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Prospective Utilization of Nanocarriers Loaded with Drug Combination for Treating Alzheimer's Disease. 纳米载体载药联合治疗阿尔茨海默病的前景研究。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-15 DOI: 10.2174/0113816128348877241202053633
Saif Ahmad Khan, Zufika Qamar, Aashish Rohilla, Pirthi Pal Singh, Suhel Parvez, Sanjula Baboota, Javed Ali

Alzheimer's disease (AD) is a debilitating condition that significantly affects the elderly. Early diagnosis is not only critical for improving patient outcomes but also directly influences the success of emerging therapeutic interventions. A therapeutic strategy targeting only one pathogenic mechanism is unlikely to be very effective, as there is increasing evidence that AD does not have a single pathogenic cause. Therefore, combining medications or developing therapies that address multiple pathways may be beneficial. Most clinical trials can be classified under added therapy rather than combination therapy. Effective treatment of AD likely requires targeting multiple mechanisms, such as amyloid-beta (Aβ) and tau pathology. However, many medications face challenges, including poor solubility, low permeability, and the inability to cross the blood- -brain barrier (BBB). This is where nanocarriers come into play, as they can be loaded with these medications to facilitate targeted drug delivery. This approach enhances the pharmacokinetic profile of drugs in both the blood and the brain. Therefore, this paper provides a concise overview of the use of various nanocarriers loaded with drug combinations for treating AD.

阿尔茨海默病(AD)是一种严重影响老年人的衰弱性疾病。早期诊断不仅对改善患者预后至关重要,而且还直接影响新兴治疗干预措施的成功。仅针对一种致病机制的治疗策略不太可能非常有效,因为越来越多的证据表明AD没有单一的致病原因。因此,联合用药或开发针对多种途径的疗法可能是有益的。大多数临床试验可以归类为附加治疗而不是联合治疗。AD的有效治疗可能需要针对多种机制,如淀粉样蛋白- β (Aβ)和tau病理。然而,许多药物面临挑战,包括溶解度差,渗透性低,无法穿过血脑屏障(BBB)。这就是纳米载体发挥作用的地方,因为它们可以装载这些药物,以促进靶向药物的递送。这种方法增强了药物在血液和大脑中的药代动力学特征。因此,本文简要概述了各种载药纳米载体在治疗AD中的应用。
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引用次数: 0
Cinacalcet Improves Erythropoietin Resistance in Patients with Secondary Hyperparathyroidism Receiving Dialysis Treatment. Cinacalcet改善透析治疗继发性甲状旁腺功能亢进患者的促红细胞生成素抵抗。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-14 DOI: 10.2174/0113816128321721241118171041
Wenjuan Weng, Yingjuan Li, Yongda Lin, Jiali Wang, Xiutian Chen, Tianbiao Zhou

Introduction: Chronic Kidney Disease (CKD) is recognized as a major global public health problem. Dialysis is the mainstay of treatment for patients with end-stage renal disease and can prolong survival in patients with CKD. As patient survival increases, the treatment of complications becomes more important. CKD-mineral and bone disorders (CKD-MBD) and renal anemia are common complications in patients with CKD. Cinacalcet is a calcimimetic for the treatment of Secondary Hyperparathyroidism (SHPT) in adult dialysis patients, which regulates the synthesis and secretion of parathyroid hormone by increasing the sensitivity of calcium-sensitive receptors. This retrospective study evaluated the efficacy of cinacalcet in dialysis patients.

Method: Forty-seven patients on dialysis with elevated parathyroid hormone were included. The selected patients have regular follow-up visits in our outpatient clinic and regular use of cinacalcet for no less than 6 months.

Result: During the 6-month efficacy evaluation phase, cinacalcet not only reduced the levels of the intact parathyroid hormone (iPTH, P ≤ 0.05), serum calcium (P ≤ 0.01), and Ca×P (P ≤ 0.05) but also reduced weekly erythropoietin dosage (P ≤ 0.01) and erythropoietin resistance index (ERI, P ≤ 0.05).

