Sulphate conjugation of minoxidil in rat skin.

Abstract:

:Minoxidil sulphotransferase (MST) activity was determined in the cytosolic fraction of rat skin and liver. MST of rat skin is similar to the P (phenol)-form of phenosulphotransferase (PST) of human tissues with respect to thermostability and inhibition by 2,6-dichloro-4-nitrophenol (DCNP). p-Nitrophenol, a prototype substrate of human P-PST form, inhibits MST at micromolar concentration while millimolar concentrations of dopamine and tyramine, substrates of human M-(monoamine)-PST, are required to elicit a similar degree of inhibition. The enzymatic transfer of 35S from sodium 35sulphate to minoxidil was also demonstrated suggesting that the rat skin is potentially capable of synthesizing 3'-phosphoadenosine-5'-phosphosulphate (PAPS) from inorganic sulphate and utilizing it for the biosynthesis of minoxidil sulphate, its active metabolite. Thus, it is conceivable that the pharmacological action of minoxidil as a promoter of hair growth could be carried out by the cutaneous tissues without the contribution of hepatic or other extrahepatic organs.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Wong KO,Tan AY,Lim BG,Wong KP

doi

10.1016/0006-2952(93)90268-2

subject

Has Abstract

pub_date

1993-03-09 00:00:00

pages

1180-2

issue

5

eissn

0006-2952

issn

1873-2968

pii

0006-2952(93)90268-2

journal_volume

45

pub_type

杂志文章
  • Malvidin-3-O-β glucoside, major grape anthocyanin, inhibits human macrophage-derived inflammatory mediators and decreases clinical scores in arthritic rats.

    abstract::Polyphenolic anthocyanins are major colorful compounds in red fruits, known to prevent cardiovascular and other diseases. Grape polyphenols are a mixture of various molecules and their exact contribution to above bioactivities remains to be clarified. In the present study, we first analyzed the effect of purified grap...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.06.010

    authors: Decendit A,Mamani-Matsuda M,Aumont V,Waffo-Teguo P,Moynet D,Boniface K,Richard E,Krisa S,Rambert J,Mérillon JM,Mossalayi MD

    更新日期:2013-11-15 00:00:00

  • Methylation of 21-23 kD membrane proteins by a membrane-associated protein carboxyl methyltransferase in neuroblastoma cells. Increased methylation in differentiated cells.

    abstract::Membranes of neuroblastoma N1E-115 cells contain a specific protein carboxyl methyltransferase that methylates a 70 kD protein and a group of 21-23 kD proteins which are tightly bound to the membranes. The enzyme catalyzes the transfer of [methyl-3H] groups from [methyl-3H]S-adenosyl-L-methionine (Km = 0.22 microM) to...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90405-a

    authors: Haklai R,Kloog Y

    更新日期:1990-09-15 00:00:00

  • The acetaminophen-derived bioactive N-acylphenolamine AM404 inhibits NFAT by targeting nuclear regulatory events.

    abstract::AM404 is a synthetic TRPV1/CB(1) hybrid ligand with inhibitory activity on the anandamide transporter and is used for the pharmacological manipulation of the endocannabinoid system. It has been recently described that acetaminophen is metabolised in the brain to form the bioactive N-acylphenolamine AM404 and therefore...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.12.001

    authors: Caballero FJ,Navarrete CM,Hess S,Fiebich BL,Appendino G,Macho A,Muñoz E,Sancho R

    更新日期:2007-04-01 00:00:00

  • Mechanisms of toxicity of 3'-azido-3'-deoxythymidine. Its interaction with adenylate kinase.

    abstract::Recent experiments from our laboratory have indicated that the inhibitory effect of 3'-azido-3'-deoxythymidine (AZT) on oxidative phosphorylation may occur directly, in addition to being brought about by its inhibition of mtDNA replication. We report here studies on the effect of AZT on adenylate kinase, an enzyme cru...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90564-9

    authors: Barile M,Valenti D,Hobbs GA,Abruzzese MF,Keilbaugh SA,Passarella S,Quagliariello E,Simpson MV

