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Saikosaponin D improves nonalcoholic fatty liver disease via gut microbiota-bile acid metabolism pathway
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作者 Lan Li Shengye Yang +5 位作者 Xinyu Liang Yameng Liu Hualing Xu Xiaozhen Guo Cen Xie Xiaojun Xu 《Food Science and Human Wellness》 SCIE CAS CSCD 2024年第5期2703-2717,共15页
Non-alcoholic fatty liver disease(NAFLD)is the main cause of chronic liver disease worldwide.Bupleurum is widely used in the treatment of non-alcoholic fatty liver,and saikosaponin D(SSD)is one of the main active comp... Non-alcoholic fatty liver disease(NAFLD)is the main cause of chronic liver disease worldwide.Bupleurum is widely used in the treatment of non-alcoholic fatty liver,and saikosaponin D(SSD)is one of the main active components of Bupleurum.The purpose of this study was to investigate the efficacy of SSD in the treatment of NAFLD and to explore the mechanism of SSD in the improvement of NAFLD based on“gut-liver axis”.Our results showed that SSD dose-dependently alleviated high fat diet-induced weight gain in mice,improved insulin sensitivity,and also reduced liver lipid accumulation and injury-related biomarkers aspartate aminotransferase(AST)and alanine aminotransferase(ALT).Further exploration found that SSD inhibited the mRNA expression levels of farnesoid X receptor(Fxr),small heterodimer partner(Shp),recombinant fibroblast growth factor 15(Fgf15)and apical sodium dependent bile acid transporter(Asbt)in the intestine,suggesting that SSD improved liver lipid metabolism by inhibiting intestinal FXR signaling.SSD can significantly reduce the gut microbiota associated with bile salt hydrolase(BSH)expression,such as Clostridium.Decreased BSH expression reduced the ratio of unconjugated to conjugated bile acids,thereby inhibiting the intestinal FXR.These data demonstrated that SSD ameliorated NAFLD potentially through the gut microbiota-bile acidintestinal FXR pathway and suggested that SSD is a promising therapeutic agent for the treatment of NAFLD. 展开更多
关键词 saikosaponin D(SSD) Non-alcoholic fatty liver disease Bile acids Gut microbiota Farnesoid X receptor
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Saikosaponin q-1 from Bupleurum chinense 被引量:10
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作者 梁鸿 韩紫岩 +4 位作者 赵玉英 王邠 崔育新 杨文修 余奕 《Acta Botanica Sinica》 CSCD 2001年第2期198-200,共3页
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
关键词 Bupleurum chinense saikosaponin q_1
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Saikosaponin D inhibits proliferation and induces apoptosis via C/EBPβ-p53 signal pathway in human hepatoma HepG2 cells 被引量:3
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作者 Xin-Lan Lu,Xi Liang,Ya-Xin Zhang,Ya-Nan Hu,Shui-Xiang He Department of Gastroenterology,the First Affiliated Hospital,Medical School of Xi’an Jiaotong University,Xi’an 710061,China 《Journal of Pharmaceutical Analysis》 SCIE CAS 2010年第4期252-254,259,共4页
Objective To investigate the anticancer effects and detailed mechanisms of Saikosaponin D(SSD)in human hepatoma HepG2 cells.Methods Cell proliferation and apoptosis were tested by MTT assay and Annexin-V/PI assay resp... Objective To investigate the anticancer effects and detailed mechanisms of Saikosaponin D(SSD)in human hepatoma HepG2 cells.Methods Cell proliferation and apoptosis were tested by MTT assay and Annexin-V/PI assay respectively.The expressions of CCAAT enhancer binding protein β(C/EBPβ)and p53 were detected by RT-PCR and Western blotting.Results SSD inhibited cell proliferation in a dose-dependent manner and induced apoptosis at the concentration of 5.0 mg/L.SSD significantly increased the mRNA and protein levels of C/EBPβ and p53 in a dose-dependent manner.Conclusion SSD exerts its anticancer effect by inhibiting cell proliferation and inducing apoptosis partly through C/EBPβ-p53 signal pathway in HepG2 cells. 展开更多
关键词 saikosaponin D P53 CCAAT enhancer binding protein β APOPTOSIS
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Saikosaponin a increases interleukin-10 expression and inhibits scar formation after sciatic nerve injury 被引量:3
