A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was ac...A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was accomplished by HRESI -MS,1D and 2D NMR methods.展开更多
A new jatrophane-type diterpenoid,7β,14β,15β-triacetoxy-3β-benzoyloxy-9-oxojatropha-5E,11E-diene,named euphornin N was isolated from Euphorbia helioscopia L.The structure and relative stereochemistry of the new co...A new jatrophane-type diterpenoid,7β,14β,15β-triacetoxy-3β-benzoyloxy-9-oxojatropha-5E,11E-diene,named euphornin N was isolated from Euphorbia helioscopia L.The structure and relative stereochemistry of the new compound was elucidated by spectroscopic methods.展开更多
Two new tetrahydronaphthalenes,lα,2α-diol-4α-ethoxy-1,2,3,4-tetrahydronaphthalene(1) and 1a,2a,4β-triol-1,2,3,4- tetrahydronaphthalene(2),were isolated from the stem of Impatiens balsamina L.Their structures were ...Two new tetrahydronaphthalenes,lα,2α-diol-4α-ethoxy-1,2,3,4-tetrahydronaphthalene(1) and 1a,2a,4β-triol-1,2,3,4- tetrahydronaphthalene(2),were isolated from the stem of Impatiens balsamina L.Their structures were elucidated by various spectroscopic methods.展开更多
A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil ag...A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil against human hepatoma cells(HepG2) in vitro.展开更多
A series of novel 7 -azaindirubin(1a-g) and 7-azaindirubin(2a,2c,2e and 2f) derivatives were designed and synthesized.Their structures were characterized by ~1H NMR and MS spectroscopy as well as by elemental analysis...A series of novel 7 -azaindirubin(1a-g) and 7-azaindirubin(2a,2c,2e and 2f) derivatives were designed and synthesized.Their structures were characterized by ~1H NMR and MS spectroscopy as well as by elemental analysis.Their inhibitory properties against CDK2/cylinA were evaluated in vitro.In contrast to indirubin,some of the described azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound 2b had more potent activity.Biological tests also showed that nitrogen atom at 7-position of azaindirubi...展开更多
A microwave-assisted solid phase synthesis for endothelin 1 is presented.Reduced endothelin 1 was synthesized efficiently on Wang resin under microwave irradiation using Fmoc/tBu orthogonal protection strategy.The who...A microwave-assisted solid phase synthesis for endothelin 1 is presented.Reduced endothelin 1 was synthesized efficiently on Wang resin under microwave irradiation using Fmoc/tBu orthogonal protection strategy.The whole peptide was cleaved from the resin and two disulphide bridges were formed under air oxidation at room temperature.The purity and efficiency of synthesizing the peptide is much higher than other methods used before.展开更多
A convenient method for the synthesis of ezetimibe analogs as cholesterol absorption inhibitors was described.The key step in the synthesis was the intramolecular ring formation through Mitsunobu reaction.Furthermore,...A convenient method for the synthesis of ezetimibe analogs as cholesterol absorption inhibitors was described.The key step in the synthesis was the intramolecular ring formation through Mitsunobu reaction.Furthermore,a new series of analogs was designed and synthesized.展开更多
Two new taxane diterpenoids, 2-deacetoxy-7,9-dideacetyltaxinine J (1) and 2-deacetoxytaxinine B (3), were isolated from the barks of Taxus chinensis. Their structures were elucidated by spectroscopic methods.
