灰树花子实体醇提物生物活性研究

对灰树花子实体95%乙醇提取物的不同萃取分部(石油醚分部、氯仿分部、乙酸乙酯分部、正丁醇分部和剩余分部)进行了化学成分的定性检验和体外抗肿瘤、抑制DPP-IV酶的活性研究。结果表明:灰树花子实体的醇提取物中可能含有生物碱、氨基酸或蛋白、有机酸、酚类或鞣质、甾体、蒽醌等物质。石油醚分部、氯仿分部、乙酸乙酯分部和正丁醇分部对正常细胞WPMY-1的增殖无抑制作用而对三种肿瘤细胞L1210、SW620、K562全部或部分的增殖有一定的抑制作用,其中氯仿分部对L1210细胞增殖的抑制作用最强,其IC50达到0.13μg/m L。这说明这四个分部具有抗肿瘤活性。剩余分部对肿瘤细胞L1210、K562和正常细胞WPMY-1的增殖均具有抑制作用,说明该分部可能具有细胞毒性。灰树花子实体的氯仿分部、乙酸乙酯分部和正丁醇分部具有较强的抑制DPP-IV酶的活性,这三个萃取分部对DPP-IV酶抑制的IC50分别为497.33、776.51、704.24μg/m L,该结果说明此三个分部具有降血糖的潜力。     

不同生长期草菇提取物的生物活性研究

对草菇不同生长期的菌丝体及子实体分别用95%乙醇提取,对获得的5个提取物进行了化学成分定性检验、HPLC图谱分析和体外抗肿瘤、抑制DPP-IV酶的活性研究。结果表明：草菇不同生长期的菌丝体及子实体中均含有生物碱、有机酸、甾类（或三萜）、糖类、氨基酸（蛋白）等物质。草菇4个生长期的菌丝体醇提物对正常细胞WPMY-1的增殖无抑制作用而对3种肿瘤细胞L1210、SW620、K562全部或部分的增殖有一定的抑制作用。说明这4个生长期的菌丝体醇提物具有抗肿瘤活性。子实体95%醇提物对肿瘤细胞L1210、SW620、K562和正常细胞WPMY-1的增殖均具有抑制作用,说明该部分可能具有细胞毒性。草菇不同生长期的菌丝体和子实体提取物均有一定抑制DPP-IV酶的活性,其中生长2周的菌丝体醇提物对DPP-IV酶的抑制活性较强,IC₅₀值达到0.32mg/mL,该结果说明生长2周的草菇菌丝体具有最佳的抗肿瘤和降血糖潜力。     

桑黄菌丝体和子实体中次级代谢产物及其活性的比较

研究桑黄发酵菌丝体次级代谢产物及活性与子实体的差异性,探讨其替代子实体的可能性。研究通过高效液相色谱分析和化学法比较菌丝体和子实体石油醚、氯仿、乙酸乙酯和正丁醇4个萃取相中的成分差异,以二苯基三硝基苯肼自由基（DPPH）清除率和Trolox当量抗氧化能力（TEAC）作为抗氧化活性的指标、HepG2和MCF-7癌细胞的抑制率作为抑制肿瘤细胞生长的指标,比较其活性差异。结果表明,菌丝体和子实体4个萃取相在化学成分上存在差异;在活性方面,菌丝体各萃取相的抗氧化活性高于子实体,而子实体抗肿瘤活性优于菌丝体。菌丝体醇提取的总黄酮含量高于子实体醇提物,抗氧化活性和总黄酮含量有显著相关性,发酵菌丝体在抗氧化活性方面具有替代子实体的可行性。     

草菇培养物中粗三萜和黄酮含量及抗氧化抗肿瘤活性研究

采用液体摇瓶法培养草菇菌丝体,并用不同有机溶剂对培养液及菌丝体中的代谢成分分别进行分离提取,获得了不同来源的次生代谢提取物。对各提取物的成分分析表明,石油醚相、乙酸乙酯相和乙醇相提取物中均含有粗三萜和黄酮类物质,但菌丝体提取物中粗三萜和黄酮含量明显高于培养液提取物中的含量。石油醚抽提菌丝体获得的提取物中粗三萜含量最高,达17%,而乙酸乙酯抽提菌丝体获得的提取物中黄酮含量最高,达9.31%。抗氧化活性检测结果显示,石油醚相、乙酸乙酯相、乙醇相中的代谢提取物均有较高的抗氧化活性,但乙酸乙酯相提取物的抗氧化活性明显高于石油醚相提取物,具最高抗氧化活性的提取物分别来自乙酸乙酯、乙醇对菌丝体的抽提物。MTT法检测各提取物对胃癌细胞增殖的抑制作用,结果显示各组分均有较高的抗肿瘤活性,且抗肿瘤活性与提取物浓度存在明显的量效关系。     

