Effect of Zuogui Jiangtang Tongmai Prescription on Astrocyte Injury by AGEs Combined with Oxygen-glucose Deprivation Based on AMPK/mTOR/ULK1 Pathway Related to Autophagy / 中国实验方剂学杂志

ObjectiveTo explore the effect and mechanism of Zuogui Jiangtang Tongmai prescription （ZGJTTMP） on astrocytes （ASs） injured by advanced glycation end products（AGEs） combined with oxygen-glucose deprivation （OGD）. MethodCell counting kit-8 （CCK-8） was used to determine the optimal concentration of AGEs and the action time of OGD， and the optimal blood concentration of ZGJTTMP was selected for follow-up experiments. ASs were divided into normal group， model group （AGEs + OGD）， ZGJTTMP group， an adenosine 5'-monophosphate-activated protein kinase （AMPK） inhibitor （Compound C） group， AMPK activator （AICAR） group， and combination group （ZGJTTMP + AICAR）. The morphological changes in ASs in each group were observed under an inverted microscope. The cell survival rate in each group was detected by CCK-8. The content of interleukin-1β（IL-1β）， interleukin-6（IL-6）， and tumor necrosis factor-α（TNF-α） was detected by enzyme-linked immunosorbent assay （ELISA）. The number of autophagosomes in each group was counted under an electron microscope. The expression of microtubule-associated protein light chain 3 （LC3） was observed by immunofluorescence. The protein expression of LC3， p62， p-AMPK， AMPK， p-mammalian target of rapamycin （mTOR）， mTOR， p-UNC-51 like kinase 1 （ULK1）， and ULK1 was detected by Western blot. ResultAccording to the results of cell survival rate， 200 mg·L-1 AGEs and OGD for 6 h were selected as the optimal modeling conditions for the model group， and 5% was selected as the optimal blood concentration of ZGJTTMP. Under the inverted microscope， the cells were severely damaged after modeling， but the cell injury in the ZGJTTMP group and the Compound C group was significantly improved. As revealed by ELISA results， the content of IL-1β， IL-6， and TNF-α in the model group increased （P<0.01）， and the content of inflammatory factors in the ZGJTTMP group and the Compound C group decreased （P<0.01）. Under the electron microscope， the number of autophagosomes in the model group increased significantly. The immunofluorescence results showed that the expression area of LC3 increased in the model group （P<0.01）， and the ZGJTTMP group and the Compound C group showed decreased number of autophagosomes and reduced expression area of LC3 （P<0.01）. As demonstrated by the results of Western blot， compared with the normal group， the model group showed increased expression of LC3Ⅱ/LC3Ⅰ and p-AMPK/AMPK （P<0.01） and decreased p62， p-mTOR/mTOR， and p-ULK1/ULK1 （P<0.01）. Compared with the model group， the ZGJTTMP group and the Compound C group showed decreased expression of LC3Ⅱ/LC3Ⅰ and p-AMPK/AMPK （P<0.01） and increased p62， p-mTOR/mTOR， and p-ULK1/ULK1 （P<0.01）. ConclusionZGJTTMP possesses a protective effect on ASs with inflammatory injury by AGEs combined with OGD， which may be achieved by inhibiting the activation of the AMPK/mTOR/ULK1 pathway related to autophagy， thus inhibiting the overexpression of autophagy.

Investigation and research of physics technique and quality assurance for radiotherapy in east guangdong province / 中华放射肿瘤学杂志

