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Exploring the Role of Cathelicidin Antimicrobial Peptide, Toll-Like Receptor 4, and HMGB-1 in Bacterial Infection 探索卡特里西丁抗菌肽、Toll-Like 受体 4 和 HMGB-1 在细菌感染中的作用
Q4 Medicine Pub Date : 2024-01-11 DOI: 10.2174/0122113525284634231222071749
Ami Febriza, H. Idrus, V. Kasim
Lipopolysaccharides (LPS) from Salmonella typhi will attach with Toll-Like Receptor 4 (TLR-4) and trigger an inflammatory response to fight the pathogen. Due to infection, the HMGB1 is produced by immune cells or secreted passively from dead cells. Fur-thermore, the antimicrobial peptide, cathelicidin was secreted to neutralize and eliminate these path-ogens. This study aims to examine the interaction of Cathelicidin antimicrobial peptide (CAMP), TLR-4, and HMGB-1 on inhibiting bacterial growth in Salmonella infection.This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony.This study aim to examine the interaction of Cathelicidin antimicrobial peptide (CAMP), TLR-4, and HMGB-1 on inhibiting bacterial growth in Salmonella infection.Our finding observed that the expression of mRNA CAMP was inversely related to bacte-rial colony count, which means that higher CAMP mRNA expression was associated with reduced bacterial colony count in groups A and B. The expression of HMGB-1 mRNA was found to be positively correlated with bacterial growth in group A. Meanwhile, TLR-4 mRNA expression did not significantly correlate with bacterial colony count in any groups.This study is an experiment that uses a pre-post-test design. Mice balb/c were separated into three groups; group A received levofloxacin for five days, group B received a placebo, and group C was the control. Both groups, A and B, received an injection of S. Typhi strain thy1. Blood samples were taken from three groups on the 4th, 10th, and 30th day to calculate CAMP, TLR-4, and HMGB-1 mRNA gene expression levels. To determine bacterial colony, peritoneal fluid was taken three times on the 4th, 10th, and 30th day to calculate bacterial colony.CAMP, TLR-4, and HMGB-1 affect bacterial infections. Higher expression CAMP mRNA levels lower colony counts. Meanwhile, decreasing TLR-4 and HMGB-1 mRNA expression were found during the study, due to reducing growth bacteria.The expression of mRNA CAMP and bacterial colony count correlated negatively. The expression of HMGB-1 mRNA correlated with bacterial growth. Higher CAMP mRNA expression was found to relate to reduced bacterial colony count in groups A and B using linear regression.
