OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detect...OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.展开更多
Safety of a compound Lonicera rupicola Hook. f. et & Thomson injection was evaluated by local irritation experiments including conjunctiva,skin and muscle irritant experiments,and the effect on weight gain was stu...Safety of a compound Lonicera rupicola Hook. f. et & Thomson injection was evaluated by local irritation experiments including conjunctiva,skin and muscle irritant experiments,and the effect on weight gain was studied. The results showed that the compound L. rupicola Hook. f. et & Thomson injection had no irritation to rabbit eyes and weak irritation to rabbit ears,and had relatively strong irritation to the leg muscles of the mice. Its metabolism in mice had no abnormal toxicity.展开更多
The physical properties and chemical components of three oil samples extracted from Illicium verum Hook. f. by steam distillation （SD）, solvent extraction （SE） and supercritical fluid extraction （SFE） were compa...The physical properties and chemical components of three oil samples extracted from Illicium verum Hook. f. by steam distillation （SD）, solvent extraction （SE） and supercritical fluid extraction （SFE） were compared with one another and analyzed by Gas Chromatography-Mass Spectrometry （GC-MS）. The quality parameters of star anise essential oil from SFE were close to that of those came from SD and SE. Although the extraction yield of star anise by SFE （9.2 %） was close to the value from SE （9.3%）, it was yet higher than that came from SD （8.2%）. For sensory evaluation, however, three oils were significantly different. The odor and taste of the products from SFE and SE were generally more natural and vivid than that came from distilled oil. The volatile compound revealed that significant differences of the composition existed in the distilled oil and the oleoresins prepared by SFE and SE.展开更多
目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R...目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R3软件对2000-2021年雷公藤与类风湿性关机炎相关的英文文献进行文献计量学分析,从机构发文量、作者发文量、关键词以及发展趋势等研究方面进行可视化分析。结果:研究纳入252篇英文文献,2017-2021年发文量占比35.3%,主要集中在亚洲国家及地区,包括中国、日本和中国台湾,而《民族药理学杂志》是发文量最多的英文期刊,发文量最多的作者是以Aiping Lu、Cheng Lu、Cheng Xiao等为代表的团队,研究内容是雷公藤治疗类风湿性关节炎的基础研究及临床应用,共计发文26篇,发文机构主要集中在国内高校,其中中国中医研究院是发文量最多的研究机构,多达42篇,并形成以中国中医科学院、中国药科大学和北京中医药大学为中心的主要发文研究机构。关键词可视化分析显示研究方向主要集中在甲氨蝶呤联合用药、活化作用、定量分析等方面,而未来研究热点主要集中在信号通路、机制研究等方面。结论:雷公藤和类风湿性关节炎相关英文文献发文量逐年上升,预测未来研究热点和发展方向主要集中于调控信号通路和挖掘治疗疾病的基础机制研究方面。目前,雷公藤治疗类风湿性关节炎的研究仍处在发展深入阶段,而相关研究团队应该进一步加强国际间的合作,促进后续该领域研究的发展,并提供参考依据。展开更多
目的阐明藏药长毛风毛菊的药效及化学成分,探讨其有效成分、关键靶点和相关通路,明确其治疗肾性水肿的作用机制。方法将SD大鼠分为空白组、阿霉素诱导肾性水肿模型组,长毛风毛菊给药低剂量组、高剂量组。测定血清生化指标,探讨各组总蛋...目的阐明藏药长毛风毛菊的药效及化学成分,探讨其有效成分、关键靶点和相关通路,明确其治疗肾性水肿的作用机制。方法将SD大鼠分为空白组、阿霉素诱导肾性水肿模型组,长毛风毛菊给药低剂量组、高剂量组。测定血清生化指标,探讨各组总蛋白(total protein,TP)、尿素氮(blood u-rea nitrogen,BUN)、血肌酐(serum creatinine,SCr)、甘油三酯(triglyceride,TG)、总胆固醇(serum total cholestero,TC)、低密度脂蛋白(low density lipoprotein,LDL-C)、高密度脂蛋白(high density lipopro-tein,HDL-C)指标的情况。采用UPLC-Q-TOF-MS/MS技术对藏药长毛风毛菊的化学成分进行分析;在SwissTargetPrediction、GeneCards数据库分别获取长毛风毛菊化学成分靶点和肾性水肿靶点,取交集获得治疗肾性水肿作用靶点;通过STRING数据库进行蛋白互作分析;利用Metascape平台进行gene ontology(GO)功能和京都基因和基因组百科全书(kyoto encyclopedia of genes and genomes,KEGG)通路分析;将药物、靶点等导入到Cytoscape3.7.2构建“药物-成分-靶点-疾病-通路”网络图。筛选出排名靠前的6个基因和12个有效成分,通过分子对接技术验证网络药理预测的准确性,揭示长毛风毛菊治疗肾性水肿的作用机制。结果大鼠血清中TP、HDL-C指标上调,BUN、SCr、TC、TG和LDL-C指标均下调。从藏药长毛风毛菊提取物中共鉴定了71个化合物,包括7个苯丙素类、16个绿原酸类和39个黄酮类等成分。通过预测得出75个长毛风毛菊治疗肾性水肿靶点,GO富集共涉及生物过程、细胞组分、分子功能3个方面,KEGG富集结果显示PI3K/AKT、AGE-RAGE、MAPK等是显著通路。分子对接结果显示,有效成分与关键靶点结合能Vina评分均小于0,高效验证了网络药理预测的准确性。结论该研究基于药效学实验,结合UPLC-Q-TOF-MS/MS鉴定、网络药理学分析和分子对接技术,表明长毛风毛菊能够治疗肾性水肿,可能通过调控PI3K/AKT、AGE-RAGE、MAPK信号通路中TP53、PI3K、AKT等相关靶点来发挥作用。展开更多
