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β-pinene is a monoterpene isolated from turpentine oil and numerous other plants’ essential oils, which has a broad spectrum of biological activities. In the current work, six novel β-pinene quaternary ammonium (β-PQA) salts were synthesized and evaluated in vitro for their antifungal, antibacterial and anticancer activities. The in vitro assay results revealed that compounds 4a and 4b presented remarkable antimicrobial activity against the tested fungi and bacteria. In particular, compound 4a showed excellent activities against F. oxysporum f.sp. niveum, P. nicotianae var.nicotianae, R. solani, D. pinea and Fusicoccumaesculi, with EC50 values of 4.50, 10.92, 9.45, 10.82 and 6.34 μg/mL, respectively. Moreover, compound 4a showed the best antibacterial action against E. coli, P. aeruginosa, S. aureus and B. subtilis, with MIC at 2.5, 0.625, 1.25 and 1.25 μg/mL, respectively. The anticancer activity results demonstrated that compounds 4a, 4b, 4c and 4f exhibited remarkable activity against HCT-116 and MCF-7 cell lines, with IC50 values ranged from 1.10 to 25.54 μM. Notably, the compound 4c displayed the strongest cytotoxicity against HCT-116 and MCF-7 cell lines, with the IC50 values of 1.10 and 2.46 μM, respectively. Furthermore, preliminary antimicrobial mechanistic studies revealed that compound 4a might cause mycelium abnormalities of microbial, cell membrane permeability changes and inhibition of the activity of ATP. Altogether, these findings open interesting perspectives to the application of β-PQA salts as a novel leading structure for the development of effective antimicrobial and anticancer agents.

Vasculogenic mimicry (VM) is a vascular formation mechanism used by aggressive tumor cells. VM provides an alternative pathway for adequate blood perfusion and challenges the traditional angiogenesis mechanism that depends only on endothelial cells (ECs), as VM-forming tumor cells express a mixed endothelial/tumor phenotype. VM is closely correlated with tumor invasion, migration, and progression. Hence, anticancer therapeutic strategies targeting VM biogenesis are essential. It is widely acknowledged that the VM formation mechanism involves multiple pathways. The purpose of this review is to describe the potential molecular mechanisms related to different pathways and discuss the involvement of microRNAs (miRNAs), long non-coding RNAs (lncRNAs), and circular RNAs (circRNAs) in VM formation. Moreover, we discuss the significance of VM in clinical practice and present new anticancer therapeutic strategies that target VM.

The pretreatment of bamboo with dilute alkali and the effects on chemical components and enzymatic hydrolysis were studied, and the fiber structural properties of pretreated residues were studied with Scanning electron microscope (SEM) and Fourier transform infrared spectroscopy (FTIR). The results showed that dilute alkali was highly effective in delignification of the biomass, reducing the lignin content by 50-70%. Bamboo solid recovery was 74.40%, and cellulose, hemicellulose and lignin content were 60.02%, 25.93% and 9.08%, respectively, when pretreated with 1.0% sodium hydroxide, with a solid-liquid ratio of 1:10 at 100 °C for 40 min. Under the conditions, the pretreated residue was hydrolyzed for 72 h with cellulose and xylanase dosage 40 FPU/g cellulose, and the hydrolysis yield of cellulose was 81.38% and that of hemicelluloses was 84.78%, resulting in a total of 66.74 g fermentable sugars from 100 g dry bamboo. The SEM pictures indicated that the biomass structure was deformed and its fibers were exposed, and FTIR results verified the lignin removal by the pretreatment.

Three new sesquiterpene alkaloids, 1-desacetylwilforgine (1), 1-desacetylwilforine (2), and 9′-hydroxy-2-nicotinoylwilforine (3) were isolated from the roots of Tripterygium wilfordii Hook f., along with six known alkaloids. Their structures were established on the basis of spectral analysis.

