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Otostegia fruticosa (Forssk.) – A comprehensive insight of its ethnopharmacology, phytochemistry, and pharmacological activities Otostegia fruticosa (Forssk.) - 对其民族药理学、植物化学和药理活性的全面了解
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-11-01 DOI: 10.1016/j.jsps.2024.102189
Otostegia fruticosa (Forssk.) is a shrub of the Lamiaceae family with a wide geographic distribution in Saudi Arabia, Western and Eastern Africa, Ethiopia, and the Middle East. The current study provides an overview of recent developments in the knowledge of O. fruticosa’s ethnobotanical, pharmacological, and phytochemical properties. In folkloric medicine, it has been used since ancient times for gastrointestinal disorders, oral health, ocular irritation, antiparasitic, diarrhea, tonsillitis, arthritis, respiratory complications, and sunstroke treatment. Pharmacological investigations of its antibacterial, antioxidant, anti-inflammatory, cytotoxic, analgesic, larvicidal, nephroprotective, and other effects further validated its folklore practice. A range of diterpenoids, triterpenes, flavonoids, and essential oils have been found in O. fruticosa, according to phytochemical studies, which are thought to be responsible for the pharmacological effects of this plant species. This scientific review summarizes the most important secondary metabolites isolated from the O. fruticosa. It also summarizes the biological activities, providing insights into further scientific exploration.
Otostegia fruticosa(Forssk.)是一种唇形科灌木,广泛分布于沙特阿拉伯、非洲西部和东部、埃塞俄比亚和中东地区。目前的研究概述了有关 O. fruticosa 的民族植物学、药理学和植物化学特性的最新进展。在民间医药中,它自古以来就被用于治疗胃肠道疾病、口腔健康、眼部刺激、抗寄生虫、腹泻、扁桃体炎、关节炎、呼吸系统并发症和中暑。对其抗菌、抗氧化、抗炎、细胞毒性、镇痛、杀幼虫、保护肾脏等功效的药理研究进一步验证了其民间做法。根据植物化学研究发现,O. fruticosa 中含有一系列二萜类、三萜类、黄酮类和精油,这些物质被认为是该植物物种药理作用的主要成分。这篇科学综述总结了从 O. fruticosa 分离出来的最重要的次生代谢物。它还总结了其生物活性,为进一步的科学探索提供了启示。
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引用次数: 0
Cytochrome c and cancer cell metabolism: A new perspective 细胞色素 c 与癌细胞代谢:新视角
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-31 DOI: 10.1016/j.jsps.2024.102194
Cytochrome c is a vital electron carrier in the mitochondrial respiratory chain. When the outer membrane of mitochondria becomes permeable, cytochrome c is discharged into the cytoplasm, where it initiates the intrinsic apoptosis pathway. The complex interaction between cytochrome c and apoptosis protease-activating factor-1 (Apaf-1) leads to the formation of the apoptosome and activation of a cascade of caspases, highlighting the critical role of cytochrome c in controlling cell death mechanisms. Additionally, cytochrome c undergoes post-translational modifications, especially phosphorylation, which intricately regulate its roles in both respiration and apoptosis. These modifications add layers of complexity to how cytochrome c effectively controls cellular functions. cytochrome c becomes a lighthouse in the intricate web of cancer, its expression patterns providing hints about prognosis and paths toward treatment. Reduced levels of cytochrome c have been observed in cancer tissues, indicating a potential inhibition of apoptosis. For instance, in glioma tissues, cytochrome c levels were lower compared to healthy tissues, and this reduction became more pronounced in advanced stages of the disease. However, the role of cytochrome c in cancer becomes more intricate as it becomes intertwined with the metabolic reprogramming of cancer cells. This suggests that cytochrome c plays a crucial role in tumor progression and resistance to treatment. Viewing cytochrome c as a molecular mosaic reveals that it is not merely a protein, but also a central player in determining cellular fate. This realization opens up exciting avenues for potential advancements in cancer diagnosis and treatment strategies. Despite the advancements made, the narrative surrounding cytochrome c remains incomplete, urging further exploration into its complexities and the biological implications linked to cancer. cytochrome c stands as a beacon of hope and a promising target for therapy in the battle against cancer, particularly due to its significant involvement in tumor metabolism. It holds the potential for a future where innovative solutions can be developed to address the intricate challenges of cellular fate. In this review, we have endeavored to illuminate the multifaceted domain of cytochrome c drawing connections among apoptosis, metabolic reprogramming, and the Warburg effect in the context of cancer.
