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A New Carbohydrate of Aquilaria Agallocha 沉香属一种新的碳水化合物
Pub Date : 2023-06-30 DOI: 10.33425/2689-1050.1049
Yang TL, Yeh HC, Li HT, Liu SL, Chen CY
A new carbohydrate, agalloside ((2R,3S,4R,5R,6S)-2-(hydroxymethyl)-6- methoxytetrahydro-2H-pyran-3,4,5- triol) (1) was isolated from the flowers of Aquilaria agallocha. The structure was elucidated on the basis of physical and spectral analysis.
从沉香属植物沉香花中分离到新的碳水化合物沉香苷((2R,3S,4R,5R,6S)-2-(羟甲基)-6-甲氧基四氢- 2h -吡喃-3,4,5-三醇)(1)。在物理和光谱分析的基础上对其结构进行了表征。
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引用次数: 0
A New Tetrahydrofuran of Cinnamomum Burmannii 缅甸肉桂中一种新的四氢呋喃
Pub Date : 2023-06-30 DOI: 10.33425/2689-1050.1047
Yang TL, Yeh HC, Li HT, Liu SL, Chen CY
A new tetrahydrofuran, burmafuranic acid (1) was isolated from the mushroom supreme by Cinnamomum burmannii (Nees & T. Nees) Blume (Lauraceae). The structure of the new tetrahydrofuran was elucidated by chemical and physical evidence.
用肉桂(Cinnamomum burmannii; Nees &;)从香菇中分离到一种新的四氢呋喃——burmanuric酸(1)。布卢姆(樟科)。新的四氢呋喃的结构通过化学和物理证据得到了证实。
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引用次数: 0
A Benzoate of Synsepalum Dulcificum 一种杜仲的苯甲酸盐
Pub Date : 2023-06-30 DOI: 10.33425/2689-1050.1048
TRAN THUY TIEN, Wang SJ, Yeh HC, Kao CL, Li HT, Li WJ, Liu SL, Chen CY
A benzoate, ethyl 4-hydroxybenzoate (1) was isolated from the stems of Synsepalum dulcificum Daniell (Sapotaceae). The structure of the benzoate was elucidated by chemical and physical evidence.
从菝葜(菝葜)茎中分离得到一种苯甲酸酯,4-羟基苯甲酸乙酯(1)。用化学和物理证据对苯甲酸酯的结构进行了分析。
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引用次数: 0
Nano therapy Spotlight: Arestin™ Minocycline Microspheres 纳米治疗焦点:Arestin™米诺环素微球
Pub Date : 2023-06-30 DOI: 10.33425/2689-1050.1046
Drew Plemmons, KB Sneed, Yashwant Pathak
Within the last ten years, recent advancements in nanotechnology and repurposed pharmaceutical development has led several successful therapeutics through clinical trials and subsequently onto the market. On the nanotechnology side, size, shape, charge, and formulation are all considered in improving the overall efficacy or delivery of the therapeutic. Nanoparticle therapies hit the market in the late 90’s when the FDA approved CosmoFer®, an iron sugar colloid that also saw use in the European market. While these early nano pharmaceuticals were primitive compared to today’s standards, these medications proved that a nanoparticulate therapeutic can and would be accepted by the FDA, albeit under much scrutiny. On the pharmaceutical side, older legend drugs that have been proved efficacious for many years are beginning to be repurposed for other uses. For example, Pfizer’s 2015 approval of Rapamune® (Rapamycin) is indicated for the treatment of Lymphangioleiomyomatosis (LAM) a rare lung disease infecting mostly women in early adulthood. The drug, however, was first approved in 1999 and was used in the prophylaxis of organ rejection as an immunosuppressant. Another indication for Rapamycin is in age related diseases; a 2006 paper published by Dr. Blagosklonny at the Roswell Park Comprehensive