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Expert Opinion on Drug Metabolism & Toxicology Volume 2, 2006 - Issue 5
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Review

In vitro assays and biomarkers for drug-induced phospholipidosis

David K Monteith Toxicology and ADME Manager, Eli Lilly and Company, Lilly Laboratory for Clinical Research, 550 N University Blvd, Indianapolis, Indiana 46202, USA
,
Ryan E Morgan Scientist, Amgen, Thousand Oaks, CA, USA
&
Bartley Halstead Senior Toxicologist, Eli Lilly and Company, Indianapolis, IN 46202, USA
Pages 687-696 | Published online: 03 Oct 2006

Bibliography

  • HALLIWELL WH: Cationic amphiphilic drug-induced phospholipidosis. Toxicol. Pathol. (1997) 25(1):53-60.
  • HOSTETLER KY: Molecular studies of the induction of cellular phospholipidosis by cationic amphiphilic drugs. Fed. Proc. (1984) 43(11):2582-2585.
  • JOSHI UM, RAO P, KODAVANTI S, LOCKARD VG, MEHENDALE HM: Fluorescence studies on binding of amphiphilic drugs to isolated lamellar bodies: relevance to phospholipidosis. Biochim. Biophys. Acta (1989) 1004(3):309-320.
  • KODAVANTI UP, MEHENDALE HM: Cationic amphiphilic drugs and phospholipid storage disorder. Pharmacol. Rev. (1990) 42(4):327-354.
  • LAURENT G, CARLIER MB, ROLLMAN B, VAN HOOF F, TULKENS P: Mechanism of aminoglycoside-induced lysosomal phospholipidosis: in vitro and in vivo studies with gentamicin and amikacin. Biochem. Pharmacol. (1982) 31(23):3861-3870.
  • LULLMANN-RAUCH R, WATERMANN D: Fusion of storage lysosomes in experimental lipidosis and glycogenosis. Exp. Mol. Pathol. (1987) 46(1):136-143.
  • REASOR MJ: A review of the biology and toxicologic implications of the induction of lysosomal lamellar bodies by drugs. Toxicol. Appl. Pharmacol. (1989) 97(1):47-56.
  • REASOR MJ, HOSTETLER KY: Chloroquine treatment does not cause phospholipid storage by depleting rat liver lysosomes of acid phospholipase A. Biochim. Biophys. Acta (1984) 793(3):497-501.
  • REASOR MJ, KACEW S: Drug-induced phospholipidosis: are there functional consequences? Exp. Biol. Med. (Maywood) (2001) 226(9):825-830.
  • RUBEN Z, RORIG KJ, KACEW S: Perspectives on intracellular storage and transport of cationic-lipophilic drugs. Proc. Soc. Exp. Biol. Med. (1993) 203(2):140-149.
  • REASOR MJ, HASTINGS KL, ULRICH RG: Drug-induced phospholipidosis: issues and future directions. Expert Opin. Drug Saf. (2006) 5:567-583.
  • LULLMANN-RAUCH R: Histochemical evidence for lysosomal storage of acid glycosaminoglycans in splenic cells of rats treated with tilorone. Histochemistry (1982) 76(1):71-87.
  • KALOYANIDES GJ: Drug-phospholipid interactions: role in aminoglycoside nephrotoxicity. Ren. Fail. (1992) 14(3):351-357.
  • MASSEY TE, LEEDER RG, RAFEIRO E, BRIEN JF: Mechanisms in the pathogenesis of amiodarone-induced pulmonary toxicity. Can. J. Physiol. Pharmacol. (1995) 73(12):1675-1685.
  • MONTENEZ JP, VAN BAMBEKE F, PIRET J et al.: Interactions of macrolide antibiotics (erythromycin A, roxithromycin, erythromycylamine [dirithromycin], and azithromycin) with phospholipids: computer-aided conformational analysis and studies on acellular and cell culture models. Toxicol. Appl. Pharmacol. (1999) 156(2):129-140.
  • CASARTELLI A, BONATO M, CRISTOFORI P et al.: A cell-based approach for the early assessment of the phospholipidogenic potential in pharmaceutical research and drug development. Cell Biol. Toxicol. (2003) 19(3):161-176.
  • CRAMER CT, ULRICH RG: Cytotoxicity and lamellar body induction potential of a racemic benzamide antiarrhythmic compound and enantiomers in cultured rat hepatocytes. Toxicol. In Vitro (1994) 8(5):1083-1090.
  • GUM RJ, HICKMAN D, FAGERLAND JA et al.: Analysis of two matrix metalloproteinase inhibitors and their metabolites for induction of phospholipidosis in rat and human hepatocytes(1). Biochem. Pharmacol. (2001) 62(12):1661-1673.
  • MCMILLIAN MK, GRANT ER, ZHONG Z et al.: Nile red binding to HepG2 cells: an improved assay for in vitro studies of hepatosteatosis. In Vitr. Mol. Toxicol. (2001) 14(3):177-190.
  • ULRICH RG, KILGORE KS, SUN EL, CRAMER CT, GINSBERG LC: An in vitro fluorescence assay for the detection of drug-induced cytoplasmic lamellar bodies. Toxicol Methods (1991) 1(2):89-105.
  • XIA Z, APPELKVIST EL, DEPIERRE JW, NASSBERGER L: 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. Biochem. Pharmacol. (1997) 53(10):1521-1532.
  • SAWADA H, TAKAMI K, ASAHI S: A toxicogenomic approach to drug-induced phospholipidosis: analysis of its induction mechanism and establishment of a novel in vitro screening system. Toxicol. Sci. (2005) 83:282-292.
