紫皮石斛总酚提取工艺优化及其抗氧化活性研究

目的：研究紫皮石斛总酚提取工艺及体外抗氧化活性。方法：在单因素试验的基础上，采用响应面法优化紫皮石斛总酚的超声波辅助提取工艺条件，通过测定紫皮石斛总酚对超氧阴离子、DPPH自由基及羟自由基的清除率，评价其抗氧化活性。结果：紫皮石斛总酚最优提取工艺条件为乙醇浓度69%，料液比1∶40 (g/mL)，提取时间31 min，在此条件下总酚提取量为1.56 mg/g，与理论值1.58 mg/g接近。紫皮石斛总酚对超氧阴离子、羟自由基及DPPH自由基的半数抑制浓度(IC₅₀)分别为19.40μg/mL、118.35μg/mL及30.75μg/mL。结论：优选的紫皮石斛总酚提取工艺合理可行，且其具有较强的体外抗氧化活性。     

海藻多糖的单糖组成对体外抗氧化活性的影响

比较广西北部湾石莼(Ulva lactuca L.)、海带(Laminaria japonica)、裙带菜(Undaria pinnatifida Surin-gar)、紫菜(Porphyra)的单糖组成及抗氧化活性的差异,揭示多糖结构与其体外抗氧化活性的关系。利用PMP柱前衍生化HPLC分析海藻多糖的单糖组成,采用羟自由基清除试验、超氧阴离子自由基清除试验及DPPH自由基清除试验指征其体外抗氧化活性,结果表明,4种海藻多糖的单糖组成在主成分空间分布离散,石莼及紫菜主要由葡萄糖组成,海带主要由甘露糖组成,裙带菜则主要由半乳糖组成;其体外抗氧化活性存在显著差异,裙带菜多糖对DPPH的清除能力(半抑制浓度IC₅₀值为0. 56±0. 02 mg/mL)显著高于其他3种海藻多糖;石莼、裙带菜与海带对羟自由基均有较强的清除活性,而紫菜多糖对羟自由基的清除能力较差(IC₅₀值为26. 59±0. 98mg/mL);石莼与裙带菜对超氧阴离子的清除活性较强,显著高于海带与紫菜,其中石莼显著高于裙带菜,IC₅₀值分别为1. 61±0. 17、2. 73±0. 06 mg/mL。相关性分析及冗余分析结果表明,对抗氧化活性影响较为显著的因子为葡萄糖(Glc)、核糖(Rib)、木糖(Xyl)(P <0. 01)。     

朱砂根抑制α-葡萄糖苷酶与抗氧化活性研究

对朱砂根抑制α-葡萄糖苷酶与抗氧化活性进行研究.利用96微孔板法筛选α-葡萄糖苷酶抑制活性;采用DPPH、ABTS和FRAP方法分析抗氧化活性.结果表明,乙酸乙酯部位抑制α-葡萄糖苷酶的活性最高(IC50=39.27 μg/mL),石油醚部位次之(IC50 =56.11 μg/mL),正丁醇部位活性最弱(IC50=62.05μg/mL),但均远大于阳性对照Acarbose(IC50=1081.27 μg/mL);乙酸乙酯部位抗氧化能力最强,正丁醇部位次之.乙酸乙酯部位清除DPPH自由基(IC50=38.55 mg/L)的能力比BHT( IC50=18.71 mg/L)低1/2,清除ABTS自由基的能力(IC50=3.60 mg/L)比BHT(IC50=7.44 mg/L)强,但比BHA(IC50=1.74 mg/L)弱,还原Fe3+的能力(FRAP=512.99 ±6.80 μmoTE/g)为BHT(FRAP=1581.68±97.41μmol TE/g)的1/3.结果显示朱砂根乙酸乙酯部位抑制α-葡萄糖苷酶和抗氧化活性最好.     

