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Elevated plasma low-density lipoprotein cholesterol (LDL-C) is associated with an increased risk for atherosclerosis and development of cardiovascular disease. An elevated plasma LDL-C concentration is the result of enhanced C synthesis, C absorption, and/or altered C homeostasis. Plasma LDL-C lowering can be achieved using pharmaceutical means. Statin therapy inhibits endogenous C synthesis and leads to a mean 40% LDL-C reduction. Ezetimibe inhibits C absorption and achieves an average 20% LDL-C reduction with a 10 mg daily intake. Phytosterol therapy is established by dietary supplements enriched in phytosterols and/or phytostanols. A dosage of 2 to 3 g a day reduces C absorption and leads to an average 10% LDL-C reduction. This dosage expresses a 10-fold increased daily intake for phytosterols or a 100-fold increased intake of phytostanols. Phytosterol- and -stanol-enriched dietary supplements are freely available in the supermarket. The majority of consumers may be healthy subjects with a plasma LDL-C in the normal range. Scientific evidence reveals that increased phytosterol intake may be associated with the development of atherosclerosis. The degree of increased risk is dependent on the patient's genetic polymorphisms in NPC1L1 and ABCG5/G8 transport proteins as well as on the established risk reduction due to LDL-C lowering. Subjects with a normal or only slightly elevated LDL-C have only minimal LDL-C lowering and lack the compensation for the potential increased risk for atherosclerosis by phytosterols. [ABSTRACT FROM AUTHOR]

Stinging nettle (Urtica dioica) is an herbaceous perennial plant native to Eurasia, wildly distributed throughout the temperate parts of the world. Although generally considered as a weed due to its fast growth and invasive capacity, stinging nettle is well suited to cultivation and is currently experiencing a revival as a beneficial crop due to its numerous potential applications. This interest reflects in an increasing number of scientific articles related to nettle in the last years. However, reports mostly focus on the aerial parts of the plant. Roots are rich in numerous phytochemicals such as phytosterols, lignans, coumarins, sugars, and lectins. By compiling the most relevant publications, the aim of this review is to gather the current knowledge about nettle roots, such as root system functioning, biochemical composition, and related functional activities. A special emphasis is placed on lectins (or UDA for Urtica dioica agglutinin) due to their functional activities. This review highlights the potential of nettle root as a source of biomolecules. Gaps of knowledge and possible future directions for nettle root research, production, and uses are discussed. [ABSTRACT FROM AUTHOR]

ABSTRACT: Background: To evaluate the efficacy of alternative medications such as Ayurveda, Sidha, and Unani, the application of advanced analytical tools is essential. Aim: In this study, the Ayurvedic oil Balaswagandhadi tailam, which is prescribed for treating fever, muscle weakness, bone and joint issues, muscle wasting, arthritic pain, neuralgia, and paralysis. Methods: The presence of active component was analyzed using gas chromatography–mass spectrometry (GC-MS) following a prescribed protocol. Results: The GC-MS study disclosed the presence of several essential bioactive compounds, including trans-2-methyl-4-n-pentylthiane, S, S-dioxide, chloroacetic acid, tetradecyl ester, 1,2-benzenedicarboxylic acid, bis(2-methylpropyl) ester, methyl 12,15-octadecadienoate, 11-octadecenoic acid, methyl ester, cis-10-heptadecenoic acid, tetradecanedioic acid, 15-hydroxypentadecanoic acid, octadecanoic acid, levo-menthoxyacetic acid, β-eudesmol trimethylsilyl ether, 1-heptatriacotanol, vitamin E, campesterol, and γ-sitosterol. Conclusion: The compounds identified are known for their various medicinal properties, potentially contributing to the therapeutic effects of Balaswagandhadi tailam. Further research is warranted to explore these findings. [ABSTRACT FROM AUTHOR]

Water deficit and heat are the primary abiotic stresses affecting plants. We conducted in vitro experiments to investigate how citron watermelon seedlings respond to water deficit and heat, focusing on growth, water status, reserve mobilization, hydrolase activity, and metabolite partitioning, including non-structural carbohydrate availability, during the vulnerable stage of seedling establishment crucial for crop production. To reveal the involvement of phytosterols (stigmasterol, sitosterol, and campesterol) in combined stress tolerance, four citron watermelon genotypes were investigated under varying osmotic potential [−0.05 MPa, −0.09 MPa and −0.19 MPa] and temperature (26 °C and 38 °C). Phytosterols were analyzed by gas chromatography–mass spectrometry (GC–MS). Seedlings subjected to osmotic stress from polyethylene glycol (PEG) exhibited reduced growth, linked to relative water content (RWC) changes, delayed starch mobilization in cotyle-dons, and decreased non-structural carbohydrate availability in roots. High temperature retarded the photosynthetic apparatus’s establishment and compromised photosynthetic pigment activity and dry matter production. The results suggest that inherent stress tolerance in citron watermelon is characterized by the increased accumulation of lipids, mainly sterols, especially in heat/drought-stressed plants. This study provides valuable information about the metabolic response of citron watermelon to combined stress and metabolites identified, which will encourage further study in transcriptome and proteomics to improve drought tolerance.

