ent-Kaurane diterpenoids from the plant Wedelia trilobata

Four new ent-kaurane diterpenoids,namely,3α-tigloyloxypterokaurene L_(3)(1),ent-17-hydroxy-kaura-9(11),15-dien-19-oic acid(2),and wedelobatins A(3)and B(4),together with 11 known ent-kaurane diterpenoids(5-15),were isolated from the ethanol extract of Wedelia trilobata.All the structures of 1-15 were elucidated on the basis of spectroscopic studies.

Two New ent-Kaurane Diterpenoids from Isodon xerophilus

Two new ent-kaurane diterpenoids, xerophilusin E (1) and xerophilusin F (2), were isolated from the leaves of Isodon xerophilus. Their structures were determined as 3, 20: 7, 20-diepoxy-ent-kaur-16-en-15-one and 7 beta, 14 beta, 20 (R)-trihydroxy-11 beta-acetoxy-7,20-cyclo-ent-kaur-16-en-6, 15-dione, respectively, by spectral methods and X-ray crystallographic analysis.

Two new ent-kaurane diterpenoids from Isodon henryi

Two new ent-kaurane diterpenoids, minheryins H （1） and I （2）, were isolated from the leaves of Isodon henryi. Their structures were elucidated by means of spectroscopic analysis, including 2D NMR spectra.

Isorosthornins A-C,new ent-kaurane diterpenoids from Isodon rosthornii

Three new ent-kauranoids,isorosthornins A-C(1-3),and a new natural product,dihydroponicidin(4),together with five known ones were isolated from the aerial parts of Isodon rosthornii.The structures were determined by means of extensive spectroscopic analysis.All diterpenoids isolated were evaluated for their cytotoxicity against HL-60,SMMC-7721,A-549,MCF-7,and SW480 cell lines,and compounds 5 and 7 showed significant inhibitory effects on all cell lines.

Two new ent-kaurane diterpenoids from Isodon excisoides

Two new ent-kaurane diterpenoids taihangexcisoidesin A and B （1 and 2）, were isolated from the EtOAc extract of the leaves of lsodon excisoides. Their structures were determined on the basis of spectroscopic methods.

Characterization of New Ent-kaurane Diterpenoids of Yunnan Arabica Coffee Beans

Five new ent-kaurane diterpenoids,named mascaroside Ⅲ–Ⅴ(1–3),and 20-nor-cofaryloside Ⅰ–Ⅱ(4–5),together with seven known diterpenoids,were isolated from methanol extracts of the green coffee beans of Yunnan Arabica Coffee.Their chemical structures were elucidated by extensive spectroscopic analyses.Meanwhile,cytotoxicity assay against HL-60,A-549,SMMC-7721,MCF-7 and SW480 cell lines showed that they have not evident inhibition of cytotoxicity.

A New ent-Kaurane Diterpenoid from Isodon enanderianus

A new spirosecokaurenoid, enanderinanin F 1 and its C-6 epimer, angustifolin were isolated from the aerial parts of Isodon enanderianus. The structure of 1 was determined on the basis of spectral data, especially by 2D techniques. The C-13 NMR data of angustifolin were revised by 2D NMR.

ent-Kaurane Diterpenoids from Isodon eriocalyx var. laxiflorat

Four new ent-kaurane diterpenoids, 6fl,13ct,15fl-trihydroxy-16-ene-3a,20-epoxy-ent-kaur- 1,7-dione （1）, 6-hydroxy-3a,20-epoxy-5（6）-ene-ent-kaur-l,7,15-trione （2）, 6-hydroxy-15fl-acetoxy-3a,20-epoxy-16]3,17-epoxy- 5（6）-ene-ent-kaur-l,7-dione （3）, 3ct,17-dihydroxy-15（16）-ene-ent-kaur-7-one （4）, along with four known com- pounds 5--8 were isolated from the leaves oflsodon eriocalyx var. laxiflora. The structures were elucidated by ex- tensive spectroscopic methods （IR, UV, MS and NMR）. The cytotoxic activities of these compounds were evaluated by MTT assay. Compound 8 showed moderate inhibitory effects on HL-60, SMMC-7721, MCF-7 and SW-480 cell lines.

Two new ent-kaurane diterpenoids from the aerial parts of Isodon excisoides

Two new ent-kaurane diterpenoids, ent-7α,14β-dihydroxykaur-16-en-15-one-20-oic acid （1） and 1,7α,12β,14β-tetrahydroxy-1,10-seco-ent-kaur-10,16-dien-15-one （2）, together with six known ones （3-8）, were isolated from the EtOAc extract of the aerial parts of lsodon excisoides. Their structures were elucidated on the basis of 1D NMR and 2D NMR analyses as well as HR-ESI-MS experiments.

6,7-seco-ent-Kaurane diterpenoids from Isodon sculponeatus and their bioactivity

One new 6,7-seco-ent-kaurane diterpenoid, sculponin T （1）, was isolated from the aerial parts of lsodon sculponeatus, along with four known analogs, sculponeatin J （2）, sculponeatin K （3）, sculponeatin C （4）, and sculponeatin Q （5）. Their structures were elucidated by extensive spectroscopic analysis and by comparison with data reported in the literature. Significant cytotoxic activity was observed for compound 2 against five human tumor cell lines with IC50 values ranging from 1.8 μmol/L to 3.3 μmol/L, and it also inhibited NO production in LPS-stimulated RAW264.7 cells, with IC50 value of 3.3 μmol/L.

