2015年, 第5卷, 第2期　
刊出日期：2015-04-24

  

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Original article
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  Cycloartane Glycosides from the Roots of Cimicifuga foetida with Wnt Signaling Pathway Inhibitory Activity

  Di-Fan Zhu, Guo-Lei Zhu, Ling-Mei Kong, Ni-Man Bao, Lin Zhou, Yin Nian, Ming-Hua Qiu

  应用天然产物. 2015, 5(2): 61-67. https://doi.org/10.1007/s13659-015-0053-7

  摘要 ( 7604) PDF全文 ( 11054 )   可视化   收藏

  Four new 9, 19-cycloartane triterpenoids, cimilactone E(1), cimilactone F(2), 20-O-(E)-butenoyl-23-epi-26-deoxyactein(3), and 20, 12β-O-diacetylcimiracemonol-3-O-β-D-xylopyranoside(4), together with four known constituents(5-8) were isolated from the roots of Cimicifuga foetida. The new structures were elucidated by extensive spectroscopic analysis. In addition, compounds 7 and 8 showed significant Wnt signaling pathway inhibitory activity, with IC₅₀ values of 3.33 and 13.34 μM, respectively, using the luciferase reporter gene assay.
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  New Diterpenes from Cultures of the Fungus Engleromyces goetzii and Their CETP Inhibitory Activity

  Yang Wang, Ling Zhang, Fang Wang, Zheng-Hui Li, Ze-Jun Dong, Ji-Kai Liu

  应用天然产物. 2015, 5(2): 69-75. https://doi.org/10.1007/s13659-015-0055-5

  摘要 ( 7417) PDF全文 ( 10965 )   可视化   收藏

  One new cleistanthane-type diterpene named engleromycenolic acid A(1), one new rosane-type diterpene named engleromycenolic acid B(2) and one new natural rosane-type diterpene, engleromycenol(3), along with three known rosanetype diterpenes, rosololactone(4), rosenonolactone(5) and 7-deoxyrosenonolactone(6) were isolated from cultures of the fungus Engleromyces goetzii, where it naturally grows on Alpine bamboo culms. The new compounds were elucidated based on their spectroscopic data. In addition, compounds 1-6 were evaluated for their cholesterol ester transfer protein(CETP) inhibition activity. This paper reports the isolation, structural elucidation, and CETP inhibition activity of these compounds.
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  New Dimeric and seco-Abietane Diterpenoids from Salvia wardii

  Qiu-Li Xiao, Fan Xia, Xing-Wei Yang, Yang Liao, Li-Xin Yang, Yu-Kun Wei, Xian Li, Gang Xu

  应用天然产物. 2015, 5(2): 77-82. https://doi.org/10.1007/s13659-015-0054-6

  摘要 ( 7686) PDF全文 ( 11040 )   可视化   收藏

  Two dimeric abietane diterpenoids, salviwardins A and B(1 and 2), and a seco-abietane diterpenoid salviwardin C(3), along with five known analogues(4-8), were isolated from the roots of Salvia wardii. The structures of these isolates were elucidated by extensive spectroscopic methods. The inhibitory activities of these isolates against five human cancer cell lines in vitro were also tested.
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  Synthesis and Anticancer Activity of 4β-Triazole-podophyllotoxin Glycosides

  Cheng-Ting Zi, Gen-Tao Li, Yan Li, Jun Zhou, Zhong-Tao Ding, Zi-Hua Jiang, Jiang-Miao Hu

  应用天然产物. 2015, 5(2): 83-90. https://doi.org/10.1007/s13659-015-0057-3

  摘要 ( 7552) PDF全文 ( 11108 )   可视化   收藏

  A series of novel 4β-triazole-podophyllotoxin glycosides were synthesized by utilizing the Click reaction. Evaluation of cytotoxicity against a panel of five human cancer cell lines(HL-60, SMMC-7721, A-549, MCF-7, SW480) using MTT assay shows that most of these compounds show weak cytotoxicity. It was observed that compound 16 shows the highest activity with IC₅₀ values ranging from 2.85 to 7.28 μM, which is more potent than the control drugs etoposide and cisplatin against four of five cancer cell lines tested. Compound 16 is characterized with an α-D-galactosyl residue directly linked to the triazole ring and a 4'-OH group on the E ring of the podophyllotoxin scaffold. HPLC investigation of representative compound indicates that incorporation of a sugar moiety seems to improve the chemical stability of the podophyllotoxin scaffold.
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  Biflavone Ginkgetin,a Novel Wnt Inhibitor,Suppresses the Growth of Medulloblastoma

