Phytosterols are a group of steroids alcohols which had been regarded as a functional factor. An unknown compound in phytosterol samples and phytosterol standard samples was detected by HPLC using symmetry C18 column....Phytosterols are a group of steroids alcohols which had been regarded as a functional factor. An unknown compound in phytosterol samples and phytosterol standard samples was detected by HPLC using symmetry C18 column. The quan- tity of the compound was increased with the enrichment of β-sitosterol. After being collected and analyzed by GC-MS and compared with standard diagram from Wiley and Nist standard chart library, it proved to be γ-sitosterol, a 24β epimer of β-sitosterol.展开更多
A new series of fatty alkenoates were synthesized using an appropriate synthetic route involving DCC and DMAP as catalysts. Compounds were characterized by their spectral data.All the synthesized compounds were evalua...A new series of fatty alkenoates were synthesized using an appropriate synthetic route involving DCC and DMAP as catalysts. Compounds were characterized by their spectral data.All the synthesized compounds were evaluated for their in vitro antimicrobial activity.The minimum inhibitory concentration(MIC),minimum bacterial concentration(MBC) and minimum fungicidal concentration(MFC) were determined for test compounds as well as for reference standards.Among the compounds tested, compounds having hydroxy group at the fatty acid chain showed the most potent antibacterial as well as antifungal activities.展开更多
Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effec...Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effect of isolated compound（β-Sitosterol triacontenate） was investigated by MTT assay on A549 solid tumor cells.Results:IC<sub>50</sub> value of theβ-Sitosterol triacontenate was found to be 1μM.The cytotoxic activity increased in a dose dependent manner in case ofβ-Sitosterol triacontenate.Conclusions:The data therefore provide direct evidence for the role ofβ-Sitosterol triacontenate as a potent antimetastatic agent,which can markedly inhibit the metastatic and invasive capacity of malignant cells.展开更多
The title compound β-sitosterol（C29H50O）, an active phytosterol in many medicinal and edible plants, was characterized by X-ray diffraction analysis and extensive nuclear magnetic resonance（NMR） data. It crystall...The title compound β-sitosterol（C29H50O）, an active phytosterol in many medicinal and edible plants, was characterized by X-ray diffraction analysis and extensive nuclear magnetic resonance（NMR） data. It crystallizes in monoclinic system, space group P21 with C29H50O·1/2H2O, a = 9.4226（7）, b = 7.4824（9）, c = 36.889（3） , V = 2597.0（4） 3, Z = 4, Dx = 1.084 g/cm3, Mr = 423.70, F（000） = 948, and μ = 0.064 mm-1. The final R = 0.0886 and wR = 0.2234 for 10157 observed reflections（I 〉 2σ（I））. The molecular crystal structure of β-sitosterol shows relative stereochemistry of 24R-ethylcholest-5-en-3β-ol. The molecule is composed of one steroid nucleus（3 six-membered rings and 1 five-membered ring） and one sidechain of 10 carbons. There are two C29H50O molecules and one H2O molecule in a symmetrical unit, and the title compound is stacked into a special laminated structure through hydrogen bonds and van der Waal forces. The special laminated structure was first reported.展开更多
