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Preparation of astaxanthin/zeaxanthin-loaded nanostructured lipid carriers for enhanced bioavailability: Characterization-, stability-and permeability study Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Kristina Radić, Ana Isabel Barbosa, Salette Reis, Marijan Marijan, Sofia Antunes Costa Lima, Dubravka Vitali Čepo
Astaxanthin (ASTA) and zeaxanthin (ZEA) are xanthophyll carotenoids showing a wide spectrum of health-promoting properties. However, their utilization is limited, mostly due to poor water solubility, limited bioavailability, and a tendency to oxidate, as well as photo- and thermal instability. The aim of this work was to develop ASTA- and ZEA-loaded nano-structured lipid carriers (NLCs) that would
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Effects of epidurally administered dexmedetomidine and dexamethasone on postoperative pain, analgesic requirements, inflammation, and oxidative stress in thoracic surgery Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Jasminka Peršec, Andrej Šribar, Monika Ilić, Ivan Mamić, Domagoj Kifer, Ana-Marija Domijan, Željan Maleš, Petra Turčić
The aim of this study was to compare the effects of dexmedetomidine and dexamethasone as adjuvants to preoperative epidural administration of local anesthetic (ropivacaine) in thoracic surgery on the postoperative level of pain, use of analgesics, inflammation, and oxidative stress. The study enrolled 42 patients who underwent elective thoracic surgery in a one-year period at the University Hospital
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Oleuropein in olive leaf, branch, and stem extracts: stability and biological activity in human cervical carcinoma and melanoma cells Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Đani Benčić, Monika Barbarić, Ana Mornar, Daniela Amidžić Klarić, Anamaria Brozovic, Sanja Dabelić, Mihaela Fadljević, Ana Karković Marković
Olive leaves as a main byproduct of olive oil and fruit industry are a valuable source of phytochemicals such as polyphenols, with multiple biomedical effects. Apart from leaves, olive branches and stems make up a significant amount of olive waste. It is well known that the drying process and long-term storage affect the stability and concentration of polyphenols present in raw materials. For that
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Exploring adherence in patients with advanced breast cancer: focus on CDK4/6 inhibitors Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Matea Baković, Martina Bago, Lucija Benić, Magdalena Krajinović, Tajana Silovski, Natalija Dedić Plavetić, Lu Turković, Miranda Sertić, Maja Ortner Hadžiabdić
Treatment adherence is crucial for optimal outcomes in advanced breast cancer, but can be challenging due to various factors, i.e. patients’ attitudes and behavior upon diagnosis, and complex therapies with high adverse effect rates. Our aim was to explore the adherence to oral anticancer medications (OAM) in women with advanced breast cancer, focusing on cyclin-dependent kinase 4 and 6 inhibitors
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The impact of cryoprotectant exposure time on post-thaw viability of autologous and allogeneic hematopoietic stem cells and leukocyte subpopulations Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Vladimira Rimac, Ines Bojanić, Sanja Dabelić, Branka Golubić Ćepulić
Although the use of cryoprotectant dimethyl sulfoxide (DMSO) is the gold standard in cryopreservation of hematopoietic stem cells, it is well known that it has a negative effect on cell viability. The aim of this prospective study was to examine how the length of post-thaw exposure to DMSO affects the cell viability and stability of peripheral blood stem cell (PBSC) samples. Additionally, the effects
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Azithromycin-loaded liposomal hydrogel: a step forward for enhanced treatment of MRSA-related skin infections Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Zora Rukavina, May Wenche Jøraholmen, Dunja Božić, Ivana Frankol, Petra Golja Gašparović, Nataša Škalko-Basnet, Maja Šegvić Klarić, Željka Vanić
Azithromycin (AZT) encapsulated into various types of liposomes (AZT-liposomes) displayed pronounced in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA) (1). The present study represents a follow-up to this previous work, attempting to further explore the anti-MRSA potential of AZT-liposomes when incorporated into chitosan hydrogel (CHG). Incorporation of AZT-liposomes into
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Beliefs about medicines’ association with endocrine therapy adherence in early breast cancer survivors in Croatia Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Ana Dugonjić Okroša, Tajana Silovski, Natalija Dedić Plavetić, Hrvoje Silovski, Ana Kovačić, Iva Mucalo
This observational, cross-sectional study conducted at the University Hospital Centre Zagreb (UHC Zagreb) aimed to explore patients’ beliefs about adjuvant endocrine therapy (AET) as well as their association with non-adherence and sociodemographic and clinical factors. Out of 420 early breast cancer (BC) patients included in the study, 79.5 % perceived AET necessary and important for their health
