家蝇幼虫抗菌肽MDL-1的构象分析

用红外光谱、圆二色谱和荧光光谱研究家蝇幼虫抗菌肽MDL-1的结构特征及其在不同条件下的构象变化. 红外光谱检测结果显示抗菌肽MDL-1结构中含有螺旋、无规卷曲、折叠构象的吸收特征; 圆二色谱显示抗菌肽MDL-1结构相对比较稳定, 抗菌肽在不同浓度溶液中的构象发生改变; 荧光光谱法研究发现家蝇幼虫抗菌肽MDL-1在280 nm波长的激发光下, 荧光光谱为Tyr残基和Trp残基共同提供, 而且Trp残基不是位于抗菌肽分子的表面, 而是位于分子的内部, 该研究结果为进一步探讨抗菌肽的抗菌机理奠定了基础.     

HRMS Characterization,Antioxidant and Cytotoxic Activities of Polyphenols in Malus domestica Cultivars from Costa Rica

There is increasing interest in research into fruits as sources of secondary metabolites because of their potential bioactivities. In this study, the phenolic profiles of Malus domestica Anna and Jonagold cultivars from Costa Rica were determined by Ultra Performance Liquid Chromatography coupled with High Resolution Mass Spectrometry (HRMS) using a quadrupole-time-of-flight analyzer (UPLC-QTOF-ESI MS), on enriched-phenolic extracts from skins and flesh, obtained through Pressurized Liquid Extraction (PLE). In total, 48 different phenolic compounds were identified in the skin and flesh extracts, comprising 17 flavan-3-ols, 12 flavonoids, 4 chalcones, 1 glycosylated isoprenoid and 14 hydroxycinnamic acids and derivatives. Among extracts, the flesh of Jonagold exhibits a larger number of polyphenols and is especially rich in procyanidin trimers, tetramers and pentamers. Evaluating total phenolic content (TPC) and antioxidant activities using ORAC and DPPH procedures yields higher values for this extract (608.8 mg GAE/g extract; 14.80 mmol TE/g extract and IC₅₀ = 3.96 µg/mL, respectively). In addition, cytotoxicity evaluated against SW620 colon cancer cell lines and AGS gastric cancer cell lines also delivered better effects for Jonagold flesh (IC₅₀ = 62.4 and 60.0 µg/mL, respectively). In addition, a significant negative correlation (p < 0.05) was found between TPC and cytotoxicity values against SW620 and AGS adenocarcinoma (r = −0.908, and −0.902, respectively). Furthermore, a significant negative correlation (p < 0.05) was also found between the number of procyanidins and both antioxidant activities and cytotoxicity towards SW620 (r = −0.978) and AGS (r = −0.894) cell lines. These results align with Jonagold flesh exhibiting the highest abundance in procyanidin oligomers and yielding better cytotoxic and antioxidant results. In sum, our findings suggest the need for further studies on these Costa Rican apple extracts—and particularly on the extracts from Jonagold flesh—to increase the knowledge on their potential benefits for health.     

Chemical composition and antioxidant activities of the essential oil from Nandina domestica fruits

The chemical composition and antioxidant activities of the essential oil from Nandina domestica fruits were studied for the first time. Twenty-two compounds, representing 82.79% of the oil, were identified from the oil. The major compounds were 3-hexen-1-ol (12.9%), linalool (12.3%), 2-methoxy-4-vinylphenol (9.9%), oleic acid (8.0%), furfural (5.8%) and 2,6-di-tert-butyl-4-methylphenol (5.7%). The antioxidant activities of the oil were evaluated using reducing power, metal chelating ability and scavenging capacity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis-3-ethylbenzthiazoline-6-sulfonate (ABTS) and superoxide anion free radical. The oil exhibited significant antioxidant activities.     

The Binary Mixtures of Lambda-Cyhalothrin,Chlorfenapyr, and Abamectin,against the House Fly Larvae,Musca domestica L.

