enzyme-inhibitory activity

酶抑制活性
  • 文章类型: Journal Article
    不知道它们的化学成分,许多文化已将牡丹根用于药用。用于人类治疗的现代植物修复需要有关牡丹根的化学及其生物活性的特定知识。在这项研究中,乙醇-水提取物是通过浸渍以及微波和超声辅助提取制备的(MAE和UAE,分别)为了从牡丹根中获得生物活性分子,PaeoniaperegrinaMill.,和塞尔维亚野生牡丹。化学表征;多酚和类黄酮含量;抗氧化剂,多抗酶,和提取物的抗菌活性;并进行了热水提取物的体外胃肠消化(GID)。在PT提取物中观察到最强的抗胆碱酯酶活性。在PP提取物中观察到最高的抗ABTS(2,2'-氮杂-双(3-乙基苯并噻唑啉-6-磺酸)自由基电位,而对于DPPH(2,2-二苯基-1-吡啶酰肼基),用PO提取物取得了最好的结果。关于抗菌活性,提取物对蜡样芽孢杆菌具有很强的效力。进行分子对接模拟以收集对多酚和其他芍药特异性分子在测试酶的活性位点中的结合亲和力和相互作用的见解。Paeonia茶的体外GID显示出单个生物活性物质的不同恢复和行为,没食子酸甲酯和二没食子酸甲酯的回收率增加,芍药苷及其衍生物的回收率降低。UAE和M获得的PT(Gulenovci)和PP(Pirot)提取物在大多数生物活性测定中更有效。这项研究代表了Paeonia根提取物在药学上可能应用的第一步,医学,和食品技术。
    Without being aware of their chemical composition, many cultures have used herbaceous peony roots for medicinal purposes. Modern phytopreparations intended for use in human therapy require specific knowledge about the chemistry of peony roots and their biological activities. In this study, ethanol-water extracts were prepared by maceration and microwave- and ultrasound-assisted extractions (MAE and UAE, respectively) in order to obtain bioactive molecules from the roots of Paeonia tenuifolia L., Paeonia peregrina Mill., and Paeonia officinalis L. wild growing in Serbia. Chemical characterization; polyphenol and flavonoid content; antioxidant, multianti-enzymatic, and antibacterial activities of extracts; and in vitro gastrointestinal digestion (GID) of hot water extracts were performed. The strongest anti-cholinesterase activity was observed in PT extracts. The highest anti-ABTS (2,2\'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical potential was observed in PP extracts, whereas against DPPH (2,2-diphenyl-1-picrylhydrazyl radicals), the best results were achieved with PO extracts. Regarding antibacterial activity, extracts were strongly potent against Bacillus cereus. A molecular docking simulation was conducted to gather insights into the binding affinity and interactions of polyphenols and other Paeonia-specific molecules in the active sites of tested enzymes. In vitro GID of Paeonia teas showed a different recovery and behavior of the individual bioactives, with an increased recovery of methyl gallate and digallate and a decreased recovery of paeoniflorin and its derivatives. PT (Gulenovci) and PP (Pirot) extracts obtained by UAE and M were more efficient in the majority of the bioactivity assays. This study represents an initial step toward the possible application of Paeonia root extracts in pharmacy, medicine, and food technologies.
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  • 文章类型: Journal Article
    SwertiaperennisLinnaeus(SP)已用于治疗胃炎。我们报告了定性和定量的植物化学分析,SP的抗氧化和酶抑制活性。还通过多变量分析研究了提取物的生物活性与总生物活性含量之间的相关性。甲醇提取物含有许多活性化合物,并表现出良好的抗氧化活性。因此,这被选择用于进一步的植物化学分析和稳定性研究.通过超高效液相色谱-电喷雾电离-轨道阱-质谱法首次从该植物中鉴定出14种化合物。Iridoids,黄原酮,和黄酮类化合物是主要成分。甲醇提取物在稳定性研究中表现出良好的稳定性和抗氧化能力,低毒性,并对橄榄油和葵花籽油的氧化具有保护作用。SP具有开发和用作抗氧化剂的潜力,或者作为脲酶和XO抑制剂,其甲醇提取物可用作天然油稳定剂。
    Swertia perennis Linnaeus (SP) has been utilised to treat gastritis. We report the qualitative and quantitative phytochemical analysis, antioxidant and enzyme inhibitory activities of SP. The correlation between the biological activities and total bioactive contents of the extracts was also studied via multivariate analysis. Methanol extract contained many active compounds and exhibited good antioxidant activity. Therefore, this was selected for further phytochemical profiling and stability studies. Fourteen compounds were identified by ultra-performance liquid chromatography-electrospray ionisation-orbitrap-mass spectrometry for the first time from this plant. Iridoids, xanthones, and flavonoids were the main components. Methanol extract exhibited good stability and antioxidant capacity in stability studies, with low toxicity, and showed a protective effect on the oxidation of olive and sunflower oils. SP has the potential to be developed and used as an antioxidant, or as urease and XO inhibitors, and its methanol extract could be used as a natural oil stabiliser.
