竹叶提取物的体外抑菌及抗氧化活性的研究

本文用水提取竹叶有效成分,将提取液浓缩至含生药量约1.0 g/mL,经醇沉后取清液浓缩,再经石油醚、三氯甲烷、乙酸乙酯、正丁醇分步萃取,得不同极性的各部分提取物。以金黄色葡萄球菌和大肠杆菌为供试菌,采用抑菌圈法(琼脂扩散法)和最低抑菌浓度(MIC)法测定其抑菌效果。结果显示,石油醚、三氯甲烷、乙酸乙酯部分均表现抑菌活性。各供试样对两种菌的抑菌圈直径达9.8～18.4 mm,最低抑菌浓度分别为1.25 mg/mL2,.50 mg/mL和5.00 mg/mL。最后采用亚硝基红盐-Co2+褪色法研究了竹叶提取物对.OH的清除作用,结果表明三氯甲烷和乙酸乙酯部分萃取物的抗氧化性明显优于水提物,其中乙酸乙酯部分萃取物的IC50值为1.06 mg/mL。     

香茅精油的抑菌和抗氧化活性研究

选用产自福建厦门的香茅(Cymbopogon nardus),测定香茅精油对白色粘性沙雷氏菌、红色粘性沙雷氏菌、大肠杆菌、金黄葡萄球菌、铜绿假单胞菌和紫色杆菌等6种菌的抑菌活性,并利用ABTS^.+自由基清除法以及超氧阴离子清除法研究香茅精油的抗氧化活性。结果表明,新鲜香茅精油的平均提取率为0.29,对6种供试菌种都有较高的抑制作用,其中对紫色杆菌的抑制活性最强,且香茅精油有极高的清除ABTS^.+自由基以及超氧阴离子自由基的能力,证明香茅精油具有广谱抑菌活性及强抗氧化活性。     

Phenolic Profiling,Antioxidant, and Antibacterial Activities of Selected Medicinal Plants from Tunisia

Phytochemical screening of aqueous extract from six medicinal wild plants grown in South-eastern of Tunisia: Atriplex halimus, Teucrium polium, Moricandia arvensis, Deverra tortuoa, Haplophyllum tuberculatum and Polygonum equisetiforme were evaluated. Both decoction and ultrasound assisted extraction were used. Antioxidant, antibacterial proprieties, and phenolic profiling, using LC-ESI-MS method, were assessed. Total polyphenols, flavonoids, and condensed tannins contents ranged from 7.47±0.19 to 22.25±0.49 mg GAE/g Dw, 5.47±0.06 to 7.55±0.07 mg RE/g Dw, and 0.33±0.02 to 19.43±0.64 mg TAE/g Dw, respectively. Moreover, the reducing power and DPPH tests showed that P. equisetiforme (EC₅₀: 12.50±0.50 μg/ml; DPPH⋅⁺: 213.49±4.24 mg TEAC/g DW), T. polium (EC₅₀: 25.00±1.00 μg/ml; DPPH⋅⁺: 181.39±9.47 mg TEAC/g DW) as well as H. tuberculatum (EC₅₀: 56.25±0.25 μg/ml; DPPH⋅⁺: 177.83±5.85 mg TEAC/g DW) extracts were the most effective natural antioxidants. For anti-bacterial activity, the ultrasonic extract of H. tuberculatum showed the highest activity against both P. aeruginosa (13.50±0.71 mm) and S. aureus (13.00±0.00 mm) at 10 mg/ml. Furthermore 24 phenolic compounds were identified, with predominance of quinic acid, gallic acid, protocatechuic acid, syringic acid, p-coumaric acid, trans-ferulic acid, catechin (+), trans-cinnamic and silymarin. These results were further consolidated by to heatmap clustering with P. equisetiforme, H. tuberculatum, T. polium as the main antioxidant and antibacterial sources which supports their domestication and industrial use.     

