Magnoline(1),a new isoquinoline derivative,was isolated from the leaves of Magnolia sieboldii K.Koch(Magnoliaceae).Its structure was elucidated on the basis of spectral analysis including 1D,2D NMR and HR-TOF-MS.
The crystal structure of 3-(4-methoxyphenyl)-2-(4-methylbenzoyl)-6,7-dihydro-5H-furo[3,2-g]chromene was obtained by X-ray single-crystal diffraction. The molecule is in the triclinic crystal system, space group P1...The crystal structure of 3-(4-methoxyphenyl)-2-(4-methylbenzoyl)-6,7-dihydro-5H-furo[3,2-g]chromene was obtained by X-ray single-crystal diffraction. The molecule is in the triclinic crystal system, space group P1 with a = 11.0745(4), b = 13.0953(7), c = 15.8773(8) ?, α = 92.811(4), β = 104.815(4), γ = 111.797(4)o, Z = 4, the final R = 0.0567 and w R = 0.1540. X-ray crystal structure data revealed that one asymmetric structure unit of the title compound contained two molecules. The existence of methyl group changed the dihedral angle between furan ring and the phenyl ring at the C2 position of the furo[3,2-g]chromene scaffold as well as the conformation, and had a further influence on the bioactivity of the furo[3,2-g]chromene derivatives.展开更多
In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crys...In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crystal diffraction analysis.The biological activity results showed that the target compounds exhibited certain inhibitory activity of osteosarcoma cells U2OS-EGFP.Compounds 6a,6g and 6j exhibited more than 70%inhibition ratio at the concentration of 50μmol·L^-1,and especially,the IC5o value of compound 6j was 11.58μmol·L^-1.The crystal of 6h was obtained and analyzed;some related weak interactions were discussed.The molecular docking results showed that the target compounds were supposed to be ERK1/2 inhibitors.展开更多
In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR...In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1 Hbenzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) ?, Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702.展开更多
Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol ...Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosis. Herein, we report the development of a ligand-based pharmacophore model and pharmacophore-based virtual screening of the ZINC/big-n-greasy database, leading to the identification of compound H-10 as a potential CETP inhibitor in vitro. Based on H-10, a series of 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides were designed, synthesized, and evaluated against CETP. Compound 41 was found to have the best activity, resulting in 85.0% inhibition of CETP at l0 μmol/L.展开更多
A series ofN-(furan-2-ylmethyl)-lH-indole-3-carboxamide derivatives(6a--6p) was designed and synthe- sized for developing novel indole scaffolds as anticancer agents targeting the epidemal growth factor receptor ...A series ofN-(furan-2-ylmethyl)-lH-indole-3-carboxamide derivatives(6a--6p) was designed and synthe- sized for developing novel indole scaffolds as anticancer agents targeting the epidemal growth factor receptor (EGFR), and the cytotoxic activities of the target compounds were evaluated against three EGFR high-expressed cancer cell lines[human lung adenocarcinoma cell line(A549), Henrietta Lacks strain of cancer cell line(HeLa) and human colorectal cancer cell line(SW480)], one EGFR low-expressed cell line(human liver cancer cell line, HepG2) and one human liver normal cell line(HL7702) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, Some target compounds exhibited potent anficancer activities against A549, HeLa, SW480 and weak activities on HepG2, which signifies that the target compounds are likely to be EGFR inhibitors as expected. And they showed weak cytotoxic effects on HL7702, which implies the target compounds are probably to be of low toxicity against normal cells. Among them, the target compound 1-ethyl-N-(fttran-2-ylmethyl)-5-{2-{ [2-(2-methoxy- phenoxy)ethyl]amino}-2-oxoethoxy}-2-methyl-1H-indole-3-carboxamide(6p) with 2-{[2-(2-methoxyphenoxy)ethyl]- amino}-2-oxoethoxy group at the C5 position of the N-(furan-2-ylmethyl)-lH-indole-3-carboxamide scaffold exhibited the most potent anticancer activity. Also the binding interaction of the target compound 6p with EGFR was explored by molecular docking. Conclusively, the novel indole scaffold may be beneficial to investigate new anticancer agents for targeting the EGFR.展开更多
A series of sulfenimine cephalosporin sulfoxide derivatives (Ta-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested c...A series of sulfenimine cephalosporin sulfoxide derivatives (Ta-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested compounds showed enhanced inhibitory activity against class C β-lactamase cephalospor- inase compared with the tazobactam. The most promising compounds 7c and 7n (IC50 ~ 7.6 and 8.6 μmol/L, respectively) were further investigated in combination with cefradine against a variety of clinical isolated fi-lactamase-producing bacterial strains.展开更多