烟曲霉GZWMJZ-152茶粕发酵代谢产物

在茶粕培养基摇床培养条件下,烟曲霉GZWMJZ-152将茶粕中的山茶苷A (1)和山茶苷B (2)代谢为山奈酚-3-O-芸香糖苷(3);在茶粕培养基静置发酵条件下,从发酵提取物中分离得到5个化合物,分别为山奈酚(4)、(-)Chaetominine (5)、trypacidin (6)、1,2-seco-trypacidin (7)、(-)-丁香脂素(8)。测试了8个化合物的α-葡萄糖苷酶抑制活性和DPPH自由基清除活性,其中化合物1-3,5-8具有较好的α-葡萄糖苷酶抑制活性,IC₅₀值在133.9-308.6μg/mL;化合物1,4,8具有较好的自由基清除活性,IC₅₀值在0.43-5.06μg/mL。     

民族药马利筋内生真菌生物活性研究

药用植物内生真菌能产生与宿主相同或相似的活性物质,民族药马利筋生物活性广泛。为获得马利筋活性内生真菌资源,该研究基于“民族药-内生真菌-活性成分”的思路,考察了168株马利筋内生真菌代谢产物的生物活性,并分别采用SRB法、Griess法、PNPG法和DPPH法对内生真菌发酵液乙酸乙酯提取物进行抗肿瘤、抗炎、α-葡萄糖苷酶抑制和抗氧化等生物活性测定,对活性菌株进行ITS菌种鉴定。结果表明：（1）所筛选的168株内生真菌中有22株表现出不同程度的生物活性。其中,9株内生真菌具有显著抗肿瘤活性,其IC₅₀值在0.1～40μg·mL^-1之间;菌株MJF-53在2.5μg·mL^-1时对LPS诱导的Raw264.7释放的NO和IL-1β均具有明显的抑制作用;7株内生真菌表现出不同程度的α-葡萄糖苷酶抑制活性,其IC₅₀值在1.0～4.0 mg·mL^-1之间,其中MYF-16和MYF-55对α-葡萄糖苷酶抑制活性接近阿卡波糖;19株内生真菌具有不同程度的DPPH自由基清除活性,其中菌株MYF...     

香蕉皮抗氧化和抑制人肝癌HepG2细胞活性研究

对香蕉皮提取物（banana peel extraction,BPE）的体外抗氧化作用和抗肿瘤活性进行了研究。使用福林酚和硝酸铝法测定BPE中总多酚和总黄酮含量;通过检测DPPH和O₂^-自由基清除能力测定BPE的体外抗氧化活性;采用Alamar Blue法检测BPE对HepG2细胞活性的影响;荧光染色及流式技术检测HepG2细胞凋亡;免疫印迹技术检测凋亡蛋白的变化;Caspase活性检测试剂盒测定Caspase-3和Caspase-9的活性;Caspase-9和Caspase-3抑制剂验证BPE抗肿瘤相关的信号转导通路。结果表明,BPE中总多酚和总黄酮含量分别为39.23 ± 2.35 mg·L^-1和26.53 ± 1.97 mg·L^-1;BPE显示出一定的DPPH和O₂^-自由基清除能力（65.31%±3.82%和51.29%±4.23%）,可明显抑制HepG2细胞的增殖（IC₅₀=54.32 mL·L^-1）;BPE通过上调Caspase-3、Bax、Bid、Apaf-1、Bak、p53、Caspase-9的表达,下调Bcl-2、Bcl-xl的表达诱导HepG2细胞凋亡;Caspase-9和Caspase-3抑制剂（Z-LEHD-FMK、Ac-DEVD-CHO）在一定程度上逆转了BPE的增殖抑制活性。BPE具有一定的自由基清除能力,对HepG2细胞具有明显增殖抑制作用,这些结果为香蕉皮的进一步开发利用提供了数据支撑。     

