Objective: In this study, one of the objectives was to investigate the total flavonoid contents of Fupenzi (R. chingii Hu.) obtained from different regions of China and to evaluate their anatioxidant activities. And t...Objective: In this study, one of the objectives was to investigate the total flavonoid contents of Fupenzi (R. chingii Hu.) obtained from different regions of China and to evaluate their anatioxidant activities. And the second objective of this study was to develop a validated HPLC method for chromatographic fingerprints of the samples extracts of Fupenzi. Method: The total flavonoid contents were determined by a colorimetric method and the antioxidant activity was determined spectrophotometrically by DPPH and ABTS radical scavenging assays. The chromatographic fingerprint was developed by high-performance liquid chromatography coupled with diode array detection for the control of Fupenzi. Results: A significant correlation between antioxidant activity and the total flavonoid content was observed for the DPPH assay (r2 = 0.758, ρ = 0.004) and the ABTS assay (r2 = 0.788, ρ = 0.002). Under the optimized chromatographic conditions, the validated method was successfully applied to assessment of chemical fingerprinting of 12 batches of FPZ collected from different regions of China. Comparisons of the chromatograms showed that 15 characteristic peaks could be selected as markers for identification and evaluation of Fupenzi. In addition, the proposed method was also successfully applied to simultaneous determination of five compounds (including puerarin, rutin, hyperin, quercetin and kaempferol) in these samples. Conclusions: The qualitative and quantitative analysis described in this paper could be used for identification and evaluation of Fupenzi.展开更多
Rubus chingii Hu, a member of the rosaceae family, is extensively distributed in China and Japan. Its unripe fruits(Fupenzi in Chinese) have a long history of use as an herbal tonic in traditional Chinese medicine for...Rubus chingii Hu, a member of the rosaceae family, is extensively distributed in China and Japan. Its unripe fruits(Fupenzi in Chinese) have a long history of use as an herbal tonic in traditional Chinese medicine for treating various diseases commonly associated with kidney deficiency, and they are still in use today. Phytochemical investigations on the fruits and leaves of R. chingii indicate the presence of terpenoids, flavonoids, steroids, alkaloids, phenylpropanoids, phenolics, and organic acids. Extracts or active substances from this plant are reported to have various pharmacological properties, including antioxidant, anti-inflammatory, antitumor, antifungal, antithrombotic, antiosteoporotic, hypoglycemic, and central nervous system-regulating effects. This review provides up-to-date information on the botanical characterizations, traditional usages, chemical constituents, pharmacological activities, toxicity,and quality control of R. chingii. Possible directions for future research are also briefly proposed. This review aims to supply fundamental data for the further study of R. chingii and contribute to the development of its clinical use.展开更多
Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a...Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a kind of dietary traditional Chinese medicine. The methanolic extract of R. chingii fruits exhibited significant PTP1 B inhibitory activity. Further bioactivity-guided fractionation resulted in the isolation of three PTP1 B inhibitory ursane-type triterpenes: ursolic acid(1), 2-oxopomolic acid(2), and 2α, 19α-dihydroxy-3-oxo-urs-12-en-28-oic acid(3). Kinetics analyses revealed that 1 was a non-competitive PTP1 B inhibitor, and 2 and 3 were mixed type PTP1 B inhibitors. Compounds 1-3 and structurally related triterpenes(4-8) were further analyzed the structure-activity relationship, and were evaluated the inhibitory selectivity against four homologous protein tyrosine phosphatases(TCPTP, VHR, SHP-1 and SHP-2). Molecular docking simulations were also carried out, and the result indicated that 1, 3-acetoxyurs-12-ene-28-oic acid(5), and pomolic acid-3β-acetate(6) bound at the allosteric site including α3, α6, and α7 helix of PTP1 B.展开更多
