摘要：
Capsaicin is the main active ingredient of chili peppers and the most pungent alkaloid. It is reported that capsaicin has many pharmacological effects such as analgesia, anticancer, anti-inflammatory, antibacterial, and anti-obesity. However, the application of capsaicin is limited by its adverse side effects, such as stomach irritation, stomach cramps, and burning sensation. In recent years, many capsaicin derivatives have been synthesized and their biological activities have been evaluated. Some capsaicin derivatives have shown promising activities in cells and animal models. Herein, we described the synthesis and biological activity of capsaicin and its derivatives. It is hoped that the insights obtained in this perspective will facilitate the synthesis of a second generation of capsaicin analogs with improved biological activities.
摘要：
BACKGROUND: Potassium bismuth citrate is a gastric mucosal protector and a key drug for treating peptic ulcers. OBJECTIVE: To evaluate the pharmacokinetic characteristics and safety of 120-mg bismuth potassium citrate formulations administered orally under fasting conditions in healthy Chinese subjects. METHOD: A single-center open two-cycle trial was conducted on 12 healthy subjects who received a single oral dose of 120 mg of bismuth potassium citrate. The plasma concentration of bismuth was determined using a validated inductively coupled plasma mass spectrometry (ICP‒MS) method. The pharmacokinetic parameters, including maximum serum concentration (C(max)) and area under the curve concentration-time curve (AUC(0-t) and AUC(0-∞)), and safety were evaluated via noncompartment analysis. RESULTS: The ratios of the least square geometric mean ratio between the test (T) and reference (R) formulations for C(max), AUC(0-t), and AUC(0-∞) were 44.8%, 55.5%, and 64.4%, respectively; the bilateral 95% confidence intervals (Cis) for these parameters were 20.2-99.6%, 24.1-127.5%, and 23.7-175.0%, respectively, and the non-inferior limits for these parameters were 169.4%, 198.8%, and 200.5%, respectively. The upper limits of the one-sided 97.5% confidence interval for the least squares geometric mean ratio (T/R) were lower than the non-inferior limits. No serious adverse reactions or adverse reactions leading to detachment were observed among the subjects. CONCLUSION: The concentration of bismuth in the blood of healthy subjects in the T formulation was not greater than that in the R formulation. Similarly, the safety of oral administration of 120 mg of bismuth potassium citrate formulations to healthy subjects was good. The trial registration number (TRN) was [2018] 013, 6 December 2018.
作者机构：
[Feng, Wen-Jie; Wu, Xiao-Ping; Zhu, Hong -Bo; He, Zhi-Long; Tan, Ye-Ru; Xun, Yi; Li, Yue-Hua; Jiang, Yi-Ling; Zhu, HB] Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Dept Med Oncol, Hengyang, Hunan, Peoples R China.;[Jiang, Bao-Hong] Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Dept Pharm, Hengyang, Hunan, Peoples R China.
通讯机构：
[Zhu, HB ] U;Univ South China, Affiliated Hosp 1, Hengyang Med Sch, Dept Med Oncol, Hengyang, Hunan, Peoples R China.
关键词：
AIFM2;GPX4;circRNAs;hepatocellular cancer (HCC);miR-6085
摘要：
BACKGROUND: Circular RNAs (circRNAs) represent a subset of non-coding RNAs implicated in the regulation of diverse biological processes, including tumorigenesis. However, the expression and functional implications of circ0060467 in hepatocellular carcinoma (HCC) remain elusive. In this study, we aimed to elucidate the role of circ0060467 in modulating the progression of HCC. METHODS: Differentially expressed circRNAs in HCC tissues were identified through circRNA microarray assays. Quantitative reverse transcription polymerase chain reaction (qRT-PCR) assays revealed the upregulation of circ0060467 in both HCC cell lines and tissues. Various assays were conducted to investigate the roles of circ0060467 in HCC progression. Additionally, RNA immunoprecipitation (RIP) assays and luciferase assays were carried out to assess the interactions between circ0060467, microRNA-6085 (miR-6085), apoptosis-inducing factor mitochondria-associated 2 (AIFM2), and glutathione peroxidase 4 (GPX4) in HCC. RESULTS: Microarray and qRT-PCR analyses demonstrated a marked elevation of circ0060467 in HCC tissues and cell lines. Knockdown of circ0060467 suppressed HCC cell proliferation. Luciferase reporter and RIP assays confirmed the binding of circ0060467, AIFM2, and GPX4 to miR-6805. Subsequent experiments revealed that circ0060467 competes with AIFM2 and GPX4, thereby inhibiting cancer cell ferroptosis by binding to miR-6085 and promoting hepatocellular carcinoma progression. CONCLUSIONS: Collectively, circ0060467 modulates the levels of AIFM2 and GPX4, crucial regulators of tumor cell ferroptosis, by acting as a sponge for miR-6085 in HCC. Thus, circ0060467 may represent a novel diagnostic marker and therapeutic target for HCC.