A series of pyrrolopyrazinone-chalcone hybrids(12a-12q) was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone(10a) ...A series of pyrrolopyrazinone-chalcone hybrids(12a-12q) was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone(10a) and 5-fluorouracil(5-FU),nearly all the tested compounds showed significantly-improved antitumor activities.The most promising compounds 12e and 12k(IC50=0.25 and 0.88 μmol/L) respectively show activities of 123and 35 times that of compound 10a(IC50=30.74 μmol/L) against HeLa cell line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.展开更多
Objective To optimize the extraction technology of the active component, rosmarinic acid, an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid, in perilla oil meal for the first time by a new homogenizing techn...Objective To optimize the extraction technology of the active component, rosmarinic acid, an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid, in perilla oil meal for the first time by a new homogenizing technology called smashing tissue extraction (STE). Methods Orthogonal design was used to optimize the extraction condition. The content of rosmarinic acid was quantified from the methanol crude extract with the help of HPLC. Results The optimization of STE process to get rosmarinic acid from the perilla oil meal was the ratio of liquid to solid material at 10:1 and the power of extraction at 150 V, extracting twice (2 min for each time). Conclusion STE could be applied to extracting the active ingredients from the oil meals due to its high extraction efficiency. This new homogenizing technology has advantages on saving extraction time, raising extraction efficiency, and maintaining the temperature sensitive constituents.展开更多
Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by si...Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by silica gel column chromatography and preparative HPLC.The structures of the isolated compounds were identified by spectral analyses,physical constants,and chemical evidences.Results Two cucurbitane triterpenoids were isolated and identified as 5β,19-epoxy-cucurbita-6,22E,24-trien-3β-ol(1)and cucurbita-6,22(E),24-trien-3β-ol-19,5β-olide(2).Conclusion Compound 1 is a new compound.展开更多
Objective To optimize the extract technology of active lignins from the fruits of Schisandra chinensis. Methods The content of schizandrin, gomisin A, and deoxyschizandrin were selected as standards to evaluate the ef...Objective To optimize the extract technology of active lignins from the fruits of Schisandra chinensis. Methods The content of schizandrin, gomisin A, and deoxyschizandrin were selected as standards to evaluate the efficiency of smashing tissue extraction (STE). Solid-liquid ratio, extracting times, ethanol concentration, and extracting time were investigated through orthogonal test. Results The optimized conditions for STE were ten times amount of 80% EtOH, extracting for three times, and 2 min for each time. Conclusion STE could obtain relatively higher yield, simplicity of operation, and benefit for environment protection. It could be better choice for the extraction of S. chinensis.展开更多
Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolate...Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolated from the seeds of Holarrhena antidysenteriaca Wall.ex A.DC. Their intrinsic antibacterial activities and synergistic effects with penicillin and vancomycin were analyzed in methicillin sensitive staphylococcus aureus(MSSA) and methicillin resistant staphylococcus aureus(MRSA). Two of the steroidal alkaloids including one new compound(N-formylconessimine) showed potential antibacterial activity and possessed synergistic effects with penicillin and vancomycin, respectively.展开更多
The present study was designed to further investigate the C_(21) steroidal glycosides in Cynanchum plants.Two new steroidal glycosides based on a 13,14:14,15-disecopregnane-type aglycone,komaroside P(1) and komaroside...The present study was designed to further investigate the C_(21) steroidal glycosides in Cynanchum plants.Two new steroidal glycosides based on a 13,14:14,15-disecopregnane-type aglycone,komaroside P(1) and komaroside Q(2),together with three known compounds(3-5) were isolated from the whole herbs of Cynanchum komarovii.The aglycones of compounds 1 and 2 were two new disecopregnane.Their structures were elucidated on the basis of 1 D,2 D NMR spectroscopic data and acid hydrolysis.All the compounds(1-5) showed potent inhibitory activities against human leukemia cell lines(HL-60) with IC50 values ranging from 16.6 to 26.3 μmol·L^(-1),compared to the positive control 5-fluorouracil(6.4 μmol·L^(-1)).展开更多
