ferulic acid

阿魏酸
  • 文章类型: Journal Article
    目的综合评价阿魏酸(FA)在阿尔茨海默病(AD)体外模型中对乙酰胆碱酯酶(AChE)酶活性和淀粉样β(Aβ)肽斑块形成的影响。背景:AD是一种以胆碱能信号中断为特征的进行性神经系统疾病,积累Aβ肽,和tau蛋白过度磷酸化。目前,目前尚无直接的抗阿尔茨海默病药物能有效预防AD导致的认知功能下降的报道.为了解决这个问题,解决几个分子方面的多靶点药物对于AD是理想的。天然化合物由于其可及性而优于合成药物,成本效益,和较低的毒性多酚消耗和预防AD之间的已证实的关联导致对FA的影响的研究,多酚化合物,乙酰胆碱酯酶酶活性和Aβ肽形成,AD的主要目标。材料和方法通过黄嘌呤氧化酶抑制活性评估FA的自由基清除能力。此外,还评估了FA对AChE酶和淀粉样β肽形成的抑制活性,以评估FA的神经保护潜力。结果结果表明,FA具有成为AChE抑制剂的潜力,从而有助于阻断AChE的活性,并减少淀粉样β斑块形成的发生率。此外,该化合物还表现出显著的抗氧化性能,这由黄嘌呤氧化酶抑制作用证明。结论从观察到的结果来看,与各自的标准相比,FA具有显着的抗氧化和神经保护作用。需要更多的研究来确定该化合物作为治疗神经退行性疾病如AD的功效和安全性,因为其在大脑中的AChE抑制作用的确切机制和程度仍然难以捉摸。一个强大的,选择性,迫切需要有效的药物来治疗AD患者和有发展该疾病风险的患者。
    Aim This study aims to comprehensively evaluate the effects of ferulic acid (FA) on acetylcholinesterase (AChE) enzyme activity and amyloid beta (Aβ) peptide plaque formation in an in vitro model of Alzheimer\'s disease (AD). Background AD is a progressive neurological condition marked by disrupted cholinergic signaling, accumulation of Aβ peptide, and tau protein hyperphosphorylation. Currently, no direct anti-Alzheimer drug that effectively prevents the cognitive decline from AD has been reported. To combat this, a multi-target drug addressing several molecular aspects would be ideal for AD. Natural compounds are preferred over synthetic drugs due to their accessibility, cost-efficiency, and lower toxicity The proven association between polyphenol consumption and the prevention of AD has led to the investigation of the effect of FA, a polyphenolic compound, on acetylcholinesterase enzyme activity and Aβ peptide formation, the key targets of AD. Materials and method The free radical scavenging ability of FA was assessed by xanthine oxidase inhibitory activity. Furthermore, FA was also evaluated for its inhibitory activity against AChE enzyme and amyloid beta peptide formation to evaluate the neuroprotective potential of FA. Results The results showed that FA has the potential to be an AChE inhibitor, thus helping in blocking the activity of AChE and also reducing the incidence of amyloid beta plaque formation. Furthermore, the compound also exhibited a significant antioxidant property which was demonstrated by the xanthine oxidase enzyme inhibitory effect. Conclusion From the observed results, FA has significant antioxidant and neuroprotective effects which are compared with those of their respective standards. More research is required to determine the efficacy and safety of this compound as a treatment for neurodegenerative diseases like AD because the precise mechanism and degree of its AChE inhibitory effects in the brain are still elusive. A potent, selective, and effective drug is desperately needed to treat patients with AD and those at risk of developing the disease.