通讯机构：
[Zhou, Yu-Sheng] U;[Yu, DH; Xiao, JC] C;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prof Key Lab Tumor Microenvironm Respons Dr, Inst Pharm & Pharmacol,Affiliated Hosp 2, Hengyang 421001, Hunan, Peoples R China.;Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China.
会议名称：
75th International Symposium on Molecular Spectroscopy (ISMS)
会议时间：
JUN 22-26, 2020
会议地点：
Champaign Urbana, IL
会议主办单位：
[Xiang, Ya-Qing;Yao, Xu;Li, Rong;Zhou, Yu-Sheng] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prof Key Lab Tumor Microenvironm Respons Dr, Inst Pharm & Pharmacol,Affiliated Hosp 2, Hengyang 421001, Hunan, Peoples R China.^[Xiang, Ya-Qing;Lin, Jin-Hong;Yu, Dong-Hai;Xiao, Ji-Chang] Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China.^[Ou, Xiao-Jian] Jinchuan Grp, Ltd Laterite Leaching Project Team, Jinchang 737104, Gansu, Peoples R China.
摘要：
To provide feasible methods for the extraction of valuable metals from spent batteries or low-grade primary ores, the extraction behavior of some representative acidic phosphorus-containing compounds (APCCs) as extractants is evaluated from the perspective of experimental and theoretical investigations in this work. Aqueous solutions containing five metal ions, Ca(II), Co(II), Mg(II), Mn(II), and Ni(II), were made to simulate leaching liquids, and the extraction of these metals was investigated. A simplified calculated model was used to evaluate the interaction between each extractant and metal ions. The calculation results agree well with the experimental tests in trend. This work not only provides potential extractants for the extraction of valuable metals from spent batteries or low-grade primary ores but also demonstrates the practicability of the simplified calculation model.
期刊：
TECHNOLOGY AND HEALTH CARE,2019年27(S1):S307-S316 ISSN：0928-7329
通讯作者：
Yang, Jun;Chu, Chun
作者机构：
[Long, Junrong; Liu, Maojun; Liu, Shengquan; Tang, Feng; Tan, Wenting; Xiao, Ting; Yang, Jun] Univ South China, Affiliated Hosp 1, Dept Cardiol, Hengyang, Hunan, Peoples R China;[Chu, Chun] Univ South China, Dept Pharm, Affiliated Hosp 2, Hengyang, Hunan, Peoples R China
通讯机构：
[Yang, Jun; Chu, Chun] U;Univ South China, Affiliated Hosp 1, Dept Cardiol, Hengyang, Hunan, Peoples R China. Univ South China, Dept Pharm, Affiliated Hosp 2, Hengyang, Hunan, Peoples R China.
会议名称：
7th International Conference on Biomedical Engineering and Biotechnology (iCBEB)
会议时间：
OCT 17-20, 2018
会议地点：
Nanjing, PEOPLES R CHINA
关键词：
DM rats;ERK1/ 2mitogen-activated protein kinase;Exogenous hydrogen sulfide;MMPs/TIMPs expression dysregulation;inflammatory reaction;myocardial fibrosis;protein kinase C
摘要：
OBJECTIVE To investigate the roles and underlying mechanism of exogenous H2S (hydrogen sulfide) in attenuating the myocardial fibrosis in diabetic rats. METHODS: A total of 40 SD rats were randomly divided into 4 groups: control group, STZ group, STZ + H2S group and H2S group. To build the DM rat model, the rats in the STZ group and STZ + H2S group were injected streptozotocin (STZ) intraperitoneally, While the rats in the STZ + H2S group and the H2S group received sodium hydrosulfide (NaHS), which provides exogenous H2S. Eight weeks later, the myocardial tissues of rats were used to detecting the collagen deposition through Masson staining, as well as some protein expressions related to myocardial fibrosis and signaling pathway by western blotting. RESULTS: Comparing to control group, the collagen deposition of myocardial matrix remarkably increased in the STZ group, and almost all the proteins that are relative to myocardial fibrosis, inflammatory and signaling pathway show an overexpression, except for PPARG and NF-kappa Bp65. When Compared with the STZ group, the collagen deposition was obviously attenuated in STZ + H2S group, as well as the protein expressions above-mentioned, While PPARG was up-regulated. CONCLUSION: The myocardial fibrosis in DM rats can be attenuated effectively by exogenous H2S, and the underlying mechanism is likely to regulating PKC-ERK1/2MAPK signaling pathway, improving the MMPs/TIMPs expression dysregulation and inhibiting inflammatory reaction.