  Zhen-Nan Ye, Mu-Yuan Yu, Ling-Mei Kong, Wei-Hua Wang, Yuan-Feng Yang, Jie-Qing Liu, Ming-Hua Qiu, Yan Li

  应用天然产物. 2015, 5(2): 91-97. https://doi.org/10.1007/s13659-015-0056-4

  摘要 ( 7384) PDF全文 ( 11071 )   可视化   收藏

  Medulloblastoma(MB) is a form of malignant brain tumor that predominantly arises in infants and children, of which approximately 25% is due to upregulation of canonical Wnt pathway with mainly mutations in CTNNB1. Therefore, Wnt inhibitors could offer rational therapeutic strategies and chemoprevention for this malignant cancer. In our present study, we undertook a screening for antagonists of Wnt signaling from 600 natural compounds, and identified Ginkgetin, a biflavone isolated from Cephalotaxus fortunei var. alpina. Ginkgetin inhibited Wnt pathway with an IC₅₀ value around 5.92 μM and structure-activity relationship analysis suggested the methoxy group in Ginkgetin as a functional group. Biflavone Ginkgetin showed obvious cytotoxicity in Daoy and D283 MB cells. Cell cycle analysis by flow cytometry showed that Ginkgetin induced efficiently G₂/M phase arrest in Daoy cells. Further mechanism studies showed that Ginkgetin reduced the expression of Wnt target genes, including Axin2, cyclinD1 and survivin in MB cells. The phosphorylation level of β-catenin also decreased in a time-and concentration-dependent manner. Collectively, our data suggest that Ginkgetin is a novel inhibitor of Wnt signaling, and as such warrants further exploration as a promising antimedulloblastoma candidate.
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  A Viscidane Diterpene and Polyacetylenes from Cultures of Hypsizygus marmoreus

  Ling Zhang, Zheng-Hui Li, Ze-Jun Dong, Yan Li, Ji-Kai Liu

  应用天然产物. 2015, 5(2): 99-103. https://doi.org/10.1007/s13659-015-0058-2

  摘要 ( 7720) PDF全文 ( 11075 )   可视化   收藏

  Investigation on the cultures of Hypsizygus marmoreus resulted in the isolation of a new viscidane diterpene, 8-oxoviscida-3, 11(18)-diene-13, 14, 15, 19-tetraol(1) and two new polyacetylenes,(E)-10-(1, 1-dimethyl-2-propenyloxy)-2-decene-4, 6, 8-triyn-1-ol(2) and 10-(1, 1-dimethyl-2-propenyloxy) deca-4, 6, 8-triyn-1-ol(3), together with two known polyacetylenes,(E)-2-decen-4, 6, 8-triyn-1-ol(4) and 4, 6, 8-decatriyn-1-ol(5). Their structures were elucidated on the basis of extensive spectroscopic studies. Compound 1 is the first finding of viscidane diterpene in mushrooms. Compounds 1, 3 and 5 were tested for cytotoxicity against human tumor cell lines HL-60, SMMC-7721, A-549, MCF-7 and SW-480. None of the compounds showed cytotoxic activity(IC₅₀>40 μM).
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  Minor Prenylated Flavonoids from the Twigs of Macaranga adenantha and Their Cytotoxic Activity

  Da-Song Yang, Shuang-Mei Wang, Wei-Bing Peng, Yong-Ping Yang, Ke-Chun Liu, Xiao-Li Li, Wei-Lie Xiao

  应用天然产物. 2015, 5(2): 105-109. https://doi.org/10.1007/s13659-015-0059-1

  摘要 ( 7636) PDF全文 ( 10857 )   可视化   收藏

  Three new minor prenylated flavonoids, named macadenanthins A-C(1-3), together with three known ones(4-6), were isolated from the twigs of Macaranga adenantha. Their structures were elucidated on the basis of extensive spectroscopic analysis including NMR, UV and MS. The prenyl moieties in compounds 1-3 were further modified by cyclization and hydroxylation. The new compounds were tested for their cytotoxicity against four cancer cell lines(MCF-7, Hep G2, Hela and P388) and showed IC₅₀ values in the range of 13.76-22.27 μM.