Aim: To reinvestigate the chemical constituents of the ethanolic extract of Meconopsis quintuplinervia Regel which is a traditional Tibetan medicine used for treatments of hepatitis, tuberculosis etc..; Methods: The compounds were enriched by column chromatography techniques over silica gel, macro porous resin and Sephadex LH-20 absorbents, and finally purified by reverse phase preparative HPLC methods with isocratic mobile phase systems of methanol-H2O-acetic acid (500:500:1) and acetonitrile-H2O-acetic acid (200:800:1). Structural determination of the pure compounds were based on extensive analyses of modern spectroscopic methods including IR, MS, HRMS, 1D- and 2D-NMR spectra.; Results: Three alkaloids were obtained and their structures were elucidated as norsanguinarine (I), O-methylflavinantine (II) and 6-methoxy-17-methyl-2, 3-[methylenebis (oxy)]-morphin-5-en-7-one (III).; Conclusion: Norsanguinarine (I) was isolated from genus Meconopsis for the first time, and 6-methoxy-17-methyl-2,3-[methylenebis(oxy)]-morphin-5-en-7-one (III) is a new alkaloid named as meconoquintupline.;
Background: Swertia chirayita, has been commonly used under the name "Zang-yin-chen" for the treatment of liver infections, inflammation, abdominal pain, and bacterial infection in traditional Tibetan medicine. However, the bioactive components with anti-inflammatory activities and underlying mechanisms remain poorly evaluated.Study Design/methods: Repeated column chromatography yielded two main xanthones from petroleum ether (PE) and ethyl acetate fractions of whole plants of S. chirayita, and their structures were determined as bellidifolin (1) and swerchirin (2) on the basis of spectroscopic data and literature analysis. The anti-inflammatory activities and mechanisms of anti-inflammation of these two isolated xanthones were determined via enzyme-linked immunosorbent assay (ELISA) and western blot in lipopolysaccharide (LPS)-stimulated RAW 264.7 murine macrophages in vitro.Results: Anti-inflammation assay demonstrated that 1 and 2 inhibit the production of the pro-inflammatory cytokines interleukin-6 (IL-6) and TNF-α in LPS-stimulated RAW 264.7 macrophages. Xanthone 1 also potently inhibited the production of prostaglandin E2 (PGE2) by suppressing the protein expression of cyclooxygenase-2 (COX-2) in LPS-stimulated RAW 264.7 macrophages. Western blot showed that the phosphorylation of c-Jun N-terminal kinases (JNK), extracellular signal-regulated kinase (ERK), and p38 MAPKs were remarkably attenuated by 1 in a concentration-dependent manner. Particularly, Compound 1 suppressed the phosphorylation of the inhibitor κB kinase-β (IKK-β), Akt, and p65 subunit of nuclear factor-kappaB (NF-κB).Conclusion: The potent suppressive effects of 1 from S. chirayita on inflammatory mediators by blocking the expression of COX-2 and phosphorylation of Akt, IKK-β, MAPK and NF-κB, activation in LPS-stimulated macrophages suggest that 1 can be a preventive therapeutic candidate for the management of inflammatory-mediated immune disorders.
