Inhibitory Effects of 4-Halobenzoic Acids on the Diphenolase and Monophenolase Activity of Mushroom Tyrosinase

The effects of 4-halobenzoic acids (4-fluorobenzoic acid, 4-chlorobenzoic acid, and 4-bromobenzoic acid) on the activity of mushroom tyrosinase have been studied. The results show that 4-halobenzoic acids can strongly inhibit both monophenolase activity and diphenolase activity of the enzyme, and the inhibition displays a reversible course. The IC50 values were estimated as 0.26, 0.20, and 0.18 mM for diphenolase activity and as 1.03, 0.75, and 0.60 mM for monophenolase activity, respectively. Kinetic analyses show that the inhibition mechanism of all three 4-halobenzoic acids is noncompetitive inhibition to the diphenolase activity, and the inhibition constants (K1) were determined to be 0.25, 0.20, and 0.17 mM, respectively. The lag time of the monophenolase was obviously lengthened by these three 4-halobenzoic acids. When the concentration of inhibitors reached 1.4 mM, the lag time was lengthened from 30 s to 120, 125, and 150 s, respectively.     

Identification of Antibacterial Phenolics in Selected Plant Species from Mexican Cloud Forest by Mass Spectrometry Dereplication

Fifteen plant species from a protected cloud forest (CF) in Veracruz, Mexico, were screened for their in vitro capacity to inhibit the growth of the phytopathogenic bacteria Chryseobacterium sp., Pseudomonas cichorii, Pectobacterium carotovorum and Pantoea stewartii, causal agents of damage to crops like ‘chayote’, lettuce, potato and corn. As a result, the bioactivity of Turpinia insignis and Leandra cornoides is reported for the first time against Chryseobacterium sp. and P. cichorii. In addition, 24 and 18 compounds not described for these species were dereplicated by an UPLC/MS‐MS method, respectively. The identified compounds included simple phenols, hydroxycinnamic acids, flavonoids and coumarins. The antibacterial assay of 12 of them demonstrated the bacteriostatic effect of vanillin, trans‐cinnamic acid, scopoletin and umbelliferone against Chryseobacterium sp. These findings confirm for the first time the value of the CF plants from Veracruz as sources of bioactive natural products with antimicrobial properties against phytopathogenic bacteria.     

Caffeoylquinic Acids,Cytotoxic, Antioxidant,Acetylcholinesterase and Tyrosinase Enzyme Inhibitory Activities of Six Inula Species from Bulgaria

Chlorogenic (5‐CQA), 1,5‐, 3,5‐, 4,5‐ and 3,4‐dicaffeoylquinic (DCQA) acids were identified and quantified in the methanol extracts of Inula oculus‐christi L., I. bifrons L., I. aschersoniana Janka var. aschersoniana, I. ensifolia L., I. conyza (Griess .) DC. and I. germanica L. by HPLC analysis. The amount of 5‐CQA varied from 5.48 to 28.44 mg/g DE and the highest content was detected in I. ensifolia. 1,5‐DCQA (4.05–55.25 mg/g DE) was the most abundant dicaffeoyl ester of quinic acid followed by 3,5‐DCQA, 4,5‐DCQA and 3,4‐DCQA. The extract of I. ensifolia showed the highest total phenolic content (119.92±0.95 mg GAE/g DE) and exhibited the strongest DPPH radical scavenging activity (69.41±0.55 %). I. bifrons extract was found to be the most active sample against ABTS^.+ (TEAC 0.257±0.012 mg/mL) and the best tyrosinase inhibitor. The studied extracts demonstrated a low inhibitory effect towards acetylcholinesterase and possessed low cytotoxicity in concentration range from 10 to 300 μg/mL toward non‐cancer (MDCK II) and cancer (A 549) cells.     

New Tricks for Old Guys: Recent Developments in the Chemistry,Biochemistry, Applications and Exploitation of Selected Species from the Lamiaceae Family

Lamiaceae is one of the largest families of flowering plants comprising about 250 genera and over 7,000 species. Most of the plants of this family are aromatic and therefore important source of essential oils. Lamiaceae are widely used as culinary herbs and reported as medicinal plants in several folk traditions. In the Mediterranean area oregano, sage, rosemary, thyme and lavender stand out for geographical diffusion and variety of uses. The aim of this review is to provide recent data dealing with the phytochemical and pharmacological studies, and the more recent applications of the essential oils and the non‐volatile phytocomplexes. This literature survey suggests how the deeper understanding of biomolecular processes in the health and food sectors as per as pest control bioremediation of cultural heritage, or interaction with human microbiome, fields, leads to the rediscovery and new potential applications of well‐known plants.     

