Discovery of novel 4-phenylquinazoline-based BRD4 inhibitors for cardiac fibrosis

Bromodomain containing protein 4 (BRD4), as an epigenetic reader, can specifically bind to the acetyl lysine residues of histones and has emerged as an attractive therapeutic target for various diseases, including cancer, cardiac remodeling and heart failure. Herein, we described the discovery of hit 5 bearing 4-phenylquinazoline skeleton through a high-throughput virtual screen using 2,003,400 compound library (enamine). Then, structure-activity relationship (SAR) study was performed and 47 new 4-phenylquinazoline derivatives toward BRD4 were further designed, synthesized and evaluated, using HTRF assay set up in our lab. Eventually, we identified compound C-34, which possessed better pharmacokinetic and physicochemical properties as well as lower cytotoxicity against NRCF and NRCM cells, compared to the positive control JQ1. Using computer-based molecular docking and cellular thermal shift assay, we further verified that C-34 could target BRD4 at molecular and cellular levels. Furthermore, treatment with C-34 effectively alleviated fibroblast activation in vitro and cardiac fibrosis in vivo, which was correlated with the decreased expression of BRD4 downstream target c-MYC as well as the depressed TGF-β1/Smad2/3 signaling pathway. Taken together, our findings indicate that novel BRD4 inhibitor C-34 tethering a 4-phenylquinazoline scaffold can serve as a lead compound for further development to treat fibrotic cardiovascular disease.

Identification of ferroptosis as a novel mechanism for antitumor activity of natural product derivative a2 in gastric cancer

Ferroptosis is a type of cell death accompanied by iron-dependent lipid peroxidation, thus stimulating ferroptosis may be a potential strategy for treating gastric cancer, therapeutic agents against which are urgently required. Jiyuan oridonin A (JDA) is a natural compound isolated from Jiyuan

Discovery of thiosemicarbazone derivatives as effective New Delhi metallo-β-lactamase-1 (NDM-1) inhibitors against NDM-1 producing clinical isolates

@#New Delhi metallo-β-lactamase-1 (NDM-1) is capable of hydrolyzing nearly all β-lactam antibiotics, posing an emerging threat to public health. There are currently less effective treatment options for treating NDM-1 positive “superbug”, and no promising NDM-1 inhibitors were used in clinical practice. In this study, structure–activity relationship based on thiosemicarbazone derivatives was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds 19bg and 19bh exhibited excellent activity against 10 NDM-positive isolate clinical isolates in reversing MEM resistance. Further studies demonstrated compounds 19bg and 19bh were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44 μmol/L, respectively. Molecular docking speculated that compounds 19bg and 19bh were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities even at concentrations of 1000 mg/mL against red blood cells. In vivo experimental results showed combination of MEM and compound 19bh was markedly effective in treating infections caused by NDM-1 positive strain and prolonging the survival time of sepsis mice. Our finding showed that compound 19bh might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug.

Discovery of 1,2,3triazolo4,5-pyrimidine derivatives as highly potent, selective, and cellularly active USP28 inhibitors

Ubiquitin specific peptidase 28 (USP28) is closely associated to the occurrence and development of various malignancies, and thus has been validated as a promising therapeutic target for cancer therapy. To date, only few USP28 inhibitors with moderate inhibitory activity have been reported, highly potent and selective USP28 inhibitors with new chemotypes remain to be discovered for pathologically investigating the roles of deubiquitinase. In this current study, we reported the synthesis and biological evaluation of new [1,2,3]triazolo[4,5-]pyrimidine derivatives as potent USP28 inhibitors. Especially, compound potently inhibited USP28 (IC = 1.10 ± 0.02 μmol/L,  = 40 nmol/L), showing selectivity over USP7 and LSD1 (IC > 100 μmol/L). Compound was cellularly engaged to USP28 in gastric cancer cells. Compound reversibly bound to USP28 and directly affected its protein levels, thus inhibiting the proliferation, cell cycle at S phase, and epithelial-mesenchymal transition (EMT) progression in gastric cancer cell lines. Docking studies were performed to rationalize the potency of compound . Collectively, compound could serve as a new tool compound for the development of new USP28 inhibitors for exploring the roles of deubiquitinase in cancers.

