ArticleLiterature Review

Health benefit of fucosterol from marine algae - A Review

Wiley
Journal of The Science of Food and Agriculture
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Abstract

Background: Seaweeds belong to a group of marine plants known as algae which consumed as sea vegetables in several Asian countries. Recent studies have focused on the biological and pharmacological activities of seaweeds and its highly bioactive secondary metabolites due to its possibility in the development of new pharmaceutical agents. Although several varieties of bioactive novel compounds such as phlorotannins, diterpenes, and polysaccharides from seaweeds have been already well scrutinized, fucosterol as phytosterols still need to reinvent itself. Results: Fucosterol (24-ethylidene cholesterol) is a sterol that can be isolated from algae, seaweed, and diatoms. Fucosterol exhibits various biological therapeutics, including anti-cancer, anti-diabetic, anti-oxidant, hepatoprotective, anti-hyperlipidemic, anti-fungal, anti-histaminic, anti-cholinergic, anti-adipogenic, anti-photodamaging, anti-osteoporotic, blood cholesterol reducing, blood vessel thrombosis preventive, and butyrylcholinesterase inhibitory activities. Conclusion: In this review, we address some potential approaches for arbitrating novel fucosterol biologics in the medical field, focusing on the selection of personalized drug candidates and highlighting the challenges and opportunities regarding medical breakthroughs. We also highlight the recent advances made in the design of this novel compound, as the significant health benefits from using these optimized applications apply to the nutraceutical and pharmaceutical fields.

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... Fucosterol (Figure 1a), a phytosterol, is abundant in edible brown algae. Studies have demonstrated that fucosterol possesses anti-diabetes, anti-cancer, and antioxidant properties [8]. Notably, fucosterol has been documented to be a robust anti-inflammatory phytosterol that inhibits inducible nitric oxide synthase and pro-inflammatory cytokine secretion through the suppression of both the nuclear factor-kappa B (NF-κB) and p38 mitogenactivated protein kinase (MAPK) signaling pathways in lipopolysaccharide-treated macrophages [8][9][10]. ...
... Studies have demonstrated that fucosterol possesses anti-diabetes, anti-cancer, and antioxidant properties [8]. Notably, fucosterol has been documented to be a robust anti-inflammatory phytosterol that inhibits inducible nitric oxide synthase and pro-inflammatory cytokine secretion through the suppression of both the nuclear factor-kappa B (NF-κB) and p38 mitogenactivated protein kinase (MAPK) signaling pathways in lipopolysaccharide-treated macrophages [8][9][10]. However, whether fucosterol has anti-muscle atrophy properties in vitro or in vivo has not yet been determined. ...
... Studies have shown that an intake of fucosterol in the range of 20-300 mg/kg/day has beneficial effects [8]. Also, fucosterol is found in brown seaweed at concentrations of 8.2 to 32.2 mg/g dry weight [14]. ...
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The objective of this study was to examine whether fucosterol, a phytosterol of marine algae, could ameliorate skeletal muscle atrophy in tumor necrosis factor-alpha (TNF-α)-treated C2C12 myotubes and in immobilization-induced C57BL/6J mice. Male C57BL6J mice were immobilized for 1 week to induce skeletal muscle atrophy. Following immobilization, the mice were administrated orally with saline or fucosterol (10 or 30 mg/kg/day) for 1 week. Fucosterol significantly attenuated immobilization-induced muscle atrophy by enhancing muscle strength, with a concomitant increase in muscle volume, mass, and myofiber cross-sectional area in the tibialis anterior (TA) muscle in mice. In both the TNF-α-treated C2C12 myotubes and the TA muscle of immobilized mice, fucosterol significantly prevented muscle protein degradation, which was attributed to a reduction in atrogin-1 and muscle ring finger 1 gene expression through an increase in forkhead box O3α (FoxO3α) phosphorylation. Continuously, fucosterol stimulated muscle protein synthesis by increasing the phosphorylation of the mammalian target of the rapamycin (mTOR), 70 kDa ribosomal protein S6 kinase, and 4E binding protein 1, which was mediated through the stimulation of the phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway. Thus, fucosterol alleviated skeletal muscle atrophy in TNF-α-treated C2C12 myotubes and immobilized C57BL/6J mice through the regulation of the Akt/mTOR/FoxO3α signaling pathway.
... com/8-unbel ievab le-health-benefi ts-of-rhodo dendr on/). Detected terpenoids reported as anti-inflammatory were; RFD metabolites-cis-citral [43], patchoulane [44], beta-copaene [45], alpha-curcumene [46], squalene, vitamin E, methyl commate A [7], fucosterol [47]; exclusive GW metabolites-bornyl acetate and lupeol (major terpenoid of GW) [7]; and exclusive GR metabolite-cis-α-irone [48]. RFD compounds-citral, beta-copaene, alpha-curcumene, squalene, vitamin E and fucosterol; and GW metabolites-bornyl acetate and lupeol can possess significant antioxidant activity [7,8,43,45,47,[49][50][51]. ...
... Detected terpenoids reported as anti-inflammatory were; RFD metabolites-cis-citral [43], patchoulane [44], beta-copaene [45], alpha-curcumene [46], squalene, vitamin E, methyl commate A [7], fucosterol [47]; exclusive GW metabolites-bornyl acetate and lupeol (major terpenoid of GW) [7]; and exclusive GR metabolite-cis-α-irone [48]. RFD compounds-citral, beta-copaene, alpha-curcumene, squalene, vitamin E and fucosterol; and GW metabolites-bornyl acetate and lupeol can possess significant antioxidant activity [7,8,43,45,47,[49][50][51]. RFD metabolites such as citral, beta-copaene, alphacurcumene, squalene, beta-amyrone and fucosterol; and GW metabolites-lupeol and bornyl acetate were previously reported as antimicrobials [8,43,45,47,[52][53][54][55][56]. ...
... RFD compounds-citral, beta-copaene, alpha-curcumene, squalene, vitamin E and fucosterol; and GW metabolites-bornyl acetate and lupeol can possess significant antioxidant activity [7,8,43,45,47,[49][50][51]. RFD metabolites such as citral, beta-copaene, alphacurcumene, squalene, beta-amyrone and fucosterol; and GW metabolites-lupeol and bornyl acetate were previously reported as antimicrobials [8,43,45,47,[52][53][54][55][56]. Earlier, Muktar et al. [55] discovered the antibacterial potential of lupeol against Bacillus subtilis. ...
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Guras or Rhododendron wine and its Raksi are popular and therapeutic traditional drinks served in the rhododendron growing regions of the Himalayas; mainly in northern and north eastern part of India, Nepal and Indo-Nepal Singalila ridge. Earlier research showed that samples such as unfermented Guras decoction, wine and distilled liquor Raksi collected from Singalila ridge—the land of Guras exhibited potential bioactivities through various in vitro assays. In this follow-up research, GC–MS analysis was carried out that revealed responsible bioactive candidates which also exhibited correlations with reported physicochemical and biochemical properties. Abundance of phytochemicals including major compound quinic acid (34.97% peak area) was recorded in the unfermented decoction while the wine and Raksi were rich in bioactive fermented products i.e., metabolites of the fermenting microbes of the starter- Marcha. Furthermore, biosynthesis pathways of metabolites were proposed following microbial fermentation. Graphical Abstract
... These organisms produce several essential polyunsaturated fatty acids (PUFAs), including eicosapentaenoic acid (EPA 20:5 ω-3), docosahexaenoic acid (DHA 22:6 ω-3), α-linolenic acid (ALA 18:3 ω-3), γ-linolenic acid (GLA 18:3 ω-6), and arachidonic acid (ARA 20:6 ω-6) [104]. On the other hand, sterols are primarily found in many eukaryotic organisms and are an integral part of the plasma membrane, which is also quite common in microalgal species [105,106]. It has been observed that extracts from Schizochytrium (Bigryra phylum, class Labyrinthulea) have a potent influence on the relationship between intestinal gene expression and cholesterol intake [107]. ...
... This algae, considered a nutritious food source, is rich in macro and micro components, including essential amino acids, omega-3 polyunsaturated fatty acids, minerals, and vitamins. These compounds have been linked to potential benefits for cardiovascular health, immune function, and modulation of the gut microbiota [105,149,166,167]. After being approved for its safety, it has begun to be used as a food supplement and food additive. ...
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Microalgae are photosynthetic microorganisms that have a rapid growth cycle and carbon fixation ability. They have diverse cellular structures, ranging from prokaryotic cyanobacteria to more complex eukaryotic forms, which enable them to thrive in a variety of environments and support biomass production. They utilize both photosynthesis and heterotrophic pathways, indicating their ecological importance and potential for biotechnological applications. Reproducing primarily through asexual means, microalgae have complex cell cycles that are crucial for their growth and ability to adapt to changing conditions. Additionally, microalgae possess bioactive compounds that make them both nutritious and functional. Thanks to their content of proteins, lipids, carbohydrates, vitamins, and minerals, they play an important role in the development of functional food products, particularly by enhancing nutritional content and product quality. Furthermore, studies have demonstrated that algae and algal bioactive compounds support cardiovascular health, immune function, and gut health, especially in relation to obesity and other metabolic diseases. They also contribute to skin health and cognitive functions, including memory. This review article explores the biological, nutritional, and functional properties of microalgae based on the studies conducted.
... It can be found in brown macroalgae and isolated from species of the genera Laminaria, Undaria, Sargassum, and Ecklonia [84,85]. It is known to present several health benefits [86], and it is also known that fucosterol (27) has effects on several inflammatory pathways, such as decreasing the expression of p50 and p65 mRNA and the activity of NF-κB promoter in a dose-dependent manner, inhibiting the expression of TNF-α, COX-2, IL-1β, and IL-6 [87,88]. It also reduced the inflammatory response caused by solar ultraviolet radiation (UVR) [89]. ...
