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1.
Chinese Journal of Cardiology ; (12): 136-142, 2021.
Article in Chinese | WPRIM | ID: wpr-941249

ABSTRACT

Objective: To explore the long-term effect of intravascular ultrasound (IVUS) guidance on patients with chronic kidney disease (CKD) undergoing drug-eluting stent (DES) implantation. Methods: Data used in this study derived from ULTIMATE trial, which was a prospective, multicenter, randomized study. From August 2014 to May 2017, 1 448 patients with coronary heart disease undergoing DES implantation were selected from 8 domestic centers and randomly divided into two groups in the ratio of 1∶1 (IVUS or coronary angiography guided stent implantation). A total of 1 443 patients with the baseline serum creatine available were enrolled. The patients were divided into CKD group and non CKD group. CKD was defined as the estimated glomerular filtration rate (eGFR) derived from Cockcroft Gault (CG) formula< 60 ml·min-1·1.73 m-2 for at least 3 months. Primary endpoint of this study was target vessel failure (TVF) at 3 years, including cardiac death, target vessel myocardial infarction, and clinically-driven target vessel revascularization. Kaplan Meier method was used for survival analysis, and log rank test was used to compare the occurrence of end-point events in each group. Cox proportional hazards model was used to calculate HR and 95%CI, and interaction was tested. Multivariate Cox regression was used to analyze the independent influencing factors of TVF. Results: A total of 1 443 patients with coronary heart disease were enrolled in this study, including 349 (24.2%) patients in CKD group and 1 094 patients in non CKD group. In CKD group, IVUS was used to guide stent implantation in 180 cases and angiography was used in 169 cases; in non CKD group, IVUS was used to guide stent implantation in 543 cases and angiography was used in 551 cases. Three-year clinical follow-up was available in 1 418 patients (98.3%). The incidence of TVF in CKD group was 12.0% (42/349), which was higher than that in non CKD group (7.4% (81/1 094) (P = 0.01). The difference was mainly due to the higher cardiac mortality in CKD group (4.6% (16/349) vs. 1.5% (16/1094), P<0.001). In CKD group, the incidence of TVF in patients who underwent IVUS guided stent implantation was lower than that in angiography guided stent implantation (8.3% (15/180) vs. 16.0% (27/169), P = 0.03). There was no significant difference in the incidence of TVF between IVUS guided stent implantation and angiography guided stent implantation in non CKD group (5.9% (32/543) vs. 8.9% (49/551), P = 0.06), and there was no interaction (P = 0.47). Multivariate Cox regression analysis showed that IVUS guidance (HR = 0.56, 95%CI 0.39-0.81, P = 0.002), CKD (HR = 1.83, 95%CI 1.17-2.87, P = 0.010) and stent length (every 10 mm increase) (HR = 1.11, 95%CI 1.04-1.19, P = 0.002) were independent risk factors for TVF within 3 years after DES implantation. Conclusions: CKD patients undergoing DES implantation are associated with a higher risk of 3-year TVF. More importantly, the risk of TVF could be significantly decreased through IVUS guidance in comparison with angiography guidance in patients with CKD.


Subject(s)
Humans , Coronary Angiography , Coronary Artery Disease/surgery , Drug-Eluting Stents , Percutaneous Coronary Intervention , Prospective Studies , Renal Insufficiency, Chronic , Treatment Outcome , Ultrasonography, Interventional
2.
Chinese Pharmacological Bulletin ; (12): 38-41, 2020.
Article in Chinese | WPRIM | ID: wpr-857041

ABSTRACT

Aim To study the effects of melatonin on glucose output in insulin resistant HepG2 cells and the related mechanism. Methods Insulin resistant HepG2 cells were induced by high glucose and insulin (HGI) (25 mmol • L"1 and 1 (irnol • L"1 respectively) co-culture for 24 h,and then melatonin (10 nmol • L"1) was supplied. The glucose uptake and the gly-cogen content were measured. Levels of protein p-Akt, p-FoxOl as well as p-GSK-30 were evaluated by Western blot. The nuclear export of FoxOl and its intracellular localization were detected by immunofluorescence. Results HGI incubation led to significant decrease in insulin-stimulated glucose uptake and glyco-gen synthesis in HepG2 cells (P < 0. 0( ). However, melatonin reversed these inhibitory effects by increasing glucose uptake and glycogen synthesis significantly (P<0. 01). The results also showed that melatonin not only up-regulated levels of protein p-GSK-3 (3, p-Akt and p-FoxOl but also promoted cytoplasm translocation of FoxOl. Conclusions Melatonin could regulate glycogenesis and gluconeogenesis ih insulin resistant HepG2 cells via Akt/GSK-3(3 and Akt/FoxOl pathway. It thus suppresses the endogenous glucose output and improves the glucose metabolism.