Identification of Specific Chondroitin Sulfate Species in Cutaneous Autoimmune Disease

Cutaneous lupus erythematosus and dermatomyositis (DM) are chronic inflammatory diseases of the skin with accumulated dermal mucin. Earlier work has shown chondroitin sulfate (CS) accumulation within the dermis of discoid lupus erythematosus (DLE), subacute cutaneous lupus erythematosus (SCLE), and DM lesions compared with control skin. Immunohistochemistry for C4S revealed a greater density in DLE and DM lesions, whereas SCLE lesions did not differ from controls. Scleredema and scleromyxedema are attributed to increased hyaluronic acid, and lesional samples from these diseases also demonstrated accumulated dermal C4S. Interferon-γ and interleukin-1α, but not interferon-α, treatment of cultured dermal fibroblasts induced mRNA expression of CHST-11, which attaches sulfates to the 4-position of unsulfated chondroitin. These studies on possible CS core proteins revealed that serglycin, known to have C6S side chains in endothelial cells, had greater density within DM dermal endothelia but not in DLE or SCLE, following the pattern of C6S overexpression reported previously. CD44 variants expand the CS binding repertoire of the glycoprotein; CD44v7 co-localized to the distribution of C4S in DLE lesions, a finding not observed in DM, SCLE lesions, or controls. Because C4S and C6S have immunologic effects, their dysregulation in cutaneous mucinoses may contribute to the pathogenesis of these disorders.     

Iduronic Acid in Chondroitin/Dermatan Sulfate: Biosynthesis and Biological Function

The ability of chondroitin/dermatan sulfate (CS/DS) to convey biological information is enriched by the presence of iduronic acid. DS-epimerases 1 and 2 (DS-epi1 and 2), in conjunction with DS-4-O-sulfotransferase 1, are the enzymes responsible for iduronic acid biosynthesis and will be the major focus of this review. CS/DS proteoglycans (CS/DS-PGs) are ubiquitously found in connective tissues, basement membranes, and cell surfaces or are stored intracellularly. Such wide distribution reflects the variety of biological roles in which they are involved, from extracellular matrix organization to regulation of processes such as proliferation, migration, adhesion, and differentiation. They play roles in inflammation, angiogenesis, coagulation, immunity, and wound healing. Such versatility is achieved thanks to their variable composition, both in terms of protein core and the fine structure of the CS/DS chains. Excellent reviews have been published on the collective and individual functions of each CS/DS-PG. This short review presents the biosynthesis and functions of iduronic acid-containing structures, also as revealed by the analysis of the DS-epi1- and 2-deficient mouse models.     

Preparation and Evaluation of Gallate Ester Derivatives Used as Promising Antioxidant and Antibacterial Inhibitors

Many gallate esters have been applied as food additives due to their good biological properties. Herein, nine novel gallate ester derivatives were synthesized by a Friedel-Crafts alkylation reaction and characterized by melting point (m.p.), infrared (IR) spectroscopy, nuclear magnetic resonance (¹H- and ¹³C-NMR) spectra, and high-resolution mass spectrometry (HR-ESI-MS). Their antioxidant and antibacterial activities were measured using a series of classical assays. Studies found that the products showed favorable antioxidant and antibacterial activities. Their 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH ^⋅ ) scavenging effect IC₅₀ values were less than 5.00 μg mL⁻¹ and their reducing power was not less than that of vitamin C (Vc). Furthermore, the antibacterial results showed that the minimum inhibitory concentration (MIC) values of the products were not greater than 8.00 μg mL⁻¹, and their antibacterial rates were over 95 % at 300 μg mL⁻¹. The above data add valuable and novel information that gallate ester derivatives can be considered potential food additives to address food safety issues because of their high biological activity and health benefits.     

