anti-inflammatory agents

抗炎药
  • 文章类型: Journal Article
    Salaciareticulata,药用木本攀援灌木,用于我们的研究,CuO纳米粒子的绿色合成,通过扫描电镜分析,EDX,FTIR,XRD,和紫外可见光谱。这项研究评估了对斑马鱼胚胎的毒性,并探索了抗菌,细胞毒性,抗糖尿病药,和合成的纳米颗粒的抗炎特性。在结果中,CuO纳米粒子的紫外吸收表明,纳米粒子绿色胶体悬浮液的强度由蓝色变为绿色,这也证实了绿色CuONPs的光谱从无色变为黑色。在FT-IR和XRD光谱分析中鉴定官能团并确定通过绿色和化学方法制备的CuONPs的粒径。它显示CuONPs(绿色)的尺寸约为42.2nm,而CuONP(化学)的尺寸约为84nm。使用SEM-EDX分析这些NP的形态。与化学制备的同行相比,绿色合成的CuO纳米粒子表现出优异的分散性。此外,绿色和化学CuO纳米颗粒浓度为200µL/mL时都会导致斑马鱼胚胎和幼虫的发育异常和死亡率增加。绿色和化学CuONP在10至50µL/mL的浓度下抑制α-葡萄糖苷酶活性,IC50值分别为22微升/毫升和26微升/毫升,分别。提取物表现出抗炎活性,IC50值为274和109µL/mL。作者得出结论,这种绿色纳米粒子方法具有作为传统合成方法的更环保和更具成本效益的替代方法的潜力。NP广泛应用于人类接触领域(医学和农业),因此,不涉及有毒物质的合成方法变得越来越重要。
    The Salacia reticulata, a medicinal woody climbing shrub, was utilized for our study, the green synthesis of CuO nanoparticles, which were analyzed through SEM, EDX, FTIR, XRD, and UV‒Vis spectroscopy. This study assessed the toxicity to zebrafish embryos and explored the antibacterial, cytotoxic, antidiabetic, and anti-inflammatory properties of the synthesized nanoparticles. In results, the UV absorption of the CuO NPs showed that the intensity of nanoparticle green colloidal suspension changed from blue to green, which also confirmed that the spectrum of the green CuO NPs changed from colorless to black. in FT-IR and XRD spectral analysis to identify functional groups and determine the particle size of CuO NPs prepared by green and chemical methods. Its showed that CuO NPs (green) had a size of approximately 42.2 nm, while CuO NPs (chemical) had a size of approximately 84 nm. The morphology of these NPs was analyzed using SEM-EDX. Compared with their chemically prepared counterparts, the green-synthesized CuO nanoparticles demonstrated superior dispersion. Additionally, both green and chemical CuO nanoparticles at a concentration of 200 µL/mL caused developmental anomalies and increased mortality in zebrafish embryos and larvae. The green and chemical CuO NPs inhibited α-glucosidase enzyme activity at concentrations between 10 and 50 µL/mL, with IC50 values of 22 µL/mL and 26 µL/mL, respectively. The extract exhibited anti-inflammatory activity, with IC50 values of 274 and 109 µL/mL. The authors concluded that this green nanoparticle method has potential as a more eco-friendly and cost-effective alternative to traditional synthetic methods. NPs are widely used in human contact fields (medicine and agriculture), hence synthesis methods that do not involve toxic substances are becoming increasingly important.
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  • 文章类型: Systematic Review
    豆科植物广泛分布于世界各地,尤其是在欧洲,亚洲和北美。它们是异黄酮的丰富来源,具有雌激素样活性的化合物,怀疑对激素依赖性癌症有化学预防作用。按照PRISMA准则,我们进行了系统综述,旨在评估豆科植物提取物对激素依赖性癌细胞的影响以及植物原料中活性化合物的含量。我们分析了来自体外和体内研究的63篇文章的结果,这些文章描述了含异黄酮的植物提取物对癌细胞的影响,以及它们的抗炎和抗氧化潜力。在这个过程中,我们确定了研究的局限性和未来的研究方向。收集的结果表明植物物种具有潜在的高含量的植物雌激素和抗炎,抗氧化和细胞毒性。他们指出,植物在饮食中的潜在用途是提供癌症预防的化合物的来源。
    Plants from the Fabaceae family are widely distributed around the world, especially in Europe, Asia and North America. They are a rich source of isoflavones, compounds with estrogen-like activity, which are suspected of having a chemopreventive effect against hormone-dependent cancers. Following the PRISMA guidelines, we conducted a systematic review aimed at assessing the impact of Fabaceae plant extracts on hormone-dependent cancer cells and the content of active compounds in plant raw materials. We analyzed the results of 63 articles from in vitro and in vivo studies describing the effect of plant extracts containing isoflavones on cancer cells, along with their anti-inflammatory and antioxidant potential. In the process, we determined the research limitations and future research directions. The collected results indicate the plant species with potentially high contents of phytoestrogens and anti-inflammatory, antioxidant and cytotoxic properties. They point to the potential use of plants in the diet as a source of compounds offering cancer prevention.
