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The effects of plant flavonoids on mammalian cells: Implications for inflammation, heart disease and cancer
Abstract
Flavonoids are nearly ubiquitous in plants and are recognized as the pigments responsible for the colors of leaves, especially in autumn. They are rich in seeds, citrus fruits, olive oil, tea, and red wine. They are low molecular weight compounds composed of a three-ring structure with various substitutions. This basic structure is shared by tocopherols (vitamin E). Flavonoids can be subdivided according to the presence of an oxy group at position 4, a double bond between carbon atoms 2 and 3, or a hydroxyl group in position 3 of the C (middle) ring. These characteristics appear to also be required for best activity, especially antioxidant and antiproliferative, in the systems studied. The particular hydroxylation pattern of the B ring of the flavonoles increases their activities, especially in inhibition of mast cell secretion. Certain plants and spices containing flavonoids have been used for thousands of years in traditional Eastern medicine. In spite of the voluminous literature available, however, Western medicine has not yet used flavonoids therapeutically, even though their safety record is exceptional. Suggestions are made where such possibilities may be worth pursuing.
... The anticancer properties of Z. rhetsa can be largely ascribed to its complex phytochemical composition. Flavonoids, which are ubiquitous in the Zanthoxylum genus, exhibit anti-proliferative effects by inducing apoptosis and inhibiting angiogenesis (Middleton et al., 2000) [20] . These compounds operate synergistically, enhancing the plant's overall anticancer potential. ...
... The anticancer properties of Z. rhetsa can be largely ascribed to its complex phytochemical composition. Flavonoids, which are ubiquitous in the Zanthoxylum genus, exhibit anti-proliferative effects by inducing apoptosis and inhibiting angiogenesis (Middleton et al., 2000) [20] . These compounds operate synergistically, enhancing the plant's overall anticancer potential. ...
... They exert wide range of biological activities includes, antibacterial anti-inflammatory, antiviral, anti-allergic activities (Cushnie and Lamb 2005) [22] , treatment of neurodegenerative diseases, cytotoxic, antitumour, vasodilator action (Williams et al., 2004) [99] and (Chebil et al., 2006) [16] . They influence these effects as antioxidants, free radical scavengers, chelators of divalent cation (Chebil et al., 2006 [16] , Middleton et al., 2000) [62] . Petals of lotus have the potential to act as a source of useful drugs because of the existence of various phytochemical components such as carbohydrate, protein, phenols, tannin, flavonoids and alkaloids (Saraswathi and Gricilda Shoba 2015) [86] . ...
... They exert wide range of biological activities includes, antibacterial anti-inflammatory, antiviral, anti-allergic activities (Cushnie and Lamb 2005) [22] , treatment of neurodegenerative diseases, cytotoxic, antitumour, vasodilator action (Williams et al., 2004) [99] and (Chebil et al., 2006) [16] . They influence these effects as antioxidants, free radical scavengers, chelators of divalent cation (Chebil et al., 2006 [16] , Middleton et al., 2000) [62] . Petals of lotus have the potential to act as a source of useful drugs because of the existence of various phytochemical components such as carbohydrate, protein, phenols, tannin, flavonoids and alkaloids (Saraswathi and Gricilda Shoba 2015) [86] . ...
The national flower of our country [Nelumbo nucifera, (2n = 16)} should tie in with the culture, history and heritage of a nation. There are two species in lotus-Nelumbo nucifera and Nelumbo lutea. The alkaloids of lotus embryos were found to possess hypotensive effects. The plant parts of lotus are edible and are used as food sources. They are the natural bioactive compounds found in plants, which are solely responsible for their medicinal activity. The secondary metabolites viz., alkaloids, steroids, tannins, cardiac glycosides, flavonoids, etc. play a major role against various activities. In the traditional system of medicine, the different parts of the plant are reported to possess beneficial effects for the treatment of common infections, skin, respiratory and reproductive diseases. Hence, it is considered as an ornamental and medicinal plant for the current era. Here, we comprehensively reviewed floral biology, medicinal, nutritional, ornamental importance and so on. This will kindle the interest of the researchers to take up studies on pharmaceutical aspects.
... Natural polyphenols, secondary metabolites of plants involved in the defense against several types of stress, have many potential benefits in human health and reduce the risk for many cancers [7,8]. Positive effects of polyphenols are mainly attributed to their antioxidants properties supporting their anti-tumor effect which results from their direct action on malignant cell proliferation by inducing different programs of cell death including apoptosis [9,10], or indirectly by inhibiting matrix metalloproteinases [11] and vascular endothelial growth factor [12] which contribute in counteracting angiogenesis and metastasis development. Hence, natural polyphenolic compounds may be useful for prevention of cancers or may be used as chemotherapeutic agents [13]. ...
Dietary polyphenols, derived from natural products, have received a great interest for their chemopreventive properties against cancer. In this study, we investigated the effects of phe-nolic extract of the oleaster leaves (PEOL) on tumor growth in mouse model and on cell death in colon cancer cell lines. We assessed the effect of oleaster leaf infusion on HCT116 (human colon cancer cell line) xenograft growth in athymic nude mice. We observed that oleaster leaf polyphenol-rich infusion limited HCT116 tumor growth in vivo. Investigations of PEOL on two human CRC cell lines showed that PEOL induced apoptosis in HCT116 and HCT8 cells. We demonstrated an activation of caspase-3,-7 and-9 by PEOL and that pre-treatment with the pan-caspase inhibitor, N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethylke-tone (z-VAD-fmk), prevented PEOL-induced cell death. We observed an involvement of the mitochondrial pathway in PEOL-induced apoptosis evidenced by reactive oxygen species (ROS) production, a decrease of mitochondrial membrane potential, and cytochrome c release. Increase in intracellular Ca 2+ concentration induced by PEOL represents the early event involved in mitochondrial dysfunction, ROS-induced endoplasmic reticulum (ER) stress and apoptosis induced by PEOL, as ruthenium red, an inhibitor of mitochondrial calcium uptake inhibited apoptotic effect of PEOL, BAPTA/AM inhibited PEOL-induced ROS generation and finally, N-acetyl-L-cysteine reversed ER stress and apoptotic effect of PEOL. These results demonstrate that polyphenols from oleaster leaves might have a strong potential as chemopreventive agent in colorectal cancer.
... Flavonoids such as quercetin and kaempferol Helps reduce oxidative stress. which is linked to cancer and other chronic diseases and cardiovascular disorders (Middleton et al., 2000). Flavonoids also inhibit mediators that promote inflammation. ...
Hippeastrum puniceum, a plant native to tropical Africa, including Nigeria, has garnered increasing attention due to its rich phytochemical profile and diverse bioactivities. This review highlights the key phytochemical constituents—alkaloids, flavonoids, saponins, terpenoids, tannins, and starch—found in Hippeastrum puniceum. These compounds contribute to the plant's significant antioxidant, antimicrobial, and anti-inflammatory properties, positioning it as a valuable resource for various industrial applications. Flavonoids and alkaloids primarily contribute to the antioxidant activity, which helps mitigate oxidative stress and potentially prevent chronic diseases like cancer and cardiovascular disorders. Its antimicrobial effects, driven by alkaloids and flavonoids, offer promising natural alternatives to combat antibiotic-resistant pathogens. Additionally, the plant's anti-inflammatory properties suggest potential therapeutic applications in treating inflammatory conditions like arthritis and asthma. The review also explores the potential applications of Hippeastrum puniceum across different industries. In the pharmaceutical industry, it holds promise for developing novel drugs targeting oxidative stress, microbial infections, and inflammation. The food industry can leverage its antioxidant and antimicrobial properties as natural preservatives and functional food additives. In the cosmetic industry, its bioactive compounds could be used in anti-ageing and skincare products. Despite these promising findings, further research is needed to isolate and characterise specific compounds, conduct clinical trials, and assess the pharmacokinetics and toxicity of Hippeastrum puniceum. This comprehensive review underscores the importance of continued exploration of Hippeastrum puniceum, emphasising its potential to contribute to advancements in phytochemistry, pharmacology, and various industrial applications.