Reduced Sulfation of Chondroitin Sulfate but Not Heparan Sulfate in Kidneys of Diabetic db/db Mice

Heparan sulfate proteoglycans are hypothesized to contribute to the filtration barrier in kidney glomeruli and the glycocalyx of endothelial cells. To investigate potential changes in proteoglycans in diabetic kidney, we isolated glycosaminoglycans from kidney cortex from healthy db/+ and diabetic db/db mice. Disaccharide analysis of chondroitin sulfate revealed a significant decrease in the 4-O-sulfated disaccharides (D0a4) from 65% to 40%, whereas 6-O-sulfated disaccharides (D0a6) were reduced from 11% to 6%, with a corresponding increase in unsulfated disaccharides. In contrast, no structural differences were observed in heparan sulfate. Furthermore, no difference was found in the molar amount of glycosaminoglycans, or in the ratio of hyaluronan/heparan sulfate/chondroitin sulfate. Immunohistochemical staining for the heparan sulfate proteoglycan perlecan was similar in both types of material but reduced staining of 4-O-sulfated chondroitin and dermatan was observed in kidney sections from diabetic mice. In support of this, using qRT-PCR, a 53.5% decrease in the expression level of Chst-11 (chondroitin 4-O sulfotransferase) was demonstrated in diabetic kidney. These results suggest that changes in the sulfation of chondroitin need to be addressed in future studies on proteoglycans and kidney function in diabetes.     

侧柏叶精油的抗细菌和抗氧化活性(英文)

采用水蒸气蒸馏法提取侧柏叶精油,通过GC和GC-MS分析精油的组成。从侧柏叶精油中鉴定出29种成分,主要为单萜和倍半萜,含量较高的化合物有:8-丙氧基-柏木烷(15.41%)、松油烯-4-醇(12.98%)、α-蒎烯(9.85%)、桧烯(9.92%)和3-蒈烯(6.77%)。侧柏叶精油具有广谱的抗细菌活性,对供试细菌的最低杀菌浓度(MBC)在0.1 mg/mL和1.0 mg/mL之间,最低抑菌浓度(MIC)在0.063 mg/mL和0.90 mg/mL之间,半抑制浓度(IC50)在0.044 mg/mL和0.763 mg/mL之间。侧柏叶精油能有效抑制菲啰嗪与Fe2+的螯合(IC50值为0.409mg/mL)和β-胡萝卜素-亚油酸的氧化(IC50值为0.526 mg/mL)。     

Analysis of Chemical Composition and Assessment of Antioxidant,Cytotoxic and Synergistic Antibacterial Activities of Essential Oils from Different Plant Parts of Piper boehmeriifolium

The essential oils (EOs) from leaves, stems, and whole plant of Piper boehmeriifolium were analyzed using GC/FID and GC/MS. The main constituents of P. boehmeriifolium EOs were β‐caryophyllene, caryophyllene oxide, β‐elemene, spathulenol, germacrene D, β‐selinene, and neointermedeol. The antioxidant potential of the EOs were determined using DPPH^?, ABTS^?+ and FRAP assays. In ABTS^?+ assay, the leaf oil exhibited a remarkable activity with an IC₅₀ value of 7.36 μg/mL almost similar to BHT (4.06 μg/mL). Furthermore, the antibacterial activity of the oils as well as their synergistic potential with conventional antibiotics were evaluated using microdilution and Checkerboard assays. The results revealed that the oils from different parts of P. boehmeriifolium inhibited the growth of all tested bacteria and the minimum inhibitory concentrations were determined to be 0.078 – 1.250 mg/mL. In combination with chloramphenicol or streptomycin, the oils showed significant synergistic antibacterial effects in most cases. Besides, the results of MTT assay indicated that the oil of the whole plant exhibited significant cytotoxic activities on human hepatocellular carcinoma cells (HepG2) and human breast cancer cells (MCF‐7). In summary, the P. boehmeriifolium oils could be regarded as a prospective source for pharmacologically active compounds.     

