A new diterpene from the processed roots of Euphorbia Kansui

A new diterpene has been isolated from the processed roots of Euphorbia Kansui. By means of physico-chemical evidences and spectral analysis, the structure was identified as 4-O-acetyl-5-O-benzoyl-3β-hydroxy-20-deoxyingenol (1).     

A new diterpene from the processed roots of Euphorbia Kansui

A new diterpene has been isolated from the processed roots of Euphorbia Kansui. By means of physico-chemical evidences and spectral analysis, the structure was identified as 4-O-acetyl-5-O-benzoyl-3beta-hydroxy-20-deoxyingenol (1).     

Two new casbane diterpenoids from the roots of Euphorbia pekinensis

From the roots of Euphorbia pekinensis, two new casbane diterpenoids, named pekinenins A (1) and B (2), were isolated. Their structures were elucidated as 18-hydroxy-1βH,2αH-casba-3E,7E,11E-trien-5-one (1), 5α-methoxy-1βH,2αH-casba-3Z,7E,11E-trien-18-oic acid (2) by a combination of 1D and 2D NMR spectroscopy and mass spectrometry. In the cytotoxicity assay of the two new compounds against Hela, MCF-7, and C6 human cancer cell lines, compound 1 showed moderate cytotoxic activity against two human cancer cell lines, Hela and C6, with IC₅₀ values of 42.97 and 50.00 μM, respectively.     

An isopimarane diterpene from Euphorbia ebracteolata Hayata

From the ethanolic extract of the roots of Euphorbia ebracteolata Hayata four compounds were isolated. They are 24-methylenecycloartanone, tirucallol, procesterol and a new isopimarane diterpene, namely yuexiandajisu C. The structure of yuexiandajisu C was elucidated by spectral analysis. The bioassay in vitro showed yuexiandajisu C exhibited immunomodulatory activity.     

Diterpenoids from the roots of Euphorbia fischeriana

Six tigliane-type diterpenoids (1–6) were isolated from the roots of Euphorbia fischeriana. Their structures were elucidated by various spectral analyses. Among them, compounds 1 and 3 were new, and compounds 2, 4, and 5 were naturally obtained for the first time. All compounds were tested against two human cancer cell lines, MDA-MB-231 and HepG2, and one human immortalized cell line, and only compound 6 showed cytotoxicity for MDA-MB-231 cells with an IC₅₀ value of 6.694 μM.     

Irritant and co-carcinogenic diterpene esters from the latex of Euphorbia cauducifolia L.

Ten (1–10) irritant and mild co-carcinogenic diterpene esters were isolated from the latex of Euphorbia cauducifolia L. using bioassay-guided countercurrent distribution and other chromatographic techniques. The isolated compounds were characterized on the basis of spectroscopic results and mass measurements. As an outcome, the ingenane-type esters were established with the following structures: 3-O-angeloyl-17-O-palmatoylingenol (1), 3-O-palmatoyl-5-O-angeloylingenol (2), 5-O-angeloyl-17-O-palmatoylingenol (3), 3-O-angeloyl-5-O-palmatoylingenol (4), 17-O-(2Z,4E,6Z)-2,4,6-tetradecatrienoyl-20-O-palmatoylingenol (5), 5-O-angeloyl-17-O-benzoylingenol (6), 5-O-angeloyl-17,20-diacetoxyingenol (7), 3-O-angeloyl-17-O-benzoyl-20-acetoxyingenol (8), 3-acetoxy-5-O-angeloyl-17-O-benzoylingenol (9), and 5-O-angeloyl-3,17,20-triacetoxyingenol (10). Their biological screening revealed that they are moderate irritants, and low to moderate tumor promoters compared to TPA, but hardly showed any solitary carcinogenic activity. The isolated esters represent new compounds and were not reported before from any source.     

Two new triterpenes from Euphorbia alatavica

A phytochemical investigation on Euphorbia alatavica Boiss resulted in the isolation of nine compounds, including two new ones, alatavolide and alatavoic acid (1–2). Chemical structures of these compounds were established on the basis of 1D, 2D NMR, and HR-MS techniques, and by comparison with data reported in the literature. Compounds 1, 2, 4, 6, 8, and 9 were screened for cytotoxicity using the MTT assay. Among these compounds, the new compound 2 showed moderate cytotoxicity against Hela, MCF-7 and A549 cell lines (IC₅₀ values of 16.4 ± 3.2, 14.5 ± 2.8, 22.3 ± 3.1 μM, respectively), while the known compound 8 exhibited the most potent cytotoxicity with the IC₅₀ values of 6.5 ± 3.1, 1.9 ± 0.9, 8.6 ± 3.5 μM, respectively.     

