Current Bioactive Compounds - Volume 20, Issue 1, 2024

Background: Emesis is a complex and distressing protective mechanism that helps to remove toxic substances from the stomach and prevent further ingestion. The emetics and cathartics are predominantly used for accidental and intentional ingestion of poisons or toxins. The availability and usage of emetics in humans are limited because of their side effects. Therefore, to treat poisoned people, we need effective medications. Sapindus emarginatus Vahl., often called soapnut, is a member of the Sapindaceae family. They have historically been used as emetic, antipruritic, laxative, antifertility, and anti-inflammatory medicines. Objective: This study aims to assess the gut serotonin level and emetic effect of Sapindus emarginatus hydroethanolic pericarp extract (HESE) by using animal models. Methods: Gravimetric analysis was used to determine the HESE's saponin content. The emetic effect of the HESE at a dose of 250, 500, 1000, and 2000 mg/kg was evaluated by copper sulfateinduced emesis in the chick model and cisplatin-induced emesis in the rat-pica model. The serotonin level in rat intestinal mucosa was measured by spectrofluorimetry. Results: HESE was estimated to contain 11.92% saponin. The extract at high doses of 1000 and 2000 mg/kg showed emetic activity evidenced by increased frequency of retching in chick, increased kaolin intake, and anorexia in the rat-pica model. The extract showed a significant increase in serotonin levels in the proximal part of the small intestine in comparison with normal animals. Conclusion: According to the results of the current investigation, which employed various animal models, the HESE demonstrated appreciable emetic activity. The extract at a high dose showed a significant emetic effect due to increased serotonin levels in the gut. The HESE was discovered to be a strong contender for the treatment of poisoned patients. More research are required to validate their adverse effects of frequent usage.

Background: Curcumin is a natural compound obtained from Curcuma longa that possesses a vast therapeutic potential for disease treatment. It is a potent anticancer, anti-inflammatory, antioxidant, and anti-aging phytochemical as evident from numerous studies. Curcumin's antiinflammatory and antioxidant properties are thought to be more potent than its other biological actions. Curcumin's anti-inflammatory properties can lead to an improvement in symptoms and make it a viable candidate for the treatment and prevention of pro-inflammatory disorders. Objective: The goal of this review is to analyse curcumin's anti-inflammatory properties and mechanisms in the treatment of various disorders. The effect of different curcumin-based nanoformulations on anti-inflammatory potential is also reviewed, as the therapeutic use of curcumin is influenced by its solubility, bioavailability, and pharmacokinetic profile. Methodology: The literature searched during the last ten years using keywords such as curcumin, anti-inflammatory mechanisms, cytokines, and nanoformulations from multiple databases, such as PubMed, Science Direct, Scopus, and others. The quality research and review articles containing the aforementioned keywords were chosen for this review article. Conclusion: This review focuses on the anti-inflammatory properties of curcumin against a variety of inflammatory disorders that arise over the course of various illnesses. It also emphasises the importance of developing alternative nanoformulations to address the limitations of curcumin usage. Further, it will aid the scientific community's understanding of curcumin and its anti-inflammatory mechanisms, prompting them to devise innovative treatment options.

Background: Olive oil is rich in monounsaturated fatty acids and is an essential Mediterranean diet component. Many of its health benefits are associated with the presence of phenolic compounds. Several strategies for the enhancement of the phenolic content and, more specifically, the concentration of hydroxytyrosol derivatives in olive oils have been proposed, as extra virgin olive oil (EVOO) of high phenolic content is preferred by health-conscious consumers. Methods: The supplementation of EVOO with hydroxytyrosol derivatives from olive leaf extract was performed with the employment of ultrasound-assisted maceration at different concentration levels (2 g·L^-1 oil and 4 g·L^-1 oil), temperatures (20 and 40°C), and maceration times (20 and 40 min). The phenolic contents of enriched EVOOs were determined by spectrophotometric and HPLC methods. In addition, the effect of supplementation on the physicochemical parameters of EVOOs, namely acidity and extinction coefficients (K232 and K270), was also studied. Results: The addition of extract slightly increased the acidity values and extinction coefficients of the samples, and at the same time, it significantly improved their phenolic composition. The use of appropriate ultrasound-assisted maceration parameters (addition of olive leaf extract at a concentration level of 2 g L^-1 at 20°C for 20 min) provided EVOO with acceptable values for total acidity (<0.8%), K232 (<2.5), and K270 (<0.22), high contents of total phenolics and flavonoids, and improved hydroxytyrosol derivative contents. Conclusion: The enrichment of EVOO with leaf extract is a promising strategy to enhance its content in hydroxytyrosol derivatives, providing premium EVOOs with respect to their bioactive composition.