伤寒沙门氏菌的脂多糖(LPS)会附着在 Toll-Like Receptor 4(TLR-4)上,引发炎症反应以对抗病原体。由于感染,免疫细胞会产生或从死亡细胞中被动分泌 HMGB1。此外,抗菌肽 cathelicidin 也被分泌出来,以中和并消除这些病原体。本研究旨在探讨猫科动物抗菌肽(CAMP)、TLR-4 和 HMGB-1 在沙门氏菌感染中抑制细菌生长的相互作用。小鼠 balb/c 被分为三组:A 组接受左氧氟沙星治疗五天,B 组接受安慰剂治疗,C 组为对照组。三组分别在第 4 天、第 10 天和第 30 天抽取血液样本,计算 CAMP、TLR-4 和 HMGB-1 mRNA 基因表达水平。本研究旨在探讨猫科动物抗菌肽(CAMP)、TLR-4 和 HMGB-1 在沙门氏菌感染中抑制细菌生长的相互作用。我们的研究结果表明,mRNA CAMP 的表达与细菌菌落数成反比,即 CAMP mRNA 表达越高,A 组和 B 组的细菌菌落数越少。小鼠 balb/c 被分为三组:A 组接受左氧氟沙星治疗五天,B 组接受安慰剂治疗,C 组为对照组。三组分别在第 4 天、第 10 天和第 30 天抽取血液样本,计算 CAMP、TLR-4 和 HMGB-1 mRNA 基因表达水平。为确定细菌菌落,在第 4 天、第 10 天和第 30 天分三次抽取腹腔液计算细菌菌落。CAMP、TLR-4 和 HMGB-1 对细菌感染有影响。CAMP mRNA 表达水平越高,菌落数越低。同时,在研究过程中发现,TLR-4 和 HMGB-1 mRNA 的表达量减少,这是因为细菌的生长速度降低了。HMGB-1 mRNA 的表达与细菌生长相关。使用线性回归法发现,CAMP mRNA 的高表达与 A 组和 B 组细菌菌落数的减少有关。
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引用次数: 0
Current Status of Potential Antiviral Drugs Derived from Plant, Marine,and Microbial Sources 从植物、海洋和微生物资源中提取的潜在抗病毒药物的现状
Q4 Medicine Pub Date : 2024-01-09 DOI: 10.2174/0122113525272349231210055403
Rashmi Saini, Mohammad I. Ali, Maya Pant, Ashish Warghane
Natural substances have been the principal source of medications since antiquity.Natural goods are gaining popularity as a source of novel medications. This article investigates a variety of variables like plant, marine, and microbial sources that contribute to thegrowing interest in natural goods as a source of novel medications. Viruses have remainedresistant to treatment and prevention for a longer period than other forms of life. Viral diseases can currently only be treated with a limited number of drugs. Significant research initiatives have been committed to identifying novel antiviral natural compounds to fight virusesthat harm people, plants, insects, animals, fungi, and microbes. A recent study of the prevalence and sources of antiviral medications licensed by the Food and Drug Administration(FDA) has focused on natural products. Out of the estimated 250,000 higher plant species,only 5 to 15 percent have been thoroughly evaluated for the existence of bioactive substancesin them, and the ability of the other species has hardly been investigated. This review aims tooffer an overview of the crucial role played by natural products in the discovery and development of novel antiviral drugs with potent antiviral activity, including phytochemicals suchas carbohydrates, coumarins, flavonoids, chromones, alkaloids, lignans, phenols, tannins,proteins, peptides, antiviral plant extracts, other marine, and microbial sources.
自古以来,天然物质一直是药物的主要来源。本文研究了植物、海洋和微生物来源等各种变量,这些变量促使人们对天然物品作为新型药物来源的兴趣与日俱增。与其他生命形式相比,病毒在更长的时期内一直对治疗和预防具有抗药性。目前,只有有限的几种药物可以治疗病毒性疾病。人们一直致力于寻找新型抗病毒天然化合物,以对抗危害人类、植物、昆虫、动物、真菌和微生物的病毒。最近,一项关于美国食品和药物管理局(FDA)许可的抗病毒药物的普遍性和来源的研究将重点放在了天然产品上。在约 25 万种高等植物中,只有 5% 至 15% 的植物因含有生物活性物质而得到过全面评估,其他物种的能力几乎没有得到过研究。本综述旨在概述天然产品在发现和开发具有强效抗病毒活性的新型抗病毒药物中发挥的关键作用,包括植物化学物质,如碳水化合物、香豆素、黄酮类、色酮类、生物碱、木脂素、酚类、单宁酸、蛋白质、肽、抗病毒植物提取物、其他海洋生物和微生物来源。
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引用次数: 0
Comparative Analysis of Chemical Composition and Antibacterial Activities of Essential Oils from Two Ocimum Species 两种欧加木精油的化学成分和抗菌活性对比分析
Q4 Medicine Pub Date : 2023-12-20 DOI: 10.2174/0122113525274800231120065500
