高坤
目前的研究方向是天然有机化学,主要从事西北特色药用植物生物活性成分的提取分离、结构鉴定、生物活性筛选及以计算机辅助手段进行活性分子的构效关系研究,进而进行结构改造或半合成。
个性化签名
- 姓名:高坤
- 目前身份:
- 担任导师情况:
- 学位:
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学术头衔:
博士生导师
- 职称:-
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学科领域:
有机化学
- 研究兴趣:目前的研究方向是天然有机化学,主要从事西北特色药用植物生物活性成分的提取分离、结构鉴定、生物活性筛选及以计算机辅助手段进行活性分子的构效关系研究,进而进行结构改造或半合成。
高坤,女,教授,博士生导师,生于1962年。1983年毕业于兰州大学化学系并留校任教至今,期间于1989获硕士学位,1997年获博士学位,并于2000年9月至2001年9月、2001年10月至2002年1月以及2003年11月先后三次赴法国巴黎第七大学拓扑和动力学研究所留学或做访问教授。现为国家自然科学基金委员会批准的“有机化学创新群体”学术骨干,中国药学会甘肃分会理事,兰州大学化学化工学院有机化学一所所长。目前的研究方向是天然有机化学,主要从事西北特色药用植物生物活性成分的提取分离、结构鉴定、生物活性筛选及以计算机辅助手段进行活性分子的构效关系研究,进而进行结构改造或半合成。近年来在国内外核心刊物发表论文40余篇,半数以上为《SCI》收录论文。 目前负责的在研课题有: 1. 几种西部菊科植物中抑制组蛋白去乙酰化酶的抗癌活性成分萜和苷的研究 (国家自然科学基金)。 2. 化学合成和化学生物学(国家自然科学基金委“有机化学创新群体”基金)。 3. 计算机辅助搜寻药用植物中的药物先导化合物(留学回国人员科研启动基金)。 4. 以组蛋白去乙酰化酶为靶点研究西部药用飞蓬属植物中的抗癌活性成分(教育部重点项目)。 5. 飞蓬属植物的活性成分研究(功能有机分子化学国家重点实验室课题)。
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成果数
10
【期刊论文】Eudesmane derivatives and other constituents from Saussurea parviflora
高坤, Zhong-Duo Yang, Kun Gao, Zhong-Jian Jia*
Phytochemistry 62(2003)1195-1199,-0001,():
-1年11月30日
A survey of the whole plant of Saussurea parviflora afforded three compounds 11,12,13-trihydroxy-4 (15), 8-eudesmadiene-9-one, eudesman-813,12-olide-l-O-13-D-glucoside and 113,313-dihydroxyursa-9(11), 12-diene-3-octadecanoate, as well as 13 known compounds. Their structures were elucidated on the basis of spectral evidence, especially by using NMR spectroscopic techniques. In addition, encelin exhibited effective antitumor activity on L02, SMMC-7721 and HO-8910 cells.
Saussurea parviflora, Compositae, Eudesmane derivatives, Antitumor activity
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高坤, 王文蜀, 贾忠建*
化学学报,2003,61(7):1065-1070,-0001,():
-1年11月30日
从假橐吾全草中分离得到四对新的(1/2,3/4,5/6,7/8)和一对已知的(9/10)8,9-开环艾里莫芬内酯型倍半萜。每一对均为C-8位差向异构体。它们的结构通过波谱方法阐明并通过酰化或酯化分离后得到证实。活性筛选实验表明,1/2和3/4具有细胞毒活性。
假橐吾,, 开链艾里莫芬内酯型倍半萜,, 差向异构体,, 细胞毒活性
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【期刊论文】Eremophilenolides and Other Constituents from the Roots of Liaularia saaitta
高坤
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-1年11月30日
Chemical investigation of the roots of Ligularia sagitta has resulted in the characterization of six eremophilenolides 6β,8βdimethoxy-1Oβ-hydroxyeremophil-7(11)-en-12,8a-olide (1), 6βan-geloyloxy-1Oβ-hydroxy-8β-methoxyeremophil-7(11)-en-12,8a-olide (2), 6/3-(2'-methylbutanoyloxy)-10β-hydroxy-8β-methoxy-eremophil-7(11)-en-12,8a-olide (3), 6β-angeloyloxy-1Oβ-hydro-xy-8a-methoxyeremophil-7(11)-en-12,8β-olide (4), 6β-(2'me-thylbutanoyloxy)-10β-hydroxy-8a-methoxyeremophil-7(11)-en-12.8β-olide (5) and 8β. lOβ-dihvdroxv-6β-methoxveremoohil-7(ll)-en-12,8a-olide (6), together with one monoterpene (3R,4R,65)-3,6-dihydroxy-l-menthene (7), two triterpenes lupeoi (8) and ursolic acid (9), and β-sitosterol (10). The structures of five new constituents (1-5) were elucidated by spectroscopic methods including 2D-NMR experiments. The compounds 1, 5 and 7 showed antibacterial activity by being assayed against Staphylococcus aureus, Bacillus subtilis and Escherichia coll.
