{"title":"Radiolabeled HER2-targeted molecular probes in breast cancer imaging: current knowledge and future prospective.","authors":"Fatemeh Movahed, Ouldouz Navaei, Shiva Taghlidi, Maryam Nurzadeh, Maryam Eslami Gharaati, Maryam Rabiei","doi":"10.1007/s00210-024-03691-7","DOIUrl":"https://doi.org/10.1007/s00210-024-03691-7","url":null,"abstract":"<p><p>Breast cancer is the most frequent non-dermatologic malignancy in women. Breast cancer is characterized by the expression of the human epidermal growth factor receptor type 2 (HER2), and the presence or lack of estrogen receptor (ER) and progesterone receptor (PR) expression. HER2 overexpression is reported in about 20 to 25% of breast cancer patients, which is usually linked to cancer progression, metastases, and poor survival. Immunohistochemistry (IHC) and fluorescence in situ hybridization (FISH) are the gold standards for determining HER2 status, even though IHC has largely focused on quantifying HER2<sup>+</sup> status versus \"other\" HER2 status (including variants with low or no expression). Recent findings regarding the beneficial therapeutic effects of anti-HER2 monoclonal antibodies (mAb) in HER2<sup>low</sup> metastatic patients lead to changes in the classic definition of advanced breast cancer, and methods for precise assessment of HER2 status are being developed. As a result, various radiolabeled HER-targeted mAbs and antibody fragments have been designed to avoid repeated biopsies with potential bias due to tumor heterogeneity, including single-chain variable fragment (scFv), F(ab')2, affibody, and nanobody. These small targeting radiotracers displayed favorable biodistributions, clearance, and stability, allowing for higher image quality, shorter circulation half-life, and lower immunogenicity. This study aimed to comprehensively review the application of radiolabeled anti-HER2 antibody fragments in breast cancer in vivo imaging and provide a better understanding of targeted HER2 quantification.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142922034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jaka Fadraersada, Raúl Alva-Gallegos, Pavel Skořepa, František Musil, Kristýna Mrštná, Lenka Javorská, Kateřina Matoušová, Lenka Kujovská Krčmová, Markéta Paclíková, Alejandro Carazo, Milan Bláha, Vladimír Blaha, Přemysl Mladěnka
{"title":"Coagulation in familial hypercholesterolemic patients: effect of current hypolipidemic treatment and anticoagulants.","authors":"Jaka Fadraersada, Raúl Alva-Gallegos, Pavel Skořepa, František Musil, Kristýna Mrštná, Lenka Javorská, Kateřina Matoušová, Lenka Kujovská Krčmová, Markéta Paclíková, Alejandro Carazo, Milan Bláha, Vladimír Blaha, Přemysl Mladěnka","doi":"10.1007/s00210-024-03740-1","DOIUrl":"https://doi.org/10.1007/s00210-024-03740-1","url":null,"abstract":"<p><p>Familial hypercholesterolemia (FH) is a relatively rare genetic disease associated with high serum cholesterol levels but also with abnormalities in blood coagulation. Novel pharmacotherapeutic approaches in FH including proprotein convertase subtilisin/kexin type 9 antibodies (PCSK9Ab) are very efficient in decreasing cholesterol levels but their impact on coagulation in FH is not yet established. Therefore, we hypothesized that these novel antidyslipidemic drugs can positively impact blood coagulation due to their more potent effect on cholesterol. A total of 15 healthy volunteers and all 15 available patients with severe FH treated at the University Hospital Hradec Králové were enrolled, coagulation was assessed by mechanic coagulometer, and the impact of four clinically used direct anticoagulants was analyzed ex vivo. FH patients were treated effectively as their total cholesterol was 4.11 ± 1.57 mM and LDL cholesterol was 2.44 ± 1.46 mM, which were even lower values than detected in our generally healthy controls. Twelve from the 15 FH patients were finally analyzed as 3 were treated with anticoagulants. Coagulation in FH patients was prolonged more extensively by dabigatran and rivaroxaban, when compared to healthy controls. Treatment with PCSK9Ab or lipid apheresis did not seem to have a significant effect on coagulation. The latter procedure however significantly decreased serum levels of one vitamin K form, MK4. Shorter coagulation time was associated with higher levels of LDL, non-HDL, and total cholesterol. Current treatment of FH seems to improve the effects of direct anticoagulants beyond known effects on LDL cholesterol levels.