2.Effect of Dexamethasone on Excitatory Amino Acid and Monoamine Neurotransmitter in Cerebral Tissue of Neonatal Rats with Hypoxia-Ischemia
bao-hong, WANG ; yu, JIN ; cai-xia, AN ; xin-hua, YE
Journal of Applied Clinical Pediatrics 1994;0(04):-
Objective To explore the value of dexamethasone(DEX) for neuronal cell injury and death by observing the effect of DEX on excitatory amino acid(EAA) and monoamine neurotransmitter in cerebral tissue of neonatal rat with hypoxia-ischemia.Methods Hypoxic-ischemic neonatal rat models were established,the levels of EAA and monoamine neurotransmitter in cerebral tissue were analyzed by using capillary electrophoresis and fluorospectrophotometry method.The rats were divided into 4 groups: small dose DEX group pre-treated with DEX(0.5 mg/kg) prior to hypoxia-ischemia,large dose DEX group pre-treated with DEX(10 mg/kg) prior to hypoxia-ischemia,HIE group and shamful operation group.Results The levels of EAA and monoamine neurotransmitter contents in HIE group were significantly higher than those in shamful operation group(P0.05).EAA contents of large dose DEX group greatly decreased compared with HIE group (P
4.Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles.
Zhizhong ZUO ; Hang ZHONG ; Ting CAI ; Yu BAO ; Zhiqiang LIU ; Dan LIU ; Linxiang ZHAO
Acta Pharmaceutica Sinica 2015;50(7):868-74
Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
5.A Research on the Anti-tumor Effects of Acid-Soluble Polysaccharides from Gloeostereum incamatum in H22 Tumor Bearing Mice
Hong WANG ; Yan ZHAO ; Enbo CAI ; Tolgor BAU ; Wei LI ; Yu LI ; Haiying BAO
World Science and Technology-Modernization of Traditional Chinese Medicine 2017;19(1):142-148
This study aimed at exploring the inhibitory effect behind its mechanism on acid-soluble polysaccharides from G.incamatum in transplanted H22 tumor mice.Different indices,including tumor inhibitory rate,organ index of liver,thymus and spleen,IL-2,IFN-γ and TNF-α were detected for the evaluation of anti-tumor effects and the mechanism.Furthermore,HE staining and TUNEL assay were adopted to investigate the pathological changes of tumor tissue and cell apoptosis,respectively.As a result,the three dose groups of acidsoluble polysaccharides of G.incamatum successfully inhibited the proliferation of tumor cells,while organ indexes of spleen and thymus were improved and serum IL-2,IFN-γ and TNF-α increased.H&E staining and TUNEL assay showed the polysaccharides induced cell apoptosis,playing a significant role in the inhibition of tumor growth.In conclusion,acid-soluble polysaccharides of G.incamatum possessed significant anti-tumor effects,behind which the mechanism could be related to the regulation of immune regulation,cell apoptosis,and the protection of liver function.
6.Expression of wild type and variant estrogen receptors in human hepatocellular carcinoma
Bao-Cai XING ; Jia-Hong WANG ; Yi WANG ; Chun-Yi HAO ; Xin-Fu HUANG ; Yu WANG ;
Journal of Peking University(Health Sciences) 2003;0(06):-
Objective:To investigate the expression of wild type estrogen receptor(wER)and the ex-on-5 deleted ER(variant ER,vER)in human hepatocellular carcinoma(HCC)samples,and thereafteranalyze the possibility of HCC treatment by endocrine therapy.Methods:The mRNA expressions of wERand vER were analysed from 28 cases of HCC by RT-PCR.The expression of ER at the protein level wasdetected by immunohistochemistry(IHC).Results:IHC results showed that 39.3% of the HCC speci-mens expressed ER.The mRNA of wER was detected in 89.3%(25/28)of the HCC specimens whilethat of vER was detected in 96.4%(27/28).Twenty four out of 28 HCC cases(85.7%)expressedboth wER and vER.One out of 28 patients(3.5%)expressed only wER whereas 3 patients out of 28(10.7%)expressed vER only.Conclusion:Ninety six percent(27/28)of the HCC patients expressedvER,which suggests that the expression of vER is an important event in the development of HCC.
7.Dynamic changes of IL-1β in rat myocardium during hypoxia/ reoxygenation transition.
Jin-bo HE ; Cai-ying BAO ; Yu-zhu YE ; Zi-yin LUO ; Lei YING ; Wan-tie WANG
Chinese Journal of Applied Physiology 2015;31(1):27-30
OBJECTIVETo investigate the expression profile of interleuki-1β (IL-1β) in rat myocardium at different time points during hypoxia/reoxygenation(H/R)transition.
METHODSThe isolated Langendorff perfused rat heart model was established.Forty SD rats were randomly divided into sham group (A group) and hypoxia/reoxygenation group (H/R group). The H/R group rats were subdivided into H/R 0.5 h group(B group), H/R 1 h group(C group), H/R 2 h group(D group)according to reoxygenation time. The left ventricular development pressure(LVDP), maximal rates of increase/decrease of the left ventricular pressure(±dp/dtmax) were continuously recorded. The concentration of interleukin-1β(IL-lβ) and creatine kinase-MB (CK-MB) in myocardium was measured by ELISA. The mRNA expression of IL-lβ in myocardium was determined by RT-PCR. Microstructure of myocardium was observed under light microscopy.
