25-Hydroxycholesterol, which is an important intermediate for the synthesis of 25-hvdroxyvitamin D_3 and 1α, 25-dihydroxyvitamin D_3, was prepared efficiently from hyodeoxycholic acid in 31% overall yield in seven st...25-Hydroxycholesterol, which is an important intermediate for the synthesis of 25-hvdroxyvitamin D_3 and 1α, 25-dihydroxyvitamin D_3, was prepared efficiently from hyodeoxycholic acid in 31% overall yield in seven steps.展开更多
Calculus bovis is commonly used for the treatment of stroke in traditional Chinese medicine. Hyodeoxycholic acid(HDCA) is a bioactive compound extracted from calculus bovis. When combined with cholic acid, baicalin an...Calculus bovis is commonly used for the treatment of stroke in traditional Chinese medicine. Hyodeoxycholic acid(HDCA) is a bioactive compound extracted from calculus bovis. When combined with cholic acid, baicalin and jas-minoidin, HDCA prevents hypoxia-reoxygenation-induced brain injury by suppressing endoplasmic reticulum stress-mediated apoptotic signaling. However, the effects of HDCA in ischemic stroke injury have not yet been studied. Neurovascular unit(NVU) dysfunction occurs in ischemic stroke. Therefore, in this study, we investigated the effects of HDCA on the NVU under ischemic conditions in vitro. We co-cultured primary brain microvascular endothelial cells, neurons and astrocytes using a transwell chamber co-culture system. The NVU was pre-treated with 10.16 or 2.54 μg/mL HDCA for 24 hours before exposure to oxygen-glucose deprivation for 1 hour. The cell counting kit-8 assay was used to detect cell activity. Flow cytometry and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling were used to assess apoptosis. Enzyme-linked immunosorbent assay was used to measure the expression levels of inflammatory cytokines, including interleukin-1β, interleukin-6 and tumor necrosis factor-α, and neurotrophic factors, including brain-derived neurotrophic factor and glial cell line-derived neurotrophic factor. Oxidative stress-related factors, such as superoxide dismutase, nitric oxide, malondialdehyde and γ-glutamyltransferase, were measured using kits. Pretreatment with HDCA significantly decreased blood-brain barrier permeability and neuronal apoptosis, significantly increased transendothelial electrical resistance and γ-glutamyltransferase activity, attenuated oxidative stress damage and the release of inflammatory cytokines, and increased brain-derived neurotrophic factor and glial cell line-derived neurotrophic factor expression. Our findings suggest that HDCA maintains NVU morphological integrity and function by modulating inflammation, oxidation stress, apoptosis, and the expression of neurotrophic factors. Therefore, HDCA may have therapeutic potential in the clinical management of ischemic stroke. This study was approved by the Ethics Committee of Experimental Animals of Beijing University of Chinese Medicine(approval No. BUCM-3-2016040201-2003) in April 2016.展开更多
An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed.Its main advantages are short reaction times,good ...An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed.Its main advantages are short reaction times,good conversions and the environmentally friendly nature of the process.The preliminary results indicate that some of these compounds possess inhibitory effects against E.coli.展开更多
The purpose of this research was to investigate how different bile acids impact lipid metabolism and carcass characteristics in finishing pigs,along with the potential mechanisms involved.Twenty-one finishing pigs(Dur...The purpose of this research was to investigate how different bile acids impact lipid metabolism and carcass characteristics in finishing pigs,along with the potential mechanisms involved.Twenty-one finishing pigs(Duroc×Landrace×Yorkshire[DLY];average BW=144.38±8.92 kg)were assigned to three dietary treatments,with each treatment containing seven replicates,each consisting of one pig.The three dietary treatments included:a basic diet,a basic diet supplemented with 500 mg/kg of hyodeoxycholic acid(HDCA),and a basic diet supplemented with 500 mg/kg of lithocholic acid(LCA).The trial lasted for 28 d.Hyodeoxycholic acid was used in the in vitro experiments and added to mature 3T3-L1 adipocytes for 4 d to elucidate the mechanism by which bile acids regulate lipid metabolism.The results suggested that HDCA tended to decrease backfat thickness in finishing pigs(P=0.094)and reduced the size of lipid droplets in 3T3-L1 adipocytes(P=0.012),whereas LCA increased backfat thickness(P=0.016)and induced larger lipid droplets in the abdominal adipose tissue(P=0.003).Furthermore,HDCA enhanced the expression of Takeda G-protein-coupled receptor 5 protein and hormone-sensitive lipase(HSL)gene in backfat of pigs(P<0.05)and increased the protein expression of phosphorylated HSL(p-HSL)in vitro(P=0.093).Compared to HDCA,LCA addition increased the gene and protein expression of peroxisome proliferator activated receptor gamma in backfat of pigs(P<0.05)and enhanced the expression of hepatic genes sterol regulatory element-binding protein-1c and fatty acid synthase(P<0.05).In conclusion,HDCA enhanced lipolysis and partially decreased backfat thickness in finishing pigs,while LCA promoted lipid synthesis and increased backfat thickness of pigs.The variations in the effects of various bile acids on bile acid receptors could explain these functional differences.展开更多
文摘25-Hydroxycholesterol, which is an important intermediate for the synthesis of 25-hvdroxyvitamin D_3 and 1α, 25-dihydroxyvitamin D_3, was prepared efficiently from hyodeoxycholic acid in 31% overall yield in seven steps.
