Sesquiterpenoids and Cytochalasins with Immunosuppressive Activity from Sonchus wightianus.

The plant species, Sonchus wightianus DC., was historically used in China for both medicinal and dietary uses. In present study, seven new guaiane sesquiterpenoids (1-7) and one cytochalasin (8), along with five known guaianes (9-13) and two known cytochalasins (14 and 15), were isolated from the whole plants of S. wightianus. These guaianes showed structural variations in the substituents at C-8 and/or C-15, and compounds 6 and 7 are two sesquiterpenoid glycoside derivatives. Their structures were determined by extensive analysis of spectroscopic, electronic circular dichroism, and X-ray diffraction data, and chemical method. Biological tests revealed that compounds 5 and 8 are potent and selective immunosuppressive reagents.

Diterpenoids from Sauropus spatulifolius Leaves with Antimicrobial Activities.

As a plant used in both food and medicine, Sauropus spatulifolius is consumed widely as a natural herbal tea, food source, and Chinese medicine. Inspired by its extensive applications, we conducted a systematic phytochemical study of the leaves of S. spatulifolius. Thirteen new diterpenoids, sauspatulifols A-M (1-13), including four ent-cleistanthane-type diterpenoids (1-4), eight 15,16-di-nor-ent-cleistanthane-type diterpenoids (5-12), and one 17-nor-ent-pimarane-type diterpenoid (13) as well as one known diterpenoid, cleistanthol (14), were isolated. All of these diterpenoids feature a 2α,3α-dihydroxy unit within the A ring, and their structures were elucidated by spectroscopic data analysis, electronic circular dichroism calculations, and single-crystal X-ray diffraction analysis. Compound 14 displayed moderate inhibitory activity against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, and Shigella flexneri with the same minimum inhibitory concentration value of 12 µg/mL as well as activity against vesicular stomatitis virus and influenza A virus.

Isolation, purification and structural characterization of two pectin-type polysaccharides from Coreopsis tinctoria Nutt. and their proliferation activities on RAW264.7 cells.

Coreopsis tinctoria Nutt. (C.tinctoria) is an annual herb of the Compositae family with many health benefits, such as clearing heat, antioxidant and anticancer activity. In this paper, two polysaccharides were isolated from C.tinctoria, named CTAP-1 and CTAP-2, respectively. Structure of CTAP-1and CTAP-2 were elucidated by high-performance gel permeation chromatography, chemical derivative analyses, GC-MS and NMR techniques. Results reveal that they both CTAP-1 and CTAP-2 consisted of predominant amounts of galacturonic acid residues along with small amounts of arabinose, rhamnose and galactose.Both them contain homogalacturonan and rhammnogalcturan I regions in different ratio, suggesting their pectin-type features. The proliferation activities of CTAP-1 and CTAP-2 on RAW264.7 cells in vitro were detected. Results show both them have the significant proliferation effect on RAW264.7 cells when the concentration from 40 to 200 µg/mL. Given their structural characteristics and proliferation activities, the pectins are expected to be potential natural immune modulators, which need further study.

Ginsenoside Rd attenuates mitochondrial permeability transition and cytochrome C release in isolated spinal cord mitochondria: involvement of kinase-mediated pathways.

Ginsenoside Rd (Rd), one of the main active ingredients in Panax ginseng, has multifunctional activity via different mechanisms and neuroprotective effects that are exerted probably via its antioxidant or free radical scavenger action. However, the effects of Rd on spinal cord mitochondrial dysfunction and underlying mechanisms are still obscure. In this study, we sought to investigate the in vitro effects of Rd on mitochondrial integrity and redox balance in isolated spinal cord mitochondria. We verified that Ca2+ dissipated the membrane potential, provoked mitochondrial swelling and decreased NAD(P)H matrix content, which were all attenuated by Rd pretreatment in a dose-dependent manner. In contrast, Rd was not able to inhibit Ca2+ induced mitochondrial hydrogen peroxide generation. The results of Western blot showed that Rd significantly increased the expression of p-Akt and p-ERK, but had no effects on phosphorylation of PKC and p38. In addition, Rd treatment significantly attenuated Ca2+ induced cytochrome c release, which was partly reversed by antagonists of Akt and ERK, but not p-38 inhibitor. The effects of bisindolylmaleimide, a PKC inhibitor, on Rd-induced inhibition of cytochrome c release seem to be at the level of its own detrimental activity on mitochondrial function. Furthermore, we also found that pretreatment with Rd in vivo (10 and 50 mg/kg) protected spinal cord mitochondria against Ca2+ induced mitochondrial membrane potential dissipation and cytochrome c release. It is concluded that Rd regulate mitochondrial permeability transition pore formation and cytochrome c release through protein kinases dependent mechanism involving activation of intramitochondrial Akt and ERK pathways.

