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981-15-7

中文名稱 臭椿酮
英文名稱 ailanthone
CAS 981-15-7
分子式 C20H24O7
分子量 376.403
MOL 文件 981-15-7.mol
更新日期 2024/12/18 02:46:25
981-15-7 結構式 981-15-7 結構式

基本信息

中文別名
臭椿酮
臭椿酮對照品
臭椿酮(臭椿苦酮)
AILANTHONE 臭椿酮
英文別名
ailanthone
Δ13-Dehydrochaparrinone
13,21-Didehydrochaparrinone
11β,20-Epoxy-1β,11,12α-trihydroxypicrasa-3,13(21)-diene-2,16-dione
(1β,11β,12α)-11,20-Epoxy-1,11,12-trihydroxypicrasa-3,13(21)-diene-2,16-dione
Picrasa-3,13(21)-diene-2,16-dione,11,20-epoxy-1,11,12-trihydroxy-, (1b,11b,12a)-
Picrasa-3,13(21)-diene-2,16-dione, 11,20-epoxy-1,11,12-trihydroxy-, (1β,11β,12α)-
所屬類別
天然產物:萜類

物理化學性質

熔點235-237 °C
沸點641.0±55.0 °C(Predicted)
密度1.47
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度DMSO:100.0(Max Conc. mg/mL);265.67(Max Conc. mM)
酸度系數(pKa)11.85±0.70(Predicted)
形態(tài)結晶固體
顏色White to off-white
LogP-0.760 (est)

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H300

常見問題列表

植物提取物
臭椿酮是一種植物提取物,是從臭椿皮中提取出來的一種物質,具有抗菌、抗原蟲及抗腫瘤作用,100%煎劑在體外對福氏痢疾桿菌、宋氏痢疾桿菌和大腸桿菌有抑制作用。對阿米巴原蟲與陰道滴蟲有強烈的抑制作用,并能抑制其它寄生蟲的活動,煎液與鞣質有收斂、止血作用。
臭椿酮對人體鼻咽癌(KB)細胞有細胞毒活性,其ED50為10-2-10-3ug/ml在0.12-4.00mg/kg劑量時,對淋巴細胞白血病P388顯示一定活性。
臭椿皮為植物苦木科臭椿的根皮或樹皮。主產於山東省、遼寧省、河南省、安徽省等地。春夏采挖,除去栓皮,切片,曬干,生用,亦用鮮品。
制備方法
取臭椿新鮮樹皮或者新鮮根皮,加入其質量5-10倍量體積pH=9-13的堿水浸泡24-72小時,濾過,濾液用酸調節(jié)pH至中性,濃縮,濃縮液通過大孔吸附樹脂柱吸附,水洗脫除雜,60-85%乙醇洗脫,收集3-8倍量柱體積洗脫液,減壓回收乙醇至盡,冷藏12-36小時析晶,濾過,取濾渣,加入丙酮重結晶,洗滌、干燥即得臭椿酮。
生物活性
Ailanthone (AIL, Δ13-Dehydrochaparrinone) 是一種來自臭椿Ailanthus altissima的天然通過抗肝癌(HCC)成分,可通過降低 cyclins 和 CDKs 的表達、提高 p21 和 p27 的表達來誘導G0/G1期細胞周期阻滯。Ailanthone 可觸發(fā)DNA損傷,其特征為 ATM/ATR 通路的激活。Ailanthone 可在Huh7細胞中誘導線粒體介導、涉及 PI3K/AKT 信號通路的細胞凋亡。Ailanthone 也是全長 Androgen Receptor (AR-FL)和組成型活性截斷AR剪接變體(AR-Vs, AR1-651)的抑制劑,對應的IC50值分別為69 nM和309 nM。
靶點
TargetValue
CDK
()
AR-FL
(Cell-free assay)
69 nM
AR 1-651
(Cell-free assay)
309 nM
體外研究

Ailanthone is a potent inhibitor of both full-length AR (AR-FL) and constitutively active truncated AR splice variants (AR-Vs). Ailanthone binds to the co-chaperone protein p23 and prevents AR's interaction with HSP90, thus resulting in the disruption of the AR-chaperone complex followed by ubiquitin/proteasome-mediated degradation of AR as well as other p23 clients including AKT and Cdk4, and downregulates AR and its target genes in PCa cell lines and orthotopic animal tumours. In addition, Ailanthone blocks tumour growth and metastasis of CRPC. Ailanthone has been shown to possess an growth-inhibitory effect against several cancer cell lines including HepG2, Hep3B, R-HepG2, Jurkat, HeLa, MCF-7, MDA-MB-231 and A549 cells. Ailanthone inhibits Huh7 cell growth through the induction of mitochondrion-mediated cell apoptosis and G0/G1 cell cycle arrest. Ailanthone-induced apoptosis is mitochondrion-mediated and involved the PI3K/AKT signaling pathway in Huh7 cells.

體內研究

Not only i.p. administration but also p.o. administration of Ailanthone has excellent efficiency for blocking the growth of CRPC xenografts. In pharmacokinetic studies, Ailanthone exhibits good solubility in water and good bioavailability (>20%). In addition, Ailanthone effectively suppresses CRPC tumour growth, despite not reaching a steady state of plasma drug concentration during the course of treatment.

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