Dithiolane analogs of lignans inhibit interferon-gamma and lipopolysaccharide-induced nitric oxide production in macrophages.

Abstract:

AIM:To investigate the effect of a group of novel synthetic dithiolane analogs of lignans and a well characterized platelet-activating factor (PAF) receptor antagonist, L659,989 on PAF-receptor binding, IFN-gamma- and lipopolysaccharide (LPS)-induced NO production, and steady-state inducible nitric-oxide synthase (iNOS) mRNA expression. METHODS:PAF-receptor binding study was performed by displacement of 3H-PAF from rabbit platelet membrane; NO production was quantitated by measuring the NO oxidation product, nitrite, in conditioned culture medium; expression of iNOS mRNA was assessed by Northern blot analysis. RESULTS:The dithiolane analogs inhibited the production of NO, decreased iNOS mRNA expression and antagonized PAF-receptor binding. L659,989 had no effect on NO production and iNOS mRNA expression. Among the compounds tested, there was no simple correlation between their PAF-receptor antagonistic and iNOS inhibitory activities. CONCLUSION:The dithiolane analogs are a new synthetic chemical class of iNOS expression regulators with dual biologic functions: inhibiting iNOS induction and blocking PAF-receptor.

journal_name

Acta Pharmacol Sin

authors

Hussaini IM,Zhang YH,Lysiak JJ,Shen TY

subject

Has Abstract

pub_date

2000-10-01 00:00:00

pages

897-904

issue

10

eissn

1671-4083

issn

1745-7254

journal_volume

21

pub_type

杂志文章
  • Association of apolipoprotein E 4 polymorphism with cerebral infarction in Chinese Han population.

    abstract:AIM:To study the association between APOE polymorphisms and cerebral infarction through a case-control study among the Chinese Han population. METHODS:First-ever cerebral infarction patients (n=226) whose ages ranged from 40 to 60 years old were recruited from Department of Neurology, Zhongshan Hospital, Shanghai, and...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Jin ZQ,Fan YS,Ding J,Chen M,Fan W,Zhang GJ,Zhang BH,Yu SJ,Zhang YS,Ji WF,Zhang JG

    更新日期:2004-03-01 00:00:00

  • Effects of chiral 3-n-butylphthalide on apoptosis induced by transient focal cerebral ischemia in rats.

    abstract:AIM:To investigate the effects of 3-n-butylphthalide (NBP) on apoptosis induced by transient focal cerebral ischemia in rats, compare the action potency of s-(-)-, r-(+)- and (+/-)-NBP, and clarify the enantiomer that played a main role. METHODS:DNA fragmentation was detected by the terminal deoxynucleotidyl transfera...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Chang Q,Wang XL

    更新日期:2003-08-01 00:00:00

  • Microbial transformation of naproxen by Cunninghamella species.

    abstract:AIM:The metabolites of naproxen produced by Cunninghamella species were isolated and identified, and further to compare the similarities between microbial transformation and mammalian metabolism. METHODS:Naproxen was transformed by three strains of Cunninghammella species (Cunninghamella blakeslesna AS 3.153, Cunningh...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Zhong DF,Sun L,Liu L,Huang HH

    更新日期:2003-05-01 00:00:00

  • Ex vivo pulsed dendritic cell vaccination against cancer.

    abstract::As the most powerful antigen-presenting cell type, dendritic cells (DCs) can induce potent antigen-specific immune responses in vivo, hence becoming optimal cell population for vaccination purposes. DCs can be derived ex vivo in quantity and manipulated extensively to be endowed with adequate immune-stimulating capaci...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1038/s41401-020-0415-5

    authors: Gu YZ,Zhao X,Song XR

    更新日期:2020-07-01 00:00:00

  • Composite glycidyl methacrylated dextran (Dex-GMA)/gelatin nanoparticles for localized protein delivery.

