journal
https://read.qxmd.com/read/38530582/novel-method-of-measurement-of-in-vitro-drug-uptake-in-oatp1b3-overexpressing-cells-in-the-presence-of-dextran
#1
JOURNAL ARTICLE
Anna Kowal-Chwast, Ewelina Gabor-Worwa, Nilesh Gaud, Dawid Gogola, Agnieszka Piątek, Adrian Zarębski, Peter Littlewood, Marek Smoluch, Krzysztof Brzózka, Kamil Kuś
BACKGROUND: In predictions about hepatic clearance (CLH ), a number of studies explored the role of albumin and transporters in drug uptake by liver cells, challenging the traditional free-drug theory. It was proposed that liver uptake can occur for transporter substrate compounds not only from the drug's unbound form but also directly from the drug-albumin complex, a phenomenon known as uptake facilitated by albumin. In contrast to albumin, dextran does not exhibit binding properties for compounds...
March 26, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38526651/ginsenoside-rg5-as-an-anticancer-drug-a-comprehensive-review-on-mechanisms-structure-activity-relationship-and-prospects-for-clinical-advancement
#2
REVIEW
Tilal Elsaman, Ali Mahmoud Muddathir, Ebtihal A M Mohieldin, Irmanida Batubara, Min Rahminiwati, Kosei Yamauchi, Magdi Awadalla Mohamed, Shadila Fira Asoka, Dietrich Büsselberg, Solomon Habtemariam, Javad Sharifi-Rad
Cancer remains one of the leading causes of death in the world. Despite the considerable success of conventional treatment strategies, the incidence and mortality rates are still high, making developing new effective anticancer therapies an urgent priority. Ginsenoside Rg5 (Rg5) is a minor ginsenoside constituent obtained exclusively from ginseng species and is known for its broad spectrum of pharmacological activities. This article aimed to comprehensively review the anticancer properties of Rg5, focusing on action mechanisms, structure-activity relationship (SAR), and pharmacokinetics attributes...
March 25, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38519733/the-effect-of-valproate-on-the-amino-acids-monoamines-and-kynurenic-acid-concentrations-in-brain-structures-involved-in-epileptogenesis-in-the-pentylenetetrazol-kindled-rats
#3
JOURNAL ARTICLE
Aleksandra Wisłowska-Stanek, Danuta Turzyńska, Alicja Sobolewska, Karolina Kołosowska, Janusz Szyndler, Anna Skórzewska, Piotr Maciejak
BACKGROUND: The study aimed to assess the influence of a single valproate (VPA) administration on inhibitory and excitatory neurotransmitter concentrations in the brain structures involved in epileptogenesis in pentylenetetrazol (PTZ)-kindled rats. METHODS: Adult, male Wistar rats were kindled by repeated intraperitoneal (ip) injections of PTZ at a subconvulsive dose (30 mg/kg, three times a week). Due to the different times required to kindle the rats (18-22 injections of PTZ), a booster dose of PTZ was administrated 7 days after the last rats were kindled...
March 22, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38519732/cannabidiol-may-prevent-the-development-of-congestive-hepatopathy-secondary-to-right-ventricular-hypertrophy-associated-with-pulmonary-hypertension-in-rats
#4
JOURNAL ARTICLE
Anna Krzyżewska, Marta Baranowska-Kuczko, Anna Galicka, Irena Kasacka, Krzysztof Mińczuk, Hanna Kozłowska
BACKGROUND: Pulmonary hypertension (PH) can cause right ventricular (RV) failure and subsequent cardiohepatic syndrome referred to as congestive hepatopathy (CH). Passive blood stasis in the liver can affect inflammation, fibrosis, and ultimately cirrhosis. Cannabidiol (CBD) has many beneficial properties including anti-inflammatory and reduces RV systolic pressure and RV hypertrophy in monocrotaline (MCT)-induced PH in rats. Thus, it suggests that CBD may have the potential to limit CH development secondary to RV failure...
March 22, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38502301/migraine-and-the-microbiota-can-probiotics-be-beneficial-in-its-prevention-a-narrative-review
#5
REVIEW
Aneta Kiecka, Marian Szczepanik
Migraine is a recurrent disease of the central nervous system that affects an increasing number of people worldwide causing a continuous increase in the costs of treatment. The mechanisms underlying migraine are still unclear but recent reports show that people with migraine may have an altered composition of the intestinal microbiota. It is well established that the gut-brain axis is involved in many neurological diseases, and probiotic supplementation may be an interesting treatment option for these conditions...
