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1.
Acta Pharmaceutica Sinica ; (12): 1621-1626, 2021.
Article in Chinese | WPRIM | ID: wpr-881566

ABSTRACT

Hyperuricemia is not only the biochemical basis of gout, but also closely related to the development of metabolic syndrome, cardiovascular diseases, chronic kidney disease, etc. Xanthine oxidase (XOD) is the key catalytic enzyme for uric acid biosynthesis, therefore the vital target for anti-hyperuricemic drugs. In this study, compound CC18022 was designed and synthesized specifically targeting to XOD. Molecular docking analysis indicated a fairly tight binding between CC18022 and XOD. In the in vitro study, CC18022 significantly inhibited XOD activity with a half maximal inhibitory concentration (IC50) value in the order of nmol·L-1, which is relative to the XOD inhibitor febuxostat. By using both acute and chronic hyperuricemic mice model, compound CC18022 was found to have serum uric acid-lowering effect in a dose-dependent manner in vivo. The animal welfare and experimental processes were in accordance with the provisions of the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences. In the acute hyperuricemic mice, CC18022 significantly inhibited serum XOD activity, and also the XOD activity in intestine and liver, which were related to purine absorption and metabolism. Therefore, the novel compound CC18022 exhibited significant inhibition on XOD activity and anti-hyperuricemic effects, making it a favorable candidate for further research.

2.
Chinese Medical Journal ; (24): 1450-1456, 2021.
Article in English | WPRIM | ID: wpr-878191

ABSTRACT

BACKGROUND@#Drug-coated balloons (DCBs) have emerged as potential alternatives to drug-eluting stents in specific lesion subsets for de novo coronary lesions. Quantitative flow ratio (QFR) is a method based on the three-dimensional quantitative coronary angiography and contrast flow velocity during coronary angiography (CAG), obviating the need for an invasive fractional flow reserve procedural. This study aimed to assess the serial angiographic changes of de novo lesions post-DCB therapy and further explore the cut-off values of lesion and vessel QFR, which predict vessel restenosis (diameter stenosis [DS] ≥50%) at mid-term follow-up.@*METHODS@#The data of patients who underwent DCB therapy between January 2014 and December 2019 from the multicenter hospital were retrospectively collected for QFR analysis. From their QFR performances, which were analyzed by CAG images at follow-up, we divided them into two groups: group A, showing target vessel DS ≥50%, and group B, showing target vessel DS <50%. The median follow-up time was 287 days in group A and 227 days in group B. We compared the clinical characteristics, parameters during DCB therapy, and QFR performances, which were analyzed by CAG images between the two groups, in need to explore the cut-off value of lesion/vessel QFR which can predict vessel restenosis. Student's t test was used for the comparison of normally distributed continuous data, Mann-Whitney U test for the comparison of non-normally distributed continuous data, and receiver operating characteristic (ROC) curves for the evaluation of QFR performance which can predict vessel restenosis (DS ≥50%) at mid-term follow-up using the area under the curve (AUC).@*RESULTS@#A total of 112 patients with 112 target vessels were enrolled in this study. Group A had 41 patients, while group B had 71. Vessel QFR and lesion QFR were lower in group A than in group B post-DCB therapy, and the cut-off values of lesion QFR and vessel QFR in the ROC analysis to predict target vessel DS ≥50% post-DCB therapy were 0.905 (AUC, 0.741 [95% confidence interval, CI: 0.645, 0.837]; sensitivity, 0.817; specificity, 0.561; P < 0.001) and 0.890 (AUC, 0.796 [95% CI: 0.709, 0.882]; sensitivity, 0.746; specificity, 0.780; P < 0.001).@*CONCLUSIONS@#The cut-off values of lesion QFR and vessel QFR can assist in predicting the angiographic changes post-DCB therapy. When lesion/vessel QFR values are <0.905/0.890 post-DCB therapy, a higher risk of vessel restenosis is potentially predicted at follow-up.