The β-sitosterol imprinted polymer was prepared for selective extraction and analysis of β-sitosterol from Old-enlandia diffusa （0. diffusa） followed by HPLC with UV detection. The imprinted polymers show high aff...The β-sitosterol imprinted polymer was prepared for selective extraction and analysis of β-sitosterol from Old-enlandia diffusa （0. diffusa） followed by HPLC with UV detection. The imprinted polymers show high affinity and selectivity to β-sitosterol. Using this molecularly imprinted polymer （MIP） cartridge as solid-phase extraction （SPE） material, the interferences could be quickly washed out and β-sitosterol was selectively retained and enriched. HPLC analysis method was used to evaluate the characteristics of this MIP material. At the condition of mobile phase composed of MeOH/H20/H3PO4 （99/1/0.1, V/V/V, pH=6.0） and the flow rate of 1.0 mL·min -1, a good linear relationship was demonstrated when the concentrations of β-sitosterol were in the range of 0.50--100.0 μg·mL-1. The recoveries ranged from 75.3% to 86.5% and the inter-day and intra-day relative standard deviations were less than 5%. This developed HPLC method was proved to be acceptable for extraction offl-sitosterol from O. diffusa.展开更多
The increasing medicinal importance of 19-norsteroids, particularly for oral contraceptives, has stimulated intensive research to continuously find more economic methods of either partial and total direct synthesis or...The increasing medicinal importance of 19-norsteroids, particularly for oral contraceptives, has stimulated intensive research to continuously find more economic methods of either partial and total direct synthesis or indirect synthesis via estrone of this class of compound.展开更多
目的 通过检测白前Cynanchi Stauntonii Rhizoma et Radix中主要药效成分含量及醇溶性浸出物、总灰分和酸不溶性灰分,建立用于白前质量等级预测的化学计量学及Logistic回归分析方法。方法 对12省36批白前样品进行回流提取,以熊果酸为内...目的 通过检测白前Cynanchi Stauntonii Rhizoma et Radix中主要药效成分含量及醇溶性浸出物、总灰分和酸不溶性灰分,建立用于白前质量等级预测的化学计量学及Logistic回归分析方法。方法 对12省36批白前样品进行回流提取,以熊果酸为内参物,采用一测多评(quantitative analysis of multi-components by single-marker,QAMS)法检测提取物中白薇苷A、白薇苷B、白前苷B、熊果酸、胡萝卜苷、β-谷甾醇含量,并与外标法测得结果进行比较,同时对醇溶性浸出物、总灰分和酸不溶性灰分进行检测;采用化学识别模式、因子分析法及Logistic回归分析建立白前质量优劣评价模型,对其质量差异性进行综合评价。结果 熊果酸为内参物时,相对校正因子耐用性良好,相对保留时间值法可用于色谱峰定位,外标法与QAMS法所得含量结果无明显差异;白薇苷A、白薇苷B、白前苷B、熊果酸、胡萝卜苷、β-谷甾醇6个成分线性范围分别为0.37~9.25、1.56~39.00、1.85~46.25、0.29~7.25、0.58~14.50和1.15~28.75μg/mL,平均加样回收率为97.66%~100.12%,RSD为0.69%~1.51%;主成分分析(principal component analysis,PCA)和正交偏最小二乘判别分析法(orthogonal partial least squares-discriminant analysis,OPLS-DA)能明确区分不同产地的白前药材,提取了2个主成分,3个质量差异因子;因子分析法结果显示36批白前的综合得分在-1.225~0.966,其中S25综合得分最高。Logistic回归模型结果与因子分析法分析结果一致。结论PCA、OPLS-DA、因子分析和Logistic回归模型可以用于评价不同产地白前的质量差异,为白前质量控制提供参考。展开更多
目的:采用网络药理学和分子对接技术探讨鸦胆子抗食管癌、胃癌、肝癌及肺癌的主要成分、作用靶点和信号通路,阐释其共性作用机制。方法:采用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Databas...目的:采用网络药理学和分子对接技术探讨鸦胆子抗食管癌、胃癌、肝癌及肺癌的主要成分、作用靶点和信号通路,阐释其共性作用机制。方法:采用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)筛选鸦胆子的主要成分及其作用靶点;在GeneCards及在线人类孟德尔遗传数据库(online mendelian inheritance in man,OMIM)中搜索食管癌、胃癌、肝癌及肺癌的相关靶点,并筛选出四种癌症的共有靶点;将共有靶点与鸦胆子化合物靶点取交集,筛选出鸦胆子治疗食管癌、胃癌、肝癌及肺癌的潜在靶点;采用Cytoscape 3.10.2构建潜在靶点的蛋白质-蛋白质相互作用(protein-protein interaction,PPI)网络,并采用R语言进行基因本体(Gene Ontology,GO)及京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)信号通路富集分析,构建“活性成分-靶点-通路”网络;将鸦胆子的主要活性成分与鸦胆子抗食管癌、胃癌、肝癌及肺癌的共同核心靶点进行分子对接。结果:鸦胆子筛选得到15个化合物,主要活性成分2个(木犀草素、β-谷甾醇),作用靶点73个。食管癌相关靶点7227个,胃癌相关靶点12919个,肝癌相关靶点16868个,肺癌相关靶点20846个,四者共有的靶点为5458个,与鸦胆子活性成分的共同靶点63个。PPI分析筛选出5个共同核心靶点为AKT1、MAPK1、BAX、TP53、CDKN1A。GO分析得到生物学过程2001个,分子功能110种,细胞组分76种;KEGG分析得到99条信号通路。分子对接结果显示鸦胆子主要活性成分木犀草素、β-谷甾醇与上述5种共同核心靶点具有较好的结合活性,并且结合体构象稳定。结论:鸦胆子对食管癌、胃癌、肝癌及肺癌具有潜在共性作用,该作用可能与活性化合物木犀草素、β-谷甾醇作用于AKT1、MAPK1、TP53、BAX、CDKN1A等靶点,调节PI3K-AKT、p53、细胞凋亡等多种信号通路发挥抑制肿瘤细胞增殖、诱导其凋亡等作用有关。展开更多
文摘Phytosterols are a group of steroids alcohols which had been regarded as a functional factor. An unknown compound in phytosterol samples and phytosterol standard samples was detected by HPLC using symmetry C18 column. The quan- tity of the compound was increased with the enrichment of β-sitosterol. After being collected and analyzed by GC-MS and compared with standard diagram from Wiley and Nist standard chart library, it proved to be γ-sitosterol, a 24β epimer of β-sitosterol.