... Flavonoids, major class of antioxidants, prove interesting to pharmacologists due to various beneficial bioactivities [1,2]. ...
... The host plant can recognize and identify these nod factors, which subsequently leads to various cellular responses such as root hair deformation, ion fluxes, and the formation of a root nodule. Middleton et al. (2000) have reported that specific flavonoids demonstrate inhibitory properties against plant pathogenic pathogens, including Fusarium oxysporum. The product has garnered substantial popularity because of its myriad health advantages. ...
This review centers on the classification of secondary metabolites into three main groups, as previously mentioned. The objective is to present their pharmacological properties, which possess the capacity to facilitate the identification and advancement of novel pharmaceuticals. The analysis of plant constituents necessitates careful examination of a complex amalgamation of diverse chemical compounds, with the objective of optimizing the methodology to discern and
extract a biologically active compound. To examine the biological characteristics of a specific medicinal plant, it is often necessary to utilize purification methods or isolate a particular compound.
... The pharmacological activities of these molecules have significant implications for human health, as they are capable of reducing inflammation, preventing allergies, combating bacterial and viral infections, and protecting against cancer. Additionally, they can aid in the treatment of cardiovascular diseases and facilitate blood vessel widening [13,14]. Furthermore, they can hinder the oxidative alteration caused by free radicals, scavenge oxygen, and break down peroxides using their antioxidant properties [15]. ...
Anabasis aretioïdes contain numerous bioactive compounds that provide several advantages, including antioxidant, antibacterial, anticancer, neuroprotective, anti-inflammatory, and antidiabetic characteristics. This study aimed to make a hydroethanolic extract from the aerial part of the plant, analyze its biochemical compounds, and test its biological activities. From HPLC-DAD analysis, cinnamic acid, sinapic acid, and vanillin bioactives were found to be the main compounds in the extract. The spectrometric tests revealed that the extract was rich in flavonoids (8.52 ± 0.32 mg RE/100 g DW), polyphenols (159.32 ± 0.63 mg GAE/100 g DW), and condensed tannins (8.73 ± 0.23 mg CE/100 g DW). The extract showed significant antioxidant activity. There were strong correlations between the amount of flavonoid or polyphenol and the antioxidant assays, including ABTS, DPPH, β-carotene, and TAC. The extract also showed highly effective results against Gram-positive bacteria Staphylococcus aureus and Enterococcus faecalis as well as against Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa, and showed promising cytotoxicity against breast cancer cell lines MCF-7 and MDA-MB-231. The in silico modeling of the bioactive compounds contained in the extract illustrated their interaction mode with the active sites of particular target proteins, and it showed that rutin had the strongest effect on stopping NADPH oxidase enzyme, with a glide score of −6.889 Kcal/mol. Sinapic acid inhibited E. coli beta-ketoacyl-[acyl carrier protein] synthase (−7.517 kcal/mol), and apigenin showed high binding affinity to S. aureus nucleoside di-phosphate kinase, with −8.656 kcal/mol. Succinic acid has the strongest anticancer effect for caspase-3, with a glide score of −8.102 kcal/mol. These bioactive components may be beneficial as antioxidant and antibacterial applications in medicine, foods, natural cosmetics, and breast cancer prevention in the future. As a result, the use of this indigenous plant must be considered to maximize its value and preservation.
... ± 16.03 mg/100 g [15]. These chemicals have shown favorable effects in treating coronary heart disorders, possess anticancer capabilities, and several indicate potential anti-human immunodeficiency virus (HIV) functions [16]. ...
Guava seeds, often overlooked as waste in
guava processing, have a rich nutritional profile and
bioactive compounds with significant pharmacolog�ical and industrial applications. They contain pro�tein, lipids, vitamins, minerals, and antioxidant prop�erties. Guava seeds have a diverse set of bioactive
and functional qualities that offer great promise for
use in the biomedical and food industries. They are
rich in polysaccharides, protein, lipids, minerals, vit�amins, phenolics, carotenoids, and dietary fiber.
However, the presence of some antinutritional fac�tors in guava seeds restricts their usage in the food
industry. Guava seed extracts have shown potential
in reducing glycemia, triglycerides, cholesterol, and
treating obesity and diabetes. Industrial applications
include biosurfactant production, waste fermenta�tion, amino acid supplementation, and food supple�ments. Further research is needed to optimize their
utilization and capitalize on their nutritional and
functional benefits.
... Antioxidants are very important in preventing human illnesses by acting as scavengers of free radicals, pro-oxidant metal complexes, reducing agents, and quenchers of singlet oxygen production [47]. Because of their ability to scavenge, antioxidants are able to manage certain conditions, including as AIDS, cancer, heart disease, neurological disorders, and cataracts [48]. Scientific knowledge regarding the antioxidant abilities of many plants is currently insufficient, particularly those less commonly used in food and medicine. ...
The Rutaceae family includes Aegle marmelos L., a moderately sized aromatic tree that is also known as Bael, Bengal quince, golden apple, Japanese bitter orange, stone apple, or wood apple. It is mostly found in tropical or subtropical regions. Fever, seminal weakness, nausea, vomiting, swellings, diarrhea, dyspepsia, and intermittent fever are the most common ailments that bael leaves are used to treat. Because of their high phenolic and flavonoid content, leaves have anti-allergic, anti-inflammatory, anti-microbial, anti-thrombotic, cardioprotective, and vasodilatory properties. Therefore, the aim of the present study was to determine the phytochemical components, antioxidant capacity, GC-MS analysis, total phenolic & flavonoid contents in the methanolic extracts of A. marmelos leaves. Various secondary metabolites were observed in the aqueous and methanolic A. marmelos leaf extracts. TLC analysis of methanolic extracts revealed five distinct spots having different Rf values. Total phenolic content was found to be 33 ± 7.62 mg GAE/g, flavonoid content was 307.8 ± 130.12 mg QE/g. The highest antioxidant activity of methanolic extract of A. marmelos leaves was obtained at 1000 µg/ml conc. and it was dose dependent. Many biologically active compounds were present as analysed by GC-MS. The highest peak area of Perylo[1,12-def]-1,3-dioxepin-5,11-dione, 6,12-dihydroxy-8,9-bis(2-hydroxypropyl)-7,10-dimethoxy-, stereoisomer (3.502%) was observed.
... They can also decrease oxidative damage through a free radical scavenging activity because they have hydroxyl groups [58]. ...
Background: Metabolic dysfunction-associated steatotic liver disease (MASLD) is the most recent definition for steatotic liver disease associated with metabolic syndrome. The results of recent metabolic and observational studies suggest a potential beneficial effect of food-derived flavonoids in some chronic diseases, including MASLD. The study aims to evaluate the protective role of diet flavonoids in subjects with and without MASLD belonging to a cohort living in the South of Italy. Methods: The study cohort comprised 1297 participants assessed in the NUTRIHEP cohort (2015–2018), divided into two groups, based on presence or absence of MASLD. Results: The results indicated statistically significant flavonoid consumption, showing a protective role against MASLD, at an optimal concentration of 165 mg/day, with an OR value of 0.63, (p = 0.001, 95% C.I.: 0.47; 0.83 t). The OR remained almost unchanged when the intake increased from 165 mg per day to 185 mg per day. Conclusions: In conclusion, our study results show a protective role of flavonoids against MASLD. Consuming only 165 mg of flavonoids daily can activate this protective function, reducing the risk of MASLD.