3.
Singapore medical journal ; : 87-93, 2018.
Article in English | WPRIM | ID: wpr-773459

ABSTRACT

INTRODUCTION@#Dental caries, which is prevalent in Singapore preschoolers, is a disease that has a major impact on children's health and places a high cost on the society and health services. Oral health programmes for young children implemented in some parts of the world have been shown to be effective in the prevention of dental caries. We aimed to examine the clinical efficacy of a two-year oral health programme for infants and toddlers in Singapore.@*METHODS@#90 children and their caregivers participated in the programme, and 64 children, who were 24 months older than the intervention group at the initial visit, were recruited as controls in a quasi-experimental study design. We evaluated the presence of severe early childhood caries (SECC) and dmfs in the control group at the initial visit and in the intervention group after the completion of the two-year programme.@*RESULTS@#Some children in the intervention (7.8%) and control (31.3%) groups (p < 0.001) had SECC (difference 23.5%, 95% confidence interval 11%-36%). A higher percentage of children in the intervention group had dmfs = 0 and habits associated with low risk for caries. The odds of SECC in the control group were three times higher than that for the intervention group, and the effect was significant (p = 0.037) after adjustment for other significant risk factors.@*CONCLUSION@#The preventive oral health programme in Singapore was successful in reducing SECC among infants and toddlers when targeted behaviour modifications were implemented.


Subject(s)
Child, Preschool , Female , Humans , Infant , Male , Caregivers , Dental Caries , Dentistry , Methods , Health Care Costs , Health Promotion , Oral Health , Pediatrics , Program Evaluation , Regression Analysis , Research Design , Risk Factors , Singapore
4.
Chinese journal of integrative medicine ; (12): 336-342, 2018.
Article in English | WPRIM | ID: wpr-687924

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the effect and safety of Kuanxiong Aerosol (, KA) on patients with angina pectoris.</p><p><b>METHODS</b>Block randomization was performed to randomly allocate 750 patients into KA (376 cases) and control groups (374 cases). During an angina attack, the KA group received 3 consecutive sublingual sprays of KA (0.6 mL per spray). The control group received 1 sublingual nitroglycerin tablet (NT, 0.5 mg/tablet). Log-rank tests and Kaplan-Meier estimations were used to estimate the angina remission rates at 6 time-points after treatment (1, 2, 3, 4, 5, and >5 min). Logistic regression analysis was performed to observe the factors inflfluencing the rate of effective angina remission, and the remission rates and incidences of adverse reactions were compared for different Canadian Cardiovascular Society (CCS) classes of angina.</p><p><b>RESULTS</b>The 5-min remission rates in the KA and control groups were not signifificantly different (94.41% vs. 90.64%, P>0.05). The angina CCS class signifificantly inflfluenced the rate of remission (95% confidence interval = 0.483-0.740, P<0.01). In the CCS subgroup analysis, the 3-and 5-min remission rates for KA and NT were similar in the CCSII and III subgroups (P>0.05), while they were signifificantly better for KA in the CCSI and II subgroups (P<0.05 or P<0.01). Furthermore, the incidence of adverse reactions was signifificantly lower in the KA group than in the control group for the CCSII and III subgroups (9.29% vs. 26.22%, 10.13% vs. 20.88%, P<0.05 or P<0.01).</p><p><b>CONCLUSIONS</b>KA is not inferior to NT in the remission of angina. Furthermore, in CCSII and III patients, KA is superior to NT, with a lower incidence of adverse reactions. (Registration No. ChiCTRIPR-15007204).</p>


Subject(s)
Female , Humans , Male , Middle Aged , Aerosols , Therapeutic Uses , Angina Pectoris , Drug Therapy , Case-Control Studies , Drugs, Chinese Herbal , Therapeutic Uses , Kaplan-Meier Estimate , Logistic Models , Remission Induction , Treatment Outcome
5.
China Journal of Chinese Materia Medica ; (24): 2470-2473, 2018.
Article in Chinese | WPRIM | ID: wpr-687432

