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The synthetic approach of benzimidazole derivatives as anti-inflammatory agents 抗炎药苯并咪唑衍生物的合成方法
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.4826
Jugnu Jahan, Satyajit Barik, Bharath Kumar Chagaleti, Muthu Kumaradoss Kathiravan, Priya Deivasigamani
Anti-inflammatory drugs are a ubiquitous class of analgesics used by millions of people worldwide. Owing to the widespread and prolonged use of Anti-inflammatory drugs, chronic and acute toxicities have been reported in many human physiological systems. As a result, new anti-inflammatory drugs have been created recently, and several of them are in advanced phases of clinical studies. Chemists have been quite interested in heterocyclic compounds because of how similar they are to various biological precursors. One such heterocycle is benzimidazole and the most recent advancements of anti-inflammatory agents bearing benzimidazole have been emphasized in the current review. The review focuses on the synthetic route and the most promising benzimidazole derivative as an anti-inflammatory agent. The lead compound according to the literature will aid in the design and development of novel anti-inflammatory agents that target a diversity of factors contributing to inflammation.
消炎药是全世界数百万人普遍使用的一类镇痛药。由于抗炎药的广泛和长期使用,在许多人体生理系统中已经报道了慢性和急性毒性。因此,最近出现了新的抗炎药物,其中一些已进入临床研究的后期阶段。化学家们对杂环化合物非常感兴趣,因为它们与各种生物前体非常相似。其中一种杂环化合物就是苯并咪唑,本文综述了含苯并咪唑类抗炎药的最新进展。综述了苯并咪唑类抗炎药的合成路线和最有前景的衍生物。根据文献,先导化合物将有助于设计和开发针对多种导致炎症的因素的新型抗炎剂。
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引用次数: 0
Formulation and optimization of Ambrisentan self-micro emulsifying drug delivery system (SMEDDS) tablet by wet granulation 湿造粒法制备氨布里森坦自微乳化给药系统(SMEDDS)片的工艺及优化
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5673.
Nisarg Bhatt, Hitesh Patel
Ambrisentan is an orally administered endothelin receptor antagonists used for the treatment of pulmonary hypertension. As it is fall under BCS class 2 medicine, its solubility, stability and oral bio availability are poor. Here, a self-micro-emulsifying drug delivery system (SMEDDS) was developed to improve its solubility and drug dissolution. The objective of our investigation was to formulate a self-micro-emulsifying drug delivery system (SMEDDS) of Ambrisentan using minimized quantity of oil, surfactant and co-surfactant that could improve its solubility, stability, and dissolution. The composition of optimized formulation consists of Maisine CC as oil, Acrysol EL 135 as surfactant and Capryol PGMC as cosurfactant, containing 200 mg of Ambrisentan showing mean droplet size (155.12 nm), rate of self-emulsification (56 sec) and Polydispersibility index (0.331). This optimized liquid SMEDDS is used as a liquid component in wet granulation and prepare tablet of Ambrisentan having 5 mg strength. A prepared tablet is evaluated further for tablet evaluation tests and dissolution. This research results in good dissolution and stability.
Ambrisentan是一种用于治疗肺动脉高压的口服内皮素受体拮抗剂。由于属于BCS二类药物,其溶解度、稳定性和口服生物利用度较差。本研究开发了一种自微乳化给药系统(SMEDDS),以提高其溶解度和药物溶出度。本研究的目的是通过最小化油、表面活性剂和助表面活性剂的用量来制备一种自微乳化给药系统(SMEDDS),以提高其溶解度、稳定性和溶解性。优化后的配方以Maisine CC为油,丙烯溶胶EL 135为表面活性剂,癸醇PGMC为助表面活性剂,含200 mg Ambrisentan,平均滴度为155.12 nm,自乳化速率为56秒,多分散性指数为0.331。该液体SMEDDS作为湿法制粒的液体组分,制备强度为5mg的氨布里森坦片剂。制备的片剂进一步进行片剂评价试验和溶出度评价。研究结果表明,该产品具有良好的溶出性和稳定性。
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引用次数: 0
Synthesis and biological activities of flavonoid sulfamates as steroid sulfatase inhibitors 类黄酮磺胺酸酯类类固醇磺胺酶抑制剂的合成及生物活性研究
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5576
Hatem A Hejaz, Atul Purohit, Barry V L Potter
Synthesis of potent flavonoid sulfamate inhibitors of the enzyme steroid sulfatase (STS), a topical target in treating postmenopausal women with hormone-dependent breast cancer, is described in the current article. Novel compounds were examined for estrone sulfatase (E1-STS) inhibition in intact MCF-7 breast cells. The strategies adopted to develop STS inhibitors which, while active in vivo, are devoid of any estrogenicity that would limit their use for breast cancer therapy (e.g. estrone 3-O-sulfamate, EMATE), were broadly successful. Several molecules of flavonoid sulfamates were synthesized that potentially possess both aromatase and steroid sulfatase inhibitory properties. The isoflavane-4',7-O,O-bis-sulfamate (equol bis-sulfamate) and flavone-6,4'-O,O-bis-sulfamate were found to be the most potent inhibitors of all the flavonoid sulfamate analogs in vitro, inhibiting STS by about 99% at 0.1μM in MCF-7 cells. Some of these flavonoid sulfamates were also found to be active against both enzymes’ STS and aromatase (e.g., 5-hydroxy-7-methoxyflavone-4'-O-sulfamate, 5-hydroxy-flavone-4',7-O,O-bis-sulfamate, and 5,7-dihydroxy flavanone-4'-O-sulfamate), thus demonstrating the novel concept of a dual inhibitor. The availability of flavonoid sulfamates as STS inhibitors may enable to use of them as a therapy in the treatment of breast cancer.
