Dragon Boat Festival herbal markets in the Qianxinan Buyi and Miao Autonomous Prefecture of southwestern Guizhou have a long well-conserved history.These markets,which are a feature of Buyi and Miao traditional medici...Dragon Boat Festival herbal markets in the Qianxinan Buyi and Miao Autonomous Prefecture of southwestern Guizhou have a long well-conserved history.These markets,which are a feature of Buyi and Miao traditional medicines,contain a rich diversity of medicinal plants and traditional medical knowledge.Today,people in southwestern Guizhou still believe that using herbs during the Dragon Boat Festival prevents and can treat disease.In this study,we identified the fresh herbal plants sold at the herbal markets of Xingren City and Zhenfeng County in Qianxinan Buyi and Miao Autonomous Prefecture and quantified their importance.We identified 141 plant species(belonging to 114 genera and 61 families).The plant family with the most species was Asteraceae(14 species).Informants reported that most medicinal plants are herbaceous,with 95.7%of plants used for decoction and 30.5%used for medicinal baths.Medicinal plants are most commonly used to treat rheumatism,injury,and abdominal diseases.The utilization frequency index and relative importance values indicated that Artemisia argyi and Acorus calamus are the most important plants sold at herbal markets during the Dragon Boat Festival.The price of medicinal materials sold in the market may serve as an indicator of the conservation status of species in the region.These findings indicate that the Dragon Boat Festival herbal markets in the Qianxinan Buyi and Miao Autonomous Prefecture fully embodies the characteristics of indigenous ethnomedicine and culture,and also exhibits the diversity of plant resources.We recommend that rare and endangered plants in this region be domesticated and protected.展开更多
[Objectives]To explore the therapeutic effect of Polygonum capitatum on renal calculus in rats based on network pharmacology.[Methods]Through the preliminary construction of P.capitatum-urolithiasis disease target net...[Objectives]To explore the therapeutic effect of Polygonum capitatum on renal calculus in rats based on network pharmacology.[Methods]Through the preliminary construction of P.capitatum-urolithiasis disease target network,explore the active components,action pathway and action target of P.capitatum-urolithiasis treatment,and use 1%ethylene glycol+2%ammonium chloride to induce SD rat kidney calcium oxalate stone model to verify the efficacy of P.capitatum-urolithiasis treatment.[Results]Through the network pharmacological prediction,it is found that the important active components in P.capitatum were quercetin,gallic acid,rutin,silybin,catechin,kaempferol and so on;potential active targets include INS,CAT,IL-6,MOCOS,etc.The results also suggest that forkhead transcription factor signaling pathway(FoxO signaling pathway),tumor necrosis factor signaling pathway(TNF signaling pathway)and hypoxia-inducible factor signaling pathway(HIF-1 signaling pathway)are the core pathways.The results of biochemical indicators in animal experiment showed that the contents of serum urea nitrogen(BUN),creatinine(Cr)and malondialdehyde(MDA)in renal tissue in the treatment group(200,500 mg/kg)were significantly lower than those in the model group,while the content of superoxide dismutase(SOD)was significantly higher than that in the model group.In addition,the kidney tissue H&E staining sections showed that P.capitatum alcohol extract administration group rats kidney calcium oxalate crystals were significantly reduced compared with the model group,the degree of renal tubular lumen expansion was lighter than the model group,suggesting that P.capitatum alcohol extract has the effect of improving renal calculus in rats.[Conclusions]This study provides a theoretical reference for the deep development of P.capitatum in the treatment of renal calculus.展开更多
Perovskite nanocrystals(PNCs)have recently become promising optoelectronic materials due to their excellent photophysical properties.However,the highly dynamic binding state between ligands and the surface of PNCs has...Perovskite nanocrystals(PNCs)have recently become promising optoelectronic materials due to their excellent photophysical properties.However,the highly dynamic binding state between ligands and the surface of PNCs has severely restricted their luminescent properties and stabilities.In this work,1,3-bisbenzyl-2-oxoimidazolidine-4,5-dicarboxylic acid(cycle acid,CA)is introduced as both an etchant and a ligand upon post-synthetic surface treatment of PNCs.By removing the imperfect octahedrons[Pb X_(6)]^(4-)and passivating the surface defects synergistically,this treatment improves photoluminescence quantum yields from 76%to 95%and enhances the stability of PNCs against polar solvent,moisture,heat,and illumination.Meanwhile,CA can effectively and instantly recover the luminescence emission for aged PNCs.As a result,the CA-Cs Pb Br_(3)PNCs and CA-Cs Pb IxBr_(3-x)PNCs are applied as color-converting layers on a blue LED chip for warm white light-emitting diodes(WLEDs)with a color coordinate of(0.41,0.40).Importantly,the CA-based WLED device exhibits superior stability in operational conditions.展开更多