... be found in brown macroalgae and isolated from species of the genera Laminaria, Undaria, Sargassum, and Ecklonia [84,85]. It is known to present several health benefits [86], and it is also known that fucosterol (27) has effects on several inflammatory pathways, such as decreasing the expression of p50 and p65 mRNA and the activity of NF-κB promoter in a dose-dependent manner, inhibiting the expression of TNF-α, COX-2, IL-1β, and IL-6 [87,88]. It also reduced the inflammatory response caused by solar ultraviolet radiation (UVR) [89]. ...
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Inflammation is an organism’s response to chemical or physical injury. It is split into acute and chronic inflammation and is the last, most significant cause of death worldwide. Nowadays, according to the World Health Organization (WHO), the greatest threat to human health is chronic disease. Worldwide, three out of five people die from chronic inflammatory diseases such as stroke, chronic respiratory diseases, heart disorders, and cancer. Nowadays, anti-inflammatory drugs (steroidal and non-steroidal, enzyme inhibitors that are essential in the inflammatory process, and receptor antagonists, among others) have been considered as promising treatments to be explored. However, there remains a significant proportion of patients who show poor or incomplete responses to these treatments or experience associated severe side effects. Seaweeds represent a valuable resource of bioactive compounds associated with anti-inflammatory effects and offer great potential for the development of new anti-inflammatory drugs. This review presents an overview of specialized metabolites isolated from seaweeds with in situ and in vivo anti-inflammatory properties. Phlorotannins, carotenoids, sterols, alkaloids, and polyunsaturated fatty acids present significant anti-inflammatory effects given that some of them are involved directly or indirectly in several inflammatory pathways. The majority of the isolated compounds inhibit the pro-inflammatory mediators/cytokines. Studies have suggested an excellent selectivity of chromene nucleus towards inducible pro-inflammatory COX-2 than its constitutive isoform COX-1. Additional research is needed to understand the mechanisms of action of seaweed’s compounds in inflammation, given the production of sustainable and healthier anti-inflammatory agents.
... Farasat et al. [80], and Cho et al. [81] studied and proved the high radical scavenging activities of various green (Chlorophyta) species such as Ulva clathrata, U. compressa (formerly known as Enteromorpha compressa), U. intestinalis, U. linza, U. flexuosa, U. australis (formerly known as Ulva pertusa), Capsosiphon fulvescens, and Chaetomorpha moniligera. In their findings, antibacterial and cytotoxic effects on breast ductal carcinoma cell lines were verified in the phenolic fraction of U. clathrata and U. flexuosa [82,83]. In a more recent study, Lavoie et al. [84] reported C. socialis-derived phenolic compounds, such as 2, 3,8,9- The functions of phenol compounds in red marine algae have barely been studied, but they probably have multipurpose actions in cell life, such as antioxidant, chelation, and anti-infection actions, as well as cofactors or hormones [85]. ...
... phenolic fraction of U. clathrata and U. flexuosa [82,83]. In a more recent study, Lavoie et al. [84] reported C. socialis-derived phenolic compounds, such as 2,3,8,9-tetrahydrobenzo[c]chromen-6-one (Figure 2a The functions of phenol compounds in red marine algae have barely been studied, but they probably have multipurpose actions in cell life, such as antioxidant, chelation, and anti-infection actions, as well as cofactors or hormones [85]. ...
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Marine macroalgae have an interesting profile of bioactive compounds and have gained tremendous attention in cosmeceuticals with negligible toxicity effects (cytotoxicity, reproductive toxicity, genotoxicity, mutagenicity, carcinogenicity, etc.) on humans and exhibit strong benefits for the skin. Among the diversified compounds, phenolic compounds are the group of phytochemicals found in high amounts with great structural diversity. Phlorotannin is the most studied polyphenol compound in brown algae, but besides there are some other phenolic compounds observed and studied in macroalgae such as terpenoids, bromophenols, mycosporine amino acids (MAAs), and flavonoids. These compounds are already characterized and studied for their full range of cosmeceutical benefits such as skin whitening, moisturizing, photoprotection, antiaging, antiwrinkle, anti-melanogenic, and antioxidant activities as well as in the treatment of pruritus (caused by acne, eczema, dermatitis, hives, psoriasis), photoaging, and skin pigmentation disorders (hypopigmentation due to the absence of melanocytes and hyperpigmentation caused by skin irritation or metabolic disorders). This review study mainly focuses on marine algae-derived phenolic compounds and their extraction, characterization, and skin cosmetic benefits described in the literature. The present study aims to provide a detailed insight into the phenolic compounds in marine algae.
... These results confirmed previous treatments of Fusarium culmorum Fc37 and Fusarium culmorum CBS122 macroconidia with an unfractionated scCO 2 extract of Fucus vesiculosus [31] and indicated that fucosterol may play an important role in this context. Fucosterol was found before to act as an antifungal agent against certain phytopathogens (Pyricularia oryzae, Staphylococcus epidermidis, Aspergillus niger, Candida albicans, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Fusarium culmorum) and yeast species (Curvularia lunata, Stachybotrys atra, Microsporum canis) and the mode of action was supposed to be inhibiting fungal growth by causing structural degradation in fungal cells [24,31,64]. ...
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The exploration of natural antifungal substances from algal origins is significant due to the increasing resistance of pathogens to conventional antifungal agents and the growing consumer demand for natural products. This manuscript represents the inaugural investigation into the antifungal attributes of bioactive compounds extracted from Fucus vesiculosus via supercritical carbon dioxide (scCO2) extraction utilizing contemporary countercurrent chromatography (CCC). In aligning with the prospective utilization of this extract within the agricultural sector, this study also serves as the preliminary report demonstrating the capability of Fucus vesiculosus scCO2 extract to enhance the activity of plant resistance enzymes. The fractions obtained through CCC were subjected to evaluation for their efficacy in inhibiting the macrospores of Fusarium culmorum. The CCC methodology facilitated the successful separation of fatty acids (reaching up to 82.0 wt.% in a given fraction) and fucosterol (attaining up to 79.4 wt.% in another fraction). All CCC fractions at the concentration of 1.0% were found to inhibit 100% of Fusarium culmorum growth. Moreover, Fucus vesiculosus scCO2 extract was able to activate plant resistance enzymes (Catalase, Ascorbic Peroxidase, Guaiacol Peroxidase, Phenylalanine Ammonia-Lyase, and Phenylalanine Ammonia-Lyase Activity).
... To further examine the therapeutic potential of C/EBPα in DKD, we used Fucosterol, a C/EBPα inhibitor, to treat db/db mice. Fucosterol, a phytosterol abundant in brown seaweed, could regulate lipid generation by inhibiting C/EBPα [34,35]. Recent studies have highlighted the significant anti-inflammatory effects of Fucosterol on various diseases, including neurological disorders, lung fibrosis, and COVID-19 [36][37][38][39]. ...
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Diabetic kidney disease (DKD) is a prevalent and debilitating complication of diabetes characterized by progressive renal function decline and a lack of effective treatment options. Here, we investigated the role of the transcription factor CCAAT/enhancer binding protein alpha (C/EBPα) in DKD pathogenesis. Analysis of renal biopsy samples revealed increased C/EBPα expression in patients with DKD. Using RNA sequencing and proteomics, we explored the mechanisms through which the C/EBPα contributes to DKD. Our findings demonstrated that C/EBPα exacerbated tubular injury by promoting acyl-CoA synthetase long-chain family member 4 (ACSL4)-dependent ferroptosis. We identified that C/EBPα upregulated ACSL4 expression by binding to its transcription regulatory sequence (TRS), leading to elevated lipid peroxidation and ferroptosis. Furthermore, inhibition or genetic ablation of C/EBPα attenuated ferroptosis and mitigated tubular injury in DKD. These results highlighted the C/EBPα-ACSL4-ferroptosis pathway as a promising therapeutic target for DKD treatment.
... Phycocyanin pigment derived from Spirulina has reno-protective effects. Similarly, various seaweeds derived metabolites such as fucosterol (Abdul et al. 2016), alginic acid (Sarithakumari et al. 2013), dieckol (Sanjeewa et al. 2020), eckol (Wei et al. 2016), diphlorethohydroxycarmalol (Fernando et al. 2017), gallic acid (Lajili et al. 2016), mojabanchromanol (Jeong et al. 2014), phlorotannins (Kim et al. 2009), and flavonoids (Shoubaky et al. 2016) are reported to possess anti-inflammatory properties. ...
Chapter
Ethnomedicinal plants have been the source of drugs since the dawn of human civilization. A number of systems of traditional medicine have evolved from the application of ethnomedicinal plants for treating human disorders. Producing drugs from medicinal plants largely relied on chemical techniques like solvent extraction, distillation, fermentation, digestion, decoction, percolation, and chromatography until the advent of omics technologies during the early twenty-first century. The availability of human genome sequence data has propelled drug discovery, where knowledge of disease-susceptibility genes can be used to design drugs with minimal off-target effects. Understanding biochemical pathways using the genome sequence data can help identify new targets for drug development. Sequencing of medicinal plant genomes can help in understanding the metabolite pathways and uncover key intermediates that can be tweaked to enhance the production of bioactive chemicals. Metabolomic approaches are playing a crucial role in discovery of new drug molecules, as a major category of plant drugs are secondary metabolites. Metabolic engineering, combining the power of genetics, biochemistry, and system biology, has facilitated the development of novel drug molecules. Using a semi-synthetic approach to drug production involving metabolic engineering, we can scale up the production of plant-based drugs without negatively affecting endangered or threatened plant species. A lot of plant proteins have been discovered to play a role in combating diseases like cancer, diabetes, HIV, and microbial diseases. Developments in proteomic technologies like 2D-PAGE, mass spectrometry, MALDI-TOF, NMR, and protein interaction networks can minimize the time period required to develop new drugs and help in studying drug interactions and biosafety. We are witnessing a new era in the identification, purification, and production of plant-based medicinal compounds, greatly assisted by omics technologies enabling the mankind to effectively fight against severe and emerging diseases.
