Synthesis of ester derivatives of Rhein and their in vitro antitumor activities on cervical cancer cells (Hela)

Taking Rhein as the lead compound, ten esters of rhein were synthesized by esterification. For synthesis of smaller steric hindrance alcohols, SOCl2 was used as a catalyst to synthesize methyl, ethyl and butyl esters. For lager steric hindrance alcohols, dicyclohexyl carbodiimide (DCC) was used as dehydrating agent, and 4-dimethylaminopyridine (DMAP) was used as the catalyst to synthesize isopropyl, isobutyl, tertbutyl, isoamyl, benzyl, 2-phenyl ethyl, 2-chloroethyl esters. Structural characterization of the target compounds were done using melting point, 1H NMR, 13C NMR and HRMS. Five out of the 10 compounds were new. All the compounds were evaluated for antitumor activities in vitro against Hela human cervical carcinoma cell lines. Study found that all the ten compounds showed differences in their growth inhibitory effect on tumor cells. Compound with benzyl groups improved the antitumor activity. Results showed that compound 3b exhibited maximum activity against Hela cell lines at 100 μg mL–1 (IC50 value) with an inhibition rate of 70%, while the derivative 3i showed the lowest inhibitory activity (IC50 <64.3 μg mL–1)

Synthesis of ester derivatives of Rhein and their in vitro antitumor activities on cervical cancer cells (Hela)

1359-1363Taking Rhein as the lead compound, ten esters of rhein were synthesized by esterification. For synthesis of smaller steric hindrance alcohols, SOCl2 was used as a catalyst to synthesize methyl, ethyl and butyl esters. For lager steric hindrance alcohols, dicyclohexyl carbodiimide (DCC) was used as dehydrating agent, and 4-dimethylaminopyridine (DMAP) was used as the catalyst to synthesize isopropyl, isobutyl, tertbutyl, isoamyl, benzyl, 2-phenyl ethyl, 2-chloroethyl esters. Structural characterization of the target compounds were done using melting point, 1H NMR, 13C NMR and HRMS. Five out of the 10 compounds were new. All the compounds were evaluated for antitumor activities in vitro against Hela human cervical carcinoma cell lines. Study found that all the ten compounds showed differences in their growth inhibitory effect on tumor cells. Compound with benzyl groups improved the antitumor activity. Results showed that compound 3b exhibited maximum activity against Hela cell lines at 100 μg mL–1 (IC50 value) with an inhibition rate of 70%, while the derivative 3i showed the lowest inhibitory activity (IC50 –1)

Prevalence survey on pterygium among people aged 40 and above in Hengli Town of Dongguan

AIM:To investigate the prevalence of pterygium of the household population aged 40 and above in Hengli Town of Dongguan.<p>METHODS: Using the method of cluster random sampling, select 3 628 people aged 40 and above in four villages and one community for visual examination, intraocular pressure check, slit lamp examination and questionnaire.<p>RESULTS: The actual number of subjects was 3 393 people, and examination rate was 93.52%. We detected 843 patients with pterygium. The prevalence of pterygium was 24.85%.<p>CONCLUSION: There is high prevalence of pterygium in Dongguan area. The prevalence of pterygium is related with age and working environment, but has no relation with gender

外用喜疗妥致严重皮肤反应1例

Objective: To explore the clinical characteristics, diagnosis and prognosis of local severe cutaneous reactions as result of the treatment with Hirudoid. Methods: One case of severe cutaneous reactions as result of the treatment with Hirudoid was reported and the relevant literatures were reviewed. Results: The site of puncture of left arm occurred non-leakage phlebitis with local pain after chemotherapy. The patient was applied the Hirudoid to the affected areas 2 times daily. After 2 days, local skin felt a kind of burning pain and it seems to be getting worse. The skin lesions began as pruritic red macules or papules. It became swelled and bleeding after scratching. We considered that the cutaneous reactions were an allergic response to Hirudoid. We discontinued the Hirudoid and desensitization treatment was used on cure, but it failed to respond to the medical treatment. A hot compress with 50% magnesium sulphate solution can reduce swelling and alleviate pain. Scales of skin peel off and weaved the new skin after 10 days. Conclusion: The case of local severe cutaneous reactions as result of the treatment with Hirudoid is very rare. A hot compress with 50%  magnesium sulphate solution can help to relieve the discomfort. 目的  探讨外用喜疗妥致严重皮肤反应的临床特征及治疗和预后。方法  报道1例外用喜疗妥致严重皮肤反应患者的临床资料并结合相关文献进行分析。结果  患者，女，60岁，化疗后穿刺部位左侧手臂出现非渗漏性静脉炎，局部疼痛。给予喜疗妥每日2次外涂。2天后，患者突感涂抹局部烧灼样疼痛，并可见大片红色斑丘疹奇痒难忍，抓挠后充血肿胀。考虑喜疗妥过敏所致，立即停用喜疗妥，并应用脱敏治疗，效果不佳，局部颜色由红色渐变为暗紫色且肿痛剧烈，给予50%硫酸镁溶液湿热敷。3天后患者症状逐渐减轻，肿胀消退，10天后患处皮肤全部脱落并被新的完好皮肤覆盖。结论  外用喜疗妥致严重皮肤反应非常罕见，50%硫酸镁溶液热敷患处皮肤，可以缓解肿痛，消除症状

