Pseudoamaolide P, a 1,2:3,4:9,10:9,19-tetraseco-cycloartane triterpene spiroketal lactone from seeds of Pseudolarix amabilis.

A 1,2:3,4:9,10:9,19-tetraseco-cycloartane triterpene spiroketal lactone, pseudoamaolide P (1), two new labdane-type diterpenoids, pseudoamains A and B (2-3), and four known cembrane-type diterpenoids (4-7) were isolated from the seeds of Pseudolarix amabilis. The structures of these compounds were elucidated by spectroscopic analyses, including HRESIMS, 1D-, and 2D-NMR. The anti-inflammatory activities of the compounds were evaluated by suppressing the transcription of the NF-κB-dependent reporter gene in LPS-induced 293 T/NF-κB-luc cells. All compounds do not show potent activity.

[Diterpenoid constituents in Pseudolarix amabilis and their antitumor activities in vitro].

By various chromatographic techniques and extensive spectroscopic methods, 17 abietane diterpenoids were isolated from the dichloromethane fraction of the 95% ethanol cold-soak extracts of the seeds of Pseudolarix amabilis, namely pseudoamaol A(1), 12α-hydroxyabietic acid(2), 12-methoxy-7,13-abietadien-18-oic acid(3), 13-hydroxy-8,11,13-podocarpatrien-18-oic acid(4), 15-hydroxy-7,13-abietadien-12-on-18-oic acid(5), 8(14)-podocarpen-13-on-18-oic acid(6), holophyllin K(7), metaglyptin B(8), 7α-hydroxydehydroabietinsaure-methylester(9), 7-oxodehydroabietic acid(10), 15-hydroxy-7-oxodehydroabietinsaure-methy-lester(11), 15-methoxydidehydroabietic acid(12), 7-oxo-15-hydroxy-dehydroabietic acid(13), 15-hydroxydehydroabietic acid(14), 8,11,13-abietatriene-15,18-diol(15), 8,11,13-abietatriene-15-hydroxy-18-succinic acid(16), and 7ß-hydroxydehydroabie-tic acid(17). Compound 1 was a new compound. The isolated compounds were evaluated for their antitumor activities(HepG2, SH-SY5Y, K562), and compounds 8 and 17 showed potential cytotoxic activity against K562 cells, with IC_(50) values of 26.77 and 37.35 µmol·L~(-1), respectively.

Efficient decomposition of perfluorooctane sulfonate by electrochemical activation of peroxymonosulfate in aqueous solution: Efficacy, reaction mechanism, active sites, and application potential.

The electrochemical oxidation method is a promising technology for the degradation of perfluorooctane sulfonate (PFOS). However, the elimination processes of PFOS are still unknown, including the electron transfer pathway, key reactive sites, and degradation mechanism. Here, we fabricated diatomite and cerium (Ce) co-modified Sb2O3 (D-Ce/Sb2O3) anode to realize efficient degradation of PFOS via peroxymonosulfate (PMS) activation. The transferred electron and the generated hydroxyl radical (•OH) can high-effectively decompose PFOS. The electron can be rapidly transferred from the highest occupied molecular orbital of the PFOS to the lowest unoccupied molecular orbital of the PMS via the D-Ce/Sb2O3 driven by a potential energy difference under electrochemical process. The active site of Ce-O in the D-Ce/Sb2O3 can greatly reduce the migration distance of the electron and the •OH, and thus improving the catalytic activity for degrading various organic micropollutants with high stability. In addition, the electrochemical process shows strong resistance and tolerance to the changing pH, inorganic ions, and organic matter. This study offers insights into the electron transfer pathway and PMS activation mechanism in PFOS removal via electrochemical oxidation, paving the way for its potential application in water purification.

Two new diterpenoids from the stems of Rhododendron dauricum as GABAA receptor agonists.

