Article
Medicine, Research & Experimental
Tarfa Albrahim, Mona A. Alonazi
Summary: The study found that LYC effectively reversed the changes induced by HFD through its antioxidant, anti-inflammatory, and anti-fibrotic properties, showing therapeutic potential in managing obesity and its associated pathologies.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Shaista Amin, Khursheed A. Sheikh, Ashif Iqubal, Mohammad Ahmed Khan, M. Shaquiquzzaman, Sharba Tasneem, Suruchi Khanna, A. K. Najmi, Mymoona Akhter, Anzarul Haque, Tarique Anwer, M. Mumtaz Alam
Summary: Despite advancements in Diabetes mellitus management, designing and synthesizing drug molecules that effectively improve hyperglycemia and associated complications in diabetic patients remains challenging. In this study, pyrimidine-thiazolidinedione derivatives were synthesized, characterized, and evaluated for their anti-diabetic properties. The synthesized compounds were analyzed using various techniques, including NMR, FTIR, and Mass Spectrometry. In-silico ADME studies confirmed the compounds met Lipinski's rule of five. In-vivo evaluation in diabetic rats showed that compounds 6e and 6m significantly reduced blood glucose levels without causing weight gain. Biochemical and histopathological analyses further supported the anti-diabetic effects of these compounds. Based on these findings, pyrimidine-based thiazolidinedione derivatives could be considered as novel anti-diabetic agents with minimal side effects.
BIOORGANIC CHEMISTRY
(2023)
Article
Cell Biology
Fangfang Li, Jingfeng Peng, Hui Feng, Yiming Yang, Jianbo Gao, Chunrui Liu, Jie Xu, Yanru Zhao, Siyu Pan, Yixiao Wang, Luhong Xu, Wenhao Qian, Jing Zong
Summary: This study reveals that KLF9 exacerbates cardiac dysfunction, inflammatory response, and oxidative stress in diabetic cardiomyopathy. KLF9 may be a potential therapeutic target for diabetic cardiomyopathy.
Article
Biochemistry & Molecular Biology
Meei-Ling Sheu, Liang-Yi Pan, Huai-Yun Hu, Hong-Lin Su, Jason Sheehan, Hsi-Kai Tsou, Hung-Chuan Pan
Summary: This study investigates the potential therapeutic effect of PPAR gamma agonists on malignant glioma. The results demonstrate that ciglitazone inhibits tumor growth, angiogenesis, colony formation, and migration in glioma cells. Ciglitazone also affects protein phosphorylation and triggers the autophagy pathway in glioma cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Si-ping Xiong, Hai-jian Sun, Xu Cao, Zhi-yuan Wu, Meng-yuan Zhu, Lei Cao, Xiao-wei Nie, Jin-song Bian
Summary: In this study, the therapeutic effects of polysulfide in diabetic cardiomyopathy were investigated using Na2S4. The results showed that Na2S4 protected cardiomyocytes against high glucose-induced injury and improved pathological changes. Mechanistically, Na2S4 exerted its protective effects by sulfhydrating PPAR gamma and SIRT-3. These findings suggest that polysulfide may be a potential agent for treating diabetic cardiomyopathy.
ANTIOXIDANTS & REDOX SIGNALING
(2023)
Article
Biochemistry & Molecular Biology
Liping Huang, Yanlin Ma, Lu Chen, Jiang Chang, Mei Zhong, Zhijian Wang, Ying Sun, Xia Chen, Fei Sun, Lu Xiao, Jianing Chen, Yingjun Lai, Chuming Yan, Xiaojing Yue
Summary: Preeclampsia is a life-threatening disease in pregnant women associated with mitochondrial-mediated placental oxidative stress. The down-regulation of Rnd3 in primary trophoblasts from PE patients leads to excessive ROS generation, cell apoptosis, and mitochondrial damage. Rnd3 acts as a protective factor in placental mitochondria through the PPARγ-UCP2 signaling pathway.