摘要：
OBJECTIVE: To explore the effect of gefitinib-coated balloon suppressive action on the excessive hyperplasia of intima after balloon injury of common carotid artery in rats and on the PI3K/AKT signal pathway. METHODS: MTT method and the expression of Bcl-2 and Caspase-3 proteins were detected in vitro; Adult SD rats were randomly split into 5 groups, namely sham group, model group, low-dosage gefitinib-coated balloon group, high-dosage gefitinib-coated balloon group, and paclitaxel-coated balloon group. The intimal proliferation of arteries, PCNA, P-AKT and PI3K protein expression, the cell apoptosis, expression of MMP9, TGF beta and IL6 mRNA were measured by hematoxylin and eosin (H&E) staining, immunohistochemistry, TUNEL staining, and RT-qPCR. RESULTS: At the same time and concentration, Gefitinib suppressed the proliferation of smooth muscle cell more significantly than paclitaxel. Bcl-2 and Caspase-3 in vascular smooth muscle and endothelial cells (VSMC, EC) were significantly downregulated and up-regulated after the cells were treated with gefitinib and paclitaxel. In gefitinib- and paclitaxel-coated balloon groups, significant up-regulations were found in the area of lumen. Furthermore, the expression of PCNA suggested that all coated balloons could suppress the excessive proliferation of smooth muscle cells in the hyperplastic intima compared with the control group. In gefitinib- and paclitaxel-coated balloon group, the expression of PI3K/AKT was significantly down-regulated. The use of drug-coated balloons mitigated the cell apoptosis in TUNEL. The expressions of MMP9, TGF beta and IL6 mRNA in the model group were obviously up-regulated; and they were obviously down-regulated in the high-dose gefitinib-coated balloon group compared with the model group. CONCLUSIONS: Gefitinib-coated balloons were able to suppress the excessive proliferation in the common carotid arterial intima of rats more effectively than the paclitaxel-coated ones. The underlying mechanism may cover the PI3K/AKT signal pathway.
作者机构：
[Tan, Huaxin; Zhang, Peng; Liu, Zhonghua; Liang, Songping; Huang, Yazhou] Hunan Normal Univ, Natl & Local Joint Engn Lab Anim Peptide Drug Dev, Coll Life Sci, Changsha 410081, Hunan, Peoples R China.;[Tan, Huaxin; Xu, Jianghong; Ye, Zhongju; Xiao, Lehui; Chen, Bo] Hunan Normal Univ, Key Lab Phytochem R&D Hunan Prov, Coll Chem & Chem Engn, Changsha 410081, Hunan, Peoples R China.;[Xiao, Lehui] Nankai Univ, State Key Lab Med Chem Biol, Coll Chem, Tianjin Key Lab Biosensing & Mol Recognit, Tianjin 300071, Peoples R China.;[Tan, Huaxin] Univ South China, Dept Biochem & Mol Biol, Sch Pharmaceut & Biol Sci, Hengyang 421001, Peoples R China.
通讯机构：
[Lehui Xiao] K;[Zhonghua Liu] T;The National & Local Joint Engineering Laboratory of Animal Peptide Drug Development, College of Life Sciences, Hunan Normal University, Changsha 410081, Hunan, China<&wdkj&>Key Laboratory of Phytochemical R&D of Hunan Province, College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha, Hunan, 410081, China<&wdkj&>State Key Laboratory of Medicinal Chemical Biology College of Chemistry, Tianjin Key Laboratory of Biosensing and Molecular Recognition, Nankai University, Tianjin, 300071, China
会议名称：
19th World Congress of the International-Society-on-Toxinology (IST) / 11th Asia Pacific Congress of the International-Society-on-Toxinology (IST) / 13th Chinese Conference on Toxins and Medical Applications
摘要：
Here, we report a new approach of on-resin peptide ligation using C-terminal benzyl ester as the stabilized precursor of thioester, which enables both N-terminal elongation and C-terminal peptide ligation on a Rink Amide resin. On-resin native chemical ligation and auxiliary-assisted peptide ligation were successfully achieved. This method is compatible to both protected and unprotected peptide fragments and has potential application in poor water-soluble peptide ligation.
