Huperzine V, a new Lycopodium alkaloid, was isolated from the whole plant of Huperzia serrata, and the absolute stereochemistry was determined by X-ray crystallographic analysis.
Huperzine W, a novel 14 carbons Lycopodium alkaloid, was isolated from the whole plant of Huperzia serrata, and its stucture was determined by spectroscopic analysis.
Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations w...Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations with the established reference formulation of huperzine A in a fasting, healthy Chinese male population. This was a randomized, single-dose, 3-period, 6-sequence crossover study. The plasma concentrations of huperzine A were determined by liquid chromatography tandem mass spectrometry. Tolerability was assessed based on subject interview, vital sign monitoring, physical examination, and routine blood and urine tests. The mean（SD） pharmacokinetic parameters of the reference drug were Cmax, 1.550（0.528） ng/m L; t1/2, 12.092（1.898） h; AUC0-72 h, 17.550（3.794） ng·h/m L. Those of the test formulation A and test formulation B were Cmax, 1.412（0.467）, 1.521（0.608） ng/m L; t1/2, 12.073（2.068）, 12.271（1.678） h; AUC0-72 h, 15.286（3.434） ng·h/mL, 15.673（3.586） ng·h/m L. The 90% confidence intervals for the AUC0-72 h and Cmax were between 0.80 and 1.25. No adverse events were reported by the subjects or found with results of clinical laboratory test. The test and reference products met the regulatory criteria for bioequivalence in these fasting, healthy Chinese male volunteers. All three formulations appeared to be well tolerated.展开更多
Objective:To study the various processes involved in transcellular transport(TT) of huperzine A alone or in combination with ginkgolide B in Caco-2 and Madin-Darby canine renal(MDCK)cell monolayer.Methods:The transepi...Objective:To study the various processes involved in transcellular transport(TT) of huperzine A alone or in combination with ginkgolide B in Caco-2 and Madin-Darby canine renal(MDCK)cell monolayer.Methods:The transepithelial passage was assayed in the apical-to-basolateral(AP to BL) direction and opposite direction(BL to AP) in both cell lines.The determination of huperzine A and ginkgolide B were performed by high performance liquid chromatography(HPLC).The passage rates of huperzine A and ginkgolide B were calculated.Bi-directional TT(absorption and secretion) were taken in huperzine A and ginkgolide B in Caco-2 and MDCK cell monolayer.Results:TT absorption and secretion kinetics of huperzine A and ginkgolide B across two cells existed at the same time.The passage rates of huperzine A were increased significantly with adding different concentrations of ginkgolide B.Conclusions:The compound preparations of HA in combination with CB for dementia caused by cerebral ischemic have synergistic effects on the pharmacodynamics,and improve the bioavailability through BBB.展开更多
Huperzine A (1), a new Lycopodium alkaloid isolated from Chinese traditional medicine Huperzia Serrata, is a potent acetylcholinesterase inhibitor and a promising drug candidate of treating Alzheimer's disease as ...Huperzine A (1), a new Lycopodium alkaloid isolated from Chinese traditional medicine Huperzia Serrata, is a potent acetylcholinesterase inhibitor and a promising drug candidate of treating Alzheimer's disease as well. Several analogues of huperzine A, compound 8, 10, 14, 15 and 17were prepared and their inhibitory activities of acetylcholinesterase were evaluated展开更多
A new Lycopodium alkaloid huperzine A (1) possesses a potent inhibitory activity of acetylcholinesterase. Six structurally simplified analogues of huperzine A, compound 6, 7, 8, 12, 13 and 15, were prepared and the in...A new Lycopodium alkaloid huperzine A (1) possesses a potent inhibitory activity of acetylcholinesterase. Six structurally simplified analogues of huperzine A, compound 6, 7, 8, 12, 13 and 15, were prepared and the inhibitory activities were evaluated.展开更多
The first total synthesis of(-)-huperzine W(1)has been achieved.Key element of the synthesis is a highly convergent assemblage for the two rings system of target molecule utilizing an efficient Suzuki-Miyaura coupling...The first total synthesis of(-)-huperzine W(1)has been achieved.Key element of the synthesis is a highly convergent assemblage for the two rings system of target molecule utilizing an efficient Suzuki-Miyaura coupling reaction between chiral iodide 2 and 2-allylpyrrolidinone 4.Evaluation of the AchE inhibition of synthetic huperzine W was also carried out.展开更多
This work interrogates why certain real-world events that meet criteria for being considered causative events cannot be expressed using Hupa’s morphological or syntactic causative constructions,but must be encoded us...This work interrogates why certain real-world events that meet criteria for being considered causative events cannot be expressed using Hupa’s morphological or syntactic causative constructions,but must be encoded using one of two periphrastic constructions in which the Causer or cause is not marked as an argument.Based on fieldwork with a native speaker,I probe into these two periphrastic constructions in depth,accounting for their distributions through an appeal to Næss’s(2007)account of semantic transitivity.展开更多
文摘Huperzine V, a new Lycopodium alkaloid, was isolated from the whole plant of Huperzia serrata, and the absolute stereochemistry was determined by X-ray crystallographic analysis.