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Mendeleev’s discovery of the periodic table and the first European Academy of Sciences to honour him Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Vanja Horvat Flegar, Suzana Inić
The chemical science community will commemorate the 155th anniversary of Mendeleev’s groundbreaking discovery of the periodic table of elements in 2024. This paper aims to underscore the significance of Mendeleev’s honorary membership in the Academy of Sciences in Zagreb, Croatia, which occurred in 1882, making it the first scientific academy in Europe to extend this recognition. Additionally, we seek
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Prescribers’ approval rate of pharmacist-initiated interventions to optimise patients’ clinical status of hypertension in the ambulatory care setting Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Andrea Brajković, Lucija Ana Bićanić, Helena Orehovački, Ingrid Prkačin, Djenane Ramalho De Oliveira, Iva Mucalo
This perspective, pre- and post-intervention study with a one-year follow-up primarily aimed to ascertain prescribers’ approval rate of pharmacists’ interventions and clinical status of hypertension following comprehensive medication management (CMM) intervention in the ambulatory care clinic. Between January 2018 and January 2022 overall 100 patients with hypertension and other comorbidities were
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Functionalization of selenium nanoparticles with olive polyphenols – impact on toxicity and antioxidative activity Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Emerik Galić, Kristina Radić, Nikolina Golub, Jakov Mlinar, Dubravka Vitali Čepo, Tomislav Vinković
Selenium nanoparticles (SeNPs) represent novel selenium (Se) formulation characterized by improved biocompatibility and a wider therapeutic range in comparison to inorganic Se. The aim of this work was to investigate the possibilities of functionalization of SeNPs with olive pomace extract (OPE), rich in health-promoting polyphenols, and to obtain innovative forms of nutraceuticals. Cytotoxic and antioxidative
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Size exclusion chromatography as green support for forced degradation study of adalimumab Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Jelena Kovačić, Daniela Amidžić Klarić, Nikša Turk, Ana Mornar
Size exclusion chromatography (SEC) has become a powerful tool for analysing size variants of biologic drugs in their native form. Modern SEC can be defined by the use of chromatographic columns packed with sub-3 µm particles, allowing an increase in method throughput compared to that of conventional SEC. We performed the forced degradation study of adalimumab, the first genetically engineered fully
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Synthesis, antiproliferative and antiplasmodial evaluation of new chloroquine and mefloquine-based harmiquins Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Kristina Pavić, Goran Poje, Lais Pessanha De Carvalho, Jana Held, Zrinka Rajić
Here we present the synthesis and evaluation of the biological activity of new hybrid compounds, ureido-type (UT) harmiquins, based on chloroquine (CQ) or mefloquine (MQ) scaffolds and β-carboline alkaloid harmine against cancer cell lines and Plasmodium falciparum. The hybrids were prepared from the corresponding amines by 1,1′-carbonyldiimidazole (CDI)-mediated synthesis. In vitro evaluation of the
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Simultaneous determination of macrolides in water samples by solid-phase extraction and capillary electrophoresis Acta Pharm. (IF 2.8) Pub Date : 2023-12-26 Dragana Mutavdžić Pavlović, Sandra Babić, Mirta Čizmić, Miranda Sertić, Tea Pinušić
Solid-phase extraction (SPE) coupled with capillary electrophoresis (CE) for the determination of macrolide antibiotics (azithromycin, clarithromycin, roxithromycin, tylosin) and tiamulin in water samples was described in this article. These compounds were extracted with different types of sorbents ( Oasis HLB, C18, C8, SDB, and Strata-X) and different masses of sorbents (60 mg, 200 mg, and 500 mg)
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A novel 4-(1,3,4-thiadiazole-2-ylthio)pyrimidine derivative inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Weiwei Li, Zhifu Yang, Likun Ding, Ying Wang, Xian Zhao, Jian Jie Chu, Qing Ji, Minna Yao, Jingwen Wang
Colorectal cancer (CRC) is one of the most common types of malignant cancers worldwide. Although molecularly targeted therapies have significantly improved treatment outcomes, most of these target inhibitors are resistant. Novel inhibitors as potential anticancer drug candidates are still needed to be discovered. Therefore, in the present study, we synthesized a novel 4-(1,3,4-thiadiazole-2-ylthio)pyrimidine
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Xanthoxyletin blocks the RANK/RANKL signaling pathway to suppress the growth of human pancreatic cancer cells Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Xin Zhang, Luming Li, Yan Wu
