Theaflavin

茶黄素
  • 文章类型: Journal Article
    目前,消费者越来越青睐对健康副作用较小的天然食品防腐剂。绿茶儿茶素和红茶茶黄素引起了相当大的兴趣,它们的抗菌作用在文献中被广泛报道。表儿茶素(EC),没有没食子酸酯部分的绿茶儿茶素,显示无杀菌活性,而茶黄素(TF),也缺乏没食子酸酯部分,表现出有效的杀菌活性,绿茶儿茶素和红茶茶黄素的抗菌作用与其破坏细菌细胞膜的能力密切相关。在我们目前的研究中,通过分子动力学模拟,探讨了TF和EC的膜相互作用模式和行为机制。已证明,与EC相比,TF对POPG双层表现出明显更强的亲和力。此外,托罗酮/儿茶酚环与酰基链部分的疏水相互作用可以显着促进TF渗透到POPG双层中。还发现间苯二酚/吡喃环是TF中与POPG双层形成氢键的关键官能团。我们相信,我们目前的研究结果可以提供有用的见解,以更好地了解TF与EC相比更强的抗菌作用。
    At present, consumers increasingly favored the natural food preservatives with fewer side-effects on health. The green tea catechins and black tea theaflavins attracted considerable interest, and their antibacterial effects were extensively reported in the literature. Epicatechin (EC), a green tea catechin without a gallate moiety, showed no bactericidal activity, whereas the theaflavin (TF), also lacking a gallate moiety, exhibited potent bactericidal activity, and the antibacterial effects of green tea catechins and black tea theaflavins were closely correlated with their abilities to disrupt the bacterial cell membrane. In our present study, the mechanisms of membrane interaction modes and behaviors of TF and EC were explored by molecular dynamics simulations. It was demonstrated that TF exhibited markedly stronger affinity for the POPG bilayer compared to EC. Additionally, the hydrophobic interactions of tropolone/catechol rings with the acyl chain part could significantly contribute to the penetration of TF into the POPG bilayer. It was also found that the resorcinol/pyran rings were the key functional groups in TF for forming hydrogen bonds with the POPG bilayer. We believed that the findings from our current study could offer useful insights to better understand the stronger antibacterial effects of TF compared to EC.
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  • 文章类型: Journal Article
    结节性皮肤病病毒(LSDV)感染是严重威胁全球养牛业的重大社会经济问题。这里,重组病毒LSDV-ΔTK/EGFP,表达增强型绿色荧光蛋白(EGFP),用同源重组系统构建并应用于抗病毒药物的高通量筛选。LSDV-ΔTK/EGFP在各种肾细胞系中复制,与野生型LSDV一致。细胞病变效应,病毒颗粒形态学,LSDV-ΔTK/EGFP的生长性能与野生型LSDV的生长性能一致。高通量筛选允许鉴定抑制LSDV-ΔTK/EGFP复制的几种分子。在体外筛选出100种抗病毒药物后,确定了茶黄素对LSDV的强抑制作用。感染时间分析表明,茶黄素在LSDV进入细胞和随后的病毒复制阶段中起作用。这种重组病毒的开发将有助于LSDV定向抗病毒药物的开发以及病毒复制和作用机制的研究。
    Lumpy skin disease virus (LSDV) infection is a major socio-economic issue that seriously threatens the global cattle-farming industry. Here, a recombinant virus LSDV-ΔTK/EGFP, expressing enhanced green fluorescent protein (EGFP), was constructed with a homologous recombination system and applied to the high-throughput screening of antiviral drugs. LSDV-ΔTK/EGFP replicates in various kidney cell lines, consistent with wild-type LSDV. The cytopathic effect, viral particle morphology, and growth performance of LSDV-ΔTK/EGFP are consistent with those of wild-type LSDV. High-throughput screening allowed to identify several molecules that inhibit LSDV-ΔTK/EGFP replication. The strong inhibitory effect of theaflavin on LSDV was identified when 100 antiviral drugs were screened in vitro. An infection time analysis showed that theaflavin plays a role in the entry of LSDV into cells and in subsequent viral replication stages. The development of this recombinant virus will contribute to the development of LSDV-directed antiviral drugs and the study of viral replication and mechanisms of action.
