Cyclooctanes

环辛烷
  • 文章类型: Journal Article
    五味子(S.chinensis)作为传统中药具有悠久的历史,有益于生命能量,补肾,使心脏平静,等。重要的是,五味子A(SA)是从中国五味子中提取的,显示出令人惊讶和令人满意的生物活性,包括消炎药,保肝,心血管保护,和抗肿瘤特性,在其他人中。在众多的药理作用中,SA对中枢受损神经具有更明显的保护作用,通过保护受损的神经细胞和增强抗氧化能力,改善神经退行性疾病,如阿尔茨海默氏症和帕金森氏症。药代动力学研究表明,SA具有快速吸收的药代动力学特征,分布广泛,肝脏中的最大浓度,主要是肾脏排泄。然而,肝脏和肠道首过代谢会影响SA的生物利用度。此外,SA的含量,作为中国药典的指标成分,不应低于0.40%,用高效液相色谱法(HPLC)测定复方中SA的含量,这是一种稳定可靠的方法,为后续质量控制奠定基础。因此,本文系统地回顾了准备工作,药理作用,药代动力学特性,和SA的内容确定,目的是更新和加深对SA的理解,为后期SA的研究提供理论依据。
    Schisandra chinensis (S. chinensis) has a long history as a traditional Chinese medicine that is astringent, beneficial to vital energy, tonifies the kidney, tranquilizes the heart, etc. Significantly, Schisandrol A (SA) is extracted from S. chinensis and shows surprising and satisfactory biological activity, including anti-inflammatory, hepatoprotective, cardiovascular protection, and antitumor properties, among others. SA has a more pronounced protective effect on central damaged nerves among its numerous pharmacological effects, improving neurodegenerative diseases such as Alzheimer\'s and Parkinson\'s through the protection of damaged nerve cells and the enhancement of anti-oxidant capacity. Pharmacokinetic studies have shown that SA has a pharmacokinetic profile with a rapid absorption, wide distribution, maximal concentration in the liver, and primarily renal excretion. However, hepatic and intestinal first-pass metabolism can affect SA\'s bioavailability. In addition, the content of SA, as an index component of S. chinensis Pharmacopoeia, should not be less than 0.40%, and the content of SA in S. chinensis compound formula was determined with the help of high-performance liquid chromatography (HPLC), which is a stable and reliable method, and it can lay a foundation for the subsequent quality control. Therefore, this paper systematically reviews the preparation, pharmacological effects, pharmacokinetic properties, and content determination of SA with the goal of updating and deepening the understanding of SA, as well as providing a theoretical basis for the study of SA at a later stage.
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  • 文章类型: Journal Article
    五味子属,木兰科的一员,是我国历史悠久的传统药用和功能性食品的著名补品中药。多糖是其主要活性成分之一,具有广泛的生物活性,如抗炎,抗肿瘤,神经保护,抗糖尿病,肝脏保护,免疫调节,和抗疲劳。在本文中,我们回顾了提取,隔离,净化,结构表征,生物活性,以及五味子属多糖的构效关系。总之,我们希望这篇综述可以为后续的结构研究提供参考,生物活性,五味子属多糖的开发与应用。
    The genus Schisandra, a member of the Magnoliaceae family, is a well-known tonic traditional Chinese medicine with a long history of traditional medicinal and functional food used in China. Polysaccharides are one of its main active constituents, which have a wide range of bioactivities, such as anti-inflammatory, anti-tumor, neuroprotection, anti-diabetes, hepatoprotection, immunomodulation, and anti-fatigue. In this paper, we review the extraction, isolation, purification, structural characterization, bioactivities, as well as structure-activity relationship of polysaccharides from the genus Schisandra. In conclusion, we hope that this review could provide reference for the subsequent research on structural, bioactivities, development and application of the genus Schisandra polysaccharides.
