Objective To identify whether sarsasapogenin, a sapogenin from the Chinese medicinal herb Anemarrhena Asphodeloides Bunge, would augment the efficacy of risperidone and significantly improve cognitive functions in pat...Objective To identify whether sarsasapogenin, a sapogenin from the Chinese medicinal herb Anemarrhena Asphodeloides Bunge, would augment the efficacy of risperidone and significantly improve cognitive functions in patients with negative symptoms dominated schizophrenia. Methods The trial was a double-blind, placebo-controlled, parallel- group design. The eligible patients were randomized into 2 treatment groups： sarsasapogenin group （sarsasapogenin plus risperidone for 8 weeks, n = 41） and placebo group （risperidone only for 8 weeks, n = 39）. At the baseline, as well as at weeks 2, 4 and 8 of treatment, the therapeutic response was measured by using scales including Positive and Nega- tive Symptoms Scale （PANSS）, Wechsler Memory Scale （WMS）, modified Chinese Wechsler Adult Intelligence Scale （mWAIS）, Clinical Global Impression （CGI） and Brief Psychiatry Rating Scale （BPRS）. The study period for each subject was 8 weeks and duration of overall trial was 2 years. Results Patients treated with sarsasapogenin plus risperidone demonstrated no statistically significant differences in changes in PANSS, WMS or mWAIS score at the end-point of the trial compared with patients treated with placebo plus risperidone. The incidence of treatment-emergent adverse events in patients treated with sarsasapogenin was not different from that observed in placebo group. Conclusion Sarsasapogenin did not augment the efficacy of risperidone in treating negative symptoms dominated schizophrenia. Sarsasapogenin at a dosage of 200 mg per day added to a flexible dosage of risperidone at 2-4 mg per day is safe and well tolerated by patients with negative symptoms dominated schizophrenia.展开更多
[ Objective ] We aimed to establish the identification method of gardenoside and sarsasapogenin in Qingwen baidu granules. [ Method] With ethyl ace- tate-acetone-formic acid-water （10：7：2：0.5） as the developer an...[ Objective ] We aimed to establish the identification method of gardenoside and sarsasapogenin in Qingwen baidu granules. [ Method] With ethyl ace- tate-acetone-formic acid-water （10：7：2：0.5） as the developer and 10% sulfuric acid ethanol solution as the chromogenic reagent, the samples were heated at 100 ~C until the spots were clearly visible, and the existence of gardenoside was checked under natural light. With toluene-acetone（9：l ） as the developer and 5% vanillin sulfuric acid solution as the chromogenic reagent, the samples were heated at 105 ~C until the spots were clearly visible, and the existence of sarsasapogenin was checked under natural light. [Result] Qingwen baidu granules had the same spots with gardenoside and sarsasapogenin at the same Rfvalue under natural light. [ Conclusion] A TLC method detecting gardenoside and sarsasapogenin in Qingwen baidu granules was established, which had good specificity and repeatability, suitable for rapid detection of gardenoside and sarsasapogenin.展开更多
In this paper,the pharmacological effects and molecular mechanisms of sarsasapogenin,such as anti-oxidant,anti-inflammatory and anti-diabetic effects,are reviewed in order to provide a theoretical basis for the subseq...In this paper,the pharmacological effects and molecular mechanisms of sarsasapogenin,such as anti-oxidant,anti-inflammatory and anti-diabetic effects,are reviewed in order to provide a theoretical basis for the subsequent development and clinical application of sarsasapogenin.展开更多
