Willipelletierine,a new diterpenoid alkaloid from Consolida scleroclada (Boiss.) Schrod

From the aerial parts of Consolida scleroclada (Boiss.) Schrod. collected in Turkey, a new diterpenoid alkaloid named willipelletierine has been isolated along with the known diterpenoid alkaloids aconitine, lapaconidine, and delcosine. The structure for willipelletierine was established on the basis 1H, 13C, DEPT, homonuclear 1H COSY, HETCOR and NOESY NMR studies.     

Diterpenoid alkaloids from the aerial parts of Aconitum anthora L

Isolation and identification of six diterpenoid alkaloids, from Aconitum anthora L. are described. All proton detected 2D NMR techniques have been used for unambiguous 1H and 13C chemical shift assignments of guan-fu-base-Y (6). This is the first investigation of the diterpenoid alkaloids of this plant species.     

雷公藤中的二萜内酯类成分

目的研究雷公藤(Tripterygium wilfordii Hook.F.)的化学成分。方法应用各种色谱技术进行分离纯化，用UV，IR，¹H NMR，MS，HRMS，¹H-¹H COSY，¹H-¹³C COSY和NOESY等光谱鉴定化合物的结构。结果共分离得到4个化合物：I为16-羟基雷公藤内酯醇(16-hydroxytriptolide)，II为15-羟基雷公藤内酯醇(雷醇内酯，triptolidenol)，III为雷公藤乙素(tripdiolide)，IV为雷公藤乙素的差向异构体，命名为2-表雷公藤乙素(2-epitripdiolide)。结论化合物IV为新二萜内酯化合物。     

Two new diterpenoid alkaloids, beiwusines A and B, from Aconitum kusnezoffii

Two new atisine-type diterpenoid alkaloids, beiwusine A (1) and B (2), have been isolated from the roots of Aconitum kusnezoffii Reichb. Their structures were established on the basis of spectroscopic data. Beiwusines A and B are the first examples of atisine-type diterpenoid alkaloids having a hydroxyl group at C-1. In addition, one known diterpenoid alkaloid spiramine H (3) has been isolated.     

温郁金二萜类化合物C对幽门螺杆菌诱导人胃GES-1上皮细胞炎症的抑制作用及其对NF-κB信号通道的影响

目的通过体外实验研究温郁金二萜类化合物C对幽门螺杆菌(helicobacter pylori,Hp)诱导炎症的抑制作用及对NF-κB信号通路的影响。方法选用Hp I型菌株感染人胃上皮细胞株GES-1,建立体外Hp感染细胞模型,并予不同浓度温郁金二萜类化合物C、阿莫西林等进行干预,ELISA法检测上清液中IL-8、IL-4,并应用Wester blot方法检测NF-κB中p65、IKKα、IKKβ蛋白表达。结果 MTT法显示温郁金二萜类化合物C对胃GES-1细胞的IC5为5 mg.L-1,阿莫西林为5 mg.L-1,Hp作用于人胃GES-1上皮细胞后,上清液中IL-8明显升高,其中以12 h浓度最高,而予不同浓度温郁金二萜类化合物C、阿莫西林组干预后,IL-8水平在各个时间段均低于模型组,其中以高浓度温郁金二萜类化合物C组下降最为明显(P<0.05)。而IL-4水平在Hp作用于人胃GES-1细胞后下降,予中浓度温郁金二萜类化合物C组、高浓度二萜类化合物C组干预后IL-4水平明显升高(P<0.05)。温郁金二萜类化合物C具有抑制Hp促p65进入胞核,抑制Hp所刺激的IkBα的降解,抑制p65、IkBα磷酸化,抑制蛋白IKKα、IKKβ的表达等作用。结论 NF-κB信号通路在Hp引起慢性胃炎的发病机制中起到核心作用,采用温郁金二萜类化合物C可阻断NF-κB信号通路,可以有效减少Hp诱导的促炎性因子的分泌与增加抑炎因子的分泌。     

Diterpenoid alkaloids from the roots of Aconitum brachypodum Diels

A new diterpenoid alkaloid, named bullatine H (1), along with 10 known diterpenoid alkaloids were isolated from the roots of Aconitum brachypodum Diels (Ranunculaceae). The structure of 1 was elucidated by analysis of its spectroscopic data. It should be noted that compound 1 is the first example with 11, 13-dioxygenated denudatine-type diterpenoid alkaloid isolated from Aconitum brachypodum.     

