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Chinese Journal of Natural Medicines 2019年第1期17卷 3-14页

作者： SUN Shan-Shan WANG Kai MA Ke BAO Li LIU Hong-Wei School of Life Sciences University of Science and Technology of China State Key Laboratory of Mycology Institute of MicrobiologyChinese Academy of Sciences University of Chinese Academy of Sciences

Metabolic syndrome characterized by obesity, hyperglycemia and liver steatosis is becoming prevalent all over the world. Herein, a water insoluble polysaccharide(WIP) was isolated and identified from the sclerotium of Poria cocos, a widely used Traditional Chinese Medicine. WIP was confirmed to be a(1-3)-β-D-glucan with an average Mw of 4.486 × 10~6 Da by NMR and SEC-RI-MALLS analyses. Furthermore, oral treatment with WIP from P. cocos significantly improved glucose and lipid metabolism and alleviated hepatic steatosis in ob/ob mice. 16 S DNA sequencing analysis of cecum content from WIP-treated mice indicated the increase of butyrate-producing bacteria Lachnospiracea, Clostridium. It was also observed that WIP treatment elevated the level of butyrate in gut, improved the gut mucosal integrity and activated the intestinal PPAR-γ pathway. Fecal transplantation experiments definitely confirmed the causative role of gut microbiota in mediating the benefits of WIP. It is the first report that the water insoluble polysaccharide from the sclerotium of P. cocos modulates gut microbiota to improve hyperglycemia and hyperlipidemia. Thereby, WIP from P. cocos, as a prebiotic, has the potential for the prevention or cure of metabolic diseases and may elucidate new mechanism for the efficacies of this traditional herbal medicine on the regulation of lipid and glucose metabolism.

关键词： Poria cocos Water insoluble polysaccharide Metabolic syndrome Prebiotics Gut microbiota

Rearranged Dichapetalin-Type Triterpenoids with Cytotoxic Activity from Dichapetalum gelonioides

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Chinese Journal of Chemistry 2022年第21期40卷 2531-2538页

作者： Xin-Hua Gao Xi-Yuan Wang Jun-Su Zhou Yan Zhang Hong-Chun Liu Bin Zhou Jian-Min Yue State Key Laboratory of Drug Research Shanghai lnstitute of Materia MedicaChinese Academy of SciencesShanghai 201203China Research Units of Discovery of New Drug Lead Molecules Chinese Academy of Medical SciencesShanghai 201203china Shandong Laboratory of Yantai Drug Discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantaiShandong 264117China

Dichagelinoids A—C(1—3),three unusual dichapetalin-type triterpenoids,together with two biogenetically related derivatives dichagelinoids D and E(4 and 5)were isolated and characterized by solid data from Dichapetalum *** 1—3 possess a common rearranged C ring and different C6—C2 modified motifs at the A *** evaluation revealed that compounds 1—3 showed distinct cytotoxic activity against the tested human cancer cell lines.

关键词： Dichapetalum gelonioides Natural products Dichapetalin-type triterpenoids Structural elucidation Cytotoxic activity

Suadimins D—J,Monoterpenoid Indole-Quinoline and Bisindole Alkaloids from Melodinus suaveolens

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Chinese Journal of Chemistry 2023年第18期41卷 2296-2304页

作者： Xin-Hua Gao Pei-Qian Wu Yao-Yue Fan Bin Zhou Jian-Min Yue State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203China shandong Laboratory of Yantai Drug Discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantaiShandong 264117China Research Units of Discovery of New Drug Lead Molecules Chinese Academy of Medical SciencesShanghai 201203China

Comprehensive Summary,Compounds 1—12,including seven complex monoterpenoid indole-quinoline and bisindole alkaloids,suadimins D—J(1—7)with previously unreported carbon-carbon linkages,were isolated and identified from the twigs and leaves of Melodinus *** structures were elucidated by a combination of diverse methods,especially the extensive spectroscopic data analysis and electric circular dichroism(ECD)*** cytotoxicity of these compounds against three cancer cell lines was evaluated,some of which showed moderate activities with IC50 values ranging from 2.4 to 8.0μM.

