chou G, et al. J Agric Food Chem 2009 Feb 11;57(3):1076-83.
Related Products: Rubus Suavissimus Extract
- 28. [Study on quality control of Rubus suavissimus].
OBJECTIVE:
To control the quality of Rubus suavissimus.
METHODS:
We inspected the character observation, microscopic, physical and chemical identification, TLC, the examination of water and extraction of Rubus suavissimus, then used HPLC to assay the contents of the principal sweet taste component.
RESULTS:
The quality control indexes of Rubus suavissimus were founded.
CONCLUSIONS:
The method is feasible and can control the quality of Rubus suavissimus....(more)
Yin SG, et al. Zhong Yao Cai 2008 Nov;31(11):1734-7. Chinese.
Related Products: Rubus Suavissimus Extract
- 29. [Anti-allergic effects of Rubus suavissimus extract].
OBJECTIVE:
To investigate the effects of Rubus suavissimus S. Lee extract (RSE) on mice, and its influence on release of histamine from rat peritoneal mast cells induced by compound 48/80 in vitro.
METHODS:
To establish murine delayed-type-hypersensitive model induced by 2,4-dinitrofluotobenzene (DNFB) and sheep red blood cell (SRBC); murine type I allergic reaction induced by PCA, and then to observe the anti-allergic effect of RSE. HPLC-ECD methods were performed to detect the contents of histamine released from rat peritoneal mast cells induced by compound 48/80 in vitro.
RESULTS:
Compared with the model group, RSE could ameliorate the ear swelling and capillary permeability in mice induced by DNFB and PCA. RSE also reduced the thickness of the mice hind paw induced by SRBC in significant dose-dependent manner. Meanwhile, RSE obviously inhibited the release of histamine in rat peritoneal mast in vitro, a dose-dependent manner.
CONCLUSION:
RSE exerts potential anti-allergy effects and the mechanisms may be partly related to its inhibitory effect on the release of histamine from mast cells....(more)
Fang YG, et al. Zhong Yao Cai 2008 May;31(5):710-4. Chinese.
Related Products: Rubus Suavissimus Extract
- 30. [Studies on the chemical constituents of Rubus suavissimus S. Lee].
OBJECTIVE:
To study the bioactive constituents from leaves of Rubus suavissimus S. Lee.
METHODS:
Column chromatography with silic gel was employed to isolate and purify the constituents. Their structures were elucidated by means of IR, MS, NMR and chemical methods respectively.
RESULTS:
Two consituents were obtained, which were elucidated as ent-13-hydroxy-kauran-16-en-19-oic acid (I), ent-kaura-16-en-19-oic-13-O-beta-D-glucoside (II), respectively.
CONCLUSION:
Compound II was seperated from Rubus suavissimus S. Lee for the first time....(more)
Wang JX, et al. Zhong Yao Cai 2007 Jul;30(7):800-2. Chinese.
Related Products: Rubus Suavissimus Extract
- 31. Rubusuaviins A-F, monomeric and oligomeric ellagitannins from Chinese sweet tea and their alpha-amylase inhibitory activity.
Six new ellagitannins herein, rubusuaviins A-F, were isolated from the aqueous acetone extract of Chinese sweet tea (Tien-cha, dried leaves of Rubus suavissimus S. LEE) together with seven known tannins. Rubusuaviin A was characterized as 1-O-galloyl-2,3-O-(S)-HHDP-4,6-O-(S)-sanguisorboyl-beta-D-glucopyranose. Rubusuaviins B, C, and E are dimeric, trimeric, and tetrameric ellagitannins, respectively, in which the sanguisorboyl groups were connected ellagitannin units. Rubusuaviins D and F were desgalloyl derivatives of rubusuaviins C and E, respectively. The inhibition of alpha-amylase activity by rubusuaviins and related ellagitannins was compared. Ellagitannins with beta-galloyl groups at the glucose C-1 positions showed stronger inhibition compared with the alpha-galloyl and desgalloyl compounds. The molecular weight of these compounds was not important for the inhibition of alpha-amylase activity....(more)
Li H, et al. Chem Pharm Bull (Tokyo) 2007 Sep;55(9):1325-31.
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- 32. 2-(2-indolyl-)-4(3H)-quinazolines derivates as new inhibitors of AChE: design, synthesis, biological evaluation and molecular modelling.
We recently reported that synthetic derivatives of rutaecarpine alkaloid exhibited high acetyl cholinesterase (AChE) inhibitory activity and high selectivity for AChE over butyrylcholinesterases (BuChE). To explore novel effective drugs for the treatment of Alzheimer's disease (AD), in this paper, further research results were presented. Starting from a structure-based drug design, a series of novel 2-(2-indolyl-)-4(3H)-quinazolines derivates were designed and synthesized as the ring-opened analogues of rutaecarpine alkaloid and subjected to pharmacological evaluation as AChE inhibitors. Among them, derivates 3a-c and 3g-h exhibited strong inhibitory activity for AChE and high selectivity for AChE over BuChE. The structure-activity relationships were discussed and their binding conformation and simultaneous interactions mode were further clarified by kinetic characterization and the molecular docking studies....(more)
Li Z, et al. J Enzyme Inhib Med Chem 2013 Jun;28(3):583-92.
