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Role of Apolipoprotein A-I in Protecting against Endotoxin Toxicity

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Acta Biochimica et Biophysica Sinica 2004年第6期36卷 419-424页

作者： Juan MA, Xue-Ling LIAO, Bin LOU, and Man-Ping WU* department of Biochemistry, School of pharmacy, Fudan University, Shanghai 200032, China department of Biochemistry School of Pharmacy Fudan UniversityShanghai 200032 China

High density lipoprotein (HDL) binds lipopolysaccharide (LPS or endotoxin) and neutralizes its toxicity. We investigated the function of Apolipoprotein A-I (ApoA-I), a major apolipoprotein in HDL, in this process. Mouse macrophages were incubated with LPS, LPS+ApoA-I, LPS+ApoA-I+LFF (lipoprotein-free plasma fraction d>1.210 g/ml), LPS+HDL, LPS+HDL+LFF, respectively. MTT method was used to detect the mortality of L-929 cells which were attacked by the release-out cytokines in LPS-activated macrophages. It was found that ApoA-I significantly decreased L-929 cells mortality caused by LPS treatment (LPS vs. LPS+ApoA-I, P<0.05) and this effect became even more significant when LFF was utilized (LPS vs. LPS+ApoA-I+LFF, P<0.01; LPS vs. LPS+HDL+LFF, P<0.01). There was no significant difference between LPS+ApoA-I+LFF and LPS+HDL+LFF treatment, indicating that ApoA-I was the main factor. We also investigated in vivo effects ofApoA-I on mouse mortality rate and survival time after LPS administration. We found that the mortality in LPS+ApoA-I group (20%) and in LPS+ApoA-I+LFF group (10%) was signifi- cantly lower than that in LPS group (80%) (P<0.05, P<0.01, respectively); the survival time was (43.20 ± 10.13) h in LPS+ApoA-I group and (46.80 ± 3.79) h in LPS+ApoA-I+LFF group, which were significantly longer than that in LPS group (16.25 ± 17.28) h (P<0.01). We also carried out in vitro binding study to investigate the binding capacity of ApoA-I and ApoA-I+LFF to fluorescence labeled LPS (FITC-LPS). It was shown that both ApoA-I and ApoA-I+LFF could bind with FITC-LPS, however, the binding capacity of ApoA-I+LFF to FITC-LPS (64.47 ± 8.06) was significantly higher than that of ApoA-I alone (24.35 ± 3.70) (P<0.01). The results suggest that: (1) ApoA-I has the ability to bind with and protect against LPS; (2) LFF enhances the effect of ApoA-I; (3) ApoA-I is the major contributor for HDL anti-endotoxin function.

关键词： Apolipoprotein-I lipopolysaccharide (LPS) macrophages FITC-lipopolysaccharide (FITC-LPS) L-929 cells

Synthesis and Anticonvulsant Activity of γ-Aminobutyric Acid Derivatives

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Chinese Chemical Letters 1998年第4期9卷 369-371页

作者： Mu YUAN Yu Guo ZHONG Qi Jie PANG(department of pharmacy, Guiyang Medical College, Gujyang 550004 School of pharmacy, West China University of Medical Sciences, Chengdu 610044) Guiyang Med Coll Dept Pharm Gujyang 550004 Peoples R China W China Univ Med Sci Sch Pharm Chengdu 610044 Peoples R China

Under physiological conditions, γ-aminobutyric acid poorly crosses the blood-brain barrier. It is likely that a non-toxic derivative of γ-aminobutyric acid which enters the brain easily will have useful anticonvulsant activity. 16 derivatives of γ-aminobutyric acid with an imine link to a lipophilic carrier were prepared and tested for anticonvulsant activity; six compounds show anticonvulsant activity.