    abstract:AIM:Localized delivery of growth factors has significant potential as a future therapeutic strategy in tissue engineering and regenerative medicine. A nanoparticle vehicle was created and evaluated in this study with the intent to deliver growth factors for periodontal regeneration. METHODS:Novel composite nanoparticl...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2009.15

    authors: Chen FM,Ma ZW,Dong GY,Wu ZF

    更新日期:2009-04-01 00:00:00

  • In vitro metabolic characteristics of cytochrome P-450 2A6 in Chinese liver microsomes.

    abstract:AIM:To investigate the metabolic characteristics of cytochrome P-450 C YP2A6 in human liver microsomes. METHODS:Cytochrome P-450 enzyme activities were measured by biochemical assays. Xenobiotics were employed to observe their effects on CYP2A6 in vitro. The kinetics of coumarin 7-hydroxylase was determined, and the c...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Xia XY,Peng RX,Yu JP,Wang H,Wang J

    更新日期:2002-05-01 00:00:00

  • A novel STAT3 inhibitor negatively modulates platelet activation and aggregation.

    abstract::The signal transducer and activator of transcription 3 (STAT3) plays a critical role in platelet functions. This study sought to understand the effects of the STAT3 inhibitor SC99 on platelet activation and aggregation. Immunoblotting assays were applied to measure the effects of SC99 on the STAT3 signaling pathway. A...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2016.155

    authors: Xu Z,Xu YJ,Hao YN,Ren LJ,Zhang ZB,Xu X,Cao BY,Dai KS,Zhu L,Fang Q,Kong Y,Mao XL

    更新日期:2017-05-01 00:00:00

  • Betulinic acid regulates generation of neuroinflammatory mediators responsible for tissue destruction in multiple sclerosis in vitro.

    abstract:AIM:To investigate the influences of betulinic acid (BA), a triterpenoid isolated from birch bark, on neuroinflammatory mediators involved in the pathogenesis of multiple sclerosis and experimental autoimmune encephalomyelitis in vitro. METHODS:Encephalitogenic T cells were prepared from draining lymph nodes and spina...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2012.181

    authors: Blaževski J,Petković F,Momčilović M,Paschke R,Kaluđerović GN,Mostarica Stojković M,Miljković D

    更新日期:2013-03-01 00:00:00

  • Polymorphisms of the KCNQ1 gene are associated with the therapeutic responses of sulfonylureas in Chinese patients with type 2 diabetes.

    abstract::KCNQ1 channel is a member of the voltage-gated potassium channel KQT-like subfamily. The KCNQ1 gene has recently been identified as a susceptibility locus for type 2 diabetes mellitus (T2DM). In the present study, we examined the effects of KCNQ1 variants on the therapeutic response to modified-release gliclazide (gli...

    journal_title:Acta pharmacologica Sinica

    pub_type: 临床试验,杂志文章

    doi:10.1038/aps.2016.103

    authors: Li Q,Tang TT,Jiang F,Zhang R,Chen M,Yin J,Bao YQ,Cheng X,Hu C,Jia WP

    更新日期:2017-01-01 00:00:00

  • The combination of baicalin and baicalein enhances apoptosis via the ERK/p38 MAPK pathway in human breast cancer cells.

    abstract:AIM:To examine whether the cell growth inhibitory effect of the combination of baicalin and baicalein is related to apoptosis. Moreover, to determine whether the expression of some apoptosis-related proteins is regulated by the ERK/p38 MAPK pathway. METHODS:Cell viability was measured using a 3-(4,5-dimethylthiazol-2-...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2009.166

    authors: Zhou QM,Wang S,Zhang H,Lu YY,Wang XF,Motoo Y,Su SB

    更新日期:2009-12-01 00:00:00

  • MicroRNA expression profile and functional analysis reveal their roles in contact inhibition and its disruption switch of rat vascular smooth muscle cells.

    abstract::Contact inhibition and its disruption of vascular smooth muscle cells (VSMCs) are important cellular events in vascular diseases. But the underlying molecular mechanisms are unclear. In this study we investigated the roles of microRNAs (miRNAs) in the contact inhibition and its disruption of VSMCs and the molecular me...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2018.6

    authors: Sun YY,Qin SS,Cheng YH,Wang CY,Liu XJ,Liu Y,Zhang XL,Zhang W,Zhan JX,Shao S,Bian WH,Luo BH,Lu DF,Yang J,Wang CH,Zhang CX

