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Tea tree (Melaleuca alternifolia) essential oil concentration in micro-emulsion with antibacterial and antifungal activity: An Overview 茶树精油在微乳液中的抑菌抑菌活性研究进展
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-28 DOI: 10.2174/1574885518666230228103854
P. Upadhyay, Pooja Malik, S. Upadhyay
The tea tree (Melaleuca alternifolia), a member of the Myrtaceae family, is a valuable medicinal and aromatic plant. Tea Tree essential oil (TTO) has many medical applications, including antibacterial, antifungal, antiviral, antiprotozoal, anti-inflammatory, antioxidant, and anticancer properties. Although the concentration of TTO in a microemulsion is of economic interest, very few studies on this product have been conducted. In this study, we look at how different tea tree oil concentrations in microemulsion formulations affect susceptibility to various bacteria and fungi. TTO susceptibility in a diverse range of microbial species has now been studied using data from a previously published literature review survey. Most bacteria are resistant to TTO at concentrations as low as 1.0 percent, but mucosal skin staphylococci and micrococci, Enterococcus faecalis, and Pseudomonas aeruginosa have minimum inhibitory concentrations much higher than 2 percent. TTO susceptibility in fungi has only recently been scrutinized. Fungicidal dosages range from 0.12 to 2 percent, with minimum inhibitory concentrations ranging from 0.03 to 0.5 percent and the only notable exception is Aspergillus niger, which contains fungicidal concentrations of up to 8%. The review emphasizes the importance of new antibacterial and antifungal formulations, as well as the role of natural essential oils in the discovery of new antibacterial and antifungal agents, and discusses, in brief, all constituents derived from the essential oil (tea tree) that are in preclinical and clinical development. This paper summarizes human and food-borne bacteria and fungi susceptibility to tea tree essential oils and their constituents. Among the many tested, essential oils of spices and herbs (Melaleuca alternifolia) were found to have the strongest antimicrobial properties. This review looks at a wide range of scientific literature, including Sci-hub, Google Scholar, Pub, Chem, NCBI, and web books.
茶树(互叶千层)是杨梅科的一员,是一种珍贵的药用芳香植物。茶树精油(TTO)具有许多医学应用,包括抗菌、抗真菌、抗病毒、抗原生动物、抗炎、抗氧化和抗癌特性。尽管TTO在微乳液中的浓度具有经济意义,但很少对该产品进行研究。在这项研究中,我们观察了微乳制剂中不同茶树油浓度如何影响对各种细菌和真菌的易感性。现在已经使用先前发表的文献综述调查的数据研究了不同微生物物种的TTO易感性。大多数细菌对浓度低至1.0%的TTO具有耐药性,但粘膜皮肤葡萄球菌和微球菌、粪肠球菌和铜绿假单胞菌的最低抑制浓度远高于2%。真菌对TTO的敏感性直到最近才被仔细研究。杀菌剂量在0.12至2%之间,最小抑制浓度在0.03至0.5%之间,唯一显著的例外是黑曲霉,其杀菌浓度高达8%。该综述强调了新的抗菌和抗真菌制剂的重要性,以及天然精油在发现新的抗菌剂和抗真菌剂中的作用,并简要讨论了从精油(茶树)中提取的所有处于临床前和临床开发中的成分。本文综述了人类和食源性细菌和真菌对茶树精油及其成分的敏感性。在众多测试中,香料和草药的精油(互叶千层)被发现具有最强的抗菌性能。这篇综述着眼于广泛的科学文献,包括Sci hub、Google Scholar、Pub、Chem、NCBI和网络书籍。
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引用次数: 0
Antifungal Properties of Pinus eldarica and Pinus longifolia Fruit Extracts against Candida Species Isolated from Vulvovaginal Candidiasis Patients 接骨木和长叶松果实提取物对外阴念珠菌属念珠菌的抗菌作用
