OBJECTIVE:To assess the lipid-lowering activity and safety of a dietary supplement containing monacolin Kβ-hydroxy acid form(MKA),Heye(Folium Nelumbinis),and Cangzhu(Rhizoma Atractylodis Lanceae),compared to lifestyl...OBJECTIVE:To assess the lipid-lowering activity and safety of a dietary supplement containing monacolin Kβ-hydroxy acid form(MKA),Heye(Folium Nelumbinis),and Cangzhu(Rhizoma Atractylodis Lanceae),compared to lifestyle modifications.METHODS:Totally 117 subjects with moderate to severe dyslipidemia(according to Chinese guidelines)and low CV risk were randomly assigned into three treatment groups:lifestyle modification(LM),LM plus a low dosage of MKA,LM plus a high dosage of MKA,and treated for 60 d.The primary endpoint was the reduction of low density lipoprotein cholesterol(LDL-C)and total cholesterol(TC).Safeties along with Traditional Chinese Medicine Syndromes were assessed through the study.RESULTS:A low dosage of MKA along with lifestyle modifications caused a significant decrease in LDL-C by 15.6%on average(95%CI,9.6%to 21%)with,a decrease in TC by 15.3%on average(95%CI,9.26%to 21.4%),and a decrease in non-HDL-C by 35.4%(95%CI,25.76%to 41.34%).Weak evidence of a reduction of triglycerides but an increment of HDL-C was observed in patients with severe hyperlipidemia.No severe adverse events occurred during the study.CONCLUSION:Our results confirm the LDL-C and TC lowering properties of MKA is clinically meaningful.It also produces a significant reduction of non-HDL-C,and slightly effects on TG and HDL-C as well.展开更多
In order to clarify the possible relationship between the changes of behavior/personality and metabolic changes of 5 hydroxytryptamine (5 HT) in Antarctic expedition members, plasma tryptophan (Trp) and urinary 5 ...In order to clarify the possible relationship between the changes of behavior/personality and metabolic changes of 5 hydroxytryptamine (5 HT) in Antarctic expedition members, plasma tryptophan (Trp) and urinary 5 hydroxy 3 indoleacetic acid (5 HIAA) were studied for 24 winter over and 19 summer over members of the 8th and 11th CHINARE respectively. Results showed that plasma Trp decreased significantly after residing 1￣3 months at Great Wall Station and did not recover on returning back to Beijing from Antarctica by two weeks travelling. Urinary 5 HIAA increased significantly after residing 6 months at Great Wall Station, and recovered on returning back to Beijing from Antarctica in the winter over members. The decrease of plasma Trp may be related to the decline of brain 5 HT which might play a role in the changes of behavior/personality . Increase of urinary 5 HIAA might reflect metabolic changes of 5 HT as a whole, but cold weather involving in the release response of platelet should be considered. Therefore, supplement of related food rich in Trp or intervention of L Trp might be valuable.展开更多
?-Phenyl－4－aroylfuran－3－carboxylic acids were reduced in aqueous alkaline solutions ofNaBH4 to afford hydroxy acids in excellent yields． Under the catalysis of boron trifluoride etherate，the hydroxy acids were c...?-Phenyl－4－aroylfuran－3－carboxylic acids were reduced in aqueous alkaline solutions ofNaBH4 to afford hydroxy acids in excellent yields． Under the catalysis of boron trifluoride etherate，the hydroxy acids were converted to lactones smoothly．展开更多
When lipopolysaccharide(LPS)enters the cell cytosol,it can bind to mouse caspase-11 and human caspase-4/5 and induce self-cleavage of these molecules[1].After self-cutting,caspase-11 assembles into homodimers and clea...When lipopolysaccharide(LPS)enters the cell cytosol,it can bind to mouse caspase-11 and human caspase-4/5 and induce self-cleavage of these molecules[1].After self-cutting,caspase-11 assembles into homodimers and cleaves gasdermin D(GSDMD)[2,3].With the help of the nuclear orphan receptor NUR77[4],non-canonical inflammasomes can also activate the nucleotide-binding and oligomerization domain(NOD)-like receptor(NLR)family pyrin domain containing 3(NLRP3)inflammasome to secrete inflammatory cytokines interleukin-1b(IL-1b).展开更多