In this study,the sources of potentially toxic elements(PTEs)from atmospheric deposition in the waters of Guizhou’s Caohai Lake were investigated in addition to the potential risks to human health.Moss bags were used...In this study,the sources of potentially toxic elements(PTEs)from atmospheric deposition in the waters of Guizhou’s Caohai Lake were investigated in addition to the potential risks to human health.Moss bags were used to enrich PTEs from atmospheric deposition,and eight monitoring sites that best represented geographic variation were established around Caohai Lake.Moss bags were collected and examined at every 3 months to identify spatiotemporal patterns of dry and wet atmospheric deposition of PTEs.Zn was the most abundant metal identified from deposition in Caohai(72.07%–95.94%),followed by Pb and Cd,while Hg was the least abundant(0.008%–0.354%).The contributions of wet deposition of PTEs were greater than those of dry deposition,and deposition during the heating season from December to April was greater than that between April to July.Hg was mainly derived from atmospheric dry deposition(65.38%–84.44%).Spatial distribution analysis indicated that atmospheric deposition was associated with the intensity of human activities and heating emissions.Exposure via hand-to-mouth contact accounted for over 99%of the total exposure risk although overall exposure was lower than threshold acceptable levels for carcinogenic and non-carcinogenic metals,indicating an overall lack of risk towards human health.Nevertheless,the health risk from atmospheric deposition of PTEs in Caohai Lake may be reduced by focusing on Zn,Pb,and Cd deposition in rainfall and minimizing the hazards associated with hand-to-mouth exposure to PTEs.展开更多
Bletilla striata belongs to the family Orchidaceae,and it is mainly distributed in East Asia.The tubers of B.striata have been utilized in Traditional Chinese Medicine for various ailments,such as hematemesis,tubercul...Bletilla striata belongs to the family Orchidaceae,and it is mainly distributed in East Asia.The tubers of B.striata have been utilized in Traditional Chinese Medicine for various ailments,such as hematemesis,tuberculosis,malignant ulcers,hemorrhoids,traumatic bleeding,and chapped skin.Phytochemical investigation on B.striata has resulted in the identification of 192 monomeric compounds,including bibenzyls,phenanthrene derivatives,triterpenoids and its saponins,steroids and its saponins,malic acid derivatives,and anthocyanins.Moreover,B.striata polysaccharide is another typical chemical constituent of this plant.Pharmacology studies have shown that the plant possesses wound healing,antimicrobial,anticancer,antioxidative,and antiviral activities.This review aims to provide the latest and comprehensive information on chemical constituents,pharmacological activities,and quality control of B.striata and to identify future research needs.展开更多
This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic propert...This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties.Hypericum sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry calculations.Six compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.展开更多
Four new sesquiterpene lactones(SLs)(1–4),along with a biosynthetically related SL(5),have been isolated from the leaves of Magnolia grandiflora.Magrandate A(1)is notable as the first C18 homogemarane type SL,featuri...Four new sesquiterpene lactones(SLs)(1–4),along with a biosynthetically related SL(5),have been isolated from the leaves of Magnolia grandiflora.Magrandate A(1)is notable as the first C18 homogemarane type SL,featuring a unique 1,7-dioxaspiro[4.4]nonan-6-one core.Compounds 2 and 3,representing the first instances of chlorine-substituted gemarane-type SL analogs in natural products,were also identified.The structures of these isolates were elucidated through a combination of spectroscopic data analysis,electronic circular dichroism calculations,and X-ray single-crystal diffraction analysis.All isolates demonstrated anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 cells.Notably,3–5 showed a significant inhibitory effect on nitric oxide production,with IC50 values ranging from 0.79 to 4.73μmol·L^(−1).Additionally,4 and 5 exhibited moderate cytotoxic activities against three cancer cell lines,with IC50 values between 3.09 and 11.23μmol·L^(−1).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
