antifungal activity

抗真菌活性
  • 文章类型: Journal Article
    根据地中海地区循环蓝色生物经济的框架,这项研究的目的是评估从ChottElJerid分离的Ncardiopsishalophila菌株TN-X8产生的细胞外几丁质酶从Sfax港口获得的蓝色泳蟹(Portunussegnis)残留物的生物转化(Tozeur,突尼斯)。从多个极端放线菌的分析,确定菌株TN-X8仅利用60g/L的原始蓝梭子蟹作为其碳源和能源,在40°C孵育6天后,几丁质酶活性约为950U/mL。纯几丁质酶,命名为ChiA-NH30,是在热处理后获得的,然后进行硫酸铵分馏和Sephacryl®S-200柱层析。在pH3和75°C下观察到最大ChiA-Nh30活性。有趣的是,与环己脒相比,ChiA-Nh30对4种病原真菌表现出良好的抗真菌作用。此外,当使用胶体甲壳素作为底物时,ChiA-Nh30表现出比市售的壳聚糖糊精酶更高的催化效率。此外,ChiA-Nh30可以通过应用包封和包封-吸附技术固定。高岭土和木炭作为优良的粘合剂,导致改善的ChiA-Nh30稳定性。对于固定化的ChiA-Nh30,从20%(w/v)的蓝蟹残留物中释放的N-乙酰基-D-葡糖胺单体的产量增加了3.1(高岭土)和2.65(木炭)倍,分别。
    In accordance with the framework of the Circular Blue Bioeconomy in the Mediterranean region, the objective of this study was to evaluate the biotransformation of blue swimming crab (Portunus segnis) residues obtained from the port of Sfax by an extracellular chitinase produced by Nocardiopsis halophila strain TN-X8 isolated from Chott El Jerid (Tozeur, Tunisia). From the analysis of multiple extremophilic Actinomycetota, it was determined that strain TN-X8 exclusively utilized 60 g/L of raw blue swimming crab as its carbon and energy source, achieving a chitinase activity of approximately 950 U/mL following a 6-day incubation period at 40 °C. Pure chitinase, designated as ChiA-Nh30, was obtained after heat treatment, followed by ammonium sulfate fractionation and Sephacryl® S-200 column chromatography. The maximum ChiA-Nh30 activity was observed at pH 3 and 75 °C. Interestingly, compared with cyclohexamidine, ChiA-Nh30 showed a good antifungal effect against four pathogenic fungi. Furthermore, when using colloidal chitin as substrate, ChiA-Nh30 demonstrated a higher degree of catalytic efficiency than the commercially available Chitodextrinase®. In addition, ChiA-Nh30 could be immobilized by applying encapsulation and encapsulation-adsorption techniques. The kaolin and charcoal used acted as excellent binders, resulting in improved ChiA-Nh30 stability. For the immobilized ChiA-Nh30, the yield of N-acetyl-D-glucosamine monomers released from 20% (w/v) blue swimming crab residues increased by 3.1 (kaolin) and 2.65 (charcoal) times, respectively.
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  • 文章类型: Journal Article
    Hinokitiol是一种天然的广谱抗菌单萜,它被广泛用作食品中的防腐剂,化妆品和其他产品。在本研究中,研究了hinokitiol对植物病原菌菌核病的毒性作用。菌丝体生长抑制的EC50值为2.63μg/mL,并且在希诺和多菌灵之间没有正或负交叉抗性。制备了30%的Hinokitiol乳油,在菌核病和灰霉病的防治中具有良好的应用前景。Hinokitiol是一种有前途的用于茎和叶而不是种子和根的喷雾杀真菌剂。
    Hinokitiol is a natural broad-spectrum antimicrobial monoterpenoid, which is widely used as an antiseptic in food, cosmetics and other products. In the present study, the toxic actions of hinokitiol to the plant pathogen Sclerotinia sclerotiorum were investigated. The EC50 value for mycelial growth inhibition was 2.63 μg/mL, and there was no positive or negative cross-resistance between hinokitiol and carbendazim. The emulsifiable concentrate of 30% hinokitiol was prepared, which has excellent application prospect in the prevention of sclerotinia and gray mould. Hinokitiol is a promising spray fungicide for stems and leaves rather than seeds and roots.