The current study evaluated antioxidant activity of <i>Dracocephalum rupestre</i> Hance, characterized by the polyphenolic compounds in the ethyl acetate fraction (EAF) from <i>D. rupestre</i> and investigated the protective mechanisms of EAF in carbon tetrachloride (CCl₄)-induced hepatic injury. EAF showed the largest antioxidant capacity as demonstrated by DPPH, ABTS, OH, and FRAP assays (<i>p</i> ≤ .05). Using LC-MS, two polyphenolics, for example, rosmarinic acid, and eriodictyol were identified in EAF. Total phenol content of <i>D. rupestre</i> was correlated significantly with FRAP value (<i>r</i> = .999, <i>p</i> ≤ .001). The results also showed that EAF decreased serum ALT and AST activities compared with model group, as well as the histological findings. In addition, EAF remarkably decreased MDA and LDH levels in liver. This is the first time to reveal the hepatoprotective effect of EAF from <i>D. rupestre</i>, which may be developed as a new drug for treatment of liver injury in future.<br>Practical applications: <i>Dracocephalum rupestre</i> Hance is known as Chinese herbal medicine with pharmacological functions of antioxidant, anti-inflammatory and has been mainly used in the treatment of damp-heat, headache, fever, jaundice, hepatitis, liver toxicity, and other diseases. In order to detect the potential application of this plant, the antioxidant and hepatoprotective activities of <i>D. rupestre</i> were investigated. It was found that the ethyl acetate fraction (EAF) from <i>D. rupestre</i> displayed strong antioxidant activity. We also demonstrate that EAF could lessen CCl₄-induced acute liver injury in mice. Also, rosmarinic acid may play an important role in the antioxidant activity and hepatoprotective effect for EAF.
<br>Display Omitted<br> Two new phenolic acids (<b>1</b>⿿<b>2</b>) were isolated from the aerial parts of <b>Asterothamnus centrali-asiaticus</b>. Five knownphenolic acids (<b>3</b>⿿<b>7</b>) were also obtained from the title plant. <b>1</b>⿿<b>7</b> were evaluated for their anti-oxidant activity. <b>1</b>⿿<b>7</b> showed anti-oxidant activity with IC50 values ranging from 7.65 to 22.44 μg/mL.<br>Two new phenolic acids 2-hydroxy-5-[(6⿲-<b>O</b>-(<b>E</b>)-caffeoyl)-β-d-glucopyranosyl]-oxybenzoic acid (<b>1</b>) and 2-hydroxy-5-[(3⿲-<b>O</b>-(<b>E</b>)-caffeoyl)-β-d-glucopyranosyl]-oxybenzoic acid (<b>2</b>) were isolated from the aerial parts of <b>Asterothamnus centrali-asiaticus</b>, together with five known ones (<b>3</b>-<b>7</b>). Their structures were elucidated by extensive 1D and 2D NMR studies and HRESIMS investigations. The anti-oxidant activity of the isolates was evaluated through ABTS radical cation decolorization assay. The results showed that all of them exhibited anti-oxidant activity, and compound <b>7</b> was the most active compound with an IC50 value of 7.65 μg/mL.
The young leaves and shoots of Sibiraea laevigata, known as "Liucha", are used as tea by Tibetans to improve digestion after meals. Long-term consumption of "Liucha" will cause weight loss. In present work, we reported on the isolation and NMR and chemical analysis-based elucidation of seven new sorbitol O-caffeic acid ester derivatives named sorbitol esters A-G (1-7) and eighteen known phenolic compounds from S. laevigata. All of the isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Among them sorbitol ester A (1), sorbitol ester D (4), sorbitol ester F (6), sorbitol ester G (7), isoferulic acid (15), methyl caffeate (18), trans-p-hydroxycinnamic acid (19), and kaempferol 3-O-β-d-(6″-E-p-coumaroyl)-glucopyranoside (25) showed more potent α-glucosidase inhibitory activity than the clinical drug acarbose.
Seven phenolic compounds, <b>1</b> - <b>7</b>, including a new organic acid gallate, mucic acid 1-ethyl 6-methyl ester 2-<i>O</i>-gallate (<b>7</b>), were isolated from the MeOH extract of the fruits of <i>Phyllanthus emblica</i> L. (Euphorbiaceae). The structures were elucidated on the basis of extensive spectroscopic analysis and comparison with literature data. Upon evaluated for their antioxidant abilities by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. The inhibitory activities against melanogenesis in B16 melanoma cells induced by <i>α</i>-MSH, as well as cytotoxic activities against four human cancer cell lines were also evaluated. All phenolic compounds, <b>1</b> - <b>7</b>, exhibited potent antioxidant abilities (DPPH:<i> IC</i><sub>50</sub> 5.6 - 12.9 μm; ABTS: 0.87 - 8.43 μm <i>Trolox</i>/μm; FRAP: 1.01 - 5.79 μm Fe<sup>2+</sup>/μm, respectively). Besides, <b>5</b> - <b>7</b>, also exhibited moderate inhibitory activities against melanogenesis (80.7 - 86.8% melanin content), even with no or low toxicity to the cells (93.5 - 101.6% cell viability) at a high concentration of 100 μm. Compounds <b>1</b> - <b>3</b> exhibited cytotoxic activity against one or more cell lines (<i>IC</i><sub>50</sub> 13.9 - 68.4%), and compound <b>1</b> with high tumor selectivity for A549 (<i>SI</i> 3.2).