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作者 Meng-Qiang Huang Xiao-Yu Cao +7 位作者 Xu-Yi Chen Ying-Fu Liu Shuang-Long Zhu Zhong-Lei Sun Xian-Bin Kong Jing-Rui Huo Sai Zhang Yun-Qiang Xu 《Neural Regeneration Research》 SCIE CAS CSCD 2018年第9期1650-1656,共7页
Nerve scarring after peripheral nerve injury can severely hamper nerve regeneration and functional recovery.Further,the anti-inflammatory cytokine,interleukin-10,can inhibit nerve scar formation.Saikosaponin a(SSa) ... Nerve scarring after peripheral nerve injury can severely hamper nerve regeneration and functional recovery.Further,the anti-inflammatory cytokine,interleukin-10,can inhibit nerve scar formation.Saikosaponin a(SSa) is a monomer molecule extracted from the Chinese medicine,Bupleurum.SSa can exert anti-inflammatory effects in spinal cord injury and traumatic brain injury.However,it has not been shown whether SSa can play a role in peripheral nerve injury.In this study,rats were randomly assigned to three groups.In the sham group,the left sciatic nerve was directly sutured after exposure.In the sciatic nerve injury(SNI) + SSa and SNI groups,the left sciatic nerve was sutured and continuously injected daily with SSa(10 mg/kg) or an equivalent volume of saline for 7 days.Enzyme linked immunosorbent assay results demonstrated that at 7 days after injury,interleukin-10 level was considerably higher in the SNI + SSa group than in the SNI group.Masson staining and western blot assay demonstrated that at 8 weeks after injury,type I and III collagen content was lower and nerve scar formation was visibly less in the SNI + SSa group compared with the SNI group.Simultaneously,sciatic functional index and nerve conduction velocity were improved in the SNI + SSa group compared with the SNI group.These results confirm that SSa can increase the expression of the anti-inflammatory factor,interleukin-10,and reduce nerve scar formation to promote functional recovery of injured sciatic nerve. 展开更多
关键词 nerve regeneration saikosaponin a anti-inflammatory factor inflammation interleukin-l O nerve scar peripheral nerve injury sciatic nerve injury sciatic functional index nerve conduction velocity neuroelectrophysiological function neural regeneration
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Radix Paeoniae Alba attenuates Radix Bupleuri-induced hepatotoxicity by modulating gut microbiota to alleviate the inhibition of saikosaponins on glutathione synthetase 被引量:4
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作者 Congcong Chen Wenxia Gong +4 位作者 Junshen Tian Xiaoxia Gao Xuemei Qin Guanhua Du Yuzhi Zhou 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2023年第6期640-659,共20页
Radix Bupleuri(RB)is commonly used to treat depression,but it can also lead to hepatotoxicity after longterm use.In many anti-depression prescriptions,RB is often used in combination with Radix Paeoniae Alba(RPA)as an... Radix Bupleuri(RB)is commonly used to treat depression,but it can also lead to hepatotoxicity after longterm use.In many anti-depression prescriptions,RB is often used in combination with Radix Paeoniae Alba(RPA)as an herb pair.However,whether RPA can alleviate RB-induced hepatotoxicity remain unclear.In this work,the results confirmed that RB had a dose-dependent antidepressant effect,but the optimal antidepressant dose caused hepatotoxicity.Notably,RPA effectively reversed RB-induced hepatotoxicity.Afterward,the mechanism of RB-induced hepatotoxicity was confirmed.The results showed that saikosaponin A and saikosaponin D could inhibit GSH synthase(GSS)activity in the liver,and further cause liver injury through oxidative stress and nuclear factor kappa B(NF-kB)/NOD-like receptor thermal protein domain associated protein 3(NLRP3)pathway.Furthermore,the mechanisms by which RPA attenuates RBinduced hepatotoxicity were investigated.The results demonstrated that RPA increased the abundance of intestinal bacteria with glycosidase activity,thereby promoting the conversion of saikosaponins to saikogenins in vivo.Different from saikosaponin A and saikosaponin D,which are directly combined with GSS as an inhibitor,their deglycosylation conversion products saikogenin F and saikogenin G exhibited no GSS binding activity.Based on this,RPA can alleviate the inhibitory effect of saikosaponins on GSS activity to reshape the liver redox balance and further reverse the RB-induced liver inflammatory response by the NFkB/NLRP3 pathway.In conclusion,the present study suggests that promoting the conversion of saikosaponins by modulating gut microbiota to attenuate the inhibition of GSS is the potential mechanism by which RPA prevents RB-induced hepatotoxicity. 展开更多
