The Janus kinases(JAKs)are a family of intracellular tyrosine kinases that play an essential role in many basic biological processes,such as apoptosis and inflammation.Thus any dysfunction of the proteins in this path...The Janus kinases(JAKs)are a family of intracellular tyrosine kinases that play an essential role in many basic biological processes,such as apoptosis and inflammation.Thus any dysfunction of the proteins in this pathway may lead to a variety of diseases,including cancer and diseases that affect the immune system,such as severe combined immune deficient(SCID).Marine biological resources have become an important source in new drug research and development due to their diversity,complexity and speciality.In this study,Marine alkaloid Neobacillamide A was isolated from the greedy and stubborn sponge symbiotic Bacillus atrophicus C89 in the South China Sea.Totally 24 novel marine alkaloid Neobacillamide A derivatives were designed and synthesized,which were evaluated for their inhibitory activity against JAK/STAT signaling pathway and their cytotoxicity to A549 cells.Compounds 13c,13o,14d,14g and 14h showed potent JAK/STAT inhibition capability(concentration of 25μmol L^(-1),all inhibitory potencies were above 60%),especially compound 14g exhibited superior JAK/STAT inhibition effect(89.70%inhibition).In addition,all these compounds with a concentration of 25μmol L^(-1)displayed weak or no cytotoxicity to A549 cells,which means that these Neobacillamide A derivatives with JAK/STAT inhibition capability may have potential anti-inflammatory function.展开更多
In this study, the chemical analysis of the marine sponge spieces, Haliclona cymaeformis, collected from the South China Sea was carried out, Two pairs of regioisomers of alkyl substitutional 6-oxy purine alkaloids(1a...In this study, the chemical analysis of the marine sponge spieces, Haliclona cymaeformis, collected from the South China Sea was carried out, Two pairs of regioisomers of alkyl substitutional 6-oxy purine alkaloids(1a/1b and 2a/2b) were isolated. All of them possess two structural moieties, a 6-oxy purine nucleus and a pentan-2-one or hexan-2-one alkyl chain. Among them, 1a and 2a are the major N-9-substitutional regioisomers, and 1b and 2b are the minor N-7-substitutional regioisomers.展开更多
Lamellarins and related pyrrole-derived alkaloids are a large family of marine alkaloids with novel structures and promising bioactivities. They have been isolated from diverse marine organisms and all of them feature...Lamellarins and related pyrrole-derived alkaloids are a large family of marine alkaloids with novel structures and promising bioactivities. They have been isolated from diverse marine organisms and all of them feature a 3,4-diarylpyrrole 2-carboxylic acid ester or amide moiety. This article provides an overview of recent literatures on lamellarins and related pyrrole-derived alkaloids, including their isolation, total synthesis, biological and structure activity relationship （SAR） studies.展开更多
Natural products derived from marine microorganisms have received great attention as a potential resource of new compound entities for drug discovery.The unique marine environment brings us a large group of sulfur-con...Natural products derived from marine microorganisms have received great attention as a potential resource of new compound entities for drug discovery.The unique marine environment brings us a large group of sulfur-containing natural products with abundant biological functionality including antitumor,antibiotic,anti-inflammatory and antiviral activities.We reviewed all the 484 sulfur-containing natural products(non-sulfated)isolated from marine microorganisms,of which 59.9%are thioethers,29.8%are thiazole/thiazoline-containing compounds and 10.3%are sulfoxides,sulfones,thioesters and many others.A selection of 133 compounds was further discussed on their structure-activity relationships,mechanisms of action,biosynthesis,and druggability.This is the first systematic review on sulfur-containing natural products from marine microorganisms conducted from January 1987,when the first one was reported,to December 2020.展开更多
