Co-delivery of cisplatin and oleanolic acid by silica nanoparticles-enhanced apoptosis and reverse multidrug resistance in lung cancer.

Multidrug resistance (MDR) of chemotherapy is one of the significant concerns in cancer therapy. Here in our study, cisplatin (DDP) and oleanolic acid (OA) were co-loaded in mesoporous silica nanoparticles (Nsi) to construct DDP/OA-Nsi and solve the DDP-resistance in lung cancer therapy. The cytotoxicity and apoptosis assays demonstrated that in DDP-resistant A549/DDP cells, the cytotoxicity of DDP/OA-Nsi was significantly higher than that of free DDP or DDP single delivery system (DDP-Nsi). The intracellular drug accumulation study revealed that the intracellular DDP concentration in the DDP/OA-Nsi group was also higher than that in free DDP and DDP-Nsi groups. In the A549/DDP xenograft tumor model, DDP/OA-Nsi showed the best anticancer effect. In summary, DDP/OA-Nsi was a promising drug delivery system to solve MDR in lung cancer therapy.

New steroidal alkaloid and furostanol glycosides isolated from Solanum lyratum with cytotoxicity.

Two previously undescribed steroidal compounds, 16, 23-epoxy-22, 26-epimino-cholest-22(N), 23, 25(26)-trien-3ß-ol-3-O-ß-D-glucopyranosyl-(1→2)-ß-D-glucopyranosyl-(1→4)-ß-D-galactopyranoside (1) and 26-O-ß-D-glucopyranosyl-(25R)-5α-furost-20(22)-en-3ß, 26-diol (2), together with 7 known ones including 26-O-ß-D-glucopyranosyl-(25R)-5, 20(22)-dien-furost-3ß, 26-diol (3), (25R)-5-en-spirost-3ß-ol-O-ß-D-glucopyranosyl-(1→4)-[α-L-rhmanopyranosyl-(1→2)]-ß-D-galactopyranoside (4), funkioside D (5), aspidistrin (6), tigogenin-3-O-ß-D-lucotrioside (7), desglucolanatigonin II (8), and degalactotigonin (9), were isolated from Solanum lyratum Thunb. Their cytotoxic activities were tested in two cancer cell lines by MTT method. One of the steroidal glycosides (6) showed significant cytotoxic activity against gastric cancer SGC7901 and liver cancer BEL-7402 cells.

[Nitrogen Release from Sediment Under Dry and Rainy Season Alternation and Its Contribution to N Export from Xiangxi Watershed in Jiangxi Province].

In this study, N export from Xiangxi River Basin in Qianyanzhou station was measured by long-term monitoring, and simulation study on N. release law from the sediment in watershed was carried out based on orthogonal experiment, and at last the contributions of N release from sediment to N transport from watershed under dry and rainy season alternation were estimated. The results showed that the maximum of TN release rate was 36 mg x (m2 x d)(-1) in stable status, which decreased with increasing time; the impact of the three controlling factors on the N release followed the order of temperature > disturbance > pH, and the effect of temperature and pH on N release from the sediment was significant when disturbance was considered as the error term; TN release rate increased with increase of temperature, and acidic and alkaline conditions could also promote N release from sediment, wherein the effect of acidic conditions on N release was stronger; the changes of TN and available N content in sediment were 414.7-899.6 mg x kg(-1) and 17.5-58.9 mg x kg(-1), so the percentage of available N only accounted for 3%-10% of TN; the TN transport concentrations were 0.58-2.40 mg x L(-1) and 1.73-4.87 mg x L(-1) in dry and wet seasons, respectively, the N release flux from sediment was about 106.34 kg x a(-1), the total N transport from watershed was 864.15 kg x a(-1), and the contribution rate of N release from sediment to N transport from watershed was about 12.31%, so we should pay much attention to the contribution of N release from sediment to water eutrophication.

[Characteristics of Atmospheric Nitrogen Wet Deposition and Associated Impact on N Transport in the Watershed of Red Soil Area in Southern China].