关键词 Radix Bupleuri Radix Paeoniae Alba HEPATOTOXICITY Gut microbiota saikosaponinS Combination mechanisms
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Comparative permeability of three saikosaponins and corresponding saikogenins in Caco-2 model by a validated UHPLC-MS/MS method 被引量:3
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作者 Siqi Ren Jingjing Liu +5 位作者 Yunwen Xue Mei Zhang Qiwei Liu Jie Xu Zunjian Zhang Rui Song 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2021年第4期435-443,共9页
Saikosaponins(SSs)are the main active components extracted from Bupleuri Radix(BR)which has been used as an important herbal drug in Asian countries for thousands of years.It has been reported that the intestinal bact... Saikosaponins(SSs)are the main active components extracted from Bupleuri Radix(BR)which has been used as an important herbal drug in Asian countries for thousands of years.It has been reported that the intestinal bacteria plays an important role in the in vivo disposal of oral SSs.Although the deglycosylated derivatives(saikogenins,SGs)of SSs metabolized by the intestinal bacteria are speculated to be the main components absorbed into the blood after oral administration of SSs,no studies have been reported on the characteristics of SGs for their intestinal absorption,and those for SSs are also limited.Therefore,a rapid UHPLC-MS/MS method was developed to investigate and compare the apparent permeability of three common SSs(SSa,SSd,SSb2)and their corresponding SGs(SGF,SGG,SGD)through a bidirectional transport experiment on Caco-2 cell monolayer model.The method was validated according to the latest FDA guidelines and applied to quantify the six analytes in transport medium samples extracted via liquid-liquid extraction(LLE).The apparent permeability coefficient(Papp)determined in this study indicated that the permeability of SGs improved to the moderate class compared to the corresponding parent compounds,predicting a higher in vivo absorption.Moreover,the efflux ratio(ER)value demonstrated an active uptake of SSd and the three SGs,while a passive diffusion of SSa and SSb2. 展开更多
关键词 Bupleuri Radix saikosaponin Saikogenin UHPLC-MS/MS Caco-2 cells PERMEABILITY
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Saikosaponins-b suppresses tumor growth and angiogenesis of hepatocellular carcinoma by regulating VEGF/ERK/HIF-1α signal pathway 被引量:2
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作者 Rui-fang LI Jun-min FU +3 位作者 Xing-zhi LYU Zi-han GAO Hong-wei WANG Jian-gang WANG 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2017年第10期962-963,共2页
OBJECTIVE Angiogenesis therapy has attracted interest as a potential treatment for hepatocellular carcinoma(HCC).In this study,we investigated the anti-proliferative activities and antiangiogenesis effects of saikosap... OBJECTIVE Angiogenesis therapy has attracted interest as a potential treatment for hepatocellular carcinoma(HCC).In this study,we investigated the anti-proliferative activities and antiangiogenesis effects of saikosaponins(SS)-b on hepatocellular carcinoma(HCC)and its regulation on VEGF/ERK/HIF-1 αsignal pathway.METHODS H22 hepatoma-bearing mice model and HepG-2 cells were used to study the anti-tumor and anti-angiogenesis effects of SS-b in vivo and in vitro.Pathological change of tumor tissue was observed by HE staining,the microvascular changes were detected by immunohistochemical method.The effects of SS-b on angiogenesis were examined by using the chick embryo chorioallantoic membrane(CAM)model.The