ABSTRACT

There are 400 thousand patients with long-term hemodialysis in China nowadays. Hemodialysis, as the most common alternative to renal replacement therapy, prolongs the life span of patients with end stage renal failure. However, there are still many complications of hemodialysis treatment. These complications reduce the quality of life of patients and may even endanger their life, and sometimes they are difficult to deal with. Classical prescriptions, commonly referred to as classical effective prescriptions in modern medicine, mainly indicating the formulas recorded in Treatise on Febrile Diseases and Synopsis of Golden Chamber, were relative to contemporary prescriptions emerging after Song and Yuan dynasties. Prescriptions corresponding to syndromes means one-to-one correspondence between syndromes and prescriptions, with many advantages and that is the key of clinical efficacy. Many complications of hemodialysis patients have typical clinical manifestations, which can match the syndromes corresponding to classical prescriptions, thus quickly relieving the symptoms of patients in clinical application. Six clinical cases of dialysis muscle spasm, disequilibrium syndrome, restless legs syndrome, uremic encephalopathy, post dialysis arrhythmia, and secondary hyperparathyroidism were used in this paper, to explore the intervention strategies for hemodialysis related complications.

6.
Chongqing Medicine ; (36): 1457-1462, 2017.
Article in Chinese | WPRIM | ID: wpr-511931

ABSTRACT

Objective To investigate the expression and effect of high mobility group box 1(HMGB1) and its signaling pathway(HMGB1 RAGE/TLR4-NF-κB-cytokines)in rats with dilatd cardiomyopathy(DCM).Methods The rats were divided into two groups:normal control group (control,n=20) which treated with physiological saline,and DCM group(n=22) which treated with adriamycin(1 mg/kg twice a week)for 6 weeks,and then observed for 2 weeks.Echocardiography was performed at the end of the study.Plasma IL-1,IL-6,TNF-α level were measured by the flow cytometry.The CRP,BNP concentrations were measured by enzyme linked immunosorbent assay (ELISA).The expression of HMGB1 mRNA,TLR4 mRNA,RAGE mRNA,NF κB mRNA were measured by real time PCR.Results There were four rats dead in the DCM group;two rats were randomly selected from the DCM group to certified modeled successfully by echocardiography and pathological examination.Left ventricular end-diastolic diameter (LVEDD) and left ventricular end systolic diameter (LVESD) in DCM group were significantly higher than those in the normal control group(P<0.05);left ventricular ejection fraction (LVEF),left ventricular short axis contractility(FS) in DCM group was significantly lower than that in normal control group(P<0.05).The expression of H MGB1 mRNA,TLR4 mRNA,RAGE mRNA and NF-κB mRNA in myocardial tissue were significantly increased in DCM group than in the normal control saline group (P< 0.05),The expression of HMGB1 mRNA were positively correlated with TLR4 mRNA,RAGE mRNA and NF κB mRNA(r=0.873,P=0.005;r=0.949;P=0.000;r=0.898,P=0.002).The serum levels of IL-1,IL 6,TNF α and CRP were significantly higher in DCM group.The expression of HMGB1 mRNA in myocardial tissue was positively correlated with IL 1,IL-6,TNF-α and CRP(r=0.944,P=0.002;r=0.988,P=0.000;r=0.968,P=0.000;r=0.961,P=0.000).Conclusion HMGB1 and it's inflammation signaling pathway (HMGB1-TLR4/RAGE-NF-κB-cytokines) were highly expressed in dilated cardiomyopathy,and have relationship with left ventricular diameter and cardiac function,they may be involved in the development of DCM.

7.
Journal of Shanghai Jiaotong University(Medical Science) ; (12): 1588-1593, 2017.
Article in Chinese | WPRIM | ID: wpr-665392

