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1.
目的对白花前胡丙素[(+)-praeruptorin A]进行结构修饰,半合成C-3′和C-4′反式结构类似物,寻找活性化合物。方法首先从白花前胡(Peucedanum praeruptorum)根中分离得到白花前胡丙素,从白花前胡丙素出发,运用碱水解及各种酰化反应,半合成各种结构修饰产物。结果首次合成了17个白花前胡丙素C-3′和C-4′反式结构类似物,通过IR,1HNMR,MS等方法确定它们的结构。结论17个化合物均为新化合物,其中一些新化合物有显著的钙离子拮抗活性,首次证明C-3′和C-4′反式结构的这类化合物同样具有活性。  相似文献   

2.
目的 对白花前胡丙素 [( ) praeruptorinA]进行结构修饰 ,半合成C 3′和C 4′反式结构类似物 ,寻找活性化合物。方法 首先从白花前胡 (Peucedanumpraeruptorum)根中分离得到白花前胡丙素 ,从白花前胡丙素出发 ,运用碱水解及各种酰化反应 ,半合成各种结构修饰产物。结果 首次合成了 1 7个白花前胡丙素C 3′和C 4′反式结构类似物 ,通过IR ,1 HNMR ,MS等方法确定它们的结构。结论  1 7个化合物均为新化合物 ,其中一些新化合物有显著的钙离子拮抗活性 ,首次证明C 3′和C 4′反式结构的这类化合物同样具有活性。  相似文献   

3.
目的:根据RGD肽及目前活性较好的非肽类纤维。0蛋白原受体拮抗剂的结构特点,设计、合成一系列有抗血小板聚集活性的化合物。方法:以酪氨酸及对硝基苯甲酸等为主要原料经多步合成,对所得化合物用比浊法测定在1×10-6 mol.L-1时对体外血小板聚集的抑制率。结果:合成了18个N-取代-O-对甲脒苯胺基羰甲基-L-酪氨酸甲酯类化合物(Ia~r),均为新化合物。结论:其中10个化合物(Ia,f,g,i~m,q,r)显示一定的活性,活性最高的(Ig)抑制率达64%。  相似文献   

4.
梁侨丽  闵知大 《药学学报》2007,42(11):1159-1161
为寻找毒性低、活性强的化合物,对地胆草倍半萜内酯化合物进行结构修饰。本文首先从地胆草全草中分离得到去氧地胆草内酯(deoxyelephantopin)和地胆草种内酯(scabertopin),再对这两个化合物进行氧化和氢化反应,制备不同结构修饰产物。共得到5个大环化合物,通过IR、 1H NMR和MS等方法确定其结构。其中4个化合物(2~5)为新化合物,部分化合物有一定的抗肿瘤活性。  相似文献   

5.
赤芝子实体新三萜化合物的结构鉴定   总被引:8,自引:1,他引:7  
罗俊  林志彬 《药学学报》2001,36(8):595-598
目的 对赤芝子实体的化学成分进行研究。方法 利用各种色谱技术进行分离,采用1HNMR ,13CNMR ,1H-1HCOSY ,HMQC和HMBC谱进行结构鉴定。结果 从赤芝子实体中分离得到3个化合物,分别鉴定为:lucidenicacidA (1) ,3β,7β-dihydroxy-4,4,14α-trimethyl-11,15-dioxo-5α-chol-8-en-24-oic acid (2 )和lucidenic acid C (3)。结论 化合物2为新化合物,命名为赤芝酸LM1(lucidenicacidLM1)。  相似文献   

6.
亮叶杨桐的三萜皂苷类成分   总被引:6,自引:0,他引:6  
为研究亮叶杨桐(Adinandra nitida Merr. ex Li)叶的化学成分,亮叶杨桐叶的乙醇提取物经大孔树脂、硅胶、Sephadex LH-20以及ODS柱色谱分离得到6个化合物,通过波谱(1H NMR、 13C NMR、 HR-ESI-MS)和化学方法进行结构鉴定,6个化合物分别被鉴定为2α,3α,19α-trihydroxy-olean-12-en-28-oic acid-28-O-β-D-glucopyranoside (1)、 arjunetin (2)、 sericoside (3)、 glucosyl tormentate (4)、 nigaichigoside F1 (5)和arjunglucoside I (6)。化合物1为新化合物,化合物2~6均为首次从该植物中分离得到。  相似文献   

