Expression of Concern: Conjugation of substituted naphthalimides to polyamines as cytotoxic agents targeting the Akt/mTOR signal pathway.

Expression of Concern for 'Conjugation of substituted naphthalimides to polyamines as cytotoxic agents targeting the Akt/mTOR signal pathway' by Zhi-Yong Tian et al., Org. Biomol. Chem., 2009, 7, 4651-4660, https://doi.org/10.1039/B912685F.

[Research progress on chemical compositions and pharmacological action of Drynariae Rhizoma].

Drynariae Rhizoma is warm in nature and bitter in taste, mainly acting on liver and kidney systems. It is a common Chinese herbal medicine for the treatment of fracture and bone injury. The chemical compositions of Drynariae Rhizoma mainly include flavonoids, triterpenoids, phenylpropanoids and lignans. At present, modern pharmacological and clinical studies have shown that Drynariae Rhizoma has the effects of anti osteoporosis, promoting fracture healing, kidney protection, anti-inflammatory, promoting tooth growth, preventing and treating aminoglycoside ototoxicity and lowering blood lipid. In addition, the toxicity evaluation experiment of Drynariae Rhizoma has also shown that it has no obvious toxic and side effects. Naringin is a kind of dihydroflavone in Drynariae Rhizoma. Many studies have shown that naringin and other total flavonoids play an important role in anti-osteoporosis, promoting fracture healing, anti-inflammation, promoting tooth growth and lowering blood lipid. In this study, the research progresses on chemical consti-tuents and pharmacological activities of Drynariae Rhizoma in recent years were reviewed, and some mechanisms of action were summarized, to provide references for the further research and development of Drynariae Rhizoma.

[Killing effect of Huaier combined with DC-CIK on nude mice bearing colon cancer HT29 stem cells in vivo].

To compare the therapeutic effects of different treatment methods on the nude mice bearing colon cancer HT29 cells. BalB/C nude mice colon cancer stem cell models were established and randomly divided into the following four groups, with 8 nude mice in each group: blank control group, DC-CIK group, Huaier group, and Huaier combined with DC-CIK group (combined treatment group). The mice in DC-CIK group and combined treatment group received 1×106 DC-CIK cells treatment by tail vein injectionafter the tumor stem cells were inoculated for 4 days,2 times a week for three weeks. The mice in Huaier group and combined treatment group received intragastric administration at the dose of 20 g/60 kg body weight, 0.2 mL/time, once a day for a total of three weeks. The mice in control group received equal volume of normal saline. Tumor size and body weight of nude mice were measured every 2 days during treatment for three weeks in each group. After the treatment, the nude mice were sacrificed to measure the tumor weight and the tumor inhibition rate was calculated. The RT-PCR method was used to detect the expression levels of the key genes in the signal pathway. After the end of the treatment, the quality of the tumor in the Huaier group, DC-CIK group and combined treatment group was significantly lower than that in the control group; the quality in combined treatment group was significantly lower than that in Huaier group and DC-CIK group.Among them, the tumor inhibition rate reached 46.77% in the combined treatment group. In respect of changes in expression levels of key genes in the signaling pathway, the mRNA expression levels of key genes PI3KR1 and Akt in PI3K/Akt pathway, key genes Wnt1 and CTTNB1 in Wnt/ß-catenin pathway, and key genes Notch1, Notch2, Notch3 in Notch pathway in the combined treatment group were lower than those in DC-CIK group and Huaier group. The Huaier combined with DC-CIK group showed best therapeutic effect among different treatment methods for HT29 stemcell colon tumors in nude mice, providing a new idea for clinical treatment of colon cancer.

Time-cumulated blood pressure exposure and incident impairment of glucose tolerance and diabetes mellitus.