Conclusion: While controlling SHPT in patients with CKD, cinacalcet reduced EPO resistance and improved renal anemia. In conclusion, cinacalcet not only decreased the levels of the iPTH, serum calcium, and Ca×P but also reduced weekly EPO dosage and ERI levels. Controlling SHPT in patients with CKD, cinacalcet also reduced ERI and improved renal anemia.

慢性肾脏疾病(CKD)是公认的一个主要的全球公共卫生问题。透析是终末期肾病患者的主要治疗方法,可以延长CKD患者的生存期。随着患者存活率的提高,并发症的治疗变得更加重要。CKD-矿物质和骨骼疾病(CKD- mbd)和肾性贫血是CKD患者常见的并发症。Cinacalcet是一种治疗成人透析患者继发性甲状旁腺功能亢进症(SHPT)的拟钙化剂,通过增加钙敏感受体的敏感性来调节甲状旁腺激素的合成和分泌。本回顾性研究评估了cinacalcet在透析患者中的疗效。方法:对47例甲状旁腺激素升高的透析患者进行分析。入选患者在我院门诊定期随访,并定期使用cinacalcet,疗程不少于6个月。结果:在6个月疗效评价期,cinacalcet不仅降低了完整甲状旁腺激素(iPTH, P≤0.05)、血钙(P≤0.01)、Ca×P水平(P≤0.05),而且降低了周促红细胞生成素剂量(P≤0.01)和促红细胞生成素抵抗指数(ERI, P≤0.05)。结论:在控制CKD患者SHPT的同时,cinacalcet可降低EPO抵抗并改善肾性贫血。综上所述,cinacalcet不仅降低了iPTH、血清钙和Ca×P的水平,而且降低了EPO的周剂量和ERI水平。在CKD患者中控制SHPT, cinacalcet也降低ERI和改善肾性贫血。
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引用次数: 0
Effect of Fibrates on Lipoprotein-associated Phospholipase A2 Mass and Activity: A Systematic Review and Meta-analysis of Controlled Clinical Trials. 贝特类药物对脂蛋白相关磷脂酶A2质量和活性的影响:对照临床试验的系统回顾和荟萃分析
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-13 DOI: 10.2174/0113816128345231240925095400
Luis E Simental-Mendía, Mario Simental-Mendía, Claudia I Gamboa-Gómez, Tannaz Jamialahmadi, Amirhossein Sahebkar

Background: In vascular tissue, macrophages and inflammatory cells produce the enzyme lipoprotein- associated phospholipase A2 (Lp-PLA2). Treatment with fibrates decreases Lp-PLA2 levels in individuals with obesity and metabolic syndrome; however, these findings have not been fully clarified.

Objective: The goal of this study was to investigate the possible effects of fibrate therapy on Lp-PLA2 mass and activity through a meta-analysis of clinical trials.

Methods: Web of Science, PubMed, Scopus, Google Scholar, and ClinicalTrials.gov databases were searched using MeSH terms and keywords. Randomized controlled trials (RCT) evaluating the effect of statins on Lp- PLA2 mass and/or activity were included in the meta-analysis. Quantitative data were analyzed using a random- effects model and the generic inverse variance method.

Results: The meta-analysis of 10 clinical trials indicated that fibrate treatment has no significant effect on Lp- PLA2 mass (fibrate vs. placebo/nothing = WMD: -3.29 ng/ml, 95% CI: -21.35, 14.78, p = 0.72; fibrate vs. active control = WMD: -1.08 ng/ml, 95% CI: -51.38, 49.22, p = 0.97); Lp-PLA2 activity (fibrate vs. active control = WMD: 0.84 nmol/ml/min, 95% CI: -0.17, 1.84, p = 0.10); HDL-LpPLA2 activity (fibrate vs. active control = WMD: 0.77 nmol/ml/min, 95% CI: -0.33, 1.88, p = 0.17); and secretory PLA2 (fibrate vs. active control = WMD: 0.37 ng/ml, 95% CI: -1.22, 1.97, p = 0.65). Also, the results of the sensitivity analysis were robust for all these parameters.

