This paper reports a continous study of the use of short chain peptides as carriers of a potential antitumor agents: 2,6-dimethoxyhydroquinone-3-mercaptoacetic acid (DMQ-MA). In an effort to carry out anti-cancer drug...This paper reports a continous study of the use of short chain peptides as carriers of a potential antitumor agents: 2,6-dimethoxyhydroquinone-3-mercaptoacetic acid (DMQ-MA). In an effort to carry out anti-cancer drug design, we synthesized another two new DMQ-MA-peptide-chlorambucil (CRB) derivatives: DMQ-MA-Lys(CRB)-Arg-OMe, DMQ-MA-Lys(DMQ-MA)Lys(CRB)-Arg-OMe. These peptide-chlorambucil conjugates were synthesized by coupling protected amino acids in solution and the next conjugation was achieved by reacting with pentafluorophenyl ester of DMQ-MA in DMF. The CRB in side chain was coupled by deblocking the lysyl-carbobenzyloxy protecting group Z and then reacting with the pentafluorophenyl ester of chlorambucil (CRB). Further study on cytotoxicity, DNA binding, and sequence specificity of DNA alkylation of these two new conjugates are investigating.展开更多
The present work aimed to develop and evaluate a colloidal system composed of poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) associated with chlorambucil (CHB) and its effects on cancer cells. The nanoparti...The present work aimed to develop and evaluate a colloidal system composed of poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) associated with chlorambucil (CHB) and its effects on cancer cells. The nanoparticles showed %EE (>92%), a mean particle size in the range of 240 to 334 nm and zeta potential of -16.7 to -26.0 mV. In vitro release profile showed a biphasic pattern, with an initial burst for all formulations. The scanning electron microscopy of CHB-nanoparticles showed regular spherical shapes, smooth surface without aggregations. Differential scanning calorimetry thermograms, UV-vis absorption, fluorescence emission and Fourier transform infrared spectroscopy were performed showing the entrapment of the antitumoral in drug delivery system. CHB encapsulated in PLGA nanoparticles decrease the survival rates of the breast cancer cells: 68.9% reduction of cell viability on MCF-7 cell line and 59.7% on NIH3T3. Our results indicated that polymeric nanoparticles produced by classical methods are efficient drug delivery systems for CHB.展开更多
Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of World Journal of Gastrointestinal
We acknowledge our sincere thanks to our reviewers. Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of our World Series Journals. Both the editors ...We acknowledge our sincere thanks to our reviewers. Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of our World Series Journals. Both the editors of the journals and authors of the manuscripts submitted to the journals are grateful to the following reviewers展开更多
Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of World Journal of Gastrointestinal
We acknowledge our sincere thanks to our reviewers.Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of our World Series Journals.Both the editors of ...We acknowledge our sincere thanks to our reviewers.Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of our World Series Journals.Both the editors of the journals and authors of the manuscripts submitted to the journals are grateful to the following reviewers for reviewing the articles(either published or rejected) over the past period of time.展开更多
Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of World Journal of Gastrointestinal Pharmacology and Therapeutics. The editors
Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of World Journal of Gastrointestinal Pharmacology and Therapeutics.The editors and authors of the ar...Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of World Journal of Gastrointestinal Pharmacology and Therapeutics.The editors and authors of the articles submitted to the journal are grateful to the展开更多
目的:比较研究槲皮素与芦丁对离体大鼠胸主动脉环的作用及其可能的途径。方法:采用累积加药法,检测槲皮素和芦丁对去氧肾上腺素(pheny lephrine,PE)预收缩的胸主动脉环张力的影响。结果:槲皮素对离体大鼠内皮完整和去内皮的胸主动脉环...目的:比较研究槲皮素与芦丁对离体大鼠胸主动脉环的作用及其可能的途径。方法:采用累积加药法,检测槲皮素和芦丁对去氧肾上腺素(pheny lephrine,PE)预收缩的胸主动脉环张力的影响。结果:槲皮素对离体大鼠内皮完整和去内皮的胸主动脉环均有浓度依赖性的舒张作用,而芦丁对PE预收缩血管的舒张作用是内皮依赖性的。槲皮素和芦丁对内皮完整的胸主动脉环的最大舒张反应分别为(77.20±6.11)%和(44.28±7.48)%,但两者对内皮完整的胸主动脉环最大舒张的半数有效浓度无明显差异。用一氧化氮合酶抑制剂L-NAM E(0.1 mm o l/L)预处理后,可阻断芦丁诱导的舒张血管作用,但不能阻断槲皮素引起的舒张血管作用;用鸟苷酸环化酶抑制剂亚甲蓝(10μm o l/L)预处理后,两者的血管舒张作用均被阻断。用环氧合酶抑制剂吲哚美辛(10μm o l/L)预处理后可减弱槲皮素诱导的舒张血管作用,但不能阻断芦丁引起的舒张血管作用。结论:槲皮素的舒血管作用强于芦丁,槲皮素可能是通过鸟苷酸环化酶和环氧合酶途径产生非内皮依赖性的血管舒张作用,而芦丁可能是通过NO-鸟苷酸环化酶途径产生内皮依赖性的血管舒张作用。展开更多
Echinacea is a most famous "immune herb" in western countries, and continues to be the best selling herb for many years. For the last five years, our research group has cooperated with Institute of Medicinal...Echinacea is a most famous "immune herb" in western countries, and continues to be the best selling herb for many years. For the last five years, our research group has cooperated with Institute of Medicinal Plants in Huairou District of Beijing, carrying out studies on Echinacea purpurea, which involved botany, cultivation, pharmacognosy, phytochemistry, quality control, pharmacology and toxicology of the species. Two other species introduced from Canada, Echinacea angustifolia and Echinacea pallida, were also included in the taxonomic, cultivated and pharmacognostic studies. The results acquired have opened up the path to introduce Echinacea species into Traditional Chinese Medicine, thus established the possibility of developing more promising drugs from them.展开更多
基金Provincial Natural Foundation of Shanxi Province.