Sixty-nine specimens from Tripterygium Wilfordii Hook.f. (TWH) users were investigated by electron microscopy. No macrophages were demonstrated in the 21 specimens collected prior to the administration of TWH. However...Sixty-nine specimens from Tripterygium Wilfordii Hook.f. (TWH) users were investigated by electron microscopy. No macrophages were demonstrated in the 21 specimens collected prior to the administration of TWH. However, it was found in 23 out of the 48 semen specimens obtained following the TWH administration. The macrophages were functionally active as shown by the presence of a large number of cytoplasmic processes and pseudopodia on the surface, and primary and secondary lysosomes in the cytoplasm. The macrophages phagocytized sperm debris and degenerated or dead spermatids with formation of specific phagosomes. Around those macrophages, lymphocytes were commonly noted. The cytoplasmic processes of the two cell types could come into contact or even fuse with each other, leading to tight junction-like structure; in some of the contacts, the plasma membranes were found dissolved so as to form direct cytoplasmic linkage.展开更多
Prostate cancer(PCa)is one of the most common malignant tumours and a leading cause of cancer deaths.Treatment failure of PCa is often due to bone-metastasis.Celastrol,an active constituent of the roots of Tripterygiu...Prostate cancer(PCa)is one of the most common malignant tumours and a leading cause of cancer deaths.Treatment failure of PCa is often due to bone-metastasis.Celastrol,an active constituent of the roots of Tripterygium wilfordii,has shown antitumour effects in previous studies in accordance with its use in TCM.Here we report for the first time an in-depth study of the effects of celastrol on展开更多
文摘OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.
基金Supported by Project of Science and Technology Department of Sichuan Province,China(2016KZ0007)Innovative Scientific Research Project for Postgraduates of Southwest Minzu University(CX2018SZ44)
文摘Safety of a compound Lonicera rupicola Hook. f. et & Thomson injection was evaluated by local irritation experiments including conjunctiva,skin and muscle irritant experiments,and the effect on weight gain was studied. The results showed that the compound L. rupicola Hook. f. et & Thomson injection had no irritation to rabbit eyes and weak irritation to rabbit ears,and had relatively strong irritation to the leg muscles of the mice. Its metabolism in mice had no abnormal toxicity.
基金Supported by the Science and Technology Key Project of Guangxi Province (0424008-1C)
文摘The physical properties and chemical components of three oil samples extracted from Illicium verum Hook. f. by steam distillation （SD）, solvent extraction （SE） and supercritical fluid extraction （SFE） were compared with one another and analyzed by Gas Chromatography-Mass Spectrometry （GC-MS）. The quality parameters of star anise essential oil from SFE were close to that of those came from SD and SE. Although the extraction yield of star anise by SFE （9.2 %） was close to the value from SE （9.3%）, it was yet higher than that came from SD （8.2%）. For sensory evaluation, however, three oils were significantly different. The odor and taste of the products from SFE and SE were generally more natural and vivid than that came from distilled oil. The volatile compound revealed that significant differences of the composition existed in the distilled oil and the oleoresins prepared by SFE and SE.