ABSTRACT

Objective·To investigate the influence of blocking receptor for advanced glycation end products (RAGE) on macrophages infiltration in diabetic wound healing. Methods·Ninety-six male C57BL/6J mice (8-week-old) were divided into diabetic group (n=72) and normal group (n=24) randomly. Diabetic mice were induced by streptozocin multiple intraperitoneal injection. One full-thickness excisional wound (diameter of 9 mm) was created by a sterilized punch. Diabetic mice were divided into 3 groups in which different topical treatments were applied to the wounds. Anti-RAGE antibody were applied in group R, rabbit IgG applied in group I, normal saline applied in group C. Normal mice were applied with saline topically (group N). All treatments were repeated on day 3 and day 7 after wounded. The wound healing conditions were observed. The wound and surrounding tissues from animals in each group were excised on day 1, 3, and 7 after wounded. Immunohistochemistry was utilized to investigate the changes of macrophages infiltration in quantity. Macrophages were also analyzed with respect to morphology by transmission electron microscopy (TEM). Results·① The wound closure ratio of group R was higher than those of group C and group I on day 14 after being wounded (P=0.000). ② On day 1, the numbers of macrophages in group R and group N were both bigger than those of group C and group I, but smaller on day 14 (P=0.000). ③ The morphological characters of macrophages also existed great differences under TEM. Conclusion·Number and morphology of macrophages are both abnormal in diabetic wound in a RAGE pathway depending manner. Based on macrophages, it suggests that impaired healing of diabetic wound is closely related to RAGE pathway.

8.
Chinese Circulation Journal ; (12): 802-806, 2016.
Article in Chinese | WPRIM | ID: wpr-495231

ABSTRACT

Objective: To explore the application of18F-lfuorodeoxyglucose (FDG) micro- positron emission tomography (PET) myocardial metabolism imaging for evaluating dilated cardiomyopathy model (DCM) in experimental rats. Methods: A total of 12 male SD rats were randomly divided into 2 groups: DCM group, the rats received intraperitoneal injection of adriamycin at 1.0 mg/kg twice per week and Control group, the rats received intraperitoneal injection of normal saline, all animals were treated for 6 weeks followed by 2 weeks observation.n=6 in each group. Echocardiography was performed at pre- and post-modeling,18F-FDG micro-PET myocardial metabolism imaging was conducted after modeling and plasma level of BNP was examined as well. Finally, the rats were scariifed to observe the pathological changes of myocardial tissue. Results: 1 rat died in DCM group and the rest were with successful modeling conifrmed by echocardiography and pathology. Compared with Control group, DCM group showed decreased standard uptake value of18F-FDG (1.23 ± 0.55) vs (6.65 ± 0.41),P<0.01; the standard uptake value of18F-FDG was negatively related to left ventricular end diastolic diameter (LVEDD) (R=-0.709,P=0.015), LVESD (R=-0.924, P=0.000) and plasma level of BNP (R=-0.948,P=0.000), while positively related to LVEF (R=0.968,P=0.000) and fractional shortening (R=0.863,P=0.001). Conclusion:18F-FDG micro-PET myocardial metabolism imaging combining echocardiography, biochemical and pathological examinations may evaluate DCM modeling in rats, which provide a non-invasive and intravital tool for small animal experiment.

9.
Chinese Traditional and Herbal Drugs ; (24): 1236-1242, 2016.
Article in Chinese | WPRIM | ID: wpr-853628

ABSTRACT

Currently, Chinese materia medica is a research hotspot on the treatment of Alzheimer's disease (AD). The extracts from Acorus tatarinowii have a variety of pharmacological effects on the central nervous system, among which the volatile oil and β-asarone are the main active ingredients in A. tatarinowii reported on the effect on improving the learning and memory and prevention of AD. This review focuses on the main active ingredients in A. tatarinowii and progresses in their different therapeutic effects and proposed pharmacological mechanisms for AD on the basis of referring to the relevant literatures at home and abroad.

10.
China Journal of Chinese Materia Medica ; (24): 350-353, 2016.
Article in Chinese | WPRIM | ID: wpr-304848

ABSTRACT

Chinese patent medicines for orthopedics are among the hotspot and difficulty in the rational medication of traditional Chinese medicine (TCM), because they mostly contain toxic medicinal herbs and oriented to special patients. According to the hospital pharmacy practices and the therapeutic theories of TCM, this paper focused on a novel model of rational drug use of Chinese patent medicine for orthopedics based on the principles of ″syndrome-dosage-toxicity differentiation″. We also proposed relevant specifications for guiding their clinical use. Firstly, we proposed a list of the primary clinical application characteristics for rational drug use of orthopedic TCMs, including the syndromes of patient, the dosage of medicine and the toxic ingredients in medicine. Secondly, a database was established for recording the package inserts of all of the 81 orthopedic patent medicines in our hospital, and 2 000 retrospective recipes were analyzed for looking for the high-frequency medicines and common irrational factors. Then clinical case reports involving the adverse reactions and side effects of related drugs were searched from CNKI, VIP and WanFang databases. Then the key information for rational application of each medicine was extracted from these resources and some survey questionnaires. Finally, we established a guide named instructions for clinical use of orthopedic Chinese patient medicines (ICUOCPM) after the discusstion with experts. According to the effect after the practice in hospital for 2 months, the proposed principles of ″syndrome-dosage-toxicity differentiation″ in this paper were believed to be the core elements and the most important clinical monitoring points in TCM for orthopedic patents. It would provide innovative ideas, theoretical guarantee and data support for the development of TCM clinical pharmacy.

