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 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.
t Three new lycodine-type Lycopodium alkaloids,namely 1-methyllycodine(1),8a-hydroxy-15,16-dehydro-desN-methyl-a-obscurine(2),N-methyl-16-hydroxyhuperzine B(3),and one new natural lycodine-type Lycopodium alkaloid,N-...t Three new lycodine-type Lycopodium alkaloids,namely 1-methyllycodine(1),8a-hydroxy-15,16-dehydro-desN-methyl-a-obscurine(2),N-methyl-16-hydroxyhuperzine B(3),and one new natural lycodine-type Lycopodium alkaloid,N-methylhuperzine A(4),along with 11 known analogues(5–15),were isolated from the whole plants of club moss Huperzia serrata.The structures of 1–4 were elucidated on the basis of NMR spectroscopic and mass spectrometry data.Among them,compound 1 was the first lycodine-type alkaloid possessing a methyl group at C-1.In addition,the structure of 5 was confirmed by the single-crystal X-ray crystallography data and its^(13)C NMR was reported for the first time in current study.Compounds 1–5 were tested their BACE1 inhibitory activity.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
Through dual quadratic rotary regression orthogonal design experiment with four factors,the effects of microwave power,microwave pretreatment time,the amount of ethanol and ethanol concentration on the yield of total ...Through dual quadratic rotary regression orthogonal design experiment with four factors,the effects of microwave power,microwave pretreatment time,the amount of ethanol and ethanol concentration on the yield of total alkaloid were investigated,and a mathematical model describing the relationship between the yield of total alkaloid and influence parameters was developed.Results showed that the regression equation is significant.The optimum extracting conditions were obtained that the microwave power was 500W,pretreatment time was 95s,the volume of ethanol was 9.8mL and ethanol concentration was 0.66,under which the yield of total alkaloid was 690.4μg/g.展开更多
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 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.
基金the NSFC-Joint Foundation of Yunnan Province(No.U1502223)the National Natural Science Foundation of China(No.21402212)+1 种基金the Science and Technology Program of Yunnan province(No 2015FB173)the CAS"Light of West China"Program and Youth Innovation Promotion Association CAS(X.D.Wu).
文摘t Three new lycodine-type Lycopodium alkaloids,namely 1-methyllycodine(1),8a-hydroxy-15,16-dehydro-desN-methyl-a-obscurine(2),N-methyl-16-hydroxyhuperzine B(3),and one new natural lycodine-type Lycopodium alkaloid,N-methylhuperzine A(4),along with 11 known analogues(5–15),were isolated from the whole plants of club moss Huperzia serrata.The structures of 1–4 were elucidated on the basis of NMR spectroscopic and mass spectrometry data.Among them,compound 1 was the first lycodine-type alkaloid possessing a methyl group at C-1.In addition,the structure of 5 was confirmed by the single-crystal X-ray crystallography data and its^(13)C NMR was reported for the first time in current study.Compounds 1–5 were tested their BACE1 inhibitory activity.
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Through dual quadratic rotary regression orthogonal design experiment with four factors,the effects of microwave power,microwave pretreatment time,the amount of ethanol and ethanol concentration on the yield of total alkaloid were investigated,and a mathematical model describing the relationship between the yield of total alkaloid and influence parameters was developed.Results showed that the regression equation is significant.The optimum extracting conditions were obtained that the microwave power was 500W,pretreatment time was 95s,the volume of ethanol was 9.8mL and ethanol concentration was 0.66,under which the yield of total alkaloid was 690.4μg/g.