The synthesis of hydroxy fatty acids(HFAs) from renewable oil feedstock by addition of water onto C_C bonds has attracted great attention in recent years. Given that selective asymmetric hydration of non-activated C_C...The synthesis of hydroxy fatty acids(HFAs) from renewable oil feedstock by addition of water onto C_C bonds has attracted great attention in recent years. Given that selective asymmetric hydration of non-activated C_C bonds has been proven difficult to achieve with chemical catalysts, enzymatic catalysis by fatty acid hydratases(FAHs) presents an attractive alternative approach to produce value-added HFAs with high regio-, enantioand stereospecificity, as well as excellent atom economy. Even though FAHs have just been investigated as a potential biocatalyst for a decade, remarkable information about FAHs in different aspects is available;however, a comprehensive review has not been archived. Herein, we summarize the research progresses on biochemical characterization, structural and mechanistic determination, enzyme engineering, as well as biotechnological application of FAHs. The current challenges and opportunities for an efficient utilization of FAHs in organic synthesis and industrial applications are critically discussed.展开更多
Herein, we report the first visible-light photoredox-catalyzed carboxylation of aryl epoxides with CO_(2)to synthesize hydroxy acid derivatives. A variety of valuable β-, γ-, δ-, ε–hydroxy acid derivatives are ob...Herein, we report the first visible-light photoredox-catalyzed carboxylation of aryl epoxides with CO_(2)to synthesize hydroxy acid derivatives. A variety of valuable β-, γ-, δ-, ε–hydroxy acid derivatives are obtained in moderate to high yields under mild conditions. This protocol shows noteworthy functionalgroup compatibility, high chemo-and regioselectivities under transition-metal-free conditions with an inexpensive organo-dye as photosensitizer. Mechanistic studies indicate that the benzylic carbanion is generated as an intermediate via the sequential single electron transfer(SSET) process.展开更多
Proton ligand stability constants of hydroxybenzoic acid containing nitro group （2-Hydroxy-4-nitrobenzoic acid and 3-Hydroxy-4- nitrobenzoic acid） were determined through lrving-Rossoti pH titration technique. The s...Proton ligand stability constants of hydroxybenzoic acid containing nitro group （2-Hydroxy-4-nitrobenzoic acid and 3-Hydroxy-4- nitrobenzoic acid） were determined through lrving-Rossoti pH titration technique. The stability constants of rare earth metal chelates containing 2-Hydroxy-4-nitrobenzoic acid and 3-Hydroxy-4-nitrobenzoic acid as ligands were studied in aqueous medium at different ionic strength （p=0.01, 0.05 and 0.1 mol/L） and temperatures （298, 308 and 318± 0.1 K）. The values of stability constant were evaluated through different computational methods like successive approximation, least square treatment, correction term method, and convergence method. The observed value of thermodynamic parameters （△G°, △H° and △S°） favors the complex formation between metal and ligands. The order of stabifity constant was found to be Pr（III）〈Nd（III）〈Sm（III）〈Tb（III）〈Ho（III）〈Er（III） as reported by Stagg and Powell.展开更多
Objectives: This study aimed to identify the contaminating bacteria in the extract of Garcinia cambogia, which is regularly used as a dietary supplement for addressing obesity in humans. Methods: The Garcinia cambogia...Objectives: This study aimed to identify the contaminating bacteria in the extract of Garcinia cambogia, which is regularly used as a dietary supplement for addressing obesity in humans. Methods: The Garcinia cambogia extract was used and experiments were conducted to isolate the contaminating bacteria and antibiotic susceptibility was tested. The organism was identified using BIOLOG system. Such an extract was used in a placebo-controlled animal study when 6 eight adult male rats weighing between 200 and 220 g were randomly distributed into three groups (n = 3) and in test group 1, a single dose of 100 mg/kg bw of Garcinia cambogia extract was given while in the test group 2, 100 mg Garcinia cambogia extract + 116 mg Picrorhiza kurroa extract were administered through oral gavage. The normal control rats were given distilled water, and the treatment lasted for 30 days. Blood plasma and liver tissues were prepared for biochemical analysis and histology studies. Results: Nearly ~10<sup>3</sup> cfu/g of Bacillus atrophaeus was present in the Garcinia cambogia extract and we demonstrate >99% reduction in the microbial load with tetracycline. Such an extract at a dose of 100 mg/kg, showed weight loss in Wistar