Fimbrialtols K–M, highly functionalized ent-kaurane diterpenoids from traditional Chinese plant Flickingeria fimbriata(B1.) Hawkes

Three new ent-kaurane diterpenoids fimbrialtols K–M（3–5） with highly substituted functionalities were isolated from the extract of Flickingeria fimbriata（B1.） Hawkes. The structures of these new compounds were determined by NMR and HR-ESIMS. The relative configurations of these compounds were determined by analysis of NOESY correlations. The absolute configurations of these new compounds were established by CD methods together with considering the biosynthetic pathway. Compounds 3 and4 contain a cinnamic carboxyl group, whereas compound 5 possesses a benzoic carboxyl group representing the first report in more than known 600 ent-kaurane diterpenoids.

Scopariusols L–T, nine new ent-kaurane diterpenoids isolated from Isodon scoparius

Nine new ent-kaurane diterpenoids, named scopariusols L–T(1–9), were isolated from the aerial parts of Isodon scoparius. Their structures were characterized mainly by analyzing the NMR and HR-ESI-MS data, and the absolute configuration of 1 was determined by single-crystal X-ray diffraction. Compound 1 was active against five human tumor cell lines(HL-60, SMMC-7721, A-549, MCF-7, and SW-480), and it also inhibited NO production in LPS-stimulated RAW264.7 cells, with an IC50 value of 0.6 μmol·L-1.

New ent-kaurane-type diterpenoids from Isodon nervosus

二新 ent-kaurane-type diterpenoids， 6 β， 7 β， 13-trihydroxy-1-acetoxy-7,20-epoxy-ent-kaur-16-en-15-one (1 ) 和 15 β - hydroxy-6,7-seco-6,11 β: 6,20-diepoxy-1,7-olide-ent-kaur-16-ene (2 ) 从 Isodon nervosus 被孤立，并且结构被分光镜分析阐明。

Isolation and Crystal Structure of Ent-kaurane Diterpenes from Rubus corchorifolius L. f.

In this study, ent-Kaurane-3β,16β,17-trioi （1） and ent-kaurane-2a,16β,17-triol （2）, were isolated from the leaves ofRubus corchorifolius L. f. Their structures were elucidated based on extensive spectroscopic analysis. NMR experiments identified the two compounds and X-ray crystallographic analysis confirmed their crystal structures. The crystal of 1 belongs to monoclinic with space group P21 and a = 10.7641（3）, b = 7.2789（3）, c = 11.7862（4） A, β = 95.275（3）°, V = 919.55（6） A3, Z = 2, C20H34O4, Mr = 322.49 g/mol, Dc = 1.230 g/m3, F（000） = 376, 2 = 1.54178 A,μ = 0.661 mm-1, R = 0.0319, and wR = 0.0811 for 10889 observed reflections （I〉 2σ（I））. The crystal of 2 is classified as orthorhombic with space group P212121 and a = 10.7641（3）, b = 12.72224（19）, c = 21.3929（3） A, V= 1748.94（4） A3, Z= 4, C20H3404, Mr = 322.47, De = 1.225 Mg/m3 F（000） = 712, λ = 1.54184 A,μ = 0.625 mm-1, R = 0.0303 and wR = 0.0759 for 10470 observed reflections （1〉 2σ（I））. Meanwhile, the compound revealed low inhibitory activities toward HepG2, MCF-7, and SCG-7901 cells.

醋乳香现代研究进展及质量标志物的预测

醋乳香是乳香Olibanum经醋炙法加工后的炮制品,炮制后可除去部分挥发油成分,消除其对胃黏膜的刺激性,同时能引药入经增强活血止痛、收敛生肌等功效。通过总结文献报道,从醋炙后化学成分与功效变化,刺激性研究,成分特有性、有效性、可测性,配伍环境及体内过程相关性等方面对醋乳香的质量标志物(Q-marker)进行预测分析,初步确定3-乙酰基-9,11-去氢-β-乳香酸、3-乙酰基-α-乳香酸、3-乙酰基-β-乳香酸、11-羰基-β-乳香酸、11-羰基-β-乙酰乳香酸5个三萜类成分和挥发油类成分乙酸辛酯为其可能的Q-marker,以期为醋乳香的全程质量评价、临床应用研究提供理论依据。

马醉木二萜成分及其乙酰胆碱酯酶抑制活性研究

为研究马醉木叶中的二萜成分及其乙酰胆碱酯酶抑制活性,该研究根据薄层色谱显色特征,使用硅胶、MCI和半制备高效液相等色谱技术对其进行分离与纯化,并通过波谱数据(NMR和MS)分析且结合文献报道数据进行对比,鉴定了所得化合物的结构,同时采用Ellman法首次对其乙酰胆碱酯酶抑制活性进行评价。结果表明:从马醉木叶中分离并鉴定了8个二萜化合物,分别是pierisformoside F(1)、3-epi-grayanotoxinⅩⅧ(2)、3-epi-grayanotoxin B(3)、asebotoxin-X(4)、pierisformosin B(5)、asebotoxinⅢ(6)、rhodojaponinⅢ(7)和pierisformosin C(8)。其中,化合物1为首次从该植物中分离得到,化合物8表现出乙酰胆碱酯酶抑制活性。综上表明,马醉木中含有丰富的二萜成分和活性成分。该研究结果丰富了马醉木的化学成分多样性,为其后续综合开发和利用提供了一定的理论依据,也为寻求更多的活性成分提供了借鉴。