Aims Perivascular adipose tissue (PVAT) inhibits vascular smooth muscle cell (VSMC) contraction and stimulates VSMC proliferation by releasing protein factors. The present study was to determine whether visfatin is involved in these paracrine actions of PVAT, and if so, to explore the underlying mechanisms. Methods and results Visfatin was preferentially expressed in Sprague–Dawley rat and monkey aortic PVAT, compared with subcutaneous and visceral adipose tissues. The PVAT-derived visfatin was found to be a VSMC growth factor rather than a VSMC relaxing factor, which was proved by visfatin-specific antibody/inhibitor and direct observation of recombinant visfatin. Exogenous visfatin stimulated VSMC proliferation in a dose- and time-dependent manner via extracellular signal-regulated kinase (ERK 1/2) and p38 signalling pathways. This proliferative effect was further confirmed by enhancement of DNA synthesis and upregulation of proliferative marker Ki-67. Visfatin had no anti-apoptotic effect on normal cultured VSMCs, and it exerted an anti-apoptotic effect only during cell apoptosis induced by H2O2, excluding a role of anti-apoptosis in the visfatin-induced VSMC proliferation. Insulin receptor knockdown did not show any action on the visfatin effect. However, visfatin acted as a nicotinamide phosphoribosyltransferase to biosynthesize nicotinamide mononucleotide (NMN), which mediated proliferative signalling pathways and cell proliferation similar to the visfatin effect. Conclusion Visfatin stimulates VSMC proliferation via NMN-mediated ERK1/2 and p38 signalling. The present study provides a molecular link of visfatin to the paracrine action of PVAT, demonstrates a novel function of visfatin in promoting VSMC proliferation, and reveals NMN as a novel signalling molecule that triggers the proliferative process.

This paper studied the fluorescence spectral characteristic of chlorin e6-C15-monomethyl ester in different solvents to develop a fluorescence spectrometry for determining the concentration of chlorin e6-C15-monomethyl ester in plasma. By comparing the fluorescence spectral characteristics of chlorin e6-C15-monomethyl ester in six different solvents including methanol, ethanol, acetone, acetonitrile, phosphate buffered saline and water, the influence of different solvents on the fluorescence spectral characteristic of chlorin e6-C15-monomethyl ester has been examined. The results indicated that methanol and acetonitrile are the ideal solvent system, and the effect of phosphate buffered saline is better than water. The effect of organic solvent content and solution pH value on emission wavelength and fluorescence intensity was further evaluated. It was found that the fluorescence intensity of chlorin e6-C15-monomethyl ester was strong and stable in pH 7.2 phosphate buffered saline -acetonitrile (3 : 7) solution and can be detected at the excitation wavelength of 498.00 nm and the emission wavelength of 664.05 nm. Based on this, we developed the fluorescence spectrometry for determining chlorin e6-C15-monomethyl ester. It is specific and sensitive with good linearity over the range of 0.5-50 microg x mL(-1). The intra-batch and inter-batch precisions (RSD) were less than 10%, the extraction recoveries were all over 90%. The established method in this paper was simple, fast, effective and could be successfully applied to study the pharmacokinetics of chlorine e6-C15-monomethyl ester in SD rats.

A method was developed for online monitoring of the constituents of ginsenoside of Folium Ginseng in the column separation and purification process using near-infrared (NIR) spectroscopy technology. Determination method of ginsenoside Rg1, Re and Rb1 was developed by high performance liquid chromatography (HPLC). After collecting 40%-ethanol eluant, their NIR spectra were detected and the contents of Rg1, Re and Rb1 were determined by the above HPLC method. The quantitative analysis models of the above three compounds and the total ginsenosides were established using partial least squares (PLS). During modeling, coefficient of determination (R2) and root mean square errors of cross-validation (RMSECV) were regarded as the indexes to select optimal wave numbers and preprocessing methods. The optimal wave numbers of ginsenoside Rg1, Re, Rb1 and total ginsenosides were all in the range of 12 000. 8 approximately 7499.8 cm-1; R2 were 0.9887, 0. 9603, 0.9905 and 0.9701, respectively; RMSECV were 0.0597, 0.0722, 0.00488 and 0.0755, respectively. A lot of samples, collected during the column separation and purification process of Folium Ginseng extract, were used to validate the predicttion effect of quantitative analysis model of total ginsenosides. As a result, the correlation coefficient of NIR predicted value and HPLC value of total ginsenosides was 0.9928 and the mean prediction recovery was 100.52%, which indicated that the prediction effect of the developed model was satisfactory. This method was proved to be fast, convenient and precise. It can be used for assaying and quality control of total ginsenosides in manufacture.