Objective To develop a simple,efficient,and reliable method for routine quantitative analysis of main constituents presented in the fruits of Rubus chingii,which is widely used in Chinese materia medica(CMM),known as ...Objective To develop a simple,efficient,and reliable method for routine quantitative analysis of main constituents presented in the fruits of Rubus chingii,which is widely used in Chinese materia medica(CMM),known as Fupenzi(FPZ) in Chinese.Methods An ultra performance liquid chromatography-photo diode array(UPLC-PDA) system was employed for simultaneous quantification of eight compounds,i.e.adenosine,gallic acid,brevifolin carboxylic acid,ethyl gallate,ellagic acid,kaempferol-3-O-rutinoside,kaempferol-3-O-β-D-glucopyranoside,and tiliroside.The chromatographic analysis was performed on a C_(18) column using a gradient elution of acetonitrile-0.1%formic acid aqueous solution within a runtime of 25 min.Results All calibration curves were linear(R^2> 0.9997) over the tested ranges.The intra- and inter-day precisions as determined from sample solutions were both less than 2.45%and 2.78%,respectively.The average recoveries for the eight constituents ranged from 94.77%to 101.35%with RSD ≤ 4.41%.The newly-developed method was applied to the quality assessment of various R.chingii samples,including both ripe and unripe fruits of R.chingii from different habitats.Conclusion The relative levels of the investigated compounds vary remarkably in the fruits of R.chingii collected from different habitats.As only two of the eight compounds,adenosine and ellagic acid,are determined in the ripe fruits of R.chingii,the results may explain the reason why only the unripe fruits can be used in CMM.展开更多
单宁类化合物是覆盆子的主要活性成分,具有降血糖、降血脂、抗炎、延缓衰老及预防心脑血管疾病等功能。本实验从覆盆子中提取富集单宁,通过体外模拟消化模型探究覆盆子单宁富集组分消化前后单宁含量及抗氧化活性、α-葡萄糖苷酶抑制活...单宁类化合物是覆盆子的主要活性成分,具有降血糖、降血脂、抗炎、延缓衰老及预防心脑血管疾病等功能。本实验从覆盆子中提取富集单宁,通过体外模拟消化模型探究覆盆子单宁富集组分消化前后单宁含量及抗氧化活性、α-葡萄糖苷酶抑制活性变化,通过体外厌氧发酵模型分析模拟消化对其肠道菌群调节作用的影响,最后采用超高效液相色谱-四极杆飞行时间串联质谱法(ultra-high performance liquid chromatography-quadrupole time offlight-tandem mass spectrometry,UPLC-ESI-QTOF-MS/MS)比较体外消化和酵解产物中单宁组成及其代谢产物含量变化情况。结果表明,在胃、肠消化过程中水解单宁含量均呈先增加后降低趋势,胃肠消化提升了覆盆子单宁富集组分的1,1-二苯基-2-三硝基苯肼自由基清除能力(半抑制质量浓度为29.15~39.65µg/mL),但对2,2’-联氮基-双(3-乙基苯并噻唑啉-6-磺酸)阳离子自由基清除能力无显著性影响(P>0.05),经肠道模拟消化后,样品的α-葡萄糖苷酶抑制能力提升了7.16~7.86倍。体外结肠发酵实验结果表明,覆盆子单宁显著增加了粪球菌属(Coprococcus)、丁酸弧菌(Anaerostipes)、瘤胃球菌属(Ruminococcus)、粪便杆菌属(Faecalibaterium)等有益菌的相对丰度,胃肠模拟消化降低其对双歧杆菌等有益菌的改善效果。UPLC-ESI-QTOF-MS/MS分析结果表明,胃、肠消化过程中,单宁代谢物含量均呈现先下降后上升的趋势,结肠发酵后样品中的尿石素A和尿石素B含量明显下降,而尿石素C和尿石素D未检测到。本研究可为覆盆子单宁稳态递送体系的构建,提高其体内的生物利用率提供理论依据。展开更多
文摘Objective: In this study, one of the objectives was to investigate the total flavonoid contents of Fupenzi (R. chingii Hu.) obtained from different regions of China and to evaluate their anatioxidant activities. And the second objective of this study was to develop a validated HPLC method for chromatographic fingerprints of the samples extracts of Fupenzi. Method: The total flavonoid contents were determined by a colorimetric method and the antioxidant activity was determined spectrophotometrically by DPPH and ABTS radical scavenging assays. The chromatographic fingerprint was developed by high-performance liquid chromatography coupled with diode array detection for the control of Fupenzi. Results: A significant correlation between antioxidant activity and the total flavonoid content was observed for the DPPH assay (r2 = 0.758, ρ = 0.004) and the ABTS assay (r2 = 0.788, ρ = 0.002). Under the optimized chromatographic conditions, the validated method was successfully applied to assessment of chemical fingerprinting of 12 batches of FPZ collected from different regions of China. Comparisons of the chromatograms showed that 15 characteristic peaks could be selected as markers for identification and evaluation of Fupenzi. In addition, the proposed method was also successfully applied to simultaneous determination of five compounds (including puerarin, rutin, hyperin, quercetin and kaempferol) in these samples. Conclusions: The qualitative and quantitative analysis described in this paper could be used for identification and evaluation of Fupenzi.
基金the National Natural Science Foundation of China(No.81803794)the Program for Excellent Talents in Zhejiang Chinese Medical University(No.112123A12201/001/004/019)。
文摘Rubus chingii Hu, a member of the rosaceae family, is extensively distributed in China and Japan. Its unripe fruits(Fupenzi in Chinese) have a long history of use as an herbal tonic in traditional Chinese medicine for treating various diseases commonly associated with kidney deficiency, and they are still in use today. Phytochemical investigations on the fruits and leaves of R. chingii indicate the presence of terpenoids, flavonoids, steroids, alkaloids, phenylpropanoids, phenolics, and organic acids. Extracts or active substances from this plant are reported to have various pharmacological properties, including antioxidant, anti-inflammatory, antitumor, antifungal, antithrombotic, antiosteoporotic, hypoglycemic, and central nervous system-regulating effects. This review provides up-to-date information on the botanical characterizations, traditional usages, chemical constituents, pharmacological activities, toxicity,and quality control of R. chingii. Possible directions for future research are also briefly proposed. This review aims to supply fundamental data for the further study of R. chingii and contribute to the development of its clinical use.