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  • 文章类型: Journal Article
    在这项研究中,我们检查并比较了两种不同的基于脂质的纳米系统(LBN),即转铁蛋白体(TFs)和单油酸甘油酯水分散体(MAD),作为局部应用阿魏酸(FA)的输送系统,一种天然来源的抗氧化剂分子。我们的结果,正如弗朗兹细胞实验所证明的,表明用泊洛沙姆188在其组成中产生的LBN产生多层系统。该系统有效地控制药物的释放。尽管如此,我们发现非离子表面活性剂的类型可以影响药物的释放速率。关于FA从MAD的扩散,这显示了与TF相比更低的扩散速率。就体内应用而言,斑贴试验表明,当在闭塞条件下应用48小时时,所有测试的LBN制剂都是安全的。此外,人类皮肤活检用于确定含FA的制剂是否可以影响皮肤组织形态或提供针对O3暴露的保护。分析表明,用泊洛沙姆188和MAD制剂组成的TF治疗可能会防止结构性皮肤损伤(如在苏木精/伊红染色中观察到的)和氧化环境的发展(如4-hyroxinonenal(4HNE)表达水平所示)由O3暴露诱导。相比之下,不含活性成分的制剂不能提供对O3暴露有害影响的保护。Inizio模。
    In this study, we examined and compared two different lipid-based nanosystems (LBNs), namely Transferosomes (TFs) and Monoolein Aqueous Dispersions (MADs), as delivery systems for the topical application of Ferulic Acid (FA), an antioxidant molecule derived from natural sources. Our results, as demonstrated through Franz-cell experiments, indicate that the LBNs produced with poloxamer 188 in their composition create a multilamellar system. This system effectively controls the release of the drug. Nonetheless, we found that the type of non-ionic surfactant can impact the drug release rate. Regarding FA diffusion from the MAD, this showed a lower diffusion rate compared with the TF. In terms of an in vivo application, patch tests revealed that all LBN formulations tested were safe when applied under occlusive conditions for 48 h. Additionally, human skin biopsies were used to determine whether FA-containing formulations could influence skin tissue morphology or provide protection against O3 exposure. Analyses suggest that treatment with TFs composed of poloxamer 188 and MAD formulations might protect against structural skin damage (as observed in hematoxylin/eosin staining) and the development of an oxidative environment (as indicated by 4-hyroxinonenal (4HNE) expression levels) induced by O3 exposure. In contrast, formulations without the active ingredient did not offer protection against the detrimental effects of O3 exposure.Inizio modulo.
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  • 文章类型: Journal Article
    阿魏酸是西兰花的重要生物活性成分,小麦,和米糠,也是经过重大研究的重要天然产品。阿魏酸的精确作用方式和对系统水平蛋白质网络的影响尚未得到彻底研究。使用STRING数据库和Cytoscape工具构建了一个交互组,利用从PubMed文献中收集的788种关键蛋白质来鉴定阿魏酸对蛋白质相互作用网络(PIN)的调控作用。阿魏酸重新布线的PIN的无标度生物网络是高度互连的。我们发现了使用MCODE工具进行亚模块化分析的15个子模块和153个富集的信号通路。Further,顶级瓶颈蛋白的功能富集揭示了FoxO信号通路参与增强细胞对氧化应激的防御。阿魏酸重新连接的PIN的关键调节蛋白的选择是通过进行拓扑特征的分析完成的,例如GO术语/途径分析。学位,瓶颈,分子对接,和动态调查。目前的研究得出了阿魏酸对人体作用的精确分子机制。这种深入的硅模型将有助于理解阿魏酸如何在人体中产生其抗氧化和清除特性。由RamaswamyH.Sarma沟通。
    Ferulic acid is a crucial bioactive component of broccoli, wheat, and rice bran and is also an essential natural product that has undergone significant research. Ferulic acid\'s precise mode of action and effect on system-level protein networks have not been thoroughly investigated. An interactome was built using the STRING database and Cytoscape tools, utilizing 788 key proteins collected from PubMed literature to identify the ferulic acid-governed regulatory action on protein interaction network (PIN). The scale-free biological network of ferulic acid-rewired PIN is highly interconnected. We discovered 15 sub-modules using the MCODE tool for sub-modulization analysis and 153 enriched signaling pathways. Further, functional enrichment of top bottleneck proteins revealed the FoxO signaling pathway involved in enhancing cellular defense against oxidative stress. The selection of the critical regulatory proteins of the ferulic acid-rewired PIN was completed by performing analyses of topological characteristics such as GO term/pathways analysis, degree, bottleneck, molecular docking, and dynamics investigations. The current research derives a precise molecular mechanism for ferulic acid\'s action on the body. This in-depth in silico model would aid in understanding how ferulic acid origins its antioxidant and scavenging properties in the human body.Communicated by Ramaswamy H. Sarma.