BACKGROUND: With the marked increase in the prevalence of diabetes mellitus, it was the purpose of our study to assess a potential association of time-cumulated exposure to systolic (CumSBP) and of diastolic blood pressure (CumDBP) with onset of impaired glucose tolerance and diabetes mellitus. METHODS: The prospective investigation included participants of the longitudinal Kailuan Study with three baseline examinations in 2006-2007, 2008-2009 and 2010-2011, re-examination in 2012-2013, and no diabetes mellitus at baseline. Cumulative blood pressure (BP) was calculated as cumBP = [(BP1 + BP2)/2 × time1-2] + [(BP2 + BP3)/2 × time2-3]. Based on cumSBP, the study population was stratified into four groups (cumSBP < 480mmHgxyear;n = 15,339; 480mmHgxyear ≤ cumSBP < 520mmHgxyear;n = 7214; 520mmHgxyears ≤ cumSBP < 560mmHgxyears;n = 5675; and cumSBP ≥ 560mmHgxyears;n = 10,576). RESULTS: After adjusting for demographic, anthropomorphic, biochemical, socioeconomic and lifestyle parameters and as compared with the first group, the second, third and fourth group showed a significantly higher incidence of diabetes (P-trend < 0.001;hazard ratio (HR);95% confidence interval (CI):1.28(1.08,1.51),1.54(1.29,1.84), and 2.33(1.98,2.73), respectively), higher incidence of impairment of glucose tolerance (P-trend < 0.001;HR;95% CI1.17(1.02,1.33), 1.43(1.25,1.64), and 2.09(1.85,2.37), respectively), and higher incidence of diabetes developing out of an impairment of glucose tolerance (P-trend < 0.001;HR;95% CI:1.22(0.97,1.54),1.47(1.16,1.86), and 2.01(1.62,2.50), respectively). An increase in cumSBP by 10 mmHg/year or an increase in cumDBP by 5 mmHg/year was associated with a hazard ratio of incident diabetes of 1.04 (95% CI:1.03,1.04) and 1.02(1.02,1.03), respectively, with a hazard ratio of incident impairment of glucose tolerance of 1.04(95% CI:1.03,1.04) and 1.03(95% CI:1.02,1.03), respectively, and with a hazard ratio of incident diabetes developing from impairment of glucose tolerance of 1.04(95% CI:1.03,1.04) and 1.03(95% CI:1.02,1.03), respectively. CONCLUSIONS: Time-cumulated exposure to elevated blood pressure was significantly associated with an elevated incidence of impaired glucose tolerance and diabetes.

[Application of plant tissue culture in field of Chinese medicine resources].

Plant tissue culture technology has been widely used in the field of traditional Chinese medicine(TCM) resources with its unique advantages, playing an important role in the protection of TCM resources. In this review, some applications of plant tissue culture were summarized, including production of active compounds by using plant tissue culture, genetic diversity analysis, Dao-di herbs, elicitor application, biosynthesis and transgenic plants. Through the above researches will promote the further development of plant tissue culture technology, making it play a greater role in the field of TCM resources.

[A survey on ecological environment of wild Adiantum reniforme var. sinense in Three Gorges Reservoir region].

The study aims at investigating the ecological environment Adiantum reniforme var. sinense of in Three Gorges Reservoir region, and providing a reference basis for the protection of resources and artificial cultivation of A. reniforme var. sinense. By using the method of investigation, field survey and experimental analysis, the vegetation, natural geographical environment, climate, soil nutrients of A. reniforme var. sinense were studied and analyzed. The survey found that A. reniforme var. sinense distribution area reduced fast in Three Gorges region, a lot of distribution has diminished and vanished due to excessive digging, currently only in 3 towns of Wanzhou there exist 4 wild distribution areas. The growth of A. reniforme var. sinense needs an environment with low altitude, steep slope and thin soil, northeast slope, canopy height and warm and humid climate characteristics, and the soil in distribution has the characteristics of high organic matter, available nitrogen, available potassium, and low available phosphorus content.

[Characterization of tissue expression of ginsenoside biosynthetic gene expression in Panax ginseng].

The study is aimed to characterize the tissue expression of 10 key ginsenoside biosynthetic genes using bioinformatics method and real-time quantitative PCR. Heatmap and cluster analysis of 10 ginsenoside biosynthetic genes were performed in four-year-old Jilin ginseng. Using real-time quantitative PCR, the expression correlation of 10 key genes involved in ginsenoside biosynthesis was analyzed in different organs of four-year-old Jilin ginseng including, tissue culture seedling and adventitious root. Pearson correlation was used to analyze the relation between those 10 key genes involved in ginsenoside biosynthesis. The results showed that ß-AS and CYP716A52v2 were expressed highly in root of Jilin ginseng and ginseng culture seedling, which was consistent with Ro distribution. In addition, CYP716A53v2 and CYP716A47 which involved in dammarane type ginsenoside biosynthesis were positively correlated, which revealed that the difference of ginsenoside distribution was caused by transport system.

[Pharmacokinetics of magnolol and honokiol in Weichang'an pill].