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  • 文章类型: Journal Article
    肠道微生物群落是其宿主内各种过程的调控阵列的一部分,从营养到病原体控制。最近的证据表明,粪甲虫的肠道微生物群落释放具有抗真菌活性的物质。由于粪便中肠道微生物的巨大多样性,有可能发现具有抗真菌特性的新型化合物。我们测试了雌性粪甲虫的肠道微生物群落对9种植物病原真菌菌株(Colletotrichumasianum-339,C.asianum-340,C.kahawae-390,C.karstii-358,C.siamense-220,尖孢镰刀菌-ATCC338,Nectriotrichia-232,Verticillium-22。我们的测试包括三种粪甲虫的肠道微生物群落:Canthoncyanellus(辊甲虫),Digitonthophagusgazella(洞穴甲虫),和Onthophagusbatesi(洞穴甲虫),我们遵循双重对抗协议,即,我们在含有培养基的培养皿中,用每种甲虫的微生物群落挑战每种真菌菌株。我们的结果表明,三种粪甲虫的肠道微生物群落对9种植物病原性真菌菌株中的至少7种具有抗真菌活性。肉桂的肠道微生物群落显着降低了9种植物病原真菌菌株的菌丝生长;Canthoncyanellus和Digitonthophagusgazella的肠道微生物群落显着降低了7种菌株的菌丝生长。这些结果为研究粪甲虫肠道微生物群落中的新型抗真菌物质提供了基础。
    Gut microbial communities are part of the regulatory array of various processes within their hosts, ranging from nutrition to pathogen control. Recent evidence shows that dung beetle\'s gut microbial communities release substances with antifungal activity. Because of the enormous diversity of gut microorganisms in dung beetles, there is a possibility of discovering novel compounds with antifungal properties. We tested the antifungal activity mediated by gut microbial communities of female dung beetles against nine phytopathogenic fungi strains (Colletotrichum asianum-339, C. asianum-340, C. asianum-1, C. kahawae-390, C. karstii-358, C. siamense-220, Fusarium oxysporum-ATCC338, Nectria pseudotrichia-232, Verticillium zaelandica-22). Our tests included the gut microbial communities of three species of dung beetles: Canthon cyanellus (roller beetle), Digitonthophagus gazella (burrower beetle), and Onthophagus batesi (burrower beetle), and we followed the dual confrontation protocol, i.e., we challenged each fungal strain with the microbial communities of each species of beetles in Petri dishes containing culture medium. Our results showed that gut microbial communities of the three dung beetle species exhibit antifungal activity against at least seven of the nine phytopathogenic fungal strains. The gut microbial communities of Onthophagus batesi significantly decreased the mycelial growth of the nine phytopathogenic fungi strains; the gut microbial communities of Canthon cyanellus and Digitonthophagus gazella significantly reduced the mycelial growth of seven strains. These results provide a basis for investigating novel antifungal substances within gut microbial communities of dung beetles.
