Naunyn-Schmiedeberg's archives of pharmacology最新文献_第10页

Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity. 吡唑酰胺-查耳酮共轭物：合成与抗原生动物活性。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-10-21 DOI: 10.1007/s00210-024-03524-7

Devesh S Agarwal, Richard M Beteck, Dorien Mabille, Guy Caljon, Lesetja J Legoabe

引用次数: 0

Enhanced behavioral impact of optimized bupropion-encapsulated bilosomes over traditional niosomes treating depression. 优化后的安非他酮胶囊双糖体对抑郁症患者的行为影响优于传统的niosomes。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-10-30 DOI: 10.1007/s00210-024-03549-y

Karthick Harini, Koyeli Girigoswami, Mohammed Vajagathali, Debosreeta Bose, Anbazhagan Thirumalai, Venkatakrishnan Kiran, Pazhani Durgadevi, Agnishwar Girigoswami

{"title":"Enhanced behavioral impact of optimized bupropion-encapsulated bilosomes over traditional niosomes treating depression.","authors":"Karthick Harini, Koyeli Girigoswami, Mohammed Vajagathali, Debosreeta Bose, Anbazhagan Thirumalai, Venkatakrishnan Kiran, Pazhani Durgadevi, Agnishwar Girigoswami","doi":"10.1007/s00210-024-03549-y","DOIUrl":"10.1007/s00210-024-03549-y","url":null,"abstract":"Bupropion (Bpn), an FDA-approved NDRI (norepinephrine-dopamine reuptake inhibitor), poses risks of seizures and liver failure due to its stimulant properties, necessitating the development of alternative formulations. This research aims to develop a Bpn nanoformulation within bilosomal vesicles to enhance therapeutic efficacy at lower doses, using three bile salts, span 20 surfactants, and cholesterol via thin-film hydration. Optimization of bilosomal stability is achieved by trialing various ingredient concentrations, identifying a surfactant-to-cholesterol-to-bile salt ratio of 1.5:1:0.17 µM, with sodium cholate (B.SCF) yielding the most stable system. Bpn encapsulated in the optimized bilosomal vesicle (Bpn@B.SC F) demonstrated high encapsulation efficiency of 78.142 ± 11.07% and drug-retaining capacity compared to the niosomal system. The in vitro and in vivo toxicity profile of the product is superior to the niosomal system and shows negligible toxicity with a viability rate of not less than 95%, with a sustained release profile in artificial cerebrospinal fluid (ACSF). In vivo, behavioral analysis on zebrafish revealed that Bpn@B.SC F treatment more effectively improved depressive behavior compared to free Bpn and other treatments, evidenced by increased exploration rates and reduced irregular movements, as shown through statistical and trajectory data. Hence, it is concluded that the bilosomal structure, compared to the niosomal system, is a better carrier of drugs to achieve brain delivery and improve mood.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"4373-4392"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142546455","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Neuroprotective effect of chelidonic acid through oxidative stress reduction in paclitaxel-induced peripheral neuropathy in rats. 在紫杉醇诱导的大鼠周围神经病变中，诃子油酸通过减少氧化应激发挥神经保护作用。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-10-31 DOI: 10.1007/s00210-024-03550-5