To study the dynamic changes and its clinical significance of integrated traditional Chinese and western medicine (TCM-WM) on IL-2 system, T cell and erythrocyte immune system in patients of lung cancer. Forty-eight patients with lung cancer were randomly divided into two groups: TCM-WM group (Group I ) and the chemotherapy group(Group II). The relevant immune indices, clinical symptoms and signs, changes of solid tumor and quality of life were dynamically observed and compared with those in 20 healthy subjects for control. The serum IL-2 level of lung cancer patients were originally significantly lower, while sIL-2R level higher than that of the healthy subjects. And they were raised and lowered respectively after treatment, especially in Group I, but still remained different from the control group yet. And there were highly negative correlation between IL-2 and sIL-2R levels. The percentage of CD3, CD4 and the CD4/CD8 ratio were decreased markedly in both groups. And the percentage of RBC-C3bRR was obviously lower, while that of RBC-ICR obviously higher. But the above-mentioned indices could be improved after treatment, especially in Group I, and there were highly positive correlation between CD4/CD8 ratio and RBC-C3bRR. However, in regard to the degree of improvement, the patients of Group I were in better position than those of Group II. At the same time, improvement of their clinical symptoms and signs, change of entity tumor and quality of life of Group I all proved to be better than those of Group II. The therapeutic superiority of TCM-WM on lung cancer may be related to the modulation on immune function. The effect of TCM-WM is better than that of chemotherapy alone.

Cnidium monnieri Cusson (Umbelifera) is an annual herbs, widely grows in all parts of China except Xizang, and their fruits mainly contains coumarins. The chemical distinction as well as their variation in Cnidium fruits from different geographical sources was determined using reversed phase-high performance liquid chromatography (RP-HPLC) analysis. The concentrations of these coumarins were as follows: osthole 0.091i½ž2.467%; imperatorin 0.014 ~ 0.877%; bergapten 0.030 ~ 0.168%; isopimpineline 0.074 ~ 0.287% and xanthotoxin 0.023 ~ 0.181%. These results indicated that chemical composition and the amounts of coumarins in Cnidium fruits from different geographic sources varied significantly. The Cnidium fruits that grow in low latitude regions (such as Zhejiang, Jiangsu province) contain higher osthole and linear furancoumarins; The Cnidium fruits that grow in high latitude regions (such as Heilongjiang province) almost have no osthole and linear furancoumarins, but contain other type coumarins; The Cnidium fruits that grow between high latitude and low latitude not only contain osthole and linear furancoumarins, but also contain other type coumarins, they are the transition types from low latitude regions to high latitude regions. Key words: Chemical diversity, Cnidium monnieri Cusson, coumarins, high performance liquid chromatography (HPLC) analysis.

To study the optimal technologies for the purification of total flavones from Trollius ledebouri with macroporous resin.Static and dynamic adsorption-desorption methods were adopted to choose the optimal type of resin. The adsorption function of D101 macroporous resin and the effects of sample concentration, pH, flow rate and eluant etc. were studied. Then the orthogonal design L9 (3(4)) was used to select the optimum purification process conditions.The appropriate technological conditions were as follows: the sample concentration was 0.5 g/mL, pH 6.0, the ratio of sample to D101 macroporous resin was 1:1 (W/W), 4 BV of water was used as purificant and 6 BV of 30% alcohol was used as eluant. Under these conditions, the average content of total flavonoids extract was over 60%.

