共查询到19条相似文献,搜索用时 78 毫秒
1.
2.
利用不同的芳香醛和乙酰丙酮缩合反应,合成了4种姜黄素类似物(A1~A4),化合物的结构经IR1、HNMR及MS等测试技术表征确证。采用邻苯三酚法研究化合物的体外抗氧化活性,台盼蓝细胞计数法研究体外抗肿瘤活性。结果表明,化合物A1、A2、A3的抗氧化活性和对K562细胞增殖的抑制活性均高于姜黄素,其活性与酚羟基密切相关。 相似文献
3.
4.
Statine及其类似物的合成 总被引:2,自引:0,他引:2
Statine及其类似物存在于一些具有抗肿瘤、抗病毒、抗炎症等生理活性的天然产物之中。本文简要介绍Statine及其类似物的存在及生理活性,并从不同的起始原料出发,介绍它们的立体选择性合成。 相似文献
5.
胸腺相关肽及其自旋标记类似物的抗氧化活性研究杨国玲,文永均(兰州大学生物系,730000)胡晓愚,佘世望(南昌中德联合研究院,330047)关键词胸腺五肽(TP-5);脂质过氧化物;超氧阴离子自由基;羟自由基;自旋标记类似物胸腺素水平随着人的年龄的增... 相似文献
6.
7.
8.
代涛李松涛赵红玲王小青王良友 《天然产物研究与开发》2015,(7):1140-1145
先采用Fmoc固相多肽合成法,以2-Chlorotrityl chloride(2-CTC)树脂做载体,DIC/HOBt做缩合剂,逐步缩合得到全保护谷胱甘肽树脂,以TFA/EDT/m-Cresol为裂解液脱除保护基团,粗肽经半制备反相高效液相色谱法纯化得α-GSH、γ-GSH纯品,后将所得γ-GSH纯品分别采用空气,双氧水,碘氧化得GSSG,经纯化得GSSG纯品,合成的α-GSH、γ-GSH纯品纯度达99%,GSSG纯度达98%,利用标准品,经外标法计算总收率分别为60%、64%、57%。并观察三者对CCl4诱导的小鼠急性肝损伤的治疗效果结果显示都能显著降低ALT与AST的活性,且与注射用γ-GSH没有显著性差异,可以为工业化生产提供借鉴。 相似文献
9.
10.
Statine及其类似物存在于一些具有抗肿瘤、抗病毒、抗炎症等生理活性的天然产物之中.本文简要介绍Statine及其类似物的存在及生理活性,并从不同的起始原料出发,介绍它们的立体选择性合成. 相似文献
11.
Barbara Biondi Dante Goldin Elisa Giannini Roberta Lattanzi Lucia Negri Pietro Melchiorri Luigi Ciocca Raniero Rocchi 《International journal of peptide research and therapeutics》2006,12(2):139-144
Syntheses are described of the nociceptin (1–13) amide [NC(1–13)-NH2] and of several analogues in which either one or both the phenylalanine residues (positions 1 and 4), the arginine residues (positions 8 and 12) and the alanine residues (positions 7 and 11) have been replaced by N-benzyl-glycine, N-(3-guanidino-propyl)-glycine and β-alanine, respectively. The preparation is also described of NC(1–13)-NH2 analogues in which either galactose or N-acetyl-galactosamine are β-O-glycosidically linked to Thr5 and/or to Ser10. Preliminary pharmacological experiments on mouse vas deferens preparations showed that Phe4, Thr5, Ala7 and Arg8 are crucial residues for OP4 receptor activation. Manipulation of Phe1 yielded peptides endowed with antagonist activity but [Nphe1] NC(1–13)-NH2 acted as an antagonist still possessing weak agonist activity. Introduction of the βAla residue either in position 7 or 11 of the [Nphe1] NC(1–13)-NH2 sequence, abolished any residual agonist activity and [Nphe1, βAla7] NC(1–13)-NH2 and [Nphe1, βAla11] NC(1–13)-NH2 acted as competitive antagonists only. Modification of both Ala7 and Ala11 abolished the antagonist activity of [Nphe1]NC(1–13)-NH2 probably by hindering receptor binding. Changes at positions 10 and 11 gave analogues still possessing agonist activity. [Ser(βGal)10] NC(1–13)-NH2 displayed an activity comparable with that of NC(1–13)-NH2, [Ser(βGalNAc)10] NC(1–13)-NH2 and [βAla11] NC(1–13)-NH2 were five and 10 times less active, respectively.The α-amino acid residues are of the l-configuration. Standard abbreviations for amino acid derivatives and peptides are according to the suggestions of the IUPAC-IUB Commission on Biochemical Nomeclature (1984), Eur. J. Biochem. 138, 9–37. Abbreviations listed in the guide published in (2003), J. Peptide Sci. 9, 1–8 are used without explanation. 相似文献
12.
降钙素和降钙素基因相关肽的选择性表达 总被引:3,自引:0,他引:3
降钙素和降钙素基因相关肽(CT/CGRP)由同一基因编码,该基因结构及其5'端侧翼序列决定了它能够在甲状腺C细胞以及中枢和外周神经细胞生成不同的表达产物.这种选择表达调控决定多细胞生物的发育、性别分化和进化.如果表达失控将导致甲状腺髓样瘤(MTC)和骨质疏松症等疾病.文章对该基因的结构和选择性表达调控进行了综述. 相似文献
13.