7.
前胡香豆素A的分离和结构鉴定   总被引:11,自引:0,他引:11  
从中药白花前胡(Peucedanum praeruptorum Dunn)根中分离得到7个化合物,经理化常数和波谱数据的测定以及化学反应,鉴定为补骨脂素(Ⅱ)、5-甲氧基补骨脂素(Ⅲ)、8-甲氧基补骨脂素(Ⅳ)、北美芹素(Ⅴ)、peucedanocoumarin Ⅱ(Ⅵ)、β-谷甾醇(Ⅶ)和前胡香豆素A(Ⅷ)。Ⅷ为一新化合物,通过和凯林内酯的化学沟通确定了其绝对构型,化学结构为3′(R)-羟基-4′(E)-惕各酰氧基-3′,4′-二氢邪蒿内酯。Ⅱ~Ⅳ和Ⅶ为首次从白花前胡中分离得到。  相似文献   

8.
白花前胡中前胡香豆素D和前胡香豆素E的分离和鉴定   总被引:7,自引:0,他引:7  
从中药白花前胡(Peucedanum Praeruptorum Dunn)根中分到5个化合物,经理化常数、波谱数据及化学反应分别鉴定为前胡香豆素D(I),Pd-Ib(II),前胡香豆素E(III),nodakenetin(IV)和scopoletin(V)。其中化合物I和III为两个新化合物,与巳知化合物凯林内酯的化学沟通确定了其绝对构型,其化学结构分别为3'(S),4'(S)-二乙酰氧基-3',4'-二氢邪蒿内酯(I)和3'(R)-惕各酰氧基-4'-酮基-3',4'-二氢邪蒿内酯(III)。化合物IV和V为首次从该植物中分离得到。通过DEPT,1H-1HCOSY和13C-1HCOSY等实验归属了II的碳氢信号。  相似文献   

9.
白花丹参化学成分的研究   总被引:30,自引:0,他引:30  
从白花丹参(Salvia miltiorrhiza f.alba)中分离出14个二萜醌类化合物,其中2个为新化合物,由光谱分析推定为1,2,15,16-四氢丹参醌(Ⅰ)和丹参醛(Ⅱ);另一个化合物Ⅲ与R0-090680的结构相同。化合物Ⅰ和Ⅲ对淋巴白血病细胞P388均有较强的抑制作用。  相似文献   

10.
目的:寻找高效低毒的抗真菌化合物。方法和结果:根据违法传递概念设计合成了12个碳端含有MEDP(N3-[(2R,3R)-4-methoxyepoxysucinyl]-L-2,3-diaminopropanoicacid)的二肽和三肽(1~12),均系新化合物。结论:体外抗白念珠菌实验表明:有些二肽三肽体外实验显示了较强的抑菌活性,其中Val MEDP的活性最强,其MMIC为45nmol·mL-1,较母体MEDP提高960倍。  相似文献   

11.
中药白花前胡化学成分的研究——四种新香豆素的结构   总被引:12,自引:0,他引:12  
中药白花前胡(Peucedanum praeruptorum Dunn.)根的醚提部分中分得四种新香豆素,命名为白花前胡甲素((±)-praeruptorin A)、白花前胡乙素((±)-praeruptorin B)、白花前胡丙素((±)-praeruptorin A)和白花前胡丁素((+)-praeruptorinB),分别确定了它们的化学结构为[Ⅰ],[Ⅱ]、[Ⅲ]和[Ⅳ]式。其中[Ⅰ]和[Ⅲ]、[Ⅱ]和[Ⅳ]分别是消旋体和化学活性体的关系。此外,由纸层析检出了紫花前胡甙[Ⅴ]的存在并分得了D-甘露醇。白花前胡丙素[Ⅲ]及其双氢化物[ⅩⅥ]在离体豚鼠心上具有明显增加冠脉血流量的作用。  相似文献   

12.
Du SJ  Gariboldi P  Jommi G 《Planta medica》1986,52(4):317-320
From the ethyl acetate extract of the Chinese drug "Shashen", the root of ADENOPHORA AXILLIFLORA Borb., three triterpenoids, cycloartenol acetate ( 1), lupenone ( 2) and beta-sitosterol ( 3), two triterpenoid derivatives, beta- D-glucopyranosyl-(1-->3)-beta-sitosterol ( 7) and its 6- O-palmitoyl ester ( 6), along with two coumarins, (+)-praeruptorin A ( 4) and 3'-angeloyl-4'-isovaleryl-(3' S, 4' S) CIS-khellactone ( 5) have been isolated. A detailed (1)H-NMR analysis of compounds 6, 7 and their acetates is reported. The structure of the partial hydrolysis product of 5 is revised on the basis of spectroscopic evidences and mechanistic considerations.  相似文献   