    更新日期:2018-05-01 00:00:00

  • Interaction between M-CSF and IL-10 on productions of IL-12 and IL-18 and expressions of CD14, CD23, and CD64 by human monocytes.

    abstract:AIM:To Study the interaction of macrophage colony-stimulating factor (M-CSF) and interleukin-10 (IL-10) in productions of IL-12 and IL-18 and expressions of CD14, CD23, and CD64 by human monocytes. METHODS:Purified adherent human monocytes were cultured with M-CSF or IL-10 alone, or with M-CSF+IL-10 and 2-3d later, th...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Ji XH,Yao T,Qin JC,Wang SK,Wang HJ,Yao K

    更新日期:2004-10-01 00:00:00

  • Hyperoside exerts anti-inflammatory and anti-arthritic effects in LPS-stimulated human fibroblast-like synoviocytes in vitro and in mice with collagen-induced arthritis.

    abstract:AIM:Hyperoside is a flavonol glycoside mainly found in plants of the genera Hypericum and Crataegus, which has shown anti-oxidant, anti-cancer and anti-inflammatory activities. In this study, we investigated the effects of hyperoside on human rheumatoid fibroblast-like synoviocytes (FLSs) in vitro and on mouse collagen...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2016.7

    authors: Jin XN,Yan EZ,Wang HM,Sui HJ,Liu Z,Gao W,Jin Y

    更新日期:2016-05-01 00:00:00

  • Application of EGFP-EGF fusions to explore mechanism of endocytosis of epidermal growth factor.

    abstract:AIM:To develop a simple method for monitoring protein localization of epidermal growth factor (EGF) in living cells. METHODS:Enhanced green fluorescent protein (EGFP) was used as an autofluorescent tag to label EGF ligands. SDS-PAGE and Western blot analysis were used to detect the expression of the EGFP-tagged EGF (E...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2007.00481.x

    authors: Jiang H,Zhang J,Shi BZ,Xu YH,Li ZH,Gu JR

    更新日期:2007-01-01 00:00:00

  • Neural circuits and nicotinic acetylcholine receptors mediate the cholinergic regulation of midbrain dopaminergic neurons and nicotine dependence.

    abstract::Midbrain dopaminergic (DA) neurons are governed by an endogenous cholinergic system, originated in the mesopontine nuclei. Nicotine hijacks nicotinic acetylcholine receptors (nAChRs) and interferes with physiological function of the cholinergic system. In this review, we describe the anatomical organization of the cho...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1038/s41401-019-0299-4

    authors: Xiao C,Zhou CY,Jiang JH,Yin C

    更新日期:2020-01-01 00:00:00

  • Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules.

    abstract::Human ether-a-go-go related gene (hERG) potassium (K(+)) channels play a critical role in cardiac action potential repolarization. Mutations that reduce hERG conductance or surface expression may cause congenital long QT syndrome (LQTS). However, the channels can be inhibited by structurally diverse small molecules, r...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章,评审

    doi:10.1038/aps.2011.70

    authors: Zhou PZ,Babcock J,Liu LQ,Li M,Gao ZB

    更新日期:2011-06-01 00:00:00

  • Potency of nondepolarizing muscle relaxants on muscle-type acetylcholine receptors in denervated mouse skeletal muscle.

    abstract:AIM:to investigate the changing resistance to nondepolarizing muscle relaxants (NDMRs) during the first month after denervation. METHODS:the denervated and innervated skeletal muscle cells were examined on days 1, 4, 7, 14, 21, and 28 after denervation. Individual denervated and innervated cells were prepared from the...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2010.163

    authors: WANG H,YANG B,HAN GW,LI ST

    更新日期:2010-12-01 00:00:00

  • Low initial trough concentration of rituximab is associated with unsatisfactory response of first-line R-CHOP treatment in patients with follicular lymphoma with grade 1/2.