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  • 文章类型: Journal Article
    开发欧洲等地的药用和食用植物资源,这项研究集中在其不同提取物的生物活性成分。通过UPLC-DAD-ESI-Q-TOF-MSn分析评估MeOH提取物的植物化学组成。体外抗氧化性能,评估了从Althaeaofficinalis(APAO)的地上部分获得的部分的酶抑制作用和一氧化氮(NO)产生抑制活性。结果确定了76种化合物,包括8种酚酸,17类黄酮,6香豆素,9个三萜和11个生物碱。Fr.发现APAO的C-2在DPPH中具有最高的TPC(175.8±1.5mgGAE/g)和TFC(466.9±5.0mgRE/g),具有最高的抗氧化能力,ABTS,CUPRAC,FRAP和β-胡萝卜素漂白试验。Fr.A显示出明显的α-葡糖苷酶抑制作用,IC50值为3.8±0.1μg/mL。然而,Fr.B对5-脂氧合酶的抑制活性强于槲皮素,IC50值为8.4±1.6μg/mL。此外,Fr.B对LPS激活的RAW264.7细胞的NO产生也具有有效的抑制活性,IC50值为15.7±1.6μg/mL。我们的发现表明,不同的Althaeaofficinalis提取物可能被认为是酚类和类黄酮化合物的来源,具有作为天然抗氧化剂的高潜力,抗炎药和血糖调节剂。此外,它们也可以用于具有增强生物活性的食品和营养产品。
    To develop the medicinal and edible plant resources of Althaea officinalis Linn in Europe and other places, this study concentrated on the bioactive ingredients of its different extracts. The phytochemical compositions of MeOH extracts were evaluated by UPLC-DAD-ESI-Q-TOF-MSn analysis. The in vitro antioxidant properties, enzymes inhibitory effects and nitric oxide (NO) production inhibitory activities of fractions obtained from the aerial parts of Althaea officinalis (APAO) were evaluated. The results identified 76 compounds, including 8 phenolic acids, 17 flavonoids, 6 coumarins, 9 triterpenes and 11 alkaloids. Fr. C-2 of APAO was found to have the highest TPC (175.8 ± 1.5 mg GAE/g) and TFC (466.9 ± 5.0 mg RE/g) with the highest antioxidant capacity in DPPH, ABTS, CUPRAC, FRAP and β-carotene bleaching assays. Fr. A showed noticeable inhibition of α-glucosidase with an IC50 value of 3.8 ± 0.1 μg/mL. However, Fr. B displayed stronger inhibitory activity on 5-lipoxygenase than quercetin, with the IC50 value of 8.4 ± 1.6 μg/mL. In addition, Fr. B also possessed potent inhibitory activities on NO production toward LPS-activated RAW 264.7 Cells with an IC50 value of 15.7 ± 1.6 μg/mL. Our findings suggest that different Althaea officinalis extracts may be considered sources of phenolic and flavonoid compounds with high potential as natural antioxidants, anti-inflammatory agents and blood sugar regulators. In addition, they can also be used in food and nutraceutical products with enhanced bioactivities.
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  • 文章类型: Journal Article
    本研究调查了阿多尼斯ramosaFranch(AR)的三种溶剂提取物的含量和生物活性,其中含有12种植物化学物质。水提物的总产率和总蛋白含量最高,它表现出最高的羟基和超氧自由基清除能力,铜螯合能力,和铜减少抗氧化能力。乙醇提取物具有最高的总酚,类黄酮,和碳水化合物含量,它显示出最高的铁螯合活性,以及清除HClO和亚硝酸盐的能力。甲醇AR提取物含有最高的总类固醇和单宁含量;它还表现出高自由基和活性氧清除能力,并具有最佳的铁还原抗氧化能力,这使得它能够有效地防止β-胡萝卜素漂白。甲醇提取物也显示出良好的稳定性和低毒性。所有测试的AR溶剂提取物对四种酶(α-葡萄糖苷酶,α-淀粉酶,乙酰胆碱酯酶和丁酰胆碱酯酶)。总的来说,AR可以作为天然抗氧化剂。
    This study investigated the content and biological activity of three solvent extracts of Adonis ramosa Franch (AR), which contains 12 types of phytochemicals. The overall yield and total protein content of the aqueous extract were the highest, and it exhibited the highest hydroxyl and superoxide radical-scavenging abilities, copper chelating abilities, and cupric reducing antioxidant capacity. Ethanol extract had the highest total phenolic, flavonoid, and carbohydrate contents, and it showed the highest iron chelating activity, and HClO- and nitrite-scavenging abilities. Methanol AR extract contained the highest total steroid and tannin contents; it also demonstrated high radical- and reactive oxygen species-scavenging abilities and had the best ferric reducing antioxidant power, which allowed it to effectively prevent β-carotene bleaching. Methanol extract also showed good stability and low toxicity. All tested solvent extracts of AR exhibited weak enzyme-inhibitory activities for four enzymes (α-glucosidase, α-amylase, acetylcholinesterase and butyrylcholinesterase). Overall, AR can serve as a natural antioxidant.