Subject(s)
Constriction, Pathologic , Coronary Angiography , Coronary Artery Disease/therapy , Coronary Restenosis , Follow-Up Studies , Fractional Flow Reserve, Myocardial , Humans , Pharmaceutical Preparations , Predictive Value of Tests , Retrospective Studies , Treatment Outcome
3.
Article in Chinese | WPRIM | ID: wpr-876168

ABSTRACT

Objective:Nivolumab is one of the most common programmed death 1 (PD-1) inhibitors used as an immune checkpoint inhibitor (ICI). It brings significant therapeutic effects but often accompanied by serious drug toxicity. The pulmonary toxicities of nivolumab are not clear. This study aims to systematically explore the nivolumab-associated pulmonary toxicities and provide reference for clinical treatment. Methods:Data were extracted from US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) database from January 1, 2016 to September 30, 2019. Two types of disproportionality analysis, information component (IC) and reporting odds ratio (ROR), were applied in nivolumab-associated pulmonary adverse events (AEs) signal detection. Results:A total of 28 489 309 records were extracted from FAERS database and 8 181 records were associated with nivolumab. Analysis was conducted in 179 AEs and 86 signals were detected. Notably, potent signals were detected in radiation pneumonitis (IC025: 3.99, ROR025: 17.25), pneumonitis (IC025: 3.34, ROR025: 10.64) and bronchial fistula (IC025: 2.94, ROR025: 8.78). Nivolumab-associated pulmonary toxicities were more frequently reported in dyspnoea (IC025: 0.50, ROR025: 1.44), pneumonia (IC025: 0.08, ROR025: 1.07) and pneumonitis (IC025: 3.34, ROR025: 10.64). Results of IC and ROR methods were similar to each other. Most pulmonary toxicities were observed in patients with non-small cell lung cancer (N=3 711, 32.13%), malignant melanoma (N=1 658, 14.36%) and renal cell carcinoma (N=731, 6.33%). Conclusion:Significant pulmonary toxicities were detected in patients treated with nivolumab. Thus, it is highly important for clinicians to be vigilant about nivolumab-associated pulmonary AEs and be prepared to take immediate action for patient safety.

4.
Article in English | WPRIM | ID: wpr-881027

ABSTRACT

Lobane-type diterpenoids are not frequently discovered from marine soft corals. In this paper, three new lobane type diterpenes, 13-methoxyloba-8,10,15(16),17(18)-tetraene (1), 8,10,13(15)Z,16E-lobatetraene (2) and 19-hydroxy-lobatetraene (3), and a new natural compound, 17,18-epoxyloba-16-acetoxy-8,10,13(15)-trien (4), co-occurring with a known related diterpenoid, 18-methoxyloba-8,10,13(15),16(17)-tetraene (5), were isolated from the South China Sea soft coral Sinularia polydactyla. The structures of new compounds were determined by extensive spectroscopic analysis and by comparison with those reported in the literature. In bioassay, all the isolates were inactive on antibacterial, PTP1B inhibitory, and immunological activities. This study increased the chemical diversity of marine diterpenoids.

5.
Chinese Medical Journal ; (24): 2415-2421, 2020.
Article in English | WPRIM | ID: wpr-877827

ABSTRACT

BACKGROUND@#Acute coronary syndromes mainly result from abrupt thrombotic occlusion caused by atherosclerotic vulnerable plaques (VPs) that suddenly rupture or erosion. Fibrous cap thickness (FCT) is a major determinant of the propensity of a VP to rupture and is recognized as a key factor. The intensive use of statins is known to have the ability to increase FCT; however, there is a risk of additional adverse effects. However, lower dose statin with ezetimibe is known to be tolerable by patients. The present study aimed to investigate the effect of intensive statin vs. low-dose stain + ezetimibe therapy on FCT, as evaluated using optical coherence tomography.@*METHOD@#Patients who had VPs (minimum FCT 90°) and deferred from intervention in our single center from January 2014 to December 2018 were included in the trial. They were divided into the following two groups: intensive statin group (rosuvastatin 15-20 mg or atorvastatin 30-40 mg) and combination therapy group (rosuvastatin 5-10 mg or atorvastatin 10-20 mg + ezetimibe 10 mg). At the 12-month follow-up, we compared the change in the FCT (ΔFCT%) between the two groups and analyzed the association of ΔFCT% with risk factors. Fisher exact test was used for all categorical variables. Student's t test or Mann-Whitney U-test was used for analyzing the continuous data. The relationship between ΔFCT% and risk factors was analyzed using linear regression analysis.@*RESULT@#Total 53 patients were finally enrolled, including 26 patients who were in the intensive statin group and 27 who were in the combination therapy group. At the 12-month follow-up, the serum levels of total cholesterol (TC), total triglyceride, low-density lipoprotein (LDL-C), hypersensitive C-reactive protein (hs-CRP), and lipoprotein-associated phospholipase A2 (Lp-PLA2) levels were reduced in both the groups. The ΔTC%, ΔLDL-C%, and ΔLp-PLA2% were decreased further in the combination therapy group. FCT was increased in both the groups (combination treatment group vs. intensive statin group: 128.89 ± 7.64 vs. 110.19 ± 7.00 μm, t = -9.282, P < 0.001) at the 12-month follow-up. The increase in ΔFCT% was more in the combination therapy group (123.46% ± 14.05% vs. 91.14% ± 11.68%, t = -9.085, P < 0.001). Based on the multivariate linear regression analysis, only the serum Lp-PLA2 at the 12-month follow-up (B = -0.203, t = -2.701, P = 0.010), ΔTC% (B = -0.573, t = -2.048, P = 0.046), and Δhs-CRP% (B = -0.302, t = -2.963, P = 0.005) showed an independent association with ΔFCT%.@*CONCLUSIONS@#Low-dose statin combined with ezetimibe therapy maybe provide a profound and significant increase in FCT as compared to intensive statin monotherapy. The reductions in Lp-PLA2, ΔTC%, and Δhs-CRP% are independently associated with an increase in FCT.