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  • 文章类型: Journal Article
    在这项研究中,建立了一种新的茶黄素(TF)的制备方法。我们的发现表明,使用冰浴(2-3°C)可显着增强TF的形成。此外,在冰浴条件下增加(-)-表没食子儿茶素(EGC)的比例可以进一步提高其收率。这种方法在3小时内防止了深色溶液的出现,有效保护TF免受氧化。我们对TF生成机理的研究表明,基于双环[3.2.1]辛烷型中间体的逆合成分析,具有两个碳阴离子的EGC-醌I(EGC-Q-I)可能作为合成子之一。随后,量子力学计算进一步支持了这一假设。实际应用:在这项研究中,我们开发了一种合成茶黄素(TF)的新方法,证明使用冰浴显著提高了产量。在冰浴下增加(-)-表没食子儿茶素(EGC)的比例,进一步提高TF产量,并防止溶液变黑至少3小时,从而保护TF免受氧化。我们的研究表明,基于双环[3.2.1]辛烷型中间体(BOI)的反合成分析,EGC-醌I是潜在的合成子。QM计算支持这一假设。
    In this study, a novel preparation method of theaflavin (TF) has been established. Our findings indicated that the formation of TF was significantly enhanced by using an ice bath (2-3°C). Additionally, increasing the ratio of (-)-epigallocatechin (EGC) under the ice bath could further improve its yield. This approach prevented the appearance of a dark solution within 3 h, effectively protecting TF from oxidation. Our study on the generation mechanism of TF suggested that EGC-quinone I (EGC-Q-I) with two carbanions could potentially serve as one of synthons based on the retrosynthetic analysis of the bicyclo[3.2.1]octane-type intermediate. Subsequently, quantum mechanical calculations further supported this hypothesis. Practical Application: In this study, we have developed a novel method for the synthesis of theaflavin (TF), demonstrating that the use of ice bath significantly enhanced its yield. Increasing the ratio of (-)-epigallocatechin (EGC) under the ice bath further improved TF yields and prevented darkening of the solution for at least 3 h, thereby protecting TF from oxidation. Our study suggested that EGC-quinone I is a potential synthon based on the retrosynthetic analysis of the bicyclo[3.2.1]octane-type intermediate (BOI). This hypothesis is supported by QM calculations.
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  • 文章类型: Journal Article
    氧化应激诱导的细胞凋亡是肾缺血再灌注损伤(RIRI)的重要病理过程。茶黄素(TF)是红茶中主要的活性色素和多酚。由于其生物活性,可以减少氧化应激并预防许多疾病,因此已被广泛报道。这里,探讨茶黄素在RIRI病理过程中的作用。在本研究中,建立C57BL/6J雄性小鼠缺血45min、再灌注24h的RIRI模型,茶黄素被用作干预措施。与RIRI组相比,肾脏过滤功能,茶黄素干预组肾组织损伤和抗氧化能力明显改善,而细胞凋亡水平降低。将TCMK-1细胞在缺氧下孵育48小时,然后复氧6小时以体外模拟RIRI。茶黄素的应用显著促进p53从细胞质到细胞核的易位,上调谷胱甘肽过氧化物酶1(GPx-1)在细胞中的表达,并抑制氧化应激损伤和细胞凋亡。p53siRNA转染可以部分抑制茶黄素的作用。因此,茶黄素通过调节p53/GPx-1通路抑制细胞凋亡和氧化应激对RIRI具有保护作用。我们得出结论,茶黄素有可能成为预防和治疗RIRI的候选药物。
    Oxidative stress-induced apoptosis is an important pathological process in renal ischemia/reperfusion injury (RIRI). Theaflavin (TF) is the main active pigment and polyphenol in black tea. It has been widely reported because of its biological activity that can reduce oxidative stress and protect against many diseases. Here, we explored the role of theaflavin in the pathological process of RIRI. In the present study, the RIRI model of 45 min ischemia and 24 h reperfusion was established in C57BL/6 J male mice, and theaflavin was used as an intervention. Compared with the RIRI group, the renal filtration function, renal tissue damage and antioxidant capacity of the theaflavin intervention group were significantly improved, while the level of apoptosis was reduced. TCMK-1 cells were incubated under hypoxia for 48 h and then reoxygenated for 6 h to simulate RIRI in vitro. The application of theaflavin significantly promoted the translocation of p53 from cytoplasm to nucleus, upregulated the expression of glutathione peroxidase 1 (GPx-1) in cells, and inhibited oxidative stress damage and apoptosis. Transfection with p53 siRNA can partially inhibit the effect of theaflavin. Thus, theaflavin exerted a protective effect against RIRI by inhibiting apoptosis and oxidative stress via regulating the p53/GPx-1 pathway. We conclude that theaflavin has the potential to become a candidate drug for the prevention and treatment of RIRI.
