In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[（1-methyl-ethyl）amino]-2-pyridinyl}-4-{ [5-（4-{5[（1E）-2-（hydroxyphenyl）ethenyl]-1,3-benzenedioyl-carbon...In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[（1-methyl-ethyl）amino]-2-pyridinyl}-4-{ [5-（4-{5[（1E）-2-（hydroxyphenyl）ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino）-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of IH NMR, ~3C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield（46%） than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.展开更多
The dry root and rhizome of Panax ginseng C. A. Mey has garnered much interest owing to its medicinal properties against diabetes and cardiovascular diseases. In this study, an ultra-high performance liquid chromatogr...The dry root and rhizome of Panax ginseng C. A. Mey has garnered much interest owing to its medicinal properties against diabetes and cardiovascular diseases. In this study, an ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS)-based metabolomics approach was used to illustrate the therapeutic mechanisms of ginseng extract on the serum and urinary metabolic profiles in streptozotocin-induced type 1 diabetes mellitus (T1DM) rats. Pharmacological and renal parameters in response to the administration of ginseng were also evaluated. In total, 16 serum endogenous metabolites and 14 urine endogenous metabolites, including pyruvic acid, indoleacetic acid, and phenylacetylglycine, were identified as potential biomarkers for diabetes. Pathway enrichment and network analysis revealed that the biomarkers modulated by ginseng were primarily involved in phenylalanine and pyruvate metabolism, as well as in arginine biosynthesis. Moreover, the levels of several renal injury-related biomarkers in T1DM rats were significantly restored following treatment with ginseng. The administration of the extract helped maintain tissue structure integrity and ameliorated renal injury. The findings suggest that the regulatory effect of ginseng extract on T1DM involves metabolic management of diabetic rats, which subsequently attenuates T1DM-induced early renal dysfunction.展开更多
基金Supported by Scientific and Technological Development Program Foundation of Jilin Province, China(No.20020503-11)
文摘In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[（1-methyl-ethyl）amino]-2-pyridinyl}-4-{ [5-（4-{5[（1E）-2-（hydroxyphenyl）ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino）-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of IH NMR, ~3C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield（46%） than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.
基金supported by the National Key Research and Development Project(No.2017YFC1702105)Education Department of Jilin Province Project(No.JJKH20201033KJ).
文摘The dry root and rhizome of Panax ginseng C. A. Mey has garnered much interest owing to its medicinal properties against diabetes and cardiovascular diseases. In this study, an ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS)-based metabolomics approach was used to illustrate the therapeutic mechanisms of ginseng extract on the serum and urinary metabolic profiles in streptozotocin-induced type 1 diabetes mellitus (T1DM) rats. Pharmacological and renal parameters in response to the administration of ginseng were also evaluated. In total, 16 serum endogenous metabolites and 14 urine endogenous metabolites, including pyruvic acid, indoleacetic acid, and phenylacetylglycine, were identified as potential biomarkers for diabetes. Pathway enrichment and network analysis revealed that the biomarkers modulated by ginseng were primarily involved in phenylalanine and pyruvate metabolism, as well as in arginine biosynthesis. Moreover, the levels of several renal injury-related biomarkers in T1DM rats were significantly restored following treatment with ginseng. The administration of the extract helped maintain tissue structure integrity and ameliorated renal injury. The findings suggest that the regulatory effect of ginseng extract on T1DM involves metabolic management of diabetic rats, which subsequently attenuates T1DM-induced early renal dysfunction.