Subject(s)
Anticholesteremic Agents/therapeutic use , Drug Therapy, Combination , Ezetimibe/therapeutic use , Humans , Hydroxymethylglutaryl-CoA Reductase Inhibitors/therapeutic use , Plaque, Atherosclerotic/drug therapy , Rosuvastatin Calcium/therapeutic use , Tomography, Optical Coherence , Treatment Outcome
6.
Article in Chinese | WPRIM | ID: wpr-879349

ABSTRACT

OBJECTIVE@#To compare the clinical efficacy of three minimally invasive methods of anterior column screw, plate and screw rod system in the treatment of anterior pelvic ring fracture.@*METHODS@#From December 2015 to September 2018, 77 patients with pelvic anterior ring fracture were treated and followed up, including 45 males and 32 females, aged 19 to 73 years. According to AO / OTA classification, there were 26 cases of type B1, 20 cases of type B2, 17 cases of type B3 and 14 cases of type C. According to the different internal fixation methods, they were divided into three groups:anterior column screw group(35 cases), plate group(20 cases), and screw rod system group(22 cases). The operation time, intraoperative fluoroscopy times, blood loss, fracture reduction quality, complications and curative effect of the three groups were compared.@*RESULTS@#All 77 patients were followed up for 12 to 33 (16.5±5.7) months. The operation time, intraoperative blood loss and incision length of anterior column screw group were significantly shorter than those of plate group and screw rod system group, and intraoperative fluoroscopy times of plate group were significantly less than those of anterior column screw group and screw rod system group (@*CONCLUSION@#Minimally invasive internal fixation with anterior column screw, plate and screw rod system can obtain good clinical effect, but anterior column screw fixation has less trauma and lower incidence of surgicalcomplications.


Subject(s)
Adult , Aged , Bone Plates , Bone Screws , Female , Fracture Fixation, Internal , Fractures, Bone/surgery , Humans , Male , Middle Aged , Minimally Invasive Surgical Procedures , Pelvic Bones/surgery , Retrospective Studies , Treatment Outcome , Young Adult
7.
Article in Chinese | WPRIM | ID: wpr-775859

ABSTRACT

OBJECTIVE@#To explore and quantify the intervention effect of auricular point sticking on perioperative psychological stress in patients with anorectal diseases.@*METHODS@#Eighty patients who underwent anorectal surgery were randomly divided into an observation group (40 cases) and a control group (40 cases). The routine preoperative guidance, preoperative visits, and informed of the postoperative condition were received in the control group. On the basis of the treatment in the control group, auricular point sticking was immediately applied at Shenmen (TF), Shen (CO), Wei (CO), Gan (CO), Pi (CO), Pizhixia (AT), E (AT), Nie (AT) and Zhen (AT) in the observation group.The patients were pressed by themselves, 3 to 5 min per point each time, 5 times a day, and the contralateral auricular points were replaced every 2 or 3 days until 1 week after surgery. The Hamilton anxiety scale (HAMA), Hamilton depression scale (HAMD), and Pittsburgh sleep quality index (PSQI) scores were compared between the two groups before and 7 days after surgery.@*RESULTS@#There was no significant difference in the total HAMA scores between after and before surgery in the observation group (>0.05). The total HAMA score in the control group was higher than that before surgery (0.05). The scores of somatic anxiety factor in the two groups were higher than those before surgery (0.05). The total score of PSQI in the two groups was lower than that before surgery (<0.05), and the total score of PSQI in the observation group was lower than that in the control group (<0.05).@*CONCLUSION@#Auricular point sticking can effectively improve some psychological stress problems during perioperative period in patients with anorectal diseases.


