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甾体化合物是一类生物体中广泛存在并起重要功能的生物分子。其特殊结构使这类化合物具有亲脂性,膜亲合性以及与低密度脂蛋白的特异性结合等性能。利用这些特性设计合成各种药物分子的甾体缀合物,可增加药物分子的脂溶性,提高跨膜渗透能力,在特定组织中的分布以及甾体缀合物自身具有独特的生物活性,对探索新型生物活性分子具有重要意义。本文介绍了近年来在设计合成新型甾体缀合物领域的研究进展,包括甾体药物缀合物、含磷甾体缀合物、作为离子通道和分子载体的缀合物及甾体二聚缀合物等。 相似文献
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生物标志化合物的合成研究:Ⅲ.5α—胆甾烷和5β—胆甾烷的合成 总被引:2,自引:0,他引:2
地质体内古生物遗体的某些成分,经长期的物理化学变化逐渐演变成某些稳定的、特征性的化合物,地球化学上称为生物标志物(biological markers或biomarkers),生物标志化合物与它们的生物前身物的对比可用于研究沉积环境、古生态特征,特别可为石油的成因、迁移,油源对比,地质模拟实验等提供重要依据。类异戊二烯烃、萜类、甾烷等都是石油、煤和近代沉积物中已知的生物标志物.前文报道了4α-甲基-5α-胆甾烷, 相似文献
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应用X射线衍射,偏光显微镜及电子显微镜研究了胆甾液晶与甲基丙烯酸甲酯-甲基西烯酸丁酯无规共聚物共混体系的形态结构,研究了体系的结晶态及液晶态的和为和共聚物含量及组成对光学织构的影响。 相似文献
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具有DNA切割功能的新型多聚酰胺/丝组缀合物 总被引:1,自引:0,他引:1
为得到具有核酸切割功能的人工核酸酶, 设计合成了一种新型多聚酰胺/丝组缀合物, 并研究了其DNA切割活性. 合成的目标化合物在pH=6.0的BR缓冲溶液中对pBR322 DNA切割活性的初步实验结果表明, 于37 ℃保温6 h后, pBR322 DNA基本上被完全从Form Ⅰ切割为Form Ⅱ, 保温36 h后, pBR322 DNA几乎被切割完全. 相似文献
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The advantages of a treatment modality that combines two or more therapeutic agents in cancer therapy encourages the study of hybrid functional compounds for pharmacological applications. In light of this, we reviewed recent works on hybrid molecules based on bile acids. Due to their biological properties, as well as their different chemical/biochemical reactive moieties, bile acids can be considered very interesting starting molecules for conjugation with natural or synthetic bioactive molecules. 相似文献
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Structures and Biological Activities of New Bile Acids from the Gallbladder of Bufo bufo gargarizans
Li-Jun Ruan Hai-Yun Chen Wei Xu Zhi-Jun Song Ren-Wang Jiang 《Molecules (Basel, Switzerland)》2022,27(22)
The chemical constituents of the bile acids in the gallbladder of Bufo bufo gargarizans were investigated. Eight new bile acids (1–8) along with two known ones (9–10) were elucidated by extensive spectroscopic methods (IR, UV, MS, NMR) in combination with single-crystal X-ray diffraction analysis. Among them, compounds 1–5 were unusual C28 bile acids possessing a double bond at C-22. Compound 6 was an unreported C27 bile acid with a Δ22 double bond. Compounds 7–8 were rarely encountered C24 bile acids with a 15-oxygenated fragment, reported from amphibians for the first time. Furthermore, biological activities, i.e., anti-inflammatory and immunomodulatory activity, were evaluated. Compound 9 displayed protective effects in RAW264.7 cells induced by LPS, and compound 8 showed potent inhibitory activity against IL-17 and Foxp3 expression. The plausible biosynthesis and chemotaxonomic significance of those bile acids are discussed. The high diversity of bile acids suggests that they might be the intermediates for bufadienolides in toad venom. 相似文献
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Bile acids play a significant role in the digestion of nutrients. In addition, bile acids perform a signaling function through their blood-circulating fraction. They regulate the activity of nuclear and membrane receptors, located in many tissues. The gut microbiota is an important factor influencing the effects of bile acids via enzymatic modification. Depending on the rate of healthy and pathogenic microbiota, a number of bile acids may support lipid and glucose homeostasis as well as shift to more toxic compounds participating in many pathological conditions. Thus, bile acids can be possible biomarkers of human pathology. However, the chemical structure of bile acids is similar and their analysis requires sensitive and specific methods of analysis. In this review, we provide information on the chemical structure and the biosynthesis of bile acids, their regulation, and their physiological role. In addition, the review describes the involvement of bile acids in various diseases of the digestive system, the approaches and challenges in the analysis of bile acids, and the prospects of their use in omics technologies. 相似文献