Five days of integrative body-mind training (IBMT) improves attention and self-regulation in comparison with the same amount of relaxation training. This paper explores the underlying mechanisms of this finding. We measured the physiological and brain changes at rest before, during, and after 5 days of IBMT and relaxation training. During and after training, the IBMT group showed significantly better physiological reactions in heart rate, respiratory amplitude and rate, and skin conductance response (SCR) than the relaxation control. Differences in heart rate variability (HRV) and EEG power suggested greater involvement of the autonomic nervous system (ANS) in the IBMT group during and after training. Imaging data demonstrated stronger subgenual and adjacent ventral anterior cingulate cortex (ACC) activity in the IBMT group. Frontal midline ACC theta was correlated with highfrequency HRV, suggesting control by the ACC over parasympathetic activity. These results indicate that after 5 days of training, the IBMT group shows better regulation of the ANS by a ventral midfrontal brain system than does the relaxation group. This changed state probably reflects training in the coordination of body and mind given in the IBMT but not in the control group. These results could be useful in the design of further specific interventions.
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The first phytochemical investigation on the roots of <b>Ligularia purdomii</b> led to the isolation and identification of 18 compounds, including two eremophilane sesquiterpenoids (<b>1</b> and <b>2</b>), three benzofuran derivatives (<b>3</b>-<b>5</b>), a triterpenoid (<b>6</b>), two steroids (<b>7</b> and <b>8</b>), nine phenolic components (<b>9</b>-<b>17</b>), and a monofatty glyceride (<b>18</b>). The structural elucidation of the isolated compounds was performed by spectroscopic data and comparison with the literature. Compounds (−)-syringaresinol (<b>11</b>), scopoletin (<b>13</b>), 3,5-dimethoxy-4-hydroxy-benzaldehyde (<b>14</b>), and glycerol monolinoleate (<b>18</b>) have not been recorded in <b>Ligularia</b> genus previously. The chemotaxonomic significance of these isolated compounds has been summarized.<br>• First phytochemical investigation on <b>L. purdomii.</b> • 18 compounds were identified from the acetone extract of <b>L. purdomii.</b> • Four compounds were reported from the genus <b>Ligularia</b> for the first time. • The results had important significance for chemotaxonomy of <b>L. purdomii.</b>
The present work is to study the chemical constituents from petroleum ether fraction of Tibetan medicine Swertia chirayita by column chromatography and recrystallization. The structures were identified by physical and chemical properties and spectral data as swerchirin (1), decussatin (2), 1,8-dihydroxy-3,5,7-trimethoxyxanthone (3), 1-hydroxy-3,5,7,8-tetramethoxyxanthone (4), bellidifolin (5), 1-hydroxy-3, 7-dimethoxyxanthone (6), methylswertianin (7), 1-hydroxy-3,5-dimethoxyxanthone (8), erythrodiol (9), oleanolic acid (10), gnetiolactone (11), scopoletin (12), sinapaldehyde (13), syringaldehyde (14), and β-sitosterol (15). Compounds 3, 4, 9, 11-14 were isolated from S. chirayita for the first time. Compounds 9 and 12 were firstly isolated from the genus Swertia. The cytotoxic activities of compounds 1, 2, 5, 7 and 8 against human pancreatic cancer cell lines SW1990 and BxPC-3,and the protective effects of these compounds against hydrogen peroxide (H2O2)-induced oxidative stress in human endothelium-derived EA.hy926 were investigated in vitro. The results showed no obvious effect at the high concentration of 50 μmol•L⁻¹.
