摘要：
Primary dysmenorrhea (PD) constitutes a common gynecological disease among young women. The NLRP3 inflammasome may be activated and expressed in PD, but the mechanistic link between NLRP3 inflammasome activation and PD is still unclear. To investigate the potential role of NLRP3 inflammasome activation in the pathogenesis of PD, 30 female Kunming mice without pregnancy were used for experiments. The PD mouse model was constructed by 11 days of successive co-treatment with estradiol and oxytocin. MCC950, a potent and specific small-molecule inhibitor of the NLRP3 inflammasome, was used to treat PD mice. The disease level was assessed by the writhing response and hot water tail-flick test. The levels of prostaglandin E2 (PGE2) and prostaglandin F2 alpha (PGF2α) in the uterine tissues of mice were detected by ELISA. The expression levels of protein and cytokines, including NLRP3, cysteine aspartic acid-specific protease 1 (caspase-1), interleukin (IL)-1β, IL-18, nuclear factor kappa B (NF-κB) p65, phospho-NF-κB p65, and cyclooxygenase-2 (COX-2) were revealed by western blot analysis. MCC950 greatly ameliorated the writhing response induced by the combination of oxytocin and estradiol, with an increasing length of tail-flick latency. MCC950 also significantly decreased the levels of PGF2α and PGE2, and the expressions of NLRP3, caspase-1, IL-1β, IL-18, phospho-NF-κB p65, NF-κB p65, and COX-2 in the uterus. MCC950 markedly alleviated the pain and pathological damage in PD mice by inhibiting NLRP3 activation. The underlying mechanism may be related to hypoactive uterine inflammation via suppression of NLRP3 activation and the NF-κB/COX-2/PG pathway in uteruses of PD mice.
通讯机构：
[Qiu, RH; Yin, SF; Chen, Yi] H;Hunan Univ, Coll Chem & Chem Engn, State Key Lab Chemo Biosensing & Chemometr, Changsha 410082, Hunan, Peoples R China.;Hunan Univ Chinese Med, Sch Med, Changsha 410208, Hunan, Peoples R China.
摘要：
A series of organoantimony(iii) halide complexes with a tetrahydrodibenzo[c,f][1,5]azastibocine framework were synthesized and employed as water tolerant Lewis acid catalysts. The results of a systematic structure-activity relationship study demonstrated that the strength of N -> Sb donor-acceptor interaction could be synergistically modulated by tuning the properties of the nitrogen substituents and halogen atoms adjacent to the central antimony atom, and consequently resulted in distinct catalytic performances towards organic reactions such as Mannich, cross-condensation, cyclization-aromatization and epoxide aminolysis reaction. The fluorinated organoantimony(iii) derivatives were found to be more active than those of the chlorinated, brominated and iodinated analogues, owing to the use of an Sb-F moiety as a hydrogen bond acceptor. By comparison, the compound 6-cyclohexyl-12-fluoro-5,6,7,12-tetrahydrodibenzo[c,f][1,5] azastibocine (1d) is found to exhibit the highest catalytic activity, together with facile reusability in scale enlarged synthesis.
摘要：
Heilaohu, the roots of Kadsura coccinea, has a long history of use in Tujia ethnomedicine for the treatment of rheumatoid arthritis and gastroenteric disorders, and a lot of work has been done in order to know the material basis of its pharmacological activities. The chemical investigation led to the isolation and characterization of three new (1(-)3) and twenty known (4(-)23) lignans. Three new heilaohulignans A-C (1(-)3) and seventeen known (4(-)20) lignans possessed dibenzocyclooctadiene skeletons. Similarly, one was a diarylbutane (21) and two were spirobenzofuranoid dibenzocyclooctadiene (22(-)23) lignans. Among the known compounds, 4(-)5, 7, 13(-)15 and 17(-)22 were isolated from this species for the first time. The structures were established, using IR, UV, MS and NMR data. The absolute configurations of the new compounds were determined by circular dichroism (CD) spectra. The isolated lignans were further evaluated for their cytotoxicity and antioxidant activities. Compound 3 demonstrated strong cytotoxic activity with an IC50 value of 9.92 microM, compounds 9 and 13 revealed weak cytotoxicity with IC50 values of 21.72 microM and 18.72 microM, respectively in the HepG-2 human liver cancer cell line. Compound 3 also showed weak cytotoxicity against the BGC-823 human gastric cancer cell line and the HCT-116 human colon cancer cell line with IC50 values of 16.75 microM and 16.59 microM, respectively. A chemiluminescence assay for antioxidant status of isolated compounds implied compounds 11 and 20, which showed weak activity with IC50 values of 25.56 microM and 21.20 microM, respectively.