期刊：
Journal of the American College of Cardiology,2017年69(11, Supplement):1881-1881 ISSN：0735-1097
作者机构：
Hunan Childrens Hosp, Dept Cardiol, Changsha, Hunan, Peoples R China.;Univ South China, Inst Pharm & Pharmacol, Hengyang, Peoples R China.;[Xiao, Yunbin; Peng, Hongyan; Qin, Xuping; Chen, Zhi; Hong, Chenliang; Deng, Xicheng; Luo, Jinwen] Department of Cardiology, Hunan Children's Hospital, Changsha, People's Republic of China<&wdkj&>Institute of Pharmacy and Pharmacology, University of South China, Hengyang, People's Republic of China
会议名称：
66th Annual Scientific Session and Expo of the American-College-of-Cardiology (ACC)
作者：
Li Fang;Yang Jun;Zeng Ou;Luo Jian;Wu Zhixiong;...
作者机构：
[Yang Jun; Luo Jian; Zeng Ou; Wu Zhixiong; Li Fang; Xiao Ting] Univ South China, Affiliated Hosp 1, Dept Cardiol, Hengyang 421001, Peoples R China.;[Chu Chun] Univ South China, Affiliated Hosp 2, Dept Pharm, Hengyang 421001, Peoples R China.
会议名称：
Joint Conference of 6th International Congress on Electrical and Engineering (ICECE) / 4th International Conference on Material Science and Manufacturing (ICMSM)
会议时间：
AUG 14-15, 2015
会议地点：
Shanghai, PEOPLES R CHINA
会议主办单位：
[Li Fang;Yang Jun;Zeng Ou;Luo Jian;Wu Zhixiong;Xiao Ting] Univ South China, Affiliated Hosp 1, Dept Cardiol, Hengyang 421001, Peoples R China.^[Chu Chun] Univ South China, Affiliated Hosp 2, Dept Pharm, Hengyang 421001, Peoples R China.
摘要：
Objective: To explore the special cytotoxicity of TGF alpha-SAP and bFGF-SAP on proliferating vascular smooth muscle cells(VSMCs) and endothelial cells(ECs). Methods: Conjugation of saporin to TGF alpha and bFGF-SAP were accomplished after derivatization of saporin,TGF alpha and bFGF-SAP with N-succinimidyl-3 (2-pyridyldithio) proprionate and final purification of the conjugate were achieved within Eppendorf Centrifugal Filter Tubes. Cytotoxicity assays were measured by MTS method. The influence of TGF alpha-SAP and bFGF-SAP on values of Thymidine incorporation into SMCs and ECs was measured by H-3-thymidine uptake, respectively. Results: Cytotoxicity assays testified that TGF alpha-SAP conjugation could inhibit more remarkably the proliferation of SMCs in cell culture, compared with bFGF-SAP. The values of thymidine incorporation of TGF alpha-SAP group (10(-9)M and 10(-7)M) decreased to 60.9% and 56.0% respectively of the control group, suggesting that cellular DNA synthesis obviously decreased as TGF alpha-SAP was added. But Saporin did not affect cellular DNA synthesis even at higher level(10(-3)M). After SMCs were exposed to TGF alpha-SAP and bFGF-SAP at the same level (10(-9)M), the values of thymidine incorporation of TGF alpha-SAP group decreased 29.5% compared with control group while that of bFGF-SAP group only decreased 9.86%. TGF alpha-SAP at higher level did not affect DNA synthesis of ECs while bFGF-SAP did. Conclusion: The results indicated that TGF alpha-SAP possessed more efficient and specific cytotoxicity on proliferating VSMCs than bFGF-SAP.
作者：
Ling, H. Y.;Ou, H. S.;Lei, X. Y.;Zhu, B. Y.;Yin, W. D.;...
