Rubuphenol (1), a new polyphenolic compound, was isolated together with the known ellagic acid (2) as new cell cycle inhibitors from Rubus aleaefolius Poir. through a bioassay-guided separation procedure and the struc...Rubuphenol (1), a new polyphenolic compound, was isolated together with the known ellagic acid (2) as new cell cycle inhibitors from Rubus aleaefolius Poir. through a bioassay-guided separation procedure and the structure of 1 was elucidated by spectroscopic method. Compounds 1 and 2 inhibited the cell cycle of tsFT210 cells at the G0/G1 phase respectively with the MIC values of 14.6 mM and 10.3 mM.展开更多
Actinolactomycin 1, a new 2-oxonanonoidal antitumor antibiotic, was isolated from the fermentation broth of Streptomyces flavoretus 18522 through a bioassay-guided separation procedure. The structure of 1 was determ...Actinolactomycin 1, a new 2-oxonanonoidal antitumor antibiotic, was isolated from the fermentation broth of Streptomyces flavoretus 18522 through a bioassay-guided separation procedure. The structure of 1 was determined as 4,7-dihydroxy-3,9-dimethyl-2-oxonanone by the spectroscopic methods. Compound 1 inhibited the proliferation of A2780, K562, HCT-15, A549 and HeLa cells with the IC50 values of 1.4 ± 0.4 μmol/L, 8.4 ± 4.7 μmol/L, 9.4 ± 2.2 μmol/L, 15.4 ± 5.6 μmol/L and 13.7 ± 2.0 μmol/L, respectively. Flow cytometric analysis indicated that 1 could inhibit the cell cycle of tsFT210, A2780 and K562 cells mainly at the G0/G1 phase and could also induce apoptosis in K562 cells.展开更多
Pterocarine (1), a new diarylheptanoidal compound, was isolated from Pterocaryatonkinesis (Franch.) Dode. together with a known diarylheptanoid, myricatomentogenin (2), througha bioassay-guided fractionation procedure...Pterocarine (1), a new diarylheptanoidal compound, was isolated from Pterocaryatonkinesis (Franch.) Dode. together with a known diarylheptanoid, myricatomentogenin (2), througha bioassay-guided fractionation procedure. The structure of 1 was elucidated as (+)-3', 4''-epoxy-1-(4'-hydroxyphenyl)-7-(3''-hydroxyphenyl)-heptane-3-one by the spectroscopic methods.Pterocarine (1) inhibited the proliferation of tsFT210, HCT-15 and K562 cells with the inhibitionrates of 20.2±2.4, 23.8±2.4 and 50.5±1.2% at 100 μg/mL, respectively. Flow cytometric analysisindicated that 1 could inhibit the cell cycle of tsFT210, HCT-15 and K562 cells at the G0/G1 phaseand could also induce apoptosis in HCT-15 (19%) and K562 (11%) cells.展开更多
Dysregulation of the cell cycle is a molecular hallmark of cancer,which leads to uncontrolled proliferation and self-renewal of neoplastic cells.To maintain this phenotype,cells acquire multiple molecular alterations ...Dysregulation of the cell cycle is a molecular hallmark of cancer,which leads to uncontrolled proliferation and self-renewal of neoplastic cells.To maintain this phenotype,cells acquire multiple molecular alterations and bypass several cellular checkpoints that are involved in the prevention of genomic instability and uncontrolled cell proliferation.Therefore,targeting cell cycle regulators could prove to be a promising anti-cancer approach.Recent advancements in the understanding of cancer cell susceptibilities have revealed a therapeutic opportunity to selectively target the cell cycle in malignant cells.This review highlights major cell cycle dysregulation in cancerous cells and the latest developments on anti-cancer agents that target cell cycle factors which are either in clinical practice or in clinical trials at present.In light of increasing drug resistance in cancer patients,the article also discusses mechanistic insights for the exploration of probable therapies that could be used to target these cell cycle factors.Additionally,it outlines the future research necessary to develop new therapies and optimize existing ones to achieve maximum efficacy.Thus,this article aims to provide a comprehensive understanding of the advancements in cancer therapies targeting dysregulated cell cycle factors.展开更多
The present study aimed at identifying cell cycle inhibitors from the fermentation broth of Streptomyces pseudoverticillus YN17707. Activity-guided isolation was performed on ts FT210 cells. Compounds were isolated th...The present study aimed at identifying cell cycle inhibitors from the fermentation broth of Streptomyces pseudoverticillus YN17707. Activity-guided isolation was performed on ts FT210 cells. Compounds were isolated through various chromatographic methods and elucidated by spectroscopic analyses. Flow cytometry was used to evaluate the cell cycle inhibitory activities of the fractions and compounds. Two compounds were obtained and identified as pteridic acid hydrate(1) and pteridic acid C(2), which arrested the ts FT210 cells at the G0/G1 phase with the MIC values being 32.8 and 68.9 μmol·L-1, respectively. These results provide a basis for future development of Compounds 1 and 2 as novel cell cycle inhibitors for cancer therapy.展开更多
文摘Rubuphenol (1), a new polyphenolic compound, was isolated together with the known ellagic acid (2) as new cell cycle inhibitors from Rubus aleaefolius Poir. through a bioassay-guided separation procedure and the structure of 1 was elucidated by spectroscopic method. Compounds 1 and 2 inhibited the cell cycle of tsFT210 cells at the G0/G1 phase respectively with the MIC values of 14.6 mM and 10.3 mM.