Ligularia sagitta
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【期刊论文】Comparative Study of Activities between Verbascoside and Rutin by Docking Method
高坤, Kun Gaoa, b, B o Tao Fan*a, Nadia El Fassia, Krystyna Zakrzewskac, Zhongjian Jiab, Rongliang Zhengd, Annick Panayea, T. Couesnona, and Jean-Pierre Douceta
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-1年11月30日
Verbascoside and rutin possess anti-cancer properties and are capable of repairing DNA damaged by oxygen radicals, acting as powerful antioxidants. Based on kinetic measurements and experiments on tumor cells, docking studies of the two ligand molecules with the receptor telomeric DNA fragments have been carried out. The docking calculations performed using JUMNA software showed that the both molecules can be docked into the minor groove of telomeric DNA and form complexes with suitable geometry for electron transfer between guanine radicaland ligands. The reaction mechanism via the electron transfer process is further confirmed through energy calculations for transition states using MOPAC 93 program. Complexes can be formed without major distortion of DNA structure and are further stabilized by the interaction of DNA with the saccharide side-groups. By comparing their energies, the difference of activities of the two compounds can be explained.
Verbascoside, Rutin, Biological activity, Telomeric Fragment, Docking study
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【期刊论文】Two New Diterpene Acetylxylosides from Aster veitchianus
高坤, Er Wei LI, Kun GAO*, Zhong Jian JIA*
Chinese Chemical Letters Vol. 15, No. 4, pp 425-427, 2004,-0001,():
-1年11月30日
Two new acetylxylosides, ent-manool-13-O-β-D-2'-acetylxylopyranoside (1) and entmanool 13-O-β-D-2', 4'-diacetylxylopyranoside (2) were isolated from Aster veitchianus. Their structures were elucidated by spectroscopic methods.
Aster veitchianus,, Compositae,, diterpene,, xylosides.,
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【期刊论文】A New Stigmasterol and a New Eremophilenolide from Ligularia dolichobotrys
高坤, Er Wei LI, Kun GAO*, Zhong Jian JIA*
Chinese Chemical Letters Vol.15, No.2, pp 194-196, 2004,-0001,():
-1年11月30日
A new stigmasterol 3β, 7α, 22-trihydoxystigmast-5-ene (1) and a new eremophilenolide 8α-methoxy-6β-angeloyloxyeremophil-7(11)-en-8β, 12-olide-14-oic acid (2) were isolated from Ligularia dolichobotrys Diels. Their structures were deduced on the basis of spectral data.
Ligularia dolichobotrys Diels,, Compositae,, stigmasterol,, eremophilanolide.,
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【期刊论文】New Sesquiterpenes from Ligulariopsis shichuana
高坤, Wen-Shu Wang, Kun Gao* and Zhong-Jian Jia*
Journut of the Chinese Chemical Society, 2004, 51, 417-422,-0001,():
-1年11月30日
A thorough investigation of Ligulariopsis shichuana afforded five new sesquiterpenes, including 1β, 10β-epoxy-3a-angeloyloxy-9β-acetoxy-8a, 11β-dihydroxybakkenolide (1), 1β, 7-dihydroxy-3β-acetoxy-noreremophil-6(7),9(10)-dien-8-one (2), 8a-hydroxy-3-oxoeremophil-1 (2),7(11), 9(10)-trien-813(12)-elide (3), 1β, 10β-dihydroxy-3β-acetoxyeremophil-7(11), 8 (9)-dien-8(12)-elide (4) and 1β, 10β-epoxy-8,12-dihy-droxy-3β-acetoxy-9β-angeloyloxyeremophil-7(11)-en-8, 12-disemiketal (5). Their structures were estab-lished by spectroscopic methods and 2D NMR techniques. In addition, bakkenolide (1) and eremophileno-lides (5) showed antibacterial and cytotoxic activities.
Ligulariopsis shichuana, Compositae, Sesquiterpenes, Antibacterial activity, Cytotoxic activity.,
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【期刊论文】Two new compounds from Ligularia dolichobotrys
高坤, ER-WEI LI, KUN GAO, ZHONG-JIAN JIA
,-0001,():
-1年11月30日
Two new compounds, a stigmasterol (1) and an eremophilenolide (2), were isolated from Ligularia dolichobotrys (Diels) together with ten known sesquiterpenoids, two known triterpenes and five known sterols. Their structures were elucidated by spectroscopic methods (IR, MS, 1H, 13C and 2D NMR). In addition, bakkenolide A (3) exhibited effective antitumor activity to human leukemia cells (HL-60), human hepatorna cells (Bel-7402) and human ovarian neoplasm cells (HO-8910).
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【期刊论文】New Eremophilenolides from Ligulariopsis shichuana
高坤, Wenshu Wang, Kun Gao, and Zhongjian Jia*
J. Nat. Prod. 2002, 65, 714-717,-0001,():
-1年11月30日
Four new eremophilenolides, 1-4, have been isolated from the whole plant of Ligulariopsis shichuana. Their structures were elucidated by spectroscopic methods, including 2D NMR experiments. Structures of compounds 1 and 2 were unequivocally established by X-ray diffraction experiments. All of these sesquiterpenes have eremophilane skeletons with 7(11)-en-8(12) lactone units. Compounds 1 and 2 showed moderate antibacterial activities against E. coli and B. subtilis.
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【期刊论文】Bieremoligularolide and eremoligularin, two novel sesquiterpenoids from Ligularia muliensis
高坤, Qiu-Hong Wua, Chun-Ming Wangb, Sheng-Gao Chenga and Kun Gaoa, *
Tetrahedron Letters 45(2004)8855-8858,-0001,():
-1年11月30日
From the roots of Ligularia muliensis, a novel bieremophilanolide and a new eremophilanolide have been isolated and their structures were elucidated by spectroscopic techniques, including HRMS, IR, UV, 1D-NMR, 2D-NMR, and CD spectra.
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