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Simultaneous detection of oleanolic acid and ursolic acid in rat blood by in vivo microdialysis can provide important pharmacokinetics information. Microwave-assisted derivatization coupled with magnetic dispersive solid phase extraction was established for the determination of oleanolic acid and ursolic acid by liquid chromatography tandem mass spectrometry. 2'-Carbonyl-piperazine rhodamine B was first designed and synthesized as the derivatization reagent, which was easily adsorbed onto the surface of Fe3O4/graphene oxide. Simultaneous derivatization and extraction of oleanolic acid and ursolic acid were performed on Fe3O4/graphene oxide. The permanent positive charge of the derivatization reagent significantly improved the ionization efficiencies. The limits of detection were 0.025 and 0.020 ng/mL for oleanolic acid and ursolic acid, respectively. The validated method was shown to be promising for sensitive, accurate, and simultaneous determination of oleanolic acid and ursolic acid. It was used for their pharmacokinetics study in rat blood after oral administration of Arctiumlappa L. root extract.

The method of capillary zone electrophoresis (CZE) with direct UV detection was developed for the determination of oleanolic acid, ursolic acid, quercetin and apigenin. and then for the first time successfully applied to the analysis of four analytes in <i>Swertia mussotii</i> Franch and its preparations. Various factors affecting the CZE procedure were investigated and optimized, and the optimal conditions were: 50 × 10<sup>−3</sup> mol/L borate-phosphate buffer (pH 9.5) with 5.0 × 10<sup>−3</sup> mol/L <i>β</i>-cyclodextrin, 15 kV separation voltage, 20 °C column temperature, 250 nm detection wavelength and 5 s electrokinetic injection time (voltage 20 psi). Under the conditions, oleanolic acid, ursolic acid, quercetin and apigenin could be determined within the test ranges with a good correlation coefficient (<i>r</i>² > 0.9991). The limits of detection for conditions, oleanolic acid, ursolic acid, quercetin and apigenin were 0.3415, 0.2003, 0.0062 and 0.2538 µg/mL, respectively, and the intra- and inter-day relative standard deviations were no more than 4.72%. This procedure provided a convenient, sensitive and accurate method for simultaneous determination of oleanolic acid, ursolic acid, quercetin and apigenin in <i>S. mussotii</i> Franch. Copyright © 2014 John Wiley & Sons, Ltd.

This study is to develop an UPLC-PDA method for determination of 10 major components in Pterocephalus. The UPLC-PDA assay was performed on a Waters Acquity UPLCR BEH C₁₈(2.1 mm ×100 mm,1.7 μm), and the column temperature was at 30 ℃. The mobile phase consists of water containing 0.2% phosphoric acid (A) and acetonitrile (B) in gradient elution at a flow rate of 0.4 mL•min⁻¹. The detection wave length was set at 237 and 325 nm, and the injection volume was 1 μL in the UPLC system. The linear range of 10 detected compounds were good (r≥0.999 7), and the overall recoveries ranged from 96.30% to 103.0%, with the RSD ranging from 0.72% to 2.9%. The method was simple, accurate and reproducible, which can be used for the simultaneous determination of the content of ten major components in P. hookeri.