Cancer center showed that Rapamycin could inhibit certain pathways that are related to aging. Many other medications on the market such as monoclonal antibody therapies have also seen a rise in new implication discovery and there is much evidence to suggest other drugs will be researched in the future for other alternative treatments. Because of such developments, pharmaceutical companies have tapped into the nanoparticle development world to find novel therapies for diseases we once thought were unavoidable. This is shown by the sheer expected market growth of about two billion dollars from 2021-2026, and the fifteen different nanoparticle-based therapeutics that have already been FDA approved since in just the last three years. Although the nanoparticle technology scope may seem to hover over novel cancer therapies, autoimmune disorders, blood borne diseases and neurological disorders, many therapies have come about in some interesting fields of study. One such therapeutic is called Arestin®, a new dentistry medication for the treatment of severe periodontitis, better known as gum disease. Gum disease is caused by poor oral hygiene and is attributed to various bacterial infections within the gum-line and if left untreated it can cause soft tissue damage or jawbone degradation. Typically, an antibiotic mouthwash or ultrasonic dental cleaner can be used to treat minor periodontitis but, in severe cases where there is significant gum-line recession, a more direct therapeutic is needed to treat the infection directly at the source. Arestin® is a nanoparticle formulation containing minocycline HCl impregnated within a bio-reabsorable polymer that is delivered direc
在过去的十年里,纳米技术的最新进步和重新定位的药物开发已经导致一些成功的治疗方法通过临床试验并随后进入市场。在纳米技术方面,大小、形状、电荷和配方都被考虑在提高整体疗效或治疗的递送。纳米颗粒疗法在90年代末进入市场,当时FDA批准了CosmoFer®,这是一种铁糖胶体,也在欧洲市场上使用。虽然与今天的标准相比,这些早期的纳米药物是原始的,但这些药物证明了纳米颗粒治疗可以并且将被FDA接受,尽管要经过严格的审查。在制药方面,多年来被证明有效的古老传奇药物开始被重新用于其他用途。例如,辉瑞公司2015年批准的Rapamune®(雷帕霉素)用于治疗淋巴管平滑肌瘤病(LAM),这是一种罕见的肺部疾病,主要感染成年早期女性。然而,该药物于1999年首次获得批准,并作为免疫抑制剂用于预防器官排斥反应。雷帕霉素的另一个适应症是与年龄有关的疾病;Blagosklonny博士2006年在罗斯威尔公园综合癌症中心发表的一篇论文表明,雷帕霉素可以抑制与衰老有关的某些途径。市场上的许多其他药物,如单克隆抗体疗法,也看到了新的蕴涵发现的增加,有很多证据表明,其他药物将在未来研究其他替代治疗。由于这些发展,制药公司已经进入纳米颗粒开发领域,为我们曾经认为不可避免的疾病寻找新的治疗方法。从2021年到2026年,预计市场将增长约20亿美元,过去三年里,15种不同的纳米颗粒疗法已经获得了FDA的批准。虽然纳米粒子技术的范围似乎徘徊在新的癌症治疗,自身免疫性疾病,血液传播疾病和神经系统疾病,许多治疗已经出现在一些有趣的研究领域。其中一种治疗药物叫做Arestin®,这是一种用于治疗严重牙周炎(俗称牙龈疾病)的新型牙科药物。牙龈疾病是由口腔卫生不良引起的,是由牙龈线内的各种细菌感染引起的,如果不及时治疗,可能会导致软组织损伤或颌骨退化。通常,抗生素漱口水或超声波洁牙器可用于治疗轻微的牙周炎,但在严重的情况下,牙龈线明显萎缩,需要更直接的治疗方法,直接从源头治疗感染。Arestin®是一种纳米颗粒配方,含有米诺环素HCl浸渍在生物可重新吸收的聚合物中,通过钝尖注射器直接输送到牙龈线。二甲胺四环素是一种久经考验的抗生素,作为第二代四环素衍生物,在市场上有30多年的丰富历史。它同时是革兰氏阳性和革兰氏阴性[广谱]抗生素,在患者中耐受性很好,使其成为晚期牙龈疾病干预的绝佳候选药物。在此,本文综述了Arestin®和随后的盐酸米诺环素的历史、作用机制、配方/生产、副作用以及重新配制的纳米药物的未来,这些药物正在继续提高市场份额。
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引用次数: 0
The Protection and Antioxidant Mechanisms of Corticosteroids in LPSTreated Retinal Pigment Epithelial Cells 皮质类固醇对lps处理视网膜色素上皮细胞的保护作用及抗氧化机制
Pub Date : 2023-06-30 DOI: 10.33425/2689-1050.1050
Wang SJ, Yeh HC, Kao CL, Li HT, Li WJ, Liu SL, Chen CY