In this article the classics textual research to the origin of "Zha-xun" was carried out, the ethnobotanical research methods, the origin of visits, key informant interviews, sample collection and textual research were applied in the research. The results showed that the hypothesis of Zha-xun"s origin mainly included "source of mine", "source of feces", "source of monkey menstrual blood" in China. There were "source of fossil", "source of the plant secretion" abroad. The authors had interviewed the villagers at origin, herbalists, Tibetan doctors, herb dealers, foreign scholars for a total of 18 people, and collecting 45 batches medicinal materials. According to ancient Tibetan classics textual and Tibetan medicine doctors' views, medicinal materials were divided into the genuine and the substitutes. The genuine was identified as ancient so-called "iron" type "Zha-xun", and the substitute was fecal pellet bonding briquette. According to the field survey and literature research, "source of fossil" more in line with substance of Zha-xun was derived from the rock. As the results, the author believed that Zha-xun was the mixture of organic fossils from the rock seepage with flying squirrel, pika feces. So it is needed to be set up Zha-xun classification standard to evaluate the quality of medicinal materials. Meanwhile, it was necessary to further clarify fecal pellet substitute rationality. Above all, this article clarified the status of the use of Tibetan medicine-"Zha-xun", and laid the foundation of species systematics and quality standards research of "Zha-xun".
The comparative study of bloodletting therapy between traditional Chinese medicine and Tibetan medicine in view of history development, theoretic basis, bloodletting location, bloodletting tool, operation method, bloodletting amount, indications, contraindications and the others are conducted in this paper. It is pointed out that the bloodletting therapy could be better carried forward and developed through the interaction and integration of bloodletting therapy between traditional Chinese medicine and Tibetan medicine in term of the theoretic, practical and development patterns under the guidance of these two different medical theoretical systems.
The study aims at providing a new suitable way to promote artificial cultivation, solving the problem of resources increasingly endangered wild medicine, and protecting the wild resources of Tibetan medicine. The content of quercetin,kaempferol and isorhamnetin was determined by HPLC. The correlation between flavonoids components and ecological factors was analyzed using partial least-squares regression (PLSR). Based on Maxent model combining using ArcGIS software, suitable regionalization for H.rhamnoides subsp. sinensis was studied.The results showed that the difference of quercetin,kaempferol and isorhamnetin content in samples from different regions were obvious. The main factors effecting quercetin content accumulation were the altitude andthe average monthly precipitation in January and August. The main factors effecting kaempferol accumulation were the altitude andthe average monthly precipitation in the coldest quarter and December. The main factors effecting isorhamnetin accumulation were the average monthly precipitation in August, January and the coldest quarter.The regional distribution suitability index for H.rhamnoides subsp. sinensis was 0-0.708. The suitable area 590 500 km², accounting for 6.13% of the total area. The preferably suitable area was 552 500 km², accounting for 5.73% of the total area.The methods used in the study is simple and feasible, the result is reliable which provide a new approach for Tibetan medicine resources sustainable exploitation and utilization.