... As this study exclusively focused on evaluating anti-inflammatory properties, therefore, a brief literature study has been done to identify the anti-inflammatory biomolecules. This revealed fifteen compounds with reported anti-inflammatory properties: UGD's major phenolic compound quinic acid (Lingwan et al., 2023;Majumder et al., 2022b); 2-hydroxy-gamma-butyrolactone (Salat et al., 2012); 2,3-dihydrobenzofuran (Closse et al., 1981;Chen et al., 2019;Nousheen et al., 2022); GW's tyrosol (Hu et al., 2020;Majumder et al., 2022b;); UGD's terpenoid metabolites-cis-citral (Ganjewala et al., 2012), patchoulane (Chavan et al., 2012), beta-copaene (Al-Rekaby, 2020), alphacurcumene (Lenfeld et al., 1986), squalene, vitamin E, methyl commate A (detected in all samples) (Majumder et al., 2020), fucosterol (Abdul et al., 2016); exclusive GW metabolites-bornyl acetate and lupeol (major terpenoid of GW) (Majumder et al., 2020); and exclusive GR metabolite-cis-α-irone (Lim, 2016). Among these fifteen biomolecules eleven signature compounds (Fig. 4) with considerably high relative peak areas were used in the docking analysis. ...
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This in vitro and in silico study was designed to validate acclaimed anti-inflammatory or pain-relieving properties of fermented ethnic beverages prepared from Rhododendron or Guras flowers in the Singalila ridge-the famous Rhododendron growing region of the Himalayas. Traditional beverages Guras wine and its distilled version Guras Raksi were considered in this study which were collected from Gairibas, a village situated in Indo-Nepal Singalila Ridge of the Himalayas. In vitro protein (albumin) denaturation inhibition assay was conducted to evaluate anti-inflammatory activity of the samples and later GC-MS analysis was carried out to identify anti-inflammatory compounds present in those beverages. From GC-MS results, eleven major metabolites such as 5-hydroxymethylfurfural; quinic acid; clionasterol; l-(+)-ascorbic acid, 2,6-dihexadecanoate; d-sorbitol; cis-cinnamic acid; tyrosol; lupeol; methyl commate A; 2-hydroxy-gamma-butyrolactone; and 1,3-propanediol, 2-(hydroxymethyl)-2-nitro-were chosen for molecular docking with human cyclooxygenase-1 (hCOX-1), an important targets in the drug-design for nonsteroidal anti-inflammatory drugs. Among all query compounds, phytosterol-clionasterol and triterpenoid-lupeol and methyl commate A exhibited considerably high binding energy scores (<-8 kcal/mol) even compared to anti-inflammatory drugs-acetaminophen and ibuprofen. Outcome of this research affirmed the potential of Guras-based traditional drinks in the healing of different forms of high-altitudinal stress induced pain.
... Red and brown macroalgae have a high proportion of total fatty acids in EPA and arachidonic acid ( Jiang and Chen, 2000 ). Red algae having a high proportion of fatty acids like EPA may not meet dietary recommendations for daily EFA alone ( Khotimchenko and Vaskovsky, 1990 ). Fucosterol, occurring in many red and brown macroalgae, has been used to treat health-related complications like diabetes and hypertension ( Abdul et al., 2016 ). ...
... Other biologically active phytochemicals detected were stigmasterol, tricyclo-triacontane, fucosterol, pregnenolone, cyclodecasiloxane, and alpha-amyrin. Stigmasterol is wellknown for its anti-inflammatory action [17], fucosterol is known for its antioxidant activity which is correlated to its anticancer potential [18]. Alpha-amyrin and tricyclo-triacontane are very well-known compounds for their anticancer activity [19,20]. ...
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Several in vitro investigations of the therapeutic characteristics of B. bulbocastanum have shown that it has cytotoxic, antifungal, and antibacterial effects. It also exhibits antioxidant and anticancer effects. When the ethyl acetate fraction of B. bulbocastanum was examined for its phytochemical composition, it was found to be rich in phenolic compounds and had significant cytotoxic effects on PC-3 cell lines. The prostate length-to-weight ratio was significantly higher in vivo in the ethyl acetate fraction-treated group. Compared to the disease control group, his-topathological examination of the ethyl acetate-treated group revealed a reduction in inflammation and malignant lesions, confirming its antiproliferative efficacy. According to serum biochemistry, acid phosphatase and PSA levels in the ethyl acetate fraction treatment group were significantly lower than those in the disease control group. When compared to the disease control group, malondialdehyde levels in the ethyl acetate fraction treatment group were likewise reduced dramatically. However, in the group treated with the ethyl acetate fraction, glutathione levels increased considerably. The ethyl acetate fraction of B. bulbocastanum may have cytotoxic and antiproliferative potential, both in vitro and in vivo.
... Anti-cancerous, anti-diabetic, antifungal, anti-osteoporotic, and anti-cholinergic; reduces blood cholesterol level [24,26] Plants 2024, 13, x FOR PEER REVIEW 3 of 22 ...
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Plants are an important source of essential bioactive compounds that not only have a beneficial role in human health and nutrition but also act as drivers for shaping gut microbiome. However, the mechanism of their functional attributes is not fully understood despite their significance. One such important plant is Crocus sativus, also known as saffron, which possesses huge medicinal, nutritional, and industrial applications like food and cosmetics. The importance of this plant is grossly attributed to its incredible bioactive constituents such as crocins, crocetin, safranal, picrocrocin, and glycosides. These bioactive compounds possess a wide range of therapeutic activities against multiple human ailments. Since a huge number of studies have revealed negative unwanted side effects of modern-day drugs, the scientific communities at the global level are investigating a large number of medicinal plants to explore natural products as the best alternatives. Taken into consideration, the available research findings indicate that saffron has a huge scope to be further explored to establish alternative natural-product-based drugs for health benefits. In this review, we are providing an update on the role of bioactive compounds of saffron as therapeutic agents (human disorders and antimicrobial activity) and its nutritional values. We also highlighted the role of omics and metabolic engineering tools for increasing the content of key saffron bioactive molecules for its mass production. Finally, pre-clinical and clinical studies seem to be necessary to establish its therapeutic potential against human diseases.
... Desmosterol exhibits a high concentration in brain tissues, particularly in regions associated with memory and cognition (Cenik et al., 2022). In contrast, fucosterol showcases potent antioxidant characteristics, acting as an effective scavenger of free radicals and reducing oxidative stress, which is linked to various diseases (Abdul et al., 2016). By neutralizing harmful reactive oxygen species, fucosterol safeguards cells and tissues from oxidative damage, contributing to overall health and well-being. ...
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The genus Asparagopsis has garnered escalating attention in the spheres of marine biology and biotechnology due to its diverse chemical composition and promising biological capabilities. This all-encompassing review is dedicated to conducting an exhaustive inquiry into the chemical identification and biological importance of Asparagopsis species. By meticulously dissecting the array of chemical compounds found in genus Asparagopsis, encompassing polysaccharides, lipids, proteins, sterols, and bromoform. We unveil their potential utility in realms such as biomedicine, biotechnology, and the conservation of the environment. Furthermore, we delve into the bioactive attributes inherent in these compounds, encompassing effects such as antioxidative, antimicrobial, and anti-inflammatory properties, as well as their conceivable role in cancer treatments. Furthermore, this review underscores the environmental pertinence of genus Asparagopsis, particularly its capacity to mitigate climate change through the generation of compounds that alleviate greenhouse gas effects. Additionally, we delve into the economic facets of this genus, spanning from its integration into food additives to its contributions in cosmetics and sustainable agriculture. This comprehensive review furnishes a multi-faceted comprehension of Asparagopsis, illuminating its chemical diversity and biological significance, thereby paving the way for further explorations into its potential contributions across a spectrum of sectors.
... HRLCMS analysis of methanol flower and seed extract of C.ternatea showed the presence of more numbers of bioactive compounds which were had different pharmacological activities. Bioactive compounds present in methanol flower extract of C.ternatea such as Adenine is used in the treatment of HIV, HBV, CMV and other virus -infected diseases [31], Quercetin is to treat anticancer, cardiovascular protection, antiinflammatory, antidiabetic, gastroprotection effects, anti-infective and inhibits gastric acid secretion and inhibits Helicobacter pylori infection [33], 6-C Galactosylluteolin had employed in therapeutic treatment for coronavirus disease (COVID-19) [34], 6-Hydroxy-2-(4-hydroxyphenyl)-5,7dimethoxy-4H-1-benzopyran-4-one and Phytosphingosine has shown Antimicrobial activity [35 & 44], Morindone is used to treat a variety of health issues including, high blood pressure, arthritis, ulcers, depression, menstrual cramps, pain relief, inflammation, burns, fever, food poisoning, intestinal worms, and joint problems [36], Formononetin has effective treatment for cancer [38], Garbogiol is used in Inhibition of α-glucosid [37], Betavulgarin has emerged as Anticancer agent against breast cancer [39], Afrormosin, Bowdichione and Pheophytin a had Anti-inflammatory properties [40, 43 & 49], Aspulvinone E, is a marine metabolite used to develop novel antiinfluenza virus agents with high efficiency and low toxicity [41], Ganoderic acid F inhibits the growth of cancer cells, anti-angiogenic and displays significant cytotoxicity against cancer cells [46], Goyaglycoside c is used as a bitter stomachic, laxative, is used as an antidiabetic, and anthelmintic for children [47], Fucosterol help to reduce blood cholesterol, blood vessel thrombosis preventive and butyrylcholinesterase inhibitory activities [48], Theophylline were used in the treatment of asthma, chronic obstructive lung diseases [50], Calpeptin suppresses the pancreatic cancer [73] and also to treat acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection, inhibit chronic inflammation, tissue damage and pulmonary fibrosis [51]. ...
