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Study of a water-soluble supramolecular complex of curcumin andβ-cyclodextrin polymer with electrochemical property and potential anti-cancer activity
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作者 Wang Zhang Ping Xiao +4 位作者 Liwei Lin Fang Guo Qingyue Wang Yuanzhe Piao Guowang Diao 《Chinese Chemical Letters》 SCIE CAS CSCD 2022年第8期4043-4047,共5页
As a member of the curcuminoid compound family,curcumin(Cur)has many interesting therapeutic properties.However,its low aqueous solubility and stability have resulted in poor bioavailability and restricted clinical ef... As a member of the curcuminoid compound family,curcumin(Cur)has many interesting therapeutic properties.However,its low aqueous solubility and stability have resulted in poor bioavailability and restricted clinical efficacy.Based on size matching,β-cyclodextrin polymer(β-CDP),with its hydrophilic polymer chains and hydrophobic cavities,can form an inclusion complex with Cur.To improve the water solubility and stability of Cur,a simple and eco-friendly grinding method was designed to formβ-CDP inclusion complexes.According to the Boltzmann-Hamel's method and Job's method,the molar ratio of theβ-CD unit inβ-CDP to Cur was determined to be 1:1.The diffusion coefficient and diffusion activation energy of Cur-β-CDP were calculated in an electrochemical study.This supramolecular complex worked well in vitro to inhibit the proliferation of hepatoma carcinoma cells HepG2.Remarkably,this method visibly reduced the undesirable side effects on normal cells,without weakening the anti-cancer activity of the drugs.We expect that the obtained host-vip complex will provide a new approach for delivering natural drug molecules,having low water solubility. 展开更多
关键词 Cyclodextrin polymer CURCUMIN SOLUBILITY anti-cancer activity Supramolecular complex
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Anti-cancer activity of an ethyl-acetate extract of the fruits of Terminalia bellerica(Gaertn.)Roxb.through an apoptotic signaling pathway in vitro 被引量:6
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作者 Shi Li Ting Ye +4 位作者 Linjin Liang Wenyi Liang Ping Jian Kun Zhou Lanzhen Zhang 《Journal of Traditional Chinese Medical Sciences》 2018年第4期370-379,共10页
Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapid... Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica(Gaertn.)Roxb.(hereafter termed T.bellerica)and estimate the anti-cancer activity of different polar extracts.Methods:To rapidly screen and identify the biochemical constituents of ethyl acetate(EA)extracts of T.bellerica,ultra performance liquid chromatography-electrospray ionization/mass spectrometry(UPLC-ESI-MSn)was done.The CellTiter-BlueTM cell-viability assay was used to ascertain the anti-cancer activity of different polar extracts in 10 human cancer cell lines.Results:Forty polyphenols of the EA extract of T.bellerica were characterized tentatively.The EA extract exhibited significant anti-cancer activity against ZR-75-1 cells(half-maximal inhibitory concentration=27.33(0.98)μg/mL)and Colo-205 cells(39.65(2.99)μg/mL)in vitro.Treatment of ZR-75-1 cells with 20 and 60μg/mL of the EA extract elicited dosedependent apoptosis percentages at an early stage of 17.58(0.74)%and at a late stage of 29.20(1.22)%;Colo-205 cells at the same concentration of EA extract had values of 21.33(1.03)%and 40.55(0.34)%,respectively.Western blotting suggested that ZR-75-1 and Colo205 cells treated with the EA extract showed a similar increasing tendency for expression of cleaved anti-poly adenosine diphosphate ribose polymerase I.Conclusion:We identified a total of 40 chemical constituents,of which 11 were first obtained from the Terminalia Linn.genus using UPLC-ESI-MSn.Meanwhile,we observe that the EA extract of T.bellerica possesses anti-cancer activity,especially against breast and colon cancers. 展开更多
关键词 TERMINALIA bellerica anti-cancer activity UPLC-ESI-MSn CellTiter-blue
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Potential Anti-cancer Activity of Furanodiene 被引量:7
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作者 Zhen-zhen Ba Yan-ping Zheng Hui Zhang Xiu-yan Sun Dong-hai Lin 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 2009年第2期154-158,共5页