Preparation of New Spiropyrazole,Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin heterocycles is reported by three component reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69–91 %). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6–96.2 %) using DPPH inhibitory potency. Among these compounds, hydantoin derivatives displayed higher antioxidant activities (93.7–96.2 %) comparing with spiropyrazoles and pyrazoles. The obtained results showed that Cl and Br substituents on the phenyl ring increased antioxidant activities of the related heterocycles. The antibacterial activities of the synthesized compounds were examined against two Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and two Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacteria. Among the synthesized heterocycles, 2-[1,3-dimethyl-2,5-dioxo-4-(2-oxo-2-phenylethyl)imidazolidin-4-yl]hydrazine-1-carbothioamide exhibited the excellent antibacterial activity against both Gram-positive and Gram-negative bacteria.     

黄鳝骨硫酸软骨素提取纯化的初步研究

在稀碱-酶解提取基础上,辅以超声波破碎从黄鳝（Monopterus albus）骨中提取硫酸软骨素（Chondroitin Sulfate,CHS）。比较了三氯乙酸（TCA）法、Sevag法和等电点法除蛋白的效果,并进行了多糖的乙醇分级沉淀实验;粗品经离子交换树脂（CM22）和透析膜（3500Da）透析进一步分离纯化。研究结果表明酶解后用TCA法除蛋白效果好,再加入除蛋白液2倍体积95％乙醇可使大部分CHS沉淀析出;精制品经鉴定含有硫酸基,CHS含量达92．31％;琼脂糖凝胶电泳和红外吸收光谱结果显示精制品与标准CHS相似,初步确定提取物为CHS类多糖。     

Evaluation of Antioxidant,Antibacterial and Enhancement of Antibiotic Action by Punica granatum Leaves Crude Extract and Enriched Fraction against Multidrug-Resistant Bacteria

The aim of this study was to evaluate the phytochemical composition, antioxidant, and antimicrobial potential of crude extract and fractions of Punica granatum leaves. The extract was produced by turbo extraction, after which hexanic, ethyl acetate, and aqueous fractions were obtained by partitioning. The chemical analyses were performed by thin layer chromatography and high-performance liquid chromatography, and the antioxidant activities were assayed by DPPH^. and ABTS^.+. Minimal inhibitory and bactericidal concentrations (MIC/MBC) were applied to twenty-two bacteria. Most strains susceptible to extract/fractions and resistant to antibiotics were selected, and ampicillin, azithromycin, ciprofloxacin, and gentamicin were associated with the ethyl acetate fraction (EAF) against multidrug-resistant strains in modulatory and checkboard models. The data from chromatographic analyses showed flavonoids and tannins in the extract, as well as the enrichment of EAF in phenols, mainly flavonoids. The flavonoids were connected to the electron transfer activity demonstrated in the DPPH^. and ABTS^.+ assays. Gram-positive strains are more susceptible to EAF. The subinhibitory concentrations of P. granatum enhanced the antimicrobial activity of the agents and reduced the EAF individual MIC, and the combination of EAF and antibiotics demonstrated a synergistic effect. These results present a promising approach for developing a therapy in which antioxidant extracts and fractions can be used in combination with antibiotics.     

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。     

蔓茎堇菜和柔毛堇菜多糖的抑菌抗氧化活性

利用乙醇沉淀法提取蔓茎堇菜Viola diffusa和柔毛堇菜V.principis多糖并分别进行抑菌及抗氧化试验。结果表明,蔓茎堇菜和柔毛堇菜多糖提取率分别为7.0%和8.3%。不同倍数体积无水乙醇沉淀提取的多糖抑菌和抗氧化能力不同。抑菌效果显示,蔓茎堇菜多糖对大肠杆菌和枯草芽孢杆菌的抑菌圈分别可达8.46mm和8.59mm,柔毛堇菜对大肠杆菌和枯草芽孢杆菌的抑菌圈均可达9.13mm,但两种堇菜多糖对黑曲霉和啤酒酵母未呈现抑制活性;抗氧化研究发现,蔓茎堇菜多糖抗氧化活性为243.64U·mL^-1,柔毛堇菜多糖抗氧化活性为411.78U·mL^-1。由此可见,无论是抑菌还是抗氧化活性方面,柔毛堇菜极显著优于蔓茎堇菜(P<0.01)。蔓茎堇菜和柔毛堇菜多糖都具有一定的抑菌抗氧化活性,均可作为食药两用植物资源进行开发利用。     

