作者机构：
[Liao, Lan-Qing; Guo, Yu; Zhang, Ye; Zeng, Yao-Fu; Long, Xiao-kang; Xiao, Fang] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;[Li, Chong] Univ South China, Nanhua Affiliated Hosp, Hengyang, Peoples R China.
通讯机构：
[Guo, Yu; Li, Chong] U;Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;Univ South China, Nanhua Affiliated Hosp, Hengyang, Peoples R China.
关键词：
amino acid;anti-tumor;genistein
摘要：
<jats:title>Abstract</jats:title><jats:p>Thirty‐one novel genistein amino acid ester derivatives were synthesized and evaluated for their anti‐proliferative activities against HUVEC cells and five cancer cells lines (HCT‐116, HeLa, HepG‐2, MCF‐7, MGC‐803). Most of the amino acid ester derivatives exhibited more inhibitory activity than their parent compound genistein. In particular, compound <jats:bold>8 j</jats:bold> (methyl(4‐((5‐hydroxy‐3‐(4‐hydroxyphenyl)‐4‐oxo‐4H‐chromen‐7‐yl)oxy)butanoyl)tryptophanate) bearing tryptophan chain showed the most cytotoxicity against HCT‐116 cells with IC<jats:sub>50</jats:sub> value of 2.76 μM. Further mechanistic studies indicated that compound <jats:bold>8 j</jats:bold> suppressed HCT‐116 cell metastasis and induced cell apoptosis in a dose‐dependent manner. Cell cycle assay showed that compound <jats:bold>8 j</jats:bold> arrested the HCT‐116 cells to G1 phase. These studies suggested compound <jats:bold>8 j</jats:bold> might be a potential candidate for developing new anticancer drugs.</jats:p>
摘要：
Flavan-3-ols are a series of natural products widely present in plants and show versatile biological activities. The structures of such compounds are characterized by owing two adjacent chiral centers and three rings. Their interesting structures and promising biological activities have driven increasing research developments toward the preparation of enantioenriched flavan-3-ols. This review summarizes the recent approaches for the asymmetric synthesis of chiral flavan-3-ols from two strategies in the construction of chiral centers. The key steps in the synthetic protocol involve Sharpless asymmetric dihydroxylation, Shi asymmetric epoxidation and Sharpless asymmetric epoxidation.
作者机构：
[Xiao, Jianhua; Cao, Jingsong] Univ South China, Med Coll, Inst Pathogen Biol, Hunan Prov Key Lab Special Pathogens Prevent & Co, Hengyang 421001, Hunan, Peoples R China.;[Xiao, Jianhua; Cao, Jingsong] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Wang, Yi; Zhang, Yunsheng; Xiao, JH; Wang, Y; Xiao, Jianhua; Liu, Luogen; Cao, Jingsong] Univ South China, Affiliated Hosp 2, Inst Pathogen Biol, Clin Res Ctr,Med Coll, Hengyang 421001, Hunan, Peoples R China.;[Wang, Yi] Univ South China, Affiliated Hosp 2, Urinary Surg, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Xiao, Jianhua; Xiao, JH; Wang, Y] U;Univ South China, Med Coll, Inst Pathogen Biol, Hunan Prov Key Lab Special Pathogens Prevent & Co, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Affiliated Hosp 2, Inst Pathogen Biol, Clin Res Ctr,Med Coll, Hengyang 421001, Hunan, Peoples R China.