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  • 文章类型: Journal Article
    深海生物的生存和适应的特殊性引起了人们对将其代谢物作为有前途的药物进行研究的兴趣。在这项工作中,溶血,细胞毒性,抗菌,和五种海葵的触手提取物的酶抑制活性(Cnidaria,首次评估了在俄罗斯远东千岛群岛和指挥官群岛附近收集的Actiniaria和Corallimorpharia)订单。利波内马和Actinostolacalllosa的提取物表现出最大的溶血活性,而在Actinostolafeculenta的提取物中发现了对小鼠脾细胞和Ehrlich癌细胞的高细胞毒性活性。Corallimorphuscf.的提取物。pilatus对Ehrlich癌细胞具有最大的活性,但对小鼠脾细胞没有毒性。海葵C.cf.pilatus和Stomphiacoccinea是抗菌和抗真菌化合物的有希望的来源,对革兰氏阳性菌枯草芽孢杆菌有活性,金黄色葡萄球菌,和白色念珠菌.此外,所有海葵都含有α-半乳糖苷酶抑制剂。短肢乳杆菌和C.的肽质量指纹图谱。pilatus提取物提供了广泛的肽,主要分子量为4000-5900Da,可能属于已知的或新的结构类毒素。获得的数据可以得出结论,深海海葵是药物发现化合物的有希望的来源。
    The peculiarities of the survival and adaptation of deep-sea organisms raise interest in the study of their metabolites as promising drugs. In this work, the hemolytic, cytotoxic, antimicrobial, and enzyme-inhibitory activities of tentacle extracts from five species of sea anemones (Cnidaria, orders Actiniaria and Corallimorpharia) collected near the Kuril and Commander Islands of the Far East of Russia were evaluated for the first time. The extracts of Liponema brevicorne and Actinostola callosa demonstrated maximal hemolytic activity, while high cytotoxic activity against murine splenocytes and Ehrlich carcinoma cells was found in the extract of Actinostola faeculenta. The extracts of Corallimorphus cf. pilatus demonstrated the greatest activity against Ehrlich carcinoma cells but were not toxic to mouse spleen cells. Sea anemones C. cf. pilatus and Stomphia coccinea are promising sources of antimicrobial and antifungal compounds, being active against Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus, and yeast Candida albicans. Moreover, all sea anemones contain α-galactosidase inhibitors. Peptide mass fingerprinting of L. brevicorne and C. cf. pilatus extracts provided a wide range of peptides, predominantly with molecular masses of 4000-5900 Da, which may belong to a known or new structural class of toxins. The obtained data allow concluding that deep-sea anemones are a promising source of compounds for drug discovery.
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  • 文章类型: Journal Article
    薄荷是广泛使用的药用植物,具有杰出的生物活性潜力,因此,本工作的目的是通过应用传统和新兴的分离技术开发具有高活性的新型薄荷提取物。传统的加氢蒸馏和微波辅助加氢蒸馏(MWHD)用于精油(EO)的回收,而有机溶剂萃取使用索氏装置,微波辅助和超声辅助过程以及超临界流体萃取(SFE)用于薄荷亲脂性提取物的非选择性回收。提取物根据萜类化合物进行了表征,特别强调了主要化合物的含量(mentol,薄荷酮,异薄荷醇和桉树脑)。抗氧化活性(DPPH,ABTS,CUPRAC,FRAP,螯合和磷钼测定)和酶抑制测定(乙酰胆碱酯酶,丁酰胆碱酯酶,酪氨酸酶,淀粉酶和葡萄糖苷酶抑制作用)用于筛选薄荷生物活性。MWHD被认为是传统EO回收过程的替代方法,而SFE提取物可用于绿色生产富含萜类化合物和其他亲脂性生物活性物质的无溶剂薄荷提取物。
    Peppermint is widely used medicinal plant with distinguished bioactive potential, therefore, the aim of present work was to develop novel peppermint extracts with high activity by application of traditional and emerging separation techniques. Conventional hydrodistillation and microwave-assisted hydrodistillation (MWHD) were applied for recovery of essential oil (EO), while organic solvent extraction using Soxhlet apparatus, microwave-assisted and ultrasound-assisted process and supercritical fluid extraction (SFE) were applied for non-selective recovery of peppermint lipophilic extracts. Extracts were characterized in terms of terpenoids profile with special emphasis on content of major compounds (mentol, menthone, isomenthol and eucalyptol). Antioxidant activity (DPPH, ABTS, CUPRAC, FRAP, chelating and phosphomolybdenum assay) and enzyme-inhibitory assays (acetylcholinesterase, butyrylcholinesterase, tyrosinase, amylase and glucosidase inhibition) were used for screening of peppermint bioactivity. MWHD was recognized as alternative for traditional process in EO recovery, while SFE extracts were useful for green production of solvent-free peppermint extracts rich in terpenoids and other lipophilic bioactives.
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  • 文章类型: Journal Article
    In the last decades, marine natural products (MNPs), have attracted extensive interest from both chemists and pharmacologists due to their chemical and bioactive diversities. This special issue, collecting total synthesis and structural modification of six different type of bioactive MNPs, is expected to inspire and attract more research effects invested into MNP research.
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