细胞色素 c 是线粒体呼吸链中的重要电子载体。当线粒体外膜发生渗透时,细胞色素 c 就会被释放到细胞质中,从而启动内在凋亡途径。细胞色素 c 与凋亡蛋白酶激活因子-1(Apaf-1)之间的复杂相互作用导致凋亡小体的形成和 caspases 级联反应的激活,从而凸显了细胞色素 c 在控制细胞死亡机制中的关键作用。此外,细胞色素 c 还会发生翻译后修饰,特别是磷酸化,从而错综复杂地调节其在呼吸和细胞凋亡中的作用。这些修饰使细胞色素 c 如何有效控制细胞功能变得更加复杂。细胞色素 c 成为癌症复杂网络中的灯塔,其表达模式为预后和治疗提供了提示。在癌症组织中观察到细胞色素 c 水平降低,这表明细胞凋亡可能受到抑制。例如,在胶质瘤组织中,细胞色素 c 的水平比健康组织低,这种降低在疾病晚期更为明显。然而,细胞色素 c 在癌症中的作用变得更加复杂,因为它与癌细胞的代谢重编程交织在一起。这表明,细胞色素 c 在肿瘤进展和抗药性方面起着至关重要的作用。将细胞色素 c 看作分子马赛克揭示了它不仅仅是一种蛋白质,还是决定细胞命运的核心角色。这一认识为癌症诊断和治疗策略的潜在进步开辟了令人兴奋的途径。尽管取得了进展,但围绕细胞色素 c 的叙述仍不完整,这就需要进一步探索其复杂性以及与癌症相关的生物学意义。细胞色素 c 是抗击癌症的希望灯塔和有前途的治疗目标,特别是因为它在肿瘤代谢中的重要作用。在未来,细胞色素 c 具有开发创新解决方案的潜力,以应对细胞命运的复杂挑战。在这篇综述中,我们试图阐明细胞色素 c 的多面性,并在癌症的背景下将细胞凋亡、新陈代谢重编程和沃伯格效应联系起来。
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引用次数: 0
Rise of implantable drugs: A chronicle of breakthroughs in drug delivery systems 植入式药物的兴起:给药系统突破纪事
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-30 DOI: 10.1016/j.jsps.2024.102193
In recent years, implantable drug delivery systems (IDDSs) have undergone significant advancements because they offer many advantages to patients and health care professionals. Miniaturization has reduced the size of these devices, making them less invasive and easier to implant. Remote control provides more precise medication delivery and dosage. Biodegradable implants are an additional advancement in implantable drug delivery systems that eliminate the need for surgical removal. Smart implants can monitor a patient’s condition and adjust their drug doses. Long-acting implants also provide sustained drug delivery for months or even years, eliminating the need for regular medication dosing, and wireless power and data transmission technology enables the use of devices that are more comfortable and less invasive. These innovations have enhanced patient outcomes by enabling more precise administration, sustained drug delivery, and improved health care monitoring. With continued research and development, it is anticipated that IDDSs will become more effective and provide patients with improved health outcomes. This review categorizes and discusses the benefits and limitations of recent novel IDDSs for their potential therapeutic use.