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-23 DOI: 10.2174/1574885518666230223120624
M. Madani, P. Shakib, Zohreh Norouzi, L. Amjad
Candidiasis is a disease with serious problems in women. With the increasing drug resistance and risks of the drugs, we investigated the effect of different cone extracts of Pinus eldarica and Pinus longifolia against Candida species isolated from vulvovaginal candidiasis patients.Candidiasis is a disease with serious problems in women. With increasing drug resistance and risks of these drugs, we decided to investigate the effect of different cone extracts of Pinus eldarica and Pinus longifolia against candidate species isolated from vulvovaginal candidiasis patients.Candida species isolated from 50 patients were identified by routine mycological methods, including morphology of corn mil agar, chromium agar, germination, and biochemical methods. The anti-candida properties of the extracts and essential oils of Pinus eldarica and Pinus longifolia were investigated using agar diffusion and microdilution test. The essential oil was then analyzed by Gas chromatography-mass spectrometry (GC-MS).Candidiasis is a disease with serious problems in women. With increasing drug resistance and risks of these drugs, we decided to investigate the effect of different cone extracts of Pinus eldarica and Pinus longifolia against candidate species isolated from vulvovaginal candidiasis patients.The major constituents of Pinus longifolia essential oil included 23.16% alpha-pinene, 2.59% beta-caryophyllene, 23.61% delta-3-carene, 0.24% carcin-4-hydroxy, 13.56% m-cymene, 0.45% alpha-humulene, and 2.12% junipene. The major constituents of Pinus eldarica essential oil included 29.13% alpha-pinene, 14.22% beta-caryophyllene, 11.70% delta-3-carene, -14.22% carcin-4-hydroxy, 4.29% beta-pinene, 3.59%, alpha humulene, and 8.86% junipene. The results of antifungal tests showed that aqueous, ethanolic, and methanolic extracts had a weak anti-candida effect. By changing the solvent and using petroleum ether solvent, it was found that petroleum ether extract and cone essential oil of Pinus longifolia and Pinus eldarica exhibited a relatively strong anti-candida effect.Candida species isolated from 50 patients were identified by routine mycological methods including morphology on corn mil agar, chromium agar, germination and biochemical methods. After extraction and essential oil extraction, the anti-candida properties of the extracts and essential oils of Pinus eldarica and Pinus longifolia were investigated using agar diffusion and microdilution test. The essential oil was then analyzed by GC / MS.Comparison of Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC) of four extracts of Pinus longifolia and Pinus eldarica against different Candida showed that the lowest MIC and MFC were related to essential oil, petroleum ether extract, methanolic extract, ethanolic extract, and aqueous extract, respectively.Keywords: Pinus longifolia, Pinus eldarica, essential oil, Candida species, anti-fungal