effects of SS-b on proliferation,migration and invasion were investigated by MTT assay,scratch wound healing assay and transwell assay inhuman umbilical vein endothelial cell(HUVEC)and HepG2 cells in vitro.Vascular endothelial growth factor(VEGF),matrix metalloproteinase-2/9(MMP-2/9),hypoxia-inducible factor-1α(HIF-1α)expression and the phosphorylation of extracellular regulated kinase(ERK)were analyzed using RT-PCR and Westernblot.RESULTS SS-b effectively inhibited the tumor growth of H22 mice in vivo.The inhibitory rate of tumor was 49.1%,50.7%,66.1%in SS-b 5,10 and 20 mg·kg-1group respectively.HE staining results showed that SS-b induced tumor necrosis and nuclear dissolution in H22 mice.Moreover,SS-b also reduced the number of microvessels of tumor tissue in H22 mice significantly and suppressed the angiogenesis of CAM induced by b-FGF.SS-b had an obvious inhibitory effect on cell proliferation,migration and invasion of HUVEC cells and HepG-2 cells.These effects were associated with downregulation of the expression of MMP2/9 and suppression of VEGF/ERK/HIF-1αsignaling in H22 mice and Hep-G2 cells.CONCLUSION Our findings showed that SS-b exerts anti-tumor effects by inhibiting tumor angiogenesis via regulating VEGF/ERK/HIF-1α signal pathway in vivo and in vitro. 展开更多
关键词 saikosaponins-b ANGIOGENESIS hepatocellular carcinoma chorioallantoic membrane HUVEC cells
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Three New Saikosaponin-like Compounds from Polycarpon prostratum 被引量:1
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作者 Zhong Tao DING Jun ZHOU +1 位作者 Ning Hua TAN Shi Ming DENG 《Chinese Chemical Letters》 SCIE CAS CSCD 2001年第8期705-708,共4页
Three new saikosaponin-like compounds (named prostratoside F-H) were isolated from the whole plants of Polycarpon prostratum (Forssk.) Aschers. et Schwein. ex Aschers. By detailed spectroscopic analysis, their structu... Three new saikosaponin-like compounds (named prostratoside F-H) were isolated from the whole plants of Polycarpon prostratum (Forssk.) Aschers. et Schwein. ex Aschers. By detailed spectroscopic analysis, their structures were determined as 13 beta, 28-epoxy-16-keto-22 alpha, 23-dihydroxyolean-11-en-3 beta -yl-alpha -L-arabinopyranoside, 13 beta, 28-epoxy-16-keto-23-hydroxy-olean-11-en-3 beta -yl-alpha -L-arabinopyranoside and 13 beta, 28-epoxy-16-keto-22 alpha -hydroxyolean-11-en-3 beta -yl-alpha -L-arabinopyranoside, respectively. 展开更多
关键词 Polycarpon prostratum CARYOPHYLLACEAE saikosaponin-like compound
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柴胡中Saikosaponin b_2的提取工艺研究
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作者 李军 姜华 +2 位作者 张延萍 张倩 吕茂平 《时珍国医国药》 CAS CSCD 北大核心 2012年第11期2670-2671,共2页
目的优选柴胡中Saikosaponin b2的提取工艺。方法采用高效液相色谱法测定Saikosaponin b2含量。以提取量为指标,用正交设计方法优选最佳提取工艺。结果最佳提取工艺为:用30%乙醇,提取3次,每次1.5 h,溶剂用量为8倍。结论优选得到的工艺... 目的优选柴胡中Saikosaponin b2的提取工艺。方法采用高效液相色谱法测定Saikosaponin b2含量。以提取量为指标,用正交设计方法优选最佳提取工艺。结果最佳提取工艺为:用30%乙醇,提取3次,每次1.5 h,溶剂用量为8倍。结论优选得到的工艺稳定可行,可作为Saikosaponin b2的提取工艺。 展开更多
关键词 柴胡 柴胡皂苷 正交设计
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Saikosaponin v-2 from Bupleurum chinense
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作者 Hong LIANG Yan Jun CUI +3 位作者 Yu Ying ZHAO Bin WANG Wen Xiu YANG Yi YU 《Chinese Chemical Letters》 SCIE CAS CSCD 2001年第4期331-332,共2页
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
关键词 Bupleurum chinense DC. UMBELLIFERAE saikosaponin v-2.
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Effect of saikosaponin A on Treg and Th17 immune balance in depressive rats
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作者 Xu-Tong Guo Ji-Dong An Jian-Qiang Mei 《Journal of Hainan Medical University》 2020年第22期6-9,共4页