11.
Journal of Southern Medical University ; (12): 526-529, 2015.
Article in Chinese | WPRIM | ID: wpr-355335

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the prevalence of PLA2R1 in renal biopsy specimens of patients with idiopathic membranous nephropathy (IMN) and explore the relationship between PLA2R1 and IMN.</p><p><b>METHODS</b>A total of 108 adult patients with biopsy-proved glomerular diseases were enrolled in this study, including 41 with IMN, 2 with hepatitis B-associated membranous nephropathy, 8 with V lupus nephritis, 27 with IgA nephropathy, 19 with minimal change nephropathy, 5 with mild mesangial proliferative glomerulonephritis, and 6 with focal segmental glomeruloselerosis (FSGS). Indirect immunofluorescence assay was used to detect PLA2R1 in the biopsy specimens and the clinical variables of the IMN patients were analyzed.</p><p><b>RESULTS</b>In 35 of the 41 (85.37%) patients with IMN, PLA2R1 was detected with a fine granular pattern in the subepithelial deposits along the glomerular capillary loops. PLA2R1 antigen was not detected in patients with other glomerulopathies. No significant differences were found in age, serum creatinine, serum albumin, or 24-h urinary protein level between PLA2R1-positive and negative patients with IMN (P>0.05).</p><p><b>CONCLUSION</b>According to our results, 85.37% of adult patients with biopsy-proven IMN are positive for PLA2R1 antigen, which, however, does not contribute to variations of the patients' clinical manifestations.</p>


Subject(s)
Adult , Humans , Biopsy , Glomerulonephritis, Membranous , Metabolism , Kidney , Metabolism , Pathology , Kidney Function Tests , Kidney Glomerulus , Pathology , Nephrosis, Lipoid , Metabolism , Receptors, Phospholipase A2 , Metabolism
12.
Chinese Journal of Integrated Traditional and Western Medicine ; (12): 396-401, 2014.
Article in Chinese | WPRIM | ID: wpr-312811

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the anginal attack-relieving efficacy and safety of Kuanxiong Aerosol (KA) in patients with coronary heart disease (CHD).</p><p><b>METHODS</b>A total of 780 patients confirmatively diagnosed as CHD angina from November 2011 to December 2012 in 13 medical centers in the mainland area were assigned to 2 groups by blocked randomization, the treatment group (376 cases) and the control group (374 cases). When the angina attacked, patients in the treatment group received sublingual spray three times, 0.6 mL each time, while those in the control group sublingually dissolved Nitroglycerin Tablet (NT), 0.5 mg each tablet. The effective rate of angina relief, efficacy of electrocardiogram (ECG), and the incidence of adverse reactions were observed.</p><p><b>RESULTS</b>The 3 min and 5 min remission rates of angina attack were 53.72% (202/376) and 94.41% (355/376) in the treatment group, and 47.86% (179/374) and 90.64% (339/374) in the control group. The 95% confidence interval (CI) of the difference between the 2 groups of 3 min and 5 min remission rates of angina attacks were [(-1.84%, 12.32%) and (-1.33%, 6.85%) respectively, P > 0.05]. The total improvement rates of ST-T changes in the treatment group and the control group after treatment were 74.07% and 73.13% respectively (P > 0.05). The adverse reaction rate was 9.31 (35/376 cases) in the treatment group and 22.46% (84/374 cases) in the control group (P < 0.01).</p><p><b>CONCLUSION</b>KA was not inferior to NT in relieving anginal attacks and improving ischemic ECG changes, and had obviously less adverse reaction.</p>