Some derivatives of neo-clerodane diterpenes ajugacumbin A and B isolated from Ajuga decumbens were prepared by various chemical transformations, and the results achieved in the biological assay as insect antifeedants...Some derivatives of neo-clerodane diterpenes ajugacumbin A and B isolated from Ajuga decumbens were prepared by various chemical transformations, and the results achieved in the biological assay as insect antifeedants of these neo-clerodane derivatives are also reported.展开更多
Two new taraxastane-type triterpenoids,20-taraxastene-3β,12β,16β-triol 1 and 3β-feruloyloxy-20-taraxastene-16β,28-diol 2, were isolated from the fruit of Cicuta virosa L.var latisecta Celak.There structures were ...Two new taraxastane-type triterpenoids,20-taraxastene-3β,12β,16β-triol 1 and 3β-feruloyloxy-20-taraxastene-16β,28-diol 2, were isolated from the fruit of Cicuta virosa L.var latisecta Celak.There structures were elucidated by ESI-MS,1D- and 2D-NMR spectroscopic methods.展开更多
Fatty acid modified glucagon-like peptide-1(7-36) amide was synthesized efficiently on Rink-Amide-MBHA resin by microwave-assisted solid phase method.The method of thermal and controlled microwave irradiation provided...Fatty acid modified glucagon-like peptide-1(7-36) amide was synthesized efficiently on Rink-Amide-MBHA resin by microwave-assisted solid phase method.The method of thermal and controlled microwave irradiation provided impressive enhancements in product yield,selectivity,and reaction rate.The coupling time was dramatically decreased to 6 min,and the desired products were obtained in high yield and purity.展开更多
A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inh...A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.展开更多
A practical synthesis of trans-3,4-diol derivatives of substituted chromans via epoxidation with combined use of mangenese (III) salen complex 3 and hydrogen peroxide has been developed. These diol derivatives are key...A practical synthesis of trans-3,4-diol derivatives of substituted chromans via epoxidation with combined use of mangenese (III) salen complex 3 and hydrogen peroxide has been developed. These diol derivatives are key intermediates for the synthesis of a series of biologically important chroman compounds.展开更多
The metabolism of 7-(4-Chlorbenzyl)-7,8,13,13a-tetrahydroberberine chloride (CTHB), a potential anti-arrhythmia and anti-ischemia drug,was studied in rat bile. A metabolite and unchanged CTHB were found in the bile. C...The metabolism of 7-(4-Chlorbenzyl)-7,8,13,13a-tetrahydroberberine chloride (CTHB), a potential anti-arrhythmia and anti-ischemia drug,was studied in rat bile. A metabolite and unchanged CTHB were found in the bile. Characterization and structural elucidation of the metabolite was achieved by LC/MS and LC/NMR.展开更多
Abstract: The α,β-unsaturated γ-lactones of neo-clerodane diterpenoids teucvidin, teupernin E and ajugacumbin A were selectively transformed into saturated γ-lactones and unsaturated diol derivatives with NaBH4. T...Abstract: The α,β-unsaturated γ-lactones of neo-clerodane diterpenoids teucvidin, teupernin E and ajugacumbin A were selectively transformed into saturated γ-lactones and unsaturated diol derivatives with NaBH4. These transformations are of interest due to their selective reduction as compared with catalytic hydrogenation and LiAlH4 reduction of these diterpenoid compounds.展开更多
The 2024 updates of the Chinese Society of Clinical Oncology(CSCO)Clinical Guidelines for the diagnosis and treatment of colorectal cancer emphasize standardizing cancer treatment in China,highlighting the latest adva...The 2024 updates of the Chinese Society of Clinical Oncology(CSCO)Clinical Guidelines for the diagnosis and treatment of colorectal cancer emphasize standardizing cancer treatment in China,highlighting the latest advancements in evidence-based medicine,healthcare resource access,and precision medicine in oncology.These updates address disparities in epidemiological trends,clinicopathological characteristics,tumor biology,treatment approaches,and drug selection for colorectal cancer patients across diverse regions and backgrounds.Key revisions include adjustments to evidence levels for intensive treatment strategies,updates to regimens for deficient