Polycyclic Compounds

多环化合物
  • 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
    Dechlorane Plus is a polychlorinated compound which has exclusively anthropic origin. This compound has been manufactured for close to 60 years for various applications, but mainly as flame retardant. Dechlorane Plus and other Dechlorane-related compounds (DRCs) are currently marketed as a replacement for Dechlorane, also known as Mirex, banned in 1978. These compounds share comparable properties to persistent organic pollutants (POPs), such as persistence in the environment, high lipophilicity, bioaccumulation through the food web and adverse effects on the environment and human health. Despite their long production history, they have been only recently reported in various environmental compartments, such as air, soil, and foodstuff. The aim of this review is to provide a picture of the current state of knowledge on worldwide DRC levels in food, in order to highlight gaps and research needs. The review compares the data on DRC contamination available in literature, considering different food categories and sampling country. In addition, it is specified whether the data were obtained from studies on foodstuff to estimate dietary intake, to evaluate the contamination near the e-waste treatment area or for environmental monitoring purposes.
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  • 文章类型: Journal Article
    Dechlorane Plus (DP) is an unregulated, highly chlorinated flame retardant. It has been manufactured from past 40 years but its presence in the environment was initially reported in 2006. Later, it has been found in various biotic and abiotic environmental matrices. However, little attention has been paid to monitor its presence in Asia. Many studies have reported the occurrence of DP in the environment of Asia, yet the data are scarce, and studies are limited to few regions. The objective of present review is to summarize the occurrence, distribution, and toxicity of this ubiquitous pollutant in various environmental matrices (biotic and abiotic). DP has also been reported in the areas with no emission sources, which proves its long-range transport. Moreover, urbanization and industrialization also affect the distribution of DP, i.e., high levels of DP have been found in urban areas relative to the rural. Tidal movement also incorporates in transport of DP across the aquatic system. Further, bioaccumulation trend of DP in various tissues is kidney > liver > muscle tissues, whereas, blood brain barrier resists its accumulation in brain tissues. Additionally, gender-based accumulation trends revealed high DP levels in females in comparison to males due to strong metabolism of males. Furthermore, methodological aspects and instrumental analysis used in previous studies have also been summarized here. However, data on biomagnification in aquatic ecosystem and bioaccumulation of DP in terrestrial food web are still scarce. Toxicity behavior of syn-DP and anti-DP is still unknown which might gain the interest for future studies.
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  • 文章类型: Journal Article
    Lefamulin is a novel systemic, semi-synthetic pleuromutilin class of antimicrobials that has been shown to be effective against common respiratory pathogens associated with community-acquired bacterial pneumonia (CABP). CABP, a common infection among older people, leads to an increase in hospitalizations and mortality. Therefore, the use of lefamulin could be beneficial for CABP treatment in patients who are 65 years of age or older.
    The Food and Drug Administration (FDA) approved lefamulin for the treatment of CABP, which is available in both intravenous and oral formulations. This medication offers the benefit of not having any cross-resistance to other antibiotics and is highly concentrated in lung tissues. Lefamulin is unique because it has an induced-fit mechanism of action which inhibits bacterial protein synthesis. The clinical efficacy of lefamulin has demonstrated noninferiority to current standard-of-care for CABP, and patients, generally, have tolerated it well in clinical trials.
    Lefamulin does not require dosage adjustment in renal impairment. However, the drug does requires dosage adjustment in severe hepatic impairment, based on Child-Pugh scores and clinical consideration in patients with severe hepatic impairment based on Child-Pugh scores. Though the benefit of adding lefamulin to a formulary is still in question; its potential to be a beneficial treatment for CABP is encouraging.
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  • 文章类型: Journal Article
    A wide variety of sampling techniques and strategies are needed to analyze polycyclic aromatic compounds (PACs) and interpret their distributions in various environmental media (i.e., air, water, snow, soils, sediments, peat and biological material). In this review, we provide a summary of commonly employed sampling methods and strategies, as well as a discussion of routine and innovative approaches used to quantify and characterize PACs in frequently targeted environmental samples, with specific examples and applications in Canadian investigations. The pros and cons of different analytical techniques, including gas chromatography - flame ionization detection (GC-FID), GC low-resolution mass spectrometry (GC-LRMS), high performance liquid chromatography (HPLC) with ultraviolet, fluorescence or MS detection, GC high-resolution MS (GC-HRMS) and compound-specific stable (δ13C, δ2H) and radiocarbon (Δ14C) isotope analysis are considered. Using as an example research carried out in Canada\'s Athabasca oil sands region (AOSR), where alkylated polycyclic aromatic hydrocarbons and sulfur-containing dibenzothiophenes are frequently targeted, the need to move beyond the standard list of sixteen EPA priority PAHs and for adoption of an AOSR bitumen PAC reference standard are highlighted.
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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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