期刊：
RECENT ADVANCES IN CARDIOVASCULAR DISEASE: PROCEEDINGS OF THE 13TH WORLD CONGRESS HEART DISEASE,2007年:263-267
通讯作者：
Liao, D. F.
作者机构：
[Zhu, B. Y.; Yin, W. D.; Lei, X. Y.; Ou, H. S.; Liao, D. F.; Ling, H. Y.] Univ S China, Inst Pharm & Pharmacol, Div Pharmacoprote, Hengyang, Peoples R China.
通讯机构：
[Liao, D. F.] U;Univ S China, Inst Pharm & Pharmacol, Div Pharmacoprote, Hengyang, Peoples R China.
关键词：
MicroRNA;adipocyte;3T3-L1;differentiation;insulin signal
摘要：
This study investigated the MicroRNA expression profile during the differentiation from 3T3-L1 preadipocytes into adipocytes by miRNAs microarray analysis. We found both 3T3-L1 preadipocytes and adipocytes express 331 miRNAs. In adipocyte, 26 miRNAs were upregulated and 2 miRNAs were downregulated compared to 3T3-L1 preadipocytes. Interestingly, we observed that the target genes of miR-21, miR-298, let-7e were associated with insulin signal pathway.
作者：
Luo, D. X.;Xia, C. L.;He, S. Y.;Tong, S. S.;Xu, C. X.;...
期刊：
RECENT ADVANCES IN CARDIOVASCULAR DISEASE: PROCEEDINGS OF THE 13TH WORLD CONGRESS HEART DISEASE,2007年:47-52
通讯作者：
Li, K.
作者机构：
[He, S. Y.; Luo, D. X.; Xia, C. L.; Xu, C. X.; Li, K.; Liao, D. F.; Tong, S. S.] Univ S China, Inst Pharm & Pharmacol, Div Pharmacoproteom, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Li, K.] U;Univ S China, Inst Pharm & Pharmacol, Div Pharmacoproteom, Hengyang 421001, Hunan, Peoples R China.
摘要：
To investigate the mechanism of sustained static pressure-dependent smooth muscle cells (SMCs) proliferation, SMCs from rat aorta were treated with different static pressures for 24 hrs or were cultured under constant static pressure of 120 mmHg for different time periods. SMCs proliferation and extracellular signal-regulated protein kinase1/2 (ERK1/2) activation significantly increased in pressure-dependent manner with the peak at the pressure of 120 mmHg and in time-dependent manner with the peak at 4 hrs. Static pressure obviously inhibited caveolin-1 expression, which was negative correlated with the ERK1/2 activation. The proliferation was selectively inhibited by PD98059 through blocking ERK1/2 phosphorylation. These findings demonstrate that sustained static pressure stimulates SMCs proliferation via the ERK1/2 pathway. Key words: pressure, smooth muscle cell, caveolin-1, extracellular signal-regulated protein kinase.
作者：
Ling, H. Y.;Ou, H. S.;Lei, X. Y.;Gao, Z. P.;Yin, W. D.;...
期刊：
RECENT ADVANCES IN CARDIOVASCULAR DISEASE: PROCEEDINGS OF THE 13TH WORLD CONGRESS HEART DISEASE,2007年:269-274
通讯作者：
Liao, D. F.
作者机构：
[Gao, Z. P.; Yin, W. D.; Lei, X. Y.; Ou, H. S.; Liao, D. F.; Ling, H. Y.] Univ S China, Inst Pharm & Pharmacol, Div Pharmacoprote, Hengyang, Peoples R China.
通讯机构：
[Liao, D. F.] U;Univ S China, Inst Pharm & Pharmacol, Div Pharmacoprote, Hengyang, Peoples R China.
关键词：
microRNA;adipocyte;3T3-L1;insulin resistance
摘要：
MicroRNAs (miRNAs) are a class of small non-coding RNAs which play an important role in metabolism of glucose and lipid in adipocyte. This study investigated miRNAs expression profiles during the formation process of insulin-resistant adipocyte derived from 3T3-L1 adipocyte. miRNAs were examined by miRNAs microarray analysis..The results showed that 71 miRNAs were upregulated and 33 miRNAs were downregulated during the formation of insulin resistance. Among them, miRNA (miR)-320, -494, -503, -202, -185 and -129-5p were significantly increased. Western blotting analysis showed that Anti-miR-320 increased GLUT4 expression.