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Since ancient times, plants and plant products were used against numerous diseases. In this context, Clitoria ternatea (C. ternatea) was used for the various treatments of infectious diseases as a therapeutic role containing various phytochemical, antibacterial and antioxidant properties. The methanol flower and seed extracts of C.ternatea were analysed for antibacterial activity against Helicobacter pylori (H. pylori) using the agar well diffusion method. However, the probe of the antibacterial activity in both the methanol flower and methanol seed showed more or less the same zone of inhibition at 200 µg/ml. Furthermore, antioxidant properties were analysed by DPPH (1, 1-diphenyl-2-picrylhydrazyl) radical scavenging activity and reducing power assay. Results on the DPPH assay showed better results in the methanol flower (42.79±0.0819) extract than methanol seed extract (37.41±0.0265) 200µg/ml. Likewise, the reducing assay manifested in the extract of methanol flower (0.90737±0.00375) was supremacy. Moreover the High resolution liquid 40 chromatography-mass spectrometry (HRLCMS) analysis of methanol flower and seed extract of C. ternatea contained 32 and 51 major bioactive compounds, respectively in positive and negative modes. In light of the study, the extracts of methanol flower and seed extract of C. ternatea are utilized in the mode of action against H. pylori. The methanolic flower and seed extracts authenticated the presence of extensive identified and unidentified phytochemicals in C. ternatea and through more light on the important bioactive compounds to be explored for medicinal applications in future research.
... HRLCMS analysis of methanol flower and seed extract of C.ternatea showed the presence of more numbers of bioactive compounds which were had different pharmacological activities. Bioactive compounds present in methanol flower extract of C.ternatea such as Adenine is used in the treatment of HIV, HBV, CMV and other virus -infected diseases [31], Quercetin is to treat anticancer, cardiovascular protection, antiinflammatory, antidiabetic, gastroprotection effects, anti-infective and inhibits gastric acid secretion and inhibits Helicobacter pylori infection [33], 6-C Galactosylluteolin had employed in therapeutic treatment for coronavirus disease (COVID-19) [34], 6-Hydroxy-2-(4-hydroxyphenyl)-5,7dimethoxy-4H-1-benzopyran-4-one and Phytosphingosine has shown Antimicrobial activity [35 & 44], Morindone is used to treat a variety of health issues including, high blood pressure, arthritis, ulcers, depression, menstrual cramps, pain relief, inflammation, burns, fever, food poisoning, intestinal worms, and joint problems [36], Formononetin has effective treatment for cancer [38], Garbogiol is used in Inhibition of α-glucosid [37], Betavulgarin has emerged as Anticancer agent against breast cancer [39], Afrormosin, Bowdichione and Pheophytin a had Anti-inflammatory properties [40, 43 & 49], Aspulvinone E, is a marine metabolite used to develop novel antiinfluenza virus agents with high efficiency and low toxicity [41], Ganoderic acid F inhibits the growth of cancer cells, anti-angiogenic and displays significant cytotoxicity against cancer cells [46], Goyaglycoside c is used as a bitter stomachic, laxative, is used as an antidiabetic, and anthelmintic for children [47], Fucosterol help to reduce blood cholesterol, blood vessel thrombosis preventive and butyrylcholinesterase inhibitory activities [48], Theophylline were used in the treatment of asthma, chronic obstructive lung diseases [50], Calpeptin suppresses the pancreatic cancer [73] and also to treat acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection, inhibit chronic inflammation, tissue damage and pulmonary fibrosis [51]. ...
Article
Since ancient times, plants and plant products were used against numerous diseases. In this context, Clitoria ternatea (C. ternatea) was used for the various treatments of infectious diseases as a therapeutic role containing various phytochemical, antibacterial and antioxidant properties. The methanol flower and seed extracts of C.ternatea were analysed for antibacterial activity against Helicobacter pylori (H. pylori) using the agar well diffusion method. However, the probe of the antibacterial activity in both the methanol flower and methanol seed showed more or less the same zone of inhibition at 200 µg/ml. Furthermore, antioxidant properties were analysed by DPPH (1, 1-diphenyl-2-picrylhydrazyl) radical scavenging activity and reducing power assay. Results on the DPPH assay showed better results in the methanol flower (42.79±0.0819) extract than methanol seed extract (37.41±0.0265) 200µg/ml. Likewise, the reducing assay manifested in the extract of methanol flower (0.90737±0.00375) was supremacy. Moreover the High resolution liquid 40 chromatography-mass spectrometry (HRLCMS) analysis of methanol flower and seed extract of C. ternatea contained 32 and 51 major bioactive compounds, respectively in positive and negative modes. In light of the study, the extracts of methanol flower and seed extract of C. ternatea are utilized in the mode of action against H. pylori. The methanolic flower and seed extracts authenticated the presence of extensive identified and unidentified phytochemicals in C. ternatea and through more light on the important bioactive compounds to be explored for medicinal applications in future research.
... One compound found in seaweed that has been studied is fucosterol, which is thought to affect bone regeneration. 78 Studies have investigated the use of fucosterol in osteoblast cell culture and ovariectomized female rats (an animal model of osteoporosis). Interestingly, the obtained results indicated that fucosterol increased ALP activity, mineralization, and bone density and significantly increased bone cell proliferation. ...
Article
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Novel tissue regeneration strategies are constantly being developed worldwide. Research on bone regeneration is noteworthy, as many promising new approaches have been documented with novel strategies currently under investigation. Innovative biomaterials that allow the coordinated and well-controlled repair of bone fractures and bone loss are being designed to reduce the need for autologous or allogeneic bone grafts eventually. The current engineering technologies permit the construction of synthetic, complex, biomimetic biomaterials with properties nearly as good as those of natural bone with good biocompatibility. To ensure that all these requirements meet, bioactive molecules are coupled to structural scaffolding constituents to form a final product with the desired physical, chemical, and biological properties. Bioactive molecules that have been used to promote bone regeneration include protein growth factors, peptides, amino acids, hormones, lipids, and flavonoids. Various strategies have been adapted to investigate the coupling of bioactive molecules with scaffolding materials to sustain activity and allow controlled release. The current manuscript is a thorough survey of the strategies that have been exploited for the delivery of biomolecules for bone regeneration purposes, from choosing the bioactive molecule to selecting the optimal strategy to synthesize the scaffold and assessing the advantages and disadvantages of various delivery strategies.
... The most abundant fatty acids are gamma-linolenic acid, arachidonic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), but other lipid molecules such as sterols (iso fucosterol, fucosterols, and clionasterol) and phospholipids are also important (Neto et al., 2018;Saadaoui et al., 2020). Being a structural component of the cell membrane, sterols control the fluidity of the membrane and have antioxidant, antiproliferation, antiaging, and antiinflammatory activity (Abdul et al., 2016;Hannan et al., 2020;Hwang et al., 2014;Lee et al., 2003). Marine macroalgae derive different types of fatty acids, such as glycolipids, phospholipids, triglycerides, and sterols. ...
... Δ5 Avenasterol (isofucosterol), a characteristic sterol of algae, seaweed, and diatom, was found in the four different types of MSOs by percentages ranging from 2.82 to 4.04 %. It has antidiabetic, anticancer, and antiinflammatory effects [42]. lanosta-8, 24-dien-3-one (triterpenoid) was also found in both SMLO and SMKO in a considerable percentage, especially in SMKO ( 5.44 and 14.5% respectively). ...
... Similarly α, and β-amyrin is reported to have gastroprotective, anticancer, antifungal, and hypolipidemic activity (Vázquez et al., 2012). Fucosterol, a phytosterol found in brown seaweed also exhibits anticancer, antidiabetic, antioxidant, hepatoprotective, antihyperlipidemic, antifungal, antihistaminic, anticholinergic, antiadipogenic, antiphotodamaging, anti-osteoporotic, blood cholesterolreducing, blood vessel thrombosis preventive and butyrylcholinesterase inhibitory activities (Abdul et al., 2016). Stigmasta-5, 22-dien-3-ol is reported to have antioxidant, antibacterial, anti-inflammatory, antiarthritic, antiasthma, and diuretic activity (Payum, 2017). ...
Article
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Marine macro alga are known to produce a plethora of bioactive metabolites with potential application in pharmaceutical and nutritional product development. In this study, the brown algae Sargassum wightii was collected along the coast of Kovalam, Thiruvananthapuram and subjected to in vitro analysis to determine their bioactive properties. The chloroform-methanol extract of S. wightii was utilized to screen and quantify phytochemical components. Further, the study examined the antioxidant potentials by lipid peroxidation inhibition, DPPH, and ABTS radical scavenging assays followed by an antibacterial activity. The capability of the extract to inhibit DNA damage and protein oxidation was also evaluated in vitro . Finally, the chemical characterization was attained using UV-Visible, FTIR, and GC-MS spectral data. Alkaloids, coumarins, flavonoids, phenols, and tannins, were detected in preliminary qualitative phytochemical analysis and their quantitative estimation revealed a significant concentration of these phytocomponents. The extract showed an IC50 value of 310.53 ± 0.35 µg/mL and 242.85 ± 0.377 µg/mL for DPPH and ABTS free radicals respectively. Whereas an IC50 of 205.42 ± 0.20 µg/mL was estimated for lipid peroxidation inhibition assay. A significant antimicrobial activity against four bacterial pathogens with a maximum zone of inhibition of > 40 mm was also observed against Staphylococcus aureus 1.5 µg/mL). The extract also demonstrated a high capability for concentration-dependent prevention of DNA damage and protein oxidation. The GC-MS spectral peaks confirmed the occurence of 17 active components with reported biological activities. These findings suggest that the extract of S. wightii , can be a lead compound for the development of a promising pharmaceutical product.
... Another phytosterol, fucosterol, was reported to have multiple biological activities, including anticancer activity. It was found to induce apoptosis in human promyelocytic leukemia HL-60 cells and human colon cancer HCT-116 cells [52]. Marisa et al. [53] identified several phytosterols from S. palustris leaf extract including α-tocopherol, campesterol, stigmasterol, β-sitosterol, and fucosterol to be potent antibreast cancer compounds. ...
