Glutamate excitotoxicity has been shown to play an important role in glaucoma, and glutamate can induce ferroptosis. The p38 mitogenactivated protein kinase(MAPK) pathway inhibitor SB202190 has a potential ability to ...Glutamate excitotoxicity has been shown to play an important role in glaucoma, and glutamate can induce ferroptosis. The p38 mitogenactivated protein kinase(MAPK) pathway inhibitor SB202190 has a potential ability to suppress ferroptosis, and its downstream targets, such as p53, have been shown to be associated with ferroptosis. However, whether ferroptosis also occurs in retinal ganglion cells in response to glutamate excitotoxicity and whether inhibition of ferroptosis reduces the loss of retinal ganglion cells induced by glutamate excitotoxicity remain unclear. This study investigated ferroptosis in a glutamate-induced glaucoma rat model and explored the effects and molecular mechanisms of SB202190 on retinal ganglion cells. A glutamate-induced excitotoxicity model in R28 cells and an N-methyl-D-aspartate-induced glaucoma model in rats were used. In vitro experiments showed that glutamate induced the accumulation of iron and lipid peroxide and morphological changes of mitochondria in R28 cells, and SB202190 inhibited these changes. Glutamate induced the levels of p-p38 MAPK/p38 MAPK and SAT1 and decreased the expression levels of ferritin light chain, SLC7A11, and GPX4. SB202190 inhibited the expression of iron death-related proteins induced by glutamate. In vivo experiments showed that SB202190 attenuated N-methyl-D-aspartate-induced damage to rat retinal ganglion cells and improved visual function. These results suggest that SB202190 can inhibit ferroptosis and protect retinal ganglion cells by regulating ferritin light chain, SAT1, and SLC7A11/Gpx4 pathways and may represent a potential retina protectant.展开更多
Acupuncture is an effective treatment for ischemic stroke(IS)and plays a key role in neurological rehabilitation after IS.Acupuncture can improve the clinical symptoms of various complications after IS,including motor...Acupuncture is an effective treatment for ischemic stroke(IS)and plays a key role in neurological rehabilitation after IS.Acupuncture can improve the clinical symptoms of various complications after IS,including motor dysfunction,swallowing disorders,speech disorders,cognitive impairment,depression,insomnia,and fatigue.However,the mechanisms underlying the effects of acupuncture in IS remain unclear.Available evidence suggests that acupuncture may exert neuroprotective effects through neuroplasticity(neurogenesis and synaptogenesis),angiogenesis,cell proliferation and apoptosis,and regulation of oxidative stress,inflammation,and immunity.Further studies should be conducted to improve the high-quality evidence-based system of acupuncture intervention for IS,by focusing on the clinical and basic research design,increasing the sample size,standardizing and quantifying the standards of acupuncture operations,using multidisciplinary techniques and methods to systematically explore the key targets of acupuncture intervention for IS,and reveal the efficacy and mechanism of acupuncture in the treatment of IS.展开更多
Acupuncture therapy is widely used in the clinic,and its therapeutic effects have been proven by numerous studies.The dose–effect relationship of acupuncture is a fundamental aspect of the acupuncture research system...Acupuncture therapy is widely used in the clinic,and its therapeutic effects have been proven by numerous studies.The dose–effect relationship of acupuncture is a fundamental aspect of the acupuncture research system.Recent studies found that different acupuncture dosages altered study results directly,indicating the importance of screening the optimal stimulation dosage.However,the system for studying the acupuncture dose–effect relationship is still in its infancy,and the methodology of the system needs to be improved.This review aimed to define the factors impacting acupuncture“dosage”and“effect,”and to improve the methodological system for research on the dose–effect relationship of acupuncture.By summarizing the current findings of acupuncture dose–effect studies,we discussed the vital acupuncture parameters and methodological problems that influence the relationship between acupuncture dosage and its effects.These factors consist of specific influencing factors(acupoint selection,acupuncture manipulation parameters,de qi response)and nonspecific influencing factors(comparison selection,blinding procedure,patient expectancy).Our perspectives offer suggestions for the design of acupuncture dosage–effect trials.Further studies need to be conducted to establish the methodological system and provide systematic evidence of the acupuncture dose–effect relationship.展开更多