In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of ...In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of extensive NMR spectroscopic analysis,HR-ESIMS data,and ECD calculations.The anti-leukemia activities of all compounds towards three cell lines(HEL,KG-1a,and K562)were evaluated in vitro.Compounds 1–3 exhibited moderate cytotoxicity with IC50 values ranging from 1.59 to 5.47μmol·L^(−1).Mechanistic studies indicated that 2 induced apoptosis by decreasing anti-apoptotic protein Bcl-2 and activating the caspase family in K562 cells.These results suggest that compound 2 is a potential anti-leukemia agent.展开更多
In the present study,four new sesquiterpenoids,chimonols A–D(compounds 1–4),together with four known compounds(5–8) were isolated from the Et OAc extract of Chimonanthus praecox Link.The structures of these new com...In the present study,four new sesquiterpenoids,chimonols A–D(compounds 1–4),together with four known compounds(5–8) were isolated from the Et OAc extract of Chimonanthus praecox Link.The structures of these new compounds were elucidated on the basis of spectroscopic techniques(UV,IR,MS,and 1 D and 2 D NMR),and their absolute configurations were established by comparing experimental and calculated electronic circular dichroism(ECD) spectra.Compounds 1–8 were evaluated for antimicrobial activities and the minimum inhibitory concentrations(MICs) were determined by the broth microdilution method in 96-well culture plates.Compounds 1,2,and 7 exhibited weak antibacterial effects for S.aureus(ATCC 6538),E.coli(ATCC 11775),and P.aeruginosa(ATCC 10145) with MIC values being 158–249 μg·mL^(-1).Compounds 3–7 showed activities against C.glabrata(ATCC 2001) and S.aureus(ATCC 43300) with MIC values being 128–197 μg·mL^(-1).Compounds 1–4 showed activity against S.aureus(ATCC 25923) with MIC values being 162–254 μg·mL^(-1).The present study provided a basis for future evaluation of these compounds as antibacterial agents.展开更多
Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 p...Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 possessed an unprecedented 6/5/6 tricyclic skeleton,while compounds 2 and 3 characterized by rare 6/6/5/6 tetracyclic system and 6/6/6/6/6 pentacyclic system respectively.Moreover,compound 4 possessed an unprecedented 6/7/6/6 tetracyclic core,and compound 5 characterized by rare 6/6/6/6tetracyclic skeleton.Their structures were elucidated by comprehensive spectroscopic data analysis and electronic circular dichroism(ECD)calculations.Biological tests indicated that compound 5 displayed significant anti-tobacco mosaic virus(TMV)activity compared with the positive control ningnanmycin.展开更多
A one-pot and efficient tliree-component reaction of indoles, acrylates and maleimides for the synthesis of pyrrolo[3,4-α]carbazole-1,3-dione derivatives was developed. Three C-C bonds and one ring were created in a ...A one-pot and efficient tliree-component reaction of indoles, acrylates and maleimides for the synthesis of pyrrolo[3,4-α]carbazole-1,3-dione derivatives was developed. Three C-C bonds and one ring were created in a single step via an indole-to-carbazole transformation triggered by Pd(II)-catalyzed direct C3-alkenylation of indoles.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
Eleven biogenetically related polyprenylated acylphloroglucinols(PPAPs),including four novel skeletons(1-4)and five new com-pounds(5-9),were isolated from the flowers of Hypericum monogynum.Hypermonones A-D(1-4)repres...Eleven biogenetically related polyprenylated acylphloroglucinols(PPAPs),including four novel skeletons(1-4)and five new com-pounds(5-9),were isolated from the flowers of Hypericum monogynum.Hypermonones A-D(1-4)represented the first example of a unique dilactone structure containing carbonyl bonded single 5-lactone and tricyclic γ-lactone moieties.Their structures were elucidated by NMR analysis,X-ray crystallography,and ECD calculations.Moreover,we revised the structure of hyperibrin B to hy perm on one I(9)via NMR an alysis,a qua ntum computational chemistry method,and hypothetic bios yn thetic con siderations.Three compounds(5,6,and 9)with significant MDR reversal activity(RF ranging from 61 to 223)were superior to the positive control verapamil(MCF-7/ADR,RF:53;HepG2/ADRz RF:124).Mechanism study for compound 5 indicated that this compound could inhibit the function of P-gp tran sport rather tha n its expressi on,and the possible recog nition mechanism betwee n compo und 5 and P-gp was predicted by molecular docking.展开更多
基金This work was supported by the grants from the National Natural Science Foundation of China(31860074,U1812403)the Science and Technology project of Guizhou Province(QKHZC[2018]2799)and Guizhou Province Engineering Research Center for Natural Drugs.