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  • 文章类型: Journal Article
    离子液体(IL)是具有广泛的工业和科学应用的令人感兴趣的化合物。它们有非凡的性能,例如它们许多物理性质的可调性,因此,他们的活动;以及合成方法的简易性。因此,它们成为催化的重要组成部分,提取,电化学,分析,生物技术,等。本研究通过最小抑制浓度(MIC)估算方法确定了各种基于咪唑鎓的离子液体对酿酒酵母的抗真菌活性。增加连接到咪唑鎓阳离子的烷基的长度,增强了IL的抗真菌活性,以及它们破坏细胞膜完整性的能力。在用IL处理的酿酒酵母细胞上进行的FTIR研究揭示了这些细胞的生化组成的改变。有趣的是,在连接的烷基的长度增加时,脂肪酸含量的变化与分子活性的增加同时发生。统计分析和机器学习方法证实了这一趋势。根据酿酒酵母细胞的FTIR光谱对抗真菌活性进行分类,预测准确率为83%,这表明制药和医药行业可以从机器学习方法中受益。此外,合成的离子化合物在药物和医学应用中表现出巨大的潜力。
    Ionic liquids (ILs) are interesting chemical compounds that have a wide range of industrial and scientific applications. They have extraordinary properties, such as the tunability of many of their physical properties and, accordingly, their activities; and the ease of synthesis methods. Hence, they became important building blocks in catalysis, extraction, electrochemistry, analytics, biotechnology, etc. This study determined antifungal activities of various imidazolium-based ionic liquids against yeast Saccharomyces cerevisiae via minimum inhibitory concentration (MIC) estimation method. Increasing the length of the alkyl group attached to the imidazolium cation, enhanced the antifungal activity of the ILs, as well as their ability of the disruption of the cell membrane integrity. FTIR studies performed on the S. cerevisiae cells treated with the ILs revealed alterations in the biochemical composition of these cells. Interestingly, the alterations in fatty acid content occurred in parallel with the increase in the activity of the molecules upon the increase in the length of the attached alkyl group. This trend was confirmed by statistical analysis and machine learning methodology. The classification of antifungal activities based on FTIR spectra of S. cerevisiae cells yielded a prediction accuracy of 83%, indicating the pharmacy and medicine industries could benefit from machine learning methodology. Furthermore, synthesized ionic compounds exhibit significant potential for pharmaceutical and medical applications.
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  • 文章类型: Journal Article
    念珠菌是最常见的真菌感染之一,与高发病率和死亡率相关。喹喔啉衍生物是一组显示有希望的抗微生物活性的小分子。本研究以两性霉素B为对照,探讨3-肼基喹喔啉-2-硫醇对念珠菌的杀菌效果。此外,我们旨在使用小鼠口腔念珠菌病模型评估3-肼基喹喔啉-2-硫醇的体内疗效。通过肉汤微量稀释法对56株念珠菌分离株进行了3-肼基喹喔啉-2-硫醇和两性霉素B的药敏试验。因此,评估和比较最小抑制浓度(MIC)。口腔念珠菌病小鼠模型用于评估3-肼基喹喔啉-2-硫醇的体内活性。本研究使用进展的微生物学评估和ELISA。3-肼基喹喔啉-2-硫醇对大多数白色念珠菌临床分离株比两性霉素B更有效。对光滑念珠菌和近针型念珠菌分离株的有效性更高。然而,对热带念珠菌分离株的效率各不相同。3-肼基喹喔啉-2-硫醇对库德里亚夫泽维毕赤酵母和lusitaniae也有效。3-肼基喹喔啉-2-硫醇在小鼠模型中显示针对白色念珠菌细胞ATCC10231的良好功效。3-肼基喹喔啉-2-硫醇对不同的念珠菌物种显示出有希望的抗真菌和抗炎活性。需要更多的测试和实验。
    Candida ranks as among the most frequently encountered fungal infections that associated with high morbidity and mortality. Quinoxaline derivatives are a group of small molecules that showed a promising antimicrobial activity. This study aimed to investigate the fungicidal effects of 3-hydrazinoquinoxaline-2-thiol against Candida in comparison with Amphotericin B in vitro as a reference. Also, we aim to assess the efficacy of 3-hydrazinoquinoxaline-2-thiol in vivo using mice oral candidiasis model. Fifty-six Candida isolates were subjected to susceptibility testing by broth microdilution method for 3-hydrazinoquinoxaline-2-thiol and Amphotericin B. Therefore, Minimal inhibitory concentrations (MIC) were assessed and compared. The oral candidiasis mice model was used to evaluate the activity of 3-hydrazinoquinoxaline-2-thiol in vivo. Microbiological evaluation of progression and ELISA were used in this study. 3-hydrazinoquinoxaline-2-thiol was more effective than Amphotericin B against most clinical isolates of Candida albicans. Higher effectiveness was seen against Candida glabrata and Candida parapsilosis isolates. However, the efficiency against Candida tropicalis isolates varies. 3-hydrazinoquinoxaline-2-thiol was also effective against Pichia kudriavzevii and Clavispora lusitaniae. 3-hydrazinoquinoxaline-2-thiol showed a good efficacy in mice model against C. albicans cells ATCC 10231. 3-hydrazinoquinoxaline-2-thiol has shown promising antifungal and anti-inflammatory activity against different Candida species. More tests and experiments are needed.
