Journal of Receptors and Signal Transduction最新文献_第6页

SMILES-based QSAR and molecular docking study of xanthone derivatives as α-glucosidase inhibitors. 基于smiles的山酮类α-葡萄糖苷酶抑制剂QSAR与分子对接研究。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-08-12 DOI: 10.1080/10799893.2021.1957932

Shahin Ahmadi, Zohreh Moradi, Ashwani Kumar, Ali Almasirad

{"title":"SMILES-based QSAR and molecular docking study of xanthone derivatives as α-glucosidase inhibitors.","authors":"Shahin Ahmadi, Zohreh Moradi, Ashwani Kumar, Ali Almasirad","doi":"10.1080/10799893.2021.1957932","DOIUrl":"https://doi.org/10.1080/10799893.2021.1957932","url":null,"abstract":"Increasing diabetic population is one of the major health concerns all over the world. Inhibition of α-glucosidase is a clinically proved and attractive strategy to manage diabetes. In this study, robust and reliable QSAR models to predict α-glucosidase inhibitory potential of xanthone derivatives are developed by the Monte Carlo technique. The chemical structures are represented by SMILES notation without any 3D-optimization. The significance of the index of ideality correlation (IIC) with applicability domain (AD) is also studied in depth. The models developed using CORAL software by considering IIC criteria are found to be statistically more significant and robust than simple balance of correlation. The QSAR models are validated by both internal and external validation methods. The promoters of increase and decrease of activity are also extracted and interpreted in detail. The interpretation of developed models explains the role of different structural attributes in predicting the pIC50 of xanthone derivatives as α-glucosidase inhibitors. Based on the results of model interpretation, modifications are done on some xanthone derivatives and 15 new molecules are designed. The α-glucosidase inhibitory activity of novel molecules is further supported by docking studies.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"361-372"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39304983","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Adrenergic receptor behaviors of mesenchymal stem cells obtained from different tissue sources and the effect of the receptor blockade on differentiation. 不同组织来源间充质干细胞肾上腺素能受体行为及受体阻断对分化的影响。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-07-29 DOI: 10.1080/10799893.2021.1957931

Erkan Maytalman, Arash Alizadeh Yegani, Ilknur Kozanoglu, Fazilet Aksu

{"title":"Adrenergic receptor behaviors of mesenchymal stem cells obtained from different tissue sources and the effect of the receptor blockade on differentiation.","authors":"Erkan Maytalman, Arash Alizadeh Yegani, Ilknur Kozanoglu, Fazilet Aksu","doi":"10.1080/10799893.2021.1957931","DOIUrl":"https://doi.org/10.1080/10799893.2021.1957931","url":null,"abstract":"In this study, it was aimed to analyze behavioral changes of adrenergic receptors (ARs) in first three passages and osteogenic/adipogenic differentiation of mesenchymal stem cells (MSCs) derived from placenta fetal membrane (FM) and bone marrow (BM). It was also aimed to evaluate effects of receptor blockade on differentiation. We obtained first three passages of MSCs from placenta and BM samples. For cell identification, the cells were analyzed by flow cytometry using CD34, CD45 and CD3, CD105 antibodies in each passage. The effects of propranolol and phenoxybenzamine at incremental doses were analyzed by MTT. In addition, cell cultures were separately maintained with the blockers or without after second passage. After each passage and differentiation, α1A, α1B, α2A, α2B, β1, β2, β3 AR-mRNA expressions analyzed by RT-qPCR technique. BMP6 and PPARG mRNA expressions only after differentiation and passage 3 were analyzed. A microscopic examination was also performed. Our results showed that AR expression behaviors were different in MSCs obtained from different tissue sources. In particular, α1A-AR and α2A-AR were expressed with considerably high coefficients in differentiation under blocker effect in BM-derived MSCs. No such coefficients were observed in any group of placental MSCs. In addition, it was found that the blockers stimulated adipogenesis in BM-derived MSCs during osteogenic differentiation. MSCs exhibit protein expressions that vary according to source of tissue and differentiation. Given that MSCs from different sources are used for repair and modulation, our study makes implications of this variable expression intriguing in the clinical practice.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"349-360"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/10799893.2021.1957931","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39255185","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

