A new cinnamic acid ester derivative from Liquidambaris Resina / 中国中药杂志

Twelve compounds were isolated from Liquidambaris Resina by silica gel column chromatography and thin layer chromatography. Their structures were identified on the basis of spectral data, electron capture detector data, and physicochemical properties as(2'R, 3'R)-2',3'-dihydroxy-hydrocinnamyl-(E)-cinnamate(1),(E)-cinnamyl-(E)-cinnamate(2), cinnamic acid(3), 28-norlup-20(29)-en-3-one-17β-hydroperoxide(4), erythrodiol(5), 13β,28-epoxy-30-hydroxyolean-1-en-3-one(6),(3β)-olean-12-ene-3,23-diol(7), 2α,3α-dihydroxy-olean-12-en-28-oic acid(8), 28-hydroxyolean-12-en-3-one(9), 3-epi-oleanolic acid(10), 3-oxo-oleanolic acid(11), and hederagenin(12). Compound 1 was a new cinnamic acid ester derivative and compounds 2-4,6-8, and 12 were isolated from Liquidambaris Resina for the first time. Compounds 4, 5, 10, and 12 exerted inhibitory effects on the proliferation of human umbilical vein endothelial cells(HUVEC) with the IC_(50) values of(17.43±2.17),(35.32±0.61),(27.50±0.80), and(46.30±0.30) μmol·L~(-1), respectively.

Postoperative quality of life after gastrectomy in gastric cancer patients: a prospective longitudinal observation study

Purpose@#The European Organization for Research and Treatment of Cancer quality of life (QOL) questionnaires (QLQ-C30, QLQ-OG25, and QLQ-STO22) are widely used for the assessment of gastric cancer patients. This study aimed to use these questionnaires to evaluate QOL in postgastrectomy patients. @*Methods@#We prospectively evaluated 106 patients with distal gastrectomy (DG), 57 with pylorus-preserving gastrectomy (PPG), and 117 with total gastrectomy (TG). Body weight and QOL questionnaires were evaluated preoperatively and postoperatively (at 3 weeks, and 3, 6, and 12 months). @*Results@#TG patients had significantly more weight loss than DG/PPG patients. Compared with DG, patients after PPG had less dyspnea (P = 0.008) and trouble with coughing (P = 0.049), but more severe symptoms of insomnia (P = 0.037) and reflux (P = 0.030) at postoperative 12 months. Compared with DG/PPG, TG was associated with worse body image, dysphagia, eating, and taste in both OG25 and STO22. Moreover, OG25 revealed worse QOL in the TG group with respect to odynophagia, eating with others, choked when swallowing, trouble talking, and weight loss. The QOL of patients who received chemotherapy was worse than those in the chemo-free group in both physical functioning and symptoms such as nausea/vomiting, appetite loss, and trouble with taste; however, these side effects would soon disappear after finishing chemotherapy. @*Conclusion@#PPG was similar to DG in terms of postoperative QOL and maintaining body weight, while TG was always inferior to both DG and PPG. Adjuvant chemotherapy can affect both body weight and QOL despite being reversible.

Design and application of a new magnetic joint for electroacupuncture instrument / 中国针灸

Combined with the material characteristics of acupuncture needle, new connection technology and injection moulding technology, and through mechanical test, a new type of magnetic joint for electroacupuncture instrument, with regular appearance and simple manufacturing process, is developed, which can be connected with acupuncture needle in close range. This joint is composed of the inner magnet joint and the outer joint protective sleeve. The new conductive adhesive is used to simplify the manufacturing process. Its advantages include connection with acupuncture needle by magnetic force, being convenient to store when idle and easy to switch to the working state, and quick disconnection in case of emergency. This joint is connected safely and firmly with acupuncture needle by magnetic force, which shortens the operation time, improves the working efficiency, and effectively solves the problems existing in the crocodile clip connector.