March 19, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38498260/effect-of-polyphenols-against-complications-of-covid-19-current-evidence-and-potential-efficacy
#6
REVIEW
Mahdi Vajdi, Arash Karimi, Shirin Hassanizadeh, Mahdieh Abbasalizad Farhangi, Mohammad Bagherniya, Gholamreza Askari, Basil D Roufogalis, Neal M Davies, Amirhossein Sahebkar
The COVID-19 pandemic that started in 2019 and resulted in significant morbidity and mortality continues to be a significant global health challenge, characterized by inflammation, oxidative stress, and immune system dysfunction.. Developing therapies for preventing or treating COVID-19 remains an important goal for pharmacology and drug development research. Polyphenols are effective against various viral infections and can be extracted and isolated from plants without losing their therapeutic potential. Researchers have developed methods for separating and isolating polyphenols from complex matrices...
March 18, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38498259/protective-effect-of-hygrolansamycin-c-against-corticosterone-induced-toxicity-and-oxidative-stress-mediated-via-autophagy-and-the-mapk-signaling-pathway
#7
JOURNAL ARTICLE
Jongtae Roh, Jun-Pil Jang, Taehoon Oh, Jihong Kim, Byeongsan Lee, Young-Soo Hong, Jae-Hyuk Jang, Sung-Kyun Ko
BACKGROUND: Excessive stress, a major problem in modern societies, affects people of all ages worldwide. Corticosterone is one of the most abundant hormones secreted during stressful conditions and is associated with various dysfunctions in the body. In particular, we aimed to investigate the protective effects of hygrolansamycin C (HYGC) against corticosterone-induced cellular stress, a manifestation of excessive stress prevalent in contemporary societies. METHODS: We isolated HYGC from Streptomyces sp...
March 18, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38485859/liquid-chromatography-tandem-mass-spectrometry-method-for-mycophenolic-acid-and-its-glucuronide-determination-in-saliva-samples-from-children-with-nephrotic-syndrome
#8
JOURNAL ARTICLE
Joanna Sobiak, Matylda Resztak, Weronika Sikora, Jacek Zachwieja, Danuta Ostalska-Nowicka
BACKGROUND: Saliva sampling is one of the methods of therapeutic drug monitoring for mycophenolic acid (MPA) and its metabolite, mycophenolic acid glucuronide (MPAG). The study describes the liquid chromatography tandem mass spectrometry (LC-MS/MS) method developed for saliva MPA and MPAG determination in children with nephrotic syndrome. METHODS: The mobile phase consisted of methanol and water at gradient flow, both with 0.1% formic acid. Firstly, 100 µL of saliva was evaporated at 45 °C for 2 h to dryness, secondly, it was reconstituted in the mobile phase, and finally 10 µL was injected into the LC-MS/MS system...
March 15, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38480667/further-proof-on-the-role-of-accumbal-nnos-in-cocaine-seeking-behavior-in-rats
#9
JOURNAL ARTICLE
Małgorzata Frankowska, Irena Smaga, Kinga Gawlińska, Renata Pieniążek, Małgorzata Filip
BACKGROUND: Cocaine use disorder (CUD) remains a severe health problem with no effective pharmacological therapy. One of the potential pharmacological strategies for CUD pharmacotherapy includes manipulations of the brain glutamatergic (Glu) system which is particularly involved in drug withdrawal and relapse. Previous research indicated a pivotal role of ionotropic N-methyl-D-aspartate (NMDA) receptors or metabotropic receptors' type 5 (mGlu5 ) receptors in controlling the reinstatement of cocaine...
March 14, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38480666/are-there-sex-differences-in-oxytocin-and-vasopressin-v1a-receptors-ligand-binding-affinities
#10
JOURNAL ARTICLE
Jack H Taylor, H Elliott Albers
BACKGROUND: There is substantial evidence for sex differences in the functioning of one of the most common receptor systems; G protein-coupled receptors (GPCRs). There are many points along the GPCR-mediated molecular signaling pathway at which males and females may differ, one of the first of which, chronologically, is in the stability of the interaction between the ligand and the receptor, or its binding affinity. Here we investigate the binding affinities of oxytocin (OT) and vasopressin (AVP) at the oxytocin receptor (OTR) and the vasopressin V1a receptor (V1aR), both of which are present in numerous in brain regions associated with social behavior...