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142921945","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Echinatin inhibits osteoarthritis through the NF-κB signaling pathway.","authors":"Peng Zhan, Shiming Huang, Daohua Chen, Ying Li, Dongfeng Chen","doi":"10.1007/s00210-024-03756-7","DOIUrl":"https://doi.org/10.1007/s00210-024-03756-7","url":null,"abstract":"<p><p>Osteoarthritis (OA) is currently the most common degenerative joint disease in China and even worldwide and is the leading cause of disability in the elderly population. So far, due to an insufficient understanding of the pathogenesis and etiology of the disease, there is still no effective targeted treatment for early OA. Pro-inflammatory cytokine interleukin-1 is an important inflammatory mediator secreted in early OA, and IL-1β plays a crucial role in the pathogenesis of OA, affecting chondrocytes and the extracellular matrix of CARTILAGE. Echinatin has been used for years as a health supplement, retaining its antioxidant, anti-inflammatory, and autophagy-promoting effects. However, whether echinatin has inhibitory effects on OA is still unknown. In this study, we used an in vitro OA model of chondrocytes induced by IL-1β and an in vivo OA model of rats induced by anterior cruciate ligament transection (ACLT), and through experiments such as western blotting and IHC, we demonstrated that echinatin can be used as a novel drug for treating OA. Mechanistically, we found that echinatin inhibits the activity of chondrocytes induced by IL-1β through the NF-kB signaling pathway. This study can provide more effective treatment options for OA patients and further diagnostic and therapeutic methods for clinical treatment.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142922025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mohammad Abbas Bejeshk, Hamid Najafipour, Mohammad Khaksari, Mohammad Hadi Nematollahi, Mohammad Amin Rajizadeh, Tania Dehesh, Fatemeh Bagheri, Gholamreza Sepehri
{"title":"Myrtenol-loaded niosomes can prevent lung ischemia-reperfusion injury model in rats by balancing the Nrf2/Keap1 and NF-κB signaling pathways.","authors":"Mohammad Abbas Bejeshk, Hamid Najafipour, Mohammad Khaksari, Mohammad Hadi Nematollahi, Mohammad Amin Rajizadeh, Tania Dehesh, Fatemeh Bagheri, Gholamreza Sepehri","doi":"10.1007/s00210-024-03748-7","DOIUrl":"https://doi.org/10.1007/s00210-024-03748-7","url":null,"abstract":"<p><p>Lung Ischemia-reperfusion injury (LIRI) is a risk during lung transplantation that can cause acute lung injury and organ failure. In LIRI, the NF-E2-related factor 2(Nrf2)/ Kelch-like ECH-associated protein 1 (Keap1) signaling pathway and the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling pathway are two major pathways involved in regulating oxidative stress and inflammation, respectively. Myrtenol, a natural compound with anti-inflammatory and antioxidant properties, has potential protective effects against IRI. This study aimed to explore the impact of myrtenol encapsulated within niosomes on the prevention of LIRI and examine the role of the two pathways mentioned in this process. Wistar rats were segregated into four groups. Animals received the myrtenol (MN) (32 mg/kg) or vehicle through daily inhalation for a week before LIRI. Expression of IκB, p-IκB, Nrf2, Keap1, Heme Oxygenase-1(HO-1), NF-κB signaling proteins, reactive oxygen species (ROS) level, caspase-3 expression, arterial blood gases, lung edema, and histopathological indices were assessed. Niosomal myrtenol significantly reduced lung edema, ROS, Keap1, p-IκB, NF-kB, Caspase-3, PaCO2 (the carbon dioxide pressure in arterial blood), and histopathological indices. Additionally, the expression of IκB, Nrf2, HO-1, and PaO2 (the oxygen pressure in arterial blood) increased significantly in the pretreated group compared to the IR group. Overall, inhalation of the niosomal myrtenol protects against lung ischemia-reperfusion injury, presumably through the balance between Nrf2/Keap1 and NF-κB pathways. The findings suggest that the niosomal form of myrtenol may be a potential candidate for developing new drugs to prevent and treat LIR damage.