合成有效的类黄酮磺胺酸抑制剂的酶类固醇磺胺酶(STS),一个局部目标治疗绝经后妇女激素依赖性乳腺癌,在当前的文章中进行了描述。在完整的MCF-7乳腺细胞中检测了新化合物对雌酮硫酸酯酶(E1-STS)的抑制作用。开发STS抑制剂所采用的策略是广泛成功的,这些抑制剂虽然在体内有活性,但没有任何雌激素原性,这将限制其用于乳腺癌治疗(例如雌酮3- o -氨基磺酸,EMATE)。合成了几种可能同时具有芳香化酶和类固醇磺化酶抑制特性的类黄酮磺酸盐分子。异黄酮-4′,7-O, o -双磺胺酸酯(马酚双磺胺酸酯)和黄酮-6,4′-O, o -双磺胺酸酯是所有类黄酮磺酸类似物的最有效的体外抑制剂,在0.1μM的MCF-7细胞中抑制STS约99%。其中一些类黄酮磺酸盐还被发现对酶的STS和芳香化酶都有活性(例如,5-羟基-7-甲氧基黄酮-4'- o -氨基磺酸盐,5-羟基黄酮-4',7-O, o -双氨基磺酸盐和5,7-二羟基黄酮-4'- o -氨基磺酸盐),从而证明了双重抑制剂的新概念。类黄酮磺酸盐作为STS抑制剂的可用性可能使其成为乳腺癌治疗的一种疗法。
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引用次数: 0
PCR- A Paradigm Shift with A Robust Quantum Jump 聚合酶链反应-具有稳健量子跃迁的范式转变
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5828
Anamitra Goswami, Nabanita Mukherjee, Moumita Sil, Arunava Goswami, Prashant Ratnaparkhi
Nature Communications has recognized the article titled "Engineered Helicase Replaces Thermocycler in DNA Amplification While Retaining Desired PCR Characteristics" as one of the top 25 best papers published in 2022. Gavrilov et al. (2022) engineered helicase which replaces thermocycler in DNA amplification while retaining desired PCR characteristics. No experiment was so advanced that of Gavrilov et al. LAMP (Loop-Mediated Isothermal Amplification) is limited to producing only short amplicons. SHARP (SSB-Helicase Assisted Rapid PCR) was invented in 2022. We were waiting over a year for reactions from scientific community and then employed SHARP. Gavrilov et al. showed costly PCR machine is not needed for SHARP. It has huge implication for Covid-19 research and prevention in India.