In this study, Qianyanzhou Xiangxi River Basin in the rainy season was monitored to measure different nitrogen form concentrations of rainfall and rainfall-runoff process, in order to explore the southern red soil region of nitrogen wet deposition characteristics and its influence on N output in watershed. The results showed that there were 27 times rainfall in the 2014 rainy season, wherein N wet deposition load reached 43.64-630.59 kg and N deposition flux were 0.44-6.43 kg · hm(-2), which presented a great seasonal variability. We selected three rainfall events to make dynamic analysis. The rainfall in three rainfall events ranged from 8 to 14mm, and the deposition load in the watershed were from 18.03 to 41.16 kg and its flux reached 0.18 to 0.42 kg · hm(-2). Meanwhile, this three rainfall events led to 4189.38 m3 of the total runoff discharge, 16.72 kg of total nitrogen (TN) load and 4.64 kg · hm(-2) of flux, wherein dissolved total nitrogen (DTN) were 9.64 kg and 2.68 kg · hm(-2), ammonium-nitrogen (NH(4+)-N) were 2.93 kg and 0.81 kg · hm(-2), nitrate-nitrogen (NO(3-)-N) were 5.60 kg and 1.56 kg · hm(-2). The contribution rate of N wet deposition to N output from watershed reached 56%-94% , implying that the rainfall-runoff had tremendous contribution to N loss in this small watershed. The concentrations of TN in water had exceeded 1.5 mg · L(-1) of eutrophication threshold, which existed an eutrophication potential.

[Soil C, P and microbial biomass C, P response to different fertilizations in the hillslope cropland of purple soil].

The aim of this study is to explore the changes and coupling characteristics of carbon (C), phosphorus (P) and microbial C, P in a hillslope cropland of purple soil. The results showed that total organic carbon (TOC) ranged from 90.8 to 100.8 g . kg-1 under organic fertilizer or straw combined with inorganic fertilizer treatments (including N, NP and NPK) as compared with nitrogen (N) application only (62.2 g . kg-1). Total phosphorus (TP) ranged from 0.65 to 0.84 g . kg-1 in organic combined with inorganic fertilization treatments, and that under straw combined with inorganic fertilizer treatments was 23%-38% of organic fertilizer combined with inorganic fertilization treatments. The microbial biomass phosphorus (MBP) under N fertilizer was significantly decreased as compared with combined fertilization treatments. The ratios of microbial biomass carbon (MBC) to MBP under combined fertilization treatments were between 5 to 26, and the TOC/TP ratios under organic fertilizer and straw combined treatments were between 92 to 137 and 296 to 653, respectively, while those under N fertilizer treatment were 59 and 2000, respectively. The results indicated that combined organic and inorganic fertilizers would be helpful for enhancing P availability and increasing its potential capacity in purple soil.

Studies on chemical constituents of Ophiopogon japonicus.

Two new and six known steroidal glucosides were isolated from the tuber of Ophiopogon japonicus. The new steroidal glucosides were established as (20R,25R)-26-O-ß-d-glucopyranosyl-3ß,26-dihydroxycholest-5-en-16,22-dioxo-3-O-α-l-rhamnopyranosyl-(1 â†’ 2)-ß-d-glucopyranoside (1) and 26-O-ß-d-glucopyranosyl-(25R)-furost-5-en-3ß,14α,17α,22α,26-pentaol-3-O-α-l-rhamnopyranosyl-(1 â†’ 2)-ß-d-glucopyranoside (3) on the basis of spectroscopic data as well as chemical evidence.

[Nitrogen leaching and associated environmental health effect in sloping cropland of purple soil].