Objective: To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin (C15H200), a primary sesquiterpene compound YH Chen et C. Ling(Wen Ezhu), in vi... Objective: To study the isolated from the essential oil VIVO anti-tumor activities of furanodiene of the rhizome of Curcuma wenyujin (C15H200), a primary sesquiterpene compound YH Chen et C. Ling(Wen Ezhu), in vitro and in Methods: In vitro MTT assay was used to further study the effects of time and dosage on anti-proliferation of furanodiene against the sensitive Hela, Hep-2, HL-60, U251 cells, based on the cytotoxic effects of furanodiene on 12 human malignant tumor cell lines with the essential oil of Wen Ezhn as control., and the half-inhibitory concentration (IC50) was observed. In vivo uterine cervix (U14) tumor cell was selected and the conventional assay method of anti-tumor activity was employed. Furanodiene liposome was administered intraperitoneally, and tumor-inhibitory rate, thymus and spleen indexes were observed. Results: The inhibitive effects on cell proliferation were shown in all of the twelve cell lines and the cytotoxic effects of furanodiene against Hela, Hep-2, HL-60, U251 cells were observed after 12 h of administration, the effect could last for at least 48 h in a dose dependent manner, and the IC50 values were 0.6, 1.7, 1.8, 7.0μg/ml, respectively. Furanodiene was also found to show inhibitive effects on the proliferation of uterine cervix (U14) tumor induced in mice. The tumor inhibition rates were 36.09% (40 mg/kg), 41.55% (60 mg/kg), 58.29% (80 mg/kg), respectively. Conclusion: Furanodiene is one of primary anti-cancer active components in the essential oil of Wen Ezhu, and also a very effective agent against uterine cervix cancer, and has protection effect on the immune function. 展开更多
关键词 Essential oil of Wen Ezhu FURANODIENE anti-cancer Uterine cervix cancer
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Quantitative Structure Anti-Cancer Activity Relationship (QSAR) of a Series of Ruthenium Complex Azopyridine by the Density Functional Theory (DFT) Method 被引量:5
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作者 Kouakou Nobel N’guessan Mamadou Guy-Richard Koné +2 位作者 Kafoumba Bamba Ouattara Wawohinlin Patrice Nahossé Ziao 《Computational Molecular Bioscience》 2017年第2期19-31,共13页
A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) an... A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules. 展开更多
关键词 RUTHENIUM Azopyridine Complex anti-cancer QSAR DFT METHOD
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Sesamum indicum(sesame) enhances NK anti-cancer activity, modulates Th1/Th2 balance, and suppresses macrophage inflammatory response 被引量:1
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作者 Amin FMajdalawieh Jenna F.Farraj Ronald I.Carr 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2020年第7期316-324,共9页
Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of nat... Objective:To evaluate the potential immunomodulatory effects of an aqueous extract of Sesamum indicum seeds with regard to splenocyte proliferation,Th1/Th2 balance,macrophage function,and the cytotoxic activity of natural killer(NK)cells.Methods:Splenocyte proliferation was measured by[~3H]-thymidine incorporation.Griess assay was performed to evaluate the production of nitric oxide by macrophages.The levels of cytokines secreted by splenocytes and macrophages were measured by ELISA.JAM assay was performed to examine the cytotoxic activity of NK cells against YAC-1 tumor cells.Results:Sesamum indicum significantly enhanced splenocyte proliferation in a dose-dependent manner.Sesamum indicum also increased and suppressed the secretion of Th1 and Th2 cytokines,respectively,by splenocytes.The secretion of key pro-inflammatory mediators(IL-6,TNFα,and nitric oxide)by primary macrophages was significantly inhibited by Sesamum indicum.Moreover,Sesamum indicum increased the cytotoxic activity of NK cells against YAC-1 tumor cells.Conclusions:Sesamum indicum shows potent immunomodulatory,anti-inflammatory,and anti-cancer effects.Constituents of Sesamum indicum may be used as effective therapeutic agents in regulating immune reactions implicated in various infectious and noninfectious conditions including cancer. 展开更多
关键词 Sesamum indicum anti-cancer Inflammation IMMUNOMODULATION MACROPHAGES NK cells
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Study on the Synthesis and in vitro Photodynamic Anti-cancer Activity of Tetra(trifluoroethoxy) Germanium Phthalocyanine 被引量:3
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作者 吴丽荣 黄丽英 林振华 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2014年第7期1081-1090,共10页
