1.Metabolites from the endophytic fungus Penicillium sp. FJ-1 of Ceriops tagal.
Pengfei JIN ; Wenjian ZUO ; Zhikai GUO ; Wenli MEI ; Haofu DAI
Acta Pharmaceutica Sinica 2013;48(11):1688-91
To investigate the chemical constituents of the endophytic fungus Penicillium sp. FJ-1 of Ceriops tagal, the chemical constituents were isolated by column chromatography on silica gel and Sephadex LH-20. Their structures were elucidated on the basis of spectroscopic analysis. Their antibacterial activity was tested by paper disco diffusion method. Two compounds were isolated and identified as 7-hydroxy-deoxytalaroflavone (1), and deoxytalaroflavone (2). Compound 1 is a new compound, and compounds 1 and 2 showed weak activity against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus.
2.Anti-proliferation of Angong Niuhuang pill on tumor cells via inducement of apoptosis and down-regulation of mitochondrial membrane potential
Zhikai DAI ; Jiaoe HUANG ; Jinyu JIANG ; Hailu ZHAO ; Yong LUO
Chinese Journal of Pharmacology and Toxicology 2012;26(3):269-275
OBJECTIVE To validate the anticancer effect of Angong Niuhuang pill (AGNH) and pinpoint associated molecular mechanisms using human cancer cells.METHODS Human MGC-803 gastric carcinoma and human BEL-7402 hepatocarcinoma cells were incubated with AGNH 9,30,90,300 and 900 mg·L-1 for 24,48and 72 h,respectively.Cell viability was detected with 3-(4,5-dimethylthiazol-2-yl) -5-( 3-carboxymethoxyphe-nyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay and colony formation assay.Apoptosis was measured with flow cytometry and Hoechst 33258/PI staining.Change in mitochondrial membrane potential (△qψ) was detected by spectrofluorophotometer.RESULTS AGNH inhibited MGC-803 cell proliferation ( for 48 h,r =0.996,P =0.002; for72 h,r=0.756,P=0.024 ) and BEL-7402 cells (for 48 h,r =0.732,P=0.030; for72 h,r=0.702,P =0.037) in a concentration-dependent manner,as showed by MTS assay.AGNH inhibited colony formation on MGC-803 cells (r =0.914,P =0.011 ) and BEL-7402 cells (r =0.871,P =0.024) in a concentration-dependent manner for 24 h.Hoechst 33258/PI staining and flow cytometry assay showed that AGNH 900 mg·L-1 for 24 h induced apoptosis of MGC-803 and BEL-7402 cells,and the apoptosis rate was 27.2% and 19.7%,respectively.Compared with normal control group,AGNH 900 mg·L-1 for 3 min decreased the mitochondrial membrane potential of MGC-803 and BEL-7402 cells to 15.9% and 15.0% of control group.CONCLUSION AGNH inhibits proliferation of human cancer cells.Apoptosis and depolarization of mitochondrial transmembrane potential are probablly its mechanism.
3.Neuroprotective effect of taurine against acute cortical neuron injury induced by oxygen-glucose deprivation
Can LUO ; Lianjun GUO ; Zhikai DAI ; Qin WU ; Jingshan SHI
Chinese Journal of Pharmacology and Toxicology 2006;20(1):1-6
AIM Taurine was reported neuroprotective under several ischemic models in vivo. In this study, the direct effect of taurine against oxygen-glucose deprivation (OGD) inducing acute neuronal injury and the underlying mechanisms in vitro were investigated. METHODSFour hours OGD was used to induce in vitro ischemic injury in rat cortical neurons. Taurine 5, 10 and 20 mmol·L-1 was added 20 h before and during 4 h OGD period respectively. Mortality rate of neuron was assayed by MTT and flow cytometry methods. Level of neuronal [Ca2+]i was detected by Fura 2/AM loading. Amino acid concentrations in culture media were measured by high performance liquid chromatography. RESULTS Under OGD conditions, neuronal death was markedly increased, and the levels of neuronal [Ca2+]i and extracellular glutamate level were enhanced obviously. Taurine pretreatment obviously decreased the percentage of neuronal death induced by OGD. In addition, abnormal elevation of neuronal [Ca2+]i and extracellular glutamate level induced by OGD both were markedly repressed by taurine. CONCLUSION Taurine can alleviate rat cortical neuron injury induced by OGD, the mechanisms were likely due to repressing calcium overload and inhibiting excessive release or leakage of glutamate under such conditions.
