189453-10-9
189453-10-9 結(jié)構(gòu)式
基本信息
埃博霉素
埃博霉素D
埃坡西龍 D
埃博霉素D 埃坡西龍 D
埃博霉素 D(埃坡西龍 D、埃博霉素D、愛博霉素D)
KOS 862
NSC 703147
Epothilone D
Desoxyepothilone B
12,13-Desoxyepothilone B
(4S,7R,8S,9S,13Z,16S)-4,8-Dihydroxy-5,5,7,9,13-pentaMethyl-16-[(1E)-1-Methyl-2-(2-Methyl-4-thiazolyl)ethenyl]oxacyclohexadec-13-ene-2,6-dione
(3S,7S,14S,15S,16R)-3,15-Dihydroxy-2,2,10,14,16-pentamethyl-7-[1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-6-oxacyclohexadec-9-ene-1,5-dione
Oxacyclohexadec-13-ene-2,6-dione, 4,8-dihydroxy-5,5,7,9,13-pentamethyl-16-(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl-, (4S,7R,8S,9S,13Z,16S)-
Oxacyclohexadec-13-ene-2,6-dione, 4,8-dihydroxy-5,5,7,9,13-pentamethyl -16-(1-methyl-2-(2-methyl-4-thiazolyl)ethenyl)-, (4S-(4R*,7S,8R*,9R*,1 3Z,16R*(E)))-
物理化學性質(zhì)
常見問題列表
圖1為埃博霉素B結(jié)構(gòu)式
培養(yǎng)基：CNST 培養(yǎng)基：KNO30.05%，Na2HPO40.025%，MgSO4·7H2O 0.1%，F(xiàn)eC30.001%，瓊脂 2%，微量元素液 1 mL/L，pH7.2。1×105Pa 高壓蒸汽滅菌 20 min。
M26培養(yǎng)基：土豆淀粉 8.0 g/L，大豆蛋白胨 2.0g/L，葡萄糖 2.0 g/L，酵母粉 2.0 g/L，MgSO4·7H2O1.0 g/L，CaCl21.0 g/L，EDTA-Fe3+1 mL/L，微量元素1 mL/L，以 KOH 調(diào)節(jié) pH 值為 7.2。
初始發(fā)酵培養(yǎng)基：糊精 0.3%，蔗糖 0.07%，葡萄糖 0.02%，豆餅粉 0.17%，七水硫酸鎂 0.17%，無水氯化鈣 0.3%，EDTA-Fe3+2 mL/L，微量元素（TE）0.5 mL/L，pH7.2，樹脂 XAD-16 2%。1×105Pa 高壓蒸汽滅菌 20 min。
培養(yǎng)方法
種子培養(yǎng)：：將保藏在固體斜面培養(yǎng)基的菌種接入放有已滅菌濾紙片的 CNST 平板上，倒置于恒溫培養(yǎng)箱中在 30℃條件下培養(yǎng) 5-7 d 后，轉(zhuǎn)接于 M26 培養(yǎng)基中，裝液量為 50 mL/250 mL 三角瓶，在 30℃、170 r/min 的條件下?lián)u床培養(yǎng) 72 h 后，得到作為發(fā)酵培養(yǎng)的種子液。
發(fā)酵培養(yǎng)：以 5%（V/V）接種量將所得種子液接種到發(fā)酵培養(yǎng)基中進行搖床培養(yǎng)，發(fā)酵體系為300 mL 三角瓶裝液量為 50 mL，在 30℃、170 r/min的條件下?lián)u床培養(yǎng) 5 d。
有關(guān)埃博霉素B的概述、制備方法、應用是由Chemicalbook的丁紅編輯整理。（2015-12-21）
Microtubule/Tubulin
Epothilone D (KOS-862) is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Epothilone D also shows a definite advantage over paclitaxel in drug-resistant cell lines, and retained its cytotoxicity against a multidrug resistant cell line over-expressing P-glycoprotein. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent.
To evaluate whether Epothilone D (EpoD) improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Epothilone D (EpoD) (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D (EpoD) or vehicle. The 3 mg/kg Epothilone D (EpoD) dose corresponds to ~10-fold less than that used in a Phase II clinical study, which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D (EpoD) show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D (EpoD)-treated mice. The motor performance of Epothilone D (EpoD)-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts. Finally, although there is minor group-to-group variability, there are no significant differences in white blood cell counts or neutrophil content between any of the treatment cohorts. Thus, the low doses of Epothilone D (EpoD) utilized in these studies appeared to be well tolerated.