[Water holding characteristics of litters of typical forest in loess area of Western Shanxi Province, China]. / æ™‹è¥¿é»„åœŸåŒºå ¸åž‹æž—åˆ†æž¯è½ç‰©æŒæ°´ç‰¹æ€§.

It is of great significance to investigate the volume and water holding characteristics of litters for the accurate evaluation of forest water conservation function. With Pinus tabuliformis, Robinia pseudoacacia, Populus davidiana, Quercus wutaishanica and Platycladus orientalis as the research objects in the Loess Plateau of Western Shanxi Province, we analyzed the thickness of undecomposed layer and semi-decomposed layer, the volume of litter, and the relationship between the litter water-holding characteristics and the immersion time for different stands by the combination of sample survey and indoor immersion test. The results showed that the total thickness of litter layer was 4.06-5.12 cm, with the thickest layer in R. pseudoacacia forest and the thinnest in P. tabuliformis forest. The storage volume of litter was the largest in Q. wutaishanica (24.39 t·hm-2), followed by P. davidiana (23.64 t·hm-2), P. orientalis (22.51 t·hm-2), and R. pseudoacacia (22.48 t·hm-2), and the smallest in P. tabuliformis (20.42 t·hm-2). The volume in the undecomposed layer was less than that in the semi-decomposed layer. The maximum water holding of litter was 40.41-79.56 t·hm-2, with the highest of Q. wutaishanica and the lowest of P. tabuliformis. The effective interception rate of litter was 108%-188%. The changes of water capacity and water absorption rate of litter were most rapid in Q. wutaishanica, P. davidiana and R. pseudoacacia, and the changes were faster in the semi-decomposed layer than in the undecomposed layer. The water-holding capacity of litter in five forests was following an order of Q. wutaishanica>P. davidiana>R. pseudoacacia>P. orientalis>P. tabuliformis.

Tumor-derived exosomal circRNA_102481 contributes to EGFR-TKIs resistance via the miR-30a-5p/ROR1 axis in non-small cell lung cancer.

Exosomes are messengers for intercellular communication and signal transduction. Circular RNA (circRNA) abnormal expression and regulation are involved in the occurrence and development of a variety of tumors. In the present study, exosomes in the serum of five patients with non-small cell lung cancer (NSCLC) were isolated before and after EGFR-TKIs resistance, and the circRNA expression profile was screened using a circRNA microarray. The effects of the exosome circRNA_102481 on cell proliferation and apoptosis were analyzed. The interaction between miR-30a-5p and circRNA_102481 or ROR1 was predicted by starBase software, and was confirmed by RNA pull-down and dual-luciferase reporter assays. The results showed that exosomes containing circRNA_102481 were significantly up-regulated in NSCLC with EGFR-TKIs resistance (p<0.05), and that circRNA_102481 was mainly secreted by EGFR-TKIs resistance cell via exosomes (p<0.05). Both circRNA_102481 silencing and si-circRNA_102481 transported by exosomes could inhibit EGFR-TKIs resistance cell proliferation and promote cell apoptosis and circRNA_102481 overexpression could promote EGFR-TKIs sensitive cell proliferation and inhibit cell apoptosis in vitro (p<0.05). CircRNA_102481 served as a miR-30a-5p sponge to regulate ROR1 expression (p<0.05). Furthermore, the expression of circRNA_102481 in exosomes was associated with TNM stage, tumor differentiation status, brain metastasis, and PFS and OS duration. Therefore, it was concluded that tumor-derived exosomal circRNA_ 102481 could contribute to EGFR-TKIs resistance via the microRNA-30a-5p/ROR1 axis in NSCLC. Exosomal circRNA_102481 may serve as a novel diagnostic biomarker and a therapeutic target for EGFR-TKIs resistance in NSCLC.