基金supported by the National Natural Science Foundation of China,No.81430102(to QGW)
文摘Calculus bovis is commonly used for the treatment of stroke in traditional Chinese medicine. Hyodeoxycholic acid(HDCA) is a bioactive compound extracted from calculus bovis. When combined with cholic acid, baicalin and jas-minoidin, HDCA prevents hypoxia-reoxygenation-induced brain injury by suppressing endoplasmic reticulum stress-mediated apoptotic signaling. However, the effects of HDCA in ischemic stroke injury have not yet been studied. Neurovascular unit(NVU) dysfunction occurs in ischemic stroke. Therefore, in this study, we investigated the effects of HDCA on the NVU under ischemic conditions in vitro. We co-cultured primary brain microvascular endothelial cells, neurons and astrocytes using a transwell chamber co-culture system. The NVU was pre-treated with 10.16 or 2.54 μg/mL HDCA for 24 hours before exposure to oxygen-glucose deprivation for 1 hour. The cell counting kit-8 assay was used to detect cell activity. Flow cytometry and terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling were used to assess apoptosis. Enzyme-linked immunosorbent assay was used to measure the expression levels of inflammatory cytokines, including interleukin-1β, interleukin-6 and tumor necrosis factor-α, and neurotrophic factors, including brain-derived neurotrophic factor and glial cell line-derived neurotrophic factor. Oxidative stress-related factors, such as superoxide dismutase, nitric oxide, malondialdehyde and γ-glutamyltransferase, were measured using kits. Pretreatment with HDCA significantly decreased blood-brain barrier permeability and neuronal apoptosis, significantly increased transendothelial electrical resistance and γ-glutamyltransferase activity, attenuated oxidative stress damage and the release of inflammatory cytokines, and increased brain-derived neurotrophic factor and glial cell line-derived neurotrophic factor expression. Our findings suggest that HDCA maintains NVU morphological integrity and function by modulating inflammation, oxidation stress, apoptosis, and the expression of neurotrophic factors. Therefore, HDCA may have therapeutic potential in the clinical management of ischemic stroke. This study was approved by the Ethics Committee of Experimental Animals of Beijing University of Chinese Medicine(approval No. BUCM-3-2016040201-2003) in April 2016.
基金the Natural Science Foundation of the State Ethnic Affairs Commission of China(No.09XN08) for the financial support
文摘An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed.Its main advantages are short reaction times,good conversions and the environmentally friendly nature of the process.The preliminary results indicate that some of these compounds possess inhibitory effects against E.coli.
基金Funding for this research was provided by the National Natural Science Foundation of China under grant number 31730091.
文摘The purpose of this research was to investigate how different bile acids impact lipid metabolism and carcass characteristics in finishing pigs,along with the potential mechanisms involved.Twenty-one finishing pigs(Duroc×Landrace×Yorkshire[DLY];average BW=144.38±8.92 kg)were assigned to three dietary treatments,with each treatment containing seven replicates,each consisting of one pig.The three dietary treatments included:a basic diet,a basic diet supplemented with 500 mg/kg of hyodeoxycholic acid(HDCA),and a basic diet supplemented with 500 mg/kg of lithocholic acid(LCA).The trial lasted for 28 d.Hyodeoxycholic acid was used in the in vitro experiments and added to mature 3T3-L1 adipocytes for 4 d to elucidate the mechanism by which bile acids regulate lipid metabolism.The results suggested that HDCA tended to decrease backfat thickness in finishing pigs(P=0.094)and reduced the size of lipid droplets in 3T3-L1 adipocytes(P=0.012),whereas LCA increased backfat thickness(P=0.016)and induced larger lipid droplets in the abdominal adipose tissue(P=0.003).Furthermore,HDCA enhanced the expression of Takeda G-protein-coupled receptor 5 protein and hormone-sensitive lipase(HSL)gene in backfat of pigs(P<0.05)and increased the protein expression of phosphorylated HSL(p-HSL)in vitro(P=0.093).Compared to HDCA,LCA addition increased the gene and protein expression of peroxisome proliferator activated receptor gamma in backfat of pigs(P<0.05)and enhanced the expression of hepatic genes sterol regulatory element-binding protein-1c and fatty acid synthase(P<0.05).In conclusion,HDCA enhanced lipolysis and partially decreased backfat thickness in finishing pigs,while LCA promoted lipid synthesis and increased backfat thickness of pigs.The variations in the effects of various bile acids on bile acid receptors could explain these functional differences.
