CAS: 545-26-6; Gitoxigenin

上下游产品

毛地黄毒苷配基 (+)-Digitoxigenin 143-62-4
格列苯脲杂质a Gitoxin 4562-36-1
欧夹竹桃甙丙 Oleandrin 465-16-7

📜欧夹竹桃甙丙置于三氟乙酸体系中,用 正丁醇 作为反应溶剂,化学反应 1.5H,以25%的收率获得产物芰皂配基
参考文献:内毒素性真菌alternatearia Eureka 1E1Bl1对gitoxigenin的生物转化产生的新的胡萝卜素:表征和细胞毒活性.
标题:内毒素性真菌alternatearia Eureka 1E1Bl1对gitoxigenin的生物转化产生的新的胡萝卜素:表征和细胞毒活性.
摘要:微生物生物转化是药物发现和代谢研究的重要工具.为了通过修饰扩展我们的生物活性天然产物库并鉴定可能的哺乳动物代谢物,使用内生真菌链格孢(alternaria Eureka)1E1Bl1对细胞毒性的烯醇内酯(gitoxigenin)进行了生物转化.最初,从干燥的夹竹桃叶中分离出夹竹桃苷,并进行酸催化水解,得到底物皂苷配基(收率;〜25%).温育后的21天,五个新的卡烯内酯1,3,4,6,和8和三个previously-鉴定的化合物2,5用色谱法分离出7和7.通过1D / 2D NMR,Hr-Esi-Ms和ft-Ir分析完成结构阐明.a.尤里卡(eureka)催化底物上的氧化,氧化,差向异构化和二甲基乙缩醛形成反应.使用mtt细胞生存力方法评估代谢产物的细胞毒性,而阿霉素和夹竹桃苷用作阳性对照.生物转化产物显示出比底物小的细胞毒性.新的代谢物8表现出最高的ic 50活性分别针对a549,Panc-1和mia
DOI:10.3390/molecules26103030

专利信息

专利号:US-4259240-A
优先权日:1979-09-28
标 题:Synthesis of furyl intermediates, and cardenolides and their isomers prepared therefrom
发明人：WIESNER KAREL; TSAI THOMAS Y R
权利人:ADVANCE BIOFACTURES CORP
摘要:The invention relates to furyl intermediates and the preparation thereof, said intermediates being particularly useful in the preparation of synthetic cardenolides and their isomers. The process provides for the reaction of an unsaturated steroidal 17 ketone with a β-furyl compound to produce an allylic alcohol which is subjected to acetylation and allylic rearrangement. The resulting material is then hydrogenated to produce the furyl intermediate. Cardenolides are formed therefrom by oxidation of the furyl intermediates.

专利号:US-9889182-B2
优先权日:2009-09-15
标 题 :Assisted enzyme replacement therapy
发明人：ESKO JEFFREY D; TOR YITZHAK
权利人:ESKO JEFFREY D; TOR YITZHAK; UNIV CALIFORNIA
摘要:Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.

专利号:US-6699676-B1
优先权日:1999-06-03
标题:Uses of ouabain and ouabain-like molecules in apoptosis related pathologies
发明人：ORLOV SERGEI N; HAMET PAVEL; TREMBLAY JOHANNE
权利人:CORP DU CT DE RECH DU CT HOSPI
摘要:Longterm elevation of the intracellular Na + /K + ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells (VSMC). We report here that inhibition of the Na + ,K + pump in VSMC by ouabain or 1 hour preincubation in K + -depleted medium attenuated apoptosis triggered by serum withdrawal, staurosporine or okadaic acid. In the absence of ouabain, both DNA degradation and caspase-3 activation in VSMC undergoing apoptosis were insensitive to modification of the extracellular Na + /K + ratio as well as to hyperosmotic cell shrinkage. In contrast, protection of VSMC from apoptosis by ouabain was abolished under equimolar substitution of Na + o with K + o , showing that the anti apoptotic action of Na + ,K + pump inhibition was caused by inversion of the intracellular Na + /K + ratio. Unlike VSMC, the same level of increment of the [Na + ] i /[K + ] i ratio caused by 2 hours preincubation of Jurkat cells with ouabain did not affect chromatin cleavage and caspase-3 activity triggered by treatment with Fas ligand, staurosporine or hyperosmotic shrinkage. Thus, our results show for the first time that similarly to cell proliferation, maintenance of a physiologically low intracellular Na + /K + ratio is required for progression of VSMC apoptosis.

专利号:US-8071535-B2
优先权日:2003-09-12
标 题 :Guanidinium derivatives for improved cellular transport
发明人：TOR YITZHAK; LUEDTKE NATHAN
权利人:TOR YITZHAK; LUEDTKE NATHAN; UNIV CALIFORNIA
摘要:Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.

专利号:US-11293060-B2
优先权日:2017-04-12
标 题 :Method for labeling of aldehyde containing target molecules
发明人：BERGMANN FRANK; CHAU IAN QUANG; CRISALLI PETER; KALLEWAARD-LUM HANNAH MARIE; KUCHELMEISTER HANNES; POMPLUN SEBASTIAN JOHANNES; SAQIB HASHAM; WELLNER CHRISTIAN
权利人:ROCHE SEQUENCING SOLUTIONS INC
摘要:The present invention relates to improving the processing rate of a sequencing reaction, for example in a nanopore sequencing reaction, by means of using improved nucleoside-tags. The tags are linked to the nucleoside phosphate via a Pictet Spengler reaction. Exemplary sequencing reactions that are improved by the present methods include nanopore-based nucleic acid sequencing-by-synthesis reactions.

专利号:US-4331802-A
优先权日:1980-10-01
标题:Organometallic reagents and their use in the synthesis of cardenolides and isocardenolides
发明人：WIESNER KAREL; MARINI-BETTOLO RINALDO; TSAI CONNIE S J; TSAI THOMAS Y R
权利人:ADVANCE BIOFACTURES CORP
摘要:A method for synthesizing a cardenolide or isocardenolide by subjecting an α,β-unsaturated steroidal 17-ketone to a double bond shift and hydrogenation to produce a (C/D cisoid) ketone which is treated with an organometallic reagent to yield a tertiary alcohol and the acidifying said alcohol to produce said cardenolide or isocardenolide is shown. The invention also relates to organometallic reagents particularly useful in such method.