期刊：
Rapid Communications in Mass Spectrometry,2017年31(5):397-410 ISSN：0951-4198
通讯作者：
Zeng, Jianguo;Zhao, Zhongzhen
作者机构：
[Liu, Xiubin; Zheng, Yajie; Liu, Yisong; Tang, Qi; Zeng, Jianguo; Zuo, Zi] Hunan Agr Univ, Natl & Prov Union Engn Res Ctr, Vet Herbal Med Resources & Initiat, Changsha 410128, Hunan, Peoples R China.;[Liang, Zhitao; Zhao, Zhongzhen] Hong Kong Baptist Univ, Sch Chinese Med, Kowloon, Hong Kong, Peoples R China.;[Zuo, Zi] Hunan Univ Chinese Med, Affiliated Hosp 2, Changsha 410005, Hunan, Peoples R China.
通讯机构：
[Zeng, Jianguo; Zhao, Zhongzhen] H;Hunan Agr Univ, Natl & Prov Union Engn Res Ctr, Vet Herbal Med Resources & Initiat, Changsha 410128, Hunan, Peoples R China.;Hong Kong Baptist Univ, Sch Chinese Med, Kowloon, Hong Kong, Peoples R China.
摘要：
Two new anthraquinones, 1,3-dihydroxy-5-methoxy-6-methoxymethyl-2-methyl-9,10-anthraquinone (1) and 1,3-dihydroxy-5-methoxy-2,6-bismethoxymethyl-9,10-anthraquinone (2), together with ten known anthraquinone derivatives (3-12), three coumarin derivatives (13-15), and 6-gingerol (16) were isolated from the barks of Morinda citrifolia (Noni) collected in the Yongxing island of Xisha. The structures of compounds (1-16) were determined on the basis of extensive spectroscopic analyses, as well as by comparison with literature reports. The new compounds 1 and 2 were tested for their antiviral, cytotoxic, and antibacterial activities. In the primary bioassays, compounds 1 and 2 displayed weak antiH1N1 activity with IC50 values of 66.1 and 10.5 mu M, respectively. In addition, compound 2 showed weak anti-H3N2 activity with IC50 value of 11.5 mu M, and had weak antimicrobial activity against Staphylococcus aureus with MIC value of 24.5 mu M. (C) 2015 Phytochemical Society of Europe. Published by Elsevier B.V. All rights reserved.
摘要：
The present study was to determine the targeting effect of M13 phage peptide ZL4 (MppZL4) on Schistosoma japonicum (S.j). Mice infected with S.j were injected with MppZL4. Real-time PCR was used to detect the distribution and metabolism of MppZL4 in the livers and lungs of mice. In vivo refusion test was performed to detect the targeting of MppZL4. Western blotting was employed to determine the expression of MppZL4. Live imaging was used to detect the distribution of oligopeptide MppZL4. Immunohistochemistry was employed to determine MppZL4 location on adult S.j body surface. Gomori method was employed to detect the influence of oligopeptide MppZL4 on alkaline phosphatase activity. The distribution and metabolism of MppZL4 and M13KE are not significantly different from each other at each time point. The abundance of MppZL4 is changed as S.j migrates in mice. The targeted binding effect of MppZL4 varies at different stages. ZL4 oligopeptide targets S.j in mice. The specific binding sites of MppZL4 on S.j body are mainly located in syncytial cells. The binding sites of MppZL4 on S.j body surface might be ALP or ALP-related proteins. MppZL4 had targeted binding effect on S.j with its binding site being associated with proteins related to S.j alkaline phosphatase. S.j tegument had a specifically binding site with exogenous peptides, offering new means to explore the interactions between hosts and parasites. Additionally, MppZL4 can possibly be used as targeting molecules in worm-resistant drugs or as tracing molecules in imaging diagnosis technologies.
