The pathophysiology of visceral adipose tissues in cardiometabolic diseases
Biochem Pharmacol. 2024 Mar 7:116116. doi: 10.1016/j.bcp.2024.116116. Online ahead of print.ABSTRACTCentral pattern of fat distribution, especially fat accumulation within the intraabdominal cavity increases risks for cardiometabolic diseases. Portal hypothesis combined with a pathological remodeling in visceral fat is considered the major etiological factor explaining the independent contribution of visceral obesity to cardiometabolic diseases. Excessive remodeling in visceral fat during development of obesity leads to dysfunctions in the depot, characterized by hypertrophy and death of adipocytes, hypoxia, inflammation, ...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Mi-Jeong Lee Jeehoon Kim Source Type: research
Potential role of modulating autophagy levels in sensorineural hearing loss
Biochem Pharmacol. 2024 Mar 7;222:116115. doi: 10.1016/j.bcp.2024.116115. Online ahead of print.ABSTRACTIn recent years, extensive research has been conducted on the pathogenesis of sensorineural hearing loss (SNHL). Apoptosis and necrosis have been identified to play important roles in hearing loss, but they cannot account for all hearing loss. Autophagy, a cellular process responsible for cell self-degradation and reutilization, has emerged as a significant factor contributing to hearing loss, particularly in cases of autophagy deficiency. Autophagy plays a crucial role in maintaining cell health by exerting cytoprotecti...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Ting Zou Renwei Xie Sihan Huang Dingkun Lu Jun Liu Source Type: research
Daurisoline suppress glioma progression by inhibiting autophagy through PI3K/AKT/mTOR pathway and increases TMZ sensitivity
Biochem Pharmacol. 2024 Mar 7:116113. doi: 10.1016/j.bcp.2024.116113. Online ahead of print.ABSTRACTGlioma is one of the most common primary malignant tumors of the central nervous system. Temozolomide (TMZ) is the only effective chemotherapeutic agent, but it easily develops resistance and has unsatisfactory efficacy. Consequently, there is an urgent need to develop safe and effective compounds for glioma treatment. The cytotoxicity of 30 candidate compounds to glioma cells was detected by the CCK-8 assay. Daurisoline (DAS) was selected for further investigation due to its potent anti-glioma effects. Our study revealed th...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Hai-Tang Yin None Hui-Lu Ji-Hong Yang Qin Li Ming Li Qing-Qing Zhao Zhi-Peng Wen Source Type: research
Corynoxine triggers cell death via activating PP2A and regulating AKT-mTOR/GSK3 β axes in NSCLC
This study investigates the anticancer activity and pharmacological mechanisms of Corynoxine (Cory) in non-small cell lung cancer (NSCLC). Cory, a natural product derived from the Chinese herbal medicine Uncaria rhynchophylla, demonstrates promising pharmacological activity. Cell proliferation and viability were evaluated via MTT and colony formation assays. Flow cytometry was employed to analyze cell apoptosis, cycle distribution, and mitochondrial membrane potential. Autophagy was detected using fluorescence microscopy and electron microscopy. Western blotting, protein overexpression, gene knockdown, co-immunoprecipitati...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Guoqing Hou Weihua Hu Yazhou Sang Xiaocai Gan Hui Xu Qiongying Hu Xuan Cao Source Type: research
The pathophysiology of visceral adipose tissues in cardiometabolic diseases
Biochem Pharmacol. 2024 Mar 7:116116. doi: 10.1016/j.bcp.2024.116116. Online ahead of print.ABSTRACTCentral pattern of fat distribution, especially fat accumulation within the intraabdominal cavity increases risks for cardiometabolic diseases. Portal hypothesis combined with a pathological remodeling in visceral fat is considered the major etiological factor explaining the independent contribution of visceral obesity to cardiometabolic diseases. Excessive remodeling in visceral fat during development of obesity leads to dysfunctions in the depot, characterized by hypertrophy and death of adipocytes, hypoxia, inflammation, ...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Mi-Jeong Lee Jeehoon Kim Source Type: research
Potential role of modulating autophagy levels in sensorineural hearing loss
Biochem Pharmacol. 2024 Mar 7:116115. doi: 10.1016/j.bcp.2024.116115. Online ahead of print.ABSTRACTIn recent years, extensive research has been conducted on the pathogenesis of sensorineural hearing loss (SNHL). Apoptosis and necrosis have been identified to play important roles in hearing loss, but they cannot account for all hearing loss. Autophagy, a cellular process responsible for cell self-degradation and reutilization, has emerged as a significant factor contributing to hearing loss, particularly in cases of autophagy deficiency. Autophagy plays a crucial role in maintaining cell health by exerting cytoprotective a...
