Saikosaponins are the major pharmacologically active components in Bupleurum genus and exhibit significant application potential in multiple fields such as immune regulation and anti-tumor activity.To elucidate the bi...Saikosaponins are the major pharmacologically active components in Bupleurum genus and exhibit significant application potential in multiple fields such as immune regulation and anti-tumor activity.To elucidate the biosynthetic pathway of saikosaponins,we identified two cytochrome P450 monooxygenases,CYP716A41 and CYP716Y4,in Bupleurum chinense.These enzymes catalyze the C-28 oxidation and C-16 hydroxylation of oleanane-type triterpene skeletons,respectively.The catalytic efficiency of CYP716A41 from a southern B.chinense variety was significantly higher than that from a northern variety.Molecular docking and mutagenesis experiments revealed that amino acid residues at sites 9 and 35 may contribute to this difference in catalytic efficiency.Additionally,under cold stress,the expression levels of both CYP450 genes and the saikosaponin contents in the leaves of southern varieties were significantly higher compared to those in northern varieties.The variation in the catalytic efficiency of CYP716A41 and the differential expression of the two CYP450 genes under cold stress during winter are associated with the differences in saikosaponin biosynthesis in the leaves of southern and northern B.chinense varieties.This is consistent with the distinct medicinal usage practices observed between southern and northern China.展开更多
The present study aimed to investigate the effects of polysaccharides extracted from Bupleurum chinense DC(BCPs) on macrophage functions. In the in vivo experiment, 1 m L of 5% sodium thioglycollate was injected into ...The present study aimed to investigate the effects of polysaccharides extracted from Bupleurum chinense DC(BCPs) on macrophage functions. In the in vivo experiment, 1 m L of 5% sodium thioglycollate was injected into the abdomen of the mice on Day 0 and macrophages were harvested on Day 4. The macrophages were cultured in plates and treated with different concentrations of BCPs and stimulus. Effects of BCPs on macrophage functions were assessed by chemotaxis assay, phagocytosis assay and Enzyme-Linked Immunosorbent Assay(ELISA). Our results showed the enhanced chemotaxis, phagocytosis and secretion of nitric oxide(NO) and inflammatory cytokines by macrophages when treated with BCPs. However, when chemotaxis and phagocytosis were up-regulated by complement components or opsonized particles, BCPs inhibited these effects. Also, the NO production induced by lipopolysaccharides(LPS) was suppressed by BCPs mildly. Moreover, BCPs had an inhibitory effect on the [Ca^(2+)]i elevation of macrophages. These results suggested that BCPs exerted modulatory effects on macrophage functions, which may contribute to developing novel approaches to treating inflammatory diseases.展开更多
A quantitative evaluation method for the quality consistency of Bupleurum chinense DC. was developed by combining multiwavelength fusion fingerprint with chemometric methods. The fingerprint information of Bupleurum a...A quantitative evaluation method for the quality consistency of Bupleurum chinense DC. was developed by combining multiwavelength fusion fingerprint with chemometric methods. The fingerprint information of Bupleurum at five wavelengths (210, 254, 265, 280 and 320 nm) collected by HPLC-DAD instrument was fused to overall control its quality. The fusion fingerprints and four components (saikosaponin a, saikosaponin d, rutin, quercitrin) were studied by systematic quantitative fingerprint method and principal component analysis, respectively. Besides, fingerprint-efficacy relationship was constructed in vitro using partial least-squares model. In conclusion, all work can serve as a valid reference for the quality control of Bupleurum .展开更多
A new saikosaponin was isolated from Bupleurum chinense DC., and its structure was identified as 3β,16α,23,28,30_pentahydroxy_olean_11,13(18)_dien_3_O_β_D_glucopyranosyl(1→6)_[α_L_rhamnopyranosyl (1→4)]_β_D...A new saikosaponin was isolated from Bupleurum chinense DC., and its structure was identified as 3β,16α,23,28,30_pentahydroxy_olean_11,13(18)_dien_3_O_β_D_glucopyranosyl(1→6)_[α_L_rhamnopyranosyl (1→4)]_β_D_glucopyranoside on the basis of chemical and spectral evidence, named as saikosaponin q_1. In addition, two known saikosaponins, 3″_O_acetyl_saikosaponin d and 3″_O_acetyl_saikosaponin b 2, were also isolated and identified from this plant for the first time.展开更多
5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was...5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2 C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2 C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d(1), was determined by extensive spectroscopic analyses(HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2 C receptor agonistic activity. Saikosaponin a(3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2 C receptor with an EC50 value of 21.08 ± 0.33 μmol×L^(–1) in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg×kg^(–1) in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.展开更多
A new chromone glycoside,saikochromoside A(1),was isolated from the roots of Bupleurum chinense DC.Its structure was determined on the bases of chemical and spectral analyses.