The house fly Musca domestica L. is one of the medical and veterinary pests that can develop resistance to different insecticides. Mixing insecticides is a new strategy for accelerating pest control; furthermore, it can overcome insect resistance to insecticides. This study aims to evaluate three insecticides, chlorfenapyr, abamectin, and lambda-cyhalothrin, individually and their binary mixtures against 2nd instar larvae of M. domestica laboratory strain. Chlorfenapyr exhibited the most toxic effect on larvae, followed by abamectin then the lambda-cyhalothrin. The half-lethal concentrations (LC₅₀) values were 3.65, 30.6, and 94.89 ppm, respectively. These results revealed that the high potentiation effect was the mixture of abamectin/chlorfenapyr in all the mixing ratios. In contrast, the tested combination of lambda-cyhalothrin/abamectin showed an antagonism effect at all mixing ratios against house fly larvae. The total protein, esterases, glutathione-S-transferase (GST), and cytochrome P-450 activity were also measured in the current investigation in the larvae treated with chlorfenapyr. Our results indicate that GST may play a role in detoxifying chlorfenapyr in M. domestica larvae. The highest activity of glutathione-S-transferase was achieved in treated larvae with chlorfenapyr, and an increase in cytochrome P-450 activity in the larvae was observed post-treatment with Abamectin/chlorfenapyr.     

Antioxidant, anti-glycation and anti-inflammatory activities of phenolic constituents from Cordia sinensis

Nine compounds have been isolated from the ethyl acetate soluble fraction of C. sinensis, namely protocatechuic acid (1), trans-caffeic acid (2), methyl rosmarinate (3), rosmarinic acid (4), kaempferide-3-O-β-D-glucopyranoside (5), kaempferol-3-O-β-D-glucopyranoside (6), quercetin-3-O-β-D-glucopyranoside (7), kaempferide-3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside (8) and kaempferol-3-O-α-L-rhamno-pyranosyl (1→6)-β-D-glucopyranoside (9), all reported for the first time from this species. The structures of these compounds were deduced on the basis of spectroscopic studies, including 1D and 2D NMR techniques. Compounds 1-9 were investigated for biological activity and showed significant anti-inflammatory activity in the carrageen induced rat paw edema test. The antioxidant activities of isolated compounds 1-9 were evaluated by the DPPH radical scavenging test, and compounds 1, 2, 4 and 7-9 exhibited marked scavenging activity compared to the standard BHA. These compounds were further studied for their anti-glycation properties and some compounds showed significant anti-glycation inhibitory activity. The purity of compounds 2-5, 8 and 9 was confirmed by HPLC. The implications of these results for the chemotaxonomic studies of the genus Cordia have also been discussed.     

Antioxidant activities of extracts and metabolites isolated from the fungus Antrodia cinnamomea

Three different solvent partitions (n-hexane, ethyl acetate [EtOAc] and n-BuOH) of the culture broth from Antrodia cinnamomea were assayed with two different radical scavenging methods: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and superoxide radical scavenging (SOD) assay. The EtOAc layer exhibited the best antioxidant activity. Two major antioxidant metabolites were isolated from the active EtOAc layer. The antioxidant activities of compounds 1-6 were further evaluated by DPPH, SOD and trolox equivalent antioxidant capacity (TEAC) assays. Compounds 3 and 5 showed stronger free radical scavenging than the reference BHA, ED???=?1.36 and 34.24 μM. Compound 5 displayed moderate SOD activity (ED???=?310.0?μM), and its antioxidant capacity of TEAC value was 2.2 mM trolox equivalency.     

Antioxidant activities of extracts and fractions from Eupatorium lindleyanum DC

The antioxidant activities of water extract (WE), ethanol extract (EE), residue water extract (RWE) and petroleum ether (PF), ethyl acetate (EF), n-BuOH (BF) and water (WF) fractions of the ethanol extract from Eupatorium Lindley DC were investigated for the first time. Total phenolics content, DPPH radical scavenging activities, superoxide radical scavenging activities, total reduction capability, and ferrous ions chelating activities were determined for all the extracts and fractions. The results showed that all the extracts and fractions exhibited antioxidant activities with different magnitudes of potency. Among all the samples, WE and RWE exhibited the best antioxidant capacities, the BF also exhibited high antioxidant abilities in all tests except for the metal chelating activity, while the other extracts and fractions were relatively weak antioxidants. The BF had the highest total phenolics contents in all extracts and fractions, and the WE and RWE were found to be rich in tannins. Furthermore, the content of total phenolics showed good correlation with DPPH radical scavenging activity, superoxide anion radical scavenging activity, and the reducing power. Phenolic composition of all the extracts and fractions was identified and quantified by HPLC. The results indicate that the extracts of E. Lindley DC might be a useful potential source of natural antioxidant ingredients.     