Objective:To investigate the Effect of saikosaponin A on Treg and Th17 immune balance in depressive rats.Methods:The rat depression model was established with reference to the Katz method,and the rats were randomly di... Objective:To investigate the Effect of saikosaponin A on Treg and Th17 immune balance in depressive rats.Methods:The rat depression model was established with reference to the Katz method,and the rats were randomly divided into control group,model group,western medicine group,and saikosaponin A group.The western medicine group was given 1.2 mg/kg/d of fluoxetine,and the saikosaponin A group was given 25 mg/kg/d of saikosaponin A,while the control group and model group were given the same volume of normal saline.The evaluation of depression in Rats was analyzed by Openfield-test and sugar water preference test.Flow cytometry was used to detect the expression of Th17 and Treg cells.And the expression of IL-17,IL-23,TNF-α,IL-10,TGF-βwere detected by enzyme-linked immunosorbent assay(ELISA).Results:Compared with the control group,the horizontal exercise score,vertical exercise score,and sugar preference of the model group decreased significantly(P<0.05).Compared with the model group,the above indicators were significantly increased in the western medicine group and saikosaponin A group(P<0.05).Flow cytometry showed that compared with the control group,the Th17 cells,Th17/Treg cell ratio in model group increased significantly,whereas the Treg cells decreased significantly(P<0.05).Compared with the model group,The Th17 cells and Th17/Treg ratio in western medicine group and saikosaponin A group decreased,while the Treg cells increased significantly(P<0.05).ELISA showed that compared with control group,the serum levels of IL-17,IL-23 and TNF-αin model group increased,while the levels of IL-10 and TGF-βdecreased(P<0.05).Compared with model group,the levels of IL-17,IL-23 and TNF-αdecreased,while the levels of IL-10 and TGF-βincreased in western medicine group and saikosaponin A group(P<0.05).Conclusion:Saikosaponin A can reduce the degree of depression by regulating the imbalance of Th17/Treg cells and the secretion of inflammatory cytokines in depressed rats. 展开更多
关键词 saikosaponin A DEPRESSION Th17/Treg cell CYTOKINES
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Saikosaponin-b regulates the proliferation and apoptosis of HepG2 cells by targeting the MACC1/c-Met/Akt signaling pathway
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作者 Xing-zhi LYU Rui-fang LI +3 位作者 Zi-han GAO Hong-wei WANG Sang-qiang LI Jian-gang WANG 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2017年第10期965-966,共2页
OBJECTIVE Metastasis-associated in colon cancer-1(MACC1)is an oncogene that has been newly identified.It promotes tumor proliferation and invasion via the MET pathway.Our study investigated the effects of Saikosaponin... OBJECTIVE Metastasis-associated in colon cancer-1(MACC1)is an oncogene that has been newly identified.It promotes tumor proliferation and invasion via the MET pathway.Our study investigated the effects of Saikosaponin-b(SS-b)on the proliferation and apoptosis of HepG2 cells and its regulation on MACC1/c-Met/Akt signaling pathway.METHODS HepG2 cells were treated with SS-b(10-800 g·L^(-1))for 48 h in vitro.The CCK-8 assay was used to assess cell proliferation,and cell apoptosis was determined by Hoechst33258 staining,AnnexinⅤ/PI staining and caspase 3 assay.RT-PCR was used to examine the expression of MACC1,c-MET and hepatocyte growth factor(HGF)mR NA.MACC1 protein was detected by Western blot and immunohistochemistry.The protein expressions of p-cMET,c-MET,p-AKT,AKT,p-BAD,BAD were measured by Western blot.RESULTS SS-b inhibited the growth of HepG2 cells in dose-dependent way and induced cell apoptosis significantly.HepG2 cells showed karyopyknosis,fragmentation and fluorescence highlight in SS-b treatment group.FCM results showed that apoptosis rate of HepG2 cells increased with SS-b concentration.The immunofluorescence results showed that the MACC1 expression decreased significantly in HepG2 cells treated with SS-b.The expression levels of MACC1,c-MET and HGF mR NA in HepG2 cells were significantly inhibited by SS-b.SS-b also significantly decreased the protein expressions of MACC1,p-c-MET and p-AKT while increased the expression of p-BAD and caspase 3 in HepG2 cells(P<0.05).CONCLUSION SS-b inhibited the proliferation and induced the apoptosis of HepG2 cells by targeting the MACC1/c-Met/Akt signaling pathway. 展开更多