Source: Biochemical Pharmacology - March 9, 2024 Category: Drugs & Pharmacology Authors: Ting Zou Renwei Xie Sihan Huang Dingkun Lu Jun Liu Source Type: research
SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux
In this study, we constructed a library to screen compounds inhibiting bladder cancer cells growth. Among them, SRT1720 was identified to inhibit bladder cancer cell proliferation in vitro and in vivo. SRT1720 treatment also suppressed bladder cancer cells migration, invasion and induced apoptosis. Mechanism studies shown that SRT1720 promoted autophagosomes accumulation by inducing early-stage autophagy but disturbed the late-stage of autophagy by blocking fusion of autophagosomes and lysosomes. SRT1720 appears to induce autophagy related proteins expression and alter autophagy-related proteins acetylation to impede the a...
Source: Biochemical Pharmacology - March 8, 2024 Category: Drugs & Pharmacology Authors: Lanlan Li Shengjun Fu Jianliang Wang Jianzhong Lu Yan Tao Liangtao Zhao Beitang Fu Lanpeng Lu Caifei Xiang Xince Sun Shanhui Liu Degui Wang Zhiping Wang Source Type: research
The role of telomerase reverse transcriptase in the mitochondrial protective functions of Angiotensin-(1-7) in diabetic CD34 < sup > + < /sup > cells
This study tested if the protective functions of Ang-(1-7) or TGFβ1-silencing are mediated by mitoTERT and that diabetes decreases FL-TERT expression by inducing splicing. CD34+ cells were isolated from the peripheral blood mononuclear cells of nondiabetic (ND, n = 68) or DB (n = 74) subjects. NO and mitoROS levels were evaluated by flow cytometry. TERT splice variants and mitoDNA-lesions were characterized by qPCR. TRAP assay was used for telomerase activity. Decoy peptide was used to block mitochondrial translocation (mitoXTERT). TERT inhibitor or mitoXTERT prevented the effects of Ang-(1-7) on NO or mitoROS levels in D...
Source: Biochemical Pharmacology - March 8, 2024 Category: Drugs & Pharmacology Authors: Jesmin Jahan Shrinidh Joshi Ildamaris Montes de Oca Andrew Toelle Christine Lopez-Yang Carmen V Chacon Andreas W Beyer Charles A Garcia Yagna Pr Jarajapu Source Type: research
Columbianadin suppresses glioblastoma progression by inhibiting the PI3K-Akt signaling pathway
Biochem Pharmacol. 2024 Mar 6:116112. doi: 10.1016/j.bcp.2024.116112. Online ahead of print.ABSTRACTGlioblastoma (GBM) is the most common malignant glioma among brain tumors with low survival rate and high recurrence rate. Columbianadin (CBN) has pharmacological properties such as anti-inflammatory, analgesic, thrombogenesis-inhibiting and anti-tumor effects. However, it remains unknown that the effect of CBN on GBM cells and its underlying molecular mechanisms. In the present study, we found that CBN inhibited the growth and proliferation of GBM cells in a dose-dependent manner. Subsequently, we found that CBN arrested th...
