European Journal of Pharmaceutical Sciences 
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This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.Broad-Spectrum Activity of Membranolytic Cationic Macrocyclic Peptides Against Multi-Drug Resistant Bacteria and Fungi
Eur J Pharm Sci. 2024 Apr 23:106776. doi: 10.1016/j.ejps.2024.106776. Online ahead of print.ABSTRACTThe emergence of multidrug-resistant (MDR) strains causes severe problems in the treatment of microbial infections owing to limited treatment options. Antimicrobial peptides (AMPs) are drawing considerable attention as promising antibiotic alternative candidates to combat MDR bacterial and fungal infections. Herein, we present a series of small amphiphilic membrane-active cyclic peptides composed, in part, of various nongenetically encoded hydrophilic and hydrophobic amino acids. Notably, lead cyclic peptides 3b and 4b showe...
Source: European Journal of Pharmaceutical Sciences - April 25, 2024 Category: Drugs & Pharmacology Authors: Sandeep Lohan Anastasia G Konshina Rakesh K Tiwari Roman G Efremov Innokentiy Maslennikov Keykavous Parang Source Type: research
A potential therapeutic agent for the treatment of hyperuricemia and gout: 3,4-Dihydroxy-5-nitrobenzaldehyde phenylthiosemicarbazide
Eur J Pharm Sci. 2024 Apr 21:106778. doi: 10.1016/j.ejps.2024.106778. Online ahead of print.ABSTRACTUric acid, the metabolic product of purines, relies on xanthine oxidase (XOD) for production. XOD is a target for the development of drugs for hyperuricemia (HUA) and gout. Currently, treatment options remain limited for gout patients. 3, 4-Dihydroxy-5-nitrobenzaldehyde (DHNB) is a derivative of the natural product protocatechualdehyde with good biological activity. In this work, we identify a DHNB thiosemicarbazide class of compounds that targets XOD. 3,4-Dihydroxy-5-nitrobenzaldehyde phenylthiosemicarbazone can effectively...
Source: European Journal of Pharmaceutical Sciences - April 23, 2024 Category: Drugs & Pharmacology Authors: Xiongying Yu Shuaiwei Ren Jun Zhou Yongcui Liao Yousheng Huang Dong Huanhuan Source Type: research
A potential therapeutic agent for the treatment of hyperuricemia and gout: 3,4-Dihydroxy-5-nitrobenzaldehyde phenylthiosemicarbazide
Eur J Pharm Sci. 2024 Apr 21:106778. doi: 10.1016/j.ejps.2024.106778. Online ahead of print.ABSTRACTUric acid, the metabolic product of purines, relies on xanthine oxidase (XOD) for production. XOD is a target for the development of drugs for hyperuricemia (HUA) and gout. Currently, treatment options remain limited for gout patients. 3, 4-Dihydroxy-5-nitrobenzaldehyde (DHNB) is a derivative of the natural product protocatechualdehyde with good biological activity. In this work, we identify a DHNB thiosemicarbazide class of compounds that targets XOD. 3,4-Dihydroxy-5-nitrobenzaldehyde phenylthiosemicarbazone can effectively...
Source: European Journal of Pharmaceutical Sciences - April 23, 2024 Category: Drugs & Pharmacology Authors: Xiongying Yu Shuaiwei Ren Jun Zhou Yongcui Liao Yousheng Huang Dong Huanhuan Source Type: research
Modeling an evaluation of the efficacy of the novel neuroanalgesic drug mirogabalin for diabetic peripheral neuropathic pain and postherpetic neuralgia therapy
Eur J Pharm Sci. 2024 Apr 20:106777. doi: 10.1016/j.ejps.2024.106777. Online ahead of print.ABSTRACTDiabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN) are challenging and often intractable complex medical conditions, with a substantial impact on the quality of life. Mirogabalin, a novel voltage-gated Ca2+ channel α2δ ligand, was approved for the indication of DPNP and PHN. However, the time course of effects has not yet been clarified.We aimed to establish pharmacodynamic and placebo effect models of mirogabalin and pregabalin in DPNP and PHN, and to quantitatively compare the efficacy character...