rats when administered orally for 1 month with no significant changes in liver histopathology. Picrorhiza kurroa, also known for its hepatoprotective properties, has been administered at a dose of 116 mg/kg along with Garcinia extract at 100 mg/kg orally and found to improve levels of hepatic enzymes as similar to control animals, although not statistically significant. Conclusions: The study revealed that Garcinia cambogia could prevent weight gain in Wistar rats when given orally and the weight gain in Garcinia-treated animals was almost 4 times less (7.31%), as against weight gain of 25.36% seen in vehicle control animals. The antibiotic susceptibility data indicated that the isolated bacterium is resistant to many antibiotics with a strong susceptibility to tetracycline.展开更多
This study investigated the composition of long-chain alkyl diols, triols, sec-alcohols, hydroxyl acids, and other hydroxylated compounds in Azolla imbricata and compared the organic alcohol components of Azolla filic...This study investigated the composition of long-chain alkyl diols, triols, sec-alcohols, hydroxyl acids, and other hydroxylated compounds in Azolla imbricata and compared the organic alcohol components of Azolla filiculoides, Azolla microphylla, and South China Sea （SCS） sediments in order to investigate the possible indication of Azolla being the biological source of diols and triols in SCS sediment. Large amounts of diols, monohydroxy acids, and sec-alcohols with internal hydroxy groups at ω20 were detected in the three types of Azolla. Among these, 1,ω20-diol and ω20-hydroxy acid exhibited strong even-odd predominance distribution, whereas co20-sec-alcohol exhibited strong odd-even predominance distribution. In addition, small amounts of diols, triols, and dihydroxy acids with internal hydroxy groups at 9, 10 or ω9, ω 10 were detected, among which the chain length of C29 was predominate. Compounds having similar structures as those in Azolla reflected a similar biosynthetic pathway： ω20-hydroxy acid exhibiting even-odd predominance distribution is decarboxylated to ω20-sec-alcohol exhibiting odd-even predominance distribution and converted to 1, ω20-diol with even-odd predominance distribution by acyl reduction; ω9,ω10-hydroxy acid is converted to 1,20,21（1, ω9, ω10）-triol by acyl reduction, and then converted to 9,10-diol by hydrogenation and dehydration. The alcohol components in A. imbricata were clearly not the biological source of 1,13/1,14/1,15-C28, 30, 32 diols and 1,3,4-C27.29 triols in the SCS sediment. Certain marine diatoms might be the source of 1,14-C28.30 diol in inshore sediment, but the biological source of diols and triols in the SCS sediment requires further investigation.展开更多
基金Supported by Guangzhou Science and Technology Plan project(No.201710010107)Joint Innovation Specific Project in Key areas from Guangdong Branch Institute of China Academy of Chinese Medical Sciences(No.ZZ0908065)Project of Administration of Traditional Chinese Medicine of Guangdong Province of China(No.201811389)。
文摘OBJECTIVE:To assess the lipid-lowering activity and safety of a dietary supplement containing monacolin Kβ-hydroxy acid form(MKA),Heye(Folium Nelumbinis),and Cangzhu(Rhizoma Atractylodis Lanceae),compared to lifestyle modifications.METHODS:Totally 117 subjects with moderate to severe dyslipidemia(according to Chinese guidelines)and low CV risk were randomly assigned into three treatment groups:lifestyle modification(LM),LM plus a low dosage of MKA,LM plus a high dosage of MKA,and treated for 60 d.The primary endpoint was the reduction of low density lipoprotein cholesterol(LDL-C)and total cholesterol(TC).Safeties along with Traditional Chinese Medicine Syndromes were assessed through the study.RESULTS:A low dosage of MKA along with lifestyle modifications caused a significant decrease in LDL-C by 15.6%on average(95%CI,9.6%to 21%)with,a decrease in TC by 15.3%on average(95%CI,9.26%to 21.4%),and a decrease in non-HDL-C by 35.4%(95%CI,25.76%to 41.34%).Weak evidence of a reduction of triglycerides but an increment of HDL-C was observed in patients with severe hyperlipidemia.No severe adverse events occurred during the study.CONCLUSION:Our results confirm the LDL-C and TC lowering properties of MKA is clinically meaningful.It also produces a significant reduction of non-HDL-C,and slightly effects on TG and HDL-C as well.