To conduct multiple-reaction monitoring(MRM) quantitative analysis with high-performance liquid chromatography coupled with mass spectrometry method, establish the quantification method of magnolol and honokiol in blood sample under negative ion mode with ibuprofen as internal standard, investigate the pharmacokinetic process of lignans constituents after oral administration of Weichang'an pill(WCA) at different doses, and provide theoretical basis to further reveal the material basis of WCA's anti-diarrhea effect. In the plasma samples, the linear relationship was good over the concentration range of 5.25 to 1 344.00 µg•L ⁻¹ for magnolol and 10.08 to 2 580.00 µg•L ⁻¹ for honokiol. The results of precision, stability, and extraction recovery tests showed that the determination method of plasma concentration for such compositions was stable and reliable. Dose-dependence was shown for magnolol and honokiol in the plasma concentration-time profile. The results indicated that the time to reach the maximum plasma concentration(Tmax) for lignanoids was 0.55-1.42 h, when the maximum plasma concentration(Cmax) could reach 996.36-2 330.96,189.87-1 469.43 µg•L ⁻¹ respectively for magnolol and honokiol. The lignanoids could be absorbed rapidly in the blood after oral administration of WAC pills, providing experimental basis to prove rapid and long-acting anti-diarrhea effect of WAC pills after oral administration.

Comparison of starches from five plants of Sect. Stenophora Uline and Sect. Lasiophyton Uline of Dioscorea grown in China.

BACKGROUND: Dioscorea resources with vital medicinal and functional values are abundant in south-west regions of China, especially in Sichuan Province. However, the resource in this region has received less attention compared with that of the north. D. zingiberensis, D. collettii, D. kamoonensis cv. Emei and Jinfo, and D. melanophyma from Sichuan Province and Chongqing City were studied with regard to the most abundant carbohydrate (starch) to search for new medicinal and food resources. RESULTS: The starches were small round granules or small oval granules and large elongated granules, except D. zingiberensis starch granules, which were disc-like in shape. D. zingiberensis and D. collettii starches showed higher values in total starch content, water-binding capacity and infrared ratio of absorbance bands at 1047/1035 and 1047/1022 cm⁻¹. Differential scanning calorimetry analysis demonstrated a higher gelatinisation temperature required more energy during the gelatinisation process. D. zingiberensis and D. collettii starches showed higher resistant starch content of 724.0 and 693.2 g kg⁻¹, respectively, with lower hydrolysis index and estimation of glycaemic index. All the starches exhibited an A-type pattern except D. melanophyma starch, which showed a C-type pattern evaluated by X-ray diffraction. CONCLUSION: These results showed that the starches with their low hydrolysis index values possessed potential values as healthy food.

Research on contents of anthraquinones in Cassiae Semen by principal component analysis.

Cassiae Semen is a common traditional Chinese medicine, and contents of anthraquinones of Cassiae Semen different significantly from area to area. According to Chinese Pharmacopoeia (2010 edition), only contents of aurantio obtusin and chrysophanol were used to evaluate the quality of Cassiae Semen, another data could be added later. Ten batches of Cassiae Semen from different areas were determined, and total anthraquinones, total free anthraquinones and total combined anthraquinones contents were assessed by ultraviolet visible spectrophotometer, contents of aurantio obtusin, rhein, aloe emodin, emodin, chrysophanol and physcion were determined by HPLC. After that, principal components analysis was used to evaluate these data determined previous by dimension reduction analysis. At last, the result suggests that three main components were found out, it shows that content of aloe emodin could be used to evaluate the quality of Cassiae Semen as well as contents of aurantio obtusin and chrysophanol. And Cassiae Semen from Hebei province posseses higher quality than Cassiae Semen from other different areas. All these results can provide a good reference for quality evaluating of Cassiae Semen medicinal materials at a certain extent.

[Studies on genetic relationship of Dioscorea].

Based on the results of the morphologic studies on genus Dioscorea, the paper summarized the entire chemical constituent that isolated from this genus and analyzed it with the methods of chemotaxonomy. The rules of the chemical constituent and pharmacodynamic effects were analyzed. Seventeen species which belong to Sect. Stenophora Uline of Dioscorea contain steroidal sapogenin. Other species with different main components such as polysaccharide and tannin have have different effects. This chemotaxonomic view point will conduce to establish a phylogeny of the genus Dioscorea.

[Pharmacokinetics study on costunolide and dehydrocostuslactone after administration of traditional Chinese medicine Weichang'an pills].