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  • 文章类型: Comparative Study
    生物膜细胞对食品工业中常用的消毒剂表现出比它们的浮游对应物更高的抗性。酚酸是有希望的替代品,提供比传统抗生素更小的选择压力。本研究旨在评估阿魏酸(FA)和对香豆酸(p-CA)对肠炎沙门氏菌生物膜形成的抑制作用,并探讨其潜在的抑制机制。FA和p-CA的最小抑制浓度(MIC)分别为1.0和0.5mg/ml,分别。亚抑制浓度(1/8MIC)显着降低了生物膜的形成,而没有生长抑制作用。当暴露于亚MIC浓度的FA和p-CA时,肠炎沙门氏菌生物膜的生物量和细胞外聚合物(EPS)以及细菌游动和趋化能力显着降低。这两种酚酸对与鞭毛运动有关的蛋白质显示出高亲和力,并抑制了肠炎沙门氏菌生物膜形成相关的基因表达。此外,这两种酚酸在模拟食品加工条件下保持了很高的抗生物膜效率。本研究为肠炎沙门氏菌对这两种酚酸的多种表型和分子反应提供了有价值的信息。
    Biofilm cells exhibit higher resistance than their planktonic counterparts to commonly used disinfectants in food industry. Phenolic acids are promising substitute offering less selective pressure than traditional antibiotics. This study aims to evaluate the inhibitory effects of ferulic acid (FA) and p-coumaric acid (p-CA) on Salmonella Enteritidis biofilm formation and explore the underlying inhibitory mechanisms. The minimal inhibitory concentration (MIC) of FA and p-CA were 1.0 and 0.5 mg/ml, respectively. The sub-inhibitory concentration (1/8 MIC) significantly decreased biofilm formation without growth inhibitory effects. The biomass and extracellular polymeric substances (EPS) of S. Enteritidis biofilm as well as the bacterial swimming and chemotaxis abilities were significantly decreased when exposed to sub-MIC concentrations of FA and p-CA. These two phenolic acids showed high affinity to proteins involved in flagella motility and repressed the S. Enteritidis biofilm formation-related gene expressions. Furthermore, these two phenolic acids maintained high antibiofilm efficiency in simulated food processing conditions. This study provided valuable information of multiple phenotypic and molecular responses of S. Enteritidis to these two phenolic acids.
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  • 文章类型: Journal Article
    背景:桃红四物汤(THSWD)是基于妇科第一配方。它广泛用于各种血瘀和虚证,主要在妇科血瘀,月经不调,痛经.THSWD对中药有很大的需求,妇科,骨科,和内科。根据古典记录,三种药材,即地黄,当归,和红花,用在THSWD中需要用“黄酒洗”。在中医方剂的研究中,药材的加工方法不仅要遵循传统的记载,还要考虑现代的技术条件。经典方剂中的许多药材都涉及黄酒加工。确定药材的炮制方法是经典方剂研发的重点和难点问题。
    目的:以THSWD为代表,本研究分析了无处理方法之间的差异,现代加工方法“用黄酒炒料,“黄酒”和“黄酒”的传统加工方法洗涤。\“我们集中在三个方面:组成,功效,和内源性代谢。本研究旨在为经典方剂药材的炮制方法研究提供参考。
    方法:使用UPLC-Q-OrbitrapHRMS对THSWD的主要化学化合物进行快速鉴定和分类。使用苯甲酸雌二醇联合催产素建立原发性痛经(PD)模型。潜伏期和扭体时间;血清PGF2α水平,观察PGE2,ET-1和β-EP;和子宫的病理切片以确定它们的药效学差异。采用GC-TOF/MS分析大鼠血清代谢产物的差异。
    结果:共鉴定出54种活性化合物,结果表明,黄酒加工后,catalpol和rehmapicroside消失了。与传统方法加工的材料相比,15种成分的相对含量,如5-羟甲基糠醛和洋地黄C,用现代方法加工的材料增加了。然而,16种成分的相对含量,如羟基红花黄色素A,Verbascoside,和阿魏酸,在现代加工方法中有所下降。现代和经典的加工方法通过不同的代谢途径作用于PD。通过经典加工方法获得的THSWD主要通过抗炎和雌激素代谢途径治疗PD,而通过现代加工方法获得的THSWD主要通过抗炎代谢途径治疗PD。
    结论:该研究揭示了不同黄酒加工方法在获得的THSWD化学成分方面的差异,以及治疗PD的作用机制。本研究为THSWD的临床应用及经典方剂的研制提供了参考。