富硒菊花提取物的抗氧化活性及其对α-淀粉酶和α-葡萄糖苷酶活力的影响

本研究比较了富硒菊花与普通菊花的抗氧化活性与α-淀粉酶、α-葡萄糖苷酶抑制作用。富硒菊花甲醇提取物清除ABTS·+、DPPH·、OH自由基的EC50分别为0.078 5、0.068 0、0.346 9 mg/mL,普通菊花分别为0.128 9、0.121 2、0.313 3 mg/mL。富硒菊花提取物的总还原力与ABTS·+、DPPH·自由基清除能力一定强于普通菊花。富硒菊花提取物抑制α-淀粉酶、α-葡萄糖苷酶的IC50分别为2.190 9、4.123 9 mg/mL,普通菊花分别为3.449 5、10.696 3 mg/mL。富硒菊花提取物的抗氧化活性以及α-淀粉酶、α-葡萄糖苷酶抑制率呈现出一定的剂量依赖性,量效关系拟合方程具有较高的拟合度。富硒菊花的抗氧化活性与α-淀粉酶、α-葡萄糖苷酶抑制作用普遍优于普通菊花,这可能与其中所含的多酚、黄酮类化合物有关。本研究为富硒菊花资源的科学开发和综合利用提供了参考。     

球毛壳菌H6次级代谢产物及其α-葡萄糖苷酶抑制活性

采用体外α-葡萄糖苷酶抑制模型对一株球毛壳菌H6的发酵液和菌丝体两种乙酸乙酯提取物进行活性评价,结果表明,发酵液乙酸乙酯提取物对α-葡萄糖苷酶具有较强的抑制活性,其IC₅₀值为(510.76±23.46)μg/mL。采用硅胶、Sephadex LH-20、半制备高效液相等色谱技术从其发酵液乙酸乙酯提取物中分离得到12个化合物。通过各种光谱分析,依次鉴定为chaetoviridins A-B(1-2),chaetoglobosins A-D(3-6),chaetoglobosin J(7),chaetoglobosin Q(8),prochaetogobosinsⅠ-Ⅲ(9-11),vibratilicin(12),其中化合物12为首次从毛壳属中分离得到。对化合物进行α-葡萄糖苷酶抑制活性测定发现,化合物12显示弱的抑制活性,其IC₅₀为(1 182.75±19.14)μg/mL。     

裂片石莼水提物清除ABTS和DPPH自由基的光谱学研究

研究了大型海藻裂片石莼和富硒裂片石莼水提物清除 2,2'-连氮基-双-(3-乙基苯并二氢噻唑啉-6-磺酸)(ABTS)及 1,1-二苯基-2-三硝基苯肼(DPPH)自由基能力及其光谱学特征。分光光度计法测定,水提物 ABTS 自由基体系测定波长为 734 nm,体系稳定时间为 6 min;DPPH 自由基体系测定波长为 515 nm,体系稳定时间为 30 min。结果表明,裂片石莼水提物具有良好的抗氧化活性,能有效、快速地抑制溶液中 ABTS 和 DPPH 自由基。在优化选择的反应体系中,裂片石莼、富硒裂片石莼和标准抗氧化剂 VC 对 ABTS 自由基的半数抑制浓度(IC₅₀)分别为 76.40 μg/ml、54.11 μg/ml 和 60.69 μg/ml,说明富硒裂片石莼水提取的总抗氧化活性明显优于 VC,富硒培养可以显著提高裂片石莼的抗氧化活性。裂片石莼、高硒裂片石莼和标准抗氧化剂 VC 对 DPPH 自由基的 IC₅₀ 值分别为 123.29 μg/ml、 76.825 μg/ml 和 24.787 μg/ml。综合上述,富硒培养裂片石莼水提物具有优良的抗氧化活性,对水溶性自由基的抑制率明显高于脂溶性自由基,有广阔的开发前景。     