The synthesis and in vitro photodynamic anticancer activity of a new photosen- sitizer, tetra(trifluoroethoxy) germanium phthalocyanine (GePcF), were studied. GePcF was characterized by UV-Vis, IR, MS and elementa... The synthesis and in vitro photodynamic anticancer activity of a new photosen- sitizer, tetra(trifluoroethoxy) germanium phthalocyanine (GePcF), were studied. GePcF was characterized by UV-Vis, IR, MS and elemental analysis. The in vitro photodynamic activity of GePcF was studied by MTT. IC50 of GePcF for SW480 cells of human colonic adenocarcinoma and HeLa cells of cervical cancer were 36.53 and 45.78 μmol/L, respectively. GePcF as a photosensitizer may be used to treat cancers due to its photodyrmmic anticancer activity. 展开更多
关键词 tetra(trifluoroethoxy) germanium phthalocyanine synthesis characterization photodynamic activity
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DT-13, a saponin of dwarf lilyturf tuber, exhibits anti-cancer activity by down-regulating C-C chemokine receptor type 5 and vascular endothelial growth factor in MDA-MB-435 cells 被引量:7
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作者 ZHAO Ren-Ping LIN Sen-Sen +4 位作者 YUAN Sheng-Tao YU Bo-Yang BAI Xian-Shu SUN Li ZHANG Lu-Yong 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2014年第1期24-29,共6页
AIM: To investigate the anticancer activity of DT-13 under normoxia and determine the underlying mechanisms of action. METHODS: MDA-MB-435 cell proliferation, migration, and adhesion were performed to assess the ant... AIM: To investigate the anticancer activity of DT-13 under normoxia and determine the underlying mechanisms of action. METHODS: MDA-MB-435 cell proliferation, migration, and adhesion were performed to assess the anticancer activity of DT-13, a saponin from Ophiopogonjaponicus, in vitro. In addition, the effects of DT-13 on tumor growth and metastasis in vivo were evaluated by orthotopic implantation of MDA-MB-435 cells into nude mice; mRNA levels of vascular endothelial growth factor (VEGF), C-C chemokine receptor type 5 (CCR5) and hypoxia-inducible factor 1a (HIF-1a) were evaluated by real-time quantitative PCR; and CCR5 protein levels were detected by Western blot assay. RESULTS: At 0.01 to 1 umol·L -1, DT-13 inhibited MDA-MB-435 cell proliferation, migration, and adhesion significantly in vitro. DT-13 reduced VEGF and CCR5 mRNAs, and decreased CCR5 protein expression by down-regulating HIF-1 a. In addition, DT-13 inhibited MDA-MB-435 cell lung metastasis, and restricted tumor growth slightly in vivo. CONCLUSION: DT-13 inhibited MDA-MB-435 cell proliferation, adhesion, and migration in vitro, and lung metastasis in vivo by reducing VEGF, CCR5, and HIF-la expression. 展开更多
关键词 DT- 13 SAPONIN Ophiopogonjaponicus Anticancer activity CCR5 VEGF HIF- 1 a
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Prenylated flavonoids from Glycyrrhiza uralensis as promising anti-cancer agents: a preliminary structure-activity study 被引量:8
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作者 唐叔南 黄维 +4 位作者 季帅 王永瑞 裴道勇 叶敏 余四旺 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2016年第1期23-29,共7页
Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangusto... Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangustone A(IAA) from licorice(Glycyrrhiza uralensis), which induces apoptosis in colorectal cancer cells by disrupting mitochondrial functions. In the present study, we compared a group of flavonoids from licorice with IAA for their anti-proliferation activities and effects on intracellular signaling. The results indicated that the isoprenyl groups on the A and B rings, the hydroxyl groups at the ortho position of isoprenyl on A ring and the conjugated plane of C ring might contribute to the anti-cancer activity of prenylated flavonoids. Based on the above structure-activity relationship, we further identified four prenylated flavonoids with similar anti-cancer activities from licorice. Taken together, our present study established a preliminary structure-activity relationship of anti-cancer prenylated flavonoids, and our data provided important leading compounds from licorice, which deserved further research and development. 展开更多
关键词 Prenylated flavonoids LICORICE anti-cancer Structure-activity relationship
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Preoperative butyrylcholinesterase activity and risk of postoperative delirium:A meta-analysis
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作者 Yuan-Li Qiu Cheng Song +1 位作者 Cui-Wan Huang Wei-Gang Shen 《World Journal of Psychiatry》 2026年第1期385-399,共15页