... Plant flavonoids in general-polyphenolic compounds in which two benzene rings are bound together with a heterocyclic pyran or a pyrrole ring-are biologically active. These naturally occurring compounds have been described as having anti-inflammatory, anticarcinogenic, antiallergic, and neuroprotective properties [22,[40][41][42][43][44]. The HPLC-UV/ESI-MS analysis of a methanol extract of the press juice of fresh or fresh-frozen BP leaves revealed flavonoid glycosides as characteristic constituents [45]. ...
Background/Objectives: Bryophyllum spp. preparations are widely used in Anthroposophic Medicine, most often for mental and behavioral disorders, including anxiety. Studies in animals revealed various anxiolytic and neurosedative effects for Bryophyllum pinnatum. We set out to investigate the effectiveness of Bryophyllum 50% chewable tablets, a product registered without indication by means of notification in Switzerland, in the treatment of anxiety symptoms in psychiatric and psychosomatic patients. Methods: A total of 99 patients with anxiety symptoms were recruited from the waiting list for an inpatient stay at the hospital “Klinik Arlesheim”, Department of Psychiatry and Psychosomatics; of these, 54 completed the study and returned fully completed questionnaires. Patients were treated with Bryophyllum 50% chewable tablets (350 mg tablets, made from leaf press juice, 3 × 2 per day; Weleda AG Arlesheim, Switzerland) and filled out questionnaires at baseline and after two and three weeks of tablet intake. The primary endpoint of the study was the change in anxiety symptoms measured with the Beck Anxiety Inventory (BAI). Results: A clinically relevant decrease in BAI score from baseline (27.4 ± 12.0) to after two (22.4 ± 12.1; p < 0.001) and three (20.6 ± 12.9; p < 0.001) weeks of treatment was observed. Additional improvements were observed in the secondary endpoints (including in depression, sleep quality, and stress); tolerability and compliance were very good. Conclusions: The results suggest that Bryophyllum 50% chewable tablets have beneficial effects on anxiety-related symptoms. Since the study design does not allow us to conclude causality between treatment and observed improvements, a randomized clinical trial is urgently needed.
... Normally, ROS levels are kept non-toxic by various antiox-idative enzymes and antioxidants (Mittler et al., 2004), with superoxide dismutase (SOD), catalase (CAT), ascorbate peroxidase (APX), and peroxidase (POD) being the primary enzymes involved. Phenolic compounds, as secondary metabolites, play a crucial role in balancing ROS levels (Middleton et al., 2000). Thus, maintaining a higher antioxidant activity is essential to eliminate excess ROS. ...
The effects of different doses of UV‐C irradiation (0, 0.5, 1.0, 2.0, and 4.0 kJ m⁻²) on the quality and antioxidant capacity of peach fruit were examined. Results showed that irradiation at 2.0 kJ m⁻² led to higher firmness and total soluble solids, as well as lower weight loss and decay index. Additionally, peach fruits irradiated with 2.0 kJ m⁻² UV‐C exhibited increased production of reactive oxygen species, which in turn stimulated the synthesis of total phenolics and total flavonoids and enhanced the activities of superoxide dismutase, catalase, peroxidase, and ascorbate peroxidase. Overall, the best abiotic stress effect was observed with 2.0 kJ m⁻² UV‐C irradiation, resulting in improved shelf quality and increased antioxidant capacity of peach fruits during storage.
Practical Application
This study provides a theoretical basis for the application of UV‐C irradiation in peach fruit preservation.
... The application of exogenous plant derived antioxidant is likely to improve health status of male animals (Agarwal and Prabakaran 2005;Nantia et al., 2009). Numbers of flavonoid-containing plants are known to have antioxidant, androgenic, and anti-infertility activities and have been extensively used against animal reproductive diseases (Middleton et al., 2000;Dobrzyñska et al., 2004;Purdy et al., 2004). ...
Fruits are medicinal and also contain essential phytonutrients that gives the fruits potency that keeps the body healthy. The aim of the study is to ascertain the Effects of Smoothies (banana, apple and pineapple) on Oxidative Stress Markers following administration of monosodium glutamate in Male Wistar Rats. Thirty (30) animals weighing 130kg to 180kg were randomly selected into 6 groups with 5 animals per group. Group 1 received 5mls of distilled water, group 2 received 1ml/kg (low dose) of smoothies, group 3 received 2ml/kg (medium dose), group 4 received 3ml/kg (high dose), group 5 received 400mg/kg of monosodium glutamate, group 6 received 400mg/kg of monosodium glutamate and 3ml/kg (high dose) of smoothies co-administered. Administration was carried out for 14 days and on the 15th day, the animals were sacrificed, semen was harvested and 5ml blood was collected via cardiac puncture. Statistical analysis was done using ANOVA and expressed as Mean±SEM. Statistically P < 0.05 was said to be significant. SPSS version 26 was used. The results showed significant increase in SOD in the group that was administered smoothies (high dose) and decrease in the group that was administered 400mg of monosodium glutamate (MSG). MDA increases in the groups that was administered MSG alone and when co-administered with smoothies (high dose). MDA also decreases in the groups given medium and high dose smoothies. Catalase decrease in the group that was given MSG alone. Gluthione increases in the groups that was given medium and high dose smoothies and decrease in the group that was given MSG only.
... These include several subgroups, such as flavonols, flavones, isoflavones and chalcones (Panche et al., 2016). Bioflavonoids that are produced from plants have been demonstrated to have antimicrobial activities against viruses, bacteria and fungi (Middleton et al., 2000;Nair et al., 2006;Russo et al., 2020). Flavonoids usually display a broad spectrum of activities because of their antioxidant properties as well as their potentials to modulate several cell receptors and/or enzymes (Panche et al., 2016). ...
Notably, severe acute respiratory syndrome (SARS), Middle East respiratory syndrome (MERS) and coronavirus disease 2019 (COVID-19) have all had significant negative impact on global health and economy. COVID-19 alone, has resulted to millions of deaths with new cases and mortality still being reported in its various waves. The development and use of vaccines have not stopped the transmission of SARS coronavirus 2 (SARS-CoV-2), the etiological agent of COVID-19, even among vaccinated individuals. The use of vaccines and curative drugs should be supplemented with adoption of simple hygiene preventive measures in the fight against the spread of the virus, especially for healthcare workers. Several virucidal topical antiseptics, such as povidone-iodine (PVP-I), citrox, cyclodextrins among others, have been demonstrated to be efficacious in the inactivation of SARS-CoV-2 and other coronaviruses in both in vitro and in vivo studies. The strategic application of these virucidal formulations could provide the additional impetus needed to effectively control the spread of the virus. We have here presented a simple dimension towards curtailing the dissemination of COVID-19, and other coronaviruses, through the application of effective oral, nasal and eye antiseptics among patients and medical personnel. We have further discussed the mechanism of action of some of these commonly available virucidal solutions while also highlighting some essential controversies in their use.
