Phytochemical investigation on the whole plant of Inula cappa led to the isolation of two new germacrane-type sesquiterpene lactones,ineupatolides D and E（1 and 2）,together with three known analogs.The structures of...Phytochemical investigation on the whole plant of Inula cappa led to the isolation of two new germacrane-type sesquiterpene lactones,ineupatolides D and E（1 and 2）,together with three known analogs.The structures of the new compounds were established by extensive analysis of 1Dand 2DNMR spectra,as well as MS data.Their absolute configurations were determined by CD spectra.All compounds showed moderate inhibitory effects on A431,A549,BGC-823,HL-60,HT-29,and MCF-7 cancer cell lines with IC50 values ranging from 2.1 to 36.3 μM.展开更多
Two new sesquiterpene esters, 3b, 6b, 8a-triacetyl-4b, 5a-epoxy -1- oxogermacr- 10(14)-ene (1) and 3b, 6b, 8a-triacetyl-4b, 5a-epoxygermacr-1(10)-ene (2) were isolated from the whole plant of Salvia roborowskii Maxim....Two new sesquiterpene esters, 3b, 6b, 8a-triacetyl-4b, 5a-epoxy -1- oxogermacr- 10(14)-ene (1) and 3b, 6b, 8a-triacetyl-4b, 5a-epoxygermacr-1(10)-ene (2) were isolated from the whole plant of Salvia roborowskii Maxim. Their structures were elucidated by means of spectral data (2DNMR and HRMS).展开更多
榄香烯是我国拥有自主知识产权的抗肿瘤药物之一,因其抗肿瘤活性强、作用范围广、毒副作用轻微和不易产生耐药性等优点,被广泛应用于各类恶性肿瘤的临床治疗中。榄香烯的生产主要依靠药用植物温郁金的分离提取。但温郁金的榄香烯含量低...榄香烯是我国拥有自主知识产权的抗肿瘤药物之一,因其抗肿瘤活性强、作用范围广、毒副作用轻微和不易产生耐药性等优点,被广泛应用于各类恶性肿瘤的临床治疗中。榄香烯的生产主要依靠药用植物温郁金的分离提取。但温郁金的榄香烯含量低、分离纯化难度大、得率低且成本高,严重阻碍了榄香烯的大规模生产与应用。随着合成生物学的发展,利用微生物构建细胞工厂用于生物合成天然药物成为研究热点,也为榄香烯的生产提供了新的思路。近年来,对榄香烯的生物合成研究在不断深入。研究者通过代谢工程、组合生物学和基因工程等手段,阐明榄香烯生物合成途径和关键酶,已经成功克隆了榄香烯生物合成途径上的一些关键酶基因,初步实现榄香烯的异源生物合成。本文以合成生物学研究思维概述榄香烯生物合成途径及其工程菌的优化,重点综述关键酶吉马烯A合酶(germacrane A synthase,GAS)。从限速酶基因的过表达和分流基因的敲除,融合表达酶工程策略、吉马烯A合酶的体外进化几方面,对其生物合成途径的改造策略进行阐述。同时,也分析提高异源生物合成榄香烯产量所面临的问题与挑战,为榄香烯的高效生物合成提供参考。展开更多
A new sesquiterpene with a unusual modified germacrane skeleton was isolated from the ethanol extracts of the roots of Biondia hemsleyana and its structure was elucidated as 3β-hydroxy- 4,14-cyclogermacra-11-en-9-one...A new sesquiterpene with a unusual modified germacrane skeleton was isolated from the ethanol extracts of the roots of Biondia hemsleyana and its structure was elucidated as 3β-hydroxy- 4,14-cyclogermacra-11-en-9-one by the spectroscopic methods and X-ray crystallography.展开更多
Nine new germacranolides,sylvaticalides A−H(1-9),and three known analogues(10-12)were isolated from the aeri-al part of Vernonia sylvatica.Their structures were established using comprehensive spectroscopic analysis,i...Nine new germacranolides,sylvaticalides A−H(1-9),and three known analogues(10-12)were isolated from the aeri-al part of Vernonia sylvatica.Their structures were established using comprehensive spectroscopic analysis,including high-resolution electrospray ionization mass spectroscopy(HR-ESI-MS)and 1D and 2D nuclear magnetic resonance(NMR)spectra.Their absolute configurations were determined by X-ray diffraction experiments.The anti-inflammatory activities of all isolated compounds were as-sessed by evaluating their inhibitory effects on the nuclear factor kappa B(NF-κB)pathway,which was activated by lipopolysacchar-ide(LPS)-stimulated human THP1-Dual cells,and the interferon-stimulated gene(ISG)pathway,activated by STING agonist MSA-2 in the same cell model.Compounds 1,2 and 6 showed inhibitory effects on the NF-κB and ISG signaling pathways,with IC_(50)values ranging from 4.12 to 10.57μmol·L^(−1).展开更多