BACKGROUND Postoperative delirium(POD)is a common and serious complication in surgical patients,particularly older adults.Alterations in cholinergic function have been implicated in its pathophysiology.AIM To evaluate... BACKGROUND Postoperative delirium(POD)is a common and serious complication in surgical patients,particularly older adults.Alterations in cholinergic function have been implicated in its pathophysiology.AIM To evaluate the association between preoperative serum cholinesterase(ChE)activity—specifically butyrylcholinesterase(BuChE)and acetylcholinesterase(AChE)—and the risk of POD in adult surgical patients in a meta-analysis.METHODS A systematic search was conducted in PubMed,EMBASE,and Web of Science up to March 28,2025 for studies reporting preoperative serum BuChE or AChE activity in relation to subsequent POD incidence.Standardized mean differences(SMDs)and odds ratios(ORs)with 95%confidence intervals(CIs)were pooled using random-effects models.Subgroup and sensitivity analyses were performed based on follow-up duration and analytic models.RESULTS Thirteen studies(n=2730 patients)were included.Patients who developed POD had significantly lower preoperative BuChE activity than those who did not(SMD=-0.28;95%CI:-0.39 to-0.16;I²=18%).Higher BuChE activity was associated with a reduced risk of POD(OR per 100 unit increment=0.97;95%CI:0.95-0.99;I2=0%).In contrast,pooled AChE activity did not differ significantly between POD and non-POD groups(SMD=-0.25;95%CI:-0.53 to 0.03;P=0.08;I2=80%),and the ORs per 1 unit increment in AChE activity were not statistically significant(OR=0.98;95%CI:0.95-1.01).CONCLUSION Lower preoperative serum BuChE activity is associated with an increased risk of POD in adults undergoing surgery.BuChE activity may serve as a potential preoperative biomarker for POD risk stratification. 展开更多
关键词 ACETYLCHOLINESTERASE BUTYRYLCHOLINESTERASE activity Postoperative delirium META-ANALYSIS
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Abnormal regional spontaneous brain activity in major depressive disorder with obesity comorbidity:A resting-state functional magnetic resonance imaging study
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作者 Xiao-Fang Hou Bo-Hui Mei +10 位作者 Xia Wang Fu-Tao Zhao Lei He Qian-Yu Chen Chen Zang Chong Wang Yu-Feng Tang Xiao-Xin Li Hui-Fang Zhang Na Wang Bing Cao 《World Journal of Psychiatry》 2026年第1期335-345,共11页
BACKGROUND Major depressive disorder(MDD)and obesity(OB)are bidirectionally comorbid conditions with common neurobiological underpinnings.However,the neurocognitive mechanisms of their comorbidity remain poorly unders... BACKGROUND Major depressive disorder(MDD)and obesity(OB)are bidirectionally comorbid conditions with common neurobiological underpinnings.However,the neurocognitive mechanisms of their comorbidity remain poorly understood.AIM To examine regional abnormalities in spontaneous brain activity among patients with MDD-OB comorbidity.METHODS This study adopted a regional homogeneity(ReHo)analysis of resting-state functional magnetic resonance imaging.The study included 149 hospital patients divided into four groups:Patients experiencing their first episode of drug-naive MDD with OB,patients with MDD without OB,and age-and sex-matched healthy individuals with and without OB.Whole-brain ReHo analysis was conducted using SPM12 software and RESTplus toolkits,with group comparisons via ANOVA and post-hoc tests.Correlations between ReHo values and behavioral measures were examined.RESULTS ANOVA revealed significant whole-brain ReHo differences among the four groups in four key regions:The left middle temporal gyrus(MTG.L),right cuneus,left precuneus,and left thalamus.Post-hoc analyses confirmed pairwise differences between all groups across these regions(P<0.05).OB was associated with ReHo alterations in the MTG.L,right cuneus,and left thalamus,whereas abnormalities in the precuneus suggested synergistic pathological mechanisms between MDD and OB.Statistically significant correlations were found between the drive and fun-seeking dimensions of the behavioral activation system,as well as behavioral inhibition and the corresponding ReHo values.CONCLUSION Our findings provide novel evidence for the neuroadaptive mechanisms underlying the MDD-OB comorbidity.Further validation could lead to personalized interventions targeting MTG.L hyperactivity and targeting healthy food cues. 展开更多
关键词 Neuroimage COMORBIDITY Brain activity OBESITY Major depression Regional spontaneous
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Illusion of inactivity:Revisiting progressive multiple sclerosis treatment paradigms
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作者 Tal Ganz Tamir Ben-Hur 《Neural Regeneration Research》 2026年第3期1134-1135,共2页