Bupleurum chinense is a genuine medicinal material in Shanxi Province,and planting B.chinense is one of the main sources for local farmers to increase their income.In B.chinense cultivation,wheat-B.chinense,maize-B.ch...Bupleurum chinense is a genuine medicinal material in Shanxi Province,and planting B.chinense is one of the main sources for local farmers to increase their income.In B.chinense cultivation,wheat-B.chinense,maize-B.chinense and soybean-B.chinense are commonly used as multiple cropping patterns.In the present study,we studied the effects of three different multiple cropping patterns on N,P and K levels of soil,photosynthetic parameters,agronomic characteristics,saikosaponin A,C and D contents,yield and economic benefits of B.chinense.The results showed that the soybean-B.chinense multiple cropping pattern was beneficial to the enrichment of N in the soil,thus promoting photosynthetic parameters,growth,saikosaponin accumulation,yield and economic benefits of B.chinense.It is suggested that soybean-B.chinense multiple cropping was an appropriate multiple cropping pattern for local cultivation of B.chinense.展开更多
Saikosaponin v-2(1). was isolated li om the roots of the title plant and thc structure was identified on rhs basis of spectral anal? sis. Saikosaponin v-2 is a new compound. which was identified as 3 beta .16 alpha .2...Saikosaponin v-2(1). was isolated li om the roots of the title plant and thc structure was identified on rhs basis of spectral anal? sis. Saikosaponin v-2 is a new compound. which was identified as 3 beta .16 alpha .23.28-tetrahydroxy-olean-11.13(18)-dien-30-oic acid-3-O-beta -D-glucopyranosyl- (1 -->2)glucopyranosyl-(1 -->3)-beta -D-fucopyranosol-30-O-xylitol ester.展开更多
In order to solve the problem of low emergence rate of Bupleurum chinense seeds, and screen out the best germination conditions, the seeds of Bupleurum chinense L. were treated with different soaking time, germinatio...In order to solve the problem of low emergence rate of Bupleurum chinense seeds, and screen out the best germination conditions, the seeds of Bupleurum chinense L. were treated with different soaking time, germination temperature and exogenous regulating substances to improve the germination rate. The results showed that the germination rate of fresh water at 12 h was significantly higher than that at 8 h and 36 h; The germination rate of seeds treated with constant temperature 15℃ and variable temperature 25 ℃/15 ℃ （day/night） was significantly higher than that of other temperature treatments. Seed soaking time and culture temperature also influenced seed germination start day and peak day. Different concentrations of regulatory substances could promote seeds germination. The germination rate of seeds induced by 0.50 mg/L 6-BA was the highest, the start day and peak day were 4 days and 5 days earlier than control check （CK） respectively.展开更多
As a traditional Chinese herbal medicine exhibiting analgesic,fever-reducing and anti-inflammatory effects,Radix Bupleuri（Chai-Hu） is commonly used for the treatment of influenza,which is derived from the dried root...As a traditional Chinese herbal medicine exhibiting analgesic,fever-reducing and anti-inflammatory effects,Radix Bupleuri（Chai-Hu） is commonly used for the treatment of influenza,which is derived from the dried roots of Bupleurum chinense DC.and Bupleurum scorzonerifolium Willd.Among of diverse chemical components,saikosaponins are the key active components of the herb medicine.In the present study,we established a method of high performance liquid chromatography（HPLC） coupled with evaporative light scattering detection（ELSD） for simultaneous determination of saikosaponin a,c and d in root,stem,leaf and flower of Bupleurum chinense（B chinense） collected from different areas of Shanxi Province,China.The results from 16 samples of root,stem,leaf and flower of B chinense demonstrated that the total contents of the three saikosaponins in the root of B chinense collected from Dongshan Taiyuan,Xishan,Tianlongshan and Pangquangou were 4.26 mg/g,3.22 mg/g,4.23 mg/g and 3.05 mg/g,respectively.However,there was scarcely any saikosaponins in the stem,leaf and flower of B chinense collected from above-mentioned areas.The method of HPLC coupled with ELSD was suitable for quality control of Radix Bupleuri.The result also confirmed that the root of B chinense was the best medicinal part.展开更多
基金supported by CARS(CARS-21),the CAMS Innovation Fund for Medical Sciences(2021-I2M-1-032)the Science and Technology Department of Xizang(XZ202401ZY0020)+2 种基金the Science and Technology Department of Sichuan Province(2023YFH0044,2023YFH0018)the Sichuan Province Science Foundation for Distinguished Young Scholars(2022JDJQ0006)the Doctoral Fund of Southwest University of Science and Technology(19ZX7117,21ZX7116).