... The brown algae contain principally fucosterol, red algae cholesterol, and green algae, a mixture of ergosterol, 28-isofucosterol, β-sitosterol, cholesterol, and poriferasterol [205]. Sterols can regulate membranes' permeability and fluidity and have antioxidant, anti-inflammatory, and antiphotodamage [206][207][208][209]. ...
Article
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Seaweeds or algae are marine autotrophic organisms. They produce nutrients (e.g., proteins, carbohydrates, etc.) essential for the survival of living organisms as they participate in biochemical processes and non-nutritive molecules (such as dietary fibers and secondary metabolites), which can improve their physiological functions. Seaweed polysaccharides, fatty acids, peptides, ter-penoids, pigments, and polyphenols have biological properties that can be used to develop food supplements and nutricosmetic products as they can act as antibacterial, antiviral, antioxidant, and anti-inflammatory compounds. This review examines the (primary and secondary) metabolites produced by algae, the most recent evidence of their effect on human health conditions, with particular attention to what concerns the skin and hair's well-being. It also evaluates the industrial potential of recovering these metabolites from biomass produced by algae used to clean wastewater. The results demonstrate that algae can be considered a natural source of bioactive molecules for well-being formulations. The primary and secondary metabolites' upcycling can be an exciting opportunity to safeguard the planet (promoting a circular economy) and, at the same time, obtain low-cost bioactive molecules for the food, cosmetic, and pharmaceutical industries from low-cost, raw, and renewable materials. Today's lack of methodologies for recovering bioactive molecules in large-scale processes limits practical realization.
... Fucosterol is generally found in brown algae and is known for its anti-inflammatory effect. It is not detected or is found in only low amounts in the seeds of some plants (Abdul, Choi, Jung, & Choi, 2016). This suggests that β-sitosterol is likely to be the main phytosterol in DM seed extracts. ...
... It caused mitochondrial membrane potential (MMP) loss in ES2 cells with an IC50 of 25.75 µg/mL versus 21.21 µg/mL in OV90 cells [56]. One study demonstrated that fucosterol (K) attenuated oxidative stress by upregulating antioxidant enzymes such as SOD and CAT by activating Nrf-2 [95]. In carcinogenesis, mitochondrial malfunction increases mitochondrial calcium, which can affect the release of apoptotic factors [56]. ...
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The process by which cancer cells evade or inhibit apoptosis is considered one of the characteristics of cancer. The ability of cancer cells to escape apoptosis contributes to tumor proliferation and promotes metastasis. The discovery of new antitumor agents is essential for cancer treatment due to the lack of selectivity of drugs and cellular resistance to anticancer agents. Several studies showed that macroalgae produce various metabolites with different biological activities among marine organisms. This review discusses multiple metabolites extracted from macroalgae and their pro-apoptotic effects through regulating apoptosis signaling pathway target molecules and the structure-activity relationship. Twenty-four promising bioactive compounds have been reported, where eight of these compounds exhibited values of maximum inhibitory concentration (IC50) of less than 7 μg/mL. Fucoxanthin was the only carotenoid reported that induced apoptosis in HeLa cells with an IC50 below 1 µg/mL. Se-PPC (a complex of proteins and selenylated polysaccharides) is the magistral compound because it is the only one with an IC50 of 2.5 µg/mL which regulates the primary proteins and critical genes of both apoptosis pathways. Therefore, this review will help provide the basis for further studies and the development of new anticancer drugs, both as single agents and adjuvants, decreasing the aggressiveness of first-line drugs and offering patients better survival and quality of life.
... Lipids in the coral holobiont are derived from algal biosynthesis (Muscatine 1990;Papina et al. 2003;Teece et al. 2011;Baumann et al. 2014), coral biosynthesis (Chen et al. 2021), heterotrophic feeding (Tolosa et al. 2011), and conversions between existing lipids in the holobiont. The tissue sterol compositions in the present study are dominated by campesterol, stigmasterol, and brassicasterol (supplementary Fig. 2), which are all phytosterols previously observed in marine algae (Abdul et al. 2016;Lee et al. 2020). Heterotrophic feeding enhances the abundance of unsaturated fatty acids in coral tissues (Imbs 2013), and the low abundance of these forms in our samples (supplementary Fig. 5 and 9) likely indicates that the corals were predominantly autotrophic. ...
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Lipids may serve as energy reserves to support coral calcification, allow acclimation to higher temperatures, and are implicated in the control of CaCO3 precipitation. Here, we report the lipid composition of the soft tissues (including host and symbionts) of 7 massive Porites spp. coral colonies (4 × P. lutea and 3 × P. murrayensis), which were cultured under different pCO2 concentrations (180, 260, 400 and 750 µatm) and at two temperatures (25 ℃ and 28 ℃), below the thermal stress threshold. We report the fatty acid methyl esters (FAME), free fatty acid (FFA) to total fatty acid content, sterol and wax ester profiles, and identify two ketones (n-alkanone) and three long chain aldehyde (n-alkanal) derivatives. Increasing seawater temperature significantly increases the contributions of FFAs to the total lipids, of C18:2 and C20:0 to the total FFA pool, of C14:0 to total FAME, and of campesterol to total sterol. The temperature increase also reduces the contributions of unusual fatty acid derivatives to total lipids, of C14:0, C15:0, C16:0 and C17:0 saturated free fatty acids to total FFAs, and of C16:0 FA to total FAME. Fatty acids are implicated in the control of membrane structure fluidity and the observed changes may promote acclimation and thermostability as temperature varies. Seawater pCO2 has no significant effect on the composition of tissue lipids with the exception that the contribution of C14:0 FA to total lipid content is significantly lower at 180 µatm compared to 260 and 750 µatm. Decreased contribution of total sterols and unusual fatty acid derivatives and increased contribution of total FFAs to total lipids are observed in the fastest calcifying coral (a P. lutea specimen) compared to the other corals, under all pCO2 and temperature conditions. Although a rapid calcifier this genotype has been shown previously to exhibit pronounced abnormal changes in skeletal morphology in response to decreased seawater pCO2. Variations in tissue lipid composition between coral genotypes may influence their resilience to future climate change.
... Capsicoside, an outlier of AD dataset isolated from Capsicum annum which belongs to the class of steroids involved in the treatment of obesity [46]. 9,12,15 Octadecatrienoic acid belongs to the class of flavonoid isolated from Portulaca oleracea reported for obesity [47]. Crocin, another AD outlier, isolated from Crocus Sativus which belongs to prenol Lipid was found to possess anti-oxidant and anti-obesity activities [48]. ...
Article
Nature plays a major role in the development of new drugs which helps in preventing and treating human diseases. Anti-obesity compound database (AOCD) contains comprehensive information on all published small molecules from natural sources with anti-obesity potential targeting pancreatic lipase (PL), appetite suppressant (AS) and adipogenesis (AD). Presently the database contains 349 compounds isolated from 307 plants, 26 marine and 16 microbial sources. Users can query the AOCD database (https://aocd.swmd.co.in/) in several ways. The database was divided into three datasets (PL, AS and AD) to perform chemoinformatic analysis using Platform for Unified Molecular Analysis (PUMA), which were analyzed based on molecular descriptors, scaffold diversity and structural fingerprint diversity. Chemoinformatics study inferred the PL dataset has the highest diversity of compounds based on the Euclidean distance on molecular properties, scaffold diversity and pairwise similarity on fingerprint diversity. This study would hasten the process of anti-obesity drug discovery.
... Another phytosterol, fucosterol, was reported to have multiple biological activities, including anticancer activity. It was found to induce apoptosis in human promyelocytic leukemia HL-60 cells and human colon cancer HCT-116 cells [52]. Marisa et al. [53] identified several phytosterols from S. palustris leaf extract including α-tocopherol, campesterol, stigmasterol, β-sitosterol, and fucosterol to be potent antibreast cancer compounds. ...
Chapter
Stenochlaena palustris (family Blechnaceae) is a fern species that occurs in the tropics and subtropics. They have been used as edible wild vegetables and folk medicine by the indigenous people in the Asian region. Phytochemical analyses revealed the presence of flavonoids, phenolics, tannins, saponins, gums, steroids, glycosides, terpenoids, and alkaloids in S. palustris. Nonetheless, the main secondary metabolites identified from the fern are kaempferol glycosides, fatty acids and phytosterols. Phytocompounds and solvent extracts derived from the fern were demonstrated to have antioxidant, antiglucosidase, cytotoxic, antimicrobial, anti-butyrylcholinesterase, anti-metalotoxic, antipyretic, and termiticidal activities. In nursing mothers, the juice of the fern stimulated breast milk production. The antioxidant and antimicrobial potentials of the fern also contributed to their applications in food, cosmetics, and food packaging material. Thus, current literature indicates that S. palustris is a promising source of phytochemicals with potential applications in health promotion, food, and cosmetics, which deserves future research attention. This review presents an overview of the current knowledge pertaining to the biological activities of phytocompounds and extracts of S. palustris.
... Seaweeds are mainly used for direct human consumption in Asian countries, they have been used as a feed ingredient more recently, as well as in other industrial applications (i.e., bioenergy). The capability of seaweed to contribute wellbeing and health in livestock is mediated by bioactive compounds that are synthesized by a few seaweed species (8)(9)(10)(11). Some of these bioactive compounds [e.g., bromoform in red species and polyphenols or phlorotannins in brown species (12)(13)(14)] are associated with a reduction in methanogenesis in the rumen. Many seaweed species have been evaluated through in vitro studies, and some have been shown to reduce CH 4 production in the rumen (13,(15)(16)(17). ...