《Nature Communications》将题为《工程解旋酶在DNA扩增中取代热循环酶,同时保留所需的PCR特性》的文章评为2022年发表的25篇最佳论文之一。Gavrilov等人(2022)设计了解旋酶,在DNA扩增中取代了热循环酶,同时保留了所需的PCR特性。没有一个实验比Gavrilov等人的实验更先进。LAMP(环介导等温扩增)仅限于产生短扩增子。夏普(ssb -解旋酶辅助快速PCR)于2022年发明。我们花了一年多的时间等待科学界的反应,然后聘请了夏普。Gavrilov等人表明,SHARP不需要昂贵的PCR机。这对印度的Covid-19研究和预防具有重大意义。
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引用次数: 0
Novel gastroprotective activity of basella alba mucilage-based hydrogel beads on diclofenac sodium induced gastric ulcer 基于白底藻粘液的水凝胶珠对双氯芬酸钠诱发的胃溃疡的新型胃保护作用
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5648
Moumita Chowdhury, Pintu Kumar De
Natural polysaccharides are emerging gastro-protective agents that need extensive characterization and subsequent commercialization. Diclofenac sodium, a non-steroidal anti-inflammatory drug, is generally used as a model drug to induce gastric ulcers experimentally. Therefore, in the present study, Basella alba mucilage is modified to form hydrogel beads, and its gastro-protective potential is judged by incorporating Diclofenac sodium in it and administered orally to Swiss albino rats at an equivalent weight of 50mg Diclofenac sodium/ kg bw for ten days. The results were compared with the rats administered Diclofenac sodium (50 mg/kg bw) and with the group of rats administered Diclofenac sodium (50mg/kg bw) and Pantoprazole (10mg/kg bw). Another group of rats were administered blank hydrogel beads, and another group served as control. The gastro-protective property was evaluated from the gastric secretory parameters, ulcer index, biochemical tests, and histopathology studies. The administration of Basella alba mucilage-based hydrogel beads in rats decreased the ulcer index, total and free acidity, lipid peroxidation, hydrogen peroxide level, and myeloperoxidase activity. It elevated the level of enzymic antioxidants and increased gastric juice's pH significantly compared to the Diclofenac-treated rats. All the evaluated parameters showed similar results for the rats treated with Diclofenac sodium-loaded Basella alba mucilage beads and those treated with Diclofenac sodium and Pantoprazole, with no significant differences. The histopathology analysis also supports the gastro-protective property of the beads. Thus, Basella alba mucilage-based hydrogel beads can be a promising gastro-protective agent against Diclofenac sodium-induced gastric ulcers.
天然多糖是新兴的胃保护剂,需要广泛的表征和随后的商业化。双氯芬酸钠是一种非甾体抗炎药,在实验中一般作为模型药物诱导胃溃疡。因此,本研究将白底藻粘液修饰成水凝胶珠状,加入双氯芬酸钠,并以50mg双氯芬酸钠/ kg bw等量给药给瑞士白化大鼠10天,以此来判断其胃保护作用。将结果与双氯芬酸钠(50mg/kg bw)组和双氯芬酸钠(50mg/kg bw) +泮托拉唑(10mg/kg bw)组进行比较。另一组大鼠给予空白水凝胶珠,另一组作为对照组。从胃分泌参数、溃疡指数、生化试验和组织病理学研究评价其胃保护作用。大鼠给予白底菌黏液基水凝胶珠可降低溃疡指数、总酸度和游离酸度、脂质过氧化、过氧化氢水平和髓过氧化物酶活性。与双氯芬酸治疗的大鼠相比,它提高了酶抗氧化剂的水平,显著增加了胃液的pH值。所有评价参数显示,双氯芬酸钠负载的白底藻黏液珠与双氯芬酸钠和泮托拉唑处理的大鼠结果相似,无显著差异。组织病理学分析也支持这些小珠子的胃保护特性。因此,基于白底藻粘液的水凝胶珠可能是一种有前途的胃保护剂,可用于治疗双氯芬酸钠引起的胃溃疡。
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引用次数: 0
Appraisal, recent advancement, and impacts of nanomedicine in cardiac asthma 纳米药物在心脏性哮喘中的评价、最新进展及影响
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5214
Jeetendra Kumar Gupta, Abdul Razak Mohamed Sikkander, Faizan ul Haque Nagrami, Krishan Kumar, Nitin Wahi
Cardiopulmonary asthma is a type of coughing, not an external appearance of asthma. Depending on persistent symptoms, this full-to-the-brim situation can be used to survive a therapeutic emergency. Liquid composition in the lungs and the area around the airways may result from heart failure. This demonstrates how the direction causes symptoms such as shortness of breath, coughing, and bursting at the seams which are likecipher and asthma symptoms. The common condition known as asthma is brought on by airway sensitivity, which can lead to constrictions, most noticeably leading to breathing difficulty. Heart failure treatment is trained to ease the effects of cardiac asthma and heart failure symptoms. Current developments in nano science and nanotechnology point towards a wealth of novel ideas for understanding and treating cardiovascular, pulmonary, and hematological conditions. Asthma is a common complaint that provokes the airways through various causes. Additionally, these instances consistently run into issues with their management schedule pertinent to the collection of the complaints. Asthma quantifiable treatment currently relies primarily on glucocorticoid medication therapy; however, the development of more effective treatments is hampered by glucocorticoid conflict as well as numerous elevated possessions due to deprived drug delivery. Our fundamental understanding of cardiac asthma nano medicine therapy is updated in this review.