Objective To investigate the physics technique and quality assurance (QA) during radiotherapy in the institutions from the East Guangdong province,aiming to provide reference for the construction of radiotherapy discipline and rational allocation of resources in the primary hospitals from the eastern Guangdong province.Methods From March 15 to May 20,2016,the general conditions,radiotherapy equipment,available technique and quality assurance (QA) in the medical institutions from eastern Guangdong were investigated and analyzed by online combined with on-spot surgery.Results There were 8 institutions which provided radiotherapy with 966 ward beds,a daily capacity of 632 patients and 222 radiotherapy practitioners.Radiotherapy equipment included 12 linear accelerators,5 after-loading devices,1γ-knife,8 CT simulators and 9 radiotherapy planning systems.Five institutions performed IMRT/VMAT,IGRT and ART.Dose verification was performed before precision radiotherapy delivery in all institutions except for 1 center.QA procedures were missing for the linear accelerators,CT simulators and after-loading devices.Short-term advanced studies and hand-by-hand teaching were the main approaches for staff professional training.Conclusions The resource allocation for radiotherapy in the medical centers from the eastern Guangdong province is scarce.The technique and QC levels greatly differ among different institutions.Standard QA protocols are urgently to be established and implemented.Extensive attentions should be paid to the the professional training for technicians.

Experimental study of lentiviral vector-mediated bFGF gene transfection on rabbit BMSCs / 天津医药

Objective To observe the effect of lentiviral vector-mediated basic fibroblast growth factor (bFGF) gene transfection on the biological characteristics of rabbit bone marrow stromal cells(BMSCs)under in vitro culture conditions. Methods BMSCs were obtained by density gradient centrifugation and adherence screening. The bFGF gene was transfected into BMSCs by lentiviral vector and divided into bFGF transfection group,empty virus group and untransfected group according to the transfection conditions.After transfection,the morphology,expressions of bFGF mRNA and protein, cell proliferation,cell cycle and alkaline phosphatase(ALP)activity were observed in three groups of cells. Results High density BMSCs were successfully obtained by density gradient centrifugation and adherence screening.After transfection of BMSCs with bFGF gene, the cell morphology showed no significant changes, while the expressions of bFGF mRNA and protein were significantly increased, the cell proliferation curve shifted upward, the proportion of proliferating cells increased,and the activity of ALP was significantly enhanced.There were significant differences between three groups(P<0.05).Conclusion The rabbit bFGF gene is successfully introduced into the BMSCs cultured in vitro by lentiviral vector, and the target gene is stably expressed.The expression of bFGF can promote the proliferation and osteogenic differentiation of BMSCs.

Synthesis and evaluation of 2-cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide as a potent anti-inflammatory agent for intervention of LPS-induced acute lung injury / 中国天然药物

The present study was designed to synthesize 2-Cyano-3, 12-dioxooleana-1, 9(11)-en-28-oate-13β, 28-olide (1), a lactone derivative of oleanolic acid (OA) and evaluate its anti-inflammatory activity. Compound 1 significantly diminished nitric oxide (NO) production and down-regulated the mRNA expression of iNOS, COX-2, IL-6, IL-1β, and TNF-α in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Further in vivo studies in murine model of LPS-induced acute lung injury (ALI) showed that 1 possessed more potent protective effects than the well-known anti-inflammatory drug dexamethasone by inhibiting myeloperoxidase (MPO) activity, reducing total cells and neutrophils, and suppressing inflammatory cytokines expression, and thus ameliorating the histopathological conditions of the injured lung tissue. In conclusion, compound 1 could be developed as a promising anti-inflammatory agent for intervention of LPS-induced ALI.

The evaluation of popliteal fossa fixed method to reduce setup errors for postoperative cervical cancer via CBCT / 肿瘤研究与临床