Subject(s)
Acupuncture Points , Acupuncture, Ear , Anxiety Disorders , Therapeutics , Humans , Rectal Diseases , General Surgery , Stress, Psychological
8.
Article in English | WPRIM | ID: wpr-773406

ABSTRACT

OBJECTIVE@#People in Western Africa suffer greatly from febrile jaundice, which is caused by a variety of pathogens. However, yellow fever virus (YFV) is the only pathogen under surveillance in Sierra Leone owing to the undeveloped medical and public health system there. Most of the results of YFV identification are negative. Elucidation of the pathogen spectrum is required to reduce the prevalence of febrile jaundice.@*METHODS@#In the present study, we used Ion Torrent semiconductor sequencing to profile the pathogen spectrum in archived YFV-negative sera from 96 patients in Sierra Leone who presented with unexplained febrile jaundice.@*RESULTS@#The most frequently identified sequencing reads belonged to the following pathogens: cytomegalovirus (89.58%), Epstein-Barr virus (55.21%), hepatitis C virus (34.38%), rhinovirus (28.13%), hepatitis A virus (20.83%), coxsackievirus (10.42%), Ebola virus (8.33%), hepatitis E virus (8.33%), lyssavirus (4.17%), leptospirosis (4.17%), chikungunya virus (2.08%), Crimean-Congo hemorrhagic fever virus (1.04%), and hepatitis B virus (1.04%).@*CONCLUSION@#The distribution of sequencing reads suggests a broader spectrum of pathogens for consideration in clinical diagnostics and epidemiological surveillance in Sierra Leone.


Subject(s)
Adolescent , Adult , Case-Control Studies , Female , Fever , Epidemiology , Virology , Humans , Jaundice , Epidemiology , Virology , Male , Sequence Analysis , Sierra Leone , Epidemiology , Young Adult
9.
Article in Chinese | WPRIM | ID: wpr-813056

ABSTRACT

To investigate the experience and efficacy of endoscopic thyroidectomy for papillary thyroid microcarcinoma (PTMC) through total areola approach.
 Methods: A total of 117 PTMC patients, who were diagnosed pathologically in Minimally Invasive Surgical Center, Second Xiangya Hospital, Central South University from June 2016 to December 2017, were divided into a endoscopic surgery group (n=72) and an open surgery group (n=45). The number of dissected central lymph nodes, blood loss, amount of drainage, occurrence of postoperative complication and recurrence were collected and compared.
 Results: Compared with the open surgery group, the blood loss was less and the operative time was longer in the endoscopic surgery group (P0.05). The mean follow-up time was more than 20 months, and there was no recurrence in the 2 groups. 
 Conclusion: Endoscopic thyroidectomy with central compartment neck dissection through total areola approach is safe and feasible in patients with PTMC. It has many advantages, such as no scar on neck, less blood loss, shorter hospital stay and more acceptable to young patients.


Subject(s)
Carcinoma, Papillary , General Surgery , Endoscopy , Humans , Nipples , Thyroid Neoplasms , General Surgery , Thyroidectomy
10.
Acta Pharmaceutica Sinica ; (12): 1041-1047, 2019.
Article in Chinese | WPRIM | ID: wpr-780174

ABSTRACT

To investigate the effects of small molecule compound bicyclol on type 2 diabetes mellitus (T2DM) and its mechanism of action, KKAy mice were treated with various doses of bicyclol (100, 200, and 400 mg·kg-1·d-1) with metformin (200 mg·kg-1·d-1) as a positive control, respectively. Age-matched C57BL/6J mice were used as the non-diabetic control (Con). The effect on hyperglycemia was evaluated by the levels of no-fasting blood glucose, fasting blood glucose (FPG), and glucose tolerance. Whole body insulin sensitivity was evaluated by fasting plasma insulin (FPI) and homeostasis model assessment-insulin resistance (HOMA-IR). The hepatic response to insulin was evaluated by insulin-induced activation of insulin signaling pathway. Western blot was performed to detect hepatic protein expressions. All animal experimental procedures were approved by the Animal Ethics Committee of Chinese Academy of Medical Sciences. KKAy mice showed T2DM characteristics such as hyperglycemia and insulin resistance, including attenuated response to insulin in the liver. A 28-day treatment of bicyclol suppressed both FPG and no-fasting blood glucose, in a dose- and time-dependent manner. Moreover, FPI and HOMA-IR values were both significantly decreased, and hepatic insulin-induced-phosphorylation of IRβ and Akt were up-regulated in KKAy mice after bicyclol treatment. Phosphorylation of FoxO1, the key transcription factor for regulating gluconeogenesis, was also significantly elevated by bicyclol treatment. These results suggested that bicyclol has some therapeutic effects on hyperglycemia in a time- and dose-dependent manner in KKAy mice. Its mechanism might be attributed to improving insulin resistance, enhancing hepatic insulin signaling pathway, and inhibiting gluconeogenesis. No significant interference on the hypoglycemic effect of metformin by bicyclol was observed in this study.