DFT based QSAR study on quinolone-triazole derivatives as antibacterial agents. 基于DFT的喹诺酮-三唑类抗菌药物的QSAR研究。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-10-24 DOI: 10.1080/10799893.2021.1988971

Niloofar Ghasedi, Shahin Ahmadi, Sepideh Ketabi, Ali Almasirad

{"title":"DFT based QSAR study on quinolone-triazole derivatives as antibacterial agents.","authors":"Niloofar Ghasedi, Shahin Ahmadi, Sepideh Ketabi, Ali Almasirad","doi":"10.1080/10799893.2021.1988971","DOIUrl":"https://doi.org/10.1080/10799893.2021.1988971","url":null,"abstract":"QSAR modeling was performed on 39 quinolone-triazole derivatives against gram-positive Staphylococcus aureus and gram-negative Pseudomonas aeruginosa bacteria. The molecular structures were optimized using the DFT/B3LYP method and 6-31 G basis set. Molecular descriptors were extracted using quantum mechanical calculations. The hierarchical cluster analysis was performed for a rational subset division. The initial dataset was divided into calibration and validation sets, and modeling was done by stepwise MLR method for each of the two bacteria. Internal and external validation methods confirmed the robustness and predictability of the obtained models. According to the obtained model for S. aureus (R2 = 0.889, R2ext = 0.938, Q2LOO = 0.853), the four descriptors- partial atomic charges for the N1 atom in triazole and C7 of the quinolone nucleus, 4-carbonyl bond length, and 13C-NMR chemical shift of 3-carboxylic acid- were found to be the descriptors controlling the activity. According to the obtained model for P. aeruginosa (R2 = 0.957, R2ext = 0.923, Q2LOO = 0.909), the O atom's partial charge in carbonyl, LUMO-HOMO energy gap, and logP were found to be the descriptors having the highest correlation with the antibacterial activity. Finally, some new compounds with higher activities were designed and proposed.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"418-428"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39554937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

microRNA-199a downregulation alleviates hyperuricemic nephropathy via the PPARγ/β-catenin axis. microRNA-199a下调通过PPARγ/β-catenin轴缓解高尿酸血症肾病。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-08-25 DOI: 10.1080/10799893.2021.1967392

Peng Du, Ming Chen, Changcai Deng, Chonggui Zhu

{"title":"microRNA-199a downregulation alleviates hyperuricemic nephropathy via the PPARγ/β-catenin axis.","authors":"Peng Du, Ming Chen, Changcai Deng, Chonggui Zhu","doi":"10.1080/10799893.2021.1967392","DOIUrl":"https://doi.org/10.1080/10799893.2021.1967392","url":null,"abstract":"Hyperuricemia always develops into hyperuricemic nephropathy (HN). The role of microRNA (miR) in HN is less studied. We aimed to discuss the role of miR-199a in HN. The expression of miR-199a and PPARγ in renal tissues of HN rats was detected. The targeting relation between miR-199a and PPARγ was verified. The contents of SCr, UA, BUN, and mALB, renal injury-relevant biomarkers were detected, and the pathological changes of renal tissue and renal interstitial fibrosis were observed by histological staining. After miR-199a and PPARγ knockdown, the contents of SCr, BUN, and mALB and renal interstitial fibrosis were estimated. Collectively, overexpression of miR-199a aggravated the renal injury in HN rats. By contrast, inhibition of miR-199a weakened renal injury, as evidenced by decreased contents of SCr, UA, BUN, and mALB, and mitigated renal interstitial fibrosis. miR-199a targeted PPARγ. Silencing of PPARγ upregulated the levels of downstream genes of β-catenin and the contents of SCr, UA, BUN, and mALB and deteriorated renal interstitial fibrosis. Moreover, the silencing of PPARγ blocked the alleviative effects of miR-199a inhibitor on the renal injury. Overall, miR-199a targets PPARγ and activates the β-catenin pathway, thus aggravating HN, which might provide a future target for the treatment of HN.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"373-381"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39341831","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Long noncoding RNA LINC00858 promotes the progression of ovarian cancer via regulating the miR-134-5p/TRIM44 axis. 长链非编码RNA LINC00858通过调控miR-134-5p/TRIM44轴促进卵巢癌的进展。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-08-23 DOI: 10.1080/10799893.2021.1968433

