Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals DOI Creative Commons
Dong‐Oh Moon

Molecules, Год журнала: 2024, Номер 30(1), С. 91 - 91

Опубликована: Дек. 29, 2024

Cathepsin K plays a pivotal role in bone resorption and has emerged as prominent therapeutic target for treating bone-related diseases such osteoporosis. Despite significant advances synthetic inhibitor development, none have achieved FDA approval due to safety efficacy challenges. This review highlights the potential of phytochemicals alternative inhibitors, emphasizing their natural origin, structural diversity, minimal adverse effects. Key phytochemicals, including AC-5-1, Cycloaltilisin 6, 7, Nicolaioidesin C, Panduratin A, were examined inhibitory activities against cathepsin K. While these compounds exhibit varying IC50 values, docking studies revealed interactions within K’s active site, particularly involving critical residues Cys25 His162. However, challenges lower potency compared inhibitors limited vivo underscore need optimization comprehensive preclinical evaluations. discusses biological insights, current limitations, future strategies advancing phytochemical-based toward clinical applications managing K-associated diseases.

Язык: Английский

Phytochemicals in Drug Discovery - A Confluence of Tradition and Innovation DOI Open Access

Patience Chihomvu,

A. Ganesan, Simon Gibbons

и другие.

Опубликована: Июнь 13, 2024

Phytochemicals have a long and successful history in drug discovery. With recent advancements analytical techniques methodologies, discovering bioactive leads from natural compounds has become easier. Computational like molecular docking, QSAR modelling machine learning, network pharmacology are among the most promising new tools that allow researchers to make predictions concerning products' potential targets, thereby guiding experimental validation efforts. Additionally, approaches LC-MS or LC-NMR speed up compound identification by streamlining processes. Integrating structural computational biology aids lead identification, thus providing invaluable information understand how phytochemicals interact with targets body. Emerging approach is learning involving deep neural networks interrelate phytochemical properties diverse physiological activities such as antimicrobial anticancer effects.

Язык: Английский

Процитировано

6

Living Coral Displays, Research Laboratories, and Biobanks as Important Reservoirs of Chemodiversity with Potential for Biodiscovery DOI Creative Commons
Ricardo Calado, Miguel C. Leal, Ruben X. G. Silva

и другие.

Marine Drugs, Год журнала: 2025, Номер 23(2), С. 89 - 89

Опубликована: Фев. 19, 2025

Over the last decades, bioprospecting of tropical corals has revealed numerous bioactive compounds with potential for biotechnological applications. However, this search involves sampling in natural reefs, and is currently hampered by multiple ethical technological constraints. Living coral displays, research laboratories, biobanks offer an opportunity to continue unravel chemodiversity, acting as "Noah's Arks" that may support molecules interest. This issue even more relevant if one considers reefs face unprecedent threats irreversible losses impair biodiscovery new products, processes, services. displays provide controlled environments studying producing both known metabolites under varied conditions, they are not prone common bottlenecks associated such loss source replicability. Research laboratories focus on a particular species or compound using were cultured ex situ, although differ from wild conspecifics metabolite production quantitative qualitative terms. Biobanks collect preserve specimens, tissues, cells, and/or information (e.g., genes, microorganisms), which offers plethora data study compounds' mode action without having cope issues related access, standardization, regulatory compliance. Bioprospecting these settings faces several challenges opportunities. On hand, it difficult ensure complexity highly biodiverse ecosystems shape chemodiversity corals. other possible maximize biomass fine tune synthesis interest environments. Collaborative efforts needed overcome barriers foster opportunities fully harness before in-depth knowledge pool irreversibly lost due reefs' degradation.

Язык: Английский

Процитировано

0

Neuroprotective insights into epigallocatechin gallate (EGCG) for neurodegenerative disorders DOI Creative Commons
Neha Kamboj,

S.D. Sharma,

Rahul Kumar

и другие.

Exploration of neuroscience, Год журнала: 2025, Номер unknown

Опубликована: Фев. 24, 2025

Neurodegenerative disorders, including Alzheimer’s, Parkinson’s, Huntington’s, and amyotrophic lateral sclerosis, are among the most significant health concerns worldwide, characterized by neuronal dysfunction, oxidative stress, neuroinflammation, protein misfolding. Epigallocatechin gallate, a green tea polyphenol, has been reported to possess multifaceted neuroprotective properties. It reduces stress through free radical scavenging, activation of antioxidant enzymes, stabilization mitochondrial function. also inhibits neuroinflammation modulation key signaling pathways. suppresses amyloid-beta aggregation in Alzheimer’s alpha-synuclein fibrillation thus attenuating toxic accumulation. Its activity induction autophagy promotion synaptic plasticity supports survival However, low bioavailability metabolic instability hinder its translation into clinic. Strategies nanoparticle encapsulation, structural modifications, combination therapies being explored overcome these challenges. Future research could establish epigallocatechin gallate as viable candidate for managing neurodegenerative disorders.