mismatch repair(dMMR)/microsatellite instability-high(MSI-H)patients,proficient mismatch repair(pMMR)/microsatellite stability(MSS)patients who have failed standard therapies,and rectal cancer patients with low recurrence risk.Additionally,recommendations for digital rectal examination and DNA polymerase epsilon(POLE)/DNA polymerase delta 1(POLD1)gene mutation testing have been strengthened.The 2024CSCOGuidelines are based on both Chinese and international clinical research,aswell as expert consensus,ensuring their relevance and applicability in clinical practice,while maintaining a commitment to scientific rigor,impartiality,and timely updates.展开更多
Liquid state methanol and ethanol under different temperatures have been investigated by FT-NIR(Fourier transform nearinfrared) spectroscopy,generalized two-dimensional(2D) correlation spectroscopy,and PCA(principal c...Liquid state methanol and ethanol under different temperatures have been investigated by FT-NIR(Fourier transform nearinfrared) spectroscopy,generalized two-dimensional(2D) correlation spectroscopy,and PCA(principal component analysis) . First,the FT-NIR spectra were measured over a temperature range of 30-64(or 30-71) °C,and then the 2D correlation spectra were computed.Combining near-infrared spectroscopy,generalized 2D correlation spectroscopy,and references,we analyzed the molecular structures(especially the hydrogen bond) of methanol and ethanol,and performed the NIR band assignments. The PCA method was employed to verify the results of the 2D analysis.This study will be helpful to the understanding of these reagents.展开更多
文摘A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was accomplished by HRESI -MS,1D and 2D NMR methods.
文摘A new jatrophane-type diterpenoid,7β,14β,15β-triacetoxy-3β-benzoyloxy-9-oxojatropha-5E,11E-diene,named euphornin N was isolated from Euphorbia helioscopia L.The structure and relative stereochemistry of the new compound was elucidated by spectroscopic methods.
文摘Two new tetrahydronaphthalenes,lα,2α-diol-4α-ethoxy-1,2,3,4-tetrahydronaphthalene(1) and 1a,2a,4β-triol-1,2,3,4- tetrahydronaphthalene(2),were isolated from the stem of Impatiens balsamina L.Their structures were elucidated by various spectroscopic methods.
文摘A series of furoxan-based nitric oxide-releasing matrine derivatives(10a-f) were synthesized.The biological evaluation showed that compounds 10a,10b,10e and 10f had stronger cytotoxic activities than 5-fluorouracil against human hepatoma cells(HepG2) in vitro.
文摘A series of novel 7 -azaindirubin(1a-g) and 7-azaindirubin(2a,2c,2e and 2f) derivatives were designed and synthesized.Their structures were characterized by ~1H NMR and MS spectroscopy as well as by elemental analysis.Their inhibitory properties against CDK2/cylinA were evaluated in vitro.In contrast to indirubin,some of the described azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound 2b had more potent activity.Biological tests also showed that nitrogen atom at 7-position of azaindirubi...
基金supported by the key project of Chinese Ministry of Education(No.109086)
文摘A microwave-assisted solid phase synthesis for endothelin 1 is presented.Reduced endothelin 1 was synthesized efficiently on Wang resin under microwave irradiation using Fmoc/tBu orthogonal protection strategy.The whole peptide was cleaved from the resin and two disulphide bridges were formed under air oxidation at room temperature.The purity and efficiency of synthesizing the peptide is much higher than other methods used before.
文摘A convenient method for the synthesis of ezetimibe analogs as cholesterol absorption inhibitors was described.The key step in the synthesis was the intramolecular ring formation through Mitsunobu reaction.Furthermore,a new series of analogs was designed and synthesized.
文摘Two new taxane diterpenoids, 2-deacetoxy-7,9-dideacetyltaxinine J (1) and 2-deacetoxytaxinine B (3), were isolated from the barks of Taxus chinensis. Their structures were elucidated by spectroscopic methods.
文摘Some derivatives of neo-clerodane diterpenes ajugacumbin A and B isolated from Ajuga decumbens were prepared by various chemical transformations, and the results achieved in the biological assay as insect antifeedants of these neo-clerodane derivatives are also reported.