Objective To evaluate the effect of popliteal fossa fixed method to reduce the setup errors in patients with postoperative cervical carcinoma by CBCT of TrueBeam Linear accelerator.Methods 30 cases of postoperative cervical cancer patients were randomly divided into two groups,group A with popliteal fossa fixed method by trapezoidal fixation,group B with traditional vacuum pad fixation.CBCT was used to record both setup errors and rotational errors,Stroom extension formula was used to calculate the PTV expansion value coming from the two different fixation methods.Results There was significant difference in setup errors between group A and group B.The setup errors in the left-right direction (X),cranial-caudal direction (Y) and anterior-posterior direction (Z) were (0.19±0.14) cm,(0.17±0.12) cm and (0.13±0.11) cm in group A,respectively.On the contrary,the setup errors in X,Y and Z were (0.24±0.19) cm,(0.25±0.21) cm and (0.22±0.18) cm in group B,respectively.The rotational errors were 0.05°±0.02° in group A,comparing with 0.5°±0.21° in group B (P =0.00).The PTV expanded margin in group A was 0.56 cm in X direction,0.51 cm in Y direction,0.40 cm in Z direction,in comparing with 0.73 cm,0.78 cm and 0.67 cm in group B,respectively.Group A remarkably reduced the PTV,pelvis,small intestine,bladder and rectum irradiated volumes [(1 167±271) mm3 vs (1 379±297) mm3,(84±12) mm3 vs (130±17) mm3,(81±51) mm3 vs (117±64)mm3,(62±40) mm3 vs (75±47) mm3,(21±16) mm3 vs (31±21) mm3].Conclusion Popliteal fossa fixed method can reduce setup errors and improve the stability of positioning,more suitable in precise radiotherapy for postoperative cervical cancer patients,which has the value of further validation.

Quality Assurance for Truebeam Imaging System Based on MIMI Phantom / 中国医学影像学杂志

PurposeTo perform a quality assurance program for Truebeam imaging system using MIMI phantom, and to evaluate the accuracy of the imaging system center with the radiation isocenter and the accuracy of couch shift.Materials and Methods The reference images of MIMI phantom were acquired using CT scanner. The reference images were imported into the treatment planning system and a simple plan was created. The MIMI phantom was placed on the treatment couch. The images were acquired using the MV/KV imaging system, and a match registration was performed with the reference images from the TPS.Results Measured over six months, the precision of the imager and linac's isocenter was <1 mm, and the couch shift accuracy was <1 mm. The measurements over six months demonstrate that isocenters of the MV/KV imaging systems on Truebeam system are stable.Conclusion The accuracy of the Truebeam imaging system center and couch shift is safe and reliable. The error of Truebeam imaging system center and couch shift can be tested on a monthly base.

Volumetric modulation arc radiotherapy with flattening filter-free beams compared with conventional beams for nasopharyngeal carcinoma: a feasibility study / 癌症

There is increasing interest in the clinical use of flattening filter-free (FFF) beams. In this study, we aimed to investigate the dosimetric characteristics of volumetric modulated arc radiotherapy (VMAT) with FFF beams for nasopharyngeal carcinoma (NPC). Ten NPC patients were randomly selected to undergo a RapidArc plan with either FFF beams (RA-FFF) or conventional beams (RA-C). The doses to the planning target volumes (PTVs), organs at risk (OARs), and normal tissues were compared. The technical delivery parameters for RapidArc plans were also assessed to compare the characteristics of FFF and conventional beams. Both techniques delivered adequate doses to PTVs. For PTVs, RA-C delivered lower maximum and mean doses and improved conformity and homogeneity compared with RA-FFF. Both techniques provided similar maximum doses to the optic nerves and lenses. For the brain stem, spinal cord, larynx, parotid glands, oral cavity, and skin, RA-FFF showed significant dose increases compared to RA-C. The dose to normal tissue was lower in RA-FFF. The monitor units (MUs) were (536 ± 46) MU for RA-FFF and (501 ±25) MU for RA-C. The treatment duration did not significantly differ between plans. Although both treatment plans could meet clinical needs, RA-C is dosimetrically superior to RA-FFF for NPC radiotherapy.

Mutation analysis of the HBV reverse transcriptase in nucleos(t)ide-treated patients with chronic HBV infection / 中华实验和临床病毒学杂志