Pengbo Li, Gang Huang

{"title":"Long noncoding RNA LINC00858 promotes the progression of ovarian cancer via regulating the miR-134-5p/TRIM44 axis.","authors":"Pengbo Li, Gang Huang","doi":"10.1080/10799893.2021.1968433","DOIUrl":"https://doi.org/10.1080/10799893.2021.1968433","url":null,"abstract":"Recent studies have shown that many long noncoding RNAs (lncRNAs) are abnormally expressed in ovarian cancer and involved in the pathological progress of ovarian cancer. In the present study, we aimed to investigate the role of lncRNA LINC00858 and the potential mechanism in ovarian cancer. The qRT-PCR was used to measure the expression levels of LINC00858 and miR-134-5p in ovarian cancer tissue specimens and cell lines. Loss-of-function assays were performed to investigate the role of LINC00858 in ovarian cancer. MTT assay was carried out to measure cell proliferation. Transwell assays were performed to determine cell migration and invasion. Biological information analysis and luciferase report gene assay were used to verify potential downstream genes of LINC00858. The xenograft mouse model was established to analyze tumor growth in vivo. Our results showed that LINC00858 was highly expressed in human ovarian cancer tissues and cell lines. Knockdown of LINC00858 inhibited cell proliferation, migration and invasion of SKOV3 cells, and suppressed tumor growth in mouse xenograft models. Mechanistic studies revealed that LINC00858 acted as a sponge of miR-134-5p and then regulated TRIM44 expression in SKOV3 cells. Furthermore, rescue experiments illustrated that inhibition of miR-134-5p restored the inhibitory effects of LINC00858 knockdown on cell proliferation, migration and invasion. TRIM44 overexpression could counteract the inhibitory effects of miR-134-5p mimics on ovarian cancer cells. In conclusion, these findings demonstrated that LINC00858 exerted oncogenic role in ovarian cancer, which was mediated by miR-134-5p/TRIM44 axis. Thus, LINC00858 might be a therapeutic target for the treatment of ovarian cancer.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"382-389"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39336151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Zingerone suppresses proliferation, invasion, and migration of hepatocellular carcinoma cells by the inhibition of MTDH-mediated PI3K/Akt pathway. 姜酮通过抑制mtdh介导的PI3K/Akt通路抑制肝癌细胞的增殖、侵袭和迁移。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-10-13 DOI: 10.1080/10799893.2021.1988970