In this paper, we monitored different forms of nitrogen (N) transported by the subsurface flow under three different natural rainfall events and different fertilizations and conducted an associated risk evaluation on environmental health, which provides scientific basis for controlling N non-point pollution and establishing a reasonable fertilization system in purple soil area. The results showed that there were different forms of N transport by subsurface flow under different rainfall events, where in dissolved nitrogen (DN) accounted for about 53.74% - 99.21%, and nitrate (NO3(-) -N) accounted for about 35.70% - 93.65% of DN, and especially under the moderate rainfall, NO3(-) -N could reach 84.09% - 93.65% of DN. The different N fluxes were the highest under moderate rainfall among different rainfall events, in which the flux of total nitrogen (TN), DN, particle nitrogen (PN), ammonia (NH4(+) -N) and nitrite (NO2(-) -N) reached 737.17, 711.12, 26.06, 12.70 and 0.46 mg x m(-2), respectively, and the NO3(-)-N flux was as high as 686.12 mg x m(-2), showing a huge potential threat on groundwater health. Through the risk assessment on N pollution for groundwater quality, we concluded that the straw returning could be used to effectively alleviate the N leaching and groundwater N pollution; especially, the combined application of organic and chemical fertilizer could effectively mitigate the groundwater pollution, improve soil fertility and increase crop yield.

Chemical constituents from the stems of Gymnema sylvestre.

AIM: To study the chemical constituents of stems of Gymnema sylvestre (Retz.) Schult. METHODS: Chromatographic techniques using silica gel, C18 reversed phase silica gel, and prep-HPLC were used. The structures were elucidated on the basis of MS and spectroscopic analysis (1D and 2D NMR), as well as chemical methods. RESULTS: Seven compounds were isolated and their structures were elucidated as conduritol A (1), stigmasterol (2), lupeol (3), stigmasterol-3-O-ß-D-glucoside (4), the sodium salt of 22α-hydroxy-longispinogenin-3-O-ß-D-glucopyranosyl-(1→3)-ß-D-glu-curono-pyranosyl-28-O-α-L-rhamnopyranoside (5), oleanolic acid-3-O-ß-D-glucopyranosyl-(1→6)-ß-D-glucopyranoside (6), and the sodium salt of 22α-hydroxy-longispinogenin 3-O-ß-D-glucuronopyranosyl-28-O-α-L-rhamnopyranoside (7). The inhibition activities of compounds 1, 5-7 on non-enzymatic glycation of protein in vitro were evaluated. CONCLUSION: Compound 7 is a new triterpenoid saponin. It was shown that compounds 1, 5-7 have weak inhibition activities for non-enzymatic glycation of protein in vitro.

Study on chemical constituents of Cyclocarya paliurus.

A new dammarane triterpenoid glycoside named cyclocarioside J (1) and other three known triterpenoid glycosides were isolated from the leaves of Cyclocarya paliurus. Based on ESI-MS, HR-ESI-MS, (1)H NMR, (13)C NMR, and 2D NMR techniques including (1)H-(1)H COSY, HMBC, HMQC, and NOESY correlations, the structure of cyclocarioside J was elucidated as (20S,24R)-epoxydammarane 3ß,12ß,25-trihydroxy-12-O-ß-d-quinovopyranosyl-3-O-α-l-arabinopyranoside.

A new triterpenoid saponin from Gymnema sylvestre.

Besides four known compounds, a new triterpenoid saponin was isolated from the stems of Gymnema sylvestre. The structure of the new triterpenoid saponin was established as 3ß,16ß,22α-trihydroxy-olean-12-ene 3-O-ß-D-xylopyranosyl-(1 → 6)-ß-D-glucopyranosyl-(1 → 6)-ß-D-glucopyranoside (1) on the basis of 1D and 2D NMR techniques, including COSY, HMBC, HMQC, and NOESY correlations. Four known compounds 2, 3, 4, and 5 were identified on the basis of spectroscopic data.

Two new furostanol saponins from Tribulus terrestris.