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  • 文章类型: Journal Article
    透明质酸酶具有将高分子量透明质酸降解成较小片段的能力,随后启动炎症反应的级联反应和激活树突状细胞。在细菌感染的情况下,产生大量的HAase,可能导致严重的疾病,如蜂窝织炎。抑制透明质酸酶活性可提供抗炎益处。丹参,中药,具有抗炎特性。然而,它对皮肤炎症的影响尚不清楚。本研究筛选并评价了丹参抑制皮肤炎症的活性成分,使用配体捕鱼,酶活性测定,药物组合分析,和分子对接。通过将磁性纳米材料与透明质酸酶官能团结合,我们在文献中首次将透明质酸酶固定在磁性纳米材料上。然后,我们利用固定化酶特异性吸附配体;在悬空配体解吸后,通过HPLC分析鉴定了两个配体为丹酚酸B和迷迭香酸,完成丹参根中潜在抗炎活性成分的快速筛选。中值效应方程和组合指数结果表明,在固定的3:2比率下,它们对透明质酸酶的协同抑制作用随着浓度的增加而增强。动力学研究表明,它们充当透明质酸酶的混合型抑制剂。丹酚酸B的Ki和Kis值为0.22和0.96μM,分别,而迷迭香酸的值为0.54和4.60μM。分子对接显示丹酚酸B对透明质酸酶的亲和力高于迷迭香酸。此外,我们观察到SAB和RA的3:2组合显着降低TNF-α的分泌,UVB照射的HaCaT细胞中的IL-1和IL-6炎性细胞因子。这些发现确定丹酚酸B和迷迭香酸是具有抑制皮肤炎症潜力的关键成分,如在丹参中发现的。这项研究对于开发皮肤炎症治疗具有重要意义。它证明了基于磁性纳米颗粒的配体打捞方法用于筛选源自草药提取物的酶抑制剂的有效性和广泛适用性。
    Hyaluronidase possesses the capacity to degrade high-molecular-weight hyaluronic acid into smaller fragments, subsequently initiating a cascade of inflammatory responses and activating dendritic cells. In cases of bacterial infections, substantial quantities of HAase are generated, potentially leading to severe conditions such as cellulitis. Inhibiting hyaluronidase activity may offer anti-inflammatory benefits. Salvia miltiorrhiza Bunge, a traditional Chinese medicine, has anti-inflammatory properties. However, its effects on skin inflammation are not well understood. This study screened and evaluated the active components of S. miltiorrhiza that inhibit skin inflammation, using ligand fishing, enzyme activity assays, drug combination analysis, and molecular docking. By combining magnetic nanomaterials with hyaluronidase functional groups, we immobilized hyaluronidase on magnetic nanomaterials for the first time in the literature. We then utilized an immobilized enzyme to specifically adsorb the ligand; two ligands were identified as salvianolic acid B and rosmarinic acid by HPLC analysis after desorption of the dangling ligands, to complete the rapid screening of potential anti-inflammatory active ingredients in S. miltiorrhiza roots. The median-effect equation and combination index results indicated that their synergistic inhibition of hyaluronidase at a fixed 3:2 ratio was enhanced with increasing concentrations. Kinetic studies revealed that they acted as mixed-type inhibitors of hyaluronidase. Salvianolic acid B had Ki and Kis values of 0.22 and 0.96 μM, respectively, while rosmarinic acid had values of 0.54 and 4.60 μM. Molecular docking revealed that salvianolic acid B had a higher affinity for hyaluronidase than rosmarinic acid. In addition, we observed that a 3:2 combination of SAB and RA significantly decreased the secretion of TNF-α, IL-1, and IL-6 inflammatory cytokines in UVB-irradiated HaCaT cells. These findings identify salvianolic acid B and rosmarinic acid as key components with the potential to inhibit skin inflammation, as found in S. miltiorrhiza. This research is significant for developing skin inflammation treatments. It demonstrates the effectiveness and broad applicability of the magnetic nanoparticle-based ligand fishing approach for screening enzyme inhibitors derived from herbal extracts.