Jian Fang, Huifen Zhu, Pengcheng Xu, Renya Jiang

{"title":"Zingerone suppresses proliferation, invasion, and migration of hepatocellular carcinoma cells by the inhibition of MTDH-mediated PI3K/Akt pathway.","authors":"Jian Fang, Huifen Zhu, Pengcheng Xu, Renya Jiang","doi":"10.1080/10799893.2021.1988970","DOIUrl":"https://doi.org/10.1080/10799893.2021.1988970","url":null,"abstract":"Purpose: Previous studies have proved that zingerone was a therapeutic agent for many tumors. Metadherin (MTDH) acts as an oncogene and is involved in tumorigenesis. The purpose of this study was to explore the underlying mechanism of zingerone that regulates MTDH to affect hepatocellular carcinoma (HCC) progression.Methods: CCK-8 assay was performed to detect HCC cell proliferation. The invasion and migration abilities of HCC cells were evaluated using Transwell assay. The mRNA and protein levels in cells and tissues were measured using qRT-PCR and Western blot assays. Moreover, we established the HCC xenografts nude mice to evaluate the effect of zingerone on tumor growth.Results: We found that zingerone treatment significantly inhibited HCC cell malignant phenotype and tumor growth. Moreover, MTDH was highly expressed in HCC tissues and cell lines and was positively associated with poor overall survival of patients with HCC. Knockdown of MTDH notably suppressed the proliferation, invasion, and migration capacities of HCC cells. Mechanistically, inhibition of MTDH by zingerone impeded the malignant biological behavior of HCC cells by inactivating the PI3K/Akt pathway.Conclusion: These results suggested that zingerone served as an effective therapeutic agent in HCC via blocking the MTDH-mediated PI3K/Akt pathway.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"409-417"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39514698","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Discovery of polymethoxyflavones as potential cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and phosphodiesterase 4B (PDE4B) inhibitors. 发现多甲氧基黄酮作为潜在的环氧化酶-2 (COX-2)、5-脂氧化酶(5-LOX)和磷酸二酯酶4B (PDE4B)抑制剂。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-07-29 DOI: 10.1080/10799893.2021.1951756

Muhd Hanis Md Idris, Siti Norhidayah Mohd Amin, Siti Norhidayu Mohd Amin, Agustono Wibowo, Zainul Amiruddin Zakaria, Zurina Shaameri, Ahmad Sazali Hamzah, Manikandan Selvaraj, Lay Kek Teh, Mohd Zaki Salleh

{"title":"Discovery of polymethoxyflavones as potential cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and phosphodiesterase 4B (PDE4B) inhibitors.","authors":"Muhd Hanis Md Idris, Siti Norhidayah Mohd Amin, Siti Norhidayu Mohd Amin, Agustono Wibowo, Zainul Amiruddin Zakaria, Zurina Shaameri, Ahmad Sazali Hamzah, Manikandan Selvaraj, Lay Kek Teh, Mohd Zaki Salleh","doi":"10.1080/10799893.2021.1951756","DOIUrl":"https://doi.org/10.1080/10799893.2021.1951756","url":null,"abstract":"Non-steroidal anti-inflammatory drugs (NSAIDs) are widely prescribed to treat inflammatory-related diseases, pain and fever. However, the prolong use of traditional NSAIDs leads to undesirable side effects such as gastric, ulceration, and renal toxicity due to lack of selectivity toward respective targets for COX-2, 5-LOX, and PDE4B. Thus, targeting multiple sites can reduce these adverse effects of the drugs and increase its potency. A series of methoxyflavones (F1-F5) were synthesized and investigated for their anti-inflammatory properties through molecular docking and inhibition assays. Among these flavones, only F2 exhibited selectivity toward COX-2 (Selectivity Index, SI: 3.90, COX-2 inhibition: 98.96 ± 1.47%) in comparison with celecoxib (SI: 7.54, COX-2 inhibition: 98.20 ± 2.55%). For PDEs, F3 possessed better selectivity to PDE4B (SI: 4.67) than rolipram (SI: 0.78). F5 had the best 5-LOX inhibitory activity among the flavones (33.65 ± 4.74%) but less than zileuton (90.81 ± 0.19%). Docking analysis indicated that the position of methoxy group and the substitution of halogen play role in determining the bioactivities of flavones. Interestingly, F1-F5 displayed favorable pharmacokinetic profiles and acceptable range of toxicity (IC50>70 µM) in cell lines with the exception for F1 (IC50: 16.02 ± 1.165 µM). This study generated valuable insight in designing new anti-inflammatory drug based on flavone scaffold. The newly synthesized flavones can be further developed as future therapeutic agents against inflammation.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"325-337"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/10799893.2021.1951756","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39257247","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 4