Xanthoxyletin is a vital plant-derived bioactive coumarin. It has been shown to exhibit anticancer effects against different human cancers. Nonetheless, the anticancer effects of xanthoxyletin against human pancreatic cancer cells have not been evaluated. Against this backdrop, the present study was designed to evaluate the anticancer effects of xanthoxyletin in human pancreatic cancer cells and to
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Design and synthesis of amino-substituted N-arylpiperidinyl-based inhibitors of the (immuno)proteasome Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Martina Gobec, Aleš Obreza, Marko Jukič, Ana Baumgartner, Nja Mihelčič, Špela Potočnik, Julija Virant, Irena Mlinarič, Raščan Stanislav, Gobec Izidor Sosič
The constitutive proteasome and the immunoproteasome represent validated targets for pharmacological intervention in the context of various diseases, such as cancer, inflammation, and autoimmune diseases. The development of novel chemical scaffolds of non-peptidic nature, capable of inhibiting different catalytically active subunits of both isoforms, is a viable approach against these diseases. Such
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Scoulerine promotes cytotoxicity and attenuates stemness in ovarian cancer by targeting PI3K/AKT/mTOR axis Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Fang Wang, Yang Zhang, Rui Pang, Shaohong Shi, Ran Wang
In women, ovarian cancer is a common gynecological cancer associated with poor prognosis, reoccurrence and chemoresistance. Scoulerine, a benzylisoquinoline alkaloid, has been reported effective against several carcinomas. Thus, we investigated the impact of scoulerine on ovarian cancer cells (OVCAR3). Cell viability was assessed by MTT assay, migration was determined by Boyden Chamber assay, while
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Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Guadalupe Y. Solís-Cruz, Rocío Alvarez-Roman, Verónica M. Rivas-Galindo, Sergio Arturo Galindo-Rodríguez, David A. Silva-Mares, Iván A. Marino-Martínez, Magdalena Escobar-Saucedo, Luis A. Pérez-López
Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize
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Rosuvastatin effects on the HDL proteome in hyperlipidemic patients Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Ana Vavlukis, Kristina Mladenovska, Katarina Davalieva, Marija Vavlukis, Aleksandar Dimovski
The advancements in proteomics have provided a better understanding of the functionality of apolipoproteins and lipoprotein-associated proteins, with the HDL lipoprotein fraction being the most studied. The focus of this study was to evaluate the HDL proteome in dyslipidemic subjects without an established cardiovascular disease, as well as to test whether rosuvastatin treatment alters the HDL proteome
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Astragaloside IV inhibits pathological functions of gastric cancer-associated fibroblasts through regulation of the HOXA6/ZBTB12 axis Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Haibo Liu, Shicheng Luo, Xiaofeng Sha, Zhiping Chen, Dongdong Yang
Cancer-associated fibroblasts (CAFs) play critical roles in the tumor microenvironment and exert tumor-promoting or tumor-retarding effects on cancer development. Astragaloside IV has been suggested to rescue the pathological impact of CAFs in gastric cancer. This study aimed to investigate the potential mechanism of astragaloside IV in the regulation of CAF pathological functions in gastric cancer
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Synthesis and protective effect of pyrazole conjugated imidazo[1,2-a]pyrazine derivatives against acute lung injury in sepsis rats via attenuation of NF-κB, oxidative stress, and apoptosis Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Binbin Zang, Lihui Wang
The current work was conducted to elucidate the pharmacological effect of pyrazole-conjugated imidazo[1,2-a]pyrazine derivatives against acute lung injury in rats in sepsis and their mechanism of action. Various pyrazole-conjugated imidazo[1,2-a]-pyrazine derivatives have been synthesized in a straightforward synthetic route. They exhibited a diverse range of inhibitory activity against NF-ĸB with
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Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Fredrick Nwude Eze, Chaweewan Jansakul, Teerapol Srichana
Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient
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Influence of fused deposition modelling printing parameters on tablet disintegration times: a design of experiments study Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Klemen Kreft, Tijana Stanić, Petra Perhavec, Rok Dreu, Zoran Lavrič
Despite the importance of process parameters in the printing of solid dosage forms using fused deposition modelling (FDM) technology, the field is still poorly explored. A design of experiment study was conducted to understand the complete set of process parameters of a custom developed FDM 3D printer and their influence on tablet disintegration time. Nine settings in the Simplify 3D printing process