基金supported by the Public Research Projects in Jiangsu Province of Jiangsu Science and Technology Department(No.BM2006104)
文摘Two new taraxastane-type triterpenoids,20-taraxastene-3β,12β,16β-triol 1 and 3β-feruloyloxy-20-taraxastene-16β,28-diol 2, were isolated from the fruit of Cicuta virosa L.var latisecta Celak.There structures were elucidated by ESI-MS,1D- and 2D-NMR spectroscopic methods.
基金supported by the Key Project of Chinese Ministry of Education(No.109086)the Graduate Students'Scientific Research Program of Jiangsu province.
文摘Fatty acid modified glucagon-like peptide-1(7-36) amide was synthesized efficiently on Rink-Amide-MBHA resin by microwave-assisted solid phase method.The method of thermal and controlled microwave irradiation provided impressive enhancements in product yield,selectivity,and reaction rate.The coupling time was dramatically decreased to 6 min,and the desired products were obtained in high yield and purity.
文摘A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.
文摘A practical synthesis of trans-3,4-diol derivatives of substituted chromans via epoxidation with combined use of mangenese (III) salen complex 3 and hydrogen peroxide has been developed. These diol derivatives are key intermediates for the synthesis of a series of biologically important chroman compounds.
文摘The metabolism of 7-(4-Chlorbenzyl)-7,8,13,13a-tetrahydroberberine chloride (CTHB), a potential anti-arrhythmia and anti-ischemia drug,was studied in rat bile. A metabolite and unchanged CTHB were found in the bile. Characterization and structural elucidation of the metabolite was achieved by LC/MS and LC/NMR.
文摘Abstract: The α,β-unsaturated γ-lactones of neo-clerodane diterpenoids teucvidin, teupernin E and ajugacumbin A were selectively transformed into saturated γ-lactones and unsaturated diol derivatives with NaBH4. These transformations are of interest due to their selective reduction as compared with catalytic hydrogenation and LiAlH4 reduction of these diterpenoid compounds.
文摘The 2024 updates of the Chinese Society of Clinical Oncology(CSCO)Clinical Guidelines for the diagnosis and treatment of colorectal cancer emphasize standardizing cancer treatment in China,highlighting the latest advancements in evidence-based medicine,healthcare resource access,and precision medicine in oncology.These updates address disparities in epidemiological trends,clinicopathological characteristics,tumor biology,treatment approaches,and drug selection for colorectal cancer patients across diverse regions and backgrounds.Key revisions include adjustments to evidence levels for intensive treatment strategies,updates to regimens for deficient mismatch repair(dMMR)/microsatellite instability-high(MSI-H)patients,proficient mismatch repair(pMMR)/microsatellite stability(MSS)patients who have failed standard therapies,and rectal cancer patients with low recurrence risk.Additionally,recommendations for digital rectal examination and DNA polymerase epsilon(POLE)/DNA polymerase delta 1(POLD1)gene mutation testing have been strengthened.The 2024CSCOGuidelines are based on both Chinese and international clinical research,aswell as expert consensus,ensuring their relevance and applicability in clinical practice,while maintaining a commitment to scientific rigor,impartiality,and timely updates.
基金supported by the Medical Scientific Research Foundation of Guangdong Province,China(B2009043)
文摘Liquid state methanol and ethanol under different temperatures have been investigated by FT-NIR(Fourier transform nearinfrared) spectroscopy,generalized two-dimensional(2D) correlation spectroscopy,and PCA(principal component analysis) . First,the FT-NIR spectra were measured over a temperature range of 30-64(or 30-71) °C,and then the 2D correlation spectra were computed.Combining near-infrared spectroscopy,generalized 2D correlation spectroscopy,and references,we analyzed the molecular structures(especially the hydrogen bond) of methanol and ethanol,and performed the NIR band assignments. The PCA method was employed to verify the results of the 2D analysis.This study will be helpful to the understanding of these reagents.