Inflammatory bowel disease(IBD)is an autoimmune gastrointestinal disease characterized by chronic relapsing inflammation of the intestine.Excessive pyroptosis that exists in the inflamed intestine can activate damage ...Inflammatory bowel disease(IBD)is an autoimmune gastrointestinal disease characterized by chronic relapsing inflammation of the intestine.Excessive pyroptosis that exists in the inflamed intestine can activate damage signals and aggravate local inflammation in IBD.Here,we designed an oral pyroptosis nanoinhibitor,DXMS@CuM@PPADT@PSS(DCMP),which can target intestinal lesions,and respond to reactive oxygen species(ROS)to release active sites and drugs at the lesion.DCMP can inhibit the activation of the nucleotide-binding domain and leucine-rich repeat family pyrin domain containing 3(NLRP3)inflammasomes by scavenging ROS,resulting in the down-regulation of gasdermin D(GSDMD)cleavage thus inhibiting pyroptosis.It also improved intestinal barrier function,decreased inflammatory cytokine levels,and increased the diversity of gut microbiota in mice with colitis.This work is believed to expand the biomedical application of nanomaterials for innate immunity modulation.展开更多
Four new cyclohexapeptides,pyridapeptides F–I(1–4),were isolated from the fermentation broth of marine sponge-derived Streptomyces sp.OUCMDZ-4539.The pyridapeptides F–H(1–3)are composed ofβ-hydroxyleucine,alanine...Four new cyclohexapeptides,pyridapeptides F–I(1–4),were isolated from the fermentation broth of marine sponge-derived Streptomyces sp.OUCMDZ-4539.The pyridapeptides F–H(1–3)are composed ofβ-hydroxyleucine,alanine,O-methylthreonine,hexahydropyridazine-3-carboxylic acid,5-hydroxytetrahydropyridazine-3-carboxylic acid,and(2S,3R,4E,6E)-2-amino-3–hydroxy-4,6-dienoic acid residues.Pyridapeptide I(4)contains(2S,3R,4E,6E)-2-amino-3–hydroxy-8-methylnona-4,6-dienoic acid residue and a very rare glycose residue,aculose.Their structures were determined based on spectroscopic analysis and chemical methods.Pyridapeptides G–I(2–4)have the 2,3,6-trideoxyhexose units glycosylated at theγ-OH-TPDA residue,displayed significant antiproliferative activity against four(PC9,MKN45,Hep G2,K562)or two(PC9,MKN45)human cancer cell lines.展开更多
From the oligotrophic culture of a soft coral-associated actinomycetes strain, Streptomyces sp. OUCMDZ-1703, we isolated and identified two new chlorinated polyketides that we named strepchloritides A and B （1 and 2...From the oligotrophic culture of a soft coral-associated actinomycetes strain, Streptomyces sp. OUCMDZ-1703, we isolated and identified two new chlorinated polyketides that we named strepchloritides A and B （1 and 2）, three thiazole derivatives known as watasemycin A （3）, pulicatin G （4） and aerugine （5）, along with pyrrole- 2-carboxamide, furan-2-carboxamide and 1-（3,5-dihydroxyphenyl）ethanone. The new structures of 1 and 2 were determined by spectroscopic studies such as 1D- and 2D-NMR and MS analyses, while the known compounds were identified by comparison of the NMR data with those in literatures. The results showed that actinomycete strain OUCMDZ-1703 could use the relative high ratio of chlorine in the oligotrophic medium to synthesize chlorinated natural products. New compounds 1 and 2 displayed cytotoxicity against the MCF-7 ceils with ICs0 values of 9.9 and 20.2 ~tmoloL-1, respectively. Thiazole derivatives 3 and 5 were first found to be active against three clinical strains of methicillin-resistant Staphylococcus aureus （MRSA082, MRSA111 and MRSA234） with the same MIC/MBC values of 7.81/7.81 μg·mL-1.展开更多
