Lignans from the seed shells of Cerasus humilis (Bge.) Sok and their bioactivities.

The exploration of Cerasus humilis (Bge.) Sok seed shells yielded the identification of six previously uncharacterized compounds, in addition to twelve known compounds. Structure elucidation of these compounds relied on spectroscopic data analysis, and their absolute configurations were established by comparing calculated and experimental electronic circular dichroic (ECD) spectra, supplemented by interpretation of optical rotation data. Notably, none of these compounds exhibited cytotoxicity against HepG2 and A549 cell lines. Remarkably, a majority of the compounds displayed potent antioxidant activity.

Effects of initial carbon-phosphorus ratio on phosphatase, and phosphorus availability in sludge composting.

Phosphorus in wastewater sludge is one of the important nutrients for biological growth and an important non-renewable resource. Most research in the composting field focuses on the C/N ratio, but there are few reports on initial carbon-phosphorus (C/P) ratio regulation. This study investigated the effects of different initial C/P ratios on phosphatase activity, key bacteria, and phosphorus availability in compost. In this study, the activity of phosphatase was measured, and key bacteria secreting phosphatase were identified. The results showed that adjusting the initial C/P ratio could prolong the cycle of action of key bacteria, thus affecting the activity of phosphatase and promoting the production of available phosphorus, but it was also inhibited by the feedback of available phosphorus. This study demonstrated the feasibility of adjusting the initial C/P ratio of sludge composting and provided theoretical support for optimizing the application of sludge composting products with different initial C/P ratios.

Heavy grazing reduced the spatial heterogeneity of Artemisia frigida in desert steppe.

BACKGROUND: Grazing disturbance plays an important role in the desert steppe ecosystem in Inner Mongolia, China. Previous studies found that grazing affected the spatial distribution of species in a community, and showed patchiness characteristics of species under different grazing treatments. Artemisia frigida is the dominant species and semi-shrub in desert steppe, and whether grazing interference will affect the spatial distribution of A. frigida is studied. In this study, geo-statistical methods were mainly used to study the spatial distribution characteristics of A. frigida population in desert steppe of Inner Mongolia at two scales (quadrat size 2.5 m × 2.5 m, 5 m × 5 m) and four stocking rates (control, CK, 0 sheep·ha-1·month-1; light grazing, LG, 0.15 sheep·ha-1·month-1, moderate grazing, MG, 0.30 sheep·ha-1·month-1, heavy grazing, HG, 0.45 sheep·ha-1·month-1). RESULTS: The results showed that the spatial distribution of A. frigida tended to be simplified with the increase of stocking rate, and tended to be banded with increased spatial scale. The density and height of A. frigida increased with increasing scale. With increased stocking rate, the density of A. frigida population decreased linearly, while its height decreased in a step-wise fashion. The spatial distribution of A. frigida was mainly affected by structural factors at different scales and stocking rate. The density of A. frigida was more sensitive to change in stocking rate, and the patchiness distribution of A. frigida was more obvious with increase in scale. CONCLUSIONS: Stocking rate has a strong regulatory effect on the spatial pattern of A. frigida population in the desert steppe. Heavy grazing reduced the spatial heterogeneity of A. frigida in the desert steppe. The smaller dominant populations are unfavourable for its survival in heavy grazing condition, and affects the stability and productivity of the grassland ecosystem.

Association of vitamin and/or nutritional supplements with fall among patients with diabetes: A prospective study based on ACCORD and UK Biobank.

Aims: To assess the associations of vitamin and/or nutritional supplements (VNS) with falls among patients with diabetes. Methods: 9,141 and 21,489 middle-aged participants with diabetes from Action to Control Cardiovascular Risk in Diabetes (ACCORD) trial and UK Biobank were included. Use of VNS was collected at baseline, and fall events were recorded using annual questionnaires in ACCORD and electric records in UK Biobank during follow-up. The associations of VNS use with fall risk were analyzed using logistic regression models in ACCORD and Fine-Gray sub-distribution hazard models in UK Biobank. The role of specific supplements was also estimated in UK Biobank, adjusting for confounding factors and multiple comparisons. Results: 45.9% (4,193/9,141, 5.5 median follow-up years) patients in ACCORD and 10.5% (2,251/21,489, 11.9 median follow-up years) in UK Biobank experienced fall and in-patient events during follow-up, respectively. In ACCORD, VNS using was associated with an increased risk of fall (full-adjusted odds ratio [OR]: 1.26, P < 0.05). In UK Biobank, despite no significant association between VNS overall and in-patient fall, vitamin B, calcium, and iron using increased the risk of falls significantly (full-adjusted hazard ratio range: 1.31-1.37, P < 0.05). Conclusions: Use of specific VNS increased the risk of fall among patients with diabetes. The non-indicative use of nutritional supplements for patients with diabetes might be inadvisable.

