Role of enzymatic activity in the antiplatelet effects of a phospholipase A2 from Ophiophagus hannah snake venom.

Abstract:

:A phospholipase A2 (OHV A-PLA2) from the venom of Ophiophagus hannah (King cobra) is an acidic protein exhibiting antiplatelet activity. In in vitro tests, OHV APLA2 showed a marked inhibitory effect on platelet aggregation induced by ADP, collagen and arachidonic acid in both human whole blood and platelet-rich plasma in a dose-dependent manner. The antiplatelet effects of OHV A-PLA2 did not increase when preincubation times of platelets and OHV A-PLA2 were prolonged indicating phospholipid hydrolysis did not significantly contribute to the antiplatelet effects. Alkylation of active site His residue using p-bromophenacyl bromide resulted in the complete loss of enzymatic activity, but the modified enzyme retained more than 30% of its antiplatelet effects. These results indicate that the antiplatelet effects of OHV A-PLA2 appear to be independent of its enzymatic activity, and there are separate sites responsible for the catalytic and antiplatelet activities.

journal_name

Life Sci

journal_title

Life sciences

authors

Huang MZ,Gopalakrishnakone P,Kini RM

doi

10.1016/s0024-3205(97)00923-5

subject

Has Abstract

pub_date

1997-01-01 00:00:00

pages

2211-7

issue

22

eissn

0024-3205

issn

1879-0631

pii

S0024320597009235

journal_volume

61

pub_type

杂志文章
  • Inhibition of gastrointestinal transit by morphine and FK 33-824 in the rat and comparative narcotic antagonist properties of naloxone and its N-methyl quaternary analog.

    abstract::Morphine and the enkephalin-like peptide FK 33-824 given i.p. to rats potently inhibit gastrointestinal transit of a charcoal test meal, the doses inhibiting transit by 50% being respectively about 10 and 1 microgram/kg. These intestinal effects are opiate-specific, locally elicited and presumably involve the same act...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90359-9

    authors: Manara L,Bianchi G,Fiocchi R,Notarnicola A,Peracchia F,Tavani A

    更新日期:1982-09-20 00:00:00

  • The signal peptide of pro-opiomelancortin: validation of a specific radioimmunoassay.

    abstract::The N-terminus portion of the POMC leader sequence (signal peptide) was synthesized, and an antiserum was raised against it. A radioimmunoassay was developed which is effective at a dilution of 1:500,000, and sensitive at less than 1 fmole/tube. Since leader sequences often exhibit structural homologies, and since syn...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90135-7

    authors: Akil H,Shiomi H,Thompson R,Lax S,Coy D,Watson S

    更新日期:1982-11-15 00:00:00

  • Effect of electrical stimulation of the baso-lateral amygdala nucleus on defensive burying shock probe test and elevated plus maze in rats.

    abstract::In the present report, the putative effect of a single electrical stimulation (75, 150 or 300 microA) to the baso-lateral amygdala (BLA) nucleus was assessed in shock probe defensive burying behavior test (DB) and elevated plus maze (EPM). These models have been used for measuring anxiety levels and screening putative...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(02)02335-4

    authors: Saldívar-González JA,Posadas-Andrews A,Rodríguez R,Gómez C,Hernández-Manjarrez ME,Ortiz-León S,Martínez-Pineda A,Gómez-Laguna D,Salgado V,Manjarrez J,Alvarado R

    更新日期:2003-01-03 00:00:00

  • Neurotrophins and the development of cochlear innervation.

    abstract::The rapid progress in the past few years concerning neurotrophic factor research, has greatly stimulated advances in developmental neurobiology of hearing. We have summarized evidence that neurotrophins are expressed by auditory sensory epithelia during the time at which ganglion cells with neurotrophin receptors send...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0024-3205(94)00506-0

    authors: Després G,Romand R

    更新日期:1994-01-01 00:00:00

  • Inhibition of avian and mammalian hydroxy-indole-o-methyl-transferase (HIOMT) with low molecular weight fractions of mammalian pineal glands.

    abstract::Partially purified fractions from sheep pineal gland extracts, which show a fluorescence like pteridines, were shown to suppress the enzyme hydroxy-indole-o-methyltransferase (HIOMT) isolated from avian pineals and retinas. The results described demonstrate that the mechanism of inhibition of HIOMT activity is indepen...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90022-4

    authors: Ebels I,Cremer-Bartels G

    更新日期:1982-04-19 00:00:00

  • New specific radioligand for one subpopulation of brain somatostatin receptors.