气相色谱-氮磷检测器法表征家蝇对马拉硫磷的水解代谢

为明确家蝇对马拉硫磷的水解代谢能力及相关代谢抗性，在用常规模式底物α-萘乙酯表征了敏感及抗性家蝇的水解酶活性的基础上，使用气相色谱-氮磷检测器（GC-NPD）法比较了抗性及敏感家蝇水解酶对马拉硫磷的水解代谢能力的差异。结果表明，用2：1（v/v）的乙酸乙酯与正己烷混合物萃取后，GC-NPD可成功测定家蝇酶制备液与马拉硫磷温育后的马拉硫磷含量变化，从而可以表征家蝇酶制备液对马拉硫磷的代谢能力。马拉硫磷抗性家蝇水解酶代谢α-萘乙酯的能力是敏感家蝇的1.39倍，代谢马拉硫磷的能力是敏感家蝇的6.68倍，表明家蝇对马拉硫磷的抗性与其对马拉硫磷代谢能力增强有关。该法可用于家蝇等昆虫对马拉硫磷的代谢能力及相关抗性机制研究。     

Antioxidant, antitubercular and cytotoxic activities of Piper imperiale

Phenolic compounds are widely distributed in Nature and act as pharmacologically active constituents in many herbal medicines. They have multiple biological properties, most notably antioxidant, antibacterial and cytotoxic activities. In the present study an attempt to correlate the phenolic composition of leaf, flower and wood extracts of Piper imperiale, with antioxidant, antitubercular and cytotoxic activities was undertaken. The total phenol content ranged from 1.98 to 6.94 mg GAE/gDW among ethanolic extracts, and gallic acid, catechin, epicatechin, ferulic acid, resveratrol and quercetin were identified and quantified by HPLC. DPPH and ABTS assays showed high antioxidant activity of the leaf extract (EC(50ABTS) = 15.6 μg/mL, EC(50DPPH) = 27.3 μg/mL) with EC?? in the same order of magnitude as the hydroxyquinone (EC(50ABTS) = 10.2 μg/mL, EC(50DPPH) = 15.7 μg/mL). The flower extract showed strong antimicrobial activity against Mycobacterium tuberculosis H??Rv. All the extracts exhibited dose-dependent cytotoxic effects against MCF-7 cancer cells. This is the first time that a Piper extract has been found to be highly active against M. tuberculosis. This study shows the biological potential of Piper imperiale extracts and gives way to bio-guided studies with well-defined biological activities.     

Polyphenolic QTOF-ESI MS Characterization and the Antioxidant and Cytotoxic Activities of Prunus domestica Commercial Cultivars from Costa Rica