念珠菌感染是一种在女性中存在严重问题的疾病。随着耐药性和药物风险的增加,我们研究了不同的接骨木松和长叶松锥提取物对从外阴阴道念珠菌感染患者中分离的念珠菌的影响。念珠菌感染是一种在女性中存在严重问题的疾病。随着这些药物耐药性和风险的增加,我们决定研究不同的接骨松和长叶松锥提取物对从外阴阴道念珠菌感染患者中分离的候选物种的影响。采用常规真菌学方法,包括玉米琼脂、铬琼脂、发芽和生化方法,对50例患者的念珠菌进行了鉴定。采用琼脂扩散法和微量稀释法研究了接骨松和长叶松提取物和精油的抗念珠菌特性。然后通过气相色谱-质谱(GC-MS)对精油进行分析。念珠菌感染是一种在女性中存在严重问题的疾病。随着这些药物耐药性和风险的增加,我们决定研究不同的接骨松和长叶松锥提取物对从外阴阴道念珠菌感染患者中分离的候选物种的影响。长叶松精油的主要成分包括23.16%的α-蒎烯、2.59%的β-石竹烯、23.61%的三角洲-3-carene、0.24%的carcin-4-羟基、13.56%的m-cymene、0.45%的α-腐殖质和2.12%的杜松烯。接骨木松精油的主要成分包括29.13%的α-蒎烯、14.22%的β-石竹烯、11.70%的三角洲-3-carene、-14.22%的carcin-4-羟基、4.29%的β-蒎ne、3.59%的α-腐殖烯和8.86%的杜松烯。抗真菌试验结果表明,水提物、乙醇提物和甲醇提物的抗念珠菌作用较弱。通过改变溶剂和使用石油醚溶剂,发现长叶松和接骨木松的石油醚提取物和圆锥精油具有较强的抗念珠菌作用。采用常规真菌学方法,包括玉米琼脂形态学、铬琼脂形态学、发芽和生化方法,对50例患者的念珠菌进行了鉴定。采用琼脂扩散法和微量稀释法研究了接骨松和长叶松提取物和精油提取后的抗念珠菌特性。长叶松和接骨木松四种提取物对不同念珠菌的最低抑菌浓度(MIC)和最低杀菌浓度(MFC)的比较表明,最低MIC和MFC分别与精油、石油醚提取物、甲醇提取物、乙醇提取物和水提取物有关。关键词:长叶松、接骨木松、精油、念珠菌属、抗真菌
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引用次数: 0
Molecular Docking and simulation analysis of Cyclopeptides as Anticancer Agents 环肽抗癌作用的分子对接与模拟分析
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-22 DOI: 10.2174/1574885518666230222113033
A. Tiwari, V. Tiwari, Suresh Kumar, Manish Kumar, Renu Saharan, N. Verma, B. Sahoo, Deepak Kaushik, Rajeev Kumar Sharma
Cancer is a leading cause of death for people worldwide, in addition to the rise in mortality rates attributed to the Covid epidemic. This allows scientists to do additional research. Here, we have selected Integerrimide A, cordy heptapeptide, and Oligotetrapeptide as the three cyclic proteins that will be further studied and investigated in this context.Docking research was carried out using the protein complexes 1FKB and 1YET, downloaded from the PDB database and used in the docking investigations. Cyclopeptides have been reported to bind molecularly to human HSP90 (Heat shock protein) and FK506. It was possible to locate HSP90 in Protein Data Banks 1YET and 1FKB. HSP90 was retrieved from Protein Data Bank 1YET and 1FKB. Based on these findings, it is possible that the anticancer effects of Int A, Cordy, and Oligo substances could be due to their ability to inhibit the mTOR rapamycin binding domain and the HSP90 Geldanamycin binding domain via the mTOR and mTOR chaperone pathways. During the calculation, there were three stages: system development, energy reduction, and molecular dynamics (also known as molecular dynamics). Each of the three compounds demonstrated a binding affinity for mTOR's Rapamycin binding site that ranged from -6.80 to -9.20 Kcal/mol (FKB12).An inhibition constant Ki of 181.05 nM characterized Cordy A with the highest binding affinity (-9.20 Kcal/mol). Among the three tested compounds, Cordy A was selected for MD simulation. HCT116 and B16F10 cell lines were used to test each compound's anticancer efficacy. Doxorubicin was used as a standard drug. The cytotoxic activity of substances Int A, Cordy A, and Oligo on HCT116 cell lines was found to be 77.65 μM, 145.36 μM, and 175.54 μM when compared to Doxorubicin 48.63 μM, similarly utilizing B16F10 cell lines was found to be 68.63 μM, 127.63 μM, and 139.11 μM to Doxorubicin 45.25 μM.Compound Cordy A was more effective than any other cyclic peptides tested in this investigation.