The dietary relationship study between marine sponge Xestospongia sp.and its nudibranch predators Jorunna funebris based on the discovery of isoquinolinequinones has long been studied.In this study,chemical investigat...The dietary relationship study between marine sponge Xestospongia sp.and its nudibranch predators Jorunna funebris based on the discovery of isoquinolinequinones has long been studied.In this study,chemical investigation of the sponge Xestospongia sp.and nudibranch J.funebris from the South China Sea yielded a new marine alkaloid neopetroside C(1),together with nine known alkaloids(2-10).The chemical structures of all the compounds were elucidated by extensive spectroscopic analysis.Neopetroside C(1)featured a riboside of nicotinic acid with a rareα-N glycosildic linkage and an acyl residue of(Z)-2-methylbut-2-enoic acid attached to C-5′.The plausible chemical ecology relationship between sponge Xestospongia sp.and its nudibranch predator J.funebris was proposed based on the biogenetic relationship of the common marine alkaloids.The observation of two structural fragments,(Z)-2-methylbut-2-enoyloxy and trigonelline groups in both sponge and nudibranch,indicated that nudibranch might uptake chemicals from sponge and then modify and transform them into chemical weapons to defend against predators.展开更多
A novel alkaloid, chartrenoline(1), featuring an unusual 6/6/5/5-tetracyclic nucleus, was isolated from a marine Streptomyces chartreusis NA02069. The structure of 1 including its absolute configurations was establish...A novel alkaloid, chartrenoline(1), featuring an unusual 6/6/5/5-tetracyclic nucleus, was isolated from a marine Streptomyces chartreusis NA02069. The structure of 1 including its absolute configurations was established by extensive analyses of its high resolution mass, NMR and single-crystal X-ray diffraction data. A plausible biosynthetic pathway for chartrenoline(1) is proposed.展开更多
基金financial supports granted by the National Natural Science Foundation of China(Nos.82073759 and 82003583)the Fund of Greater Bay Area Institute of Precision Medicine(Guangzhou)(No.IPM2021C009)the National Science and Technology Major Project for Significant New Drugs Development(No.2018ZX09735004)。
文摘The Janus kinases(JAKs)are a family of intracellular tyrosine kinases that play an essential role in many basic biological processes,such as apoptosis and inflammation.Thus any dysfunction of the proteins in this pathway may lead to a variety of diseases,including cancer and diseases that affect the immune system,such as severe combined immune deficient(SCID).Marine biological resources have become an important source in new drug research and development due to their diversity,complexity and speciality.In this study,Marine alkaloid Neobacillamide A was isolated from the greedy and stubborn sponge symbiotic Bacillus atrophicus C89 in the South China Sea.Totally 24 novel marine alkaloid Neobacillamide A derivatives were designed and synthesized,which were evaluated for their inhibitory activity against JAK/STAT signaling pathway and their cytotoxicity to A549 cells.Compounds 13c,13o,14d,14g and 14h showed potent JAK/STAT inhibition capability(concentration of 25μmol L^(-1),all inhibitory potencies were above 60%),especially compound 14g exhibited superior JAK/STAT inhibition effect(89.70%inhibition).In addition,all these compounds with a concentration of 25μmol L^(-1)displayed weak or no cytotoxicity to A549 cells,which means that these Neobacillamide A derivatives with JAK/STAT inhibition capability may have potential anti-inflammatory function.
基金supported by the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (No.16KJB350005)the Yangzhou University Foundation for Fostering Talents in the Science and Technology Innovation (No.2016CXJ052)+1 种基金the National Natural Science Foundation of China (Nos.81703411,U1606403)the Taishan Scholars Program,China
文摘In this study, the chemical analysis of the marine sponge spieces, Haliclona cymaeformis, collected from the South China Sea was carried out, Two pairs of regioisomers of alkyl substitutional 6-oxy purine alkaloids(1a/1b and 2a/2b) were isolated. All of them possess two structural moieties, a 6-oxy purine nucleus and a pentan-2-one or hexan-2-one alkyl chain. Among them, 1a and 2a are the major N-9-substitutional regioisomers, and 1b and 2b are the minor N-7-substitutional regioisomers.