There is an increased interest in plum research because of their metabolites’ potential bioactivities. In this study, the phenolic profiles of Prunus domestica commercial cultivars (Methley, Pisardii and Satsuma) in Costa Rica were determined by Ultra Performance Liquid Chromatography coupled with High Resolution Mass Spectrometry using a quadrupole-time-of-flight analyzer (UPLC-ESI-QTOF MS) on enriched phenolic extracts obtained through Pressurized Liquid Extraction (PLE) under acidic and neutral extraction conditions. In total, 41 different phenolic compounds were identified in the skin and flesh extracts, comprising 11 flavan-3-ols, 14 flavonoids and 16 hydroxycinnamic acids and derivatives. Neutral extractions for the skins and flesh from all of the cultivars yielded a larger number of compounds, and were particularly rich in the number of procyanidin trimers and tetramers when compared to the acid extractions. The total phenolic content (TPC) and antioxidant potential using the DPPH and ORAC methods exhibited better results for neutral extracts with Satsuma skins and Methley flesh, which showed the best values (685.0 and 801.6 mg GAE/g extract; IC₅₀ = 4.85 and 4.39 µg/mL; and 12.55 and 12.22 mmol TE/g extract, respectively). A Two-Way ANOVA for cytotoxicity towards AGS gastric adenocarcinoma and SW620 colon adenocarcinoma indicated a significant difference (p < 0.05) for PLE conditions, with better results for neutral extractions, with Satsuma skin delivering the best results (IC₅₀ = 60.7 and 46.7 µg/mL respectively) along with Methley flesh (IC₅₀ = 76.3 and 60.9 µg/mL, respectively). In addition, a significant positive correlation was found between TPC and ORAC (r = 0.929, p < 0.05), as well as a significant negative correlation (p < 0.05) between TPC and cytotoxicity towards AGS and SW620 cell lines (r = −0.776, and −0.751, respectively). A particularly high, significant, negative correlation (p < 0.05) was found between the number of procyanidins and cytotoxicity against the AGS (r = −0.868) and SW620 (r = −0.855) cell lines. Finally, the PCA clearly corroborated that neutral extracts are a more homogenous group exhibiting higher antioxidant and cytotoxic results regardless of the part or cultivar; therefore, our findings suggest that PLE extracts under neutral conditions would be of interest for further studies on their potential health benefits.     

Evaluation of pathogenicity of certain mitosporic ascomycete fungi to the house fly,Musca domestica L. (diptera: muscidae)

The virulence of five fungal strains, Acremonium cephalosporium, Aspergillus niger, Penicillium chrysogenum, Trichoderma viride, and Verticillum albo-atrum by application of 10⁸ conidia mL^?1 to larvae and adults of house flies, Musca domestica was determined. A. niger produced the highest percentage of mortality to larvae, 85.1 ± 1.60, and adults, 98.2 ± 3.10, of house flies. Topical application of the fungal strains to larvae showed concentration-dependent response and caused mortality ranged between 41% and 83% with LT₅₀ values varying between 5.22 and 7.81 days. The highest percentage of mortality, 83.9 ± 3.52, was produced by 10⁷ conidia mL^?1 of A. niger with LT₅₀ 5.22. The lowest mortality percentage, 41.2 ± 3.00 with LT₅₀ 7.81, was produced by 10⁵ conidia mL^?1 of V. alboatrum. On the other hand, the highest percentage of mortality to adults of house flies, 97.3 ± 3.52, was produced by 10⁷ conidia mL^?1 of A. niger with LT₅₀ 3.49. While the lowest mortality percentage, 59.1 ± 2.38 with LT₅₀ 6.91, was produced by 10⁵ conidia mL^?1 of V. albo-atrum.     

Analgesic and anti-inflammatory activities of the sesquiterpene fraction from Annona reticulata L. bark

The sesquiterpene fraction of Annona reticulata bark was studied by GC/MS. Three major components were identified: copaene (35.40%), patchoulane (13.49%) and 1H-cycloprop(e)azulene (22.77%). The fraction was also screened for its analgesic and anti-inflammatory activities. The sesquiterpene fraction at doses 12.5 and 25?mg?kg?1 and the unsaponified petroleum ether extract at a dose of 50?mg?kg?1 exhibited significant central as well as peripheral analgesic and anti-inflammatory activities. These activities were comparable with the standard drugs used in the respective experiments.     

Phytochemical Content and Antioxidant Activity of Malus domestica Borkh Peel Extracts

Apple is an important dietary source of carotenoids and phenolic compounds, and its regular consumption is associated with several health benefits. The aim of this study was to evaluate the phytochemical composition of fresh peels of four red-skinned (“Champion”, “Generos”, “Idared”, “Florina”) and two yellow-skinned (“Golden Delicious”, “Reinette Simirenko”) apple varieties. Antioxidant activity of apple peel extracts was determined by ferric reducing antioxidant power (FRAP) and ABTS radical scavenging capacity assays. Total carotenoid and polyphenolic contents were determined spectrophotometrically, while the profile of individual carotenoids and anthocyanins (in red-skinned varieties) was analyzed using high-performance liquid chromatography coupled to a photodiode array detector (HPLC-PDA). Carotenoid composition was specific for each variety, and total carotenoid content was slightly higher in yellow-skinned apple peels compared to red-skinned varieties. In contrast, total phenolic content was higher in the peels of red-skinned cultivars. Anthocyanin profile was predominated by cyanidin-3-O-galactoside. Antioxidant potential followed the trend of the total polyphenolic content, being highest in “Florina”, as measured by both FRAP and ABTS assays. Our results demonstrated apple peels have high phytochemical content with diverse compositions, and their regular consumption can be an excellent source of antioxidants.     