Objective To evaluate the anti-arthritic efficacy of sarsasapogenin(SG)alone and in combination with the corticosteroid fluticasone(FC)in a rat model of rheumatoid arthritis(RA),which was induced by complete Freund’s...Objective To evaluate the anti-arthritic efficacy of sarsasapogenin(SG)alone and in combination with the corticosteroid fluticasone(FC)in a rat model of rheumatoid arthritis(RA),which was induced by complete Freund’s adjuvant(CFA).Methods Network pharmacology analysis was conducted to identify the potential molecular targets and signaling pathways of SG in RA.Targets were identified with multiple databases,including SwissTargetPrediction,GeneCards,DisGeNET,and Search Tool for the Retrieval of Interacting Genes/Proteins(STRING),and pathway enrichment analysis was performed using Kyoto Encyclopedia of Genes and Genomes(KEGG)and Gene Ontology(GO)databases.Molecular docking was performed to validate the binding affinity of key SG constituents with the predicted hub targets.Male Wistar rats were randomly divided into normal control(NC),CFA,SG,FC,and SG+FC groups(n=6 per group).RA was induced in all groups except NC group by a single intradermal injection of CFA(0.1 mL)into the left hind paw on day 1.After successfully induction of RA(day 12),treatments were administered intradermally from day 12 to 28 as follows:SG(50μg/rat,40μL per paw),FC(50μg/rat,40μL per paw),or a combination of SG and FC(25μg/rat each,total 40μL per paw).Therapeutic outcomes were evaluated via the paw volume,joint diameter,arthritis scores,hematological and biochemical indicators,oxidative stress markers,inflammatory cytokines,and histopathological assessments of rats’ankle joint.The gene expression analysis was performed by quantitative reverse transcription polymerase chain reaction(qRT-PCR).Acute toxicity,body weight,and immune organ indices(spleen and thymus)were also monitored to assess the potential mitigation of SG of corticosteroid-induced adverse effects.Results Network pharmacology analysis revealed 138 potential SG-associated targets,involving 10 key hub genes.KEGG enrichment indicated the participation of pathways involving phosphoinositide-3-kinase regulatory subunit 1(PIK3R1),estrogen receptor 1(ESR1),E1A binding protein P300(EP300),mammalian target of rapamycin(mTOR),C-X-C chemokine receptor type 4(CXCR4),signal transducer and activator of transcription 3(STAT3),and tolllike receptor 4(TLR4).GO enrichment analysis also revealed significant involvement of inflammatory and immune-related biological processes.Molecular docking confirmed strong binding interactions between major SG constituents and the identified hub targets.SG and SG+FC groups preserved body weight,and normalized spleen and thymus indices compared with FC group(P<0.05 or P<0.01),suggesting the mitigation of corticosteroid-induced adverse effects.SG and SG+FC groups significantly reduced paw volume,ankle diameter,and arthritis scores compared with CFA group(P<0.05,P<0.01,or P<0.001).These treatments also significantly normalized hematological indicators[red blood cells(RBC),white blood cells(WBC),hemoglobin(Hb),and platelets(PLT)]and biochemical indicators[aspartate aminotransferase(AST),alanine aminotransferase(ALT),and alkaline phosphatase(ALP)](P<0.05,P<0.01,or P<0.001).Serum proinflammatory cytokine levels[tumor necrosis factor(TNF)-α,interleukin(IL)-6,IL-12,and thromboxane B2(TXB2)]were markedly decreased,accompanied by restored antioxidant defenses[superoxide dismutase(SOD)and glutathione(GSH)]and reduced oxidative stress markers[malondialdehyde(MDA)and myeloperoxidase(MPO)](P<0.05,P<0.01,or P<0.001).The qRT-PCR analysis demonstrated favorable downregulation of STAT3,mTOR,and nuclear factor kappa-light-chain-enhancer of activated B cells(NF-κB)expression levels in joint tissues in all treatment groups compared with CFA group(P<0.05,P<0.01,or P<0.001).Histopathological findings corroborated these effects,indicating reduced inflammatory infiltration and preservation of joint architecture.Conclusion SG exerts protective effects against RA by modulating key inflammatory and immune pathways.The combined application of SG with FC enhances the therapeutic outcomes,while potentially reducing the corticosteroid-related adverse effects.These findings support SG as a promising adjunctive therapy in RA management,offering favorable efficacy and safety alongside conventional corticosteroid treatment.展开更多
