Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly...Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5e35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 mM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.展开更多
[Objectives] To measure and analyze chemical composition of R. crenulata. [Methods] Taking R. crenulata in Lang County of Tibet as the research object,the routine nutritional components,trace elements and amino acid w...[Objectives] To measure and analyze chemical composition of R. crenulata. [Methods] Taking R. crenulata in Lang County of Tibet as the research object,the routine nutritional components,trace elements and amino acid were determined,and the nutrition was evaluated by the international general evaluation method. [Results]The protein content of R. crenulata in Lang County of Tibet was 2. 08%,and fat was 5. 67%. Amino acid was incomplete amino acid,and Ile,Met + Cys were the first limiting amino acids of rhodiola root protein,while Leu was the second limiting amino acid of rhodiola root protein. The final amino acid score was 0. Magnesium,iron,zinc and other mineral elements were abundant,and there was no mercury,cadmium,lead and other heavy metals residues. [Conclusions]The research could provide a powerful basis for industrialization development of rhodiola.展开更多
A novel gallotannin, crenulatin (1), was isolated from the stem of Rhodiola crenulata, and its structure was determined by means of spectral analyses(including ~1H—~1H COSY, ~1H—^(13)C COSY and ~1H—^(13)C COLOC spe...A novel gallotannin, crenulatin (1), was isolated from the stem of Rhodiola crenulata, and its structure was determined by means of spectral analyses(including ~1H—~1H COSY, ~1H—^(13)C COSY and ~1H—^(13)C COLOC spectral measurements)and chemical evidence.展开更多
[Objectives]To study the optimal extraction process of total flavonoids in Rhodiola rosea L.,and further facilitate the development and utilization of Rhodiola rosea L. [Methods]With Rhodiola crenulata as raw material...[Objectives]To study the optimal extraction process of total flavonoids in Rhodiola rosea L.,and further facilitate the development and utilization of Rhodiola rosea L. [Methods]With Rhodiola crenulata as raw material,ethanol as extractant,ultrasonic extraction as the extraction method,the single factor method was first used for preliminary investigation of effect of ethanol volume fraction,solid-liquid ratio,extraction temperature and extraction time on the flavonoids extraction rate,and then the Box-Behnken response surface method was used to optimize the extraction process of total flavonoids in R. crenulata. [Results] The optimal extraction conditions: ethanol concentration of 72%;solid-liquid ratio of 1∶ 43; extraction temperature of 66℃; extraction time of 50 min. Under these conditions,the extraction rate of total flavonoids from R. crenulata was 2. 591%. [Conclusions] The results showed that the method of response surface was reasonable and feasible for the optimization of ultrasonic extraction of total flavonoids from R. crenulata.展开更多
Pulmonary arterial hypertension(PAH)is a devastating pulmonary circulation disease lacking high-efficiency therapeutics.The present study aims to decipher the therapeutic mechanism of Rhodiola crenulata,a well-known t...Pulmonary arterial hypertension(PAH)is a devastating pulmonary circulation disease lacking high-efficiency therapeutics.The present study aims to decipher the therapeutic mechanism of Rhodiola crenulata,a well-known traditional chinese medicine with cardiopulmonary protection capacity,on PAH by exploiting functional lipidomics.The rat model with PAH was successfully established for first,following Rhodiola crenulata water extract(RCE)treatment,then analysis of chemical constituents of RCE was performed,additional morphologic,hemodynamic,echocardiographic measurements were examined,further targeted lipidomics assay was performed to identify differential lipidomes,at last accordingly mechanism assay was done by combining qRT-PCR,Western blot and ELISA.Differential lipidomes were identified and characterized to differentiate the rats with PAH from healthy controls,mostly assigned to acylcarnitines,phosphatidylcholines,sphingomyelin associated with the PAH development.Excitingly,RCE administration reversed high level of decadienyl-L-carnitine by the modulation of metabolic enzyme CPT1A in mRNA and protein level in serum and lung in the rats with PAH.Furthermore,RCE was observed to reduce autophagy,confirmed by significantly inhibited PPARγ,LC3B,ATG7 and upregulated p62,and inactivated LKB1-AMPK signal pathway.Notably,we accurately identified the constituents in RCE,and delineated the therapeutic mechansim that RCE ameliorated PAH through inhibition of fatty acid oxidation and autophagy.Altogether,RCE might be a potential therapeutic medicine with multi-targets characteristics to prevent the progression of PAH.This novel findings pave a critical foundation for the use of RCE in the treatment of PAH.展开更多
基金supported by the National Natural Science Foundation of China(Grant Nos.:82160739,81922070,81973286,and 81973393)Sailing Special Project of Shanghai Rising-Star Program(Grant No.:22YF1441500)+6 种基金Program for Innovative Leading Talents of Qinghai Province(2018&2019)Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine(Grant No.:ZYYCXTD-D-202004)Shanghai Science and Technology Innovation Action Plans(Grant Nos.:20S21901500 and 20S21900900)supported by the Shanghai Science and Technology CommitteeProject of the National Multidisciplinary Innovation Team of Traditional Chinese Medicine supported by the National Administration of Traditional Chinese MedicineKey R&D and Transformation Science and Technology Cooperation Project of Qinghai Province(Grant No.:2019-HZ-819)Basic Public Welfare Research Program of Zhejiang Province(Grant No.:LGF22H280012).