关键词： Melodinus suaveolens Alkaloids Dimerization Structure elucidation ECD calculations Cytotoxic activity

Asymmetric synthesis of difluorinatedα-quaternary amino acids(DFAAs)via Cu-catalyzed difluorobenzylation of aldimine esters

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Chinese Chemical Letters 2024年第12期35卷 416-421页

作者： Xiang Huang Dongzhen Xu Yang Liu Xia Huang Yangfan Wu Dongmei Fang Bing Xia Wei Jiao Jian Liao Min Wang Chengdu Institute of Organic Chemistry Chinese Academy of SciencesChengdu 610041China Natural Product Research Center Chengdu Institute of BiologyChinese Academy of SciencesChengdu 610041China University of Chinese Academy of Sciences Beijing 100049China

Increasing interests of difluorinated amino acids(DFAAs)have been raised in recent years due to their widespread bio-organic and medical ***,to date,only few investigations focused on their asymmetric *** difluoromethyl reagent to tailor a novel pathway and developing efficient catalytic system are highly desirable for constructing structurally diverse chiral ***,a copper-catalyzed asymmetric difluorobenzylation of aldimine esters is *** usingα,α-difluorinated benzyltriflones as difluoromethyl reagents,this protocol allows the asymmetric synthesis ofα-quaternary DFAAs with wide scope,good yields and excellent enantioselectivities(90%-98%ee).Control experiments and DESI-MS analysis demonstrate the reaction probably proceeds via a key difluorocarbocation ***,polyfluoroarenes are found efficient candidates to polyfluoroaryl amino acids via C-F ***-scale experiment,late-stage functionalization,synthesis of difluorinated dipeptides and bioactive molecular analogues revealed the utility of the protocol,thereby largely enriching the structural diversity of FAAs and providing more potential opportunities in drug discovery.

关键词： Cu-catalyzed Asymmetric difluorobenzylation Difluorobenzylatedα-quaternary amino acids Polyfluoroaryl amino acids Difluorocarbocation

Two Terpenoid Derivatives with Different 3/5/6/6/5-Fused Pentacyclic Skeletons from Hedyosmum orientale

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Chinese Journal of Chemistry 2023年第4期41卷 392-398页

作者： Yao-Yue Fan Cheng-Yu Zheng Bin Zhou Flavia M.Zimbres Maria B.cassera Jian-Min Yue State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai201203 China Shandong Laboratory of Yantai Drug Discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantaiShandong264117 China Research Units of Discovery of New Drug Lead Molecules Chinese Academy of Medical SciencesShanghai201203 China Department of Biochemistry and Molecular Biology Center for Tropical and Emerging Global Diseases(CTEGD)University of GeorgiaAthensGeorgia30602 United States

Chemical investigation of Hedyosmum orientale led to the identification of two terpenoid derivatives,dyosmunoids A and B(1 and 2)featuring two different 3/5/6/6/5-fused pentacyclic ring systems,*** 1 is the second natural product of this C_(25) terpenoid compound class,and compound 2 is a rare dinor-C25 terpenoid with a peroxide *** structural elucidation was achieved by the comprehensive analysis of spectroscopic data,single-crystal X-ray diffraction,and ECD *** biosynthetic pathways for compounds 1 and 2 are *** 2 exhibited strong antimalarial activity with an IC_(50) value of 0.42μmol·L^(-1).

关键词： Natural products C_(25)Terpenoids Structure elucidation Biosynthetic pathway hypothesis Antimalarial activity

Pd-catalyzed asymmetric carbonyl alkynylation:Synthesis of axial chiral ynones

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Chinese Chemical Letters 2024年第6期35卷 293-297页

作者： Long Jin Jian Han Dongmei Fang Min Wang Jian Liao Natural Products Research Center Chengdu Institute of BiologyChinese Academy of SciencesChengdu 610041China College of Chemical Engineering Sichuan UniversityChengdu 610065China University of Chinese Academy of Sciences Beijing 100049China

Ynones are important skeletons in bioactive molecules and valuable building blocks for organic synthesis,thus great efforts have been devoted to their ***,introducing prochiral substrates to construct ynones bearing a chiral framework is unrealized to ***,we reported the first example of Pd/SOP-catalyzed asymmetric carbonylative alkynylation via a non-classical carbonylative Sonogashiratype approach(acyl-Pd(Ⅱ)species generated from nucleophiles).By using cyclic diaryliodonium salts as prochiral substrates,various axial chiral ynones with good functional group tolerance(39 examples),satisfied yields(71%-96%)and excellent enantioselectivities(generally 94%-99%ee)were *** of bioactive compounds,scale-up experiment and useful transformations were also conducted to demonstrate the utility of this process.