Md. Rokonuzzaman, Atiqur Rahman, Abu Reza, Nilufar Yasmin Liz, S. Okay, Mohammad Abu Hena Mostofa Jamal, Ibrahim Demirtas
The species of the genus Ocimum has been used since ancient times in the Indian subcontinent to cure various illnesses. Essential oil from Ocimum species has antimicrobial activity. The main objective of this study was to extract essential oils from different parts of two Ocimum species and test their antimicrobial activity Hydrodistillation was used to extract essential oils from various parts of two basil species, CG_MS was used to identify the chemical compounds, and disk diffusion method was used to assess their antimicrobial activity. A total of sixty-seven chemical compounds from Ocimum sanctum L. and Ocimum gratissimum L. were identified using GC-MS. Among them, eugenol (1.00-27.66%), methyl eugenol (0.78-28.52%), β-elemene (5.10-20.98%), caryophyllene (0.94-43.18%), caryophyllene oxide (1.1-10.81%), palmitic acid methyl ester (3.20-21.38%), oleic acid methyl ester (2.91-40.7%) and linoleic acid methyl ester (1.55-74.71%) comprised the majority of the makeup of essential oils, due to diverse plant species and body sections, the percentage differed significantly. The essential oils contained monoterpenes, sesquiterpenes, and aldehydes/ketonic derivatives in the flower and leaf parts of O. sanctum and the leaf part of O. gratissimum. The essential oils of these Ocimum species showed good antibacterial activities against the bacteria, methicillin-resistant Staphylococcus aureus (MRSA), Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, and Enterococcus faecalis with inhibition zones ranging from 10-36 mm. These two species of Ocimum showed significant variation in chemical composition and antibacterial activity.
自古以来,印度次大陆的人们就一直使用欧加木属植物来治疗各种疾病。欧加木属植物的精油具有抗菌活性。 本研究的主要目的是从两种欧加木属植物的不同部位提取精油,并测试其抗菌活性。研究人员采用水蒸馏法从两种罗勒属植物的不同部位提取精油,用 CG_MS 方法鉴定化合物,并用盘式扩散法评估其抗菌活性。 采用气相色谱-质谱法从 Ocimum sanctum L. 和 Ocimum gratissimum L. 中鉴定出了 67 种化合物。其中,丁香酚(1.00-27.66%)、甲基丁香酚(0.78-28.52%)、β-榄香烯(5.10-20.98%)、茶叶烯(0.94-43.18%)、氧化茶叶烯(1.1-10.81%)、棕榈酸甲酯(3.20-21.38%)、油酸甲酯(2.由于植物种类和身体部位的不同,所占比例也有很大差异。在圣女果(O. sanctum)的花和叶部分以及欧加桑(O. gratissimum)的叶部分中,精油含有单萜、倍半萜和醛/酮衍生物。这些欧加木物种的精油对耐甲氧西林金黄色葡萄球菌(MRSA)、肺炎克雷伯氏菌、绿脓杆菌、大肠杆菌和粪肠球菌等细菌具有良好的抗菌活性,抑菌区范围为 10-36 毫米。 这两种欧加木在化学成分和抗菌活性方面存在显著差异。
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引用次数: 0
Recent Trends on Synthesis of Benzimidazoles 苯并咪唑合成的最新趋势
Q4 Medicine Pub Date : 2023-11-30 DOI: 10.2174/0122113525276208231116121402
A. A. El-Rashedy, Asmaa A. Magd El-Din, Nabil M. Yousif, Mahmoud N. M. Yousif
Preparation of benzimidazole derivatives have become the interest of many chemists because of the versatile therapeutic activity of benzimidazoles as antiulcer, antimicrobial, anti-viral, anticancer, anti-inflammatory, analgesic and anthelmintic drugs. This review will de-scribe the most recent research on benzimidazole synthesis.