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A series of in vitro batch culture incubations were carried out to investigate changes in rumen fermentation characteristics, methane (CH4) production, and microbial composition in response to supplementation with five different red seaweed species (Amphiroa anceps, AANC; Asparagopsis taxiformis, ATAX; Chondracanthus tenellus, CTEN; Grateloupia elliptica, GELL; and Gracilaria parvispora, GPAR). Prior to the incubations, the total flavonoid and polyphenol content of the red seaweed extracts was quantified. The incubated substrate consisted of timothy hay and corn grain [60:40 dry matter (DM) basis]. Treatments were substrate mixtures without seaweed extract (CON) or substrate mixtures supplemented with 0.25 mg/mL of red seaweed extract. Samples were incubated for 6, 12, 24, 36, and 48 h. Each sample was incubated in triplicates in three separate runs. In vitro DM degradability, fermentation parameters (i.e., pH, volatile fatty acids, and ammonia nitrogen), total gas production, and CH4 production were analyzed for all time points. Microbial composition was analyzed using 16S rRNA amplicon sequencing after 24 h of incubation. The highest CH4 reduction (mL/g DM, mL/g digested DM, and % of total gas production) was observed in ATAX (51.3, 50.1, and 51.5%, respectively, compared to CON; P < 0.001) after 12 h of incubation. The other red seaweed extracts reduced the CH4 production (mL/g DM; P < 0.001) in the range of 4.6–35.0% compared to CON after 24 h of incubation. After 24 h of incubation, supplementation with red seaweed extracts tended to increase the molar proportion of propionate (P = 0.057) and decreased the acetate to propionate ratio (P = 0.033) compared to the CON. Abundances of the genus Methanobrevibacter and total methanogens were reduced (P = 0.050 and P = 0.016) by red seaweed extract supplementation. The linear discriminant analysis effect size (P < 0.05, LDA ≥ 2.0) showed that UG Succinivibrionaceae, Anaeroplasma, and UG Ruminococcaceae, which are associated with higher propionate production, starch degradation, and amylase activity were relatively more abundant in red seaweed extracts than in the CON. Our results suggest that supplementation with red seaweed extracts altered the microbiota, leading to the acceleration of propionate production and reduction in CH4 production.
... Prior studies have reported that for drug research development, algal sources were found to possess novel metabolites (Davis & Vasanthi, 2015). Recent advancements also highlighted that fucosterol belongs to the class of brown seaweeds and were found to exhibit several therapeutic activities such as antihistaminic, antihyperlipidemic, antidiabetic, anticancer, antiadipogenic, antioxidant, antifungal, antihistaminic, anticholinergic, antiadipogenic, blood cholesterol reduction, and anti-osteoporotic (Abdul et al., 2016). Furthermore, the tetraprenyltoluquinols class of compounds isolated from brown algal species Cystophora fibrosa showed anti-obesity activity (Prabhakar et al., 2022). ...
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Background Over the past three decades, with substantial changes in lifestyle, the tendency to gain weight has increased, which is resulting in significant consequences affecting an individual’s well-being. The fat mass and obesity-associated (FTO) gene is involved in food intake and energy expenditure and plays a crucial role in regulating homeostasis and controlling energy expenditure by hindering signals that generate from the brain. Edible seaweeds have been shown to enhance satiety owing to their health benefits. Methods Extensive screening of plant-derived anti-obesity compounds and seaweed compounds was conducted and validated for ADME properties and toxicity prediction. Further, the top ranked compounds were docked against the FTO protein to identify potential inhibitors and were subjected to molecular dynamic simulation studies to understand the binding stability of ligand protein complex. Finally, MM/PBSA studies were performed to calculate the binding free energy of the protein-ligand complexes. Results Through the virtual screening of 1,210 compounds, 443 compounds showed good docking scores less than −7.00 kcal/mol. Drug likeness screenings of 443 compounds showed that only 369 compounds were in accordance with these properties. Further toxicity prediction resulted in 30 non-toxic compounds. Molecular docking studies revealed four top ranked marine compounds. Finally, RL074 (2-hydroxyluzofuranone B) and RL442 (10-acetoxyangasiol) from marine red alga Laurencia sp showed good stability from molecular dynamic simulation studies. MM/PBSA results revealed that BT012 (24ε-hydroperoxy-6β-hydroxy-24-ethylcholesta-4,-28(29)-dien-3-one), an oxygenated fucosterol from brown alga Turbinaria conoides , possessed higher binding energy. Hence, with all the data obtained it could be concluded that three seaweed compounds, BT012, RL074 and RL442, may act as a potential anti-obesity lead compound in targeting FTO.
... Furthermore, sterols have been found in brown seaweed and have been associated with antidepressant and lipid-lowering properties (Ruqqia et al. 2020;Zhao et al. 2016). In particular, fucosterol, which is the characteristic sterol of all brown seaweed phylum, has antioxidant, anti-diabetic anti-inflammatory and other biological activities (Abdul et al. 2016;Jung et al. 2016Jung et al. , 2014aJung et al. , 2014bLee et al. 2003;Sun et al. 2015;Yoo et al. 2012). ...
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Seaweed has emerged as one of the most promising resources due to its remarkable adaptability, short development period, and resource sustainability. It is an effective breakthrough to alleviate future resource crises. Algal resources have reached a high stage of growth in the past years due to the increased output and demand for seaweed worldwide. Several aspects global seaweed farming production and processing over the last 20 years are reviewed, such as the latest situation and approaches of seaweed farming. Research progress and production trend of various seaweed application are discussed. Besides, the challenges faced by seaweed farming and processing are also analyzed, and the related countermeasures are proposed, which can provide advice for seaweed farming and processing. The primary products, extraction and application, or waste utilization of seaweed would bring greater benefits with the continuous development and improvement of applications in various fields. Graphical Abstract
... The endophytic fungus Aspergillus wentii EN-48 isolated from the fresh tissue of Sargassum that are commonly consumed as food and traditional medicine in Asian countries [22]. Sargassum also presents antipyretic, analgesic, antimicrobial, antiedema, antioxidant, antitumor, anti-inflammatory, and hepatoprotective activities [23,24]. Moreover, Sargassum is a source for high-value secondary metabolites with potential benefits for human health, such as fucoidans and alginates that have received great attention in the health industry. ...
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Wentilactone A (WA) is a tetranorditerpenoid isolated from marine algae. We previously found that WA inhibited cancer cell proliferation with little toxicity. In this study, we show that high expression of extracellular matrix protein-1 (ECM1) promotes cancer cell cisplatin resistance, and the secreted ECM1 activates normal fibroblasts (NFs) to transform cells with characteristics of cancer-associated fibroblasts (CAFs). Transcription of the ECM1 gene is regulated largely by NF-κB through EP881C/T-EP266C binding sites. WA supresses the phosphorylation of NF-κB through inhibition of the upstream IKK/IκB phoshorylation to block the expression of ECM1, which reverses the cisplatin-induced activation of NF-κB/ECM1. On the contrary, cisplatin facilitates phosphorylation of NF-κB to enhance the expression of ECM1. These results highlight ECM1 as a potential target for treatment of cisplatin-resistant cancers associated with the ECM1 activated signaling. In addition, WA reverses cisplatin resistance by targeting both tumor cells and the tumor microenvironment through IKK/IκB/NF-κB signaling to reduce the expression of the ECM1 protein.
... The sterol exhibits several biological benefits including anti-tumor, anti-microbial, antidiabetic, antioxidant, anti-inflammatory and anti-thrombotic effects. Moreover, they have been correlated with protection of liver, neurotransmitter regulation as well as reduction of blood cholesterol, osteoporosis and hyperlipidemia [24] . Brown macroalgae amino acids have also demonstrated significant antipathogenic actions. ...
Chapter
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Brown marine macroalgae are one of the predominant sources of bioactive compounds possessing a variety of functional benefits. These biochemicals generally belong to polyphenols, carotenoids and algal polysaccharides. The compounds are produced in marine macroalgae for their protection and survival, when subjected to highly adverse conditions such as environmental fluctuations, predation and stress. Their unique molecular structures equip them with immense potential to act as free radical scavengers, anti-inflammatory mediators, anti-microbials, signal transducers as well as texture modifiers among several other benefits. Polyphenols including phlorotannins, phenolic acids, flavonoids and halogenated phenolic compounds have displayed appreciable anti-oxidant and antipathogenic potential. Carotenoids, although chiefly involved in photosynthesis have also manifested capacity to reduce free radical mediated effects. Algal polysaccharides are valuable components owing to their rheological as well as anti-radical benefits. Due to these properties, the secondary metabolites produced by brown marine macroalgae are popular candidates in the pharmaceutical and food industries. Elevation of ROS, inflammation, microbial distress and altered signalling are some of the key abnormalities associated with common ailments. Therefore, utilization of these compounds from natural sources may not only help in current therapeutics but also aid in development of novel strategies as nutraceuticals.
... Sterols and some of their derivatives have been implicated in the reduction of cardiovascular diseases due to the reduction of cholesterol in the blood, thrombosis inhibitory activities, therapeutic values for the treatment of hypercholesterolemia, they have anti-inflammatory effects, they are essential precursors of some vitamins, important structural components of the cell membrane and with important functions in regulating the fluidity and permeability of the membrane (Hernandez-Ledesma and Herrero 2014; Hamed et al. 2015). Fucosterol exhibits several biological therapies, including anti-cancer, anti-diabetic, hepatoprotective, anti-fungal, and anti-photogenic (Abdul et al. 2016). ...