13.
Qian-Hu is a well-known traditional Chinese medicine used for the treatment of respiratory diseases and pulmonary hypertension. We compared the relaxant effects of pyranocoumarin compounds, including (+)-praeruptorin A (Pra-C), Pd-Ia (=(+/-)-praeruptorin A), pteryxin, peucedanocoumarin II (P-II) and 8-methoxy-psoralen (8-MOP) purified from Bai-Hua Qian-Hu (BQ) in isolated rabbit tracheas and pulmonary arteries. Pra-C, pteryxin and Pd-Ia produced significant relaxant effects in tracheal preparations constricted with 40 mM KCl or 10 microM acetylcholine. The relaxant response to Pra-C, pteryxin or Pd-Ia in preparations constricted with KCl was significantly more potent than that in preparations constricted with acetylcholine. Pra-C, pteryxin or Pd-Ia at a concentration of 30 microM completely relaxed tracheas constricted with 40 mM KCl, whereas P-II at the same concentration showed only partial relaxation. In pulmonary arterial preparations, 8-MOP produced a significant relaxant effect on contractions by 10 microM phenylephrine, without any effect on the contraction by 40 mM KCl. These results suggest that Pd-Ia, pteryxin and Pra-C for their calcium antagonistic action, and 8-MOP for its inhibitory effect on contraction induced by phenylephrine, may be the active principles of BQ for relaxing the smooth muscle of tracheas and pulmonary arteries, and the principle may produce a synergistic effect.  相似文献   

14.
吴彤  孔德云  李惠庭 《药学学报》2004,39(7):534-537
目的研究藤香树Schisandra propinqua (Wall.) Baill var. intermidia A.C.Smith茎藤的化学成分。方法 应用多种色谱技术进行分离纯化,根据化合物的理化性质和光谱数据分析鉴定结构。结果分离得到7个化合物,分别鉴定为6′-O-α-L-arabinofuranosylthalictoside (1), 6′-O-β-D-apiofuranosylthalictoside (2), thalictoside (3), icariside D2(4), prinsepiol (5), (+)-1-hydroxypinoresinol (6)和(+)-medioresinol (7)。结论化合物1和2为新的脂肪硝基酚苷化合物,其余均为首次从藤香树中获得。  相似文献   

15.
The kinetics of hydrolysis of oxazolidines derived from (-)-ephedrine or (+)- pseudoephedrine and benzaldehyde or salicylaldehyde was studied at 37°C to assess their suitability as pro-drug forms for β-aminoalcohols and carbonyl-containing compounds. The oxazolidines were found to undergo a facile and complete hydrolysis in the pH range 1–11. The oxazolidines derived from benzaldehyde showed bell-shaped pH-rate profiles with rate maxima occurring at pH 4–5.5. The oxazolidine from salicylaldehyde showed a sigmoidal pH-rate profile and was 100-fold more reactive than the corresponding benzaldehyde derivative at pH > 7. At pH 7.4 and 37°C half-lives of hydrolysis from 5s to 28 min were observed for the 3 oxazolidines studied. The oxazolidines are weaker bases than the parent β-aminoalcohols and are more lipophilic than these as determined by partition experiments in an octanol-phosphate buffer system. It is suggested that oxazolidines be considered as potentially useful pro-drug candidates for β-aminoalcohols or drugs containing carbonyl groups.  相似文献   

16.
紫花前胡化学成分的研究   总被引:7,自引:0,他引:7  
姚念环  孔令义 《药学学报》2001,36(5):351-355
目的研究中药紫花前胡[Peucedanum decursivum(Miq.)Maxim]根的化学成分。方法用硅胶柱色谱和制备型高效液相色谱进行分离纯化,用光谱分析和化学方法鉴定其结构。结果从紫花前胡根中分得7个线型吡喃香豆素类化合物,其结构分别鉴定为3′(S)-hydroxy-4′(R)-angeloyloxy-3′,4′-dihydroxanthyletin(1);3′(S)-acetoxy-4′(R)-hydroxy-3′,4′-dihydroxanthyletin(2);3′(S)-acetoxy-4′(R)-angeloyloxy-3′,4′-dihydroxanthyletin(3);Pd-C-IV(4);Pd-C-II(5);(+)-3′S-Decursinol(6);(+)-trans-Decursidinol(7)。结论化合物1和2为新化合物,分别命名为紫花前胡素D和紫花前胡素F;6和7为首次从该植物中分得。  相似文献   