<p><b>OBJECTIVE</b>To characterize genotypic resistance within HBV RT region in chronic hepatitis B (CHB) patients with nucleos(t)ide analogue (NA) treatment.</p><p><b>METHODS</b>Serum samples of 229 CHB patients with NA treatment were obtained. Full-length HBV RT sequences were amplified, sequenced and analyzed, on the following NA resistant (NAr) mutations belonging to different NAr pathways.</p><p><b>RESULTS</b>Among 229 HBV isolates, 14.41% (33/229) and 85.59% (196/229) were genotype B and C, respectively; and the patients with HBV genotype C may be more susceptible to develope resistant mutations than patients with HBV genotype B(chi2 = 2.95, P < 0.05). NAr mutations were detected in 63 CHB patients. Mutations were not found at rtI169, rtT184, rtA194 or rtS202. RtM204 mutations were detected at the highest frequency among 63 mutants (40/63, 63.49%) and found to display 11 combination mutation patterns, in which rtM204I were associated with rtL80I/V and rtL180M, and rtM204V were associated with rtL1l80M, respectively. Conclusions There are complicated mutation patterns in the HBV RT region for chronic hepatitis B (CHB) patients with nucleos(t)ide analogue (NA) treatment. RtM204V/I mutation was the highest.</p>

Preliminary research of docetaxel plus cisplatin regimen with concurrent intensity-modulated radiation therapy in treating locally advanced nasopharyngeal carcinoma / 肿瘤研究与临床

ObjectiveTo assess the feasibility and efficacy of a docetaxel plus cisplatin regimen for patients of locally advanced nasopharyngeal carcinoma(NPC)treated concurrently with definitive IMRT in a short-term observation.MethodsRadiation consisted of 7000 cGy given to the planning target volume (PTV) of primary tumor, 6600 cGy given to the PTV of metastatic lymph nodes and 6000 cGy to the PTV of subclinical disease in 220-228 cGy/fraction were delivered over 31-32 treatment days. Thirty-two patients with newly diagnosed NPC received definitive intensity-modulated radiation therapy(IMRT)concurrent with docetaxel 75 mg/m2 on day 1 and DDP 75 mg/m2 on day 1(or DDP 25 mg/m2 on day 1-day 3), repeating every 21 to 28 days for 2 cycles.ResultsAll patients received the full dose of radiotherapy and completed 2 cycles of chemotherapy with a median follow-up of 13 months (2-28 months).No treatment-related death was observed. Major toxicities included hematologic toxicity and mucositis. The incidence rates of grade 3-4 leucopenia,grade 3-4 neutropenia and grade 3 acute mucositis were 46.9 ％ (15/32),59.4 ％ (19/32) and 40.6 ％ (13/32) respectively.The complete remission (CR) rate was 96.9 ％ (31/32).During treatment,90.6 ％ (29/32)patients acquired granulocyte colony stimulating factor (G-CSF)for leucopenia. The 1-year overall survival, local recurrence-free survival, regional recurrence-free survival and distant metastasis-free survival were 100 ％ (31/32),96.9 ％ (31/32),96.9 ％ (31/32),96.9 ％ (31/32),respectively,for the whole cohort.Conclusions2 cycles of the docetaxel plus cisplatin regimen with concurrent IMRT are demonstrated being feasible and effective in treating locally advanced NPC with promising results.The major toxicities are leucopenia and neutropenia, but they are tolerable with the use of G-CSF. Further investigation of long-term efficacy of the regimen is required.

Proliferation of retinal pigment epithelial cells induced by (R,R)-XY-10 and (S,S)-XY-10 and their action mechanisms / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: To investigate the mechanism of proliferation effect induced by (R,R)-XY-10 and (S,S)-XY-10 on retinal pigmented epithelial cells(ARPE-19).METHODS: Human retinal pigmented epithelial cells(ARPE-19) and human umbilical vein endothelial cells (HUVECs) were used to investigate the effect of (R,R)-XY-10 and (S,S)-XY-10 on cell growth,and their mechanisms of proliferative action by using ERK、 AKT、PI3K、Protein kinase C (PKC)and Nitric oxide synthase (NOS) inhibitors.RESULTS: (R,R)-XY-10 and (S,S)-XY-10 dose-dependently increased ARPE-19 cell proliferation,but not on HUVECs. When treated with proliferative inhibitors,H7(5μmol/L)、hypericin(20μmol/L)、PD98059(2μmol/L)、LY294002(50μmol/L)、SH-5 (10μmol/L) and L-NAME (100μmol/L),the proliferative effect was reduced by H7、hypericin、PD98059 and LY294002,but not by SH-5 and L-NAME.CONCLUSION: (R,R)-XY-10 and (S,S)-XY-10 can induce cell proliferation through MAPK and PI3K dependent pathway. KEYWORDS: age-related macular degeneration; (R,R)-XY-10; (S,S)-XY-10; ARPE-19 cells; human umbilical vein endothelial cells; proliferation