Dexamethasone (DEX) and triamcinolone acetonide (TA) are two corticosteroids as anti-inflammatory agents that have been used as an anti-inflammation in several diseases to protect against oxidative damage. The present study examined the anti?oxidant effect of DEX and TA on lipopolysaccharide (LPS)-induced intracellular reactive oxygen species (ROS) in human retinol epithelium ARPE-19 cells. DEX and TA markedly inhibited the LPSinduced intracellular ROS level. DEX and TA also inhibited the expression of NADPH oxidase subunit gp91 and p22. Moreover, the expression of two antioxidant enzymes, heme oxygenase-1 (HO-1) expression and gammaglutamylcysteine synthetase (gamma-GCS), were increased by DEX and TA treatment in LPS-treated ARPE-19 cells. These results indicate that DEX and TA inhibits the intracellular ROS response by blocking the NADPH oxidase pathway and may increase some antioxidant enzymes in LPS -induced ARPE-19 cells. Therefore, DEX and TA may be useful as antioxidant agents against oxidative damage in anti-inflammatory diseases.
地塞米松(Dexamethasone, DEX)和曲安奈德(triamcinolone acetonide, TA)是两种作为抗炎剂的皮质类固醇,在多种疾病中被用作抗炎剂,以防止氧化损伤。本研究考察了抗?DEX和TA对脂多糖(LPS)诱导的人视黄醇上皮ARPE-19细胞内活性氧(ROS)的氧化作用。DEX和TA显著抑制lps诱导的细胞内ROS水平。DEX和TA还能抑制NADPH氧化酶亚基gp91和p22的表达。DEX和TA处理后,lps处理的ARPE-19细胞中血红素加氧酶-1 (HO-1)和γ -谷氨酰胺半胱氨酸合成酶(γ - gcs)两种抗氧化酶的表达均增加。这些结果表明,DEX和TA通过阻断NADPH氧化酶途径抑制细胞内ROS反应,并可能增加LPS诱导的ARPE-19细胞中的某些抗氧化酶。因此,DEX和TA可能是抗炎疾病中抗氧化损伤的有效抗氧化剂。
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引用次数: 0
COVID-19 Pandemic Spread and Containment: Perspectives COVID-19大流行的传播和遏制:观点
Pub Date : 2021-12-30 DOI: 10.33425/2689-1050.1023
B. Riccardi, S. Resta
In this manuscript we will examine the health policies unambiguously adopted by all the world governments for the containment and the fight against the pandemic by SARS-Cov-2, and document why the exclusive use of vaccinations for the prevention of contagion, is ineffective or even harmful, neglecting effective and safe alternative therapies. Looking back over the past and recent epidemiological history of infectious diseases, we realize that although there are still many contagious diseases, much more fearsome than SARS-Cov-2, never before in these two years have such restrictive health policies been imposed. While all other diseases, both infectious and degenerative, have been obscured or overshadowed, they continue to be the main causes of global death. The subject that dominates the scenes and the information is the COVID-19 that seems the unique object of the attentions of scientists, and of the obituaries of the mass media. In this desolating scenario that will see millions of forgotten people die for all the other diseases now neglected, strikes the total accomplice indifference and intellectual apathy of scientists, with very few exceptions, who suffer without discussing or raising the appropriate criticism, the repetitive information and the dominant unique thinking of health and political authorities. It’s incredible to see how many of those scientists and doctors who have helped to unravel and combat all the other diseases are now silent in the face of this incredible tragedy.