Association between resting heart rate trajectory pattern and risk of cardiovascular and cerebrovascular diseases / 中华心血管病杂志

Objective@#To examine whether the long-term resting heart rate (RHR) pattern can predict the risk of cardiovascular and cerebrovascular diseases (CVDs).@*Methods@#This prospective cohort study included 63 040 participants who took part in the health examination in 2006 and one of the health examinations on 2008 or 2010 and were free of myocardial infarction, stroke, arrhythmia, cancer and not treated with β-recepter blocker. The outcomes were the first occurrence of myocardial infarction and stroke during the follow up ended on December 31, 2015. RHRs were measured in 2006, 2008, and 2010. We used latent mixture modeling SAS Proc procedure to identify RHR trajectories. We identified 4 distinct RHR trajectory patterns based on the data derived from 2006 and on the pattern change during 2006 to 2010 (low-stable, moderate-stable, moderate-increasing, elevated-decreasing). Collected the general clinical data of the patients. Cox regression model was used to determine the association between RHR trajectory patterns and the risk of CVDs during follow up. Hazard ratio (HR) with 95% confidence intervals (CI) were calculated using Cox regression modeling.@*Results@#There were statistical significance among the 4 distinct RHR trajectory patterns on the following variables: age, gender, smoking status, drinking status, physical activity, education status, history of use antihypertensive drugs, history of hypertension,history of diabetes, body mass index, triglycerides, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, fasting blood glucose, and the level of high-sensitivity C-reactive protein (all P<0.01). The moderate-increasing pattern experienced the highest risk of developing stroke and CVDs among all 4 patterns. The cumulative incidence of cerebral infarction, cerebral hemorrhage and CVDs in the order of low-stable trajectory, moderate-stable trajectory and moderate-increasing trajectory. The cumulative incidences of cerebral infarction, cerebral hemorrhage and CVDs in elevated-decreasing trajectory group were significantly lower than those in moderate-increasing trajectory group, but higher than those in moderate-stable trajectory group. Compared to the low-stable pattern, adjusted HR was 1.3 (95%CI 1.0-1.6) for the moderate-increasing pattern after adjustment for potential confounders.@*Conclusion@#Our study finds that individuals with moderate-increasing RHR trajectory pattern are associated with higher risk of cardiovascular and CVDs.

Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor

EGFR tyrosine kinase inhibitor (EGFR-TKI) has been used successfully in clinic for the treatment of solid tumors. In the present study, we reported the discovery of from our in-house diverse compound library, which was validated to be a potent and selective EGFR-TKI. showed excellent inhibitory activities against EGFR (IC = 0.81 nmol/L), EGFR (IC = 1.2 nmol/L) and EGFR (IC = 1.1 nmol/L), but was less effective or even inactive against other nine kinases. also displayed excellent antiproliferative activities against a panel of human cancer cell lines, and exhibited the ability to reduce colony formation and wound healing the same as gefitinib. We found that upon oral administration showed better anti-tumor activity in A431 bearing xenograft mouse models compared to gefitinib. In addition, showed better intestinal absorption than gefitinib and had favorable pharmacokinetic properties and microsomal metabolic stability in different species. These studies indicate that has strong antitumor activity and , and could be used for the development of anti-lung cancer agent targeting EGFR.

Development of the triazole-fused pyrimidine derivatives as highly potent and reversible inhibitors of histone lysine specific demethylase 1 (LSD1/KDM1A)

Histone lysine specific demethylase 1 (LSD1) has been recognized as an important modulator in post-translational process in epigenetics. Dysregulation of LSD1 has been implicated in the development of various cancers. Herein, we report the discovery of the hit compound (IC = 3.93 μmol/L) and further medicinal chemistry efforts, leading to the generation of compound (IC = 49 nmol/L, and = 16 nmol/L), which inhibited LSD1 reversibly and competitively with H3K4me2, and was selective to LSD1 over MAO-A/B. Docking studies were performed to rationalize the potency of compound . Compound also showed strong antiproliferative activity against four leukemia cell lines (OCL-AML3, K562, THP-1 and U937) as well as the lymphoma cell line Raji with the IC values of 1.79, 1.30, 0.45, 1.22 and 1.40 μmol/L, respectively. In THP-1 cell line, significantly inhibited colony formation and caused remarkable morphological changes. Compound induced expression of CD86 and CD11b in THP-1 cells, confirming its cellular activity and ability of inducing differentiation. The findings further indicate that targeting LSD1 is a promising strategy for AML treatment, the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.

