(Z)-正丁烯基苯酞

(Z)-Butylidenephthalide

	产品编号	CFN96106
	CAS编号	72917-31-8
	分子式 = 分子量	C₁₂H₁₂O₂ = 188.2
	产品纯度	>=98%
	物理属性	Oil
	化合物类型	Miscellaneous
	植物来源	The roots of Angelica sinensis
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产品名称	产品编号	CAS编号	包装	QQ客服
(Z)-正丁烯基苯酞	CFN96106	72917-31-8	1mg	QQ客服：215959384
(Z)-正丁烯基苯酞	CFN96106	72917-31-8	5mg	QQ客服：215959384
(Z)-正丁烯基苯酞	CFN96106	72917-31-8	10mg	QQ客服：215959384
(Z)-正丁烯基苯酞	CFN96106	72917-31-8	20mg	QQ客服：215959384

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Description:

(Z)-Butylidenephthalide has antitumor effect, can effectively inhibit the tumor growth in the glioma.

Targets:

PKC

In vitro:

Neuro Oncol. 2011 Jun;13(6):635-48.

Local interstitial delivery of z-butylidenephthalide by polymer wafers against malignant human gliomas.[Pubmed: 21565841 ]

We have shown that the natural compound (Z)-Butylidenephthalide (Bdph), isolated from the chloroform extract of Angelica sinensis, has antitumor effects. Because of the limitation of the blood-brain barrier, the (Z)-Butylidenephthalide dosage required for treatment of glioma is relatively high. To solve this problem, we developed a local-release system with (Z)-Butylidenephthalide incorporated into a biodegradable polyanhydride material, p(CPP-SA; Bdph-Wafer), and investigated its antitumor effects.
METHODS AND RESULTS:
On the basis of in vitro release kinetics, we demonstrated that the (Z)-Butylidenephthalide-Wafer released 50% of the available (Z)-Butylidenephthalide by the sixth day, and the release reached a plateau phase (90% of (Z)-Butylidenephthalide) by the 30th day. To investigate the in situ antitumor effects of the Bdph-Wafer on glioblastoma multiforme (GBM), we used 2 xenograft animal models-F344 rats (for rat GBM) and nude mice (for human GBM)-which were injected with RG2 and DBTRG-05MG cells, respectively, for tumor formation and subsequently treated subcutaneously with (Z)-Butylidenephthalide-Wafers. We observed a significant inhibitory effect on tumor growth, with no significant adverse effects on the rodents. Moreover, we demonstrated that the antitumor effect of (Z)-Butylidenephthalide on RG2 cells was via the PKC pathway, which upregulated Nurr77 and promoted its translocation from the nucleus to the cytoplasm. Finally, to study the effect of the interstitial administration of z-butylidenephthalide in cranial brain tumor, Bdph-Wafers were surgically placed in FGF-SV40 transgenic mice. Our (Z)-Butylidenephthalide-Wafer significantly reduced tumor size in a dose-dependent manner.
CONCLUSIONS:
In summary, our study showed that p(CPP-SA) containing (Z)-Butylidenephthalide delivered a sufficient concentration of Bdph to the tumor site and effectively inhibited the tumor growth in the glioma.

In vivo:

Curr Drug Metab. 2012 Jun 1;13(5):524-34.

Metabolic conversion from co-existing ingredient leading to significant systemic exposure of Z-butylidenephthalide, a minor ingredient in Chuanxiong Rhizoma in rats.[Pubmed: 22554277]

Pharmacokinetic (PK) study of medicinal herbs is a great challenge, because which component(s) is(are) the bioactive ingredients is largely unknown. Most of the reported PK studies of herbs focused on the major ingredients regardless of their in vivo bioactivities, while PK of components with low content in herbs is often ignored.
METHODS AND RESULTS:
The present study demonstrates how PK study can reveal potential importance of a low content ingredient to the herbal bioactivities using (Z)-Butylidenephthalide (BuPh), a bioactive phthalide present in a significantly low quantity in medicinal herb Chuanxiong Rhizoma, as an example. PK of (Z)-Butylidenephthalide was investigated in rats using Chuanxiong extract, fraction containing (Z)-Butylidenephthalide and ligustilide, and pure (Z)-Butylidenephthalide, respectively. The results demonstrated that remarkable blood concentrations of (Z)-Butylidenephthalide were observed after administration of the herbal extract and its systemic exposure was significantly different between (Z)-Butylidenephthalide given in pure and mixed forms. More interestingly, AUC of (Z)-Butylidenephthalide via intake of fraction (9.3-fold) and extract (4.5-fold) was significantly greater than that obtained from pure Z-butylidenephthalide, which was further evidenced to be mainly due to metabolic conversion from ligustilide, a major component in Chuanxiong.
CONCLUSIONS:
Our findings revealed that although it naturally occurred in low amount, (Z)-Butylidenephthalide reached significant systemic concentrations via metabolic conversion from ligustilide.

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	5.3135 mL	26.5675 mL	53.135 mL	106.2699 mL	132.8374 mL
5 mM	1.0627 mL	5.3135 mL	10.627 mL	21.254 mL	26.5675 mL
10 mM	0.5313 mL	2.6567 mL	5.3135 mL	10.627 mL	13.2837 mL
50 mM	0.1063 mL	0.5313 mL	1.0627 mL	2.1254 mL	2.6567 mL
100 mM	0.0531 mL	0.2657 mL	0.5313 mL	1.0627 mL	1.3284 mL

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(Z)-正丁烯基苯酞

(Z)-Butylidenephthalide

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