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  • 文章类型: Journal Article
    通过对七叶草甲醇树皮提取物的化学研究,分离出了一种新的黄烷酮,5,7,4\'-三羟基-3\',5'-双(3-甲基丁二烯基)黄烷酮(三重命名为苯丙酮)(1),连同七种已知的化合物,苦参素-V-4'-O-甲基醚(2),苦参素V(3),Calopocarpin(4),金雀异黄素(5)豆甾醇(6)和β-谷甾醇(7)和β-谷甾醇-3-O-β-D-吡喃葡萄糖苷(8)的混合物。通过广泛的光谱和光谱分析(1D和2DNMR,ESI-MS),并与以前报告的数据进行比较。1的绝对构型是基于其实验CD与类似化合物的CD的比较来推导的。所有化合物都经过了抗菌测试,抗真菌和抗氧化活性。化合物4对肠炎沙门氏菌表现出弱的抗菌活性,MIC值为62.5μg/mL。发现所有分离物在DPPH中作为抗氧化剂是无活性的,ABTS和FRAP测定。
    The chemical investigation of the methanol trunk bark extract of Erythrina senegalensis led to the isolation of a new flavanone, 5,7,4\'-trihydroxy-3\',5\'-bis(3-methylbutadienyl)flavanone (trivially named senegalensisnone) (1), together with seven known compounds, abyssinone-V-4\'-O-methyl ether (2), abyssinone V (3), Calopocarpin (4), genistein (5) mixture of stigmasterol (6) and β-sitosterol (7) and β-sitosterol-3-O-β-D-glucopyranoside (8). The structures of the isolates were elucidated by extensive spectroscopic and spectrometric analyses (1D and 2D NMR, ESI-MS) and by comparison with previously reported data. The absolute configuration of 1 was deduced based on comparison of its experimental CD with that of similar compound. All the compounds were tested for their antibacterial, antifungal and antioxidant activities. Compound 4 displayed weak antibacterial activity against Salmonella enteritidis with MIC value of 62.5 μg/mL. All the isolates were found to be inactive as antioxidant agents in the DPPH, ABTS and FRAP assays.
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  • 文章类型: Journal Article
    山梨酯a钠(SPA)是一种天然的植物来源的光敏剂,对某些植物病原真菌具有高的光活化抗真菌活性。然而,它对食管动物的杀菌效果,一种引起油茶叶斑病的新病原体,不清楚。
    在本研究中,我们探讨了其对D.mahothocarpus孢子萌发和菌丝生长的抑制作用。然后我们确定了它对细胞膜的影响,菌丝形态,氧化还原稳态,通过生物测定和细胞死亡。最后,RNA-seq进一步用于阐明其在转录水平上的作用模式。
    我们发现SPA有效地抑制了D.mahothocarpus的生长,抑制菌丝体生长和孢子萌发的半数有效浓度为1.059和2.287mg/mL,分别。1.0mg/mLSPA处理后,D.mahothocarpus的电导率和丙二醛含量显着增加。扫描电镜和透射电镜显示SPA显著影响D.mahothocarpus菌丝的形态和超微结构,表明SPA可以破坏菌丝形态和细胞结构,尤其是D.mahothocarpus的细胞膜.此外,转录组分析显示,SPA显著抑制形态学相关基因的表达,细胞膜通透性,和氧化应激。然后,我们还发现SPA显著促进了D.mahothocarpus的活性氧(ROS)的积累,虽然它降低了还原型谷胱甘肽的含量,抑制超氧化物歧化酶和过氧化氢酶的活性,并加剧DNA损伤.膜联蛋白V-FITC/PI染色也证实1.0mg/mLSPA可显著诱导细胞凋亡和坏死。
    一般来说,SPA可以诱导ROS介导的氧化应激和细胞死亡,从而破坏细胞膜和菌丝形态,最终抑制菌丝生长,这表明SPA有多种行动模式,为使用SPA作为替代植物来源的光活化杀真菌剂对抗油茶叶斑病提供科学依据。
    UNASSIGNED: Sodium pheophorbide a (SPA) is a natural plant-derived photosensitizer, with high photoactivated antifungal activity against some phytopathogenic fungi. However, its fungicidal effect on Diaporthe mahothocarpus, a novel pathogen that causes Camellia oleifera leaf spot blight, is unclear.