Molecular targeted cancer therapy is a promising strategy to overcome the lack of specificity of anticancer drug. While the binding of c(RGDfK) (cyclic Arginine-Glycine-Aspartic acid-Phenylalanine-Lysine) to αvβ3 over-expressed on tumor cell has been validated, the underlying interaction remains poorly understood. In this work, docking calculation was applied to investigate the interactions between c(RGDfK)/c(RGDfK)-PEG and αvβ3. The calculated results indicated that c(RGDfK) interacted with αvβ3 mainly by electrostatic interaction, stabilization interaction, and hydrophobic interaction. Conjugation of PEG chain to the c(RGDfK) weakened the binding affinity of c(RGDfK) to αvβ3. Accordingly, docetaxel(DTX)-loaded target micelles (c(RGDfK)-PEG-PLA/PEG-PLA/DTX) were designed, characterized and evaluated using HeLa cells. In vitro release studies demonstrated both target and non-target micelles displayed almost the same profiles, which best fit in Ritger-Peppas model. Cellular uptake and MTT studies revealed that the target micelles with the presence of c(RGDfK) were more efficiently taken up by HeLa cells and significantly improved the cytotoxicity compared to that of non-target micelles. Cell inhibition rate of target micelles was improved by 20% after 24h. Our findings suggest that target micelles may be a potential anticancer drug delivery system in the treatment of integrin αvβ3 over-expressed on tumor cell.
In an effort to discover potent VEGFR-2 inhibitors, a series of 2,4 or 4,6-disubstituted <b>O</b>-linked indoles derivatives were designed and synthesized. The structural activity relationships led to identification of a potential VEGFR-2 inhibitor compound <b>18</b>.<br>Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of a series of <b>O</b>-linked indoles as potent inhibitors of VEGFR-2. Among these compounds, <b>18</b> showed significant anti-angiogenesis activities <b>via</b> VEGFR-2 in enzymatic proliferation assays, with IC50 value of 3.8 nmol/L. Kinase selectivity profiling revealed that <b>18</b> was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-<b>α</b> and <b>β</b>.
DNA barcoding, the identification of species using one or a few short standardized DNA sequences, is an important complement to traditional taxonomy. However, there are particular challenges for barcoding plants, especially for species with complex evolutionary histories. We herein evaluated the utility of five candidate sequences - rbcL, matK, trnH-psbA, trnL-F and the internal transcribed spacer (ITS) - for barcoding Rhodiola species, a group of high-altitude plants frequently used as adaptogens, hemostatics and tonics in traditional Tibetan medicine. Rhodiola was suggested to have diversified rapidly recently. The genus is thus a good model for testing DNA barcoding strategies for recently diversified medicinal plants. This study analyzed 189 accessions, representing 47 of the 55 recognized Rhodiola species in the Flora of China treatment. Based on intraspecific and interspecific divergence and degree of monophyly statistics, ITS was the best single-locus barcode, resolving 66% of the Rhodiola species. The core combination rbcL+matK resolved only 40.4% of them. Unsurprisingly, the combined use of all five loci provided the highest discrimination power, resolving 80.9% of the species. However, this is weaker than the discrimination power generally reported in barcoding studies of other plant taxa. The observed complications may be due to the recent diversification, incomplete lineage sorting and reticulate evolution of the genus. These processes are common features of numerous plant groups in the high-altitude regions of the Qinghai-Tibetan Plateau.
The characteristic fingerprint of conventional dairy Nanhanshuishi was established by X-ray diffraction (XRD), based on similarity of caculation on public peaks by MATLAB software, and the feasibility of new dairy technology of microwave method was explored between XRD and the dissolution rate in artificial simulation gastric juices. The result showed that similarity of shared peak in XRD of conventional dairy Nanhanshuishi was > 95%, This XRD characteristic fingerprint of conventional dairy Nanhanshuishi had strong specificity, could be used to provide a reference for identification and quality evaluation. This study also showed that the similarity of microware dairy products and conventional dairy products was good, and the sample of microwave 15 min was the best, and new dairy method by the microwave could replace the traditional method.