关键词 saikosaponin-b metastasis-associated in colon cancer-1 c-Met signaling hepatocel ular carcinoma
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Saikosaponin A induces apoptosis and upregulates autophagy in Huh7 cells
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作者 Qing-Wei Zhang Jun Bao +2 位作者 Zhi-Long Jia Jie-Xia Sheng Er-Qing Dai 《Journal of Hainan Medical University》 2019年第2期1-5,共5页
Objective: It is discussed whether saikosaponin A induces apoptosis of human hepatoma Huh7 cells is related to the change of autophagy level.Methods: The effects of different concentrations of SSA on proliferation and... Objective: It is discussed whether saikosaponin A induces apoptosis of human hepatoma Huh7 cells is related to the change of autophagy level.Methods: The effects of different concentrations of SSA on proliferation and apoptosis of Huh7 cells were detected by MTT and flow cytometry, and then constructed recombinant plasmid pEGFP-N1-LC3B and transfected into Huh7 cells. After intervened by SSA culture medium, the autophagy level was observed under confocal microscope. The expression of apoptosis proteins Bax, Bcl-2, PCNA and autophagy-related proteins LC3B, Beclin1, and Apg12-Apg5 were detected by Western Blot. Results: SSA can significantly inhibit the proliferation of Huh7 cells, promote apoptosis, increase the number of autophagy bodies in the cytoplasm, up-regulate the expression of Bax, LC3B-II, Beclin1, Apg12-Apg5 and down-regulate the expression of Bcl-2, PCNA. Conclusion:SSA induced apoptosis of Huh7 cells in vitro and upregulated the autophagy level. 展开更多
关键词 saikosaponin A(SSA) HUH7 cells AUTOPHAGY APOPTOSIS Bax PCNA LC3B BECLIN1
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Localization and Dynamic Change of Saikosaponin in Root of Bupleurum chinense 被引量:23
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作者 Ling-Ling Tan Xia Cai +1 位作者 Zheng-Hai Hu Xi-Lu Ni 《Journal of Integrative Plant Biology》 SCIE CAS CSCD 2008年第8期951-957,共7页
Anatomical, histochemical and phytochemical methods were used to investigate the structure, the localization and content changes of total saikosaponin and saikosaponin-a of the roots of Bupleurum chinense DC. at diffe... Anatomical, histochemical and phytochemical methods were used to investigate the structure, the localization and content changes of total saikosaponin and saikosaponin-a of the roots of Bupleurum chinense DC. at different developmental stages. Results showed that saikosaponin was mainly distributed in pericycle and primary phloem in the young root; but in the mature root, it was mainly distributed in vascular cambium and secondary phloem. During the whole growth period from the pre-blossom, blossom, fruit, and fruit mature periods until the pre-withering period, it was in the fruit mature period that both the total saikosaponin content and the saikosaponin-a content reached the highest level. So the last 20 d of October was considered as the right collecting season for the drug of B. chinense. In addition, the quality of 1-year-old drug was better than that of 2-year-old drug due to its higher saikosaponin content. On the other hand, judging from the external characteristics of the drug, the one with an acerose taproot and more lateral roots was of better quality. The results offered theoretical bases for selecting medicinal material of high quality and determining the most appropriate harvesting stage and part of B. chinense. 展开更多
关键词 Bupleurum chinense content dynamic change LOCALIZATION saikosaponin-a structure of root total saikosaponin
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Integrative lipidomic and transcriptomic study unravels the therapeutic effects of saikosaponins A and D on non-alcoholic fatty liver disease 被引量:26
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作者 Xiaojiaoyang Li Junde Ge +8 位作者 Yajing Li Yajie Cai Qi Zheng Nana Huang Yiqing Gu Qi Han Yunqian Li Rong Sun Runping Liu 《Acta Pharmaceutica Sinica B》 SCIE CAS CSCD 2021年第11期3527-3541,共15页