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  • 文章类型: Journal Article
    在寻找新型有效的免疫调节核因子-红细胞2相关因子2(Nrf2)激活剂时,胆酸胆汁酸的衍生物,SB140,进行了合成。SB140的合成旨在增加化合物的亲电子官能度,增强其激活Nrf2的能力。SB140对小胶质细胞的影响,骨髓衍生细胞(MDC),在(中枢神经系统)CNS自身免疫的背景下探索T细胞。SB140有效激活MDC和小胶质细胞中的Nrf2信号。它能有效降低小胶质细胞产生炎性一氧化氮的能力,白细胞介素(IL)-6和肿瘤坏死因子(TNF)。此外,SB140减少了致脑炎性T细胞的增殖及其效应细胞因子IL-17和干扰素(IFN)-γ的产生。相反,SB140对小胶质细胞和致脑病T细胞中抗炎IL-10产生的影响有限或不存在.这些结果表明,SB140是一种有效的Nrf2活化剂,以及免疫调节化合物。因此,有必要进一步研究SB140在治疗神经炎症性疾病中的应用。多发性硬化和其它炎性神经病症的动物模型将是此类研究的合适选择。
    In the search for novel potent immunomodulatory nuclear factor-erythroid 2 related factor 2 (Nrf2) activators, a derivative of cholic bile acid, SB140, was synthesized. The synthesis of SB140 aimed to increase the electrophilic functionality of the compound, enhancing its ability to activate Nrf2. Effects of SB140 on microglial cells, myeloid-derived cells (MDC), and T cells were explored in the context of (central nervous system) CNS autoimmunity. SB140 potently activated Nrf2 signaling in MDC and microglia. It was efficient in reducing the ability of microglial cells to produce inflammatory nitric oxide, interleukin (IL)-6, and tumor necrosis factor (TNF). Also, SB140 reduced the proliferation of encephalitogenic T cells and the production of their effector cytokines: IL-17 and interferon (IFN)-γ. On the contrary, the effects of SB140 on anti-inflammatory IL-10 production in microglial and encephalitogenic T cells were limited or absent. These results show that SB140 is a potent Nrf2 activator, as well as an immunomodulatory compound. Thus, further research on the application of SB140 in the treatment of neuroinflammatory diseases is warranted. Animal models of multiple sclerosis and other inflammatory neurological disorders will be a suitable choice for such studies.
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  • 文章类型: Journal Article
    子宫内膜异位症是一种慢性炎症性疾病,其特征是子宫腔外子宫内膜样组织的异常生长,影响10-15%的育龄妇女。疼痛是最常见的症状。治疗方案包括手术,效果有限,复发率高,和药物治疗。激素疗法,通常用于症状管理,会有副作用和避孕效果,导致与子宫内膜异位症相关的不孕症,疼痛和病变经常在治疗停止后再次出现。在其病因因素中,免疫和炎症失调起着重要的作用,代表开发新的治疗策略的一个有趣的目标。这篇综述批判性地分析了最近的研究,以提供正在进行的研究的最新综合,以关注病变进展的潜在新药物疗法。疼痛缓解,提高生活质量。免疫疗法,天然的抗炎和抗氧化化合物和药物的再利用显示在解决当前治疗的局限性通过针对免疫因素,可能为子宫内膜异位症的疼痛和不孕症提供非侵入性解决方案。从体外和动物模型研究中获得了有希望的结果,但临床试验仍然有限。需要更多的努力将这些发现转化为临床实践,以有效地减少疾病进展,减轻疼痛症状并保持生殖能力,改善患者的整体健康。
    Endometriosis is a chronic inflammatory disorder characterized by the abnormal growth of endometrial-like tissue outside the uterine cavity, affecting 10-15% of women of reproductive age. Pain is the most common symptom. Treatment options include surgery, which has limited effectiveness and high recurrence rates, and pharmacotherapy. Hormonal therapies, commonly used for symptom management, can have side effects and contraceptive outcomes, contributing to the infertility associated with endometriosis, with pain and lesions often reappearing after treatment cessation. Among its etiological factors, immunological and inflammatory dysregulation plays a significant role, representing an interesting target for developing new therapeutic strategies. This review critically analyzes recent studies to provide an updated synthesis of ongoing research into potential new pharmacotherapies focusing on lesion progression, pain relief, and improving quality of life. Immunotherapy, natural anti-inflammatory and antioxidant compounds and drug repurposing show promise in addressing the limitations of current treatments by targeting immunological factors, potentially offering non-invasive solutions for managing pain and infertility in endometriosis. Promising results have been obtained from in vitro and animal model studies, but clinical trials are still limited. More effort is needed to translate these findings into clinical practice to effectively reduce disease progression, alleviate pain symptoms and preserve the reproductive capacity, improving patients\' overall wellbeing.