Conclusion: In conclusion, fibrate therapy did not reduce the mass and activity of Lp-PLA2.

背景:在血管组织中,巨噬细胞和炎症细胞产生脂蛋白相关磷脂酶A2 (Lp-PLA2)。贝特类药物治疗可降低肥胖和代谢综合征患者的Lp-PLA2水平;然而,这些发现尚未得到充分澄清。目的:本研究的目的是通过临床试验的荟萃分析,探讨贝特治疗对Lp-PLA2质量和活性的可能影响。方法:使用MeSH术语和关键词检索Web of Science、PubMed、Scopus、谷歌Scholar和ClinicalTrials.gov数据库。meta分析纳入了评估他汀类药物对Lp- PLA2质量和/或活性影响的随机对照试验(RCT)。定量数据采用随机效应模型和通用逆方差法进行分析。结果:10项临床试验的荟萃分析显示,贝特治疗对Lp- PLA2质量无显著影响(贝特与安慰剂/无治疗= WMD: -3.29 ng/ml, 95% CI: -21.35, 14.78, p = 0.72;贝特与主动对照= WMD: -1.08 ng/ml, 95% CI: -51.38, 49.22, p = 0.97);Lp-PLA2活性(贝特与主动对照= WMD: 0.84 nmol/ml/min, 95% CI: -0.17, 1.84, p = 0.10);HDL-LpPLA2活性(纤维对照与主动对照= WMD: 0.77 nmol/ml/min, 95% CI: -0.33, 1.88, p = 0.17);分泌PLA2(贝特与主动对照= WMD: 0.37 ng/ml, 95% CI: -1.22, 1.97, p = 0.65)。此外,敏感性分析的结果对所有这些参数都是稳健的。结论:贝特治疗未降低Lp-PLA2的质量和活性。
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引用次数: 0
Exploration of Novel Therapeutic Targets for Breast Carcinoma and Molecular Docking Studies of Anticancer Compound Libraries with Cyclin-dependent Kinase 4/6 (CDK4/6): A Comprehensive Study of Signalling Pathways for Drug Repurposing. 乳腺癌新治疗靶点的探索以及抗癌化合物库与细胞周期蛋白依赖性激酶 4/6 (CDK4/6) 的分子对接研究:全面研究信号通路以实现药物再利用。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-13 DOI: 10.2174/0113816128346655241112104045
Asim Najmi

Aims: This study aims to identify and evaluate promising therapeutic proteins and compounds for breast cancer treatment through a comprehensive database search and molecular docking analysis.

Background: Breast cancer (BC), primarily originating from the terminal ductal-lobular unit of the breast, is the most prevalent form of cancer globally. In 2020, an estimated 2.3 million new cases were reported, resulting in approximately 685,000 deaths. Mutations in the BRCA1 and BRCA2 genes are well-established in hereditary breast cancer. The identification of effective therapeutic proteins for BC remains a complex and evolving area of research.

Objective: This study aims to identify and evaluate promising therapeutic proteins and compounds specific to breast cancer through a comprehensive database search and molecular docking analysis.

Methods: A rigorous search was conducted within the National Cancer Institute (NCI), NCI Metathesaurus, SIGnaling Network Open Resource (SIGNOR), Human Protein Atlas (HPA), and the Human Phenotype Ontology (HPO) to shortlist proteins linked to BC (CUI C0678222). Recent studies were reviewed to understand the administration of CDK4/6 inhibitors (palbociclib, ribociclib, abemaciclib) combined with endocrine therapy for HR-positive and HER2-negative breast cancer. Anticancer compound libraries available at ZINC and PubChem were analyzed. Compounds were evaluated based on their binding energies with CDK4 protein, a rationally selected druggable target.

Results: Key proteins linked to breast cancer were identified through database searches. Proliferation, apoptosis, and G1/S transition pathways were frequently found dysregulated in breast cancer. ZINC13152284 exhibited the strongest binding energy at -10.9 Kcal/mol, followed by ZINC05492794 with a binding energy of -10.4 Kcal/mol. Preexisting drugs showed lower binding energies with the CDK4 protein.