    abstract::For follicular lymphoma (FL) with grade 1/2, the complete response (CR) rate of the first-line R-CHOP treatment was significantly low. In this study, we assessed the rationality of the administration of rituximab for FL patients with grade 1/2 based on concentration-response relationship analyses. Thus, we conducted a...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/s41401-020-0479-2

    authors: Liu S,Huang H,Chen RX,Wang Z,Guan YP,Peng C,Fang XJ,Chen ZJ,Guan SX,Zhu X,Ren QG,Yao YY,Huang HB,Huang M,Wang XD,Lin TY

    更新日期:2020-07-31 00:00:00

  • Autologous transplantation of bone marrow mononuclear cells improved heart function after myocardial infarction.

    abstract:AIM:To investigate whether autologous transplantation of adult stem cells could improve post-infarcted heart function. METHODS:Bone marrow mononuclear cells (MNCs) were isolated from adult rabbits' tibias after coronary ligation. These cells were exposed to 5-azacytidine 10 micromol/L for 24 h on the third day of cult...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Lin GS,Lü JJ,Jiang XJ,Li XY,Li GS

    更新日期:2004-07-01 00:00:00

  • Effect of cholecystokinin octapeptide on diacylglycerol-PKC signaling pathway in rat pulmonary interstitial macrophages stimulated by lipopolysaccharide.

    abstract:AIM:To investigate the effect of cholecystokinin octapeptide (CCK-8) on the diacylglycerol-protein kinase C (DAG-PKC) signaling pathway in rat pulmonary interstitial macrophages (PIM) stimulated by lipopolysaccaride (LPS). METHODS:The PIM from rat lung tissues were isolated using the collagenase digestion method combi...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2005.00217.x

    authors: Xu SJ,Gao WJ,Cong B,Ma CL,Li SJ,Ling YL,Gu ZY,Yao YX

    更新日期:2005-12-01 00:00:00

  • Protective effects of apocynin on "two-hit" injury induced by hemorrhagic shock and lipopolysaccharide.

    abstract:AIM:To evaluate the protective effects of apocynin on "two-hit" injury in rats. METHODS:"Two-hit" injury model of rat was induced by hemorrhagic shock (40 mmHg for 45 min) followed by iv administration of lipopolysaccharide (LPS, 150 microg/kg). Rats were randomized into seven groups: Sham, LPS, hemorrhage, hemorrhage...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Zhou R,Hu DY,Liu LM,Zhou XW

    更新日期:2002-11-01 00:00:00

  • Characterization of HJ-PI01 as a novel Pim-2 inhibitor that induces apoptosis and autophagic cell death in triple-negative human breast cancer.

    abstract:AIM:Pim-2 is a short-lived serine/threonine kinase, which plays a key role in metastasis of breast cancer through persistent activation of STAT3. Although the crystal structure of Pim-2 has been reported, but thus far no specific Pim-2-targeted compounds have been reported. In this study, we identified a novel Pim-2 in...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2016.60

    authors: Zhao YQ,Yin YQ,Liu J,Wang GH,Huang J,Zhu LJ,Wang JH

    更新日期:2016-09-01 00:00:00

  • An improved substrate cocktail for assessing direct inhibition and time-dependent inhibition of multiple cytochrome P450s.

    abstract:AIM:The substrate cocktail is frequently used to evaluate cytochrome P450 (CYP) enzyme-mediated drug interactions and potential interactions among the probe substrates. Here, we re-optimized the substrate cocktail method to increase the reliability and accuracy of screening for candidate compounds and expanded the meth...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2016.10

    authors: Chen ZH,Zhang SX,Long N,Lin LS,Chen T,Zhang FP,Lv XQ,Ye PZ,Li N,Zhang KZ

    更新日期:2016-05-01 00:00:00

  • Influence of intralipid on free propofol fraction assayed in human serum albumin solutions and human plasma.