... However, previous work has shown a moderate inhibition of the whole X. aethiopica extract of 44.52% (at a concentration of 2 μg/mL) on poliovirus type 1. Further exploration on enveloped viruses would be warranted based on previous studies that revealed flavonoids derived from plants effectively act against respiratory syncytial virus (RSV) and herpes simplex virus (HSV) 15 . Additionally, according to Kahn et al. 16 , polyphenols could have antiviral activities. ...
Objective : The emergence of viral infections has highlighted the need for new antiviral molecules. This study is part of an exploration into finding new antiviral compounds from medicinal plants used in traditional pharmacopoeia in Côte d'Ivoire. The aim is to determine which of the extracts from Gliricidia sepium leaves and Xylopia aethiopica fruits (hydroalcoholic, hexane/water, ethyl acetate/water, aqueous) exhibits the best antiviral activity. Methodology: The cytotoxicity of each partition P1 (hydroalcoholic), P2 (hexane/water), P3 (ethyl acetate/water), P4 (aqueous) of Gliricidia sepium leaves and P1' (hydroalcoholic), P2' (hexane/water), P3' (ethyl acetate/water), P4' (aqueous) of Xylopia aethiopica fruits is determined on RD cells. The antiviral activity of these partitions was then evaluated against a type 1 enterovirus. Results: The hexane-water partition showed high antiviral activity against type 1 enterovirus, with an inhibition of 65.78±9.21% at a concentration of 1 μg/mL for Gliricidia sepium leaves, compared to a non-significant inhibition of 86.84±5.26% at 31.25 μg/mL for Xylopia aethiopica fruits. Additionally, the aqueous partition of Gliricidia sepium induced an inhibition of 50±0.01% at a concentration of 1.95 μg/mL. Conclusion: Hexane-water and aqueous partitions of Gliricidia sepium showed́ potent antiviral activitý against enterovirus 1 than those of Xylopia. aethiopica. Keywords: plant partition, RD cells, enterovirus type 1.
... Phenolic compounds have well-documented antioxidant properties due to their redox characteristics, which facilitate the scavenging of free radicals [39]. Similarly, flavonoids regulate oxidative stress and metabolic disorders such as diabetes [40,41]. These bioactive compounds may help mitigate the oxidative damage caused by chronic hyperglycaemia and insulin resistance [42]. ...
Type 2 diabetes (T2D), also known as non-insulin-dependent diabetes mellitus, represents the prevailing manifestation of diabetes, encompassing a substantial majority of cases, ~90–95%. Plant-derived antidiabetic leads are being intensively explored due to their safety and effectiveness. The main objective of the present study is to evaluate the anti-diabetic potential of the traditional formulation Karisalai Karpam through in-vitro and in-silico investigations. The in-vitro and in-silico investigation of traditional polyherbal preparation Karisalai Karpam (KK) chooranam were performed to ascertain its inhibitory potential against α-amylase and α-glucosidase enzymes along with antioxidant (DPPH and ABTS) and phytochemical analysis. The results of enzyme inhibitory activity of KK witnessed highest activity against α-glucosidase enzyme with a percentage inhibition of 84.66 ± 2.50% (IC50,187.9 ± 5.79 μg/ml) followed by moderate level of α-amylase inhibition exhibited with 72.94 ± 3.66% (IC50, 241.6 ± 9.76 μg/ml). Additionally, the strongest antioxidant activity was observed in quenching DPPH• (IC50,154.8 ± 14.53 μg/ml) and ABTS+• radicals (IC50,148.6 ± 29.74 μg/ml). The outcome of the molecular docking studies indicated that among the 17 compounds analysed, the lead such as acalyphin, apigenin, humulene, and indirubin exhibited a prominent binding affinity over the residual binding site of α-glucosidase. It’s important to note that the catalytic site of the enzyme α-amylase is primarily occupied by amyrin, apigenin, arjunolic acid, β-sitosterol, geraniol, and tricetin. In conclusion, the formulation KK demonstrates robust alpha-glucosidase and alpha-amylase inhibitory activity. It’s also worth noting that the formulation exhibits noteworthy antioxidant properties, which could provide additional health benefits. The binding mode and energies of the identified phytochemicals against the target enzymes further support the formulation’s antidiabetic potential.
... Plants have enormous amounts of antioxidant properties due to their use as protective agents to cure many illnesses. Many plant antioxidant compounds help to neutralize radicals (Middleton et al., 2000;Sudirga et al., 2023). Antioxidant properties of phytochemical agents have associations with various human diseases' treatments (Anderson et al., 2001). ...
The search for novel components with antibacterial potential has recently gained increasing significance due to growing worldwide bacterial infections by antibiotic-resistant bacterial strains. Therapeutic plants are crucial to human health due to their antiseptic potential against bacterial pathogens. Botanical sources have benefitted healthcare for many years due to the various active compounds present, such as tannins, terpenoids, alkaloids, and flavonoids. This study seeks to report the antibacterial potential of Cuminum cyminum against Escherichia coli, Bacillus subtilis, Bacillus cereus, and Staphylococcus aureus. The research proceeded with the use of methanolic extract of C. cyminum preparation using the Soxhlet extraction technique. Formulating five concentrations (150, 180, 200, 220, and 250 mg/ml) used deionized water and incurred testing at varying temperatures (40 °C, 60 °C, 80 °C, 100 °C, and 121 °C) and pH (3, 5, 7, 9, and 11 pH) ranges. The well-diffusion assay and minimum inhibitory concentration helped analyze the antimicrobial properties of C. cyminum methanolic extract as observed against selected bacterial strains. The results' analysis engaged the one-way ANOVA. It was evident that the maximum effect of plant extract against E. coli, B. subtilis, and B. cereus was at 200 mg/ml and against Staph. aureus, a maximum zone emerged at 180 mg/ml. At varying temperatures, the maximum inhibition of E. coli, Staph. aureus, and B. cereus occurred at 121 °C, with B. subtilis inhibited at 80 °C. For pH changes, it revealed that all strains were sensitive to acidic pH (3) at both concentrations (150 and 250 mg/ml).. Antibacterial effect of Cuminum cyminum against selected bacterial strains. SABRAO J. Breed. Genet. 56(2): 787-793. http://doi.
... Crataegus berries are a source of phenolics in values up to 30.63 mg gallic acid equivalent (GAE)·g -1 in ripe berries. Kostić and Middleton reported that the content of total phenolics in ethanolic extracts of dried hawthorn fruits was 35.4 ± 2.48 mg GAEg -1 dried mass [5,6]. The use of medicinal plant raw materials and fruits in the food industry increases the nutritional and functional properties of food products enriching them with biologically active substances. ...
The aim of this study was to determine some physicochemical parameters and antioxidant activity of fermented milks enriched with extracts of red hawthorn (Crataegus monogyna Jacq.) and black hawthorn (Crataegus nigra Waldst & Kit.) Antioxidant activity and the content of total phenols of water extracts of both species of hawthorn - red and black - were analyzed. The effect of the inclusion of the extracts in amounts of 5, 10 and 15 % of both species of hawthorn on the physicochemical and antioxidant properties of the obtained yogurts was monitored. Yogurts with the addition of red hawthorn extract (15 %) showed the highest phenolic content (TPC) and antioxidant properties determined by DPPH (2,2-Diphenyl-1-picrylhydrazyl) and FRAP (Ferric ion reducing antioxidant power) methods. Milk with extracts has better physicochemical properties (dry matter, syneresis and retention capacity). The use of hawthorn extracts in the production of yogurts is a new method for the development of dairy foods with functional properties.