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  • 文章类型: Journal Article
    自古以来,中国已将天然药物作为抗击疾病的主要方法,并拥有丰富的天然药物库。随着时代的进步,从天然药物中提取生物活性分子已成为天然药物新的发展方向。在众多的天然药物中,五味子C(SchC),源自五味子(Turcz。)Baill。它具有极好的发展潜力,并已被证明具有各种药理特性,包括保肝,抗肿瘤和抗炎活性。基于保肝的生物学特性,有研究表明,戊糖苷具有改善肝纤维化症状、降低大鼠血清中丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)浓度的作用,这是抗肝纤维化药物开发的重要启示。但更多的体内和离体研究仍需纳入。本文重点研究了SchC的提取和合成,生物活性和药物开发进展。讨论了SchC的未来应用前景,以进一步完善其开发工作。
    Since ancient times, China has used natural medicine as the primary way to combat diseases and has a rich arsenal of natural medicines. With the progress of the times, the extraction of bioactive molecules from natural drugs has become the new development direction for natural medicines. Among the numerous natural drugs, Schisandrin C (Sch C), derived from Schisandra Chinensis (Turcz.) Baill. It has excellent potential for development and has been shown to possess various pharmacological properties, including hepatoprotective, antitumor and anti-inflammatory activities. Based on the biological properties of hepatoprotection, scholars have explored Sch C and its synthetic products in depth; some studies have shown that pentosidine has the effect of improving the symptoms of liver fibrosis and reducing the concentration of alanine transaminase (ALT) and aspartate aminotransferase (AST) in the serum of rats, which is an essential inspiration for the development of anti-liver fibrosis drugs. But more in vivo and ex vivo studies still need to be included. This paper focuses on Sch C\'s extraction and synthesis, biological activities and drug development progress. The future application prospects of Sch C are discussed to perfect its development work further.
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  • 文章类型: Journal Article
    五味子是广泛使用的传统药用植物五味子(Turcz。)Baill。这种化合物显示出镇静剂,催眠,抗衰老,抗氧化剂,和免疫调节特性,展示其在各种肝病中的有效性,同时保持良好的安全性。然而,五味子甲素的生物利用度在很大程度上受到肝脏和肠道首过代谢的影响,这限制了五味子素的临床疗效。在本文中,本文综述了五味子素的各种药理作用及相关机制,为后续药物研究提供参考,提升其药用价值。
    Schisandrin stands as one of the primary active compounds within the widely used traditional medicinal plant Schisandra chinensis (Turcz.) Baill. This compound exhibits sedative, hypnotic, anti-aging, antioxidant, and immunomodulatory properties, showcasing its effectiveness across various liver diseases while maintaining a favorable safety profile. However, the bioavailability of schisandrin is largely affected by hepatic and intestinal first-pass metabolism, which limits the clinical efficacy of schisandrin. In this paper, we review the various pharmacological effects and related mechanisms of schisandrin, in order to provide reference for subsequent drug research and promote its medicinal value.
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  • 文章类型: Journal Article
    五味子A(SA)是从中药五味子中分离出的一种生物活性木脂素。近年来,因其具有多种药理活性而受到广泛关注。本综述首次对SA相关药理作用和药代动力学特征进行综述。结果表明,SA具有多种药理作用,比如抗炎,抗癌,肝脏保护,抗氧化,神经保护,抗糖尿病,和肌肉骨骼保护。其中,NF-κB,Nrf2,MAPK,NLRP3,PI3K/AKT,Wnt,miRNA,P-GP,CYP450,PXR,和其他信号转导途径也参与其中。药代动力学研究表明,SA具有良好的药代动力学特征,但是这些受到其他因素的影响,如药物或肝纤维化。因此,SA具有多种药理作用和良好的药代动力学特征,未来值得进一步研究和发展。
    Schisandrin A (SA) is a bioactive lignan isolated from the traditional Chinese medicine Fructus schisandrae chinensis. In recent years, it has attracted extensive attention because of its multiple pharmacological activities. This review is the first to provide an overview of SA-related pharmacological effects and pharmacokinetic characteristics. The results showed that SA had many pharmacological effects, such as antiinflammation, anticancer, hepatoprotection, antioxidation, neuroprotection, antidiabetes mellitus, and musculoskeletal protection. Among them, NF-κB, Nrf2, MAPK, NLRP3, PI3K/AKT, Wnt, miRNA, P-gp, CYP450, PXR, and other signal transduction pathways are involved. Pharmacokinetic studies showed that SA had good pharmacokinetic characteristics, but these were affected by other factors, such as drugs or hepatic fibrosis. Thus, SA has a variety of pharmacological effects and good pharmacokinetic characteristics, which is worthy of further research and development in the future.