Two new furostanol saponins were isolated from the fruits of Tribulus terrestris L. Their structures were established as 26-O-beta-D-glucopyranosyl-(25S)-5alpha-furost-20(22)-en-3beta,26-diol-3-O-alpha-L-rhamnopyranosyl-(1 --> 2)-[beta-D-glucopyranosyl-(1 --> 4)]-beta-D-galactopyranoside (1) and 26-O-beta-D-glucopyranosyl-(25S)-5alpha-furost-20(22)-en-12-one-3beta,26-diol-3-O-beta-D-galactopyranosyl-(1 --> 2)-beta-D-glucopyranosyl-(1 --> 4)-beta-D-galactopyranoside (2) on the basis of spectroscopic data as well as chemical evidence.

[Changes of plasma uPA and TGF-beta1 in patients with preeclampsia].

OBJECTIVE: To study the roles of uPA and TGF-beta1 in the etiology of preeclampsia (PE). METHODS: The plasma uPA and TGF-beta 1 were determined with enzyme linked immunosorbent assay (ELISA) in 70 patients with PE, and compared with those with normal pregnancy (n = 40). RESULTS: 1) The patients with PE had lower levels of plasma uPA (436.39 +/- 29.57) pg/mL than those with normal pregnancy [(646.54 +/- 35.39) pg/mL, P < 0.01]. No significant difference was found in the levels of plasma uPA between the patients with severe PE (417.11 +/- 48.47) pg/mL and the patients with mild PE [(468.81 +/- 14.91) pg/mL, P > 0.05]. 2) The patients with PE had higher levels of plasma TGF-beta1 (14.32 +/- 4.37) ng/mL than those with normal pregnancy [(9.85 +/- 3.19) ng/mL, P < 0. 05]. No significant difference was found in the levels of plasma TGF-beta1 between the patients with severe PE (15.37 +/- 4.93) ng/mL and the patients with mild PE [(11.21 +/- 2.32) ng/mL, P > 0.05)]. 3) There was a negative correlation between plasma uPA and plasma TGF-beta1 in the patients with PE (r = -0.497, P < 0.01). CONCLUSION: The changes of uPA and TGF-beta1 are associated with the occurrence and development of PE.

[Effect of cytoskeleton integrity on the expression of c-fos in osteoblasts induced by fluid shear stress].

OBJECTIVE: To investigate the effect of cytoskeleton integrity on the expression of c-fos gene in osteoblasts induced by fluid shear stress. METHODS: BALB/c mouse primary osteoblasts were divided into four groups (according to fluid shear stress loaded or not and cytochalasin D used or not). The Tagman probe real-time PCR and immunofluorescence were performed to detect the expression levels of c-fos mRNA, c-fos protein and cytoskeleton, respectively. The data were analysed using two-way ANOVA. RESULTS: In control group and cytochalasin D group, fluid shear stress could significantly increase the expression levels of c-fos mRNA (0.1637 +/- 0.0303 and 0.0104 +/- 0.0070, respectively) and protein (177.14 +/- 9.37 and 150.95 +/- 6.17, respectively) in osteoblasts, compared with the unloaded osteoblasts of the control group and the cytochalasin D group (0.0057 +/- 0.0021 and 0.0032 +/- 0.0014, respectively for c-fos mRNA, and 117.96 +/- 4.11 and 119.77 +/- 5.19, respectively for protein, P < 0.05). Induced by the fluid shear stress, the expression levels of c-fos mRNA and protein in cytochalasin D group were lower than control group, and the difference had statistical significance (P < 0.05). CONCLUSIONS: The cytoskeleton integrity in osteoblasts was essential to the expression of c-fos gene induced by fluid shear stress.

Two new steroidal glucosides from Tribulus terrestris L.

Two new furostanol saponins, tribufurosides D (1) and E (2), were isolated from the fruits of Tribulus terrestris L. With the help of chemical and spectral analyses (IR, MS, 1D, and 2D NMR), the structures of the two new furostanol saponins were established as 26-O-beta-d-glucopyranosyl-(25S)-5alpha-furost-12-one-2alpha,3beta,22alpha,26-tetraol-3-O-beta-d-glucopyranosyl-(1 --> 4)-beta-d-galactopyranoside (1) and 26-O-beta-d-glucopyranosyl-(25R)-5alpha-furost-12-one-2alpha,3beta,22alpha,26-tetraol-3-O-beta-d-glucopyranosyl-(1 --> 4)-beta-d-galactopyranoside (2).

