Background:Gelsemium elegans Benth(G.elegans)is a poisonous perennial evergreen vine plant that has been applied in livestock production and veterinary clinical practice.Early studies found that the toxicity of G.eleg...Background:Gelsemium elegans Benth(G.elegans)is a poisonous perennial evergreen vine plant that has been applied in livestock production and veterinary clinical practice.Early studies found that the toxicity of G.elegans showed significant gender differences in rats,but the underlying reasons for this difference are still not well understood.Methods:In order to explore whether the gender differences in the toxicity of G.elegans are related to pharmacokinetic differences,based on the previous pharmacokinetic study of multiple components of G.elegans in male rats,this study used HPLC-MS/MS method established in the laboratory to conduct a pharmacokinetic study of multiple alkaloids in the plasma of female rats after a single gavage administration of G.elegans(dose of 0.1 g/kg).Results:Through detection,17 alkaloid components in the plasma of female rats were identified,and the pharmacokinetic parameters of 11 of these alkaloids were calculated.We find that in female rats.The T_(max)values were generally less than 0.5 h,and the T_(1/2)values exceeded 3 h,with the longest reaching up to 32.80 h half elimination time.Additionally,the C_(max)and AUC results indicated that female rats had generally higher absorption and exposure levels for most alkaloids.Conclusion:These results suggest that the reason for the differences in the toxicology of G.elegans may be related to the absorption and exposure of gelsemidine-type alkaloids in animals.展开更多
The modified Hofmann degradation of koumine(1) has proved abortive. The struture and stereochemistry of the main product(3) were deduced by spectral methods and confirmed by X-ray diffration analysis. From the roots o...The modified Hofmann degradation of koumine(1) has proved abortive. The struture and stereochemistry of the main product(3) were deduced by spectral methods and confirmed by X-ray diffration analysis. From the roots of Gelsemium elegans, dihydrokounine was first isolated as a natural product.展开更多
目的探讨胆汁制钩吻总碱(胆钩吻总碱)体外抗肿瘤效果,旨在为钩吻减毒后存效的研究提供科学依据。方法通过CCK-8检测观察胆钩吻总碱对人结肠HCT-116细胞、人神经胶质瘤U87细胞、人肝癌HepG2细胞、人肺癌A549细胞的增殖作用,进一步以结肠...目的探讨胆汁制钩吻总碱(胆钩吻总碱)体外抗肿瘤效果,旨在为钩吻减毒后存效的研究提供科学依据。方法通过CCK-8检测观察胆钩吻总碱对人结肠HCT-116细胞、人神经胶质瘤U87细胞、人肝癌HepG2细胞、人肺癌A549细胞的增殖作用,进一步以结肠癌HCT-116为研究对象,以不同浓度胆钩吻总碱(50、100、200μg·mL-1)干预HCT-116细胞,通过流式细胞技术检测其对细胞周期阻滞的影响;Annexin V FITC/PI流式细胞术检测HCT-116细胞凋亡情况;进一步从蛋白水平检测凋亡相关蛋白表达。结果在钩吻总生物碱IC 50浓度下,胆钩吻总碱对U87、A549、HepG2、HCT-116肿瘤细胞的增殖抑制率均高于钩吻总生物碱组,并且各组之间的差异具有统计学意义(P<0.01)。与空白组相比,不同浓度的胆钩吻总碱处理(50、100、200μg·mL-1)可有效降低HCT-116细胞的集落形成,并将细胞周期阻滞在G 2/M期。胆钩吻总碱还能引发结肠癌HCT-116细胞的晚期凋亡,并对凋亡相关蛋白Bax、Bcl-2、caspase-3起到调控作用。结论胆钩吻总碱可以通过调控结肠癌HCT-116细胞周期和凋亡相关蛋白的表达来抑制其增殖。展开更多
Gelsemium elegans(G.elegans)(2 n=2 x=16)is genus of flowering plants belonging to the Gelsemicaeae family.Here,a high-quality genome assembly using the Oxford Nanopore Technologies(ONT)platform and high-throughput chr...Gelsemium elegans(G.elegans)(2 n=2 x=16)is genus of flowering plants belonging to the Gelsemicaeae family.Here,a high-quality genome assembly using the Oxford Nanopore Technologies(ONT)platform and high-throughput chromosome conformation capture techniques(Hi-C)were used.A total of 56.11 Gb of raw GridION X5 platform ONT reads(6.23 Gb per cell)were generated.After filtering,53.45 Gb of clean reads were obtained,giving 160 x coverage depth.The de novo genome assemblies 335.13 Mb,close to the 338 Mb estimated by k-mer analysis,was generated with contig N50 of 10.23 Mb.The vast majority(99.2%)of the G.elegans assembled sequence was anchored onto 8 pseudo-chromosomes.The genome completeness was then evaluated and 1338 of the 1440 conserved genes(92.9%)could be found in the assembly.Genome annotation revealed that 43.16%of the G.elegans genome is composed of repetitive elements and 23.9%is composed of long terminal repeat elements.We predicted 26,768 protein-coding genes,of which 84.56%were functionally annotated.The genomic sequences of G.elegans could be a valuable source for comparative genomic analysis in the Gelsemicaeae family and will be useful for understanding the phylogenetic relationships of the indole alkaloid metabolism.展开更多
基金supported by the National Natural Science Foundation of China(No.31972737).