Background:The Ulcerative Colitis Endoscopic Index of Severity(UCEIS)and the Mayo Endoscopic Score(MES)were developed as an objective method of the endoscopic severity in ulcerative colitis(UC);however,it was still un...Background:The Ulcerative Colitis Endoscopic Index of Severity(UCEIS)and the Mayo Endoscopic Score(MES)were developed as an objective method of the endoscopic severity in ulcerative colitis(UC);however,it was still unclear whether UCEIS vs MES could guide the need for colectomy in acute severe colitis(ASC).Methods:Consecutive ASC patients between January 2012 and May 2016 were retrospectively evaluated.Demographic data,previous therapy,clinical observations,laboratory parameters,medical therapy and endoscopic assessments were documented.The primary outcome was the need for colectomy during admission and follow-up.Results:Ninety-two patients were enrolled.37(40.2%)needed colectomy.UCEIS score is a predictor of requirement for colectomy inmultivariate analysis(OR,3.25;95%CI,1.77–5.97;P<0.001).Receiver-operator characteristic(ROC)area of UCEIS is 0.85,with a sensitivity of 60.3%and specificity of 85.5%using cut-off value of 7,which outperforms MES with the ROC area of 0.65;When UCEIS score7,80%of patients eventually need colectomy.Conclusion:UCEIS outperformed MES as a predictor for need for colectomy in ASC patients.The high probability of medical treatment failure and benefits of early colectomy should be discussed in patients with baseline UCEIS7.Acute severe colitis;colectomy;Ulcerative Colitis Endoscopic Index of Severity;Mayo Endoscopic Score.展开更多
Pafuranones A(1)and B(2),a pair of new epimeric polyketide dimers,were isolated from the fungus Paraconiothyrium sp.OUCMDZ-3316 associated with the marine algae Enteromorpha prolifera.Their structures,including absolu...Pafuranones A(1)and B(2),a pair of new epimeric polyketide dimers,were isolated from the fungus Paraconiothyrium sp.OUCMDZ-3316 associated with the marine algae Enteromorpha prolifera.Their structures,including absolute configurations,were fully elucidated based on spectroscopic analysis,calculated ECD,and chemical methods.Pafuranones A(1)and B(2)possess a rare dimeric furanone skeleton,which might be formed through a conjugate addition of the monomeric units followed by an intramolecular cyclization.展开更多
Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia mult...Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia multiflora. The structures of new compounds were determined in the light of spectroscopic data,X-ray and ECD calculation. Compounds 1 and 3 are racemates, while compound 2 is optically pure.Compounds 1 and 4 showed antibacterial and antifungal activities against Staphylococcus aureus,Pseudomonas aeruginosa, Clostridium perfringens, Escherichia coli and Candida albicans with MIC values ranging from 8 μg/mL to 64 μg/mL.展开更多
Five new pyrrolizidine alkaloids,bohemamines J—N(1-5),were isolated from Streptomyces sp.CPCC 200497.Their structures were assigned based on detailed spectroscopic analysis and semisynthesis.Bohemamine J(1)possesses ...Five new pyrrolizidine alkaloids,bohemamines J—N(1-5),were isolated from Streptomyces sp.CPCC 200497.Their structures were assigned based on detailed spectroscopic analysis and semisynthesis.Bohemamine J(1)possesses a new chimeric skeleton derived from bohemamine A(6)and phenylacetaldehyde.Inspired by the nonenzymatic formation mechanism of the methylene-bridged dimers isolated from this strain,we synthesized a series of chimeric derivatives(8,9,and 12-23)through natural product chimera strategy.Compounds 13,15,19,and 21 showed significant antioxidant activity.展开更多
(±)-Pyriindolin(1)with a rare molecular backbone formed by fusing a 2,2'-bipyridine nucleus into a spiro[furan-3,3'-indoline]skeleton,was isolated from the Streptomyces albolongus EA12432.The constitution...(±)-Pyriindolin(1)with a rare molecular backbone formed by fusing a 2,2'-bipyridine nucleus into a spiro[furan-3,3'-indoline]skeleton,was isolated from the Streptomyces albolongus EA12432.The constitution and the relative configuration of(±)-1 were determined by extensive spectroscopic analyses,^(13)C calculation and DP4+probability analysis.The absolute configurations of optically pure(+)-1 and(-)-1 which were obtained after a chiral high performance liquid chromatography(HPLC)separation were further identified by electronic circular dichroism(ECD)calculations.(+)-and(-)-Pyriindolins displayed moderate cytotoxicity against HCT-116 cell line with the half-maximal inhibitory concentration(IC_(50))values of 2.89±0.17μmol/L and 4.47±0.26μmol/L,respectively.展开更多