近年来,植入式给药系统(IDDS)取得了长足的进步,因为它们为患者和医护人员提供了许多优势。微型化缩小了这些设备的尺寸,使其创伤更小、更易于植入。远程控制可提供更精确的给药和剂量。生物可降解植入体是植入式给药系统的又一进步,无需手术取出。智能植入体可以监测病人的病情并调整药物剂量。长效植入体还能持续给药数月甚至数年,无需定期服药,而无线供电和数据传输技术则使设备的使用更舒适、创伤更小。这些创新技术通过实现更精确的给药、持续给药和更好的医疗监测,提高了患者的治疗效果。随着研究和开发的不断深入,预计 IDDS 将变得更加有效,并为患者提供更好的医疗效果。本综述对最近出现的新型 IDDS 进行了分类,并讨论了其潜在治疗用途的优点和局限性。
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引用次数: 0
A systematic review of obesity burden in Saudi Arabia: Prevalence and associated co-morbidities 沙特阿拉伯肥胖负担的系统回顾:患病率及相关并发症
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-24 DOI: 10.1016/j.jsps.2024.102192

Introduction

Saudi Arabia has experienced an increasing trend in obesity prevalence in the last three decades; obesity is a significant risk factor for non-communicable diseases, which may cause healthcare and economic burdens. In this systematic review, we aim to explore the obesity prevalence, obesity-related complications (ORCs), and the economic burden of obesity in Saudi Arabia.

Methods

Literature searches for relevant local studies across Saudi Arabia spanning 2012 to 2022 were performed in PubMed and EMBASE, along with supplementary searches for relevant congress abstracts. Only studies that discussed obesity prevalence in Saudi Arabia in relation to any gender or age group, the prevalence of ORCs in Saudi Arabia for any gender or age group, and/or the economic burden of obesity and how it impacts the healthcare system in Saudi Arabia, and were published in the English language, were selected for inclusion. No age or gender restrictions were imposed.

Results

The prevalence of obesity in Saudi Arabia ranged from 20% to 39% and up to 19.4% among adults and adolescents, respectively. The most reported ORCs were hypertension (67.6%), type 2 diabetes (60.7%), and hypercholesterolaemia (51.3%), and an association between obesity and ORCs was established, showing an increased risk with increasing body mass index. The economic burden of obesity across Saudi Arabia was estimated to be 6.4 billion US dollars (USD) for treatment and management.

Conclusion

Obesity affects a substantial proportion of the Saudi general population and is a significant burden on individuals, as demonstrated by the prevalence of ORCs. Multifaceted, short- and long-term approaches involving interventions that operate at multiple levels and target both individuals and communities are urgently needed; there is a particular need for a national strategy and a specific, systems-based policy. Further research will help increase awareness of obesity and its management, which will be crucial for transforming the healthcare system under Vision 2030.
导言沙特阿拉伯在过去三十年中肥胖症发病率呈上升趋势;肥胖症是非传染性疾病的重要风险因素,可能会造成医疗保健和经济负担。在这篇系统性综述中,我们旨在探讨沙特阿拉伯的肥胖患病率、肥胖相关并发症(ORCs)以及肥胖造成的经济负担。方法我们在 PubMed 和 EMBASE 中检索了 2012 年至 2022 年期间沙特阿拉伯当地的相关研究,并补充检索了相关的大会摘要。只有讨论沙特阿拉伯任何性别或年龄组的肥胖患病率、沙特阿拉伯任何性别或年龄组的ORC患病率、和/或肥胖的经济负担及其如何影响沙特阿拉伯的医疗保健系统,并以英语发表的研究才被选入。结果沙特阿拉伯成年人和青少年的肥胖患病率分别为 20% 至 39%,最高达 19.4%。报告最多的器官功能障碍是高血压(67.6%)、2 型糖尿病(60.7%)和高胆固醇血症(51.3%),肥胖与器官功能障碍之间存在关联,表明随着体重指数的增加,风险也会增加。据估计,沙特阿拉伯全国因肥胖症造成的治疗和管理经济负担达 64 亿美元。亟需采取多方面、短期和长期的方法,在多个层面开展针对个人和社区的干预活动;尤其需要制定国家战略和以系统为基础的具体政策。进一步的研究将有助于提高人们对肥胖症及其管理的认识,这对于根据《2030 年远景规划》转变医疗保健系统至关重要。
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引用次数: 0
Captagon: A comprehensive bibliometric analysis (1962–2024) of its global impact, health and mortality risks Captagon:对其全球影响、健康和死亡风险的综合文献计量分析(1962-2024 年
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-22 DOI: 10.1016/j.jsps.2024.102188