除了新冠肺炎疫情导致的死亡率上升外,癌症是全世界人们死亡的主要原因。这使得科学家可以做更多的研究。在这里,我们选择了integerriide A, cordy七肽和Oligotetrapeptide作为三个环蛋白,将在此背景下进一步研究和研究。对接研究使用从PDB数据库下载的蛋白复合物1FKB和1YET进行对接研究。据报道,环肽可与人热休克蛋白(HSP90)和FK506结合。在蛋白数据库1YET和1FKB中可以找到HSP90。HSP90从蛋白质数据库1YET和1FKB中检索。基于这些发现,Int A、Cordy和Oligo物质的抗癌作用可能是由于它们能够通过mTOR和mTOR伴侣通路抑制mTOR雷帕霉素结合域和HSP90格尔达霉素结合域。在计算过程中,有三个阶段:系统开发、能量还原和分子动力学(又称分子动力学)。这三种化合物均显示出对mTOR的雷帕霉素结合位点的结合亲和力,范围为-6.80至-9.20 Kcal/mol (FKB12)。抑制常数Ki为181.05 nM,表明Cordy A具有最高的结合亲和力(-9.20 Kcal/mol)。在三个被测化合物中,选择Cordy A进行MD模拟。采用HCT116和B16F10细胞株检测各化合物的抗癌效果。阿霉素被用作标准药物。与阿霉素48.63 μM相比,Int A、Cordy A和Oligo对HCT116细胞株的细胞毒活性分别为77.65 μM、145.36 μM和175.54 μM;对B16F10细胞株的细胞毒活性分别为68.63 μM、127.63 μM和139.11 μM。化合物Cordy A比本研究中测试的任何其他环肽都更有效。
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引用次数: 0
The Effect of Inhalation Aromatherapy on Patients with Cardiovascular Disease Seeking Pain Relief: A Systematic Review and Meta-analysis 吸入芳香疗法对寻求疼痛缓解的心血管疾病患者的影响:系统回顾和荟萃分析
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-17 DOI: 10.2174/1574885518666230217141950
S. Heidari-Soureshjani, Razieh Mohammadi-Dashtaki, C. Sherwin
Untreated cardiovascular disease (CVD) can commonly cause disability and morbidity and increase the mortality risk.This systematic review and meta-analysis study aimed to investigate the pain-relieving effects of aromatherapy with medicinal plants on patients with cardiovascular diseases.This meta-analysis followed PRISMA guidelines. Several keywords were explored using an extensive search of databases, including PubMed, Web of Science (ISI), EMBASE, and Scopus, on May 15, 2022. In addition, an excel form was designed for recording the data of the RCT studies. Standardized mean difference (SMD) and their 95% confidence intervals (CI) were used to estimate the overall effect size. The Cochran Q test and the statistic I2 were used to evaluate the heterogeneity of studies. Lastly, Egger's and Begg's tests were used to assess potential publication bias.We included studies examining the effect of inhalation aromatherapy on pain in patients with CVD after 5 minutes (five papers) and 15-30 minutes (six papers) of intervention. The results showed a significant decrease in pain in the intervention group compared to the control group after 5 minutes (SMD = -2.25, 95% CI = -3.21 to -1.29, P < 0.001) and after 15-30 minutes (SMD = -3.22, 95% CI = -4.41 to -2.03, P < 0.001) of intervention in CVD patients. No publication bias was observed related to the association between inhalation aromatherapy and pain relief.In CVD patients, inhalation aromatherapy could significantly reduce pain severity and can be used as a complementary medicine for pain reduction.
