sofalcone

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/25 18:49:07」(JST)

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Sofalcone

Systematic (IUPAC) name
[5-[(3-methylbut-2-en-1-yl)oxy]-2-((2E)-3-{4-[(3-methylbut-2-en-1-yl)oxy]phenyl}prop-2-enoyl)phenoxy]acetic acid
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ (Prescription only)
Routes of administration	Oral
Identifiers
CAS Registry Number	64506-49-6 Y
ATC code	None
PubChem	CID: 5282219
ChemSpider	4445402 N
UNII	2B668TJX8E Y
KEGG	D01956 Y
Chemical data
Formula	C27H30O6
Molecular mass	450.52 g/mol
SMILES CC(=CCOC1=CC=C(C=C1)C=CC(=O)C2=C(C=C(C=C2)OCC=C(C)C)OCC(=O)O)C
InChI InChI=1S/C27H30O6/c1-19(2)13-15-31-22-8-5-21(6-9-22)7-12-25(28)24-11-10-23(32-16-14-20(3)4)17-26(24)33-18-27(29)30/h5-14,17H,15-16,18H2,1-4H3,(H,29,30)/b12-7+  N Key:GFWRVVCDTLRWPK-KPKJPENVSA-N  N
N (what is this?)  (verify)

Sofalcone (INN) is an oral gastrointestinal medication. It is a synthetic derivative of sophoradin, a chalconoid, a type of natural phenol found in Sophora tonkinensis (or Sophora subprostrata), a herb used in traditional Chinese medicine.

References

English Journal

• Irsogladine maleate, a gastric mucosal protectant, suppresses intestinal polyp development in Apc-mutant mice.

• Onuma W1,2, Tomono S3, Miyamoto S1, Fujii G4, Hamoya T1, Fujimoto K5, Miyoshi N3, Fukai F2, Wakabayashi K3, Mutoh M1,4.
• Oncotarget.Oncotarget.2016 Feb 23;7(8):8640-52. doi: 10.18632/oncotarget.7082.
• This study aimed to identify gastric mucosal protectants that suppress intestinal tumorigenesis in a mouse model. We chose six gastric mucosal protectants (ecabet sodium hydrate, irsogladine maleate, rebamipide, sofalcone, teprenone and troxipide) and examined their effects on the activity of oxidat
• PMID 26840084

• Sofalcone upregulates the nuclear factor (erythroid-derived 2)-like 2/heme oxygenase-1 pathway, reduces soluble fms-like tyrosine kinase-1, and quenches endothelial dysfunction: potential therapeutic for preeclampsia.

• Onda K1, Tong S1, Nakahara A1, Kondo M1, Monchusho H1, Hirano T1, Kaitu'u-Lino T1, Beard S1, Binder N1, Tuohey L1, Brownfoot F1, Hannan NJ2.
• Hypertension (Dallas, Tex. : 1979).Hypertension.2015 Apr;65(4):855-62. doi: 10.1161/HYPERTENSIONAHA.114.04781. Epub 2015 Feb 9.
• Preeclampsia is a severe complication of pregnancy, characterized by hypertension, oxidative stress, and severe endothelial dysfunction. Antiangiogenic factors, soluble fms-like tyrosine kinase-1 (sFlt-1) and soluble endoglin, play key pathophysiological roles in preeclampsia. Heme oxygenase-1 (HO-1
• PMID 25667213

• "Gastric cytoprotection" is still relevant.

• Szabo S1.
• Journal of gastroenterology and hepatology.J Gastroenterol Hepatol.2014 Dec;29 Suppl 4:124-32. doi: 10.1111/jgh.12735.
• Although Andre Robert's historic article on "gastric cytoprotection" in 1979 introduced this new name and concept, gastroprotective drugs (e.g. sofalcone, sucralfate), which prevent and/or accelerate healing of gastric ulcers without inhibiting acid secretion, were known in Japan before or around th
• PMID 25521744

Japanese Journal

• Influence of Aging on Gastric Cytoprotective and Ulcer Healing Activities of Sofalcone

• ISHIHARA Masashi,KOJIMA Ryoji,ITO Mikio
• 応用薬理 80(5), 71-77, 2011-08-10
• NAID 10029468235

• P1-503 消化性潰瘍治療薬sofalconeは脂肪細胞とマクロファージの炎症性相互作用を改善し脂肪前駆細胞の分化を抑制する(一般演題 ポスター発表,薬物療法(その他),医療薬学の創る未来 科学と臨床の融合)

• 恩田 健二,田中 秀明,中村 星斗,田崎 智也,平野 俊彦
• 日本医療薬学会年会講演要旨集 19, 376, 2009-09-15
• NAID 110007485139

• Analysis of sofalcone in human plasma by high performance liquid chromatography

• WEN Aidong,WANG Zhipeng,HANG Taijun,JIA Yanyan,ZHANG Tingting,WU Yin,GAO Xuan,YANG Zhifu
• Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 856(1), 348-352, 2007-09-01
• NAID 10025808252

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関

消化性潰瘍用剤

• 抗潰瘍薬;胃プロスタグランジン増加