文摘Background:Gelsemium elegans Benth(G.elegans)is a poisonous perennial evergreen vine plant that has been applied in livestock production and veterinary clinical practice.Early studies found that the toxicity of G.elegans showed significant gender differences in rats,but the underlying reasons for this difference are still not well understood.Methods:In order to explore whether the gender differences in the toxicity of G.elegans are related to pharmacokinetic differences,based on the previous pharmacokinetic study of multiple components of G.elegans in male rats,this study used HPLC-MS/MS method established in the laboratory to conduct a pharmacokinetic study of multiple alkaloids in the plasma of female rats after a single gavage administration of G.elegans(dose of 0.1 g/kg).Results:Through detection,17 alkaloid components in the plasma of female rats were identified,and the pharmacokinetic parameters of 11 of these alkaloids were calculated.We find that in female rats.The T_(max)values were generally less than 0.5 h,and the T_(1/2)values exceeded 3 h,with the longest reaching up to 32.80 h half elimination time.Additionally,the C_(max)and AUC results indicated that female rats had generally higher absorption and exposure levels for most alkaloids.Conclusion:These results suggest that the reason for the differences in the toxicology of G.elegans may be related to the absorption and exposure of gelsemidine-type alkaloids in animals.
文摘The modified Hofmann degradation of koumine(1) has proved abortive. The struture and stereochemistry of the main product(3) were deduced by spectral methods and confirmed by X-ray diffration analysis. From the roots of Gelsemium elegans, dihydrokounine was first isolated as a natural product.
文摘目的探讨胆汁制钩吻总碱(胆钩吻总碱)体外抗肿瘤效果,旨在为钩吻减毒后存效的研究提供科学依据。方法通过CCK-8检测观察胆钩吻总碱对人结肠HCT-116细胞、人神经胶质瘤U87细胞、人肝癌HepG2细胞、人肺癌A549细胞的增殖作用,进一步以结肠癌HCT-116为研究对象,以不同浓度胆钩吻总碱(50、100、200μg·mL-1)干预HCT-116细胞,通过流式细胞技术检测其对细胞周期阻滞的影响;Annexin V FITC/PI流式细胞术检测HCT-116细胞凋亡情况;进一步从蛋白水平检测凋亡相关蛋白表达。结果在钩吻总生物碱IC 50浓度下,胆钩吻总碱对U87、A549、HepG2、HCT-116肿瘤细胞的增殖抑制率均高于钩吻总生物碱组,并且各组之间的差异具有统计学意义(P<0.01)。与空白组相比,不同浓度的胆钩吻总碱处理(50、100、200μg·mL-1)可有效降低HCT-116细胞的集落形成,并将细胞周期阻滞在G 2/M期。胆钩吻总碱还能引发结肠癌HCT-116细胞的晚期凋亡,并对凋亡相关蛋白Bax、Bcl-2、caspase-3起到调控作用。结论胆钩吻总碱可以通过调控结肠癌HCT-116细胞周期和凋亡相关蛋白的表达来抑制其增殖。
基金financially supported by Hunan Provincial Natural Science Foundation of China(grant 2017JJ1017)National Key R&D Program of China(grant 2017YFD0501403)+1 种基金National Natural Science Foundation of China(grant 31400275)Hunan Provincial Natural Science Foundation of China(2018JJ2172).
文摘Gelsemium elegans(G.elegans)(2 n=2 x=16)is genus of flowering plants belonging to the Gelsemicaeae family.Here,a high-quality genome assembly using the Oxford Nanopore Technologies(ONT)platform and high-throughput chromosome conformation capture techniques(Hi-C)were used.A total of 56.11 Gb of raw GridION X5 platform ONT reads(6.23 Gb per cell)were generated.After filtering,53.45 Gb of clean reads were obtained,giving 160 x coverage depth.The de novo genome assemblies 335.13 Mb,close to the 338 Mb estimated by k-mer analysis,was generated with contig N50 of 10.23 Mb.The vast majority(99.2%)of the G.elegans assembled sequence was anchored onto 8 pseudo-chromosomes.The genome completeness was then evaluated and 1338 of the 1440 conserved genes(92.9%)could be found in the assembly.Genome annotation revealed that 43.16%of the G.elegans genome is composed of repetitive elements and 23.9%is composed of long terminal repeat elements.We predicted 26,768 protein-coding genes,of which 84.56%were functionally annotated.The genomic sequences of G.elegans could be a valuable source for comparative genomic analysis in the Gelsemicaeae family and will be useful for understanding the phylogenetic relationships of the indole alkaloid metabolism.
