[Analysis on the gender-specific risk factors of new-onset cerebral hemorrhage].

Objective: To explore the gender-specific risk factors of new-onset cerebral hemorrhage. Methods: In this prospective cohort study,a total of 98 961 participants((51.1±12.6)years old), who underwent the 2006 to 2007 physical examination and met the inclusion criteria, were enrolled from the Kailuanstudy cohort. There were 78 908 (79.7%) male,and 20 053 (20.3%) female.The incidence of cerebral hemorrhage was observed once per year until December 31, 2016.The difference on the incidence of cerebral hemorrhage between male and female was compared. Multivariate Cox regression analysis was applied to analyze therisk factors of cerebral hemorrhage events among different genders. Results: The participants were followed up for(10.00±0.73) years,and 860 cerebral hemorrhage events were recorded during follow up. The incidence of cerebral hemorrhage in the population was 86.90/10 million person years (standardized incidence rate of 47.85/10 million person years). The incidence of cerebral hemorrhage was significantly higher in male (49.61/10 million person years) than in female (34.07/10 million person years, P<0.05). Multivariate Cox regression analysis showed that 45-59 years old, ≥ 60 years old, diabetes,and waist-hip ratio were more strongly related to new-onset of cerebral hemorrhage events in female than in male, and the hazard ratios(95%CI) were 2.33 (1.23-4.43) ,2.71 (1.30-5.66) ,2.16 (1.24-3.74) and 8.79 (1.42-54.32) in female versus 1.55 (1.21-1.97) ,2.16 (1.68-2.78) ,1.19 (0.93-1.53) and 3.21 (1.09-9.41) in male, respectively. The risk of male cerebral hemorrhage increased by 29% (HR=1.29, 95%CI 1.19-1.40) in male and 24% (HR=1.24, 95%CI 1.20-1.28) in female,when the systolic blood pressure increased 10 mmHg (1 mmHg=0.133 kPa). Conclusions: The incidence of cerebral hemorrhage is higher in male than in female in this cohort.The association between systolic blood pressure and cerebral hemorrhage is stronger in male than that in female.The associations between age, waist-hip ratio, diabetes and cerebral hemorrhage are stronger in female than in male. Trial Registration: Chinese Clinical Trail Registry, ChiCTR-TNC-11001489.

Cladonia furcata polysaccharide induced apoptosis in human leukemia K562 cells.

AIM: To study whether Cladonia furcata polysaccharide (CFP-1) might induce apoptosis in human leukemia K562 cells. METHODS: Inhibition of proliferation was measured by MTT assay. Morphological assessment of apoptosis was performed with fluorescence microscope and electron microscope. DNA fragmentation was visualized by agarose gel electrophoresis. The amount of apoptosis cells was measured by flow cytometry. RESULTS: CFP-1 (50 - 800 mg/L) inhibited K562 cell proliferation in a concentration-dependent manner. After incubation of K562 cells with CFP-1 300 mg/L for 5 d, morphological changes of typical apoptosis were observed and agarose gel electrophoresis of DNA revealed "ladder" pattern. CONCLUSION: CFP-1 induced apoptosis in human leukemia K562 cells.

[Synthesis and antitumor activity of 4-O-(halogenated) acyl-4'-demethylepipodophyllotoxin analogues].

A series of 4-(halogenated)acyl-4'-demethylepipodophyllotoxin analogues were conveniently synthesized by selective esterification in the presence of BF3.Et2O, and screened in vitro against L1210 leukemia and KB cells. Most of these compounds showed marked antitumor activity and exhibited more potent activity than that of etoposide.

[Synthesis and antitumor activity of 4-S-(5-amido-1,3,4-thiodiazol-2-yl)4-deoxy-4'-demethylepipodophyllotoxi n analogues].

By the condensation of 4'-demethylepipodophyllotoxin with 2-amino-5-mercapto-1,3,4-thiodiazole in CF3COOH and acylation in the presence of DEPC, 10 title compounds were conveniently synthesized. These compounds were screened in vitro against L1210 leukemia and KB cells, in which compounds SIPI-92-1772, 1774, 1775, 1776, 1777 and 1779 exhibited more potent anti-tumor activity.

[Synthesis and antitumor activity of 4-(2-amido-2-ethoxycarbonyl) ethylsulfenyl-4-deoxy-4'-demethylepipodophyllotoxin analogues].

Twenty three 4-(2-amido-2-ethoxycarbonyl) ethylsulfenyl-4-deoxy-4'-demethylepipodophyllotoxin analogues were synthesized by three steps, in which trifluoroacetic acid was used as a condensation agent of 4'-demethylepipodophyllotoxin with L-cysteine ethyl ester hydrochloride without any protection of phenolic hydroxy and amino groups. All compounds were screened in vitro against L1210 leukemia and KB cells, in which, compounds 11, 16 and 18 exhibited more potent antitumor activity than etoposide.

[Synthesis and antitumor activities of 4-acylamido-4-deoxy-4'-demethylepipodophyllotoxin analogues].

Twenty four 4-acylamidc-4-deoxy-4'-demethylepipodophyllotoxins were synthesized by acylation of 4-amino-4-deoxy-4'-demethylepipodophyllotoxin by means of usual methods, and screened in vitro. This type of compounds showed strong antitumor activities, most of them are superior to etoposide in the inhibition against L1210 and KB cells.

[Synthesis and antitumor activities of 4-acylthiol-4-deoxy-4'-demethylepipodophyllotoxin analogues].

This paper describes the synthesis and antitumor activity of 4-acylthiol-4-deoxy-4'-demethylepipodophyllotoxin analogues. 4-Mercapto-4-deoxy-4'-demethylepipodophyllotoxin prepared from 4'-demethylepipodophyllo-toxin with H2S in the presence of BF3.Et2O, was acylated with different acids using diethyl cyanophosphonate and thus, corresponding 4-acylthiol-4-deoxy-4'-demethyl epipodophyllotoxin analogues were synthesized. These compounds were screened in L1210 leukemia and KB cells, and one compound has activity similar to etoposide, and others were generally weaker than etoposide and corresponding 4-acylamido-4-deoxy-4'-demethylepipodophyllotoxin analogues.

[Synthesis and inhibition on beta-lactamase of 4-(3-amido-4-substituted phenyl-2-oxo-azetidinonyl-1)methyl-cyclohexane carboxylic acids and -benzoic acids].

Eleven title compounds have been synthesized from trans-4-amino-methyl-cyclohexylic acid and 4-aminomethyl-benzoic acid, and were identified via elemental analysis, IR, 1HMNR and MS. Their beta-lactamase inhibition activity was determined and contrasted with penicillanic acid S-dioxide. The results of the preliminary test show that all the products have beta-lactamase inhibition activity to some extent.