11.
Chinese Journal of Cardiology ; (12): 894-900, 2019.
Article in Chinese | WPRIM | ID: wpr-801017

ABSTRACT

Objective@#To explore the value of index of microcirculatory resistance (IMR) for early prediction of periprocedural myocardial injury (PMI) in patients with stable angina pectoris (SAP) and acute coronary syndrome (ACS) after PCI.@*Methods@#It was a prospective study. One hundred and sixty-four patients who had single coronary lesion were consecutively enrolled from May 2014 to December 2017 at Nanjing Hospital affiliated to Nanjing Medical University. According to clinical manifestation, patients were divided into SAP group (n=81) and ACS group (n=83). IMR was determined by thermal dilution with pressure guide wire. Basic clinical characteristics, coronary angiographic results, PCI procedural details, IMR after PCI, ΔIMR (IMR=post-PCI-IMR pre-PCI), levels of myocardial biomarkers before and after PCI were compared between the two groups. Multivariate logistic regression was used to analyze the relation of PMI with IMR and ΔIMR, and the predictive ability was evaluated by receiver operating characteristic (ROC).@*Results@#The levels of total cholesterol and low density lipoprotein cholesterol were significantly higher in ACS group than in SAP group (P<0.05), other clinical data at baseline were similar between the two groups (P>0.05). Quantitative coronary angiography (QCA) results and PCI related data were also similar between the two groups before PCI (P>0.05). Values of mean transit time (Tmn) of intracoronary injection with room temperature saline, post-PCI IMR and ΔIMR were significantly higher in ACS group than in SAP group after PCI (P<0.05). Plasma creatine kinase isoenzyme-MB difference (ΔCK-MB) (ΔCK-MB=CK-MB post-PCI-CK-MB pre-PCI) and cardiac troponin-I (cTnI) difference (ΔcTnI=cTnI post-PCI-cTnI pre-PCI) were significantly larger in ACS group than in SAP group (P<0.05). Multivariate logistic regression analysis showed that coronary artery disease (CHD) type (SAP and ACS) (OR=1.301, 95%CI 1.083-1.562), age (OR=1.007, 95%CI 1.000-1.013), ΔIMR (OR=1.009, 95%CI 1.000-1.017) and post-PCI IMR (OR=1.008, 95%CI 1.001-1.014) were independent predictors of PMI (P<0.05). The area under the ROC curve (AUC) of ΔIMR was 0.763 to predict PMI (P<0.05), the optimum cut-off value of ΔIMR was 5.485 with 70.0% sensitivity and 77.4% specificity. ΔIMR was positively correlated with ΔcTnI (r=0.592, P<0.05).@*Conclusions@#ΔIMR serves as an early predictor of PMI in CHD patients after PCI. As compared with SAP patients, ACS patients are more likely to develop PMI.

12.
Article in Chinese | WPRIM | ID: wpr-754411

ABSTRACT

Objective: To investigate clinicopathological features, risk of lymph node metastasis, and indications of endoscopic submu-cosal dissection (ESD) in young patients with intramucosal early gastric cancer (EGC). Methods: In total, 325 EGC patients who under-went radical gastrectomy and had complete clinicopathological data in Anhui Provincial Hospital from March 2009 to December 2016 were retrospectively evaluated. All patients were confirmed to have intramucosal cancer based on their postoperative pathology re-sults. The patients were assigned into two groups according to their age: young group (≤40 years) and old group (>40 years). The clini-copathological features and safety of ESD in the youth group were analyzed. Results: Among all patients with intramucosal EGC, 30 (9.2%) were in the youth group. Intramucosal cancer in the youth group occurred predominantly in women, and the pathological types were mainly undifferentiated and mixed, which were more likely to metastasize to the lymph nodes. In the youth group, EGC patients with intramucosal differentiated type, who had ESD indications, had no risk of lymph node metastasis. However, the rate of lymph node metastasis was up to 25% in intramucosal undifferentiated-type EGC patients who had expanded ESD indications. Conclusions:Young patients with intramucosal EGC have poor pathological differentiation and strong invasiveness, and ESD may be considered for the treatment of differentiated intramucosal cancer.