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Is epinephrine still the drug of choice during cardiac arrest in the emergency department of the hospital? A meta-analysis Acta Pharm. (IF 2.8) Pub Date : 2023-09-14 Min Hou, Su Dong, Qing Kan, Meng Ouyang, Yun Zhang
Epinephrine is the first-line emergency drug for cardiac arrest and anaphylactic reactions but is reported to be associated with many challenges resulting in its under- or improper utilization. Therefore, in this meta-analysis, the efficacy and safety of epinephrine as a first-line cardiac emergency drug for both out-of-hospital and in-hospital patients was assessed. Pertinent articles were searched
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Efficacy of BNT162b2 and CoronaVac in patients diagnosed with COVID-19 Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Mustafa Dogan, Berna Yilmaz
This retrospective observational study is aimed to determine the efficacy of BNT162b2 (Pfizer-BioNTech) and CoronaVac (Sinovac) vaccines against symptomatic or severe disease in COVID-19-diagnosed patients. The secondary aim was to define the differences between vaccinated and un-vaccinated patients in terms of age, comorbidities and course of the disease, and to determine the survival rates. Of the
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Medicarpin induces G1 arrest and mitochondria-mediated intrinsic apoptotic pathway in bladder cancer cells Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Yuan Chen, Liqi Yin, Mingxuan Hao, Wenkai Xu, Jixian Gao, Yuxin Sun, Qiao Wang, Shi Chen, Youfeng Liang, Rui Guo, Jinku Zhang, Jinmei Li, Qiongli Zhai, Runfen Cheng, Jiansong Wang, Haifeng Wang, Zhao Yang
Bladder cancer (BC) is the tenth most commonly diagnosed cancer. High recurrence, chemoresistance, and low response rate hinder the effective treatment of BC. Hence, a novel therapeutic strategy in the clinical management of BC is urgently needed. Medicarpin (MED), an isoflavone from Dalbergia odorifera, can promote bone mass gain and kill tumor cells, but its anti-BC effect remains obscure. This study
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Antibacterial activity, quality and stability study of creams with new potential silver(I) complexes and in vivo case report Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Simona Sovová, Štefánia Laca Megyesi, Dagmar Mudroňová, Pavol Mudroň, Jarmila Harvanová, Michaela Rendošová, Michal Goga, Ľudmila Tkáčiková, Zuzana Vargová
The aim of this study was to evaluate the antibacterial activity, quality and stability of creams (at 1 % concentration) prepared with synthesized silver(I) complexes: [Ag(Nam)2]NO3·H2O ( AgNam), [Ag2(HGly)2]n(NO3)2n (AgGly) (Nam – nicotin-amide, Gly – glycine) and silver(I) sulfadiazine (AgSD), which is commercially available. Antibacterial activity was evaluated by agar well diffusion method and
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Pharmaceutical approaches for COVID-19: An update on current therapeutic opportunities Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Sijia Fan, Hongling Wang, Dean Wu, Lu Liu
SARS-CoV-2, a newly discovered coronavirus, has been linked to the COVID-19 pandemic and is currently an important public health issue. Despite all the work done to date around the world, there is still no viable treatment for COVID-19. This study examined the most recent evidence on the efficacy and safety of several therapeutic options available including natural substances, synthetic drugs and vaccines
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α1-Adrenoceptor agonist methoxamine inhibits base excision repair via inhibition of apurinic/apyrimidinic endonuclease 1 (APE1) Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Aneta Kohutova, Dita Münzova, Martin Pešl, Vladimir Rotrekl
Methoxamine (Mox) is a well-known α1-adrenoceptor agonist, clinically used as a longer-acting analogue of epinephrine. 1R,2S-Mox (NRL001) has been also undergoing clinical testing to increase the canal resting pressure in patients with bowel incontinence. Here we show, that Mox hydrochloride acts as an inhibitor of base excision repair (BER). The effect is mediated by the inhibition of apurinic/apyrimidinic
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Germline variants of the genes involved in NF-kB activation are associated with the risk of COPD and lung cancer development Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Jurica Baranasic, Yasmeen Niazi, Subhayan Chattopadhyay, Lada Rumora, Lorna Ćorak, Andrea Vukić Dugac, Marko Jakopović, Miroslav Samaržija, Asta Försti, Jelena Knežević
Chronic obstructive pulmonary disease (COPD) and lung cancer (LC) are closely related diseases associated with smoking history and dysregulated immune response. However, not all smokers develop the disease, indicating that genetic susceptibility could be important. Therefore, the aim of this study was to search for the potential overlapping genetic biomarkers, with a focus on single nucleotide polymorphisms
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Adverse drug reactions in the ambulatory internal patients at the emergency department: Focus on causality assessment and drug-drug interactions Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Matej Dobravc Verbič, Miran Brvar, Mojca Kerec Kos