[A comparative study of survival time of surgery combined with chemotherapy and non-surgical chemotherapy in SCLC].

OBJECTIVE: To compare the survival time of surgery combine with chemotherapy with non-surgery chemotherapy in SCLC. METHODS: 37 SCLC post operation patients were received 4-6 cycles of chemotherapy of "etoposide + cisplatin or carboplatin". 37 SCLC patients were selected be control group, whose age, stage and site of tumor were similar to surgery combine with chemotherapy group, and received 6 cycles of chemotherapy of "etoposide + cisplatin or carboplatin". Two groups were followed up 5 year and compared with the survival time. RESULTS: The 1, 3, 5 year survival rate of surgery combined with chemotherapy group were 72.97%, 35.13%, 21.62%. The 1, 3, 5 year survival rate of control group were 54.05%, 13.51%, 5.41%. The survival rate of stage I (P = 0.01) was significantly different, but stage II (P = 0.06) and stage III (P = 0.836) were no difference between the two group of SCLC. CONCLUSION: It was found that surgery combined with chemotherapy got satisfactory effects in stage I SCLC.

Isolation, purification, and structural characterization of polysaccharides from Atractylodis Macrocephalae Rhizoma and their immunostimulatory activity in RAW264.7 cells.

Three water-soluble polysaccharides (AMAP-1, AMAP-2 and AMAP-3) were isolated and purified from Atractylodis Macrocephalae Rhizoma by using the combination of ion-exchange chromatography and gel permeation chromatography. The structures of the polysaccharides were characterized by chemical derivatization, HPGC, GC-MS, FT-IR, and NMR techniques. Structural analyses show that the three polysaccharides are pectin-type macromolecules consisting of homogalacturonan (HG) and rhamnogalacturonan type I (RG-I) regions in different ratios. Immunostimulatory assay highlighted that the RG-I-rich AMAP-1 and AMAP-2 with high molecular weights can stimulate RAW264.7 macrophages to release nitric oxide, but HG-rich AMAP-3 with a low molecular weight cannot. This finding suggests that the immune activity may be related to the side chains of the RG-I region, which provides a certain theoretical guidance for further exploring the structure-activity relationship. Meanwhile, AMAP-1 and AMAP-2, especially AMAP-2, from Atractylodis Macrocephalae Rhizoma show potential as immune adjuvants.

Structural characterization and antiviral activity of two fucoidans from the brown algae Sargassum henslowianum.

Purified fucoidans SHAP-1 and SHAP-2 with apparent molecular weights of 6.55 × 105 and 5.89 × 105, respectively, were isolated from Sargassum henslowianum by ion-exchange and gel-filtration column chromatography. They are both composed of fucose and galactose at a ratio of around 3:1 and 31.9% sulfate. The backbone of two fucoidans consists of α-(1→3)-linked L-Fucp residues which are mainly sulfated on the C-2 and C-4 positions. Side chains composed of terminally linked α-L-Fucp and α-D-Galp residues, and (1→2)-, (1→6)-, and (1→2,6)-linked ß-D-Galp residues attach mainly at O-4 position of backbone residues. Antiviral test showed that the IC50 values of SHAP-1 and SHAP-2 against HSV-1 were estimated to be 0.89 and 0.82 µg/mL by plaque reduction assay, respectively, whereas both as low as 0.48 µg/mL against HSV-2. The antiviral mechanism of the fucoidans might be at least through blocking HSV-2 virion adsorption to host cells. These results suggest that the fucoidans have potential clinical applications.

Structural characterization of three polysaccharides from the roots of Codonopsis pilosula and their immunomodulatory effects on RAW264.7 macrophages.