13.
Article in Chinese | WPRIM | ID: wpr-691480

ABSTRACT

Objective: To investigate the safety and perioperative experience of the segmental resection of the vena cava. Methods: From May 2015 to July 2017, 92 renal tumor patients with venous tumor thrombus were treated in Peking University Third Hospital, of whom 17 underwent nephrectomy with resection of the invaded vena cava for renal tumor with tumor thrombus invading vena cava. The preoperative features included that 15 patients were male and 2 female, the mean age was (59. 2 ±12.9) years (31-84 years), 6 cases were left sided and 11 right sided,and the mean diameter of the renal tumor was (9.1 ±3.7) cm (3-14.5 cm). Results: In this group of 17 cases, 5 patients underwent resection of the vena cava via laparoscopy (including 2 open conversions),and 12 via open procedures (including 2 cardiopulmonary bypasses). The mean operation time was (430.4 ± 120. 7) min (284-694 min) and the mean intraoperative blood loss was (2 918. 8 ±2 608. 2) mL (300-10 000 mL). The vena cava from the bottom to the top was transected. The median length of the tumor thrombus in the vena cava was 10 cm (3-21 cm). Postoperative complications were found in 11 patients, including grade I in 1 case,grade Ⅱ in 7 cases, grade Ⅳ in 2 cases and grade V in 1 case according to the Clavien system. The median postoperative creatinine was 116 μmol/L (79-645 μmol/L) with 2 patients needing dialysis. The postoperative pathology revealed that renal clear cell carcinoma in 10 cases, papillary carcinoma in 5 cases, urothelial carcinoma in 1 case and fusiform cell sarcoma in 1 case. During the median follow-up of 8 (1-28 ) months,1 patient died during perioperative period,1 patient died from multiple metastasis in 9 months postoperatively, 3 patients found distant metastasis and 2 cases remained lower extremity edema after operation. Conclusion: The segmental resection of the vena cava may be a good choice for non-metastatic renal tumors with tumor thrombus invading vena cava. The short term follow-up results revealed a satisfactory safety and feasibility.

14.
Article in Chinese | WPRIM | ID: wpr-691109

ABSTRACT

The diagnosis of osteochondral lesions of the talus can be based on the patients' symptoms, medical history, MRI, detailed physical examination and arthroscopy. Its treatment includes conservative treatment and surgical treatment. Conservative treatment includes rest, partial-weight bearing, plaster immobilization, wear the orthopedic support, take the non-steroidal anti-inflammatory drugs and so on. Conservative treatment is less risky and effective for mild injuries. Surgical treatment includes debridement, marrow stimulation, internal fixation and cartilage transplantation, autologous chondrocyte transplantation, articular cavity injection biological additions, ultrasonic and electromagnetic stimulation technology, tissue engineering technology, etc. Currently, there are various treatment methods, each with indications and advantages and disadvantages. Among these methods, the most commonly used ones are debridement, marrow stimulation, cartilage transplantation and autologous chondrocyte transplantation, and they deserve extensive promotion. Debridement and marrow stimulation are performed minimally traumatically under arthroscopy. The operation is simple and inexpensive with positive effects and mild pain. There is a higher rate of success for small-scale injuries, but if the operation fails, it will result in a wider range of defects, because of the fibrous cartilages formed after the operation. The cartilage transplantation can be performed in an one-stage operation. After the operation, the hyaline cartilage can be restored, but there are different levels of pathological changes in the donor sites. Chondrocytes transplantation can solve the problem of larger osteochondral defects left after the initial treatment failure, and the donor cartilage can be repaired without affecting the donor sites. But the disadvantages are its long time treatment, staged operations and higher cost. As far as all these treatments are concerned, recent treatment effects are satisfactory, but the long-term efficacy is still questionable. For the autologous chondrocyte transplantation and emerging tissue engineering treatment technology, there is still broad research prospect.

15.
Acta Pharmaceutica Sinica B ; (6): 919-932, 2018.
Article in English | WPRIM | ID: wpr-775014

ABSTRACT

Based on a non-competitive and selective PTP1B inhibitor reported by us previously, thirty-nine benzamido derivatives were designed and synthesized as novel PTP1B inhibitors. Among them, twelve compounds exhibited IC values at micromolar level against human recombinant PTP1B, and most of them exhibited significant selectivity to PTP1B over TC-PTP and CD45. Further evaluation of the most potent compound on high-fat diet (HFD)-induced insulin-resistant (IR) obese mice indicated that could modulate glucose metabolism and ameliorate dyslipidemia simultaneously.