A non-interventional retrospective study in ambulatory patients was conducted at the emergency department of the Division of internal medicine. In 2 months, 266 suspected adverse drug reactions (ADRs) were identified in 224/3453 patients (6.5 %). In 158/3453 patients (4.6 %), an ADR was the reason for emergency department visit and in 49 patients (1.4 %), ADRs led to hospitalisation. A causality assessment
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The readiness of the spontaneous reporting system for COVID-19 vaccines safety monitoring in Croatia Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Barbara Kovačić, Morana Pavičić, Nikica Mirošević Skvrce, Siniša Tomić
We aimed to identify whether a spontaneous reporting system (SRS) in Croatia could timely identify and confirm signals for COVID-19 vaccines. Post-marketing spontaneous reports of adverse drug reactions (ADRs) following COVID-19 immunisation reported to the Agency for Medicinal Products and Medical Devices of Croatia (HALMED) were extracted and analysed. 6624 cases reporting 30 655 ADRs following COVID-19
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External validation of population pharmacokinetic models of gentamicin in paediatric population from preterm newborns to adolescents Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Mateja Črček, Iztok Grabnar, Jurij Aguiar Zdovc, Štefan Grosek, Mojca Kerec Kos
The aim of this study was to externally validate the predictive performance of published population pharmacokinetic models of gentamicin in all paediatric age groups, from preterm newborns to adolescents. We first selected published population pharmacokinetic models of gentamicin developed in the paediatric population with a wide age range. The parameters of the literature models were then re-estimated
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Rosavin exerts an antitumor role and inactivates the MAPK/ERK pathway in small-cell lung carcinoma in vitro Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Rui Liu, Cuihong Jiang, Zhizheng Zhao, Yutong Lv, Gaoxing Wang
This study attempts to explore the function and mechanism of action of rosavin in small-cell lung cancer (SCLC) in vitro. The viability and clone formation of SCLC cells were assessed using cell counting kit-8 and colony formation assays, respectively. Apoptosis and cell cycle were detected using flow cytometry and cell cycle analysis, respectively. Wound healing and transwell assays were performed
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Long-term deprescription in chronic pain and opioid use disorder patients: Pharmacogenetic and sex differences Acta Pharm. (IF 2.8) Pub Date : 2023-06-12 Javier Muriel, Mónica Escorial, César Margarit, Jordi Barrachina, Cristian Carvajal, Domingo Morales, Ana M. Peiró
More than half of patients with opioid use disorder for chronic non-cancer pain (CNCP) reduced their dose through a progressive opioid withdrawal supported by a rotation to buprenorphine and/or tramadol. The aim of this research is to analyse the long-term effectiveness of opioid deprescription taking into account the impact of sex and pharmacogenetics on the inter-individual variability. A cross-sectional
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Prediction of drug-drug plasma protein binding interactions of resveratrol in combination with celecoxib and leflunomide by molecular docking combined with an ultrafiltration technique Acta Pharm. (IF 2.8) Pub Date : 2023-03-27 Peng Zhou, Fang Hua
The present study is aimed at computational prediction of the molecular interactions between resveratrol, celecoxib, leflunomide and human serum albumin (HSA) and then investigates the plasma protein binding of resveratrol combined with celecoxib or leflunomide by an ultrafiltration technique. Molecular operating environment (MOE, 2008.10) software package was used to explore molecular interactions
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Effects of 3R, 16S-2-hydroxyethyl apovincaminate (HEAPO), donepezil and galantamine on learning and memory retention in naïve Wistar rats Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Darinka Dimitrova, Damianka Getova, Kremena Saracheva
The effects of 3R,16S-2-hydroxyethyl apovincaminate (HEAPO, RGH-10885) compared with those of two cholinesterase inhibitors, donepezil and galantamine, were examined in naïve Wistar rats using standard active and passive avoidance tests. The active avoidance test (shuttle box) and two passive avoidance tests (step-through and step-down) were performed according to the experimental design. There were
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Recent approaches in the drug research and development of novel antimalarial drugs with new targets Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Naveen Kumar Reddy Chinnappanna, Gopi Yennam, Chaitanya Budagam Haima Naga Venkata Chaitanya, Shinu Pottathil, Pobitra Borah, Katharigatta N. Venugopala, Pran Kishore Deb, Raghu Prasad Mailavaram
Malaria is a serious worldwide medical issue that results in substantial annual death and morbidity. The availability of treatment alternatives is limited, and the rise of resistant parasite types has posed a significant challenge to malaria treatment. To prevent a public health disaster, novel antimalarial agents with single-dosage therapies, extensive curative capability, and new mechanisms are urgently