Active inflammation in“inactive”progressive multiple sclerosis:Traditionally,the distinction between relapsing-remitting multiple sclerosis and progressive multiple sclerosis(PMS)has been framed as an inflammatory v... Active inflammation in“inactive”progressive multiple sclerosis:Traditionally,the distinction between relapsing-remitting multiple sclerosis and progressive multiple sclerosis(PMS)has been framed as an inflammatory versus degenerative dichotomy.This was based on a broad misconception regarding essentially all neurodegenerative conditions,depicting the degenerative process as passive and immune-independent occurring as a late byproduct of active inflammation in the central nervous system(CNS),which is(solely)systemically driven. 展开更多
关键词 inflammatory versus degenerative dichotomythis treatment paradigms illusion inactivity multiple sclerosis traditionallythe central nervous system cns which progressive multiple sclerosis active inflammation progressive multiple sclerosis pms
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Non-Flat Bisbenzylisoquinoline Alkaloid Fangchinoline As a Class of Potent G-Quadruplex Stabilizer with Anti-cancer Activity
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作者 Qian Li Junfeng Xiang Yalin Tang 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2015年第9期1041-1048,共8页
Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, ... Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, showed to strongly stabilize the intermolecular and intramolecular parallel stranded G-quadruplex structure, increasing melting temperature by 20 and 23℃, respectively. The binding mode was investigated by using NMR and molec- ular modelling methods. Four human cell lines (HL-60, BGC-823, Be1-7402 and KB) were taken to test the an- ti-proliferation effects of fangchinoline and the IC50 values were ranged from 16 to 32 μmol/L. These results showed that the fangchinoline or related moiety derivatives may represent a class of telomere-targeted agents as po- tential anti-cancer drugs. 展开更多
关键词 G-QUADRUPLEX alkaloid non-flat anti-cancer drug
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New RXRα modulators with unique binding mechanisms and anti-cancer activity
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《Science Foundation in China》 CAS 2015年第1期58-58,共1页
Prof.Zhang Xiaokun’s laboratory at the School of Pharmaceutical Sciences,Xiamen University identified several new small molecule modulators of nuclear receptor RXRαwith unique binding mechanisms and anti-cancer acti... Prof.Zhang Xiaokun’s laboratory at the School of Pharmaceutical Sciences,Xiamen University identified several new small molecule modulators of nuclear receptor RXRαwith unique binding mechanisms and anti-cancer activity,which was recently published in Chemistry&Biology(2014,21:596-607)and ACS Med Chem Lett(2014,5:736—741).RXRα,a unique member of the nuclear receptor superfamily of transcription factors,is an important 展开更多
关键词 XIAMEN SUPERFAMILY screening NEW RXR ANTAGONIST activATE treating modulator analogs pocket
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Hepatitis B virus reactivation in patients with hepatocellular carcinoma undergoing anti-cancer therapy 被引量:20
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作者 Jeong Won Jang 《World Journal of Gastroenterology》 SCIE CAS 2014年第24期7675-7685,共11页
Patients with hepatocellular carcinoma (HCC) often experience hepatic morbidity. Hepatitis B virus (HBV) reactivation is well documented as a serious hepatic morbidity during anti-cancer therapy. Reported rates of HBV... Patients with hepatocellular carcinoma (HCC) often experience hepatic morbidity. Hepatitis B virus (HBV) reactivation is well documented as a serious hepatic morbidity during anti-cancer therapy. Reported rates of HBV reactivation in chronic carriers with HCC undergoing chemotherapy range from 4%-67%. Apart from chemotherapy, HBV reactivation has been increasingly identified in settings of hepatectomy and local ablation therapies. The rates of HBV reactivation vary with different levels of immunosuppression and depend on treatment, viral factors, and patient characteristics. The principal concern relating to reactivation is that a substantial proportion of patients with reactivation suffer from liver dysfunction during therapy, which often leads to disruption of planned, potentially life-prolonging treatments, adversely affecting the patients&#x02019; final outcome. The first step in the management of HBV reactivation is identification of patients at risk of reactivation by testing for HBV serology prior to commencing anti-cancer therapy. Although it is a serious complication, HBV reactivation is preventable with prophylactic anti-HBV drugs. Multiple publications have shown the benefit of prophylactic or preemptive antiviral therapy in this setting and justified such an approach before the start of therapy. Given the tumors and underlying cirrhosis, long-term use of antivirals with high potency and low risk of resistance is recommended in patients with HCC. This topic review will summarize the epidemiology, pathogenesis, and clinical issues related to HBV reactivation in HCC patients, and will discuss proper management against HBV reactivation during anti-cancer therapy for HCC. 展开更多