... Differing group of phenolic compound (flavonols, flavonoids, tannic acid, anthocyanins, phenolic acid etc.) have a perfect basic science with the expectation of complimentary radical searching action [12] and exhibit a wide range of physiological properties, such as anti-allergenic, anti-atherogenic, thrombolytic, anti-inflammatory, anti-microbial, antithrombotic, cardioprotective and vasodilatory effects [13,14,15]. The phytochemical screening tests indicated that the different constituents such as alkaloids, carbohydrates, flavonoids, glycosides and steroids were present in the plant Hygroryza aristata that have pharmacological properties (table 1). ...
Hygroryza aristata is the significantly most important traditional medicinal plant practitioners all over the country since long years. Seeds are cooling and astringent to urinary tract; useful in biliousness. By the use of this plant only a few investigations was done like: anti-inflammatory and antioxidant. The purpose of the study is to determine the thrombolytic and analgesic activity of Hygroryza aristata extract. Phytochemical screening of the methanolic extract of whole plant of Hygroriza Aristata indicates the presence of alkaloids, carbohydrates, flavonoid, glycoside, and steroid. In thrombolytic assay, methanolic extract of the Hygroriza aristata leaves exhibited a promising effect compared standard drug Streptokinase. Here, the extract exhibited 63% (for 100 mg) clot lysis activity whereas; Streptokinase exhibited 82% (for 30,000 I.U). The analgesic activity of the methanolic leaf extract of Hygroriza aristata was also observed by acetic acid induced writhing in mice. This writhing was markedly reduced with increase of the amount of extract at 250 mg/kg (63.1%) and 500 mg/kg (70.24%) respectively. Here, Diclifenac-Na 10 mg/kg (54.76%) was used as a standard drug. Thus, we can assume that, Hygroriza aristata plant have a promising effect of thrombolytic and analgesic activity that showed a ways of inventing new lead compound having such type of pharmacological effects respectively. PhOL Hossain, et al. 48 (pag 47-54)
... These plants contain bioactive compounds that influence both innate and adaptive immunity, resulting in therapeutic effects for autoimmune diseases. Relevant studies highlight that many medicinal plants work by modulating the inflammatory response, which is a key feature in the pathogenesis of autoimmune diseases [6] . One of the primary mechanisms through which medicinal plants modulate the immune system is by regulating the production of pro-inflammatory cytokines. ...
... The antioxidant compounds in Cassia occidentalis help neutralize free radicals, protecting osteoblasts (bone-forming cells) and enhancing the bone regeneration process. [40,41,42] Osteogenic Activity: Some studies suggest that extracts of Cassia occidentalis can stimulate the differentiation and activity of osteoblasts. This osteogenic potential aids in the formation of new bone tissue, crucial for effective bone healing. ...
... besides this chlorophyll, and derivatives of chlorophyll showed anti-cancer potential in cases of liver, colon, stomach, skin and gastrointestinal cancer [56][57] . The in vitro and in vivo studies have shown that chlorophyllin could reduce the activity of liver cytochrome P450, it has been observed the reduced activity of liver cytochrome P450, resulting in longer lifespan and lower cancer rates [58] . aba, rutin are other bioactive compounds of wheatgrass concerned as an anti-cancer representative and anti-cancer potential of wheatgrass is due to its anti-oxidant activity, which prevents oxidative damage of DNa [46] . ...
Plants have been utilized by humans throughout history for a variety of purposes, including sustenance and medicinal intentions. Since ancient times, wheatgrass has been utilized as a type of microgreen for therapeutic purposes. Phenolic flavonoids, vitamins, minerals, proteins and enzymes are all abundant in wheatgrass. These nutrients and bioactive substances enhanced wheatgrass’s therapeutic efficacy and made it a powerful antioxidant agent for the treatment of a range of diseases. it has been shown to have a wide variety of pharmacological potentials, including an antioxidative potential that helps to neutralize free radicals, anticancer, anti-ulcer, anti-diabetic, anti-arthritic, anti-microbial action, and many more. However, there is a dearth of scientific evidence to back up wheatgrass’s possible pharmacological effects and clinical value. To investigate its clinical utility for human welfare, in-depth research studies are needed. Through this analysis of the review literature, an attempt has been made to explain wheatgrass and its therapeutic potentials.
... According to Tirado-Kulieva et al. (2022), phenolic compounds are well recognised for their remarkable potential efficacy against a variety of human viruses. Additionally, various flavonoids have been demonstrated to have antiviral properties against several RNA viruses, containing the HSV-1, sindbis virus, and poliovirus (Middleton et al. 2000). The suppression of viral polymerase via either attaching with viral nucleic acid or viral capsid proteins are two of the flavonoids' hypothesised antiviral modes of action (Oluyemisi et al. 2015). ...
... According to Tirado-Kulieva et al. (2022), phenolic compounds are well recognised for their remarkable potential efficacy against a variety of human viruses. Additionally, various flavonoids have been demonstrated to have antiviral properties against several RNA viruses, containing the HSV-1, sindbis virus, and poliovirus (Middleton et al. 2000). The suppression of viral polymerase via either attaching with viral nucleic acid or viral capsid proteins are two of the flavonoids' hypothesised antiviral modes of action (Oluyemisi et al. 2015). ...
The current study evaluates hot water A. milleri sunflower extracts
at 40 °C temperature (AMSE40) for their antibacterial, anti-biofilm,
antiviral and anticancer activities. AMSE40 exhibited excellent antioxidant activity with an IC50 of 1.17 mg/mL (ascorbic acid) and was
found to be rich in phytochemical compounds such as alkaloids,
flavonoids, phenolics, saponins, and tannins, with concentrations of
1.23%, 351.60 mg/g, 152.50 mg/g, 0.98%, and 146.35 mg/g, respectively. AMSE40 showed strong antibacterial and anti-biofilm activity
against four multidrug-resistant isolates, comprising E. faecalis, S.
concentrations (25 mg/mL) and minimum inhibitory concentrations
viral efficacy against CoxB4 (9.1%) and HSV-1 (34.4%). Additionally,
AMSE40 induced DNA fragmentation in liver cell lines, indicating
cell death. The cytotoxic concentration of AMSE40 had a mild
impact on Vero (283.2 µg) and HepG2 cells (76.4 µg). A. milleri has
the potential to serve as a natural and eco-friendly source for innovative pharmaceutical and medical applications.
... Flavonoids work as effective free radical scavengers and powerful metal chelators. Studies have also revealed that flavonoids are much safer than other phytochemicals (Middleton et al. 2000). Flavonoids are polyphenolic compounds that possess a benzo-γ-pyrone basic nucleus that contains numerous hydroxyl groups (Mahomoodally et al. 2005). ...
Liver diseases represent a formidable global health threat. Hesperidin, a flavonoid found in citrus fruits, is the source of diosmin (DS). The in vivo and in vitro investigations of the pharmacological effects of DS reveal that it exhibits tremendous beneficial effects, such as fighting against inflammation, oxidative stress, and fibrosis. These effects have been noticed in various disease models, emphasizing the potential therapeutic value of DS in tackling diverse pathological conditions. Interestingly, DS has promising liver-defense capabilities against a range of hepatic illnesses, such as radiation-induced hepatic injury, liver ischemia/reperfusion injury, alcoholic hepatic disease, nonalcoholic fatty liver disease (NAFLD), and hepatocellular carcinoma (HCC). Furthermore, DS demonstrates potential hepatoprotective effects against environmental toxins, such as heavy metals. DS activates PPAR-γ and Nrf2, leading to antioxidant effects that reduce oxidative stress. Moreover, DS suppresses NF-κB, NLRP3, MAPK activities, and cytokine production (TNF-α and IL-1β), resulting in inflammation suppression. These anti-inflammatory effects are attributed to the activation of PPAR-γ and Nrf2, which are NF-κB inhibitors. This review aims to comprehensively discuss the hepatoprotective capacity of DS, elucidating the underlying mechanisms and identifying several research avenues that warrant further exploration to ascertain the prospective clinical advantages of DS intake as a viable strategy for the treatment of hepatic illnesses.