草菇培养物中粗三萜和黄酮含量及抗氧化抗肿瘤活性研究

采用液体摇瓶法培养草菇菌丝体,并用不同有机溶剂对培养液及菌丝体中的代谢成分分别进行分离提取,获得了不同来源的次生代谢提取物。对各提取物的成分分析表明,石油醚相、乙酸乙酯相和乙醇相提取物中均含有粗三萜和黄酮类物质,但菌丝体提取物中粗三萜和黄酮含量明显高于培养液提取物中的含量。石油醚抽提菌丝体获得的提取物中粗三萜含量最高,达17%,而乙酸乙酯抽提菌丝体获得的提取物中黄酮含量最高,达9.31%。抗氧化活性检测结果显示,石油醚相、乙酸乙酯相、乙醇相中的代谢提取物均有较高的抗氧化活性,但乙酸乙酯相提取物的抗氧化活性明显高于石油醚相提取物,具最高抗氧化活性的提取物分别来自乙酸乙酯、乙醇对菌丝体的抽提物。MTT法检测各提取物对胃癌细胞增殖的抑制作用,结果显示各组分均有较高的抗肿瘤活性,且抗肿瘤活性与提取物浓度存在明显的量效关系。     

小桐子提取物除草活性的生物测定

为全面了解小桐子(Jatropha curcas L. )提取物的除草活性,以萝卜(Raphanus sativus L. )、苋(Amaranthus tricolor L. )、苏丹草[Sorghum sudanense (Piper) Stapf]和黑麦草(Lolium perenne L. )为实验材料,对小桐子果壳和枝叶的水、乙醇(体积分数95%)、正丁醇、乙酸乙酯、氯仿和石油醚粗提物的除草活性进行了生物测定,并从中筛选出抑制作用最强的水粗提物进行进一步的活性组分分离及其除草活性的生物测定.测定结果显示,小桐子果壳和枝叶的6种溶剂提取物(10 g·L~(-1))对供试的4种植物幼苗的根长和茎高均有不同程度的抑制作用,其中水粗提物和乙醇(体积分数95%)粗提物的抑制作用较强,且水粗提物对供试的4种植物幼苗的根长和茎高的抑制作用均在75%以上,显著高于其他溶剂粗提物(P<0.05);石油醚粗提物的抑制作用最小,均在10%以下.小桐子果壳和枝叶水粗提物的石油醚、氯仿、乙酸乙酯、正丁醇和水萃取物(10 g·L~(-1))对萝卜和苏丹草幼苗的根长和茎高均有不同程度的抑制作用,其中水、正丁醇和乙酸乙酯萃取物的抑制作用显著高于氯仿和石油醚萃取物,抑制率均在70%以上;水萃取物的抑制作用最强,抑制率均在80%以上;石油醚萃取物的抑制作用最小,抑制率均在10%以下.研究结果表明,小桐子果壳和枝叶的水粗提物具有一定的除草活性,其有效成分为极性较大的组分.     

小珊瑚藻对赤潮异弯藻的化感效应

研究了不同浓度的小珊瑚藻组织4种不同极性有机溶剂(甲醇、丙酮、乙醚、氯仿)提取物对赤潮异弯藻的生长抑制作用.结果表明：小珊瑚藻组织甲醇提取物对赤潮异弯藻的生长抑制活性最强,并且在较高浓度下能使赤潮异弯藻完全死亡,其他3种有机溶剂提取物对赤潮异弯藻的生长无明显影响.表明小珊瑚藻组织中含有的对赤潮异弯藻有抑制作用的活性物质具有较高的极性.对小珊瑚藻的甲醇提取物进行液液萃取,将其分离为石油醚相、乙酸乙酯相、正丁醇相和蒸馏水相, 并对赤潮异弯藻进行生物活性检测.结果发现石油醚相和乙酸乙酯相具有较强的杀藻活性,表明脂肪酸可能是小珊瑚藻组织内抑制赤潮异弯藻生长的化感物质的重要组成成分之一.     