Alkaloids from roots of Aconitum crassicaule

From the roots of ACONITUM CRASSICAULE, four diterpenoid alkaloids were isolated. Two of these were identified as chasmanine (5) and yunaconitine (4). The other two, Crassicauline A and Crassicauline B, are new alkaloids. The structure of crassicauline A, C (35)H (49)O (10)N, has been elucidated as structure (1) on the basis of chemical and spectral data, while the structure of crassicauline B, C (27)H (31)O (4)N, is still to be determined.     

Cytotoxic diterpenoids from Euphorbia pekinensis

A new diterpenoid, named euphpekinensin, along with three known diterpenoids, was isolated from the roots of Euphorbia pekinensis for the first time and the structures were elucidated by spectral analysis. The 2D-NMR techniques such as 1H-1H COSY, HMQC, HMBC and NOESY spectra were mainly applied to determine the structure of the new diterpenoid. The four diterpenoids showed cytotoxic activity against human KB cells in vitro.     

Structures of Crassicaulisine and Crassicaulidine, two New Diterpenoid Alkaloids

From the roots of ACONITUM CRASSICAULE, two new diterpenoid alkaloids, crassicaulisine and crassicaulidine, were isolated. The structure of crassicaulisine, C (24)H (39)O (7)N, has been elucidated as 3 on the basis of chemical and spectral data, while the structure of crassicaulidine, C (24)H (39)O (8)N, has been shown as 4 on the basis of chemical data and spectral comparison with crassicaulisine.     

三叶鼠尾草中小红参醌丙的结构

从三叶鼠尾草(Salvia trijuga Diels)的干燥根中分得9种结晶性成分,经鉴定为铁锈醇(ferruginol)、柳杉酚(sugiol)及系列高级脂肪酸三十四酸、三十酸、二十八酸、十六酸,另两种酸分别为对羟苯甲酸及氨基酸(dl-homoserine),晶Ⅰ为一新化合物,定名为小红参醌丙(trijuganone C),经光谱分析及化学反应推定其结构为15,16-二氢丹参酸甲酯。     

温郁金中新二萜类化合物C诱导人结肠腺癌SW620细胞凋亡的相关通路研究

目的探讨温郁金二萜类化合物C诱导人结肠腺癌SW620细胞凋亡的作用机制。方法以5-氟脲嘧啶(5-Flu-orouracil,5-FU)为阳性对照药物;采用噻唑蓝(methyl thia-zolyl tetrazolium,MTT)还原法检测化合物C和5-FU对SW620细胞增殖的影响;用流式细胞术(flow cytometry,FCM)检测两种药物诱导细胞凋亡的情况;用Western blot法检测化合物C作用后,细胞中ERK、p-ERK、JNK、p-JNK、p38、p-p38及caspase-3蛋白水平的变化。结果化合物C能抑制SW620细胞的增殖活性,并明显诱导细胞凋亡,其抑制率和凋亡率呈时间-浓度依赖性,且都明显高于5-FU组;其24、48和72 h的IC50分别为29.75、15.91和6.55 mg.L-1;化合物C能浓度依赖性地下调细胞中ERK、JNK、p38及其相应磷酸化蛋白的水平,并刺激caspase-3的蛋白表达。结论温郁金二萜类化合物C能抑制人结肠腺癌SW620细胞的生长并诱导凋亡,其作用机制可能与抑制MAPK信号转导通路、活化caspase-3有关。     

A new cassane diterpenoid from the seeds of Caesalpinia decapetala

Phytochemical investigation on the seeds of Caesalpinia decapetala led to the isolation of a new cassane diterpenoid with an unusual O bridge between C-19 and C-20, named phanginin Q (1), together with three known cassane diterpenoids, caesaljapin (2), caesaldekarin A (3), and caesaldekarin B (4). The structure of the new compound was elucidated by spectroscopic methods, including ¹H NMR, ¹³C NMR, HSQC, ¹H ? ¹H COSY, HMBC, NOESY, and HR-ESI-MS.     