    BACKGROUND: Taohong Siwu Decoction (THSWD) is based on the \"First Recipe of Gynecology.\" It is widely used in various blood stasis and deficiency syndromes, mainly in gynecological blood stasis, irregular menstruation, and dysmenorrhea. THSWD has great demand in traditional Chinese medicine (TCM), gynecology, orthopedics, and internal medicine. According to classical records, three medicinal materials, namely Rehmanniae radix, Angelica sinensis, and Carthamus tinctorius, used in THSWD need to be \"washed with yellow rice wine.\" In the study of TCM prescriptions, the processing methods of medicinal materials not only needed to follow traditional records but also should consider modern technical conditions. Many medicinal materials in the repertoire of classical prescriptions involve yellow rice wine processing. Determining the processing method for medicinal materials is a key and difficult problem in the research and development of classical prescriptions.
    OBJECTIVE: With THSWD as the representative, this study analyzed differences between no processing method, the modern processing method of \"stir-frying the materials with yellow rice wine,\" and the traditional processing method of \"washing with yellow rice wine.\" We focused on three aspects: composition, efficacy, and endogenous metabolism. This study aimed to provide a reference for research on the processing methods of medicinal materials used in classical prescriptions.
    METHODS: UPLC-Q-Orbitrap HRMS was used to quickly identify and classify the main chemical compounds of THSWD. A model of primary dysmenorrhea (PD) was established using estradiol benzoate combined with oxytocin. The latent period and writhing time; the levels of serum PGF2α, PGE2, ET-1, and β-EP; and the pathological sections of the uterus were observed to determine their pharmacodynamic differences. GC-TOF/MS was used to analyze the differences in serum metabolites in rats.
    RESULTS: A total of 54 active compounds were identified, and the results showed that catalpol and rehmapicroside disappeared following yellow rice wine processing. Compared with materials processed by the traditional method, the relative contents of 15 components, such as 5-hydroxymethylfurfural and digitalis C, increased in materials processed by the modern method. However, the relative contents of 16 components, such as hydroxysafflor yellow A, verbascoside, and ferulic acid, decreased in the modern processing method. The modern and classic processing methods acted on PD through different metabolic pathways. THSWD obtained by classical processing methods mainly treated PD through anti-inflammatory and estrogen metabolism pathways, whereas THSWD obtained by modern processing methods mainly treated PD through anti-inflammatory metabolic pathways.
    CONCLUSIONS: The study revealed the differences in different yellow rice wine processing methods in terms of chemical composition of the THSWD obtained, as well as the mechanisms of action for the treatment of PD. This study provides a reference for the clinical application of THSWD and development of classical prescription preparations.