Source: European Journal of Pharmaceutical Sciences - April 22, 2024 Category: Drugs & Pharmacology Authors: Li-Mian Hong Jian-Min Liu Lei Lin Chun-Chun Huang Rui Chen Wei-Wei Lin Source Type: research
Modeling an evaluation of the efficacy of the novel neuroanalgesic drug mirogabalin for diabetic peripheral neuropathic pain and postherpetic neuralgia therapy
Eur J Pharm Sci. 2024 Apr 20:106777. doi: 10.1016/j.ejps.2024.106777. Online ahead of print.ABSTRACTDiabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN) are challenging and often intractable complex medical conditions, with a substantial impact on the quality of life. Mirogabalin, a novel voltage-gated Ca2+ channel α2δ ligand, was approved for the indication of DPNP and PHN. However, the time course of effects has not yet been clarified.We aimed to establish pharmacodynamic and placebo effect models of mirogabalin and pregabalin in DPNP and PHN, and to quantitatively compare the efficacy character...
Source: European Journal of Pharmaceutical Sciences - April 22, 2024 Category: Drugs & Pharmacology Authors: Li-Mian Hong Jian-Min Liu Lei Lin Chun-Chun Huang Rui Chen Wei-Wei Lin Source Type: research
The Allostery and Modification of hGHRH Molecules and Specific Dimer Produced Significant Fertility Effect by Proliferating and Activating in-situ Ovarian Mesenchymal Stem Cells
Eur J Pharm Sci. 2024 Apr 19:106768. doi: 10.1016/j.ejps.2024.106768. Online ahead of print.ABSTRACTThe negative coordination of growth hormone secretagogue receptor (GHS-R) and growth hormone-releasing hormone receptor (GHRH-R) involves in the repair processes of cellular injury. The allosteric U- or H-like modified GHRH dimer Grinodin and 2Y were comparatively evaluated in normal Kunming mice and hamster infertility models induced by CPA treatment. 1-3-9 µg of Grinodin or 2Y per hamster stem-cell-exhaustion model was subcutaneously administered once a week, respectively inducing 75-69-46 or 45-13-50% of birth rates. In ...
Source: European Journal of Pharmaceutical Sciences - April 21, 2024 Category: Drugs & Pharmacology Authors: Xu-Dong Zhang Qun Luo Yan Du Li Yang Li-Cheng Yu Lan Feng Dan Rao Jing-Xuan Tang Hong-Mei Tan Xiao-Yuan Guo Song-Shan Tang Tao Liu Feng Yue Hui-Xian Huang Source Type: research
Development of a dry powder insufflation device with application in in vitro cell-based assays in the context of respiratory delivery
Eur J Pharm Sci. 2024 Apr 19:106775. doi: 10.1016/j.ejps.2024.106775. Online ahead of print.ABSTRACTResearch on pharmaceutical dry powders has been increasing worldwide, along with increased therapeutic strategies for an application through the pulmonary or the nasal routes. In vitro methodologies and tests that mimic the respiratory environment and the process of inhalation itself are, thus, essential. The literature frequently reports cell-based in vitro assays that involve testing the dry powders in suspension. This experimental setting is not adequate, as both the lung and the nasal cavity are devoid of abundant liquid...