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The opposite effect of convulsant drugs on neuronal and endothelial nitric oxide synthase – A possible explanation for the dual proconvulsive/anticonvulsive action of nitric oxide Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Lourdes A. Vega Rasgado, Eva Ramón-Gallegos, Lorena Rodríguez-Páez, Verónica Alcántara-Farfán
Nitric oxide (NO) participates in processes such as endothelium-dependent vasodilation and neurotransmission/neuromodulation. The role of NO in epilepsy is controversial, attributing it to anticonvulsant but also proconvulsant properties. Clarification of this dual effect of NO might lead to the development of new antiepileptic drugs. Previous results in our laboratory indicated that this contradictory
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Ampelopsin induces MDA-MB-231 cell cycle arrest through cyclin B1-mediated PI3K/AKT/mTOR pathway in vitro and in vivo Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Minjun Meng, Qiaolu Yang, Zhong Ouyang, Qingmo Yang, Xinyi Wu, Yufan Huang, Yonghui Su, Shuanglong Chen, Wenlin Chen
Breast cancer is one of the most common malignant tumors in women and it is the most frequently diagnosed cancer in the world. Ampelopsin (AMP) is a purified component from the root of Ampelopsis grossedentata. It is reported that AMP could significantly inhibit the proliferation of breast cancer cells. However, the antitumor mechanism against breast cancer has not yet been fully elucidated. The purpose
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Tablet characteristics and pharmacokinetics of orally disintegrating tablets containing coenzyme Q10 granules prepared by different methods Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Yasuharu Kashiwagura, Shota Takusagawa, Yasuyuki Ikematsu, Shimako Tanaka, Noriyuki Namiki, Shinya Uchida
This study aimed to elucidate the characteristics and pharmacokinetics of orally disintegrating tablets (ODTs) containing coenzyme Q10 (CoQ10) granules prepared by spray drying, hot-melting, and wet granulation. The hardness and disintegration times of CoQ10-ODTs containing 5 % crospovidone were 61.6–81.8 N and < 30 s, respectively; these values indicate that the as-prepared ODTs were adequate for
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Diethylene glycol monoethyl ether-mediated nanostructured lipid carriers enhance trans-ferulic acid delivery by Caco-2 cells superior to solid lipid nanoparticles Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Hongyu Zhang, Jingwen Guo, Zhi Wang, Na Wang, Nianping Feng, Yongtai Zhang
This work aimed to compare the performance of trans-ferulic acid-encapsulated nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) for transport by Caco-2 cells. The NLC particles (diameter: 102.6 nm) composed of Compritol® 888 ATO, ethyl oleate, Cremophor® EL, and Transcutol® P were larger than the SLNs (diameter: 86.0 nm) formed without liquid lipid (ethyl oleate), and the former
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Effects of tranquilization therapy in elderly patients suffering from chronic non-communicable diseases: A meta-analysis Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Jing Li, Jing Li, Yulan Cui, Honggeng Li, Xiaoxuan Hou, Fang Zhao, Qing Zhao, Junlan Zhao, Pengchao Lin
The current meta-analysis searched the literature connected to different tranquilizers used to treat elderly people and assessed it in terms of dose, types of outcomes and adverse effects, to determine a safe and acceptable tranquilizer and its optimal dose. A systematic literature review was undertaken for randomized controlled trials, case-control, retrospective and prospective studies on the use
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Intensive critical care and management of asthmatic and smoker patients in COVID-19 infection Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Dongming Lu, Obaid Yaqoob, Manish Kumar, Ajay Singh Kushwah, Rahul Kumar Sharma, Devinder Kumar, Yogendra Mavai, Rukaiya Khan
This century’s most serious catastrophe, COVID-19, has been dubbed “the most life-threatening disaster ever”. Asthmatic persons are even more prone to COVID-19’s complex interplay with the underlying inflammatory condition. In order to protect themselves against COVID-19, asthmatic patients must be very vigilant in their usage of therapeutic techniques and drugs (e.g., bronchodilators, 5-lipoxygenase
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The in vitro anticancer effects of FS48 from salivary glands of Xenopsylla cheopis on NCI-H460 cells via its blockage of voltage-gated K+ channels Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Weichen Xiong, Huizhen Fan, Qingye Zeng, Zhenhui Deng, Guanhui Li, Wancheng Lu, Bei Zhang, Shian Lai, Xin Chen, Xueqing Xu
Voltage-gated K+ (Kv) channels play a role in the cellular processes of various cancer cells, including lung cancer cells. We previously identified and reported a salivary protein from the Xenopsylla cheopis, FS48, which exhibited inhibitory activity against Kv1.1-1.3 channels when assayed in HEK 293T cells. However, whether FS48 has an inhibitory effect on cancer cells expressing Kv channels is unclear
