Medicines (Basel, Switzerland)最新文献

{"title":"Gabapentin-Associated Movement Disorders: A Literature Review.","authors":"Jamir Pitton Rissardo,&nbsp;Ursula Medeiros Araujo de Matos,&nbsp;Ana Letícia Fornari Caprara","doi":"10.3390/medicines10090052","DOIUrl":"https://doi.org/10.3390/medicines10090052","url":null,"abstract":"<p><strong>Background: </strong>Gabapentin (GBP)-induced movement disorders (MDs) are under-recognized adverse drug reactions. They are commonly not discussed with patients, and their sudden occurrence can lead to misdiagnosis. This literature review aims to evaluate the clinical-epidemiological profile, pathological mechanisms, and management of GBP-associated MD.</p><p><strong>Methods: </strong>Two reviewers identified and assessed relevant reports in six databases without language restriction between 1990 and 2023.</p><p><strong>Results: </strong>A total of 99 reports of 204 individuals who developed a MD associated with GBP were identified. The MDs encountered were 135 myoclonus, 22 dyskinesias, 7 dystonia, 3 akathisia, 3 stutterings, 1 myokymia, and 1 parkinsonism. The mean and median ages were 54.54 (SD: 17.79) and 57 years (age range: 10-89), respectively. Subjects were predominantly male (53.57%). The mean and median doses of GBP when the MD occurred were 1324.66 (SD: 1117.66) and 1033 mg/daily (GBP dose range: 100-9600), respectively. The mean time from GBP-onset to GBP-associated MD was 4.58 weeks (SD: 8.08). The mean recovery time after MD treatment was 4.17 days (SD: 4.87). The MD management involved GBP discontinuation. A total of 82.5% of the individuals had a full recovery in the follow-up period.</p><p><strong>Conclusions: </strong>Myoclonus (GRADE A) and dyskinesia (GRADE C) were the most common movement disorders associated with GBP.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10536490/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41158765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Histological Alterations in Hashimoto's Disease: A Case-Series Ultrastructural Study.","authors":"Eleni Avramidou,&nbsp;Antonios Gkantaras,&nbsp;Iasonas Dermitzakis,&nbsp;Konstantinos Sapalidis,&nbsp;Maria Eleni Manthou,&nbsp;Paschalis Theotokis","doi":"10.3390/medicines10090051","DOIUrl":"https://doi.org/10.3390/medicines10090051","url":null,"abstract":"<p><strong>Background: </strong>Hashimoto's thyroiditis (HT) is an autoimmune disease exhibiting stromal fibrosis and follicular cell destruction due to lymphoplasmacytic infiltration. Besides deprecated analyses, histopathological approaches have not employed the use of electron microscopy adequately toward delineating subcellular-level interactions.</p><p><strong>Methods: </strong>Biopsies for ultrastructural investigations were obtained from the thyroids of five patients with HT after a thyroidectomy. Transmission electron microscopy (TEM) was utilized to study representative tissue specimens.</p><p><strong>Results: </strong>Examination indicated interstitial extravasated blood cells and a plethora of plasma cells, based on their subcellular identity landmarks. These antibody-secreting cells were profoundly spotted near follicular cells, fibroblasts, and cell debris entrenched in collagenous areas. Pathological changes persistently affected subcellular components of the thyrocytes, including the nucleus, endoplasmic reticulum (ER), Golgi apparatus, mitochondria, lysosomes, and other intracellular vesicles. Interestingly, significant endothelial destruction was observed, specifically in the larger blood vessels, while the smaller vessels appeared comparatively unaffected.</p><p><strong>Conclusions: </strong>Our TEM findings highlight the immune-related alterations occurring within the thyroid stroma. The impaired vasculature component and remodeling have not been described ultrastructurally before; thus, further exploration is needed with regards to angiogenesis in HT in order to achieve successful prognostic, diagnostic, and treatment-monitoring strategies.