    UNASSIGNED: In the present study, we explored its inhibitory effects on spore germination and mycelial growth of D. mahothocarpus. Then we determined its effects on the cell membrane, mycelial morphology, redox homeostasis, and cell death through bioassay. Finally, RNA-seq was used further to elucidate its mode of action at the transcriptional level.
    UNASSIGNED: We found that SPA effectively inhibited the growth of D. mahothocarpus, with half-maximal effective concentrations to inhibit mycelial growth and spore germination of 1.059 and 2.287 mg/mL, respectively. After 1.0 mg/mL SPA treatment, the conductivity and malondialdehyde content of D. mahothocarpus were significantly increased. Scanning electron microscopy and transmission electron microscopy indicated that SPA significantly affected the morphology and ultrastructure of D. mahothocarpus hyphae, revealing that SPA can destroy the mycelial morphology and cell structure, especially the cell membrane of D. mahothocarpus. Furthermore, transcriptome analysis revealed that SPA significantly suppressed the expression of genes involved in morphology, cell membrane permeability, and oxidative stress. Then, we also found that SPA significantly promoted the accumulation of reactive oxygen species (ROS) in of D. mahothocarpus, while it decreased the content of reduced glutathione, inhibited the enzyme activities of superoxide dismutase and catalase, and exacerbated DNA damage. Annexin V-FITC/PI staining also confirmed that 1.0 mg/mL SPA could significantly induce apoptosis and necrosis.
    UNASSIGNED: Generally, SPA can induce ROS-mediated oxidative stress and cell death, thus destroying the cell membrane and hyphal morphology, and ultimately inhibiting mycelial growth, which indicates that SPA has multiple modes of action, providing a scientific basis for the use of SPA as an alternative plant-derived photoactivated fungicide against C. oleifera leaf spot blight.
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  • 文章类型: Journal Article
    一项针对新型抗真菌代谢物的研究鉴定了针对链霉菌属的丙酮提取物中关键植物病原体的有效体外抗真菌活性。菌株CA-296093。基于特征的分子网络揭示了抗霉素相关化合物的存在,导致分离出四种新化合物:escuzarmycinsA-D(1-4)。广泛的结构阐明,使用1D和2DNMR,高分辨率质谱,Marfey的分析,和噪声相关性,确认了他们的结构。测试了这些化合物对六种真菌植物病原体的生物活性,化合物3和4表现出很强的疗效,特别是针对ZymoseptoriaTritici,化合物3表现出最高效力(EC50:11nM)。两种化合物对灰葡萄孢菌和炭疽菌也显示出显著的抗真菌活性,化合物4被证明是最有效的。尽管对人类癌细胞系HepG2具有中等的细胞毒性,但化合物3和4仍可作为有希望的杀真菌剂用于对抗SeptoriaTritici斑点,炭疽病,和灰色霉菌。
    A study targeting novel antifungal metabolites identified potent in vitro antifungal activity against key plant pathogens in acetone extracts of Streptomyces sp. strain CA-296093. Feature-based molecular networking revealed the presence in this extract of antimycin-related compounds, leading to the isolation of four new compounds: escuzarmycins A-D (1-4). Extensive structural elucidation, employing 1D and 2D NMR, high-resolution mass spectrometry, Marfey\'s analysis, and NOESY correlations, confirmed their structures. The bioactivity of these compounds was tested against six fungal phytopathogens, and compounds 3 and 4 demonstrated strong efficacy, particularly against Zymoseptoria tritici, with compound 3 exhibiting the highest potency (EC50: 11 nM). Both compounds also displayed significant antifungal activity against Botrytis cinerea and Colletotrichum acutatum, with compound 4 proving to be the most potent. Despite moderate cytotoxicity against the human cancer cell line HepG2, compounds 3 and 4 emerge as promising fungicides for combating Septoria tritici blotch, anthracnose, and gray mold.
