Current Topics in Medicinal Chemistry - Volume 25, Issue 17, 2025

Circadian rhythms of innate 24 h cycles comprise well-conserved biological phenomena from cyanobacteria to mammalian. They are driven by light and regulated by clock genes that work as transcription factors and control the expression of many other genes and physiological functions in the cells. The expression of ~ 40% of protein-coding genes shows 24 h oscillation patterns in mice, implying their importance in normal body functions. Indeed, the physiological and behavioural rhythmicity generated through clock genes-mediated multiple mechanisms affects the quality of life at large. Disrupted circadian rhythmicity is associated with several kinds of diseases. For example, cancer cells show abnormal expression patterns for circadian rhythm genes that have been shown to regulate oncogenesis, drug responses, and disease prognosis. Furthermore, the modern globalisation of human lifestyle and business and social activities have disrupted innate circadian rhythm, resulting in a variety of diseases through disrupted humoral, immunological, and neuronal pathways. Safe and sustainable modulation of circadian rhythm has become a prevalent need that warrants basic and interventional research, as well as clinical investigations. Although traditional systems of medicine suggest some natural compounds with circadian rhythm- modulating potential, most of these have not been validated in laboratory or clinical studies. Reliable read-outs of the effects of test compounds on circadian rhythmicity have been limited by the availability of live cell assays. We have, herein, provided an overview of living cell-embedded real-time reporter gene assays designed for screening compounds that modulate circadian rhythm, and discussed the potential of some natural compounds for circadian rhythm modulation as validated by cell-based assay systems, and their role in disease therapeutics.

For many centuries, traditional medicine has played an essential role in health care. The treatment of many illnesses, including cancer, has greatly benefited from using herbal remedies derived from traditional medicine. The bioactive compounds, such as curcumin, silibinin, berberine, ginseng, and others present in traditional medicine have shown a wide range of properties, such as anti-inflammatory, antimicrobial, anti-oxidant as well as potent anti-cancer properties both in laboratory studies and animal experiments (in vitro and in vivo). In this review, we mainly emphasized the anticancer role of bioactive compounds present in traditional medicine, such as curcumin, cardamonin, piperine, berberine, ginseng, silibinin, epigallocatechin gallate, and asafoetida. We also discussed molecular evidence of these compounds in chemoprevention and anticancer effects. These compounds have the potential to interfere with cancer growth, proliferation, metastasis, and angiogenesis and induce apoptosis by targeting different pathways and the cell cycle. This review article also focuses on how these compounds can help overcome drug resistance and enhance the availability of other clinically approved drugs. The usage of these compounds synergistically with other forms of treatment is also of great fascination to new and upcoming research. Finally, we have discussed the bioavailability of these compounds and strategies employed to improve them so their full potential can be exploited.

Cancer stands as a prominent global cause of mortality, with chemotherapy using synthetic drugs being the predominant treatment method. Despite its high success rate, this approach is constrained by substantial side effects. Herbal medicines, known for their diverse bioactive components, exhibit promising anticancer attributes. The drug delivery systems can improve the precision of delivering these herbal compounds, enhancing efficacy while minimizing potential side effects. Various platforms, such as nanoparticle-based carriers, liposomes, and polymeric micelles, are investigated for encapsulating and delivering herbal components to cancer cells. These systems not only enhance the bioavailability of herbal compounds but also facilitate controlled release, sustained drug circulation, and improved cellular uptake. This comprehensive review focuses on the recent advancement in the field of drug delivery systems employed in the delivery of plant-derived anticancer compounds. It categorizes carriers into organic and inorganic nanoparticles, addressing their application in enhancing the safety and efficacy of plant-derived anticancer compounds alongside associated challenges. The review concludes by outlining recent investigations into drug delivery systems aimed at increasing the efficacy of plant-derived anticancer compounds. Future research in this field should emphasize experiments in animal models and potential clinical translation.

Diosmetin, also known as 3´, 5, 7-trihydroxy-4´-methoxyflavone, is a bioflavonoid that can be found in several food sources. These include mainly citrus fruits and plants, such as Rosmarinus officinalis, Citrus sinensis, Galium verum, and Rosa agrestis. It has been shown that diosmetin has pharmacological actions that include neuroprotective, antioxidant, and anticancer properties. The objective of this manuscript is to provide a comprehensive review of the pharmacological, pharmacokinetic, and toxicological profile of diosmetin. The information has been collected from several research papers found in various databases, including Web of Science, Pubmed, Scopus, and ScienceDirect. Diosmetin has the potential to reduce inflammation, and it can also improve vascular functions and protect against oxidative stress, both of which are essential for the prevention and management of several diseases.