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142922031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Diosmin induces mitochondrial-mediated apoptosis and anti-inflammatory effects in Hep-2 cells: an integrated in vitro and in silico analysis.","authors":"Muthusamy Rajasekar, Kathiresan Suresh, Azhamuthu Theerthu, Ravichandran Pugazhendhi, Kathiresan Sivakumar","doi":"10.1007/s00210-024-03690-8","DOIUrl":"https://doi.org/10.1007/s00210-024-03690-8","url":null,"abstract":"<p><p>The present study aims to explore the anticancer efficacy of Diosmin by inducing mitochondrial-mediated apoptosis in human epidermoid carcinoma cells (Hep-2). This is done by cell line assays and studying crucial inflammatory and apoptotic signaling molecules. The cytotoxicity property of Diosmin was evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Marker expression study was done by western blotting for studying apoptotic markers like Bax, Bcl-2, p53, Bak, and Bcl-xl, proinflammatory cytokine (TNF-α), interleukins (IL-1, IL-6, IL-8), and signal transduction (STAT-3). The docking study confirms the affinity of Diosmin with apoptotic and important markers. Through the MTT assay, a dose-dependent cytotoxic effect of Diosmin was unveiled, with an IC<sub>50</sub> value of effective inhibition of cell proliferation. Diosmin treatment resulted in noteworthy downregulation of Bcl-xl, Bak, Bcl-2, IL-1, 6, 8, TNF-α, and STAT-3 while upregulating the p53 and Bax expression levels, highlighting its inhibitory role in inducing apoptosis. Docking studies further exposed robust binding affinities between Diosmin and target apoptotic proteins, suggesting its efficacy in disrupting cellular functions and inflammatory signaling pathways in Hep-2 cells. The cytotoxic effects on Hep-2 cells and suggested activation of Bax, p53, and inhibition of Bcl-xl, Bak, Bcl-2, IL-1, 6, 8, TNF-α, as well as STAT-3 lead to the activation of mitochondrial-mediated apoptosis in Diosmin-treated Hep-2 cells. Further, its anti-inflammatory properties locate Diosmin as a conclusive compound for further studies for effective oral and other related squamous carcinoma treatments.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142921949","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Network pharmacology and molecular docking to explore the potential mechanism of chlorogenic acid in septic acute liver injury and experimental validation of TLR4/NF-κB pathway in vivo.","authors":"Shangping Fang, Hui Su, Jiameng Liu, Kecheng Zhai, Yangmengna Gao, Yu Xiang, Huan Li, Renke Sun, Huixian Cheng","doi":"10.1007/s00210-024-03712-5","DOIUrl":"https://doi.org/10.1007/s00210-024-03712-5","url":null,"abstract":"<p><p>The objective of this study was to investigate the biological activities and mechanisms of chlorogenic acid (CGA) in the treatment of septic acute liver injury (SALI) based on the network pharmacology, molecular docking, in vivo studies, and other techniques. Chlorogenic acid and potential related targets of septic acute liver injury were searched from the public databases. Then, the protein-protein interaction (PPI), Gene Ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted. Subsequently, molecular docking was performed to predict the binding of the active compound to the core target. Finally, in vivo experiments were carried out for further validation. A total of 60 common targets were identified between acute septic liver injury and chlorogenic acid, among which 9 common core targets (EGFR, ESR1, GSK3B, PTGS2, TLR4, PPARA, HSP90AA1, ACE, and MMP9) were screened with Cytoscape. Molecular docking indicated that these core targets had good binding activity to chlorogenic acid (- 7.2, - 6.8, - 7.7, - 8.7, - 6.1, - 6.8, - 7.3, - 8.4, and - 8.6 kcal/mol respectively). In the SALI mouse model, chlorogenic acid can improve pathological damage to the liver and apoptosis of liver cells, and anti-inflammatory properties significantly by the TLR4/NF-κB pathway (all P < 0.05). The biological activity and regulatory network of CGA on SALI were revealed, and the anti-inflammatory effect of CGA was verified, which could be associated with the TLR4/NF-κB pathway.