未经治疗的心血管疾病(CVD)通常会导致残疾和发病率,并增加死亡风险。这项系统综述和荟萃分析研究旨在研究药用植物芳香疗法对心血管疾病患者的止痛效果。该荟萃分析遵循PRISMA指南。2022年5月15日,通过广泛搜索数据库,包括PubMed、Web of Science(ISI)、EMBASE和Scopus,对几个关键词进行了探索。此外,还设计了一个excel表格,用于记录随机对照试验研究的数据。标准化平均差(SMD)及其95%置信区间(CI)用于估计总体效应大小。Cochran Q检验和统计I2用于评估研究的异质性。最后,使用Egger和Begg检验来评估潜在的发表偏倚。我们纳入了研究吸入芳香疗法对CVD患者在干预5分钟(5篇论文)和15-30分钟(6篇论文)后疼痛的影响。结果显示,与对照组相比,干预组在CVD患者干预5分钟后(SMD=-2.25,95%CI=-3.21--1.29,P<0.001)和15-30分钟后(SMD=-3.22,95%CI=-4.41--2.03,P<0.001。没有观察到与吸入芳香疗法和疼痛缓解之间的相关性相关的发表偏倚。在CVD患者中,吸入芳香疗法可以显著降低疼痛的严重程度,并可作为减轻疼痛的补充药物。
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引用次数: 0
Advances and Prospects in Antimicrobial Research Using Nanomedicines 纳米药物抗菌研究进展与展望
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-14 DOI: 10.2174/1574885518666230214104252
S. Agrawal, Saraswathy Nagendran, Avdhoot Pimpale
Nanotechnology is moving toward future goals in the field of medicines, cosmetics and hospitality due to the size reduction of material in the range of 1-100nm, enhancing the stability and bioavailability of the material.This review includes the progress in the field of nanotechnology, its advantages, understanding and applications in antimicrobial therapy.The manuscripts were collected in the field of antimicrobial research with the help of nanotechnology platforms from different sources like PubMed, ScienceDirect and Google. A total of 236 manuscripts were collected and analyzed, out of which 93 were relevant and considered for the present manuscript.There are diverse forms of metallic nanomaterials that show antimicrobial properties, such as gold, silver, copper, zinc, titanium and many such metal oxides. Various carriers are used to deliver the drug at targeted sites via encapsulating the nanomaterial in polymers, liposomes or in the lipoidal structure. The inhibition of microorganism growth may be attributed to different mechanisms like destroying the synthesis of a cell wall, nucleic acid, injury to the bacteria cell wall and inhibiting the metabolic pathways in bacteria. This enhanced the antimicrobial activity and reduced the toxicity that could be significant due to a reduction in the dose proportionality.The recent advances in drug delivery with the help of liposomes, solid lipid nanoparticles, dendrimers, and various nanoparticles led to effective prevention, treatment and diagnosis of various microbial infections and this could dramatically change the way antimicrobial therapy explored for reducing drug resistance.
纳米技术将材料的尺寸缩小到1-100nm范围内,提高了材料的稳定性和生物利用度,正朝着医药、化妆品和酒店等领域的未来目标迈进。本文综述了纳米技术的研究进展、纳米技术的优势、对纳米技术的认识及其在抗菌治疗中的应用。这些手稿是在不同来源的纳米技术平台(如PubMed、ScienceDirect和b谷歌)的帮助下在抗菌研究领域收集的。共收集和分析了236份手稿,其中93份与本手稿有关。有多种形式的金属纳米材料显示出抗菌性能,如金、银、铜、锌、钛和许多这类金属氧化物。通过将纳米材料包裹在聚合物、脂质体或脂质结构中,各种载体被用于将药物递送到目标位点。抑制微生物生长可能有不同的机制,如破坏细胞壁的合成、核酸、损伤细菌细胞壁和抑制细菌的代谢途径。这增强了抗菌活性并降低了毒性,这可能是由于剂量比例的降低而显着的。在脂质体、固体脂质纳米颗粒、树状大分子和各种纳米颗粒的帮助下,药物递送的最新进展导致了各种微生物感染的有效预防、治疗和诊断,这可能会极大地改变探索减少耐药性的抗菌治疗方式。
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引用次数: 0
PICOSCIENCE: PICOTECHNOLOGY’s ADVENT IN HEALTH AND MEDICINE PICOSCERICE:PICOTECHOLOGY在健康和医学方面的优势
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-14 DOI: 10.2174/1574885518666230214100128
Hrishikesh Bhagawati, Mrinal Kashyap Sarma, Abhijita Talukder, Sumanjit Das, Debabrata Nath
As the human race evolves, numerous diseases have dominated humans, causing scientists to encounter myriad challenges with formulations. To rectify these issues, Nanoparticle (10-9 m) formulation approach or nanotechnology has been developed. Since nanoparticles have legion benefits, encompassing better bioavailability, target-specific, confined, accurate dose delivery, and increased surface area, are pertinent for effective treatment. Toxicity, inflammation, limited penetrating ability, accumulation, and aggregation are some of the downsides of nanoparticles. Picoscale along with nanoparticle technology in drug delivery, will enhance the permeability and myriad factors. Also, picometer (10-12 m) and futuristic femtometer (10-15 m) particles will allow scientists to deal with atomic and subatomic levels in some cases and improve the properties of nanotechnology in others. Herein, picotechnology, formulation, synthesis, and some unique properties concluding with femtotechnology have been addressed.