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Sodium butyrate attenuate hyperglycemia-induced inflammatory response and renal injury in diabetic mice Acta Pharm. (IF 2.8) Pub Date : 2023-01-24 Man Yan, Yan-Yan Zhang, Yue Xi, Long-Kun Ding, Chang Sun, Li-Juan Qu, Xin Qian, Jing-Wen Xu, Wen Sun, Liang Wu
The activation of the monocyte-macrophage system and the damage to the renal and pancreatic tissue are common complications in patients with diabetes induced by hyper-glycemia. This study aimed to evaluate the effect and mechanism of butyrate (NaB), a metabolite of intestinal flora, on inhibiting the inflammatory response of human monocyte-macrophages (THP-1 cells) induced by high glucose and the damage
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Relaxin inhibits 177Lu-EDTMP associated cell death in osteosarcoma cells through notch-1 pathway Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Junhua Xu, Song Wan, Wei Chen, Yi Zhang, Zhenzhong Ji
177Lu-EDTMP (Ethylenediamine tetramethylene phosphonic acid) is the most used radioactive agent for pain palliation in bone cancer patients. The present study aims to study the impact of relaxin-2 on the 177Lu-EDTMP associated cell toxicity and death in osteosarcoma cells. MG63 and Saos-2 cells were cultured with 177Lu-EDTMP (37 MBq) for 24 h with and without pretreatment of recombinant relaxin 2 (RLXH2)
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Direct oral anticoagulants (DOACs): From the laboratory point of view Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Sandra Margetić, Sandra Šupraha Goreta, Ivana Ćelap, Marija Razum
Direct oral anticoagulants (DOACs) represent a new generation of drugs that have been increasingly used in the prevention and treatment of thromboembolic states. According to the mechanism of anticoagulant action, DOACs are divided into two groups: direct inhibitors of thrombin (dabigatran) and direct inhibitors of activated factor X (FXa) (rivaroxaban, apixaban, edoxaban, betrixaban). Compared to
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In vitro effects of ascorbic acid on viability and metabolism of patients’ osteosarcoma stem cells Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Marijana Šimić Jovičić, Maja Pušić, Maja Antunović, Maja Ledinski, Lucija Librenjak, Robert Kolundžić, Tomislav Ribičić, Vladimir Trkulja, Inga Urlić
Stagnation in novelties of osteosarcoma (OS) treatment indicates the need for new therapeutic methods. OS cancer stem cells (OS-CSC) are taught to have the ability to self-renew and develop mechanisms of anticancer drug resistance, and this is why it is difficult to eradicate them. Their metabolism has been recognized as a potential target of therapeutic action. Ascorbic acid (AA) is considered to
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Punicalagin attenuated allergic airway inflammation via regulating IL4/IL-4Rα/STAT6 and Notch- GATA3 pathways Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Li Yu, Jianying Li
Allergic asthma is an inflammatory disease of the airways which has a complex etiology. Punicalagin, a major polyphenol present in pomegranates, is reported to possess various biological properties including antioxidant and antiproliferative effects. The current research aimed to evaluate the antiasthmatic effects of punicalagin in an ovalbumin (OVA)-induced experimental model of asthma in female BALB/c
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Effect of in vitro gastrointestinal digestion on the chemical composition and antioxidant properties of Ginkgo biloba leaves decoction and commercial capsules Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Yubo Zhou, Yingxin Yang, Minyan Ma, Lingyun Xie, Aijuan Yan, Wen Cao
In this study Ginkgo biloba leaves (GBL) decoction and commercial capsules were digested using an in vitro model. Thirty-six active compounds were identified and quantified by HPLC-ESI-MS analysis based on the MS/MS patterns (precursor ions and product ions) and retention times, in comparison with reference standards. Most compounds in GBL showed a significant decrease during intestinal digestion,
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Anti-inflammatory effects of NaB and NaPc in Acinetobacter baumannii-stimulated THP-1 cells via TLR-2/NF-κB/ROS/NLRP3 pathway Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Chen Shu, Zhang Yan-Yan, Zhang Hai, Ding Long-Kun, Xi Yue, Yan Man, Sun Chang, Wu Liang, Hu Hao
This study evaluated the anti-inflammation effect of the three main short-chain fatty acids (SCFAs) on Acinetobacter baumannii-induced THP-1 cells. The three main SCFAs could inhibit A. baumannii-stimulated THP-1 cell NF-κB pathway activity and the expressions of NLRP3 inflamma-some and GSDMD, and increase autophagy. The three main SCFAs, especially the sodium butyrate (NaB), had the effect of down-regulation
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Therapeutic alliance impact on analgesic outcomes in a real-world clinical setting: An observational study Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Jordi Barrachina, César Margarit, Blanca Andreu, Thomas Zandonai, Pura Ballester, Javier Muriel, Esperanza Cutillas, Ana M. Peiró