本文概述了目前已发表的天然产物黄檀内酯在植物中分布、生物合成、全合成及生物活性的研究进展。 相似文献
14.
将合成的人胰高血糖素样肽-1类似物基因插入到原核表达质粒pGEX-4T-3中,构建成rhGLP-1类似物与谷胱甘肽巯基转移酶(glutathione-S-transferases,GST)的融合表达载体pGEX-rhGLP-1类似物,转化大肠杆菌BL21(DE3)获得重组菌株。IPTG诱导表达的菌体经高压均质机破碎后,离心收集包涵体,经尿素变性、Glutathione-Sepharose 4B亲和层析、肠激酶酶切、SP-Sepharose FF层析和反相层析RP-C18脱盐后冻干,得到纯度大于96%的rhGLP-1类似物,经质谱测定,分子量与理论值一致。生物学活性分析表明,rhGLP-1类似物具有促进表达有GLP-1受体的HEK293细胞cAMP增加的活性。 相似文献
15.
Kerti Ausmees Anastasia Selyutina Kristel Kütt Kristin Lippur Tõnis Pehk Margus Lopp 《Nucleosides, nucleotides & nucleic acids》2013,32(11):897-907
A new enantiomerically pure carbacyclic nucleoside analogue with bimorpholine as a nonaromatic nucleobase was synthesized. The nucleoside analogue and bimorpholine were tested for cytotoxicity using an MTT assay and the xCELLigence System. Both assays revealed that compound 3 was highly cytotoxic at a 50 μM concentration while the cytotoxic effect of compound 1 was much less prominent. No antiretroviral activity was detected for this compound. In contrast, it acted as a potent inhibitor of hepatitis C virus (HCV) replication. Most likely this effect originates largely from the cytotoxicity of the compound; however, it is possible that a specific mechanism of HCV inhibition also exists. 相似文献
16.
Agata Kozio Mateusz Jasnowski Ewa Grela Maryla Szczepanik Beata Gabry Katarzyna Dancewicz Stanisaw Lochyski 《化学与生物多样性》2019,16(2)
In the synthesis performed in this study, derivatives of 4‐tert‐butylcyclohexanone 1 were obtained using typical reactions of organic synthesis. The bioactivity of the selected compounds was evaluated. 1‐(Bromomethyl)‐8‐tert‐butyl‐2‐oxaspiro[4.5]decan‐3‐one ( 5 ) was characterized by attractant properties against larvae and a weak feeding deterrent activity against adults of Alphitobius diaperinus Panzer . This bromolactone was a moderate antifeedant towards Myzus persicae Sulzer . In addition, ethyl (4‐tert‐butylcyclohexylidene)acetate ( 2 ) and bromolactone 5 displayed antibacterial activity. The strongest bacteriostatic effect was observed against Gram‐positive strains: Bacillus subtilis and Staphylococcus aureus. The bromolactone 5 also limited the growth of Escherichia coli strain. 相似文献
17.
Ludovic Colombeau Karine Teste Amel Hadj-Bouazza Vincent Chaleix Rachida Zerrouki Michel Kraemer 《Nucleosides, nucleotides & nucleic acids》2013,32(2):110-120
The synthesis and biological activity of chloroethyl pyrimidine nucleosides is presented. One of these new nucleosides analogues significantly inhibited cell proliferation, migration and invasion as tested in vitro on the A431 vulvar epidermal carcinoma cell line. 相似文献
18.
目的:制备重组谷氨酰胺∶6-磷酸果糖酰胺转移酶(GFAT),检测其活性。方法:利用RT-PCR扩增人肝脏cDNA中GFAT1基因全长片段,克隆到表达载体pET32b中;在大肠杆菌Origami(DE3)中诱导表达,用镍离子螯合柱(Ni-NTA)纯化重组GFAT1;用体外酶学的方法检测GFAT的活性。结果:构建了pET32b-GFAT1质粒,经诱导表达及纯化,得到具有一定生物活性的GFAT。结论:利用原核表达系统可得到具有良好生物学活性的重组人GFAT1。 相似文献
19.
重组人KGF制备工艺和活性检测方法的建立 总被引:1,自引:0,他引:1
目的:在毕赤酵母中实现了KGF的高效表达,并初步建立了生物学活性检测方法.方法:合成5'端缺失69个核苷酸的KGF基因序列,克隆入pPIC9并转化毕赤酵母菌株GS115中,经诱导表达.发酵液上清采用脱盐层析和阳离子交换层析进行分离纯化.利用貂肺上皮细胞(Mv-1-Lu)检测其生物学活性.结果:表达水平达到了110mg/L发酵液;表达产物经一步离子交换层析就能得到有效分离,总收率在50mg/L发酵液以上;纯化的rhKGF生物学活性与KepivanceTM相当.结论:rhKGF制备工艺和检测方法的建立将为该因子的规模化生产和进一步的临床应用提供良好基础. 相似文献