Current Bioactive Compounds - Volume 21, Issue 8, 2025

Epilepsy is a growing concern for the scientific community globally as less than 80% of individuals experience reduced seizure severity with existing antiepileptic medications and the chances of relapses are very high with those medications. Therefore, the existing problem requires more attention to unravel the chances of relapses and adverse effects of available medications. Isoindole-1,3-diones serve as a valuable scaffold with diverse biological activities, including analgesic, anti-inflammatory, and hypolipidemic properties. This review will emphasize the antiepileptic behaviours of the Isoindole-1,3-diones with diversified synthetic procedures and modes of action. For this purpose, an extensive literature survey was undertaken through different online platforms such as PubMed, Web of Science, Scopus, SciFinder, Google Scholar, Science Direct, etc. Some N-substituted Isoindole-1,3-diones have demonstrated promising anticonvulsant activity, primarily by effectively blocking sodium channels. Epilepsy is often linked to channelopathies involving α, and β-subunits, and medications have specific mechanisms for binding with the α-subunit of the sodium channel. Analyzing the structural features of phenytoin, carbamazepine, and lamotrigine revealed that benzene or phenol substitution, along with the addition of a chloro group, enhances their activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) tests. This review focuses on the role of specific sodium channels in electrical signalling and neurological conditions, emphasizing the significance of Isoindole-1,3-diones and their derivatives in designing potent anticonvulsant agents, particularly in the development of selective sodium channel inhibitors.

Bakuchiol, a meroterpene natural product found in various plants, exhibits diverse biological activities, notably anticancer properties. Researchers have synthesized numerous analogs targeting different positions, such as alcoholic OH, ethenyl, and isopropylidene groups within bakuchiol, aiming to enlighten potent therapeutic agents with enhanced pharmaceutical characteristics. The review aims to focus on the extensive potential of the bioactive molecule, bakuchiol describing SAR that may lead to the development of a variety of bakuchiol derivatives. Literature survey has been carried out to determine the potential of bakuchiol and its derivatives. This review comprehensively outlines the biosynthesis, isolation, patent, and clinical studies of bakuchiol, and pharmacological potential of bakuchiol derivatives documented to date. Additionally, it explores the structure-activity relationships observed in its derivatives. Collectively, findings from various studies underscore the significant potential of bakuchiol and its derivatives in the development of potent anticancer and other therapeutic agents. Ultimately, this review serves as a valuable resource for researchers interested in both the chemistry and biology of bakuchiol, offering insights into its multifaceted applications and paving the way for further exploration in this field.

The aurone derivatives are a subfamily of flavonoids. Aurones can be easily broken down into two major parts, a benzofuranone and an exocyclic arylidene, often made from an aldehyde, despite having the normal 15-carbon structure. However, aurone derivatives have recently received considerable attention due to their diverse biological effects. These derivatives are synthesized by different chemical methods and exhibit different types of biological actions such as antibacterial, antiviral, antimalarial, anticancer, antiplasmodial, antiparasitic, anti-inflammatory, antioxidant, and other beneficial biological activities. Furoaurone (a semi-synthetic compound), also known as benzofuran-3(2H)-one, is made from naturally occurring furanochromones collected from Ammivisnaga fruits. In this review, we study the numerous synthetic techniques for aurone and furanone derivatives and various biological functions.

The prevalence of diabetes mellitus continues to be a worldwide health concern, which calls for the ongoing investigation of novel therapeutic options. This review aims to examine the developing field of herbal dipeptidyl peptidase-4 (DPP-4) inhibitors as a potentially useful approach to managing diabetes. Because of their ability to suppress the breakdown of incretin hormones, DPP-4 inhibitors have become increasingly popular due to their role in improving glycemic control. This review focuses on the rising evidence supporting the efficacy and safety of herbal alternatives, although synthetic DPP-4 inhibitors have been used extensively in the past. The pharmacological actions of several herbal substances with DPP-4 inhibitory characteristics are extensively examined in this review. These natural chemicals have anti-inflammatory, antioxidant, and anti-diabetic properties derived from traditional medicinal plants. This study also sheds light on the molecular processes via which these herbal medicines inhibit DPP-4. In addition, the study assesses the efficacy of herbal DPP-4 inhibitors in both animal and human studies, providing a critical evaluation of both types of research. The research of natural alternatives to synthetic pharmaceuticals not only broadens the therapeutic landscape but also highlights the significance of merging traditional wisdom with modern scientific breakthroughs. This is because natural alternatives were not previously available. Herbal DPP-4 inhibitors may emerge as significant additions to the arsenal of anti-diabetic drugs as research in this field continues to advance. These inhibitors would provide a holistic and sustainable approach to the treatment of diabetes.

Cancer is a highly fatal disease that is typified by aberrant cells proliferating out of control. The properties of acquired cells, including as genomic instability and mutations, cellular death evasion, and proliferative signaling sustenance, are evidenced by the hallmarks of cancer and contribute to the establishment of malignant tumors. A protein called poly(ADP-ribose) polymerase-1 (PARP1) is essential for both cell survival and DNA damage repair, two processes that affect cellular control. Since homologous recombination deficient cells exhibit cellular death upon suppression of PARP1, the PARP protein has gained attention as a potential target for anticancer treatments. The Food and Drug Administration (FDA) has already approved a number of effective PARP1 inhibitors, including olaparib and niraparib. The final chemical has a 1,3,4-thiadiazole core in its structure. In fact, heterocyclic moieties have gained attention due to their numerous medicinal advantages, which include their capacity to combat cancer. The compounds derived from these substances have been studied as PARP1 inhibitors, with promising results. Thus, the goal of this study is to go over the importance of PARP1 in cancer as well as its role in cell regulation. It also attempts to offer a comprehensive assessment of the literature that has been published in the previous fifteen years about PARP1 inhibitors, including the different scaffolds, with an emphasis on features of the structure-activity relationship. This will provide vital information for the creation of fresh, more effective PARP1 inhibitors.