    更新日期:1994-10-07 00:00:00

  • Discovery of substituted sulfonamides and thiazolidin-4-one derivatives as agonists of human constitutive androstane receptor.

    abstract::The constitutive androstane receptor (CAR; NR1I3) is a nuclear receptor responsible for the recognition of potentially toxic endo- and exogenous compounds whose elimination from the body is accelerated by the CAR-mediated inducible expression of metabolizing enzymes and transporters. Despite the importance of CAR, few...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.08.014

    authors: Küblbeck J,Jyrkkärinne J,Poso A,Turpeinen M,Sippl W,Honkakoski P,Windshügel B

    更新日期:2008-11-15 00:00:00

  • In vivo chronic exposure to heroin or naltrexone selectively inhibits liver microsome formation of estradiol-3-glucuronide in the rat.

    abstract::We have previously found that repeated exposure to heroin reduces liver synthesis of morphine-3-glucuronide (M3G) and increases the production of morphine-6-glucuronide (M6G), which normally is not formed in the rat. By contrast repeated exposure to naltrexone does not activate M6G synthesis but increases the V(max) o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.06.011

    authors: Antonilli L,Brusadin V,Milella MS,Sobrero F,Badiani A,Nencini P

    更新日期:2008-09-01 00:00:00

  • Effects of perfluoro fatty acids on xenobiotic-metabolizing enzymes, enzymes which detoxify reactive forms of oxygen and lipid peroxidation in mouse liver.

    abstract::Male mice were exposed via their diet to perfluoro fatty acids of various chain-lengths (2-10 carbon atoms) at different doses (0.02 and 0.1% weight) and for different periods of time (2-10 days). Thereafter, we monitored effects on liver and body weights and a number of hepatic parameters, including mitochondrial pro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90383-t

    authors: Permadi H,Lundgren B,Andersson K,DePierre JW

    更新日期:1992-09-25 00:00:00

  • Down-regulation of cytochrome P450 proteins and its activities by Shiga-like toxin II from Escherichia coli O157:H7.

    abstract::Escherichia coli O157:H7 infection frequently induces clinical complications such as hemolytic uremic syndromes and intestinal dysfunctions. These changes could alter the disposition of drugs, consequently changing their efficacy. However, the possible changes of drug-metabolizing activities by E. coli O157:H7 infecti...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2003.12.009

    authors: Kitaichi K,Nakayama H,Ueyama J,Nadai M,Baba K,Takagi K,Takagi K,Ohta M,Hasegawa T

    更新日期:2004-04-15 00:00:00

  • Integrated cytochrome P450 reaction phenotyping: attempting to bridge the gap between cDNA-expressed cytochromes P450 and native human liver microsomes.

    abstract::With the increased availability of human liver tissue, recombinant (cDNA-expressed) cytochrome P450 proteins (rCYPs), and knowledge of the human CYP pool (e.g. immunoquantitated levels of each CYP form in native liver microsomes), it is now possible to carry out in vitro "CYP reaction phenotyping" in an integrated man...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0006-2952(98)00268-8

    authors: Rodrigues AD

    更新日期:1999-03-01 00:00:00

  • Increased Na+/K(+)-pump activity and adenosine triphosphate utilization after compound 48/80-induced histamine secretion from rat mast cells.

    abstract::The Na+/K(+)-pump activity and the utilization of adenosine triphosphate (ATP) were studied in rat peritoneal mast cells after histamine secretion induced by compound 48/80. We measured the ouabain-sensitive K(+)-uptake by a radioactive technique (86Rb+). The ATP content and the glycolytic ATP-production were measured...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90299-2

    authors: Johansen T,Praetorius H

    更新日期:1994-05-18 00:00:00

  • Apoptosis induced by calcein acetoxymethyl ester in the human histiocytic lymphoma cell line U-937 GTB.