Shraddha I Khairnar, Yogesh A Kulkarni, Kavita Singh

{"title":"Neuroprotective effect of chelidonic acid through oxidative stress reduction in paclitaxel-induced peripheral neuropathy in rats.","authors":"Shraddha I Khairnar, Yogesh A Kulkarni, Kavita Singh","doi":"10.1007/s00210-024-03550-5","DOIUrl":"10.1007/s00210-024-03550-5","url":null,"abstract":"The present study evaluated the effect of chelidonic acid on paclitaxel-induced neuropathy in male Wistar rats. Neuropathy was induced by administering paclitaxel (2 mg/kg, i.p.) on 0, 2, 4, and 6 days of the protocol. Chelidonic acid treatment (at doses of 10, 20, and 40 mg/kg orally, for 21 days) was initiated simultaneously with paclitaxel administration. After completion of the protocol, mechanical allodynia, hyperalgesia, and thermal hyperalgesia were measured. Additionally, nerve conduction velocity was assessed. The study investigated inflammatory cytokines, oxidative stress, and histological changes in the sciatic nerve. Furthermore, the Nrf2 was measured, and the protein expression of pAMPK and HIF-1α was assessed using western blotting. The results showed that chelidonic acid significantly normalized mechanical allodynia, hyperalgesia, and thermal hyperalgesia. It also led to a significant improvement in motor and sensory nerve conduction velocity and reduced oxidative stress compared with paclitaxel alone. Inflammatory markers such as TNF-alpha, IL-6, and IL-1β concentrations, as well as nitric oxide and C-reactive protein, were significantly decreased in the chelidonic acid-treated group. Histopathological examination revealed reduced neuronal damage, demyelination, and leukocyte infiltration with chelidonic acid treatment. Chelidonic acid treatment also resulted in a considerable rise in Nrf2 levels (p < 0.001) and increased protein expression of pAMPK in the sciatic nerve. Conversely, HIF-1α expression was significantly declined in the chelidonic acid treatment. Overall, the findings suggest that chelidonic acid treatment attenuates paclitaxel-induced neuropathic pain.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"4435-4447"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142558283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Characterisation of autophagy induction by the thiopurine drugs azathioprine, mercaptopurine and thioguanine in THP-1 macrophages. 硫嘌呤类药物硫唑嘌呤、巯基嘌呤和硫鸟嘌呤在 THP-1 巨噬细胞中诱导自噬的特征。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-11-01 DOI: 10.1007/s00210-024-03563-0

Connan D Masson, Fern Findlay-Greene, Filipa Henderson Sousa, Paul Henderson, Jennifer A Fraser, Peter G Barlow, Craig Stevens

{"title":"Characterisation of autophagy induction by the thiopurine drugs azathioprine, mercaptopurine and thioguanine in THP-1 macrophages.","authors":"Connan D Masson, Fern Findlay-Greene, Filipa Henderson Sousa, Paul Henderson, Jennifer A Fraser, Peter G Barlow, Craig Stevens","doi":"10.1007/s00210-024-03563-0","DOIUrl":"10.1007/s00210-024-03563-0","url":null,"abstract":"Activating autophagy may be therapeutically beneficial, and we have previously shown that azathioprine (AZA), an immunomodulatory drug, induces autophagy. Here, we evaluated the induction of autophagy by the thiopurines AZA, mercaptopurine (6-MP) and thioguanine (6-TG) in THP-1 macrophages and investigated the mechanism of action in the context of this cellular process. The cytotoxicity of thiopurines was evaluated using an LDH assay. Induction of endogenous LC3 by thiopurines was evaluated using immunostaining. To confirm autophagy activation by thiopurines, a GFP-RFP-LC3 reporter plasmid was used to monitor the maturation of autophagosomes to autolysosomes. Induction of apoptosis by thiopurines was evaluated using Annexin V/PI staining, and ER stress was assessed via RT‒PCR analysis of XBP1 splicing. To gain insight into the mechanism of action of thiopurines, mTORC1 activity and eIF2α-S51 phosphorylation were evaluated by immunoblotting. Thiopurines were not cytotoxic to cells and induced strong time- and concentration-dependent autophagy. Thiopurines activate autophagy with complete progression through the pathway. Induction of autophagy by thiopurines occurred independently of apoptosis and ER stress. Immunoblotting revealed that AZA inhibited mTORC1 activity, and AZA and 6-TG increased eIF2α-S51 phosphorylation. In contrast, 6-MP had a minor effect on either signalling pathway. Thiopurines are strong inducers of autophagy, and autophagy induction should be considered among the mechanisms responsible for patient response to thiopurines.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"4467-4478"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142562459","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A single-dose, randomized, crossover bioequivalence study of levamlodipine besilate tablets in healthy subjects. 健康受试者服用苯磺酸左旋氨氯地平片的单剂量随机交叉生物等效性研究

