Thirteen novel oleanolic acid (OA) derivatives were designed and synthesized with modification at positions of C-3, C-12 and C-28 of OA. Their structures were confirmed by MS, 1H NMR and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (SGC7901, MCF-7 and A549) were evaluated by MTT assay. The results indicated that the tested derivatives were found to have stronger cell growth inhibitory activity than OA. Among them, compounds II2 and II3 showed more potent cytotoxicity on MCF-7 and A549 tumor cells than gefitinib (positive control). They are worthy to be studied further.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; Drug Design ; Humans ; Oleanolic Acid ; chemical synthesis ; pharmacology

Objective To evaluate the clinical value of determination of composition of kidney stones by shap and density and of prediction of the efficacy of extracorporeal shock-wave lithotripsy (ESWL) by X-rays. Methods The data of 358 patients were analyzed,with 204 male and 154 female and with 276 cases of solitary stones and 82 cases of multiple stones.Determine the composition of kidney stones by shap and density,predict the efficacy of ESWL by X-rays,and choose the appropriate method of treatment.Analyze stone chemical property by Infrared stone composition automatic analyzer to checkout the prediction results before surgeries. Results 339 cases were successful to remove stones after treatment.The prediction results of 308 cases (86.0％) were consistent in stone chemical property,and the preperative prediction results of 339 cases (94.7％) were consistent in ESWL efficacy. Conclusions Determination of composition of kidney stones and prediction of the efficacy of ESWL by X-rays were feasible.

Objective To investigate the diagnostic significance of endoscopic findings in Henoch-Schonlein purpura(HSP),especially when abdominal pain preceded the cutaneous lesions.Methods The clinical data and gastroscopic findings in 37 cases of children with HSP were studied and analysed retrospectively in order to detect the pathological changes in the stomach and duodenum mucosa.The biopsy was taken in the pathological changeing place,and the relationship between clinical and endoscopic findings was analyzed.Results Detection rate of the pathological changes in the stomach and duodenum mucosa was 62.2%,31.3% of which experienced only cutaneous lesions,100% of which presented the acute abdominal pain.Three patients were not checked up the pathological changes.Of them,1 had arthritis,2 had Henoch-Schonlein nephritis.Characteristically endoscopic findings in the stomach and duodenum mucosa were found.The endoscopic findings included anabrosis,hyperemia,edema and hemorrhage.Conclusions Detection rate of the pathological changes in the stomach and duodenum mucosa is higher.Endoscopy is very helpful to the early diagnosis of HSP in children,especially abdominal pain presented firstly.

Objective To investigate muscle MRI characteristics of lower limbs in Chinese patients with dysferlinopathy. Methods Detailed clinical information of 42 patients with dysferlinopathy confirmed by Western blot or DYSF genetic test were studied retrospectively, including age, course, serum creatinine kinase (CK) and modified Gardner?Medwin and Walto score, and T1WI, STIR image. Each muscle was scored according to its fatty degeneration evaluated on T1WI (fat replacement score). The patients were divided into 3 groups:Miyoshi myopathy (MM), limb girdle muscle dystrophy 2B (LGMD 2B) and preclinical stage (asymptomatic hyperCKemia or exercise intolerance). The data including the scores of each muscle between MM and LGMD 2B were compared by ANOVA analysis and Chi square test. The relationship of fatty replacement score with course and GM?W score was analyzed by Spearman rank correlation analysis. Results Thirty nine patients underwent thigh MR scanning and 36 patients underwent leg MR scanning. At the thigh level, there is no specificity that the fatty replacement was found in both the anterior and posterior parts while the rectus femoris, sartorius and gracilis were rarely involved. At the leg level, the most severely involved muscle was the soleus, followed by gastrocnemius. It formed a sandwich?like pattern that the anterior part (anterior and posterior tibial muscle and peroneus longus muscle) and the posterior part (medial and lateral gastrocnemius) were less involved than the middle part (soleus). Of 42 patients, 14 cases were MM, and 24 were LGMD 2B. The fat replacement score of each muscle between two groups showed no significant differences (F=0.066 to 3.907,P all>0.05) except for the adductor muscle (F=5.239, P=0.028), semimembranosus (F=6.703, P=0.014) and semitendinosus (F=7.689, P=0.009). Of 4 pre?symptomatic cases, 3 showed edema of posterior part of leg on STIR, especially soleus. In all patients, the fat replacement score correlated positively with course (rs=0.732, P=0.000) and GM-W score (rs=0.485, P=0.001). Conclusions The MRI of Chinese patient with dysferlinopathy was characterized by the milder involvement of rectus femoris, sartorius and gracilis muscle in the thigh and a sandwich?like pattern in the leg, which is helpful for differential diagnosis of inflammatory Myopathy versus other types of muscular dystrophy.