Subject(s)
Aged , Female , Humans , Male , Middle Aged , Angina Pectoris , Drug Therapy , Coronary Disease , Drug Therapy , Drug Combinations , Drugs, Chinese Herbal , Therapeutic Uses , Oils, Volatile , Therapeutic Uses , Phytotherapy
13.
Shanghai Journal of Preventive Medicine ; (12): 581-583,584, 2013.
Article in Chinese | WPRIM | ID: wpr-789252

ABSTRACT

[Objective] To explore the value of the Pressure Ulcer Scale for Healing ( PUSH) tool in evaluating the effect of debridement on pressure ulcers in elder patients . [ Methods] A group of 60 patients with (82 sites) II-IV grade pressure ulcers were recruited in the study .The ulcers were randomly assigned into autolytic debridement group ( n=42 ) and combined debridement group ( n=40 ) .Two groups of wounds were assessed and debrided by consensus procedure porcess respectively .The wounds were ob-served and evaluated by trained nurses at 7,14,21days after debredement , and the results used in PUSH scoring were recorded and subjected to statistical analysis with the SPSS 11.0 software. [Results] The value of pressure ulcer scale for healing ( PUSH) for autolytic、combined debridement group , at 7days( P>0.05) were not significantly different, at 14 days(P<0.05),and at 21days (P<0.01) were significantly different.With wounds in combined debridement group , PUSH scores decreased faster than those in the au-tolytic debridement group . [ Conclusion] The combined debridement method used in elder patients is safe and effective , which can shorten debridement time and improve wounds healing as well .The Pressure Ulcer Scale for Healing is easy to use and its result is reliable , giving a quantitative objective evaluation of debridement effect on pressure ulcers .

14.
Chinese Journal of Surgery ; (12): 641-644, 2013.
Article in Chinese | WPRIM | ID: wpr-301217

ABSTRACT

<p><b>OBJECTIVES</b>To evaluate the expression of synuclein-γ (SNCG) and metalloproteinase 9 (MMP-9) both in the invasive ductal breast cancer samples and T47D and T47D(SNCG)- cell lines, to investigate the correlation between SNCG and MMP-9.</p><p><b>METHODS</b>Totally 96 invasive ductal breast cancer samples (female, mean age of (56 ± 8) years) were collected between June 2009 and June 2012. The expressions of SNCG and MMP-9 were investigated by immunohistochemistry. T47D and SNCG knock down T47D(SNCG)- cell lines were established and SNCG and MMP-9 protein expression were investigated by Western blot and gene expression by real-time PCR.</p><p><b>RESULTS</b>Among 96 samples, 26 (27.1%) of them co-expressed SNCG and MMP-9, 30(31.2%) of them expressed neither SNCG nor MMP-9. The expression of SNCG was correlated with the expression of MMP-9 (r = 0.655, P = 0.000).SNCG mRNA level of T47D cell line was 13.5 fold of T47D(SNCG)- cell line and SNCG protein expression was 2.1 fold. While MMP-9 mRNA level of T47D cell line was 7.3 fold of T47D(SNCG)- cell line and MMP-9 protien expression was 1.6 fold.When SNCG was knocked down, the expression of MMP-9 decreased.</p><p><b>CONCLUSIONS</b>SNCG and MMP-9 are significantly correlated with each other in breast cancer. SNCG may promote the invasion and metastasis of breast cancer mediated by up-regulating the expression of MMP-9.</p>


Subject(s)
Aged , Female , Humans , Middle Aged , Breast Neoplasms , Metabolism , Gene Expression , Matrix Metalloproteinase 9 , Metabolism , Neoplasm Proteins , Metabolism , RNA, Messenger , Genetics , Real-Time Polymerase Chain Reaction , gamma-Synuclein , Metabolism
15.
Acta Pharmaceutica Sinica ; (12): 709-717, 2013.
Article in English | WPRIM | ID: wpr-235606

ABSTRACT

A novel series of benzyl urea analogues based on the structural modification of sorafenib were synthesized. Their in vitro antitumor activities against MX-1, HepG2, Ketr3 and HT-29 were evaluated using the standard MTT assay. While several target compounds showed inhibitory activity against multiple cancer cell lines, compound 9 was of particular interest, demonstrating IC50 values (5.69-13.6 micromol x L(-1)) comparable to those of sorafenib. Furthermore, compounds 20 and 23 showed more potent inhibitory activity against HT-29 and MX-1 when compared to sorafenib. In particular, compound 20 bearing the N-3-pyridyl moiety not only exhibited greater inhibitory activity against HT-29 cell line (IC50 3.82 micromol x L(-1)), but also had improved solubility at pH 7.2, is worthy of further investigation as a lead to identify novel antitumor agents.