17.
猫儿刺(Ilex pernyi)为冬青科冬青属植物,民间常用于清热解毒,润肺止咳。本文对猫儿刺叶的化学成分进行研究,应用硅胶、Sephadex LH-20、反相硅胶和半制备RP-HPLC等分离纯化方法从其乙醇提取物中分离并鉴定了6个化合物:(E)-异丁香酚-α-L-吡喃阿拉伯糖基(1→6)- β-D-吡喃葡糖苷(1),山柰酚-3-O-桑布双糖苷(2),槲皮素-3-O-桑布双糖苷(3),异槲皮苷(4),丁香树脂酚葡糖苷(5),反枝苋苷IV(6)。其中,化合物1为一新酚苷类化合物,命名为猫儿刺酚苷A。化合物2~6为首次从该植物中分离得到。  相似文献   

18.
Stereoselective hydrolysis at pH 7.5 and 37 degrees of C(+/-)P(+/-)-soman by liver homogenate and plasma from rat, guinea pig and marmoset, and by human plasma is studied by using the four single stereoisomers. The fast hydrolysis of the C(+/-)P(+)-isomers is monitored titrimetrically, whereas the decay of the much slower reacting C(+/-)P(-)-isomers is followed by gas chromatographic determination of the residual concentration. Values of Km and Vmax are evaluated for the enzymatic hydrolysis of the two relatively nontoxic C(+/-)P(+)-isomers. The plasma enzymes have a high affinity for these isomers (Km: 0.01-0.04 mM); the Km values of the liver enzymes vary between 0.04 and 0.7 mM. Except for rat liver homogenate, only first-order rate constants can be obtained for catalyzed hydrolysis (kc) of the highly toxic C(+/-)P(-)-isomers: most measurements with C(+/-)P(-)-isomer concentrations greater than 0.3 mM are complicated by epimerization to C(+/-)P(+)-isomers, which may conceal enzyme saturation with the C(+/-)P(-)-isomers. The first-order rate constants of catalyzed hydrolysis (Vmax/Km or kc) by all liver homogenates and plasmata decrease in the order: C(+)P(+)- greater than C(-)P(+)- much greater than C(-)P(-)- greater than C(+)P(-)-soman. The highest P(+)-/P(-)-stereoselectivity is found for rat plasma. Rat liver homogenate is more potent than the other liver homogenates in catalyzing the hydrolysis of both the C(+/-)P(+)- and the C(+/-)P(-)-isomers. Rat plasma shows the highest activity for degradation of the C(+/-)P(+)-isomers, but is approximately as active as marmoset and human plasma for degradation of the C(+/-)P(-)-isomers.  相似文献   

19.
He WJ  Chu HB  Zhang YM  Han HJ  Yan H  Zeng GZ  Fu ZH  Olubanke O  Tan NH 《Planta medica》2011,77(17):1924-1931
Seven new compounds, including four lignans, (+)-(8S,8′S)-9,9′-dibenzoylsecoisolariciresinol (1), (+)-(8S*,8′R*)-4,4′-dimethyloxomatairesinol (2), (+)-(7S*,8R*,8′R*,9′S*)-9′-n-butoxytsugacetal (3), and pseudolarkaemin A (4), a pyronane glycoside, pseudolarkaemin B (5), an ent-beyerene glycoside, pseudolarkaemin C (6), and a triterpene, 25-epi-pseudolarolide Q (7), along with 25 known compounds (8–32) were isolated from the twigs of Pseudolarix kaempferi. Their structures were elucidated mainly by the analysis of their NMR and MS data. Pseudolarolide C acid (24) was isolated for the first time as a natural product. All compounds were evaluated for antimicrobial activity against Candida albicans and Staphylococcus aureus, and cytotoxic activity against K562, HT-29, B16, BGC-823, BEL-7402, SGC-7901, U251, and A549 cancer cell lines were assayed. Results indicated that the new compounds 3, 7, and some known compounds showed antimicrobial and cytotoxic activities.  相似文献   

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