Background: Several concerns regarding the safety of sodium benzoate/ascorbic acid combination have been highlighted in various scientific investigations. However, there is a dearth of scientific literature on its effect on the brain. This study investigated the effects of dry-feed added sodium benzoate/ascorbic acid combination on neurobehaviour, oxidative stress, and inflammatory cytokines in mice. Methods: Adult male mice were assigned into ten groups of 10 mice each. One group was fed a standard diet, three groups were fed a diet containing sodium benzoate (NaB) at 125 mg/kg with ascorbic acid (AA) at 100, 200, or 300 mg/kg of feed, another three groups were fed NaB at 250 mg/kg with AA at 100, 200, or 300 mg/kg of feed, respectively, and the last three groups were fed NaB at 500 mg/kg with AA at 100, 200 or 300 mg/kg, respectively. Behavioural tests were assessed, following which animals were sacrificed, and their brains were homogenised for the assessment of biochemical parameters. Results: The result showed a decrease in body weight, self-grooming, total antioxidant capacity, inflammatory cytokines, mixed response with food intake, locomotor activity, Y maze spatial working memory, and anxiety-related behaviours and an increase in rearing and radial arm maze spatial working memory. Conclusion: Dry-feed added NaB/AA altered behavioural, oxidative stress, and inflammatory markers in mice. It was found that both beneficial and deleterious effects might be possible, depending on the concentrations ingested in food. However, further investigations are required to ascertain its effects on humans.

Background: The use of medicinal plants as supplemental or alternative medicine is widespread around the world. For the development of new drugs, studies on these medicinal plants that include pharmacological and toxicological assessments are crucial. Objective: This work aimed to find the total phenolic and flavonoid content, antioxidant, antibacterial, and antidiabetic potential of the traditionally used medicinal plant Mimosa rubicaulis Lam. Methods: The in vitro antidiabetic potential of methanolic extract and its fractions of the roots of M. rubicaulis were performed via enzyme (α-glucosidase and α-amylase) inhibition assays. Antioxidant and anti-inflammatory activities were carried out using 2,2 Diphenyl-1-picrylhydrazyl (DPPH), and reactive oxygen species (ROS) inhibiting methods. Well diffusion method is applied for antibacterial activity. Results: The crude extract reported the highest inhibition activity against α-glucosidase with an IC50 value of 10.29 ± 0.35 μg/mL compared to the standard acarbose’s IC50 value of 5.653 ± 0.29 μg/mL. Similarly, the ethyl acetate (EA) fraction disclosed significant inhibition against α-amylase with an IC50 value of 108.7 ± 0.66 μg/mL compared to the standard acarbose's IC50 value of 6.01 ± 0.14 μg/mL. Likewise, the EA fraction showed the maximum antioxidant activity with an IC50 value of 11.89 ± 1.05 μg/mL among the crude extract and its fractions. Conclusion: Mimosa rubicaulis was found to have α-glucosidase and α-amylase inhibition, antiinflammatory, and antibacterial activity. To the best of our knowledge, this is the first report of α- glucosidase and α-amylase inhibition activity of this plant. Further studies on this plant are required to isolate potent compounds.

A Proprotein convertase subtilisin/kexin type-9 is considered a zymogen, extensively found in the liver. PCSK9 is found in circulation in the plasma, where it attaches to low-density lipoprotein (LDL) receptors on the cell surface, is internalized, and subsequently directs the receptors to be degraded by lysosomes. Investigations of naturally or organically found PCSK9 gene variations, which generated high levels of plasma LDL cholesterol deviations and varied atherosclerosis proportion factors, released floods of pharmaceutical along with biological and live sciences research into the world. Significant advances in our understanding of the physiological control of PCSK9 led quickly to the development of biological inhibitors of PCSK9 that are now available for purchase. These inhibitors decreased LDL cholesterol levels with other improved cardiovascular outcomes. The current manuscript will show the rapid development of PCSK9, beginning with its discovery as a novel gene and progressing through its use as a therapeutic target, followed by its testing on animals and humans and, eventually, its use in outcome trials and clinical applications.