Mitochondrial dysfunction is associated with the emergence of several neurological and cardiovascular diseases. Hence, mitochondria-targeting delivery strategies are highly significant and critically needed. In this s...Mitochondrial dysfunction is associated with the emergence of several neurological and cardiovascular diseases. Hence, mitochondria-targeting delivery strategies are highly significant and critically needed. In this study, we developed a small library of peptides simulating the mitochondria-targeting peptide SS-31, a promising tetra-peptide with antioxidant character, and subsequently evaluated the toxicity, antioxidant ability and mitochondrial delivery of nanoparticles. Among the designed peptides, RF-2 (DArg-Dmt-Arg-Phe-NH2) showed controlled toxicity and excellent protection against gentamicin-induced hair cell damage, as compared with SS-31. More importantly, RF-2-modified PLGA nanoparticles demonstrated high colocalization with mitochondria and comparable specific subcellular accumulation, when compared with SS-31. Taken together, the obtained results supported RF-2 as a mitochondriatargeting peptide with high potential as a targeted carrier.展开更多
Two new iridoid glycosides,named scrophularianoids A(1) and B(2),were isolated from the roots of Scrophularia ningpoensis.The chemical structures were established on the basis of extensive analyses of spectroscopi...Two new iridoid glycosides,named scrophularianoids A(1) and B(2),were isolated from the roots of Scrophularia ningpoensis.The chemical structures were established on the basis of extensive analyses of spectroscopic data.Compounds 1 and 2 were inactive in our preliminary in vitro myocardial protective bioassay.展开更多
A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epi...A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549, human lung cancer cell H460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyldiphenyltetrazoliumromide(MTT) assay. Six compounds(Tb--7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 μmol/L against A549, H460 and HT-29 cell lines respectively, which is comparable to sorafenib.展开更多
Based on the molecular docking studies, which were performed to position Erlotinib and the target com- pounds into the active site of the epidermal growth factor receptor(EGFR) to determine the probable binding mode...Based on the molecular docking studies, which were performed to position Erlotinib and the target com- pounds into the active site of the epidermal growth factor receptor(EGFR) to determine the probable binding model, a novel series of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives as the novel potential EGFR kinase inhibitors was designed and synthesized. The antitumor activity of all the target compounds against human pulmonary carcinoma cell line A549 has been screened. Of all the target compounds, 4-[2-(l-piperidyl)carbonylmethoxyl- phenthio]-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine(Tj) demonstrated the most potent antitumor activity. Several of the target compounds exhibited moderate antitumor activity. The preliminary structure-activity relation- ships of some target compounds were summarized.展开更多
Curcumfa phaeocaulis Valeton is used in traditional Chinese medicines for the treatment of blood-related disorders such as blood stasis and inflammation.Our previous studies have found that sesquiterpenes were mainly ...Curcumfa phaeocaulis Valeton is used in traditional Chinese medicines for the treatment of blood-related disorders such as blood stasis and inflammation.Our previous studies have found that sesquiterpenes were mainly isolated from C.wenyujin and C.phaeocaulis,while diarylheptanoids were the major compounds from C.kwangsiensis.And most of the isolated compounds exhibited remarkable展开更多
Macleayine (1), a new natural occurring alkaloid with a unique spiro [furanone-piperidinedione] framework, was isolated from the aerial parts ofMacleaya cordata. Its unusual structure was established by extensive sp...Macleayine (1), a new natural occurring alkaloid with a unique spiro [furanone-piperidinedione] framework, was isolated from the aerial parts ofMacleaya cordata. Its unusual structure was established by extensive spectroscopic analyses, computer-assisted structure elucidation software (ACD/Structure Elucidator), quantum chemistry calculations and ECD calculation. The result of virtual molecular docking predicted the compound can enhance the effects of insulin, and may be used to treat tvpe II diabetes.展开更多
文摘Magnoline(1),a new isoquinoline derivative,was isolated from the leaves of Magnolia sieboldii K.Koch(Magnoliaceae).Its structure was elucidated on the basis of spectral analysis including 1D,2D NMR and HR-TOF-MS.