关键词： Pd-catalyzed Axial chiral ynones Cyclic diaryliodonium High-valent palladium catalyzed Asymmetric carbonyl alkynylation

Highly Aromatic Norditerpenoid Heterodimers and Monomers from Trigonostemon fragilis

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Engineering 2024年第7期38卷 144-154页

作者： Jun-Su Zhou Long Cheng Yuan Gao Zhan-Peng Ge Bin Zhou Jing-Ya Li Jin-Xin Zhao Jian-Min Yue State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China Shandong Laboratory of Yantai Drug Discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantai 264117China

Four new norditerpenoid heterodimers with different dimerization patterns-namely,trigofragiloids A-C(denoted as compounds 1-3)and(+)-and(-)-trigofragiloid D(compound 4)-and three new phenanthrenone norditerpenoids-namely,trigofragiloids E-G(compounds 5-7)-were isolated from Trigonostemon *** 1 and 2 feature a novel heterodimeric carbon skeleton formed by the conjugation of a tetra-norditerpenoid and an ennea-norditerpenoid;they have been identified as class 2 atropisomers by means of quantum chemical *** 3 is an unprecedented phenylpropanoid-norditerpenoid adduct with a new dimerization ***(+)-and(-)-4 are the first example of S-shaped 1,4-dioxane-fused norditerpenoid *** by the structure elucidation of compound 4,two co-occurring analogues,actephilol A and epiactephilol A,were structurally revised as a pair of geometrical isomers and were identified as two pairs of enantiomers,(+)-and(-)-8 and(+)-and(-)-9,*** structures were characterized using a combined ***,compound 7 exhibits remarkable adenosine triphosphate-citrate lyase(ACLY)inhibition with a halfmaximal inhibition concentration(IC50)value of(0.46±0.11)lmol·L^(-1),as active as the positive control BMS-303141,and a molecular docking study offers deep insight into the interaction between compound 7 and ACLY.

关键词： Norditerpenoid heterodimer Trigonostemon fragilis Euphorbiaceae Trigofragiloid Structural revision Adenosine triphosphate-citrate lyase(ACLY) inhibitory activity

Antitumor Research on Artemisinin and Its Bioactive Derivatives

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Natural Products and Bioprospecting 2018年第4期8卷 303-319页

作者： Yunqin Zhang Guowei Xu Shuqun Zhang Dong Wang PSaravana Prabha Zhili Zuo State Key Laboratory of Phytochemistry and Plant resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201China University of the Chinese Academy of Sciences Beijing 100049China Yunnan Key Laboratory of Natural Medicinal Chemistry Kunming 650201YunnanChina

Cancer is the leading cause of human death which seriously threatens human *** antimalarial drug artemisinin and its derivatives have been discovered with considerable anticancer ***,a variety of target-selective artemisinin-related compounds with high efficiency have been *** researches indicated that artemisinin-related compounds have cytotoxic effects against a variety of cancer cells through pleiotropic effects,including inhibiting the proliferation of tumor cells,promoting apoptosis,inducing cell cycle arrest,disrupting cancer invasion and metastasis,preventing angiogenesis,mediating the tumor-related signaling pathways,and regulating tumor *** importantly,artemisinins demonstrated minor side effects to normal cells and manifested the ability to overcome multidrug-resistance which is widely observed in cancer ***,we concentrated on the new advances and development of artemisinin and its derivatives as potential antitumor agents in recent 5 *** is our hope that this review could be helpful for further exploration of novel artemisinin-related antitumor agents.

关键词： Artemisinin Artemisinin derivatives Antitumor Activity Mechanism

Taxonomic Revision of Raorchestes menglaensis(Kou,1990)(Amphibia:Anura),with Descriptions of Two New Species from Yunnan,China

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Asian Herpetological Research 2020年第4期11卷 263-281页

作者： Ke JIANG Jinlong REN Jian WANG Junfeng GUO Zeng WANG Yonghong LIU Dechun JIANG Jiatang LI cas Key Laboratory of Mountain Ecological Restoration and Bioresource Utilization Ecological Restoration and Biodiversity Conservation Key Laboratory of Sichuan Province Chengdu Institute of BiologyChinese Academy of SciencesChengdu 610041SichuanChina Southeast Asia Biodiversity Research Institute Chinese Academy of SciencesYezinNay Pyi Taw 05282Myanmar College of Life Science and Technology Honghe UniversityMengzi 661199YunnanChina Xishuangbanna Tropical Botanical Garden Chinese Academy of SciencesXishuangbanna 666303YunnanChina University of Chinese Academy of Sciences Beijing 100049China cas Center for Excellence in Animal Evolution and Genetics Chinese Academy of SciencesKunming 650223YunnanChina