Nonalcoholic fatty liver disease(NAFLD)has become one of the most prominent causes of chronic liver diseases and malignancies.However,few therapy has been approved.Radix Bupleuri(RB)is the most frequently used herbal ... Nonalcoholic fatty liver disease(NAFLD)has become one of the most prominent causes of chronic liver diseases and malignancies.However,few therapy has been approved.Radix Bupleuri(RB)is the most frequently used herbal medicine for the treatment of liver diseases.In the current study,we aim to systemically evaluate the therapeutic effects of saikosaponin A(SSa)and saikosaponin D(SSd),the major bioactive monomers in RB,against NAFLD and to investigate the underlying mechanisms.Our results demonstrated that both SSa and SSd improved diet-induced NAFLD.Integrative lipidomic and transcriptomic analysis revealed that SSa and SSd modulated glycerolipid metabolism by regulating related genes,like Lipe and Lipg.SSd profoundly suppressed the fatty acid biosynthesis by downregulating Fasn and Acaca expression and promoted fatty acid degradation by inducing Acox1 and Cpt1 a expression.Bioinformatic analysis further predicted the implication of master transcription factors,including peroxisome proliferator-activated receptor alpha(PPARα),in the protective effects of SSa and SSd.These results were further confirmed in vitro in mouse primary hepatocytes.In summary,our study uncoded the complicated mechanisms underlying the promising anti-steatosis activities of saikosaponins(SSs),and provided critical evidence inspiring the discovery of innovative therapies based on SSa and SSd for the treatment of NAFLD and related complications. 展开更多
关键词 saikosaponin Nonalcoholic fatty liver disease LIPIDOME TRANSCRIPTOME Lipid metabolism
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Effects of Saikosaponin-D on syndecan-2,matrix metalloproteinases and tissue inhibitor of metalloproteinases-2 in rats with hepatocellular carcinoma 被引量:13
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作者 Xiaoli Jia Shuangsuo Dang +4 位作者 Yanan Cheng Xin Zhang Mei Li Yaping Li Siyuan Li 《Journal of Traditional Chinese Medicine》 SCIE CAS CSCD 2012年第3期415-422,共8页
OBJECTIVE:To investigate effects of Saikosaponin D(SSd) on syndecan-2,matrix metalloproteinases(MMPs) and tissue inhibitor of metalloproteinases-2(TIMP-2) in livers of rat with hepatocellular carcinoma(HCC).METHODS:Ma... OBJECTIVE:To investigate effects of Saikosaponin D(SSd) on syndecan-2,matrix metalloproteinases(MMPs) and tissue inhibitor of metalloproteinases-2(TIMP-2) in livers of rat with hepatocellular carcinoma(HCC).METHODS:Male SD rats were divided into control(n=10),model(n=20) and SSd(n=20) groups,and model and SSd groups given intragastric 0.2%(w/v) N-diethylnitrosamine to induce HCC.SSd group received 0.03%(w/v) SSd in saline.Liver samples were analysed immunohistochemically for syndecan-2,MMP-2,MMP-13 and TIMP-2 at 16 weeks.RESULTS:The model group had more malignant nodules than the SSd group;all model-group HCC cells were grade III;SSd-group HCC cells were grades I-II.Controls showed normal hepatic cell phenotypes and no syndecan-2 + staining.Syndecan-2 + staining was greater in the model group(35.2%,P≤0.001) than in controls or the SSd group(16.5%,P ≤ 0.001).The model group had more intense MMP-2 + staining than controls(0.37 vs 0.27,P≤0.01) or the SSd group(0.31 vs 0.37,P≤0.05);and higher MMP-13 + staining(72.55%) than in controls(12.55%,P≤0.001) and SSd group(20.18%,P≤0.01).The model group also had more TIMP-2 + staining(57.2%) than controls(20.9%,P≤0.001) and SSd group(22.7%,P≤0.001).Controls and SSd group showed no difference in TIMP-2 + rates.CONCLUSION:SSd inhibited HCC development,and downregulated expression of syndecan-2,MMP-2,MMP-13 and TIMP-2 in rat HCC liver tissue. 展开更多
关键词 Carcinoma Hepatocellular saikosaponin Syndecan-2 Matrix metalloproteinases Tissue inhibitor of metalloproteinase inhibitor-2
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Simultaneous determination of Saikosaponin a, c and d in different parts of wild bupleurum from Shanxi Province 被引量:9
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作者 Rui Wang Ximei Yuan +2 位作者 Boya Ju Rui Liu Hongxia Yuan 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2018年第10期703-710,共8页