Subject(s)
Humans , Antineoplastic Agents , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Drug Screening Assays, Antitumor , HT29 Cells , Inhibitory Concentration 50 , Molecular Structure , Niacinamide , Chemistry , Pharmacology , Phenylurea Compounds , Chemistry , Pharmacology , Solubility , Structure-Activity Relationship , Urea , Chemistry , Pharmacology
16.
Chinese journal of integrative medicine ; (12): 235-240, 2012.
Article in English | WPRIM | ID: wpr-347198

ABSTRACT

This paper reviewed the retrieved literature published in the last 10 years, regarding the mechanism of Radix Astragalus in treating heart failure, in aspects of myocardial contraction improvement, cardiac muscle cell protection, neuro-endocrinal system regulation, relative cytokine regulation, and left ventricular remodeling inhibition, etc.


Subject(s)
Humans , Astragalus Plant , Biomedical Research , Cytoprotection , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Heart Failure , Drug Therapy , Myocardial Contraction , Myocytes, Cardiac , Pathology
17.
Chinese journal of integrative medicine ; (12): 146-149, 2011.
Article in English | WPRIM | ID: wpr-308682

ABSTRACT

<p><b>OBJECTIVE</b>To explore the dose-effect relationship of Astragalus granule (AG) on improving the quality of life (QOL) of the patients with chronic heart failure (CHF).</p><p><b>METHODS</b>Ninety CHF patients of Fei ()-qi-deficiency and/or Xin ()-Shen () yang-deficiency syndromes were equally randomized divided with a random number table into three groups; they received the high (7.5 g), moderate (4.5 g), and low dosage (2.25 g) of AG orally taken twice a day, respectively, and 4 mg of perindopril tablet once a day for 30 successive days. The heart function grade, patients' left ventricular ejection fraction (LVEF) and walking distance in 6 min (6mWD) were measured before and after treatment, and the patients' QOL was scored by the Minnesota Questionnaire for QOL evaluation in the patients with CHF at the same time.</p><p><b>RESULTS</b>The heart function grades of all the three groups after treatment were improved compared with those before treatment, but the improvements in high-dose group and moderate dose group were better than that in the low dose group (P<0.05). LVEFs were increased significantly in all the three groups, but the improvements in the high-dose group (59.42%±7.50%) and moderate dose group (61.98%±6.82%) were better than that in the low dose group (51.45%±6.80%, P<0.01); the 6mWDs in the all groups were also significantly increased (P<0.01), up to 419.80±36.23 m, 387.15±34.13 m, and 317.69±39.97 m, respectively; and Minnesota scores in them were lowered to 29.59±4.69 scores, 35.74±5.89 scores, and 42.78±6.06 scores, respectively; comparisons in aspects on 6mWD and Minnesota score showed that the effectiveness with high dose is the most effective, moderate dose as the second, and low dose as the lowest (P<0.01).</p><p><b>CONCLUSIONS</b>AG was sufficient to display an optimal effect on improving heart contraction at the moderate dose. In aspects of improving the QOL of CHF patients, the effectiveness of AG showed a dose-dependent trend. It should be applied discriminatively depending on the actual condition of patients and the aim of treatment in clinic.</p>


Subject(s)
Aged , Female , Humans , Male , Middle Aged , Astragalus Plant , Chemistry , Chemistry, Pharmaceutical , Chronic Disease , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Heart , Physiology , Heart Failure , Drug Therapy , Psychology , Heart Function Tests , Plant Preparations , Quality of Life , Treatment Outcome , Ventricular Function, Left , Physiology
18.
Chinese journal of integrative medicine ; (12): 473-477, 2011.
Article in English | WPRIM | ID: wpr-328482

ABSTRACT

Radix Astragali, a Chinese herbal medicine possessing important cardiovascular pharmacologic effects, is widely applied for the treatment of chronic heart failure (CHF) in clinical practice. This paper summarizes briefly the researches in the last 10 years on its chemical compositions, effective ingredients for improving cardiac function, dose-effect relationship in treating CHF, and adverse reactions that occurred in clinical practice.


