作者机构：
[Xiaowang Liu; Jian Tu; Ping Yu; Lei Xiang; Weike Ding; Kaiqiang Lu; Xiaoyong Lei; Linxi Chen] Institute of Pharmacy and Pharmacology,Learning Key Laboratory for Pharmacoproteomics,University of South China,Hengyang 421001,China;[Zhigang Zhou; Kai Yin] Medical college,University of South China,Hengyang 421001,China;[Zhigang Zhou] the First Affiliated Hospital,University of South China,Hengyang 421001,China
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：
Chemotherapy is one of the most common treatments used for hepatocellular carcinoma (HCC), which effectively improves outcome and reduces tumor recurrence. However, the drug resistance mechanisms involved in chemotherapy, which is the predominant challenge in HCC treatment, remain to be fully elucidated. Therefore, there is an urgent requirement for the identification of novel therapeutic strategies or drugs. MicroRNAs (miRs) have become an area of interest, and in the present study, the effects of miR133a and miR326 on HepG2 cells, and their function on Bcell lymphomaextra large (Bclxl) in HepG2 cells were investigated. Using computational programs, Bclxl was predicted as the common target gene of miR133a and miR326. A dualluciferase reporter assay was used to verify the target genes of miRs. The mRNA and protein levels of Bclxl were observed to be downregulated following transfection with miR133a or miR326 mimics. Combining miR133a or miR326 with 5fluorouracil (5FU) or cisplatin (DDP) resulted in increased cell death. The results of the present study indicated that miR133a, miR326 and Bclxl acted protectively against the apoptosis, induced by 5FU or DDP, in HepG2 cells. This suggested the potential use of miRs either as ancillary anticancer drugs or as anticancer drugs themselves.
摘要：
B-cell lymphoma-extra large (Bcl-xl) is an anti-apoptotic member of the B-cell lymphoma 2 (Bcl-2) family that is often found to be overexpressed in human hepatocellular carcinoma (HCC), therefore conferring a survival advantage to tumor cells. microRNA (miRNA) let-7b is downregulated in HCC and its expression correlates with multidrug resistance. Using computational programs, it was predicted that the 3' untranslated region (UTR) of the Bcl-xl gene contains a potential miRNA binding site for let-7b, and that a single nucleotide polymorphism (SNP) site rs3208684 (A or C allele) resides within this binding site. Luciferase assays and western blot analysis demonstrated that let7b targeted Bcl-xl gene expression and negatively regulated the amount of Bcl-xl protein. SNP rs3208684 (A>C) variation enhanced the expression of Bcl-xl by disrupting the binding of let-7b to the 3'UTR of Bcl-xl. The effects of the two polymorphic variants on chemotherapeutic drug sensitivity were determined by cell counting kit 8 assays. Overexpression of the Bcl-xl mutated (C) allele in BEL-7402 HCC cells significantly decreased fluorouracil (5-FU) sensitivity, as compared with mock transfection and overexpression of the wild-type allele. From this, it was concluded that let-7b increased 5-FU sensitivity by repressing Bcl-xl expression in HCC cells. These results suggest that SNP (rs3208684) may be a potential marker for personalized treatment.
作者机构：
[Zhang Cai-Ping] Univ South China, Coll Med, Hengyang 421001, Peoples R China.;[Lin Li-Mei; Tuo Qin-Hui; Sun Shao-Wei; Gong Yong-Zhen; Liao Duan-Fang] Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410205, Hunan, Peoples R China.;[Zhang Cai-Ping; Zheng Xing; Sun Shao-Wei; Ou Lu; Lei Xiao-Yong] Univ South China, Coll Pharm & Biol Sci, Hengyang 421001, Peoples R China.;[Tuo Qin-Hui; Gong Yong-Zhen; Liao Duan-Fang] Hunan Univ China, Sinoluxembourg Cooperat Res Ctr Chinese Med, Med, Changsha 410208, Hunan, Peoples R China.
通讯机构：
[Liao Duan-Fang] H;Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha 410205, Hunan, Peoples R China.
作者机构：
[Tang, Huifang] Univ South China, Affiliated Hosp 1, Hengyang 421001, Hunan, Peoples R China.;[Yang, Xiaoyan; Yin, Jie; Xiang, Qiong; Lei, Xiaoyong; Zhang, Pengfei; Yu, Jia] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Lei, Xiaoyong] Univ South China, Inst Pharm & Pharmacol, 28 Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Lei, Xiaoyong] U;Univ South China, Inst Pharm & Pharmacol, 28 Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
摘要：
Let-7 microRNA is expressed in lower lever in a variety of human tumors and is involved in tumorigenesis. This study investigated the inhibitory effect of the let-7 g microRNA on the expression of the HMGA2 gene in the fluorouracil (5-Fu)-resistant human hepatoma cell line Bel-7402/5-Fu, and the effect of let-7 g microRNA on drug sensitization in Bel-7402/5-Fu cells. Let-7 g microRNA and negative microRNA plasmids were constructed and transient transfected into Bel-7402/5-Fu cells. Expression levels of HMGA2 mRNA and protein in microRNA transient transfectants were clearly reduced as compared with negative microRNA transfectants and untreated cells. Flow cytometry revealed increased in S phase in let-7 g microRNA cells. dimethylthiazol-diphenyltetrazolium bromide (MTT) results indicated that microRNA transfectants had a higher cell inhibition rate than the negative vector or untreated cells after treatment with 0.13-13 μg/ml 5-Fu. In addition, cyclinA was down-regulated in the let-7 g transfectants cells.The results showed that let-7 g microRNA contributed to an increase of 5-Fu-induced cell cycle inhibit in human hepatoma cell and sensitized cells to 5-Fu, leading to increased the effectiveness of the drug in treating hepatoma cancer.
摘要：
Aims & ScopeThe Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.Coverage in the Journals@Ovid database begins with the January 1999 issue.
作者机构：
[Tang, Huifang] Univ South China, Affilitated Hosp 1, Hengyang 421001, Hunan, Peoples R China.;[Lei, Xiaoyong] Univ South China, Inst Pharm & Pharmacol, 28 Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Lei, Xiaoyong] U;Univ South China, Inst Pharm & Pharmacol, 28 Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
摘要：
This study was done to explore the role of microRNA-98 (miR-98) in cisplatin sensitization in human lung adenocarcinoma cell line. Differential expressions of miRNAs were analysed between cisplatin-resistant human lung adenocarcinoma cell line A549/DDP and its parental cell A549 by miRNAs microarray, of which 14 miRNAs were showed to be significantly (> 2-fold) up-regulated and 8 miRNAs had marked down-regulation (< 0.5-fold) in A549/DDP cells compared with in A549 cells. MiR-98, a member in the let-7 family, acts as a negative regulator in the expression of HMGA2 (high mobility group A2) oncogene, and it has been shown to have a nearly 3-fold decrease in A549/DDP cells. We found that elevated expression of miR-98 led to a higher sensitivity of A549/DDP cells to cisplatin, and the protein level of HMGA2, was clearly up-regulated in both A549/DDP and A549 cells by miR-98. Moreover, both Bcl-XL and Bcl-2, were down-regulated in the Pre-miR-98(TM) transfectants cells. We for the first time demonstrated that the expression of miR-98 increases cells spontaneous apoptosis and sensitizes cells to cisplatin at least in part via HMGA2 up-regulation. Our findings provided insight into some specific miRNAs in lung cancer as potential therapeutic targets.