Effect of Fe-Mn-Ce modified biochar composite on microbial diversity and properties of arsenic-contaminated paddy soils.

In this study, we investigated the mechanism of decrease in arsenic (As) bioavailability after addition of biochar (BC) supplemented with iron (Fe)- manganese (Mn)- cerium (Ce) oxide (FMCBC) to As-contaminated paddy soil. We explored the effects of these composites on the oxidation, reduction, microbial community, and soil enzyme activity of As-contaminated paddy soil. Results showed that FMCBCs improve soil pH, significantly improve the redox capacity of soil, and reduce bioavailable forms of As. FMCBCs can convert As from a specifically or non-specifically bound form into amorphous hydrous oxide bound- and crystalline hydrous oxide bound form. The application of FMCBCs increased soil enzyme activity (urease, catalase, alkaline phosphatase, and peroxidase), and greatly influenced the relative abundance of certain microorganisms (Proteobacteria, Acidobacteria, and Gemmatimonadetes), which improved soil enzyme heavy metal tolerance and prevented their denaturation. Thus, FMCBCs can not only change the form and distribution of As in soil but also create an environment suitable for microbial growth, consequently affecting the geochemical cycling of As in soil.

Flavonoid glucosides from the flowers of Trollius chinensis Bunge.

Four new flavonoid glucosides, 2″-O-(6‴-O-caffeoyl)-galactopyranosylvitexin (1), 2″-O-(6‴-O-veratroyl)-galactopyranosylvitexin (2), 2″-O-(6‴-O-feruloyl)-galactopyranosylorientin (3), 2″-O-(2‴-O-methylbutyryl)-glucopyranosylisoswertisin (4), along with three known compounds were isolated from the flowers of Trollius chinensis Bunge. Their structures were determined by extensive spectroscopic analyses.

Two new secoiridoid glucosides and a new lignan from the roots of Ilex pubescens.

Two new secoiridoid glucosides, ilexpublignoside (1), pubzenoside (2), and a new lignan, ilexlignan B (3), along with seven known compounds (4-10) were isolated from the roots of Ilex pubescens for the first time. Their chemical structures were elucidated on the basis of extensive spectroscopic methods, including IR, UV, HR-ESI-MS, CD, NMR experiments, as well as comparison with the reported data.

New phenanthrene and 9, 10-dihydrophenanthrene derivatives from the stems of Dendrobium officinale with their cytotoxic activities.

Two new phenanthrene and 9, 10-dihydrophenanthrene derivatives (1-2) with six known congeners (3-8) were isolated from the extraction of stems of Dendrobium officinale. Compounds 1 and 2 were based on carbon skeleton in which phenanthrene and 9, 10-dihydrophenanthrene moiety were linked with a phenylpropane unit through a dioxane bridge, respectively. Their structures were determined by comprehensive NMR spectroscopic data, the absolute configuration of new compounds were determined by comparing their experimental and calculated ECD for the first time. All the compounds were investigated contains two cancer cell lines (HI-60, THP-1). All the isolates showed cytotoxicity, especially compound 4 showed markedly cytotoxic activities against HI-60 and THP-1 cell lines with IC50 values of 11.96 and 8.92 µM.

An HPLC method for simultaneous quantitative determination of seven secoiridoid glucosides separated from the roots of Ilex pubescens.

A simple and specific high-performance liquid chromatographic method has been developed and validated to simultaneously determine seven secoiridoid glucosides for the first time. Three of them were separated from the ethanolic extract of the roots of Ilex pubescens for the first time, namely nuezhenide A, ligusides B and oleonuezhenide. In quantitative analysis, all of the calibration curves showed good linear regression (r > 0.999) within the tested ranges, and the mean recoveries of three different concentrations ranged from 97.6 to 101.2%. The limit of detection and limit of quantification were <4.18 and 11.63 ng mL-1 , respectively. The relative standard deviation for repeatability and the precision of seven analytes were <3.4 and 1.9%, respectively. The established method was successfully applied to simultaneous determination of seven secoiridoid glucosides in 11 batches of samples collected from different habitats in China.