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  • 文章类型: Letter
    背景:寨卡病毒(ZIKV)的流行和感染最近对全球公共卫生安全构成了重大威胁。然而,目前缺乏针对ZIKV感染的特异性疫苗和有效的抗病毒药物。
    方法:通过评价四种茶黄素的体外抗寨卡病毒活性,选择茶黄素TF1和TF2。随后,在体内,我们研究了TF1和TF2对体重的影响,生存,组织病毒载量,和ZIKV感染小鼠的细胞因子。
    结果:我们比较了四种茶黄素(TF)在细胞中的抗ZIKV活性,发现TF1和TF2b通过抑制ZIKV的复制和释放,显著抑制了ZIKV/Z16006毒株在BHK和Vero细胞中的复制,而对于TF2a和TF3没有观察到类似的效果。体内试验,我们只发现TF2b提高了感染小鼠的存活率。在ZIKV感染小鼠的组织中,脾脏和血液中的病毒载量较高,其次是肝脏,附睾,和睾丸,肌肉最低。此外,TF2b处理显著降低细胞因子的表达(IL-6,IL-1β,ZIKV感染诱导的TNF-α)和趋化因子(CCL2,CCL5,CXCL10)。
    结论:这些发现表明TF2b具有有效的抗病毒作用,可用作治疗ZIKV感染的潜在候选药物。
    BACKGROUND: The prevalence and infection of the Zika virus (ZIKV) have recently posed a major threat to global public health security. However, there is currently a lack of specific vaccines and effective antiviral drugs for ZIKV infection.
    METHODS: Theaflavins TF1 and TF2 were selected by evaluating the anti-Zika virus activity of four kinds of theaflavins in vitro. Subsequently, in vivo, we investigated the effects of TF1 and TF2 on weight, survival, tissue viral load, and cytokines in ZIKV-infected mice.
    RESULTS: We compared the anti-ZIKV activity of four theaflavins (TFs) in cells and found that TF1 and TF2b significantly inhibited the replication of ZIKV/Z16006 toxic strain in BHK and Vero cells by inhibiting the replication and release of ZIKV, while no similar effects were observed for TF2a and TF3. In vivo assay, we only found that TF2b improved the survival rate of infected mice. In tissues of ZIKV-infected mice, the viral load was higher in spleen and blood, followed by liver, epididymis, and testis, the lowest in muscle. Additionally, TF2b treatment significantly reduced the expression of cytokines (IL-6, IL-1β, TNF-α) and chemokines (CCL2, CCL5, CXCL10) induced by ZIKV infection.
    CONCLUSIONS: These findings suggest that TF2b has a potent antiviral effect and can be used as a potential candidate for the treatment of ZIKV infection.