Graphical Abstract
... The high FRAP values in the Nigerian and Haitian varieties suggest their potential use in nutraceuticals and functional foods aimed at combating oxidative stress [37]. Antioxidants from these sources could play a significant role in preventing chronic diseases such as cardiovascular diseases and cancers [38,39] highlighted the potential of Moringa oleifera leaves as a natural source of antioxidants for health promotion and disease prevention [40,41,42]. ...
Moringa oleifera is a native plant from Asia, grown in the tropics. The leaves, bark, flowers, fruits, seeds, and roots are rich sources of phytochemicals and antioxidants; hence, they have been extensively utilized for medicinal purposes. This study aimed to determine the Antioxidant Activities of methanolic and ethanolic extracts of five varieties of Moringa leaves from Nigeria, Ghana, Haiti, India, and USA. The leaves were extracted using aqueous methanol and ethanol. 2, 2, -diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, Ferric Reducing Antioxidant Power (FRAP), and Trolox equivalent antioxidant capacity (TEAC) were then determined. Results indicated there were significant differences were recorded in DPPH, FRAP, and TEAC respectively. A significant difference in DPPH radical scavenging activities in the leaves from Haiti (94.83µmol TE g-1) and Ghana (86.69µmol TE g-1), Haiti (94.83µmol TE g-1) and Nigeria (84.94µmol TE g-1) respectively. Highest activity was observed in the ethanolic extract from the USA (123.48 µmol TE g⁻¹), while the lowest was in the methanolic extract from Nigeria (84.94 µmol TE g⁻¹). A similar result was also recorded for TEAC with ethanolic extracts from Ghana (61.59µmol TE g-1) significantly different from Nigeria (63.36µmol TE g-1), India (63.34µmol TE g-1), Haiti (62.42µmol TE g-1) and USA (62.36µmol TE g-1). FRAP methanolic extracts from Nigeria (232.96mg GAE g-1), USA (214.24mg GAE g-1) and India (201.81mg GAE g-1) were significantly different, while extracts from Haiti (222.16mg GAE g-1) and Ghana (221.35mg GAE g-1), USA (214.24mg GAE g-1) and Ghana (221.35mg GAE g-1) were in range.
Background
Hyperoside (quercetin-3-O-β-D-galactopyranoside) is a flavonol glycoside compound derived from plants in the Hypericum and Crataegus genera that reportedly exhibits an array of anti-inflammatory, antioxidant, and antitumor properties such that it has been used to treat various diseases. Whether it can serve as an effective treatment for chronic myeloid leukemia (CML) cells, however, has yet to be established. The present study was thus devised to assess the therapeutic effects of hyperoside on CML cells and to clarify the underlying mechanism of action.
Methods
Cellular viability, proliferative activity, migration, and apoptotic death were respectively analyzed through CCK-8, EDU, transwell, and flow cytometry assays. RNA-seq and bioinformatics approaches were further employed to evaluate the mechanisms through which hyperoside influences CML cells, while analyses of reactive oxygen species (ROS) and free iron were detected with commercial kits. Transmission electron microscopy was used to assess mitochondrial morphology. Molecular docking, cellular thermal shift assay (CETSA), and drug affinity responsive target stability (DARTS) approaches were also used to explore the ability of hyperoside to target NRF2.
Results
From a mechanistic perspective, hyperoside was able to inhibit SLC7A11/GPX4 signaling in a manner that was abrogated by the ferroptosis inhibitor ferrostatin-1. NRF2 was also closely associated with the inactivation of the SLC7A11/GPX4 axis mediated by hyperoside such that overexpressing NRF2 ablated the benefits associated with hyperoside treatment.
Conclusions
The present analyses indicate that hyperoside can target the NRF2/SLC7A11/GPX4 axis to induce ferroptotic CML cell death.
Plant-derived phenolic compounds are recognized to provide several health benefits for humans, including anticancer, anti-inflammatory, and antioxidant proprieties. Their bioavailability in the human body has a significant impact on these outcomes. Their bioaccessibility and bioavailability are highly dependent on the structure and manner in which phenolics enter into the organism, through a complex food matrix, for instance, or as pure isolates. Furthermore, the bioaccessibility of phenolic compounds in the body is greatly impacted by interactions with a broad range of other macromolecules (such as proteins, lipids, dietary fibers, and polysaccharides) in food or during digestion. Encapsulation is a process that can improve bioaccessibility and bioavailability by guaranteeing coating of the active ingredients, controlled release, and targeted distribution to specific parts of the digestive system. However, this field has not yet received enough attention, due to the complex mechanisms through which phenolics act in the body. This review attempts to shed light on the results of research that has been performed on the potential and therapeutic benefits of encapsulated polyphenols in both health and disease.
Diabetes mellitus is a chronic metabolic disease characterized by hyperglycemia. Prolonged hyperglycemia leads to oxidative stress, which plays a crucial role in causing further complications, including liver damage characterized by increased levels of Serum Glutamate Pyruvate Transaminase (SGPT) and Serum Glutamate Oxaloacetate Transaminase (SGOT). This study aimed to examine the effects of Cinnamomum burmanii bark extract on SGPT and SGOT levels in a mouse model of diabetes mellitus. The research employed an experimental design using a completely randomized design. It consisted of five treatment groups: K- (normal mice), K+ (diabetic mice), P1, P2, and P3 (diabetic mice treated with Cinnamomum burmanii bark extract at doses of 125, 250, and 500 mg/kg BW). Streptozotocin was injected into groups K+, P1, P2, and P3 at a dose of 0.1 ml per mouse for 14 days. If blood glucose levels increased, extracts were administered to groups P1, P2, and P3 according to the predetermined doses for 14 days. On day 28, surgery was performed to collect blood serum for SGPT and SGOT analysis.. The results of the study indicated that Cinnamomum burmanii bark extract could reduce SGPT and SGOT levels in the diabetic mouse model. This demonstrates the potential of Cinnamomum burmanii as a therapeutic agent that may help reduce liver damage often observed in diabetes mellitus
Introduction. Centaurea cyanus L. is an annual herbaceous plant whose funnel-shaped flowers are used as medicinal plant raw materials in official medicine. The biological activity (diuretic, choleretic, anti-inflammatory) of Centaurea cyanus flowers is associated with a complex of biologically active substances of phenolic nature. Anthocyanins act as the leading group used for the standardization of raw materials, according to the requirements of the State Pharmacopoeia of the Russian Federation, XV edition. Studies of the composition of flavonoids and phenolpropanoids of Centaurea cyanus flowers are relevant in terms of the value of their pharmacological properties.
Aim. To conduct TLC screening of phenolic compounds (flavonoids and phenolpropanoids) of Centaurea cyanus L. flowers.