Discussion on traditional Chinese medicine treatment models of depression named "three phases, five internal organs and ten syndromes" / 国际中医中药杂志

Based on the inheritance, the research group summarized the transmissive pathogenesis of depression in three typical stages, formulating the stepward treatment units which included Chinese medicine, acupuncture and TCM characterized psychotherapy, and formed a sequential treatment plan that balanced the principle of strengthening healthy Qi to eliminate pathogens, active and passive treatment, physical therapy and psychotherapy. Based on the retrospective analyses, ten typical clinical syndromes have been formed, constituting the pattern differentiation of "Three Phases, Five internal organs and Ten syndromes" for depression, which sysmatically showed the TCM syndrome differentiation. This work promoted the experiences and methods of treating depression by Chinese medicine.

Risk factors of cholecystitis after radical gastrectomy for gastric cancer / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To investigate the risk factor of cholecystitis after radical gastrectomy for gastric cancer.</p><p><b>METHODS</b>Clinicpathological data of 553 gastric cancer patients with normal gallbladders undergoing radical gastrectomy in Tianjin Medical University Cancer Institute and Hospital between March 2013 and March 2015 were analyzed retrospectively. Univariate and multivariate analysis were applied to evaluate factors influencing the cholecystitis after radical gastrectomy using log-rank and logistic regression model.</p><p><b>RESULTS</b>There were 360 males and 193 females with a median age of 60 years. All patients were followed up from 6 months to 2 years. The incidence of cholecystitis after radical gastrectomy for gastric cancer was 33.1%(183/553), while incidence of cholecystolithiasis was 4.9%(27/553). In addition, the cholecystitis incidence of patients with No.12 lymph node cleaning was 39.6%(89/225), while with No.8a lymph node cleaning was 38.0%(151/397), with No.5 lymph node cleaning was 38.0%(68/179), with No.7 lymph node cleaning was 34.4%(138/402), with No.9 lymph node cleaning was 34.7%(136/392). Univariate log-rank test indicated that the lymphadenectomy of No.8a(χ(2)=15.530, P=0.000), No.12 group(χ(2)=7.157, P=0.007) and surgical methods (χ(2)=7.427, P=0.024) were significantly associated with cholecystitis after radical gastrectomy. Multivariate analysis showed that the lymphadenectomy of No.8a was independent factor of cholecystitis after radical gastrectomy (OR=2.016, 95% CI:1.244 to 3.267, P=0.004).</p><p><b>CONCLUSIONS</b>Vagal nerve trunk and sympathetic ganglion should be protected carefully during No.8a lymphadenectomy in radical gastrectomy for gastric cancer, in order to reduce the incidence of postoperative cholecystitis.</p>

Jaridonin induces apoptosis in human esophageal cancer cells by depleting GSH and inducing DNA damage / 中华肿瘤杂志

<p><b>OBJECTIVE</b>The aim of this study was to explore the molecular mechanism of apoptosis in esophageal cancer cells induced by Isodon rubescens.</p><p><b>METHODS</b>The DNA-damage effect of Jaridonin was detected by single cell gel electrophoresis (SCGE). The p53 protein was determined by Western blot. GSH assay kit was employed to determine the GSH content in human esophageal cancer EC-1 cells. Intracellular levels of hydrogen peroxide (H2O2) or superoxide (O(2).-) were determined using the redox-sensitive probes 2', 7'-dichlorodihydrofluorescein diacetate (DCF) or dihydroethidium (DHE), and the fluorescence signal was assayed by fluorescence microscopy and by flow cytometry.</p><p><b>RESULTS</b>Jaridonin induced DNA damage in EC-1 cells remarkably. The olive tail moments (OTM) of control and 20, 40 µmol/L Jaridonin were 3.2, 45.2 and 89.0, respectively. Compared with the control, the differences were significant (P < 0.01 for both). Jaridonin resulted in extensive p53 up-regulation in the EC-1 cells. More importantly, the p53 up-regulation occurred as early as 2 h after Jaridonin incubation, and in a time-dependent manner (P < 0.05). p53 siRNA transfection inhibited apoptosis in the EC-1 cells, and the Jaridonin-induced apoptosis rate was reduced from 38.5% to 8.8%. Intracellular level of H2O2 was increased by Jaridonin, whereas the level of O(2).- was barely changed. The GSH content in EC-1 cells was reduced from (10.3 ± 1.6) nmol/mg protein to (4.6 ± 2.1) nmol/mg protein after 20 µmol/L Jaridonin incubation for 8 h, and it was further reduced with the increase of Jaridonin concentration. Jaridonin induced DNA damage, H2O2 accumulation and apoptosis were significantly attenuated in the presence of GSH, but Jaridonin showed little effect on normal human liver L-02 cells.</p><p><b>CONCLUSIONS</b>Jaridonin selectively induces apoptosis in esophageal cancer EC-1 cells through H2O2-mediated DNA damage by depleting GSH.</p>