文摘This paper reports a continous study of the use of short chain peptides as carriers of a potential antitumor agents: 2,6-dimethoxyhydroquinone-3-mercaptoacetic acid (DMQ-MA). In an effort to carry out anti-cancer drug design, we synthesized another two new DMQ-MA-peptide-chlorambucil (CRB) derivatives: DMQ-MA-Lys(CRB)-Arg-OMe, DMQ-MA-Lys(DMQ-MA)Lys(CRB)-Arg-OMe. These peptide-chlorambucil conjugates were synthesized by coupling protected amino acids in solution and the next conjugation was achieved by reacting with pentafluorophenyl ester of DMQ-MA in DMF. The CRB in side chain was coupled by deblocking the lysyl-carbobenzyloxy protecting group Z and then reacting with the pentafluorophenyl ester of chlorambucil (CRB). Further study on cytotoxicity, DNA binding, and sequence specificity of DNA alkylation of these two new conjugates are investigating.
文摘The present work aimed to develop and evaluate a colloidal system composed of poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) associated with chlorambucil (CHB) and its effects on cancer cells. The nanoparticles showed %EE (>92%), a mean particle size in the range of 240 to 334 nm and zeta potential of -16.7 to -26.0 mV. In vitro release profile showed a biphasic pattern, with an initial burst for all formulations. The scanning electron microscopy of CHB-nanoparticles showed regular spherical shapes, smooth surface without aggregations. Differential scanning calorimetry thermograms, UV-vis absorption, fluorescence emission and Fourier transform infrared spectroscopy were performed showing the entrapment of the antitumoral in drug delivery system. CHB encapsulated in PLGA nanoparticles decrease the survival rates of the breast cancer cells: 68.9% reduction of cell viability on MCF-7 cell line and 59.7% on NIH3T3. Our results indicated that polymeric nanoparticles produced by classical methods are efficient drug delivery systems for CHB.
文摘Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of World Journal of Gastrointestinal
文摘We acknowledge our sincere thanks to our reviewers. Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of our World Series Journals. Both the editors of the journals and authors of the manuscripts submitted to the journals are grateful to the following reviewers
文摘Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of World Journal of Gastrointestinal
文摘We acknowledge our sincere thanks to our reviewers.Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of our World Series Journals.Both the editors of the journals and authors of the manuscripts submitted to the journals are grateful to the following reviewers for reviewing the articles(either published or rejected) over the past period of time.
文摘Many reviewers have contributed their expertise and time to the peer review, a critical process to ensure the quality of World Journal of Gastrointestinal Pharmacology and Therapeutics. The editors
文摘Many reviewers have contributed their expertise and time to the peer review,a critical process to ensure the quality of World Journal of Gastrointestinal Pharmacology and Therapeutics.The editors and authors of the articles submitted to the journal are grateful to the
文摘目的:比较研究槲皮素与芦丁对离体大鼠胸主动脉环的作用及其可能的途径。方法:采用累积加药法,检测槲皮素和芦丁对去氧肾上腺素(pheny lephrine,PE)预收缩的胸主动脉环张力的影响。结果:槲皮素对离体大鼠内皮完整和去内皮的胸主动脉环均有浓度依赖性的舒张作用,而芦丁对PE预收缩血管的舒张作用是内皮依赖性的。槲皮素和芦丁对内皮完整的胸主动脉环的最大舒张反应分别为(77.20±6.11)%和(44.28±7.48)%,但两者对内皮完整的胸主动脉环最大舒张的半数有效浓度无明显差异。用一氧化氮合酶抑制剂L-NAM E(0.1 mm o l/L)预处理后,可阻断芦丁诱导的舒张血管作用,但不能阻断槲皮素引起的舒张血管作用;用鸟苷酸环化酶抑制剂亚甲蓝(10μm o l/L)预处理后,两者的血管舒张作用均被阻断。用环氧合酶抑制剂吲哚美辛(10μm o l/L)预处理后可减弱槲皮素诱导的舒张血管作用,但不能阻断芦丁引起的舒张血管作用。结论:槲皮素的舒血管作用强于芦丁,槲皮素可能是通过鸟苷酸环化酶和环氧合酶途径产生非内皮依赖性的血管舒张作用,而芦丁可能是通过NO-鸟苷酸环化酶途径产生内皮依赖性的血管舒张作用。
文摘Echinacea is a most famous "immune herb" in western countries, and continues to be the best selling herb for many years. For the last five years, our research group has cooperated with Institute of Medicinal Plants in Huairou District of Beijing, carrying out studies on Echinacea purpurea, which involved botany, cultivation, pharmacognosy, phytochemistry, quality control, pharmacology and toxicology of the species. Two other species introduced from Canada, Echinacea angustifolia and Echinacea pallida, were also included in the taxonomic, cultivated and pharmacognostic studies. The results acquired have opened up the path to introduce Echinacea species into Traditional Chinese Medicine, thus established the possibility of developing more promising drugs from them.