苯并咪唑具有抗溃疡、抗菌、抗病毒、抗癌、消炎、镇痛和驱虫等多种治疗活性,因此制备苯并咪唑衍生物已成为许多化学家的兴趣所在。本综述将介绍有关苯并咪唑合成的最新研究。
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引用次数: 0
Preliminary Study of Antibiotics Susceptibility Testing and Pathogens Associated with Nosocomial Infections in a Tertiary Hospital 某三级医院抗生素药敏试验及院内感染病原菌的初步研究
Q4 Medicine Pub Date : 2023-10-27 DOI: 10.2174/0122113525259607231020063637
Zahra Tolou Ghamari
Health care associated with multiresistant pathogens is rising globally. As nosocomial infections (NIs) could increase hospital stay, morbidity, mortality and disability, therefore the aim of this preliminary study was to define antibiotics and pathogens associated with NIs in a main tertiary hospital in Isfahan, Iran. The data were extracted from the official database of hospital NIs records. For each patient, the reported infections were abbreviated as: UTI-SUTI, VAE-PVAP, BSI-LCBI, SSI-DIP and so on. For continuous variables, mean ± standard deviation, and for categorical varia-bles, frequency was used. To define and rank nosocomial infections in a tertiary hospital The study population was 5542 patients, comprised of males (n=3282) and females (n=2260). With a minimum of 15 and a maximum of 99, the mean age in 5313 patients was 58.5 ± 19.1 years old. The highest reported NIs (n= 77%) were associated with the ages between 30-80 years old. Sites of NIs in 93% were as: VAE-PVAP- VAE-IVAC; 31%, UTI-SUTI; 30%, SSI-DIP; 19%, BSI-LCBI; 13%, and other individual infection (7%) with the main pathogens associated with Acinetobacter baumannii, Klebsiella pneumonia, Candida and Staphylococcus spp. Antibiotic susceptibilty testing showed the most sensitivity of isolates against Vancomycin (62%), Gentamicin (59%), Ampicillin (44%), Amikacin (35%) and Co-trimoxazol (32%). The data were extracted from the official database of hospital nosocomial infections records that were included 9152 vertical row. For each patient the reported infections were coded by number as: UTI-SUTI; Code 55, VAE-PVAP; Code 56, BSI-LCBI Code 19, SSI-DIP; Code 14 and so on. For continuous variables mean ± standard deviation and for categorical variables frequency were used. As most NIs are avoidable, for commissioning an efficient surveillance system, further study of pathogens in relation to evidence-based antibiotic-therapy and advanced infection control program is suggested to be valuable. The study population were 5542 patients, comprised of males (n=3282) and females (n=2260). With a minimum of 15 and a maximum of 99, the mean age in 5313 patients was 58.5 ± 19.1 years old. The highest reported nosocomial infections (n= 77%) were associated with the ages between 30-80 years old. Sites of nosocomial infections in 87% were as: VAE-PVAP; 27.3%, VAE-IVAC; 7.7, UTI-SUTI; 29.5%, BSI-LCBI; 12.9%, SSI-DIP; 9.5% and other individual infection (13%) with the main pathogens associated with klebsiella, acinetobacter baumannii and staphylococcus. Antibiotics reported to R and S were ranked as; Co-trimoxazol (R; 2244, S; 1019), Amikacin (R; 1878, S; 1011), Ceftazidim (R; 2332, S; 546), Meropenem (R; 1920, S; 951) and Cefipime (R; 2243, S; 588).