Conclusion: The study highlights the importance of drug repurposing as a strategy for the safe and effective treatment of breast cancer. Synthetic inhibitors often cause severe side effects, emphasizing the need for novel targets and compounds with better therapeutic profiles. Molecular docking identified promising compounds from the ZINC database, suggesting potential new avenues for breast cancer therapy.

目的:本研究旨在通过全面的数据库检索和分子对接分析,鉴定和评价有前景的乳腺癌治疗蛋白和化合物。背景:乳腺癌(BC),主要起源于乳腺末端导管小叶单位,是全球最常见的癌症形式。2020年,估计报告了230万例新病例,导致约68.5万人死亡。BRCA1和BRCA2基因突变在遗传性乳腺癌中是公认的。鉴别治疗BC的有效蛋白仍然是一个复杂和不断发展的研究领域。目的:本研究旨在通过全面的数据库检索和分子对接分析,鉴定和评价有前景的乳腺癌特异性治疗蛋白和化合物。方法:在美国国家癌症研究所(NCI)、NCI meta - thesaurus、信号网络开放资源(SIGNOR)、人类蛋白质图谱(HPA)和人类表型本体(HPO)中进行严格的搜索,以筛选与BC相关的蛋白质(CUI C0678222)。我们回顾了最近的研究,以了解CDK4/6抑制剂(palbociclib, ribociclib, abemaciclib)联合内分泌治疗hr阳性和her2阴性乳腺癌的管理。对ZINC和PubChem网站上现有的抗癌化合物文库进行了分析。化合物是根据其与CDK4蛋白的结合能来评估的,CDK4蛋白是一个合理选择的药物靶点。结果:通过数据库搜索确定了与乳腺癌相关的关键蛋白质。在乳腺癌中,细胞增殖、细胞凋亡和G1/S转化途径经常被发现失调。ZINC13152284的结合能最强,为-10.9 Kcal/mol, ZINC05492794次之,结合能为-10.4 Kcal/mol。先前存在的药物与CDK4蛋白的结合能较低。结论:该研究强调了药物再利用作为一种安全有效治疗乳腺癌的策略的重要性。合成抑制剂通常会引起严重的副作用,因此需要新的靶点和具有更好治疗效果的化合物。分子对接从锌数据库中发现了有希望的化合物,为乳腺癌治疗提供了潜在的新途径。
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引用次数: 0
Use of SGLT2 Inhibitors in Frail Older Adults is Associated with Increased Survival: A Retrospective Study. 一项回顾性研究:在虚弱的老年人中使用SGLT2抑制剂与增加生存率相关
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-13 DOI: 10.2174/0113816128347041241129055001
Francesco Saverio Ragusa, Nicola Veronese, Stefano Ciriminna, Diletta Agnello, Rosella Capitummino, Chiara Cavaleri, Alessandro D'Aleo, Chiara Maria Errera, Maria Chiara Garlisi, Chiara Giannettino, Alessandra Lo Nigro, Sofia Elena Montana Lampo, Ottavia Giovanna Plano, Gerlando Speziale, Pascal Roberto Titone, Mario Barbagallo, Ligia J Dominguez

Background: In recent years, sodium-glucose co-transporter 2 inhibitors (SGLT2i) have emerged as a valuable treatment for type 2 diabetes (T2D) and heart failure. Despite these medications seeming to be safe in older people, the literature about SGLT2i and frailty is still limited. This study aims to evaluate whether SGLT2i use is associated with increased survival in older adults and if frailty can affect the findings.

Material and methods: We enrolled over 65 patients admitted to the Geriatrics Wards at the University Hospital 'P. Giaccone' in Palermo, Italy, between December 2022 and May 2023. After 12 months of follow-up, various outcomes were assessed, including mortality, hospitalization, glycemic dysregulation, urinary tract infections, and falls. The association between SGLT2i use and mortality was analyzed and reported as hazard ratios (HRs) with their 95% confidence intervals (CIs).