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  • 文章类型: Journal Article
    本研究旨在研究柑橘类黄酮金胆素和二十二碳六烯酸(DHA)的协同抗炎作用,n-3长链多不饱和脂肪酸之一,在组合。在没有细胞毒性的情况下,用天麻素和DHA同时处理协同抑制用脂多糖(LPS)刺激的小鼠巨噬细胞样RAW264.7细胞产生一氧化氮(组合指数<0.9)。另一方面,川陈皮素和DHA联合对促炎细胞因子产生的抑制作用没有协同作用。景别素和DHA均不影响LPS刺激的RAW264.7细胞的吞噬活性。免疫印迹分析显示,通过同时用山黄精处理,DHA对ERK和p38磷酸化以及NF-κB核易位的抑制作用显着增强。这可能导致协同抗炎作用。总的来说,我们的发现显示了川陈皮素和DHA联合使用具有协同抗炎作用的潜力.
    This study aimed to investigate a synergistic anti-inflammatory effect of a citrus flavonoid nobiletin and docosahexaenoic acid (DHA), one of n-3 long-chain polyunsaturated fatty acids, in combination. Simultaneous treatment with nobiletin and DHA synergistically inhibited nitric oxide production (combination index < 0.9) by mouse macrophage-like RAW 264.7 cells stimulated with lipopolysaccharide (LPS) without cytotoxicity. On the other hand, the inhibitory effect of nobiletin and DHA in combination on proinflammatory cytokine production was not synergistic. Neither nobiletin nor DHA affected the phagocytotic activity of RAW 264.7 cells stimulated with LPS. Immunoblot analysis revealed that the inhibition potency of DHA on the phosphorylation of ERK and p38 and nuclear translocation of NF-κB is markedly enhanced by simultaneously treating with nobiletin, which may lead to the synergistic anti-inflammatory effect. Overall, our findings show the potential of the synergistic anti-inflammatory effect of nobiletin and DHA in combination.
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  • 文章类型: Journal Article
    幽门螺杆菌感染影响了世界上50%以上的人口,并导致慢性炎症和胃部疾病,是与胃癌发展相关的主要病原体。增加抗生素抗性水平是全球关注的主要问题,需要替代疗法。大豆肽和其他化合物可能是治疗中避免的替代方法,根除和/或控制幽门螺杆菌感染的症状。本研究旨在使用蛋白质组学工具表征富含露纳辛的大豆提取物(LSE),并评估其抗氧化剂,抗幽门螺杆菌感染的抗炎和抗菌特性。通过LC-MS/MS分析,鉴定了124种蛋白质,其中2S白蛋白(lunasin和大链亚基)是第四丰富的蛋白质(8.9%)。Lunasin由44个氨基酸残基和一个分子内二硫键组成。低剂量(0.0625mg/mL)的LSE降低了幽门螺杆菌感染和未感染的AGS胃细胞中的ROS产生。这导致促炎性白介素(IL)-8水平显著降低6.71%。LSE还显示出对幽门螺杆菌的抗菌活性,这可以归因于其他大豆蛋白和酚类化合物。我们的研究结果表明,LSE可能是治疗幽门螺杆菌感染及其相关症状的一种有希望的替代方法。
    Helicobacter pylori infection affects over 50% of the world\'s population and leads to chronic inflammation and gastric disorders, being the main pathogen correlated to gastric cancer development. Increasing antibiotic resistance levels are a major global concern and alternative treatments are needed. Soybean peptides and other compounds might be an alternative in the treatment to avoid, eradicate and/or control symptoms of H. pylori infection. This study aimed to characterize a lunasin-enriched soybean extract (LSE) using proteomics tools and to evaluate its antioxidant, anti-inflammatory and antibacterial properties against H. pylori infection. By LC-MS/MS analysis, 124 proteins were identified, with 2S albumin (lunasin and large-chain subunits) being the fourth most abundant protein (8.9%). Lunasin consists of 44 amino acid residues and an intramolecular disulfide bond. LSE at a low dose (0.0625 mg/mL) reduced ROS production in both H. pylori-infected and non-infected AGS gastric cells. This led to a significant reduction of 6.71% in the levels of pro-inflammatory interleukin (IL)-8. LSE also showed antibacterial activity against H. pylori, which can be attributed to other soybean proteins and phenolic compounds. Our findings suggest that LSE might be a promising alternative in the management of H. pylori infection and its associated symptoms.