RESULTSThe value of LVDP and ±dp/dtmax in hypoxia/reoxygenation group rat were significantly lower than that in sham group(P < 0.05). The expression of IL-lβ and CK-MB at protein level and the expression of IL-1β at mRNA level in hypoxia /reoxygenation group were higher than that in sham group(P < 0. 05). There were significant differences of the above parameters among H/R 0.5 h, 1 h, 2 h group(P <0.05). The concentration of IL-1β and CK-MB, the mRNA expression of IL-1β were higher in H/R 2 h group than that of other groups(P < 0.05).
CONCLUSIONThe high expression of IL-Iβ in myocardium after myocardial hypoxia /reoxygenation in rats might lead to. ischemia/reperfusion injury.
Animals ; Creatine Kinase, MB Form ; metabolism ; Disease Models, Animal ; Hypoxia ; metabolism ; pathology ; Interleukin-1beta ; metabolism ; Myocardial Ischemia ; metabolism ; Myocardium ; metabolism ; pathology ; Rats ; Rats, Sprague-Dawley
8.Effect and mechanism of total flavonoids of bugloss on rats with myocardial ischemia and reperfusion injury.
Xiao-Na XU ; Zi-Ran NIU ; Shou-Bao WANG ; Yu-Cai CHEN ; Li GAO ; Lian-Hu FANG ; Guan-Hua DU
Acta Pharmaceutica Sinica 2014;49(6):875-881
This study is to investigate the effect of total flavonoids of Uygur medicine bugloss (BTF) on rats with myocardial ischemia/reperfusion injury, and to explore the mechanisms by which it acts. Left anterior descending (LAD) coronary artery in rats was occluded for 30 min followed by 4 h reperfusion. Meanwhile, BTF dissolved in saline was administered intraperitoneally at dosage of 10, 30 and 50 mg x kg(-1). Electrocardiograph, infarction index, serum myocardial enzymes and heart function were determined to evaluate the effect of BTF. Some other observations were carried out to explore whether inhibiting inflammation and apoptosis is involved in the mechanisms underlying BTF. Our results showed that in ischemia/reperfusion injured rats BTF could dose-dependently reduce myocardial infarction index and myocardial enzyme leakage, and enhance heart function, indicating that it possesses significant cardio protection. ELISA analysis showed that BTF could decrease the content of myocardial inflammatory cytokines such as IL-1beta, IL-6 and TNF-alpha. Western-blotting confirmed that BTF could increase the expression of anti-apoptotic protein Bcl-2 and reduce the expression of proapoptosis protein Bax. Further more, the phosphorylation level of PI3K and Akt was upregulated by BTF treatment. BTF can protect rat against myocardial ischemia/reperfusion injury. Anti-inflammation and inhibition of apoptosis through upregulating PI3K/Akt signal pathway may contribute to the protective effect of BTF.
Animals
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Apoptosis
;
Apoptosis Regulatory Proteins
;
Boraginaceae
;
chemistry
;
Flavonoids
;
pharmacology
;
Heart
;
Interleukin-6
;
Myocardial Infarction
;
Myocardial Reperfusion Injury
;
drug therapy
;
Myocardium
;
Phosphatidylinositol 3-Kinases
;
Phosphorylation
;
Protective Agents
;
Proto-Oncogene Proteins c-akt
;
Rats
;
Signal Transduction
;
Tumor Necrosis Factor-alpha
;
bcl-2-Associated X Protein
9.Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles.
Zhi-zhong ZUO ; Hang ZHONG ; Ting CAI ; Yu BAO ; Zhi-qiang LIU ; Dan LIU ; Lin-xiang ZHAO
Acta Pharmaceutica Sinica 2015;50(7):868-874
Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
Antineoplastic Agents
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chemical synthesis
;
chemistry
;
Artemisinins
;
chemical synthesis
;
chemistry
;
Breast Neoplasms
;
pathology
;
Cell Proliferation
;
Doxorubicin
;
Drug Design
;
HL-60 Cells
;
drug effects
;
Humans
;
MCF-7 Cells
;
drug effects
10.Advances in studies of renal adverse reactions of Leonurus heterophyllus.
Jie YU ; Jing WANG ; Ronghua ZHAO ; Zhaorigetu BAO ; Shaoqing CAI
China Journal of Chinese Materia Medica 2010;35(9):1213-1216
Motherwort (Herb of Leonurus heterophyllus) was a traditional Chinese medicine used for the treatment of various kinds of gynaecological diseases, which was considered as non-toxic medicine since ancient times. However, adverse effects such as kidney damage, uterus damage, allergy and diarrhea were frequently reported recently. This paper reviews the possible target site, toxic dosage, chemical substance and other related factors of these kidney damage caused by motherwort from both the clinic and animal experiment view.
Animals
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Drugs, Chinese Herbal
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adverse effects
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Humans
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Kidney
;
drug effects
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pathology
;
Leonurus
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chemistry