In order to discover structurally new and bioactive conipounds from marine life,we studied the secondary metabolites of the marine-derived fungi associated with a marine sponge(XS-3)from the Xisha islands.As a result,...In order to discover structurally new and bioactive conipounds from marine life,we studied the secondary metabolites of the marine-derived fungi associated with a marine sponge(XS-3)from the Xisha islands.As a result,4-O-methylcandidusin A(1),a new p-terphenyl alcohol,along with nine known analogs(2-10),were isolated and identified from the marine spongederived fungus Aspergillus candidus OUCMDZ-1051.The structures of these compounds were determined by analyzing spectroscopic data,especially ID and 2D NMR.The new compound 1 selectively inhibited the growth of the MDA-MB-46&BT474 and A431 human cancer cell lines with the IC_(50) values of 1.84,6.05 and 0.98 pmol/L,respectively.Compound 1 also displayed a selective antimicrobial activity against Escherichia coli with an MIC value of 27.3 pmol/L.The results indicated 4-O-methylcandidusin A(1)as a potential lead in the new drug discovery for triple negative breast cancer,invasive ductal breast cancer and epidermoid cancer.The antimicrobial metabolites also evidenced a clue for chemical defense of sponges by their associated microorganisms.展开更多
基金supported by the National Natural Science Foundation of China,Nos.81974132,81770927Hunan Provincial Health Commission,No.20220702839+1 种基金the Natural Science Foundation of Hunan Province of China,No.2022JJ30076National Key R&D Program of China,No.2021YFA1101202(all to WS)。
文摘Glutamate excitotoxicity has been shown to play an important role in glaucoma, and glutamate can induce ferroptosis. The p38 mitogenactivated protein kinase(MAPK) pathway inhibitor SB202190 has a potential ability to suppress ferroptosis, and its downstream targets, such as p53, have been shown to be associated with ferroptosis. However, whether ferroptosis also occurs in retinal ganglion cells in response to glutamate excitotoxicity and whether inhibition of ferroptosis reduces the loss of retinal ganglion cells induced by glutamate excitotoxicity remain unclear. This study investigated ferroptosis in a glutamate-induced glaucoma rat model and explored the effects and molecular mechanisms of SB202190 on retinal ganglion cells. A glutamate-induced excitotoxicity model in R28 cells and an N-methyl-D-aspartate-induced glaucoma model in rats were used. In vitro experiments showed that glutamate induced the accumulation of iron and lipid peroxide and morphological changes of mitochondria in R28 cells, and SB202190 inhibited these changes. Glutamate induced the levels of p-p38 MAPK/p38 MAPK and SAT1 and decreased the expression levels of ferritin light chain, SLC7A11, and GPX4. SB202190 inhibited the expression of iron death-related proteins induced by glutamate. In vivo experiments showed that SB202190 attenuated N-methyl-D-aspartate-induced damage to rat retinal ganglion cells and improved visual function. These results suggest that SB202190 can inhibit ferroptosis and protect retinal ganglion cells by regulating ferritin light chain, SAT1, and SLC7A11/Gpx4 pathways and may represent a potential retina protectant.
基金funded by the Ministry of Science and Technology of the People’s Republic of China,National Key Research and Development Program(2018YFC1706001)Tianjin Municipal Science and Technology Bureau,Tianjin Science and Technology Plan Project(21JCQNJC01560)+5 种基金Tianjin Education Commission scientific research project(2022KJ170)Tianjin Municipal Education commissionTianjin Graduate Research Innovation Project(Service Industry Project)(2022BKYZ046)Tianjin University of Traditional Chinese MedicineTianjin University of Traditional Chinese Medicine Graduate Research Innovation Project(Clinical Research Project YJSKC-20222002)the First Teaching Hospital of Tianjin University of Traditional Chinese Medicine,Exploration and Innovation Project(YB202112).