16.
Acta Pharmaceutica Sinica B ; (6): 944-955, 2018.
Article in English | WPRIM | ID: wpr-775012

ABSTRACT

Eight cembrane-type diterpenoids, namely, (+)-(6)-6-hydroxyisosarcophytoxide (), (+)-(6)-6-acetoxyisosarcophytoxide (), (+)-17-hydroxyisosarcophytoxide (), sarcomililatins A-D (-), and sarcomililatol (), were isolated from the soft coral collected from Weizhou Island, Guangxi Autonomous Region, together with 2 known related analogues, (+)-isosarcophytoxide () and (+)-isosarcophine (). The structures of these compounds were elucidated by a combination of detailed spectroscopic analyses, chemical methods, and comparison with reported data. The absolute configuration of compound was established by the modified Mosher׳s method, while the absolute configurations of compounds and were assigned by electronic circular dichroism (ECD) spectroscopy and that of compound was established by time-dependent density functional theory electronic circular dichroism (TD-DFT ECD) calculation. In bioassays, compound displayed significant cytotoxicity against the human cancer cell lines human promyelocytic leukemia cells (HL-60) and human lung adenocarcinoma cells (A-549) with IC values of 0.78±0.21 and 1.26±0.80 μmol/L, respectively. Compounds and also showed moderate inhibitory effects on the TNF-induced Nuclear factor kappa B (NF-B, a therapeutical target in cancer) activation, showing IC values of 35.23±12.42 and 22.52±4.44 μmol/L, respectively.

17.
Article in Chinese | WPRIM | ID: wpr-807706

ABSTRACT

Objective@#To investigate the current status of prevention and control of occupational hazards in a city in 2017, to understand the capability to prevent and control occupational hazards and the level of occupational health supervision and management, and to propose measures to urge employers to assume the main responsibility for the prevention and control of occupational diseases.@*Methods@#An analysis of the main factors influencing the prevention and control of occupational hazards in the city was performed to screen out six semi-quantitative assessment indicators (including the training of the main responsible persons and occupational health management personnel in companies) and four qualitative assessment indicators (including the coverage of supervision and inspection of occupational hazards performed by the district safety supervision department) , which could be used to measure the prevention and control effects of regional occupational hazards. Each indicator was scored. The typical investigation method was used to do data review and on-site inspection of 170 companies, 17 district-level occupational health supervision departments, and 16 sub-district (township) occupational health supervision departments in the city from October to December, 2017. The prevention and control of occupational diseases in each district was scored, and the completion rate and completion situation of each indicator in the city were analyzed.@*Results@#The mean score of prevention and control of occupational hazards in the city was 84.9. The scores of two districts were relatively high, being 88.9 and 88.7, respectively; the scores of 9 (52.9%) districts were higher than 85. The pass rate of training for the main responsible persons and occupational health management personnel in companies in the city was 95.9%, the pass rate of occupational health training for workers was 84.7%, the pass rate of occupational health examination for workers was 96.5%, the pass rate for the inspection of occupational hazardous factors in workplaces was 95.3%, the pass rate for notifying occupational hazards in workplaces is 95.9%, and the pass rate for applying the warning signs of occupational hazards in workplaces was 76.5%.@*Conclusion@#The awareness of the importance of prevention and control of occupational hazards in all districts of the city has been increased, but the effectiveness of occupational health training for workers needs to be strengthened. The supply and demand of occupational health technical services are still not matched, and the ways and methods of occupational health supervision and inspection need to be improved.