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  • 文章类型: Journal Article
    这篇综述的目的是介绍樟脑-双环单萜酮在预防皮肤感染中的潜在应用。皮肤病代表一组异质性疾病,其特征在于显著降低生活质量的延长症状。它们影响真皮,表皮,甚至是皮下组织.它们通常具有细菌或真菌背景。皮肤病学皮肤病的治疗是困难和长期的。因此,找到一个化合物很重要,最好是天然来源的,(i)防止这种感染的开始和(ii)支持皮肤的修复过程。根据其记录的抗炎作用,抗菌,抗真菌药,抗痤疮,麻醉剂,加强,和变暖特性,樟脑可用作皮肤传染病的预防措施,也可用作医疗和化妆品的成分。这项工作讨论了樟脑的结构和理化性质,它的发生,以及从天然来源以及通过化学合成获得它的方法。还介绍了樟脑在工业制剂中的用途。此外,在详细查阅文献后,樟脑的新陈代谢,它与其他药用物质的相互作用,讨论了其对皮肤病中涉及的细菌和真菌的抗微生物特性。
    The aim of this review is to present the potential application of camphor-a bicyclic monoterpene ketone-in the prevention of skin infections. Skin diseases represent a heterogeneous group of disorders characterized by prolonged symptoms that significantly diminish the quality of life. They affect the dermis, the epidermis, and even subcutaneous tissue. They very often have a bacterial or fungal background. Therapy for dermatological skin disorders is difficult and long-term. Therefore, it is important to find a compound, preferably of natural origin, that (i) prevents the initiation of this infection and (ii) supports the skin\'s repair process. Based on its documented anti-inflammatory, antibacterial, antifungal, anti-acne, anesthetic, strengthening, and warming properties, camphor can be used as a preventative measure in dermatological infectious diseases and as a component in medical and cosmetic products. This work discusses the structure and physicochemical properties of camphor, its occurrence, and methods of obtaining it from natural sources as well as through chemical synthesis. The use of camphor in industrial preparations is also presented. Additionally, after a detailed review of the literature, the metabolism of camphor, its interactions with other medicinal substances, and its antimicrobial properties against bacteria and fungi involved in skin diseases are discussed with regard to their resistance.
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  • 文章类型: Journal Article
    氟康唑(2-(2,4-二氟苯基)-1,3-双(1H-1,2,4-三唑-1-基)丙-2-醇),它于1981年获得专利,并于1988年引入商业用途,是一种广泛使用的抗真菌药物,其作用机理涉及抑制14-α羊毛甾醇脱甲基酶的活性。其安全性和有效性已将其确立为最常用的抗真菌剂之一。对唑类抗真菌药物的耐药性越来越普遍。它可能与编码该酶的基因的突变有关。为了解决这个问题,在氟康唑的三个主要区域修饰的分子,即羟基,芳香环,还有1,2,4-三唑环,已经被合成,试图创造更有效的抗真菌药物。这些修饰旨在增强对微生物的有效性并改善合成化合物的药代动力学参数和安全性。本文综述了氟康唑衍生物的合成,伴随着对评估这些化合物治疗效果的生物学研究结果的见解。
    Fluconazole (2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol), which was patented in 1981 and introduced for commercial use in 1988, is a widely utilized antifungal drug whose mechanism of action involves inhibition of the activity of 14-α lanosterol demethylase. Its safety and effectiveness have established it as one of the most frequently employed antifungal agents. Resistance to azole antifungal drugs is becoming more common. It may be related to a mutation of the gene encoding the enzyme. To address this issue, molecules with modifications in three main regions of fluconazole, namely the hydroxyl group, the aromatic ring, and the 1,2,4-triazole rings, have been synthesized in an attempt to create more potent antifungal drugs. These modifications aim at enhancing the effectiveness against microorganisms and improving pharmacokinetic parameters and safety profiles of the synthesized compounds. The present review explores the synthesis of fluconazole derivatives, accompanied by insights into the results of biological studies evaluating the therapeutic effects of these compounds.
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