Results: A total of 80 patients were included in the study (mean age 79.5 ± 8.5 years; 50% were women). Patients using SGLT2i had a higher prevalence of T2D (p = 0.02) and cirrhosis (p = 0.001). After adjusting for potential confounders, SGLT2i use was significantly associated with a reduced mortality risk (HR = 0.53; 95% CI: 0.20-0.93; p = 0.02). When stratified by the presence of multidimensional frailty, SGLT2i use was significantly associated with a lower risk of mortality in frail patients (HR = 0.27; 95% CI: 0.06-0.88; p = 0.008), but not in robust ones.

Conclusion: In older frail patients, the use of SGLT2i is associated with reduced mortality after 12 months of follow-up. Further larger studies are needed to evaluate the role of these medications in older adults.

背景:近年来,钠-葡萄糖共转运蛋白2抑制剂(SGLT2i)已成为治疗2型糖尿病(T2D)和心力衰竭的一种有价值的药物。尽管这些药物对老年人似乎是安全的,但关于SGLT2i和虚弱的文献仍然有限。本研究旨在评估SGLT2i的使用是否与老年人的生存率增加有关,以及虚弱是否会影响研究结果。材料和方法:我们在2022年12月至2023年5月期间招募了意大利巴勒莫大学医院P. Giaccone老年病房收治的65名以上患者。随访12个月后,评估各种结果,包括死亡率、住院率、血糖失调、尿路感染和跌倒。分析SGLT2i使用与死亡率之间的关系,并以风险比(hr)及其95%置信区间(ci)报告。结果:共纳入80例患者(平均年龄79.5±8.5岁;50%是女性)。使用SGLT2i的患者有更高的T2D患病率(p = 0.02)和肝硬化患病率(p = 0.001)。在对潜在混杂因素进行校正后,SGLT2i的使用与降低死亡风险显著相关(HR = 0.53;95% ci: 0.20-0.93;P = 0.02)。当根据多维虚弱的存在分层时,SGLT2i的使用与虚弱患者较低的死亡风险显著相关(HR = 0.27;95% ci: 0.06-0.88;P = 0.008)。结论:在老年体弱患者中,使用SGLT2i与随访12个月后死亡率降低相关。需要进一步的大规模研究来评估这些药物在老年人中的作用。
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引用次数: 0
Oral Administration of Hydrogen-rich Water: Biomedical Activities, Potential Mechanisms, and Clinical Applications. 口服富氢水:生物医学活性、潜在机制和临床应用。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-10 DOI: 10.2174/0113816128330516241121150719
Fanxianzi Meng, Zhichao Liu, Shucun Qin, Boyan Liu

Molecular hydrogen (H2) is considered a biological antioxidant. Hydrogen-rich Water (HRW) is regular water that contains dissolved H2 and has become more widely used in recent years. This review summarizes the basic research and clinical applications of HRW consumption to support its use for daily health and clinical treatment. The biological effects of HRW include reducing oxidative stress, exerting antiinflammatory effects, regulating glucose and lipid metabolism, protecting mitochondrial function, and regulating apoptosis. Hypotheses about the mechanisms of H2 include the direct scavenging of toxic free radicals, the Fe-porphyrin biosensor hypothesis, the effect of H2 on biological enzymes, the lipoprotein regulation of H2, and H2 acting on the intestinal barrier. Clinically, HRW has been used for adjuvant treatment, disease prevention, and quality of life improvement. In the future, more in-depth studies and large-scale clinical trials are needed.