Related Products: Rutaecarpine
- 33. Stimulation of calcitonin gene-related peptide release through targeting capsaicin receptor: a potential strategy for gastric mucosal protection.
Calcitonin gene-related peptide (CGRP) is a predominant neurotransmitter from capsaicin-sensitive sensory nerves, which are widely distributed in the gastrointestinal system. These sensory nerves are reported to be involved in the protection of gastric mucosa against damage by various stimuli, and CGRP is a potential mediator in this process. In addition to increase in gastric mucosal blood flow, the beneficial effects of CGRP on gastric mucosa include inhibition of gastric acid secretion, prevention of cellular apoptosis and oxidative injury. The synthesis and release of CGRP is regulated by the capsaicin receptor which is known as transient receptor potential vanilloid subfamily member 1 (TRPV1) and the agonists of TRPV1 have the potential for gastric mucosal protection. So far, multiple TRPV1 agonists, including capsaicin, capsiate, anandamide and rutaecarpine are reported to exert beneficial effects on gastric mucosal injury induced by various stimuli. Therefore, the TRPV1/CGRP pathway represents a novel target for therapeutic intervention in human gastric mucosal injury....(more)
Luo XJ, et al. Dig Dis Sci 2013 Feb;58(2):320-5.
Related Products: Rutaecarpine
- 34. Simultaneous Determination of Six Bioactive Compounds in Evodiae Fructus by High-Performance Liquid Chromatography with Diode Array Detection.
A simple and reliable high-performance liquid chromatography method with diode array detection (HPLC-DAD) was developed and validated for the simultaneous determination of six bioactive components, rutaevine, limonin, evodiamine, rutaecarpine, N-formyldihydrorutaecarpine and dihydroevocarpine, in the traditional Chinese medicine Evodiae Fructus (Wuzhuyu in Chinese). HPLC separation was conducted on an Agilent Eclipse C18 column (4.6 × 150 mm, 5 µm) at 35°C with a mixture of mobile phase A [tetrahydrofuran-0.02% phosphoric acid (16 : 35)] and mobile phase B (acetonitrile) (gradient elution as follows: 0 min, 22% B; 23 min, 22% B; 24 min, 75% B) at a flow rate of 1 mL/min, and the DAD detection wavelength was set at 220 nm. A linear relationship within the range of investigated concentrations was observed for the six compounds, with correlation coefficients greater than 0.999. The average recovery yields of the six compounds ranged from 98.39 to 104.96%. The HPLC-DAD method was validated by its repeatability [relative standard deviation (RSD) < 2.0%] and intra-day and inter-day precision (RSD < 2.0%). The method was successfully applied to the simultaneous determination of the six previously mentioned components in Evodiae Fructus. It is the first report of a simultaneous qualitative and quantitative analysis for three classes of bioactive components in Wuzhuyu, including the indolequinazoline alkaloids, quinolone alkaloid and limonoids. Based on these results, it is suggested, for possible future revision of the Chinese Pharmacopoeia, that the total contents of evodiamine and rutaecarpine are not less than 0.15% and the total contents of rutaevine and limonin are not less than 0.50%....(more)
Tang X, et al. J Chromatogr Sci 2013 Feb 1.
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- 35. Antidiarrheal properties of different extracts of Chinese herbal medicine formula Bao-Xie-Ning.
OBJECTIVE:
Bao-Xie-Ning (BXN), a traditional Chinese herbal medicine (CHM) formula composed of Fructus Evodiae, Flos Caryophylli and Cortex Cinnamomi, and used for the treatment of infant diarrheal illness, was subject to systematic assessment for its putative multiple pharmacodynamic effects and pharmacological antidiarrheal mechanisms.
METHODS:
High-performance liquid chromatography-diode array detector-electrospray ionization-mass spectrometric/mass spectrometry was developed and validated for identification and quantification of the main constituents in different extracts of BXN. Male Kunming mice weighing 20 to 25 g were used for detecting the antidiarrheal activity of the extracts. Ethanolic extract (EE), volatile oil extract (VOE), and aqueous extract (AE) of BXN were respectively subjected to pharmacodynamic and pharmacological comparison in assessing antidiarrheal effects with senna-induced diarrhea, castor oil-induced diarrhea, acetic acid-induced writhing assay, and isolated duodenum test.
RESULTS:
The highest yields of three detected components of BXN, rutaecarpine, eugenol and cinnamaldehyde were observed in EE. EE showed the most remarkable antidiarrheal activity in dose-dependent and time-dependent manners in both senna- and castor oil-induced diarrhea models, and presented dose-dependent analgesic activity in acetic acid-induced algesthesia model. In addition, EE extract of BXN also exhibited strong antimobility action on the intestine and strongest depression on spontaneous contraction of isolated duodenum.
CONCLUSION:
Ethanol extraction is an efficient method to extract the active constituents of BXN. BXN extract demonstrated multiple pharmacological activities affecting the main mechanisms of diarrhea, which validated BXN's usage in the comprehensive clinical treatment of diarrhea....(more)
Li J, et al. J Integr Med 2013 Mar;11(2):125-34.
Related Products: Rutaecarpine