随着人类的进化,许多疾病主宰了人类,导致科学家在配方方面遇到了无数挑战。为了纠正这些问题,已经开发了纳米颗粒(10-9m)配方方法或纳米技术。由于纳米颗粒有很多好处,包括更好的生物利用度、靶向性、限制性、精确的剂量递送和增加的表面积,因此与有效治疗有关。毒性、炎症、有限的穿透能力、积聚和聚集是纳米颗粒的一些缺点。Picoscale与纳米颗粒技术一起用于药物递送,将增强渗透性和无数因素。此外,在某些情况下,皮米(10-12米)和未来的毫米(10-15米)粒子将使科学家能够处理原子和亚原子水平,并在其他情况下改善纳米技术的性能。本文介绍了微微技术、配方、合成和一些独特的特性,最后总结了女性技术。
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引用次数: 0
Neuroprotective effect of levetiracetam in combination with berberine on scopolamine induced-cognitive impairment in mice: A behavioral and biochemical approach 左乙拉西坦联合小檗碱对东莨菪碱诱导的小鼠认知障碍的神经保护作用:行为和生化方法
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-13 DOI: 10.2174/1574885518666230213151508
Dhaneshwar Suneela, S. Anuradha, M. Avijit, Saxena S.K, Kumar Swatantra
Presently, only four drugs have been approved by FDA for Alzheimer’s disease (AD). A drug repurposing approach can be fruitful in searching for promising candidates for AD.The objective of the work was to evaluate the neuroprotective effect of levetiracetam (LEV) in combination with berberine (BER) in scopolamine-induced cognitive impairment in mice by applying a drug repositioning approach owing to their antioxidant potential.Cognitive impairment was induced in mice by scopolamine. Morris water maze, elevated plus maze, and Y-maze were used to evaluate behavioral parameters. Assays for acetylcholinesterase (AChE), reduced glutathione (GSH), malondialdehyde (MDA), catalase, nitrite, TNF-α, and brain histopathology were performed.The transfer latency time and percentage of spontaneous alternation were significantly reduced and significant alterations in AChE and MDA levels, GSH concentration, and improvement in nitrite and catalase levels were also evidenced after the treatment of mice with a combination of LEV and BER in comparison to independent drugs, standard and disease control groups. The antioxidant defense was also improved and TNF-α levels were significantly reduced by a combination of LEV and BER. Improvement in neuronal damage by restoration of the cytoarchitecture of the brain was also seen in the histopathological study of the brain of treatment groups.The present study has demonstrated that the combination of LEV and BER has significantly improved cognition in mice by lipid peroxidation inhibition, augmentation of endogenous antioxidant enzymes, the decline in TNF- α levels, and AChE activity in the brain when compared to individual drugs, standard and disease control owing to their strong antioxidant and anti-inflammatory potentials.
