[Ligusticum cycloprolactam inhibits IL-1ß-induced apoptosis and inflammation of rat chondrocytes via HMGB1/TLR4/NF-κB signaling pathway].

Chondrocytes are unique resident cells in the articular cartilage, and the pathological changes of them can lead to the occurrence of osteoarthritis(OA). Ligusticum cycloprolactam(LIGc) are derivatives of Z-ligustilide(LIG), a pharmacodynamic marker of Angelica sinensis, which has various biological functions such as anti-inflammation and inhibition of cell apoptosis. However, its protective effect on chondrocytes in the case of OA and the underlying mechanism remain unclear. This study conducted in vitro experiments to explore the molecular mechanism of LIGc in protecting chondrocytes from OA. The inflammation model of rat OA chondrocyte model was established by using interleukin-1ß(IL-1ß) to induce. LIGc alone and combined with glycyrrhizic acid(GA), a blocker of the high mobility group box-1 protein(HMGB1)/Toll-like receptor 4(TLR4)/nuclear factor-kappa B(NF-κB) signaling pathway, were used to intervene in the model, and the therapeutic effects were systematically evaluated. The viability of chondrocytes treated with different concentrations of LIGc was measured by the cell counting kit-8(CCK-8), and the optimal LIGc concentration was screened out. Annexin V-FITC/PI apoptosis detection kit was employed to examine the apoptosis of chondrocytes in each group. The enzyme-linked immunosorbent assay(ELISA) was employed to measure the expression of cyclooxygenase-2(COX-2), prostaglandin-2(PGE2), and tumor necrosis factor-alpha(TNF-α) in the supernatant of chondrocytes in each group. Western blot was employed to determine the protein levels of B-cell lymphoma-2(Bcl-2), Bcl-2-associated X protein(Bax), caspase-3, HMGB1, TLR4, and NF-κB p65. The mRNA levels of HMGB1, TLR4, NF-κB p65, and myeloid differentiation factor 88(MyD88) in chondrocytes were determined by real-time fluorescent quantitative PCR(RT-qPCR). The safe concentration range of LIGc on chondrocytes was determined by CCK-8, and then the optimal concentration of LIGc for exerting the effect was clarified. Under the intervention of IL-1ß, the rat chondrocyte model of OA was successfully established. The modeled chondrocytes showed increased apoptosis rate, promoted expression of COX-2, PGE2, and TNF-α, up-regulated protein levels of Bax, caspase-3, HMGB1, TLR4, and NF-κB p65 and mRNA levels of HMGB1, TLR4, NF-κB p65, and MyD88, and down-regulated protein level of Bcl-2. However, LIGc reversed the IL-1ß-induced changes of the above factors. Moreover, LIGc combined with GA showed more significant reversal effect than LIGc alone. These fin-dings indicate that LIGc extracted and derived from the traditional Chinese medicine A. sinensis can inhibit the inflammatory response of chondrocytes and reduce the apoptosis of chondrocytes, and this effect may be related to the HMGB1/TLR4/NF-κB signaling pathway. The pharmacological effect of LIGc on protecting chondrocytes has potential value in delaying the progression of OA and improving the clinical symptoms of patients, and deserves further study.

[Research progress in pharmacological effects and chemical components of processed Angelicae Sinensis Radix products].

Angelicae Sinensis Radix is one of the main Chinese medicinal materials with both medicinal and edible values. It has the functions of tonifying and activating blood, regulating menstruation and relieving pain, and moistening intestines to relieve constipation. It is mainly produced in the southeastern Gansu province, and that produced in Minxian, Gansu is praised for the best quality. The chemical components of Angelicae Sinensis Radix mainly include volatile oils, organic acids, and polysaccharides, which have anti-inflammatory, pain-relieving, anti-tumor, anti-oxidation, immunomodulatory and other pharmacological effects. Therefore, this medicinal material is widely used in clinical practice. By reviewing the relevant literature, this study systematically introduced the research status about the chemical constituents and pharmacological effects of processed Angelicae Sinensis Radix products, aiming to provide a theoretical reference and support for the future research, development, and clinical application of related drugs.