• In situ derivatization-UADLLME was firstly reported for NTs in rat brain microdialysates. • Lissamine rhodamine B sulfonyl chloride was firstly used as derivatization reagent. • The method was simple, rapid, green, efficient, sensitive and low matrix effect. • This method was successfully applied for Parkinson’s rat brain microdialysates.<br>Simultaneous monitoring of several neurotransmitters (NTs) linked to Parkinson’s disease (PD) has important scientific significance for PD related pathology, pharmacology and drug screening. A new simple, fast and sensitive analytical method, based on in situ derivatization-ultrasound-assisted dispersive liquid-liquid microextraction (in situ DUADLLME) in a single step, has been proposed for the quantitative determination of catecholamines and their biosynthesis precursors and metabolites in rat brain microdialysates. The method involved the rapid injection of the mixture of low toxic bromobenzene (extractant) and acetonitrile (dispersant), which containing commercial Lissamine rhodamine B sulfonyl chloride (LRSC) as derivatization reagent, into the aqueous phase of sample and buffer, and the following in situ DUADLLME procedure. After centrifugation, 50 μL of the sedimented phase (bromobenzene) was directly injected for ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) detection in multiple reaction monitoring (MRM) mode. This interesting combination brought the advantages of speediness, simpleness, low matrix effects and high sensitivity in an effective way. Parameters of in situ DUADLLME and UHPLC-MS/MS conditions were all optimized in detail. The optimum conditions of in situ DUADLLME were found to be 30 μL of microdialysates, 150 μL of acetonitrile containing LRSC, 50 μL of bromobenzene and 800 μL of NaHCO3-Na2CO3 buffer (pH 10.5) for 3.0 min at 37 °C. Under the optimized conditions, good linearity was observed with LODs (S/N > 3) and LOQs (S/N > 10) of LRSC derivatized-NTs in the range of 0.002-0.004 and 0.007-0.015 nmol/L, respectively. It also brought good precision (3.2-12.8%, peak area CVs%), accuracy (94.2-108.6%), recovery (94.5-105.5%) and stability (3.8-8.1%, peak area CVs%) results. Moreover, LRSC derivatization significantly improved chromatographic resolution and MS detection sensitivity of NTs when compared with the reported studies through the introduction of a permanent charged moiety from LRSC into NTs. Taken together, this in situ DUADLLME method was successfully applied for the simultaneous determination of six NTs in biological samples.

An imbalance in osteogenesis and osteoclastogenesis is a crucial pathological factor in the development of osteoporosis. Osteoclasts (OCs) play a pivotal role in osteoporosis, whose new therapy exploration has been focused on the suppression of OC formation. Sophoridine is found from the Chinese traditional food sophora flower to exhibit anti-osteoporosis capacity by screening. This study is focused on its anti-osteoporosis mechanism evaluation. The anti-osteoporosis effect of sophoridine, (15 mg kg-1 body), was evaluated in ovariectomized (OVX) mice by monitoring changes in bone histomorphometry index, formation of osteoclasts from blood-derived mononuclear cells, and changes in the synthesis of pro-osteoclastogenic cytokines. Signal pathways were investigated by QPCR, Western blot, and immunofluorescence. Sophoridine has a significant anti-osteoporosis effect in vivo, which can inhibit RANKL-induced OC formation, the appearance of OC-specific marker genes, and OC marker protein in vitro. Mechanistically, sophoridine dose- and time-dependently blocks the RANKL-induced OC formation and the activation of ERK and c-Fos as well as the induction and nucleus translocation of NFATc1. Sophora flower might be a useful alternative functional food in preventing or treating osteoporosis.

OBJECTIVE: To investigate the chemical constituents of Tibetan medicine Phyllanthus emblica.METHOD: Various chromatographic techniques were employed for isolation and purification of the constituents, and the structures were elucidated by chemical and spectral analyses. RESULT: 11 compounds were isolated and identified as gallic acid (I), ellagic acid (II), 1-O-galloyl-beta-D-glucose (III), 3,6-di-O-galloyl-D-glucose (IV), chebulinic acid (V), quercetin (VI), chebulagic acid (VII), corilagin (VIII), 3-ethylgallic acid (3-ethoxy-4,5-dihydroxy-benzoic acid, IX), isostrictiniin (X), 1,6-di-O-galloyl-beta-D-glucose (XI). CONCLUSION: 3-Ethylgallic acid (3-ethoxy-4,5-dihydroxy-benzoic acid) is a novel compound, and isostrictiniin was found from P. emblica for the first time.