基金supported by the National Natural Science Foundation of China(No.J1103606)the Program for Innovative Research Team of the Ministry of Education of China(No.IRT_14R36)
文摘The crystal structure of 3-(4-methoxyphenyl)-2-(4-methylbenzoyl)-6,7-dihydro-5H-furo[3,2-g]chromene was obtained by X-ray single-crystal diffraction. The molecule is in the triclinic crystal system, space group P1 with a = 11.0745(4), b = 13.0953(7), c = 15.8773(8) ?, α = 92.811(4), β = 104.815(4), γ = 111.797(4)o, Z = 4, the final R = 0.0567 and w R = 0.1540. X-ray crystal structure data revealed that one asymmetric structure unit of the title compound contained two molecules. The existence of methyl group changed the dihedral angle between furan ring and the phenyl ring at the C2 position of the furo[3,2-g]chromene scaffold as well as the conformation, and had a further influence on the bioactivity of the furo[3,2-g]chromene derivatives.
基金supported by the National Natural Science Foundation of China(No.21342006)the Program for Innovative Research Team of the Ministry of Education of China(No.IRT_14R36)
文摘In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crystal diffraction analysis.The biological activity results showed that the target compounds exhibited certain inhibitory activity of osteosarcoma cells U2OS-EGFP.Compounds 6a,6g and 6j exhibited more than 70%inhibition ratio at the concentration of 50μmol·L^-1,and especially,the IC5o value of compound 6j was 11.58μmol·L^-1.The crystal of 6h was obtained and analyzed;some related weak interactions were discussed.The molecular docking results showed that the target compounds were supposed to be ERK1/2 inhibitors.
基金supported by the National Natural Science Foundation of China(No.21342006)the Program for Innovative Research Team of the Ministry of Education of China(No.IRT_14R36)
文摘In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1 H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1 Hbenzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) ?, Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702.
文摘Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosis. Herein, we report the development of a ligand-based pharmacophore model and pharmacophore-based virtual screening of the ZINC/big-n-greasy database, leading to the identification of compound H-10 as a potential CETP inhibitor in vitro. Based on H-10, a series of 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides were designed, synthesized, and evaluated against CETP. Compound 41 was found to have the best activity, resulting in 85.0% inhibition of CETP at l0 μmol/L.
基金Supported by the National Natural Science Foundation of China(No.21342006) and the Program for the Innovative Research Team of the Ministry of Education of China(No.IRT_14R36).
文摘A series ofN-(furan-2-ylmethyl)-lH-indole-3-carboxamide derivatives(6a--6p) was designed and synthe- sized for developing novel indole scaffolds as anticancer agents targeting the epidemal growth factor receptor (EGFR), and the cytotoxic activities of the target compounds were evaluated against three EGFR high-expressed cancer cell lines[human lung adenocarcinoma cell line(A549), Henrietta Lacks strain of cancer cell line(HeLa) and human colorectal cancer cell line(SW480)], one EGFR low-expressed cell line(human liver cancer cell line, HepG2) and one human liver normal cell line(HL7702) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, Some target compounds exhibited potent anficancer activities against A549, HeLa, SW480 and weak activities on HepG2, which signifies that the target compounds are likely to be EGFR inhibitors as expected. And they showed weak cytotoxic effects on HL7702, which implies the target compounds are probably to be of low toxicity against normal cells. Among them, the target compound 1-ethyl-N-(fttran-2-ylmethyl)-5-{2-{ [2-(2-methoxy- phenoxy)ethyl]amino}-2-oxoethoxy}-2-methyl-1H-indole-3-carboxamide(6p) with 2-{[2-(2-methoxyphenoxy)ethyl]- amino}-2-oxoethoxy group at the C5 position of the N-(furan-2-ylmethyl)-lH-indole-3-carboxamide scaffold exhibited the most potent anticancer activity. Also the binding interaction of the target compound 6p with EGFR was explored by molecular docking. Conclusively, the novel indole scaffold may be beneficial to investigate new anticancer agents for targeting the EGFR.