Captagon is a synthetic stimulant combining amphetamine and theophylline. Initially introduced in 1961 as a treatment for hyperactivity, depression, and narcolepsy, Captagon was later classified as a Schedule 1 controlled substance due to its addictive and hallucinogenic properties. Despite its global prohibition in 1986, the trade of counterfeit products is widespread, especially in south-east Europe and far-east Asia, with its production being on the rise in Middle Eastern regions. This paper presents a quantitative data-driven bibliometric analysis of the existing literature on Captagon up to July 2024. It aims to delineate the structure and development of knowledge surrounding the substance, including key contributing countries, authors, prominent sources, and recurring thematic keywords. The quantitative and data-driven results were then used to guide the narrative discussion on Captagon. Findings indicate that current research predominantly focuses on Captagon’s use and impact in conflict zones, often exploring its interaction with other substances used by civilians and militias. Results also show a growing trend in Captagon research, with Saudi Arabia, Jordan, and Iraq emerging as main contributors to the literature. Despite the attention in specific regions, a considerable gap remains in understanding the mechanisms of action of Captagon (particularly regarding its metabolism, toxicology, mortality risk), and in developing protocols for its discontinuation. Additionally, the drug’s inconsistent composition requires further analyses to better predict risks and establish effective management strategies. Addressing these gaps will be crucial for the development of novel interventions and policies to mitigate the adverse effects of Captagon and improve public health systems worldwide.
卡普他酮是一种结合了苯丙胺和茶碱的合成兴奋剂。Captagon 最初于 1961 年问世,用于治疗多动症、抑郁症和嗜睡症,后因其成瘾和致幻特性被列为附表 1 受控物质。尽管 Captagon 于 1986 年被全球禁用,但假冒产品的交易却非常普遍,尤其是在东南欧和远东亚洲,中东地区的生产量也在不断上升。本文对截至 2024 年 7 月有关 Captagon 的现有文献进行了定量数据驱动的文献计量分析。其目的是勾勒出围绕该物质的知识结构和发展,包括主要贡献国、作者、主要来源和重复出现的主题关键词。定量和数据驱动的结果随后被用于指导有关 Captagon 的叙述性讨论。研究结果表明,目前的研究主要侧重于 Captagon 在冲突地区的使用和影响,通常探讨其与平民和民兵使用的其他物质之间的相互作用。研究结果还显示出 Captagon 研究的增长趋势,沙特阿拉伯、约旦和伊拉克成为文献的主要贡献者。尽管特定地区的研究备受关注,但在了解 Captagon 的作用机制(特别是其代谢、毒理学、死亡风险)和制定停药方案方面仍存在相当大的差距。此外,还需要进一步分析该药物不一致的成分,以便更好地预测风险和制定有效的管理策略。缩小这些差距对于制定新型干预措施和政策以减轻 Captagon 的不良影响并改善全球公共卫生系统至关重要。
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引用次数: 0
Pharmacological investigations of newly synthesized oxazolones and imidazolones as COX-2 inhibitors 作为 COX-2 抑制剂的新合成噁唑酮和咪唑酮的药理研究
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-19 DOI: 10.1016/j.jsps.2024.102191
Oxazoles and Imidazoles are heterocyclic compounds with significant biological activities. The present study explores the pharmacological effects of some new oxazole and imidazole derivatives as potential COX-2 inhibitors. Docking studies of the compounds against targeted proteins COX-2 and TACE manifested good binding affinities for both the targets supporting their anti-inflammatory potential. Compounds (3F-A, 3F-B, N-A, N-B) were evaluated for in vivo anti-inflammatory effects by carrageenan-induced paw edema. Among all, compound N-A was found to be the most effective as it displayed most pronounced reduction in inflammation that was comparable to indomethacin. The in vivo tissue antioxidant activity was performed for estimation of the level of catalase, GSH, GST, and thiobarbituric acid in paw tissue. The results exhibited that targeted compounds improved the oxidative stress and restored the expression of enzymes. H &E staining revealed that aforesaid compounds displayed well-defined restoration of cellular damage. Compound NA exhibited maximum structural and functional preservation. Reduction in the expression of inflammatory markers was also analyzed by ELISA and maximum reduction in protein expression (COX-2 and TNF-a) was observed for compound N-B. Quantification of mRNA was done using PCR and a decrease in the expression of COX-2 mRNA level in treatment groups was depicted by all the new compounds but N-B showed maximum reduction in enzyme expression. All the results obtained from the present study have shown the significant anti-inflammatory potential of new compounds via the COX-2 inhibition pathway.
