26791-73-1
26791-73-1 結(jié)構(gòu)式
基本信息
蒼耳亭對(duì)照品
蒼耳亭(反式)
蒼耳亭(標(biāo)準(zhǔn)品)
(3aR)-3-Methylene-7β-methyl-6-(3-oxo-1-butenyl)-3,3aα,4,7,8,8aβ-hexahydro-2H-cyclohepta[b]furan-2-one
(3aR)-3,3aα,4,7,8,8aβ-Hexahydro-7β-methyl-3-methylene-6-(3-oxo-1-butenyl)-2H-cyclohepta[b]furan-2-one
(3aR,7S,8aS)-7-methyl-3-methylidene-6-[(E)-3-oxobut-1-enyl]-4,7,8,8a-tetrahydro-3aH-cyclohepta[b]furan-2-one
2H-Cyclohepta[b]furan-2-one,3,3a,4,7,8,8a-hexahydro-7-Methyl-3-Methylene-6-(3-oxo-1-buten-1-yl)-,(3aR,7S,8aS)-
(3aR,7S,8aS)-7-methyl-3-methylidene-6-[(1E)-3-oxobut-1-en-1-yl]-3,3a,4,7,8,8a-hexahydro-2H-cyclohepta[b]furan-2-one
2H-Cyclohepta[b]furan-2-one, 3,3a,4,7,8,8a-hexahydro-7-methyl-3-methylene-6-[(1E)-3-oxo-1-buten-1-yl]-, (3aR,7S,8aS)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
蒼耳亭（標(biāo)準(zhǔn)品）用于含量測(cè)定、鑒別、藥理實(shí)驗(yàn)、活性篩選等。
蒼耳子的毒性源于其富含的倍半帖內(nèi)酯類(lèi)化合物,這類(lèi) 成分常含有α,β不飽和y內(nèi)酯結(jié)構(gòu),是其生物活性的一個(gè)主要基團(tuán)。研究表明，從蒼耳屬(Xanthium L.)植物(如蒼耳 子)中提取得到的倍半黏內(nèi)酯化合物蒼耳亭( Xanthatin),在 體內(nèi)外實(shí)驗(yàn)中均顯示出較強(qiáng)的抗腫瘤活性,其對(duì)非小細(xì)胞肺 癌的生長(zhǎng)存在顯著的抑制作用,且對(duì)正常肺上皮細(xì)胞生長(zhǎng)影響較小。
IC50: apoptosis; 3.8 μM (VEGFR2 kinase); 2.63?μg/mL ( T. b. brucei )
Xanthatin?is against T. b. brucei with an?IC 50 value of 2.63?μg/mL and exhibits weak irreversible inhibition of parasite specific trypanothione reductase.Xanthatin (0-40 μM; 24 hours) has obscure inhibition effect on the proliferation of HUVEC in the absence of VEGF.Xanthatin (5-40 μM; 24 hours) inhibits breast cancer cell proliferation in a dose responsive manner. Xanthatin inhibits HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 with IC 50 values of 81 μM, 31 μM, 38 μM, 30 μM, and 17 μM, respectively.Xanthatin (0-10 μM; 24 hours) dose dependently suppresses the phosphorylation of STAT3 (Ser727), at the same time, it also results in a rapid dephosphorylation of down-stream kinases of STAT3, including PI3K and Akt, including PI3K (p-PI3K p85 tyr458 ) and Akt.
Cell Proliferation Assay
| Cell Line: | HUVEC cells |
| Concentration: | 0 μM, 5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited cell growth from dose 10 μM in the presence of vEGF. |
Cell Viability Assay
| Cell Line: | HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 cells |
| Concentration: | 5, 10, 15, 20, 30, and 40 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited breast cancer cell growth. |
Western Blot Analysis
| Cell Line: | HUVEC cells |
| Concentration: | 0, 3, and 10 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited VEGFR2 downstream signaling pathways and blocked VEGF-induced STAT3 activation in HUVEC. |
Xanthatin (intragastric administration; 20 mg/kg; once daily; 25 days) leads to significant inhibition of tumor volume. And this compound is well-tolerated and exhibits no significant difference in weight compares to the vehicle group.
| Animal Model: | Transplanted MDA-MB-231 cells into mice and constucted human breast cancer xenograft mouse model |
| Dosage: | 20 mg/kg; once daily; 25 days |
| Administration: | Intragastric administration |
| Result: | Supressed tumor growth and tumor angiogenesis in vivo. |