文摘Dragon Boat Festival herbal markets in the Qianxinan Buyi and Miao Autonomous Prefecture of southwestern Guizhou have a long well-conserved history.These markets,which are a feature of Buyi and Miao traditional medicines,contain a rich diversity of medicinal plants and traditional medical knowledge.Today,people in southwestern Guizhou still believe that using herbs during the Dragon Boat Festival prevents and can treat disease.In this study,we identified the fresh herbal plants sold at the herbal markets of Xingren City and Zhenfeng County in Qianxinan Buyi and Miao Autonomous Prefecture and quantified their importance.We identified 141 plant species(belonging to 114 genera and 61 families).The plant family with the most species was Asteraceae(14 species).Informants reported that most medicinal plants are herbaceous,with 95.7%of plants used for decoction and 30.5%used for medicinal baths.Medicinal plants are most commonly used to treat rheumatism,injury,and abdominal diseases.The utilization frequency index and relative importance values indicated that Artemisia argyi and Acorus calamus are the most important plants sold at herbal markets during the Dragon Boat Festival.The price of medicinal materials sold in the market may serve as an indicator of the conservation status of species in the region.These findings indicate that the Dragon Boat Festival herbal markets in the Qianxinan Buyi and Miao Autonomous Prefecture fully embodies the characteristics of indigenous ethnomedicine and culture,and also exhibits the diversity of plant resources.We recommend that rare and endangered plants in this region be domesticated and protected.
基金Supported by Guizhou Provincial Science and Technology Plan Project (Gui Qian He Ji Chu-ZK[2022]General 362)Guizhou Provincial Department of Education Science and Technology Achievement Transfer and Transformation Project (Gui Jiao Ji[2022]064)+2 种基金Guizhou Provincial Department of Education Higher Education Engineering Research Center (Gui Jiao Ji[2023]035)China National University Student Innovation&Entrepreneurship Development Program (202210660131&202310660082)Guizhou s Emerging University Think Tank Alliance Construction Project (Qian Jiao Zhe[2023]ZK01).
文摘[Objectives]To explore the therapeutic effect of Polygonum capitatum on renal calculus in rats based on network pharmacology.[Methods]Through the preliminary construction of P.capitatum-urolithiasis disease target network,explore the active components,action pathway and action target of P.capitatum-urolithiasis treatment,and use 1%ethylene glycol+2%ammonium chloride to induce SD rat kidney calcium oxalate stone model to verify the efficacy of P.capitatum-urolithiasis treatment.[Results]Through the network pharmacological prediction,it is found that the important active components in P.capitatum were quercetin,gallic acid,rutin,silybin,catechin,kaempferol and so on;potential active targets include INS,CAT,IL-6,MOCOS,etc.The results also suggest that forkhead transcription factor signaling pathway(FoxO signaling pathway),tumor necrosis factor signaling pathway(TNF signaling pathway)and hypoxia-inducible factor signaling pathway(HIF-1 signaling pathway)are the core pathways.The results of biochemical indicators in animal experiment showed that the contents of serum urea nitrogen(BUN),creatinine(Cr)and malondialdehyde(MDA)in renal tissue in the treatment group(200,500 mg/kg)were significantly lower than those in the model group,while the content of superoxide dismutase(SOD)was significantly higher than that in the model group.In addition,the kidney tissue H&E staining sections showed that P.capitatum alcohol extract administration group rats kidney calcium oxalate crystals were significantly reduced compared with the model group,the degree of renal tubular lumen expansion was lighter than the model group,suggesting that P.capitatum alcohol extract has the effect of improving renal calculus in rats.[Conclusions]This study provides a theoretical reference for the deep development of P.capitatum in the treatment of renal calculus.