The value and key point of function preserving gastrectomy in early gastric cancer / 中国实用外科杂志

With the detection rate of early gastric cancer increases annually, more and more patients can survive for a long time after surgery. Thus, surgeons have paid more attention to preserve the function of the remnant stomach, limit the surgical trauma and improve the quality of life. Pylorus-preserving gastrectomy andlocal gastrectomy are the most common kind of function preserving gastrectomy. The key points we concern are whether they will bring about the risk of radical tumors, whether they will increase the occurrence of surgical complications and whether they are difficult to popularize. The systematic and in-depth study of the key aspects of these function preserving gastrectomy and the provision of a strong evidence-based medical basis will contribute to a new round of innovation in the surgical treatment of early gastric cancer.

Applications of ionic liquids in drug research / 药学学报

Ionic liquids are not limited to the traditional use of solvents because of their high permeability and excellent physicochemical and unique biological properties. Nowadays, with the deep understanding of their toxicity and biocompatibility, ionic liquids have been tailored as novel solutions to address potential problems of marketed drugs. Based on the research and development of modified new drugs, ionic liquids have been incorporated into drug synthesis and emerged as attractive environmental-friendly reaction media with milder reaction conditions, higher yields and easier reaction workups and drug delivery systems. In addition, they have been designed for effective drug carriers removing undesirable properties of solid drugs. Further, ionic liquids forming active pharmaceutical ingredients dedicated to the liquefaction of drugs for promising clinical applications.

Effect of PKA Gene on Acute Lymphoblastic Leukemia in Children and Its Mechanism / 中国实验血液学杂志

<p><b>OBJECTIVE</b>To explore the effect of PKA gene on acute T lymphocyte leukemia cells in children and its mechanism.</p><p><b>METHODS</b>Jurkat and Sup-T1 cells were divided into 2 group: control group (Jurkat and Sup-T1 cells treated with non-specific siRNA) and transfected group (Jurkat and Sup-T1 cells transfected with PKA siRNA). The effects of down-regulating the expression of PKA gene on the viability, proliferotion, migration and cell cycle distribution of Jurkat and Sup-T1 cells in 2 groups were analyzed by CCK-8 assay, transwell experiment, cell colony-formation test and flow cytometry; the cyclin-related protein levels after transfection with PKA siRNA were detected by Western blot.</p><p><b>RESULTS</b>It was revealed that the expression of PKA in Jurkat and Sup-T1 cells decreased to different degree after siRNA transfection(P<0.05). CCK-8 assay showed that the proliferation of Jurkat and Sup-T1 cells in the transfected group was slower than that in the control group(P<0.05). Transwell experiment showed that the migration and invasion ability of Jurkat cells in the transfection group was weaker than that in the control group (P<0.05). The cell colong formation number of Jurkat and Sup-T1 cells in the transfection group decreased significantly (P<0.05). The cell level of Jurkat and Sup-T1 cells in G/Gphase increased after tansfection (P<0.05). Western blot assay revealed that the expression levels of CDK2, CyclinD1 and p-Rb in the Jurkat and Sup-T1 cells of the transfection group were suppressed (P<0.05).</p><p><b>CONCLUSION</b>The down-regulating PKA gene expression can decrease the proliferation and migration of tumor cells, and also can restrict the cell proliferation through related cell cycle proteins.</p>

Design, synthesis and cholinesterase inhibitory activity of quinoline-polyamine conjugates / 药学学报

A series of quinoline-polyamine conjugates (8a-8n) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). Some of these compounds had potent ChEs inhibitory activity with IC50 values at micromolar range. Compound 8n exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 8.78 micromol x L(-1), and compound 8i showed the most potent inhibition on butyrylcholinesterase (BChE) with IC50 value of 1.60 micromol x L(-1) which was slightly better than rivastigmine. The structure-activity relationship revealed that the chain length of polyamine and linker played important roles for inhibitory activity. Molecular modeling studies showed that 8i targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of cholinesterases.