    abstract::Cyclic octapeptide analogues of somatostatin (SS) like SMS 201-995 [H-(D) Phe-Cys-Phe-(D) Trp-Lys-Thr-Cys-Thr(ol)] or its Tyr3-derivative 204-090, displaced [125I-Tyr11]-SS 100% from pancreatic membranes but only 62-75% from brain membranes; the remaining sites were displaced by SS. These data indicate that some mini-...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(85)90155-9

    authors: Reubi JC

    更新日期:1985-05-13 00:00:00

  • Synthesis and binding characteristics of the highly specific, tritiated delta opioid antagonist [3H]TIPP.

    abstract::The recently discovered highly specific delta opioid antagonist H-Tyr-Tic-Phe-Phe-OH (TIPP) was radiolabelled by catalytic tritiation of its precursor [Tyr (3', 5'-I2)1]TIPP. The tritiated ligand labelled rat brain membrane binding sites with a Kd value of 0.64 nM and a Bmax of 82 fmol/mg protein. Binding competition ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(93)90649-n

    authors: Nevin ST,Toth G,Nguyen TM,Schiller PW,Borsodi A

    更新日期:1993-01-01 00:00:00

  • miR424-5p functions as an anti-oncogene in cervical cancer cell growth by targeting KDM5B via the Notch signaling pathway.

    abstract:AIMS:Aberrant expression of miRNAs exert the critical roles in carcinogenesis, including cervical cancer. Recent study corroborated the down-regulation of miR424-5p in uterine cervix adenocarcinoma. This research aimed to investigate the function and underlying mechanisms of miR424-5p in cervical cancer cell growth. M...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2017.01.006

    authors: Zhou Y,An Q,Guo RX,Qiao YH,Li LX,Zhang XY,Zhao XL

    更新日期:2017-02-15 00:00:00

  • Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors.

    abstract::A series of cyclic conformationally restricted penicillamine containing somatostatin octapeptide analogues have been prepared by standard solid phase synthetic techniques and tested for their ability to inhibit specific [125I]CGP 23,996 (des-Ala1-,Gly2-[desamino-Cys3Tyr11]-dicarba3, 14-somatostatin), [3H]naloxone or [...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(86)90574-6

    authors: Gulya K,Pelton JT,Hruby VJ,Yamamura HI

    更新日期:1986-06-16 00:00:00

  • Metabolic profiling of radioreceptor-assayable opioid peptides in a human pituitary ACTH-secreting tumor.

    abstract::The profile of endogenous opioid peptides in the peptide-rich fraction obtained from a homogenate of an ACTH-secreting human pituitary tumor is presented. Gradient RP-HPLC is used to separate the mixture into peptide constituents. A preparation of opioid receptors is used in a radioreceptor assay with ethorphine - a r...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(85)90225-5

    authors: Desiderio DM,Cezayirli RC,Fridland G,Robertson JT,Sacks H

    更新日期:1985-11-11 00:00:00

  • Phospholipid hydroperoxides are significantly less toxic to cultured endothelial cells than fatty acid hydroperoxides.

    abstract::Optically active hydroperoxides of phospholipids including phosphatidylcholine, phosphatidylethanolamine, phosphatidylglycerol, and phosphatidic acid were synthesized, and their cytotoxicity to cultured bovine pulmonary artery endothelial cells was examined. Phospholipid hydroperoxides were readily incorporated into c...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)00684-9

    authors: Kaneko T,Baba N,Matsuo M

    更新日期:1994-01-01 00:00:00

  • Effect of estradiol and relaxin on collagen and non-collagen protein synthesis by mammary fibroblasts.

    abstract::In order to determine the effect of relaxin and estradiol on collagen and noncollagen synthesis by mammary gland fibroblasts, fibroblasts isolated from guinea pig mammary glands were grown on plastic or Cytodex-3 collagen coated microcarriers. On plastic, estradiol (600 pg/ml) increased the incorporation of tritiated ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(84)90460-0

    authors: Sheffield LG,Anderson RR

    更新日期:1984-11-26 00:00:00

  • CNS depressants accelerate the dissociation of 35S-TBPS binding and GABA enhances their displacing potencies.

    abstract::The specific binding of 35S-t-butylbicyclophosphorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex. The displacing potencies of eleven CNS depressants and three convulsants were determined in the presence of 1 microM GABA and 10 nM R 5135. GABA enhanced the displacing potencies of depressa...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(88)90589-9

    authors: Maksay G,Ticku MK

    更新日期:1988-01-01 00:00:00

  • Steroidogenic impairment due to reduced ovarian transcription of cytochrome P450 side-chain-cleavage (P450scc) and steroidogenic acute regulatory protein (StAR) during experimental nephrotic syndrome.

    abstract::The nephrotic syndrome is a renal disease characterized by proteinuria, hypoproteinemia, edema and hyperlipidemia. It has been reported that female nephrotic rats are characterized by loss of the oestrus cycle, follicle atresia, low gonadotropin and steroid concentrations; particularly, undetectable estradiol levels. ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2006.02.023

    authors: Peña-Rico M,Guadalupe Ortiz-López M,Camacho-Castillo L,Cárdenas M,Pedraza-Chaverri J,Menjívar M

