Article
Biochemistry & Molecular Biology
Luis Felipe Hernandez-Ayala, Eduardo Gabriel Guzman-Lopez, Annia Galano
Summary: Quinoline and its derivatives have been shown to have diverse biological activities. In this study, 8536 quinoline derivatives were designed and screened using the CADMA-Chem protocol. The selected derivatives were further investigated for their acid-base, antioxidant and neuroprotective properties. The results indicate that some derivatives exhibit promising antioxidant and neuroprotective activities, making them potential candidates for the treatment of Alzheimer's and Parkinson's diseases.
Article
Biochemistry & Molecular Biology
Matic Proj, Mitja Zidar, Blaz Lebar, Nika Strasek, Goran Milicic, Ales Zula, Stanislav Gobec
Summary: This study utilized computational chemistry approaches to discover 44 new viscosity-reducing agents for the development of concentrated monoclonal antibody formulations for subcutaneous administration.
COMPUTATIONAL AND STRUCTURAL BIOTECHNOLOGY JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Seulah Lee, Yeon Ji Suh, Seonguk Yang, Dong Geun Hong, Akihito Ishigami, Hangun Kim, Jae-Seoun Hur, Seung-Cheol Chang, Jaewon Lee
Summary: The study demonstrates that evernic acid (EA) has neuroprotective and anti-inflammatory effects, protecting neurons against MPP+-induced cell death, mitochondrial dysfunction, and oxidative stress, and reducing astroglial activation. In mouse models, EA ameliorated MPTP-induced symptoms of PD, including motor dysfunction, dopaminergic neuronal loss, and neuroinflammation in the nigrostriatal pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Zichao Yang, Yangcheng Ai, Guowu Wu, Fengqiu Guo, Zilong Yang, Beijun Cheng, Lishun Zhang, Mingxia Li, Jianjun Chen, Jiajie Zhang, Tingting Zhang
Summary: Based on previous work, researchers designed a novel c-Abl inhibitor A6 and evaluated its pharmacological activities. A6 showed superior inhibitory activity against c-Abl and higher neuroprotective effects against SH-SY5Y cell death.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Leila Elyasi, Jessica M. Rosenholm, Fatemeh Jesmi, Mehrdad Jahanshahi
Summary: Neurodegenerative diseases are the main cause of dementia in the elderly, and currently there is no cure available. It is important to investigate treatments that can slow down or halt disease progression in order to improve patient outcomes. Recent research has focused on disease-modifying treatments with neuroregenerative or neuroprotective effects. Oxidative stress and accumulation of certain proteins play important roles in the pathogenesis of these diseases. Some natural compounds found in herbs have been studied for their neuroprotective and antioxidative properties. However, there is limited research on the effectiveness of herbal compounds for neurodegenerative diseases and some herbs have been disregarded.
Article
Neurosciences
Faramarz Khosravi, Vida Hojati, Sepideh Mirzaei, Mehrdad Hashemi, Maliheh Entezari
Summary: This study investigated the effects of rotenone-induced Parkinson's disease (PD) on the cerebral tissue of female mice and their fetuses, as well as the potential protective effects of curcumin supplementation. The results showed that curcumin improved cerebral cell viability by preventing cell apoptosis and necrosis in both PD mice and their fetuses. Additionally, curcumin upregulated bcl-2 expression and downregulated bax, miR-211, and circRNA 0001518 expression in cerebral neurons.