Protective Effects of α-Boswellic Acids in a Pulmonary Arterial Hypertensive Rat Model.

The purpose of this study was to observe the protective effects of α-boswellic acids on hypoxia-induced pulmonary vascular structural remodeling in pulmonary arterial smooth muscle cells in a hypertensive rat model. Pulmonary arterial smooth muscle cells were cultured and then randomly divided into four groups: normoxia, hypoxia (3 % O2; 24 h), hypoxia plus α-boswellic acids, and hypoxia plus DMSO (as a positive control), according to the different concentrations of α-boswellic acids (21.90 µM, 43.79 µM, and 87.58 µM). Apoptosis and proliferation of pulmonary arterial smooth muscle cells significantly decreased in the hypoxia plus α-boswellic acids group compared with the hypoxia and hypoxia plus DMSO groups (n = 8, p < 0.05). The mRNA and protein phosphorylation levels of c-Jun N-terminal kinase 1 and extracellular regulated protein kinase 1 were significantly elevated in hypoxic cells compared with normal cells. However, the mRNA and protein phosphorylation levels of c-Jun N-terminal kinase 1 and extracellular regulated protein kinase 1 markedly decreased in the hypoxia plus α-boswellic acids group compared with the hypoxia plus DMSO group (n = 8, p < 0.05; n = 13, p < 0.05, respectively). Our findings suggest that α-boswellic acids can inhibit inappropriate apoptosis and excessive proliferation of pulmonary arterial smooth muscle cells and pulmonary vascular remodeling by repressing the expression of c-Jun N-terminal kinase 1 and extracellular regulated protein kinase 1 under hypoxic conditions.

Seladoeflavones A-F, six novel flavonoids from Selaginella doederleinii.

Six new flavonoids, seladoeflavones A-F (1-6), were isolated from the whole herbs of Selaginella doederleinii, together with one known flavonoid (7). Their structures including absolute configuration were characterized on the basis of extensive spectroscopic methods including NMR, HRMS, and electronic circular dichroism (ECD). All compounds consist of an aryl substituent at the C-3' position of naringenin or apigenin skeletons, and compounds 1 and 6 were identified as R configurations, which are uncommonly encountered in nature. A possible biosynthetic pathway was postulated. In addition, bioassay of the isolates revealed that 5-7 exhibited moderate cytotoxicity against three human cancer cell lines NCI-H460, A549, and K562 in vitro with IC50 values ranging from 8.17 to 18.66µM.

Design and evaluation of a novel potential carrier for a hydrophilic antitumor drug: Auricularia auricular polysaccharide-chitosan nanoparticles as a delivery system for doxorubicin hydrochloride.

To improve the low loading content of hydrophilic drugs in nanodrug delivery systems, a natural watersoluble polysaccharide, Auricularia auricular polysaccharide (AAP), was extracted and purified as a vehicle for the hydrophilic drug doxorubicin hydrochloride (Dox·HCl). This involved the preparation of polyelectrolyte complexes nanoparticles (PEC NPs) using the electrostatic interaction between cationic chitosan (CS) and anionic AAP. The formation of AAP-CS-NPs was confirmed by FT-IR and TEM. It was found that Dox-loaded AAP-CS-NPs possessed a spherical morphology with average diameters of 237.6nm and 74.1% Dox·HCl encapsulation efficiency. The stability of Dox AAP-CS-NPs was examined by suspending the nanoparticles in PBS (pH 7.4) at room temperature. The particle size of the nanoparticle samples remained stable and exhibited no obvious variations in drug content after half a month. In addition, in vitro cytotoxicity studies showed that blank AAP-CS-NPs did not exhibit any cytotoxic effects, while Dox AAP-CS-NPs increased the Dox·HCl cytotoxicity against MCF-7 cells as the result of significantly increased cellular uptake, compared with free Dox·HCl. Hence, the overall results obtained suggest that AAP-CS-NPs are very effective in entrapping Dox·HCl and to penetrate into tumor cells, rendering them promising carriers for hydrophilic antitumor drugs.

Carboxymethyl flavonoids and a chromone with antimicrobial activity from Selaginella moellendorffii Hieron.

