Article
Biochemistry & Molecular Biology
Kandrakonda Yelamanda Rao, Shaik Jeelan Basha, Kallubai Monika, Navya Naidu Gajula, Irla Sivakumar, Sandeep Kumar, Ramakrishna Vadde, Bindu Madhava Reddy Aramati, Rajagopal Subramanyam, Amooru Gangaiah Damu
Summary: A series of novel quinazolinone and vanillin cyanoacetamide based acrylamide derivatives were designed, synthesized, and evaluated for their activity against Alzheimer's Disease (AD) targets. Five analogs showed elevated inhibitory activity against acetylcholinesterase, selectivity over butyrylcholinesterase, and good radical scavenging activity. These active analogs were non-toxic to cells and exhibited neuroprotective effects. They also demonstrated strong modulation of the A beta aggregation process.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Phoebe F. Lamie, Maha M. Abdel-Fattah, John N. Philoppes
Summary: A novel series of indole-based compounds were designed and synthesised as anti-Alzheimer's and anti-neuroinflammatory agents. Some of the designed compounds showed selectivity for AChE and BuChE inhibitory activities, while others exerted dual inhibitory activities. Additionally, certain compounds demonstrated the ability to inhibit self-induced A beta amyloid aggregation.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Elisa Uliassi, Christian Bergamini, Nicola Rizzardi, Marina Naldi, Angel Cores, Manuela Bartolini, J. Carlos Menendez, Maria Laura Bolognesi
Summary: Multi-target drug discovery is an active field in the search for new drugs against Alzheimer's disease. In this study, a novel set of multi-target-directed ligands (MTDLs) was designed and synthesized, with the most interesting hybrid 3 showing excellent inhibition of cholinesterase enzymes and antioxidant effects. The study uncovered the potential of the quinolinetrione scaffold as a novel motif for anti-amyloid aggregation and antioxidant properties in the development of anti-AD drugs.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Seongmin Park, Mingeun Kim, Yuxi Lin, Mannkyu Hong, Geewoo Nam, Adam Mieczkowski, Jozsef Kardos, Young-Ho Lee, Mi Hee Lim
Summary: This study reports the design of flavonoids that can effectively target multiple pathological elements involved in Alzheimer's disease (AD). The findings reveal key structural features necessary for flavonoids to simultaneously regulate pathogenic targets. Mechanistic studies confirm that the versatile reactivities of the flavonoid are driven by its redox potential and direct interactions with pathogenic factors. This work highlights the potential of multi-target-directed flavonoids as a novel solution in the fight against AD.
Review
Biochemistry & Molecular Biology
Bhupinder Kumar, Amandeep Thakur, Ashish Ranjan Dwivedi, Rakesh Kumar, Vinod Kumar
Summary: Alzheimer's disease is a complex neurological disorder with multiple pathological factors involved. The use of single-target drugs has been unsuccessful in treating the disease, highlighting the importance of multi-target-directed ligands as a potential therapeutic approach.
CURRENT MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Sandipan Chakraborty, Jyotirmoy Rakshit, Jaya Bandyopadhyay, Soumalee Basu
Summary: Through multiple approaches, neohesperidin is found to inhibit both BACE1 and Aβ aggregation, presenting as a potential non-toxic multi-potent scaffold for the development of Alzheimer's disease therapeutics.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Review
Chemistry, Medicinal
Pankaj Teli, Nusrat Sahiba, Jay Soni, Ayushi Sethiya, Dinesh Kumar Agarwal, Shikha Agarwal
Summary: Dementia is a chronic neurodegenerative disease, with Alzheimer's disease being the main cause, posing a national crisis in India with over 4 million cases. Traditional drugs target only one factor, leading scientists to focus on developing multi-target-directed agents incorporating multiple active scaffolds.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Naveen Kumar, Vijay Kumar, Piyush Anand, Vinay Kumar, Ashish Ranjan Dwivedi, Vinod Kumar
Summary: This article discusses various hypotheses for Alzheimer's disease (AD) and the effectiveness of multi target directed ligands (MTDLs) in treating the disease. Different chemical scaffolds and their synthetic strategies are described, along with the identification of important functionalities that have the potential to bind to multiple targets. The study identifies important leads with MTDL characteristics that have the potential to be developed into drug candidates for the effective treatment of AD.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Review
Clinical Neurology
Rohit Bhatia, Sankha S. Chakrabarti, Upinder Kaur, Gaurav Parashar, Anindita Banerjee, Ravindra K. Rawal
Summary: Alzheimer's disease is an age-associated neurodegenerative disorder characterized by memory loss and cognitive decline. The exact pathogenesis of the disease is still unknown, with mechanisms such as decreased acetylcholine concentration and amyloid deposition believed to be involved. Current drugs against Alzheimer's provide only symptomatic relief, prompting the investigation of molecular hybrids as potential multi-target therapies. Coumarin hybrids show promise in targeting multiple pathways associated with Alzheimer's, but further research is needed to fully understand their therapeutic potential.
