Chemical composition and protective effect of oregano (Origanum heracleoticum L.) ethanolic extract on oxidative damage and on inhibition of NO in LPS-stimulated RAW 264.7 macrophages

The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid content, showed a significant radical-scavenging activity (IC₅₀ value of 12.8 μg/mL) using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) test and an interesting antioxidant activity with the β-carotene bleaching test (IC₅₀ values of 12.9 and 14.1 μg/mL at 30 and 60?min of incubation, respectively). The test for the inhibition of NO production, performed using the murine monocytic macrophage RAW 264.7 cell line, showed that the extract had significant activity with an IC₅₀ value of 108.5 μg/mL. The cytotoxic effect of O. heracleoticum extract in presence of lipopolysaccharide (LPS) (1 μg/mL) was evaluated but found to be negligible.     

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.     

Evaluation of in vitro alpha-glucosidase inhibitory,antimicrobial, and cytotoxic activities of secondary metabolites from the endophytic fungus,Nigrospora sphaerica,isolated from Helianthus annuus

This study aimed to evaluate alpha-glucosidase inhibition and antimicrobial activity as well as cytotoxic activity of extracts from the endophytic fungus, Nigrospora sp., isolated from leaves of Helianthus annuus, which is widely cultivated for food and used as a medicinal plant. The fungus (TSU-CS003) was identified based on internal transcribed spacer ribosomal DNA sequences and fungal biomass, and fermentation broth was subjected to extraction by solvents (hexane and ethyl acetate). All extracts were tested for their antimicrobial activity, alpha-glucosidase inhibition, and cytotoxicity activity. In addition, the active extract was analyzed by using gas chromatography mass spectrometry (GC-MS) TSU-CS003 was identified as Nigrospora sphaerica. The fermentation broth extract (BE) showed strong antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (Gram-positive bacteria) with minimum inhibitory concentration (MIC) values in the range of 16–32 μg/mL and a few yeasts with MIC values ranging from 64 to 128 μg/mL, especially Talaromyces marneffei with an MIC value of 4 μg/mL. The effects of BE were observed by SEM. The results showed that this extract affected the cell morphology of T. marneffei. The half-maximal inhibitory concentration (IC50) of BE from alpha-glucosidase inhibition was recorded as 17.25 μg/mL and also showed significant cytotoxicity against A549 human cancer cell lines with an IC50 value of 22.41 μg/mL. Furthermore, BE was analyzed by using GC-MS and divided into three main compounds, including 5-pentyldihydrofuran-2(3H)-one, (Z)-methyl 4-(isobutyryloxy)but-3-enoate, and 2-phenylacetic acid. This was the first report of the endophytic fungus N. sphaerica from H. annuus. It is a potential source of active metabolites, which gave the strong antifungal activity, antioxidant activity, and cytotoxicity to A549 cancer cell lines.     

Pharmacological and pharmacognostical valuation of Canna indica leaves extract by quantifying safety profile and neuroprotective potential

The current study primarily focused on the pharmacognostical and phytochemical screening of Canna indica and further analyzing the leaves extract for toxicological profile and neuroprotective potential. The microscopic, dry powder properties of the leaf material and phytochemical, physicochemical analysis was evaluated for pharmacognostical assessment. Dry leaves of C. indica were extracted using methanol and then further studied for both in vitro and in vivo toxicological study. The acute toxicity was measured by estimating the antioxidant defense system and anatomical impairment in the rat's organs. Also, the neuroprotective activity of the plant extract was assessed using anticholinesterase enzymatic inhibitory assay. The extract was found to be hemocompatible and showed absences of induction of behavioural changes. Likewise, no changes were seen on the anatomical structure of the rat’s organs. The methanolic extract portrayed a significant upsurge in the reduced glutathione level and showed a comparable acetylcholinesterase inhibition in a dosedependent manner with an IC50 value of 14.53 μg/mL compared to the standard Donepezil with an IC50 value of 13.31 μg/mL. C. indica has compelling pharmacognostical characteristics, good safety reports, and significant antioxidant as well as the neuroprotective potential that shows great potential for its further in-depth research for pharmacological use.     