野葛花醇提物中异黄酮含量及其抗氧化活性测定

以葛花苷为标准品,对野葛花醇提物的氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分中的异黄酮含量进行测定,并采用DPPH·法对各萃取物进行自由基清除实验.结果显示,(1)氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分的异黄酮含量分别为35.27%、53.42%、52.13%和2.34%.(2)抗氧化实验显示, 4 部分清除DPPH·的IC50值分别为252、49、197和344 μg/mL.(3)相关性分析表明,野葛花醇提物各萃取部分的抗氧化活性主要来自于其中含有的异黄酮类化合物.研究表明野葛花醇提物的乙酸乙酯和正丁醇萃取部分异黄酮含量较高;氯仿、乙酸乙酯、正丁醇萃取物及水溶物4部分对DPPH自由基均有一定的清除作用,其中以乙酸乙酯萃取物的效果最佳;表明异黄酮是一种天然的抗氧化剂,具有较强的抗氧化作用.     

复方枳葛橘提取物体外抗氧化活性评价(英文)

复方枳葛橘水提液依次用氯仿、乙酸乙酯和正丁醇萃取,与水层得到4个不同极性部位萃取物,以清除DPPH·、ABTS+·,以及络合Fe2+能力,综合评价其抗氧化作用;采用芦丁显色法检测各部位总黄酮含量,并分析黄酮类物质含量与抗氧化活性的相关性;采用HPLC法分析其抗氧化能力较强部位可能的化学成分。结果显示4个不同极性部位均具有不同程度的抗氧化能力,其中乙酸乙酯部位抗氧化能力最强,其次是正丁醇、水层,而氯仿层较弱;其抗氧化能力与总黄酮含量呈正相关,且与黄酮类化合物结构类型相关;HPLC分析结果显示乙酸乙酯合并正丁醇部位主要成分为柚皮苷、野漆树苷和槲皮素等黄酮类化合物。复方枳葛橘提取物可以作为天然抗氧化剂用于药物研究和相关疾病的防治。     

担子菌黄硬皮马勃杀虫活性研究

研究了担子菌黄硬皮马勃 SclerodermacitrinumPer. 子实体提取物对3龄粘虫的杀虫活性.黄硬皮马勃甲醇-氯仿总浸膏及其石油醚萃取物在浓度为25mg·mL-1时,对3龄粘虫的48h拒食率分别为96.8%和81.3%,而其氯仿及正丁醇萃取物的拒食活性相对较弱;石油醚浸膏具有较强的毒杀作用,在浓度10mg·mL-1时,3龄粘虫的48h校正死亡率均大于80%;石油醚萃取物的触杀活性相对较弱,25mg·mL-1剂量对3龄粘虫7d内的校正死亡率小于60.0%.     

Anti-inflammatory activities of triterpenoid saponins from Polygala japonica

Bioassay-guided investigation was performed to identify the active constituents from a methanol extract of Polygala japonica, a folk medicinal plant widely used in China to treat inflammatory diseases. The n-BuOH and EtOAc fractions of the P. japonica methanol extract, which show significant anti-inflammatory activity in in vivo test, were further subjected to column chromatography to afford six triterpene glycosides, marked here as saponins 1–6. All compounds were evaluated for their anti-inflammatory activity in the carageenan-induced mouse paw edema test, and saponins 1, 4 and 5 showed significantly anti-inflammatory effects on both phases of carageenan-induced acute paw edema in mice. Saponin 5 was also found to significantly inhibit the production of inflammatory mediators – nitric oxide (NO) in LPS-stimulated RAW264.7 macrophages, with no obvious effects on macrophage viability.     

瓜果腐霉菌丝中除草活性物质的初步研究

将瓜果腐霉进行液体发酵,其菌丝用等体积乙酸乙酯和甲醇进行依次萃取,甲醇萃取液旋转蒸发去溶剂后进行硅胶柱层析,以乙酸乙酯和石油醚(V/V=3:1和V/V=2:1)的混合液进行梯度洗脱,每50 mL收集为一个馏分,共收集到40个馏分。生物测定结果表明,以乙酸乙酯和石油醚(V/V=2:1)洗脱得到的馏分21 24对供试杂草马唐表现出了较强的活性,其对马唐的生长抑制作用均为4级。合并馏分21 24,以乙酸乙酯和石油醚(V/V=2:1)的混合液为展开剂进行等度洗脱,每50 mL收集为一个馏分,共收集到20个馏分。生物测定结果表明,馏分3对马唐有较强的抑制活性。HPLC分析发现,该馏分主要含有3个组分,其保留时间分别为12.7、14.0和30.5 min。     