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  • 文章类型: Journal Article
    由金黄色葡萄球菌引起的感染目前是影响数百万人的全球威胁。金黄色葡萄球菌的致病性与多种毒力因子有关,包括细胞表面蛋白,多糖,分泌毒素.成孔α-溶血素,被称为α毒素,由几乎所有的金黄色葡萄球菌毒力菌株产生,并与包括皮肤和软组织感染在内的多种疾病有关,特应性皮炎,和肺炎。目前没有可用于预防金黄色葡萄球菌感染的疫苗,并且可获得的抗生素的效力正在消退。在这项研究中,我们使用AutoDockVina作为分子对接工具,通过分子对接研究了茶黄素-3,3'-digalate抗耐甲氧西林金黄色葡萄球菌的α-溶血素的抗溶血活性模式。茶黄素-3,3'-二等位基因对接Hla的分子序列(PDBID:7ahl)。获得的前10种结合模式的得分在-9.0至-8.5kcalmol-1之间,最佳结合模式为-9.0kcalmol-1。揭示了茶黄素-3,3'-digalate与Hla的“茎”结构域的直接结合位点,主要靶向残基Met113,Thr117,Asn139。这种潜在结合模式的公开保证了对茶黄素-3,3'-二烷基酯作为抗溶血化合物的进一步临床评估,以实际验证我们的结果。
    Infections caused by Staphylococcus aureus are currently a worldwide threat affecting millions of individuals. The pathogenicity of S. aureus is associated with numerous virulence factors, including cell surface proteins, polysaccharides, and secreted toxins. The pore-forming α-hemolysin, known as α-toxin, is produced by nearly all virulent strains of S. aureus and is implicated in several diseases including skin and soft tissue infections, atopic dermatitis, and pneumonia. There are currently no vaccines available for the prevention of S. aureus infections and the efficacy of available antibiotics has been fading. In this study we examined the mode of antihemolytic activity of theaflavin-3,3\'-digallate against α-hemolysin of methicillin-resistant S. aureus by molecular docking using AutoDock Vina as the molecular docking tool. The theaflavin-3,3\'-digallate docked the molecular sequence of the Hla (PDB ID:7ahl). The scores of the top 10 binding modes obtained were between -9.0 and -8.5 kcal mol-1, and the best binding mode was -9.0 kcal mol-1. Direct binding sites of theaflavin-3,3\'-digallate to the \"stem\" domain of Hla were revealed which primarily targeted of the residues Met113, Thr117, Asn139. The disclosure of this potential binding mode warrants further clinical evaluation of theaflavin-3,3\'-digallate as an anti-hemolytic compound in order to practically validate our results.
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  • 文章类型: Journal Article
    在这项研究中,探讨了茶黄素与肌球蛋白的相互作用机制,以证实茶黄素在肉类蛋白质系统中的潜在应用。制备了一系列茶黄素和肌球蛋白溶液用于光谱研究。光谱学结果表明,茶黄素与肌球蛋白形成复合物,并影响肌球蛋白的微环境。添加茶黄素会导致肌球蛋白溶液的静态猝灭。茶黄素和牛肌球蛋白通过疏水相互作用结合形成复合物,逐渐升高温度有利于茶黄素与牛肌球蛋白的结合。这种相互作用导致肌球蛋白的α-螺旋含量降低。分子动力学模拟结果证实,疏水相互作用和氢键使蛋白质结构更加紧凑和稳定。并对体外消化过程进行了模拟。结果表明,添加茶黄素能显著降低肌球蛋白的消化率。
    In this study, the interaction mechanism between theaflavin and myosin was explored to confirm the potential application of theaflavin in the meat protein system. A series of theaflavin and myosin solutions were prepared for spectroscopic studies. Spectroscopy results showed that theaflavins formed complexes with myosin and affected the microenvironment of myosin. And that addition of theaflavin cause static quenching of the myosin solution. Theaflavin and bovine myosin combined through hydrophobic interaction to form a complex, and gradually increasing the temperature was conducive to the binding of theaflavin and bovine myosin. This interaction results in a decrease in the α -helix content of myosin. Molecular dynamics simulation results confirmed that hydrophobic interactions and hydrogen bonds made the protein structure more compact and stable. And the in vitro digestion process was simulated. The results showed that the addition of theaflavin could significantly reduce the digestibility of myosin.