菜籽饼提取物抑制黑色素生成作用

为了研究菜籽饼提取物对黑色素合成的抑制作用,为菜籽饼提取物作为美白化妆品的天然添加剂提供实验依据。采用ABTS法、DPPH法检测菜籽饼提取物清除自由基的能力,测定A-375黑色素细胞中酪氨酸酶活性和黑色素含量,并利用各自的试剂盒检测A-375细胞中抗氧化相关因子(MDA, SOD, GSH)。研究结果表明:菜籽饼提取物具有清除DPPH和ABTS的能力,对DPPH和ABTS的半数抑制率分别为304μg/mL和305.8μg/mL。菜籽饼提取物具有显著的抑制A-375黑色素的作用,药物作用48 h后,其IC50为113.3μg/m L,同时能够显著的降低黑色素的含量和酪氨酸酶的活性。与空白对照组(17.66 mol/ng)相比,菜籽饼提取物能显著降低A-375细胞内MDA含量,其抑制率为9.21 mol/ng,且能够显著提高SOD的含量,当浓度为125μg/m L时,SOD的含量较空白对照组提高了36.54 U/mL,与此同时,菜籽饼提取物亦能增加GSH的含量,当浓度为62.5μg/mL时,细胞中GSH的含量为6.43 mol/ng,其含量显著高于空白对照组。因此,菜籽饼提取物在降低黑色素含量、抑制酪氨酸酶活性的同时,也能够通过显著的抗氧化能力和清除自由基的能力,抑制A-375细胞中黑色素的生成。     

肉桂抑制α-葡萄糖苷酶活性成分研究

为寻找肉桂中具有抑制α-葡萄糖苷酶活性的化学成分,采用高效液相色谱结合体外抑制α-葡萄糖苷酶活性筛选模型的方法,进行活性成分的跟踪分离,并对活性化合物进行酶抑制动力学研究.结果显示,肉桂石油醚提取物(IC50=350.37 μg/mL)的活性明显高于阳性对照阿卡波糖(IC50=1028.99 μg/mL),从中分离出2个活性成分,分别鉴定为桂皮醛( IC50 =277.89 μg/mL)和肉桂酸(IC50=286.22 μg/mL).酶抑制动力学结果表明它们对α-葡萄糖苷酶的抑制类型均为非竞争性抑制,Ki值分别为178.07 μg/mL和229.43 μg/mL.     

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.     

Ixorapeptide I and ixorapeptide II, bioactive peptides isolated from Ixora coccinea

Two novel derivatized peptides, designated as ixorapeptide I (1) and ixorapeptide II (2), in addition to 28 other known compounds, were isolated from the MeOH extract of Ixora coccinea using bioassay-guided fractionation. The structures of metabolites 1 and 2 were determined by interpretation of the spectroscopic data and Marfey's method. Compound 1 exhibited selective potency against Hep3B liver cancer cell line with an IC(50) value of 3.36 μg/mL, and compound 2 did not show notable cytotoxicity toward cancer cell lines but could inhibit superoxide anion generation and elastase release with IC(50) values of 0.21 and 0.27 μg/mL, respectively. Moreover, kaempferol and luteolin from this plant showed inhibition with IC(50) values of 3.55 and 2.56 μg/mL, respectively on platelet aggregation induced by collagen.     

Antioxidant,antimicrobial and cytotoxicity potential of n-hexane extract of Cayratia trifolia L

It is of interest to analyze the antioxidant, antimicrobial and cytotoxicity activity of n-hexane extract of Cayratia trifolia L. (C. trifolia). The antimicrobial activity of n-hexane extract of C. trifolia was determined using disc diffusion method against six selected pathogenic microorganisms. The cytotoxicity potential of n-hexane plant extract was also studied against A2780 cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Results, n-hexane extract of C. trifolia possess significant antioxidant activity with significant IC50 values in radical scavenging assays. In antimicrobial studies, the maximum zone of inhibition was found in the range of 19.0 ± 0.1 to 22.0 ± 0.1 mm. In MTT assay, inhibition of cell growth with minimal IC50 values of 46.25±0.42μg/mL against A2780 cell lines was observed. Thus, n-hexane extract of C. trifolia is a possible antioxidant, antimicrobial and cytotoxicity agent.     