目的探索菝葜皂苷元(SAR)对异氟醚(ISO)麻醉诱导老年大鼠认知功能障碍的影响。方法将大鼠随机分为5组:对照组、1.4%ISO组、1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组,每组12只。对照组和1.4%ISO组大鼠灌胃2 ml 0.5%CMC-Na溶液...目的探索菝葜皂苷元(SAR)对异氟醚(ISO)麻醉诱导老年大鼠认知功能障碍的影响。方法将大鼠随机分为5组:对照组、1.4%ISO组、1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组,每组12只。对照组和1.4%ISO组大鼠灌胃2 ml 0.5%CMC-Na溶液,1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组大鼠依次灌胃2 ml 20、40和80 mg/kg的SAR,共给药7 d。给药第7天时,对照组大鼠正常饲养,其他组大鼠使用1.4%ISO麻醉6 h。麻醉结束24 h后进行Morris水迷宫实验,检测逃避潜伏期(EL)和穿越平台次数(NPC)。对海马组织进行Nissl染色、TUNEL染色和HE染色。检测海马组织丙二醛(MDA)和超氧化物歧化酶(SOD)水平。通过qRT-PCR检测海马组织β-淀粉样前体蛋白裂解酶1(BACE1)、肿瘤坏死因子-α(TNF-α)、白细胞介素-1β(IL-1β)和白细胞介素-6(IL-6)的mRNA水平。通过Western blot检测海马组织BACE1、β-淀粉样蛋白1-42(Aβ1-42)、核因子-κB(NF-κB)p65和NF-κB p-p65的蛋白表达水平。结果与对照组比较,1.4%ISO组大鼠的EL延长(P<0.05),NPC减少(P<0.05),海马组织尼氏体和神经元数量减少,TUNEL阳性率升高(P<0.05),MDA水平升高(P<0.05),SOD水平降低(P<0.05),TNF-α、IL-1β、IL-6和BACE1的mRNA水平均升高(P<0.05),BACE1、Aβ1-42和p-p65的蛋白相对表达量、p-p65/p65均升高(P<0.05)。与1.4%ISO组相比,1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组大鼠的NPC逐渐增加(P<0.05),海马组织尼氏体和神经元数量增多,TUNEL阳性率逐渐降低(P<0.05),MDA水平逐渐降低(P<0.05),TNF-α、IL-1β、IL-6和BACE1的mRNA水平均逐渐降低(P<0.05),BACE1、Aβ1-42和p-p65的蛋白相对表达量、p-p65/p65均逐渐降低(P<0.05)。1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组的EL较1.4%ISO组缩短(P<0.05),1.4%ISO+80SAR组的EL较1.4%ISO+20SAR组和1.4%ISO+40SAR组缩短(P<0.05)。1.4%ISO组SOD水平低于1.4%ISO+20SAR组、1.4%ISO+40SAR组和1.4%ISO+80SAR组(P<0.05),1.4%ISO+20SAR组SOD水平低于1.4%ISO+40SAR组和1.4%ISO+80SAR组(P<0.05)。结论SAR减轻了ISO诱导的老年大鼠认知功能障碍、海马氧化应激和炎症,SAR可能通过抑制BACE1介导的Aβ过度生成和NF-κB信号通路改善ISO诱导的认知功能障碍。展开更多
基金supported by thegrant of Stanley Medical Research Institute(No.02I-005),USA
文摘Objective To identify whether sarsasapogenin, a sapogenin from the Chinese medicinal herb Anemarrhena Asphodeloides Bunge, would augment the efficacy of risperidone and significantly improve cognitive functions in patients with negative symptoms dominated schizophrenia. Methods The trial was a double-blind, placebo-controlled, parallel- group design. The eligible patients were randomized into 2 treatment groups： sarsasapogenin group （sarsasapogenin plus risperidone for 8 weeks, n = 41） and placebo group （risperidone only for 8 weeks, n = 39）. At the baseline, as well as at weeks 2, 4 and 8 of treatment, the therapeutic response was measured by using scales including Positive and Nega- tive Symptoms Scale （PANSS）, Wechsler Memory Scale （WMS）, modified Chinese Wechsler Adult Intelligence Scale （mWAIS）, Clinical Global Impression （CGI） and Brief Psychiatry Rating Scale （BPRS）. The study period for each subject was 8 weeks and duration of overall trial was 2 years. Results Patients treated with sarsasapogenin plus risperidone demonstrated no statistically significant differences in changes in PANSS, WMS or mWAIS score at the end-point of the trial compared with patients treated with placebo plus risperidone. The incidence of treatment-emergent adverse events in patients treated with sarsasapogenin was not different from that observed in placebo group. Conclusion Sarsasapogenin did not augment the efficacy of risperidone in treating negative symptoms dominated schizophrenia. Sarsasapogenin at a dosage of 200 mg per day added to a flexible dosage of risperidone at 2-4 mg per day is safe and well tolerated by patients with negative symptoms dominated schizophrenia.
基金Supported by Technical Innovation Project of Shandong Province(201210916001)
文摘[ Objective ] We aimed to establish the identification method of gardenoside and sarsasapogenin in Qingwen baidu granules. [ Method] With ethyl ace- tate-acetone-formic acid-water （10：7：2：0.5） as the developer and 10% sulfuric acid ethanol solution as the chromogenic reagent, the samples were heated at 100 ~C until the spots were clearly visible, and the existence of gardenoside was checked under natural light. With toluene-acetone（9：l ） as the developer and 5% vanillin sulfuric acid solution as the chromogenic reagent, the samples were heated at 105 ~C until the spots were clearly visible, and the existence of sarsasapogenin was checked under natural light. [Result] Qingwen baidu granules had the same spots with gardenoside and sarsasapogenin at the same Rfvalue under natural light. [ Conclusion] A TLC method detecting gardenoside and sarsasapogenin in Qingwen baidu granules was established, which had good specificity and repeatability, suitable for rapid detection of gardenoside and sarsasapogenin.