Subject(s)
Humans , Astragalus Plant , Chemistry , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Therapeutic Uses , Heart Failure , Drug Therapy , Phytotherapy , Research
19.
Chinese Journal of Integrated Traditional and Western Medicine ; (12): 699-701, 2010.
Article in Chinese | WPRIM | ID: wpr-313219

ABSTRACT

<p><b>OBJECTIVE</b>To explore the effects of Astragalus on cardiac function and serum tumor necrosis factor-alpha (TNF-alpha) level in patients with chronic heart failure (CHF).</p><p><b>METHODS</b>Forty-five patients of Xin-qi deficiency or Xin-yang deficiency types were assigned to the Chinese medicine (CM) group and the Western medicine (WM) group by a randomizing digital table. Standard treatment for correcting heart failure, including digoxin, diuretics, etc. was administered to both groups, but to the CM group oral medication of Astragalus granule was given additionally at the dosage of 2.25 g twice a day, the treatment for both was continued for two weeks. NYHA cardiac functional grading, serum TNF-alpha level, left ventricular ejection fraction (LVEF) and walk distance in 6 min (WD) were measured before and after treatment, and a correlation analysis was carried out.</p><p><b>RESULTS</b>After therapy, the level of TNF-alpha in the two groups decreased (P < 0.05) and it was lower in the CM group [(54.77 +/- 9.34) microg/L] than in the WM group [(62.10 +/- 9.94) microg/L] (P < 0.05); LVEF in the two groups increased (P < 0.05) and it was higher in the CM group [(64.45 +/- 12.47)%] than that in the WM group [(56.03 +/- 13.33)%] (P < 0.05); both groups' WD increased (P < 0.05) and it was longer in the CM group [(446.97 +/- 68.82) m] than in the WM group [(345.40 +/- 63.62) m] (P < 0.05); the improvement of cardiac functional grading in the CM group was outstriper than the WM group (P < 0.05). The improvement in cardiac function was negatively correlated with TNF-alpha level.</p><p><b>CONCLUSION</b>Astragalus can alleviate the calcium overload-induced myocardial damage and improve both systolic and diastolic functions of heart in patients with CHF.</p>


Subject(s)
Aged , Female , Humans , Male , Middle Aged , Astragalus propinquus , Chemistry , Chronic Disease , Coronary Disease , Drugs, Chinese Herbal , Therapeutic Uses , Heart Failure , Drug Therapy , Phytotherapy , Tumor Necrosis Factor-alpha , Blood , Ventricular Function, Left , Physiology
20.
Chinese Journal of Integrated Traditional and Western Medicine ; (12): 361-364, 2010.
Article in Chinese | WPRIM | ID: wpr-231522

ABSTRACT

<p><b>OBJECTIVE</b>To observe the intervention effects of Liandou Qingmai Recipe (LQR) on atherogenic indices of plasma (AIP) and high-sensitivity c-reactive protein (hs-CRP) level in patients with coronary heart disease (CHD).</p><p><b>METHODS</b>Sixty-eight CHD patients were randomly assigned to two groups, 35 patients in the treatment group and 33 in the control group, all were treated by the regular CHD treatment, but to patients in the treatment group, LQR was given additionally. AIP value was calculated before and after treatment through measuring plasma levels of triglyceride (TG), high-density and low-density lipoprotein cholesterol (HDL-C and LDL-C). Besides, the levels of hs-CRP and peripheral blood leucocyte (PBL) were observed as well.</p><p><b>RESULTS</b>No significant difference existed between groups in all the detected parameters before treatment (P > 0.05). After treatment, levels of LDL-C, HDL-C, hs-CRP and PBL lowered significantly in the control group, but the changes of AIP and TG were insignificant (P > 0.05); while in the treatment group, all the parameters lowered significantly, with the levels of AIP, TG, hs-CRP and PBL significantly lower than those in the control group respectively (P < 0.05).</p><p><b>CONCLUSION</b>LQR can decrease levels of AlP and hs-CRP in CHD patients, amplify the diameters of LDL-C granule, and further lower hs-CRP and PLB levels, showing anti-atherosclerosis and anti-inflammation effects.</p>


Subject(s)
Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Biomarkers , Blood , C-Reactive Protein , Metabolism , Cholesterol , Blood , Cholesterol, LDL , Blood , Coronary Artery Disease , Blood , Drug Therapy , Drugs, Chinese Herbal , Therapeutic Uses , Lipoproteins, LDL , Blood , Phytotherapy , Risk Factors , Triglycerides , Blood
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