Article
Biochemistry & Molecular Biology
Nataliya Finiuk, Edyta Kaleniuk, Serhii Holota, Rostyslav Stoika, Roman Lesyk, Konrad A. Szychowski
Summary: Hybrid heterocyclic molecules show promise in developing anticancer drugs. In this study, pyrrolidinedione-thiazolidinone hybrid molecules were designed as potent anticancer agents. The results showed that these derivatives effectively inhibited the growth and metabolism of tongue squamous cell carcinoma cells (SCC-15), reduced the level of reactive oxygen species, and increased caspase 3 activity. However, these effects were not mediated by direct interaction with the PPAR? molecule.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Food Science & Technology
Al Borhan Bayazid, Jae Gon Kim, Shofiul Azam, Soo Ah Jeong, Da Hee Kim, Chae Won Park, Beong Ou Lim
Summary: The study evaluated the neuroprotective effects of sodium butyrate (NaB) on high-fat diet (HFD)-fed mice. The results showed that NaB restored bodyweight and attenuated oxidative stress, inflammation, and dysregulation in the brains of HFD-fed mice. NaB also enhanced the expression of endogenous antioxidants and exhibited potential as a therapeutic agent for neurodegenerative diseases (NDDs).
FOOD AND CHEMICAL TOXICOLOGY
(2022)
Article
Food Science & Technology
Mahdi Daryagasht, Mehrnoosh Moosavi, Layasadat Khorsandi, Reza Azadnasab, Mohammad Javad Khodayar
Summary: The objective of this study was to evaluate the effects of ferulic acid (FA) in mitigating glucose intolerance and hepatotoxicity caused by sodium arsenite (SA). The results showed that FA prevented SA-induced glucose intolerance and hepatotoxicity by reducing oxidative stress, inflammation, and hepatic overexpression of PPAR-γ and GLUT2 proteins.
FOOD AND CHEMICAL TOXICOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Priyaranjini Rao, S. Ashwini, Ghazala Masood, Raviraj Kusanur, Vidya Niranjan, Swarna M. Patra
Summary: The research on molecular docking technology for the treatment of diabetes is of great significance, as it can improve the efficiency and effectiveness of drug development, bringing new hope for disease treatment.
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Sheryar Afzal, Munavvar Abdul Sattar, Edward James Johns, Olorunfemi A. Eseyin
Summary: The study demonstrates that adiponectin and PPAR-γ agonists have significant effects on modulating metabolic dysregulation and oxidative stress in diabetic WKY rats, with even better outcomes when used in combination.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Review
Oncology
Tiange Chi, Mina Wang, Xu Wang, Ke Yang, Feiyu Xie, Zehuan Liao, Peng Wei
Summary: PPARs are lipid sensors and metabolic regulators, with PPAR-γ showing potential in inhibiting cell proliferation, inducing apoptosis, and disrupting inflammation. However, safety concerns including drug interactions need to be addressed for clinical applications.
FRONTIERS IN ONCOLOGY
(2021)
Article
Medicine, Research & Experimental
Aya E. Mohamed, Ayman M. Mahmoud, Wafaa R. Mohamed, Tarek Mohamed
Summary: This study aimed to investigate the therapeutic potential and underlying mechanism of low-level laser therapy (LLLT) for liver fibrosis in rats. The results showed that LLLT attenuated CCl4-induced liver fibrosis by suppressing extracellular matrix (ECM) production and deposition, reducing oxidative injury and inflammation, and upregulating PPAR gamma and Nrf2/HO-1 signaling.