4.Calcineurin signal transduction pathway involves in cardiomyocyte hypertrophy induced by prostaglandin F_(2?)
Qingsong JIANG ; Xienan HUANG ; Qixin ZHOU ; Guizhong YANG ; Zhikai DAI ; Qin WU ; Jingshan SHI
Chinese Journal of Pathophysiology 2000;0(07):-
AIM:To study the role of prostaglandin F2?(PGF2?) in cardiac hypertrophy and its relation with calcineurin(CaN) signal transduction pathway in vitro.METHODS:The cultured neonatal rat cardiomyocyte was used to observe the hypertrophic effect of PGF2?,and the hypertrophic response was assayed by measuring the cell diameter,protein content and atrial natriuretic factor(ANF) mRNA expression.For mechanism studies,the intracellular free calcium concentration([Ca2+]i) in cultured cardiomyocytes was measured by using Fura-2/AM as a fluorescent indicator.ANF and CaN mRNA expressions,and the expressions of CaN and its downstream effectors,NFAT3 and GATA4 proteins were assayed by RT-PCR and Western blotting,respectively.RESULTS:In cultured cardiomyocytes,PGF2? induced profound hypertrophic morphology change and the significant increase in cell diameter,and protein content in a concentration-dependent manner compared with those in vehicle control(P
5.XP-16, a new xanthono-pyridine derivative, induces apoptosis in human lung carcinoma A549 cells
Zhikai DAI ; Chengfang YANG ; Yifei CHEN ; Junnan JIANG ; Guanhua CHE ; Jiangke QIN
Chinese Pharmacological Bulletin 2014;(6):838-842
Aim To investigate the anticancer effect of a new xanthono-pyridine derivative N, N '-( 7-oxo-7H-chromeno[3,2-h] quinoline-5,9-diyl)-bis(2-( pyrroli-din-1-yl)acetamide) (XP-16) on human lung carcino-ma cell line A549 and the potential mechanism. Meth-ods Antiproliferative effect of XP-16 on A549 cells was evaluated by MTT assay, morphological examina-tion and colonial assay. Apoptosis detection was car-ried out using Hoechst 33258 and PI double-dyeing method. Intracellular Ca2+ concentration ( [ Ca2+] i ) and mitochondria membrane potential were detected by fluorospectrophotometer. A549 cells treated with XP-16 were collected for Bad and metallothionein 1 A ( MT-1 A ) transcript analysis by real-time reverse tran-scriptase-polymerase chain reaction ( qRT-PCR) . Re-sults XP-16 inhibited A549 cell proliferation in dose-and time-dependent manner. Typical apoptotic mor-
phology such as chromatin aggregation and nuclear fragmentation was observed in A549 cells treated with XP-16 for 24 h, and the apoptosis was showed in a dose-dependent manner. After treated with XP-16, [ Ca2+] i and mitochondria membrane potential of A549 cells were decreased, and relative mRNA level of Bad and MT-1A was up-regulated. Conclusions XP-16 has anticancer effect on A549 cells through apoptosis, which might be associated with decreasing intracellular Ca2+ concentration and mitochondria membrane poten-tial. Up-regulation of MT-1A expression might be the result of decreased [ Ca2+] i .
6.Apoptosis inducing effect of tanshinone II(A) on human nasopharyngeal carcinoma CNE cells.