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10534781/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41165030","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Collagen Hydrolysates: A Source of Bioactive Peptides Derived from Food Sources for the Treatment of Osteoarthritis.","authors":"Christina E Larder,&nbsp;Michèle M Iskandar,&nbsp;Stan Kubow","doi":"10.3390/medicines10090050","DOIUrl":"https://doi.org/10.3390/medicines10090050","url":null,"abstract":"<p><p>Osteoarthritis (OA) is the most common joint disorder, with a social and financial burden that is expected to increase in the coming years. Currently, there are no effective medications to treat it. Due to limited treatment options, patients often resort to supplements, such as collagen hydrolysates (CHs). CHs are products with low molecular weight (MW) peptides, often between 3 and 6 kDa, and are a result of industrialized processed collagen. Collagen extraction is often a by-product of the meat industry, with the main source for collagen-based products being bovine, although it can also be obtained from porcine and piscine sources. CHs have demonstrated positive results in clinical trials related to joint health, such as decreased joint pain, increased mobility, and structural joint improvements. The bioactivity of CHs is primarily attributed to their bioactive peptide (BAP) content. However, there are significant knowledge gaps regarding the digestion, bioavailability, and bioactivity of CH-derived BAPs, and how different CH products compare in that regard. The present review discusses CHs and their BAP content as potential treatments for OA.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10538231/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41170589","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Somatosensory Auras in Epilepsy: A Narrative Review of the Literature.","authors":"Ana Leticia Fornari Caprara,&nbsp;Hossam Tharwat Ali,&nbsp;Ahmed Elrefaey,&nbsp;Sewar A Elejla,&nbsp;Jamir Pitton Rissardo","doi":"10.3390/medicines10080049","DOIUrl":"https://doi.org/10.3390/medicines10080049","url":null,"abstract":"<p><p>An aura is a subjective experience felt in the initial phase of a seizure. Studying auras is relevant as they can be warning signs for people with epilepsy. The incidence of aura tends to be underestimated due to misdiagnosis or underrecognition by patients unless it progresses to motor features. Also, auras are associated with seizure remission after epilepsy surgery and are an important prognostic factor, guiding the resection site and improving surgical outcomes. Somatosensory auras (SSAs) are characterized by abnormal sensations on one or more body parts that may spread to other parts following a somatotopic pattern. The occurrence of SSAs among individuals with epilepsy can range from 1.42% to 80%. The upper extremities are more commonly affected in SSAs, followed by the lower extremities and the face. The most common type of somatosensory aura is paresthetic, followed by painful and thermal auras. In the primary somatosensory auras, sensations occur more commonly contralaterally, while the secondary somatosensory auras can be ipsilateral or bilateral. Despite the high localizing features of somatosensory areas, cortical stimulation studies have shown overlapping sensations originating in the insula and the supplementary sensorimotor area.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10456342/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10101866","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Clinical Effectiveness of Mirogabalin Besylate for Trigeminal Neuropathy after Skull Base Surgery: Illustrative Cases.","authors":"Kosuke Karatsu,&nbsp;Ryota Tamura,&nbsp;Tsubasa Miyauchi,&nbsp;Junki Sogano,&nbsp;Utaro Hino,&nbsp;Takashi Iwama,&nbsp;Masahiro Toda","doi":"10.3390/medicines10080048","DOIUrl":"https://doi.org/10.3390/medicines10080048","url":null,"abstract":"<p><strong>Background: </strong>Postoperative trigeminal neuropathy may be seen after surgery for middle and posterior cranial fossa lesions. Although neuropathic pain is a cause of reduced quality of life, global consensus on postoperative pain management is lacking. Mirogabalin besylate is a selective ligand for the α2δ subunit of voltage-gated calcium channels. Although mirogabalin has been used for patients with postherpetic neuralgia and painful diabetic peripheral neuropathy, few reports have assessed the effect on postsurgical neuropathy. In this report, we describe a clinical effectiveness of mirogabalin for trigeminal neuropathy after skull base surgery.