Objective: To study the chemical constituents of the Tibetan medicine Caryopteris toroetii.; Method: The crude drug was extracted with 95% EtOH and isolated by repeatedly chromatographic methods. The structures of the isolated compounds were elucidated by spectral analysis.; Result: Six compounds were yielded and identified as: phenethyl cinnamide (1), 1-hydroxy-2, 3, 4, 5-tetramethoxy-xanthone (2), 1-hydroxy-2, 3, 5-trimethoxy-xanthone (3), (2S)-5-hydroxy-7-methoxyflavanone (4), 2', 4'-dihydroxydihydrochalcone (5) and rutin (6).; Conclusion: All the above compounds were obtained from C. toroetii for the first time.;

Four common traditional tibetan medicine prescription preparations "Anzhijinghuasan, Dangzuo, Renqingchangjue and Rannasangpei" in tibetan areas were selected as study objects in the present study. The purpose was to try to establish a kind of wet digestion and flow injection-hydride generation-atomic absorption spectrometry (FI-HAAS) associated analysis method for the content determinations of lead and arsenic in traditional tibetan medicine under optimized digestion and measurement conditions and determine their contents accurately. Under these optimum operating conditions, experimental results were as follows. The detection limits for lead and arsenic were 0.067 and 0.012 µg · mL(-1) respectively. The quantification limits for lead and arsenic were 0.22 and 0.041 µg · mL(-1) respectively. The linear ranges for lead and arsenic were 25-1,600 ng · mL(-1) (r = 0.9995) and 12.5-800 ng · mL(-1) (r = 0.9994) respectively. The degrees of precision(RSD) for lead and arsenic were 2.0% and 3.2% respectively. The recovery rates for lead and arsenic were 98.00%-99.98% and 96.67%-99.87% respectively. The content determination results of lead and arsenic in four traditional tibetan medicine prescription preparations were as fol- lows. The contents of lead and arsenic in Anzhijinghuasan are 0.63-0.67 µg · g(-1) and 0.32-0.33 µg · g(-1) in Anzhijinghua- san, 42.92-43.36 µg · g(-1) and 24.67-25.87 µg · g(-1) in Dangzuo, 1,611. 39-1,631.36 µg · g(-1) and 926.76-956.52 µg- g(-1) in Renqing Changjue, and 1,102.28-1,119.127 µg-g(-1) and 509.96-516.87 µg · g(-1) in Rannasangpei, respectively. This study established a method for content determination of lead and arsenic in traditional tibetan medicine, and determined the content levels of lead and arsenic in four tibetan medicine-prescription preparations accurately. In addition, these results also provide the basis for the safe and effective use of those medicines in clinic.

Traditional Chinese medicine inheritance support system (TCMISS, V2.5) was used in this study to analyze the common medicines, frequency of medicine combination, core herbal combinations and new prescriptions for the treatment of plateau disease from the Four-Volume Medical Code, Mannose Herbal Mirror and other related books. TCMISS V2.5 software was used to construct the database of drug treatment for plateau disease. The frequency analysis and association rules apriori algorithm, improved mutual information method and other data mining methods were used to explore the law of drug compatibility. After the analysis of 531 prescriptions for plateau disease, 20 common symptoms of plateau disease were summarized such as insomnia and tinnitus. There were 539 kinds of herbs in the plateau disease prescriptions, including 33 kinds of herbs whose medicinal frequency>=50, such as Terminalia chebula and Myristica fragrans, and T. chebula had the highest medicinal frequency; 14 commonly used herbal combinations, and "Aucklandia lappa-T. chebula" had the highest frequency; 13 core herbal combinations were obtained after entropy clustering analysis, including 8 combinations of three herbs such as "Allium sativum-Carum carvi-Ferula sinkiangensis" and 5 combinations of four herbs such as "A. lappa-Aquilaria sinensis-Ewgewia caryophyllata-Myristica fragrans", and 5 new prescriptions such as "A. sativum-C. carvi-F. sinkiangensis-A. lappa-Choerospondia axillaris-A. sinensis-M. fragrans". The main symptom of "insomnia" was chosen to analyze the treatment of insomnia, and the core herbal combinations mainly including A. sinensis, T. chebula, and C. axillaris as well as the new prescriptions mainly containing Carthamus tinctorius, Meconopsis horridnla, and Punica granatum were obtained. The prescriptions for the treatment of plateau disease were clarified by TCM inheritance system, and the clinical prescription regularity and characteristics of the combination of common medicines were summarized, to provide reference and new ideas for its clinical application and development of new drug research.; Copyright© by the Chinese Pharmaceutical Association.