Current developments provide an overview of alginate electrospinning for biopolymers in pharmaceutical and biological applications, but their volatile nature and susceptibility to degradation pose challenges to their storage and use. Due to their innate medicinal qualities, pure essential oils have drawn a lot of attention to their many uses, such as aromatherapy and medicine. However, the stability, regulated release, and sustained efficacy of EOs are complicated by their brittleness and sensitivity. Bio-based small carriers as well as polymers have recently come to light as a viable solution to these problems. To improve the stability and therapeutic efficacy of essential oils, this review study investigates the novel use of bio-based microcarriers and polymers. By encapsulating essential oils within biocompatible materials, such as microcarriers and polymers derived from natural sources, researchers have been able to extend their shelf life, improve their controlled release, and enhance their bioavailability. The general stability, as well as bioavailability of these encapsulated EOs, are improved by the interaction of the natural qualities of essential oils with the specific properties of bio-based polymers. This paper examines the design and manufacturing concepts of bio-based microcarriers, emphasizing encapsulating techniques and the variables affecting release kinetics. Additionally, it highlights the potential uses of EO-loaded tiny carriers in various fields, such as cosmetics, agriculture, and medicine. This paper also delves into recent advancements in this field, discussing the fabrication techniques, characterization methods, and application areas of bio-based microcarriers and polymers for essential oil delivery.

Phenothiazine derivatives are a significant class of heterocyclic compounds with a wide range of pharmacological activities. Among these, their antioxidant properties have garnered considerable interest due to potential therapeutic applications in mitigating oxidative stress-related diseases. A new series of phenothiazine derivatives [5a-5h] was reported, produced by conjugating phenothiazine with arylamines via an acetyl group. The freshly synthesized compounds were analyzed using MS spectroscopy, ¹H-NMR, and ¹³C-NMR spectral analysis. Two in vitro pharmacological techniques-human low-density lipoprotein (LDL) oxidation inhibition assay and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay-were used to measure the antioxidant activity. While all the conjugates showed good antioxidant activity, compound 5h exhibited less antioxidant activity. However, compound 2e, which contains a 4-amino-2-methoxyphenol moiety, demonstrated strong antioxidant activity in all experiments and was found to be more effective than the reference antioxidant butylated hydroxyanisole (BHA). This study aims to synthesize a series of novel phenothiazine derivatives, characterize their structures using various analytical techniques, and evaluate their antioxidant activities. A series of phenothiazine derivatives were synthesized using standard organic synthesis protocols. The chemical structures of the synthesized compounds were confirmed using spectroscopic methods, including Nuclear Magnetic Resonance (NMR), Infrared (IR) spectroscopy, Mass Spectrometry (MS), and, where applicable, X-ray crystallography. The synthesized phenothiazine derivatives were successfully characterized by ¹H-NMR, ¹³C-NMR, IR, and MS, which confirmed the expected molecular structures. The purity of the compounds was determined using High-Performance Liquid Chromatography (HPLC). The antioxidant activities of the derivatives were evaluated using the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assay, the ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)) assay, and the FRAP (Ferric Reducing Antioxidant Power) assay. The results demonstrated that several of the synthesized phenothiazine derivatives exhibited significant antioxidant activity, with some compounds showing higher potency than standard antioxidants, such as ascorbic acid and Trolox. The structure-activity relationship (SAR) analysis indicated that the presence of electron-donating groups on the phenothiazine ring enhanced antioxidant activity.

The impact of naturally occurring flavonoids on human health and illnesses is crucial, as they are closely linked to dietary components and human health. Flavonoids may be able to shield people against disease in both in vitro and in vivo research settings. The flavonoid chrysin has demonstrated several intriguing pharmacological properties, including immune modulation, anti-cancer, anti-diabetic, antidepressant, and anti-asthmatic effects. Furthermore, it showed possible defenses against various toxins in the liver, brain, kidney, and heart, among other organs. Numerous investigations have been carried out to investigate potential targets for its potential mechanism of action. However, because of its low oral bioavailability, its medicinal uses have been restricted. Its broad first-pass metabolism is the leading cause of its low bioavailability. There hasn't been a thorough discussion of the pharmacological characteristics of chrysin and the molecular targets that are related to it yet. Therefore, this review aims to provide a comprehensive overview of chrysin, focusing on its chemical structure, natural sources, pharmacokinetics, toxicity profile, molecular targets, and medicinal properties. By synthesizing current research findings, this paper aims to highlight the therapeutic potential of chrysin, discuss its safety and efficacy, and identify areas for future research.

The traditional use of medicinal plants holds a wealth of ancient wisdom that inspires modern research. Piper betle, generally recognized as betel leaf, is valued in traditional medicine systems across various cultures for its diverse health benefits. The betel leaves have several significant uses as antioxidant, anti-inflammatory, and antiapoptotic activity which help in neuroprotection. Many phytochemicals are present in the betel leaves, including hydroxychavicol, caryophyllene, eugenols, tannins, and polyphenols, which have positive activity on neurological and other cognitive impairments. Some studies have shown that Piper betle has a cholinergic activity that directly decreases the butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), which are significantly associated with reduced levels of Acetylcholine (Ach) levels in cholinergic dysfunction. This review article delves into the historical significance of Piper betle in traditional medicine and its relevance to contemporary neuropharmacology. By revisiting the age-old wisdom surrounding Piper betle, we aim to uncover its potential as a valuable source of natural neuropharmacological agents for various neurological conditions.