文摘Huperzine W, a novel 14 carbons Lycopodium alkaloid, was isolated from the whole plant of Huperzia serrata, and its stucture was determined by spectroscopic analysis.
文摘Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations with the established reference formulation of huperzine A in a fasting, healthy Chinese male population. This was a randomized, single-dose, 3-period, 6-sequence crossover study. The plasma concentrations of huperzine A were determined by liquid chromatography tandem mass spectrometry. Tolerability was assessed based on subject interview, vital sign monitoring, physical examination, and routine blood and urine tests. The mean（SD） pharmacokinetic parameters of the reference drug were Cmax, 1.550（0.528） ng/m L; t1/2, 12.092（1.898） h; AUC0-72 h, 17.550（3.794） ng·h/m L. Those of the test formulation A and test formulation B were Cmax, 1.412（0.467）, 1.521（0.608） ng/m L; t1/2, 12.073（2.068）, 12.271（1.678） h; AUC0-72 h, 15.286（3.434） ng·h/mL, 15.673（3.586） ng·h/m L. The 90% confidence intervals for the AUC0-72 h and Cmax were between 0.80 and 1.25. No adverse events were reported by the subjects or found with results of clinical laboratory test. The test and reference products met the regulatory criteria for bioequivalence in these fasting, healthy Chinese male volunteers. All three formulations appeared to be well tolerated.
基金supported by Clinical Special Funds of China University Medical Journals(11321611)
文摘Objective:To study the various processes involved in transcellular transport(TT) of huperzine A alone or in combination with ginkgolide B in Caco-2 and Madin-Darby canine renal(MDCK)cell monolayer.Methods:The transepithelial passage was assayed in the apical-to-basolateral(AP to BL) direction and opposite direction(BL to AP) in both cell lines.The determination of huperzine A and ginkgolide B were performed by high performance liquid chromatography(HPLC).The passage rates of huperzine A and ginkgolide B were calculated.Bi-directional TT(absorption and secretion) were taken in huperzine A and ginkgolide B in Caco-2 and MDCK cell monolayer.Results:TT absorption and secretion kinetics of huperzine A and ginkgolide B across two cells existed at the same time.The passage rates of huperzine A were increased significantly with adding different concentrations of ginkgolide B.Conclusions:The compound preparations of HA in combination with CB for dementia caused by cerebral ischemic have synergistic effects on the pharmacodynamics,and improve the bioavailability through BBB.
文摘Huperzine A (1), a new Lycopodium alkaloid isolated from Chinese traditional medicine Huperzia Serrata, is a potent acetylcholinesterase inhibitor and a promising drug candidate of treating Alzheimer's disease as well. Several analogues of huperzine A, compound 8, 10, 14, 15 and 17were prepared and their inhibitory activities of acetylcholinesterase were evaluated
文摘A new Lycopodium alkaloid huperzine A (1) possesses a potent inhibitory activity of acetylcholinesterase. Six structurally simplified analogues of huperzine A, compound 6, 7, 8, 12, 13 and 15, were prepared and the inhibitory activities were evaluated.
基金the National Natural Science of China(No.20802084,21072200)Programs of“One Hundred Talented People”and“Western Light”Joint Scholar of Chinese Academy of Sciences for financial support.
文摘The first total synthesis of(-)-huperzine W(1)has been achieved.Key element of the synthesis is a highly convergent assemblage for the two rings system of target molecule utilizing an efficient Suzuki-Miyaura coupling reaction between chiral iodide 2 and 2-allylpyrrolidinone 4.Evaluation of the AchE inhibition of synthetic huperzine W was also carried out.
文摘This work interrogates why certain real-world events that meet criteria for being considered causative events cannot be expressed using Hupa’s morphological or syntactic causative constructions,but must be encoded using one of two periphrastic constructions in which the Causer or cause is not marked as an argument.Based on fieldwork with a native speaker,I probe into these two periphrastic constructions in depth,accounting for their distributions through an appeal to Næss’s(2007)account of semantic transitivity.