Swertia mussotii (Gentianaceae) is a traditional Chinese medicinal plant grown in the Qinghai-Tibet Plateau. Three fractions from S. mussotii extract, named SWF50, SWF 70 and SWF100, were screened for in vitro anti-proliferative activity on two gastric cancer cell lines, MGC-803 and BGC-823 cells using MTT assay. Our results demonstrated that SMF70 showed an anti-proliferative effect in MGC-803 cells and SMF100 showed an anti-proliferative effect in BGC-823 cells in vitro. Moreover, both two fractions induced apoptosis via depolymerization of cytoskeletal filaments, increased cytoplasmic levels of ROS and Ca2+ and disrupted mitochondrial transmembrane potential. In addition, flow cytometry analysis indicated that both two fractions could induce cell apoptosis and arrest the cell cycle at S phase. Our results indicate that SMF70 induces apoptosis of MGC-803 cells and SMF100 induces apoptosis of BGC-823 cells via a mitochondrial-dependent pathway. Meanwhile, we also investigated antitumor effect of SMF70 in vivo, and exhibited effective tumor growth inhibition. Our findings demonstrate that S. mussotii extracts could be a potential new alternative therapeutic agent gastric cancer.

In clinical practice at Tibetan area of China, Traditional Tibetan Medicine formula Wuwei-Ganlu-Yaoyu-Keli (WGYK) is commonly added in warm water of bath therapy to treat rheumatoid arthritis (RA). However, its mechanism of action is not well interpreted yet. In this paper, we first verify WGYK's anti-RA effect by an animal experiment. Then, based on gene expression data from microarray experiments, we apply approaches of network pharmacology to further reveal the mechanism of action for WGYK to treat RA by analyzing protein-protein interactions and pathways. This study may facilitate our understanding of anti-RA effect of WGYK from perspective of network pharmacology.

In clinical practice at Tibetan area of China, Traditional Tibetan Medicine formula Wuwei-Ganlu-Yaoyu-Keli (WGYK) is commonly added in warm water of bath therapy to treat rheumatoid arthritis (RA). However, its mechanism of action is not well interpreted yet. In this paper, we first verify WGYK's anti-RA effect by an animal experiment. Then, based on gene expression data from microarray experiments, we apply approaches of network pharmacology to further reveal the mechanism of action for WGYK to treat RA by analyzing protein-protein interactions and pathways. This study may facilitate our understanding of anti-RA effect of WGYK from perspective of network pharmacology.

BACKGROUND: Patients with progressive kidney disease experience increasing physiologic and psychosocial stressors and declining health-related quality of life (HRQOL). METHODS: We conducted a randomized, active-controlled, open-label trial to test whether a Mindfulness-based Stress Reduction (MBSR) program delivered in a novel workshop-teleconference format would reduce symptoms and improve HRQOL in patients awaiting kidney transplantation. Sixty-three transplant candidates were randomized to one of two arms: i) telephone-adapted MBSR (tMBSR, an 8-week program of meditation and yoga); or ii) a telephone-based support group (tSupport). Participants completed self-report questionnaires at baseline, post-intervention, and after 6-months. Anxiety, measured by the State-Trait Anxiety Inventory (STAI) post-intervention served as the primary outcome. Secondary outcomes included: depression, sleep quality, pain, fatigue, and HRQOL assessed by SF-12 Physical and Mental Component Summaries (PCS, MCS). RESULTS: 55 patients (age 54+/-12yrs) attended their assigned program (tMBSR, n=27; tSupport, n=28). 49% of patients had elevated anxiety at baseline. Changes in anxiety were small and did not differ by treatment group post-intervention or at follow-up. However, tMBSR significantly improved mental HRQOL at follow-up: +6.2 points on the MCS - twice the minimum clinically important difference (95% CI: 1.66 to 10.8, P=0.01). A large percentage of tMBSR participants (>/=90%) practiced mindfulness and reported it helpful for stress management. CONCLUSIONS: Neither mindfulness training nor a support group resulted in clinically meaningful reductions in anxiety. In contrast, finding that tMBSR was more effective than tSupport for bolstering mental HRQOL during the wait for a kidney transplant is encouraging and warrants further investigation. ClinicalTrials.govNCT01254214.