Materials and methods. The objects of the study were dried whole flowers of Centaurea cyanus manufactured by the following companies: LLC «Lekra-SET», «Russkie Korni», Fito Way, LLC «HORST Company», LLC «Travy Gornogo Kryma» and LLC «Travy Bashkirii». Macro- and microscopic analysis was performed using a Mikromed MS-1 stereomicroscope (China), a Primo Star (Carl Zeiss, Germany) equipped with a Levenhuk M1400 PLUS digital camera, and microphotography editing was performed in Photoscape 3.7 according to the requirements of the State Pharmacopoeia of the Russian Federation, 15th edition. Screening of phenolic compounds was performed on plates with a silica gel layer on an aluminum substrate (Silica gel 60 F 254 , Merck KGaA, Германия). Detection was carried out with a 10 g/l solution of aminoethyl ester of diphenylboronic acid in ethyl alcohol and a 50 g/l solution of macrogol 400 in ethyl alcohol. After detection, the chromatograms were viewed in daylight and UV light at wavelengths of 254 and 365 nm using a UFS-254/365 chromatographic irradiator (IMID LLC, Russia). The comparison solutions were the following: rutin, quercetin, isoquercitrin, hyperoside, and caffeic acid.
Results and discussion. As a result of the studies, the macro- and microscopic characteristics of the analyzed samples of Centaurea cyanus flowers corresponded to FS.2.5.0064.18 « Centaurea cyanus flowers». An adsorption zone with yellow-green fluorescence was found on the chromatogram of all the studied extracts, which, according to the Rf value, corresponds to the isoquercitrin RS. Chromatographic profiles of four of the six analyzed objects had 4 chromatographic adsorption zones related to flavonoids and phenolpropanoids. The samples of «Russkie Korni» and LLC «HORST Company» had only 3 zones, which is probably due to the low concentration of phenolic compounds in the plant material.
Conclusion. The screening of phenolic compounds (flavonoids and phenolpropanoids) of Centaurea cyanus flowers was carried out using the planar chromatography method. The chromatograms of water-alcohol extracts showed an adsorption zone corresponding to isoquercitrin RS, and there were also other adsorption zones with fluorescence in UV light.
Polyphenols are the organic compounds that available naturally in different fruits and vegetables which has many biological effects. The link between (poly) phenol-rich diets and human health has been proven in several epidemiological research. Consumer awareness about connection between nutrition, health, and illness has sparked new industrial opportunities. Consumers want functional foods and their synergistic health advantages. Polyphenols has numerous benefits in different areas. This following chapter will demonstrate about the significance of several phenolic chemicals, their biological effects basically about antioxidant activity, antimicrobial activity, and their potential for use in a variety of industries as well as their analysis, extraction methods, factor affecting bioavailability and bioaccessibility.
BACKGROUND
Flavonoids, the main class of polyphenols, exhibit antioxidant and antihypertensive properties.
AIM
To prospectively investigate the impact of flavonoids on arterial stiffness in patients with chronic kidney disease (CKD) stages I-IV.
METHODS
In this prospective, single-arm study, CKD patients with arterial hypertension and diabetes mellitus were enrolled. Baseline demographic, clinical, and laboratory variables were recorded. Patients received daily treatment with a phenol-rich dietary supplement for 3 months. Blood pressure, arterial stiffness (carotid-femoral pulse wave velocity, central pulse pressure), and oxidative stress markers (protein carbonyls, total phenolic compound, total antioxidant capacity) were measured at baseline and at study end.
RESULTS
Sixteen patients (mean age: 62.5 years, 87.5% male) completed the study. Following intervention, peripheral systolic blood pressure decreased significantly by 14 mmHg (P < 0.001). Carotid-femoral pulse wave velocity decreased from 8.9 m/s (baseline) to 8.2 m/s (study end) (P < 0.001), and central pulse pressure improved from 59 mmHg to 48 mmHg (P = 0.003). Flavonoids also reduced oxidative stress markers including protein carbonyls (P < 0.001), total phenolic compound (P = 0.001), and total antioxidant capacity (P = 0.013).
CONCLUSION
Flavonoid supplementation in CKD patients shows promise in improving blood pressure, arterial stiffness, and oxidative stress markers.
Background. Ageing is associated with progressive impairment of physical functions and increased risk of age-related chronic diseases. Polyphenols such as mangiferin, quercetin and trans-cinnamic acid are also used for the treatment and prevention of chronic diseases. Toxicological research was important in biomedical research, as some high-dose extracted polyphenols could contribute to the development and progression of cancer and other diseases. This study is aimed at assessing toxicological safety of previously isolated phenolic compounds from plants of the Siberian Federal District. Materials and methods. Rodents have been chosen as the model organism. The study of mutagenic and antimutagenic properties was carried out using a micronuclear test of bone marrow cell. Cytotoxicity in vitro was assessed using the MTT test. Results. Polyphenols studied at doses of 50.0 and 100.0 mg/kg are not mutagenic. Mangiferri and quercetin at a dose of 50.0 mg/kg do not have anti-thagenic effects. In this case, trans-cinnamic acid in the same concentration has antimutagenic effect. Mangiferin in concentrates from 4.2 to 16.7 ug/ml has a cytotoxic effect. Trans-cinnamic acid is not cytotoxic (at 2.1-33.3 ug/ml). Quercetin has a cytotoxic effect in concentrations of 0.21 and 1.67 ug/ml, and at concentrations of 3.33 ug/ml increases the viability of splenocytes, presumably due to antioxidant properties. Conclusion. Safety or low toxicity is a decisive advantage of the continued use of polyphenols as advanced heroic flow agents. Further study of biologically active substances (mangiferin, quercetin and trans-cinnamic acid) has been found to be ce-woody. The work was carried out by the state task on the topic «Development of biologically active additives consisting of metabolites of plant objects in vitro to protect the population from premature aging» (project FZSR-2024-0008) using the equipment of Center of Collective Use «Instrumental methods of analysis in the field of applied biotechnology» on the basis of KemSU.
Doxorubicin (DOX) is one of the most extensively prescribed antineoplastic agents, which evokes
oxidative stress. This agent ensues various systemic side effects especially pulmotoxicity, which
halters its clinical consumption in chemotherapy. Mangiferin (MGF) is a xanthone that exhibits
therapeutic potential with anti-tumor, antidiabetic, anti-inflammatory, and antioxidant properties.
This study is an attempt to investigate the possible therapeutic potential, and protective effect of
Mangiferin (MGF) C19H18O11 against DOX-induced pulmonary damage in rats, using biochemical
approaches. The experiment was conducted for one month at the Biocontrol Laboratory at the
University of Agriculture in Faisalabad. Twenty-four male albino rats were maintained in cages
and divided into four random groups (six rats each). The study groups were tagged as control
group, DOX, DOX+MGF and MGF. 1st group served as the control group. 2nd group was given
DOX (5 mg/kg). 3rd group was treated with DOX (5mg/kg) and MGF (25 mg/kg) simultaneously.
25 mg/kg MGF was administered into 4th group. This experiment was conducted for 30 days.
During this duration the physical as well as physiological conditions of experimental sample was
analyzed regularly. The findings indicated that when rats were exposed to doxorubicin, the activity
of antioxidant enzymes, i.e., glutathione (GSH), glutathione peroxidase (GPx), catalase (CAT),
glutathione reductase (GSR), superoxide dismutase (SOD), and glutathione S-transferase (GST)
decreased. After treatment with Mangiferin, an elevation in the antioxidant enzymes activity was
observed. In addition, doxorubicin caused inflammation of the lungs in rats. In contrast,
Mangiferin reduced the inflammation by lowering the level of the inflammatory cytokine (TNF
α, NFκB, IL-6, IL-1β, and COX-2) and acted as an anti-inflammatory drug. The consequences
demonstrated that Mangiferin reduced doxorubicin caused oxidative stress by reducing the levels
of malondialdehyde (MDA) and reactive oxygen species (ROS) in lung tissues of the rat. However,
MGF treatment recovered all the damages in the lung induced by DOX treatment. Our findings
indicated that Mangiferin might act as a natural therapeutic agent against the adverse impacts of
lung damage induced by doxorubicin.