BRAIN RESEARCH BULLETIN
(2023)
Article
Chemistry, Medicinal
Liping Jiang, Bo Liu, Shengjie Hou, Tiande Su, Qiyun Fan, Eman Alyafeai, Yaqin Tang, Mengqi Wu, Xiaohua Liu, Jing Li, Yu Hu, Wulan Li, Zhiwei Zheng, Yuan Liu, Jianzhang Wu
Summary: This study synthesized chalcone derivatives and found that half of them exhibited good anti-Toxoplasma activity, with four compounds showing potent anti-T. gondii activity and low cytotoxicity. These findings provide promising compounds for the development of anti-Toxoplasma agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Ming-Chang Chiang, Tsung-Yu Tsai, Chieh-Ju Wang
Summary: Neuroinflammation is a critical factor in the development and progression of various brain diseases. Understanding its mechanisms and developing strategies to control it is crucial for treating brain disorders. Quercetin, a flavonoid found in many fruits and vegetables, has shown anti-inflammatory and neuroprotective properties and holds promise as a therapy for neurodegenerative diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Zhongcheng Cao, Xianwu Fu, Xingyue Wang, Tianlong Zhang, Lei Zhong, Qian Xia, Jiang Zhu
Summary: A series of 2-hydroxyl-4-benzyl-xybenzyl aniline derivatives were designed, synthesized, and evaluated as novel multifunctional agents for Parkinson's disease treatment. The screening showed that compound 6h exhibited excellent MAO-B inhibition, high antioxidant activity, good metal chelating ability, BBB permeability, and significant neuroprotective effect. Moreover, compound 6h effectively alleviated neuroinflammation and improved dopamine levels in MPTP-induced Parkinson's disease mice, making it a promising candidate for further development against PD.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yi-Fan Chen, Chien-Huang Wu, Li-Hsien Chen, Hao-Wei Lee, Jinq-Chyi Lee, Teng-Kuang Yeh, Jang-Yang Chang, Ming-Chen Chou, Hui-Ling Wu, Yen-Po Lai, Jen-Shin Song, Kai-Chia Yeh, Chiung-Tong Chen, Chia-Jui Lee, Kak-Shan Shia, Meng-Ru Shen
Summary: Chemotherapy-induced neurotoxicity is a common adverse effect of cancer treatment, and there is currently no effective medication for prevention or treatment. However, the discovery of CN016 as a neuroprotective agent shows promise, as it can inhibit inflammatory responses and alleviate nerve damage caused by chemotherapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biotechnology & Applied Microbiology
Joana Silva, Celso Alves, Patricia Susano, Alice Martins, Susete Pinteus, Helena Gaspar, Amparo Alfonso, Rui Pedrosa
Summary: This study found that different fractions of the brown seaweed Bifurcaria bifurcata have significant antioxidant, neuroprotective, and anti-inflammatory activities, with the ethyl acetate fraction showing the best effects. These fractions can reduce ROS production, mitochondrial dysfunction, and cell death, while inhibiting inflammatory responses.
JOURNAL OF APPLIED PHYCOLOGY
(2022)
Article
Pharmacology & Pharmacy
Motahareh Mortazavi, Elaheh Raufi, Tahereh Damghani, Mehdi Khoshneviszadeh, Najmeh Edraki, Masoomeh Eskandari, Elisa Giovannetti, Godefridus J. Peters, Somayeh Pirhadi, Omidreza Firuzi
Summary: c-Met receptor tyrosine kinase is an important therapeutic target in pancreatic cancer. A virtual screening and experimental testing were conducted to identify potential c-Met inhibitors from a compound library. The most active compound, PhTH, demonstrated antiproliferative effects against PDAC cells, induced apoptosis, and inhibited c-Met activity. Molecular docking and simulation analysis confirmed the strong interactions between PhTH and c-Met kinase domain. These findings suggest the potential of PhTH and other compounds as c-Met inhibitors in the treatment of PDAC.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Piyong Sola, Praveen Thaggikuppe Krishnamurthy, Mamta Kumari, Gowramma Byran, Hosahalli Veerabhadrappa Gangadharappa, Kusuma Kumari Garikapati
Summary: Neurodegeneration is a significant threat in Parkinson's disease and is responsible for both motor and non-motor symptoms. Current treatments aim to increase dopamine levels but have limited effectiveness in halting disease progression. Therefore, the development of neuroprotective agents is necessary for better management of Parkinson's disease.
NEUROCHEMISTRY INTERNATIONAL
(2022)
Article
Chemistry, Medicinal
Xiaopeng Peng, Yichang Ren, Wanyi Pan, Jin Liu, Jianjun Chen
Summary: A series of novel acridane-based tubulin polymerization inhibitors were designed, synthesized, and bioevaluated as anticancer agents. The most potent compound NT-6 exhibited high tubulin polymerization inhibitory activity and remarkable antiproliferative potency against four cancer cell lines. NT-6 also showed excellent antitumor efficacy in a melanoma tumor model without apparent toxicity. Importantly, the combination of NT-6 with a small-molecule PD-L1 inhibitor NP-19 decreased tumor burden significantly and enhanced the antitumor immune response.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Rana E. Kamal, Esther Menze, Amgad Albohy, Hebatalla I. Ahmed, Samar S. Azab
Summary: This study evaluated the potential of carvedilol as an anti-Parkinson's drug and anti-tau protein target through computational simulation and in vivo experiments. The results suggest that carvedilol has neuro-protective effects and may be a candidate for the management of Parkinson's disease.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