Ten new germacrane-type sesquiterpenoids,artemyrianosins A-J(1-10),were isolated from the aerial parts of Arte-misia myriantha.Their structures were elucidated by spectral analyses including UV,IR,HRESIMS,1D and 2D NM...Ten new germacrane-type sesquiterpenoids,artemyrianosins A-J(1-10),were isolated from the aerial parts of Arte-misia myriantha.Their structures were elucidated by spectral analyses including UV,IR,HRESIMS,1D and 2D NMR,ECD and the absolute configurations of compounds 1 and 7-9 were characterized using X-ray crystallography.All isolates were tested their cytotoxicity against three human hepatoma cell lines(HepG2,Huh7,and SK-Hep-1),and com-pounds 1-3,7,and 10 showed cytotoxicity with IC50 values ranging from 43.7 to 89.3μM.Among them,the most active compound 3 exhibited activity against three human hepatoma cell lines with IC50 values of 43.7μM(HepG2),47.9μM(Huh7),and 44.9μM(SK-Hep-1).展开更多
Two new germacranes, chrysanthemumins C （1） and D （2）, and five eudesmanes, chrysanthemumols I-K （3- 5） as new ones, eudesm-4（14）-ene-3a,11-diol （6） and canusesnol E （7）, were isolated from the ethyl aceta...Two new germacranes, chrysanthemumins C （1） and D （2）, and five eudesmanes, chrysanthemumols I-K （3- 5） as new ones, eudesm-4（14）-ene-3a,11-diol （6） and canusesnol E （7）, were isolated from the ethyl acetate soluble fraction of 95% EtOH extract of the flowers of Chrysanthemum indicum. The structures of isolated sesquiterpe- noids were elucidated on basis of extensive spectroscopic evidences.展开更多
基金Financial support from the National Science and Technology Major Project"Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09301001-001,2015ZX09103002)the National Natural Science Funds of China(Nos.81302657,81573305,81473112)+3 种基金Youth Innovation Promotion Association CAS,the Ministry of Science and Technology(No.2010DFA30980)the Chinese Academy of Sciences(No.KSZD-EW-Z-004-01)the Shanghai Commission of Science and Technology(No.11DZ1970700,12JC1410300)the Research Fund of University of Macao(MYRG2014-00020-ICMS-QRCM and MYRG2015-00153ICMS-QRCM)
文摘Phytochemical investigation on the whole plant of Inula cappa led to the isolation of two new germacrane-type sesquiterpene lactones,ineupatolides D and E（1 and 2）,together with three known analogs.The structures of the new compounds were established by extensive analysis of 1Dand 2DNMR spectra,as well as MS data.Their absolute configurations were determined by CD spectra.All compounds showed moderate inhibitory effects on A431,A549,BGC-823,HL-60,HT-29,and MCF-7 cancer cell lines with IC50 values ranging from 2.1 to 36.3 μM.
基金the Natural Science Foundation of Gansu Province(No.25001-A25-001-2)
文摘Two new sesquiterpene esters, 3b, 6b, 8a-triacetyl-4b, 5a-epoxy -1- oxogermacr- 10(14)-ene (1) and 3b, 6b, 8a-triacetyl-4b, 5a-epoxygermacr-1(10)-ene (2) were isolated from the whole plant of Salvia roborowskii Maxim. Their structures were elucidated by means of spectral data (2DNMR and HRMS).