文摘A new series of fatty alkenoates were synthesized using an appropriate synthetic route involving DCC and DMAP as catalysts. Compounds were characterized by their spectral data.All the synthesized compounds were evaluated for their in vitro antimicrobial activity.The minimum inhibitory concentration(MIC),minimum bacterial concentration(MBC) and minimum fungicidal concentration(MFC) were determined for test compounds as well as for reference standards.Among the compounds tested, compounds having hydroxy group at the fatty acid chain showed the most potent antibacterial as well as antifungal activities.
文摘Objective:To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua（C.decidua）.Methods:The preliminary cytotoxic effect of isolated compound（β-Sitosterol triacontenate） was investigated by MTT assay on A549 solid tumor cells.Results:IC<sub>50</sub> value of theβ-Sitosterol triacontenate was found to be 1μM.The cytotoxic activity increased in a dose dependent manner in case ofβ-Sitosterol triacontenate.Conclusions:The data therefore provide direct evidence for the role ofβ-Sitosterol triacontenate as a potent antimetastatic agent,which can markedly inhibit the metastatic and invasive capacity of malignant cells.
基金Supported by the public welfare research special project in State Administration for Quality Supervision and Inspection and Quarantine(No.201210209)
文摘The title compound β-sitosterol（C29H50O）, an active phytosterol in many medicinal and edible plants, was characterized by X-ray diffraction analysis and extensive nuclear magnetic resonance（NMR） data. It crystallizes in monoclinic system, space group P21 with C29H50O·1/2H2O, a = 9.4226（7）, b = 7.4824（9）, c = 36.889（3） , V = 2597.0（4） 3, Z = 4, Dx = 1.084 g/cm3, Mr = 423.70, F（000） = 948, and μ = 0.064 mm-1. The final R = 0.0886 and wR = 0.2234 for 10157 observed reflections（I 〉 2σ（I））. The molecular crystal structure of β-sitosterol shows relative stereochemistry of 24R-ethylcholest-5-en-3β-ol. The molecule is composed of one steroid nucleus（3 six-membered rings and 1 five-membered ring） and one sidechain of 10 carbons. There are two C29H50O molecules and one H2O molecule in a symmetrical unit, and the title compound is stacked into a special laminated structure through hydrogen bonds and van der Waal forces. The special laminated structure was first reported.
文摘The β-sitosterol imprinted polymer was prepared for selective extraction and analysis of β-sitosterol from Old-enlandia diffusa （0. diffusa） followed by HPLC with UV detection. The imprinted polymers show high affinity and selectivity to β-sitosterol. Using this molecularly imprinted polymer （MIP） cartridge as solid-phase extraction （SPE） material, the interferences could be quickly washed out and β-sitosterol was selectively retained and enriched. HPLC analysis method was used to evaluate the characteristics of this MIP material. At the condition of mobile phase composed of MeOH/H20/H3PO4 （99/1/0.1, V/V/V, pH=6.0） and the flow rate of 1.0 mL·min -1, a good linear relationship was demonstrated when the concentrations of β-sitosterol were in the range of 0.50--100.0 μg·mL-1. The recoveries ranged from 75.3% to 86.5% and the inter-day and intra-day relative standard deviations were less than 5%. This developed HPLC method was proved to be acceptable for extraction offl-sitosterol from O. diffusa.