</p><p><strong>Case description: </strong>Case 1: A 51-year-old female with right trigeminal schwannoma was operated on via the anterior transpetrosal approach. She had tingling and numb feelings in the right face postoperatively. Mirogabalin was orally administered after the operation. Her continuous facial numbness immediately improved. Case 2: A 55-year-old female with left middle fossa base meningioma extending into the infratemporal fossa was operated on via the infratemporal fossa approach. She had a tingling feeling in the left face postoperatively. Mirogabalin was orally administered for this symptom after the operation, which gradually improved.</p><p><strong>Conclusions: </strong>Mirogabalin may show significant pain relief for patients with trigeminal neuropathy after skull base surgery. Further studies using a larger number of patients are warranted to confirm these findings.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10456499/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10106920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Spectrum of Thyroid Dysfunction in Patients with Chronic Kidney Disease in Benin City, Nigeria.","authors":"John O Obasuyi,&nbsp;Mathias A Emokpae","doi":"10.3390/medicines10080047","DOIUrl":"https://doi.org/10.3390/medicines10080047","url":null,"abstract":"<p><p>There is an indication of abrupt rise in chronic kidney disease (CKD) in Nigeria and thyroid function involvement has not been sufficiently evaluated. This study determined thyroid gland function among subjects with CKD in Benin City, Nigeria. A total of 184 randomized CKD patients attending specialist clinic and 80 healthy control subjects were recruited for this study. A well-structured questionnaire was used to obtain data on socio-demography. Blood specimens were collected and used for the determination of thyroid function parameters; thyroid stimulating hormone (TSH), triiodothyronine (T3), free triiodothyronine (fT3), thyroxine (T4), free thyroxine (fT4), thyroid peroxidase antibody (TPO-Abs), thyroid globulin antibody (Tg-Abs) and Deiodinase enzyme Type 1 (D1). SPINA GD and SPINA GT were calculated using Michaelis-Menten model. The CKD was classified into stages using Modification of Drug in Renal Disease (MDRD) formula. Thyroid dysfunctions observed were clinical hyperthyroidism 1 (0.54%), non-thyroidal illness 78 (42.4%), clinical hypothyroidism 11 (6.0%), sub-clinical hyperthyroidism 3 (1.60%), and sub-clinical hypothyroidism 11 (6.0%), while euthyroid were 80 (43.5%). SPINA GD of CKD patients (33.85 ± 10.94) was not significantly different when compared with controls (24.85 ± 1.57), whereas, SPINA GT was significantly higher (<i>p</i> < 0.01) among CKD patients (3.74 ± 0.31) than controls (2.68 ± 0.11). Autoimmune thyroid disease demonstrated by positive Tg-Abs and TPO-Abs were observed among approximately 7.9% of CKD patients. Serum TPO-Abs concentration increased with CKD progression. Thyroid dysfunction is involved in the pathogenesis of CKD patients. The etiologies are multifactorial and immunological mechanisms of autoimmune thyroid disease may be a contributing factor.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10456670/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10106923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Contrast-Induced Encephalopathy in Patients with Chronic Kidney Disease and End-Stage Kidney Disease: A Systematic Review and Meta-Analysis.","authors":"Paul W Davis,&nbsp;Pajaree Krisanapan,&nbsp;Supawit Tangpanithandee,&nbsp;Charat Thongprayoon,&nbsp;Jing Miao,&nbsp;Mohamed Hassanein,&nbsp;Prakrati Acharya,&nbsp;Michael A Mao,&nbsp;Iasmina M Craici,&nbsp;Wisit Cheungpasitporn","doi":"10.3390/medicines10080046","DOIUrl":"https://doi.org/10.3390/medicines10080046","url":null,"abstract":"<p><p><b>Background:</b> Contrast-induced encephalopathy (CIE) is an infrequent but serious neurological