Water deficit and heat are the primary abiotic stresses affecting plants. We conducted in vitro experiments to investigate how citron watermelon seedlings respond to water deficit and heat, focusing on growth, water status, reserve mobilization, hydrolase activity, and metabolite partitioning, including non-structural carbohydrate availability, during the vulnerable stage of seedling establishment crucial for crop production. To reveal the involvement of phytosterols (stigmasterol, sitosterol, and campesterol) in combined stress tolerance, four citron watermelon genotypes were investigated under varying osmotic potential [−0.05 MPa, −0.09 MPa and −0.19 MPa] and temperature (26 °C and 38 °C). Phytosterols were analyzed by gas chromatography–mass spectrometry (GC–MS). Seedlings subjected to osmotic stress from polyethylene glycol (PEG) exhibited reduced growth, linked to relative water content (RWC) changes, delayed starch mobilization in cotyle-dons, and decreased non-structural carbohydrate availability in roots. High temperature retarded the photosynthetic apparatus's establishment and compromised photosynthetic pigment activity and dry matter production. The results suggest that inherent stress tolerance in citron watermelon is characterized by the increased accumulation of lipids, mainly sterols, especially in heat/drought-stressed plants. This study provides valuable information about the metabolic response of citron watermelon to combined stress and metabolites identified, which will encourage further study in transcriptome and proteomics to improve drought tolerance. [ABSTRACT FROM AUTHOR]

Stinging nettle (Urtica dioica) is an herbaceous perennial plant native to Eurasia, wildly distributed throughout the temperate parts of the world. Although generally considered as a weed due to its fast growth and invasive capacity, stinging nettle is well suited to cultivation and is currently experiencing a revival as a beneficial crop due to its numerous potential applications. This interest reflects in an increasing number of scientific articles related to nettle in the last years. However, reports mostly focus on the aerial parts of the plant. Roots are rich in numerous phytochemicals such as phytosterols, lignans, coumarins, sugars, and lectins. By compiling the most relevant publications, the aim of this review is to gather the current knowledge about nettle roots, such as root system functioning, biochemical composition, and related functional activities. A special emphasis is placed on lectins (or UDA for Urtica dioica agglutinin) due to their functional activities. This review highlights the potential of nettle root as a source of biomolecules. Gaps of knowledge and possible future directions for nettle root research, production, and uses are discussed.

Clickable chemical tools are essential for studying the localization and role of biomolecules in living cells. For this purpose, alkyne-based close analogs of the respective biomolecules are of outstanding interest. Here, in the field of phytosterols, we present the first alkyne derivative of sitosterol, which fulfills the crucial requirements for such a chemical tool as follows: very similar in size and lipophilicity to the plant phytosterols, and correct absolute configuration at C-24. The alkyne sitosterol FB-DJ-1 was synthesized, starting from stigmasterol, which comprised nine steps, utilizing a novel alkyne activation method, a Johnson–Claisen rearrangement for the stereoselective construction of a branched sterol side chain, and a Bestmann–Ohira reaction for the generation of the alkyne moiety. [ABSTRACT FROM AUTHOR]

The main objective of this study was to determine plasma levels of PS and to study SNVs rs41360247, rs4245791, rs4148217, and rs11887534 of ABCG8 and the r657152 SNV at the ABO blood group locus in a sample of a population treated at our hospital, and to determine whether these SNVs are related to plasma PS concentrations. The secondary objective was to establish the variables associated with plasma PS concentrations in adults. Participants completed a dietary habit questionnaire and a blood sample was collected to obtain the following variables: campesterol, sitosterol, sitostanol, lanosterol, stigmasterol, biochemical parameters, and the SNVs. In addition, biometric and demographic variables were also recorded. In the generalized linear model, cholesterol and age were positively associated with total PS levels, while BMI was negatively related. For rs4245791, homozygous T allele individuals showed a significantly lower campesterol concentration compared with C homozygotes, and the GG alleles of rs657152 had the lowest levels of campesterol compared with the other alleles of the SNV. Conclusions: The screening of certain SNVs could help prevent the increase in plasma PS and maybe PNALD in some patients. However, further studies on the determinants of plasma phytosterol concentrations are needed. [ABSTRACT FROM AUTHOR]