关键词 Hepatitis B virus Virus activation Hepatic morbidity Hepatocellular carcinoma IMMUNOSUPPRESSION
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Copper complexes of anthrahydrazone bearing pyridyl side chain:Synthesis,crystal structure,anticancer activity,and DNA binding 被引量:1
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作者 HUANG Yao WU Yingshu +5 位作者 BAO Zhichun HUANG Yue TANG Shangfeng LIU Ruixue LIU Yancheng LIANG Hong 《无机化学学报》 北大核心 2025年第1期213-224,共12页
To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bisp... To expand the study on the structures and biological activities of the anthracyclines anticancer drugs and reduce their toxic side effects,the new anthraquinone derivatives,9‑pyridylanthrahydrazone(9‑PAH)and 9,10‑bispyridylanthrahydrazone(9,10‑PAH)were designed and synthesized.Utilizing 9‑PAH and 9,10‑PAH as promising anticancer ligands,their respective copper complexes,namely[Cu(L1)Cl_(2)]Cl(1)and{[Cu_(4)(μ_(2)‑Cl)_(3)Cl_(4)(9,10‑PAH)_(2)(DMSO)_(2)]Cl_(2)}_(n)(2),were subsequently synthesized,where the new ligand L1 is formed by coupling two 9‑PAH ligands in the coordination reaction.The chemical and crystal structures of 1 and 2 were elucidated by IR,MS,elemental analysis,and single‑crystal X‑ray diffraction.Complex 1 forms a mononuclear structure.L1 coordinates with Cu through its three N atoms,together with two Cl atoms,to form a five‑coordinated square pyramidal geometry.Complex 2 constitutes a polymeric structure,wherein each structural unit centrosymmetrically encompasses two five‑coordinated binuclear copper complexes(Cu1,Cu2)of 9,10‑PAH,with similar square pyramidal geometry.A chlorine atom(Cl_(2)),located at the symmetry center,bridges Cu1 and Cu1A to connect the two binuclear copper structures.Meanwhile,the two five‑coordinated Cu2 atoms symmetrically bridge the adjacent structural units via one coordinated Cl atom,respectively,thus forming a 1D chain‑like polymeric structure.In vitro anticancer activity assessments revealed that 1 and 2 showed significant cytotoxicity even higher than cisplatin.Specifically,the IC_(50)values of 2 against HeLa‑229 and SK‑OV‑3 cancer cell lines were determined to be(5.92±0.32)μmol·L^(-1)and(6.48±0.39)μmol·L^(-1),respectively.2 could also block the proliferation of HeLa‑229 cells in S phase and significantly induce cell apoptosis.In addition,fluorescence quenching competition experiments suggested that 2 might interact with DNA by an intercalative binding mode,offering insights into its underlying anticancer mechanism.CCDC:2388918,1;2388919,2. 展开更多
关键词 anthrahydrazone metal complex crystal structure anticancer activity cell apoptosis
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Research progress on the effects of sedentary behavior and physical activity on diabetes mellitus 被引量:1
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作者 CHEN Qi LI Chuan-Fen JING Wen 《生理学报》 北大核心 2025年第1期62-74,共13页
Diabetes mellitus(DM)has become one of the most serious and common chronic diseases around the world,leading to various complications and a reduction in life expectancy.Increased sedentary behavior(SB)and decreased ph... Diabetes mellitus(DM)has become one of the most serious and common chronic diseases around the world,leading to various complications and a reduction in life expectancy.Increased sedentary behavior(SB)and decreased physical activity(PA)are important contributors to the rising prevalence of DM.This article reviews the research progress on the pathogenesis of DM,the effects of SB and PA on the risk of DM,aiming to explore the influence of different PA intensities,amounts,frequencies,durations and types on the incidence of DM.Research has shown that blood glucose levels tend to increase with the prolongation of SB.Within a certain range,PA intensity and PA amount are negatively correlated with the risk of DM;Performing PA for more than 3 days per week maintains normal glucose tolerance and lower blood pressure;Engaging in 150–300 min of moderate intensity exercise or 75–150 min of high-intensity exercise per week reduces the risk of DM;PA during leisure time reduces the risk of DM,while PA during work increases the risk of DM;Both aerobic training and resistance training reduce the risk of DM,and the combination of the two training methods produces better benefits;Various types of exercises,such as cycling,soccer,aerobics,yoga,tai chi,all reduce the risk of DM.In summary,prolonged SB increases the risk of DM,while appropriate PA reduces the risk of DM.As the intensity,amount,and frequency of PA increase,the effect of reducing DM risk becomes more significant.Different exercise methods have different effects on reducing DM risk. 展开更多