Mushroom Species Stereum hirsutum as Natural Source of Phenolics and Fatty Acids as Antioxidants and Acetylcholinesterase Inhibitors

Many lignicolous mushroom species are used as a food supplement and may represent an alternative treatment of Alzheimer's disease (AD). This study aimed to evaluate acetylcholinesterase inhibition (AChEI) of Stereum hirsutum together with antioxidant activity (AO) and cytotoxic activity against HepG2 cells. Different extracts (water, ethanol, methanol, polysaccharide) were analyzed, with respect to their mineral composition and chemical content. Ethanol extract was the most potent in AChEI (98.44 %) and demonstrated cytotoxic activity (91.96 % at 900.00 μg/mL), while the highest AO was demonstrated for polar extracts (methanol and water) as well. These activities may be attributed to determined phenolics (hydroxybenzoic and quinic acid) and fatty acids (FA), while biflavonoid amentoflavone may be responsible for cytotoxic activity. The most prevalent FA was linoleic (40.00 %) and the domination of unsaturated FA (UFA) (71.91 %) over saturated (26.96 %) was observed. This is the first report of AChEI of S. hirsutum extracts and first detection of amentoflavone. Due to high amount of UFA and well-expressed AChEI, this species can be considered as a potent food supplement in the palliative therapy of AD.     

Variations in the Components and Antioxidant and Tyrosinase Inhibitory Activities of Styphnolobium japonicum (L.) Schott Extract during Flower Maturity Stages

Styphnolobium japonicum (L.) S chott is widely cultivated in China, and its flowers and flower buds (FFB‐SJ) are commonly used as traditional Chinese medicine. This work aimed to assess variations in the chemical components and antioxidant and tyrosinase inhibitory activities of S. japonicum extract during five flower maturity stages (ES1–ES5). The results showed that the contents of total flavonoids, rutin, and narcissin were highest at ES1, whereas the contents of quercetin and isorhamnetin were highest at ES3. ES1 presented considerable antioxidant activities in terms of reducing power (RP) and 1,1‐diphenyl‐2‐picrylhydrazyl radical (DPPH^.) and hydroxyl radical (^.OH) scavenging capacity, whereas ES3 showed excellent tyrosinase inhibitory activity and 2,2′‐azinobis(3‐ethylbenzothiazoline‐6‐sulfonic acid) radical (ABTS^.+)‐ and O₂^.?‐scavenging capacity. Rutin and quercetin are the main bioactive components of FFB‐SJ with antioxidant and tyrosinase inhibition, and the immature flower buds of S. japonicum (S2 and S3) with excellent biological activities and relatively high extract yields were the best for product development.     

Phytochemical Diversity,Classification and Antibacterial Activity of Some Medicinal Plant Species from Tabuk (Saudi Arabia)

The main objectives of this study were to investigate the intra-specific and inter-specific phytochemical diversity and classification of nine important medicinal plant species from Tabuk region (KSA), namely (Pulicaria undulata L., Pulicaria incisa Lam., Artemisia herba-alba Asso., Artemisia monosperma Delile, Artemisia judaica L. and Achillea fragrantissima Forssk. from Asteraceae family, Ducrosia flabellifolia Boiss. from Apiaceae family, Thymus vulgaris L. and Lavandula coronopifolia Poir. from Lamiaceae family); to evaluate the antibacterial potentials of the plant extracts, and to inspect the possible associations between phytochemical diversity and contents of different phytochemical classes with the antibacterial activities of plant extracts. GC/MS technique was used to identify phytochemicals in the plant extracts. The standard disk diffusion technique was used to conduct the antibiotic susceptibility against four pathogenic bacterial species (two Gram positive: Staphylococcus aureus and Bacillus subtilis and two Gram negative species: Pseudomonas aeruginosa and Escherichia coli. A total of 160 different phytochemicals belonging to 30 compound classes were separated and identified. A. fragrantissima had the highest phytochemical diversity and P. incisa had the lowest one. Phytochemical beta diversity was 6.2362. Ethanol outperformed other extraction solvents in terms of antibacterial activity, while Pulicaria undulata and T. vulgaris ranked highest among plants in this regard. Gram positive bacterial species were more sensitive to plant extracts compared to Gram negative species. Phytochemical diversity and antibacterial activity of plant extracts against E. coli and P. aeruginosa were positively correlative, terpenoid and benzene & substituted derivative contents exhibited significant (p<0.05) positive correlations with the antibacterial activity against E. coli, terpenoid contents also showed positive correlation with activity against P. aeruginosa; benzene & derivative showed positive correlation with activity against the rest of bacterial species,     

Natural Multi‐Target Inhibitors of Cholinesterases and Monoamine Oxidase Enzymes with Antioxidant Potential from Skin Extracts of Hypsiboas cordobae and Pseudis minuta (Anura: Hylidae)