噁唑和咪唑是具有重要生物活性的杂环化合物。本研究探讨了一些新的噁唑和咪唑衍生物作为潜在 COX-2 抑制剂的药理作用。这些化合物与靶蛋白 COX-2 和 TACE 的对接研究表明,它们与这两个靶蛋白都有很好的结合亲和力,支持它们的抗炎潜力。通过卡拉胶诱导的爪水肿评估了化合物(3F-A、3F-B、N-A、N-B)的体内抗炎作用。结果发现,在所有化合物中,化合物 N-A 的消炎效果最明显,与吲哚美辛相当。体内组织抗氧化活性是通过评估爪组织中过氧化氢酶、谷胱甘肽、谷胱甘肽和硫代巴比妥酸的水平来实现的。结果显示,靶向化合物改善了氧化应激,恢复了酶的表达。Hamp;E 染色显示,上述化合物对细胞损伤有明确的修复作用。化合物 NA 表现出最大程度的结构和功能保护。还通过 ELISA 分析了炎症标志物表达的减少情况,发现化合物 N-B 蛋白表达(COX-2 和 TNF-a)的减少幅度最大。利用 PCR 对 mRNA 进行了定量分析,结果显示,所有新化合物都降低了处理组中 COX-2 mRNA 的表达水平,但 N-B 的酶表达降低幅度最大。本研究的所有结果都表明,新化合物通过 COX-2 抑制途径具有显著的抗炎潜力。
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引用次数: 0
Celebrating the 30th Anniversary of the Saudi Pharmaceutical Journal: A Special Issue 庆祝《沙特药学杂志》创刊 30 周年:特刊
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-17 DOI: 10.1016/j.jsps.2024.102190
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引用次数: 0
Prevalence of carbapenem-resistant Enterobacterales (CRE) in Saudi Arabia: A systematic review and meta-analysis 沙特阿拉伯耐碳青霉烯类肠杆菌(CRE)的流行情况:系统回顾和荟萃分析
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-14 DOI: 10.1016/j.jsps.2024.102186
Antimicrobial resistance is a significant public health issue. In addressing the threat of multidrug resistant bacterial infections, carbapenems have been used. The carbapenem-resistant Enterobacterales (CRE) are, however, rapidly expanding worldwide. Since the issue of CRE is also a problem in Saudi Arabia, the current meta-analysis was performed to comprehensively evaluate the resistance rates to the main carbapenem antibiotics and determine the actual prevalence of CRE in the country. Preferred Reporting Items for Systematic Reviews and Meta-analyses (PRISMA) guidelines was followed. Different web databases including PubMed, Scopus, Web of Science, and ScienceDirect were searched for relevant records. Data were extracted, and summary estimates for resistance to carbapenems were calculated using DerSimonian-Laird method of meta-analysis and the random-effects model. From a total of 787 retrieved records, 69 studies were found fully eligible and were included in the final analyses. More than 50 % of all the studies were conducted after 2010, and the most frequently examined members of the Enterobacterales were Escherichia coli and Klebsiella pneumoniae. The pooled prevalence estimate for imipenem resistance was 6.6 % (95 % CI: 4.7–9.2), 9.1 % (95 % CI: 6.7–12.3) for meropenem, and 18.6 % (95 % CI: 11.9–27.9) for ertapenem. High heterogeneity (I2 > 97 %, p < 0.001) was observed for all the estimates. Compared to other regions of the country, there was higher resistance rates in the Al-Qassim and Al-Jouf provinces. Additionally, resistance to ertapenem was as high as 34.2 % in the most recent study period (2021–2024). Proteus spp was the most prevalent CRE (26.2 %). This review highlights an increasing rate of carbapenem resistance among Enterobacterales, emphasizing the need for collaborative efforts to implement strict infection control and prevention measures. Consistent surveillance is indispensable for safeguarding public health, guiding clinical decisions, and strengthening efforts to tackle the challenges of antibiotic resistance.