[Correlation of toll-like receptor 3 and tumor necrosis factor-alpha with idiopathic fetal growth restriction.].

OBJECTIVE: To investigate the expression and the significance of toll-like receptor 3 (TLR-3) in placenta, tumor necrosis factor-alpha(TNF-alpha) in maternal and cord blood of idiopathic fetal growth restriction (IFGR), and their correlation with the pathogenesis of symmetric and asymmetric IFGR. METHODS: From April 2008 to April 2009, 42 primiparae of singleton pregnancy and their IFGR babies, who delivered at term through cesarean section, in the Third Affiliated Hospital of Zhengzhou University were enrolled. All subjectects were divided into symmetric IFGR group (n = 20) and asymmetric IFGR group (n = 22). Another 42 non-IFGR pairs were randomly selected as the control group. The polink-2 plus polymerized horseradish peroxidase (HRP) immunohistochemical method and the enzyme linked immunosorbent assay (ELISA) were applied to detect TLR-3 and TNF-alpha levels. RESULTS: (1) The expression of TLR-3 protein were observed in all maternal placenta of the three groups. TLR-3 essentially expressed in syncytiotrophoblasts and hofbouer cells in the symmetric IFGR and control group, but expressed mostly in hofbouer cells and less in syncytiotrophoblasts in the asymmetric IFGR group. (2) The expression of TLR-3 in the syncytiotrophoblasts of the symmetric and asymmetric IFGR group was significantly lower than in the control group (111 +/- 14 and 118 +/- 11 vs. 156 +/- 9, P < 0.01). The number of TLR-3 positive in Hofbourer cell in the symmetric IFGR group was lower than the control group (8.9 +/- 2.8 vs 17.5 +/- 2.8, P < 0.01), but the number in the asymmetric IFGR group was higher (23.8 +/- 3.7) compared with the control group (P < 0.01). (3) The TNF-alpha levels in the maternal and cord blood of the symmetric and the asymmetric group were higher than that of the control group [maternal: (90 +/- 10) microg/L and (86 +/- 11) microg/L vs. (73 +/- 9) microg/L; cord blood: (92 +/- 12) microg/L and (96 +/- 8) microg/L vs. (79 +/- 9) microg/L; P < 0.01]. (4) Neither symmetric nor the asymmetric IFGR group showed any correlations between the maternal and cord blood levels of TNF-alpha (P > 0.05). (5) Significant correlation was found between the TNF-alpha level of the cord blood and TLR-3 expression in the placenta in both the symmetric and asymmetric IFGR group (P < 0.05), but no relationship was found between the maternal blood TNF-alpha level and TLR-3 expression in the placenta (P > 0.05). CONCLUSIONS: The variantions of TLR-3 expression in placenta and the increased expression of TNF-alpha in cord blood are associated with the genesis IFGR. The reduced expression of TLR-3 may related to symmetric IFGR, while the increased TLR-3 level in hofbouer cells may lead to asymmetric IFGR.

A novel triterpenoid saponin from Polygala tenuifolia Willd.

A new triterpenoid saponin, tenuifoside A, was isolated together with three known triterpenoid saponins 2, 3, and 4 from the roots of Polygala tenuifolia Willd. With the help of chemical and spectral analyses (IR, MS, 1D-NMR, and 2D-NMR), the structure of the new saponin was elucidated as 3-O-beta-d-glucopyranosyl presenegenin 28-O-beta-d-xylopyranosyl-(1 --> 3)-beta-d-xylopyranosyl-(1 --> 4)-[beta-D-apiofuranosyl-(1 --> 3)]-alpha-L-rhamnopyranosyl-(1 --> 2)-[4-O-p-methoxycinnamoyl]-[alpha-l-rhamnopyranosyl-(1 --> 3)]-beta-d-fucopyranosyl ester (1). Three known triterpenoid saponins (2-4) were identified on the basis of spectroscopic data.