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  • 文章类型: Journal Article
    非洲猪瘟病毒(ASFV)是非洲猪瘟(ASF)的病原,这是养猪业中最有害的猪病之一,因为它在家猪中的死亡率接近100%,并造成无法估量的经济损失。自从ASF最初被报道以来,科学家一直致力于开发抗ASF疫苗;然而,目前尚无临床上有效的ASF疫苗。因此,制定预防ASFV感染和传播的新措施至关重要。在这项研究中,我们旨在研究茶黄素(TF)的抗ASF活性,一种主要从红茶中分离出来的天然化合物。我们发现TF在原代猪肺泡巨噬细胞(PAMs)中在非细胞毒性浓度下有效抑制ASFV复制。机械上,我们发现TF通过作用于细胞而不是直接与ASFV相互作用来抑制病毒复制,从而抑制ASFV复制.Further,我们发现TF在ASFV感染和未感染的细胞中上调AMPK(5'-AMP激活的蛋白激酶)信号通路,和用AMPK激动剂MK8722治疗上调AMPK信号传导途径并以剂量依赖性方式抑制ASFV增殖。值得注意的是,TF对AMPK激活和ASFV抑制的影响被AMPK抑制剂dorsomorphin部分逆转。此外,我们发现TF下调与脂质合成相关的基因的表达,并降低ASFV感染细胞中总胆固醇和总甘油三酯的细胞内积累,提示TF可能通过破坏脂质代谢来抑制ASFV的复制。总之,我们的结果表明,TF是一种ASFV感染抑制剂,并揭示了抑制ASFV复制的机制,为开发抗ASFV药物提供了新的机制和潜在的先导化合物。
    African swine fever virus (ASFV) is the etiological agent of African swine fever (ASF), which is one of the most harmful swine diseases in the pig industry because of its nearly 100% mortality rate in domestic pigs and results in incalculable economic loss. Ever since ASF was initially reported, scientists have worked to develop anti-ASF vaccines; however, currently no clinically effective vaccine for ASF is available. Therefore, the development of novel measures to prevent ASFV infection and transmission is essential. In this study, we aimed to investigate the anti-ASF activity of theaflavin (TF), a natural compound mainly isolated from black tea. We found that TF potently inhibited ASFV replication at non-cytotoxic concentrations ex vivo in primary porcine alveolar macrophages (PAMs). Mechanistically, we found that TF inhibited ASFV replication by acting on cells rather than interacting directly with ASFV to inhibit viral replication. Further, we found that TF upregulated the AMPK (5\'-AMP-activated protein kinase) signaling pathway in ASFV-infected and uninfected cells, and treatment with the AMPK agonist MK8722 upregulated the AMPK signaling pathway and inhibited ASFV proliferation in a dose-dependent manner. Notably, the effects of TF on AMPK activation and ASFV inhibition were partially reversed by the AMPK inhibitor dorsomorphin. In addition, we found that TF down-regulated the expression of genes related to lipid synthesis and decreased the intracellular accumulation of total cholesterol and total triglycerides in ASFV-infected cells, suggesting that TF may inhibit ASFV replication by disrupting lipid metabolism. In summary, our results demonstrated that TF is an ASFV infection inhibitor and revealed the mechanism by which ASFV replication is inhibited, providing a novel mechanism and potential lead compound for the development of anti-ASFV drugs.
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  • 文章类型: Journal Article
    当前调查的任务是阐明红茶的治疗和抗氧化观点。故意,红茶成分分析,多酚提取和抗氧化表征。此外,还通过溶剂分配法从红茶提取物中分离出茶黄素。最后,通过一项生物功效试验评估了分离的茶黄素的神经保护作用.结果表明,红茶显示出有希望的营养成分,特别涉及蛋白质和纤维。在萃取溶剂中,与甲醇和水相比,乙醇的性能更好,在60分钟后90分钟和30分钟观察到更高的提取。所有提取物都表明抗氧化活性通过显著的DPPH反映,TPC,FRAP,β-胡萝卜素分别为-69.13±3.00、1148.92±14.01、752.44±10.30和65.74±3.28。然而,对于TPC,分离的茶黄素表现出更高的抗氧化能力,分别为737.74±12.55、82.60±2.33和853.77±9.55,DPPH,和FRAP,分别,与提取物相比。在15天内,坐骨神经损伤和坐骨神经损伤物理诱导了疗效,并用离体茶黄素治疗。将总共12只健康的白化病小鼠随机分配到对照组(n=6)或茶黄素(5.0mg/kg(n=6))组。在这些群体中,行为测试用于评估和比较增强的功能恢复以及骨骼肌质量测量。血清样品包括氧化应激标志物。在茶黄素叶中,行为测试显示感觉运动功能恢复有统计学意义(p<.001)的改善,肌肉质量恢复,TOS大幅下降,TAC大幅增加,并增强抗氧化酶活性。考虑到茶黄素的上述治疗观点,目前的研究计划优化从红茶中分离茶黄素,并探讨其在小鼠模型中的神经保护作用。