Exploration and Practice of Industry-university-institute Unification Mode for Pharmacy Professionals / 中国药房

OBJECTIVE:To explore the new mode of industry-university-institute unification for pharmacy professionals. METHODS:The research-teaching interactive platform was established through the principles of“complementary advantages, shared interests and mutual benefits”. RESULTS:It changed the traditional teaching mode,and it ensured the professional plan-ning,curriculum development and training objectives of students based on“4 analysis,2 setting and 1 implementation”. CONCLU-SIONS:The opportunities for cooperation between students and employers were broadened and students’awareness of innovation and entrepreneurship was enhanced. It cultivates project-based pharmaceutical,technical and skilled personnel,solves the problem of industry-university-institute unification and has certain significance for the development of China’s pharmaceutical education.

Jaridonin:Selective killing of cancer cells through oxidative stress / 中国药理学通报

Aim To investigate Jaridonin′s selective killing of cancer cells and explore the related molecular mechanism. Methods After treatment by Jaridonin for 24 h, the effect of Jaridonin on the cell viability was examined using MTT assay. The effect of Jaridonin on cytomorphology and mitochondrial membrane poten-tial (Δψm) was observed by a fluorescence microsco-py. The apoptosis of cell lines treated with Jaridonin, as well as the level of reactive oxygen species ( ROS ) was analyzed by flow cytometry. Expression of the pro-teins related with mitochondria apoptosis pathways was detected by Western blot. Results Jaridonin caused strong antiproliferative and apoptotic effects on MGC-803 cells, but there were not remarkable effects on GES-1 cells. Furthermore, the expression of Bax was up-regulated, and the release of cytochrome c from mi-tochondria to cytosol was also promoted in MGC-803 cells treated by Jaridonin. The cleavage of caspase-3 in MGC-803 cells was also observed. Jaridonin increased persistently intracellular levels of ROS in MGC-803 cells, whereas the level of ROS in GES-1 rose in the first stage, and then decreased, and dropped to the basic level after 6 h. More interestingly, Jaridonin-in-duced ROS accumulation and the inhibition of MGC-803 cell proliferation were almost completely attenuated in the presence of GSH. Conclusions Jaridonin se-lectively kills cancer cells and induces apoptosis in MGC-803 through ROS-mediated mitochondrial dam-age.

Clinical observation of abdominal regional fluorouracil implants in advanced gastric cancer patients during operation / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To investigate the postoperative adverse events and survival of patients with sustained-released fluorouracil implanted during operation.</p><p><b>METHODS</b>Data of 124 patients with advanced gastric cancer undergoing radical operation in Tianjin Medical University Cancer Institute and Hospital from January 2007 to January 2009 were analyzed retrospectively. All the patients were divided into two groups according to whether intra-operative fluorouracil was implanted or not. The treatment group(n=64) was implanted with fluorouracil in abdominal cavity after radical resection. The control group(n=60) did not receive fluorouracil implant in abdominal cavity after radical resection. Abdominal drainage fluid, temperature and adverse events within 15 postoperative days and 3-year survival were observed and compared between the two groups.</p><p><b>RESULTS</b>Pathological findings of the two groups were similar. No statistical significances existed in abdominal drainage fluid, temperature and adverse events within 15 postoperative days(P>0.05). The 3-year survival rate was higher in treatment group(64.3% vs. 42.4%, P=0.018).</p><p><b>CONCLUSION</b>Intra-operative sustained-released fluorouracil implants are safe and tolerable, and can improve the survival rate of patients with advanced gastric cancer.</p>

Operation and management of specialized course of clinical medicine based on ‘ cooperation between schools and hospitals’ / 中华医学教育探索杂志

On the basis of ‘ cooperation between schools and hospitals’,teaching of specialized course of clinical medicine in the second academic year was arranged in affiliated hospitals and teaching hospitals.According to the teaching content and features of specialized courses,flexible teaching methods were adopted,including theoretical instruction,bedside teaching,case studies,situational teaching,integration of teaching,practicing and studying and clinical internships etc.Through selecting and training qualified teachers,establishing practical training base and strengthening teaching management and quality control,the quality of teaching was effectively guaranteed and satisfactory teaching effect was received.