condition that occurs shortly after the administration of contrast during endovascular and angiography procedures. Patients suffering from chronic kidney disease (CKD) or end-stage kidney disease (ESKD) are considered to be at a higher risk of contrast medium neurotoxicity, due to the delayed elimination of the contrast medium. However, the occurrence and characteristics of CIE in CKD/ESKD patients have not been extensively investigated. <b>Methods:</b> We conducted a comprehensive literature search, utilizing databases such as MEDLINE, EMBASE, the Cochrane Central Register of Controlled Trials, and the Cochrane Database of Systematic Reviews, up to September 2022. The purpose was to identify documented cases of CIE among patients with CKD or ESKD. Employing a random-effects model, we calculated the pooled incidence and odds ratio (OR) of CIE in CKD/ESKD patients. <b>Results:</b> Our search yielded a total of eleven articles, comprising nine case reports and two observational studies. Among these studies, 2 CKD patients and 12 ESKD patients with CIE were identified. The majority of the CKD/ESKD patients with CIE (93%) had undergone intra-arterial contrast media and/or endovascular procedures to diagnose acute cerebrovascular disease, coronary artery disease, and peripheral artery disease. The male-to-female ratio was 64%, and the median age was 63 years (with an interquartile range of 55 to 68 years). In the two observational studies, the incidence of CIE was found to be 6.8% in CKD patients and 37.5% in ESKD patients, resulting in a pooled incidence of 16.4% (95% CI, 2.4%-60.7%) among the CKD/ESKD patients. Notably, CKD and ESKD were significantly associated with an increased risk of CIE, with ORs of 5.77 (95% CI, 1.37-24.3) and 223.5 (95% CI, 30.44-1641.01), respectively. The overall pooled OR for CIE in CKD/ESKD patients was 32.9 (95% CI, 0.89-1226.44). Although dialysis prior to contrast exposure did not prevent CIE, approximately 92% of CIE cases experienced recovery after undergoing dialysis following contrast exposure. However, the effectiveness of dialysis on CIE recovery remained uncertain, as there was no control group for comparison. <b>Conclusions:</b> In summary, our study indicates an association between CIE and CKD/ESKD. While patients with CIE showed signs of recovery after dialysis, further investigations are necessary, especially considering the lack of a control group, which made the effects of dialysis on CIE recovery uncertain.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10456913/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10459670","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bridging the Gap between Basic Research and Clinical Practice: The Growing Role of Translational Neurorehabilitation.","authors":"Mirjam Bonanno,&nbsp;Rocco Salvatore Calabrò","doi":"10.3390/medicines10080045","DOIUrl":"https://doi.org/10.3390/medicines10080045","url":null,"abstract":"<p><p>Translational neuroscience is intended as a holistic approach in the field of brain disorders, starting from the basic research of cerebral morphology and with the function of implementing it into clinical practice. This concept can be applied to the rehabilitation field to promote promising results that positively influence the patient's quality of life. The last decades have seen great scientific and technological improvements in the field of neurorehabilitation. In this paper, we discuss the main issues related to translational neurorehabilitation, from basic research to current clinical practice, and we also suggest possible future scenarios.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10456256/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10101865","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intermittent Proton Pump Inhibitor Therapy in Low-Risk Non-Variceal Upper Gastrointestinal Bleeding May Be Significantly Cost-Saving.","authors":"Yang Lei,&nbsp;Jennifer Halasz,&nbsp;Kerri L Novak,&nbsp;Stephen E Congly","doi":"10.3390/medicines10070044","DOIUrl":"https://doi.org/10.3390/medicines10070044","url":null,"abstract":"<p><strong>Background: </strong>High-dose proton pump inhibitor (PPI) therapy, given either intermittently or continuously for non-variceal upper gastrointestinal bleeding (NV-UGIB), is efficacious. Using intermittent PPI for low-risk patients may be cost-saving. Our objective was to estimate the annual cost savings if all low-risk NV-UGIB patients received intermittent PPI therapy.