基金financial from the National Natural Science Foundation of China(22279039 and 20181194)the Chinese National 1000-Talent-Plan program+2 种基金the Innovation Project of Optics Valley Laboratory(OVL2021BG008)the Frontier of the Application Foundation of Wuhan Science and Technology Plan Project(2020010601012202)the Foundation of State Key Laboratory of New Textile Materials and Advanced Processing Technologies(FZ2021011)。
文摘Perovskite nanocrystals(PNCs)have recently become promising optoelectronic materials due to their excellent photophysical properties.However,the highly dynamic binding state between ligands and the surface of PNCs has severely restricted their luminescent properties and stabilities.In this work,1,3-bisbenzyl-2-oxoimidazolidine-4,5-dicarboxylic acid(cycle acid,CA)is introduced as both an etchant and a ligand upon post-synthetic surface treatment of PNCs.By removing the imperfect octahedrons[Pb X_(6)]^(4-)and passivating the surface defects synergistically,this treatment improves photoluminescence quantum yields from 76%to 95%and enhances the stability of PNCs against polar solvent,moisture,heat,and illumination.Meanwhile,CA can effectively and instantly recover the luminescence emission for aged PNCs.As a result,the CA-Cs Pb Br_(3)PNCs and CA-Cs Pb IxBr_(3-x)PNCs are applied as color-converting layers on a blue LED chip for warm white light-emitting diodes(WLEDs)with a color coordinate of(0.41,0.40).Importantly,the CA-based WLED device exhibits superior stability in operational conditions.
基金supported by the National Natural Science Foundation of China(21767006)The Science and Technology of Guizhou Province,China([2018]2349)。
文摘In this study,the sources of potentially toxic elements(PTEs)from atmospheric deposition in the waters of Guizhou’s Caohai Lake were investigated in addition to the potential risks to human health.Moss bags were used to enrich PTEs from atmospheric deposition,and eight monitoring sites that best represented geographic variation were established around Caohai Lake.Moss bags were collected and examined at every 3 months to identify spatiotemporal patterns of dry and wet atmospheric deposition of PTEs.Zn was the most abundant metal identified from deposition in Caohai(72.07%–95.94%),followed by Pb and Cd,while Hg was the least abundant(0.008%–0.354%).The contributions of wet deposition of PTEs were greater than those of dry deposition,and deposition during the heating season from December to April was greater than that between April to July.Hg was mainly derived from atmospheric dry deposition(65.38%–84.44%).Spatial distribution analysis indicated that atmospheric deposition was associated with the intensity of human activities and heating emissions.Exposure via hand-to-mouth contact accounted for over 99%of the total exposure risk although overall exposure was lower than threshold acceptable levels for carcinogenic and non-carcinogenic metals,indicating an overall lack of risk towards human health.Nevertheless,the health risk from atmospheric deposition of PTEs in Caohai Lake may be reduced by focusing on Zn,Pb,and Cd deposition in rainfall and minimizing the hazards associated with hand-to-mouth exposure to PTEs.
文摘Bletilla striata belongs to the family Orchidaceae,and it is mainly distributed in East Asia.The tubers of B.striata have been utilized in Traditional Chinese Medicine for various ailments,such as hematemesis,tuberculosis,malignant ulcers,hemorrhoids,traumatic bleeding,and chapped skin.Phytochemical investigation on B.striata has resulted in the identification of 192 monomeric compounds,including bibenzyls,phenanthrene derivatives,triterpenoids and its saponins,steroids and its saponins,malic acid derivatives,and anthocyanins.Moreover,B.striata polysaccharide is another typical chemical constituent of this plant.Pharmacology studies have shown that the plant possesses wound healing,antimicrobial,anticancer,antioxidative,and antiviral activities.This review aims to provide the latest and comprehensive information on chemical constituents,pharmacological activities,and quality control of B.striata and to identify future research needs.
基金supported by the National Natural Science Foundation of China(No.32270413,U1812403)the Science and Technology Department of Guizhou Province(No.QKH 2020-1Z076)+5 种基金the 13th batch of Outstanding Young Scientific and Technological Talents in Guizhou Province(No.QKHPTRC[2021]5633)Cultivation project of National Natural Science Foundation of Guizhou Medical University(No.19NSP003)the Education Department of Guizhou Province(No.QJH KY[2021]189)the Natural Science Foundation of Guizhou Province(No.QKHZYD[2022]4015)High-level Innovative Talents in Guizhou Province(Thousand Levels of Talent for Chunmao Yuan in 2018)“Light of the West”Talent Cultivation Program of Chinese Academy of Sciences for Chunmao Yuan(No.RZ[2020]82).