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-10-08 DOI: 10.1007/s00210-024-03513-w

Qiaohuan Deng, Debin Yang, Yang Cheng, Zhengzhi Liu, Yannan Zhou, Yanli Wang, Zhengjie Su, Haimiao Yang

{"title":"A single-dose, randomized, crossover bioequivalence study of levamlodipine besilate tablets in healthy subjects.","authors":"Qiaohuan Deng, Debin Yang, Yang Cheng, Zhengzhi Liu, Yannan Zhou, Yanli Wang, Zhengjie Su, Haimiao Yang","doi":"10.1007/s00210-024-03513-w","DOIUrl":"10.1007/s00210-024-03513-w","url":null,"abstract":"Levamlodipine, the levorotatory form of amlodipine racemate, has a blood pressure-lowering effect that is twice that of the racemate. The study aims to establish a foundation for the clinical application of the test drug by conducting a phase I clinical bioequivalence trial, comparing its bioequivalence and safety with the reference drug in healthy Chinese subjects. Recruiting 26 healthy subjects for separate bioequivalence trials in both fasting and fed conditions. The subjects will orally administer 2.5-mg test drug and 5-mg reference drug. A chiral method was used for bioanalytics and liquid chromatography-tandem mass spectrometry was employed to quantify the (S)-amlodipine concentrations at various time points after administration. In fasting condition, the geometric mean ratios (GMRs) for the primary pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ are 100.24%, 103.63%, and 103.24%, respectively. The 90% confidence intervals (CIs) fall within the range of 80-125%, satisfying the established bioequivalence criteria. Similarly, upon oral administration of the drugs in the fed condition, the GMRs for Cmax, AUC0-t, and AUC0-∞ are 96.48%, 99.90%, and 99.62%, respectively. The corresponding 90% CIs are within the limits of 80-125%, meeting the predefined bioequivalence standards. Furthermore, both drugs exhibited favorable safety profiles. The results show that the two drugs are bioequivalent in healthy Chinese subjects under both fasting and fed conditions. The two drugs both had similar PK parameters and good safety.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"3955-3964"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142391923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Molecular, cellular, and metabolic insights of cinnamon (Cinnamomum zeylanicum) advantages in diabetes and related complications: condiment or medication? 肉桂（Cinnamomum zeylanicum）在糖尿病及相关并发症中的分子、细胞和代谢优势：调味品还是药物？

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-11-26 DOI: 10.1007/s00210-024-03644-0

Anahita Sadat Beheshti, Mohammad Mahdi Qazvini, Mahsa Abeq, Ermia Abedi, Mohammad Saleh Fadaei, Mohammad Reza Fadaei, Vafa Baradaran Rahimi, Vahid Reza Askari

{"title":"Molecular, cellular, and metabolic insights of cinnamon (Cinnamomum zeylanicum) advantages in diabetes and related complications: condiment or medication?","authors":"Anahita Sadat Beheshti, Mohammad Mahdi Qazvini, Mahsa Abeq, Ermia Abedi, Mohammad Saleh Fadaei, Mohammad Reza Fadaei, Vafa Baradaran Rahimi, Vahid Reza Askari","doi":"10.1007/s00210-024-03644-0","DOIUrl":"10.1007/s00210-024-03644-0","url":null,"abstract":"Diabetes mellitus (DM) is a growing concern in public health, which affects about 10% of the population. There are several chronic complications due to DM, including kidney failure, blindness, amputations, myocardial infarction, and stroke. Cinnamon zeylanicum (C. verum, Ceylon cinnamon, or true cinnamon) has been shown to have desirable effects such as anti-obesity, anti-diabetic, anti-dyslipidemia, and anti-inflammatory effects in experimental studies. In this regard, Scopus, PubMed, and Google Scholar databases have been investigated with keywords of \"Cinnamon,\" \"Cinnamomum zeylanicum,\" \"diabetes mellitus,\" \"diabetes complication,\" \"hypoglycemic,\" \"anti-hyperglycemic,\" and \"anti-diabetic\" from incept to June 2024. This study aimed to review all pharmacological effects and molecular pathways of C. zeylanicum in DM and its complications in vitro, in vivo, and in clinical. Based on these studies, C. zeylanicum has good potential to design human studies for controlling and modifying DM and its related disorders.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"3513-3526"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142716274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Current mechanistic insights into Withaferin A: a promising potential adjuvant anticancer agent from Withania somnifera. Withaferin A：一种有潜力的辅助抗癌剂，来自Withania somnifera。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 Epub Date: 2024-11-30 DOI: 10.1007/s00210-024-03662-y