心肺哮喘是一种咳嗽,不是哮喘的外在表现。根据持续的症状,这种完全溢出的情况可以用于治疗紧急情况。肺部和气道周围的液体成分可能是心力衰竭的结果。这说明了方向是如何引起呼吸急促、咳嗽和爆裂等症状的,这些症状类似于肺结核和哮喘症状。常见的哮喘是由气道敏感引起的,这可能导致收缩,最明显的是导致呼吸困难。心力衰竭治疗的目的是缓解心脏哮喘和心力衰竭症状的影响。当前纳米科学和纳米技术的发展为理解和治疗心血管、肺部和血液疾病指明了丰富的新思路。哮喘是一种常见的疾病,它通过各种原因刺激呼吸道。此外,这些实例总是遇到与收集投诉相关的管理时间表问题。哮喘可量化治疗目前主要依靠糖皮质激素药物治疗;然而,更有效的治疗方法的发展受到糖皮质激素冲突的阻碍,以及由于药物输送被剥夺而导致的大量高拥有量。这篇综述更新了我们对心脏哮喘纳米药物治疗的基本认识。
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引用次数: 0
Perception of plagiarism factors among students from the health careers training institute 卫生职业培训学院学生对抄袭因素的认知
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5120
Lahcen Bandadi, Nadia Chamkal
Plagiarism is an act that negatively affects the quality of students training and the professional skills development. The aim of this study is to examine the perception of plagiarism factors among students from the health careers training institute. To carry out this quantitative study, seventy students were recruited. To collect the data, we used a questionnaire that included participants' socio-demographic characteristics and plagiarism factors. The results highlighted factors attributed to the students, factors relating to the teacher and factors relating to the training institution. Thus, the inability to manage time was raised by 61.3% of participants, ignorance of the rules for citing references (57%), easy access to information (46.8%), lack of awareness (51.6%), insufficient training (52%) and lack of disciplinary measures (76%). Minimizing plagiarism as much as possible requires the involvement of all actors in the teaching-learning process. An approach based on prevention, detection and sanction is proposed. Penalty should only be applied as a last resort, and need be accompanied by an in-depth analysis of the causes of plagiarism.
抄袭是一种影响学生培养质量和专业技能发展的行为。摘要本研究旨在探讨卫生职业培训学院学生对抄袭因素的认知。为了进行这项定量研究,我们招募了70名学生。为了收集数据,我们使用了一份调查问卷,其中包括参与者的社会人口统计学特征和抄袭因素。结果突出了归因于学生的因素、与教师有关的因素和与培训机构有关的因素。因此,61.3%的参与者提出了无法管理时间的问题,不知道引用参考文献的规则(57%),容易获取信息(46.8%),缺乏意识(51.6%),培训不足(52%)和缺乏纪律措施(76%)。尽可能减少抄袭需要所有参与者参与到教学过程中。提出了一种基于预防、发现和制裁的方法。处罚只能作为最后的手段,并且需要对抄袭的原因进行深入的分析。
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引用次数: 0
The Frequency of Topically Applied Corticosteroid Abuse Among Outpatients with Dermatology-Related Conditions 皮肤相关疾病门诊患者局部应用皮质类固醇滥用的频率
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5702.
Ning Bo
Topically applied corticosteroids are commonly prescribed medications for the treatment of various dermatology-related conditions. However, their misuse and abuse have become a growing concern. This study aims to determine the frequency of topically applied corticosteroid abuse among outpatients with dermatology-related conditions. A cross-sectional study design was employed, and data were collected from a sample of outpatients attending dermatology clinics. The participants were assessed for the presence of corticosteroid abuse based on clinical presentation, medical history, and examination findings. The frequency of abuse was determined, and factors associated with abuse were analyzed using statistical methods. The results of this study will contribute to a better understanding of corticosteroid abuse and provide insights for improving prescribing practices and patient education.