关键词 sedentary behavior physical activity diabetes mellitus sports rehabilitation health promotion
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Passive activity enhances residual control ability in patients with complete spinal cord injury 被引量:2
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作者 Yanqing Xiao Mingming Gao +6 位作者 Zejia He Jia Zheng Hongming Bai Jia-Sheng Rao Guiyun Song Wei Song Xiaoguang Li 《Neural Regeneration Research》 SCIE CAS 2025年第8期2337-2347,共11页
Patients with complete spinal cord injury retain the potential for volitional muscle activity in muscles located below the spinal injury level.However,because of prolonged inactivity,initial attempts to activate these... Patients with complete spinal cord injury retain the potential for volitional muscle activity in muscles located below the spinal injury level.However,because of prolonged inactivity,initial attempts to activate these muscles may not effectively engage any of the remaining neurons in the descending pathway.A previous study unexpectedly found that a brief clinical round of passive activity significantly increased volitional muscle activation,as measured by surface electromyography.In this study,we further explored the effect of passive activity on surface electromyographic signals during volitional control tasks among individuals with complete spinal cord injury.Eleven patients with chronic complete thoracic spinal cord injury were recruited.Surface electromyography data from eight major leg muscles were acquired and compared before and after the passive activity protocol.The results indicated that the passive activity led to an increased number of activated volitional muscles and an increased frequency of activation.Although the cumulative root mean square of surface electromyography amplitude for volitional control of movement showed a slight increase after passive activity,the difference was not statistically significant.These findings suggest that brief passive activity may enhance the ability to initiate volitional muscle activity during surface electromyography tasks and underscore the potential of passive activity for improving residual motor control among patients with motor complete spinal cord injury. 展开更多
关键词 complete spinal cord injury cycle training epidural electrical stimulation motor training passive activity physiological state spinal cord circuit surface electromyography volitional control task
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In vitro antioxidant and anti-cancer activities and phytochemical analysis of Commelina benghalensis L. root extracts 被引量:1
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作者 Riffat Batool Ejaz Aziz +4 位作者 Javed Iqbal Hina Salahuddin Benny Kwong-Huat Tan Saira Tabassum Tariq Mahmood 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2020年第9期417-425,共9页
Objective:To explore antioxidant potential,anti-cancer activity,and phytochemicals of Commelina benghalensis L.Methods:The roots of Commelina benghalensis were extracted in different solvents(methanol,ethanol,benzene,... Objective:To explore antioxidant potential,anti-cancer activity,and phytochemicals of Commelina benghalensis L.Methods:The roots of Commelina benghalensis were extracted in different solvents(methanol,ethanol,benzene,chloroform,n-hexane)with a range of polarity.Antioxidant activity was evaluated by reducing power assay,DPPH radical scavenging activity and phosphomolybdenum method,cytotoxicity by MTT assay,apoptotic and cell cycle analysis by flow cytometry,migratory and invasive potential by wound scratch assay and invasion assay,respectively,functional groups analysis by FT-IR spectroscopy and phytochemicals by aluminum chloride colorimetric and FolinCiocalteu methods.Results:The extracts showed worthy antioxidant potential.The chloroform extract demonstrated the most significant cytotoxic effect on MDA-MB-231(breast cancer)cell line,induced apoptosis and reduced migratory and invasive potential of MDA-MB-231 cells.Methanol and ethanol extracts presented good yield of total phenolic and total flavonoid contents.The FTIR spectroscopic studies revealed different characteristic peak values with various functional compounds such as alkenes,alkanes,aliphatic amines,aromatics,alkyl halides,carboxylic acid,alcohols,ester,aldehydes and ketones.Conclusions:The results demonstrate the potential use of Commelina benghalensis as a good antioxidant with significant anticancer effect. 展开更多
