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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/16 18:18:40」(JST)

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Probucol is an anti-hyperlipidemic drug^[1] initially developed in the treatment of coronary artery disease.

However, clinical trials were stopped after it was found that it may lower HDL in patients with a previous history of heart disease.

Probucol was initially developed in the 1970s by a chemical company to maximize airplane tire longevity.

Mechanism[edit]

Probucol lowers the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism. Additionally, probucol may inhibit cholesterol synthesis and delay cholesterol absorption.^[2] Probucol is a powerful antioxidant which inhibits the oxidation of cholesterol in LDLs; this slows the formation of foam cells, which contribute to atherosclerotic plaques.

It is believed to act at ABCA1.^[3]

It also lowers levels of HDL.^[4]

References[edit]

^ Yamamoto A (December 2008). "A Uniqe Antilipidemic Drug - Probucol". J. Atheroscler. Thromb. 15 (6): 304–5. doi:10.5551/jat.E621 . PMID 19075491.
^ "Probucol. Drugs.com web site. [1]
^ Favari E, Zanotti I, Zimetti F, Ronda N, Bernini F, Rothblat GH (December 2004). "Probucol inhibits ABCA1-mediated cellular lipid efflux". Arterioscler. Thromb. Vasc. Biol. 24 (12): 2345–50. doi:10.1161/01.ATV.0000148706.15947.8a . PMID 15514211.
^ Miida T, Seino U, Miyazaki O, et al. (October 2008). "Probucol markedly reduces HDL phospholipids and elevated prebeta1-HDL without delayed conversion into alpha-migrating HDL: putative role of angiopoietin-like protein 3 in probucol-induced HDL remodeling". Atherosclerosis 200 (2): 329–35. doi:10.1016/j.atherosclerosis.2007.12.031 . PMID 18279878.

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English Journal

Structural evaluation of probucol nanoparticles in water by atomic force microscopy.

Moribe K, Limwikrant W, Higashi K, Yamamoto K.SourceGraduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.
International journal of pharmaceutics.Int J Pharm.2012 May 10;427(2):365-71. Epub 2012 Feb 20.
Structural evaluation of probucol nanoparticles coground with polyvinylpyrrolidone K17 and sodium dodecyl sulfate for 90min was performed by solid-state nuclear magnetic resonance (NMR) spectroscopy and atomic force microscopy (AFM) with force-distance curve analysis. The results of solid-state NMR
PMID 22370474

Development of a probucol-releasing antithrombogenic drug eluting stent.

Vedantham K, Chaterji S, Kim SW, Park K.SourceDepartment of Industrial and Physical Pharmacy, Purdue University, West Lafayette, Indiana 47907.
Journal of biomedical materials research. Part B, Applied biomaterials.J Biomed Mater Res B Appl Biomater.2012 May;100(4):1068-77. doi: 10.1002/jbm.b.32672. Epub 2012 Feb 14.
The success of drug eluting stents (DESs) has been challenged by the manifestation of late stent thrombosis after DES implantation. The incomplete regeneration of the endothelial layer poststenting triggers adverse signaling processes precipitating in thrombosis. Various approaches have been attempt
PMID 22331580

Japanese Journal

ニコチン酸誘導体とプロブコール (特集脂質異常症診療のエビデンスと将来展望) -- (脂質異常症の治療薬--エビデンスと選択基凖)

久米典昭
綜合臨床 60(7), 1563-1567, 2011-07
NAID 40018908310

プロブコール-ポリビニルピロリドン固体分散体の安定性

久保儀忠,八木直美,関川彬
YAKUGAKU ZASSHI 131(4), 629-634, 2011
… After solid dispersion systems of probucol-polyvinylpyrrolidone K30 (1 : 9 in weight ratio) were exposed to light (10000 lx) for 7 days, 84% of the probucol remained. … Commercial probucol fine granules were thus fairly stable under light exposure. … When these solid dispersion systems were dissolved in water, the probucol concentration decreased with the duration of storage. …
NAID 130000678844

Related Pictures

★リンクテーブル★

リンク元

「プロブコール」

Probucol
Systematic (IUPAC) name
	4,4'-[propane-2,2-diylbis(thio)]bis(2,6-di-tert-butylphenol)
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a611037
Legal status	?
Identifiers
CAS number	23288-49-5
ATC code	C10AX02
PubChem	CID 4912
DrugBank	DB01599
ChemSpider	4743
UNII	P3CTH044XJ
KEGG	D00476
ChEBI	CHEBI:8427
ChEMBL	CHEMBL608
Synonyms	2,6-di-tert-butyl-4-({2-[(3,5-di-tert-butyl-4-hydroxyphenyl)sulfanyl]propan-2-yl}sulfanyl)phenol
Chemical data
Formula	C31H48O2S2
Mol. mass	516.844 g/mol
	SMILES S(c1cc(c(O)c(c1)C(C)(C)C)C(C)(C)C)C(Sc2cc(c(O)c(c2)C(C)(C)C)C(C)(C)C)(C)C;
	InChI InChI=1S/C31H48O2S2/c1-27(2,3)21-15-19(16-22(25(21)32)28(4,5)6)34-31(13,14)35-20-17-23(29(7,8)9)26(33)24(18-20)30(10,11)12/h15-18,32-33H,1-14H3 ; Key:FYPMFJGVHOHGLL-UHFFFAOYSA-N ;
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　　[★]

英: probucol
商: クラフェデン、サクベルコート、シンレスタール、ダウンオイール、ピヨコール、フッコラート、プロスエード、ライドラース、ロレルコ、ワニール

高脂血症治療薬
家族性高コレステロール血症(FHホモ)にも適応可能
黄色腫・動脈硬化巣の退縮作用がある
強い抗酸化作用→酸化LDL産生を抑制

産生LDLの産生抑制により、マクロファージの貪食を抑制する→CETP活性亢進→コレステロールの逆転送活性化

薬理作用

血症TG↓、血症TC↓
LDL受容体非依存的にLDL異化→胆汁への排泄作用↑

→家族性高コレステロール血症の適応となる

作用機序

副作用

QT延長を伴う心室性不整脈(torsades de pointes)
HDL-C低下作用

CETP活性亢進による

[pmid19075491-1] Yamamoto A (December 2008). "A Uniqe Antilipidemic Drug - Probucol". J. Atheroscler. Thromb. 15 (6): 304–5. doi:10.5551/jat.E621 . PMID 19075491.

[2] "Probucol. Drugs.com web site. [1]

[pmid15514211-3] Favari E, Zanotti I, Zimetti F, Ronda N, Bernini F, Rothblat GH (December 2004). "Probucol inhibits ABCA1-mediated cellular lipid efflux". Arterioscler. Thromb. Vasc. Biol. 24 (12): 2345–50. doi:10.1161/01.ATV.0000148706.15947.8a . PMID 15514211.

[4] Miida T, Seino U, Miyazaki O, et al. (October 2008). "Probucol markedly reduces HDL phospholipids and elevated prebeta1-HDL without delayed conversion into alpha-migrating HDL: putative role of angiopoietin-like protein 3 in probucol-induced HDL remodeling". Atherosclerosis 200 (2): 329–35. doi:10.1016/j.atherosclerosis.2007.12.031 . PMID 18279878.

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案内

案内

probucol