背景:与多重耐药病原体相关的卫生保健正在全球范围内上升。由于医院感染(NIs)可能增加住院时间、发病率、死亡率和残疾,因此本初步研究的目的是确定伊朗伊斯法罕一家主要三级医院与NIs相关的抗生素和病原体。方法:数据来源于医院NIs官方数据库。每个患者报告的感染情况缩写为:UTI-SUTI、VAE-PVAP、BSI-LCBI、SSI-DIP等。对于连续变量,使用平均值±标准差,对于分类变量,使用频率。目的:对某三级医院的医院感染进行定义和排序。结果:研究人群5542例,其中男性3282例,女性2260例。5313例患者的平均年龄为58.5±19.1岁,最小15岁,最大99岁。最高报告的NIs (n= 77%)与年龄在30-80岁之间有关。93%的NIs位点分别为:VAE-PVAP- VAE-IVAC;31%, UTI-SUTI;30%, SSI-DIP;19%, BSI-LCBI;其他个体感染占7%,主要病原菌为鲍曼不动杆菌、肺炎克雷伯菌、念珠菌和葡萄球菌。抗生素敏感性试验显示,分离株对万古霉素(62%)、庆大霉素(59%)、氨苄西林(44%)、阿米卡星(35%)和复方新诺新唑(32%)的敏感性最高。方法:数据取自医院医院感染记录官方数据库,纵列9152行。对每个患者报告的感染按编号编码为:UTI-SUTI;代码55,VAE-PVAP;代码56,BSI-LCBI代码19,SSI-DIP;代码14等等。连续变量用均值±标准差,分类变量用频率。结论:由于大多数NIs是可以避免的,为建立有效的监测系统,进一步研究病原体与循证抗生素治疗和先进的感染控制方案的关系是有价值的。结果:研究人群5542例,其中男性3282例,女性2260例。5313例患者的平均年龄为58.5±19.1岁,最小15岁,最大99岁。最高报告的医院感染(n= 77%)与年龄在30-80岁之间相关。87%的医院感染部位为:VAE-PVAP;27.3%, VAE-IVAC;7.7, UTI-SUTI;29.5%, BSI-LCBI;12.9%, SSI-DIP;9.5%和其他个体感染(13%),其主要病原体与克雷伯氏菌、鲍曼不动杆菌和葡萄球菌有关。报告R和S的抗生素为;Co-trimoxazol (R;2244年代;1019),阿米卡星(R;1878年代;1011),头孢他啶(R;2332年代;546),美罗培南(R;1920年代;951)和头孢吡肟(R;2243年代;588)。
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引用次数: 0
Nosocomial Urinary Tract Infections in a Tertiary Hospital; Preliminary Study of Antibiotics Susceptibility Testing and Pathogen Types 某三级医院院内尿路感染病例分析抗生素药敏试验与病原菌类型的初步研究
Q4 Medicine Pub Date : 2023-10-25 DOI: 10.2174/0122113525258170231016081424
Zahra Tolou-Ghamari
Nosocomial urinary tract infections (NUTIs) are the most frequentlyacquired infection worldwide. This retrospective study aimed to determine the type of pathogensand antibiotic susceptibility testing in hospital-acquired UTIs.Information from the recorded official database of the Alzahra, Isfahan/Iran tertiaryspecialist hospital was obtained. Urine was collected based on two methods: 1) central streamand 2) with a urinary catheter in place. The incidence of acquired infections (NUTIs-SUTI; Code55) was described as a percentage. The statistical calculations were conducted using the statistical software. There were 2210 recorded NUTIs comprised of 1115 males and 1095 females.Among the total recorded data with NUTIs, 251 records were associated with deaths. The distribution of hospital stays in 57% was between 2-30 days. Available data showed that Candida(23%), Escherichia coli (22%), Klebsiella pneumonia (17%), and Enterococcus (faeciumfecalis; 12%) were the most ranked microorganisms in patients with NUTIs.Sensitivity tests for Escherichia coli associated with different antibiotics were rankedas; 1) Meropenem (n= 160; S= 66%), 2) Vancomycin (n= 53; S= 64%), 3) Piperacillin/Tazobactam (n= 144; S= 58%), 4) Amikacin (n= 146; S= 44%), 5) Co-trimoxazole (n= 153; S=42%),6) Penicillin (n=79; S=41%), 7) Cefepime (n=143; S=31%), 8) Ceftazidime (n=142; S=31%),9) Ciprofloxacin (n=204; S=25%). Sensitivity tests