Synthesis and bioactivity of the folate receptor targeted gamma-cyclodextrin-folate inclusion-coated CdSe/ZnS quantum dots / 药学学报

The gamma-cyclodextrin-folate (gamma-CD/FA) inclusion-coated CdSe/ZnS quantum dots (QDs) with folate-receptor (FR) targeted were synthesized by simple and convenient sonochemical method. The products were studied using Fourier transform infrared (FTIR), proton nuclear magnetic resonance (1H NMR), utraviolet-visible spectrometry (UV-vis), fluorescence spectrum and transmission electron micrographs (TEM). The results showed that the gamma-CD/FA-coated CdSe/ZnS QDs not only have good monodispersity and smaller size, but also have good optical performance, such as higher quantum yield (QY) and a long fluorescence lifetime. The cytotoxicity experiments showed that the gamma-CD/FA-coated CdSe/ZnS QDs have lower cytotoxicity and could more effectively enter cancer cells with FR over-expression. The QDs with 4-5 nm in diameter were relatively easy to enter the cell and to be removed through kidneys, so it is more suitable for biomedical applications for bioprobes and bioimaging.

NNIspm, a polyamine derivative, induces cellular senescence of human hepatoma HepG2 cells and its molecular mechanism / 药学学报

This study is to examine the effects of NNIspm-mediated cellular senescence of HepG2 cells and elucidate its potential molecular mechanism. Cellular senescence was detected with senescence-associated beta-galactosidase staining. Cell cycle distribution, intracellular fluorescence intensity and accumulation of intracellular reactive oxygen species (ROS) were detected by high content screening (HCS). Protein expression was detected by Western blotting. Polyamines content was analyzed by high performance liquid chromatography (HPLC). The results demonstrated that NNIspm significantly induced HepG2 cells senescence. This effect was due to the decrease of intracellular polyamines, the arrest at G0/G1 phase and an increase of ROS level. The molecular senescence marker p21 increased significantly after NNIspm treatment. In contrast, the protein expressions of Cyclin E and CDK2 were obvious down-regulation. The results indicated that cellular senescence induced by NNIspm was one of its antitumor mechanisms.

Design, synthesis and evaluation of tacrine-methoxybenzene hybrids as cholinesterases inhibitors / 药学学报

A series of tacrine-methoxybenzene hybrids (5a-5i) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs). All the compounds had better ChEs inhibitory activities than tacrine with IC50 values at the nanomolar range. Compound 5h exhibited the strongest inhibition on acetylcholinesterase (AChE) with an IC50 value of 6.74 nmol x L(-1) and compound 5f showed the most potent inhibition on butyrylcholinesterase with IC50 value of 3.83 nmol x L(-1). Kinetic and molecular modeling studies showed that these hybrids targeted both the catalytic active site and the peripheral anionic site of AChE.

Acetylsalicylic acid strengthens the effects of ANISpm against hepatocellular carcinoma and its molecular mechanism / 药学学报

The objective of this study is to examine the effects of ANISpm, a novel polyamine naphthalimide conjugate, with acetylsalicylic acid against hepatocellular carcinoma in vivo and in vitro and elucidate its potential molecular mechanism. The proliferation inhibition was detected by MTT assay. Cell apoptosis, intracellular fluorescence intensity and mitochondrial membrane potential (MMP) were detected by high content screening (HCS) analysis. Polyamines content was analyzed by reverse-phase high performance liquid chromatography Protein expression levels were quantified by Western blotting assay. The combination treatment strongly inhibited cell proliferation, induced cell apoptosis in HepG2 cells and H22 hepatoma cells, which was mediated by enhanced ANISpm uptake via up-regulation of spermidine/spermine N1-acetyltransferase (SSAT) and depression of intracellular polyamine. Furthermore, this synergistic apoptosis was involved in mitochondria and death-receptor signal pathway. All these findings demonstrated that the combination treatment with acetylsalicylic acid and ANISpm resulted in synergistic antitumor effects on hepatoma cells. Thus, combination therapy with these agents may be useful as a potential template for the development of better chemotherapeutic strategy against hepatoma.