猴头菌子实体小分子提取物的分离与体外抑制幽门螺旋杆菌的分析

本研究以甲硝唑为阳性对照,利用HPD-100大孔树脂和95%乙醇将猴头菌子实体中小分子活性物质进行富集,得到乙醇制备液（MREEs）;然后对乙醇制备液分别使用石油醚（60-90℃）和氯仿进行多次萃取,得到石油醚萃取物（A1、A2）和氯仿萃取物（B）,并进行GC-MS测定;对MREEs和A1、A2、B分别进行药敏试验,同时对5种幽门螺旋杆菌进行最低抑菌浓度测定。结果表明,使用大孔树脂得到的MREEs有较好的抑菌活性,得到的A1、A2和B对幽门螺旋杆菌的抑菌率均高于40.0%,其中石油醚萃取物A1在Helicobacter pylori SSI中的抑菌率甚至高达62.9%;A1、A2和B使用GC-MS测定出的主要成分分别是邻苯二甲酸二丁酯（A1,4.53%和A2,6.93%）和棕榈酸2.87%,但仍有大量成分没有被测出。另外,在最低抑菌浓度试验中,A1相应组分对Helicobacter pylori W₂504、Helicobacter pylori 9和Helicobacter pylori ATCC 43504的最低抑菌浓度都为0.25mg/mL,A2对Helicobacter pylori 78的最低抑菌浓度仅为0.25mg/mL,而B对Helicobacter pylori W₂504、Helicobacter pylori 9的最低抑菌浓度均仅为0.125mg/mL,说明通过石油醚和氯仿萃取得到的猴头菌子实体提取物对幽门螺旋杆菌具有潜在的抑菌作用。     

Bioactivity-based analysis and chemical characterization of hypoglycemic and antioxidant components from Artemisia argyi

Diabetes is one of the metabolic disorders in the world. It is the prime reason of mortality and morbidity owing to hyperglycemia which is link with numerus obstacles. Artemisia argyi is commonly used as an ingredient in healthy foods as well as an herbal medicine in Asian countries. The present research aims to evaluate the hypoglycemic effects of A. argyi and reveal its the potentially active constituents. The chemical composition was identified by HPLC-DAD-Q-TOF-MS, and fractionation was performed by extraction. The fractions were assessed by the blood glucose level, oral glucose tolerance and small intestinal α-glucosidase inhibitory tests, and an analysis of the total phenolic content (TPC), antioxidant and α-glucosidase inhibitory activities. In our efforts to characterize the compounds responsible for hypoglycemic effect, bioactivity-guided fraction of the MeOH extract and chemical investigation of its active EtOAc fraction led to the successful identification of caffeoylquinic acids, which were elucidated by molecular docking, using the crystal structure of S. cerevisiae isomaltase (PD code: 3AXI). In summary, this bio-guided search revealed that caffeoylquinic acids from A. argyi as potential active constituents displayed with hypoglycemic activity, which provided a basis for further study of pharmacological activity.     

Protective effect of Ecklonia cava enzymatic extracts on hydrogen peroxide-induced cell damage

In this study, Ecklonia cava was enzymatically hydrolyzed to prepare water-soluble extracts, using five carbohydrases (Viscozyme, Celluclast, AMG, Termamyl, and Ultaraflo) and five proteases (Protamex, Kojizyme, Neutase, Flavourzyme, and Alcalase), and the potential antioxidant activity of each was assessed. The Celluclast and Viscozyme extracts of E. cava evidenced good hydrogen peroxide (H₂O₂) scavenging activities (73.25% and 72.92%, respectively) as compared to those of other enzymatic extracts. Therefore, the Celluclast enzymatic extract was selected for use in further experiments, and separated into four different molecular weight fractions (<1, 1–10, 10–30 and >30 kDa). Among these fractions, the >30 kDa fraction manifested the most profound H₂O₂ scavenging activity, with a measured IC₅₀ of 13 μg/ml. The >30 kDa fraction also strongly enhanced cell viability against H₂O₂-induced oxidative damage, and evidenced relatively good lipid peroxidation inhibitory activity in a Chinese hamster lung fibroblast (V79-4) cell line. This fraction also effected a reduction in the proportion of cells undergoing H₂O₂-induced apoptosis, as was demonstrated by a decreased quantity of sub-G₁ hypodiploid cells and decreased apoptotic body formation on the flow cytometry assay. These results clearly indicate that the >30 kDa fraction of E. cava possesses good antioxidant activity against H₂O₂ mediated cell damage in vitro.     