关键词 Commelina benghalensis anti-cancer ANTIOXIDANT FT-IR
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Anti-hemolytic, antibacterial and anti-cancer activities of methanolic extracts from leaves and stems of Polygonum odoratum 被引量:1
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作者 Nittaya Chansiw Narisara Paradee +1 位作者 Kamonnaree Chotinantakul Somdet Srichairattanakool 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2018年第12期580-585,共6页
Objective: To investigate anti-hemolytic, antibacterial and anti-cancer activities of leaf and stem extracts from Polygonum odoratum. Methods: Leaves and stems of Polygonum odoratum were extracted using methanol and t... Objective: To investigate anti-hemolytic, antibacterial and anti-cancer activities of leaf and stem extracts from Polygonum odoratum. Methods: Leaves and stems of Polygonum odoratum were extracted using methanol and their anti-hemolytic activity was assessed using 2, 2′-Azobis(2-methylpropionamidine) dihydrochloride which is known to generate free radical damage on cell membranes of red blood cells. This damage, represented by hemolysis, was measured using spectrophotometry. Antibacterial activity was tested by using a broth microdilution method to find minimal inhibitory concentrations against eight bacterial strains. Anti-cancer activity of the extracts was evaluated against a human promyelocytic leukemic cell line(HL-60) by using MTT assay for cell viability and flow cytometry for apoptosis induction and cell cycle analysis. Results: Both leaf and stem extracts have anti-hemolytic activity. The results showed a significantly increased percentage of inhibition in a concentration-dependent manner. Interestingly, the leaf extract showed anti-hemolytic activity to a greater extent than the stem extract. Antibacterial activity of the extracts, as indicated by their minimal inhibitory concentration, using 12.5, 50, 25, 25 μg/mL, was measured against Staphylococcus epidermidis, Enterococcus faecium, Enterococcus faecalis and Staphylococcus aureus. The leaf extracts also exhibited anti-cancer activity, demonstrated by significantly decreased cell viability of human promyelocytic cells(HL-60), with an IC_(50) of(350.00±1.85) μg/mL for 48 h and(38.00±0.92) μg/mL for 72 h. Additionally, HL-60 became apoptotic and accumulated in G_1-phase after 48 hours of treatment. Conclusions: The extracts of Polygonum odoratum exhibit potential antihemolytic activity. They also have antibacterial activity by inhibiting growth of Gram-positive bacteria. The leaf extract shows anti-cancer activity against HL-60 to a greater extent than the stem extract, causing decreased viability, increased G_1-phase accumulation and apoptosis induction. 展开更多
关键词 Polygonum odoratum Anti-hemolysis Antibacterial agents anti-cancer agents
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New diterpenoids from Euphorbia wallichii with antioxidant activity 被引量:1
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作者 Yali Wang Juan Chen +4 位作者 Wenshuo Zheng Ziyan Gao Yuxin Gan Hua Li Lixia Chen 《Chinese Journal of Natural Medicines》 2025年第10期1248-1258,共11页
Thirteen novel diterpenoids,comprising seven tiglianes(walliglianes G−M,1−7),four rhamnofolanes(wallinofolanes A−D,8−11),and two daphnanes(wallaphnanes A and B,12 and 13),together with two known rhamnofolane diterpeno... Thirteen novel diterpenoids,comprising seven tiglianes(walliglianes G−M,1−7),four rhamnofolanes(wallinofolanes A−D,8−11),and two daphnanes(wallaphnanes A and B,12 and 13),together with two known rhamnofolane diterpenoids(euphorwallside H and euphorwallside I,14 and 15),were isolated and characterized from Euphorbia wallichii(E.wallichii).The chemical structures of these compounds were elucidated through nuclear magnetic resonance(NMR),mass spectrometry(MS),and quantum chemical calculations.Compounds 9 and 11 demonstrated protective effects against H2O2-induced BV-2 microglial cell damage.Molecular docking analyses indicated that compound 9 exhibited binding affinity to the anti-oxidant-related targets HMGCR,GSTP1,and SHBG. 展开更多
关键词 Euphorbia wallichii Tiglianes Rhamnofolanes Daphnanes Antioxidant activity
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