抗菌药耐药性是一个重大的公共卫生问题。为应对耐多药细菌感染的威胁,人们一直在使用碳青霉烯类药物。然而,耐碳青霉烯类肠杆菌(CRE)正在全球迅速蔓延。由于 CRE 在沙特阿拉伯也是一个问题,因此本研究进行了荟萃分析,以全面评估主要碳青霉烯类抗生素的耐药率,并确定 CRE 在该国的实际流行率。研究遵循了《系统综述和荟萃分析首选报告项目》(Preferred Reporting Items for Systematic Reviews and Meta-analyses,PRISMA)指南。在不同的网络数据库(包括 PubMed、Scopus、Web of Science 和 ScienceDirect)中搜索相关记录。提取数据后,使用DerSimonian-Laird荟萃分析法和随机效应模型计算碳青霉烯类耐药性的汇总估计值。在检索到的总共 787 条记录中,有 69 项研究完全符合条件并被纳入最终分析。在所有研究中,50% 以上的研究是在 2010 年之后进行的,最常见的肠杆菌科细菌是大肠埃希菌和肺炎克雷伯菌。亚胺培南耐药性的汇总流行率估计值为 6.6%(95 % CI:4.7-9.2),美罗培南为 9.1%(95 % CI:6.7-12.3),厄他培南为 18.6%(95 % CI:11.9-27.9)。所有估计值均存在高度异质性(I2 > 97 %, p < 0.001)。与该国其他地区相比,卡西姆省和朱夫省的耐药率较高。此外,在最近的研究期间(2021-2024 年),对厄他培南的耐药性高达 34.2%。变形杆菌是最常见的 CRE(26.2%)。本综述强调了肠杆菌科细菌对碳青霉烯类耐药率的不断上升,强调需要共同努力实施严格的感染控制和预防措施。持续的监测对于保障公众健康、指导临床决策以及加强应对抗生素耐药性挑战的工作都是不可或缺的。
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引用次数: 0
Salubrious effects of proanthocyanidins on behavioral phenotypes and DNA repair deficiency in the BTBR mouse model of autism 原花青素对自闭症 BTBR 小鼠模型的行为表型和 DNA 修复缺陷的有益影响
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-13 DOI: 10.1016/j.jsps.2024.102187
Autism is a neurodevelopmental disorder distinguished by impaired social interaction and repetitive behaviors. Global estimates indicate that autism affects approximately 1.6% of children, with the condition progressively becoming more prevalent over time. Despite noteworthy progress in autism research, the condition remains untreatable. This serves as a driving force for scientists to explore new approaches to disease management. Autism is linked to elevated levels of oxidative stress and disturbances in the DNA repair mechanism, which may potentially play a role in its comorbidities development. The current investigation aimed to evaluate the beneficial effect of the naturally occurring flavonoid proanthocyanidins on the behavioral characteristics and repair efficacy of autistic BTBR mice. Moreover, the mechanisms responsible for these effects were clarified. The present findings indicate that repeated administration of proanthocyanidins effectively reduces altered behavior in BTBR animals without altering motor function. Proanthocyanidins decreased oxidative DNA strand breaks and accelerated the rate of DNA repair in autistic animals, as evaluated by the modified comet test. In addition, proanthocyanidins reduced the elevated oxidative stress and recovered the disrupted DNA repair mechanism in the autistic animals by decreasing the expressions of Gadd45a and Parp1 levels and enhancing the expressions of Ogg1, P53, and Xrcc1 genes. This indicates that proanthocyanidins have significant potential as a new therapeutic strategy for alleviating autistic features.