BACKGROUND: Patients with progressive kidney disease experience increasing physiologic and psychosocial stressors and declining health-related quality of life (HRQOL). METHODS: We conducted a randomized, active-controlled, open-label trial to test whether a Mindfulness-based Stress Reduction (MBSR) program delivered in a novel workshop-teleconference format would reduce symptoms and improve HRQOL in patients awaiting kidney transplantation. Sixty-three transplant candidates were randomized to one of two arms: i) telephone-adapted MBSR (tMBSR, an 8-week program of meditation and yoga); or ii) a telephone-based support group (tSupport). Participants completed self-report questionnaires at baseline, post-intervention, and after 6-months. Anxiety, measured by the State-Trait Anxiety Inventory (STAI) post-intervention served as the primary outcome. Secondary outcomes included: depression, sleep quality, pain, fatigue, and HRQOL assessed by SF-12 Physical and Mental Component Summaries (PCS, MCS). RESULTS: 55 patients (age 54+/-12yrs) attended their assigned program (tMBSR, n=27; tSupport, n=28). 49% of patients had elevated anxiety at baseline. Changes in anxiety were small and did not differ by treatment group post-intervention or at follow-up. However, tMBSR significantly improved mental HRQOL at follow-up: +6.2 points on the MCS - twice the minimum clinically important difference (95% CI: 1.66 to 10.8, P=0.01). A large percentage of tMBSR participants (>/=90%) practiced mindfulness and reported it helpful for stress management. CONCLUSIONS: Neither mindfulness training nor a support group resulted in clinically meaningful reductions in anxiety. In contrast, finding that tMBSR was more effective than tSupport for bolstering mental HRQOL during the wait for a kidney transplant is encouraging and warrants further investigation. ClinicalTrials.govNCT01254214.

Integrating textual criticism literatures with field survey, the name, classification and botanical originals of breeds of Tibetan medicine "Dida" were discussed in this paper. The results showed that it's very intricate and confusion in the names, breeds and botanical originals of "Dida", and those were the key restricting factors resulting in shortfall and difficult formulation in quality standard of "Dida". The similar situations are existing universally in ethnodrugs, and reflecting the necessity and urgency to collate ethnodrug breeds. On the other hand, Because of the morphologic description on the botanical origins of drug was often simple in the ancient literatures, and in most cases, the botanical origins of the drug were difficult to identify accurately on the basis of the literatures. So, in the collating the breeds, it's necessary to follow the principle of "according to the ancient literatures but no rigidly", and to pay attention to the historical vicissitude of the drug breeds and origins, and the survey of present resources and clinical using, draw actively on outcome of chemical and biological active researches. That inherited the characteristics and advantages of ethnodrugs, and promoted them them modernization.

In a search for naturally occurring antibacterial compounds in medicinal plants, six hitherto unknown thiophene acetylenes, named 10,11-threo-xanthopappin D, 10,11-erythro-xanthopappin D, 10,11-cis-xanthopappin B, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(E)-pent-3-ene-1-ynylthiophene, 5-(but-3,4-dihydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene and two furanosesquiterpenes, as well as fifteen known compounds, were isolated from Xanthopappus subacaulis, which has been used as a traditional Tibetan medicine in China. A biosynthetic pathway to thiophene acetylenes was proposed and, the isolated compounds were tested for their antibacterial activity against five bacteria. Within the series of thiophene acetylenes tested, 10,11-threo-xanthopappin D with a threo configuration exhibited strong activity against Bacillus subtilis, with a minimum inhibitory concentration (MIC) of 7.25μg/mL, whereas 10,11-erythro-xanthopappin D with erythro configuration possessed broad-spectrum antibacterial activity against Escherichia coli, Bacillus cereus, Staphylococcus aureus and Erwinia carotovora, with MICs of 12.5, 15.5, 7.25 and 7.25μg/mL, respectively. Meanwhile, the compounds 10,11-cis-xanthopappin B, xanthopappin B, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene and 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(E)-pent-3-ene-1-ynylthiophene substituted with a Cl atom at C-14 showed moderate inhibitory activity against E. coli, B. cereus, S. aureus, E. carotovora and B. subtilis, with MICs ranging from 31.25 to 62.5μg/mL. The structures of these compounds were elucidated through the comprehensive analysis of spectroscopic data, including UV, IR, MS and NMR.