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
关键词 Bupleurum chinense DC. Different parts saikosaponinS Content analysis
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Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity 被引量:3
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作者 SUN Chang-Li GENG Chang-An +7 位作者 HUANG Xiao-Yan MA Yun-Bao ZHENG Xiao-Hong YANG Tong-Hua CHEN Xing-Long YIN Xiu-Juan ZHANG Xue-Mei CHEN Ji-Jun 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2017年第6期467-473,共7页
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
关键词 Bupleurum chinense 5-hydroxytryptamine 2C(5-HT2C) receptor ANTI-OBESITY saikosaponinS
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Identification of WRKY Transcription Factors Related to Saikosaponin Biosynthesis in Adventitious Roots of Bupleurum chinense 被引量:4
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作者 Su-rui Wu Ke Gao +3 位作者 Xuan Liu Jiao Xu Jian-he Wei Chun Sui 《Chinese Herbal Medicines》 CAS 2017年第2期153-160,共8页
Objective To identify the genes of WRKY transcription factors(TFs) from roots of Bupleurum chinense and genes that potentially regulate saikosaponin(SS) biosynthesis.Methods Firstly,the subfamily cluster analysis ... Objective To identify the genes of WRKY transcription factors(TFs) from roots of Bupleurum chinense and genes that potentially regulate saikosaponin(SS) biosynthesis.Methods Firstly,the subfamily cluster analysis was mainly based on Arabidopsis thaliana WRKYs for 27 putative WRKY TFs selected from previous transcriptome sequencing data.Secondly,qPCR was used to screen such genes of WRKY TFs that could be induced by NaCI and PEG6000 in adventitious roots of B.chinense.Meanwhile,saikosaponins(SSs) in treated adventitious roots were determined by HPLC.The roots were collected at 0,2,4,8,12,24,48,and 72 h after treatments,and 120 h only for PEG.Finally,the tissue-specific expression was analyzed on screened genes by qPCR.Results The 27 genes were grouped into three categories:There were nine in Group Ⅰ,15 in Group Ⅱ,and two in Group Ⅲ.Four genes of WRKYTFs,BCWRKY6,BCWRKY16,BCWRKY32,and BCWRKY35 were obviously induced by NaCI in adventitious roots of B.chinense,while only BCWRKY32 was induced by PEG.The content of SSs increased at different levels in NaCI and PEG6000 treatment.Three genes including BCWRKY6,BCWRKY32,and BCWRKY35,expressed most in roots,were similar to the accumulation pattern of SS.Conclusion The three WRKY genes,BCWRKY6,BCWRKY32,and BCWRKY35,may be involved in the biosynthesis of SS. 展开更多
关键词 adventitious roots NaCl treatment PEG treatment saikosaponins WRKY transcription factors genes
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柴胡皂苷A调节cAMP/PKA/CREB信号通路对失眠大鼠的改善作用及机制研究 被引量:3
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作者 乔明亮 梁硕 +4 位作者 孟毅 李锋森 谭高峰 齐丹丹 陈豪攀 《中药新药与临床药理》 CAS CSCD 北大核心 2024年第5期633-638,共6页
目的基于cAMP/PKA/CREB通路探讨柴胡皂苷A对失眠大鼠的改善作用及机制。方法将75只SD大鼠随机分为空白组、模型组、柴胡皂苷A低剂量组(0.625 mg·kg^(-1))、柴胡皂苷A高剂量组(2.500 mg·kg^(-1))、艾司唑仑组(0.1 mg·kg^(... 目的基于cAMP/PKA/CREB通路探讨柴胡皂苷A对失眠大鼠的改善作用及机制。方法将75只SD大鼠随机分为空白组、模型组、柴胡皂苷A低剂量组(0.625 mg·kg^(-1))、柴胡皂苷A高剂量组(2.500 mg·kg^(-1))、艾司唑仑组(0.1 mg·kg^(-1)),每组15只。采用腹腔注射苯丙氨酸(PCPA,0.1 mg·kg^(-1))复制失眠大鼠模型。观察大鼠一般情况及昼夜节律;采用戊巴比妥钠翻正实验测定大鼠睡眠潜伏期及睡眠持续时间;观测大鼠睡眠时相,记录慢波睡眠第1期(SWS1)、慢波睡眠第2期(SWS2)、快速眼球运动睡眠期(REMS)时长以及总睡眠时长(TST);qRT-PCR法测定下丘脑节律基因Clock、Bmal1 mRNA及钟控基因Rev-erbα、RorαmRNA的表达水平;免疫荧光法测定海马组织NeuN表达水平;ELISA法测定脑组织中的cAMP水平;Western Blot法测定脑组织中Clock、Bmal1、Rev-erbα、Rorα及cAMP/PKA/CREB通路相关蛋白表达水平。结果与空白组比较,模型组大鼠昼伏夜出的节律紊乱,极度兴奋,易激惹,睡眠减少;睡眠潜伏期明显延长(P<0.05),睡眠持续时间及SWS1、SWS2、REMS、TST均明显缩短(P<0.05);神经元排列紊乱,NeuN阳性神经元IOD值明显降低(P<0.05);脑组织Clock、Bmal1、Rev-erbα、RorαmRNA及蛋白表达水平明显降低(P<0.05);脑组织cAMP、p-PKA/PKA、p-CREB/CREB蛋白表达水平明显降低(P<0.05)。与模型组比较,给药组大鼠的攻击性明显减弱,昼伏夜出有节律性,活动减少,睡眠增多;睡眠潜伏期明显缩短(P<0.05),睡眠持续时间及SWS1、SWS2、REMS、TST均明显延长(P<0.05);神经元排列紊乱情况有所恢复,NeuN阳性神经元IOD值明显升高(P<0.05);脑组织Clock、Bmal1、Rev-erbα、RorαmRNA及蛋白表达水平明显升高(P<0.05);脑组织cAMP、p-PKA/PKA、p-CREB/CREB蛋白表达水平明显升高(P<0.05)。结论柴胡皂苷A可能通过激活cAMP/PKA/CREB通路改善失眠大鼠的昼夜节律。 展开更多
关键词 柴胡皂苷A 失眠 cAMP/PKA/CREB信号通路 昼夜节律 节律基因 钟控基因 大鼠
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