自闭症是一种神经发育障碍,主要表现为社交互动障碍和重复行为。据估计,全球约有 1.6% 的儿童患有自闭症,而且随着时间的推移,发病率会逐渐升高。尽管自闭症研究取得了显著进展,但这种疾病仍然无法治疗。这促使科学家们探索新的疾病治疗方法。自闭症与氧化应激水平升高和 DNA 修复机制紊乱有关,这可能是自闭症合并症发展的潜在因素。目前的研究旨在评估天然类黄酮原花青素对自闭症 BTBR 小鼠行为特征和修复功效的有益影响。此外,还阐明了产生这些影响的机制。目前的研究结果表明,反复服用原花青素可有效减少 BTBR 动物的行为改变,而不会改变其运动功能。根据改良彗星试验的评估,原花青素可减少自闭症动物的氧化 DNA 链断裂,加快 DNA 修复速度。此外,原花青素通过降低 Gadd45a 和 Parp1 的表达水平,提高 Ogg1、P53 和 Xrcc1 基因的表达水平,减少了自闭症动物体内升高的氧化应激,恢复了被破坏的 DNA 修复机制。这表明,原花青素作为一种新的治疗策略,在缓解自闭症特征方面具有巨大潜力。
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引用次数: 0
Identification of compounds from Origanum compactum and Origanum elongatum using HPLC/UV-ESI-MS and comparative analysis of their antioxidant, antimicrobial, anticoagulant, and antidiabetic properties 利用 HPLC/UV-ESI-MS 鉴定小叶牛至和长叶牛至中的化合物,并比较分析其抗氧化、抗菌、抗凝血和抗糖尿病特性
IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-10-02 DOI: 10.1016/j.jsps.2024.102184
<div><div>The aim was to assess the phytochemical composition, phenolic component levels, and biological properties of the flowering tops of <em>Origanum compactum</em> and <em>Origanum elongatum</em>. The study employed phytochemical assays, spectrophotometric techniques for quantitative analysis of polyphenols, flavonoids, and tannins, and compound identification using HPLC/UV-ESI-MS. The antimicrobial, antioxidant, anticoagulant, and antidiabetic properties were examined both <em>in vitro</em> and <em>in vivo</em>. The results showed that the <em>O. compactum</em> extract had significantly high levels of total polyphenols, measuring 47.368 mg gallic acid equivalents per gram, and flavonoids, measuring 14.839 mg quercetin equivalents per gram. The phytochemical examination of <em>O. compactum</em> revealed that lithospermic acid accounted for 36.82 % of the chemicals detected, followed by salvianolic acid C at 12.57 % and ros-marinic acid at 6.01 %. The main constituents of <em>O. elongatum</em> are salvianolic acid C (14.46 %), luteolin-3-O-glucuronide (13.51 %), salvianolic acid B (12.24 %), rosmarinic acid (7.83 %), and rutin (6.18 %). The results demonstrated different levels of effectiveness against the investigated microorganisms, with the extract from <em>O. compactum</em> exhibiting better activity, particularly against Gram-negative bacteria, certain yeasts, and the fungus Aspergillus niger. The aqueous extracts of both <em>Origanum</em> species demonstrate significant antioxidant activity. <em>O. compactum</em> has a higher total antioxidant capacity (IC<sub>50</sub> of 35.083 μg/mL) compared