A new triterpenoid saponin from Albizia julibrissin Durazz.

A new triterpenoid, saponin hehuanoside A, was isolated together with the known triterpenoid saponins 2, 3, and 4 from the stem bark of Albizia julibrissin. With the help of chemical and spectral analyzes (IR, MS, 1D-NMR, and 2D-NMR), the structure of the new triterpenoid saponin was elucidated as 21-O-[(6S)-2-trans-2,6-dimethyl-6-O-beta-d-quinovopyranosyl-2,7-octadienoyl]-3-O-beta-d-xylopyranosyl-(1 --> 2)-beta-d-fucopyranosyl-(1 --> 6)-beta-d-2-deoxy-2-acetamidoglucopyrasyl acacic acid 28-O-alpha-l-arabinofuranosyl-(1 --> 4)-[-beta-d-glucopyranosyl-(1 --> 3)]-alpha-l-rhamnopyranosyl-(1 --> 2)-beta-d-glucopyranosyl ester (1). Three known triterpenoid saponins 2-4 were identified on the basis of spectroscopic data.

Two new furostanol saponins from Tribulus terrestris L.

Two new furostanol saponins, tribufurosides B (1) and C (2), were isolated from the fruits of Tribulus terrestris L. With the help of chemical and spectral analyses (IR, MS, 1D NMR and 2D NMR), the structures of two new furostanol saponins were established as 26-O-beta-d-glucopyranosyl-(25S)-5alpha-furost-20(22)-en-2alpha,3beta,26-triol-3-O-beta-d-galactopyranosyl(1 --> 2)-beta-d-glucopyranosyl(1 --> 2)-beta-d-galactopyranoside (1) and (25S)-5alpha-furost-20(22)-en-12-one-3beta, 26-diol-26-O-beta-d-glucopyranoside (2).

A novel steroidal glycoside, ophiofurospiside A from Ophiopogon japonicus (Thunb.) Ker-Gawl.

A new furospirostanol saponin, ophiofurospiside A (1), was isolated together with the known steroidal glycosides 2, 3, and 4 from the tubers of Ophiopogon japonicus (Thunb.) Ker-Gawl. Using chemical and spectral analyses (IR, MS, 1D NMR, and 2D NMR), the structure of 1 was established as 26-O-beta-d-glucopyranosyl-(22S, 25R)-furospirost-5-ene-3beta, 17alpha, 26-triol-3-O-[alpha-l-rhamnopyranosyl-(1 --> 2)]-[beta-d-xylopyranosyl-(1 --> 4)]-glucopyranoside (1). Three known steroidal saponins 2-4 were identified on the basis of spectroscopic data.

Two new triterpenoid saponins from Pulsatilla cernua (Thunb.) Bercht. et Opiz.

Two new triterpenoid saponins, named cernuaside C and D, have been isolated from Pulsatilla cernua (Thunb.) Bercht. et Opiz. The structures of the two new triterpenoid saponins were elucidated as 3-O-beta-D-xylopyranosyl(1 --> 2)-[alpha-L-rhamnopyranosyl(1 --> 3)]-alpha-L-arabinopyranosyl oleanolic acid 28-alpha-L-rhamnopyranosyl(1 --> 4)-beta-D-glucopyranosyl(1 --> 6)-beta-D-glucopyranoside. (1) and 3-O-alpha-L-arabinopyranosyl (1 --> 3)-alpha-L-rhamnopyranosyl(1 --> 2)-alpha-L-arabinopyranosyl oleanolic acid 28-O-beta-D-glucopyranoside (2) by 1D, 2D-NMR techniques, ESI-MS analysis as well as chemical methods.