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  • 文章类型: Journal Article
    本研究介绍了通过常规方法从黑皮诺(PN)葡萄果渣中制备的乙醇提取物的特性,超声辅助或溶剂热提取。通过HPLC鉴定提取物的组分。多酚的总含量,黄酮类化合物,花青素,和浓缩的单宁,使用UV-vis光谱法评估提取物的抗氧化活性和α-葡萄糖苷酶抑制活性。所有提取物都富含酚类化合物,证明了良好的自由基清除活性。通过在80°C下常规提取获得的提取物显示出与(-)-表没食子儿茶素没食子酸酯接近的最佳α-葡萄糖苷酶抑制活性。为了提高多酚的化学稳定性,选择的提取物被掺入多孔二氧化硅基载体:胺官能化二氧化硅(MCM-NH2),岩藻依聚糖包覆的胺官能化二氧化硅(MCM-NH2-Fuc),MCM-41和硅藻土。PN提取物对革兰氏阳性金黄色葡萄球菌(MIC=156.25μg/mL)表现出优于对革兰氏阴性大肠杆菌(MIC=312.5μg/mL)的中等活性。PN提取物的生物相容性,游离并掺入MCM-NH2和MCM-NH2-Fuc,在RAW264.7小鼠巨噬细胞上进行评估,样品在10µg/mL浓度下显示出良好的细胞相容性。在这个浓度下,PN和PN@MCM-NH2-Fuc通过抑制NO产生减少炎症。评估了选定样品的抗COX和LOX酶的抗炎潜力,并将其与吲哚美辛和齐留通进行了比较。分别。当PN提取物负载在MCM-NH2-Fuc支持物上时,观察到最好的抗炎活性。
    This study presents properties of hydroethanolic extracts prepared from Pinot Noir (PN) grape pomace through conventional, ultrasound-assisted or solvothermal extraction. The components of the extracts were identified by HPLC. The total content of polyphenols, flavonoids, anthocyanins, and condensed tannins, as well as antioxidant activity and α-glucosidase inhibitory activity of extracts were evaluated using UV-vis spectroscopy. All extracts were rich in phenolic compounds, proving a good radical scavenging activity. The extract obtained by conventional extraction at 80 °C showed the best α-glucosidase inhibitory activity close to that of (-)-epigallocatechin gallate. To improve the chemical stability of polyphenols, the chosen extract was incorporated in porous silica-based supports: amine functionalized silica (MCM-NH2), fucoidan-coated amine functionalized silica (MCM-NH2-Fuc), MCM-41, and diatomite. The PN extract exhibited moderate activity against Gram-positive S. aureus (MIC = 156.25 μg/mL) better than against Gram-negative E. coli (MIC = 312.5 μg/mL). The biocompatibility of PN extract, free and incorporated in MCM-NH2 and MCM-NH2-Fuc, was assessed on RAW 264.7 mouse macrophage cells, and the samples showcased a good cytocompatibility at 10 µg/mL concentration. At this concentration, PN and PN@MCM-NH2-Fuc reduced the inflammation by inhibiting NO production. The anti-inflammatory potential against COX and LOX enzymes of selected samples was evaluated and compared with that of Indomethacin and Zileuton, respectively. The best anti-inflammatory activity was observed when PN extract was loaded on MCM-NH2-Fuc support.