    abstract:AIM:It is generally assumed that only unbound drugs can reach the site of action by diffusing across the membranes and exerting pharmacological effects by interacting with receptors. Recent research has shown that the percentage of free drugs may depend on the total drug concentration. The aim of the paper is to verify...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2006.00454.x

    authors: Kalitynski R,Dawidowicz AL,Poszytek J

    更新日期:2006-12-01 00:00:00

  • Pharmacokinetic characteristics of L-valyl-ara-C and its implication on the oral delivery of ara-C.

    abstract:AIM:To evaluate the pharmacokinetic characteristics of L-valyl-ara-C, a peptidomimetic prodrug of ara-C. METHODS:After the synthesis of L-valyl-ara-C, the in vitro stability of L-valyl-ara-C was examined in various biological media. Plasma pharmacokinetic profiles of ara-C and L-valyl-ara-C were also evaluated in rats...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2007.00474.x

    authors: Cheon EP,Han HK

    更新日期:2007-02-01 00:00:00

  • W2476 ameliorates β-cell dysfunction and exerts therapeutic effects in mouse models of diabetes via modulation of the thioredoxin-interacting protein signaling pathway.

    abstract::Recent evidence shows that high glucose levels recruit carbohydrate response element-binding protein, which binds the promoter of thioredoxin-interacting protein (txnip), thereby regulating its expression in β-cells. Overexpression of txnip not only induces β-cell apoptosis but also reduces insulin production. Thus, t...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1038/aps.2017.15

    authors: Li T,Lin GY,Zhong L,Zhou Y,Wang J,Zhu Y,Feng Y,Cai XQ,Liu Q,Nosjean O,Boutin JA,Renard P,Yang DH,Wang MW

    更新日期:2017-07-01 00:00:00

  • IL-12p40 is not required for islet allograft rejection.

    abstract:AIM:To investigate whether IL-12p40 plays a crucial role in regulating islet allograft rejection in a streptozotocin (STZ)-induced diabetes mouse model. METHODS:C57BL/6 and IL-12p40 gene knockout mice were selected as recipient mice, to which the diabetes was induced with a treatment of STZ (150-200 mg/kg) by a single...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:10.1111/j.1745-7254.2006.00341.x

    authors: Bi EG,Shi W,Zou J,Hao ZH,Li ZH,Cai D,Zhang HQ,Sun B

    更新日期:2006-08-01 00:00:00

  • Stimulation of mucin secretion from human bronchial epithelial cells by mast cell chymase.

    abstract:AIM:To investigate the effect of chymase on the mucin secretion from human bronchial epithelial cells. METHODS:Primarily-cultured human bronchial epithelial (PCHBE) cells and normal human bronchial epithelial (NHBE) cells were cultured with chymase or other stimulus in a mixture of bronchial epithelial growth medium (...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: He SH,Zheng J

    更新日期:2004-06-01 00:00:00

  • M2 muscarinic receptor of spinal cord mediated increase of nNOS expression in locus coeruleus during morphine withdrawal.

    abstract:AIM:To investigate the effects of different muscarinic receptor (M) subtypes in the spinal cord on the scores of naloxone-precipitated morphine-withdrawal symptoms and the changes of nNOS expression in locus coeruleus (LC). METHODS:nNOS immunohistochemistry, intrathecal injection (it), and antisense oligonucleotides (...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: Chou WB,Zeng YM,Duan SM,Zhou WH,Gu J,Yang GD

    更新日期:2002-08-01 00:00:00

  • Expression of dopamine D1 receptor in Sf9 insect cells and agonism of l-12-chloroscoulerine on recombinant D1 receptor.

    abstract:AIM:To express dopamine D1 receptor in baculovirus-Sf9 cell system, and to investigate the effects of l-12-chloroscoulerine (l-CSL) on the recombinant D1 receptor (D1R). METHODS:The recombinant baculovirus, Autographa californica nuclear polyhedrosis virus bearing D1R (AcNPV- D1R) was generated, and then was used to p...

    journal_title:Acta pharmacologica Sinica

    pub_type: 杂志文章

    doi:

    authors: He Y,Jin WQ,Shen QX,Chen XJ,Jin GZ

    更新日期:2003-03-01 00:00:00