Source: European Journal of Pharmaceutical Sciences - April 21, 2024 Category: Drugs & Pharmacology Authors: Jorge F Pontes Herm ínio P Diogo Eus ébio Conceição Maria P Almeida Rui M Borges Dos Santos Ana Grenha Source Type: research
Hierarchical cluster analysis and nonlinear mixed-effects modelling for candidate biomarker detection in preclinical models of cancer
CONCLUSION: Application of NLME, as well as HCA of candidate biomarkers may provide additional avenues to assess the effect of RT in MC38 syngeneic tumour models. Additional studies would need to be conducted to confirm association between DD7 and biomarkers in RT/DDRi treated mice.PMID:38641123 | DOI:10.1016/j.ejps.2024.106774 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - April 19, 2024 Category: Drugs & Pharmacology Authors: David Hodson Hitesh Mistry James Yates Sofia Guzzetti Michael Davies Leon Aarons Kayode Ogungbenro Source Type: research
HLM chip - A microfluidic approach to study the mechanistic basis of cytochrome P450 inhibition using immobilized human liver microsomes
In this study, we conceptualize a microfluidic approach to mechanistic CYP inhibition studies using human liver microsomes (HLMs) immobilized onto the walls of a polymer micropillar array. We evaluated the feasibility of these HLM chips for CYP inhibition studies by establishing the stability and the enzyme kinetics for a CYP2C9 model reaction under microfluidic flow and determining the half-maximal inhibitory concentrations (IC50) of three human CYP2C9 inhibitors (sulfaphenazole, tienilic acid, miconazole), including evaluation of their inhibition mechanisms and nonspecific microsomal binding on chip. Overall, the enzyme ...
Source: European Journal of Pharmaceutical Sciences - April 19, 2024 Category: Drugs & Pharmacology Authors: Tea Pihlaja Iiro Kiiski Tiina Sikanen Source Type: research
Bifunctional HDAC and DNMT inhibitor induces viral mimicry activates the innate immune response in triple-negative breast cancer
In this study, the bifunctional HDAC and DNMT inhibitor J208 exhibited antitumour activity in TNBC cell lines. J208 effectively induced apoptosis and cell cycle arrest at the G0/G1 phase, inhibiting cell migration and invasion in TNBC. Moreover, this bifunctional inhibitor induced the expression of endogenous retroviruses (ERVs) and elicited a viral mimicry response, which increased the intracellular levels of double-stranded RNA (dsRNA) to activate the innate immune signalling pathway in TNBC. In summary, we demonstrated that the bifunctional inhibitor J208, which is designed to inhibit HDAC and DNMT, has potent anticance...
Source: European Journal of Pharmaceutical Sciences - April 18, 2024 Category: Drugs & Pharmacology Authors: Weiwen Fan Wenkai Li Lulu Li Meirong Qin Chengzhou Mao Zigao Yuan Ping Wang Bizhu Chu Yuyang Jiang Source Type: research
Bifunctional HDAC and DNMT inhibitor induces viral mimicry activates the innate immune response in triple-negative breast cancer
In this study, the bifunctional HDAC and DNMT inhibitor J208 exhibited antitumour activity in TNBC cell lines. J208 effectively induced apoptosis and cell cycle arrest at the G0/G1 phase, inhibiting cell migration and invasion in TNBC. Moreover, this bifunctional inhibitor induced the expression of endogenous retroviruses (ERVs) and elicited a viral mimicry response, which increased the intracellular levels of double-stranded RNA (dsRNA) to activate the innate immune signalling pathway in TNBC. In summary, we demonstrated that the bifunctional inhibitor J208, which is designed to inhibit HDAC and DNMT, has potent anticance...
Source: European Journal of Pharmaceutical Sciences - April 18, 2024 Category: Drugs & Pharmacology Authors: Weiwen Fan Wenkai Li Lulu Li Meirong Qin Chengzhou Mao Zigao Yuan Ping Wang Bizhu Chu Yuyang Jiang Source Type: research
Current uncertainties and challenges of publicly available pharmaceutical environmental risk assessment data
Eur J Pharm Sci. 2024 Apr 16;197:106769. doi: 10.1016/j.ejps.2024.106769. Online ahead of print.ABSTRACTPharmaceutical residues are widely detected in aquatic environment worldwide mainly arising from human excretions in sewage systems. Presently, publicly available, high quality environmental risk assessment (ERA) data for pharmaceuticals are limited. However, databases like the Swedish Fass offer valuable resources aiding healthcare professionals and environmental scientists in identifying substances of significant concern. In this review, we provide a concise overview of the regulatory ERA process for medicinal products...