Gerardianin A, a new abietane diterpenoid from Isodon lophanthoides var. gerardianus

A new abietane diterpenoid, gerardianin A (1), along with a known compound 6,7-dehydroroyleanone (2), has been isolated from the aerial parts of Isodon lophanthoides var. gerardianus [Bentham] H. Hara. The structure of 1 was determined on the basis of spectroscopic methods and X-ray single-crystal diffraction analysis.     

C19型二萜生物碱药理活性和毒性研究进展

C19型二萜生物碱是一类来源广泛、结构复杂、生物活性多样的植物成分,一直以来为化学家和药理学家所重视.本文综述了近年来C19型二萜生物碱的药理活性和毒性研究进展,为其深度开发利用提供一定参考.     

Structures of two diterpenoid dimers from bulbs of Fritillaria ebeiensis

A new ent-kaurane diterpenoid dimer, fritillebinide C (1) together with one known diterpenoid dimer fritillebinide B (2) were isolated from the bulbs of Fritillaria ebeiensis G.D. Yu et G.Q. Ji. Compound 1 has been determined to be ent-3β-acetoxy-kauran-16β, 17-acetal entβ-kauran-17(S)-aldehyde (1) by means of spectral analysis and chemical evidence.     

A new diterpenoid alkaloid from Aconitum jaluense

A new diterpenoid alkaloid, jaluenine (1), has been isolated from the roots of Aconitum jaluense. The structure of jaluenine was determined by spectroscopic methods including two dimensional NMR (¹H-¹H COSY, HMQC, HMBC, NOESY).     

假细锥香茶菜新二萜成分——假细锥甲素的结构

从假细锥香茶菜(Rabdosia coetsoides C.Y.Wu)叶分离得到新二萜成分,根据紫外光谱、红外光谱、质谱、核磁共振氢谱及碳谱等分析,推定了化学结构,并经X-射线衍射确证,命名为假细锥甲素。     

Biological activity of guanacastepene, a novel diterpenoid antibiotic produced by an unidentified fungus CR115

Fermentation extracts of culture CR115, an unknown plant endophyte originally isolated from Costa Rica, were found to be active against antibiotic-resistant bacteria. The metabolite responsible for activity was identified as a novel diterpenoid antibiotic guanacastepene (mol. wt. 374.47 and mol. formula C22H30O5). Mechanistic studies done in an E. coli imp strain suggested membrane damage as the primary mode of bactericidal action. This compound also lysed human RBCs and caused leakage of intracellular potassium from E. coli imp.     

New diterpenoid antibiotics, spirocardins A and B

New antibiotics spirocardins A and B were isolated from the culture broth of an actinomycete isolated from a soil sample collected near Lake Hibara, Fukushima Prefecture, Japan. The producing strain was classified as Nocardia sp. SANK 64282. The antibiotics were isolated from the culture filtrate by solvent extraction and purified further by silica gel and preparative reverse phase column chromatography. They were primarily active against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus and limited species of Gram-negative bacteria such as Bacteroides fragilis and Klebsiella pneumoniae. They were also moderately active against several species of Mycoplasma. The molecular formulae of spirocardins A and B were C20H30O6 and C20H32O6, respectively. From their physico-chemical characteristics they were revealed to be diterpenoid antibiotics with closely related structures and the former was easily converted to the latter by the reduction with NaBH4.     

直缘乌头根中生物碱成分的研究

目的：研究直缘乌头（Aconitum transsectum Diels.）根中的生物碱成分。方法：采用pH梯度、中压柱层析、常压硅胶柱层析及离心薄层层析法。结果：分得11个已知二萜生物碱，由光谱法分别鉴定为：滇乌碱（yunaconitine）、印乌碱（indaconitine）、黄草乌碱甲（vilmorrianine A）、黄草乌碱丙（vilmorrianine C）、草乌甲素(crassialine A)、膝乌碱（geniconitine）、查斯曼宁（chasmanine）、８－去乙酰滇乌碱（8-deacetylyunaconitine）、塔拉萨敏（talatisamine）、14-乙酰塔拉萨敏（14-acetyltalatisamine）和chasmaconitine。结论：黄草乌碱甲和chasmaconitine是首次从该植物中分离得到。