关键词： γ-aminobutyric acid synthesis anticonvulsant activity

SPECTROFLUOROMETRIC DETERMINATION OF URINARY TOTAL ESTROGENS

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中华医学杂志(英文版) 1981年第3期94卷 195-198页

作者： Research Institute of Obstetrics and Gynecology and Division of Analytical Chemistry, department of pharmacy, Shanghai First Medical College, Shanghai Research Institute of Obstetrics and Gynecology and Division of Analytical Chemistry Department of Pharmacy Shanghai First Medical College Shanghai

A rapid, reliable, simple and practical fluorometric method for determining total urine estrogens is described. Three different methods of determining fluorescence reaction were compared and it was found that the one with 65% H2SO4as reaction reagent produces the most stable and intensive fluorescence. The experimental conditions such as the time of processing, temperature, solvent etc. were *** our results a routine procedure was designed, including the processes of hydrolysis, extraction, solvent partition and fluorescent reaction. The procedure is greatly simplified and 20-30 samples can be done *** efficiency of estrogen recovery by this method is 87.9-113.73%, coefficient of variation is 4.56-10.5% and sensitivity is 1μg/24 hr urine. These satisfy the criteria for clinical analysis. It is recommended that the fluorometrie method for estrogen determination can be used for evaluation of ovarian activity instead of the tedious spectrophotometric method.

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Sodium dimercaptopropane sulfonate as antidote against non-metallic pesticides

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Acta Pharmacologica Sinica 2004年第4期25卷 136-146页

作者： Zhi-kang CHEN, Zhong-qiu LU1,2 department of Pharmacology, School of pharmacy, Wenzhou Medical College, Wenzhou 325035 2Emergency department, TheFirst Affiliated Hospital of Wenzhou Medical College, Wenzhou 325000, China department of Pharmacology School of Pharmacy Wenzhou Medical College Emergency department The First Affiliated Hospital of Wenzhou Medical College China

With the advent of World War II, dimercaptol was first developed in Englandas an effective antidote against arsenical agents. In 1950''s, scientists from the Soviet Uniondeveloped a water-soluble compound, sodium dimercaptopropane sulfonate (Na-DMPS) named as Unithiol(or Unitiol), which was able to chelate heavy metals and metalloids. Unithiol was collected in thePharmacopeia of the Soviet Union. After a lot of efforts of scientists from several countries, thisdrug has been widely used in the treatment of the poisoning of heavy metals and metalloids, as awell-known specific antidote. Considering the importance of sulfhydryl groups in human body, wefirst initiated the possibility of sulfhydryl compounds as antidotes against some non-metaltoxicants. In 1970''s, they screened many sulfhydryl compounds as antidotes against acute poisoningof nereistoxin insecticides (NTXI), and found that dithiol compounds were much better than monothiolcompounds in the treatment for NTXI poisoning. Na-DMPS and sodium dimercapto-succinate (Na-DMS)were among the best antidotes (Fig 1). The accumulation of experimental studies and clinical trialshas confirmed that they were specific effective antidotes against NTXI. In 1990''s, Na-DMPS was firstapplied to treat the acute poisoning of chlordimeform (CDM) an organoni-trogen insecticide, andbactericide 402, an organosulfur pesticide, and tetramine, a rodenticide. Through thoroughpharmacological and toxicological studies of these non-metallic pesicides, the application ofNa-DMPS as an antidote has been widened, and the development of antidotes against pesticides hasbeen prospected. The application of Na-DMPS as an antidote against non-metallic pesticides is asuccessful example, which shows important theoretical basis and practical value.

关键词： sodium dimercaptopropane sulfonate antidotes pesticides nereistoxin insecticides chlordimeform bactericide 402 tetramine poisoning

WA, a new Antifungal Antibiotic from a Soil Fungus Strain 38

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Chinese Chemical Letters 1998年第6期9卷 539-540页

作者： Jun YANG Xiu Lan QI Wen LI Gang SHAO Xin Sheng YAO S. KITANAKA(department of Natural Medicinal Chemistry, Shenyang Pharmaceutical University, Shenyang 110015)(department of Pharmacognosy, College of pharmacy, Nihon University, Japan) Shenyang Pharmaceut Univ Dept Natl Med Chem Shenyang 110015 Peoples R China Nihon Univ Dept Pharmacognosy Coll Pharm Tokyo 102 Japan

A new antifungal antibiotics, WA, was isolated from the secondary metabolites of soil fungus strain 38, and its structure was elucidated as 4-(2-hydroxy-3-butynoxy)benzoic acid by means of the spectral data (H-1-and C... 详细信息

关键词： WA structure elucidation activity against P-oryzae

Novel Antifungal Antibiotic, WB Produced by the Fungus Strain 38

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Chinese Chemical Letters 1998年第9期9卷 833-834页