Serum albumin is the most abundant protein in plasma. It can bind with many intrinsic and extrinsic materials. The study of the interaction between serum albumin and drugs is a very important task in life science and chemistry. Quinolone drug is a kind of antibacterial drugs which have been used widely in clinical medicine, but its pharmacology and toxicology still have to be studied further. Sinafloxacin is a new quinolone antibiotics. The interaction between sinafloxacin and bovine serum albumin (BSA) at different temperatures and pH was investigated by fluorescence and UV absorption spectroscopy. The experimental results demonstrate that the fluorescence quenching of BSA by sinafloxacin is a result of the formation of sinafloxacin-BSA complex and the quenching mechanism is mainly static quenching. The interaction association constants of BSA and sinafloxacin were determined from the double reciprocal Lineweaver-Burk plot. The binding distance(r = 3.64 Rnm) and energy transfer efficiency (E = 0.163) between donor (BSA) and acceptor (sinafloxacin) were obtained based on Förster's non-radiative energy transfer theory. There is a strong interaction between sinafloxacin and BSA. From thermodynamic coordination it can be judged that the binding force between sinafloxacin and BSA is mainly electro-static force. The effect of sinafloxacin on the conformation of BSA was analyzed by synchronous fluorescence spectrometry and three-dimensional fluorescence spectrometry. The emission maximum of tyrosine residues does not show a significant shift, while the small blue shift of tryptophan residues indicates that the hydrophobicity of microenvironment was increased. In addition, in the plasma, there are some metal ions, which can participate in many important vital actions and affect the reactions of the drugs with the serum albumins. So the effect of Cu(II), Fe(III), Zn( II) and Mg(II) on the binding constant of sinafloxacin to BSA was also discussed and it was shown that the interaction between BSA and sinafloxacin was decreased. In short, the results offer a reference for the studies on the biological effects and action mechanism of sinafloxacin with albumins in vivo.

To study the chemical constituents of Patrinia villosa Juss.Solvent extraction, silica gel column and preparative liquid chromatography were used to separate the chemical constituents, and the chemical structures were elucidated by physico-chemical properties and spectra data.Eight compounds were isolated and identified as bolusanthol B (1), (2S)-5, 7, 2', 6'-tetrahydroxy-6,8-di (gamma,gamma-dimethylallyl) flavanone (2), orotinin (3), (2S)-5, 7, 2', 6'-tetrahydroxy-6-lavandulylated flavanone (4), 3'-prenyl-apigenine (5), luteolin (6), quercetin (7) and apigenin (8).Compound 2 and 4 are new compounds, compounds 1, 3 and 5 were separated from Patrinia genius for the first time, compounds 6, 7 and 8 were isolated from Patrinia vollosa Juss for the first time.

To investigate the chemical constituents of Patrinia villosa.The chemical constituents were isolated by silica gel column chromatography and semi-preparative high-performance liquid chromatography, and identified by physicochemical properties and spectral analysis (MS, 1H-NMR and 13C-NMR).Seven compounds were isolated from ethyl acetate and n-butanol extract and identified as: 5-hydroxyl-7, 3', 4'-trimethoxy flavone (I), 5-hydroxyl-7, 4'-dimethoxy flavone (II), luteolin (III), quercetin (IV), isoorientin (V), isovitexin (VI) and 8-C glucosylprunetin (VII).Compounds I , II, III, V, VI and VIII were obtained from the plant of genus Patrinia for the first time, compound IV was separated from P. villosa for the first time.

To investigate the stereoselective pharmacokinetic process of tetrahydropalmatine (THP) in rats.The concentrations of tetrahydropalmatine enantiomers in rat plasma were determined by coupled achiral and chiral HPLC method. The differences in plasma concentrations and pharmacokinetic parameters between the two enantiomers were compared by paired t-test.The plasma levels of l-THP were always higher than those of d-THP in eight rats. There was significant difference between the main pharmacokinetic parameters of the two enantiomers.Tetrahydropalmatine showed significant stereoselective pharmacokinetics in rats after an ig dose of the racemate.