在本文中,我们将研究世界各国政府为遏制和抗击SARS-Cov-2大流行而明确采取的卫生政策,并记录为什么只使用疫苗来预防传染是无效的,甚至是有害的,而忽视了有效和安全的替代疗法。回顾过去和最近的传染病流行病学历史,我们意识到,尽管仍然有许多比SARS-Cov-2可怕得多的传染病,但这两年从未实施过如此严格的卫生政策。虽然所有其他疾病,无论是传染性疾病还是退行性疾病,都被掩盖或掩盖,但它们仍然是全球死亡的主要原因。主导场景和信息的主题是COVID-19,它似乎是科学家关注的唯一对象,也是大众媒体讣告的唯一对象。在这种凄凉的情景中,数百万被遗忘的人将死于现在被忽视的所有其他疾病,科学家们的完全冷漠和知识冷漠,只有极少数例外,他们没有讨论或提出适当的批评,重复的信息和占主导地位的独特思维的健康和政治当局。令人难以置信的是,有多少科学家和医生曾经帮助解开和对抗所有其他疾病,现在面对这场令人难以置信的悲剧却保持沉默。
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引用次数: 0
Applications of Precision Medicine in the Treatment of Psychiatric Disorders: A Literature Review 精准医学在精神疾病治疗中的应用:文献综述
Pub Date : 2021-12-30 DOI: 10.33425/2689-1050.1020
H. Hare, K. Sneed, Y. Pathak
Background: Scientific understanding of precision medicine is rapidly evolving as new associations are made between genetic variants and tolerance to pharmaceuticals [1]. Although pharmacogenetic testing and guidelines exist for many medications, there is limited clinical application of these technologies in part due to limitations of the evidence supporting its use in psychiatric treatment as well as lack of awareness by providers and patients [2]. This narrative literature review aims to assess and summarize the past decade of research in the field of psychiatric pharmacogenetics. Specifically, it will focus on the relationship between antidepressant/antipsychotic drug responses and polymorphisms in nine commonly studied genes: CYP1A2, CYP2B6, CYP2C19, CYP2D6, CYP3A4, CYP3A5, SLC6A4, HTR2A, and DRD2. Methods: Literature from PubMed and Embase that was published between the years 2010 and 2020 was found using strategic keywords and search phrases. Each study represented was a randomized controlled trial or clinical trial tested in adults over the age of eighteen. Results: Of the six CYP450 enzymes that were evaluated, all displayed impacts on the metabolism of psychiatric drugs except CYP3A4, although only one polymorphism (*1B) was included in analysis of that particular gene. Inconclusive results were discovered regarding SLC6A4 5-HTTLPR polymorphisms and further review should be done to determine its relationship with SSRI response. Additionally, review of literature pertaining to DRD2 showed unsubstantial evidence, as four out of seven articles found no connection between treatment or adverse drug reactions (ADR) associated with DRD2. In contrast, influential findings were documented by literature concerning HTR2A polymorphisms and therapeutic consequences and the evidence collected on benefits of pharmacogenomic testing supports the implementation of testing to guide psychiatric treatment with confidence that use may result in fewer failed trials prior to response or remission. Conclusion: Many polymorphic mutations have a significant impact on individual responses to psychiatric treatment and implementation of pharmacogenomic testing in a clinic setting may be beneficial to psychiatric patients. Further review of polymorphic relationships should be done, especially in the case of SLC6A4 and DRD2 variations.