Article
Biochemistry & Molecular Biology
Dohee Ahn, Jinsoo Kim, Gibeom Nam, Xiaodi Zhao, Jihee Kwon, Ji Young Hwang, Jae Kwan Kim, Sun-Young Yoon, Sang J. Chung
Summary: The coexistence of type 2 diabetes and obesity, known as diabesity, has led to the exploration of potential therapeutic agents. In this study, ethyl gallate was discovered to be a selective inhibitor of PTPN6 and a potent antagonist of PPAR gamma. It showed promising effects in suppressing adipogenesis and promoting glucose uptake, making it a potential candidate for diabesity treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Medicine, Research & Experimental
Srinivasa R. Vulichi, Atul Kabra, Rupak Kumar, Kapur Suman, Chunduri Venkata Rao, Natalia Cruz-Martins
Summary: Glitazones are synthetic derivatives of thiazolidinedione that primarily act on peroxisome proliferator-activated receptor-gamma (PPAR-y) receptors to regulate metabolic pathways linked to glucose and lipid metabolism at a transcriptional level. Despite their high efficacy and selectivity in clinical settings, glitazones are restricted for long-term usage due to potential adverse effects such as weight gain and heart-related complications.
Article
Biochemistry & Molecular Biology
Poonam Parashar, Ifrah Mazhar, Jovita Kanoujia, Abhishek Yadav, Pranesh Kumar, Shubhini A. Saraf, Sudipta Saha
Summary: The present study focused on the transdermal delivery of colchicine-loaded chitosan nanoparticles and evaluated its therapeutic potential for gout treatment. By optimizing the formulation and preparation process, CHNPgel demonstrated high drug entrapment efficiency, permeation, stability, and release efficacy.
ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY
(2022)
Review
Chemistry, Medicinal
Archana Sonkar, Pranesh Kumar, Anurag Gautam, Biswanath Maity, Sudipta Saha
Summary: This review summarizes the current understanding of different signaling pathways in lung cancer, describing the main molecular pathways and changes involved in the development, progression, and cellular breakdown of the disease. It also focuses on targeted therapies for lung cancer.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Lloyd Wei Tat Tang, Tino Woon Huai Cheong, Eric Chun Yong Chan
Summary: The study suggests that febuxostat and febuxostat AG have strong inhibitory effects on OAT3, potentially leading to clinically significant drug-drug interactions and increased risk of bleeding.
BIOPHARMACEUTICS & DRUG DISPOSITION
(2022)
Article
Pharmacology & Pharmacy
Eleanor Jing Yi Cheong, Daniel Zhi Wei Ng, Sheng Yuan Chin, Ziteng Wang, Eric Chun Yong Chan
Summary: This study established a PBPK-DDDI model to predict the interactions between rivaroxaban and protein kinase inhibitors (PKIs) and provide guidance for the safe and effective management of CA-VTE.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Article
Cardiac & Cardiovascular Systems
Ziteng Wang, Eleanor Jing Yi Cheong, Pipin Kojodjojo, Eric Chun Yong Chan
Summary: Concurrent use of rivaroxaban and amiodarone increases the risk of bleeding. The study found that human renal organic anion transporter 3 (hOAT3) plays a key role in the renal secretion of rivaroxaban and amiodarone inhibits hOAT3. When prescribed together, a dose reduction of rivaroxaban to 10 mg in elderly people with moderate renal impairment results in persistently higher rivaroxaban peak concentrations. To manage the increased bleeding risk, a further dose reduction of rivaroxaban to 2.5 mg twice daily is recommended.
CARDIOVASCULAR DRUGS AND THERAPY
(2023)
Article
Biochemistry & Molecular Biology
Shuaibing Liu, Ziteng Wang, Eric Chan, Yibo Zhao, Jian Kang, Xiaojian Zhang, Xin Tian
Summary: Vicagrel, an antiplatelet drug candidate targeting platelet P2Y12 receptor, exhibits potent inhibitory effects on several enzymes, including CYP2B6, CYP2C19, and UGT1A6. Physiological-based pharmacokinetic simulation suggests no clinically significant drug-drug interactions between vicagrel and bupropion or S-mephenytoin.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Analytical
Ziteng Wang, Ching Yee Fong, Evelyn Mei Ling Goh, Hooi Yan Moy, Eric Chun Yong Chan
Summary: Concurrent use of synthetic cannabinoids (SCs) and alcohol has been observed among drug abusers. This study investigated the susceptibility of three indazole-3-carboxamide type SCs to transesterification in the presence of ethanol, as well as its potential augmented toxicity. Results showed that all three SCs underwent transesterification to ethyl ester analogs in the presence of ethanol, which was time- and concentration-dependent. The co-abuse of SCs and alcohol could lead to increased toxicity and further research is warranted.