for Klebsiella pneumonia associated withdifferent antibiotics were ranked as; 1) Piperacillin/Tazobactam (n= 110; S= 55%), 2) Amikacin(n= 125; S= 55%), and 3) Ciprofloxacin (n=177; S=23%). Sensitivity tests for Enterococcus(faecium-fecalis) associated with different antibiotics were ranked as; 1) Piperacillin/Tazobactam (n= 79; S= 62%), 2) Amikacin (n= 83; S= 64%) and 3) Ciprofloxacin (n=120; S=30%).Within the population studied, while Ciprofloxacin showed less than 30% sensitivity, Piperacillin/Tazobactam and Amikacin exhibited a sensitivity of more than 50% regardingEscherichia coli, Klebsiella pneumonia, and Enterococcus (faecium-fecalis) need further evidence-based investigations
摘要医院性尿路感染是世界范围内最常见的获得性感染。本回顾性研究旨在确定医院获得性尿路感染的病原体类型和抗生素敏感性检测。方法:从伊朗伊斯法罕Alzahra三级专科医院的官方数据库中获取资料。收集尿液的方法有两种:1)中央静脉和2)放置导尿管。获得性感染的发生率(NUTIs-SUTI;代码55)以百分比表示。采用统计软件进行统计计算。共有2210例nuti记录,其中男性1115例,女性1095例。在NUTIs记录的全部数据中,251条记录与死亡有关。57%的患者住院时间分布在2 ~ 30天之间。现有数据显示,念珠菌(23%)、大肠杆菌(22%)、肺炎克雷伯菌(17%)和肠球菌(粪肠球菌;12%)是NUTIs患者中排名最高的微生物。结果:不同抗生素对大肠杆菌的敏感性试验均为;1)美罗培南(n= 160);S= 66%), 2)万古霉素(n= 53;S= 64%), 3)哌拉西林/他唑巴坦(n= 144;S= 58%), 4)阿米卡星(n= 146;S= 44%), 5)复方新诺明(n= 153;S=42%), 6)青霉素(n=79;S=41%), 7)头孢吡肟(n=143;S=31%), 8)头孢他啶(n=142;S=31%), 9)环丙沙星(n=204;S = 25%)。肺炎克雷伯菌与不同抗生素的敏感性试验为;1)哌拉西林/他唑巴坦(n= 110);S= 55%), 2)阿米卡星(n= 125;S= 55%), 3)环丙沙星(n=177;S = 23%)。肠球菌(粪-粪)与不同抗生素的敏感性试验为;1)哌拉西林/他唑巴坦(n= 79;S= 62%), 2)阿米卡星(n= 83;S= 64%)和3)环丙沙星(n=120;S = 30%)。结论:在所研究的人群中,环丙沙星的敏感性低于30%,而哌拉西林/他唑巴坦和阿米卡星对大肠杆菌、肺炎克雷伯菌和肠球菌(粪-粪)的敏感性超过50%,需要进一步的循证调查
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引用次数: 0
Monkey Pox: Virology, Epidemiology, Vaccines, and Therapeutic Approaches 猴痘:病毒学,流行病学,疫苗和治疗方法
Q4 Medicine Pub Date : 2023-10-12 DOI: 10.2174/0122113525258072230920074245
Abin V. Geevarghese
Abstract: The monkeypox virus, which was historically common in West and Central Africa, is the source of the zoonotic disease known as monkeypox. Instances, however, have recently been confirmed in a few non-endemic nations outside of Africa. In light of the COVID-19 pandemic, the WHO labeled the current monkeypox epidemic a public health emergency of global concern on July 23, 2022. The international society may be in jeopardy due to the rapidly increasing number of confirmed cases. Current epidemiological statistics indicate that the high frequency of transmission from person to person might result in additional epidemics, especially among guys who have sex with males. Despite certain therapeutic benefits of already prescribed pharmaceuticals, there is an urgent need for the creation of antiviral therapies and vaccinations to ward off the monkeypox virus. We offer pertinent information to help people understand the monkeypox virus and help medical professionals in stopping the spread of the monkeypox virus.