Objective To evaluate the relationship between clinical or subclinical hypothyroidism and positive thyroid autoantibody before 20 weeks pregnancy and risk of preterm birth.Methods Literature search was done in PubMed,EMBASE,Wanfang Medical Database,China Academic Journal Network Publishing Database and China Biology Medicine disc databases from January 1st,1980 to December 31th,2013.The following search terms were used:hypothyroidism,subclinical hypothyroidism,hypothyroxinnism,thyroid antibody,preterm labor,preterm birth,etc.(1) Criteria for inclusion:cohort studies and clinical studies were included; only articles that described at least l0 patients were eligible;the exposure was clinical or subclinical hypothyroidism and positive thyroid autoantihody,and outcome was preterm birth.(2) The excluded subjects were articles that described less than 10 patients; controls were pregnant women without eurothyrodisim.Meta-analysis was performed by RevMan 5.The relationship between clinical or subclinical hypothyroidism and positive thyroid autoantibody and risk of preterm birth was evaluated by OR or RR.Results (1) Twenty cohort studies were enrolled.A total of 39 596 cases of preterm birth occurred among 498 418 pregnant women.The controls in these studies were pregnant women with eurothyrodisim.(2) Clinical hypothyroidism in pregnancy:eight studies were included,reported data on 478 418 pregnant women (5 473 women with clinical hypothyroidism and 472 945 euthyroid pregnant women).The risk of preterm birth in pregnant women with clinical hypothyroidism was higher than those eurothyroid pregnant women in control group (OR=1.25,95％ CI:1.15-1.36,P＜0.01).(3) Subclinical hypothyroidism in pregnancy:ten studies were included,reported data on 277 531 pregnant women (5 257 women with subclinical hypothyroidism and 272 274 euthyroid pregnant women).The risk of preterm birth in pregnant women with subclinical hypothyroidism was higher than those in control group by random effects analysis (OR=1.25,95％ CI:1.14-1.36,P＜0.01).(4) Thyroid autoantibodys positive in pregnancy:eleven studies were included,reported data on 28 781 pregnant women (3 036 women with thyroid autoanti body positive and 25 745 euthyroid pregnant women).The risk of preterm birth in pregnant women with positive thyroid autoantibody was higher than those negative thyroid autoantibody in control group (OR=1.47,95％ CI:1.27-1.70,P＜0.01).The funnel plots presented symmetrical graphics,indicating that there was no publication bias.Conclusion Clinical or subclinical hypothyroidism and positive thyroid autoantibody in pregnant women is risk factors of preterm birth.

Objective To investigate the composite prevention strategy for shoulder dystocia.Methods The published articles of randomized controlled trial (RCT)of comparison about the prevention of shoulder dystocia were searched in PubMed,EMBASE,EBSCO databases and Cochrane Library,and these studies were screened under inclusion and exclusion criteria.The quality of included studies were evaluated.And the Meta-analysis using statistic software RevMan 5.1 was completed.Results Totally 16 articles,all English published with no one Chinese article being searched out,were included in this analysis,published from 1993 to 2009.(1)To the gestational diabetes mellitus (GDM)patients,reviewed from 2 articles,it was found that the incidence of shoulder dystocia was reduced significantly by prenatal intervention versus usual care (OR=0.40,95％ CI:0.21-0.75,P=0.004).(2)To the GDM patients with intensive prenatal intervention,reviewed form 5 articles,it was found that the incidence of shoulder dystocia was reduced significantly by intensive intervention (diet control combined with insulin if necessary)versus less intensive intervention (only diet control),OR=0.29 (95 ％ CI:0.11-0.73,P=0.009).(3) To the non-GDM patients with suspected macrosomia,reviewed from 4 articles,it was found that the incidence of shoulder dystocia was not reduced by early artificial induction of parturition (OR=0.85,95 ％ CI:0.41-1.75,P=0.660).(4)To the GDM patients,reviewed form 2 articles,it was found that the incidence of shoulder dystocia was reduced marginal significantly by artificial induction of parturition in 38-39 gestational weeks compared with all spontaneous parturition patients (OR=0.18,95 ％ CI:0.03-0.97,P=0.050) and significantly reduced when compared with those spontaneous parturition patients after 40 gestational weeks (OR=0.13,95 ％ CI:0.02-0.75,P=0.020).(5)To the GDM patients with suspected macrosomia,reviewed from only one article,it was found that the incidence of shoulder dystoeia was reduced marginal significantly by early artificial induction of parturition (OR=0.34,95 ％ CI:0.12-0.99,P=0.050).(6)Reviewed from 2 articles,it was found that the incidence of shoulder dystocia was not significantly reduced by the intrapartum prophylactic maneuvers (OR=0.44,95％ CI:0.16-1.18,P=0.100).Conclusion Some varieties of intervention for the high risk patients could reduced the occurrence of shoulder dystocia.