18.
Chinese Journal of Cardiology ; (12): 536-542, 2018.
Article in Chinese | WPRIM | ID: wpr-806861

ABSTRACT

Objective@#To investigate the characteristics of acute myocardial infarction caused by spontaneous coronary artery dissection(SCAD) in young female patients. @*Methods@#In this casecontrolstudy,127 young(≤55 years) female patients with acute myocardial infarction onset within 1 week in Nanjing first hospital, Xuzhou central hospital, affiliated hospital of Xuzhou medical university, and Lianyungang first people's hospital were enrolled between January 2013 and February 2017,and the clinical data were retrospectively analyzed. According to their clinical manifestations and coronary angiography(CAG) results,the patients were divided into coronary atherosclerosis disease(CAD) group(CAG evidenced atherosclerosis, n=83) and SCAD group(CAG detected coronary artery dissection,n=44).The SCAD patients were subdivided into definite group (the results affirmed from intravenous ultrasound or optical coherence tomography, n=21) and probable group (the CAG results highly confirmed to characteristics of SCAD,but no intravenous ultrasound or optical coherence tomography image affirmation,n=23). Then, according to the different treatment strategies, the SCAD patients were subdivided into conservative treatment group(treated with drugs,n=19) and interventional therapy group(treated with percutaneous coronary intervention,n=25). @*Results@#(1)Compared to CAD group, patients in the SCAD group had less risk factors, such as hypertension history (25.0% (11/44) vs. 45.8% (38/83) , P=0.022) and diabetes history (6.8% (3/44) vs. 21.7% (18/83) , P=0.043),and had lower levels of fasting blood glucose (5.34(4.59,5.87) mmol/L vs. 7.12(5.18,8.60)mmol/L, P=0.001),total cholesterol((3.94±1.14) mmol/L vs. (4.91±1.50) mmol/L, P=0.001),triglyceride(1.42 (0.91,1.64) mmol/L vs. 1.89 (1.23,2.45) mmol/L, P=0.005),and low density lipoprotein cholesterol ((2.24±0.91) mmol/L vs. (2.94±1.16) mmol/L, P=0.001),CAG results showed that patients in the SCAD group had more single vessel lesion (88.6% (39/44) vs. 39.8% (33/83) , P=0.001), and their target lesion stenosis was less severe ( (79.2±22.4) % vs. (91.5±12.1) %, P=0.001). (2) The clinical risk factors such as hypertension history, diabetes history, smoking history, family history of cardiology disease, fasting blood glucose,total cholesterol,triglyceride and low density lipoprotein cholesterol were similar between definite group and probable group (all P>0.05). CAG results showed that prevalence of single vessel lesion (100% (21/21) vs. 78.3% (18/23) , P=0.050) and percent of target lesion stenosis ( (76.9±20.6) % vs. (81.2±24.1) %, P=0.529) were similar between definite group and probable group.(3)There were no significant difference in single vessel(84.0% (21/25) vs. 94.7% (18/19) , P=0.370), target lesion stenosis(85.0(70.0,100.0)% vs. 75.0(50.0,90.0)%, P=0.186),and survival rates in hospital(96.0% (24/25) vs. 100% (19/19) , P=1.000) between interventional therapy group and conservative treatment group.@*Conclusions@#Prevalence of SCAD is highin young female patients with acute myocardial infarction. Acute myocardial infarction patients with less risk factors of CAD and with CAG showing smooth lesion of narrowing segment and normal finding in the other vessels, are more likely to be diagnosed with SCAD.Acute myocardial infarction patients caused by SCAD have high survival rate either receiving percutaneous coronary intervention or drug treatment.

19.
Article in Chinese | WPRIM | ID: wpr-806655

ABSTRACT

Objective@#To establish a method for detection of human antibodies against monkeypox virus.@*Mothds@#The enzyme linked immunosorbent assay (ELISA) plates were coasted with two monkeypox virus peptides from B21R protein, to establish an indirect ELISA for detecting monkeypox virus IgG antibody. The healthy individuals serum samples, monkeypox virus infected patient serum samples and other virus infected patient sera samples were applied to evaluate specificity of the peptides antigen. The reaction conditions were optimized.@*Results@#Synthesized two peptides from monkeypox virus BR21R protein did not cross react obviously with healthy person serum and other virus infected serum. It was shown that the reaction condition was best with sera dilution at 1∶50 when two combined peptides were coated at 100 ng /well, and second-antibody was diluted at 1∶20 000. At this condition the cut off value of IgG antibody in serum samples for ELISA were A450 reading of 0.393. The detected results of two serum samples collected from the monkeypox patient in Sierra Leone were strongly positive, the titers of IgG antibody in two sera were both 1∶6 400.@*Conclusions@#The indirect ELISA for detection of monkeypox virus infection was established preliminarily which provided useful tools for epidemiological study and diagnosis.

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Article in Chinese | WPRIM | ID: wpr-743051

ABSTRACT

Objective To quantitatively determine the bioactive chemical components, polysaccharides, total flavonoids and total saponins, in the Astragali radix from the Liupan mountain area (Liupan mountain Astragali radix) in Ningxia of China. Methods With colorimetry and high-performance liquid chromatography with evaporative light-scattering detection (HPLC-ELSD), the total quantity of polysaccharides flavonoids and saponins were determined for the one year-old and four years-old Liupan mountain Astragali radix, which was further analyzed in comparison with the results of the Astragali radix from Shanxi province (Shanxi Astragali radix) of China. Results The content of total polysaccharides, total flavonoids and total saponins was 4.10%, 0.088% and 4.67%, respectively, in the four-year-old Liupan mountain Astragali radix. Among them, the total polysaccharide content was higher than that in Shanxi Astragali radix, the others were all lower than those in Shanxi Astragali radix. Further, the contents of the three total components in the one year-old Liupan mountain Astragali radix were all lower than those in the four years-old Liupan mountain Astragali radix and in the Shanxi Astragali radix. Conclusion Prolonging the growth period could significantly increase total content of the polysaccharides but not the flavonoids and saponins in the Liupan mountain Astragali radix.

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