文摘Acupuncture is an effective treatment for ischemic stroke(IS)and plays a key role in neurological rehabilitation after IS.Acupuncture can improve the clinical symptoms of various complications after IS,including motor dysfunction,swallowing disorders,speech disorders,cognitive impairment,depression,insomnia,and fatigue.However,the mechanisms underlying the effects of acupuncture in IS remain unclear.Available evidence suggests that acupuncture may exert neuroprotective effects through neuroplasticity(neurogenesis and synaptogenesis),angiogenesis,cell proliferation and apoptosis,and regulation of oxidative stress,inflammation,and immunity.Further studies should be conducted to improve the high-quality evidence-based system of acupuncture intervention for IS,by focusing on the clinical and basic research design,increasing the sample size,standardizing and quantifying the standards of acupuncture operations,using multidisciplinary techniques and methods to systematically explore the key targets of acupuncture intervention for IS,and reveal the efficacy and mechanism of acupuncture in the treatment of IS.
基金funded by the Ministry of Science and Technology of the People’s Republic of ChinaNational Key Research and Development Program(2010CB530506,2018YFC1706001,2019YFC0840709)+2 种基金Tianjin Municipal Science and Technology BureauTianjin Science and Technology Plan Project(18PTLCSY00060)the First Teaching Hospital of Tianjin University of Traditional Chinese Medicine,Exploration and Innovation Project(YB202112)
文摘Acupuncture therapy is widely used in the clinic,and its therapeutic effects have been proven by numerous studies.The dose–effect relationship of acupuncture is a fundamental aspect of the acupuncture research system.Recent studies found that different acupuncture dosages altered study results directly,indicating the importance of screening the optimal stimulation dosage.However,the system for studying the acupuncture dose–effect relationship is still in its infancy,and the methodology of the system needs to be improved.This review aimed to define the factors impacting acupuncture“dosage”and“effect,”and to improve the methodological system for research on the dose–effect relationship of acupuncture.By summarizing the current findings of acupuncture dose–effect studies,we discussed the vital acupuncture parameters and methodological problems that influence the relationship between acupuncture dosage and its effects.These factors consist of specific influencing factors(acupoint selection,acupuncture manipulation parameters,de qi response)and nonspecific influencing factors(comparison selection,blinding procedure,patient expectancy).Our perspectives offer suggestions for the design of acupuncture dosage–effect trials.Further studies need to be conducted to establish the methodological system and provide systematic evidence of the acupuncture dose–effect relationship.
基金supported by the National Natural Science Foundation of China(Nos.82270543,82170573,81770556 and 21874066)the National Key R&D Program of China(No.2019YFA0709200)+3 种基金the Key Research and Development Program of Jiangsu Province(No.BE2021373)the Natural Science Foundation of Jiangsu Province(No.BK20200336)the Fundamental Research Funds for Central Universities,and the Program for Innovative Talents and Entrepreneur in Jiangsu.All animal studies were approved by the Ethics Committee of Jinling Hospital(No.2021JLHDWLSZ-0010)Surgical specimens were collected from Department of Gastroenterology and Hepatology,General Hospital of Eastern Theater Command.The use of human biopsies was approved by the Ethics Committee of Jinling Hospital(No.2022DZKY-048-01).All patients enrolled were given informed written consent.
文摘Inflammatory bowel disease(IBD)is an autoimmune gastrointestinal disease characterized by chronic relapsing inflammation of the intestine.Excessive pyroptosis that exists in the inflamed intestine can activate damage signals and aggravate local inflammation in IBD.Here,we designed an oral pyroptosis nanoinhibitor,DXMS@CuM@PPADT@PSS(DCMP),which can target intestinal lesions,and respond to reactive oxygen species(ROS)to release active sites and drugs at the lesion.DCMP can inhibit the activation of the nucleotide-binding domain and leucine-rich repeat family pyrin domain containing 3(NLRP3)inflammasomes by scavenging ROS,resulting in the down-regulation of gasdermin D(GSDMD)cleavage thus inhibiting pyroptosis.It also improved intestinal barrier function,decreased inflammatory cytokine levels,and increased the diversity of gut microbiota in mice with colitis.This work is believed to expand the biomedical application of nanomaterials for innate immunity modulation.
