Sequences of 479 bp region of the mitochondrial COI gene were applied to detect population genetic diversity and structure ofDendroctonus valens populations. By comparing the genetic diversity between native and invas...Sequences of 479 bp region of the mitochondrial COI gene were applied to detect population genetic diversity and structure ofDendroctonus valens populations. By comparing the genetic diversity between native and invasive populations, it was shown that the genetic diversity of Chinese populations was obviously lower than that of native populations with both indices of haplotype diversity and Nei's genetic diversity, suggesting genetic bottleneck occurred in the invasive process of D. valens, and was then followed by a relatively quick population buildup. According to phylogenetic analyses of haplotypes, we suggested that the origin of the Chinese population was from California, USA. Phylogenetic and network analysis of native populations of D. valens revealed strong genetic structure at two distinct spatial and temporal scales in North America. The main cause resulting in current biogeographic pattern was supposedly due to recycled glacial events. Meanwhile, a cryptic species might exist in the Mexican and Guatemalan populations.展开更多
A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine(1)and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suita...A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine(1)and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suitable substituent at the N’-end of matrinic amide might greatly enhance the potency.Among them,matrinic acid 17 and N’-substituted matrinic amides 18a-d exhibited promising potency with low micromolar EC50 values ranging from 1.03μmol/L to 7.54 μmol/L,and better therapeutic window with SI from 66 to 132.Moreover,compound 17 displayed an excellent PK and safety profile in vivo,demonstrating good drug-like characteristics.Thus,it has been selected for further investigation,with an advantage of decreased chances of inducing drug-resistance mutations.展开更多
基金This work was supported by the National Basic Research Program of China (No. 2002CB 111400) and the National Natural Science Foundation of China (No. 3037027).
文摘Sequences of 479 bp region of the mitochondrial COI gene were applied to detect population genetic diversity and structure ofDendroctonus valens populations. By comparing the genetic diversity between native and invasive populations, it was shown that the genetic diversity of Chinese populations was obviously lower than that of native populations with both indices of haplotype diversity and Nei's genetic diversity, suggesting genetic bottleneck occurred in the invasive process of D. valens, and was then followed by a relatively quick population buildup. According to phylogenetic analyses of haplotypes, we suggested that the origin of the Chinese population was from California, USA. Phylogenetic and network analysis of native populations of D. valens revealed strong genetic structure at two distinct spatial and temporal scales in North America. The main cause resulting in current biogeographic pattern was supposedly due to recycled glacial events. Meanwhile, a cryptic species might exist in the Mexican and Guatemalan populations.
基金supported by the National Natural Science Foundation of China (Nos. 21472246 and 81321004)the Beijing Natural Science Foundation (No. 7152097)National Mega-Project for Innovation Drugs (No. 2012ZX09103101-037)
文摘A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine(1)and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suitable substituent at the N’-end of matrinic amide might greatly enhance the potency.Among them,matrinic acid 17 and N’-substituted matrinic amides 18a-d exhibited promising potency with low micromolar EC50 values ranging from 1.03μmol/L to 7.54 μmol/L,and better therapeutic window with SI from 66 to 132.Moreover,compound 17 displayed an excellent PK and safety profile in vivo,demonstrating good drug-like characteristics.Thus,it has been selected for further investigation,with an advantage of decreased chances of inducing drug-resistance mutations.