文摘A series of sulfenimine cephalosporin sulfoxide derivatives (Ta-v) were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested compounds showed enhanced inhibitory activity against class C β-lactamase cephalospor- inase compared with the tazobactam. The most promising compounds 7c and 7n (IC50 ~ 7.6 and 8.6 μmol/L, respectively) were further investigated in combination with cefradine against a variety of clinical isolated fi-lactamase-producing bacterial strains.
文摘A series of pyrrolopyrazinone-chalcone hybrids(12a-12q) was designed,synthesized and screened for their antitumor activity against SKOV-3,A549 and HeLa cell lines in vitro.Compared with the pyrrolopyrazinone(10a) and 5-fluorouracil(5-FU),nearly all the tested compounds showed significantly-improved antitumor activities.The most promising compounds 12e and 12k(IC50=0.25 and 0.88 μmol/L) respectively show activities of 123and 35 times that of compound 10a(IC50=30.74 μmol/L) against HeLa cell line.The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.
基金E&T Modern Center for Natural Products of Liaoning Province of China (2008402021)
文摘Objective To optimize the extraction technology of the active component, rosmarinic acid, an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid, in perilla oil meal for the first time by a new homogenizing technology called smashing tissue extraction (STE). Methods Orthogonal design was used to optimize the extraction condition. The content of rosmarinic acid was quantified from the methanol crude extract with the help of HPLC. Results The optimization of STE process to get rosmarinic acid from the perilla oil meal was the ratio of liquid to solid material at 10:1 and the power of extraction at 150 V, extracting twice (2 min for each time). Conclusion STE could be applied to extracting the active ingredients from the oil meals due to its high extraction efficiency. This new homogenizing technology has advantages on saving extraction time, raising extraction efficiency, and maintaining the temperature sensitive constituents.
基金National New Drug Incubation(Benxi)Base Construction of Liaoning Province(2010ZX09401-304-105B)the Doctoral InitiatingFoundation Project of Liaoning Province(20101108)
文摘Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by silica gel column chromatography and preparative HPLC.The structures of the isolated compounds were identified by spectral analyses,physical constants,and chemical evidences.Results Two cucurbitane triterpenoids were isolated and identified as 5β,19-epoxy-cucurbita-6,22E,24-trien-3β-ol(1)and cucurbita-6,22(E),24-trien-3β-ol-19,5β-olide(2).Conclusion Compound 1 is a new compound.
基金E&T modern center for Natural Products of Liaoning Province of China (2008402021)
文摘Objective To optimize the extract technology of active lignins from the fruits of Schisandra chinensis. Methods The content of schizandrin, gomisin A, and deoxyschizandrin were selected as standards to evaluate the efficiency of smashing tissue extraction (STE). Solid-liquid ratio, extracting times, ethanol concentration, and extracting time were investigated through orthogonal test. Results The optimized conditions for STE were ten times amount of 80% EtOH, extracting for three times, and 2 min for each time. Conclusion STE could obtain relatively higher yield, simplicity of operation, and benefit for environment protection. It could be better choice for the extraction of S. chinensis.
基金supported by the Natural Science Foundation of Liaoning Province(No.201602208)
文摘Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolated from the seeds of Holarrhena antidysenteriaca Wall.ex A.DC. Their intrinsic antibacterial activities and synergistic effects with penicillin and vancomycin were analyzed in methicillin sensitive staphylococcus aureus(MSSA) and methicillin resistant staphylococcus aureus(MRSA). Two of the steroidal alkaloids including one new compound(N-formylconessimine) showed potential antibacterial activity and possessed synergistic effects with penicillin and vancomycin, respectively.