JOURNAL OF ANALYTICAL TOXICOLOGY
(2023)
Article
Cardiac & Cardiovascular Systems
Xin Qin Soh, Doreen Su-Yin Tan, Eric Chun Yong Chan
Summary: This study identifies a potential association between concurrent use of simvastatin and rivaroxaban with bleeding events in Singaporean Asians.
CARDIOVASCULAR DRUGS AND THERAPY
(2023)
Article
Agriculture, Multidisciplinary
Yuxiang Gu, Haoran Chen, Xing Li, Dan Li, Yue Sun, Lin Yang, Ying Ma, Eric Chun Yong Chan
Summary: This study found that Lactobacillus paracasei IMC 502 can prevent and alleviate type 2 diabetes by mediating the gut microbiota-SCFA-hormone/inflammation pathway.
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
(2023)
Article
Pharmacology & Pharmacy
Jacqueline Wen Hui Leow, Xiao Jun Ang, Eric Chun Yong Chan
Summary: A physiologically based pharmacokinetic (PBPK) model was developed to study the drug-drug interaction between dronedarone and rivaroxaban, and the simulation results showed that reducing the dose of rivaroxaban to at least 15 mg in subjects with mild renal impairment can achieve a better balance of risk and benefit.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2023)
Letter
Pharmacology & Pharmacy
Ziteng Wang, Eric Chun Yong Chan
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2023)
Article
Pharmacology & Pharmacy
Eleanor Jing Yi Cheong, Sheng Yuan Chin, Zheng Wei Ng, Ting Jian Yap, Ervin Zhi Bin Cheong, Ziteng Wang, Eric Chun Yong Chan
Summary: This study aims to develop a physiologically based pharmacokinetic (PBPK) model for abiraterone to investigate the potential associations between its concentrations and pharmacodynamic consequences, and optimize the dosage to achieve better therapeutic outcomes.
CLINICAL PHARMACOKINETICS
(2023)
Article
Pharmacology & Pharmacy
Jacqueline Wen Hui Leow, Yuxiang Gu, Eric Chun Yong Chan
Summary: This study investigated the inhibitory effects of 16 drugs with intermediate to high risk of torsades de pointes (TdP) on the metabolism of arachidonic acid (AA) to epoxyeicosatrienoic acid (EET) by cardiac cytochrome P450 2J2 (CYP2J2). The results showed that 11 out of the 16 drugs exhibited inhibitory effects on CYP2J2 metabolism of AA. Among the high TdP risk category drugs, vandetanib and bepridil had the highest inhibitory effects. Further research is needed to determine the role of CYP2J2 metabolism in cardiac electrophysiology and the in vivo evidence of drug-AA interactions.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Food Science & Technology
Yuxiang Gu, Xing Li, Eric Chun Yong Chan
Summary: The production of cultured meat involves complex technologies and novel ingredients, which may introduce hazards and risks. Currently, there is a lack of systematic and in-depth risk assessment for cultured meat. Therefore, targeted and effective risk and safety assessment strategies should be adopted, and a harmonized regulatory framework should be established globally.
TRENDS IN FOOD SCIENCE & TECHNOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Lei Hou, Yingying Zhao, Shiyu Zhao, Xuexia Zhang, Xia Yao, Jianjun Yang, Ziteng Wang, Shuaibing Liu
Summary: This study systematically characterized the UGTs enzymes involved in the formation of M4 and the inhibitory effects of ciprofol and its metabolite M4 on P450s enzymes. In vitro-in vivo extrapolation and PBPK simulations were performed to predict potential drug-drug interactions caused by ciprofol.
CHEMICO-BIOLOGICAL INTERACTIONS
(2024)