基金National Natural Science Foundation of China （Grant No. 30930109, 20972007, 20802005）, the National Basic Research Program of China （973 Program, Grant No. 2010CB833200）, and NCET （Program for New Century Excellent Talents in University）.
文摘Lamellarins and related pyrrole-derived alkaloids are a large family of marine alkaloids with novel structures and promising bioactivities. They have been isolated from diverse marine organisms and all of them feature a 3,4-diarylpyrrole 2-carboxylic acid ester or amide moiety. This article provides an overview of recent literatures on lamellarins and related pyrrole-derived alkaloids, including their isolation, total synthesis, biological and structure activity relationship （SAR） studies.
基金This paper is dedicated to Professor Youyou Tu,the 2015 Nobel Prize Laureate of Physiology or Medicine on the occasion of her 90th Birthday.This work was supported by the Program of National Natural Science Foundation of China(Nos.U1706210,41776141 and 41322037)the Fundamental Research Funds for the Central Universities(No.201841004)+1 种基金the Marine S&T Fund of Shandong Province for Pilot National Laboratory for Marine Science and Technology(Qingdao)(No.2018SDKJ0403-2)the Taishan Scholars Program,China(No.tsqn20161010).
文摘Natural products derived from marine microorganisms have received great attention as a potential resource of new compound entities for drug discovery.The unique marine environment brings us a large group of sulfur-containing natural products with abundant biological functionality including antitumor,antibiotic,anti-inflammatory and antiviral activities.We reviewed all the 484 sulfur-containing natural products(non-sulfated)isolated from marine microorganisms,of which 59.9%are thioethers,29.8%are thiazole/thiazoline-containing compounds and 10.3%are sulfoxides,sulfones,thioesters and many others.A selection of 133 compounds was further discussed on their structure-activity relationships,mechanisms of action,biosynthesis,and druggability.This is the first systematic review on sulfur-containing natural products from marine microorganisms conducted from January 1987,when the first one was reported,to December 2020.
基金This research work was financially supported by the National Natural Science Foundation of China(NSFC)(Nos.8202290170,81991521,42076099,41676073)the NSFC/CNRS joint project(No.81811530284),and the SKLDR/SIMM Project(No.SIMM1903ZZ-04)X-W Li is also thankful for the Shanghai Rising-Star Program(No.20QA1411100),SA-SIBS Scholarship Program.
文摘The dietary relationship study between marine sponge Xestospongia sp.and its nudibranch predators Jorunna funebris based on the discovery of isoquinolinequinones has long been studied.In this study,chemical investigation of the sponge Xestospongia sp.and nudibranch J.funebris from the South China Sea yielded a new marine alkaloid neopetroside C(1),together with nine known alkaloids(2-10).The chemical structures of all the compounds were elucidated by extensive spectroscopic analysis.Neopetroside C(1)featured a riboside of nicotinic acid with a rareα-N glycosildic linkage and an acyl residue of(Z)-2-methylbut-2-enoic acid attached to C-5′.The plausible chemical ecology relationship between sponge Xestospongia sp.and its nudibranch predator J.funebris was proposed based on the biogenetic relationship of the common marine alkaloids.The observation of two structural fragments,(Z)-2-methylbut-2-enoyloxy and trigonelline groups in both sponge and nudibranch,indicated that nudibranch might uptake chemicals from sponge and then modify and transform them into chemical weapons to defend against predators.
基金financially supported by the National Natural Science Foundation of China(Nos.81522042,21572100,81773591,81421091,81500059,81673333,21672101,21761142001,21661140001,J1210026,and J1103512)Natural Science Foundation of Jiangsu Province(No.BK20151397)Fundamental Research Funds for the Central Universities(No.020814380092)
文摘A novel alkaloid, chartrenoline(1), featuring an unusual 6/6/5/5-tetracyclic nucleus, was isolated from a marine Streptomyces chartreusis NA02069. The structure of 1 including its absolute configurations was established by extensive analyses of its high resolution mass, NMR and single-crystal X-ray diffraction data. A plausible biosynthetic pathway for chartrenoline(1) is proposed.
