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.
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 alpha-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, a-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 alpha-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:
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).
期刊:
Die Pharmazie,2015年70(12):765-771 ISSN:0031-7144
通讯作者:
Zheng, Xing
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 poees 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.
摘要:
Isolation rearing induces profound behavioral and neurochemical abnormalities in rodents. However there have been many controversies with its anxiogenic-like effects using models like elevated-plus maze. In the current study we aimed to address this by using one novelty-based anxiety paradigm that has been largely overlooked in previous isolation rearing studies. We found that eight-week isolation rearing produced potent anxiogenic-like effects in novelty-induced hypophagia test in mice. We also demonstrated PSD-95 levels were elevated in the hippocampus and amygdala and reduced in the frontal cortex after social isolation. This study provides further behavioral and neurochemical evidence to support that isolation rearing can produce anxiogenic-like effects in rodents. (C) 2012 Elsevier Ireland Ltd. All rights reserved.
期刊:
Die Pharmazie,2011年66(10):798-803 ISSN:0031-7144
通讯作者:
Wang, Zongbao
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.