    abstract::Effects of calcein acetoxymethyl ester (calcein/AM) on macromolecular synthesis, mitochondrial membrane potential, and mode of death were studied in U-937 GTB lymphoma cells. This was accomplished by measurements of (14)C-labeled thymidine and leucine incorporation, 5,5',6,6'-tetrachloro-1,1',3, 3'-tetraethylbenzimida...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(00)00494-9

    authors: Liminga G,Martinsson P,Jonsson B,Nygren P,Larsson R

    更新日期:2000-12-15 00:00:00

  • Targeting the epidermal growth factor receptor for therapy of carcinomas.

    abstract::As a group, the carcinomas represent a substantial proportion of all human malignancies, but, with relatively few exceptions, current treatments are ineffective. Modification of existing chemotherapeutic agents has not led to significant improvements in the survival of carcinoma patients, and development of new therap...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/0006-2952(95)02232-5

    authors: Davies DE,Chamberlin SG

    更新日期:1996-05-03 00:00:00

  • Studies on the release of proteolytic enzymes during synovium-induced cartilage breakdown in vitro and the actions of anti-inflammatory drugs.

    abstract::Pig articular cartilage, overlaid with a minced preparation of synovium from the same joint, underwent extensive matrix degradation during a two-week culture period. This degradation was associated with de novo synthesis by the synovium of specific neutral proteoglycan- and collagen-degrading enzymes. Both enzymes exh...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90179-5

    authors: Crossley MJ,Hunneyball IM

    更新日期:1984-04-15 00:00:00

  • Stabilization of ornithine decarboxylase in mouse liver and lung by methylglyoxal bis(cyclohexylamidinohydrazone).

    abstract::The intraperitoneal injection of methylglyoxal bis(cyclohexylamidinohydrazone) (MGBC), an inhibitor of S-adenosylmethionine decarboxylase and spermidine synthase, markedly increased (7-fold of the basal level at 4 hr) ornithine decarboxylase (ODC) activity in normal mouse liver. ODC activity was also increased 2.5-fol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90104-9

    authors: Hibasami H,Maekawa S,Murata T,Nakashima K

    更新日期:1988-11-01 00:00:00

  • Effects of chronic ethanol feeding on glutathione turnover in the rat.

    abstract::Glutathione (GSH) is important in protection of cells against electrophilic drug injury and against reactive oxygen species. Both steady-state concentrations and turnover of GSH are important determinants of susceptibility of the hepatocyte to injury. Chronic ethanol administration is known to enhance susceptibility t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90699-9

    authors: Morton S,Mitchell MC

    更新日期:1985-05-01 00:00:00

  • Tricyclic antidepressant-induced lipidosis in human peripheral monocytes in vitro, as well as in a monocyte-derived cell line, as monitored by spectrofluorimetry and flow cytometry after staining with Nile red.

    abstract::Human mono- and lymphocytes from peripheral blood and the monoblastoid cell line U-937 were used in this in vitro study of drug-induced lipidosis. Mono- and lymphocytes were exposed for 4 days to three different tricyclic antidepressants (TCAs), imipramine (25 microM), clomipramine (10 microM) and citalopram (80 micro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)82443-4

    authors: Xia Z,Appelkvist EL,DePierre JW,Nässberger L

    更新日期:1997-05-15 00:00:00

  • Desulfuration of 6-mercaptopurine. The basis for the paradoxical cytotoxicity of thiopurines in cultured human leukemic cells.

    abstract::The thiopurines have a wide array of effects on purine metabolism, but the primary mechanism of cytotoxicity for both 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) appears to be incorporation of drug into DNA following conversion to the thioguanylate form. In murine leukemic cell lines exposed to a range of thiopur...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90333-r

    authors: Adamson PC,Balis FM,Hawkins ME,Murphy RF,Poplack DG

    更新日期:1993-11-02 00:00:00

  • Direct and indirect effects of sulfhydryl blocking agents on agonist and antagonist binding to central alpha 1- and alpha 2-adrenoceptors.