文摘The increasing medicinal importance of 19-norsteroids, particularly for oral contraceptives, has stimulated intensive research to continuously find more economic methods of either partial and total direct synthesis or indirect synthesis via estrone of this class of compound.
文摘目的 通过检测白前Cynanchi Stauntonii Rhizoma et Radix中主要药效成分含量及醇溶性浸出物、总灰分和酸不溶性灰分,建立用于白前质量等级预测的化学计量学及Logistic回归分析方法。方法 对12省36批白前样品进行回流提取,以熊果酸为内参物,采用一测多评(quantitative analysis of multi-components by single-marker,QAMS)法检测提取物中白薇苷A、白薇苷B、白前苷B、熊果酸、胡萝卜苷、β-谷甾醇含量,并与外标法测得结果进行比较,同时对醇溶性浸出物、总灰分和酸不溶性灰分进行检测;采用化学识别模式、因子分析法及Logistic回归分析建立白前质量优劣评价模型,对其质量差异性进行综合评价。结果 熊果酸为内参物时,相对校正因子耐用性良好,相对保留时间值法可用于色谱峰定位,外标法与QAMS法所得含量结果无明显差异;白薇苷A、白薇苷B、白前苷B、熊果酸、胡萝卜苷、β-谷甾醇6个成分线性范围分别为0.37~9.25、1.56~39.00、1.85~46.25、0.29~7.25、0.58~14.50和1.15~28.75μg/mL,平均加样回收率为97.66%~100.12%,RSD为0.69%~1.51%;主成分分析(principal component analysis,PCA)和正交偏最小二乘判别分析法(orthogonal partial least squares-discriminant analysis,OPLS-DA)能明确区分不同产地的白前药材,提取了2个主成分,3个质量差异因子;因子分析法结果显示36批白前的综合得分在-1.225~0.966,其中S25综合得分最高。Logistic回归模型结果与因子分析法分析结果一致。结论PCA、OPLS-DA、因子分析和Logistic回归模型可以用于评价不同产地白前的质量差异,为白前质量控制提供参考。
文摘目的:采用网络药理学和分子对接技术探讨鸦胆子抗食管癌、胃癌、肝癌及肺癌的主要成分、作用靶点和信号通路,阐释其共性作用机制。方法:采用中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)筛选鸦胆子的主要成分及其作用靶点;在GeneCards及在线人类孟德尔遗传数据库(online mendelian inheritance in man,OMIM)中搜索食管癌、胃癌、肝癌及肺癌的相关靶点,并筛选出四种癌症的共有靶点;将共有靶点与鸦胆子化合物靶点取交集,筛选出鸦胆子治疗食管癌、胃癌、肝癌及肺癌的潜在靶点;采用Cytoscape 3.10.2构建潜在靶点的蛋白质-蛋白质相互作用(protein-protein interaction,PPI)网络,并采用R语言进行基因本体(Gene Ontology,GO)及京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)信号通路富集分析,构建“活性成分-靶点-通路”网络;将鸦胆子的主要活性成分与鸦胆子抗食管癌、胃癌、肝癌及肺癌的共同核心靶点进行分子对接。结果:鸦胆子筛选得到15个化合物,主要活性成分2个(木犀草素、β-谷甾醇),作用靶点73个。食管癌相关靶点7227个,胃癌相关靶点12919个,肝癌相关靶点16868个,肺癌相关靶点20846个,四者共有的靶点为5458个,与鸦胆子活性成分的共同靶点63个。PPI分析筛选出5个共同核心靶点为AKT1、MAPK1、BAX、TP53、CDKN1A。GO分析得到生物学过程2001个,分子功能110种,细胞组分76种;KEGG分析得到99条信号通路。分子对接结果显示鸦胆子主要活性成分木犀草素、β-谷甾醇与上述5种共同核心靶点具有较好的结合活性,并且结合体构象稳定。结论:鸦胆子对食管癌、胃癌、肝癌及肺癌具有潜在共性作用,该作用可能与活性化合物木犀草素、β-谷甾醇作用于AKT1、MAPK1、TP53、BAX、CDKN1A等靶点,调节PI3K-AKT、p53、细胞凋亡等多种信号通路发挥抑制肿瘤细胞增殖、诱导其凋亡等作用有关。