Five new carboxymethyl flavonoids named 5-carboxymethyl-3', 4', 7-trihydroxyflavone (1), (2S)- 5-carboxymethyl-3', 4', 7-trihydroxyflavonone (2a), (2R)-5-carboxymethyl-3', 4', 7-trihydroxyflavonone (2b), (2S)-5-carboxymethyl-4', 7-dihydroxyflavonone (3), 5- carbomethoxymethyl-4', 7-dihydroxyflavone (4), and a new chromone named 5-carboxymethyl-7-hydroxychromone (5), together with two known compounds 5-carboxymethyl-4'-hydroxyflavone-7-O-ß-d-glucopyranoside (6), 5-carboxymethyl-4', 7-dihydroxyflavone (7) were isolated from Selaginella moellendorffii Hieron. Their structures including absolute configuration were elucidated by extensive spectroscopic methods and experimental electronic circular dichroism (ECD) spectra. What's worth mentioning is that a carboxymethyl substituent appeared at the C-5 position of all isolated compounds, only recently discovered in genus Selaginella. Compounds 2a and 2b were identified as a pair of chiral isomers; compound 5 was discovered as the first chromone comprising a carboxymethyl side chain. Furthermore, all compounds were evaluated for their antibacterial activities against various Gram-positives and Gram-negatives, and compared to the reference drugs amoxicillin and norfloxacin. As a result, compounds 3 and 4 exhibited as potent antimicrobial agents with a broad spectrum, and compound 5 appeared as the most promising one to combat Gram-positives.

Two new compounds from the roots of Ilex pubescens and their cytotoxic activity.

A new phenylethanoid, 1-O-ß-D-(4-hydroxyphenyl)-ethyl-6-O-vanilloyl-glucopyranoside (1), and a new furofuran lignan, (7R,7'R,7''S,8S,8'S,8''R)-4', 4''-dihydroxy-3,3',3'',5-tetramethoxy-7,9':7'9-diepoxy-4,8''-oxy-8,8'-sesquineolignan-7'',9''-diol (2), along with five known compounds (3-7) were isolated from the roots of Ilex pubescens. Their chemical structures were elucidated on the basis of extensive spectroscopic analysis, including UV, IR, MS, and NMR experiments. In addition, compounds 2-7 were evaluated in vitro for their cytotoxic effects on human HeLa cells; among them, compounds 2, 3, 6, and 7 showed cytotoxic activity against HeLa cells in the test.

Effect of direct current pulse stimulating acupoints of JiaJi (T10-13) and Ciliao (BL 32) with Han's Acupoint Nerve Stimulator on labour pain in women: a randomized controlled clinical study.

OBJECTIVE: To assess the clinical effect and safety of direct current (DC) pulse produced by Han's Acupoint Nerve Stimulator in reduction (HANS) of labor pain. METHODS: Totally 120 participants were enrolled in this clinical trial, and were randomly divided into 4 groups including: HANS group, patient controlled intravenous analgesia (PCIA) group, patient-controlled epidural analgesia (PCEA) group and control group. The HANS group was treated by stimulating the acupoints of JiaJi (T10-L3) and Ciliao (BL 32) with DC pulse of 100 Hz and 15-30 mA produced by a portable battery-powered Han's Acupoint Nerve Stimulator for 30 min. The PCIA group was intravenously infused Ondansetron (8 mg) for 5 min, then tramadol injection (1.5 mg/kg) was slowly dripped by using BaxterAP II electronic pump with 50 mL tramadol (0.70%) + ondansetron (8 mg), background infusion 2 mL/h, PCA dose of 2 mL, lockout interval of 10 min. In PCEA group, women received intrathecal injection ropivacaine (3 mg) in L2-3, and epidural catheter was connected to BaxterAP II electronic pump, with 100 mL Ropivacaine (0.1%) and Sufentanil (50 ug), background infusion 5 mL, Patient controlled analgesia (PCA) dose of 5 mL, lockout interval of 10 min. The control group was not received analgesia. The visual analogue scale (VAS), stage and manner of labor, Apgar score of newborn, neonatal weights, oxytocin dosage, postpartum hemorrhage and side effects were monitored in all groups. RESULTS: The vital signs were all stable in the four analgesic groups. After analgesia, there was statistical difference in VAS score between HANS group and control group, between PCEA group and the control group, between PCIA group and control group. The analgesic effect in the PCEA group was significantly better than that of other two groups. The second stage of labor in the PCEA group was longer than the other three groups, showing significant difference between them. The Apgar score of newborn 1 min after birth in the PCIA group was slightly lower than that of the other two groups, showing significant difference between them. The neonatal weights between four groups were not significantly different. The rate of cesarean section in the control group was significantly higher than that of the labor analgesia group, there was statistically difference in four groups. The number of PCIA group that used oxytocin was lower than that of other three groups. There was no significant difference in postpartum hemorrhage between four groups. The side effects of the PCEA group were itching, uroschesis and neonatal asphyxia and PCIA group were nausea and vomiting and neonatal asphyxia. However, fewer side-effects were observed in the HANS group. CONCLUSION: The DC pulse produced by HANS may be a non-pharmacological alternative to labor pain with fewer side effects.

Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors.

A series of novel quinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 5 cancer cell lines (HT-29, H460, MKN-45, A549, and U87MG) in vitro. Most compounds showed moderate to excellent potency, with the most promising analogue 45 (c-Met half-maximal inhibitory concentration [IC50]=1.15 nM) showing high selectivity versus 5 other tyrosine kinases, VEGFR-2, Flt-3, PDGFR-ß, c-Kit, and EGFR. Structure-activity relationship studies indicated that electron-donating groups on the phenyl ring at the 3-position of pyrimidine-2,4,6-trione were required to increase the electron density on the 5-(aminomethylene)pyrimidine-2,4,6-trione moiety.

Isolation and cytotoxic activity of selaginellin derivatives and biflavonoids from Selaginella tamariscina.

Five selaginellin derivatives, including two new selaginellins termed selaginellins M (1) and N (2), and three previously identified compounds, selaginellin (3), selaginellin A (4), and selaginellin C (5), were isolated from the Selaginella tamariscina (Beauv.) Spring plant. In addition, four known biflavonoids, namely neocryptomerin ( 6), hinokiflavone (7), pulvinatabiflavone (8), and 7''- O-methylamentoflavone (9), were also isolated. The structures of new compounds 1 and 2 were elucidated by spectroscopic analysis. The cytotoxic activity of compounds 1- 9 was evaluated against a small panel of human cancer cell lines, including U251 (human glioma cells), HeLa (human cervical carcinoma cells), and MCF-7 (human breast cancer cells). The two new selaginellins, selaginellins M (1) and N (2), showed medium activity against the human cancer cell lines.

[Studies on the chemical constituents from aerial parts of Gynura divaricata].

OBJECTIVE: To study the chemical constituents from aerial parts of Gynura divaricata. METHODS: The constituents were isolated on silica gel column chromatography, preparative TLC and Sephadex LH-20 column chromatography, identified by physicochemical properties and the structures were elucidated by spectral analysis. RESULTS: 10 compounds were isolated and identified as 2-(1', 2', 3', 4'-tetrahydroxybutyl)-6-(2", 3", 4"-trihydroxybutyl)-pyrazine (1), 2-(1', 2', 3', 4'-tetrahydroxybutyl)-5-(2", 3", 4"-trihydroxybutyl) -pyrazine (2), nicotinic acid (3), 5-hydroxy-picolinic acid(4), methyl-5-hydroxy-2- pyridinecarboxylate (5), adenosine (6), uridine (7), stigmasterol-5-O- beta-D-glucoside (8), dibutyl terephthalate (9), methyl chlorogenate (10). CONCLUSION: Compounds 1, 2, 5, 9, 10 are obtained from this genus for the first time, Compounds 3, 4 are obtained from this plant for the first time.

New naphthoquinone from the root of Lygodium japonicum (Thunb.) Sw.

A new 1,4-naphthoquinone and three known compounds were isolated from the roots of Lygodium japonicum (Thunb.) Sw. The structure of the new compound was elucidated by two-dimensional nuclear magnetic resonance and other spectral examinations.

A new compound from Lygodium japonicum (Thunb.) Sw.

A new ecdysteroside was isolated from the roots of Lygodium japonicum (Thunb.) Sw. The structure was identified as 2beta,3beta,14alpha,20R,22R-pentahydroxy-24R-methyl-5beta-cholest-7-en-6-one-3-O-beta-D-glucopyranoside by spectral and chemical methods.