Total phenolic and flavonoid contents and antioxidant activity of ginger (Zingiber officinale Rosc.) rhizome,callus and callus treated with some elicitors

The present study was aimed at determining total phenolic and flavonoid contents and studying the antioxidant activity of ginger (Zingiber officinale Rosc.) rhizome and callus, 6-gingerol and 6-shogaol and callus treated with elicitors. Petroleum ether (PE) and chloroform: methanol (1:1, v/v) (CM) extracts were prepared by maceration. Highest total phenolic content was obtained from the CM extract (60.34?±?0.43?mg gallic acid/g) of rhizome while callus showed lower content detected in the CM extract (33.6?±?0.07?mg gallic acid/g). Flavonoids were only detected in rhizome (CM extract 40.25?±?0.21?mg quercetin/g). Both rhizome extracts exhibited good antioxidant activity with higher activity recorded in PE extract (IC₅₀ value 8.29?±?1.73?μg/mL). Callus extracts revealed lower antioxidant activity (IC₅₀ value 1265.49?±?59.9?μg/mL obtained from CM extract). 6-gingerol and 6-shogaol displayed high antioxidant activity in both assays with IC₅₀ 4.85?+?0.58_DPPH and 5.35?±?0.33_ABTS μg/mL for the former and IC₅₀ 7.61?±?0.81_DPPH and IC₅₀ 7.05?±?0.23_ABTS μg/mL for the latter. Treatment of callus with elicitors showed significant (p?<?0.05) effects in enhancing phenolic content and related antioxidant activity. The highest significant increase in phenolic content (37% and 34%) and antioxidant activity in DPPH assay (34% and 30%) was observed in callus treated with 100?mg/L yeast extract and 50?mg/L salicylic acid respectively. Therefore, studying the effect of the elicitation of ginger cultured tissues in phenolic accumulation would be of immense importance for pharmacological, cosmetic and agronomic industries.     

白柄肉齿菌Sarcodon leucopus多酚生物碱提取物的体外抗氧化及降血糖活性

为探讨西藏白柄肉齿菌Sarcodon leucopus子实体多酚生物碱提取物(PAE)的抗氧化和降糖活性,本研究考察了PAE对DPPH自由基清除能力、细胞内抗氧化能力(CAA)和糖尿病关键酶(大鼠小肠来源麦芽糖酶、蔗糖酶和α-淀粉酶)活性的抑制能力.结果表明,PAE具有一定的抗氧化活性,对DPPH自由基的半数抑制浓度(...     

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.     

Phytochemical Profiling,Antimicrobial, Antiproliferative and Apoptotic Effects of Stemodia viscosa Roxb. of Western Ghats Region,India

The present study shows the chemical profile, antimicrobial, antiproliferative, and apoptotic effects of Stemodia viscosa extracts. Thirteen bioactive compounds were identified in the 80 % ethanolic extract by GC/MS analysis. The acetone extract exhibited a higher content of flavonoids and phenols of 805.10 μg QE/mg DW and 89.31 μg GAE/mg DW extracts, respectively. Furthermore, the acetone extract possessed the highest antioxidant activity (IC₅₀=9.96 μg/mL). The 80 % ethanolic extract exhibited significant antimicrobial activity; the highest activity was observed against Staphylococcus aureus with a zone of inhibition of 25±0.51 mm, MIC value of 4 mg/mL, and MBC value of 8 mg/mL. The antiproliferative results revealed the presence of anticancer activity with an IC₅₀=91.562 and 74.362 μg/mL against the B16F10 skin and COLO205 colon cancer cells, respectively. The flow cytometric analysis shows that the plant extracts cause cancer cell death through the induction of apoptosis. Our findings confirmed that Stemodia viscosa is a potential source of biologically active compounds.     

Investigations of Antibacterial,Antioxidant, and Antidiabetic Potential of Extract and Its Active Fractions from the Leaves of Horsfieldia spicata (Roxb.) J. Sinclair

