Rapid stimulation of rhodamine 123 efflux from multidrug-resistant KB cells by progesterone.


:Rhodamine 123 is a mitochondrial dye that is retained for prolonged periods by carcinoma cells. While investigating causes of retention of this dye, we found that 10 microM progesterone caused a rapid stimulation of efflux of rhodamine 123 within 15 min from KB V20C cells, which overexpress the multidrug resistance pump. Progesterone did not stimulate efflux from KB cells that do not overexpress the pump, and verapamil blocked rhodamine 123 efflux in the presence or absence of progesterone, indicating that rhodamine 123 is removed from KB V20C cells by the multidrug resistance pump. Progesterone, however, is unlikely to stimulate rhodamine 123 efflux by simply increasing pump activity for two reasons: (1) progesterone inhibited the efflux of daunomycin from KB V20C cells, so it did not stimulate efflux of all drugs, and (2) progesterone inhibited efflux of rhodamine 123 from L1210/VMDRC cells and had little effect on Adr MCF7 cells; both overexpress the multidrug resistance pump. In the experiments with KB V20C cells, progesterone was the most active steroid tested. At 10 microM, progesterone caused a 70-fold stimulation, desoxycorticosterone, testosterone, promegestone and estradiol about 20-fold, and others had little or no effect. Progesterone may act by a non-genomic mechanism to decrease intracellular binding of rhodamine 123, making the dye accessible to the multidrug resistance pump.


Biochem Pharmacol


Biochemical pharmacology


Jancis EM,Chen HX,Carbone R,Hochberg RB,Dannies PS




Has Abstract


1993-11-02 00:00:00














  • Regulation of interleukin-13 by type 4 cyclic nucleotide phosphodiesterase (PDE) inhibitors in allergen-specific human T lymphocyte clones.

    abstract::Interleukin-13 (IL-13) is a proinflammatory cytokine of T cell origin. Structural and functional studies suggest a key role for IL-13 in the genesis of chronic allergic inflammation; as such, its pharmacologic inhibition is of potential clinical utility. We studied the pharmacologic regulation of IL-13 expression by c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Essayan DM,Kagey-Sobotka A,Lichtenstein LM,Huang SK

    更新日期:1997-04-04 00:00:00

  • Stimulation of cadmium uptake by estradiol in the kidney of male rats treated with cadmium.

    abstract::The present study was carried out to analyze the sex differences in the retention of Cd in rats treated with a small amount of Cd, and its mechanisms. Cd and Zn concentrations in the kidney and liver of female rats treated with 28 nmol Cd or 1 nmole Zn were significantly higher than those in male rats. Pretreatment wi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Nishiyama S,Onosaka S,Taguchi T,Konishi Y,Tanaka K,Kinebuchi H

    更新日期:1988-08-15 00:00:00

  • The influence of picolines on glutathione transferase activity and subunit composition in human liver derived Hep G2 cells.

    abstract::Hep G2 cells, an established cell line derived from a human hepatoma, have retained a number of hepatocytic phase I and II reactions. The influence of picolines (2-, 3- and 4-methylpyridine), related compounds and some classical enzyme inducers on specific glutathione transferase (GST) activity and its subunit composi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dierickx PJ

    更新日期:1994-11-16 00:00:00

  • Comparison of the ability of dopamine receptor agonists to inhibit forskolin-stimulated adenosine 3'5'-cyclic monophosphate (cAMP) accumulation via D2L (long isoform) and D3 receptors expressed in Chinese hamster ovary (CHO) cells.

    abstract::The pharmacological properties of the human D2L (long isoform) and rat D3 dopamine receptors in functional assays were examined. A range of dopamine agonists were assessed for their ability to inhibit adenosine 3'5'-cyclic monophosphate (cAMP) accumulation via the two receptors expressed stably in Chinese hamster ovar...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hall DA,Strange PG

    更新日期:1999-07-15 00:00:00

  • Pharmacological characterization of linear analogues of vasopressin generated by the systematic substitution of positions 1 and 6 by L-amino acids.

    abstract::Eighteen linear analogues of [Arg8]vasopressin (AVP) were synthesized by systematically substituting the cysteine residues at positions 1 and 6 with a range of L-amino acids. Screening by competition ligand binding revealed that the combinations of amino acid residues tolerated at these positions was very restricted w...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Howl J,Filer AD,Parslow RA,Kirk CJ,Jurzak M,Smith AI,Wheatley M

    更新日期:1994-04-29 00:00:00

  • Helenalin bypasses Bcl-2-mediated cell death resistance by inhibiting NF-κB and promoting reactive oxygen species generation.