<br>Display Omitted<br>• Three new monoterpene glycosides (<b>1</b>-<b>3</b>) were isolated from <b>Sibiraea laevigata</b> (L.) Maxim. • Fourteen known compounds (<b>4</b>-<b>17</b>) were also obtained from the title plant. • All of the isolated compounds were evaluated for their anti-oxidant and α-glucosidase inhibitory activities. • Compounds <b>7</b> and <b>17</b> exhibited α-glucosidase inhibitory effect with IC50 values of 220.0 and 113.0 μM, respectively.<br>Three new compounds, 3,7-dimethy-7-methoxy-3-octene-5-one-1-<b>O</b>-<b>β</b>-d-glucopyranoside (1), 3,7-dimethy-7-methoxy-3(<b>Z</b>)-octene-5-one-1-<b>O</b>-<b>β</b>-d-glucopyranoside (2) and 3,7-dimethy-3-hydroxy-6-octene-5-one-1-<b>O</b>-<b>β</b>-d-glucopyranoside (3), together with fourteen known compounds (4-17) were isolated from the leaves and shoots of <b>S. laevigata</b>. The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis, including one- and two-dimensional NMR, as well as mass spectral data. All isolates were evaluated for their α-glucosidase inhibitory and antioxidant activities. The results demonstrated that 3,7-dimethyl-3(Z),6-ocatdien-5-one-1-<b>O</b>-<b>β</b>-d-glucoside (7) and sitosteryl <b>β</b>-d-glucoside (17) exhibited α-glucosidase inhibitory effects with IC50 values of 220.0 and 113.0 μM, respectively.