Two new diterpenoids, dauricumins A (1) and B (2), together with two known aromatic meroterpenoids (3 and 4), were isolated from the petroleum ether soluble fraction of the stems from Rhododendron dauricum through an HPLC-MS-SPE-NMR combination strategy. The absolute configurations of 1 and 2 were elucidated by ECD calculations and [Rh2 (OCOCF3)4]-induced CD spectrum analysis. In a membrane potential FLIPR assay, confluentin (4) showed an agonistic effect on GABAA receptor (EC50 = 20 µM).

Study of pollutant accumulation characteristics and microbial community impact at three bioretention facilities.

In this paper, three bioretention facilities (BT, RG1-A, and RG1-B) were selected for on-site testing and experimental analysis. Of which, BT is a roadside bioretention tank with layered filler, while RG1-A and RG1-B are rain gardens with conventional filler (Bioretention soil media, BSM) and modified filler (BSM+10% Water treatment residuals,WTR), respectively. The effect of pollutant accumulation on the soil microbial community structure in the facilities, and the risk of heavy metal contamination over several years of bioretention facility operation were studied. Results showed that the water quality pollutant load reduction in BT was fluctuating. This is related  to the poor water quality of road stormwater flowing into BT and the facility filler. Because RG1-B uses modified filler, RG1-B was more effective than RG1-A in regulating water quality and quantity; the changes in soil physical and chemical properties in BT, RG1-A, and RG1-B were influenced by external factors. Next, BT was at high risk of heavy metal contamination than other facilities. The microbial community structure of the facility had the following characteristics: at the phylum level, Proteobacteria was the dominant phylum in the bioretention facility, accounting for 29-45%; and at the genus level, Blastocatella was the dominant phylum, and the relative abundance in situ was higher than that in the bioretention facility. The results of the correlation analysis combining filler environmental factors and microbial community structure indicated that SMC was a highly influential factor among the three facilities.

A new ascorbic acid derivative and two new terpenoids from the leaves and twigs of Rhododendron decorum.

The phytochemical study of the ethanol extract of the leaves and twigs of Rhododendron decorum afforded a new ascorbic acid derivative (1), a new ionone analogue (2), a new ursane-type triterpenoid glucoside (3), and four known compounds (4-7). The structures were elucidated by spectroscopic analyses, including HRESIMS, 1D, and 2D NMR. The anti-neuroinflammatory activities of the compounds were evaluated by measuring inhibitory effects of LPS-induced NO production in BV2 cells.

Antinociceptive Diterpenoids from the Leaves and Twigs of Rhododendron decorum.

Three new leucothane-type (1-3), two new micrathane-type (4, 5), eight new grayanane-type diterpenoids (6-13), and four known compounds were obtained from the ethanol extract of the leaves and twigs of Rhododendron decorum. The structures were determined based on NMR spectra, quantum chemical calculations, and X-ray crystallography. The antinociceptive activities of compounds 1, 3, 4, 6, 8, 10-13, and 15-17 were evaluated via the acetic acid-induced writhing test. Compounds 1, 8, 11-13, and 15 exhibited significant antinociceptive activities. In particular, 12 and 15 were found to be effective at doses of 0.8 and 0.08 mg/kg, respectively.

Reversal of the Apoptotic Resistance of Non-Small-Cell Lung Carcinoma towards TRAIL by Natural Product Toosendanin.

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) selectively triggers cancer cell death via its association with death receptors on the cell membrane, but exerts negligible side effects on normal cells. However, some non-small-cell lung carcinoma (NSCLC) patients exhibited resistance to TRAIL treatment in clinical trials, and the mechanism varies. In this study, we described for the first time that toosendanin (TSN), a triterpenoid derivative used in Chinese medicine for pain management, could significantly sensitize human primary NSCLC cells or NSCLC cell lines to TRAIL-mediated apoptosis both in vitro and in vivo, while showing low toxicity against human primary cells or tissues. The underlying apoptotic mechanisms involved upregulation of death receptor 5 (DR5) and CCAAT/enhancer binding protein homologous protein, which is related to the endoplasmic reticulum stress response, and is further associated with reactive oxygen species generation and Ca2+ accumulation. Surprisingly, TSN also induced autophagy in NSCLC cells, which recruited membrane DR5, and subsequently antagonized the apoptosis-sensitizing effect of TSN. Taken together, TSN can be used to sensitize tumors and the combination of TRAIL and TSN may represent a useful strategy for NSCLC therapy; moreover, autophagy serves as an important drug resistance mechanism for TSN.