Article
Background:The most commonly used part of Ricinus communis is seeds known as Castor Oil. In the Traditional system of Indian Medicine, it is known as Gandharvahasta or Castor Oil, and the abundance of natural compounds in castor oil possess healing health benefits that are widely used in Traditional system of Indian Medicine. Objectives: A comprehensive review has been made through the Classical Text of Indian System of medicine. Views of their critics as well as contemporaries were also taken into consideration for compilation of Castor Oil formulations. Material & Methods: The journals, modern books and internet were also screened during the review attempt on Castor Oil and their formulations. Ricinus communis is found throughout India and has been used medicinally for centuries. Result: Among the thousands of medicinal plants, Ricinus communis or castor plant is a widely used and powerful medicinal plant. More scientifically based research on its property and various modes of administration must be conducted. A systematic review of Castor Oil provides details on its use, dosage, adverse reactions, and so on. In the current review, A thorough examination of the evidencebased activity of the formulations mentioned in Bhaishajya Ratnavali reveals that these formulations can be used effectively in all diseased conditions. Conclusion: This knowledge may be useful in developing safe and dependable therapeutic conditions for all types of diseases, which are currently unavailable on the herbal drug market.
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Plants and animals are potential sources of food, particularly lipids. They are sources of nutrients for humans, and are used in various applications in food industries. Foods whose lipids consumed, have benefits for animal and human health. Sterols are among the compounds essential to the well-being of living beings. Phytosterols are derived from plants and algae, and zoosterols from animals dominated by cholesterol. Cholesterol is found in small quantities in some plant lipids. Also, cholesterol is produced by herbivorous insects by metabolizing phytosterols. Oilseeds and vegetable oils contain sterols and are the richest natural sources of phytosterols. Vegetables and fruit also contain small quantities. These compounds play an undeniable role in our diet. Foods, particularly vegetable oils, when produced, preserved and used according to established pre scriptions, help to ensure consumer health and prevent certain pathologies. Sterols, and in particular phytosterols, play a number of roles in the pharmaceutical field (therapeutic steroids), nutrition (anti-cholesterol, anti-cancer properties). These natural molecules with their nutritional and therapeutic properties have a positive impact on human and animal health, and possibly on vegetative growth (development cycle of plants). The same is true for cholesterol, which has multiple functions in humans and animals. Also, a diet based on plants or their by-products with positive effects on human and animal health is closely in line with the objectives of the ’One health approach’. Indeed, sterols can have adverse effects on health when established standards are not respected. As a result, the health benefits of sterols (cholesterol and phytosterols) require particular attention, given their contribution to the public health problems facing our countries. The aim of the present research is to highlight the health benefits of cholesterol and phytosterols for living organisms, particularly humans, and their contribution to the One Health approach.
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In the present study, we investigated the anti-diabetic potential of fucosterol by evaluating the ability of this compound to inhibit rat lens aldose reductase (RLAR), human recombinant aldose reductase (HRAR), protein tyrosine phosphatase 1B (PTP1B), and α-glucosidase. Fucosterol displayed moderate inhibitory activity against RLAR, HRAR, and PTP1B. However, it showed weak or no activity against AGE formation and α-glucosidase. In addition, our kinetic study revealed that fucosterol showed a mixed type inhibition against RLAR and HRAR, while it noncompetitively inhibited PTP1B. Since fucosterol inhibited aldose reductase (AR), it holds great promise for use in the treatment of diabetic complications. Therefore, we predicted the 3D structure of AR in rat and human using the Autodock program to simulate binding between AR and fucosterol and evaluate the binding site-directed inhibition of AR by fucosterol. Results of the docking simulations of fucosterol demonstrated negative binding energies (-8.2 kcal/mol for RLAR and -8.5 kcal/mol for HRAR), which indicated a higher affinity and tighter binding capacity of fucosterol for the active site of the enzyme. In particular, the hydrophobic ring system and the aliphatic side chain of fucosterol were found to be tightly bound in a specificity pocket through apolar amino acid residues on AR, while the anion binding site on AR interacts with the 3-hydroxyl group and the double bond on the side chain of fucosterol. The results of the present study clearly demonstrated the potential of using fucosterol for the management and treatment of diabetes and diabetes-associated complications.
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Fucosterol, a sterol that is abundant in marine algae, has hypocholesterolemic activity, but the mechanism underlying its effect is not clearly understood. Since data suggest that fucosterol can increase plasma high-density lipoprotein concentrations, we investigated whether it could activate liver X receptors (LXRs), critical transcription factors in reverse cholesterol transport. Fucosterol dose-dependently stimulated the transcriptional activity of both LXR-α and LXR-β in a reporter gene assay, responses that were attenuated by the LXR antagonist As(2)O(3). Fucosterol also activated coactivator recruitment in cell-free time-resolved fluorescence resonance energy transfer analysis. In THP-1-derived macrophages, it induced the transcriptional activation of ABCA1, ABCG1, and apoE, key genes in reverse cholesterol transport, and thereby significantly increased the efflux of cholesterol. Fucosterol also regulated intestinal NPC1L1 and ABCA1 in Caco-2 cells. Notably, fucosterol did not induce cellular triglyceride accumulation in HepG2 cells, primarily due to its upregulation of Insig-2a, which delays nuclear translocation of SREBP-1c, a key hepatic lipogenic transcription factor. These results suggest that fucosterol is a dual-LXR agonist that regulates the expression of key genes in cholesterol homeostasis in multiple cell lines without inducing hepatic triglyceride accumulation.
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Marine algae produce different secondary metabolites with a wide range of biological activities. Many studies have been achieved on the screening of biological effects of marine organisms and a lot of active compounds were isolated and characterized. In an attempt to find cytotoxic compound of hexane fraction, isolation, identification, and cytotoxicity of active compound of this fraction were performed. In this study, total methanolic (70%) extract and partition fractions of hexane, chloroform (CHCl(3)), ethyl acetate (EtOAc), and MeOH-H(2)O of Sargassum angustifolium, Chondria dasyphylla, and Ulva flexuosa, collected from coastlines of the Persian Gulf in south of Iran, were studied against colon carcinoma (HT-29), colorectal adenocarcinoma (Caco-2), breast ductal carcinoma (T47D), and Swiss mouse embryo fibroblast (NIH 3T3) cell lines by MTT assay. IC(50) (median growth inhibitory concentration) values were calculated by Sigmaplot (10) software. Hexane fraction of Chondria dasyphylla (IC(50) 82.26 ± 4.09 μg/ml) and MeOH-H(2)O fraction of Ulva flexuosa (IC(50) 116.92 ± 8.58 μg/ml) showed cytotoxic activity against proliferation of T47D cells. Hexane fraction of Sargassum angustifolium was also observed for cytotoxicity against T47D and HT-29 cell lines (IC(50) 166.42 ± 26.7 and 190.24 ± 52.8 μg/ml), respectively. An investigation of a component from the hexane fraction of Sargassum angustifolium yielded a steroidal metabolite, fucosterol, with cytotoxicity in T47D and HT29 (IC(50) 27.94 ± 9.3 and 70.41 ± 7.5 μg/ml). These results indicated that fucosterol, the most abundant phytosterol in brown algae, is responsible for cytotoxic effect of this extract against breast and colon carcinoma cell lines.
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Considerable evidence implicates oxidative stress in the pathophysiology of many complications of human pregnancy, and this topic has now become a major focus of both clinical and basic science research. Oxidative stress arises when the production of reactive oxygen species overwhelms the intrinsic anti-oxidant defences. Reactive oxygen species play important roles as second messengers in many intracellular signalling cascades aimed at maintaining the cell in homeostasis with its immediate environment. At higher levels, they can cause indiscriminate damage to biological molecules, leading to loss of function and even cell death. In this chapter, we will review how reactive oxygen species are generated and detoxified in the human placenta, and what roles they may play at homeostatic concentrations. We will then consider their involvement in normal placental development, and in complications ranging from miscarriage to pre-eclampsia and premature rupture of the membranes.
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The purpose of this study is to investigate the effect of fucosterol on the induction of apoptosis and the molecular mechanism involved in Human promyelocytic leukemia HL-60 Cells. HL-60 Cells were treated with different concentrations of fucosterol at different time. MTT method was used to study fucosterol anti-tumor activity. Morphology observation was performed to determine the effects of fucosterol on apoptosis of HL-60 cells. Flow cytometry (FCM) was used to detect the cell cycle. Laser scanning confocal microscope (LSCM) was used to analyze the expressions of Fas, FasL, Fadd and Caspase-8. Caspase activity kits were used to determine the activity of Caspase-8 and Caspase -3. The results showed fucosterol could inhibit the growth of HL-60 cells, and the apoptosis morphology for 48 h treatment was obvious, which showed cell protuberance, cytoplasm concentrated and apoptotic body. Fucosterol treatment for 24 h increased the protein expression of Fas, FasL, Fadd and Caspase-8. It also showed that the activity of Caspase-3 and Caspase-8 has increased significantly. In conclusion, Fucosterol could induce HL-60 cells apoptosis via death receptor pathway.
Article
Fucosterol is the primary sterol found in brown algae. Recently, considerable interest has been generated regarding fucosterol due to its potential antioxidant, anti-inflammatory and antidiabetic effects. The aim of this study was to investigate the protective effects of fucosterol on tert-butyl hydroperoxide (t-BHP)- and tacrine-induced oxidative stress in HepG2 cells. Fucosterol by itself exhibited no cytotoxicity at concentrations below 100 μm by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. The increased intracellular reactive oxygen species (ROS) and decreased glutathione levels observed in t-BHP- and tacrine-treated HepG2 cells were ameliorated by fucosterol pretreatment, indicating that the protective effects of fucosterol are mediated by the induction of cellular defence mechanisms against oxidative stress. Moreover, elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in tacrine-treated mice were significantly reduced after oral administration of fucosterol. The hepatoprotective effects of fucosterol may occur via an increase in the hepatic level of glutathione and a decrease in ROS production, thereby preventing hepatic damage and the resultant increases in ALT and AST activity. These results suggest that fucosterol may be an effective hepatoprotective agent that could be useful for preventive therapies against oxidative stress-related hepatotoxicity. © 2015 Royal Pharmaceutical Society.