On the relationship between the change in waist circumference and new onset of diabetes: Study on a population of Northern China / 中华内分泌代谢杂志

Objective To explore the relationship between the change in waist circumference (WC) and new onset diabetes (NOD) in a population of north China.Methods A total of 101510 subjects took part in the health examination from 2006 to 2007 for the employees of Kailuan Group.89364 subjects with fasting plasma glucose (FPG) ＜7.0 mmol/L,no history of diabetes,with complete data of FPG and WC,and without taking hypoglycemic agents were sclected as the observation cohort.Subjects who did not participate in the health examination from 2010 to 2011 and had incomplete data were finally excluded and thus 58426 subjects were included for final analysis.According to the baseline WC measurement and its quartile in the health examination during 2006 to 2007,the observed population was divided into two groups (obese group and non-obese group) or four groups ( first,second,third,and forth quartile groups).Multiple logistic regression analysis was used to test the relation between the change in WC and NOD.Results ( 1 ) The incidence of NOD in obese group was higher than that in non-obese group (8.02％ vs 3.37％,P＜0.01 ).Along with increasing WC in the 4 quartile groups,the incidence of NOD was progressively increased,being 2.32％,3.62％,5.46％,and 8.89％ respectively in the total population ( 2.84％,3.65％,5.32％,and 8.95％ in male,and 1.50％,3.41％,6.22％,and 8.51％ in female).( 2 ) Multiple logistic regression analysis showed that compared with the first quartile group,the second,third,and forth quartile groups had increased risks of NOD after adjusting age,gender,and other risk factors,the OR value being 1.17,1.47,and 1.95,respectively.After adjusting above factors in different genders,the influence of the second group on NOD in males and females was not significant,however,they still increased the risks of NOD,with the OR value being 1.08,1.36,and 1.90 in male,and 1.35,1.70,and 1.88 in female,respectively.Conclusion The incidence of NOD is increased with increasing WC.

Application value of urine modified nucleoside's detection in prognosis of bladder transitional cell carcinoma / 中华泌尿外科杂志

Objective To study the application value of modified urine nucleoside's detection in prognosis of patients with bladder cancer. Methods We enrolled 85 patients with bladder transitional cell carcinoma confirmed by pathological examination.The 85 patients fulfilled one-year follow-up visit after TUR-BT and were reviewed every three months.The 85 patients did not relapse in the first third month after operation.At the sixth month after operation,20 cases relapsed.18 cases and 19 cases relapsed at the ninth month and the twelfth month after operation.Patients with recurrence added up to 57 cases as the recurrent group.The remaining 28 cases did not relapse at one year after operation as the no recurrent group.Of the 85 cases,55 cases were in T(is) - T1,while 30 cases were in T2 - T4.Of the 85 cases,27 cases were with G1,40 cases were with G2 and 18 cases were with G3.In T(is) -T1,there were 35 cases in recurrent group,while there were 20 cases in the no recurrent group.In T2 -T4,there were 22 cases in recurrent group,while there were 8 cases in the no recurrent group.There were 50 normal people in the control group.Highperformance liquid chromatography/electrospray ionization-quadrupole-time-of-flight mass spectromerry was used to measure the levels of change of two urine modified nucleosides (M1A,1-MeI) which the patients with bladder cancer had different pathology grades,clinical stages,before or after operation and recurrence or no recurrence. Results The levels at third month after operation in no recurrent group ( M1A:3.24 ± 0.40,1 -MeI:5.73 ± 0.67 ) were significantly lower than that before operation ( M 1A:4.34 ± 0.98,1-MeI:14.22 ± 4.05,P ＜ 0.005 ),and remained in low status at another time points after operation.The levels at the third month after operation in recurrent group (M1A:3.31 ±0.33,1-MeI:5.67 ±0.55) were significantly lower than that before operation ( M1A:4.32 ± 1.19,1-MeI:14.31 ± 4.12,P ＜ 0.005 ),which was on the rise and indicating a high level approaching the condition before operation.According to the time point before the operation,recurrent group and no recurrent group were higher than control group (M1A:2.91 ±0.84,1-MeI:5.56 ± 1.25,P ＜ 0.01 ).The levels at the sixth month,ninth month and twelfth month after operation in recurrent group ( M 1A referring to 4.04 ± 0.48,4.11 ± 0.47,4.09 ± 0.53 ;1-MeI referring to1 1.46 ± 1.34,12.14 ± 1.22,12.33 ± 1.27) were the highest (P ＜ 0.01 ).The levels of change of two urine modified nucleosides between pathology grade and clinical stage had no statistical difference ( P ＞ 0.01 ).The levels in recurrence group in T(is) - T1 ( M1 A:5.92 ± 1.28,1-MeI:20.01 ± 8.53 )were higher than the levels in no recurrent group ( M1A:4.02 ±1.22,1 -MeI:11.21 ± 6.45,P ＜ 0.05 ),which was the same in T2 - T4. Conclusion Urine modified nucleosides detection offer a certain clinical value the prognostic of operated bladder cancer patients.