Structure and physicochemical properties of barley non-starch polysaccharides—II. Alkaliextractable β-glucans and arabinoxylans

Three fractions containing hemicellulosic material were obtained by sequential extraction of barley residue (left after removal of water-extractable polysaccharides) with saturated barium hydroxide [Ba(OH)₂ fraction], distilled water [Ba(OH)₂/H₂O fraction], and 1 m sodium hydroxide [NaOH fraction]. The yields of the fractions were 1.6, 1.7, and 2.6% (w/w), respectively, of the dry barley grist. The Ba(OH)₂ fraction contained mainly arabinose and xylose, 35.8% and 60.9%, respectively. The Ba(OH)₂/H₂O fraction in addition to 26.7% Ara and 36.6% Xyl contained also 34.8% Glc. The NaOH fraction was composed of 14.2% Ara, 44.0% Xyl, and 40.9% Glc. The Ba(OH)₂/H₂O and NaOH extracts were further fractionated by stepwise (NH₄)₂SO₄ precipitation into several subfractions with varying amounts of β-glucans and arabinoxylans. β-Glucans in Ba(OH)₂/H₂O and NaOH fractions were characterized by high ratios of β-(1→4)/β-(1→3) linkages, large amounts of contiguously linked β-(1→4) segments, and high ratios of cellotriosyl/cellotetraosyl units. The alkali-extractable arabinoxylans, especially those NaOH-extractable, were characterized by a very low degree of substitution, high xylose/arabinose ratio, and a small content of doubly substituted xylose residues. Some populations of arabinoxylans displayed structural features that would enable them to self-associate or to interact with β-glucans.     

虎刺抗氧化和抗菌活性研究

考察虎刺80%乙醇提取物和石油醚、二氯甲烷、乙酸乙酯、水溶性部位的抗氧化和抗菌活性以及与总黄酮含量的关系。乙酸乙酯部位在清除DPPH自由基和还原力模型中抗氧化活性最强,水溶性部位在总抗氧化力模型中抗氧化活性最强,而石油醚部位抗氧化活性最弱。二氯甲烷部位、乙酸乙酯部位和石油醚部位具有一定的抑菌活性。虎刺黄酮类成分可能是其抗氧化的物质基础。     

Peptides from several italian cheeses inhibitory to proteolytic enzymes of lactic acid bacteria, pseudomonas fluorescens ATCC 948 and to the angiotensin I-converting enzyme

Water-soluble peptides from Mozzarella, Italico, Crescenza, and Gorgonzola cheeses were fractionated by reverse-phase fast protein liquid chromatography. Peptide fractions with inhibitory activity to amino- and endo-peptidases from Lactobacillus delbrueckii ssp. bulgaricus B397, Streptococcus thermophilus 305, and Lactococcus lactis ssp. cremoris Wg2 were found. Enzymes from Lactobacillus casei ssp. casei 2752 were less sensitive. Endopeptidase from Lactobacillus casei ssp. casei 2752 also had a different response to the effect of some inhibitors. It probably showed limited differences in catalysis and substrate positioning. Most of these inhibitory peptides were also effective in reducing the activity of the Pseudomonas fluorescens ATCC 948 endopeptidase and the angiotensin I-converting enzyme. Inhibitory peptide fractions from Mozzarella, Italico, and Crescenza cheeses had a certain degree of hydrophobicity while the peptide fraction from Gorgonzola cheese eluted in the initial part of the acetonitrile gradient. One of the inhibitory peptides contained in the water-soluble extract of Crescenza cheese was further purified and sequenced. It corresponded to the β-casein fragment 58-72.     

Inhibition of human gastric and pancreatic lipases by chiral alkylphosphonates. A kinetic study with 1,2-didecanoyl-sn-glycerol monolayer

Enantiomerically pure alkylphosphonate compounds RR′P(O)PNP (R=C_nH_2n+1, R′=OY with Y=C_n′H_2n′+1 with n=n′ or n≠n′; PNP=p-nitrophenoxy) noted (RY), mimicking the transition state occurring during the carboxyester hydrolysis were synthesized and investigated as potential inhibitors of human gastric lipase (HGL) and human pancreatic lipase (HPL). The inhibitory properties of each enantiomer have been tested with the monomolecular films technique in addition to an enyzme linked immunosorbent assay (ELISA) in order to estimate simultaneously the residual enzymatic activity as well as the interfacial lipase binding. With both lipases, no obvious correlation between the inhibitor molar fraction (₅₀) leading to half inhibition, and the chain length, R or Y was observed. (R₁₁Y₁₆)s were the best inhibitor of HPL and (R₁₀Y₁₁)s were the best inhibitors of HGL. We observed a highly enantioselective discrimination, both with the pure enantiomeric alkylphosphonate inhibitors as well as a scalemic mixture. We also showed, for the first time, that this enantioselective recognition can occur either during the catalytic step or during the initial interfacial adsorption step of the lipases. These experimental results were analyzed with two kinetic models of covalent as well as pseudo-competitive inhibition of lipolytic enzymes by two enantiomeric inhibitors.