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  • 文章类型: Journal Article
    整个金丝桃属。植物因其清热特性而被用于传统医学中,解毒,舒缓经络,放松肝脏,止血.在民间医学中,它经常用于治疗肝炎,感冒,扁桃体炎,还有瘀伤.对H.patulum新鲜成熟果实的30%乙醇提取物进行的植物化学研究已分离出两种新的pin烷型单萜苷1-2,称为patulumsideE-F,和三个新的链状单萜苷3-5,命名为patulumsideG-H,J.它们的结构是使用广泛的光谱技术确定的,如HR-ESI-MS,1D和2DNMR光谱,和电子圆二色性(ECD)计算。在LPS诱导的RAW264.7细胞中评价这些化合物的抗炎活性。这项研究代表了对H.patulum的首次全面植物化学研究,为进一步探索单萜苷奠定了基础。
    The whole Hypericum patulum Thunb. plant is utilized in traditional medicine for its properties of clearing heat, detoxifying, soothing meridians, relaxing the liver, and stopping bleeding. In folk medicine, it is frequently used to treat hepatitis, colds, tonsillitis, and bruises. Phytochemical investigation of a 30% ethanol extract of the fresh ripe fruits of H. patulum has resulted in the isolation of two new pinane-type monoterpenoid glycosides 1-2, named patulumside E-F, and three new chain-shaped monoterpenoid glycosides 3-5, named patulumside G-H, J. Their structures were determined using extensive spectroscopic techniques, such as HR-ESI-MS, 1D and 2D NMR spectroscopy, and electronic circular dichroism (ECD) calculation. The anti-inflammatory activities of these compounds were evaluated in the LPS-induced RAW264.7 cells. This research represents the inaugural comprehensive phytochemical study of H. patulum, paving the way for further exploration of monoterpenoid glycosides.
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  • 文章类型: Journal Article
    皮肤老化是一个不可避免的复杂的过程,其中,通过氧化应激。寻找抑制这种机制的天然来源是防止皮肤老化的有希望的方法。我们研究的目的是评估菜豆的胶束提取物中酚类化合物的组成。液相色谱-质谱(LC-MS)分析的结果表明,存在32种成分,包括酚酸,黄烷醇,黄烷-3-醇,黄烷酮,异黄酮,和其他化合物。随后,对提取物的抗氧化剂进行了评估,抗炎,抗胶原酶,抗弹性蛋白酶,抗酪氨酸酶,和细胞毒性,以及胶原蛋白合成的评价。结果表明,普通豆芽的胶束提取物具有很强的抗衰老性能。进行的WST-8(水溶性四唑盐)测定显示,与对照细胞相比,选择浓度的提取物以剂量依赖性方式显著增加人真皮成纤维细胞的增殖。在胶原合成方面观察到类似的趋势。我们的结果表明,菜豆芽的胶束提取物可以被认为是一种有前途的抗衰老化合物,可用于化妆品配方中。
    Skin aging is an inevitable and intricate process instigated, among others, by oxidative stress. The search for natural sources that inhibit this mechanism is a promising approach to preventing skin aging. The purpose of our study was to evaluate the composition of phenolic compounds in the micellar extract of Phaseolus vulgaris sprouts. The results of a liquid chromatography-mass spectrometry (LC-MS) analysis revealed the presence of thirty-two constituents, including phenolic acids, flavanols, flavan-3-ols, flavanones, isoflavones, and other compounds. Subsequently, the extract was assessed for its antioxidant, anti-inflammatory, anti-collagenase, anti-elastase, anti-tyrosinase, and cytotoxic properties, as well as for the evaluation of collagen synthesis. It was demonstrated that micellar extract from common bean sprouts has strong anti-aging properties. The performed WST-8 (a water-soluble tetrazolium salt) assay revealed that selected concentrations of extract significantly increased proliferation of human dermal fibroblasts compared to the control cells in a dose-dependent manner. A similar tendency was observed with respect to collagen synthesis. Our results suggest that micellar extract from Phaseolus vulgaris sprouts can be considered a promising anti-aging compound for applications in cosmetic formulations.
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