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142922032","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Mercuric chloride induced reproductive toxicity associated with oxidative damage in male Wistar albino rat, Rattus norvegicus.","authors":"M P Sampada, Muniswamy David","doi":"10.1007/s00210-024-03585-8","DOIUrl":"https://doi.org/10.1007/s00210-024-03585-8","url":null,"abstract":"<p><p>In the field of toxicology, male reproductive hazards attributed to metal exposure is a fast-developing issue. Mercury has been identified as an environmental pollutant that causes potential adverse impacts on organisms. This study aimed to assess the reprotoxic consequences of mercuric chloride (HgCl<sub>2</sub>). Five groups of sexually mature albino rats were given oral mercuric chloride (HgCl<sub>2</sub>) treatment. (G1) control group received saline treatment; (G2) (5.25 mg/kg of HgCl<sub>2</sub> for 30 days); (G3) (5.25 mg/kg of HgCl<sub>2</sub> for 60 days); (G4) (10.5 mg/kg of HgCl<sub>2</sub> for 30 days); (G5) (10.5 mg/kg of HgCl<sub>2</sub> for 60 days). The hormonal levels, sperm count, sperm motility, sperm viability, and reproductive organ weight, including body weight, were substantially reduced, whereas the sperm abnormality rate was enhanced in rat groups treated with HgCl<sub>2</sub>. The analysis revealed that the effect size (Cohen's d) for sperm parameters, including sperm count, motility and viability, were extremely high across all groups, except for sperm abnormality in group 2 (d = 0.59) and group 3 (d = 0.18), where moderate and small effect sizes were observed respectively, and this suggests a significant impact of the intervention on sperm parameters. The administration of HgCl<sub>2</sub> resulted in the induction of oxidative stress in testis that is manifested by substantially enhanced lipid peroxidation (MDA) with a substantial decrease in activity of antioxidant enzymes like catalase (CAT), superoxide dismutase (SOD), reduced glutathione (GSH), and glutathione peroxidase (GPx) in testes of mercury-treated groups. Concomitantly, there was downregulation in the mRNA levels of the genes involved in spermatogenesis, namely Hsp-70, insulin-like growth factor (IGF), glutathione-S-transferase, and p53 in the testis. The expression of antiapoptotic protein B cell lymphoma (Bcl-2) was decreased, and conversely, the expression of cell proliferative protein Ki-67 was increased in a dose- and duration-dependent manner. Histopathological studies showed degenerative changes in the testis, epididymis, prostate gland, and seminal vesicle, compared to the control group. All the evidence suggests that after mercury exposure, there may be an imbalance between the body's defenses against free radicals and antioxidants, making the testis more susceptible to oxidative damage. This imbalance could potentially have a detrimental effect on the function of the male reproductive system.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2024-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142910001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Targeted delivery of chrysin and 5-fluorouracil on MDA-MB-231 cancer cells by a peptide-functionalized L-DOPA-imprinted polymer.","authors":"Sedighe Yosefi, Majid Sirati-Sabet, Abbas Pakdel, Zahra Nabizadeh, Parviz Kokhaei, Hamid Madanchi","doi":"10.1007/s00210-024-03750-z","DOIUrl":"https://doi.org/10.1007/s00210-024-03750-z","url":null,"abstract":"<p><p>Triple-negative breast cancer (TNBC) is a very aggressive and deadly form of breast cancer for which chemotherapy is the only systemic treatment option. Therefore, novel and more effective targeted or combined therapies, such as specific drug delivery systems that selectively target cancer cells, have received much attention. This research aimed to investigate the effect of targeted delivery of chrysin (CH) and 5-fluorouracil (5FU) using polymer nanoparticles on MDA-MB-231 cells. In this regard, CH and 5FU were individually used as the template to polymerize L-DOPA on the surface of silica nanoparticles. Then, a CD138-targeting peptide was designed for the first time and immobilized on the surface of the polymeric nanocomposite to target TNBC. The results showed that poly(L-DOPA)-CH-peptide and poly(L-DOPA)-5FU-peptide are selective for MDA-MB-231 cells and deliver drugs to them in a targeted manner. In this study, peptide-containing nanocomposites targeting CD138 were more successful in reducing cell proliferation than peptide-free nanocomposites. Also, they increased apoptosis and cell cycle arrest in MDA-MB-231 cancer cells in vitro. The effective and targeted delivery of CH and 5FU to MDA-MB-231 cancer cells by the designed interference peptide in this study can promise an effective treatment method for inhibiting the growth and progression of cancer. However, animal studies are needed to understand the efficacy of the interfering peptide and the final designed construct.