March 13, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38478219/transcriptome-analysis-of-an-akt-inhibitor-resistant-endometrial-cancer-cell-line
#11
JOURNAL ARTICLE
Takafumi Onishi, Tsuyoshi Takashima, Kazuki Shibahara, Shoji Takagi, Shinichi Tanaka, Michihiro Mori, Hirokazu Odashima, Yukihiko Osawa, Manabu Hattori
BACKGROUND: Drug resistance in endometrial cancer (EC) is a serious problem and a barrier to improving prognosis. The PI3K/AKT/mTOR pathway is highly activated in EC and can serve as a potential therapeutic target. Inhibitors against AKT have been developed, but resistance to these inhibitors is a concern. This study aimed to establish AKT inhibitor resistant cell lines and identify differentially expressed genes (DEGs) between parental and AKT inhibitor resistant cell lines to understand the mechanism of drug resistance to AKT inhibitors in EC...
March 13, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38472637/mechanisms-of-norcantharidin-against-renal-tubulointerstitial-fibrosis
#12
REVIEW
Qin-Su Yun, Yu-Xin Bao, Jie-Bing Jiang, Qian Guo
Renal tubulointerstitial fibrosis (RTIF) is a common feature and inevitable consequence of all progressive chronic kidney diseases, leading to end-stage renal failure regardless of the initial cause. Although research over the past few decades has greatly improved our understanding of the pathophysiology of RTIF, until now there has been no specific treatment available that can halt the progression of RTIF. Norcantharidin (NCTD) is a demethylated analogue of cantharidin, a natural compound isolated from 1500 species of medicinal insect, the blister beetle (Mylabris phalerata Pallas), traditionally used for medicinal purposes...
March 12, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38457019/association-between-gene-polymorphisms-and-initial-warfarin-therapy-in-patients-after-heart-valve-surgery
#13
JOURNAL ARTICLE
Zhaohui Liu, Fengming Luo, Juan Zhao, Weinan Chen, Wei Gao, Zhou Zhou
BACKGROUND: Warfarin is widely used for the prevention and treatment of thrombotic events. This study aimed to examine the influence of gene polymorphisms on the early stage of warfarin therapy in patients following heart valve surgery. METHODS: Nine single nucleotide polymorphisms were genotyped using microarray chips, categorizing patients into three groups: normal responders (Group I), sensitive responders (Group II), and highly sensitive responders (Group III)...
March 8, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38457018/cannabinoids-in-the-treatment-of-glioblastoma
#14
REVIEW
Barbara Buchalska, Katarzyna Kamińska, Maja Owe-Larsson, Agnieszka Cudnoch-Jędrzejewska
Glioblastoma (GBM) is the most prevalent primary malignant tumor of the nervous system. While the treatment of other neoplasms is increasingly more efficacious the median survival rate of GBM patients remains low and equals about 14 months. Due to this fact, there are intensive efforts to find drugs that would help combat GBM. Nowadays cannabinoids are becoming more and more important in the field of cancer and not only because of their properties of antiemetic drugs during chemotherapy. These compounds may have a direct cytotoxic effect on cancer cells...
March 8, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38448729/the-protective-effects-of-statins-in-traumatic-brain-injury
#15
REVIEW
Safoora Pordel, Alice P McCloskey, Wael Almahmeed, Amirhossein Sahebkar
Traumatic brain injury (TBI), often referred to as the "silent epidemic", is the most common cause of mortality and morbidity worldwide among all trauma-related injuries. It is associated with considerable personal, medical, and economic consequences. Although remarkable advances in therapeutic approaches have been made, current treatments and clinical management for TBI recovery still remain to be improved. One of the factors that may contribute to this gap is that existing therapies target only a single event or pathology...
March 7, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38438661/the-study-of-platelet-aggregation-using-a-microtiter-plate-reader-%C3%A2-methodological-considerations
#16
REVIEW
Magdalena Boncler, Jacek Golański
Optical aggregometry by 96-well plate assay, the microplate method, is a fast, efficient, and readily available method for measuring the pharmacological effects of antiplatelet drugs. Even though recent years have witnessed growing interest in adopting the microplate method for widespread use, it remains in the shadow of the standard light transmission aggregometry (LTA). Regardless of the method used, the results of platelet aggregation depend on a variety of factors and often vary among laboratories worldwide...