基金financially supported by the National Natural Science Foundation of China(No.U1906213)the National Key Research and Development Program of China(No.2022YFC2804100)。
文摘Four new cyclohexapeptides,pyridapeptides F–I(1–4),were isolated from the fermentation broth of marine sponge-derived Streptomyces sp.OUCMDZ-4539.The pyridapeptides F–H(1–3)are composed ofβ-hydroxyleucine,alanine,O-methylthreonine,hexahydropyridazine-3-carboxylic acid,5-hydroxytetrahydropyridazine-3-carboxylic acid,and(2S,3R,4E,6E)-2-amino-3–hydroxy-4,6-dienoic acid residues.Pyridapeptide I(4)contains(2S,3R,4E,6E)-2-amino-3–hydroxy-8-methylnona-4,6-dienoic acid residue and a very rare glycose residue,aculose.Their structures were determined based on spectroscopic analysis and chemical methods.Pyridapeptides G–I(2–4)have the 2,3,6-trideoxyhexose units glycosylated at theγ-OH-TPDA residue,displayed significant antiproliferative activity against four(PC9,MKN45,Hep G2,K562)or two(PC9,MKN45)human cancer cell lines.
文摘From the oligotrophic culture of a soft coral-associated actinomycetes strain, Streptomyces sp. OUCMDZ-1703, we isolated and identified two new chlorinated polyketides that we named strepchloritides A and B （1 and 2）, three thiazole derivatives known as watasemycin A （3）, pulicatin G （4） and aerugine （5）, along with pyrrole- 2-carboxamide, furan-2-carboxamide and 1-（3,5-dihydroxyphenyl）ethanone. The new structures of 1 and 2 were determined by spectroscopic studies such as 1D- and 2D-NMR and MS analyses, while the known compounds were identified by comparison of the NMR data with those in literatures. The results showed that actinomycete strain OUCMDZ-1703 could use the relative high ratio of chlorine in the oligotrophic medium to synthesize chlorinated natural products. New compounds 1 and 2 displayed cytotoxicity against the MCF-7 ceils with ICs0 values of 9.9 and 20.2 ~tmoloL-1, respectively. Thiazole derivatives 3 and 5 were first found to be active against three clinical strains of methicillin-resistant Staphylococcus aureus （MRSA082, MRSA111 and MRSA234） with the same MIC/MBC values of 7.81/7.81 μg·mL-1.
基金funded in part by the National Natural Science Foundation of China(81270006)Jiangsu Provincial Special Program of Medical Sciences,China(BL2012006).
文摘Background:The Ulcerative Colitis Endoscopic Index of Severity(UCEIS)and the Mayo Endoscopic Score(MES)were developed as an objective method of the endoscopic severity in ulcerative colitis(UC);however,it was still unclear whether UCEIS vs MES could guide the need for colectomy in acute severe colitis(ASC).Methods:Consecutive ASC patients between January 2012 and May 2016 were retrospectively evaluated.Demographic data,previous therapy,clinical observations,laboratory parameters,medical therapy and endoscopic assessments were documented.The primary outcome was the need for colectomy during admission and follow-up.Results:Ninety-two patients were enrolled.37(40.2%)needed colectomy.UCEIS score is a predictor of requirement for colectomy inmultivariate analysis(OR,3.25;95%CI,1.77–5.97;P<0.001).Receiver-operator characteristic(ROC)area of UCEIS is 0.85,with a sensitivity of 60.3%and specificity of 85.5%using cut-off value of 7,which outperforms MES with the ROC area of 0.65;When UCEIS score7,80%of patients eventually need colectomy.Conclusion:UCEIS outperformed MES as a predictor for need for colectomy in ASC patients.The high probability of medical treatment failure and benefits of early colectomy should be discussed in patients with baseline UCEIS7.Acute severe colitis;colectomy;Ulcerative Colitis Endoscopic Index of Severity;Mayo Endoscopic Score.