文摘This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties.Hypericum sampsonii was investigated,leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols(PPAPs)(1 and 2),eight phenolic derivatives(3-10),and four terpene derivatives(11-14).The structures of compounds 1 and 2,featuring an unprecedented octahydro-2H-chromen-2-one ring system,were fully characterized using extensive spectroscopic data and quantum chemistry calculations.Six compounds(1,5-7,9,and 14)exhibited potential inhibitory effects against α-glucosidase,with IC_(50) values ranging from 0.050±0.0016 to 366.70±11.08μg·mL^(-1).Notably,compound 5(0.050±0.0016μg·mL^(-1))was identified as the most potential α-glucosidase inhibitor,with an inhibitory effect about 6900 times stronger than the positive control,acarbose(IC_(50)=346.63±15.65μg·mL^(-1)).A docking study was conducted to predict molecular interactions between two compounds(1 and 5)and α-glucosidase,and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.
基金supported by the National Natural Science Foundation of China(Nos.82060631 and 32270413)the Science and Technology Department of Guizhou Province[Nos.QKH JC(2020)1Z076 and QKH JC(2020)1Y400],the Cultivation Project of National Natural Science Foundation of Guizhou Medical University(No.2023-106)+2 种基金the Outstanding Young Scientific and Technological Talents in Guizhou Province[No.QKH PTRC(2021)5633],High-level Innovative Talents in Guizhou Province(Thousand Levels of Talent for YUAN Chunmao in 2018)“Light of the West”Talent Cultivation Program of Chinese Academy of Sciences for YUAN Chunmao[RZ(2020)82],Guizhou Science and Technology Innovation Talent Team(No.QKHPTRCCXTD[2022]007)the Natural Science Foundation of Guizhou Province[No.QKHZYD(2022)4015].
文摘Four new sesquiterpene lactones(SLs)(1–4),along with a biosynthetically related SL(5),have been isolated from the leaves of Magnolia grandiflora.Magrandate A(1)is notable as the first C18 homogemarane type SL,featuring a unique 1,7-dioxaspiro[4.4]nonan-6-one core.Compounds 2 and 3,representing the first instances of chlorine-substituted gemarane-type SL analogs in natural products,were also identified.The structures of these isolates were elucidated through a combination of spectroscopic data analysis,electronic circular dichroism calculations,and X-ray single-crystal diffraction analysis.All isolates demonstrated anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 cells.Notably,3–5 showed a significant inhibitory effect on nitric oxide production,with IC50 values ranging from 0.79 to 4.73μmol·L^(−1).Additionally,4 and 5 exhibited moderate cytotoxic activities against three cancer cell lines,with IC50 values between 3.09 and 11.23μmol·L^(−1).
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supported by the Science and Technology Department of Guizhou Province(No.QKHJC[2016]1002,81872772,81960546,and U1812403)the National Natural Science Foundation of China(Nos.81872772,81960546,and U1812403)+1 种基金the Science and Technology Department of Anshun City(No.ASKP[2019]3)the 100 Leading Talents of Guizhou Province(fund for LI Yan-Mei,Nos.P2018-KF11 and QZYY-019-022).
文摘In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of extensive NMR spectroscopic analysis,HR-ESIMS data,and ECD calculations.The anti-leukemia activities of all compounds towards three cell lines(HEL,KG-1a,and K562)were evaluated in vitro.Compounds 1–3 exhibited moderate cytotoxicity with IC50 values ranging from 1.59 to 5.47μmol·L^(−1).Mechanistic studies indicated that 2 induced apoptosis by decreasing anti-apoptotic protein Bcl-2 and activating the caspase family in K562 cells.These results suggest that compound 2 is a potential anti-leukemia agent.