March 5, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38388810/diagnostic-prognostic-and-therapeutic-potential-of-exosomal-micrornas-in-renal-cancer
#17
REVIEW
Xiaodong Yu, Zhongbo Du, Pingyu Zhu, Bo Liao
Renal cell carcinoma (RCC) arises from the tubular epithelial cells of the nephron. It has the highest mortality rate among urological cancers. There are no effective therapeutic approaches and no non-invasive biomarkers for diagnosis and follow-up. Thus, suitable novel biomarkers and therapeutic targets are essential for improving RCC diagnosis/prognosis and treatment. Circulating exosomes such as exosomal microRNAs (Exo-miRs) provide non-invasive prognostic/diagnostic biomarkers and valuable therapeutic targets, as they can be easily isolated and quantified and show high sensitivity and specificity...
February 22, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38273183/safety-of-non-standard-regimen-of-systemic-steroid-therapy-in-patients-with-graves-orbitopathy-a-single-centre-experience
#18
JOURNAL ARTICLE
Nadia Sawicka-Gutaj, Dawid Gruszczyński, Natalia Zawalna, Kacper Nijakowski, Agnieszka Skiba, Mateusz Pochylski, Jerzy Sowiński, Marek Ruchała
BACKGROUND: Graves' orbitopathy (GO) is an autoimmune disorder of the orbit and retro-ocular tissues and the primary extrathyroidal manifestation of Graves' disease. In moderate-to-severe and active GO iv glucocorticoids (GCs) are recommended as first-line treatment. The aim was to assess the safety profile of methylprednisolone administered intravenously for three consecutive days at 1 g in patients with active, moderate-to-severe or sight-threatening Graves' orbitopathy. METHODS: We retrospectively evaluated 161 medical records of patients with GO treated with high-dose systemic GCs in the Department of Endocrinology, Metabolic Disorders, and Internal Medicine in Poznań between 2014 and 2021...
January 26, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38236555/the-role-of-bidirectional-communication-between-the-adipokines-and-the-endogenous-opioid-system-in-an-experimental-mouse-model-of-colitis-associated-colorectal-cancer
#19
JOURNAL ARTICLE
Agata Szymaszkiewicz, Mikołaj Mierzejewski, Emilia Januszkiewicz, Weronika Machelak, Marcin Talar, Jakub Włodarczyk, Mikołaj Świerczyński, Radzisław Kordek, Jakub Fichna, Marta Zielińska
BACKGROUND: Colorectal cancer (CRC) is one of the leading causes of death globally. Multiple factors may contribute to the pathogenesis of CRC, including the abnormalities in the functioning of the endogenous opioid system (EOS) or adiponectin-related signaling. The aim of our study was to evaluate if differences in the expression of opioid receptors (ORs) influence the development of CRC and if modulation of adiponectin receptors using AdipoRon, a selective AdipoR1 receptor agonist, affects colorectal carcinogenesis...
January 18, 2024: Pharmacological Reports: PR
https://read.qxmd.com/read/38214881/reno-protective-effect-of-protocatechuic-acid-is-independent-of-sex-related-differences-in-murine-model-of-uuo-induced-kidney-injury
#20
JOURNAL ARTICLE
Karim M Saad, Évila Lopes Salles, Sahar Emami Naeini, Babak Baban, Marwa E Abdelmageed, Rania R Abdelaziz, Ghada M Suddek, Ahmed A Elmarakby
BACKGROUND: Obstructive nephropathy is a condition often caused by urinary tract obstruction either anatomical (e.g., tumors), mechanical (e.g., urolithiasis), or compression (e.g., pregnancy) and can progress to chronic kidney disease (CKD). Studies have shown sexual dimorphism in CKD, where males were found to have a more rapid decline in kidney function following kidney injury compared to age-matched females. Protocatechuic acid (PCA), an anti-oxidant and anti-inflammatory polyphenolic compound, has demonstrated promising effects in mitigating drug-induced kidney injuries...
January 12, 2024: Pharmacological Reports: PR
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