Antioxidant, antimicrobial and wound healing activities of Boesenbergia rotunda

The ethanolic extract of Boesenbergia rotunda (L.) Mansf was studied for its wound-healing potential. Since wound healing is interrelated with microbial infection and reactive oxygen species (ROS), this study was conducted to evaluate the antimicrobial and antioxidant activity of B. rotunda. The antimicrobial activity of B. rotunda was studied against six bacterial and two yeast strains using disc diffusion, minimum inhibitory concentration (MIC), and minimum microbicidal concentration (MMC). The B. rotunda extract displayed potential antimicrobial and antifungal activities by inhibiting the Gram-positive bacteria Staphylococcus aureus (ATCC 25923), S. epidermidis, and Bacillus subtilis (ATCC 6633), and the yeasts Candida albicans (ATCC 10231), and Saccharomyces cerevisiae. MIC and MMC values varied from 0.04 to 25 mg/mL and from 0.16 to 25 mg/mL, respectively. The antioxidant activity of B. rotunda was evaluated by measuring the Ferric Reducing/Antioxidant Power (FRAP) and DPPH free radical scavenging activity. The FRAP and DPPH values were 22.2 microM/microg and 76.3 mg/mL, respectively. In the wound-healing studies, the topical application of the B. rotunda extract indicated a significantly increased percentage of wound contraction on day 12 compared with the control group. Histological studies showed the complete epidermis and found collagen fibers and hair follicles in the dermis. The results of the present study support the continued and expanded utilization of B. rotunda in Thai folk medicine.     

Antioxidant activities, total phenolics and HPLC analyses of the phenolic compounds of extracts from common Mediterranean plants

In this study, the total phenolic amounts and antioxidant activities of plant extracts obtained from some common Mediterranean plant species collected from different places in Jordan were determined. The phenolic constituents of these extracts were also determined using HPLC. The total phenolic amounts ranged from 52.8 to 876.9 mg GAE per 100 g dry material. The antioxidant activities were evaluated according to the 2,2-diphenyl-1-picrylhydrazyl radical scavenger method. Sage (Salvia officinalis) showed the highest antioxidant activity (91%), while the lowest (11.3%) was seen in parsley (Petroselinum crispum). A strong correlation (r = 0.85) between antioxidant activity and total phenolic content was found. The phenolic compounds identified by HPLC were gallic acid, protocatechuic acid, catechin, gentisic acid, chlorogenic acid, vanillic acid, syringic acid, caffeic acid, epicatechin and benzoic acid. All the investigated plants contain gallic acid, whose phenolic content ranged from 0.4 to 37.8 mg per 100 g, catechin (0.3-339.9 mg per 100 g), protocatechuic acid (0.3-41.9 mg per 100 g) and gentisic acid (0.3-35.8 mg per 100 g), while caffeic acid (0.3-2.6 mg per 100 g) was detected in six species only. These natural plant phenolics could thus be a good source of antioxidants for applications in food.     

Antioxidant and antityrosinase activities of various extracts from the fruiting bodies of Lentinus lepideus

Lentinus lepideus is an edible mushroom currently available in Korea. The acetone, methanol and hot water extracts were prepared and assayed for their antioxidant and antityrosinase inhibitory activities. The hot water extract showed the strongest β-carotene-linoleic acid inhibition compared to the other extracts. At 8 mg/mL, the methanolic extract showed a high reducing power of 1.21. The acetone and methanol extracts were more effective in scavenging DPPH radicals than the hot water extract. The strongest chelating effect was obtained from the methanolic extract. Xanthine oxidase and tyrosinase inhibitory activities of the acetonic, methanol and hot water extracts increased with increasing concentration. Gallic acid, chlorogenic acid, vanillin, naringin, naringenin, formononetin, and biochanin-A were detected in the acetonitrile and hydrochloric acid (5:1) solvent extract. This study suggests that fruiting bodies of L. lepideus can potentially be used as a readily accessible source of natural antioxidants.     