Clinical study on simvastatin treatment of pulmonary hypertension in patients with coal worker's pneumoconiosis / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To observe simvastatin treatment of pulmonary hypertension in patients with coal workers pneumoconiosis (CWP).</p><p><b>METHODS</b>96 CWP patients with pulmonary hypertension were randomly divided into treatment and control groups. The control group was treated with 2.5 mg warfarin, once a day for four months; the treatment group was treated with 20 mg simvastatin, taken in evening, for 4 months. 6 min walking distance (6MWD) test and inspection pulmonary artery pressure were measured by echocardiography before and after treatment.</p><p><b>RESULTS</b>In the treatment group, the 6MWD were (258 ± 26) m after treatment and (225 ± 19) m before treatment, respectively. Compared with control group, pulmonary artery pressure was (41 ± 9) mm Hg in the treatment group before treatment, (36 ± 3) mm Hg in the treatment group after treatment, and (39 ± 5) mm Hg in control group, respectively, the difference was statistically significant (P < 0.05).</p><p><b>CONCLUSIONS</b>Simvastatin can improve pulmonary hypertension in coal workers pneumoconiosis, and shows a definite curative effect.</p>

Apoptotic mechanism of WJH-6, a novel polyamine conjugate, on K562 and HL-60 cells / 药学学报

In the present study, the apoptotic mechanism and polyamine transporter recognition of WJH-6, a novel polyamine conjugate, were investigated in K562 and HL-60 cells. The cytotoxicity of WJH-6 was assessed by MTT assay; cell cycle distribution and apoptosis were measured by flow cytometry; the protein expression of Caspase-3, Caspase-8, Caspase-9, Bid and mitochondrial membrane potential (MMP) were evaluated by high content screening (HCS) analysis; the protein expression of cytochrome c was measured by Western blotting. The results showed that WJH-6 could be recognized and transported by polyamine transporter (PAT). Furthermore, WJH-6 was able to inhibit K562 and HL-60 cells proliferation and induce apoptosis. This apoptotic effect was relative to MMP loss, cytochrome c release from mitochondria to cytoplasm and the activation of Caspase-8, Caspase-9, Caspase-3 and Bid. These results suggested that WJH-6-induced K562 and HL-60 cells apoptosis was related with mitochondrial damage.

Synthesis and in vitro cytotoxicity of naphthalimide polyamine conjugates as antitumor agents / 药学学报

Six naphthalimide polyamine conjugates were synthesized and their structures were confirmed by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay on Leukemia cells (K562), human breast cancer cells (MB-231) and prostate cancer cells (Ln cap cell). The results showed that most of the six compounds were superior to the control (amonafide), 6d, 6e, and 6f exhibited nice selectivity in a screen of hepatoma cells (BEL-7402) and human normal hepatocytes (QSG-7701).

Apoptosis induced by NNAMB, a novel polyamine conjugate, in human erythroleukemia K562 cells and its mechanism / 中华肿瘤杂志

<p><b>OBJECTIVE</b>To investigate the apoptosis-inducing effects of NNAMB, a novel polyamine conjugate, in erythroleukemia K562 cells and its molecular mechanism.</p><p><b>METHODS</b>Cell viability was assessed by MTT assay and trypan blue dye exclusion method. The cell morphology was observed by fluorescence microscopy. The cell cycle distribution, apoptosis and mitochondrial membrane potential were measured by flow cytometry. The expression of caspase-3, -8, -9, cytochrome c in the K562 cells was detected by Western blot.</p><p><b>RESULTS</b>NNAMB inhibited the proliferation of K562 cells. The cells treated with NNAMB showed a typical apoptotic morphology, Sub-G1 peak and loss of mitochondrial membrane potential. Western blot assay showed that NNAMB increased the expression of caspase-3, -9, cytochrome c but not caspase-8 in a dose-and time-dependent manner.</p><p><b>CONCLUSION</b>NNAMB induces apoptosis via mitochondrial pathway in K562 cells.</p>

Synthesis and antitumor activity of benzoic nitrogen mustard derivatives / 药学学报

To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard, the intermediate 4-[N,N-bis(2-chloroethyl) amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material. Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay. The result showed that some derivatives were more potent than the intermediate 4, and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.

Exploration for Less Hours' Physical Chemistry of Pharmacy / 中华医学教育探索杂志

According to the limited class hours and requirements of medicinary major curriculum application,this paper attempts to make some choice of physical chemistry teaching contents and emphasize on the first class,and also to explore bilingual teaching of partial chapters and experimental teaching.