    abstract::Evasion of cell death by overexpression of anti-apoptotic proteins, such as Bcl-2, is commonly observed in cancer cells leading to a lack of response to chemotherapy. Hence, there is a need to find new chemotherapeutic agents that are able to overcome chemoresistance mediated by Bcl-2 and to understand their mechanism...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hoffmann R,von Schwarzenberg K,López-Antón N,Rudy A,Wanner G,Dirsch VM,Vollmar AM

    更新日期:2011-09-01 00:00:00

  • IL-8 production by macrophages is synergistically enhanced when cigarette smoke is combined with TNF-alpha.

    abstract::Macrophages are key inflammatory cells in chronic obstructive pulmonary disease (COPD). The pathophysiology of cigarette smoke-induced lung emphysema is complex but there is a clear role for reactive oxygen species (ROS, such as peroxynitrite), tumor necrosis factor (TNF-alpha) and interleukin (IL)-8. We investigated ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sarir H,Mortaz E,Janse WT,Givi ME,Nijkamp FP,Folkerts G

    更新日期:2010-03-01 00:00:00

  • The critical role of porcine cytochrome P450 3A46 in the bioactivation of aflatoxin B1.

    abstract::Aflatoxin B1 (AFB1) is bioactivated by cytochrome P450 (CYP) 3A isoforms in humans to generate the highly reactive epoxide intermediate AFB1-8,9-epoxide (AFBO), causing hepatotoxicity and hepatocarcinoma. Due to the unavoidable contamination in their feed, pigs are more likely to be exposed to AFB1 and indirectly harm...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Jiang H,Wu J,Zhang F,Wen J,Jiang J,Deng Y

    更新日期:2018-10-01 00:00:00

  • Inhibition of the transport of adenosine, other nucleosides and hypoxanthine in novikoff rat hepatoma cells by methylxanthines, papaverine, N6-cyclohexyladenosine and N6-phenylisopropyladenosine.

    abstract::Theophylline, caffeine, isobutylmethylxanthine, papaverine, N6-cyclohexyladenosine, N6-allyl-N6-cyclohexyladenosine ( ACHA ) and N6-L-phenylisopropyladenosine (L-PIA) inhibited the transport of adenosine, uridine and hypoxanthine in Novikoff rat hepatoma cells. The IC50 values for the inhibition of uridine transport r...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Plagemann PG,Wohlhueter RM

    更新日期:1984-06-01 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


    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

  • Effect of nitrogen dioxide on surface membrane fluidity and insulin receptor binding of pulmonary endothelial cells.

    abstract::Nitrogen dioxide (NO2), an environmental oxidant pollutant, is known to peroxidize membrane lipids of lung cells. We evaluated the ability of NO2 to alter the surface membrane fluidity, lipid composition, and insulin receptor binding of porcine pulmonary artery endothelial cells in culture. After 3- to 24-hr exposure ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Patel JM,Edwards DA,Block ER,Raizada MK

    更新日期:1988-04-15 00:00:00

  • Covalent binding of the anticancer drug ellipticine to DNA in V79 cells transfected with human cytochrome P450 enzymes.

    abstract::Ellipticine is a potent antineoplastic agent whose mechanism of action is considered to be based mainly on DNA intercalation and/or inhibition of topoisomerase II. Recently, we found that ellipticine also forms covalent DNA adducts and that the formation of the major adduct is dependent on the activation of ellipticin...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Frei E,Bieler CA,Arlt VM,Wiessler M,Stiborová M

    更新日期:2002-07-15 00:00:00

  • S-methyl N-butylthiocarbamate sulfoxide: selective carbamoylating agent for mouse mitochondrial aldehyde dehydrogenase.

    abstract::Liver mitochondrial low-Km aldehyde dehydrogenase (ALDH2, EC, the isoform responsible for the conversion of acetaldehyde to acetate, is inhibited by the sulfoxide bioactivation products of Et2NC(O)SMe (from the alcohol aversion drug disulfiram), Pr2NC(O)SEt (the herbicide S-ethyl N,N-dipropylthiocarbamate), a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Staub RE,Quistad GB,Casida JE

    更新日期:1999-11-01 00:00:00

  • 86Rb+ efflux mediated by alpha4beta2*-nicotinic acetylcholine receptors with high and low-sensitivity to stimulation by acetylcholine display similar agonist-induced desensitization.

    abstract::The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Marks MJ,Meinerz NM,Brown RW,Collins AC

    更新日期:2010-10-15 00:00:00

  • Mouse brain opioid receptor identification by direct ultraviolet photoaffinity labeling.