局部应用皮质类固醇是治疗各种皮肤病相关疾病的常用处方药。然而,它们的误用和滥用已成为一个日益令人担忧的问题。本研究旨在确定皮肤相关疾病门诊患者局部应用皮质类固醇滥用的频率。本研究采用横断面研究设计,数据收集自皮肤科门诊患者样本。根据临床表现、病史和检查结果评估参与者是否存在皮质类固醇滥用。确定了虐待的频率,并使用统计方法分析了与虐待有关的因素。本研究的结果将有助于更好地了解皮质类固醇滥用,并为改进处方实践和患者教育提供见解。
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引用次数: 0
Effects of baclofen administered to reduce muscle spasm on balance maintenance, gait ability and quality of life in stroke patients 巴氯芬减轻肌肉痉挛对脑卒中患者平衡维持、步态能力和生活质量的影响
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5615
Yong-Jin Jeon
This study aimed to investigate the impact of Baclofen on balance, gait, functional independence, and quality of life in ischemic stroke patients. Thirty patients diagnosed with ischemic stroke by a rehabilitation medicine specialist were randomly assigned to either an experimental group that underwent exercise therapy in conjunction with Baclofen or a control group that received conventional exercise therapy without Baclofen. In this study, Berg Balance Scale, Timed Up and Go, and 10-Meter Walk Test were used to evaluate balance and walking ability. Functional Independence Measure was employed to assess functional independence, and Stroke-Specific Quality of Life was used to evaluate the quality of life. The experimental results revealed statistically significant improvements in all evaluation measures for both groups when comparing post-test to pre-test. However, in comparisons between groups, all test items in the experimental group that combined Baclofen with exercise therapy were significantly higher than those in the control group. In conclusion, these results suggest that integrating Baclofen into exercise therapy rehabilitation programs could be a promising approach to enhance recovery outcomes for patients recovering from ischemic stroke.
本研究旨在探讨巴氯芬对缺血性脑卒中患者平衡、步态、功能独立性和生活质量的影响。30名被康复医学专家诊断为缺血性中风的患者被随机分配到实验组和对照组,实验组接受运动疗法结合巴氯芬,对照组接受常规运动疗法,不含巴氯芬。本研究采用Berg平衡量表、Timed Up and Go和10米步行测试来评估平衡和步行能力。采用功能独立性量表(Functional Independence Measure)评估功能独立性,采用卒中特异性生活质量(Stroke-Specific Quality of Life)评估生活质量。实验结果显示,当测试后与测试前比较时,两组的所有评估措施都有统计学上的显着改善。但在组间比较中,巴氯芬联合运动疗法的实验组各项指标均显著高于对照组。总之,这些结果表明,将巴氯芬纳入运动治疗康复计划可能是一种有希望的方法,可以提高缺血性卒中患者的康复效果。
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引用次数: 0
Synthesis and pharmacological characterization of new curcumin ester pro-drugs with enhanced anti-inflammatory, anti-ulcerogenic and improved tissue distribution 增强抗炎、抗溃疡和改善组织分布的新型姜黄素酯前药的合成及药理研究
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5264
Nidhi Agrawal, Meenakshi Jaiswal
In this work, curcumin- Non steroidal anti-inflammatory drugs (NSAIDs) conjugates were synthesized by esterification of the phenolic group of curcumin with the acid group of NSAIDs using the Steglich esterification method to enhance the anti-inflammatory activity of curcumin and to reduce the gastrointestinal side effects of NSAIDs. A set of bis C-NSAIDs conjugates was prepared by direct coupling of curcumin with Aceclofenac and Diflunisal respectively in good yield and characterized by Fourier-transform infrared spectra (FTIR) and Proton Nuclear Magnetic Resonance Spectra (1HNMR). In vivo, studies were performed to evaluate the toxicity, anti-inflammatory activity, bio-distribution, and anti-ulcerogenic studies of selected conjugates using different animal models. In Vivo, studies reveal enhanced biological activity with better tissue distribution of conjugates than that of parent curcumin and it could be a curcumin-based therapeutic molecule that might be explored further for its efficacy in managing inflammatory diseases.
本研究采用Steglich酯化法,将姜黄素的酚基与非甾体抗炎药的酸基酯化,合成姜黄素-非甾体抗炎药(NSAIDs)偶联物,以增强姜黄素的抗炎活性,减少非甾体抗炎药的胃肠道副作用。采用姜黄素与乙酰氯芬酸和双氟尼松直接偶联制备了一组C-NSAIDs偶联物,收率高,并通过傅里叶变换红外光谱(FTIR)和质子核磁共振光谱(1HNMR)对其进行了表征。在体内,使用不同的动物模型对选定的缀合物进行了毒性、抗炎活性、生物分布和抗溃疡性研究。在体内,研究表明,与母体姜黄素相比,缀合物的生物活性增强,组织分布更好,可能是一种基于姜黄素的治疗分子,可以进一步探索其治疗炎症性疾病的功效。
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引用次数: 0
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Journal of Medical pharmaceutical and allied sciences
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