This study was undertaken to analyse the potential bioactivities including antibacterial, antioxidant and antidiabetic derived from the methanolic extract and the column chromatography ethyl acetate fraction (AcOEt Fr) of Horsfieldia spicata leaves. Methanolic extract and 4 other fractions was calculated for total phenol and flavonoid contents along with tested for antibacterial, antioxidant and antidiabetic properties. Interestingly, the AcOEt Fr had the highest value for total flavonoid content and the best antioxidant, and antidiabetic activities. Therefore, the AcOEt Fr was further separated using column chromatography technique for obtaining 9 selected fractions namely fraction 1 (F1) - fraction 9 (F9) which were further tested. The results showed that the AcOEt column chromatography fractions namely F2, F3, F4 and F6 had the best clear inhibition antibacterial value against all bacterial tested. In addition, these fractions also exhibited better Minimum Inhibitory Concentrations (MIC) and Minimum Bactericidal Concentrations (MBC) values than others. Antioxidant, 2,2-diphenylpicrylhydrazyl (DPPH) assayed indicated that AcOEt Fr had the strongest IC₅₀ value of 47.30 μg/mL. Further, F4 column chromatography fraction showed the best inhibition against α-Glucosidase enzyme related to antidiabetic activity with an IC₅₀ value of 6.11 μg/mL. Liquid chromatography tandem-mass spectrometry (LC/MS/MS) analysis identified that F4 derived from AcOEt fraction had several compounds belonging to the flavonoid and phenolics such as 3′,5-dihydroxy-7,4′-dimethoxyflavone, 5,7-dihydroxy-3-(4′-hydroxybenzyl)chromone, and Kadsurenin I.     

河南鼠尾草抑制体内外α-糖苷酶活性研究

本文采用96微孔板法,首次对河南鼠尾草抑制酵母和大鼠小肠α-葡萄糖苷酶活性进行研究。河南鼠尾草乙酸乙酯提取物(IC50=28.73μg/mL)和正丁醇提取物(IC50=73.90μg/mL)抑制酵母α-葡萄糖苷酶活性远高于阳性对照Acarbose(IC50=1081.27μg/mL),但只有乙酸乙酯提取物(IC50=366.79μg/mL)具有抑制大鼠小肠α-葡萄糖苷酶活性,阳性对照Acarbose未检测出其IC50。结果表明,河南鼠尾草乙酸乙酯提取物和正丁醇提取物均具有较好的酵母α-葡萄糖苷酶抑制活性,但只有乙酸乙酯提取物具有良好的大鼠小肠α-葡萄糖苷酶抑制活性。     

Molecular docking of phenolic compounds and screening of antioxidant and antidiabetic potential of Moringa oleifera ethanolic leaves extract from Qassim region,Saudi Arabia

IntroductionOxidative stress is crucial in diabetic pathophysiology, hence the prerequisite of ingesting naturally derived antioxidants as a remedial target. This study investigates the naturally occurring antioxidant and antidiabetic potential of Moringa oleifera ethanolic leaves extract.MethodsMoringa oleifera leaves were macerated (MOLE) by using 70% ethanol. Physiochemical and phytochemical examinations of MOLE was assayed using standard methods. The antioxidant activity was analyzed by DPPH (1, 1-diphenyl-2-picrylhydrazil) radical scavenging assay. In vitro antidiabetic was analyzed by pancreatic α-amylase enzyme inhibitory assay. The molecular docking was performed using AutoDock Vina v1.1.2 in PyRx 30.8.ResultsEthanolic extraction of MOLE by maceration technique, 14 % yield. Loss on drying, foreign organic matters and total ash value of OLE showed 0.27 w/w, 0.8 % and 19 %, respectively. Phytochemical test on MOLE confirmed starch, carbohydrate, flavonoid, gum, glycoside, saponin, tannin, and phenol presences. The total phenolic and flavonoid contents of MOLE are 260 mg GAE/g and 755 mg RUE/g of extract. MOLE (IC 50 55.6 ± 0.18 µg/mL) showed functional DPPH scavenging assay comparable to ascorbic acid (IC 50 46.71 ± 0.24 µg/mL). In the alpha-amylase inhibitory activity, Acarbose showed an IC 50 value of 19.45 ± 0.26 µg/mL, while MOLE portrayed an IC 50 value of 27.54 ± 0.07 µg/mL. Docking studies revealed that most phenolic compounds found within MOLE have minimum docking scores and high binding affinity against Human pancreatic alpha-amylase.ConclusionsThe invitro and docking results suggest that MOLE has been a viable natural bioactive source and might be a great potential source for future antidiabetic medicine.     