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  • 文章类型: Journal Article
    化妆品工业对使用对人类安全的天然和可持续来源的化合物越来越感兴趣,这鼓励了可以满足这些需求的方法的开发。绿原酸(CHA),咖啡酸(CAF)和阿魏酸(FA)是化妆品工业中广泛使用的三种化合物,因为它们具有抗氧化剂的功能,胶原蛋白改性剂甚至作为辐射防护剂。在这项工作中,采用两种先进的超临界CO2分离技术从金盏花中获得这三种化合物,然后使用计算皮肤渗透率模型对其进行评估。该模型包含在COSMO-RS模型中,其计算使得研究化合物在表皮中的行为成为可能。结果表明,CAF和FA都保留在角质层中,而CHA设法渗透到棘层。使用响应面方法通过用超临界CO2进行反溶剂分馏来浓缩这些化合物,以研究压力和CO2流速的影响。CHA,CAF和FA完全保留在沉淀容器中,浓度比原始提取物高40%至70%。该条件预测实现的最佳总收率和富集将是153巴和42g/min。
    The growing interest in the cosmetic industry in using compounds of natural and sustainable origin that are safe for humans is encouraging the development of processes that can satisfy these needs. Chlorogenic acid (CHA), caffeic acid (CAF) and ferulic acid (FA) are three compounds widely used within the cosmetic industry due to their functionalities as antioxidants, collagen modifiers or even as radiation protectors. In this work, two advanced separation techniques with supercritical CO2 are used to obtain these three compounds from Calendula officinalis, and these are then evaluated using a computational skin permeability model. This model is encompassed by the COSMO-RS model, the calculations of which make it possible to study the behaviour of the compounds in the epidermis. The results show that both CAF and FA are retained in the stratum corneum, while CHA manages to penetrate to the stratum spinosum. These compounds were concentrated by antisolvent fractionation with super-critical CO2 using a Response Surface Methodology to study the effect of pressure and CO2 flow rate. CHA, CAF and FA were completely retained in the precipitation vessel, with concentrations between 40% and 70% greater than in the original extract. The conditions predicted that the optimal overall yield and enrichment achieved would be 153 bar and 42 g/min.
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  • 文章类型: Journal Article
    mexametric(黑色素和红斑指数)的光老化迹象的评估,角膜测量(水合水平),在用抗坏血酸和阿魏酸处理后进行切割(弹性)检查。这项研究是在一组20名39-61岁(平均年龄54岁)的女性中进行的,FitzpatrickII型和III型皮肤.该研究包括每周进行一次的一系列8次治疗。两层剥皮,施用基于14%阿魏酸(脸的左半部分)和12%L-抗坏血酸血清(脸的右半部分)。要确定皮肤参数:水分,弹性,黑色素水平,和红斑强度,多探针适配器系统(勇气+Khazaka电子有限公司,科隆,德国)被使用。此外,在一系列治疗前后,使用标准化摄影系统Fotomedicus(Elfo®)拍摄照片。两种酸的黑色素水平和红斑强度的mexametric测量结果均具有统计学意义(P<0.0001)。证明抗坏血酸对皮肤的增亮作用稍大。阿魏酸和抗坏血酸水合水平的角化测量结果均具有统计学意义(P<0.0001)。最早可以在8周后观察到弹性改善的第一个有益变化,但柔韧性的增加随时间增加(12周后)。这些变化影响酸和所有测量点。参数的变化具有高度统计学意义(P<0.0001)。根据所进行的研究,不可能说明哪种测试的酸在减少光老化症状方面更有效。两种酸(抗坏血酸和阿魏酸),它们具有很高的抗氧化潜力,影响皮肤的可测量参数:色素沉着(黑色素指数),红斑(红斑指数),皮肤水合作用,和弹性。本文受版权保护。保留所有权利。
    The assessment of the signs of photoaging in mexametric (melanin and erythema index), corneometric (hydration level), and cutometric (elasticity) examination after the treatment with ascorbic acid and ferulic acid. This study was conducted in a group of 20 women aged 39-61 (mean age 54), with Fitzpatrick skin types II and III. The study included a series of 8 treatments performed once a week. Two layers of peeling, based on 14% ferulic acid (left half of the face) and 12% L-ascorbic acid serum (right half of the face) were applied. To determine skin parameters: moisture, elasticity, melanin level, and erythema intensity, the Multi Probe Adapter Systems (Courage + Khazaka electronic GmbH, Köln, Germany) were used. Additionally, before and after the series of treatments, photographs were taken with the standardized photographic system Fotomedicus (Elfo®). The results of mexametric measurement for melanin level and erythema intensity were statistically significant (P < 0.0001) for both acids. Slightly greater lightening of the skin was demonstrated for ascorbic acid. The results of corneometric measurement of hydration level for ferulic acid and ascorbic acid were both statistically significant (P < 0.0001). First beneficial changes in improved elasticity could be observed as early as after 8 weeks but the increase in flexibility grew with time (after 12 weeks). These changes affected both acids and all measurement points. The changes in parameters were highly statistically significant (P < 0.0001). Based on the conducted research, it is not possible to state which of the tested acids is more effective in reducing the symptoms of photoaging. Both acids (ascorbic and ferulic), which have a high antioxidant potential, affect the measurable parameters of the skin: pigmentation (melanin index), erythema (erythema index), skin hydration, and elasticity. This article is protected by copyright. All rights reserved.