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2024-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142910058","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Trace amine-associated receptor 1 (TAAR1): an emerging therapeutic target for neurodegenerative, neurodevelopmental, and neurotraumatic disorders.","authors":"Saher Dalvi, Lokesh Kumar Bhatt","doi":"10.1007/s00210-024-03757-6","DOIUrl":"https://doi.org/10.1007/s00210-024-03757-6","url":null,"abstract":"<p><p>Trace amines are physiologically active amines present in all organisms. They are structurally identical to traditional monoamines and are rapidly metabolized by monoamine oxidases. The mammalian neurological system generates these molecules at rates equivalent to traditional monoamines, but because of their short half-life, they are only observable in trace quantities. Their receptors are G protein-coupled receptors present in both the CNS and peripheral locations, with trace amine-associated receptor 1 (TAAR1) being the most researched. TAAR1's capacity to regulate glutamatergic and monoaminergic neurotransmission has made it a viable therapeutic target for neuropsychiatric illnesses. Although the TAAR1 role in schizophrenia and other neuropsychiatric disorders is well established, its role in the pathology of neurodegenerative and neurotraumatic disorders recently got attention. This review discusses the role of TAAR1 in neurodegenerative, neurodevelopment, and neurotraumatic disorders and explores its potential to be a novel therapeutic target in these disorders.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2024-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142910026","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tia Okselni, Abdi Wira Septama, Dian Juliadmi, Rizna Triana Dewi, Marissa Angelina, Tri Yuliani, Grace Serepina Saragih, Ariyanti Saputri
{"title":"Quercetin as a therapeutic agent for skin problems: a systematic review and meta-analysis on antioxidant effects, oxidative stress, inflammation, wound healing, hyperpigmentation, aging, and skin cancer.","authors":"Tia Okselni, Abdi Wira Septama, Dian Juliadmi, Rizna Triana Dewi, Marissa Angelina, Tri Yuliani, Grace Serepina Saragih, Ariyanti Saputri","doi":"10.1007/s00210-024-03722-3","DOIUrl":"https://doi.org/10.1007/s00210-024-03722-3","url":null,"abstract":"<p><p>Quercetin is abundant in plants and has notable pharmacological properties for skin health. This review aims to comprehensively evaluate the effects of quercetin on skin-related issues, adhering to the PRISMA guidelines and analyzing studies from ScienceDirect, Web of Science, Scopus, and PubMed. Of the 1,398 studies identified, 65 studies met the criteria for meta-analysis. The meta-analysis indicated that quercetin had powerful antioxidant properties, protecting against oxidative stress by significantly lowering levels of MDA (Z-score, 2.51), ROS (Z-score, 3.81), and LPO (Z-score, 4.46), and enhancing enzymes of GSH (Z-score, 5.46), CAT (Z-score, 5.20), and SOD (Z-score, 4.37). Quercetin acted as an anti-inflammatory by significantly suppressing protein regulators such as NF-κβ, AP-1, and MAPKs (ERK and JNK), cytokines of TNFα, IL-6, IL-1β, IL-8, and MCP-1, and enzymes of COX-2, iNOS, and MPO, while upregulating the cytokine IL-10. Additionally, quercetin significantly suppressed IL-4 (Z-score, 3.16) and IFNγ (Z-score, 3.76) cytokines involved in chronic inflammation of atopic dermatitis. Quercetin also supported wound healing by significantly decreasing inflammatory cells (Z-score, 5.60) and enhancing fibroblast distribution (Z-score, 5.98), epithelialization (Z-score, 8.57), collagen production (Z-score, 4.20), and angiogenesis factors of MVD (Z-score, 5.66) and VEGF (Z-score, 3.86). Furthermore, quercetin significantly inhibited tyrosinase activity (Z-score, 1.95), resulting in a significantly reduced melanin content (Z-score, 2.56). A significant reduction in DNA damage (Z-score, 3.27), melanoma cell viability (Z-score, 2.97), and tumor formation was also observed to ensure the promising activity of quercetin for skin issues. This review highlights quercetin's potential as a multifaceted agent in skin care and treatment.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":""},"PeriodicalIF":3.1,"publicationDate":"2024-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142910050","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}