文摘Saikosaponins are the major pharmacologically active components in Bupleurum genus and exhibit significant application potential in multiple fields such as immune regulation and anti-tumor activity.To elucidate the biosynthetic pathway of saikosaponins,we identified two cytochrome P450 monooxygenases,CYP716A41 and CYP716Y4,in Bupleurum chinense.These enzymes catalyze the C-28 oxidation and C-16 hydroxylation of oleanane-type triterpene skeletons,respectively.The catalytic efficiency of CYP716A41 from a southern B.chinense variety was significantly higher than that from a northern variety.Molecular docking and mutagenesis experiments revealed that amino acid residues at sites 9 and 35 may contribute to this difference in catalytic efficiency.Additionally,under cold stress,the expression levels of both CYP450 genes and the saikosaponin contents in the leaves of southern varieties were significantly higher compared to those in northern varieties.The variation in the catalytic efficiency of CYP716A41 and the differential expression of the two CYP450 genes under cold stress during winter are associated with the differences in saikosaponin biosynthesis in the leaves of southern and northern B.chinense varieties.This is consistent with the distinct medicinal usage practices observed between southern and northern China.
基金supported by the National Natural Science Foundation of China(Nos.30925042,81274165,and 81330089)the State Key Program for New Drugs from the Ministry of Science and Technology,China(No.2012ZX09301001-003)the Science and Technology Commission of Shanghai Municipality(Nos.10XD1405900 and 12JC1400800)
文摘The present study aimed to investigate the effects of polysaccharides extracted from Bupleurum chinense DC(BCPs) on macrophage functions. In the in vivo experiment, 1 m L of 5% sodium thioglycollate was injected into the abdomen of the mice on Day 0 and macrophages were harvested on Day 4. The macrophages were cultured in plates and treated with different concentrations of BCPs and stimulus. Effects of BCPs on macrophage functions were assessed by chemotaxis assay, phagocytosis assay and Enzyme-Linked Immunosorbent Assay(ELISA). Our results showed the enhanced chemotaxis, phagocytosis and secretion of nitric oxide(NO) and inflammatory cytokines by macrophages when treated with BCPs. However, when chemotaxis and phagocytosis were up-regulated by complement components or opsonized particles, BCPs inhibited these effects. Also, the NO production induced by lipopolysaccharides(LPS) was suppressed by BCPs mildly. Moreover, BCPs had an inhibitory effect on the [Ca^(2+)]i elevation of macrophages. These results suggested that BCPs exerted modulatory effects on macrophage functions, which may contribute to developing novel approaches to treating inflammatory diseases.
基金the National Natural Science Foundation of China (Accession no. 81573586, 90612002).
文摘A quantitative evaluation method for the quality consistency of Bupleurum chinense DC. was developed by combining multiwavelength fusion fingerprint with chemometric methods. The fingerprint information of Bupleurum at five wavelengths (210, 254, 265, 280 and 320 nm) collected by HPLC-DAD instrument was fused to overall control its quality. The fusion fingerprints and four components (saikosaponin a, saikosaponin d, rutin, quercitrin) were studied by systematic quantitative fingerprint method and principal component analysis, respectively. Besides, fingerprint-efficacy relationship was constructed in vitro using partial least-squares model. In conclusion, all work can serve as a valid reference for the quality control of Bupleurum .
文摘A new saikosaponin was isolated from Bupleurum chinense DC., and its structure was identified as 3β,16α,23,28,30_pentahydroxy_olean_11,13(18)_dien_3_O_β_D_glucopyranosyl(1→6)_[α_L_rhamnopyranosyl (1→4)]_β_D_glucopyranoside on the basis of chemical and spectral evidence, named as saikosaponin q_1. In addition, two known saikosaponins, 3″_O_acetyl_saikosaponin d and 3″_O_acetyl_saikosaponin b 2, were also isolated and identified from this plant for the first time.