文摘In order to clarify the possible relationship between the changes of behavior/personality and metabolic changes of 5 hydroxytryptamine (5 HT) in Antarctic expedition members, plasma tryptophan (Trp) and urinary 5 hydroxy 3 indoleacetic acid (5 HIAA) were studied for 24 winter over and 19 summer over members of the 8th and 11th CHINARE respectively. Results showed that plasma Trp decreased significantly after residing 1￣3 months at Great Wall Station and did not recover on returning back to Beijing from Antarctica by two weeks travelling. Urinary 5 HIAA increased significantly after residing 6 months at Great Wall Station, and recovered on returning back to Beijing from Antarctica in the winter over members. The decrease of plasma Trp may be related to the decline of brain 5 HT which might play a role in the changes of behavior/personality . Increase of urinary 5 HIAA might reflect metabolic changes of 5 HT as a whole, but cold weather involving in the release response of platelet should be considered. Therefore, supplement of related food rich in Trp or intervention of L Trp might be valuable.
文摘?-Phenyl－4－aroylfuran－3－carboxylic acids were reduced in aqueous alkaline solutions ofNaBH4 to afford hydroxy acids in excellent yields． Under the catalysis of boron trifluoride etherate，the hydroxy acids were converted to lactones smoothly．
基金supported by the National Natural Science Foundation of China(grant numbers 92369104,82271790,92169113,and 22174003)Beijing Natural Science Foundation(grant number JG23028)+1 种基金the National Key R&D Program of China(grant numbers 2021YFA1300202,2022YFC2302900,and 2022YFA1304500)Fok Ying Tung Education Foundation to P.X.
文摘When lipopolysaccharide(LPS)enters the cell cytosol,it can bind to mouse caspase-11 and human caspase-4/5 and induce self-cleavage of these molecules[1].After self-cutting,caspase-11 assembles into homodimers and cleaves gasdermin D(GSDMD)[2,3].With the help of the nuclear orphan receptor NUR77[4],non-canonical inflammasomes can also activate the nucleotide-binding and oligomerization domain(NOD)-like receptor(NLR)family pyrin domain containing 3(NLRP3)inflammasome to secrete inflammatory cytokines interleukin-1b(IL-1b).
基金Financial Supports from Novo Nordisk Foundation(NNF16OC0021740)Aarhus Universitets Forskningsfond,AUFFNOVA(AUFF-E-2015-FLS-9-12)。
文摘The synthesis of hydroxy fatty acids(HFAs) from renewable oil feedstock by addition of water onto C_C bonds has attracted great attention in recent years. Given that selective asymmetric hydration of non-activated C_C bonds has been proven difficult to achieve with chemical catalysts, enzymatic catalysis by fatty acid hydratases(FAHs) presents an attractive alternative approach to produce value-added HFAs with high regio-, enantioand stereospecificity, as well as excellent atom economy. Even though FAHs have just been investigated as a potential biocatalyst for a decade, remarkable information about FAHs in different aspects is available;however, a comprehensive review has not been archived. Herein, we summarize the research progresses on biochemical characterization, structural and mechanistic determination, enzyme engineering, as well as biotechnological application of FAHs. The current challenges and opportunities for an efficient utilization of FAHs in organic synthesis and industrial applications are critically discussed.
基金the National Natural Science Foundation of China (Nos. 22225106, 22301193)Fundamental Research Funds from Sichuan University (No. 2020SCUNL102)the Fundamental Research Funds for the Central Universities。
文摘Herein, we report the first visible-light photoredox-catalyzed carboxylation of aryl epoxides with CO_(2)to synthesize hydroxy acid derivatives. A variety of valuable β-, γ-, δ-, ε–hydroxy acid derivatives are obtained in moderate to high yields under mild conditions. This protocol shows noteworthy functionalgroup compatibility, high chemo-and regioselectivities under transition-metal-free conditions with an inexpensive organo-dye as photosensitizer. Mechanistic studies indicate that the benzylic carbanion is generated as an intermediate via the sequential single electron transfer(SSET) process.