Alzheimer's disease (AD) is the most common cause of dementia, characterized by loss of selective neuronal and normal brain functions. Every year, ten million new cases are diagnosed worldwide. AD is a complex disease associated with all kind of different pathways, making their simultaneous modulation necessary. Nowadays anti‐AD treatments are focused on enzymatic inhibitors. The study of the amphibians’ skin had acquired great importance in the fields of biology and human health and represents an attractive and novel source for natural compounds with high potential in the development of new drugs. The present work exhibits the power of amphibian skins as a source of bioactive compounds. Herein we report the activity of extracts of two species from Hylidae family (H. cordobae and P. minuta) as reversible inhibitors of acetylcholinesterase and butyrylcholinesterase enzymes. Furthermore, the extracts inhibit MAO?B enzyme and showed antioxidant activities, acting on four important pathways of AD.     

双平板对照筛选跟踪分离细菌外排泵抑制剂

建立了细菌外排泵抑制剂的筛选与活性跟踪方法.准备2个平板,一个为普通营养琼脂平板,另一个为舍小蘖碱的普通营养琼脂平板,通过比较两个平板含药纸片周围抑菌圈的直径大小判断筛选结果,方法可靠稳定.筛选发现某霉菌提取物对细菌外排泵有抑制活性,经活性跟踪分离,得到单体化合物,经NMR鉴定为4′,5,7-三羟基异黄酮.方法简便易行,成本低,适宜于对大批样本进行快速筛选并在分离时进行活性跟踪.     

Plant Quarantine as a Measure Against Invasive Alien Species: The Framework of the International Plant Protection Convention and the plant health regulations in the European Union

The introduction of several plant pests into Europe in the 19th century with disastrous consequences called for the development of plant quarantine measures to prevent the spread and introduction of pests of plants and plant products. With the purpose of harmonising these measures, and of promoting measures for pest control, the International Plant Protection Convention (IPPC) was developed to address organisms that are both directly and indirectly injurious to plants. It supplies a framework for measures against invasive alien species according to the Convention on Biological Diversity, as far as they are plant pests. Three examples of invasive alien species within the scope of the IPPC are given in the article: the fungus Ceratocystis fagacearum, the pinewood nematode Bursaphelenchus xylophilus and the flatworm Arthurdendyus triangulatus. In its 1997 revision, the IPPC provides for the establishment of International Standards for Phytosanitary Measures, being acknowledged by the Agreement on the Application of Sanitary and Phytosanitary Measures of the World Trade Organisation. Standards most important for invasive alien species are those on pest risk analysis, on requirements for the establishment of pest-free areas, on surveillance, on pest eradication programmes, and on the import and release of exotic biological agents. Phytosanitary regulations in the European Union (EU) have been harmonised and up to now have regulated about 300 plant pests. The requirements also have a protective horizontal effect against the unintentional introduction of many other species, but the existing broader IPPC mandate for alien plant pests is not fully applied by the EU regulations. This revised version was published online in July 2006 with corrections to the Cover Date.     

Copper Oxide Nanomaterials Derived from Zanthoxylum armatum DC. and Berberis lycium Royle Plant Species: Characterization,Assessment of Free Radical Scavenging and Antibacterial Activity

Copper oxide nanomaterials were synthesized by a facile sustainable biological method using two plant species (Zanthoxylum armatum DC. and Berberis lycium Royle ). The formation of materials was confirmed by FT‐IR, ATR, UV‐visible, XRD, TEM, SEM, EDX, TGA and PL. The antibacterial activity was evaluated by agar well diffusion method to ascertain the efficacy of plant species extract and extract derived copper oxide nanomaterials against six Gram‐positive bacteria namely Staphylococcus aureus, Streptococcus mutans, Streptococcus pyogenes, Corynebacterium diphtheriae, Corynebacterium xerosis, Bacillus cereus and four Gram‐negative bacteria such as Klebsiella pneumonia, Escherichia coli, Pseudomonas aeruginosa and Proteus vulgaris against the standard drug, Ciprofloxacin for Gram‐positive and Gentamicin for Gram‐negative bacteria, respectively. In both cases, copper oxide nanomaterials were found to be sensitive in all the bacterial species. Sensitivity of copper oxide nanomaterials shows an be higher as compared to plant species extract against different bacteria. Scavenging activity of plant extracts along with nanomaterials have been accessed using previously reported protocols employing ascorbic acid as standard. Scavenging activity of copper oxide nanomaterials shows an increase with increase in concentration. The biological activity (bactericidal and scavenging efficiency) of plant derived copper oxide nanomaterials revealed that these materials can be used as potent antimicrobial agent and DPPH scavengers in industrial as well as pharmacological fields.