文摘目的:通过分析雷公藤治疗类风湿性关节炎的相关英文文献,归纳该领域的研究热点,总结发展趋势,为后续雷公藤治疗类风湿性关节炎的进一步研究提供参考。方法:以Web of Science、Wiley Online Library和Embase数据库,基于CiteSpace V 5.8.R3软件对2000-2021年雷公藤与类风湿性关机炎相关的英文文献进行文献计量学分析,从机构发文量、作者发文量、关键词以及发展趋势等研究方面进行可视化分析。结果:研究纳入252篇英文文献,2017-2021年发文量占比35.3%,主要集中在亚洲国家及地区,包括中国、日本和中国台湾,而《民族药理学杂志》是发文量最多的英文期刊,发文量最多的作者是以Aiping Lu、Cheng Lu、Cheng Xiao等为代表的团队,研究内容是雷公藤治疗类风湿性关节炎的基础研究及临床应用,共计发文26篇,发文机构主要集中在国内高校,其中中国中医研究院是发文量最多的研究机构,多达42篇,并形成以中国中医科学院、中国药科大学和北京中医药大学为中心的主要发文研究机构。关键词可视化分析显示研究方向主要集中在甲氨蝶呤联合用药、活化作用、定量分析等方面,而未来研究热点主要集中在信号通路、机制研究等方面。结论:雷公藤和类风湿性关节炎相关英文文献发文量逐年上升,预测未来研究热点和发展方向主要集中于调控信号通路和挖掘治疗疾病的基础机制研究方面。目前,雷公藤治疗类风湿性关节炎的研究仍处在发展深入阶段,而相关研究团队应该进一步加强国际间的合作,促进后续该领域研究的发展,并提供参考依据。
文摘目的阐明藏药长毛风毛菊的药效及化学成分,探讨其有效成分、关键靶点和相关通路,明确其治疗肾性水肿的作用机制。方法将SD大鼠分为空白组、阿霉素诱导肾性水肿模型组,长毛风毛菊给药低剂量组、高剂量组。测定血清生化指标,探讨各组总蛋白(total protein,TP)、尿素氮(blood u-rea nitrogen,BUN)、血肌酐(serum creatinine,SCr)、甘油三酯(triglyceride,TG)、总胆固醇(serum total cholestero,TC)、低密度脂蛋白(low density lipoprotein,LDL-C)、高密度脂蛋白(high density lipopro-tein,HDL-C)指标的情况。采用UPLC-Q-TOF-MS/MS技术对藏药长毛风毛菊的化学成分进行分析;在SwissTargetPrediction、GeneCards数据库分别获取长毛风毛菊化学成分靶点和肾性水肿靶点,取交集获得治疗肾性水肿作用靶点;通过STRING数据库进行蛋白互作分析;利用Metascape平台进行gene ontology(GO)功能和京都基因和基因组百科全书(kyoto encyclopedia of genes and genomes,KEGG)通路分析;将药物、靶点等导入到Cytoscape3.7.2构建“药物-成分-靶点-疾病-通路”网络图。筛选出排名靠前的6个基因和12个有效成分,通过分子对接技术验证网络药理预测的准确性,揭示长毛风毛菊治疗肾性水肿的作用机制。结果大鼠血清中TP、HDL-C指标上调,BUN、SCr、TC、TG和LDL-C指标均下调。从藏药长毛风毛菊提取物中共鉴定了71个化合物,包括7个苯丙素类、16个绿原酸类和39个黄酮类等成分。通过预测得出75个长毛风毛菊治疗肾性水肿靶点,GO富集共涉及生物过程、细胞组分、分子功能3个方面,KEGG富集结果显示PI3K/AKT、AGE-RAGE、MAPK等是显著通路。分子对接结果显示,有效成分与关键靶点结合能Vina评分均小于0,高效验证了网络药理预测的准确性。结论该研究基于药效学实验,结合UPLC-Q-TOF-MS/MS鉴定、网络药理学分析和分子对接技术,表明长毛风毛菊能够治疗肾性水肿,可能通过调控PI3K/AKT、AGE-RAGE、MAPK信号通路中TP53、PI3K、AKT等相关靶点来发挥作用。
基金The work reported in this paper was supported by the State Family Planning commission
文摘Sixty-nine specimens from Tripterygium Wilfordii Hook.f. (TWH) users were investigated by electron microscopy. No macrophages were demonstrated in the 21 specimens collected prior to the administration of TWH. However, it was found in 23 out of the 48 semen specimens obtained following the TWH administration. The macrophages were functionally active as shown by the presence of a large number of cytoplasmic processes and pseudopodia on the surface, and primary and secondary lysosomes in the cytoplasm. The macrophages phagocytized sperm debris and degenerated or dead spermatids with formation of specific phagosomes. Around those macrophages, lymphocytes were commonly noted. The cytoplasmic processes of the two cell types could come into contact or even fuse with each other, leading to tight junction-like structure; in some of the contacts, the plasma membranes were found dissolved so as to form direct cytoplasmic linkage.
文摘Prostate cancer(PCa)is one of the most common malignant tumours and a leading cause of cancer deaths.Treatment failure of PCa is often due to bone-metastasis.Celastrol,an active constituent of the roots of Tripterygium wilfordii,has shown antitumour effects in previous studies in accordance with its use in TCM.Here we report for the first time an in-depth study of the effects of celastrol on