文摘Proton ligand stability constants of hydroxybenzoic acid containing nitro group （2-Hydroxy-4-nitrobenzoic acid and 3-Hydroxy-4- nitrobenzoic acid） were determined through lrving-Rossoti pH titration technique. The stability constants of rare earth metal chelates containing 2-Hydroxy-4-nitrobenzoic acid and 3-Hydroxy-4-nitrobenzoic acid as ligands were studied in aqueous medium at different ionic strength （p=0.01, 0.05 and 0.1 mol/L） and temperatures （298, 308 and 318± 0.1 K）. The values of stability constant were evaluated through different computational methods like successive approximation, least square treatment, correction term method, and convergence method. The observed value of thermodynamic parameters （△G°, △H° and △S°） favors the complex formation between metal and ligands. The order of stabifity constant was found to be Pr（III）〈Nd（III）〈Sm（III）〈Tb（III）〈Ho（III）〈Er（III） as reported by Stagg and Powell.
文摘Objectives: This study aimed to identify the contaminating bacteria in the extract of Garcinia cambogia, which is regularly used as a dietary supplement for addressing obesity in humans. Methods: The Garcinia cambogia extract was used and experiments were conducted to isolate the contaminating bacteria and antibiotic susceptibility was tested. The organism was identified using BIOLOG system. Such an extract was used in a placebo-controlled animal study when 6 eight adult male rats weighing between 200 and 220 g were randomly distributed into three groups (n = 3) and in test group 1, a single dose of 100 mg/kg bw of Garcinia cambogia extract was given while in the test group 2, 100 mg Garcinia cambogia extract + 116 mg Picrorhiza kurroa extract were administered through oral gavage. The normal control rats were given distilled water, and the treatment lasted for 30 days. Blood plasma and liver tissues were prepared for biochemical analysis and histology studies. Results: Nearly ~10<sup>3</sup> cfu/g of Bacillus atrophaeus was present in the Garcinia cambogia extract and we demonstrate >99% reduction in the microbial load with tetracycline. Such an extract at a dose of 100 mg/kg, showed weight loss in Wistar rats when administered orally for 1 month with no significant changes in liver histopathology. Picrorhiza kurroa, also known for its hepatoprotective properties, has been administered at a dose of 116 mg/kg along with Garcinia extract at 100 mg/kg orally and found to improve levels of hepatic enzymes as similar to control animals, although not statistically significant. Conclusions: The study revealed that Garcinia cambogia could prevent weight gain in Wistar rats when given orally and the weight gain in Garcinia-treated animals was almost 4 times less (7.31%), as against weight gain of 25.36% seen in vehicle control animals. The antibiotic susceptibility data indicated that the isolated bacterium is resistant to many antibiotics with a strong susceptibility to tetracycline.
基金the National Natural Science Foundation of China(Grant Nos.41303067,41103043&41273022)the Chinese Academy of Sciences Knowledge Innovation Project(Grant No.KGZD-EW-301)the PetroChina-Chinese Academy of Sciences Science and Technology Cooperation Project(Grant No.2015A-4813)
文摘This study investigated the composition of long-chain alkyl diols, triols, sec-alcohols, hydroxyl acids, and other hydroxylated compounds in Azolla imbricata and compared the organic alcohol components of Azolla filiculoides, Azolla microphylla, and South China Sea （SCS） sediments in order to investigate the possible indication of Azolla being the biological source of diols and triols in SCS sediment. Large amounts of diols, monohydroxy acids, and sec-alcohols with internal hydroxy groups at ω20 were detected in the three types of Azolla. Among these, 1,ω20-diol and ω20-hydroxy acid exhibited strong even-odd predominance distribution, whereas co20-sec-alcohol exhibited strong odd-even predominance distribution. In addition, small amounts of diols, triols, and dihydroxy acids with internal hydroxy groups at 9, 10 or ω9, ω 10 were detected, among which the chain length of C29 was predominate. Compounds having similar structures as those in Azolla reflected a similar biosynthetic pathway： ω20-hydroxy acid exhibiting even-odd predominance distribution is decarboxylated to ω20-sec-alcohol exhibiting odd-even predominance distribution and converted to 1, ω20-diol with even-odd predominance distribution by acyl reduction; ω9,ω10-hydroxy acid is converted to 1,20,21（1, ω9, ω10）-triol by acyl reduction, and then converted to 9,10-diol by hydrogenation and dehydration. The alcohol components in A. imbricata were clearly not the biological source of 1,13/1,14/1,15-C28, 30, 32 diols and 1,3,4-C27.29 triols in the SCS sediment. Certain marine diatoms might be the source of 1,14-C28.30 diol in inshore sediment, but the biological source of diols and triols in the SCS sediment requires further investigation.