Antioxidant and alpha-glucosidase inhibitory activities of isoflavonoids from the rhizomes of Ficus tikoua Bur

A new unique isoflavone derivatives with a cyclic-monoterpene-substituent, ficusin C (1), together with five known compounds (2–6), were isolated from the rhizomes of Ficus tikoua. Their structures were elucidated on the basis of spectroscopic data interpretation, mass spectrometric analysis and comparison with literature data of related compounds. Antioxidant and α-glucosidase inhibitory activities of these compounds were evaluated by 1,1-diphenyl-2-picryhydrazyl (DPPH) radical-scavenging assay and α-glucosidase inhibitory experiment, respectively.     

Novel silver-platinum bimetallic nanoalloy synthesized from Vernonia mespilifolia extract: Antioxidant,antimicrobial, and cytotoxic activities

In this study, bimetallic nanoparticles comprising silver and platinum with promising therapeutic activities were synthesized using ethanolic Vernonia mespilifolia plant extract for the first time. The bimetallic silver-platinum nanoparticles (AgPtNPs) were characterized using solid-state techniques including UV–vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and energy-dispersive X-ray spectroscopy (EDX) techniques. The internal morphological structure showed that the AgPtNPs were spherical with a diameter of approximately 35.5 ± 0.8 nm, while FTIR confirmed the effective capping and formation of the nanoparticles by phytoconstituents. The polyphenolic contents of the green synthesized nanoparticles from the ethanolic extract of V. mespilifolia (AgNPs and AgPtNPs) was found to be (28.0 ± 0.8 and 13.6 ± 0.1 mg GAE/g) total phenol, while the flavonoids content was (366.2 ± 17.0 and 126.6 ± 0.2 mg QE/g), and proanthocyanins content was (161.8 ± 0.6 and 70.2 ± 0.6 mg CE/g). The AgPtNPs displayed a greater ability to scavenge free radicals, especially DPPH and ABTS (IC₅₀ 19.5 and 21.6 µg/mL) respectively when compared with AgNPs and ascorbic acid. Besides, the AgPtNPs had a higher ferric reducing antioxidant power (FRAP) (44.1 mg GAE/g) when compared to AgNPs (18.5 mg GAE/g). Moreover, the AgPtNPs showed a two-fold antimicrobial activity towards pathogenic microbes compared to AgNPs and a selective cytotoxic potency towards MCF-7 breast cancer cell line compared to HEK 293 normal cell line. In summary, these fascinating bioactivities displayed by the AgPtNPs highlighted their potential in therapeutic biomedical applications.     

Antioxidant activities of Swertia decussata xanthones

The lipid peroxidation inhibitory activities of four hydroxyxanthones, isolated from the whole plant Swertia decussata, were evaluated for the first time. The most promising antioxidant among the xanthones, 1,7,8-trihydroxy-3-methoxyxanthone (swertianine, 4) was also tested for its scavenging potential against DPPH and superoxide radicals. The data clearly revealed good antioxidant activity of the xanthones, especially 4 which also showed strong protection against y-ray induced pBR322 DNA damage. A comparison of the radioprotecting activities of the monomethylated tetrahydroxyxanthone 4 with that of its congener, 1,3,7-trihydroxy-8-methoxyxanthone (5) revealed that the radioprotecting activity was not affected by the position of methylation.     

An investigation of the efficacy of organotin compounds for the control of the cotton stainer,Dysdercus cingulatus,the mosquito,Anophelese stephensi,and the common house fly,Musca domestica

A series of commercial organotin compounds was screened for efficacy against the three insect species Dysdercus cingulatus (cotton stainer), Anophelese stephensi (mosquito) and Musca domestica (house fly). Tributyltin species in the general order Bu₃SnCl>(Bu₃Sn)₂O>Bu₃Sn(linoleate) were more effective than two triphenyltin compounds. Tricyclohexyltin hydroxide, dimethyltin chloride, phenyltin trichloride and a diethyltin dichloridephenanthroline adduct were less effective.