CURRENT ALZHEIMER RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Zhipei Sang, Qing Song, Zhongcheng Cao, Yong Deng, Li Zhang
Summary: A series of novel chalcone-Vitamin E-donepezil hybrids were designed and synthesized for treating Alzheimer's disease. Compound 17f showed potent enzyme inhibitory activity, antioxidant properties, and anti-aggregation effects, as well as neuroprotective effects in vitro.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Namy George, Bushra Al Sabahi, Majed AbuKhader, Khalid Al Balushi, Md Jawaid Akhtar, Shah Alam Khan
Summary: This study synthesized a variety of coumarin-linked 1,3,4-oxadiazole hybrid derivatives and investigated their in vitro anticholinesterase, antioxidant, and anti-inflammatory activities through experimental assays and computational docking studies. The results suggest that these compounds have potential as anti-Alzheimer's drugs.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Silvia Chaves, Katalin Varnagy, M. Amelia Santos
Summary: Alzheimer's disease is the most common and severe neurodegenerative disorder worldwide, with currently available drugs providing only temporary symptomatic relief. Research indicates that the onset and progression of AD are influenced by multiple factors, highlighting the need for the development of multitarget-directed ligands to target various pathological pathways.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Georgios Papagiouvannis, Panagiotis Theodosis-Nobelos, Panos N. Kourounakis, Eleni A. Rekka
Summary: Researchers have been investigating the potential of multi-target directed compounds with antioxidant and/or anti-inflammatory properties for the treatment of Alzheimer's Disease, which has only symptomatic efficacy with current treatments.Various novel compounds with these properties have shown promising results in the treatment of neurodegenerative disorders.
MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Guoxing Wang, Jiyu Du, Jie Ma, Peipei Liu, Siqi Xing, Jucheng Xia, Shuanghong Dong, Zeng Li
Summary: In this study, two series of tryptanthrin derivatives with benzenesulfonamide substituents were synthesized and evaluated as potential multifunctional agents for the treatment of Alzheimer's disease (AD) using the multi-target-directed ligands approach. The derivatives demonstrated good cholinesterase inhibitory activity and neuroprotective properties. Compound 4h showed promising dual inhibitory effects on acetylcholinesterase and butyrylcholinesterase, as well as the potential to prevent the formation of amyloid plaques. It also exhibited significant anti-neuroinflammatory potency and suitable blood-brain barrier permeability. In vivo studies further confirmed the effectiveness of compound 4h in ameliorating learning and memory impairment in an AD mouse model.
Review
Chemistry, Medicinal
Siew Lee Cheong, Jian Kai Tiew, Yi Hang Fong, How Wan Leong, Yew Mun Chan, Zhi Ling Chan, Ethan Wei Jie Kong
Summary: Alzheimer's disease is a neurodegenerative disorder with complex pathophysiology. Current treatment mainly focuses on symptom relief. Due to the multifactorial origin of the disease, multi-target strategies have been proposed. This review provides an overview of the pathogenesis of Alzheimer's disease, current drug therapies, and the rationale and examples of multi-target drugs.
Article
Behavioral Sciences
Kholoud M. Al-Otaibi, Badrah S. Alghamdi, Maryam A. Al-Ghamdi, Rasha A. Mansouri, Ghulam Md Ashraf, Ulfat M. Omar
Summary: The combination of vitamin D3 and siponimod can enhance remyelination and modulate microglia phenotypes, leading to improved symptoms and protection of the myelin sheath in multiple sclerosis (MS) patients.