7株野生虫草菌的鉴定及其菌丝体醇提取物对HepG2细胞的抑制活性

结合形态学与ITS序列分析对7株野生虫草真菌进行分类鉴定。MTT法分析它们的菌丝体醇提取物对肝癌HepG2细胞增殖的抑制活性。鉴定结果表明菌株MF7、MF9、MF14为细脚棒束孢Isaria tenuipes,菌株MF11、MF12、MF13为蝉棒束孢Isaria cicadae,菌株MF10为球孢白僵菌Beauveria bassiana;MTT结果显示分离到的3株细脚棒束孢和3株蝉棒束孢的菌丝体醇提取物对HepG2的抑制活性较差,IC₅₀均大于500μg/mL;球孢白僵菌MF10对HepG2细胞有一定抑制作用,IC₅₀值为221.6μg/mL,略强于蝙蝠蛾拟青霉发酵菌丝粉产品金水宝胶囊（IC₅₀=364μg/mL）和中华被毛孢发酵菌丝粉产品百令胶囊（IC₅₀=268.7μg/mL）。另外,发现供对比试验的3株蛹虫草菌株（MF1、MF5、MF15）对HepG2细胞均有较好的抑制作用,其中MF15的发酵菌丝体醇提取物活性最强,IC₅₀为55.56μg/mL,暗示蛹虫草发酵菌丝体具有重要的研究价值。     

Hypoglycemic activity of the antioxidant saponarin, characterized as alpha-glucosidase inhibitor present in Tinospora cordifolia

Tinospora cordifolia, used in anti-diabetic herbal drug preparations, was reported [12] to contain an alpha-glucosidase inhibitor, characterized as saponarin (apigenin-6-C-glucosyl-7-O-glucoside). The leaf extract had appreciable antioxidant and hydroxyl radical scavenging activities and contained the flavonoid in the range of 32.1 +/- 1.5-45.5 +/- 3.5 mg/g of dry solid. Saponarin showed mixed competitive inhibition on activities of alpha-glucosidase and sucrase of different origins. IC(50), Ki and ki' values determined were 48 muM, 8 muM and 19.5 microM respectively for intestinal maltase and 35 microM, 6 microM and 13 microM respectively for intestinal sucrase. When given orally to maltose-fed rat, saponarin showed hypoglycemic activity in the range of 20-80 mg/kg compared to 100-200 mg/kg for acarbose as reported.     

Furofuran lignans as a new series of antidiabetic agents exerting α-glucosidase inhibition and radical scarvenging: Semisynthesis,kinetic study and molecular modeling

A new series of furofuran lignans containing catechol moiety were prepared from the reactions between lignans and a variety of phenolics. All 22 products obtained were evaluated against three different α-glucosidases (maltase, sucrase and Baker’s yeast glucosidase) and DPPH radical. Of furofuran lignans evaluated, β-14, having two catechol moieties and one acetoxy group, was the most potent inhibitor against Baker’s yeast, maltase, and sucrase with IC₅₀ values of 5.3, 25.7, and 12.9 µM, respectively. Of interest, its inhibitory potency toward Baker’s yeast was 28 times greater than standard drug, acarbose and its DPPH radical scavenging (SC₅₀ 11.2 µM) was 130 times higher than commercial antioxidant BHT. Subsequent investigation on mechanism underlying the inhibitory effect of β-14 revealed that it blocked Baker’s yeast and sucrase functions by mixed-type inhibition while it exerted non-competitive inhibition toward maltase. Molecular dynamics simulation of the most potent furofuran lignans (4, α-8b, α-14, and β-14) with the homology rat intestinal maltase at the binding site revealed that the hydrogen bond interactions from catechol, acetoxy, and quinone moieties of furofuran lignans were the key interaction to bind tightly to α-glucosidase. The results indicated that β-14 possessed promising antidiabetic activity through simultaneously inhibiting α-glucosidases and free radicals.     