基金supported by the Ministry of Science&Technology on China(No.2017YFD0201402)the National Natural Science Foundation of China(Nos.81160390 and 81660580)+2 种基金the Science and Technology Department of Guizhou Province,China{Nos.(QKHRCTD[2015]4026)(QKHLHZ[2015]7400)QKHRC[2016]4037,[2011]LKZ7051,and QKZHJ(2009)2150}
文摘In the present study,four new sesquiterpenoids,chimonols A–D(compounds 1–4),together with four known compounds(5–8) were isolated from the Et OAc extract of Chimonanthus praecox Link.The structures of these new compounds were elucidated on the basis of spectroscopic techniques(UV,IR,MS,and 1 D and 2 D NMR),and their absolute configurations were established by comparing experimental and calculated electronic circular dichroism(ECD) spectra.Compounds 1–8 were evaluated for antimicrobial activities and the minimum inhibitory concentrations(MICs) were determined by the broth microdilution method in 96-well culture plates.Compounds 1,2,and 7 exhibited weak antibacterial effects for S.aureus(ATCC 6538),E.coli(ATCC 11775),and P.aeruginosa(ATCC 10145) with MIC values being 158–249 μg·mL^(-1).Compounds 3–7 showed activities against C.glabrata(ATCC 2001) and S.aureus(ATCC 43300) with MIC values being 128–197 μg·mL^(-1).Compounds 1–4 showed activity against S.aureus(ATCC 25923) with MIC values being 162–254 μg·mL^(-1).The present study provided a basis for future evaluation of these compounds as antibacterial agents.
基金financially supported by the National Natural Science Foundation of China(Nos.32160103 and U1812403)the Science and Technology Department of Guizhou Province(Nos.QKH ZC-[2021]-YB181,QKH CXTD-[2022]-007 and QKH ZYD-[2022]-4015)Guizhou Provincial Engineering Research Center for Natural Drugs。
文摘Three novel matrine-type alkaloids(1-3)and two unprecedented aloperine-type alkaloids(4 and 5)were isolated from the root of Sophora tonkinensis and the seeds of Sophora alopecuroides respectively.Notably,compound 1 possessed an unprecedented 6/5/6 tricyclic skeleton,while compounds 2 and 3 characterized by rare 6/6/5/6 tetracyclic system and 6/6/6/6/6 pentacyclic system respectively.Moreover,compound 4 possessed an unprecedented 6/7/6/6 tetracyclic core,and compound 5 characterized by rare 6/6/6/6tetracyclic skeleton.Their structures were elucidated by comprehensive spectroscopic data analysis and electronic circular dichroism(ECD)calculations.Biological tests indicated that compound 5 displayed significant anti-tobacco mosaic virus(TMV)activity compared with the positive control ningnanmycin.
基金Supported by the National Natural Science Foundation of China(No.21762014)the Science Foundation of Guizhou Province, China(No.[2015] 2107).
文摘A one-pot and efficient tliree-component reaction of indoles, acrylates and maleimides for the synthesis of pyrrolo[3,4-α]carbazole-1,3-dione derivatives was developed. Three C-C bonds and one ring were created in a single step via an indole-to-carbazole transformation triggered by Pd(II)-catalyzed direct C3-alkenylation of indoles.
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.
基金supported by the National Natural Science Foundation of China(Nos.U1812403,81872772,and 81960546)the Scie nee and Tech no logy Departme nt of Guizhou Province(Nos.QKH 2020-1Z076,QKHZC[2020]4Y203z QKHJC[2018]1409,QKHZC[2019]2762,and QKHPTRC[2020]5008)+3 种基金the High-level Innovative Talents in Guizhou Provinee(Thousand Levels of Talent for Chunmao Yuan in 2018)the"Light of the West"Talent Cultivation Program of Chinese Academy of Sciences for Chunmao Yuan(No.RZ[2020]82)the 100 Leading Talents of Guizhou Provinee(fund for Y.M.L)the Guizhou Provincial Engineering Research Center for Natural Drugs.
文摘Eleven biogenetically related polyprenylated acylphloroglucinols(PPAPs),including four novel skeletons(1-4)and five new com-pounds(5-9),were isolated from the flowers of Hypericum monogynum.Hypermonones A-D(1-4)represented the first example of a unique dilactone structure containing carbonyl bonded single 5-lactone and tricyclic γ-lactone moieties.Their structures were elucidated by NMR analysis,X-ray crystallography,and ECD calculations.Moreover,we revised the structure of hyperibrin B to hy perm on one I(9)via NMR an alysis,a qua ntum computational chemistry method,and hypothetic bios yn thetic con siderations.Three compounds(5,6,and 9)with significant MDR reversal activity(RF ranging from 61 to 223)were superior to the positive control verapamil(MCF-7/ADR,RF:53;HepG2/ADRz RF:124).Mechanism study for compound 5 indicated that this compound could inhibit the function of P-gp tran sport rather tha n its expressi on,and the possible recog nition mechanism betwee n compo und 5 and P-gp was predicted by molecular docking.