Advances in the study of nitric oxide-donating drugs / 药学学报

Nitric oxide (NO) as a messenger and/or effector plays important roles in vivo. The decreased availability of NO or dysfunction in NO signaling has often been implicated in the development and progression of diseases, and design and research of NO-donating drugs has become one of the important strategies in drug discovery. In connection with authors' scientific practice, this article reviews the recent advances in the research of NO-donating drugs.

Effects of enantiomers(R,R)-XY and(S,S)-XY on ocular blood flow in rabbits / 国际眼科杂志(Guoji Yanke Zazhi)

·AIM: To evaluate the effects of two series of enantiomers [(R, R)-XY-1 through (R, R)-XY-12 and (S,S)-XY-1 through (S, S)-XY-12] on ocular blood flow in rabbits.·METHODS; Colored microsphere technique was used for in vivo experiments to determine the ocular blood flow in various tissues of ocular hypertensive (40mmHg) rabbit eyes.·RESULTS; Of the twelve compounds of ( R, R)-XY series examined, four increased choroidal blood flow at 10g/L, 50uL instilled into eyes. All compounds of (S, S)-XY series were not effective on ocular blood flow.·CONCLUSION; Some compounds of (R, R)-XY series increased the ocular blood flow, which might be useful for the prevention and treatment of ocular blood flow related eye diseases. Among all twenty-four compounds, (R, R)-XY-1and (R, R)-XY-9 seem to be the most potent ones.KEYWORDS; ocular blood flow; ischemia; enantiomer

Effect of intrauterine hepatitis B virus infection on peripheral blood mononuclear cells interferon-gamma and interleukin-4 in newborns / 中华儿科杂志

<p><b>OBJECTIVE</b>To observe the effect of intrauterine hepatitis B virus (HBV) infection on peripheral blood mononuclear cells function of secreting interferon-gamma and interleukin-4.</p><p><b>METHODS</b>Pregnant women were systematically screened for HBsAg and HBeAg when attending the antenatal clinic at the Qinhuangdao Maternal and Child Health Hospital. Totally 67 pairs of mothers and infants were enrolled into this study after obtaining the women's consent. Venous blood samples were collected from the infants within 6 hours after birth and before HBIG injection and HBVac immunization. Blood sample was taken from the mother at or after the time when the infant was born. HBV DNA in plasma and PBMC from mothers and their newborns were examined using polymerase chain reaction (PCR). According to HBV DNA in PBMC of newborns, they were divided into two groups. The PBMCs isolated from newborn were cultured with purified HBsAg or phytohemagglutinin (PHA). The supernatant interleukin-4 and interferon-gamma level was measured by using enzyme linked immunosorbent assay (ELISA).</p><p><b>RESULTS</b>In 19 newborns PBMC was positive for HBV DNA. Maternal PBMC HBV DNA positivity was associated with high rate of intrauterine HBV infection in the infants (chi2 = 7.58, P < 0.01). Compared with the infants whose PBMC HBV DNA was negative, the infants with PBMC positive for HBV DNA expressed a lower level interferon-gamma secretion after purified HBsAg stimulation (t = 4.71, P < 0.01), however, no significant difference was seen after PHA stimulation (t = 1.21, P > 0.05). The supernatant IL-4 level detected after stimulation with purified HBsAg was higher in the newborns whose PBMC HBV DNA was positive as compared with those negative for PBMC HBV DNA (t = -8.51, P < 0.05). The level of IL-4 did not show any significant difference after stimulation with PHA between the PBMC HBV DNA negative and positive groups (t = -2.40, P > 0.05).</p><p><b>CONCLUSION</b>Infection with HBV of maternal PBMC is responsible for perinatal newborn's PBMC HBV infection and it may be an important route of HBV vertical transmission. Infants whose mothers were positive for HBsAg, HBeAg and HBV DNA were at extraordinarily high risk for hepatitis B virus infection. PBMC infected with HBV could influence the status of humoral and cellular immunity resulting in persistent HBV infection and recurrent mother to infant transmission of HBV. Low responses of interferon-gamma and high interleukin-4 transcription upon specific stimulation exist in infants whose PBMC were positive for HBV DNA in uterus may contribute to immune tolerance to HBV.</p>