凹叶厚朴抑制α-糖苷酶与抗氧化活性研究

首次采用96微孔板法检测贵州和河南产凹叶厚朴抑制α-葡萄糖苷酶活性;并采用DPPH、ABTS和FRAP三种方法测定其抗氧化活性.贵州产凹叶厚朴乙酸乙酯(IC50 =7.22 μg,/mL)和正丁醇提取部位(IC50=36.59 μg/mL),河南产凹叶厚朴石油醚(IC50=107.04 μg/mL)和乙酸乙酯提取部位(IC50=17.17μg/mL),它们的活性都远高于于阳性对照Acarhose( IC50=1081.27 μg/mL).贵州产凹叶厚朴乙酸乙酯提取部位清除ABTS自由基的能力最强(IC50=8.81 μg/mL),强于阳性对照BHT(IC50=11.94 μg/mL);其次为河南产凹叶厚朴乙酸乙酯提取部位(IC50=12.73 μg/mL).研究结果表明,贵州产凹叶厚朴乙酸乙酯提取部位抑制α-葡萄糖苷酶和抗氧化活性最好.     

Antioxidant Activity and α-Glucosidase Inhibitory Activities of the Polycondensate of Catechin with Glyoxylic Acid

In order to investigate polymeric flavonoids, the polycondensate of catechin with glyoxylic acid (PCG) was prepared and its chemically antioxidant, cellular antioxidant (CAA) and α-glucosidase inhibitory activities were evaluated. The DPPH and ABTS radical scavenging activities and antiproliferative effect of PCG were lower than those of catechin, while PCG had higher CAA activity than catechin. In addition, PCG had very high α-glucosidase inhibitory activities (IC₅₀ value, 2.59 μg/mL) in comparison to catechin (IC₅₀ value, 239.27 μg/mL). Inhibition kinetics suggested that both PCG and catechin demonstrated a mixture of noncompetitive and anticompetitive inhibition. The enhanced CAA and α-glucosidase inhibitor activities of PCG could be due to catechin polymerization enhancing the binding capacity to the cellular membrane and enzymes.     

南瓜醇提物的体外抗氧化活性(英文)

采用化学体系模拟法体外测定南瓜醇提物((pumpkin ethanol extract,PEE)对1,1-二苯基-2-苦苯肼自由基(DPPH·)、超氧阴离子自由基(O2)和羟自由基(·OH)的清除能力,总还原力,对β-胡萝卜素/亚油酸自氧化体系的总抗氧化能力以及脂质过氧化的抑制能力.结果显示PEE对DPPH·、02-和·OH均有较强的清除能力,IC50值分别为18.8 mg/mL、29.0 ms/mL和44.9μg/mL,有显著的还原力和总抗氧化力,对脂质过氧化有一定的抑制作用.PEE的体外抗氧化活性均有良好的量效关系.上述结果为南瓜作为抗氧化的保健食品或功能食品开发利用提供了依据.     

Antioxidative oligostilbenes from Caragana sinica

Two new oligostilbenes, caragasinins A (5) and B (10), and eight known compounds, kobophenol A (1), (+)-α-viniferin (2), (+)-ampelopsin F (3), pallidol (4), (+)-isoampelopsin F (6), miyabenol C (7), carasinaurone (8) and caraphenol B (9) were isolated from the ethylacetate-soluble extract of the roots of Caragana sinica. The structures of the isolates were determined on the basis of extensive spectroscopic analysis including 1D, 2D NMR and HRESI-MS. These compounds were assessed for antioxidant activities. Caragasinin A (5), caraphenol B (9), and caragasinin B (10) showed moderate DPPH scavenging activity and lipid peroxidation inhibitory activities with IC(50) values ranging from 34.7±1.0 to 89.1±2.3μM.     