<i>Rheum tanguticum</i> is a widely used Chinese medicinal plant. Recently, because of the great demand, the wild populations have been declining rapidly. In this study, the levels of genetic variation of 11 wild and five cultivated populations of <i>R. tanguticum</i> were investigated by ISSR markers. The 13 selected ISSR primers amplified 306 polymorphic bands out of a total of 326 (93.87 %). Based on Nei’s gene diversity and Shannon’s index, the genetic diversity in cultivated populations of <i>R. tanguticum</i> (<i>H</i> = 0.2490; <i>I</i> = 0.3812; <i>H</i> <sub>B</sub> = 0.3033) was relatively lower than that of wild populations (<i>H</i> = 0.2666; <i>I</i> = 0.4124; <i>H</i> <sub>B</sub> = 0.3115), although no significant differences were identified. Assignment was performed with AFLPOP program, and XGM was the most likely source population of HM. The origins of the rest cultivated populations were admixture. UPGMA and PCoA analyses showed that wild and cultivated populations were not separated into two groups, indicating that a large number of wild genotypes were maintained in the cultivated gene pool. The coefficient of genetic differentiation between wild and cultivated populations was 0.0305 (<i>G</i> <sub>st</sub>), which was in good agreement with the results of analysis of molecular variance (AMOVA), in which, only 1.85 % of the total variance existed between groups of wild and cultivated populations, while 70.91 % occurred within populations and 27.24 % among populations. Together, these results indicated that cultivated populations were not genetically differentiated from wild populations. On the basis of this study, we have made some suggestions for the conservation and efficient management of the genetic resources of this important medicinal herb.
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Ethnopharmacological relevance: Saussurea laniceps Hand.-Mazz. (SL) has long been used under the herbal name Tibetan 'Snow Lotus' for the treatment of rheumatoid arthritis, stomachache and dysmenorrhea in Tibetan folk medicine. Since herbal medicine (HM) is a synergistical system with multiple components, both of the metabolism and pharmacokinetic studies of HM are interdependent. This study aimed to develop an integrated strategy based on the UPLC-DAD-QTOF-MS technique for metabolism and pharmacokinetic studies of HM.Material and methods: SL was used here as a test herb to verify the feasibility of the proposed strategy. SL was administered to rats, then, the blood plasma, urine and feces were analyzed to determine the metabolic profiles. Using our strategy, umbelliferone and scopoletin were evaluated to be the key bioactive components. Their pharmacokinetic parameters were measured and biotransformation pathways were elucidated.Results: After oral administration of SL to rats, 17 components in blood, 10 components in urine and 2 components in feces were identified and characterized using our UPLC-DAD-QTOF-MS method. Umbelliferone, scopoletin and their metabolites were found to be the major components involved in the metabolism process. Literature reports also suggest that umbelliferone and scopoletin are responsible for the therapeutic effects of SL, thus these two components were selected as the active markers for pharmacokinetic study. In the test of validity, the established method presented good linearity with R-2> 0.99. The relative standard deviation value was below 13.9% for precision, and recovery studies for accuracy were found to be within the range 91.8-112.5%.Conclusion: The present strategy offers, simultaneously, precision in quantitative analysis (metabolism study) and accuracy in quantitative analysis (pharmacokinetic study) with greater efficiency and less costs, which is therefore reliably used for integrated metabolism and pharmacokinetic studies of HM. (C) 2014 Elsevier Ireland Ltd. All rights reserved.
Nitraria tangutorum Bor., having edible berries, is valued for reputed health benefits in Qinghai-Tibet plateau. The phytochemical research on the fruit juice of N. tangutorum led to the isolation of twenty-six compounds including five new compounds, tangutorids A-D (1, 2, 3a, and 3b), and (3E,5E)-7-O-β-glucosyl-4-(2-methoxy-2-oxoethyl)hepta-3,5-dienoic acid (15). The structures of these compounds were elucidated through comprehensive spectroscopic analyses. Tangutorids A-F were the first examples of glucose-derived β-carbolines from natural products. The biogenetic pathways of 1-8 were proposed to involve Pictet-Spengler reactions and described starting from the co-isolated tryptophan (10) and corresponding aldehydes. All isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Compounds 21, 22, and 24 showed antioxidant activity with SC50 values ranging from 12.2±1.9 to 30.4±2.7μg/mL, and compound 1 showed strong α-glucosidase inhibitory effect with IC50 value of 63.3±4.6μg/mL.
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