摘要:猴痘病毒在西非和中非历史上很常见,是猴痘人畜共患疾病的来源。然而,最近在非洲以外的一些非流行国家证实了这种情况。鉴于2019冠状病毒病大流行,世卫组织于2022年7月23日将当前的猴痘疫情列为全球关注的突发公共卫生事件。由于确诊病例迅速增加,国际社会可能处于危险之中。目前的流行病学统计数据表明,人与人之间传播的高频率可能导致更多的流行病,特别是在与男性发生性关系的男子中。尽管处方药物有一定的治疗效果,但迫切需要创造抗病毒疗法和疫苗来抵御猴痘病毒。我们提供相关信息,帮助人们了解猴痘病毒,并帮助医疗专业人员阻止猴痘病毒的传播。
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引用次数: 0
A Review on Emerging Impact of Antitubercular Activity of 1,2,4-Triazole Derivatives 1,2,4-三唑类衍生物抗结核活性研究进展
Q4 Medicine Pub Date : 2023-10-11 DOI: 10.2174/0122113525268198230921071016
Vedavathi R, Umesh Laddi
Abstract: The present review aims to summarize the antitubercular profile of 1,2,4-triazole, one of the emerging entitled and most sought scaffold with a wide spectrum of biological and pharmacological activities. A systematic review of literature on ‘Heterocycles’, establishes the fact that 1,2,4-triazoles and their derivatives exhibit diverse activities. The 1,2,4-triazole core is found in therapeutically significant drugs and many new ones are in the pipeline. ‘Triazole pharmacophore’ has replaced the widely used ‘imidazole’ as ‘systemically integral azole’ by connecting synchronicity with serendipity. Triazoles are penetratingly studied as ‘diverse therapeutic agents’, due to the improved efficacy and reduced side effects. The extensive anthology of work carried out in the last two decades on 1,2,4-triazole moiety will provide imminent scope for the development of novel potential drugs having better efficacy selectivity and reduced toxicity.
摘要:本文综述了1,2,4-三唑的抗结核概况,它是一种具有广泛生物学和药理活性的新型支架材料。对“杂环”的文献进行系统回顾,确定了1,2,4-三唑及其衍生物具有多种活性的事实。1,2,4-三唑核心存在于具有重要治疗意义的药物中,许多新药物正在研发中。“三唑药效团”通过将同步性与偶然性联系起来,取代了广泛使用的“咪唑”作为“系统积分唑”。三唑类药物由于疗效提高和副作用减少而被广泛研究为“多种治疗药物”。近二十年来对1,2,4-三唑部分的广泛研究将为开发具有更好疗效、选择性和低毒性的新型潜在药物提供迫切的空间。
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引用次数: 0
Advances in Microneedle-Based Approaches for Skin Diseases: A Comprehensive Review of Therapeutic Applications and Future Perspectives 基于微针的皮肤疾病治疗方法的进展:治疗应用的综合综述和未来展望
Q4 Medicine Pub Date : 2023-09-11 DOI: 10.2174/2211352521666230911155555
Suraj Kumar, Pramod Kumar Sharma, Rishabha Malviya, Md. Aftab Alam, Sakshi Sagar
Background: Psoriasis is a persistent skin condition for which only symptom management is currently available. Topical and systemic medicines, physical therapy, and other methods are all part of the standard treatment strategy. New medication delivery methods for psoriasis are urgently needed because of the present methods' shortcomings. Objective: The objective of this article is to provide a comprehensive description of microneedles as well as their development in the treatment of psoriasis and the clinical challenges associated with them. Discussion: The microneedle (MNs) technology is better than other transdermal delivery methods because it has so many benefits, including low invasiveness, painlessness, simplicity, and enhanced patient compliance. Coated microneedles, hollow microneedles, dissolving microneedles, and solid microneedles are the four basic categories into which researchers have so far sorted the fast-expanding area of microneedles. Each of these kinds of microneedles offers its own unique advantages due to their unique properties and layout. Conclusion: MNs may significantly improve transdermal medication penetration by mechanically opening skin micropores. Meanwhile, this method demonstrates distinct benefits over injection and oral delivery, such as painless application, the least amount of intrusion, the simplicity of self-administration, and avoiding the first-pass impact.