Protective role of selenium on MPP⁺ and homocysteine-induced TRPM2 channel activation in SH-SY5Y cells. 硒对SH-SY5Y细胞MPP+和同型半胱氨酸诱导的TRPM2通道激活的保护作用。

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-09-28 DOI: 10.1080/10799893.2021.1981381

Kenan Yıldızhan, Mustafa Nazıroğlu

{"title":"Protective role of selenium on MPP+ and homocysteine-induced TRPM2 channel activation in SH-SY5Y cells.","authors":"Kenan Yıldızhan, Mustafa Nazıroğlu","doi":"10.1080/10799893.2021.1981381","DOIUrl":"https://doi.org/10.1080/10799893.2021.1981381","url":null,"abstract":"Homocysteine is an intermediate product of biochemical reactions occurring in living organisms. It is known that drugs that increase dopamine synthesis used in Parkinson's disease (PD) cause an increase in the plasma homocysteine level. As the plasma homocysteine level increases, the amount of intracellular free calcium ion ([Ca2+]i) and oxidative stress increase. As a result, it contributes to the excitotoxic effect by causing neurodegeneration. TRPM2 cation channel is activated by high [Ca2+]i and oxidative stress. The role of TRPM2 in the development of neuronal damage due to the increase in homocysteine in PD has not yet been elucidated. In current study, we aimed to investigate the role of the TRPM2 and selenium (Se) in SH-SY5Y neuronal cells treated with homocysteine (HCT) and MPP . SH-SY5Y cells were divided into four groups: control, MPP, MPP + HCT, and MPP + HCT + Se. The results of plate reader assay, confocal microscope imaging, and western blot analyses indicated upregulation of apoptosis, [Ca2+]i, mitochondrial membrane depolarization, caspase activation, and intracellular ROS values in the cells. The MPP + HCT group had considerably higher values than the other groups. The MPP + HCT + Se group had significantly lower values than all the other groups except the control group. In addition, incubation of MPP + HCT and MPP + HCT + Se groups with TRPM2 antagonist 2-APB increased cell viability and reduced intracellular calcium influx and apoptosis levels. It is concluded that the activation of TRPM2 was propagated in HCT and MPP-induced SH-SY5Y cells by the increase of oxidative stress. The antioxidant property of Se regulated the TRPM2 channel activation and neurodegeneration by providing intracellular oxidant/antioxidant balance.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"399-408"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39468507","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 14

Role of TRPV1 channels on glycogen synthase kinase-3β and oxidative stress in ouabain-induced bipolar disease. TRPV1通道在糖原合成酶激酶-3β和氧化应激中的作用

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-07-26 DOI: 10.1080/10799893.2021.1955928