Unlocking Dysprosium Constraints for China's 1.5 °C Climate Target.

Some key low-carbon technologies, ranging from wind turbines to electric vehicles, are underpinned by the strong rare-earth-based permanent magnets of the Nd, Pr (Dy)-Fe-Nb type (NdFeB). These NdFeB magnets, which are sensitive to demagnetization with temperature elevation (the Curie point), require the addition of variable amounts of dysprosium (Dy), where an elevation of the Curie point is needed to meet operational conditions. Given that China is the world's largest REE supplier with abundant REE reserves, the impact of an ambitious 1.5 °C climate target on China's Dy supply chain has sparked widespread concern. Here, we explore future trends and innovation strategies associated with the linkage between Dy and NdFeBs under various climate scenarios in China. We find China alone is expected to exhaust the global present Dy reserve within the next 2-3 decades to facilitate the 1.5 °C climate target. By implementing global available innovation strategies, such as material substitution, reduction, and recycling, it is possible to avoid 48%-68% of China's cumulative demand for Dy. Nevertheless, ongoing efforts in REE exploration and production are still required to meet China's growing Dy demand, which will face competition from the United States, European Union, and other countries with ambitious climate targets. Thus, our analysis urges China and those nations to form wider cooperation in REE supply chains as well as in NdFeB innovation for the realization of a global climate-safe future.

Ephedra sinica polysaccharide alleviates airway inflammations of mouse asthma-like induced by PM2.5 and ovalbumin via the regulation of gut microbiota and short chain fatty acid.

OBJECTIVES: Epidemiological investigations show that long-term exposure to PM2.5 is directly related to asthma-like and other respiratory diseases. This study aims to further explore the pharmacological effect of Ephedra sinica polysaccharide (ESP) on lung injury caused by atmospheric PM2.5. METHODS: To achieve the aim, we explored the therapeutic effect of ESP on an aggravated asthma-like mouse induced by PM2.5 combined with ovalbumin (OVA), and explored mechanisms underlying the connection between gut microbiota and lung function. KEY FINDINGS: Preliminary results showed that ESP alleviated the symptoms of aggravated allergic asthma-like in mice; reduced the number of eosinophils in BALF; reduced the levels of serum Ig-E, IL-6, TNF-α, and IL-1ß. Further qRT-PCR detected that ESP inhibited the NF-κB pathway. The final analysis detected by 16S rRNA and short chain fatty acid (SCFA) confirmed that ESP increased relative proportions of Bacteroides, Lactobacillus, Prevotella, Butyricicoccus and Paraprevotella, but decreased that of Enterococcus and Ruminococcus; increased acetic acid, propionic acid, butyric acid, isobutyric acid, valeric acid, isovaleric acid, and isohexanic acid in the meanwhile. CONCLUSIONS: The study showed that ESP has a potential for future therapeutical applications in the prevention and treatment of asthma-like disease induced by PM2.5 and OVA via regulation of gut microbiota and SCFA.

Experimental study on PE sport load evaluation of primary school students based on heart rate interval and training impulse / 中国学校卫生