Source: European Journal of Pharmaceutical Sciences - April 17, 2024 Category: Drugs & Pharmacology Authors: H Ahkola L Äystö T Sikanen S Riikonen T Pihlaja S Kauppi Source Type: research
Current uncertainties and challenges of publicly available pharmaceutical environmental risk assessment data
Eur J Pharm Sci. 2024 Apr 15:106769. doi: 10.1016/j.ejps.2024.106769. Online ahead of print.ABSTRACTPharmaceutical residues are widely detected in aquatic environment worldwide mainly arising from human excretions in sewage systems. Presently, publicly available, high quality environmental risk assessment (ERA) data for pharmaceuticals are limited. However, databases like the Swedish Fass offer valuable resources aiding healthcare professionals and environmental scientists in identifying substances of significant concern. In this review, we provide a concise overview of the regulatory ERA process for medicinal products int...
Source: European Journal of Pharmaceutical Sciences - April 17, 2024 Category: Drugs & Pharmacology Authors: H Ahkola L Äystö T Sikanen S Riikonen T Pihlaja S Kauppi Source Type: research
Curcumin and quercetin co-encapsulated in nanoemulsions for nasal administration: a promising therapeutic and prophylactic treatment for viral respiratory infections
Eur J Pharm Sci. 2024 Apr 12:106766. doi: 10.1016/j.ejps.2024.106766. Online ahead of print.ABSTRACTOne of the most frequent causes of respiratory infections are viruses. Viruses reaching the airways can be absorbed by the human body through the respiratory mucosa and mainly infect lung cells. Several viral infections are not yet curable, such as coronavirus-2 (SARS-CoV-2). Furthermore, the side effect of synthetic antiviral drugs and reduced efficacy against resistant variants have reinforced the search for alternative and effective treatment options, such as plant-derived antiviral molecules. Curcumin (CUR) and quercetin...
Source: European Journal of Pharmaceutical Sciences - April 14, 2024 Category: Drugs & Pharmacology Authors: Daniela Pastorim Vaiss Jamile Lima Rodrigues Virginia Campello Yurgel Frank do Carmo Guedes Lauanda Larissa Mendon ça da Matta Paula Alice Bezerra Barros Gustavo Richter Vaz Ra íssa Nunes Dos Santos Bibiana Franzen Matte Larine Kupski Jaqueline Garda-Bu Source Type: research
Curcumin and quercetin co-encapsulated in nanoemulsions for nasal administration: a promising therapeutic and prophylactic treatment for viral respiratory infections
Eur J Pharm Sci. 2024 Apr 12:106766. doi: 10.1016/j.ejps.2024.106766. Online ahead of print.ABSTRACTOne of the most frequent causes of respiratory infections are viruses. Viruses reaching the airways can be absorbed by the human body through the respiratory mucosa and mainly infect lung cells. Several viral infections are not yet curable, such as coronavirus-2 (SARS-CoV-2). Furthermore, the side effect of synthetic antiviral drugs and reduced efficacy against resistant variants have reinforced the search for alternative and effective treatment options, such as plant-derived antiviral molecules. Curcumin (CUR) and quercetin...
Source: European Journal of Pharmaceutical Sciences - April 14, 2024 Category: Drugs & Pharmacology Authors: Daniela Pastorim Vaiss Jamile Lima Rodrigues Virginia Campello Yurgel Frank do Carmo Guedes Lauanda Larissa Mendon ça da Matta Paula Alice Bezerra Barros Gustavo Richter Vaz Ra íssa Nunes Dos Santos Bibiana Franzen Matte Larine Kupski Jaqueline Garda-Bu Source Type: research