Background: The stems of Tinospora sinensis (Lour.) Merr commonly named "Kuan-Jin-Teng" in Chinese, have been used to treat rheumatoid arthritis as a Tibetan medicine.Purpose: The effects of the EtOAc fraction of ethanolic extract from the stems of T. sinensis (KJT) on the pro-inflammatory cytokines and MAPK pathway were studied in collagen-induced arthritis (CIA) model.Study Design: Anti-arthritic activity of KJT was investigated in CIA model.Methods: The chemical constituents of KJT were analyzed by LC-MS and HPLC. The CIA model was established with injecting the bovine CII emulsified in Freund's adjuvant in Wistar rats. Several doses of KJT (50.0, 100.0 and 200.0 mg/kg) were administrated via oral gavage to CIA rats daily for 4 weeks. The anti-arthritic activity of KJT was investigated by clinical arthritis scoring, paw swelling inspection and hyperalgesia measurement, as well as radiological and histological analysis in CIA rats. The impacts of KJT on the activation of MAPK pathway, production of pro-inflammatory cytokines (TNF-α, IL-1β and IL-17) in ankle joints, serum, and spleen in CIA rats were examined by western blot, immunohistochemical staining, ELISA, and quantitative real-time PCR respectively. Lastly, the effects of KJT on production of the nitric oxide (NO) and pro-inflammatory cytokines as well as the regulation of the phosphorylation of p38 and Erk were detected in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophage cells.Results: KJT significantly alleviated the paw swelling, hyperalgesia and arthritic severity, and reduced the synovial tissue proliferation and inflammatory cell infiltration in the CIA rats. Moreover, KJT suppressed the production of TNF-α, IL-1β, and IL-17 in ankle joints, serum, and spleen and reversed the up-regulation of the phosphorylation of p38 and Erk in CIA rats. KJT was also demonstrated to inhibit the production of NO and pro-inflammatory cytokines (TNF-α, IL-1β and IL-6), and phosphorylation of p38 and Erk in LPS-stimulated RAW264.7 cells.Conclusion: These results suggest the mechanisms of KJT performing its anti-arthritis effect may be attributed to inhibiting the production of pro-inflammatory cytokines and down-regulating the MAPK signaling pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: Aconitum tanguticum has been widely used as a remedy for infectious diseases in traditional Tibetan medicine in China. The total alkaloids of Aconitum tanguticum (TAA) are the main active components of Aconitum tanguticum and have been demonstrated to be effective in suppressing inflammation. Our aim was to investigate the protective effects of TAA on acute lung injury (ALI) induced by lipopolysaccharide (LPS) in rats.MATERIALS AND METHODS: TAA was extracted in 95% ethanol and purified in chloroform. After vacuum drying, the TAA powder was dissolved in dimethyl sulfoxide. Adult male Sprague-Dawley rats were randomly divided into six groups. Rats were given dexamethasone (DXM, 4 mg/kg) or TAA (60 mg/kg, 30 mg/kg) before LPS injection. The PaO2and PaO2/FiO2 values, lung wet/dry (W/D) weight ratio and histological changes in lung tissue were measured. The cell counts, protein concentration, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1β (IL-1β) in bronchoalveolar lavage fluid (BALF), and myeloperoxidase (MPO) activity in lung tissue were determined at 6, 12 or 24 h after LPS treatment. In addition, the NF-κ B activation in lung tissue was analyzed by western blot. RESULTS: In ALI rats, TAA significantly reduced the lung W/D ratio and increased the value of PaO2 or PaO2/FiO2 at 6, 12 or 24 h after LPS challenge. TAA also reduced the total protein concentration and the number of total cells, neutrophils or lymphocytes in BALF. In addition, TAA decreased MPO activity in the lung and attenuated histological changes in the lung. Furthermore, TAA inhibited the concentration of TNF-α, IL-6 and IL-1β in BALF at 6, 12 or 24 h after LPS treatment. Further study demonstrated that TAA significantly inhibited NF-κ B activation in lung tissue. CONCLUSIONS: The current study proved that TAA exhibited a potent protective effect on LPS-induced ALI in rats through its anti-inflammatory activity.

Traditional Tibetan medicine is important for discovery of drug precursors. However, knowledge of the chemical composition of traditional Tibetan medicines is very limited due to the lack of appropriate chromatographic purification methods. In the present work, Salvia prattii was taken as an example, and an off-line hydrophilic interaction liquid chromatography/reversed-phase liquid chromatography preparative method was developed for the purification of phenylpropanoids with high purity from a crude sample of Salvia prattii. Based on the separation results of four different chromatographic stationary phases, the first-dimensional preparation was performed on an XAmide preparative column with the crude sample concentration of 62.0 mg/mL, and five main fractions were obtained from the 12.4 g crude sample with a recovery of 54.8%. An XCharge C18 preparative column was applied in the second-dimensional preparation to further isolate the phenylpropanoids from the redissolved first-dimensional fractions with concentration of approximately 50.0 mg/mL. The purities of the phenylpropanoids isolated from the crude sample of Salvia prattii were higher than 98%, indicating that the method was efficient for the purification of phenylpropanoids with high purity from Salvia prattii. Additionally, this method showed great potential in the preparation of phenylpropanoids and can serve as a good example for the purification of phenylpropanoids from other plant materials.

OBJECTIVE: To study the chemical constituents of Tibetan medicine Caryopteris toroetii.METHOD: The crude drug was extracted with 95% EtOH and isolated by repeated chromatographic methods. The structures of the isolated compounds were elucidated on the basis of spectral analysis. RESULT: Two en-kaurene diterpenoid compounds: oridonin (1) and nodosin (2), were obtained from C. toroetii and their 1H and 13C-NMR data in CD3OD were reported for the first time. CONCLUSION: The en-kaurene diterpenoid compounds were obtained from genus Caryopteris for the first time.

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