分子氢(H2)被认为是一种生物抗氧化剂。富氢水(HRW)是一种含有溶解H2的普通水,近年来得到了越来越广泛的应用。本文综述了HRW消费的基础研究和临床应用,以支持其在日常健康和临床治疗中的应用。HRW的生物学作用包括降低氧化应激,发挥抗炎作用,调节糖脂代谢,保护线粒体功能,调节细胞凋亡。关于H2作用机制的假说包括:直接清除有毒自由基假说、铁卟啉生物传感器假说、H2对生物酶的影响假说、H2对脂蛋白的调节假说、H2对肠道屏障的作用假说。在临床上,HRW已被用于辅助治疗、疾病预防和生活质量的改善。未来还需要更深入的研究和大规模的临床试验。
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引用次数: 0
A Comparative Review on the Production of Factor VIII in Human and Non-human Hosts. 人与非人宿主体内因子VIII产生的比较研究。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-10 DOI: 10.2174/0113816128327353241121050134
Amirhossein Ghaemi, Hamid Moghimi, Mohammad-Hossein Sarrafzadeh

Hemophilia A (HA) is an inherited condition that is characterized by a lack of coagulation factor VIII (FVIII), which is needed for blood clotting. To produce recombinant factor VIII (rFVIII) for treatment, innovative methods are required. This study presents a thorough examination of the genetic engineering and biotechnological methods that are essential for the production of this complex process. Multiple host cells, such as animal, microbial, and human cell lines, are examined. Cultivating genetically modified cells enables the production of rFVIII, with further changes after protein synthesis, such as glycosylation, taking place in eukaryotic cells to guarantee correct folding. The extraction and purification of rFVIII require advanced methods, including affinity chromatography, to improve the purity of the protein. The purified protein undergoes rigorous quality control, which includes Sodium dodecyl-sulfate polyacrylamide gel electrophoresis (SDSPAGE) analysis, to assess its identity, purity, and functioning. The scalability of this approach allows for the synthesis of significant amounts of rFVIII for therapeutic purposes. Optimization strategies include modifying B-domain-deleted (BDD) FVIII, including introns in FVIII complementary DNA (cDNA) sequences to boost synthesis and storage, and making changes to chaperone-binding areas to optimize protein release. Furthermore, the search for a modified form of FVIII that has a longer duration of action in the body shows potential for enhancing the effectiveness of synthetic FVIII and progressing the treatment of hemophilia A. Future research should focus on improving the treatment of hemophilia A by developing a variant of FVIII that has increased stability and reduced immunogenicity.

血友病A (HA)是一种遗传性疾病,其特征是缺乏凝血因子VIII (FVIII),这是凝血所需要的。为了生产用于治疗的重组因子VIII (rFVIII),需要创新的方法。这项研究提出了基因工程和生物技术的方法,是必要的生产这一复杂过程的彻底检查。多种宿主细胞,如动物、微生物和人类细胞系,被检查。培养转基因细胞能够产生rFVIII,真核细胞在蛋白质合成后发生糖基化等进一步变化,以保证正确折叠。rFVIII的提取和纯化需要先进的方法,包括亲和层析,以提高蛋白质的纯度。纯化蛋白经过严格的质量控制,包括十二烷基硫酸钠聚丙烯酰胺凝胶电泳(SDSPAGE)分析,以评估其特性、纯度和功能。该方法的可扩展性允许合成用于治疗目的的大量rFVIII。优化策略包括修改b结构域缺失(BDD) FVIII,包括FVIII互补DNA (cDNA)序列中的内含子以促进合成和储存,以及改变伴侣结合区以优化蛋白质释放。此外,寻找在体内具有更长的作用持续时间的FVIII的修饰形式显示出增强合成FVIII的有效性和推进血友病a治疗的潜力。未来的研究应侧重于通过开发具有更高稳定性和降低免疫原性的FVIII变体来改善血友病a的治疗。
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引用次数: 0
Utilizing Plant Phytoconstituents in Metal Oxide Nanoparticle Synthesis for Cancer Therapies. 利用植物成分合成金属氧化物纳米颗粒用于癌症治疗。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-07 DOI: 10.2174/0113816128329342241120105041
Swati Dubey, Tarun Virmani, Shiv Kumar Yadav, Girish Kumar, Ashwani Sharma, Dalapathi Gugulothu

Background: The metal oxide nanoparticles possess unique properties such as biological compatibility, superior reactivity, and capacity to develop reactive oxygen species, due to this they have drawn significant interest in cancer treatment. The various MONPs such as cerium oxide, Copper oxide, Iron oxide, Titanium dioxide, and Zinc oxide have been investigated for several types of cancers including brain, breast, cervical, colon, leukemia, liver, lung, melanoma, ovarian, and prostate cancers. However, traditional physiochemical synthetic methods for MONPs commonly include toxic materials, a major concern that raises questions regarding their biocompatibility and safety.