    The mandate of the current investigation was to elucidate the therapeutic and antioxidant perspective of black tea. Purposely, black tea compositional analysis followed by polyphenol extraction and antioxidant characterization was done. Moreover, the theaflavin from black tea extract was also isolated through the solvent partition method. Lastly, the neuroprotective effect of isolated theaflavin was assessed through a bio-efficacy trial. The outcomes delineated that black tea showed promising nutritional composition with special reference to protein and fiber. Among the extraction solvent, ethanol performed better as compared to methanol and water likewise, higher extraction was noticed at 60 min followed by 90 and 30 min. All the extracts indicated antioxidant activity reflected through significant DPPH, TPC, FRAP, and beta carotene as-69.13 ± 3.00, 1148.92 ± 14.01, 752.44 ± 10.30, and 65.74 ± 3.28, respectively. However, isolated theaflavin exhibited higher antioxidant capacity as-737.74 ± 12.55, 82.60 ± 2.33, and 853.77 ± 9.55, for TPC, DPPH, and FRAP, respectively, as compared to extracts. In 15 days\' efficacy was physically induced with sciatic nerve injury h sciatic nerve injury physically and treated with isolated theaflavin. A total of 12 healthy albino mice were randomly assigned to either the control (n = 6) or theaflavin (5.0 mg/kg (n = 6)) groups. In these groups, behavioral tests were used to assess and compare enhanced functional recovery as well as skeletal muscle mass measurement. Serum samples included oxidative stress markers. In theaflavin leaves, behavioral tests revealed a statistically significant (p < .001) improvement in sensorimotor function restoration, muscle mass restoration, a substantial decrease in TOS, a significant increase in TAC, and enhanced antioxidative enzyme activity. Considering the above-mentioned therapeutic perspectives of theaflavin, the current research was planned to optimize the isolation of theaflavin from black tea and probed for their neuroprotective effect in mice models.
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  • 文章类型: Journal Article
    背景:预防龋齿一直是一个挑战。通过饮食干预预防龋齿有希望。研究表明,茶中存在的几种成分具有防龋特性。茶是广泛消费的饮料,因此可以用作合适的龋齿预防剂。这项研究的目的是确定红茶对实验动物龋齿进展的影响。
    方法:这项研究是在17天大的白化病幼鼠中进行的。这些动物被分成三组,每组八只动物。他们以致龋饮食(MIT200)喂养,并接种变异链球菌。第一组得到了麻省理工学院200的水,第二组用红茶放在MIT200上,将III组置于含有氟化水的MIT200上45天。45天后,动物在乙醚麻醉下被杀死,检查他们的牙齿是否有龋齿。
    结果:对每个象限前两个磨牙的龋齿病变进行评分。在每一组中,共检查了64颗牙齿。使用ANOVA比较上颌和下颌之间的龋齿评分。
    结论:从这项研究来看,可以推断,喝红茶可以减少以龋齿饮食喂养的幼鼠龋齿的发展。用于本研究的茶是使用无氟化物的水制备的,所以我们可以假设除了氟化物,某些成分存在于茶叶中,具有防龋特性。
    BACKGROUND: The prevention of dental caries has always remained a challenge. Caries prevention through dietary intervention holds promise. Studies have revealed that several constituents present in tea have anticariogenic properties. Tea is a widely consumed beverage and hence could be utilized as a suitable caries preventive agent. The purpose of this study was to determine the effect of black tea on caries progression in experimental animals.
    METHODS: This study was carried out in 17-day-old albino rat pups. The animals were divided into three groups, with eight animals in each group. They were fed on a cariogenic diet (MIT 200) and inoculated with Streptococcus mutans. Group I was given MIT 200 with water, Group II was placed on MIT 200 with black tea, and Group III was placed on MIT 200 with fluoridated water for a period of 45 days. After 45 days, the animals were killed under ether anesthesia, and their teeth were examined for caries.
    RESULTS: The carious lesions were scored for the first two molars in each quadrant. In each group, a total of 64 teeth were examined. The caries score between the upper and lower jaws was compared using ANOVA.
    CONCLUSIONS: From this study, it may be inferred that drinking black tea reduced the development of dental caries in young rats fed on a cariogenic diet. The tea used for this study was prepared using fluoride-free water, so we can assume that besides fluoride, certain components are present in tea leaves that possess anticariogenic properties.
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