作者： Jun YANG Xiu Lan QI Gang SHAO Yue Hu PEI Xin Sheng YAO (department of Natural Medicinal Chemistry, Shenyang Pharmaceutical University Shenyang 110015)Susumu KITANAKA (department of Pharmacognosy, College of pharmacy, Nihon University, Japan) Shenyang Pharmaceut Univ Dept Nat Med Chem Shenyang 110015 Peoples R China Nihon Univ Coll Pharm Dept Pharmacognosy Tokyo 102 Japan

WE, a new antifungal antibiotic, was isolated from the soil fungus strain 38 against Pyricularia oryzae, and its structure was elucidated as 2-[(E)-3,5-dimethyl-3,4-dihydroxy-1-eptylenyl]-4-chloro-5-oxo-6-methyl-6,7-d... 详细信息

关键词： antifungal antibiotic WB structure elucidation

Diterpenoid Alkaloids from Delphinium Tongolense

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Chinese Chemical Letters 1997年第9期8卷 791-792页

作者： Lan HE Xuan PAN Bo Gang LI Yao Zu CHEN(The Chemistry department of Zhejian Univ., Hangzhou 310027 The department of pharmacy of Lanzhou Medical College, Lanzhou 730000 The Chengdu Institute of Biology, Academia Sinica, Chengdu 610041) ZHEJIANG UNIV DEPT CHEM HANGZHOU 310027 PEOPLES R CHINA LANZHOU MED COLL DEPT PHARM LANZHOU 730000 PEOPLES R CHINA ACAD SINICA CHENGDU INST BIOL CHENGDU 610041 PEOPLES R CHINA

The phytochemical investigation of Delphinium tongolense Franch. yielded two new diterpenoid alkaloids tongolenine C and tongolenine D. Their structures were elucidated by spectroscopical methods.

关键词： DEPT ppm Diterpenoid Alkaloids from Delphinium Tongolense

Antioxidant activities of α-methyl-4-(3-oxo-2H-1,2-benzoisoselenazol-2-yl)benzeneacetic acid in vitro

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中国药理学与毒理学杂志 1998年第1期 68-69页

作者： ZENG HuaWu, JIANG YuanYing1, CAI DingGuo, TAO ZhiHua, LONG Kun1(The pharmacy Center of Navy, The Navy 411 Hospital, Shanghai 200081 1 department of Pharmacology,College of pharmacy, The Second Military Medical University, Shangh

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关键词： αmethyl4(3oxo2H1,2benzoisoselenazol2yl) benzeneacetic acid selenoorganic compound lipid peroxides

Effect of heparin on apoptosis in human nasopharyngeal carcinoma CNE2 cells

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Cell Research 2001年第4期11卷 311-315页

作者： LI HONG LIANG , KAI HE YE , HAI WEI ZHANG , YING RU LUO , XIAN DA REN, AI HUA XIONG, RUI SITU department of Pharmacology ,pharmacy College, department of Pathology Medical College, Jinan University, Guangzhou 510632, China department of Pharmacology Pharmacy College Jinan University Guangzhou China.

In order to study the mechanism of the effect of heparin on apoptosis in carcinoma cells, the nasopha- ryngeal carcinoma cell line CNE2 was used to identify the effect of heparin on apoptosis associated with the expression of c-myc,bax, bcl-2 proteins by use of Hoechst 33258 staining, terminal deoxynucleotidyl transferasemediated dUTP nick-end labeling (TUNEL), agarose gel electrophoresis, and flow cytometry, as well as Western blot analysis. The results showed that heparin induced apoptosis of cNE2 cens including the morphologic changes such as reduction in the volume, and the nuclear chromatin condensation, as well as the 'ladder pattern' revealed by agarose gel electrophoresis of DNA in a concentration-dependent manner. The number of TUNEL-positive cells was dramatically increased to 33.6+1.2% from 2.8+0.3% by treat- ment with heparin in different concentrations (10~40 kU/L). The apoptotic index was increased to 32.5% from 3.5% by detecting SubG1 peaks on flow cytometry. Western blot analysis showed that levels of bcl-2, bax and c-myc were significantly overexpressed by treatment with the increase of heparin concentrations. These results suggest that heparin induces apoptosis of CNE2 cells, which may be regulated by differential expression of apoptosis-related genes.

关键词： Heparin agarose gel electrophoresis flow cytometry apoptosis protein kinase C(PKC)