Osman Kukula, Mustafa Nusret Çiçekli, Sinan Şafak, Caner Günaydın

{"title":"Role of TRPV1 channels on glycogen synthase kinase-3β and oxidative stress in ouabain-induced bipolar disease.","authors":"Osman Kukula, Mustafa Nusret Çiçekli, Sinan Şafak, Caner Günaydın","doi":"10.1080/10799893.2021.1955928","DOIUrl":"https://doi.org/10.1080/10799893.2021.1955928","url":null,"abstract":"Bipolar disorder (BD) is a multifactorial chronic and refractory disease characterized by manic, depressive, and mixed mood episodes. Although epidemiological, and pathophysiological studies demonstrated a strong correlation between bipolar disorder and oxidative stress, precise etiology is still missing. Recent studies suggested the possible role of transient receptor potential channels (TRP) in the BD but, current knowledge is limited. Therefore, the current study investigates the possible role of TRPV1 in the ouabain-induced model of BD. The model was created with intracerebroventricular single dose ouabain (10-3 M) administration. Animals were treated with capsaicin, capsazepine, and lithium for seven days. Mania and depressive-like states were investigated with open-field, sucrose preference, and elevated plus maze tests. Oxidative stress was assessed by measuring total antioxidant and oxidant states, spectrophotometrically. The phosphorylation Glycogen synthase kinase-3β (GSK-3β) evaluated by western blotting. Our results demonstrated that capsaicin dose-dependently inhibited the ouabain-induced hyperlocomotion and depression. Although capsazepine exacerbated behavioral impairment, it did not show a significant effect on the antioxidant and oxidant states, and the effects of capsazepine on behaviors were abolished by combination with capsaicin. Additionally, capsaicin potently prevented the ouabain-induced decrease in GSK-3β phosphorylation. In contrast, capsazepine potentiated ouabain-induced decrease in GSK-3β phosphorylation and combination with capsaicin, suppressed the effect of capsazepine on GSK-3β phosphorylation. The effects of TRPV1 activation on oxidative stress and mania-like behaviors in the ouabain-induced BD model might be regulated by GSK-3β phosphorylation.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"338-348"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/10799893.2021.1955928","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39218127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

In vivo and in vitro impact of miRNA-153 on the suppression of cell growth apoptosis through mTORC2 signaling pathway in breast cancer. miRNA-153通过mTORC2信号通路抑制乳腺癌细胞生长凋亡的体内外影响

IF 2.8 4区生物学

Journal of Receptors and Signal Transduction Pub Date : 2022-08-01 Epub Date: 2021-08-29 DOI: 10.1080/10799893.2021.1970766

Haimei Liu, Hongyan Zang, Jilin Kong, Liguo Gong

{"title":"In vivo and in vitro impact of miRNA-153 on the suppression of cell growth apoptosis through mTORC2 signaling pathway in breast cancer.","authors":"Haimei Liu, Hongyan Zang, Jilin Kong, Liguo Gong","doi":"10.1080/10799893.2021.1970766","DOIUrl":"https://doi.org/10.1080/10799893.2021.1970766","url":null,"abstract":"Purpose: To investigate the effects and mechanism of miRNA-153 on breast cancer cells in vitro and in vivo.Material and methods: The cells and mice were divided into five groups: miRNA-153 mimic, miRNA-153 NC, miRNA-153 inhibitor, miRNA-153 inhibitor-NC, and blank control groups. The real-time PCR and western blot were used to detect the rictor expression regulated by miRNA-153. The western blot was used to explore the expression levels of p-Akt Ser473, p-SGK1 Ser422, and p-FOXO1 Thr24 regulated by miRNA-153. The H&E stain was used to detect the morphology and vitality of tumor cells. Flow cytometry analysis or TUNEL detection was used to evaluate the apoptosis of tumor cells.Results: MiRNA-153 was significantly reduced in breast cancer cell lines. The real-time PCR and western blot assay suggested that the miRNA-153 downregulation of rictor expression, which was correlated with the antitumor effects both in vitro and in vivo. The western blot assay also showed that the expression levels of p-Akt Ser473, p-SGK1 Ser422, and p-FOXO1 Thr24 were largely reduced in miRNA-153 treated group, which indicated that miRNA-153 inhibited breast cancer growth by regulation of mTORC2 signaling pathway. The H&E stain demonstrated that the morphology and vitality of tumor cells in tumor tissues were influenced in miRNA-153 mimic treated group. The TUNEL detection also showed a great quantity of apoptotic cells in the miRNA-153 mimic group.Conclusions: All these results uncovering that the miRNA-153 inhibited breast cancer growth via regulation of mTORC2 signaling pathway, which provided breast cancer treatment a novel direction.","PeriodicalId":16962,"journal":{"name":"Journal of Receptors and Signal Transduction","volume":"42 4","pages":"390-398"},"PeriodicalIF":2.8,"publicationDate":"2022-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39363471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0