Interaction of perchlorate and trichloroethene bioreductions in mixed anaerobic culture.

This work evaluated the interaction of perchlorate and trichloroethene (TCE), two common co-contaminants in groundwater, during bioreduction in serum bottles containing synthetic mineral salts media and microbial consortia. TCE at concentrations up to 0.3mM did not significantly affect perchlorate reduction; however, perchlorate concentrations higher than 0.1mM made the reduction of TCE significantly slower. Perchlorate primarily inhibited the reduction of vinyl chloride (VC, a daughter product of TCE) to ethene. Mechanistic analysis showed that the inhibition was mainly because perchlorate reduction is thermodynamically more favorable than reduction of TCE and its daughter products and not because of toxicity due to accumulation of dissolved oxygen produced during perchlorate reduction. As the initial perchlorate concentration increased from 0 to 600mg/L in a set of serum bottles, the relative abundance of Rhodocyclaceae (a putatively perchlorate-reducing genus) increased from 6.3 to 80.6%, while the relative abundance of Dehalococcoides, the only known genus that is able to reduce TCE all the way to ethene, significantly decreased. Similarly, the relative abundance of Proteobacteria (a phylum to which most known perchlorate-reducing bacteria belong) increased from 22% to almost 80%.

[Effect of insulin by local injection on the level of systemic blood glucose and granulation tissue formation of wound in patients with diabetic foot ulcer].

OBJECTIVE: To investigate the effects of local injection of insulin on the level of systemic blood glucose and granulation tissue formation of wound in patients with diabetic foot ulcer. METHODS: Thirty-two patients with diabetic foot ulcer hospitalized in our wards from June 2009 to June 2010 were divided into insulin (I, n = 16) and control (C, n = 16) groups according to the random number table. For patients in I group, after debridement, one half of calculated dose of insulin diluted with equal amount of normal saline was injected diffusely into the base of the ulcer, and another half dose of insulin was subcutaneously injected into abdominal wall for 7 days, two times a day. For patients in C group, after debridement, primary insulin was subcutaneously injected into abdominal wall, 1 mL saline was subcutaneously injected into basal layer of ulcer for 7 days, two times a day. Before injection and 0.5, 1.0, 2.0, and 4.0 hours after injection (PIH), level of fasting blood glucose was determined. Before injection and on post injection day (PID) 3, 5, and 7, the growth of granulation tissue was assessed, and wound specimens were harvested for observation of CD34 expression and calculation of microvessel density (MVD). Data were processed with t test. RESULTS: The levels of fasting blood glucose in both groups during observational time points ranged from 6.6 mmol/L to 12.8 mmol/L with a mean of (10.0 ± 2.2) mmol/L, and there was no statistical difference (with t values from 0.000 to 2.209, P values all above 0.05). Growth of granulation tissue in I group was more exuberant from PID 5, especially on PID 7 [(59.06 ± 1.58)%], which was significantly richer than that in C group [(23.61 ± 1.57)%, t = 17.420, P = 0.000]. New vessels were observed in I group from PID 3 as indicated by CD34 expression. There was no obvious difference in the number of MVD between I group and C group on PID 3 (t = 0.247, P > 0.05). The number of MVD per 200 times visual field in I group was respectively 8.34 ± 0.48, 11.22 ± 0.97 on PID 5 and 7, which was respectively higher than that in C group (4.42 ± 0.14, 5.44 ± 1.13, with t value respectively 16.568, 27.664, P values all below 0.01). CONCLUSIONS: Local injection of insulin has a significant effect on systemic blood glucose in patients with diabetic foot ulcer, and it can promote the growth of granulation tissue and wound healing.