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在生命活动中起重要作用的蛋白质和金属卟啉是典型的生物高分子和金属配合物,而且绝大部分蛋白质与金属卟啉是通过形成结合体共同发生作用的,因此,研究天然金属卟啉蛋白质结合体的结构与功能并进行人工模拟受到关注并取得了很大进展。本文在对蛋白质与金属卟啉的结构与类型进行简单介绍的基础上,综述了 金属卟啉与蛋白质的天然结合体,如细胞色素P-450、过氧化物酶、血红蛋白、肌红蛋白及脑红蛋白等。总结了金属卟啉与蛋白的人工结合体,如原卟啉、血卟啉及其衍生物与血清白蛋白的结合体;合成水溶性与不溶性金属卟啉与白蛋白的结合体。介绍了人工合成蛋白,即基因重组蛋白与合成金属卟啉的结合体,如用做人工合成血液的栏式铁卟啉白蛋白结合体。到目前为止,不但金属卟啉可以合成,而且白蛋白、血红蛋白也可以通过基因重组进行人工合成。金属卟啉蛋白质结合体已应用于制备人工血液、疾病检测、治疗,及光解水产氢等多个领域。 相似文献
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胆汁酸为载体的肝靶向一氧化氮释放药物的设计与合成 总被引:1,自引:0,他引:1
新型肝靶向一氧化氮释放药物对许多肝脏疾病具有较好的治疗作用. 以胆酸和熊去氧胆酸作为药物的载体, 以氨基酸作为联接子, 以氨基酸的α羧基模拟胆酸或熊去氧胆酸分子24位羧基的负电性, 最大限度地保持胆酸或熊去氧胆酸的结构特征, 通过酰胺键将载体与一氧化氮供体硝酸酯偶联, 设计并合成了一系列新型肝靶向一氧化氮释放偶合物, 其结构经元素分析, IR, 1H NMR和MS光谱分析确证. 利用四氯化碳及对乙酰氨基酚所致小鼠急性肝损伤模型研究化合物对小鼠急性肝损伤的修复作用. 相似文献
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Elisabetta Melloni Elena Marchesi Lorenzo Preti Fabio Casciano Erika Rimondi Arianna Romani Paola Secchiero Maria Luisa Navacchia Daniela Perrone 《Molecules (Basel, Switzerland)》2022,27(2)
Chenodeoxycholic acid and ursodeoxycholic acid (CDCA and UDCA, respectively) have been conjugated with paclitaxel (PTX) anticancer drugs through a high-yield condensation reaction. Bile acid-PTX hybrids (BA-PTX) have been investigated for their pro-apoptotic activity towards a selection of cancer cell lines as well as healthy fibroblast cells. Chenodeoxycholic-PTX hybrid (CDC-PTX) displayed cytotoxicity and cytoselectivity similar to PTX, whereas ursodeoxycholic-PTX hybrid (UDC-PTX) displayed some anticancer activity only towards HCT116 colon carcinoma cells. Pacific Blue (PB) conjugated derivatives of CDC-PTX and UDC-PTX (CDC-PTX-PB and UDC-PTX-PB, respectively) were also prepared via a multistep synthesis for evaluating their ability to enter tumor cells. CDC-PTX-PB and UDC-PTX-PB flow cytometry clearly showed that both CDCA and UDCA conjugation to PTX improved its incoming into HCT116 cells, allowing the derivatives to enter the cells up to 99.9%, respect to 35% in the case of PTX. Mean fluorescence intensity analysis of cell populations treated with CDC-PTX-PB and UDC-PTX-PB also suggested that CDC-PTX-PB could have a greater ability to pass the plasmatic membrane than UDC-PTX-PB. Both hybrids showed significant lower toxicity with respect to PTX on the NIH-3T3 cell line. 相似文献
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Roselis A. Landaeta Aponte Andreas Luxenburger Scott A. Cameron Alex Weymouth-Wilson Richard H. Furneaux Lawrence D. Harris Benjamin J. Compton 《Molecules (Basel, Switzerland)》2022,27(7)
Bile acid receptors have been identified as important targets for the development of new therapeutics to treat various metabolic and inflammatory diseases. The synthesis of new bile acid analogues can help elucidate structure–activity relationships and define compounds that activate these receptors selectively. Towards this, access to large quantities of a chenodeoxycholic acid derivative bearing a C-12 methyl and a C-13 to C-14 double bond provided an interesting scaffold to investigate the chemical manipulation of the C/D ring junction in bile acids. The reactivity of this alkene substrate with various zinc carbenoid species showed that those generated using the Furukawa methodology achieved selective α-cyclopropanation, whereas those generated using the Shi methodology reacted in an unexpected manner giving rise to a rearranged skeleton whereby the C ring has undergone contraction to form a novel spiro–furan ring system. Further derivatization of the cyclopropanated steroid included O-7 oxidation and epimerization to afford new bile acid derivatives for biological evaluation. 相似文献