Язык: Английский

Процитировано

0

Mandragora autumnalis Distribution, Phytochemical Characteristics, and Pharmacological Bioactivities DOI Creative Commons
Ghosoon Albahri,

Adnan Badran,

Zaher Abdel Baki

и другие.

Pharmaceuticals, Год журнала: 2025, Номер 18(3), С. 328 - 328

Опубликована: Фев. 26, 2025

In the Mediterranean and Himalayan regions, genus Mandragora (family Solanaceae), sometimes called mandrake, is widely utilized in herbal therapy well-known for its mythical associations. Objective: To compile up-to-date information on M. autumnalis’s therapeutic properties. Its pharmacological properties phytochemical composition are particularly covered managing several illnesses, including diabetes, cancer, heart disease. Methods: Articles review topic were found by searching major scientific literature databases, such as PubMed, Scopus, ScienceDirect, SciFinder, Chemical Abstracts, Medicinal Aromatic Plants Abstracts. Additionally, general online searches conducted using Google Scholar Google. The time frame search included items released from 1986 to 2023. Results:Mandragora has been shown contain a variety of phytochemicals, coumarins, withanolides, alkaloids. characteristics autumnalis, increasing macrophage anti-inflammatory activity, free radicals inhibition, bacterial fungal growth cytotoxic anticancer activities vivo vitro against cancer cell lines, enzyme-inhibitory properties, attributed these phytochemicals. Furthermore, autumnalis also inhibits cholinesterase, tyrosinase, α-amylase, α-glucosidase, radicals. On other hand, metabolic risk factors, inhibition diabetes-causing enzymes obesity, have treated dried ripe berries. Conclusions: Investigations into revealed that this plant rich reservoir new bioactive substances. This aims provide insight botanical ecological summary components antioxidant, antimicrobial, antidiabetic, anticancer, well toxicological implications, where low activity normal VERO line shown. More research necessary ensure efficacy safety. Still, it understand molecular mechanism action behind observed effects clarify potential.

Язык: Английский

Процитировано

0

Anticancer Ribosomally Synthesized and Post-Translationally Modified Peptides from Plants: Structures, Therapeutic Potential, and Future Directions DOI Creative Commons
Hye Jin Hwang,

Youngsang Nam,

Chanhee Jang

и другие.

Current Issues in Molecular Biology, Год журнала: 2024, Номер 47(1), С. 6 - 6

Опубликована: Дек. 26, 2024

Cancer remains a significant medical challenge, necessitating the discovery of novel therapeutic agents. Ribosomally synthesized and post-translationally modified peptides (RiPPs) from plants have emerged as promising source anticancer compounds, offering unique structural diversity potent biological activity. This review identifies discusses cytotoxic RiPPs across various plant families, focusing on their absolute chemical structures reported activities against cancer cell lines. Notably, plant-derived such rubipodanin A mallotumides A-C demonstrated low nanomolar IC50 values multiple types, highlighting potential. By integrating traditional ethnobotanical knowledge with modern genomic bioinformatic approaches, this study underscores importance resource for developing innovative treatments. These findings pave way further exploration RiPPs, emphasizing role in addressing ongoing challenges oncology enhancing repertoire effective therapies.

Язык: Английский

Процитировано

1

Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals DOI Creative Commons
Dong‐Oh Moon

Molecules, Год журнала: 2024, Номер 30(1), С. 91 - 91

Опубликована: Дек. 29, 2024

Cathepsin K plays a pivotal role in bone resorption and has emerged as prominent therapeutic target for treating bone-related diseases such osteoporosis. Despite significant advances synthetic inhibitor development, none have achieved FDA approval due to safety efficacy challenges. This review highlights the potential of phytochemicals alternative inhibitors, emphasizing their natural origin, structural diversity, minimal adverse effects. Key phytochemicals, including AC-5-1, Cycloaltilisin 6, 7, Nicolaioidesin C, Panduratin A, were examined inhibitory activities against cathepsin K. While these compounds exhibit varying IC50 values, docking studies revealed interactions within K’s active site, particularly involving critical residues Cys25 His162. However, challenges lower potency compared inhibitors limited vivo underscore need optimization comprehensive preclinical evaluations. discusses biological insights, current limitations, future strategies advancing phytochemical-based toward clinical applications managing K-associated diseases.

Язык: Английский

Процитировано

1