关键词：
Blood group B antigen;Blood group B antibody;HK2;B cells activation;ABOi-KT
摘要：
It is well known that ABO blood group system incompatible kidney transplantation (ABOi-KT) is an effective strategy for end-stage renal disease. The main barrier for ABOi-KT is how to keep host B cell activation and blood group antibody titer in low levels. Moreover, the mechanism of B cell activation induced by blood group antigen was unclear in ABOi-KT. In this study, HK2 cells were identified to express blood group B antigen when cocultured with lymphocytes of blood group A. Optical microscope observation demonstrated that HK2 cells in coculture group gradually decreased. Furthermore, flow cytometer assay identified that T cell phenotypes (CD3+, CD3+CD4+ and CD3+CD8+) had no significant change and B cell phenotypes (CD19+ and CD138+) were all significantly enhanced (3.07 and 3.02 folds) at day 4. In addition, immunoturbidimetry analysis demonstrated that blood group B antibody was significantly increased to 2.35 fold at day 4, IgG was significantly increased to 3.60 and 2.81 folds at days 4 and 8 respectively, while IgM had no significant change at the measured time points. Taken together, B cells were activated and secreted blood group B antibody after treatment with HK2 expressing blood group B antigen. The results of this study maybe useful for further determination of the mechanism of B cell activation after ABO incompatible kidney endothelial cells stimulation.
摘要：
The aim of this study was to investigate the relationship between endothelial-mesenchymal transition (EndoMT) and the progression of infantile hemangioma (IH) and to provide references for clinical. Sixty-five patients were enrolled in this study. Tissues obtained from these patients were analyzed by tissue microarray (TMA). Serial sections from TMA blocks underwent immunohistochemistry with the primary antibodies for EndoMT markers (Twist, Zeb1, Smad, N-cadherin, Vimentin, and α-SMA). Intensity and extent points were counted to quantitate the markers expression. All sixty-five patients were diagnosed as IH, which distributes all over the body from head to planta pedis. Progressive phases could be distinguished with H & E staining. The expressionof Twist, Zeb1, Smad, α-SMA, Vimentin and N-cadherin in the abnormal endothelial cells were significantly increased compared with normal controls (***P < 0.01). Average expression points (intensity + extent) in proliferating and involuting phases were 7.69 and 7.80 for Twist; 8 and 7.90 for Zeb1; 4.43 and 3.80 for N-cadherin; 6.72 and 6.85 for Smad; 7.31 and 6.87 for α-SMA, and 6.42 and 7.00 for Vimentin. EndoMT involves in the tumorigenesis of IH. The endothelial cells have the capacity to transdifferentiate into mesenchymal cells when IH proliferates and these mesenchymal cells may further transdifferentiate into adipocytes or fibroblasts in involuting phase.
摘要：
miR-758-3p plays an important role via regulting ABCA1-mediated cholesterol efflux in atherosclerosis. However, the mechanism of miR-758-5p in cholesterol metabolism is still unclear. Here, we revealed that miR-758-5p decreased total cholesterol accumulation in THP-1 macrophage derived foam cells through markedly reducing cholesterol uptake, and no effect on the cholesterol efflux. Interestingly, computational analysis suggests that CD36 may be a target gene of miR-758-5p. Our study further demonstrated that miR-758-5p decreased CD36 expression at both protein and mRNA levels via targeting the CD36 3'UTR in THP-1 macrophage derived foam cells. The present present study concluded that miR-758-5p decreases lipid accumulation of foam cell via regulating CD36-mediated the cholesterol uptake. Therefore, targeting miR-758-5p may offer a promising strategy to treat atherosclerotic vascular disease. (C) 2017 Published by Elsevier Inc.
摘要：
A novel series of iodo-chrysin derivatives with resorcinol as raw materials were synthesized according to Baker-Venkataraman reaction and their inhibitory activities in vitro against thyroid cancer cell lines (SW-579 and TT) were evaluated by the standard methyl thiazole tetrazolium (MTT) method. Biological test results showed that these derivatives possessed stronger anti-thyroid cancer activities than 5-FU. Compound 21 showed the strongest activity against SW-579 cell lines with IC50 value of 3.4μM and compound 10 showed the strongest activity against TT cell lines with IC50 value of 6.2μM, it was better than 5-FU (59.3μΜ, 18.4μM respectively).