基金Supported by Central Talent Training Project for the Reform and Development of Local Colleges and Universities(2020GSP16)Guidance Project of Key R&D Plan in Heilongjiang Province(GZ20220039)Innovation and Entrepreneurship Training Program for College Students in Heilongjiang Province(202310223173).
文摘In this paper,the pharmacological effects and molecular mechanisms of sarsasapogenin,such as anti-oxidant,anti-inflammatory and anti-diabetic effects,are reviewed in order to provide a theoretical basis for the subsequent development and clinical application of sarsasapogenin.
文摘Objective To evaluate the anti-arthritic efficacy of sarsasapogenin(SG)alone and in combination with the corticosteroid fluticasone(FC)in a rat model of rheumatoid arthritis(RA),which was induced by complete Freund’s adjuvant(CFA).Methods Network pharmacology analysis was conducted to identify the potential molecular targets and signaling pathways of SG in RA.Targets were identified with multiple databases,including SwissTargetPrediction,GeneCards,DisGeNET,and Search Tool for the Retrieval of Interacting Genes/Proteins(STRING),and pathway enrichment analysis was performed using Kyoto Encyclopedia of Genes and Genomes(KEGG)and Gene Ontology(GO)databases.Molecular docking was performed to validate the binding affinity of key SG constituents with the predicted hub targets.Male Wistar rats were randomly divided into normal control(NC),CFA,SG,FC,and SG+FC groups(n=6 per group).RA was induced in all groups except NC group by a single intradermal injection of CFA(0.1 mL)into the left hind paw on day 1.After successfully induction of RA(day 12),treatments were administered intradermally from day 12 to 28 as follows:SG(50μg/rat,40μL per paw),FC(50μg/rat,40μL per paw),or a combination of SG and FC(25μg/rat each,total 40μL per paw).Therapeutic outcomes were evaluated via the paw volume,joint diameter,arthritis scores,hematological and biochemical indicators,oxidative stress markers,inflammatory cytokines,and histopathological assessments of rats’ankle joint.The gene expression analysis was performed by quantitative reverse transcription polymerase chain reaction(qRT-PCR).Acute toxicity,body weight,and immune organ indices(spleen and thymus)were also monitored to assess the potential mitigation of SG of corticosteroid-induced adverse effects.Results Network pharmacology analysis revealed 138 potential SG-associated targets,involving 10 key hub genes.KEGG enrichment indicated the participation of pathways involving phosphoinositide-3-kinase regulatory subunit 1(PIK3R1),estrogen receptor 1(ESR1),E1A binding protein P300(EP300),mammalian target of rapamycin(mTOR),C-X-C chemokine receptor type 4(CXCR4),signal transducer and activator of transcription 3(STAT3),and tolllike receptor 4(TLR4).GO enrichment analysis also revealed significant involvement of inflammatory and immune-related biological processes.Molecular docking confirmed strong binding interactions between major SG constituents and the identified hub targets.SG and SG+FC groups preserved body weight,and normalized spleen and thymus indices compared with FC group(P<0.05 or P<0.01),suggesting the mitigation of corticosteroid-induced adverse effects.SG and SG+FC groups significantly reduced paw volume,ankle diameter,and arthritis scores compared with CFA group(P<0.05,P<0.01,or P<0.001).These treatments also significantly normalized hematological indicators[red blood cells(RBC),white blood cells(WBC),hemoglobin(Hb),and platelets(PLT)]and biochemical indicators[aspartate aminotransferase(AST),alanine aminotransferase(ALT),and alkaline phosphatase(ALP)](P<0.05,P<0.01,or P<0.001).Serum proinflammatory cytokine levels[tumor necrosis factor(TNF)-α,interleukin(IL)-6,IL-12,and thromboxane B2(TXB2)]were markedly decreased,accompanied by restored antioxidant defenses[superoxide dismutase(SOD)and glutathione(GSH)]and reduced oxidative stress markers[malondialdehyde(MDA)and myeloperoxidase(MPO)](P<0.05,P<0.01,or P<0.001).The qRT-PCR analysis demonstrated favorable downregulation of STAT3,mTOR,and nuclear factor kappa-light-chain-enhancer of activated B cells(NF-κB)expression levels in joint tissues in all treatment groups compared with CFA group(P<0.05,P<0.01,or P<0.001).Histopathological findings corroborated these effects,indicating reduced inflammatory infiltration and preservation of joint architecture.Conclusion SG exerts protective effects against RA by modulating key inflammatory and immune pathways.The combined application of SG with FC enhances the therapeutic outcomes,while potentially reducing the corticosteroid-related adverse effects.These findings support SG as a promising adjunctive therapy in RA management,offering favorable efficacy and safety alongside conventional corticosteroid treatment.