Although there are numerous available immunomodulators, those of natural origin would be preferable based on their safety profile and effectiveness. The research and clinical interest in immunomodulators have increased in the last decades, especially in the immunomodulatory properties of plant-based therapies. Innovative technologies and extensive study on immunomodulatory natural products, botanicals, extracts, and active moieties with immunomodulatory potential could provide us with valuable entities to develop as novel immunomodulatory medicines to enhance current chemotherapies. This review focuses on plant-based immunomodulatory drugs that are currently in clinical studies. However, further studies in this area are of utmost importance to obtain complete information about the positive effects of medicinal plants and their chemical components and molecules as an alternative to combatting various diseases and/or prevention.
Chronic liver injuries often lead to hepatic fibrosis, a condition characterized by excessive extracellular matrix accumulation and abnormal connective tissue hyperplasia. Without effective treatment, hepatic fibrosis can progress to cirrhosis or hepatocellular carcinoma. Current treatments, including liver transplantation, are limited by donor shortages and high costs. As such, there is an urgent need for effective therapeutic strategies. This review focuses on the potential of plant-based therapeutics, particularly polyphenols, phenolic acids, and flavonoids, in treating hepatic fibrosis. These compounds have demonstrated anti-fibrotic activities through various signaling pathways, including TGF-β/Smad, AMPK/mTOR, Wnt/β-catenin, NF-κB, PI3K/AKT/mTOR, and hedgehog pathways. Additionally, this review highlights the advancements in nanoparticulate drug delivery systems that enhance the pharmacokinetics, bioavailability, and therapeutic efficacy of these bioactive compounds. Methodologically, this review synthesizes findings from recent studies, providing a comprehensive analysis of the mechanisms and benefits of these plant-based treatments. The integration of novel drug delivery systems with plant-based therapeutics holds significant promise for developing effective treatments for hepatic fibrosis.
A multitude of plant-derived bioactive compounds have shown significant promise in preventing chronic illnesses, with flavonoids constituting a substantial class of naturally occurring polyphenolic compounds. Apigenin, a flavone identified as 4',5,7-trihydroxyflavone, holds immense promise as a preventative agent against chronic illnesses. Despite its extensive research and recognized nutraceutical value, its therapeutic application remains underexplored, necessitating further clinical investigations. This review delves into the biological sources, nutraceutical prospects, chemistry, pharmacological insights, and health benefits of apigenin. Through multifaceted analytical studies, we explore its diverse pharmacological profile and potential therapeutic applications across various health domains. The manuscript comprehensively examines apigenin's role as a neuroprotective , anti-inflammatory compound, and a potent antioxidant agent. Additionally, its efficacy in combating cardiovascular diseases, anti-diabetic properties, and anticancer potential has been discussed. Furthermore, the antimicrobial attributes and the challenges surrounding its bioavailability, particularly from herbal supplements have been addressed. Available in diverse forms including tablets, capsules, solid dispersions, co-crystals, inclusion complexes and nano formulations. Additionally, it is prevalent as a nutraceutical supplement in herbal formulations. While strides have been made in overcoming pharmacokinetic hurdles, further research into apigenin's clinical effectiveness and bioavailability from herbal supplements remains imperative for its widespread utilization in preventive medicine.
Secondary metabolites (SMs) produced by plants possesses important therapeutic activities which are used to treat various diseases and disorders. However, in natural plants, SMs are synthesized in limited concentration and it varies according to climatic and geographical conditions. Over the years, production of SMs is continuously increasing and to fulfil the market demand, novel techniques are being experimented. Callus cultures, organ cultures, cell suspensions cultures etc., are some biotechnological techniques for producing SMs at optimum concentration. Additionally, biotic and abiotic elicitors have also been proved promising to increase SMs level in in vitro cultures. Among various elicitors, nanoparticles have gained special attention due to their encouraging capacity to enhance SMs with several other benefits. Researchers have been captivated by nanomaterials due to their smaller size, which enables easy penetration and manipulation of the cell's metabolism, resulting in increased production of phytochemicals. Biologically synthesized nanoparticles (Green synthesis) have been investigated in different in vitro cultures to enhance these phyto-compounds level. With this background, in the present chapter, we have thoroughly reviewed recent updates on application of biologically synthesized nanoparticles to enhance SMs using in vitro cultures of important medicinal plants.
An expression vector containing the Rhizobium leguminosarum nodA promoter cloned in front of the Escherichia coli lacZ gene was used to characterize the properties of the R. leguminosarum nodA gene-inducing compound(s) present in sterile root exudate of the host plant Vicia sativa L. subsp. nigra (L.). The major inducing compound was flavonoid in nature, most likely a flavanone. The commercially available flavonoids naringenin (5,7,4'-trihydroxyflavanone), eriodictyol (5,7,3'4'-tetrahydroxyflavanone), apigenin (5,7,4'-trihydroxyflavone), and luteolin (5,7,3',4'-tetrahydroxyflavone) induced the nodA promoter to the same level as the root exudate. On the basis of chromatographic properties, it was concluded that none of these compounds is identical to the inducer that is present in root exudate. The induction of the nodA promoter by root exudate and by the most effective inducer naringenin was very similar, as judged from the genetic requirements and the kinetics of induction.
Screening of plant extracts found that a biflavone from Cephalotaxus drupacea, which was found to be ginkgetin, is active
against herpes simplex virus type 1 (HSV-1). This compound caused dose-dependent inhibition of virus replication with a 50%
cytotoxic activity at 12.8 micrograms/ml and 50% anti-HSV-1 activity at 0.91 micrograms/ml, the therapeutic index being 14.1.
Ginkgetin also showed inhibitory effects against HSV type 2 and human cytomegalovirus with therapeutic indices of 13.8 and
11.6, respectively. Ginkgetin had a weak virucidal activity against HSV-1 at more than 5 micrograms/ml. Both adsorption of
HSV-1 to host cells and virus penetration into cells were unaffected by this agent. Ginkgetin suppressed viral protein synthesis
when added at various steps of HSV-1 replication and exerted strong inhibition of transcription of the immediate-early genes.
Ro 09-0179 (4',5-dihydroxy-3,3',7-trimethoxyflavone), isolated from a Chinese medicinal herb, was found to have potent antiviral
activity. It selectively inhibited the replication of human picornaviruses, such as rhinoviruses and coxsackieviruses in tissue
culture, but not other DNA and RNA viruses. Ro 09-0298 (4',5-diacetyloxy-3,3',7-trimethoxyflavone), an orally active derivative
of Ro 09-0179, prevented coxsackievirus (B1) infection in mice. The critical time for the inhibition of rhinovirus replication
by Ro 09-0179 was 2 to 4 h after virus adsorption, i.e., in the early stages of virus replication. It markedly inhibited coxsackievirus
and rhinovirus RNA synthesis in infected HeLa cells, but not in a cell-free system using the RNA polymerase complex isolated
from the infected cells. In the infected cells, the RNA polymerase complex was not formed in the presence of Ro 09-0179. Therefore,
it is suggested that Ro 09-0179 interferes with some process of viral replication which occurs between viral uncoating and
the initiation of viral RNA synthesis.