基金supported by the National Natural Science Foundation of China(No.81628012)
文摘Protein tyrosine phosphatase 1 B(PTP1 B) has led to an intense interest in developing its inhibitors as anti-diabetes, anti-obesity and anti-cancer agents. The fruits of Rubus chingii(Chinese raspberry) were used as a kind of dietary traditional Chinese medicine. The methanolic extract of R. chingii fruits exhibited significant PTP1 B inhibitory activity. Further bioactivity-guided fractionation resulted in the isolation of three PTP1 B inhibitory ursane-type triterpenes: ursolic acid(1), 2-oxopomolic acid(2), and 2α, 19α-dihydroxy-3-oxo-urs-12-en-28-oic acid(3). Kinetics analyses revealed that 1 was a non-competitive PTP1 B inhibitor, and 2 and 3 were mixed type PTP1 B inhibitors. Compounds 1-3 and structurally related triterpenes(4-8) were further analyzed the structure-activity relationship, and were evaluated the inhibitory selectivity against four homologous protein tyrosine phosphatases(TCPTP, VHR, SHP-1 and SHP-2). Molecular docking simulations were also carried out, and the result indicated that 1, 3-acetoxyurs-12-ene-28-oic acid(5), and pomolic acid-3β-acetate(6) bound at the allosteric site including α3, α6, and α7 helix of PTP1 B.
基金National Science and Technology Major Project for"Major New Drugs Innovation and Development"(2015ZX09J15102-004-004)
文摘Objective To develop a simple,efficient,and reliable method for routine quantitative analysis of main constituents presented in the fruits of Rubus chingii,which is widely used in Chinese materia medica(CMM),known as Fupenzi(FPZ) in Chinese.Methods An ultra performance liquid chromatography-photo diode array(UPLC-PDA) system was employed for simultaneous quantification of eight compounds,i.e.adenosine,gallic acid,brevifolin carboxylic acid,ethyl gallate,ellagic acid,kaempferol-3-O-rutinoside,kaempferol-3-O-β-D-glucopyranoside,and tiliroside.The chromatographic analysis was performed on a C_(18) column using a gradient elution of acetonitrile-0.1%formic acid aqueous solution within a runtime of 25 min.Results All calibration curves were linear(R^2> 0.9997) over the tested ranges.The intra- and inter-day precisions as determined from sample solutions were both less than 2.45%and 2.78%,respectively.The average recoveries for the eight constituents ranged from 94.77%to 101.35%with RSD ≤ 4.41%.The newly-developed method was applied to the quality assessment of various R.chingii samples,including both ripe and unripe fruits of R.chingii from different habitats.Conclusion The relative levels of the investigated compounds vary remarkably in the fruits of R.chingii collected from different habitats.As only two of the eight compounds,adenosine and ellagic acid,are determined in the ripe fruits of R.chingii,the results may explain the reason why only the unripe fruits can be used in CMM.
文摘单宁类化合物是覆盆子的主要活性成分,具有降血糖、降血脂、抗炎、延缓衰老及预防心脑血管疾病等功能。本实验从覆盆子中提取富集单宁,通过体外模拟消化模型探究覆盆子单宁富集组分消化前后单宁含量及抗氧化活性、α-葡萄糖苷酶抑制活性变化,通过体外厌氧发酵模型分析模拟消化对其肠道菌群调节作用的影响,最后采用超高效液相色谱-四极杆飞行时间串联质谱法(ultra-high performance liquid chromatography-quadrupole time offlight-tandem mass spectrometry,UPLC-ESI-QTOF-MS/MS)比较体外消化和酵解产物中单宁组成及其代谢产物含量变化情况。结果表明,在胃、肠消化过程中水解单宁含量均呈先增加后降低趋势,胃肠消化提升了覆盆子单宁富集组分的1,1-二苯基-2-三硝基苯肼自由基清除能力(半抑制质量浓度为29.15~39.65µg/mL),但对2,2’-联氮基-双(3-乙基苯并噻唑啉-6-磺酸)阳离子自由基清除能力无显著性影响(P>0.05),经肠道模拟消化后,样品的α-葡萄糖苷酶抑制能力提升了7.16~7.86倍。体外结肠发酵实验结果表明,覆盆子单宁显著增加了粪球菌属(Coprococcus)、丁酸弧菌(Anaerostipes)、瘤胃球菌属(Ruminococcus)、粪便杆菌属(Faecalibaterium)等有益菌的相对丰度,胃肠模拟消化降低其对双歧杆菌等有益菌的改善效果。UPLC-ESI-QTOF-MS/MS分析结果表明,胃、肠消化过程中,单宁代谢物含量均呈现先下降后上升的趋势,结肠发酵后样品中的尿石素A和尿石素B含量明显下降,而尿石素C和尿石素D未检测到。本研究可为覆盆子单宁稳态递送体系的构建,提高其体内的生物利用率提供理论依据。