A good therapeutic alliance is relevant for healthcare providers exposed to patients’ suffering, especially since patients and physicians may understand the painful experience differently. Our aim was to explore the impact of therapeutic alliance on analgesic outcomes in a real-world interdisciplinary pain unit (PU). A cross-sectional observational study was conducted on outpatients (n = 69) using
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Synergistic action between a synthetic cannabinoid compound and tramadol in neuropathic pain rats Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Geovanna Nallely Quiñonez-Bastidas, Ulises Osuna-Martínez, Ana Laura Reda-Licea, Manuel López-Ortíz, Ignacio Regla, Andrés Navarrete
In the present study the interaction of cannabinoid, PhAR-DBH-Me [(R, Z)-18-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-18-oxooctadec-9-en-7-ylphenyl-acetate] and tramadol in two neuropathy models, as well as their possible toxic effects, was analyzed. The anti-allodynic effect of PhAR-DBH-Me, tramadol, or their combination, were evaluated in neuropathic rats. Furthermore, the effective dose
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MicroRNA-140-5p inhibits cellular proliferation, migration and invasion by downregulating AKT/STAT3/NF-κB pathway in breast carcinoma cells Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Lingli Hou, Qi Liu, Ying Zhao, Hongwei Yang, Qingying Meng, Fei Yu
MicroRNA-140-5p (miR-140-5p) plays a pivotal role in human cancers. However, its role and molecular mechanisms in breast carcinoma are not fully explored. Using miR-140-5p transfected breast cancer cell line MDA-MB-231, several in vitro experiments were performed and described in this paper. They consist of the cell proliferation assay, wound healing assay, transwell assay, colony formation assays
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Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole Acta Pharm. (IF 2.8) Pub Date : 2022-10-18 Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Usama A. Fahmy, Osama A. A. Ahmed, Nabil A. Alhakamy, Mahmoud A. Elfaky, Alaa Sirwi, Salman A. Hawsawi, Ali H. Alzahrani, Abdulrahman Y. Yaseen, Mohannad Qassim, Sabna Kotta
Fluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availability. Accordingly, this research aimed at developing a self-assembled mixed micelles topical delivery system
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Polyphenol content and antioxidant activity of phytoestrogen containing food and dietary supplements: DPPH free radical scavenging activity by HPLC Acta Pharm. (IF 2.8) Pub Date : 2022-04-13 Daniela Amidžić Klarić,Ana Mornar,Jelena Kovačić,Mario-Livio Jeličić,Edvin Brusač,Iva Brletić,Ilija Klarić
Abstract Soy, red clover, chaste tree, hop and flax have all been found to contain a wide range of phytoestrogenic compounds, and a large number of dietary supplements contain their extracts as principal ingredients. This study is aimed to evaluate the total polyphenolic content and antioxidant activity of phytoestrogen-containing food and formulated dietary supplements. The HPLC-DPPH method was applied
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Design and development of novel 1,2,3-triazole chalcone derivatives as potential anti-osteosarcoma agents via inhibition of PI3K/Akt/mTOR signalling pathway Acta Pharm. (IF 2.8) Pub Date : 2022-04-13 Qing Su,Baolin Xu,Zhoubin Tian,Ziling Gong
Abstract Osteosarcoma (OS) is an uncommon tumour that mainly affects bone in children and adolescents. The current treatment options of OS are of limited significance due to their immense side effects. In the present manuscript, we have developed a novel series of 1,2,3-triazole chalcone derivatives as potential agents against OS. The compounds were synthesized and evaluated for their PI3K and mTOR
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The effectiveness of dexamethasone as a combination therapy for COVID-19 Acta Pharm. (IF 2.8) Pub Date : 2022-04-13 Nader Namazi
Abstract Coronavirus disease 2019 (COVID-19) was reported as a global pandemic in March 2020 after invading many countries and leaving behind tens of thousands of infected patients in a brief time span. Approval of a few vaccines has been obtained and their efficacy of varying degrees established. Still, there is no effective pharmaceutical agent for the treatment of COVID-19 though several drugs are
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Dasatinib enhances curcumin-induced cytotoxicity, apoptosis and protective autophagy in human schwannoma cells HEI-193: The role of Akt/mTOR/p70S6K signalling pathway Acta Pharm. (IF 2.8) Pub Date : 2022-04-13 Pengfei Pang,Shirong Zhang
Abstract The present study was carried out in human schwannoma cells (HEI-193) to determine the combined anti-cancer effect of curcumin and dasatinib. Cells were treated with curcumin only, dasatinib only, or the combination of curcumin and dasatinib for 24 hours. Cellular toxicity, cell proliferation, and cell death were determined by LDH, MTT, and trypan blue dye assays, respectively. ELISA based