Objective@#To explore the PE sport load and its influencing factors of primary school students and to provide the basis for scientific and reasonable arrangement of PE sport load and increase its exercise effect.@*Methods@#A total of 208 students from grade 5 and grade 6 of Small Wild Goose Pagoda Primary School in Xi an were selected. Stopwatch and PolarOH1 photosensitive heart rate sensor were used to record the time of each PE lesson, the students practice time and the continuous heart rate of the students during PE lesson. The exercise intensity and sport load of PE lesson were calculated by heart rate interval and training impulse (TRIMP) to evaluate the scientific nature and effectiveness of physical education.@*Results@#The average continuous heart rate was (132.5±15.2)time per min. The primary school students PE classes were mainly of low moderate intensity, and moderate to vigorous physical activity (MVPA) accounted for 36.7% of the total class time.The average TRIMP of PE was (76.62±26.69). The average exercise density was 53.6%, and the average time of preparation, basic and end parts was 13.32, 25.57 and 0.50 min, respectively.@*Conclusion@#The PE intensity and TRIMP of primary school students are too small, the cumulative time of MVPA is insufficient, the PE exercise density is appropriate, the preparation part is too long, and the end part is too short. Therefore, the PE exercise load should be strengthened to improve the sports quality of PE students.

The treatment of asthma using the Chinese Materia Medica.

ETHNOPHARMACOLOGICAL RELEVANCE: Asthma is a costly global health problem that negatively influences the quality of life of patients. The Chinese Materia Medica (CMM) contains remedies that have been used for the treatment of asthma for millennia. This article strives to systematically summarize the current research progress so that more comprehensive examinations of various databases related to CMM anti-asthma drugs, can be performed, so as to sequentially provide effective basic data for development and application of anti-asthma drugs based on the CMM. MATERIALS AND METHODS: The research data published over the past 20 years for asthma treatment based on traditional CMM remedies were retrieved and collected from libraries and online databases (PubMed, ScienceDirect, Elsevier, Spring Link, Web of Science, PubChem Compound, Wan Fang, CNKI, Baidu, and Google Scholar). Information was also added from classic CMM, literature, conference papers on classic herbal formulae, and dissertations (PhD or Masters) based on traditional Chinese medicine. RESULTS: This review systematically summarizes the experimental studies on the treatment of asthma with CMM, covering the effective chemical components, typical asthma models, important mechanisms and traditional anti-asthma CMM formulae. The therapy value of the CMM for anti-asthma is clarified, and the original data and theoretical research foundation are provided for the development of new anti-asthmatic data and research for the CMM. CONCLUSIONS: Substantial progress against asthma has been made through relevant experimental research based on the CMM. These advances improved the theoretical basis of anti-asthma drugs for CMM and provided a theoretical basis for the application of a asthma treatment that is unique. By compiling these data, it is expected that the CMM will now contain a clearer mechanism of action and a greater amount of practical data that can be used for future anti-asthma drug research.

Birth weight, gestational age and late adolescent liver function using twin status as instrumental variable in a Hong Kong Chinese birth cohort: "Children of 1997".

Birth weight (BW) is inversely associated with diabetes and liver function in Mendelian Randomization studies. Observationally, lower BW is usually also associated with poorer liver function. However, these studies could be confounded by socioeconomic position. Here we assessed if BW is associated with liver function in a unique population with little socio-economic patterning of BW, using both instrumental variable and an observational analysis. We used instrumental variable analysis (IVA) to assess the association of BW with liver function (alanine transaminase (ALT), alkaline phosphatase (ALP), bilirubin, and albumin) at ~17 years with twin status as an instrumental variable in the prospective population-representative "Children of 1997" birth cohort (n = 8327). We also conducted an observational analysis adjusted for sex, maternal age, maternal migrant status, smoking and parental socio-economic position. A generalized linear model with gamma family was used for ALT, ALP, and bilirubin because they are not normally distributed. Using IVA, BW was not associated with ALT, ALP or bilirubin, but was possibly negatively associated with albumin (-1.12 g/L, 95% confidence interval (CI) -2.08 to -0.16). Observationally, BW was negatively associated with ALT (-1.23 IU/L, 95% CI -2.16 to -0.30), ALP (-1.72 IU/L, 95% CI -3.43 to -0.01) and higher albumin (-0.23 g/L, 95% CI -0.40 to -0.06). Poor liver function may be a pathway by which the risks of lower BW are actuated. This insight might help identify post-natal targets of intervention to mitigate the adverse health effects of lower birth weight.