  • PLOEMEN JP, KELDER J, HAFMANS T et al.: Use of physicochemical calculation of pKa and cLogP to predict phospholipidosis-inducing potential: a case study with structurally related piperazines. Exp. Toxicol. Pathol. (2004) 55(5):347-355.
  • VALKO K, DU CM, BEVAN CD, REYNOLDS DP, ABRAHAM MH: Rapid-gradient HPLC method for measuring drug interactions with immobilized artificial membrane: comparison with other lipophilicity measures. J. Pharm. Sci. (2000) 89(8):1085-1096.
  • GERBAUX C, VAN BAMBEKE F, MONTENEZ JP et al.: Hyperactivity of cathepsin B and other lysosomal enzymes in fibroblasts exposed to azithromycin, a dicationic macrolide antibiotic with exceptional tissue accumulation. FEBS Lett. (1996) 394(3):307-310.
  • AMACHER DE, MARTIN BA: Tetracycline-induced steatosis in primary canine hepatocyte cultures. Fundam. Appl. Toxicol. (1997) 40(2):256-263.
  • RORIG KJ, RUBEN Z, ANDERSON SN: Structural determinants of cationic amphiphilic amines which induce clear cytoplasmic vacuoles in cultured cells. Proc. Soc. Exp. Biol. Med. (1987) 184(2):165-171.
  • RUBEN Z, ANDERSON SN, KACEW S: Changes in saccharide and phospholipid content associated with drug storage in cultured rabbit aorta muscle cells. Lab. Invest. (1991) 64(4):574-584.
  • VAN BAMBEKE F, GERBAUX C, MICHOT JM et al.: Lysosomal alterations induced in cultured rat fibroblasts by long-term exposure to low concentrations of azithromycin. J. Antimicrob. Chemother. (1998) 42(6):761-767.
  • HOSTETLER KY, VANDE BERG J, ALDERN KA, BROPHY GT: Effect of amiodarone on the phospholipid and lamellar body content of lymphoblasts in vitro and peripheral blood lymphocytes in vivo. Biochem. Pharmacol. (1991) 41:1007-1013.
  • KASAHARA T, TOMITA K, MURANO H et al.: Establishment of an in vitro high-throughput screening assay for detecting phospholipidosis-inducing potential. Toxicol. Sci. (2006) 90:133-141.
  • MORELLI JK, BUEHRLE M, POGNAN F et al.: Validation of an in vitro screen for phospholipidosis using a high-content biology platform. Cell Biol. Toxicol. (2006) 22:15-27.
  • SUN M, ZHAO C, GFESSER GA et al.: Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency. J. Med. Chem. (2005) 48:6482-6490.
  • LULLMANN-RAUCH R: Experimental mucopolysaccharidosis: preservation and ultrastructural visualization of intralysosomal glycosaminoglycans by use of the cationic dyes cuprolinic blue and toluidine blue. Histochemistry (1989) 93(2):149-154.
  • LULLMANN-RAUCH R, MICHEL G, PETERS A: Mucopolysaccharidosis-like cellular alterations in chondrocytes of rats treated with tilorone. Exp. Mol. Pathol. (1988) 49(2):279-289.
  • BROWN WJ, SULLIVAN TR, GREENSPAN P: Nile red staining of lysosomal phospholipid inclusions. Histochemistry (1992) 97:349-354.
  • HALSTEAD B, ZWICKL CM, MORGAN RE et al.: A clinical flow cytometric biomarker strategy: validation of peripheral leukocyte phospholipidosis using Nile red. J. Appl. Toxicol. (2006) 26:169-177.
  • MORGAN RE, KRIAUCIUNAS A, BERRIDGE B, SULLIVAN J, MONTEITH D: An in vitro surrogate for drug-induced phospholipidosis. Toxicologist (2004) 78(S-1):388.
  • DAKE MD, MADISON JM, MONTGOMERY CK et al.: Electron microscopic demonstration of lysosomal inclusion bodies in lung, liver, lymph nodes, and blood leukocytes of patients with amiodarone pulmonary toxicity. Am. J. Med. (1985) 78(3):506-512.
  • RUDMANN DF, MCNERNEY ME, VANDEREIDE SL et al.: Epididymal and systemic phospholipidosis in rats and dogs treated with the dopamine D3 selective antagonist PNU-177864. Toxicol. Pathol. (2004) 32:326-336.
  • LULLMANN-RAUCH R, NASSBERGER L: Citalopram-induced generalized lipidosis in rats. Acta Pharmacol. Toxicol. (Copenh) (1983) 52(3):161-167.
  • DELANEY J, NEVILLE WA, SWAIN A et al.: Phenylacetyl glycine, a putative biomearker of phospholipidosis: its origins and relevance to phospholipids accumulation using amiodarone treated rats as a model. Biomarker (2004) 9:271-290.
  • ESPINA JR, SHOCKCOR JP, HERRON W, AL E: Detection of in vivo biomarkers of phospholipidosis using NMR-based metabonomic approaches. Magn. Reson. Chem. (2001) 39:559-565.
  • BOLLARD ME, STANLEY EG, LINDON JC, NICHOLSON JK, HOLMES E: NMR-based metabonomic approaches for evaluating physiological influences on biofluid composition. NMR Biomed. (2005) 18:143-162.
  • MORTUZA GB, NEVILLE WA, DELANEY J, WATERFIELD CJ, CAMILLERI P: Characterisation of a potential biomarker of phospholipidosis from amiodarone-treated rats. Biochim. Biophys. Acta (2003) 1631(2):136-146.
  • MARTIN WJ, STANDING JE: Amiodrone pulmonary toxicity: biochemical evidence for a cellular PLD in the bronchoalveolar lavage of human subjects. J. Pharmacol. Exp. Ther. (1988) 244:774-779.

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