Zhikai DAI ; Dalin HUANG ; Jingshan SHI ; Limei YU ; Qin WU ; Qing XU
China Journal of Chinese Materia Medica 2011;36(15):2129-2133
OBJECTIVETo investigate anticancer effect and potential mechanism of tanshinone II(A) (Tan II(A)) on human nasopharyngeal carcinoma cell line CNE cells.
METHODAntiproliferative effect of Tan II(A) on CNE cells was evaluated by morphological examination, cell growth curves, colonial assay and MTT assay. Apoptosis detection was carried out using Hoechest 33258 and PI double-dyeing method. Intracellular Ca2+ concentration and mitochondria membrane potential were detected by fluorospectrophotometer. Bad and MT-1A transcript analysis in CNE cells was analyzed by real-time reverse transcriptase-polymerase chain reaction (RT-PCR).
RESULTTan II(A) could inhibit CNE cells proliferation in dose- and time-dependent manner. 50% inhibiting concentration of Tan II(A) on CNE cells in 24, 48, 72 h was 45.7, 24.8, 3.3 mg x L(-2), respectively. Typical apoptotic morphology such as chromatin aggregation was observed in CNE cells with Tan II(A) treated for 24 h, and the apoptotic inducing effect was in a dose-dependent manner. After treated with Tan II(A), intracellular Ca2+ concentration of CNE cells was increased, mitochondria membrane potential of the cells was decreased, relative mRNA level of Bad and MT-1A was up-regulated.
CONCLUSIONTan II(A) had anticancer effect on CNE cells through apoptosis via calcineurin-dependent pathway and MT-1A downregulation.
Antineoplastic Agents, Phytogenic ; pharmacology ; Apoptosis ; drug effects ; Calcium ; metabolism ; Carcinoma ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Diterpenes, Abietane ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Gene Expression Regulation, Neoplastic ; drug effects ; Humans ; Membrane Potential, Mitochondrial ; drug effects ; Metallothionein ; genetics ; Nasopharyngeal Neoplasms ; genetics ; metabolism ; pathology ; Signal Transduction ; drug effects ; bcl-Associated Death Protein ; genetics
7.HIV-associated dyslipidemia: pathogenesis and its management.
Zhikai WAN ; Bohao DAI ; Xueling ZHU ; Ying HUANG ; Biao ZHU
Chinese Medical Journal 2023;136(22):2732-2734
8.Clinical characteristics and prognosis of AIDS related lymphoma: An analysis of 84 cases
Jiangjin HUI ; Zhikai WAN ; Guanjing LANG ; Bohao DAI ; Biao ZHU
Chinese Journal of Clinical Infectious Diseases 2022;15(6):448-453
Objective:To analyze the clinical characteristics and prognosis of patients with AIDS-related lymphoma (ARL).Methods:The clinical data of 84 patients with ARL admitted in the First Affiliated Hospital Zhejiang University School of Medicine from March 2013 to October 2021 were retrospectively reviewed, and the influencing factors for prognosis of patients were analyzed by Cox proportional risk regression model.Results:Non-Hodgkin’s lymphoma accounted for 95.2% (80/84) of all cases; 52.3% (44/84) of the patients presented with B symptoms of lymphoma such as fever, night sweats, and weight loss, and 84.5% (71/84) of them were classified as stage Ⅲ~Ⅳ by Ann Arbor staging; 58.0% (47/81) patients had CD4 + T cell count ≤200/μL at baseline; 30 (35.7%) patients had pulmonary infection, 11 (13.1%) patients had digestive tract infection, and 21.4% (18/84) patients had sepsis. The 1-year survival rate of 84 patients was 70.2% (59/84). Multivariate Cox survival analysis showed that International prognostic index (IPI) score >3 ( HR=5.094, 95% CI 1.877-13.824, P=0.001) was an independent risk factors and rituximab treatment ( HR=0.354, 95% CI 0.152-0.823, P=0.016) was an independent protective factor for the prognosis of patients with ARL. Conclusions:The clinical manifestations of ARL are diverse, and it is often diagnosed in the late stage of the disease with adverse prognosis. IPI score and Rituximab treatment are key prognostic factors in patients with ARL.