    更新日期:2006-07-10 00:00:00

  • Aerobic exercise training attenuates doxorubicin-induced ultrastructural changes in rat ventricular myocytes.

    abstract:AIMS:To investigate the effects of aerobic exercise training on cardiomyocyte ultrastructure, oxidative stress, and activation of protein synthesis pathways in a model of cardiomyopathy induced by doxorubicin (Dox). MAIN METHODS:Male Sprague Dawley rats were randomly assigned to Control (saline, sedentary), Dox/sedent...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118698

    authors: Sequeira CM,Martins MA,Alves R,Nascimento ALR,Botti GCRM,Rocha VN,Matsuura C

    更新日期:2021-01-01 00:00:00

  • The effect of GABA on in vitro binding of two novel non-benzodiazepines, PK 8165 and CGS 8216, to benzodiazepine receptors in the rat brain.

    abstract::The effect of gamma-aminobutyric acid (GABA) on the binding of PK 8165, a quinoline derivative, and CGS 8216, a pyrazoloquinoline, was assessed in two different regions of the rat brain. PK 8165, a compound with reported anxiolytic properties, inhibited [3H]-propyl beta-carboline-3-carboxylate labeled receptors in the...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(82)90403-9

    authors: Morelli M,Gee KW,Yamamura HI

    更新日期:1982-07-05 00:00:00

  • Effects of luteolin 5-O-beta-rutinoside in streptozotocin-induced diabetic rats.

    abstract::We have investigated the antidiabetic activity of luteolin 5-rutinoside in streptozotocin(STZ)-induced diabetic rats. Treatment for 20 days with 2 mg/kg increased both pancreatic insulin and DNA content. When both luteolin 5-rutinoside (2 mg/kg) and glibenclamide (1 mg/kg) were administered concurrently to STZ-diabeti...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(96)00231-7

    authors: Zarzuelo A,Jiménez I,Gámez MJ,Utrilla P,Fernadez I,Torres MI,Osuna I

    更新日期:1996-01-01 00:00:00

  • Characterisation of CGRP receptors in the human isolated middle meningeal artery.

    abstract::Although the understanding of migraine pathophysiology is still incomplete, there seems to be little doubt that dilatation of cranial blood vessels, including meningeal arteries, is involved in the headache phase of migraine. Since calcitonin gene-related peptide (CGRP) has been implicated in this vasodilatation, the ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2006.01.003

    authors: Gupta S,Mehrotra S,Avezaat CJ,Villalón CM,Saxena PR,Maassenvandenbrink A

    更新日期:2006-06-13 00:00:00

  • Branched-chain amino acids-induced cardiac protection against ischemia/reperfusion injury.

    abstract:AIMS:Amino acids, especially branched chain amino acids (BCAAs), have important regulatory roles in protein synthesis. Recently studies revealed that BCAAs protect against ischemia/reperfusion (I/R) injury. We studied the signaling pathway and mitochondrial function affecting a cardiac preconditioning of BCAAs. MAIN M...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.117368

    authors: Satomi S,Morio A,Miyoshi H,Nakamura R,Tsutsumi R,Sakaue H,Yasuda T,Saeki N,Tsutsumi YM

    更新日期:2020-03-15 00:00:00

  • Hispidulin: A promising flavonoid with diverse anti-cancer properties.

    abstract::In recent years, natural products have increasingly attracted more attention because of their potential anticancer activity and low intrinsic toxicity. Hispidulin is a natural flavonoid with a wide range of biological activities, including anti-inflammatory, antifungal, antiplatelet, anticonvulsant, anti-osteoporotic,...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2020.118395

    authors: Liu K,Zhao F,Yan J,Xia Z,Jiang D,Ma P

    更新日期:2020-10-15 00:00:00

  • Impairment of testicular function in electronic cigarette (e-cig, e-cigs) exposed rats under low-voltage and nicotine-free conditions.

    abstract::Despite the lack of knowledge of the effects of electronic cigarettes (e-cigarettes, e-cigs) on public health, they have been proposed as a part of smoking cessation efforts. Recently, several basic scientific studies have pointed out how e-cigs can generate carcinogens, such as e-cig liquid thermal degradation by-pro...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2019.04.059

    authors: Vivarelli F,Canistro D,Cirillo S,Cardenia V,Rodriguez-Estrada MT,Paolini M

    更新日期:2019-07-01 00:00:00

  • The human formyl peptide receptor as model system for constitutively active G-protein-coupled receptors.