Objective To study whether osteoblast is necessary for IGF-Ⅰ to promote bone resorption by osteoclast.Methods Mouse MC3T3 osteoblast cells and mature osteoclasts induced by RANKL were cultured in vitro.These osteoblasts and osteoclasts were subjected to treatment with recombinant human insulin-like growth factor-1 (rhIGF-Ⅰ),and the activation of IGF-Ⅰ receptor was verified by Western blotting.Thereafter,osteoclasts were cultured individually or co-cultured with osteoblast,in the absence or presence of rhIGF-Ⅰ.Osteoclast proliferation and apoptosis were observed by MTT colorimetric assay and flow cytometry.Cathepsin K gene expression was detected by real-time PCR; bone adsorption activity of osteoclast was determined by resorption pits formation on calf cortex slice with toluidine blue staining.Results Western blotting result confirmed that rhIGF-Ⅰ could effectively activate IGF-Ⅰ receptors either in osteoblast or osteoclast.In co-cultured group,in the presence of rhIGF-Ⅰ osteoclast showed inhibited apoptosis,enhanced proliferation and up-regulated cathepsin K expression (P ＜ 0.05).The functional experiment revealed that osteoclasts collected from IGF-Ⅰ treated co-cultured group resulted in more resorption pits formation (P ＜ 0.05); rhIGF-Ⅰ did not show any significant effect on the individually cultured osteoclasts.Conclusion Osteoblast is necessary for osteoclast induced bone resorption resulting from IGF-Ⅰ treatment.

OBJECTIVETo analyze the clinicopathological features and prognosis of colorectal cancer patients with preoperative cancer-related anemia.

METHODSClinical data of 354 patients with colorectal cancer in the Second Affiliated Hospital of Guangzhou Medical College from January 2003 to July 2009 were analyzed retrospectively. Those with hemoglobin(Hb)<120 g/L before surgery were defined as cancer-related anemia.

RESULTSOf the 354 colorectal cancer cases, 195 were males and 159 were females. The median age was 65(range 22-92) years. Preoperative cancer-related anemia tended to be occurred in female(P<0.01) and those with preoperative albumin ≤35 g/L (P<0.01), right colon cancer(P<0.01) and full-thickness invasion(P<0.05). Cox regression analysis showed preoperative cancer-related anemia was an independent unfavorable factor for overall survival (HR=1.60, 95% CI:1.05-2.44; P<0.05), but not for disease-free survival (HR=1.43, 95% CI:0.97-2.12; P>0.05) in colorectal cancer.

CONCLUSIONSPreoperative cancer-related anemia plays an important role in the development and prognosis of colorectal cancer and great attention should be paid to clinical practice.

Adult ; Aged ; Aged, 80 and over ; Anemia ; etiology ; Colorectal Neoplasms ; complications ; surgery ; Female ; Humans ; Male ; Middle Aged ; Prognosis ; Retrospective Studies ; Young Adult

Objective To explore the appropriately operative chance , method, and perioperative management of coronary arterybypass grafting (CABG) in the patients with severe left main artery (LMA) stenosis with three-vessel-disease.Methods A total of296 patients with severe LMA stenosis with three-vessel-disease who underwent CABG surgery was analyzed retrospectively from 2003through 2013.Of them, 276 patients underwent conventional coronary artery bypass surgery on pump ( CCABG)and 20 patients underwentoff-pump CABG( OPCAB); 172 Patients was over 60 years old (58.1%)and 246 patients (83.10%) had concomitant diseasesincluding valve lesion, hypertension, diabetes, myocardial infarction, left ventricular aneurysm with septal defect , stroke, renal failure,and cancer.Left internal mammary artery use was in 281 patients (95.1%); and 32 patients were implanted intra-aortic ballonpump(IABP) perioperatively.Results There were 7 cases(2.36 %) death of postoperative low cardiac output , ventricular fibrillation,cerebral infarction, renal failure, and multiple organ failure, respectively.Postoperative complications were low cardiac output ,respiratory failure , ventricular fibrillation, cereboembolism, cardiac tampomade, renal failure, stroke, and multiple organ failure.Afterfollow-up 2 to 84 months, there was 3 death in which 2 death of cardiac factors.Conclusions CCABG was a safe and effectivemethod in patients with severe LMA stenosis with severe three -vessel-disease.Preoperative insertion of IABP can certainly avoid the po -tential operative risk factor and significantly decrease the mortality and morbidity .

Objective To study the differentiation types of microglia induced by macrophage colony-stimulating factor (M-CSF).Methods Rat microglia cultured in vitro were inoculated on 6-well plates and divided into 3 groups (n=4 each) using a random number table method when cell confluence reached 70％:blank control group (C group),vehicle control group (P group) and M-CSF group.Group P was incubated with phosphate buffer solution for 7 days and group M-CSF with 20 ng/ml M-CSF for 7 days.The expression of a specific M1 phenotype marker tumor necrosis factor-alpha (TNF-α) and specific M2 phenotype markers interleukin-10 (IL-10) and brain-derived neurotrophic factor (BDNF) was determined by Western blot.Results Compared with C group,the expression of IL-10 and BDNF was significantly upregulated (P＜0.05),and no significant change was found in TNF-α expression in M group (P＞0.05),and no significant change was found in the expression of TNF-α,IL-10 or BDNF in P group (P＞0.05).Conclusion M-CSF can induce microglia to differentiate into a M2 phenotype.