A new bisabolane sesquiterpenoid from Euphorbia chrysocoma

The new sesquiterpenoid (6R)-2-chloro-6-[(1S)-1,5-dimethylhex-4-en-1-yl]-3-methylcyclohex-2-en-1-one (1), together with ten known compounds, (6R)-6-[(1S)-1,5-dimethylhex-4-en-1-yl]-3-methylcyclohex-2-en-1-one (2), bauerenol acetate (3), lupenone (4), α-amyrenone (5), β-sitosterol (6), stigmasterol (7), β-amyrin (8), ursolic acid (9), betulinic acid (10), scopolin (11), have been isolated from the roots of Euphorbia chrysocoma Lévl. et Vant. Their structures have been elucidated by spectroscopic data.     

Four new diterpenoids isolated from the Euphorbia rapulum

Four new diterpenoids named 1-epi-9-hydroxydepressin (1), 1-epi-8-hydroxydepressin (2), 2,13,9-trihydroxy-labda-8(17),12(E),14-triene (3) and tagalsin I (4) were isolated from Euphorbia rapulum. The structures of these compounds were elucidated by means of various spectroscopic methods. All the isolated compounds were evaluated for cytotoxic activities against HepG2, MCF-7, and C6 cell lines, and compound 4 showed moderate selective activity against MCF-7 cell line with an IC₅₀ value of 31.8 μM.     

铁棒锤砂炒炮制品中二萜生物碱化学成分的研究

目的 研究铁棒锤砂炒炮制品的化学成分.方法 运用硅胶柱色谱等方法进行分离纯化,根据波谱数据和理化常数进行结构鉴定.结果 从铁棒锤砂炒炮制品中分离并鉴定出7个化合物,分别为3-乙酰乌头碱、乌头碱、16-epi-pyrodeoxyaconitine、16-epi-pyroaconitine、polyschistine-D、...     

京大戟化学成分的分离与鉴定

目的对京大戟的化学成分进行研究。方法采用硅胶、凝胶柱色谱和制备高效液相色谱等分离方法对京大戟的体积分数为95%乙醇溶液提取物进行成分分离,通过谱学分析方法结合理化性质进行结构鉴定。结果共分离得到9个化合物,分别鉴定为环阿尔廷醇(cycloartenol,1)、月腺大戟素C(yuexiandajisu C,2)、helioscopinolide E(3)、3,3'二甲氧基鞣花酸(3,3'-di-O-methylellagicacid,4)、3,3'二甲氧基鞣花酸4'OβD吡喃木糖苷(3,3'-di-O-methylellagic acid-4'-O-β-D-xy-lopyranoside,5)、3,3'二甲氧基鞣花酸4'OβD吡喃葡萄糖苷(3,3'-di-O-methylellagic acid-4'-O-β-D-glucopyranoside,6)、鞣花酸(ellagic acid,7)、没食子酸甲酯(methyl gallate,8)、没食子酸(gallic acid,9)。结论化合物1 3、7为首次从京大戟中分离得到。     

Terpenoids from Euphorbia pekinensis

Abstract

Euphorpekone A (1) and euphorpekone B (2), two new diterpenoids, 3β-hydroxy-25-methyloxylanosta-8,23-diene, a new triterpenoid (3), together with a known triterpenoid, 3β,25-dihydroxylanosta-8,23-diene (4), were isolated from Euphorbia pekinensis Rupr. Their structures were elucidated on the basis of UV, IR, 1D (¹H, ¹³C, NOE) and 2D (¹H–¹H COSY, HSQC, HMBC) NMR, HR-ESI-MS, X-ray diffraction analysis, and CD method.     

Two new casbane diterpenoids from the roots of Euphorbia pekinensis

From the roots of Euphorbia pekinensis, two new casbane diterpenoids, named pekinenins A (1) and B (2), were isolated. Their structures were elucidated as 18-hydroxy-1βH,2αH-casba-3E,7E,11E-trien-5-one (1), 5α-methoxy-1βH,2αH-casba-3Z,7E,11E-trien-18-oic acid (2) by a combination of 1D and 2D NMR spectroscopy and mass spectrometry. In the cytotoxicity assay of the two new compounds against Hela, MCF-7, and C6 human cancer cell lines, compound 1 showed moderate cytotoxic activity against two human cancer cell lines, Hela and C6, with IC(50) values of 42.97 and 50.00?μM, respectively.     

泄水圣药论甘遂

甘遂为临床常用中药,古人推崇之为“泄水圣药”.本文通过探讨甘遂在《伤寒论》、《金匮要略》及后世医家的配伍应用,使用指征与剂量,中毒与减毒解毒之法,炮制与煎煮法及其使用注意,为临床合理运用甘遂提供一定的理论依据.     