基金financially supported by the National Natural Science Foundation of China(Nos.41876172,41806086,U150122141376148&U1606403)the Fundamental Research Funds for the Central Universities(No.201841006)
文摘Pafuranones A(1)and B(2),a pair of new epimeric polyketide dimers,were isolated from the fungus Paraconiothyrium sp.OUCMDZ-3316 associated with the marine algae Enteromorpha prolifera.Their structures,including absolute configurations,were fully elucidated based on spectroscopic analysis,calculated ECD,and chemical methods.Pafuranones A(1)and B(2)possess a rare dimeric furanone skeleton,which might be formed through a conjugate addition of the monomeric units followed by an intramolecular cyclization.
基金financially supported by the 100 Leading Talents of Guizhou Province (fund for W. Zhu and X. Hao)the Science and Technology Project of Guizhou (No. QKHT Z-20144007)the Academician Workstation of Guizhou (No. QKH YSZ2015-4009)
文摘Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia multiflora. The structures of new compounds were determined in the light of spectroscopic data,X-ray and ECD calculation. Compounds 1 and 3 are racemates, while compound 2 is optically pure.Compounds 1 and 4 showed antibacterial and antifungal activities against Staphylococcus aureus,Pseudomonas aeruginosa, Clostridium perfringens, Escherichia coli and Candida albicans with MIC values ranging from 8 μg/mL to 64 μg/mL.
基金the National Natural Science Foundation of China(41806086,U1906213,41876172)。
文摘Five new pyrrolizidine alkaloids,bohemamines J—N(1-5),were isolated from Streptomyces sp.CPCC 200497.Their structures were assigned based on detailed spectroscopic analysis and semisynthesis.Bohemamine J(1)possesses a new chimeric skeleton derived from bohemamine A(6)and phenylacetaldehyde.Inspired by the nonenzymatic formation mechanism of the methylene-bridged dimers isolated from this strain,we synthesized a series of chimeric derivatives(8,9,and 12-23)through natural product chimera strategy.Compounds 13,15,19,and 21 showed significant antioxidant activity.
基金financially supported by the National Key Research and Development Program of China(No.2019YFC0312504)the National Natural Science Foundation of China(Nos.41876172,U1906213)。
文摘(±)-Pyriindolin(1)with a rare molecular backbone formed by fusing a 2,2'-bipyridine nucleus into a spiro[furan-3,3'-indoline]skeleton,was isolated from the Streptomyces albolongus EA12432.The constitution and the relative configuration of(±)-1 were determined by extensive spectroscopic analyses,^(13)C calculation and DP4+probability analysis.The absolute configurations of optically pure(+)-1 and(-)-1 which were obtained after a chiral high performance liquid chromatography(HPLC)separation were further identified by electronic circular dichroism(ECD)calculations.(+)-and(-)-Pyriindolins displayed moderate cytotoxicity against HCT-116 cell line with the half-maximal inhibitory concentration(IC_(50))values of 2.89±0.17μmol/L and 4.47±0.26μmol/L,respectively.
基金This work is supported by the National Natural Science Foundation of China(NSFC)(Nos.U1906213,41876172.and U1606403).
文摘In order to discover structurally new and bioactive conipounds from marine life,we studied the secondary metabolites of the marine-derived fungi associated with a marine sponge(XS-3)from the Xisha islands.As a result,4-O-methylcandidusin A(1),a new p-terphenyl alcohol,along with nine known analogs(2-10),were isolated and identified from the marine spongederived fungus Aspergillus candidus OUCMDZ-1051.The structures of these compounds were determined by analyzing spectroscopic data,especially ID and 2D NMR.The new compound 1 selectively inhibited the growth of the MDA-MB-46&BT474 and A431 human cancer cell lines with the IC_(50) values of 1.84,6.05 and 0.98 pmol/L,respectively.Compound 1 also displayed a selective antimicrobial activity against Escherichia coli with an MIC value of 27.3 pmol/L.The results indicated 4-O-methylcandidusin A(1)as a potential lead in the new drug discovery for triple negative breast cancer,invasive ductal breast cancer and epidermoid cancer.The antimicrobial metabolites also evidenced a clue for chemical defense of sponges by their associated microorganisms.
