3'-去甲川陈皮素

3'-Demethylnobiletin

	产品编号	CFN93130
	CAS编号	112448-39-2
	分子式 = 分子量	C₂₀H₂₀O₈ = 388.37
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Flavonoids
	植物来源	The peels of Citrus nobilis Lour.
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产品名称	产品编号	CAS编号	包装	QQ客服
3'-去甲川陈皮素	CFN93130	112448-39-2	1mg	QQ客服：1413575084
3'-去甲川陈皮素	CFN93130	112448-39-2	5mg	QQ客服：1413575084
3'-去甲川陈皮素	CFN93130	112448-39-2	10mg	QQ客服：1413575084
3'-去甲川陈皮素	CFN93130	112448-39-2	20mg	QQ客服：1413575084

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Description:

3'-Demethylnobiletin has chemopreventive effects on colon carcinogenesis, it can significantly inhibit the growth of human colon cancer cells, cause cell-cycle arrest, induce apoptosis, and profoundly modulate signaling proteins related with cell proliferation and cell death. It significantly suppresses CD36 expression.

Targets:

LDL | LOX | AP-1 | NF-kB

In vitro:

Biofactors. 2007;31(2):107-16.

Suppressive effects of demethylated metabolites of nobiletin on phorbol ester-induced expression of scavenger receptor genes in THP-1 human monocytic cells.[Pubmed: 18806314]

Unregulated uptake of oxidized low-density lipoproteins (ox-LDL) via macrophage scavenger receptors (SRs) is a key event in atherosclerosis. We previously reported that nobiletin (NOB), a citrus polymethoxylated flavone, markedly reduced 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced SRs and adhesion molecules mRNA expression and blockade of DiI-acLDL uptake in THP-1 human monocyte-like cells.
METHODS AND RESULTS:
In this study, we examined the effects of NOB metabolites, 3'-hydroxy-5,6,7,8,4'-pentamethoxyflavone (3'-demethyl-NOB,3'-Demethylnobiletin ), 4'-hydroxy-5,6,7,8,3'-pentamethoxyflavone (4'-demethyl-NOB) and 3', 4'-dihydroxy-5,6,7,8,-tetramethoxyflavone (3', 4'-didemethyl-NOB) and NOB analog, tangeretin, on SRs and adhesion molecules mRNA expression. 3'-Demethyl-NOB(3'-Demethylnobiletin ) significantly suppressed CD36 expression, moreover, 4'-demethyl- and 3', 4'-didemethyl-NOB significantly suppressed TPA-induced expression of SR-A and LOX-1. Further, the suppressive effects of 4'-demethyl- and 3', 4'-didemethyl-NOB on the expression of CD36 mRNA were greater extent than parent NOB. The inhibitory effects of the metabolites toward TPA-induced SR mRNA expression are partly associated with the suppression of AP-1 and NF-kappaB transcriptional activities.
CONCLUSIONS:
Together, our results suggest that metabolites of NOB, such as 4'-demethyl- and 3', 4'-didemethyl-NOB, have comparable or higher potentials to attenuate SR expression than NOB.

In vivo:

Mol Nutr Food Res. 2015 Dec;59(12):2383-94.

Chemopreventive effects of nobiletin and its colonic metabolites on colon carcinogenesis.[Pubmed: 26445322 ]

Nobiletin (NBT) is a major citrus flavonoid with various health benefits. Herein, we investigated the colon cancer chemopreventive effects of NBT and its colonic metabolites in a colitis-associated colon carcinogenesis mouse model as well as in human colon cancer cell models.
METHODS AND RESULTS:
In azoxymethane/dextran sulfate sodium treated mice, oral administration of NBT effectively decreased both incidence and multiplicity of colonic tumors. NBT showed significant antiproliferative, proapoptotic, and anti-inflammatory effects in the mouse colon. HPLC analysis revealed that oral administration of NBT resulted in high levels of metabolites, i.e. 3'-Demethylnobiletin (M1), 4'-demethylnobiletin (M2), and 3',4'-didemethylnobiletin (M3) in the colonic mucosa. In contrast, the colonic level of NBT was about 20-fold lower than the total colonic level of three metabolites. Cell culture studies demonstrated that the colonic metabolites of NBT significantly inhibited the growth of human colon cancer cells, caused cell-cycle arrest, induced apoptosis, and profoundly modulated signaling proteins related with cell proliferation and cell death. All of these effects were much stronger than those produced by NBT alone.
CONCLUSIONS:
Our results demonstrated that oral administration of NBT significantly inhibited colitis-associated colon carcinogenesis in mice, and this chemopreventive effect was strongly associated with its colonic metabolites.

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.5749 mL	12.8743 mL	25.7486 mL	51.4973 mL	64.3716 mL
5 mM	0.515 mL	2.5749 mL	5.1497 mL	10.2995 mL	12.8743 mL
10 mM	0.2575 mL	1.2874 mL	2.5749 mL	5.1497 mL	6.4372 mL
50 mM	0.0515 mL	0.2575 mL	0.515 mL	1.0299 mL	1.2874 mL
100 mM	0.0257 mL	0.1287 mL	0.2575 mL	0.515 mL	0.6437 mL

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3'-去甲川陈皮素

3'-Demethylnobiletin

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