480-19-3
480-19-3 結(jié)構(gòu)式
基本信息
異鼠李素
3,5,7-TRIHYDROXY-2-(4-HYDROXY-3-METHOXYPHENYL)-4-BENZOPYRONE
3,5,7-trihydroxy-2-(4-hydroxy-3-methoxyphenyl)-4h-1-benzopyran-4-one
3,5,7-trihydroxy-2-(4-hydroxy-3-metoxyphenyl)benzopyran-4-on
3'-METHOXY-3,4',5,7-TETRAHYDROXYFLAVONE
3'-METHOXY-3,5,7,4'-TETRAHYDROXYFLAVONE
3-METHYLQUERCETIN
ISOHAMNETIN
ISORHAMNETIN
2-(3-methoxy-4-hydroxyphenyl)-3,5,7-trihydroxy-4h-1-benzopyran-4-on
3,4’,5,7-tetrahydroxy-3’-methoxy-flavon
3,5,7-trihydroxy-2-(4-hydroxy-3-methoxyphenyl)-4h-1-benzopyran-4-on
3’-methoxy-3,4’,5,7-tetrahydroxy-flavon
3’-methoxyquercetin
c.i.75680
isorhamnetol
ISOHAMNETIN:3'-METHOXY-3,4',5,7-TETRAHYDRO-XY-FLAVONE
3,5,7-trihydroxy-2-(4-hydroxy-3-methoxy-phenyl)chromen-4-one
QUERCETIN-3-METHYLETHER
QUERCETIN-3-ORTHO-METHYLETHER
物理化學(xué)性質(zhì)
常見問題列表
圖1為異鼠李素
1.胡頹子科：植物沙棘Hippophae fhamnoides L.的果實(shí)。
2.蘿藦科 (Asclepiadaceae)：臺(tái)灣眼樹蓮Dischidia formosana maxim.全草。
3.紫葳科 (Bingoniaceae)：黃鐘花 Tecoma stans H. B. K.花。
4.衛(wèi)矛科(Celastraceae)：微缺美登木Maytenus emarginata Willd. 葉。
5.菊科(Compositae)：長葉山金車Arnica longifolia D.C.Eaton花；黃花蒿 Artemisia annua L.葉，莖：茵陳蒿 Artemisia capillaris Thunb.
6.葫蘆科 (Cucurbitaceae)：喙果絞股蘭 Gynostemma yixingense C. Y. Wu et S. K. Chen地上部分。
7.豆科 (Leguminosae)：槐Sophora?japonica L.花蕾；紅車軸草 Trifolium pratense L.花瓣。
8.無患子科(Sapindaceae)：車桑子 Dodonaea viscosa (L.) Jacq.花。
9.檉柳科(Tamaricaceae)：西河柳Tamarix chinensis Lour.枝。
10.紅豆杉科(Taxaceae)：短葉紅豆杉Taxus brevifolia Nutt.葉。
11.椴樹科(Tiliaceae)：布渣葉Microcos paniculata L.
12.香蒲科(Typhaceae)：長苞香蒲Typha angustata Bory et Chaub.；狹葉香蒲 Typha angustifolia L.
13.傘形科(Umbelliferae)：秦嶺柴胡Bupleurum longicaule Wall. ex DC. var. giraldii Wolff全植物；水芹Oenanthe javanica.
14.蒺藜科(Zygophyllaceae)：甘青白刺N(yùn)itraria tangutorum Bolor種子。
2.抑制血小板聚集。
3.抗止血作用。抑制某些止血成分的作用。
4.抗肝毒成分。對CCl4和GalN誘導(dǎo)的大鼠肝細(xì)胞中毒有抑制作用。5.V9Z：調(diào)節(jié)雄性植物的繁殖能力。
6.降低大鼠血清和肝臟的膽固醇濃度。
7.抗脂質(zhì)過氧化。降低大鼠肝臟中硫代巴比妥酸反應(yīng)物質(zhì)TBARS的量。
8.抗腫瘤作用，異鼠李素主要是抑制腫瘤細(xì)胞增殖，誘導(dǎo)細(xì)胞凋亡、抑制信號(hào)轉(zhuǎn)導(dǎo)等。，異鼠李素具有顯著的抗乳腺癌作用，其作用機(jī)制與抑制細(xì)胞的增殖通路及促進(jìn)細(xì)胞的凋亡有關(guān)。
精確秤取1.0 g 左右的沙棘果渣→加入提取液→超聲波提取→過濾→濾液定容→異鼠李素
沙棘果渣中異鼠李素的最佳工藝為：在50℃條件下，超聲頻率40 kHz，用V 乙酸乙酯︰V95%乙醇為4:6 的提取液超聲提取2 次，每次1 h，料液比為1:25。以此方法提取所得異鼠李素含量可達(dá)5.09 mg·g-1。
化學(xué)合成法：以槲皮素（Ⅰ）為起始原料經(jīng)乙酰化，芐基化和甲基化反應(yīng)分別獲得槲皮素五乙酸酯（Ⅱ）和4’,7-二-O-芐基槲皮素（Ⅲ），4’,7-二-O-芐基槲皮素三乙酸酯（Ⅳ）和4’,7-二-O-芐基-3’-甲基槲皮素（Ⅴ）中間體。化合物（Ⅴ）經(jīng)芐基化反應(yīng)則得到異鼠李素（Ⅵ）。
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PI3-K
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MEK1
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Human Endogenous Metabolite
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Isorhamnetin is a plant flavonoid that occurs in fruits and medicinal herbs. Isorhamnetin binds directly to MEK1 in an ATP-noncompetitive manner and to PI3-K in an ATP-competitive manner. In vitro and ex vivo kinase assay data show that Isorhamnetin inhibits the kinase activity of MAP/ERK kinase (MEK) 1 and PI3-K and the inhibition is due to direct binding with Isorhamnetin. Isorhamnetin inhibits the Akt/mTOR and MEK/ERK signaling pathways, and promotes the activity of the mitochondrial apoptosis signaling pathway. The inhibitory effects of Isorhamnetin on breast cancer cells are determined using the CCK-8 method. Isorhamnetin inhibits the proliferation of numerous breast cancer cells (IC 50 , ~10 μM), including MCF7, T47D, BT474, BT-549, MDA-MB-231 and MDA-MB-468, whereas less inhibitory activity is observed in the MCF10A normal breast epithelial cell line (IC 50 , 38 μM).
Photographic data shows that Isorhamnetin treatment suppresses tumor development in mice. The average volume of tumors in untreated mice increases over time and reaches a volume of 623 mm 3 at 4 weeks post-inoculation; however, at this time, in mice treated with 1 or 5 mg/kg Isorhamnetin, the average tumor volume is only 280 or 198 mm 3 , respectively. At the end of the study, Isorhamnetin treatment (1 or 5 mg/kg) reduces tumor weight compared with the untreated control group.