文摘Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5e35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 mM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.
文摘[Objectives] To measure and analyze chemical composition of R. crenulata. [Methods] Taking R. crenulata in Lang County of Tibet as the research object,the routine nutritional components,trace elements and amino acid were determined,and the nutrition was evaluated by the international general evaluation method. [Results]The protein content of R. crenulata in Lang County of Tibet was 2. 08%,and fat was 5. 67%. Amino acid was incomplete amino acid,and Ile,Met + Cys were the first limiting amino acids of rhodiola root protein,while Leu was the second limiting amino acid of rhodiola root protein. The final amino acid score was 0. Magnesium,iron,zinc and other mineral elements were abundant,and there was no mercury,cadmium,lead and other heavy metals residues. [Conclusions]The research could provide a powerful basis for industrialization development of rhodiola.
文摘A novel gallotannin, crenulatin (1), was isolated from the stem of Rhodiola crenulata, and its structure was determined by means of spectral analyses(including ~1H—~1H COSY, ~1H—^(13)C COSY and ~1H—^(13)C COLOC spectral measurements)and chemical evidence.
基金Supported by Tibetan 13th Five-Year Agricultural Product Processing and Product Development Project
文摘[Objectives]To study the optimal extraction process of total flavonoids in Rhodiola rosea L.,and further facilitate the development and utilization of Rhodiola rosea L. [Methods]With Rhodiola crenulata as raw material,ethanol as extractant,ultrasonic extraction as the extraction method,the single factor method was first used for preliminary investigation of effect of ethanol volume fraction,solid-liquid ratio,extraction temperature and extraction time on the flavonoids extraction rate,and then the Box-Behnken response surface method was used to optimize the extraction process of total flavonoids in R. crenulata. [Results] The optimal extraction conditions: ethanol concentration of 72%;solid-liquid ratio of 1∶ 43; extraction temperature of 66℃; extraction time of 50 min. Under these conditions,the extraction rate of total flavonoids from R. crenulata was 2. 591%. [Conclusions] The results showed that the method of response surface was reasonable and feasible for the optimization of ultrasonic extraction of total flavonoids from R. crenulata.
基金the National Natural Science Foundation of China(No.81302764)the Science and Technology Grant for Excellent Talents of Harbin(No.2017RAXXJ-060).
文摘Pulmonary arterial hypertension(PAH)is a devastating pulmonary circulation disease lacking high-efficiency therapeutics.The present study aims to decipher the therapeutic mechanism of Rhodiola crenulata,a well-known traditional chinese medicine with cardiopulmonary protection capacity,on PAH by exploiting functional lipidomics.The rat model with PAH was successfully established for first,following Rhodiola crenulata water extract(RCE)treatment,then analysis of chemical constituents of RCE was performed,additional morphologic,hemodynamic,echocardiographic measurements were examined,further targeted lipidomics assay was performed to identify differential lipidomes,at last accordingly mechanism assay was done by combining qRT-PCR,Western blot and ELISA.Differential lipidomes were identified and characterized to differentiate the rats with PAH from healthy controls,mostly assigned to acylcarnitines,phosphatidylcholines,sphingomyelin associated with the PAH development.Excitingly,RCE administration reversed high level of decadienyl-L-carnitine by the modulation of metabolic enzyme CPT1A in mRNA and protein level in serum and lung in the rats with PAH.Furthermore,RCE was observed to reduce autophagy,confirmed by significantly inhibited PPARγ,LC3B,ATG7 and upregulated p62,and inactivated LKB1-AMPK signal pathway.Notably,we accurately identified the constituents in RCE,and delineated the therapeutic mechansim that RCE ameliorated PAH through inhibition of fatty acid oxidation and autophagy.Altogether,RCE might be a potential therapeutic medicine with multi-targets characteristics to prevent the progression of PAH.This novel findings pave a critical foundation for the use of RCE in the treatment of PAH.