背景:随着基因变异与药物耐受性之间的新联系,对精准医学的科学理解正在迅速发展[1]。尽管存在许多药物的药物遗传学测试和指南,但这些技术的临床应用有限,部分原因是支持其用于精神治疗的证据有限,以及提供者和患者缺乏认识[2]。这篇叙述性的文献综述旨在评估和总结过去十年在精神病学药物遗传学领域的研究。具体而言,它将重点关注抗抑郁/抗精神病药物反应与九个常用基因多态性之间的关系:CYP1A2, CYP2B6, CYP2C19, CYP2D6, CYP3A4, CYP3A5, SLC6A4, HTR2A和DRD2。方法:利用战略关键词和搜索短语,从PubMed和Embase检索2010 - 2020年间发表的文献。每项研究都是在18岁以上的成年人中进行的随机对照试验或临床试验。结果:在被评估的6种CYP450酶中,除CYP3A4外,所有酶都显示出对精神药物代谢的影响,尽管在对该特定基因的分析中只包含了一种多态性(*1B)。SLC6A4 5-HTTLPR多态性尚无定论,有待进一步研究以确定其与SSRI反应的关系。此外,对有关DRD2的文献的回顾显示缺乏实质性证据,因为七篇文章中有四篇没有发现与DRD2相关的治疗或药物不良反应(ADR)之间的联系。相比之下,有关HTR2A多态性和治疗后果的文献记录了有影响力的发现,并且收集的关于药物基因组学测试益处的证据支持实施测试来指导精神病学治疗,并相信使用测试可能会减少在反应或缓解之前失败的试验。结论:许多多态性突变对个体对精神病治疗的反应有显著影响,在临床环境中实施药物基因组学检测可能对精神病患者有益。应该进一步研究多态性关系,特别是SLC6A4和DRD2变异。
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引用次数: 0
Studies on the Effect of Aqueous Seed Extracts of Parkia Biglobosa on The Histology and Glycogen Profile of The Epididymis of Wistar Rats 枇杷种子水提物对Wistar大鼠附睾组织学及糖原谱影响的研究
Pub Date : 2021-06-30 DOI: 10.33425/2689-1050.1017
G. Udo-Affah, K. Obeten, A. O. Adewale, Ajaba A. Okim
This study was aimed at determining the effect of aqueous seed extract of Parkia biglobosa on the histology of the epidydimis of male wistar rats was studied. Twenty-one adult wistar rats weighing about 90-120g were use for this research work and were divided into three groups of 7 animals each. The control group was giving normal rat feed and water, the low dose group was administered (300mg/kgBw) of Parkia biglobosa extract and the high dose group was administered (500mg/kg) of the test substance. All extract were given daily by oral gavage method for thirty-one days. Twenty-four hours after the last administration, the animals in all the groups were sacrificed using cervical dislocation. The epidydimis were harvested, preserved, and fix in 10% buffer formalin and processed for hematoxylin and eosin (H&E) staining and periodic acid-Schiff (PAS) staining methods for glycogen distribution. The result of the study shows a (P<0.05) significant increase in the final body weight of the treated animals when compared with their initial body weight. The histological observation showed normal cytoarchitecture of the epididymis in the Control group. There was observable pathological appearance in the epididymis of the low dose group. However, there were prominent distortions in the high dose animals that received 500mg/kgBw of the extract. Histochemical observation shows a moderate PAS staining in the control group. While the treated groups reveals mildly stained cytoarchitechture of the epididymis.
本研究旨在研究白粉枇杷籽水提物对雄性wistar大鼠附睾组织学的影响。本研究选用21只体重约90-120g的成年wistar大鼠,分为三组,每组7只。对照组给予正常大鼠饲料和水,低剂量组给药300mg/kgBw,高剂量组给药500mg/kg。所有提取液每日灌胃,连续31 d。末次给药24 h后,各组均采用颈椎脱臼法处死。收集附睾,保存,固定在10%的缓冲福尔马林中,进行苏木精和伊红(H&E)染色和周期性酸-希夫(PAS)染色,观察糖原分布。研究结果表明,与初始体重相比,处理动物的最终体重显著增加(P<0.05)。组织学观察显示,对照组附睾细胞结构正常。低剂量组附睾有明显的病理改变。然而,在接受500mg/kgBw提取物的高剂量动物中,存在明显的扭曲。组织化学观察,对照组呈中度PAS染色。而治疗组显示附睾细胞结构轻度染色。
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引用次数: 1
Toxicological Aspect of Fatal Methamphetamine 致命甲基苯丙胺的毒理学研究
Pub Date : 2021-06-30 DOI: 10.33425/2689-1050.1016
M. Alqallaf
Drug addiction has become a worldwide problem and the leading cause of death. The global problem of addiction and drug abuse is responsible for hundreds of deaths every year. It affects not only individual users, but also their families and communities. The current study, presents the fatality of some cases caused by the complications brought about the presence of methamphetamine and other abused drugs. It has been a drug of abuse in the past and is still gaining popularity as a recreational drug because of its much longer excitatory duration of more than three hours and its biotransformation to amphetamine, the active metabolite. In present postmortem cases methamphetamine and other combined drugs have issue in cardiac major health problems and poisoning-related deaths. Many postmortem cases found positive to methamphetamine and amphetamine or combined with other drugs include different narcotics/ stimulants drugs such as : benzodiazepines, THC, opium, and lyrica. The toxic effects of methamphetamine can explain increasing reports of heart failure and consequently death in young abusers. As this recognition may prove to be of some forensic value to clarify the death in methamphetamine abusers.