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  • 文章类型: Journal Article
    Nature is a vast source of bioactive molecules and has provided an active and efficient reservoir for drug discovery. Among natural compounds, one of the most promising is Schisandrin B (Sch B), isolated from Schisandra chinensis, which was documented to possess diversified pharmacokinetic propriety, among them antioxidant, anti-inflammation, cardioprotection, and neuroprotection. Due to its large biological properties, Sch B was recorded to be a potent cure for several diseases by targeting several signaling pathways. This review is aimed at emphasizing the recent data on the biological properties of Sch B among the molecular mechanism of this drug on tumoral, cardiac, and neural diseases. The data suggest that the antitumor activities of Sch B were mainly through apoptosis and cell cycle arrest at the diver\'s stage. It is reported that Sch B could be used as effective chemotherapy, neuroprotection, and cardioprotection since it possesses a spectrum of biological activities; however, further investigations on the mechanism of its action and preclinical trials are still mandatory to further validate the potential of this natural drug candidate.
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  • 文章类型: Journal Article
    BACKGROUND: With increasing use of pharmaceuticals, drug-induced liver injury (DILI) has become a significant therapeutic challenge to physicians all over the world. Drugs based on Schisandra fruits (SF for short, the fruits of Schisandra chinensis or Schisandra sphenanthera) or synthetic analogues of schisandrin C, are commonly prescribed for treating DILI in China.
    OBJECTIVE: This review summarizes the literature regarding the application of SF-derived drugs in patients with DILI and current understanding of mechanisms underlying the protective effects of SF against liver injury.
    METHODS: Keywords related to drug-induced liver injury and Schisandra fruits were searched in the following databases: Pubmed, Cochrane Library, Google Scholar, LiverTox, China National Knowledge Infrastructure (CNKI), Chinese Scientific Journal database (VIP), and Wanfang database. All studies, published in English or Chinese, were included. Clinical study exclusion criteria: if patients received other Chinese herbal medicines in a study, the study will not be included in this review.
    RESULTS: Clinical studies have shown that SF-derived drugs are effective in inhibiting drug-induced elevation of serum levels of alanine aminotransferase, aspartate transaminase and total bilirubin. Cellular and animal studies have demonstrated that crude SF extracts, lignan compounds found in SF, and SF-derived drugs are effective in protecting the liver against xenobiotic-induced injury. Regulation of cytochrome P450 enzyme activity, anti-oxidation, anti-inflammation and acceleration of liver regeneration are involved in the hepatoprotective mechanisms of SF.
    CONCLUSIONS: SF-derived drugs are effective in ameliorating DILI in China. To verify the clinical efficacy of these drugs, high-quality clinical studies are needed.
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  • 文章类型: Journal Article
    A toxicologic and dermatologic review of 1-[5(Or 6)-Methyl-7(or 8)-1-(methylethyl)bicyclo[2.2.2]oct-5-en-2-yl]ethan-1-one when used as a fragrance ingredient is presented. 1-[5(Or 6)-Methyl-7(or 8)-1-(methylethyl)bicyclo[2.2.2]oct-5-en-2-yl]ethan-1-one is a member of the fragrance structural group Alkyl Cyclic Ketones. These fragrances can be described as being composed of an alkyl, R1, and various substituted and bicyclic saturated or unsaturated cyclic hydrocarbons, R2, in which one of the rings may include up to 12 carbons. Alternatively, R2 may be a carbon bridge of C2-C4 carbon chain length between the ketone and cyclic hydrocarbon. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for 1-[5(Or 6)-Methyl-7(or 8)-1-(methylethyl)bicyclo[2.2.2]oct-5-en-2-yl]ethan-1-one were evaluated then summarized and includes physical properties, acute toxicity, skin irritation, mucous membrane (eye) irritation, skin sensitization, phototoxicity, photoallergy, and genotoxicity, data. A safety assessment of the entire Alkyl Cyclic Ketones will be published simultaneously with this document; please refer to Belsito et al., Belsito, D., Bickers, D., Bruze, M., Calow, P., Dagli, M., Fryer, A.D., Greim, H., Miyachi, Y., Saurat, J.H., Sipes, I.G., 2013. A Toxicologic and Dermatologic Assessment of Alkyl Cyclic Ketones When Used as Fragrance Ingredients. (submitted for publication)). for an overall assessment of the safe use of this material and all Alkyl Cyclic Ketones in fragrances.
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