甘遂和醋甘遂醇提物及其不同极性部位的药效和毒性研究

目的考察甘遂和醋甘遂乙醇提取物及其不同极性部位的泻下作用和毒性。方法采用炭末推进法进行肠推进试验，观察甘遂和醋甘遂醇提物及其石油醚部位、乙酸乙酯部位、正丁醇部位和水部位对小鼠小肠推进和肠水分吸收的影响；急性毒性试验采用改良寇氏法测定其半数致死量（LD50）：结果与对照组相比，甘遂、醋甘遂醇提物、石油醚部位、乙酸乙酯部位可明显促进小肠推进运动。但与生品比较，醋制后各组墨汁推进率皆有所降低，泻下作用有所缓和；甘遂醋制后醇提物毒性下降4倍左右，石油醚部位毒性下降1倍左右，乙酸乙酯部位毒性下降4倍左右，而正丁醇部位和水部位无毒。结论甘遂醋制后泻下作用减弱，毒性显著降低：甘遂的石油醚部位和乙酸乙酯部位既是其药效学部位，又是其毒性部位。     

New 6(17)-epoxylathyrane diterpene: aellinane from Euphorbia aellenii induces apoptosis via mitochondrial pathway in ovarian cancer cell line

Euphorbia species have been used in traditional medicine in many countries for the treatment of cancer. This article aims to evaluate the capability of a new lathyrane diterpene isolated from Euphorbia aellenii to induce apoptosis in the Caov-4 cell line to determine the underlying mechanism of its anticancer effects. A new 6(17)-epoxylathyrane diterpenes: aellinane from Euphorbia aellenii was evaluated for viability of Caov-4 cells by MTT method. Apoptosis induction by lathyrane diterpene was confirmed by annexin V-FITC/PI staining, and caspase-6 activation. The Bcl2 and Bax protein content were detected by Western blot analysis. Finally, we employed the fluorescent ROS detection kit and fluorochrome JC-1 to determine ROS levels and loss of mitochondria membrane potential (ΔΨm) in Caov-4 cells, respectively. The results show that lathyrane diterpene has significant cytotoxic effect against Caov-4 cells. The IC50 value was 45?μM. Annexin V/propidium iodide (PI) staining and caspase-6 activity assay confirmed that lathyrane diterpene is able to induce apoptosis in Caov-4 cells. The results also demonstrate that lathyrane diterpene up-regulated Bax and down-regulated Bcl-2 proteins. Moreover, apoptotic effect of lathyrane diterpene was also related to ROS production and loss of mitochondrial membrane potential (ΔΨm). This study demonstrated that lathyrane diterpene has profound activity against Caov-4 cells. Analysis of apoptosis-related proteins revealed that lathyrane diterpene triggered the mitochondrion-mediated apoptosis pathway, which led to the loss of mitochondrial membrane potential (ΔΨm) and activation of caspase-6. Therefore, we believe that lathyrane diterpene might be a promising natural compound in ovarian cancer therapy.     

中药地锦草芹菜素糖苷类化合物

为了研究中药地锦草抗HBV的活性物质基础,采用大孔树脂、Sephadex LH-20、MCI GEL CHP 20P等色谱方法,从地锦草70%乙醇提取物中分离得到5个芹菜素苷类化合物,通过MS、NMR、2D-NMR等波谱分析手段鉴定了化合物的结构,分别为：芹菜素-7-O-(6"-O-没食子酰)-β-D-葡萄糖苷 (1),芹菜素-7-O-β-D-芹糖(1→2)-β-D-葡萄糖苷 (2),芹菜素-7-O-β-D-芦丁糖苷 (3),芹菜素-7-O-β-D-葡萄糖苷 (4),芹菜素 (5)。化合物1为新化合物,化合物2、3为首次从该植物中分得。
     

高山大戟化学成分的研究

目的对藏药高山大戟的化学成分进行研究。方法利用各种柱色谱对其成分进行分离纯化,通过波谱解析进行结构鉴定。结果从中分离得到15个化合物,分别鉴定为:正二十八烷醇(1),十七烷酸甘油酯(2),正二十六烷醇(3),β-谷甾醇(4),β-胡萝卜苷(5),正十八烷醇(6),豆甾醇(7),芹菜素(8),没食子酸(9),荭草苷(10),槲皮素-4'-O-D-半乳糖(11),甘露醇(12),蔗糖(13),槲皮素-4′-O-β-吡喃葡萄糖苷(14)和木犀草素-5-O-β-D-葡萄糖苷(15)。结论所有化合物均为首次从该种植物中分离得到。