吸毒成瘾已成为一个世界性问题,也是导致死亡的主要原因。成瘾和滥用药物这一全球性问题每年造成数百人死亡。它不仅影响个人用户,还影响他们的家庭和社区。目前的研究表明,由于甲基苯丙胺和其他滥用药物的存在而引起的并发症造成了一些病例的死亡。它在过去一直是一种被滥用的药物,由于它的兴奋持续时间超过3小时,并且它可以生物转化为苯丙胺,一种活性代谢物,作为一种娱乐性药物,它仍然越来越受欢迎。在目前的死后病例中,甲基苯丙胺和其他联合药物在心脏重大健康问题和中毒相关死亡方面存在问题。许多死后的病例发现甲基苯丙胺和安非他明呈阳性,或与其他药物包括不同的麻醉/兴奋剂药物,如:苯二氮卓类药物,四氢大麻酚,鸦片和甘草。甲基苯丙胺的毒性作用可以解释青少年滥用者心脏衰竭和死亡报告的增加。因为这种承认可能证明对澄清甲基苯丙胺滥用者的死亡具有一定的法医价值。
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引用次数: 1
Discovery of Novel Analgesic Agents Targeting Neuropathic Pain: Computer-Aided Drug Design 针对神经性疼痛的新型镇痛药物的发现:计算机辅助药物设计
Pub Date : 2020-12-28 DOI: 10.33425/2689-1050.1014
Nafisa Siddig Hassan Abdulrahman, Mazin Yousif Babiker Alsafi
Background: Neurotrophin family combines nerve growth factor (NGF), brain derived neurotrophic factor (BDNF), neurotrophin 3 (N3) and neurotrophin 4 (N4). p75 receptor is the target for these neurotrophins. They bind to it by tropomyosin related kinase enzyme Trk with different affinity. Trk enzyme is classified into TrkA, TrkB and TrkC with different selectivity to neurotrophins family. NGF signals preferentially through TrkA, BNDF and N4 through TrkB, and N3 through TrkC. These neurotrophins have been found to be involved in pathophysiology of neuropathic pain. Material and Method: Molecular docking approach was used to conduct this study. Prior to start docking procedure, some modifications were made including removal of water from the receptor, application of energy minimization and Lipinski rule of five to the ligands. Toxicity studies, p-glycoprotein and human intestinal absorption were studied for the docked ligands. Result: 28 ligands of FDA approved drugs and 72 non-FDA approved ligands have shown high affinity to TrkA enzyme with different energies and hence are possible to be active against neuropathic pain. These 28 ligands of FDA approved drugs and 72 ligands of non-FDA approved drugs have declined to 10 ligands and 2 ligands respectively after studying toxicity, p-glycoprotein substrate, human intestinal absorption and hepatotoxicity. The least energy was consumed was -40.8985 by the FDA-approved drug N-Hydroxy-N'-phenyloctanediamide. Conclusion: The docked ligands were assumed to possess therapeutic activity against neuropathic pain based on their affinity to TrkA enzyme.
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引用次数: 0
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Journal of chemical and pharmaceutical research
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