作者机构：
[Xiao, Yan; Song, Chen; Zheng, Qutong; Lei, Xiaoyong; Chen, Hongfei; Zeng, Xianliang; Zhang, Yinxiang; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Xiao, Yan; Song, Chen; Zheng, Qutong; Lei, Xiaoyong; Chen, Hongfei; Zeng, Xianliang; Zhang, Yinxiang; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Song, Chen; Zhang, Yinxiang] Univ South China, Res Interest Grp Pharm, Hengyang 421001, Peoples R China.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
摘要：
Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a well-known natural polyphenol compound. It is reported that resveratrol possesses strong anti-oxidative, anti-inflammatory, cardiovascular protective and cancer chemo-preventive effects. Therefore, there has been a considerable interest in its biological activity, pharmacological activity and also synthetic resveratrol analogues in recent years. Up to now, many new resveratrol derivatives have been synthesized and some new biological activities of these compounds have been found, so in the treatment of Alzheimer's disease and the inhibition of influenza H1N1 neuraminidase. Structure-activity studies revealed that crucial elements of parental components are required for specific effects. This review summarizes the available literatures on the structure-activity relationships and pharmacological properties of resveratrol analogues.
作者机构：
[Xiao, Guohua; Wang, Zongbao; Yu, Jian; Zhang, Yali; Zhang, Sujun; Yin, Weidong; Wang, Yueting] Univ S China, Inst Biochem & Mol Biol, Hengyang 421001, Peoples R China.;[Wang, Zongbao] Univ S China, Dept Lab Anim Sci, Hengyang 421001, Peoples R China.;[Zeng, Huaicai] Univ S China, Sch Publ Hlth, Hengyang 421001, Peoples R China.
通讯机构：
[Wang, Zongbao] U;Univ S China, Inst Biochem & Mol Biol, Hengyang 421001, Peoples R China.
摘要：
Objective: Endothelial dysfunction is a key event in the onset and progression of atherosclerosis associated with diabetes. Increasing cell apoptosis may lead to endothelial dysfunction and contribute to vascular complications. Therefore, we aimed to elucidate the possible role and mechanism of ibrolipim in preventing endothelial dysfunction induced by high glucose. Methods: Human umbilical vein endothelial cells (HUVECs) were cultured respectively under normal glucose level (5.5 mM), high glucose level (33 mM), and high glucose level with ibrolipim treatment. Endothelial dysfunction was identified by the expression of ET-1 and vWF through reverse transcription PCR (RT-PCR). HUVECs apoptosis was assessed by fluorescent staining with Hoechst 33258. Akt activity was analyzed by western blot. Results: High glucose condition significantly increased the rate of apoptotic cells, weakened cell viability, and decreased the expression of ET-1 and vWF. Ibrolipim treatment significantly attenuated these alterations of endothelial dysfunction. The lower concentrations (2, 4, 8 μM) of ibrolipim inhibited apoptosis of cultured HUVECs, improved cell viability, down-regulated the mRNA levels of ET-1, vWF, and attenuated the cytotoxicity; however, higher concentration (16, 32 μM) of ibrolipim aggravated the damage of HUVECs cultured under high glucose level. Meanwhile, high glucose induced a decrease of Akt activity which led to apoptosis, and ibrolipim prevented the decrease and attenuated apoptotic effect induced by high glucose. Furthermore, the PI3K inhibitor LY294002 significantly abolished the anti-apoptotic effect of ibrolipim, and decreased Akt phosphorylation. Although, the expression of Akt mRNA and total protein were not altered in cultured HUVECs. Conclusion: Ibrolipim at lower concentrations can inhibit high glucose-induced apoptosis in cultured HUVECs, which might be related to the alternation of Akt activity. Ibrolipim has the potential to attenuate endothelial dysfunction and lower the risk of diabetes-associated vascular diseases. And it might be a therapeutic agent for diabetic vascular complications.