    abstract::The effects of p-chloromercuribenzoate and N-ethylmaleimide were evaluated on the binding of (3H)-p-aminoclonidine, (3H)-rauwolscine and (3H)-prazosin on rat brain alpha-adrenergic receptors. Pretreatment of the particulate fraction with increasing concentrations of p-chloromercuribenzoate indicated that the binding o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90002-9

    authors: Quennedey MC,Bockaert J,Rouot B

    更新日期:1984-12-15 00:00:00

  • Analysis of protein synthesis in rat salivary glands after chronic treatment with beta-receptor agonists and phosphodiesterase inhibitors.

    abstract::Chronic administration of the beta-adrenergic receptor agonist isoproterenol (5 mg/200 g animal for 10 days) resulted in rat parotid and submandibular gland hypertrophy, and it induced synthesis of a series of proline-rich proteins (PRPs) and glycoproteins. Treated parotid glands additionally exhibit an increase in ac...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90277-1

    authors: Wells DJ,Humphreys-Beher MG

    更新日期:1985-12-15 00:00:00

  • AT-533, a Hsp90 inhibitor, attenuates HSV-1-induced inflammation.

    abstract::Inflammatory events are tightly associated with the death caused by Herpes simplex virus 1 (HSV-1) infection of the brain. Heat shock protein 90 (Hsp90) is a molecular chaperone that is stimulated in response to many stressful conditions (e.g., inflammation and hypoxia) and Hsp90 inhibitors are suggested to be potent ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.05.003

    authors: Li F,Song X,Su G,Wang Y,Wang Z,Qing S,Jia J,Wang Y,Huang L,Zheng K,Wang Y

    更新日期:2019-08-01 00:00:00

  • Tyramine in the assessment of regional adrenergic function.

    abstract::Regional adrenergic function is difficult to assess in humans. Tyramine given through a microdialysis probe may be a useful tool in this regard. However, tyramine data is hard to interpret given the drug's complex mode of action. We characterized the response to tyramine, isoproterenol, and dopamine in adipose tissue ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.09.004

    authors: Adams F,Boschmann M,Schaller K,Franke G,Gorzelniak K,Janke J,Klaus S,Luft FC,Heer M,Jordan J

    更新日期:2006-12-15 00:00:00

  • Butyrylcholinesterase, a stereospecific in vivo bioscavenger against nerve agent intoxication.

    abstract::Human butyrylcholinesterase (E.C. 3.1.1.8) purified from blood plasma has previously been shown to provide protection against up to five and a half times the median lethal dose of an organophosphorus nerve agent in several animal models. In this study the stoichiometric nature of the protection afforded by human butyr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.113670

    authors: Cerasoli DM,Armstrong SJ,Reeves TE,Hodgins SM,Kasten SA,Lee-Stubbs RB,Cadieux CL,Otto TC,Capacio BR,Lenz DE

    更新日期:2020-01-01 00:00:00

  • A point mutation produced a class 3 aldehyde dehydrogenase with increased protective ability against the killing effect of cyclophosphamide.

    abstract::Cyclophosphamides are pro-drugs whose killing agent is produced from an aldehyde that is formed by the action of a P450 oxidation step. The mustard from the aldehyde can destroy bone marrow cells as well as the tumor. Aldehyde dehydrogenase (EC 1.2.1.3) can oxidize the aldehyde and hence inactivate the cytotoxic inter...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.06.018

    authors: Ho KK,Mukhopadhyay A,Li YF,Mukhopadhyay S,Weiner H

    更新日期:2008-09-01 00:00:00

  • Intestinal cell-specific vitamin D receptor (VDR)-mediated transcriptional regulation of CYP3A4 gene.

    abstract::CYP3A4 is the most important drug-metabolizing enzyme that is involved in biotransformation of more than 50% of drugs. Pregnane X receptor (PXR) dominantly controls CYP3A4 inducibility in the liver, whereas vitamin D receptor (VDR) transactivates CYP3A4 in the intestine by secondary bile acids. Four major functional P...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2009.08.017

    authors: Pavek P,Pospechova K,Svecova L,Syrova Z,Stejskalova L,Blazkova J,Dvorak Z,Blahos J