Expression of CD147 on monocytes/macrophages in rheumatoid arthritis: its potential role in monocyte accumulation and matrix metalloproteinase production

Monocytes/macrophages play an important role in rheumatoid arthritis (RA) pathogenesis. They can activate fibroblasts through many molecules, including IL-1 and tumor necrosis factor-alpha, but there have been very few reports on the role of CD147 in RA. In our study, the results of flow cytometry reveal that the mean fluorescence intensity (MFI) of CD147 expression on CD14+ monocytes of peripheral blood from RA patients was higher than that in normal control and ankylosing spondylitis (AS) patients. The MFI of CD147 expression on the CD14+ monocytes in RA synovial fluid was higher than that in RA peripheral blood. Immunohistochemical staining shows that CD147 expression in RA synovium correlated with matrix metalloproteinase (MMP)-1 expression. A double immunofluorescent assay shows that CD147 was expressed on CD68+ cells in RA synovium. The potential role of CD147 in cyclophilin A (CyPA)-mediated cell migration was studied using a chemotaxis assay in vitro and it was found that the addition of anti-CD147 antibody or a CD147 antagonistic peptide significantly decreased the chemotactic index of the mononuclear cells. The role of CD147 in MMP production and cell invasion in vitro were studied through the co-culture of human CD14+ monocytes or monocytic line THP-1 cells and human fibroblasts, as well as by gel zymography and an invasion assay. Significantly elevated release and activation of MMP-9 and/or MMP-2 were seen in the co-culture of human monocytes/THP-1 cells and fibroblasts compared with cultures of the cells alone. An increased number of cells invading through the filters in the invasion assays was also observed in the co-cultured cells. The addition of CD147 antagonistic peptide had some inhibitory effect, not only on MMP production but also on cell invasion in the co-culture. Our study demonstrates that the increased expression of CD147 on monocytes/macrophages in RA may be responsible for elevated MMP secretion, cell invasion and CyPA-mediated cell migration into the joints, all of which may contribute to the cartilage and bone destruction of RA. These findings, together with a better understanding of CD147, CyPA and RA, will help in the development of innovative therapeutic interventions for RA

2-[4-(4-Methoxy­phen­yl)-5-(2-pyrid­yl)-4H-1,2,4-triazol-3-yl]phenol

In the title compound, C20H16N4O2, the benzene rings of the 2-hydroxy­phenyl and 4-methoxy­lphenyl groups form dihedral angles of 64.02 (8) and 77.39 (7)°, respectively, with the mean plane of the triazole ring. The dihedral angle between the triazole ring mean plane and the pyridyl ring is 9.61 (8)°. In the crystal, inter­molecular N—H⋯O hydrogen bonds link the mol­ecules into zigzag chains propagating in [010]

LongSAGE analysis of skeletal muscle at three prenatal stages in Tongcheng and Landrace pigs

Transcriptional profiling of Tongcheng and Landrace pigs using long serial analysis of gene expression provides insight into the molecular mechanism underlying differences in muscle growth

High Throughput Sediment DNA Sequencing Reveals Azo Dye Degrading Bacteria Inhabit Nearshore Sediments

Estuaries and coastal environments are often regarded as a critical resource for the bioremediation of organic pollutants such as azo dyes due to their high abundance and diversity of extremophiles. Bioremediation through the activities of azoreductase, laccase, and other associated enzymes plays a critical role in the removal of azo dyes in built and natural environments. However, little is known about the biodegradation genes and azo dye degradation genes residing in sediments from coastal and estuarine environments. In this study, high-throughput sequencing (16S rRNA) of sediment DNA was used to explore the distribution of azo-dye degrading bacteria and their functional genes in estuaries and coastal environments. Unlike laccase genes, azoreductase (azoR), and naphthalene degrading genes were ubiquitous in the coastal and estuarine environments. The relative abundances of most functional genes were higher in the summer compared to winter at locations proximal to the mouths of the Hanjiang River and its distributaries. These results suggested inland river discharges influenced the occurrence and abundance of azo dye degrading genes in the nearshore environments. Furthermore, the azoR genes had a significant negative relationship with total organic carbon, Hg, and Cr (p < 0.05). This study provides critical insights into the biodegradation potential of indigenous microbial communities in nearshore environments and the influence of environmental factors on microbial structure, composition, and function which is essential for the development of technologies for bioremediation in azo dye contaminated sites

Tensile behaviour of carbon fabric reinforced cementitious matrix composites as both strengthening and anode materials

Recently, a promising solution to corroded steel reinforced concrete structures was proposed in which a dual-functional carbon-fabric reinforced cementitious matrix (carbon-FRCM) composite is used for impressed current cathodic protection (ICCP) and structural strengthening (SS); this method is referred to as ICCP-SS. The tensile behaviour of carbon-FRCM must be understood for design purposes. In this study, the tensile characteristics of carbon-FRCM composites with different fabric reinforcement ratios were assessed to determine the strengthening capability of the materials. Then, using the composite as an anode material, the tensile behaviour of carbon-FRCM specimens subjected to anodic polarization in ICCP was evaluated. Direct tensile tests were conducted to obtain the tensile stress-strain behaviour of the carbon-FRCM specimens. By comparing the results from each case, the influences of different parameters on the tensile behaviour of the carbon-FRCM composites were evaluated, and useful information regarding the application of these materials in ICCP-SS was obtained