Muhammad Farrukh Nisar, Chunpeng Wan, Dietrich Büsselberg, Daniela Calina, Javad Sharifi-Rad

{"title":"Current mechanistic insights into Withaferin A: a promising potential adjuvant anticancer agent from Withania somnifera.","authors":"Muhammad Farrukh Nisar, Chunpeng Wan, Dietrich Büsselberg, Daniela Calina, Javad Sharifi-Rad","doi":"10.1007/s00210-024-03662-y","DOIUrl":"10.1007/s00210-024-03662-y","url":null,"abstract":"Cancer remains a global health challenge, with drug resistance and disease recurrence posing significant obstacles despite advances in immunotherapy and targeted treatments. This has driven interest in natural products as sources of novel anticancer agents. Withania somnifera (Ashwagandha), a well-regarded plant in Ayurvedic medicine, is noted for its various therapeutic properties, including anticancer effects. Among its bioactive compounds, Withaferin A (WFA), a steroidal lactone, has shown notable promise in reducing inflammation, angiogenesis, and tumor proliferation with minimal toxicity. This review examines the anticancer properties of WFA, with a focus on its mechanisms of action, therapeutic efficacy, and safety profile across various cancer types. A comprehensive literature review was conducted, compiling data from in vitro and in vivo studies that investigate WFA's impact on cancer hallmarks, including apoptosis induction, angiogenesis reduction, and metastasis inhibition. Key molecular interactions with NFκB, STAT, HSP90, estrogen receptors, p53, and TGFβ pathways are highlighted. Findings indicate that WFA exhibits significant anticancer activity by modulating critical signaling pathways and inducing apoptosis with minimal adverse effects. In preclinical models, WFA demonstrated therapeutic potential across multiple cancers, such as breast, colon, prostate, ovarian, lung, and brain cancers. WFA represents a promising candidate for future cancer therapies, particularly as a natural adjuvant that could enhance treatment efficacy with low toxicity. Further clinical trials are needed to explore WFA's full potential and confirm its safety in human oncology.","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"3573-3593"},"PeriodicalIF":3.1,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142770296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Targeting therapy of PI3K/AKT signaling pathway via non-coding RNAs in diabetic retinopathy. 通过非编码rna靶向治疗糖尿病视网膜病变的PI3K/AKT信号通路

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 DOI: 10.1007/s00210-025-04093-z

Shuai Lu, Jian Cai

引用次数: 0

Retraction Note: Development and evaluation of methotrexate-loaded nanoemulsion formulation for topical treatment of psoriasis. 注：甲氨蝶呤负载纳米乳剂制剂局部治疗银屑病的开发和评价。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 DOI: 10.1007/s00210-025-03968-5

Sheikh Abdur Rashid, Faiza Naseem, Pervaiz Akhtar Shah, Hamna Batool Hashmi, Mudassar Mazher, Mohammad S Mubarak, Javad Sharifi-Rad, Muhammad Badar

引用次数: 0

Retraction Note to: Betaine alleviates doxorubicin-related cardiotoxicity via suppressing oxidative stress and inflammation via the NLRP3/SIRT1 pathway. 撤回注：甜菜碱通过NLRP3/SIRT1途径抑制氧化应激和炎症，减轻阿霉素相关的心脏毒性。

IF 3.1 4区医学

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-04-01 DOI: 10.1007/s00210-025-04049-3

Yasaman Hamidavi Mohammadpour, Mohammad Javad Khodayar, Layasadat Khorsandi, Hadi Kalantar

引用次数: 0