Raorchestes is a group of Bush frogs mainly distributed in South and Southeast Asia that are poorly recognized by morphological *** recognize the true ***(Kou) based on 10 specimens newly collected from the type *** expanded description is also provided,and we delist the recently reported record,***(Boulenger) from *** with morphological and molecular data,two new species are respectively described from Menghai and Lvchun,Yunnan,*** hillisi *** distinguished from all other congeners by the following combination of morphological characters:(1) small body sized(males 15.9-17.7 mm,n=7;female 17.5 mm,n=1);(2) head longer than wide;(3) snout longer than eye diameter;(4) the tip of upper jaws slightly notched;(5) internasal space slightly less than interorbital space;(6) tympanum distinct;(7)fingers lacking lateral dermal fringe;(8) outside of toe Ⅰ and both sides of toe Ⅱ lacking lateral dermal fringe,other toes having weak lateral dermal fringes;(9) rudimentary web on toes;(10) lacking a series of tubercles along the outer sides of forearm and foot;(11) discs of fingers and toes not *** huanglianshan *** distinguished from all other congeners by the following combination of morphological characters:(1) small body size(males 17.0-19.6 mm,n=12;female 21.5 mm,n=1);(2) head slightly wider than long or equal;(3) snout longer than eye diameter;(4)the tip of upper jaws slightly notched;(5) internasal space distinctly less than interorbital space(6) tympanum distinct;(7) fingers lacking lateral dermal fringe;(8) toes lacking lateral dermal fringe;(9) rudimentary web on toes;(10)lacking a series of tubercles along the outer sides of forearm and foot;(11) discs of all fingers and toes orange or parts of them orange in life.

关键词： bush frog distribution Raorchestes hillisi sp.nov. Raorchestes huanglianshan sp.nov. Raorchestes parvulus revision taxonomy

Genetic analysis of walnut cultivars from southwest China:Implications for germplasm improvement

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Plant Diversity 2022年第6期44卷 530-541页

作者： Moses C.Wambulwa Peng-Zhen Fan Richard Milne Zeng-Yuan Wu Ya-Huang Luo Yue-Hua Wang Hong Wang Lian-Ming Gao Zuo-Ying Xiahou Ye-Chuan Jin Lin-Jiang Ye Zu-Chang Xu Zhi-Chun Yang De-Zhu Li Jie Liu cas Key Laboratory for Plant Diversity and Biogeography of East Asia Kunming Institute of BotanyChinese Academy of SciencesKunming650201YunnanChina Germplasm Bank of Wild Species Kunming Institute of BotanyChinese Academy of SciencesKunming650201YunnanChina Department of Life Sciences South Eastern Kenya University170-90200KituiKenya University of the Chinese Academy of Sciences Beijing100049China Institute of Molecular Plant Sciences School of Biological SciencesUniversity of EdinburghEdinburghUK School of School of Ecology and Environmental Science Yunnan UniversityKunming650091YunnanChina Yangbi Forestry and Grassland Administration Dali672500YunnanChina College of Life Sciences University of Chinese Academy of SciencesKunming650201YunnanChina

Walnuts are highly valued for their rich nutritional profile and wide medicinal *** demand has led to the intensification of breeding activities in major walnut production areas such as southwest China,in order to develop more superior *** the increasing number of cultivars,accurate identification becomes fundamental to selecting the right cultivar for grafting,industrial processing or development of new *** ensure proper identification of cultivars and understand the genetic structure of wild and cultivated material,we genotyped 362 cultivated and wild individuals of walnut trees from southwest China(with two additional populations from Xinjiang,plus three cultivars from Canada,France and Belgium) using 36 polymorphic microsatellite *** found relatively low indices of genetic diversity(H_(O)=0.570,H_(E)=0.404,N_(A)=2.345) as well as a high level of clonality(>85% of cultivars),indicating reliance on genetically narrow sources of parental material for *** STRUCTURE and PCoA analyses generally delineated the two species,though considerable levels of introgression were also *** significantly,we detected a distinct genetic group of cultivated Juglans sigillata,which mainly comprised individuals of the popular ’Yangbidapao’ ***,a core set of 18 SSR loci was selected,which was capable of identifying 32 *** a nutshell,our results call for more utilization of genetically disparate material,including wild walnut trees,as parental sources to breed for more *** data reported herein will significantly contribute towards the genetic improvement and conservation of the walnut germplasm in southwest China.

关键词： Cultivars Genetic diversity Juglans sigillata Southwest China Walnut