    更新日期:2010-01-15 00:00:00

  • Modulatory effect of 4 beta-phorbol 12-myristate 13-acetate (PMA) on carbachol-induced Ca2+ mobilization in rat parotid acinar cells.

    abstract::Treatment of rat parotid acinar cells with 4 beta-phorbol 12-myristate 13-acetate (PMA) significantly inhibited an increase in cytosolic free Ca2+ concentration ([Ca2+]i) induced by carbachol (CCh), a muscarinic agonist. The CCh-induced increase in [Ca2+]i was also inhibited by another active phorbol ester, 4 beta-pho...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90081-7

    authors: Tojyo Y,Tanimura A,Matsumoto Y

    更新日期:1994-06-01 00:00:00

  • Pharmacological characterization of glucocorticoid receptors in primary human bronchial epithelial cells.

    abstract::Bronchial epithelial cells play an important role in amplifying and perpetuating airway inflammation and may be a target for inhaled steroids. We have characterized glucocorticoid receptors in primary human bronchial epithelial cells. Northern and western blot analyses demonstrated the expression of glucocorticoid rec...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(99)00008-8

    authors: LeVan TD,Babin EA,Yamamura HI,Bloom JW

    更新日期:1999-05-01 00:00:00

  • Effects of protein-protein interface disruptors at the ligand of the glucocorticoid-induced tumor necrosis factor receptor-related gene (GITR).

    abstract::The tumor necrosis factor (TNF) superfamily (TNFSF) includes about thirty structurally related receptors (TNFSFRs) and about twenty protein ligands that bind to one or more of these receptors. Receptors of the tumor necrosis factor (TNF) superfamily (TNFSFRs) are pharmacological targets for treatment of inflammatory a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2020.114110

    authors: Platania CBM,Ronchetti S,Riccardi C,Migliorati G,Marchetti MC,Di Paola L,Lazzara F,Drago F,Salomone S,Bucolo C

    更新日期:2020-08-01 00:00:00

  • Calcipotriol (MC 903): pharmacokinetics in rats and biological activities of metabolites. A comparative study with 1,25(OH)2D3.

    abstract::Calcipotriol (MC 903) is a novel analogue of the physiologically active metabolite of vitamin D3, 1 alpha,25-dihydroxycholecalciferol [1,25(OH)2D3]. MC 903 and 1,25(OH)2D3 have similar effects on cell proliferation and cell differentiation in vitro using the human histiocytic lymphoma cell line U 937, but in vivo MC90...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90160-7

    authors: Kissmeyer AM,Binderup L

    更新日期:1991-06-01 00:00:00

  • SPZ1 is critical for chemoresistance and aggressiveness in drug-resistant breast cancer cells.

    abstract::It is believed that chemotherapeutic agents can enhance the malignancy of treated cancer cells in clinical situations, which is a major problem for chemotherapy. However, the underlying molecular mechanisms are still not fully understood. Here, we demonstrated that chemotherapy up-regulates the levels of spermatogenic...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2018.07.046

    authors: Liu X,Han X,Wan X,He C,Wang Y,Mao A,Yu F,Zhou T,Feng L,Zhang P,Jin J,Ma X

    更新日期:2018-10-01 00:00:00

  • In vitro-in vivo correlation for drugs and other compounds eliminated by glucuronidation in humans: pitfalls and promises.

    abstract::Enzymes of the UDP-glucuronosyltransferase (UGT) superfamily are responsible for the metabolism of many drugs, environmental chemicals and endogenous compounds. Identification of the UGT(s) involved in the metabolism of a given compound ('reaction phenotyping') currently relies on multiple confirmatory approaches, whi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2005.12.019

    authors: Miners JO,Knights KM,Houston JB,Mackenzie PI

    更新日期:2006-05-28 00:00:00