[Research on anticancer activity of isocorydine and its derivatives].

Isocorydine and its analogs were extracted from Dicranostigma leptopodum and Stephania yunnanensis through the method of natural products chemistry. Its derivatives were prepared by chemical structure modifications from isocorydine. MTT method was used to study the inhibitory effect of those compounds on the growth of HepG2, HeLa and MGC-803 cancer cell lines in vitro. The results showed that isocorydine and its analogs all have the growth inhibition for those cancer cell lines. This paper investigated the structure-activity relationship of isocorydine and its derivatives with anticancer activity in the aspect of stereochemical structure, functional groups positions of the compounds and the electron density of aromatic rings based on the single crystal diffraction structure and the molecular docking of EGFR and isocorydine.

A new quaternary protoberberine alkaloid isolated from Dicranostigma leptopodum (Maxim) Fedde.

Phytochemical investigation of the whole plants of Dicranostigma leptopodum (Maxim) Fedde has led to the isolation of two quaternary protoberberine alkaloids 5-hydroxy-coptisine (1) and berberrubine (2). This type of alkaloids was isolated from the genus Dicranostigma for the first time and the new compound structure (1) was elucidated by various spectroscopic methods including 2D NMR techniques (gCOSY, HMQC and HMBC) and HR-ESI-MS.

[Extraction and purification of isocorydine from Dicranostigma leptopodum].

OBJECTIVE: To optimize the conditions of extraction and purification of isocorydine from Dicranostigma leptopodum. METHODS: Extraction conditions of isocorydine were selected on the basis of orthogonal experimental design, the static adsorption/desorption experiments were used to evaluate the optimum resin. RESULTS: The optimum extraction parameters were as follows: the ratio of raw materials to solvent 1:15 (g/mL), extraction solvent 1% vitriol, the extraction three times and 1 h each time. LX28 resin exhibited higher adsorption efficiency. CONCLUSION: Under the above optimum conditions, the extraction yield of isocorydine is 0.88%. The purity of isocorydine can reach 85.34% with a yield rate of 68.64%.

[Study on semi-synthetic transforming technology for the natural product of isocorydione].

Transforming technology for semi-synthesized isocorydione from the natural product ofisocorydine was studied. The factors affecting on the reaction yield were investigated. UV spectrophotometry was used to indicate the semi-synthesized yield of isocorydione. The optimum reaction conditions were determined as following: reacting for 12 h in the solution of sodium dihydrogen phosphate at pH 10, the temperature was 25 degrees C and the ratio of isocorydine to Fremy's radical was 1 : 2. Under the optimum conditions, the yield could reach up to 50.0%. The molecular structure of isocorydione was elucidated by X-ray single-crystal diffraction analysis for the first time.

Cerebroside and ceramide from the pollen of Brassica napus L.

The new cerebroside 1-O-(ß-D-glucopyranosyl)-(2S, 3S, 4R, 8E)-2-[(2'R)-2'-hydroxytetracosenoilamino]-8-octadecene-1,3,4-triol (1) and ceramide (2S, 3S, 4R, 8E)-2-[(2'R)-2'-hydroxytetracosenoilamino]-8-octadecene-1,3,4-triol (2) were isolated from the ethyl acetate extract of the pollen of Brassica napus L. The structures of 1 and 2 were elucidated on the basis of chemical and spectroscopic method. Two new compounds were evaluated for activity in vitro assays for the cytotoxic activities against human tongue squamous carcinoma cell line (Tca8113).

Determination of a novel diarylheptanoid (Juglanin B) from green walnut husks (Juglans regia L.) in rat plasma by high-performance liquid chromatography.