Clinilal study of medical ozone therapy in chronic hepatitis B of 20 patients / 中华实验和临床病毒学杂志

<p><b>OBJECTIVE</b>To study the effect of medical ozone in the treatment of chronic hepatitis B.</p><p><b>METHODS</b>42 patients with chronic hepatitis B were divided randomly into two groups. 22 patients treated with basic therapy were as a control group. 20 patients treated with basic therapy plus ozone therapy were taken as a treatment group. Index of biochemistry and virology were studied at initial and post-treatment 8 weeks.</p><p><b>RESULTS</b>After the treatment, liver function of the treatment group and the control group had more significant improvement. The treatment group complete effective and partial effective were 10% and 35% difference. The control group complete effective and partial effective were 4.6% and 13.6% (P < 0.05).</p><p><b>CONCLUSION</b>Treatment of medical ozone on patients with chronic hepatitis B is effective.</p>

Effects of ZX-5 and its optical isomers on ocular blood flow in rabbits and retinal function recovery in rats / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: The effects of ZX-5, as nitric oxide (NO) donor, on ocular blood flow has been investigated using colored microsphere technique in previous study. The relationship between the production of NO by ZX-5 and ocular blood flow has been evaluated. ZX-5 has been shown to have strong positive effect on increasing choroidal blood flow. However,the effect of ZX-5 on retinal function recovery, the effects of its optical isomers, (R, R)-ZX-5 and (S, S)-ZX-5, on choroidal blood flow and retinal function recovery have not been studied and merit investigation.METHODS: Colored microsphere technique was used for in vivo experiments to determine choroidal blood flow of ocular hypertension (40mmHg) in rabbit eyes. Electroretinography was used to measure the b-wave recovery as an indication of retinal function recovery.RESULTS: (R, R)-ZX-5 increased choroidal blood flow at 10g/L, 50μL instillation into eyes at all time points (P＜0.05).(S, S)-ZX-5 was not effective in increasing choroidal blood flow. ZX-5 and (R, R)-ZX-5 showed significant effects in retinal function recovery after ischemia of the retina at all time points (P＜0.05); whereas (S, S)-ZX-5 did not show significant effect on recovery of b-wave after ischemia at most time points except at 120 and 240 minutes.CONCLUSION: ZX-5 and (R, R)-ZX-5 have high potency in increasing the choroidal blood flow and improving the retinal function recovery. It is hoped that they could be used for the prevention/treatment of ocular blood flow related eye diseases.

A novel class of anti-inflammatory and analgesic drugs--NO-donating NSAIDs / 药学学报

Traditional non-steroidal anti-inflammatory drugs (NSAIDs) and COX-2 selective inhibitors are among the most widely used drugs. However, their significant side effects in gastrointestinal and cardiovascular systems limited the use of these drugs. Recently, research and development of NO-donating NSAIDs (NO-NSAIDs) have become one of the most important strategies to reduce these side effects. NO-NSAIDs may exert a broad range of positive effects in terms of NO-mediated gastrointestinal and cardiovascular safety as well as comparable or increased anti-inflammatory, analgesic properties relative to NSAIDs. This review briefly deals with chemistry of NO-NSAIDs, more details are focused on biological significance, mechanism of action, and therapeutic potential of this novel class of drugs.