Background: In recent years, medicinal plants have received considerable attention due to the search for novel bioactive compounds. In this optic, we have been interested in Artemisia judaica subsp. sahariensis, a Saharan species widely used in phytotherapy by the Tuaregs of the Ahaggar. Objectives: This study aims to evaluate and optimize the biological activities of this plant in order to valorize its bioactive compounds. Methods: For this purpose, an extraction with methanol (70%) was carried out, then a liquid-liquid fractionation, using solvents with increasing polarity: diethyl ether, ethyl acetate, n-butanol and water. We realized an analysis of phenols, flavonoids and evaluation of antioxidant and antimicrobial activities in addition to the UPLC-ESI-MS/MS analysis of the fractions. Results: The reducing effect was proportional to the solvent polarity. The crude extract gave the best reducing power (17.55 ± 3.06 μg/mL), better phenols and flavonoids contents (20.35 ± 0.5 mgGAE/gTDM), (10.35 ± 0.56 mgGAE/gTDM) respectively compared to its fractions. The DPPH (2,2-Diphenyl-1-Picrylhydrazyl) radical scavenging assay showed that the ethyl acetate fraction was the most active with the lowest IC50 value (inhibitory concentration to 50% of DPPH) (41.43 ± 0.24 μg/ml) followed by n-butanol (58.53 ± 0.20 μg/mL), diethyl ether (135.07 ± 6.18 μg/mL) and aqueous (226.41 ± 1.51 μg/mL) fractions (p <0.0001). Moreover, hydromethanolic extract gave an IC50 value of 114.05 ± 3.37 μg/mL. The antimicrobial effect was observed on all clinical multiresistant bacteria tested except Klebsiella pneumoniae, which was resistant. The most important effect was observed by the ethyl acetate fraction against the fungal strain Candida albicans. Various phenolic acids and flavonoids (flavones, flavonols, flavanones) were detected and could be responsible for these bioactivities. Conclusion: We can conclude that liquid-liquid extraction with solvents of increasing polarity plays a major role in optimizing the biological activity of this plant, which contains polyphenols and can therefore be valued as a source of natural antioxidants and antimicrobials.

The global population's rapid expansion is a worldwide concern, which has led to higher medication and resource consumption. As a result, there is a tremendous need to seek out new means of producing reliable medications to meet the rising demand of a global populace suffering from a wide range of health problems. Various resources are available in marine habitats for the development of novel medications. Their life circumstances are radically different from those found in a terrestrial setting. In order for marine animals to thrive in the ocean, they produce a variety of secondary metabolites, which can possibly be life-saving bioactive compounds that come from an increasing variety of marine microorganisms. These metabolites have pharmacological properties that make them intriguing as a potential for human medications. Therefore, there has recently been a rise in interest in marine-derived biomolecules as potential treatments. Utilizing a wide range of screening methods, we can investigate the effects of these extracts and purified compounds from marine organisms in the medicinal industry, such as cancer prevention, inflammation reduction, virus and bacteria inhibition, ion channel/receptor modulation, and plant growth stimulation. The structures of bioactive substances will be determined after they have been isolated chromatographically. Marine-based bioactive compounds can be (semi) synthesized to make new derivatives, structural analogues, and copies that can be used to build new marine-based chemical catalogs and contribute as lead or hit molecules. This overview classifies FDA-approved marine-based drugs and provides information on their origins, chemical composition, manufacturing processes, and pharmacology. This paper outlines the supply dilemma in marine medicine development.

This review aims to provide a comprehensive summary of the pharmacological effects of isoliquiritigenin, a natural chalcone. The data was gathered from a variety of research papers published till 2022. The extensive pharmacological features of ISL, including its anti-inflammatory, anti-influenza, anti-tyrosinase, anti-bacterial, anti-sarcoma, anti-oxidative, anti-leiomyoma, anticholera, anti-asthma, anti-diabetic, and anti-cancer activity, neuroprotective, hepatoprotective, and cardioprotective effects, may explain its practical applicability in the treatment and prevention of many illnesses. However, to confirm the target-organ toxicity or side effects, more research is required. The creation and design of new ISL analogues based on previously discovered techniques may benefit from this review.