背景:牛皮癣是一种持续的皮肤状况,目前只有症状管理可用。局部和全身药物,物理治疗和其他方法都是标准治疗策略的一部分。由于现有给药方法的不足,迫切需要新的给药方法。目的:本文的目的是提供一个全面的描述,微针及其发展在治疗牛皮癣和临床挑战与他们相关。讨论:微针(MNs)技术比其他透皮给药方法更好,因为它有很多好处,包括低侵入性、无痛性、简单性和提高患者依从性。包覆微针、空心微针、溶解微针和固体微针是目前研究人员将微针快速发展的领域划分为四种基本类型。由于其独特的性质和布局,每种微针都有其独特的优势。结论:MNs可通过机械打开皮肤微孔,显著促进药物透皮渗透。同时,与注射和口服给药相比,这种方法具有明显的优点,如无痛应用,侵入量最小,自我给药简单,避免首次通过的影响。
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引用次数: 0
Fabrication of Eucalyptus Oil-loaded Ciprofloxacin Hydrochloride Topical Films for Enhanced Treatment of Post-operative Wound Infection 桉树油载盐酸环丙沙星外用膜的制备强化治疗术后伤口感染
Q4 Medicine Pub Date : 2023-09-05 DOI: 10.2174/2211352521666230905140633
Rakeshkumar Parmar, Nimisha Kalal, Janki Patel, Payal Chauhan
The efficacious penetration of antimicrobials at infectious sites and the reduction of microbial resistance development are critical in controlling the effective treatment of post-operative wound infection.To create the enhanced antimicrobial topical films, a solvent casting method for ciprofloxacin hydrochloride (CiproHCl) loaded eucalyptus oil (EO) containing low molecular weight chitosan films was used. Nine batches of CiproHCl with varying chitosan and glycerol concentrations were prepared and tested. Additionally, optimised CiproHCl films with EO were created and tested. The antimicrobial activity of CiproHCl-loaded EO containing low molecular weight chitosan films against S. Aureus, E. Coli, and B. Subtilus was tested.The FT-IR spectroscopy and DSC analysis revealed no interaction between the drug and any of the other excipients, and the drug remained amorphous in chitosan film. The SEM analysis revealed that the prepared CiproHCl-loaded EO-containing films had smooth surfaces and large agglomerates. In vitro drug release testing revealed that the EO-loaded films have a sustained release profile of up to 16 hours with a cumulative drug release of 96.83%. In an ex vivo drug permeation study, CiproHCl-loaded EO-containing films demonstrated 2.44 times more permeation flux than CiproHCl-alone films. After six months, the stability study revealed that the CiproHCl-loaded EO-loaded EO-containing film showed no significant change in drug release profile or folding endurance.This present study highlights the possible usage of CiproHCl-loaded EO containing low molecular weight chitosan films in enhanced post-operative wound treatment.
抗菌药物在感染部位的有效渗透和减少微生物耐药性的发展对于控制术后伤口感染的有效治疗至关重要。为了制备增强型抗菌局部膜,采用溶剂浇铸法制备了负载盐酸环丙沙星(CiproHCl)的低分子量壳聚糖桉树油(EO)膜。制备并测试了九批具有不同壳聚糖和甘油浓度的CiproHCl。此外,还制作并测试了具有EO的优化CiproHCl薄膜。测试了CiproHCl负载EO的低分子量壳聚糖膜对金黄色葡萄球菌、大肠杆菌和枯草芽孢杆菌的抗菌活性。FT-IR光谱和DSC分析显示,该药物与任何其他赋形剂之间没有相互作用,并且该药物在壳聚糖膜中保持无定形。SEM分析表明,制备的负载CiproHCl的EO薄膜具有光滑的表面和大的团聚体。体外药物释放测试显示,负载EO的薄膜具有长达16小时的持续释放特性,累积药物释放率为96.83%。在离体药物渗透研究中,负载CiproHCl的含EO薄膜的渗透通量是单独使用CiproHCl薄膜的2.44倍。六个月后,稳定性研究表明,CiproHCl负载的EO负载的含有EO的膜在药物释放曲线或折叠耐受性方面没有显示出显著变化。本研究强调了CiproHCl负载EO的低分子量壳聚糖膜在强化术后伤口治疗中的可能用途。
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Anti-Infective Agents
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