Three polysaccharides were isolated from the roots of Codonopsis pilosula by ion-exchange and gel-filtration chromatography. They were named RCNP, RCAP-1, and RCAP-2, and had apparent molecular weights of 1.14 × 104, 5.09 × 104, and 2.58 × 105, respectively. Their structures were characterized by HPGPC, chemical derivative analysis, GC-MS and NMR analyses. Results showed that RCNP contained arabinan and arabinogalactan regions. The arabinan region had a main chain comprising (1 → 5)-linked Araf residues, and the side chains branched at the O-3 position by the single Araf residues. The arabinogalactan region comprised alternating (1 → 4)-, (1 → 6)- or (1 → 3)-linked Galp along with small amounts of branches mainly at the O-3 position of the (1 → 6)-linked Galp or O-6 position of the (1 → 3)-linked Galp residues by terminally linked Araf residues. RCAP-1 and RCAP-2 were highly methyl-esterified pectin-type polysaccharides with long homogalacturonan regions interrupted by a short rhamnogalacturonan I (RG-I) region. The side chains of the RG-I region consisted of (1 → 2)-linked Rha residues attached to the position O-4 of rhamnose. Their degrees of methyl-esterification were approximately 60.6% and 68.1%, respectively. Bioactivity tests showed that RCAP-1 and RCAP-2 exerted a significant immunostimulatory effect based on NO production from RAW264.7 macrophages. These results suggested that these two pectin-type polysaccharides were potential immunostimulation agents.

[Effects of irrigation regimes on the variation of soil water and salt and yield of mechanically harvested cotton in Southern Xinjiang, China]. / 南疆机采棉田灌溉制度对土壤水盐变化和棉花产量的影响.

The expansion of soil salinization area is a threat to cotton production in Southern Xinjiang. How to control soil salt accumulation by developing precise irrigation strategy is currently a hot topic for the film mulching drip-irrigated cotton field. With aims for soil quality improvement and high yield, we investigated the effects of irrigation regimes on soil water and salt distribution, yield and fiber quality in major cotton production area of Southern Xinjiang. Results showed that the increase of irrigation amount contributed to a higher cotton photosynthetic product accumulation, but had no significant effect on the ratio of reproductive organs to total biomass. The degree of soil desa-lination had a positive correlation with the irrigation quotas. When the seasonal total irrigation amount exceeded 2577.83 m3·hm-2, soil salinization would not deteriorate. Irrigation amount had significant effect on WUEI, but had no effect on fiber quality. With the increasing of irrigation amount, cotton yield increased first and then decreased. In conclusion, applying 4200 m3·hm-2 seasonal irrigation amount in total and 7 d and 5 d irrigation interval for the budding and flowering stage respectively could be a suitable irrigation regime for mechanically-harvested cotton in the arid area of Southern Xinjiang.

[Modeling evapotranspiration of greenhouse tomato under different water conditions based on the dual crop coefficient method]. / åŸºäºŽåŒä½œç‰©ç³»æ•°æ³•ä¼°ç®—ä¸åŒæ°´åˆ†æ¡ä»¶ä¸‹æ¸©å®¤ç•ªèŒ„è’¸å‘è’¸è ¾é‡.