    abstract::[3H]Morphine, PL-017[prolyl-3,4-3H,D-prolyl,3,4-3H] ([3H]PL-017) and enkephalin-(2-D-penicillamine,5-D-penicillamine)[tyrosyl-2,6-3H] ([3H]DPDPE) were directly cross-linked to mouse brain opiate receptors by an ultraviolet (254 nm) irradiation procedure. [3H]Morphine preferentially and specifically labeled a 58 kDa pr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Nagamatsu K,Tagawa Y,Uchida S,Hasegawa A

    更新日期:1993-10-05 00:00:00

  • Modulation of [3H] TBOB binding to the rodent GABAA receptor by simple disaccharides.

    abstract::We have recently reported evidence that a simple beta-linked alkylated mannose reversibly increased the magnitude of GABA(A) receptor currents evoked in cultured rat pyramidal neurons whilst concomitantly reducing the incidence of spontaneous synaptic activity. In this present study, the effects of the simple beta-lin...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Rezai N,Duggan C,Cairns D,Lees G,Chazot PL

    更新日期:2003-02-15 00:00:00

  • Sulfated glycolipid PG545 induces endoplasmic reticulum stress and augments autophagic flux by enhancing anticancer chemotherapy efficacy in endometrial cancer.

    abstract::The sulfated glycolipid PG545 shows promising antitumor activity in various cancers. This study was conducted to explore the effects and the mechanism of PG545 action in endometrial cancer (EC). PG545 exhibited strong synergy as assessed by the Chou-Talalay-Method in vitro when combined with cisplatin, or paclitaxel i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hoffmann R,Sarkar Bhattacharya S,Roy D,Winterhoff B,Schmidmaier R,Dredge K,Hammond E,Shridhar V

    更新日期:2020-08-01 00:00:00

  • Effects of vitamin E deficiency and glutathione depletion on stress protein heme oxygenase 1 mRNA expression in rat liver and kidney.

    abstract::Heme oxygenase 1 (HO-1) is a stress protein and has been suggested to provide defense mechanisms against agents that may induce oxidative injury. Vitamin E (VE) is considered to function as an important cellular antioxidant. Rats were fed a VE-deficient (0E) or a VE-sufficient (10E) diet for 6 weeks and then were intr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ito K,Yano T,Hagiwara K,Ozasa H,Horikawa S

    更新日期:1997-11-15 00:00:00

  • beta-Naphthoflavone-inducible cytochrome P4501A1 activity in liver microsomes of the marine safi fish (Siganus canaliculatus).

    abstract::The cytochrome P450-dependent metabolism of benzo(a)pyrene and other xenobiotics has been investigated in liver microsomes prepared from a local marine safi fish, Siganus canaliculatus. The safi fish was found to have a well-developed microsomal monooxygenase system consisting of cytochrome P450, cytochrome b5 and NAD...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Raza H,Otaiba A,Montague W

    更新日期:1995-10-26 00:00:00

  • Hydralazine: a potent inhibitor of aldehyde oxidase activity in vitro and in vivo.

    abstract::The interaction of the vasodilator, hydralazine, with the molybdenum hydroxylases, aldehyde oxidase and xanthine oxidase has been investigated. A potent progressive inhibition of rabbit liver aldehyde oxidase, in the presence of substrate, by low concentrations of hydralazine (0.1-1 microM) was observed in vitro but n...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Johnson C,Stubley-Beedham C,Stell JG

    更新日期:1985-12-15 00:00:00

  • Nrf2 in keratinocytes protects against skin fibrosis via regulating epidermal lesion and inflammatory response.

    abstract::Nuclear factor-E2-related factor 2 (Nrf2) is a master transcription factor in antioxidant response, protecting against oxidative damage and various diseases. Previous studies suggest that Nrf2 is suppressed in fibrotic skin and Nrf2 agonists represent a therapeutic strategy, which is mainly attributed to Nrf2 function...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wu R,Zhang H,Zhao M,Li J,Hu Y,Fu J,Pi J,Wang H,Xu Y

    更新日期:2020-04-01 00:00:00

  • Emodin induces apoptosis in human promyeloleukemic HL-60 cells accompanied by activation of caspase 3 cascade but independent of reactive oxygen species production.

    abstract::Emodin (1,3,8-trihydroxy-6-methylanthraquinone) is an active constituent of Rheum palmatum, and showed inhibitory activity on lipopolysaccharide-induced NO production in our previous study. However, the apoptosis-inducing activity of emodin has remained undefined. Among three structurally related anthraquinones, inclu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chen YC,Shen SC,Lee WR,Hsu FL,Lin HY,Ko CH,Tseng SW