to <em>O. elongatum</em> (IC<sub>50</sub> of 77.080 μg/mL). However, <em>O. elongatum</em> has a higher reducing power (35.697 μg/mL) compared to <em>O. compactum</em> (42.563 μg/mL). <em>In vivo</em> evaluations revealed that the aqueous extracts of <em>O. compactum</em> and <em>O. elongatum</em> possess significant antihyperglycemic and anticoagulant properties. The extracts demonstrated a marked reduction in blood glucose levels during the oral glucose tolerance test (OGTT) in Wistar rats and effectively prolonged both prothrombin time (PT) and activated partial thromboplastin time (aPTT), highlighting their ability to inhibit coagulation pathways. Moreover, their comparable efficacy to standard antihyperglycemic medications and absence of severe toxicity, even at high doses, underscore their therapeutic potential for safe and effective treatment applications. Between the two species, <em>O. compactum</em> exhibited superior efficacy in key biological activities such as antioxidant, antimicrobial, and anticoagulant properties, making it a strong candidate for therapeutic applications. This study underscores the value of <em>Origanum</em> species as a rich source of bioactive compounds, offering significant potential in pharmaceuticals, nutraceuticals, and agri-food industries. The findings pave the way for further exploration of their diverse
目的是评估小叶牛至和长叶牛至的植物化学成分、酚类成分水平和生物特性。研究采用了植物化学测定法、分光光度法对多酚、类黄酮和单宁进行定量分析,并使用 HPLC/UV-ESI-MS 对化合物进行鉴定。此外,还对其抗菌、抗氧化、抗凝血和抗糖尿病特性进行了体外和体内检测。结果表明,O. compactum 提取物的总多酚含量很高,每克提取物中含有 47.368 毫克没食子酸当量,黄酮类化合物含量也很高,每克提取物中含有 14.839 毫克槲皮素当量。植物化学检查显示,在 O. compactum 检测到的化学物质中,石蒜酸占 36.82%,其次是丹酚酸 C(12.57%)和玫瑰橘酸(6.01%)。O. elongatum 的主要成分是丹酚酸 C(14.46 %)、木犀草素-3-O-葡萄糖醛酸苷(13.51 %)、丹酚酸 B(12.24 %)、迷迭香酸(7.83 %)和芦丁(6.18 %)。结果表明,O. compactum 的提取物对所研究的微生物具有不同程度的功效,尤其是对革兰氏阴性菌、某些酵母菌和黑曲霉菌具有更好的活性。两种牛至的水提取物都具有显著的抗氧化活性。与 O. elongatum(IC50 为 77.080 μg/mL)相比,O. compactum 的总抗氧化能力更高(IC50 为 35.083 μg/mL)。然而,与 O. compactum(42.563 μg/mL)相比,O. elongatum 的还原能力更高(35.697 μg/mL)。体内评估显示,O. compactum 和 O. elongatum 的水提取物具有显著的降血糖和抗凝特性。在对 Wistar 大鼠进行口服葡萄糖耐量试验(OGTT)时,这两种提取物能明显降低血糖水平,并能有效延长凝血酶原时间(PT)和活化部分凝血活酶时间(aPTT),突出了它们抑制凝血途径的能力。此外,它们的疗效与标准降糖药物相当,即使在高剂量下也没有严重毒性,这突出表明它们具有安全有效的治疗应用潜力。在这两个物种中,O. compactum 在抗氧化、抗菌和抗凝特性等关键生物活性方面表现出更高的功效,使其成为治疗应用的有力候选者。这项研究强调了牛至物种作为生物活性化合物丰富来源的价值,为制药、营养保健品和农业食品行业提供了巨大的潜力。研究结果为进一步探索牛至的多样化应用铺平了道路。
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Saudi Pharmaceutical Journal
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