An experiment was conducted to investigate soil evaporation (E), crop transpiration (T), evapotranspiration (ET) and the ratio of evaporation to evapotranspiration (E/ET) of drip-irrigated tomato, which was planted in a typical solar greenhouse in the North China, under different water conditions [irrigation amount was determined based on accumulated pan evaporation (Ep) of 20 cm pan evaporation, and two treatments were designed with full irrigation (0.9Ep) and deficit irrigation (0.5Ep)] at different growth stages in 2015 and 2016 at Xinxiang Comprehensive Experimental Station, Chinese Academy of Agricultural Sciences. Effects of deficit irrigation on crop coefficient (Kc) and variation of water stress coefficient (Ks) throughout the growing season were also discussed. E, T and ET of tomato were calculated with a dual crop coefficient approach, and compared with the measured data. Results indicated that E in the full irrigation was 21.5% and 20.4% higher than that in the deficit irrigation in 2015 and 2016, respectively, accounting for 24.0% and 25.0% of ET in the whole growing season. The maximum E/ET was measured in the initial stage of tomato, while the minimum obtained in the middle stage. The Kc the full irrigation was 0.45, 0.89, 1.06 and 0.93 in the initial, development, middle, and late stage of tomato, and 0.45, 0.89, 0.87 and 0.41 the deficit irrigation. The Ks the deficit irrigation was 0.98, 0.93, 0.78 and 0.39 in the initial, development, middle, and late stage, respectively. The dual crop coefficient method could accurately estimate ET of greenhouse tomato under different water conditions in 2015 and 2016 seasons with the mean absolute error (MAE) of 0.36-0.48 mm·d-1, root mean square error (RMSE) of 0.44-0.65 mm·d-1. The method also estimated E and T accurately with MAE of 0.15-0.19 and 0.26-0.56 mm·d-1, and with RMSE of 0.20-0.24 and 0.33-0.72 mm·d-1, respectively.

[Relationship between quinone oxidoreductase1 gene ns-cSNP and genetic susceptibility of esophageal cancer].

OBJECTIVE: To explore the relationship between quinone oxidoreductase1 (NQO1) gene nonsynonymous cSNP and the genetic susceptibility of esophageal cancer. METHODS: Polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) and Allele-Specific PCR (AS-PCR) were employed to assess the polymorphism of NQO1 genes both in 106 patients with esophageal cancer and control subjects matched by age, gender and origin. RESULTS: It was shown that no C/C genotype was found at 406 of NQO1. The allelic frequency of NQO1 609T was significantly higher in patients with esophageal cancer than in the control subjects (P < 0.005) and the individuals with 609T allelic genotype of NQO1 gene were at greater risk to develop esophageal cancer (OR = 4.76, 95% CI = 1.064 - 3.397). But Individuals with mutant allele of NQO1 465 genotype did not show the rising risk of esophageal cancer. CONCLUSIONS: The NQO1 C609T polymorphisms should likely be associated with the genetic susceptibility of esophageal cancer.

Clinicopathologic significance of ß-catenin and matrix metalloproteinase-2 expression in non-small cell lung cancer.

The purpose of this study was to analyze ß-catenin and matrix metalloproteinase-2 (MMP-2) expression in non-small cell lung cancer (NSCLC) and to investigate the association between their expression and clinicopathologic characteristics of NSCLC patients. Immunohistochemistry was performed to examine ß-catenin and MMP-2 protein expression in 39 resected NSCLC samples and 8 adjacent normal lung tissues. Statistical analysis with SPSS13.0 software was performed to investigate the association between ß-catenin and MMP-2 expression and clinicopathologic features of the patients. Expression of cytosolic ß-catenin in NSCLC tissue was significantly higher than that in normal tissues (P < 0.001). In addition, cytosolic protein expression of ß-catenin in lung squamous cell carcinoma was significantly elevated compared to that in lung adenocarcinoma (P = 0.02). However, cell membrane protein expression of ß-catenin in squamous cell carcinoma was lower than that in adenocarcinoma (P = 0.041). Cytosolic MMP-2 protein expression in NSCLC samples was significantly higher than that in normal tissues (P = 0.002). MMP-2 expression in N (1-2) NSCLC patients was significantly increased relative to N (0) patients (P = 0.019). However, statistical analysis showed no correlation between ß-catenin and MMP-2 expression in NSCLC samples. Collectively, our results show that cytosolic protein expression of ß-catenin in NSCLC samples is increased relative to normal lung tissues. Also, expression of ß-catenin is significantly elevated in squamous cell carcinoma compared to that in lung adenocarcinoma subtypes. Additionally, MMP-2 expression in N (1-2) NSCLC tissues is higher than that in N (0) lung tissue. There is no correlation between ß-catenin and MMP-2 expression in NSCLC, and our study suggests that evaluation of ß-catenin and MMP-2 expression may have potential in diagnosis and progression in patients with NSCLC.