白皮锦鸡儿黄酮醇类化合物及其抗菌和抗氧化活性(英文)

从豆科植物白皮锦鸡儿(Caragana leucophloea Pojark.)地上部分分离到3个黄酮醇类化合物,经理化和波谱分析鉴定为3-O-甲基山奈酚(1)、3-O-甲基槲皮素(2)和槲皮素(3)。活性测定表明,1表现出较强的抗细菌活性,对大肠杆菌和番茄疮痂病菌的半抑制浓度分别为9.00μg/mL和7.42μg/mL,最低抑制浓度均为12.5μg/mL;而2和3则表现出较强的抗氧化活性,对DPPH还原的半抑制浓度分别为14.39μg/mL和13.64μg/mL;对β-胡萝卜素-亚油酸氧化的半抑制浓度分别为10.26μg/mL和9.87μg/mL。上述黄酮醇类化合物均为首次从白皮锦鸡儿中分离得到。     

LC-ESI-MS/MS Chemical Characterization,Antioxidant and Antidiabetic Properties of Propolis Extracted with Organic Solvents from Eastern Anatolia Region

Geographic conditions (altitude, climate, and local flora) lead to significant differences in the chemical composition of propolis. Therefore, more research is needed for propolis in different geographical regions. So, the aim of this study was to evaluate the phenolic profile, total phenolic content, antioxidant, and antidiabetic properties of Pülümür propolis from Turkey. Methanol (MeOH), chloroform (CHCl₃), and hexane extracts of propolis were analyzed. LC-ESI-MS/MS analysis of the extracts showed that the most abundant phenolic compound is caffeic acid in the MeOH extract (2943.12±11.12 μg phenolics/g extract), while on the other hand, CHCl₃ extract had the highest total phenolic content (125.75±1.02 mg GAE/g extract). Antioxidant activity was measured using ABTS and DPPH assays, whereas CHCl₃ extract (IC₅₀=6.35±0.11 and 28.84±0.10 μg/mL, respectively) and MeOH extracts (IC₅₀=5.04±0.07 and 28.80±0.09 μg/mL, respectively) showed relatively high antioxidant activity. The MeOH extract showed better antidiabetic activity than the standard compound, acarbose (IC₅₀=0.544 and 0.805 mg/mL, respectively).     

Phytotoxic and antifungal metabolites from Curvularia sp. FH01 isolated from the gut of Atractomorpha sinensis

Two main phytotoxic and antifungal phthalic acid butyl isobutyl ester (1) and radicinin (2) were isolated from the culture of Curvularia sp. FH01, a fungus residing in the Atractomorpha sinensis gut. The structures of isolated metabolites were established on the basis of spectral analysis. Metabolites 1 and 2 exhibited significant phytotoxic activity against the radical growth of Echinochloa crusgalli with their IC(50) values of 61.9 and 5.9 μg/mL, respectively, which were comparable to that 2,4-dichlorophenoxyacetic acid (2.0 μg/mL) used as a positive control. The antifungal test results showed that compound 2 possessed strong antifungal activity against Magnaporthe grisea (IC(50)=16.3 μg/mL) and Valsa mali (IC(50)=18.2 μg/mL). The findings of the present study suggest that bioactive properties of the fungus FH01 can be attributed to its major components, phthalic acid butyl isobutyl ester and radicinin, and both agents have a potential to be used as herbicide and fungicide.     

鹅不食草提取物对人鼻咽癌细胞CNE-1增殖抑制和凋亡诱导作用

考察鹅不食草提取物对人高分化鼻咽癌细胞CNE-1增殖的抑制作用,初步探讨其抗鼻咽癌分子机制。95%乙醇提取鹅不食草全草,噻唑蓝(MTT)法观察不同浓度提取物在不同时间对人高分化鼻咽癌细胞CNE-1增殖的抑制作用,Hoechst 33258荧光染色观察CNE-1凋亡情况及形态学变化,Western Blot检测CNE-1细胞内抗凋亡蛋白Bcl-2和促凋亡蛋白Bax的表达。结果表明:鹅不食草醇提物能显著抑制CNE-1增殖(P<0.01),并呈现明显的时间-剂量依赖性,其中诱导48和72 h的IC50分别为30.0和25.0μg/mL。阳性对照药顺铂的IC50为0.79μg/mL。Hoechst 33258荧光染色观察发现给药组CNE-1细胞出现不同程度细胞核变圆变亮,核染色质浓缩,产生核小体等明显的凋亡特征。Bcl-2蛋白相对表达量随醇提物浓度的增大而下降,Bax蛋白相对表达量随醇提物浓度的增大而上升,二者与对照组相比均有显著性差异(P<0.01)。鹅不食草醇提物对体外人高分化鼻咽癌细胞CNE-1具有明显的增殖抑制和凋亡诱导作用,其分子作用机制可能与Bcl-2蛋白表达下调、Bax蛋白表达上调有关。