目前,只有四种药物被美国食品药品监督管理局批准用于治疗阿尔茨海默病。药物再利用方法可以在寻找有前景的AD候选药物方面取得丰硕成果。本工作的目的是通过应用药物再定位方法评估左乙拉西坦(LEV)与黄连素(BER)联合治疗东莨菪碱诱导的小鼠认知障碍的神经保护作用,因为它们具有抗氧化潜力。东莨菪碱诱发小鼠认知功能障碍。采用Morris水迷宫、抬高+迷宫和Y迷宫对行为参数进行评价。检测乙酰胆碱酯酶(AChE)、还原型谷胱甘肽(GSH)、丙二醛(MDA)、过氧化氢酶、亚硝酸盐、TNF-α和脑组织病理学。与独立药物、标准组和疾病对照组相比,用LEV和BER联合治疗小鼠后,转移潜伏期和自发变化的百分比显著降低,AChE和MDA水平、GSH浓度以及亚硝酸盐和过氧化氢酶水平的改善也得到了证明。LEV和BER的组合也改善了抗氧化防御,TNF-α水平显著降低。在治疗组大脑的组织病理学研究中,还发现通过恢复大脑的细胞结构来改善神经元损伤。本研究表明,与单独的药物、标准药物和疾病控制相比,LEV和BER的组合通过抑制脂质过氧化、增强内源性抗氧化酶、降低TNF-α水平和大脑中AChE活性,显著改善了小鼠的认知能力,因为它们具有强大的抗氧化和抗炎潜力。
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引用次数: 0
An approach to treat conundrumof skin cancer: Bioactive loaded Niosomes 一种治疗皮肤癌难题的方法:生物活性载体
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-09 DOI: 10.2174/1574885518666230209150126
S. Srivastava, D. Sharma
Skin cancer is a life-threatening disease according to the World Health Organization, majorly affecting the white population. The major concerning factors that are responsible for skin cancer are genetic factors, environmental exposure including UV rays and pollutants. The UV radiations excessively generate Reactive oxygen species (ROS) and Reactive nitrogen species (RNS)due to which the oxidative stress mediates and alters numerous signaling pathways. Quercetin is a flavonoid that plays a vital role in protecting the cell from oxidative stressin addition to possessing anticancer, antioxidant, and anti-inflammatory properties. The present article focuses on the delivery of natural flavonoid quercetin via novel carrier noisome to enhance targeting and safety efficacy.The risk of developing skin cancer arises from a combination of genetic and environmental factors, the most common cause being prolonged exposure to ultraviolet (UV) light. Quercetin is a flavanoid that plays a vital role in protecting cell from oxidative stress that are activated by reactive oxygen species. It has been hence proved that the reactive oxygen species (ROS) and reactive nitrogen species (RNS) forms on of the basic cause of cancer. The drug carrier noisome enhances the bioavailability of the natural products and have an advantage of solubilizing the lipophilic compound and prevent them from deuteriation into “antagonist” condition in human blood.Thus, current research work focuses over designing and characterization of niosomes system for the treatment of skin cancer and target oxidative stress. Though many novel drug deliveries have been designed as carrier system in skin cancer, among all niosomes have been found as potential colloidal carrier.Quercetin loaded niosomes were developed and was optimized, characterized for morphological studies, entrapment efficiency, zeta potential and In vitro drug release.The quercetin loaded niosomal vesicles under the transmission electron microscope were found in range of 120 nm with suitable zeta potential and entrapment efficiency above 80% with control release profile.Formulation was successfully prepared which can be further carried out for in vivo studies.