基金supported by the National Natural Science Foundation of China(No.31370375)
文摘The present study was designed to further investigate the C_(21) steroidal glycosides in Cynanchum plants.Two new steroidal glycosides based on a 13,14:14,15-disecopregnane-type aglycone,komaroside P(1) and komaroside Q(2),together with three known compounds(3-5) were isolated from the whole herbs of Cynanchum komarovii.The aglycones of compounds 1 and 2 were two new disecopregnane.Their structures were elucidated on the basis of 1 D,2 D NMR spectroscopic data and acid hydrolysis.All the compounds(1-5) showed potent inhibitory activities against human leukemia cell lines(HL-60) with IC50 values ranging from 16.6 to 26.3 μmol·L^(-1),compared to the positive control 5-fluorouracil(6.4 μmol·L^(-1)).
基金financially supported by the National Natural Science Foundation of China (No. 81473162)the Program for Liaoning Excellent Talents in Universitythe Young and Middleaged Career Development Planning of Shenyang Pharmaceutical University
文摘Mitochondrial dysfunction is associated with the emergence of several neurological and cardiovascular diseases. Hence, mitochondria-targeting delivery strategies are highly significant and critically needed. In this study, we developed a small library of peptides simulating the mitochondria-targeting peptide SS-31, a promising tetra-peptide with antioxidant character, and subsequently evaluated the toxicity, antioxidant ability and mitochondrial delivery of nanoparticles. Among the designed peptides, RF-2 (DArg-Dmt-Arg-Phe-NH2) showed controlled toxicity and excellent protection against gentamicin-induced hair cell damage, as compared with SS-31. More importantly, RF-2-modified PLGA nanoparticles demonstrated high colocalization with mitochondria and comparable specific subcellular accumulation, when compared with SS-31. Taken together, the obtained results supported RF-2 as a mitochondriatargeting peptide with high potential as a targeted carrier.
文摘Two new iridoid glycosides,named scrophularianoids A(1) and B(2),were isolated from the roots of Scrophularia ningpoensis.The chemical structures were established on the basis of extensive analyses of spectroscopic data.Compounds 1 and 2 were inactive in our preliminary in vitro myocardial protective bioassay.
基金Supported by the National Natural Science Foundation of China(No.21002065) and the clence & lecnnology rroject ox Liaoning Province, China(No.LJQ201107).
文摘A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549, human lung cancer cell H460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyldiphenyltetrazoliumromide(MTT) assay. Six compounds(Tb--7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 μmol/L against A549, H460 and HT-29 cell lines respectively, which is comparable to sorafenib.
基金Supported by the National Natural Science Foundation of China(No.21342006) and the Program for the Innovative Research Team of the Ministry of Education of China(No.IRT_14R36).
文摘Based on the molecular docking studies, which were performed to position Erlotinib and the target com- pounds into the active site of the epidermal growth factor receptor(EGFR) to determine the probable binding model, a novel series of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives as the novel potential EGFR kinase inhibitors was designed and synthesized. The antitumor activity of all the target compounds against human pulmonary carcinoma cell line A549 has been screened. Of all the target compounds, 4-[2-(l-piperidyl)carbonylmethoxyl- phenthio]-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine(Tj) demonstrated the most potent antitumor activity. Several of the target compounds exhibited moderate antitumor activity. The preliminary structure-activity relation- ships of some target compounds were summarized.
文摘Curcumfa phaeocaulis Valeton is used in traditional Chinese medicines for the treatment of blood-related disorders such as blood stasis and inflammation.Our previous studies have found that sesquiterpenes were mainly isolated from C.wenyujin and C.phaeocaulis,while diarylheptanoids were the major compounds from C.kwangsiensis.And most of the isolated compounds exhibited remarkable
基金financially supported by the National Natural Science Foundation of China(No.81172958)the Basic Research Subject of Key Laboratory Supported by Educational Commission of Liaoning Province of China(No.LZ2014044)
文摘Macleayine (1), a new natural occurring alkaloid with a unique spiro [furanone-piperidinedione] framework, was isolated from the aerial parts ofMacleaya cordata. Its unusual structure was established by extensive spectroscopic analyses, computer-assisted structure elucidation software (ACD/Structure Elucidator), quantum chemistry calculations and ECD calculation. The result of virtual molecular docking predicted the compound can enhance the effects of insulin, and may be used to treat tvpe II diabetes.