A simple and reliable analytical method based on high-performance liquid chromatography (HPLC) coupled with a diode array detector (DAD) was developed for the determination of a novel diarylheptanoid (Juglanin B) from green walnut husks (Juglans regia L.) in rat plasma using rhoiptelol as an internal standard. Chromatographic separation was carried out on a Sinochrom ODS-AP C(18) column (250 x 4.6 microm i.d., 5 mm) with acetonitrile-10 mM postassium dihydrogen phosphate (pH = 3; 55:45, v/v) as mobile phase, and the detection wavelength was set at 214 nm. The plasma samples were prepared using methanol as protein precipitator. The extraction recovery of Juglanin B ranged from 70.26 to 78.59%, and the calibration curve had a good linearity in the range 0.08-50 microg/mL (r(2) = 0.9932). The RSDs of intra- and inter-day precision ranged from 1.19 to 4.92% and 4.35 to 4.54%, respectively. The HPLC-DAD method described is a simple, rapid and reliable method for the determination of Juglanin B level and for use in studies involving pharmacokinetics.

Capillary zone electrophoresis for separation and analysis of four diarylheptanoids and an alpha-tetralone derivative in the green walnut husks (Juglans regia L.).

A fast capillary zone electrophoresis (CZE) method for the simultaneous determination of four cyclic diarylheptanoids (rhoiptelol, RH; juglanin A, JA; juglanin B, JB; juglanin C, JC) and an alpha-tetralone derivative (sclerone, SC) in the extract of the green walnut husks (Juglans regia L.) was developed. The optimized buffer was composed of 25 mM sodium tetraborate at pH 10.3. The applied voltage was 20 kV and the capillary temperature was kept constant at 20 degrees C. The detection wavelength was set at 220 nm using a photodiode array detection. The effects of several CE parameters, including pH value, buffer concentration, applied voltage and separation temperature on the separation were investigated systematically. Regression equations showed good linear relationships (correlation coefficients: 0.9996-0.9999) between the peak area of each compound (RH, JA, JB, JC and SC) and its concentration accordingly. The relative standard deviations (R.S.D.) of the migration time and peak area were less than 0.57 and 3.44% (intra-day), and 0.97 and 3.71% (inter-day), respectively. The contents of the five active compounds in the green walnut husks (J. regia L.) from different origins were determined with satisfactory repeatability and recovery.

Cytotoxic diarylheptanoids from the pericarps of walnuts (Juglans regia).

Two new diarylheptanoids, juglanin A (1) and B (2), together with 15 known compounds, were isolated from the extract of the seed husks of walnuts (Juglans regia L.). The structures of 1 and 2 were elucidated by various spectroscopic methods including intensive 2D-NMR techniques, HR-ESI-MS, and X-ray single-crystal diffraction analysis, and the cytotoxic activities of 1, 2, and 10 against human hepatoma (Hep G2) cells was reported.

Eremophilane sesquiterpenes from Ligularia myriocephala.

Five new eremophilenolides, 1beta-angeloyloxy-6beta,10beta-dihydroxy-8beta-methoxyeremophil-7(11)-en-8alpha,12-olide ( 1), 1beta-angeloyloxy-6beta,10alpha-dihydroxy-8alpha-methoxyeremophil-7(11)-en-8beta,12-olide ( 2), 1beta,6beta-diangeloyloxy-8beta,10beta-dihydroxyeremophil-(11)-en-8alpha,12-olide ( 3), 1beta,6beta-diangeloyloxy-8alpha,10 alpha-dihydroxyeremophil-7(11)-en-8beta,12-olide ( 4), 1beta-angeloyloxy-8-oxoeremophil-6,9-dien-12-oic acid methyl ester ( 5) and one known compound, 8beta,10beta-dihydroxyeremophilenolide ( 6) were isolated from the extract of the whole plant of Ligularia myriocephala Ling. Their structures and stereochemistry were elucidated by various spectroscopic methods including intensive 2D-NMR techniques (COSY, gHMQC, gHMBC and (1)H- (1)H NOESY) and HR-ESI-MS. A single-crystal X-ray experiment was performed for compound 1.