No drug has been approved to prevent neuronal cell loss in patients suffering from Parkinson's disease (PD) or Alzheimer's disease (AD); despite increased comprehension of the underlying molecular causes, therapies target cognitive functional improvement and motor fluctuation control. Drug design strategies that adopt the "one protein, one target" philosophy fail to address the multifactorial aetiologies of neurodegenerative disorders such as AD and PD optimally. On the contrary, restoring neurotransmitter levels by combined combinatorial inhibition of cholinesterases, monoamine oxidases, and adenosine A 2A A receptors, in conjunction with strategies to counter oxidative stress and beta-amyloid plaque accumulation, would constitute a therapeutically robust, multitarget approach. This extensive review delineates the therapeutic advantages of combining dual-acting molecules that inhibit monoamine oxidases and cholinesterases and/or adenosine A 2A A receptors, and describes the structure-activity relationships of compound classes that include, but are not limited to, alkaloids, coumarins, chalcones, donepezil-propargylamine conjugates, homoisoflavonoids, resveratrol analogs, hydrazones, and pyrazolines. In the wake of recent advances in network biology, in silico approaches, and omics, this review emphasizes the need to consider conceptually informed research strategies for drug discovery, in the context of the mounting burden posed by chronic neurodegenerative diseases with complex aetiologies and pathophysiologies involving multiple signalling pathways and numerous drug targets. K E Y W O R D Sacetylcholinesterase, adenosine antagonist, monoamine oxidase, multitarget
: The development of chalcone-based compounds for CNS disorders has been explored by many research groups. Chalcones are being considered as a potent organic scaffold with widespread applications in the field of drug discovery and medicinal chemistry. The planar or semi-planar geometry of chalcones with various functionalities impinged on the terminal aromatic systems renders the molecule its bio-activity including anti-cancer, anti-malarial, anti-microbial, anti-fungal, antileishmanial, anti-viral, anti-diabetic, anti-hypertensive properties, etc. Moreover, cutting-edge research has been executed in the domain of Central Nervous System (CNS) based scheme, further, their identification and classifications also remain of high interest in the field of medicinal chemistry but the specific reviews are limited. Hence, the present review highlights the significance of chalcones toward their CNS activities (up to 2019), which include anti-depressant activity, anxiolytic activity, activity with GABA receptors, acetylcholinesterase (AChE) and butyryl cholinesterase (BChE) inhibitions, activity as adenosine receptor antagonists anti-Alzheimer’s agents, β-amyloid plaques imaging agents, monoamine oxidase inhibition. To our knowledge, this is the first review exclusively for CNS activity profile of chalcones.
Nanotechnology has emerged as one of the leading research areas involving nanoscale manipulation of atoms and molecules. During the past decade, the growth of nanotechnology has been one of the most important developments that have taken place in the biomedical field. The new generation nanomaterials like Quantum dots are gaining much importance. Also, there is a growing interest in the development of nano-theranostics platforms in medical diagnostics, biomedical imaging, drug delivery, etc. Quantum dots are also known as nanoscale semiconductor crystals, with unique electronic and optical properties. Recently, silicon quantum dots are being studied extensively due to their less-toxic, inert nature and ease of surface modification. The silicon quantum dots (2-10nm) are comparatively stable, having optical properties of silicon nanocrystals. This review focuses on silicon quantum dots and their various biomedical applications like drug delivery regenerative medicine and tissue engineering. Also, the processes involved in their modification for various biomedical applications along with future aspects are discussed.
: Cancer, a global havoc is a group of debilitating diseases that strikes family as well as society. Cancer cases are drastically increasing these days. In spite of many therapies and surgical procedures available cancer is still difficult to control. These are due to limited effective therapies or targeted therapies. Natural products can produce lesser side effects to the normal cells which are the major demerit of chemotherapies and radiation. Wogonin, a natural product extracted from plant, Scutellaria baicalensis has been studied widely and found with a high caliber to tackle most of the cancers via several mechanisms that include intrinsic as well as extrinsic apoptosis signaling pathways, carcinogenesis diminution, telomerase activity inhibition, metastasis inhibition in the inflammatory microenvironment, anti-angiogenesis, cell growth inhibition and arrest of cell cycle, increased generation of H2O2 and accumulation of Ca2+ and also as an adjuvant along with anticancer drugs. This article discusses the role of wogonin in various cancers, its synergism with various drugs and the mechanism by which wogonin controls tumor growth.
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