文摘Actinolactomycin 1, a new 2-oxonanonoidal antitumor antibiotic, was isolated from the fermentation broth of Streptomyces flavoretus 18522 through a bioassay-guided separation procedure. The structure of 1 was determined as 4,7-dihydroxy-3,9-dimethyl-2-oxonanone by the spectroscopic methods. Compound 1 inhibited the proliferation of A2780, K562, HCT-15, A549 and HeLa cells with the IC50 values of 1.4 ± 0.4 μmol/L, 8.4 ± 4.7 μmol/L, 9.4 ± 2.2 μmol/L, 15.4 ± 5.6 μmol/L and 13.7 ± 2.0 μmol/L, respectively. Flow cytometric analysis indicated that 1 could inhibit the cell cycle of tsFT210, A2780 and K562 cells mainly at the G0/G1 phase and could also induce apoptosis in K562 cells.
基金This work was supported by the Fund from the National Natural Science Foundation of China(C.-B.CUI,No.39825126)the Fund for the 973-project from Ministry of Science and Technology(C.-B.CUI,No.1998051113),Chinathe Fund for Cheung Kong Scholar(C.B.CUI)from Cheung Kong Scholars Program,Ministry of Education of China.
文摘Pterocarine (1), a new diarylheptanoidal compound, was isolated from Pterocaryatonkinesis (Franch.) Dode. together with a known diarylheptanoid, myricatomentogenin (2), througha bioassay-guided fractionation procedure. The structure of 1 was elucidated as (+)-3', 4''-epoxy-1-(4'-hydroxyphenyl)-7-(3''-hydroxyphenyl)-heptane-3-one by the spectroscopic methods.Pterocarine (1) inhibited the proliferation of tsFT210, HCT-15 and K562 cells with the inhibitionrates of 20.2±2.4, 23.8±2.4 and 50.5±1.2% at 100 μg/mL, respectively. Flow cytometric analysisindicated that 1 could inhibit the cell cycle of tsFT210, HCT-15 and K562 cells at the G0/G1 phaseand could also induce apoptosis in HCT-15 (19%) and K562 (11%) cells.
文摘Dysregulation of the cell cycle is a molecular hallmark of cancer,which leads to uncontrolled proliferation and self-renewal of neoplastic cells.To maintain this phenotype,cells acquire multiple molecular alterations and bypass several cellular checkpoints that are involved in the prevention of genomic instability and uncontrolled cell proliferation.Therefore,targeting cell cycle regulators could prove to be a promising anti-cancer approach.Recent advancements in the understanding of cancer cell susceptibilities have revealed a therapeutic opportunity to selectively target the cell cycle in malignant cells.This review highlights major cell cycle dysregulation in cancerous cells and the latest developments on anti-cancer agents that target cell cycle factors which are either in clinical practice or in clinical trials at present.In light of increasing drug resistance in cancer patients,the article also discusses mechanistic insights for the exploration of probable therapies that could be used to target these cell cycle factors.Additionally,it outlines the future research necessary to develop new therapies and optimize existing ones to achieve maximum efficacy.Thus,this article aims to provide a comprehensive understanding of the advancements in cancer therapies targeting dysregulated cell cycle factors.
基金supported by the National Natural Science Foundation of China(No.30472079)National Basic Research Program of China(No.2006CB504100)
文摘The present study aimed at identifying cell cycle inhibitors from the fermentation broth of Streptomyces pseudoverticillus YN17707. Activity-guided isolation was performed on ts FT210 cells. Compounds were isolated through various chromatographic methods and elucidated by spectroscopic analyses. Flow cytometry was used to evaluate the cell cycle inhibitory activities of the fractions and compounds. Two compounds were obtained and identified as pteridic acid hydrate(1) and pteridic acid C(2), which arrested the ts FT210 cells at the G0/G1 phase with the MIC values being 32.8 and 68.9 μmol·L-1, respectively. These results provide a basis for future development of Compounds 1 and 2 as novel cell cycle inhibitors for cancer therapy.