    更新日期:2002-12-15 00:00:00

  • Endopeptidase-24.11 cleaves a chemotactic factor from alpha-calcitonin gene-related peptide.

    abstract::The sequence of rat alpha-calcitonin gene-related peptide (CGRP-alpha) contains the tetrapeptide eosinophil granulocyte chemotactic factor Val32-Gly-Ser-Glu35. Peptide fragments formed following hydrolysis of rat CGRP-alpha in vitro by endopeptidase-24.11 were identified. The tetrapeptide fragment was generated follow...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Davies D,Medeiros MS,Keen J,Turner AJ,Haynes LW

    更新日期:1992-04-15 00:00:00

  • Ah receptor- and Nrf2-gene battery members: modulators of quinone-mediated oxidative and endoplasmic reticulum stress.

    abstract::Quinones are ubiquitously present in mammals and their environment. They are involved in physiologic functions such as electron transport but are also toxic compounds. In particular, quinone-quinol redox cycles may lead to oxidative stress, and arylating quinones have been demonstrated to activate endoplasmic reticulu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bock KW

    更新日期:2012-04-01 00:00:00

  • The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy.

    abstract::It has become apparent of late that even in tamoxifen and/or aromatase resistant breast cancers, ERα remains a bona fide therapeutic target. Not surprisingly, therefore, there has been considerable interest in developing Selective ER Degraders (SERDs), compounds that target the receptor for degradation. Currently, ICI...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wardell SE,Marks JR,McDonnell DP

    更新日期:2011-07-15 00:00:00

  • Recovery after hypoglycemic brain injury. Action of some biological substances on the cerebral metabolism.

    abstract::In artificially ventilated beagle dogs a severe hypoglycemic condition was induced by insulin injection, while the posthypoglycemic recovery was induced by glucose treatment at the end of a 20-min period of spontaneous electroencephalographic silence. The motor area of the cerebral cortex was analyzed for glycolytic m...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Benzi G,Gorini A,Dossena M,Taglietti M,Fulle D,Pastoris O

    更新日期:1983-03-15 00:00:00

  • Evaluation of estrogen receptor, antiestrogen binding sites and calmodulin for antiestrogen resistance of two clones derived from the MCF-7 breast cancer cell line.

    abstract::Estrogen receptor (ER), antiestrogen binding sites (AEBS) and calmodulin (CaM) are potential targets of antiestrogen (AE) action. To analyse further which of these targets are primarily involved in the antiproliferative activity of these drugs against human breast cancers, two cell clones, namely the RTx6 and LY-2 var...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Borras M,Jin L,Bouhoute A,Legros N,Leclercq G

    更新日期:1994-11-29 00:00:00

  • HIF-1: master and commander of the hypoxic world. A pharmacological approach to its regulation by siRNAs.

    abstract::The hypoxia-inducible factor-1 (HIF-1) is primarily involved in the sensing and adapting of cells to changes in the O2 level, which is essential for their viability. It is important that this critical transcription factor be tightly regulated in order for cells to respond to a wide range of O2 concentrations. HIF-1 re...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Mazure NM,Brahimi-Horn MC,Berta MA,Benizri E,Bilton RL,Dayan F,Ginouvès A,Berra E,Pouysségur J

    更新日期:2004-09-15 00:00:00

  • Interaction of sanguinarine iminium and alkanolamine form with calf thymus DNA.

    abstract::The interaction of sanguinarine iminium form (structure I) and sanguinarine alkanolamine form (structure II) with calf thymus DNA has been studied in buffer of pH 5.2 and pH 10.5, respectively, where the physicochemical properties of DNA remain unchanged. The binding of sanguinarine iminium form to DNA is characterize...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sen A,Maiti M

    更新日期:1994-11-29 00:00:00

  • Effects of MCI-176, a new quinazolinone calcium antagonist, on myocardial energy and carbohydrate metabolism in ischemic dog hearts.

    abstract::The effect of 2-(2,5-dimethoxyphenylmethyl)-3-(2-dimethylaminoethyl)- 6-isopropoxy-4(3H)-quinazolinone hydrochloride (MCI-176), a calcium antagonist, on ischemic myocardial metabolism was studied in dog hearts subjected to an occlusion of the left anterior descending coronary artery (LAD) for 3 or 30 min. MCI-176 (0.0...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Abe Y,Ichihara K,Abiko Y

    更新日期:1991-02-01 00:00:00