</p><p><strong>Methods: </strong>Patients who presented to hospital in Calgary, Alberta, who received a PPI for NV-UGIB from July 2015 to March 2017 were identified using ICD-10 codes. Patients were stratified into no endoscopy, high-risk, and low-risk lesion groups and further subdivided into no PPI, oral PPI, intermittent intravenous (IV), and continuous IV subgroups. Average length of stay (LOS) in each subgroup and costs were calculated.</p><p><strong>Results: </strong>We identified 4141 patients with NV-UGIBs, (median age 61, 57.4% male). One-thousand two-hundred and thirty-one low-risk patients received continuous IV PPI, with an average LOS of 6.8 days (95% CI 6.2-7.3) versus 4.9 days (95% CI 3.9-5.9) for intermittent IV patients. If continuous IV PPI patients instead received intermittent IV PPI, 3852 patient days and CAD 11,714,390 (2017 CAD)/year could be saved.</p><p><strong>Conclusions: </strong>Using real-world administrative data, we demonstrate that a sizable portion of low-risk patients with NV-UGIB who were given continuous IV PPI if switched to intermittent IV therapy could generate significant potential cost savings.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10384205/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9901004","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Comparative Study of Tumor-Specificity and Neurotoxicity between 3-Styrylchromones and Anti-Cancer Drugs.","authors":"Tomoyuki Abe,&nbsp;Hiroshi Sakagami,&nbsp;Shigeru Amano,&nbsp;Shin Uota,&nbsp;Kenjiro Bandow,&nbsp;Yoshihiro Uesawa,&nbsp;Shiori U,&nbsp;Hiroki Shibata,&nbsp;Yuri Takemura,&nbsp;Yu Kimura,&nbsp;Koichi Takao,&nbsp;Yoshiaki Sugita,&nbsp;Akira Sato,&nbsp;Sei-Ichi Tanuma,&nbsp;Hiroshi Takeshima","doi":"10.3390/medicines10070043","DOIUrl":"https://doi.org/10.3390/medicines10070043","url":null,"abstract":"<p><p><b>Background.</b> Many anti-cancer drugs used in clinical practice cause adverse events such as oral mucositis, neurotoxicity, and extravascular leakage. We have reported that two 3-styrylchromone derivatives, 7-methoxy-3-[(1<i>E</i>)-2-phenylethenyl]-4<i>H</i>-1-benzopyran-4-one (Compound <b>A</b>) and 3-[(1<i>E</i>)-2-(4-hydroxyphenyl)ethenyl]-7-methoxy-4<i>H</i>-1-benzopyran-4-one (Compound <b>B</b>), showed the highest tumor-specificity against human oral squamous cell carcinoma (OSCC) cell lines among 291 related compounds. After confirming their superiority by comparing their tumor specificity with newly synthesized 65 derivatives, we investigated the neurotoxicity of these compounds in comparison with four popular anti-cancer drugs. <b>Methods:</b> Tumor-specificity (TS_M, TS_E, TS_N) was evaluated as the ratio of mean CC₅₀ for human normal oral mesenchymal (gingival fibroblast, pulp cell), oral epithelial cells (gingival epithelial progenitor), and neuronal cells (PC-12, SH-SY5Y, LY-PPB6, differentiated PC-12) to OSCC cells (Ca9-22, HSC-2), respectively. <b>Results:</b> Compounds <b>A</b> and <b>B</b> showed one order of magnitude higher TS_M than newly synthesized derivatives, confirming its prominent tumor-specificity. Docetaxel showed one order of magnitude higher TS_M, but two orders of magnitude lower TS_E than Compounds <b>A</b> and <b>B</b>. Compounds <b>A</b> and <b>B</b> showed higher TS_M, TS_E, and TS_N values than doxorubicin, 5-FU, and cisplatin, damaging OSCC cells at concentrations that do not affect the viability of normal epithelial and neuronal cells. QSAR prediction based on the Tox21 database suggested that Compounds <b>A</b> and <b>B</b> may inhibit the signaling pathway of estrogen-related receptors.</p>","PeriodicalId":74162,"journal":{"name":"Medicines (Basel, Switzerland)","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10386476/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9894476","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}