Research in influencing factors of job satisfaction degree among community nurses in Qiqihar city / 中国实用护理杂志

Objective To understand the influencing factors of job satisfaction degree among community nurses in Qiqihar city.Methods Using stratified systematic cluster sampling method,we conducted self-administered questionnaire,results were subsequently analyzed.Results Logistic regression analysis was introduced,influencing factors of job satisfaction degree included work location,age,marital status,professional title,properties of jobs,monthly income and work length.Conclusions The government should pay attention to community health care services,gasp the situation of job satisfaction degree of community nurses timely,take innovative measures,improve job satisfaction degree of community nurses,stabilize community nursing teams and promote the development of community health services.

Association of cathepsin L with coronary heart disease and its risk factors / 中南大学学报(医学版)

OBJECTIVE@#To explore the relationship of cathepsin L (CatL) with coronary heart disease (CHD), severity of coronary stenosis and risk factors of CHD.@*METHODS@#A total of 137 CHD patients and 48 controls were included in the study, to determined the serum levels of CatL, high sensitive C reactive protein (hs-CRP), fasting glucose (FBS), total cholesterol, triglyceride, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol (HDL-C), apolipoprotein A1(Apo-A1) and apolipoprotein B. All the subjects were invited for a coronary angiography, using the sum of the Gensini scores to assess the severity of coronary artery stenosis.@*RESULTS@#Serum CatL levels were significantly higher in CHD patients (5.63 +/= 0.12 microg/L) than non-CHD subjects (3.93 +/= 0.22 microg/L, P<0.01). CatL was an independent risk factor of CHD in Logistic regression analysis [Exp(B)=2.341, 95%CI 1.567 approximately 3.496, P<0.01]. Serum CatL levels were associated positively with the Gensini scores(r=0.228, P<0.01); In fact, CatL was an independent correlator of Gensini scores (P<0.05). CatL inversely associated with HDL-C (r=-0.228, P<0.01) and ApoA1(r=-0.187, P<0.05), and positively with FBS(r=0.161, P<0.05).@*CONCLUSION@#CatL is involved in the pathogenesis of CHD. Serum CatL levels could reflect the severity of coronary luminal narrowings. CatL might participate in glucose and lipid metabolic disorders.

Study of Key Electrochemical Problems in Transdermal Noninvasive Glucose Monitoring / 分析化学

Several key problems were analysed for the transdermal noninvasive glucose monitoring. A modified calibration equation was proposed for the high-sensitivity glucose biosensor due to its narrow linear range. The new equation has increased the sensors' linear range by 20 times. A new diffuse model was constructed for the electrode system of glucose sensor,aiming at the unique "finite space" electrochemical problem in trans-dermal technique. In addition,electrode masks were utilized to solve the problem of electrode loss in longtime glucose monitoring. In animal in-vivo experiments,70.1 % of the noninvasive glucose data points were clinically accurate,while the remains were clinically acceptable. All solutions mentioned above were based on both theoretical analysis and experimental validation,promoting the realization and optimization of transdermal noninvasive glucose monitoring techniques.

Secoiridoid glycosides from Flos Lonicerae / 中草药

Objective To study the constituents in water-extracts from Flos Lonicerae. Methods Compounds were isolated and purified by using various column chromatography such as D101, Sephadex LH-20, and silica gel, etc. Their structures were identified on the basis of physical and spectral data. Results Seven secoiridoid glycosides were obtained and identified as vogeloside (Ⅰ), 7-epi-vogeloside (Ⅱ), secologanic acid (Ⅲ), sweroside (Ⅳ), secoxyloganin (Ⅴ), secologanoside (Ⅵ), (E)-aldosecologanin (Ⅶ). Conclusion Among them, compounds Ⅲ and Ⅵ are firstly obtained from the plants in Lonicera L. The structure of compound Ⅶ is rare in nature so far.