Synthesis and antithrombotic activity of acetylsalicyl ferulic acid-coupling furoxans and nitrates / 药学学报

<p><b>AIM</b>To synthesize and study the antithrombotic activity of NO-donating aspirin derivatives.</p><p><b>METHODS</b>Furoxans and nitrates were incorporated to aspirin via antioxidant ferulic acid as a linker, and the target compounds were screened for in vitro and in vivo inhibitory activities of platelet aggregation, and for inhibitory effect on A-V hypass thromhosis in rats.</p><p><b>RESULTS</b>Fourteen novel compounds I(1-14), were synthesized and their structures were confirmed Iy MS, IR, 1H NMR and elemental analysis. Biological screening results demonstrated that some tested compounds exhibited potential antithrombotic activ it.</p><p><b>CONCLUSION</b>Acetylsalicyl ferulic acid-coupling furoxans and nitrates might he used as a lead for further study.</p>

Structural characterization of chlorobenzylidine / 药学学报

<p><b>AIM</b>To study the structure and crystal forms of chlorobenzylidine.</p><p><b>METHODS</b>Karl Fischer titrimetry, FTIR, thermal analysis, single and powder X-ray diffraction were used for the studies of the structure of chlorobenzylidine and for the identification of two forms of chlorobenzylidine.</p><p><b>RESULTS</b>Chlorobenzylidine and its diastereoisomer have been studied in this article. They can be distinguished by their different melting points. Two crystal forms of chlorobenzylidine (form A and form B) have also been detected and studied. Form A was studied by single-crystal X-ray diffraction, it crystallized in the triclinic system, space group P1(-), with two formula units per cell, is monohydrate. Karl Fischer titrimetry, FTIR, thermal analysis and powder X-ray diffraction were used for identification of the two forms.</p><p><b>CONCLUSION</b>The studies of structure and crystal forms of chlorobenzylidine are very useful for the clinical research and the selection of recrystallization process.</p>

Studies on the chemical constituents of Cirsium japonicum DC / 药学学报

<p><b>AIM</b>In order to look for new bioactive compounds, investigation on the chemical constituents, especially on the typical polyacetylenes from the rhizomes of Cirsium japonicum DC. was carried out.</p><p><b>METHODS</b>Chromatographic techniques including silica column chromatography and preparative silica thin-layer chromatography were used to separate and purify the constituents. Their structures were elucidated by physicochemical properties and spectral analyses including UV, IR, 1HNMR, 13CNMR, HMQC, HMBC and HREIMS.</p><p><b>RESULTS</b>Twelve compounds were isolated from the rhizomes of Cirsium japonicum DC., and their structures were identified as cis-8, 9-epoxy-heptadeca-1-ene-11, 13-diyne-10-ol (1), ciryneol A (2), 8,9,10-triacetoxyheptadeca-1-ene-11,13-diyne (3), ciryneone F (4), cireneol G (5), ciryneol H (6), ciryneol C (7), p-coumaric acid (8), syringin (9), linarin (10), beta-sitosterol (11) and daucosterol (12).</p><p><b>CONCLUSION</b>Compounds 4, 5 and 6 are new compounds, compound 3 is a new natural product and compound 8 was isolated from this plant for the first time.</p>

Synthesis and anti-inflammatory analgesic activities of phenylfuroxan-coupled diclofenac / 药学学报

<p><b>AIM</b>To search for new derivatives of diclofenac (DC) having higher potency than the parent drug and lacking its undesirable effects.</p><p><b>METHODS</b>Coupling DC with NO donor 3-hydroxymethyl-4-phenylfuroxan and its isomer through esterification, evaluating anti-inflammatory and analgesic activities, observing side effects in the rat gastrointestinal (GI) tract and assessing NO releasing ability both in vitro and in vivo.</p><p><b>RESULTS</b>Fifteen new compounds including nine target ones (II1-9) were synthesized, and their structures were determined by IR, 1HNMR, MS and elemental analysis. Compounds II3 and II9 showed anti-inflammatory activity comparable to DC. Compound II2 showed stronger anti-inflammatory and analgesic activities and less GI side effect than DC, and released NO in vivo.</p><p><b>CONCLUSION</b>Compound II2 is worthy to be intensively studied.</p>