A HPLC-MS/MS multiple-reaction monitoring (MRM) quantitative analysis was made to establish a determination method for drug concentrations of costunolide (Co) and dehydrocostuslactone (De) in blood samples in the positive ion mode, with diazepam as the internal standard substance, in order to study the pharmacokinetic process of sesquiterpene lactones costunolide and dehydrocostuslactone after the oral administration of Weichang'an pills, and provide an theoretical basis for further studies on the substance basis for the anti-diarrhea effect of Weichang'an pills. In the blood samples, Co and De showed a good linearity within concentration ranges 0.700 0-769.7, 2.510-956.0 µg x L(-1), respectively. The results of precision, stability and recovery experiences proved the stability and reliability of the plasma concentration determination method. After the oral administration, the concentrations of Co and De in plasma increased with the increase in dose, with T(max) between 10.65-12.98 h, indicating a long time to reach peak plasma concentrations; C(max) of costunolide and dehydrocostuslactone ranged between 3.750-5.450,15.34-44.52 µg x L(-1), respectively. The in vivo adsorption of Co and De conformed to the one-compartment model, with a longer time to attain the peak plasma concentrations. These results provided an experimental basis for revealing the active substance basis and clinical medication of Weichang'an pills.

[Graded ethanol precipitation method on physicochemical properties and antioxidant activities of polysaccharides extracted from Astragalus Radix].

Astragalus polysaccharide has been widely used in food and medicinal industry owing to its health-promoting properties. In order to characterize better the relationship among molecular weight, structure-activity and activities, a simple method was used different concentration of ethanol including 30% (PW30), 50% (PW50), 70% (PW70), 75% (PW75), 80% (PW80) and 90% (PW90) to precipitate Astragalus polysaccharides into different molecular weight. As a result, PW90 showed smooth surface and the strongest antioxidant activity among these six fractions (P < 0.05). In conclusion, graded ethanol precipitation was a simple method to separate Astragalus polysaccharides into different molecular weight with different antioxidant activity fractions.

[Research progress of drugs commonly used to anti-rheumatoid arthritis].

Rheumatoid arthritis (RA) is a kind of chronic, progressive, multiple, invasive autoimmune disease with two chief cclinical manifestations arthrosynovitis and ex-arthrosis, easy to occur in middle-aged women, also occur in children and the elderly, is characterized by progressive and break out repeatedly. RA pathogenesis is complex, there is no special treatment, used in treatment of R drug varied, new drugs and new therapies also emerge in endlessly, main including non-steroidal anti-inflammatory drugs (NSAIDs), slow action anti-rheumatism medicine (SAARDs), glucocorticoids (GCs), biological agent, traditional Chinese medicine and traditional Chinese medicine preparations, domestic market for rheumatoid main drug treatment are NSAIDs, SAARDs, GCs, traditional Chinese medicine and traditional Chinese medicine preparations. Traditional Chinese medicine and traditional Chinese medi- cine preparations for the treatment of RA have its unique advantages, show the characteristics of overall adjustment, multi-level and multiple targets, and also can alleviate and against side effects of western medicine. In recent years, more and more get people's atten- tion. This paper reviewed the research progress and treatment features of commonly used therapeutic agents for the treatment of RA in recent years, which provides reference and basis for future medicine anti-RA.

[Comparision of contents of anthraquinones and phenolic acids compounds in different processed products from Rheum officinale by principal component analysis].

The aim of this study is to compare the contents of five types of anthraquinones which mainly includes chrysophanol, physcion, emodin, rhein and physcion and phenolic acids in ten different processed products from Rheum officinale, and to investigate the effect of different initial processing method on the contents of anthraquinones and phenolic acids. Principal component analysis (PCA) was carried out by SPSS software to evaluate the quality of different processed products from Rh. officinale. In conclusion, the contents of anthraquinones in different processed products from Rh. officinale assume the certain regularity. Whether fresh-cut Rheum officinale Bail and how to dry it are derectly effect the contents of anthraquinones and phenolic compounds. The content of anthraquinones in rheum officinale of drying is obviously higher than smudging, and was more abundant in branch root than tap roots. Rh. officinale of drying which growed in Fengjie gained the highest score in PCA. Meanwhile, the procedure of wetting also help to increase the content of anthraquinones and decrease the content of phenolic acids.

[Dynamic monitoring risk of anti-hepatoma new drug development].

Risk monitoring of new Chinese patent anti-hepatoma drugs is tracking recognized risks and residual risks, identifying emerging risk and ensure the implementation of the plan, estimating the process of reducing effectiveness. The paper is mainly through understanding the status of Chinese patent anti-hepatoma drugs, the content, characteristic and analysis method of dynamic risk monitoring, and then select the risk control indicators, collect risk information. Finally, puts forward the thought of anti-hepatoma drugs listed evaluation in our country, and try to establish the model of dynamic risk management of anti-hepatoma drugs.