Article
58,050 patients entering 1086 hospitals up to 24 h (median 8 h) after the onset of suspected acute myocardial infarction (MI) with no clear contraindications to the study treatments (in particular, no cardiogenic shock or persistent severe hypotension) were randomised in a "2 x 2 x 2 factorial" study. The treatment comparisons were: (i) 1 month of oral captopril (6.25 mg initial dose titrated up to 50 mg twice daily) versus matching placebo; (ii) 1 month of oral controlled-release mononitrate (30 mg initial dose titrated up to 60 mg once daily) versus matching placebo; and (iii) 24 h of intravenous magnesium sulphate (8 mmol initial bolus followed by 72 mmol) versus open control. There were no significant "interactions" between the effects of these three treatments, and the results for each are based on the randomised comparison of about 29,000 active versus 29,000 control allocated patients. Captopril There was a significant 7% (SD 3) proportional reduction in 5-week mortality (2088 [7.19%] captopril-allocated deaths vs 2231 [7.69%] placebo; 2p = 0.02), which corresponds to an absolute difference of 4.9 SD 2.2 fewer deaths per 1000 patients treated for 1 month. The absolute benefits appeared to be larger (perhaps about 10 fewer deaths per 1000) in certain higher-risk groups, such as those presenting with a history of previous MI or with heart failure. The survival advantage appeared to be maintained in the longer term (5.4 [SD 2.8] fewer deaths per 1000 at 12 months). Captopril was associated with an increase of 52 (SD 2) patients per 1000 in hypotension considered severe enough to require termination of study treatment, of 5 (SD 2) per 1000 in reported cardiogenic shock, and of 5 (SD 1) per 1000 in some degree of renal dysfunction. It produced no excess of deaths on days 0-1, even among patients with low blood pressure at entry. Mononitrate There was no significant reduction in 5-week mortality, either overall (2129 [7.34%] mononitrate-allocated deaths vs 2190 [7.54%] placebo) or in any subgroup examined (including those receiving short-term non-study intravenous or oral nitrates at entry). Further follow-up did not indicate any later survival advantage. The only significant side-effect of the mononitrate regimen studied was an increase of 15 (SD 2) per 1000 in hypotension. Those allocated active treatment had somewhat fewer deaths on days 0-1, which is reassuring a bout the safety of using nitrates early in acute MI.(ABSTRACT TRUNCATED AT 400 WORDS)
Article
Hepatoprotective effects of Monascus pilosus mycelial ethanol extract (MPME) were examined in high-fat diet induced-obese rats. The rats were randomly divided into 2 groups; normal control (NC) and a high-fat and high cholesterol diet group (HFC). The HFC diet group was fed a 5L79 diet supplemented with 15% lard and 1% cholesterol for 3 weeks for induction of obesity. And then, the rats were divided into 4 groups (n=5); the NC, a HFC diet obesity control group (HF), 0.5% MPME supplemented HFC diet group (MPM), and 2% conjugated linoleic acid (CLA) supplemented HFC diet group for 7 weeks. Whereas the daily weight gain of NC and HFC groups were 3.48 g and 4.48 g, respectively, those of MPM and CLA were 3.09 g and 4.38 g, respectively. Furthermore, activity of serum alanine and aspartic aminotransferase in HF was markedly higher than those of NC group, but, the activity in MPM and CLA was significantly lower than HF. Hepatic reduced glutathione content in MPM and CLA was higher than HF. On the contrary, hepatic lipid peroxide content in MPM and CLA was significantly lower than HF. In conclusion, although the precise mechanisms of the hepatoprotective effects of the MPME in this study are unknown, our study provides experimental evidence that MPME may prevent obesity and hepatic damage by high-fat and high cholesterol diet via inhibition of lipid absorption and induction of reactive oxygen spices scavenging enzyme such as superoxide dismutase.
Article
The anti-hyperlipidemic effects of dietary supplementation with sea tangle Laminaria japonica were investigated using an animal model in which normal rats were fed either sea tangle, sea tangle ethanol extract (EE-ST) and sea tangle extracted residue (ER-ST). Total lipid and triglyceride levels in the serum were significantly (P < 0.05) reduced in rats fed ER-ST at a dose of 200 mg/kg body weight when compared to hyperlipidemic control rats. Significant decreases in serum total cholesterol and low density lipoprotein-cholesterol levels also occurred in rats fed ER-ST at 200 mg/kg body weight. In addition, the atherosclerosis index and superoxide dismutase in blood lipids were significantly (P < 0.05) lowered in rats fed ER-ST at 200 mg/kg body weight as compared to control rats. In conclusion, sea tangle and ER-ST exhibited beneficial anti-hyperlipidemic and anti-arteriosclerosis effects.
Article
ScopeThe aim of this study was to investigate the bone regenerative effects of fucosterol in estrogen-deficient ovariectomized (OVX) rats. Methods and resultsBone regeneration was assessed in fucosterol-treated MG63 cells in vitro via assays for osteoblast proliferation, alkaline phosphatase, and osteoclast differentiation. Osteoblast proliferation rates, alkaline phosphatase activity, and mineralization were increased in the fucosterol-treated group. Moreover, differentiation of osteoclasts was decreased in the fucosterol-treated group. In the in vivo assay, female rats were OVX. Twelve weeks after ovariectomy, rats were divided into seven groups, each oral administrate everyday for 7 weeks. The bone mineral density of femoral bones was higher in fucosterol groups than in OVX control, and body weight was lower in fucosterol groups. Among bone-quality parameters, bone volume/total volume increased and trabecular separation decreased in fucosterol groups relative to the OVX control. Bone formation and resorption were evaluated using the serum biomarkers osteocalcin and CTx. Fucosterol tripled the level of serum osteocalcin relative to the OVX group and reduced the serum level of CTx. Conclusion These results suggest that fucosterol has the dual potentials to activate osteoblasts to stimulate bone formation and suppress differentiation of osteoclasts so as to reduce bone resorption.
Article
Four fucosterol derivatives were isolated from the ethyl acetate fraction of Hizikia fusiformis. The chemical structures of the sterols were elucidated as fucosterol (1), a mixture of 24R,28R- and 24S,28R-epoxy-24-ethylcholesterol at the ratio of 3 to 2 (2), and 24R-saringosterol (3), all of which exhibited proliferation activity on MG63 cells.
Article
In this study, we investigated the effect of fucosterol on HL-60 and the molecular mechanism. HL-60 Cells were treated with fucosterol, and 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) method was used to study fucosterol anti-tumor activity. Morphology of HL-60 cells was observed. Flow cytometry (FCM) was employed to detect the cell cycle. Laser scanning confocal microscope (LSCM) was used to analyze mitochondrial membrane potential (MMP) and the expressions of Fas, FasL, Fadd and Caspase-8. Western blot was performed to analyze the expressions of Cyt-C, Pro-Caspase-9 and Pro-Caspase-3. Caspase activity kits were used to determine the activity of Caspase-9, Caspase-8 and Caspase-3. The results showed fucosterol could inhibit the growth of HL-60 cells, and the cell cycle was arrested at G2/M phase. HL-60 cells showed obvious apoptosis morphology. After being treated with fucosterol for 24 h, HL-60 cells decreased MMP, induced Cyt-C release and Caspase-9, Caspase-3 activation. Fucosterol also increased the protein expression of Fas, FasL, Fadd and Caspase-8. Moreover, the activity of Caspase-9, Caspase-8 and Caspase-3 was increased significantly. In conclusion, Fucosterol can induce HL-60 cells apoptosis, suggesting that it may be a potent agent for cancer prevention and treatment.
Article
Fucosterol is a sterol metabolite of brown algae and regulates genes involved with cholesterol homeostasis. As a part of our continuous search for anti-obesity agents from natural marine sources, the anti-adipogenic activities of Ecklonia stolonifera and its sterol, fucosterol, were evaluated for the inhibition of adipocyte differentiation and lipid formation. Oil Red O staining was used to evaluate triglyceride contents in 3T3-L1 pre-adipocytes primed by differentiation medium (DM) I and DM II. The methanolic extract of E. stolonifera showed strong anti-adipogenic activity, and was thus fractionated with several solvents. Among the tested fractions, the dichloromethane (CH2Cl2) fraction was found to be the most active fraction, with significant inhibition (40.5 %) of intracellular lipid accumulation at a non-toxic concentration, followed by the ethyl acetate fraction (30.2 %) at the same concentration, while the n-butanol and water fractions did not show inhibitory activity within the tested concentrations. The strong anti-adipogenic CH2Cl2-soluble fraction was further purified by a repeated chromatography to yield fucosterol. Fucosterol reduced lipid contents in a concentration-dependent manner without showing any cytotoxicity. Fucosterol treatment also yielded a decrease in the expression of the adipocyte marker proteins peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) in a concentration-dependent manner. Taken together, these results suggest that fucosterol inhibits expression of PPARγ and C/EBPα, resulting in a decrease of lipid accumulation in 3T3-L1 pre-adipocytes, indicating that the potential use of E. stolonifera and its bioactive fucosterol as an anti-obesity agent.
Article
All eukaryotes universally contain large amounts (20-30%) of higher sterols in their plasma membranes. It remains a mystery why different eukaryotic kingdoms have chosen different higher sterols for their membrane reinforcement, such as cholesterol in animals, ergosterol in fungi, phytosterols in plants, and e.g. desmosterol and fucosterol in algae. We have used a range of biophysical techniques, including calorimetry, fluorescence microscopy, atomic-force microscopy, and vesicle-fluctuation analysis, to assess the various physical effects of fucosterol on lipid membranes. Fucosterol and desmosterol induce acyl-chain order in liquid membranes, but less effectively than cholesterol in the order: cholesterol > desmosterol > fucosterol, reflecting the different molecular structure of the sterols. Fucosterol is much poorer that cholesterol to mechanically stiffen membranes. Both fucosterol and desmosterol are found to support liquid-ordered membrane phases and induce coexistence between liquid-ordered and liquid-disordered domains, a necessary requirement for forming small-scale domain structures which are believed to be important for membrane function.