硫酸软骨素自组装膜上草酸钙Liesegang环的AFM研究

运用原子力显微镜（Atomic Force Microscope,AFM）研究了草酸钙在硫酸软骨素自组装膜上受控凝集结晶的现象,发现当硫酸软骨素的浓度为1.0g/L时,在云母表面形成的网状基底可以诱导过饱和的草酸钙溶液凝集结晶形成Liesegang环,这是草酸钙晶粒在膜表面扩散凝聚的结果,该环的形成和基底物的浓度以及草酸钙本身的过饱和度密切相关。表明了金属离子和硫酸软骨素分子之间复杂的相互作用与尿结石中的环状结构存在着一定的关系。从电荷聚集与晶格匹配等方面对Liesegang环的形成机理作了初步的探讨,为深入研究尿结石中环结构的形成提供了一定的实验依据。     

Effects of Chondroitin Sulfate and Its Oligosaccharides on Toll-Like Receptor-Mediated IL-6 Secretion by Macrophage-Like J774.1 Cells

The effects of two types of chondroitin sulphate (CS), CS-A and CS-C, their oligosaccharides (oligo-CSs), and disaccharides (Di-CSs) on toll-like receptor (TLR)-mediated secretion of interleukin (IL)-6 were compared using macrophage-like cell line J774.1. IL-6 secretion in the J774.1 cells was markedly increased by Pam3CS4, LPS, and CpG, the ligands to TLR1/2, 4, and 9 respectively. Among these three ligands, CpG-induced IL-6 was most clearly suppressed by CSs and their digests. Suppression of IL-6 secretion by smaller sized CS-A was stronger than that by intact CS-A, whereas no such size-dependent suppression was apparent for CS-C. Di-4S, the disaccharide unit of the CS-A digest, also showed much stronger suppression than Di-6S, the disaccharide unit of the CS-C digest, and the non-sulfated disaccharide unit, Di-0S. The suppressing activity of oligo-CSs, particularly Di-CSs, against TLR-mediated inflammation was dependent on the CS structure, including the sulfation site.     

Optimizing the Production of Antioxidant and Antibacterial Alkaloids from Macleaya cordata by Subcritical Water Extraction Technology

In this work, the subcritical water extraction technology was used to extract alkaloids from Macleaya cordata, and the effects of extraction temperature and time on its yield were investigated to find the best extraction conditions. Moreover, the antioxidant capacity and antibacterial activity of Macleaya cordata extract were studied. Furthermore, through the single-factor method, it was found that properly increasing the extraction temperature and prolonging the extraction time was conducive to increasing alkaloid yield. Still, a considerable amount of alkaloids might be decomposed by heat, resulting in a decrease in their yield. The results showed that the optimal extraction temperature of alkaloids from Macleaya cordata with subcritical water is 190 °C, the time is 45 min, and the corresponding maximum yield is 35.19±0.12 mg/g (sanguinarine equivalent in raw materials). In addition, the antioxidation and bacteriostasis abilities of subcritical water extract are better than those of traditional hot water extract, indicating that it is a feasible method to extract alkaloids from Macleaya cordata with subcritical water.     