文摘榄香烯是我国拥有自主知识产权的抗肿瘤药物之一,因其抗肿瘤活性强、作用范围广、毒副作用轻微和不易产生耐药性等优点,被广泛应用于各类恶性肿瘤的临床治疗中。榄香烯的生产主要依靠药用植物温郁金的分离提取。但温郁金的榄香烯含量低、分离纯化难度大、得率低且成本高,严重阻碍了榄香烯的大规模生产与应用。随着合成生物学的发展,利用微生物构建细胞工厂用于生物合成天然药物成为研究热点,也为榄香烯的生产提供了新的思路。近年来,对榄香烯的生物合成研究在不断深入。研究者通过代谢工程、组合生物学和基因工程等手段,阐明榄香烯生物合成途径和关键酶,已经成功克隆了榄香烯生物合成途径上的一些关键酶基因,初步实现榄香烯的异源生物合成。本文以合成生物学研究思维概述榄香烯生物合成途径及其工程菌的优化,重点综述关键酶吉马烯A合酶(germacrane A synthase,GAS)。从限速酶基因的过表达和分流基因的敲除,融合表达酶工程策略、吉马烯A合酶的体外进化几方面,对其生物合成途径的改造策略进行阐述。同时,也分析提高异源生物合成榄香烯产量所面临的问题与挑战,为榄香烯的高效生物合成提供参考。
文摘A new sesquiterpene with a unusual modified germacrane skeleton was isolated from the ethanol extracts of the roots of Biondia hemsleyana and its structure was elucidated as 3β-hydroxy- 4,14-cyclogermacra-11-en-9-one by the spectroscopic methods and X-ray crystallography.
文摘Nine new germacranolides,sylvaticalides A−H(1-9),and three known analogues(10-12)were isolated from the aeri-al part of Vernonia sylvatica.Their structures were established using comprehensive spectroscopic analysis,including high-resolution electrospray ionization mass spectroscopy(HR-ESI-MS)and 1D and 2D nuclear magnetic resonance(NMR)spectra.Their absolute configurations were determined by X-ray diffraction experiments.The anti-inflammatory activities of all isolated compounds were as-sessed by evaluating their inhibitory effects on the nuclear factor kappa B(NF-κB)pathway,which was activated by lipopolysacchar-ide(LPS)-stimulated human THP1-Dual cells,and the interferon-stimulated gene(ISG)pathway,activated by STING agonist MSA-2 in the same cell model.Compounds 1,2 and 6 showed inhibitory effects on the NF-κB and ISG signaling pathways,with IC_(50)values ranging from 4.12 to 10.57μmol·L^(−1).
基金supported by the Key Program of the National Natural Science Foundation of China (22137008)the Yunnan Wanren Project (YNWR-KJLJ-2019-002).
文摘Ten new germacrane-type sesquiterpenoids,artemyrianosins A-J(1-10),were isolated from the aerial parts of Arte-misia myriantha.Their structures were elucidated by spectral analyses including UV,IR,HRESIMS,1D and 2D NMR,ECD and the absolute configurations of compounds 1 and 7-9 were characterized using X-ray crystallography.All isolates were tested their cytotoxicity against three human hepatoma cell lines(HepG2,Huh7,and SK-Hep-1),and com-pounds 1-3,7,and 10 showed cytotoxicity with IC50 values ranging from 43.7 to 89.3μM.Among them,the most active compound 3 exhibited activity against three human hepatoma cell lines with IC50 values of 43.7μM(HepG2),47.9μM(Huh7),and 44.9μM(SK-Hep-1).
文摘Two new germacranes, chrysanthemumins C （1） and D （2）, and five eudesmanes, chrysanthemumols I-K （3- 5） as new ones, eudesm-4（14）-ene-3a,11-diol （6） and canusesnol E （7）, were isolated from the ethyl acetate soluble fraction of 95% EtOH extract of the flowers of Chrysanthemum indicum. The structures of isolated sesquiterpe- noids were elucidated on basis of extensive spectroscopic evidences.