基金supported by the National Science Foundation of China(No.81573322)the Hundred-Talent Program of CAS+1 种基金the CAS"Light of West China"Programthe Youth Innovation Promotion Association of CAS
文摘5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2 C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2 C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d(1), was determined by extensive spectroscopic analyses(HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2 C receptor agonistic activity. Saikosaponin a(3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2 C receptor with an EC50 value of 21.08 ± 0.33 μmol×L^(–1) in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg×kg^(–1) in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
基金supported by the National Natural Science Foundation of China.
文摘A new chromone glycoside,saikochromoside A(1),was isolated from the roots of Bupleurum chinense DC.Its structure was determined on the bases of chemical and spectral analyses.
基金National Natural Science Foundation of China(Grant No.31601677)Natural Science Foundation of Shanxi Province(Grant No.201701D121180)+1 种基金Key Research and Development Project of Jinzhong City in Shanxi Province(Grant No.Y182018)Technological innovation team of development and utilization Chinese Geoherbs Resources in Shanxi Province,China(No.2018TD009)。
文摘Bupleurum chinense is a genuine medicinal material in Shanxi Province,and planting B.chinense is one of the main sources for local farmers to increase their income.In B.chinense cultivation,wheat-B.chinense,maize-B.chinense and soybean-B.chinense are commonly used as multiple cropping patterns.In the present study,we studied the effects of three different multiple cropping patterns on N,P and K levels of soil,photosynthetic parameters,agronomic characteristics,saikosaponin A,C and D contents,yield and economic benefits of B.chinense.The results showed that the soybean-B.chinense multiple cropping pattern was beneficial to the enrichment of N in the soil,thus promoting photosynthetic parameters,growth,saikosaponin accumulation,yield and economic benefits of B.chinense.It is suggested that soybean-B.chinense multiple cropping was an appropriate multiple cropping pattern for local cultivation of B.chinense.
基金This study was financially supported by the National Natural Science Foundation of China (29632050).
文摘Saikosaponin v-2(1). was isolated li om the roots of the title plant and thc structure was identified on rhs basis of spectral anal? sis. Saikosaponin v-2 is a new compound. which was identified as 3 beta .16 alpha .23.28-tetrahydroxy-olean-11.13(18)-dien-30-oic acid-3-O-beta -D-glucopyranosyl- (1 -->2)glucopyranosyl-(1 -->3)-beta -D-fucopyranosol-30-O-xylitol ester.
文摘In order to solve the problem of low emergence rate of Bupleurum chinense seeds, and screen out the best germination conditions, the seeds of Bupleurum chinense L. were treated with different soaking time, germination temperature and exogenous regulating substances to improve the germination rate. The results showed that the germination rate of fresh water at 12 h was significantly higher than that at 8 h and 36 h; The germination rate of seeds treated with constant temperature 15℃ and variable temperature 25 ℃/15 ℃ （day/night） was significantly higher than that of other temperature treatments. Seed soaking time and culture temperature also influenced seed germination start day and peak day. Different concentrations of regulatory substances could promote seeds germination. The germination rate of seeds induced by 0.50 mg/L 6-BA was the highest, the start day and peak day were 4 days and 5 days earlier than control check （CK） respectively.
基金Shanxi Educational Committee(Grant No.20111113)Shanxi Science and Technology Department(Grant No.2016ZD0201)
文摘As a traditional Chinese herbal medicine exhibiting analgesic,fever-reducing and anti-inflammatory effects,Radix Bupleuri（Chai-Hu） is commonly used for the treatment of influenza,which is derived from the dried roots of Bupleurum chinense DC.and Bupleurum scorzonerifolium Willd.Among of diverse chemical components,saikosaponins are the key active components of the herb medicine.In the present study,we established a method of high performance liquid chromatography（HPLC） coupled with evaporative light scattering detection（ELSD） for simultaneous determination of saikosaponin a,c and d in root,stem,leaf and flower of Bupleurum chinense（B chinense） collected from different areas of Shanxi Province,China.The results from 16 samples of root,stem,leaf and flower of B chinense demonstrated that the total contents of the three saikosaponins in the root of B chinense collected from Dongshan Taiyuan,Xishan,Tianlongshan and Pangquangou were 4.26 mg/g,3.22 mg/g,4.23 mg/g and 3.05 mg/g,respectively.However,there was scarcely any saikosaponins in the stem,leaf and flower of B chinense collected from above-mentioned areas.The method of HPLC coupled with ELSD was suitable for quality control of Radix Bupleuri.The result also confirmed that the root of B chinense was the best medicinal part.