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  • 文章类型: Journal Article
    Ferulic acid (FA) is used in skin formulations for protection against the damaging actions of the reactive oxygen species (ROS) produced by UVA radiation. Possible underlying protective mechanisms are not fully elucidated. By considering the kinetics of proton-coupled electron transfer (PCET) and radical-radical coupling (RRC) mechanisms, it appears that direct scavenging could be operative, providing that a high local concentration of FA is present at the place of •OH generation. The resulting FA phenoxyl radical, after the scavenging of a second •OH and keto-enol tautomerization of the intermediate, produces 5-hydroxyferulic acid (5OHFA). Inhibition of the lipoxygenase (LOX) enzyme, one of the enzymes that catalyse free radical production, by FA and 5OHFA were analysed. Results of molecular docking calculations indicate favourable binding interactions of FA and 5OHFA with the LOX active site. The exergonicity of chelation reactions of the catalytic Fe2+ ion with FA and 5OHFA indicate the potency of these chelators to prevent the formation of •OH radicals via Fenton-like reactions. The inhibition of the prooxidant LOX enzyme could be more relevant mechanism of skin protection against UVA induced oxidative stress than iron chelation and assumed direct scavenging of ROS.
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  • 文章类型: Journal Article
    皮质类固醇如布地奈德可有效减少不同器官的局部炎症过程。布地奈德在呼吸系统疾病中的治疗用途,比如哮喘,慢性阻塞性肺疾病,过敏性鼻炎是众所周知的。然而,布地奈德的肺部分布尚不清楚,主要是由于在不添加标记的情况下难以追踪肺样品中的分子。在本文中,我们提出了一种基质辅助激光解吸/电离质谱成像方案,该方案可用于观察表面活性剂耗尽的成年兔的布地奈德的肺部分布.考虑到布地奈德不易被MALDI电离,我们开发了一种使用Girard试剂P的组织上衍生方法,然后将阿魏酸沉积为MALDI基质。有趣的是,这种样品制备方案的结果是一个非常有效的策略,以提高敏感性不仅布地奈德,而且其他皮质类固醇,使我们能够追踪其分布并量化肺部样本中的药物。
    Corticosteroids as budesonide can be effective in reducing topic inflammation processes in different organs. Therapeutic use of budesonide in respiratory diseases, like asthma, chronic obstructive pulmonary disease, and allergic rhinitis is well known. However, the pulmonary distribution of budesonide is not well understood, mainly due to the difficulties in tracing the molecule in lung samples without the addition of a label. In this paper, we present a matrix-assisted laser desorption/ionization mass spectrometry imaging protocol that can be used to visualize the pulmonary distribution of budesonide administered to a surfactant-depleted adult rabbit. Considering that budesonide is not easily ionized by MALDI, we developed an on-tissue derivatization method with Girard\'s reagent P followed by ferulic acid deposition as MALDI matrix. Interestingly, this sample preparation protocol results as a very effective strategy to raise the sensitivity towards not only budesonide but also other corticosteroids, allowing us to track its distribution and quantify the drug inside lung samples.
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  • 文章类型: Journal Article
    We conducted a multicenter, randomized, double-blind, placebo-controlled prospective trial examining a supplement containing ferulic acid and Angelica archangelica extract (Feru-guard ®) for mild cognitive impairment (MCI). In the intention-to-treat population, Mini-Mental State Examination (MMSE) scores were significantly better at 24 weeks (p = 0.041) in the active group. In the per protocol population, MMSE was significantly better in the active group at 24 weeks (p = 0.008), and mixed effect models for repeated measures (MMRM) showed significant difference (p = 0.016). ADAS-Jcog was significantly better at 24 (p = 0.035) and 48 weeks (p = 0.015) in the active group, and MMRM was significant (p = 0.031). Thus, Feru-guard ® may be useful for MCI.
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