FRONTIERS IN BEHAVIORAL NEUROSCIENCE
(2023)
Review
Neurosciences
Mahmoud A. Ebada, Abdalrhman Mostafa, Al-Hussein A. Gadallah, Souad Alkanj, Badrah S. Alghamdi, Ghulam Md Ashraf, Adel M. Abuzenadah, Raed F. Alserihi, Ahmed Wadaa-Allah, Mohamed Salama
Summary: Finding a link between hormones and microRNAs (miRNAs) is valuable for adjusting genetic composition or cellular functions without gene-level interventions. The cleavage of precursor miRNAs by dicer is an interface link between miRNA and its regulators, disruption of which can affect neurogenesis. Hormonal regulation of miRNAs occurs directly through binding to miRNA promoter elements and indirectly through regulation of post-transcriptional processing proteins' signaling effects. Estrogenic hormones play a significant role in regulating miRNAs in the brain, and their relationship with miR-29, miR-9 could be an etiological route for various neurodegenerative disorders.
Review
Medicine, General & Internal
Manisha Singh, Vinayak Agarwal, Divya Jindal, Pranav Pancham, Shriya Agarwal, Shalini Mani, Raj Kumar Tiwari, Koushik Das, Badrah S. Alghamdi, Tukri S. Abujamel, Ghulam Md. Ashraf, Saurabh Kumar Jha
Summary: The widespread use of corticosteroids has led to an increase in corticosteroid-induced neuropsychiatric disorders. These disorders range from depression and insomnia to panic attacks and overt psychosis. This study explores the concerns surrounding these disorders, molecular biology approaches to improve therapy, and potential gene-editing-based therapeutic strategies.
Review
Cell Biology
Subham Preetam, Swathi Jonnalagadda, Lamha Kumar, Rajeswari Rath, Soham Chattopadhyay, Badrah S. Alghamdi, Adel M. Abuzenadah, Niraj Kumar Jha, Akash Gautam, Sumira Malik, Ghulam Md Ashraf
Summary: Parkinson's disease is the second most common neurodegenerative disorder, and the delivery of therapeutic compounds is hindered by the blood-brain barrier. Lipid nanosystems have been used for the precise delivery of therapeutic compounds in anti-PD therapy. This review discusses the application and clinical significance of lipid nanosystems in delivering therapeutic compounds for anti-PD treatment.
AGEING RESEARCH REVIEWS
(2023)
Review
Neurosciences
Ishfaq Ahmad Ahanger, Ghulam Md. Ashraf, Anurag Sharma, Asimul Islam
Summary: Protein misfolding and aggregation is a generic propensity of proteins that is still not fully understood. It is a major concern in biology and medicine due to its association with various debilitating human proteinopathies and neurodegenerative diseases. The mechanism of protein aggregation, associated diseases, and the development of therapeutic strategies against these diseases present significant challenges.
CNS & NEUROLOGICAL DISORDERS-DRUG TARGETS
(2023)
Review
Neurosciences
Faraz Ahmad, Siva Ramamorthy, Mohammed Y. Areeshi, Ghulam Md. Ashraf, Shafiul Haque
Summary: Mitochondria play important roles in neuronal development, physiology, plasticity, and pathology through their regulation of bioenergetic, calcium, redox, and cell survival/death signaling. However, a comprehensive discussion on the relevance of isolated brain mitochondria in neuroscience research has been lacking. This mini-review explores the commonly used analytical assays for assessing mitochondrial physiology and dysfunction in organello, with a focus on neuroscience research. It also provides protocols for isolating mitochondria, assessing their quality, and preserving them for future use.
CURRENT NEUROPHARMACOLOGY
(2023)
Review
Neurosciences
Md. Mominur Rahman, Mst. Afroza Alam Tumpa, Md. Saidur Rahaman, Fahadul Islam, Popy Rani Sutradhar, Muniruddin Ahmed, Badrah S. S. Alghamdi, Abdul Hafeez, Athanasios Alexiou, Asma Perveen, Ghulam Md. Ashraf
Summary: Mitochondria are crucial for cellular homeostasis and metabolism in eukaryotes, especially in brain functions. Dysfunction of mitochondria is associated with neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, Huntington's disease, and amyotrophic lateral sclerosis. This review focuses on the mitochondrial disturbances in these disorders and discusses the potential use of mitochondrial drugs for their treatment and control, including mitochondrial antioxidants, mitochondrial permeability transition blockade, and mitochondrial gene therapy.
CURRENT NEUROPHARMACOLOGY
(2023)
Editorial Material
Neurosciences
Md. Sahab Uddin, Badrah S. Alghamdi, Ghulam Md. Ashraf
CURRENT NEUROPHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Syed Sarim Imam, Sadaf Jamal Gilani, Ameeduzzafar Zafar, May Nasser Bin Jumah, Sultan Alshehri
Summary: The present study aimed to develop MZBSo bilosomes and MZBSo gel. MZBSo presented nano-sized vesicles with high entrapment efficiency and suitable ζ potential, while MZBSoG2 showed good pH, viscosity, spreadability, and a slower drug release. MZBSoG2 was non-irritant and exhibited significant antifungal activity. Stability study results showed no significant changes. MZ-loaded gels could improve therapeutic efficacy.