Source: Biochemical Pharmacology - March 8, 2024 Category: Drugs & Pharmacology Authors: Wei Zhang Jianhong Dong Jiayun Xu Yiming Qian Danni Chen Ziwei Fan Hao Yang Jianglei Xiang Xiumin Xue Xuan Luo Yuanyuan Jiang Yongjie Wang Zhihui Huang Source Type: research
Therapeutic potential of lipin inhibitors for the treatment of cancer
Biochem Pharmacol. 2024 Mar 3:116106. doi: 10.1016/j.bcp.2024.116106. Online ahead of print.ABSTRACTLipins are phosphatidic acid phosphatases (PAP) that catalyze the conversion of phosphatidic acid (PA) to diacylglycerol (DAG). Three lipin isoforms have been identified: lipin-1, -2 and -3. In addition to their PAP activity, lipin-1 and -2 act as transcriptional coactivators and corepressors. Lipins have been intensely studied for their role in regulation of lipid metabolism and adipogenesis; however, lipins are hypothesized to mediate several pathologies, such as those involving metabolic diseases, neuropathy and even cogn...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Elizabeth G Slane Samantha J Tambrini Brian S Cummings Source Type: research
HER2 targeted therapy in colorectal Cancer: Current landscape and future directions
Biochem Pharmacol. 2024 Mar 3:116101. doi: 10.1016/j.bcp.2024.116101. Online ahead of print.ABSTRACTColorectal cancer (CRC) is one of the most common causes of tumor-related deaths globally. Despite recent improvements in the comprehensive therapy of malignancy, metastatic CRC continues to have a poor prognosis. Human epidermal growth factor receptor 2 (HER2) is an established oncogenic driver, which is successfully targeted for breast and gastric cancers. Approximately 5% of CRC patients carry somatic HER2 mutations or gene amplification. In 2019, the U.S. Food and Drug Administration have approved trastuzumab and pertuzu...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Na Chen Ling He Qiang Zou Hongxin Deng Source Type: research
Therapeutic potential of lipin inhibitors for the treatment of cancer
Biochem Pharmacol. 2024 Mar 3:116106. doi: 10.1016/j.bcp.2024.116106. Online ahead of print.ABSTRACTLipins are phosphatidic acid phosphatases (PAP) that catalyze the conversion of phosphatidic acid (PA) to diacylglycerol (DAG). Three lipin isoforms have been identified: lipin-1, -2 and -3. In addition to their PAP activity, lipin-1 and -2 act as transcriptional coactivators and corepressors. Lipins have been intensely studied for their role in regulation of lipid metabolism and adipogenesis; however, lipins are hypothesized to mediate several pathologies, such as those involving metabolic diseases, neuropathy and even cogn...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Elizabeth G Slane Samantha J Tambrini Brian S Cummings Source Type: research
HER2 targeted therapy in colorectal Cancer: Current landscape and future directions
Biochem Pharmacol. 2024 Mar 3:116101. doi: 10.1016/j.bcp.2024.116101. Online ahead of print.ABSTRACTColorectal cancer (CRC) is one of the most common causes of tumor-related deaths globally. Despite recent improvements in the comprehensive therapy of malignancy, metastatic CRC continues to have a poor prognosis. Human epidermal growth factor receptor 2 (HER2) is an established oncogenic driver, which is successfully targeted for breast and gastric cancers. Approximately 5% of CRC patients carry somatic HER2 mutations or gene amplification. In 2019, the U.S. Food and Drug Administration have approved trastuzumab and pertuzu...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Na Chen Ling He Qiang Zou Hongxin Deng Source Type: research
Therapeutic potential of lipin inhibitors for the treatment of cancer
Biochem Pharmacol. 2024 Mar 3:116106. doi: 10.1016/j.bcp.2024.116106. Online ahead of print.ABSTRACTLipins are phosphatidic acid phosphatases (PAP) that catalyze the conversion of phosphatidic acid (PA) to diacylglycerol (DAG). Three lipin isoforms have been identified: lipin-1, -2 and -3. In addition to their PAP activity, lipin-1 and -2 act as transcriptional coactivators and corepressors. Lipins have been intensely studied for their role in regulation of lipid metabolism and adipogenesis; however, lipins are hypothesized to mediate several pathologies, such as those involving metabolic diseases, neuropathy and even cogn...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Elizabeth G Slane Samantha J Tambrini Brian S Cummings Source Type: research
HER2 targeted therapy in colorectal Cancer: Current landscape and future directions
Biochem Pharmacol. 2024 Mar 3:116101. doi: 10.1016/j.bcp.2024.116101. Online ahead of print.ABSTRACTColorectal cancer (CRC) is one of the most common causes of tumor-related deaths globally. Despite recent improvements in the comprehensive therapy of malignancy, metastatic CRC continues to have a poor prognosis. Human epidermal growth factor receptor 2 (HER2) is an established oncogenic driver, which is successfully targeted for breast and gastric cancers. Approximately 5% of CRC patients carry somatic HER2 mutations or gene amplification. In 2019, the U.S. Food and Drug Administration have approved trastuzumab and pertuzu...
Source: Biochemical Pharmacology - March 5, 2024 Category: Drugs & Pharmacology Authors: Na Chen Ling He Qiang Zou Hongxin Deng Source Type: research