Chemical Composition,Antibacterial, Antioxidant and in Vitro Antidiabetic Activities of Essential Oils from Eruca vesicaria

This work describes the study of the chemical composition and bioactivity of the essential oils (EOs) of the different organs (leaves, flowers, stems and roots) from Eruca vesicaria. According to the GC and GC/MS analysis, all the EOs were dominated by erucin (4‐methylthiobutyl isothiocyanate) with a percentage ranging from 17.9 % (leaves) to 98.5 % (roots). The isolated EOs were evaluated for their antioxidant (DPPH, ABTS and β‐carotene/linoleic acid), antibacterial and inhibitory property against α‐amylase and α‐glucosidase. Most EOs exhibited an interesting α‐glucosidase and α‐amylase inhibitory potential. The roots essential oil was found to be the most active with IC₅₀ values of 0.80±0.06 and 0.11±0.01 μg mL^?1, respectively. The essential oil of roots exhibited the highest antioxidant activity (DPPH, PI=92.76±0.01 %; ABTS, PI=78.87±0.19; and β‐carotene, PI=56.1±0.01 %). The isolated oils were also tested for their antibacterial activity against two Gram‐positive and three Gram‐negative bacteria. Moderate results have been noted by comparison with Gentamicin used as positive control.     

Evaluation of Pomelo Seed Extracts as Natural Antioxidant,Antibacterial, Herbicidal Agents,and Their Functional Components

Pomelo seeds (PS) are important by-product of pomelo fruits (Citrus grandis Osbeck). The value-added utilization of PS remains highly challenged. This study aimed to investigate the utilization potential of PS as natural antioxidant, antibacterial, herbicidal agents, and their functional components. The ethanolic extract (EE) of PS and its four fractions as PEE (petroleum ether extract), AcOEtE (ethyl acetate extract), BTE (butanol extract), and WE (water extract), were prepared and biologically evaluated. BTE exhibited the best antioxidant activity among all these extracts, in both ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and FRAP (ferric reducing antioxidant power) assays. AcOEtE was superior to other extracts in herbicidal assay against both Festuca elata Keng (IC₅₀ of 0.48 mg mL⁻¹) and Amaranthus retroflexus L. (IC₅₀ of 0.94 mg mL⁻¹). Meanwhile, both AcOEtE and BTE demonstrated inhibitory effects against Bacillus subtilis, Escherichia coli, and Xanthomonas citri subsp. citri, with MIC ranging 2.5–5.0 mg mL⁻¹. Furthermore, the primary chemical components involving naringin, deacetylnomilin, limonin, nomilin, and obacunone, were quantified in all these extracts. PCA (principal component analysis) suggested that naringin might highly contribute to the antioxidant activity of PS, and the herbicidal activity should be ascribed to limonoids. This study successfully identified AcOEtE and BTE as naturally occurring antioxidant, antibacterial, and herbicidal agents, showing application potential in food and cosmetics industries, and organic farming agriculture.     

Chondroitin Sulfate Accelerates Trans‐Golgi‐to‐Surface Transport of Proteoglycan Amyloid Precursor Protein

The amyloid precursor protein (APP) is a membrane protein implicated in the pathogenesis of Alzheimer's disease. APP is a part‐time proteoglycan, as splice variants lacking exon 15 are modified by a chondroitin sulfate glycosaminoglycan (GAG) chain. Investigating the effect of the GAG chain on the trafficking of APP in non‐polarized cells, we found it to increase the steady‐state surface‐to‐intracellular distribution, to reduce the rate of endocytosis and to accelerate transport kinetics from the trans‐Golgi network (TGN) to the plasma membrane. Deletion of the cytosolic domain resulted in delayed surface arrival of GAG‐free APP, but did not affect the rapid export kinetics of the proteoglycan form. Protein‐free GAG chains showed the same TGN‐to‐cell surface transport kinetics as proteoglycan APP. Endosome ablation experiments were performed to distinguish between indirect endosomal and direct pathways to the cell surface. Surprisingly, TGN‐to‐cell surface transport of both GAG‐free and proteoglycan APP was found to be indirect via transferrin‐positive endosomes. Our results show that GAGs act as alternative sorting determinants in cellular APP transport that are dominant over cytoplasmic signals and involve distinct sorting mechanisms.