[Regularity of drugs compatibility of anti-hepatoma traditional Chinese medicine ancient prescriptions and risk evaluation of anti-hepatoma new drug research and development].

Traditional Chinese ancient prescriptions have been used for treatment of liver cancer for a long history and the scientific and rational compatibility is a great wealth for modern research and development (R&D) of new drugs. The research and development of new drugs are often accompanied with a large investment, a long cycle and a high risk, especially for the anti-tumor drugs R&D which are facing more risks and lower successful rate. In this research, the regularity of compatibility of drugs was analyzed from 124 anti-hepatoma ancient prescriptions by computer program. The results can offer help to the R&D of anti-hepatoma new drugs and reduce the risk of drug screening. In addition, we surveyed 22 companies in this field from six provinces such as Beijing, Shanghai, Tianjin and so on and obtained 240 risk assessment questionaires. Then we used qualitative analysis method to interpret the greatest impacts for the risks in the process of R&D, production and sales of anti-hepatoma new drugs. The study provides a basis for anti-liver cancer drugs R&D researchers, who can take effective measures to reduce the R&D risks and improve successful rate.

Effect of activated carbon microstructure and adsorption mechanism on the efficient removal of chlorophyll a and chlorophyll b from Andrographis paniculata extract.

In order to reveal the effect of activated carbon (AC) properties on the adsorption of chlorophyll a (Chl a) and chlorophyll b (Chl b) in Andrographis paniculata extract, four commercial activated carbons were first tested and characterized. The results showed that activated carbon 1 (AC1) had the best surface area, pore structure and adsorption capacity. Therefore, adsorption isotherms, adsorption kinetics and adsorption mechanism were further carried out on AC1. The application of Langmuir model (R2 > 0.978) and Freundlich model (R2 > 0.977) indicated that the adsorption process of Chl a and Chl b on AC1 may be a complex adsorption process of single-layer and multilayer adsorption. The adsorption kinetics indicated that the pseudo-second-order kinetic model (R2 > 0.999) was dominant and was mainly chemisorption. The intra-particle diffusion model (R2 > 0.937) shows that the intra-particle diffusion is the rate-limiting step. The decrease of adsorption of AC1 to Chl a and Chl b due to the oxidation of acrylic acid proves the importance of π-π interaction.

PI3K signaling-regulated metabolic reprogramming: From mechanism to application.

Oncogenic signaling involved in tumor metabolic reprogramming. Tumorigenesis was not only determined by the mutations or deletion of oncogenes but also accompanied by the reprogramming of cellular metabolism. Metabolic alterations play a crucial regulatory role in the development and progression of tumors. Oncogenic PI3K/AKT signaling mediates the metabolic switch in cancer cells and immune cells in the tumor microenvironment. PI3K/AKT and its downstream effector branch off and connect to multiple steps of metabolism, such as glucose, lipids, and amino acids. Thus, PI3K inhibitor could effectively regulate metabolic pathway and impede the oncogenic process and some key metabolic proteins or critical enzymes also constitute biomarkers for tumor diagnosis and treatment. In the current review, we summarize the significant effect of PI3K/AKT signaling toward tumor metabolism, it enables us to obtain the better understanding for this interaction and develop more effective therapeutic strategies targeting cancer cell metabolism.

catena-Poly[[[aqua-(2,2'-bipyridine-κ(2) N,N')zinc]-µ-furan-2,5-dicarboxyl-ato-κ(2) O (2):O (5)] dihydrate].

In the title hydrated coordination polymer, {[Zn(C6H2O5)(C10H8N2)(H2O)]·2H2O} n , an infinite [1-10] chain is formed by the linking of [Zn(C10H8N2)(H2O)](2+) entities by bridging, monodentate furan-2,5-dicarboxyl-ate dianionic linkers. The Zn(2+) coordination geometry is a trigonal bipyramid, with one N atom (from 2,2'-bipyridine) and one O atom (from the bridging dianion) in the axial positions. For each Zn(II) atom, the dihedral angle between the furan ring of its coordinated bridging ligand and its coordinated bipyridine ring system is 87.19 (8)°. O-H⋯O hydrogen bonds involving both the coordinated and uncoordinated water mol-ecules generate a layer motif parallel to (001).