据世界卫生组织称,皮肤癌是一种危及生命的疾病,主要影响白人。导致皮肤癌的主要因素是遗传因素、环境暴露,包括紫外线和污染物。紫外线辐射过量产生活性氧(ROS)和活性氮(RNS),因此氧化应激介导和改变了许多信号通路。槲皮素是一种类黄酮,除了具有抗癌、抗氧化和抗炎的特性外,还在保护细胞免受氧化应激方面起着至关重要的作用。本文主要研究天然类黄酮槲皮素通过新型载体载体的传递,以提高靶向性和安全性。患皮肤癌的风险是由遗传和环境因素共同引起的,最常见的原因是长时间暴露在紫外线下。槲皮素是一种黄酮类化合物,在保护细胞免受活性氧激活的氧化应激中起着至关重要的作用。由此证明,活性氧(ROS)和活性氮(RNS)是形成癌症的基本原因之一。该药物载体提高了天然产物的生物利用度,具有溶解亲脂性化合物,防止其在人体血液中氘化为“拮抗剂”的优点。因此,目前的研究工作主要集中在设计和表征用于治疗皮肤癌和靶向氧化应激的纳米体系统。虽然许多新的药物递送被设计为皮肤癌的载体系统,但在所有的乳质体中都发现了潜在的胶体载体。制备并优化了槲皮素负载niosomes,并对其进行了形态学、包封效率、zeta电位和体外释药特性研究。在透射电镜下,槲皮素负载的乳质体囊泡在120 nm范围内具有合适的zeta电位,包封效率在80%以上,并具有控释轮廓。制剂制备成功,可进一步进行体内研究。
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引用次数: 0
Computational Techniques for Drug Repurposing: A Paradigm Shift in Drug Discovery 药物再利用的计算技术:药物发现的范式转变
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-07 DOI: 10.2174/1574885518666230207143523
M. Rao, Isha Sangram Ghadge, Saurav Prasanna Kulkarni, Tanya Asthana
The last two years from 2020 to 2022 have seen the world face an unparalleled crisis in the form of the corona virus, which has challenged mankind as never before. The struggle and race to find a cure for the disease kept medical professionals, pharmacists, and scientists on their toes. Drug discovery by de novo approach was not an option due to its obvious downside of the enormous time required for the process. Hitherto unknown in public parlance, repurposing existing drugs showed the way forward for scientists. Drug repurposing involves redefining medical use for drugs that have crossed the drug discovery process and were approved, discontinued, or shelved. Drug repurposing or repositioning has shown effective results in treating several diseases. This review traces the journey of some repurposed drugs and provides an overview of computational methods used for repurposing, which include signature mapping, molecular docking, and in silico approaches. The review also highlights repurposed drugs for cancer, one of the most dreaded diseases, and how repurposing can prove to be a boon for many types of cancers. Concerted efforts to study this modality of drug discovery are the need of the hour. The article discusses various drugs which have been successfully repurposed for the treatment of a plethora of diseases. Drug repurposing is a silver lining that can reduce the arduous journey of discovering a definitive cure for a disease and has the potential to change the landscape of the drug discovery process.
从2020年到2022年的过去两年里,世界面临着前所未有的冠状病毒危机,这给人类带来了前所未有的挑战。寻找治疗这种疾病的方法的斗争和竞赛使医学专家、药剂师和科学家们保持警惕。通过从头开始的方法进行药物发现不是一种选择,因为它的缺点是这个过程需要大量的时间。迄今为止,在公共用语中还不为人知的是,重新利用现有药物为科学家指明了前进的方向。药物再利用涉及重新定义药物的医疗用途,这些药物已经通过了药物发现过程,被批准、停产或搁置。药物再利用或重新定位已显示出治疗多种疾病的有效结果。这篇综述追溯了一些重新利用药物的历程,并概述了用于重新利用的计算方法,包括特征映射、分子对接和计算机方法。该评论还强调了针对癌症(最可怕的疾病之一)的重新用途药物,以及重新用途如何证明对许多类型的癌症是一种福音。共同努力研究这种药物发现方式是当务之急。这篇文章讨论了已经成功地用于治疗过多疾病的各种药物。药物再利用是一线希望,它可以减少发现一种疾病的最终治疗方法的艰辛旅程,并有可能改变药物发现过程的格局。
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-02-01 DOI: 10.2174/157488551801221122161011
Monica Mita
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引用次数: 0
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Current Drug Therapy
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