Objective: This study aims to investigate the role of plant phytoconstituents in the development of MONPs via green synthesis and explore the therapeutic effectiveness of MONPs in treating several types of cancer. Primarily, it examines the potential of plant phytoconstituents (phenolic compounds, flavonoids, glycosides, alkaloids, etc.) in the development of MONPs as well as their improved ability to target numerous types of cancer.

Methods: A systemic search was conducted on recent literature, focusing on developing green MONPs by utilizing plants' phytoconstituents (plant extracts). The study of plant phytochemicals (present in different parts of a plant such as leaves, flowers, stems, peels, and roots) and their role in the synthesis of green metal oxide nanoparticles as well as their anticancer activity against several types of cancers was analyzed. Also focusing on their anticancer mechanism that involves ROS production, generates oxidative stress, and apoptosis leads to cancer inhibition.

Results: Phytochemicals-mediated metal oxide nanoparticle synthesis revealed many advantages such as improved biological compatibility and enhanced sensitivity towards cancer cells. Phytochemicals present in plant extracts act as natural capping, reducing, and stabilizing agents, enhancing nanoparticle synthesis which leads to synergistic anticancer activity. Additionally, the natural antioxidant and anticancer activity of various phytochemicals enhances the therapeutic potential of metal oxide nanoparticles, producing them more effective against ROS-generated apoptosis and showing negligible toxicity towards normal cells.

Conclusion: The utilization of plant phytochemicals in metal oxide nanoparticle production presents a safe, eco-friendly, sustainable, and effective approach to developing effective and safer cancer nanomedicines. Green synthesis not only increases anticancer activity but also decreases the biocompatibility problems associated with the physiochemical synthetic approach. Further research needs to concentrate on improving this synergy to create a targeted phytochemical-based metal oxide nanoparticle for cancer therapeutics.

背景:金属氧化物纳米颗粒具有独特的性质,如生物相容性、优越的反应性和产生活性氧的能力,因此它们在癌症治疗中引起了极大的兴趣。各种MONPs,如氧化铈、氧化铜、氧化铁、二氧化钛和氧化锌,已经被研究用于几种类型的癌症,包括脑癌、乳腺癌、宫颈癌、结肠癌、白血病、肝癌、肺癌、黑色素瘤、卵巢癌和前列腺癌。然而,传统的单克隆肽的物理化学合成方法通常含有有毒物质,这引起了人们对其生物相容性和安全性的质疑。目的:本研究旨在通过绿色合成探讨植物成分在MONPs发育中的作用,并探讨MONPs治疗几种类型癌症的疗效。主要研究了植物成分(酚类化合物、类黄酮、苷类、生物碱等)在monp发展中的潜力,以及它们针对多种癌症的改进能力。方法:系统检索近年来的文献,重点研究利用植物成分(植物提取物)开发绿色MONPs。植物化学物质(存在于植物的不同部分,如叶、花、茎、皮和根)及其在绿色金属氧化物纳米粒子合成中的作用以及它们对几种癌症的抗癌活性的研究进行了分析。同时关注它们的抗癌机制,包括ROS的产生、氧化应激和细胞凋亡导致的癌症抑制。结果:植物化学物质介导的金属氧化物纳米颗粒合成具有改善生物相容性和增强对癌细胞敏感性等优点。存在于植物提取物中的植物化学物质作为天然的覆盖、还原和稳定剂,增强纳米颗粒的合成,从而产生协同抗癌活性。此外,各种植物化学物质的天然抗氧化和抗癌活性增强了金属氧化物纳米颗粒的治疗潜力,使它们更有效地对抗ros引起的细胞凋亡,对正常细胞的毒性可以忽略不计。结论:利用植物化学物质生产金属氧化物纳米颗粒是开发有效、安全的抗癌纳米药物的一条安全、环保、可持续、有效的途径。绿色合成不仅增加了抗癌活性,而且减少了与物理化学合成方法相关的生物相容性问题。进一步的研究需要集中在改善这种协同作用上,以创造一种靶向植物化学的金属氧化物纳米颗粒,用于癌症治疗。
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引用次数: 0
Therapeutic Role of Scutellarein in Neurological Disorders. 黄芩苷在神经系统疾病中的治疗作用。
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-07 DOI: 10.2174/0113816128336901241125092132
Rohit Kumar, Sucharitha Bai, Rahul Shukla, Saba Naqvi