Hypoglycemic activity of the antioxidant saponarin,characterized as α-glucosidase inhibitor present in Tinospora cordifolia

Tinospora cordifolia, used in anti-diabetic herbal drug preparations, was reported [12] to contain an α-glucosidase inhibitor, characterized as saponarin (apigenin-6-C-glucosyl-7-O-glucoside). The leaf extract had appreciable antioxidant and hydroxyl radical scavenging activities and contained the flavonoid in the range of 32.1 ± 1.5–45.5 ± 3.5 mg/g of dry solid. Saponarin showed mixed competitive inhibition on activities of α-glucosidase and sucrase of different origins. IC₅₀, Ki and ki′ values determined were 48 μM, 8 μM and 19.5 μM respectively for intestinal maltase and 35 μM, 6 μM and 13 μM respectively for intestinal sucrase. When given orally to maltose-fed rat, saponarin showed hypoglycemic activity in the range of 20–80 mg/kg compared to 100–200 mg/kg for acarbose as reported [27].     

桦褐孔菌子实体多糖的提取及体外降血糖活性

通过响应面设计得到桦褐孔菌子实体Inonotus obliquus多糖的优化提取条件,利用酶和细胞体外实验,探究桦褐孔菌子实体多糖的降血糖活性,确定活性多糖组分,并初步分析其降糖机理及单糖组成。优化条件下多糖得率为(2.79±0.03)%。粗多糖经乙醇分级沉淀分别获得IOP30、IOP60、IOP80组分。其中IOP30显示出最强的α-葡萄糖苷酶抑制活性（IC₅₀=38.20μg/mL）,且在酶动力学上属于非竞争性抑制。HepG2细胞经0.01、0.10、1.00mg/mL的IOP30处理,葡萄糖消耗与对照组相比差异极其显著（P<0.01）;同时添加10^-7mmol/L的胰岛素和0.10、1.00mg/mL的IOP30后葡萄糖消耗增加更显著（P<0.01）。IOP30主要由鼠李糖（7.93%）、阿拉伯糖（3.12%）、木糖（11.15%）、甘露糖（19.08%）、葡萄糖（39.17%）和半乳糖（19.15%）等单糖组成。桦褐孔菌子实体IOP30多糖组分具有显著的降血糖活性,其降糖可通过抑制α-葡萄糖苷酶活性减少餐后血糖的形成,促进细胞周围组织对葡萄糖的代谢,加强肝细胞对胰岛素的敏感性。     

Phytochemical analysis and evaluation of antioxidant activities of methanolic extracts of Maytenus emarginata

Reactive oxygen species (ROS) is a metabolic side product of oxidative stress process, which causes several diseases like atherosclerosis, cancer, etc. In defense of ROS, antioxidants play a key role in combating them. As the process of aging increases, the level of antioxidants in our body decreases and thereby needs utmost attention for its repair process, which is generally administered externally. Plant products serve a best source for controlling these activities by its own metabolic pathway. Studies on the antioxidant activities of Maytenus emarginata leaf extracts are lacking. Antioxidant activity of the methanol extract of Maytenus emarginata was determined by DPPH free radical nitric oxide scavenging assays, superoxide ion scavenging assays, ABTS, and iron chelating methods. Preliminary phytochemical screening revealed that the extract of Maytenus emarginata leaves possesses phenols, flavonoids, steroids, glycosides, saponins, tannins, and triterpenoids. The extract showed significant activities in all antioxidant assays compared to the standard antioxidant (ascorbic acid) in a dose-dependent manner, and remarkable activities to scavenge ROS may be attributed by the presence of the above active compounds in the leaves. The amount of total phenolics and flavonoid contents were also estimated. The DPPH, ABTS, Nitric oxide, superoxide, and iron chelating IC(50) values of the methanolic extracts were 12.44, 24.27, 22.41, 5.85, and 2.74?μg/mL, respectively. The total phenolic content of the methanolic extract was 10.69?mg CA/g, whereas the total flavonoid was 1.56?mg CAE/g. The antioxidant activities were correlated with the total phenolic content. This result suggests that the relatively high antioxidant activity of the methanolic extract compared to standard could be possibly be due to its high phenolic content.