    abstract::According to the two-state model of G-protein-coupled receptor (GPCR) activation, GPCRs isomerize from an inactive (R) state to an active (R*) state. In the R* state, GPCRs activate G-proteins. Agonist-independent R/R* isomerization is referred to as constitutive activity and results in an increase in basal G-protein ...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0024-3205(03)00654-4

    authors: Seifert R,Wenzel-Seifert K

    更新日期:2003-09-19 00:00:00

  • Presence of immunoreactive atrial natriuretic peptide in follicular fluid, ovary and ovarian perfusates.

    abstract::Immunoreactive atrial natriuretic peptide (ir-ANP) was measured in the follicular fluid of pig ovarian follicle, and rabbit ovarian homogenates and perfusates using a specific radioimmunoassay (RIA). Serial dilution curves made with the extracts of follicular fluid, ovarian homogenates and perfusates using SepPak C18 ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(89)90425-6

    authors: Kim SH,Cho KW,Seul KH,Ryu H,Koh GY

    更新日期:1989-01-01 00:00:00

  • Inhibitory effect of mitragynine, an alkaloid with analgesic effect from Thai medicinal plant Mitragyna speciosa, on electrically stimulated contraction of isolated guinea-pig ileum through the opioid receptor.

    abstract::Effect of mitragynine, an indole alkaloid isolated from Thai medicinal plant kratom (Mitragyna speciosa), on electrically stimulated contraction was studied in the guinea-pig ileum. Mitragynine (1 nM-3 microM) inhibited the ileum contraction elicited by electrical stimulation, and its pD2 value was 6.91 +/- 0.04 (n = ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(97)00023-4

    authors: Watanabe K,Yano S,Horie S,Yamamoto LT

    更新日期:1997-01-01 00:00:00

  • Differentially expressed CC3/TIP30 and rab11 along in vivo and in vitro intestinal epithelial cell crypt-villus axis.

    abstract::We have previously shown that transforming growth factor-beta1 (TGF-beta1) is involved in the fibroblast-induced organization and differentiation of transformed phenotypically crypt-like T84 intestinal epithelial cells into absorptive enterocyte-like cells, when cultured within a three-dimensional collagen gel. We hav...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)01216-4

    authors: Lindfors K,Halttunen T,Kainulainen H,Mäki M

    更新日期:2001-08-10 00:00:00

  • Phosphoesterase complex modulates microflora and chronic inflammation in rats with alcoholic fatty liver disease.

    abstract::Phosphoesterase complex (Pho), a major active component of barley malt, has been demonstrated to be clinically effective in relieving alcoholic fatty liver disease (AFLD), and several lines of evidence have suggested that microbial dysbiosis, caused by chronic alcohol overconsumption, plays a key role in the progressi...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118509

    authors: Ma D,Hu J,Xu W,Wang Y,Wang J,Li L,Wang S,Zhou H,Li Y,Liu L

    更新日期:2020-12-01 00:00:00

  • Resistance of obese and non-obese, spontaneously hypertensive rats to alloxan-induced diabetes.

    abstract::Male, 5 months old, massively obese, spontaneously hypertensive rats (Obese/SHR) were given 10 mg alloxan/100 g b.w., s.c., to induce diabetes. Control Obese and non-obese/SHR were given saline. Insulin therapy was withheld. All of the animals were killed at 6 months of age. Alloxan caused a slight but statistically s...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(83)90666-5

    authors: Wexler BC,Mc Murtry JP

    更新日期:1983-09-12 00:00:00

  • Insulin analogs: Glimpse on contemporary facts and future prospective.

    abstract::Insulin remains a predominant life-saving medication for type 1 and type 2 Diabetes Mellites. Natural insulin secretion limits the fluctuation of the narrow and high surge of blood glucose levels. However, imitating the same by external insulin remains a challenge as a variety of insulin analogs (rapid acting, short a...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2019.01.011

    authors: Sharma AK,Taneja G,Kumar A,Sahu M,Sharma G,Kumar A,Sardana S,Deep A

    更新日期:2019-02-15 00:00:00

  • Molecular modeling of SWR-0342SA, a beta3-selective agonist, with beta1- and beta3-adrenoceptor.

    abstract::The molecular dynamics (MD) simulations study in the formation of the complex between compound SWR-0342SA and beta-ARs suggested that upon binding SWR-0342SA stimulates receptor activation through residues network (Asp104, Leu335 in beta(1)-AR; Asp117, Ser209, Leu303, Ser191 in beta(3)-AR) in an active conformation st...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2005.09.023

    authors: Ahmed M,Ishiguro M,Nagatomo T

    更新日期:2006-03-20 00:00:00

  • 3-Nitroacridine derivatives arrest cell cycle at G0/G1 phase and induce apoptosis in human breast cancer cells may act as DNA-target anticancer agents.

    abstract::DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.05.010

    authors: Zhou Q,You C,Zheng C,Gu Y,Gu H,Zhang R,Wu H,Sun B

    更新日期:2018-08-01 00:00:00