Scutellarein, a flavone found in the perennial herb Scutellaria baicalensis, has a wide range of pharmacological actions, such as antioxidant, anti-inflammatory, and neuroprotective. Increasing evidence has emphasized the developing significance of scutellarein in several neurological illnesses, such as Alzheimer's and Parkinson's disease, cerebral ischemia, and neuroblastoma. This review is centered on the molecular processes that underlie the neuroprotective properties of scutellarein in various neurological disorders, as indicated by recent pre-clinical research. Furthermore, it critically examines the potential challenges and advantages of scutellarein inclusion within the range of treatments for neurological disorders.

黄芩苷是一种在多年生草本植物黄芩中发现的黄酮,具有抗氧化、抗炎、神经保护等广泛的药理作用。越来越多的证据强调黄芩苷在几种神经系统疾病中的发展意义,如阿尔茨海默病和帕金森病,脑缺血和神经母细胞瘤。本文综述了最近的临床前研究表明,黄芩苷在各种神经系统疾病中具有神经保护作用的分子过程。此外,它批判性地研究了在神经系统疾病治疗范围内纳入黄芩的潜在挑战和优势。
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引用次数: 0
BACE-1 and ADAM-10 as Potential Peripheral Biomarkers for Alzheimer's Disease. BACE-1和ADAM-10作为阿尔茨海默病的潜在外周生物标志物
IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-07 DOI: 10.2174/0113816128339561241120135914
Carlo Cervellati, Alessandro Trentini, Marco Zuin, Gianmarco Mola, Raffaella Riccetti, Cristina Manfrinato, Domenico Sergi, Gerhard Multhaup, Giovanni Zuliani

Amyloid beta (Aβ) dyshomeostasis is considered the main biological aberration in Alzheimer's Disease (AD) pathology. The interplay between Aβ formation and clearance is predominantly modulated by a disintegrin and a metalloproteinase 10 (ADAM10, α-secretase) and β-site APP Cleaving Enzyme 1 (BACE1), the two pivotal enzymes in both non-amyloidogenic/amyloidogenic and amyloidolytic pathways. Emerging evidence suggests that aberrations in ADAM10 and BACE1 expression, activity, and function in the brain of AD patients also manifest in peripheral fluids, suggesting their potential as blood-based biomarkers for AD diagnosis. This review provides a comprehensive overview of the literature by exploring the roles of ADAM10 and BACE1 in AD, spanning from their involvement as pathological AD drivers to their potential utility as promising biomarkers.

淀粉样蛋白(Aβ)失衡被认为是阿尔茨海默病(AD)病理中的主要生物学畸变。a β形成和清除之间的相互作用主要由崩解素和金属蛋白酶10 (ADAM10, α-分泌酶)以及β位点APP切割酶1 (BACE1)调节,这两种酶在非淀粉样蛋白生成/淀粉样蛋白生成和淀粉样蛋白分解途径中都起关键作用。新出现的证据表明,AD患者大脑中ADAM10和BACE1的表达、活性和功能的畸变也表现在外周液体中,这表明它们有可能作为AD诊断的血液生物标志物。本综述通过探讨ADAM10和BACE1在AD中的作用,从它们作为病理性AD驱动因素的参与到它们作为有前景的生物标志物的潜在效用,对文献进行了全面的综述。
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引用次数: 0
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Current pharmaceutical design
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