Article
Plant Sciences
Fatimah Al-Otibi, Nourah A. A. Alshammry, Raedah I. I. Alharbi, May N. N. Bin-Jumah, Maha M. M. AlSubaie
Summary: The aqueous and ethanolic extracts of Artemisia sieberi showed significant antibacterial and antifungal effects against various microorganisms. Additionally, the synthesized silver nanoparticles from the A. sieberi extract exhibited stronger antibacterial properties. This research suggests that A. sieberi has potential as an antimicrobial agent.
Article
Biology
Bothina Mohammed Alharbi, Tahani H. Albinhassan, Razan Ali Alzahrani, Abderrezak Bouchama, Sameer Mohammad, Awatif Abdulaziz Alomari, May Nasser Bin-Jumah, Entissar S. AlSuhaibani, Shuja Shafi Malik
Summary: Rising temperatures and heat waves caused by climate change are detrimental to human health. Exposure to extreme heat during heat waves can cause heat-related illnesses, including heat stroke, which can result in permanent disability. Heat can damage proteins, leading to their misfolding and aggregation, which can be neurotoxic and contribute to neurodegenerative disorders.
Article
Chemistry, Inorganic & Nuclear
Imran Ali, Yasir Jamil, Saeed Ahmed Khan, Yunxiang Pan, Aqeel Ahmed Shah, Ali Dad Chandio, Sadaf Jamal Gilani, May Nasser Bin Jumah, Yusra Fazal, Jun Chen, Zhonghua Shen
Summary: The qualitative study of copper-cobalt ingot sample was conducted using laser induced breakdown spectroscopy (LIBS), and CuCo2O4 nanoparticles were synthesized using the alloy as a target material for Nd:YAG laser ablation. The composition and morphology of the synthesized nanoparticles were determined using various techniques including X-ray diffraction (XRD), energy dispersive X-ray (EDX) analysis, transmission electron microscopy (TEM), scanning electron microscopy (SEM), and dynamic light scattering (DLS). The synthesized nanoparticles exhibited antibacterial activity and potential for magnetic hyperthermia.
Article
Chemistry, Inorganic & Nuclear
Imran Ali, Jun Chen, Saeed Ahmed Khan, Yasir Jamil, Aqeel Ahmed Shah, Abdul Karim Shah, Sadaf Jamal Gilani, May Nasser Bin Jumah, Yusra Fazal, Yunxiang Pan, Zhonghua Shen
Summary: Magneto-plasmonic Ag/Ni and Ag/Fe nanoparticles were synthesized using a dual-pulsed Q-switched Nd:YAG 1064 nm laser ablation method. The optical and magnetic properties were investigated, and the morphologies and phase structures of the nanoparticles were characterized. The synthesized nanoparticles exhibited plasmonic hyperthermia properties, reaching high temperatures when irradiated with a NIR 808 nm laser. These findings suggest the potential use of silver-based plasmonic nanoparticles for hyperthermia treatment.
Review
Environmental Sciences
Rajnish Kumar, Garima Yadav, Mohammed Kuddus, Ghulam Md Ashraf, Rachana Singh
Summary: The metagenomics approach revolutionized the study of genetic information from uncultured microbes and complex microbial communities. In silico research allowed for a better understanding of protein interactions, drug design, and microbial evolution. Artificial intelligence, particularly machine learning and deep learning, has enabled the analysis and utilization of large datasets generated from nucleic acid sequencing and proteomics, leading to breakthroughs in microbiology research.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Manoj M. Gadewar, G. K. Prashanth, Prabhu Chandra Mishra, Ghulam Md Ashraf, Majed N. Almashjary, Steve Harakeh, Vijay Upadhye, Abhijit Dey, Pallavi Singh, Niraj Kumar Jha, Saurabh Kumar Jha
Summary: This study evaluated the antioxidant, antidiabetic, and anti-hyperlipidaemic activity of methanolic fruit extract of Solanum indicum in streptozotocin-induced diabetic rats. The results showed that the fruit extract significantly reduced blood glucose levels and inhibited the activity of α-amylase and α-glycosidase. It also decreased cholesterol and triglyceride levels in the blood and prevented oxidative stress associated with type II diabetes.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2023)