Plant sterols (PS) are cholesterol-like terpenoids widely spread in the kingdom Plantae. Being the target of extensive research for more than a century, PS have topped with evidence of having beneficial effects in healthy subjects and applications in food, cosmetic and pharmaceutical industries. However, many gaps in several fields of PS's research still hinder their widespread practical applications. In fact, many of the mechanisms associated with PS supplementation and their health benefits are still not fully elucidated. Furthermore, compared to cholesterol data, many complex PS chemical structures still need to be fully characterized, especially in oxidized PS. On the other hand, PS molecules have also been the focus of structural modifications for applications in diverse areas, including not only the above-mentioned but also in e.g., drug delivery systems or alternative matrixes for functional foods and fats. All the identified drawbacks are also superimposed by the need of new PS sources and technologies for their isolation and purification, taking into account increased environmental and sustainability concerns. Accordingly, current and future trends in PS research warrant discussion. [ABSTRACT FROM AUTHOR]

The carnivorous pitcher plants of the genus Nepenthes exhibit many ethnobotanical uses, including treatments of stomachache and fever. In this study, we prepared different extracts from the pitcher, stem, and leaf extracts of Nepenthes miranda obtained using 100% methanol and analyzed their inhibitory effects on recombinant single-stranded DNA-binding protein (SSB) from Klebsiella pneumoniae (KpSSB). SSB is essential for DNA replication and cell survival and thus an attractive target for potential antipathogen chemotherapy. Different extracts prepared from Sinningia bullata, a tuberous member of the flowering plant family Gesneriaceae, were also used to investigate anti-KpSSB properties. Among these extracts, the stem extract of N. miranda exhibited the highest anti-KpSSB activity with an IC50 value of 15.0 ± 1.8 μg/mL. The cytotoxic effects of the stem extract of N. miranda on the survival and apoptosis of the cancer cell lines Ca9-22 gingival carcinoma, CAL27 oral adenosquamous carcinoma, PC-9 pulmonary adenocarcinoma, B16F10 melanoma, and 4T1 mammary carcinoma cells were also demonstrated and compared. Based on collective data, the cytotoxic activities of the stem extract at a concentration of 20 μg/mL followed the order Ca9-22 > CAL27 > PC9 > 4T1 > B16F10 cells. The stem extract of N. miranda at a concentration of 40 μg/mL completely inhibited Ca9-22 cell migration and proliferation. In addition, incubation with this extract at a concentration of 20 μg/mL boosted the distribution of the G2 phase from 7.9% to 29.2% in the Ca9-22 cells; in other words, the stem extract might suppress Ca9-22 cell proliferation by inducing G2 cell cycle arrest. Through gas chromatography–mass spectrometry, the 16 most abundant compounds in the stem extract of N. miranda were tentatively identified. The 10 most abundant compounds in the stem extract of N. miranda were used for docking analysis, and their docking scores were compared. The binding capacity of these compounds was in the order sitosterol > hexadecanoic acid > oleic acid > plumbagin > 2-ethyl-3-methylnaphtho[2,3-b]thiophene-4,9-dione > methyl α-d-galactopyranoside > 3-methoxycatechol > catechol > pyrogallol > hydroxyhydroquinone; thus, sitosterol might exhibit the greatest inhibitory capacity against KpSSB among the selected compounds. Overall, these results may indicate the pharmacological potential of N. miranda for further therapeutic applications. [ABSTRACT FROM AUTHOR]

The prevalence of benign prostatic hyperplasia (BPH) markedly increases with age. Phytotherapeutic approaches have been developed over time owing to the adverse side effects of conventional medications such as 5-reductase inhibitors and α1-adrenergic receptor antagonists. Therefore, dietary supplements (DS) containing active compounds that benefit BPH are widely available. Phytosterols (PSs) are well recognized for their role in maintaining blood cholesterol levels; however, their potential in BPH treatment remains unexplored. This review aims to provide a general overview of the available data regarding the clinical evidence and a good understanding of the detailed pharmacological roles of PSs-induced activities at a molecular level in BPH. Furthermore, we will explore the authenticity of PSs content in DS used by patients with BPH compared to the current legislation and appropriate analytical methods for tracking DS containing PSs. The results showed that PSs might be a useful pharmacological treatment option for men with mild to moderate BPH, but the lack of standardized extracts linked with the regulation of DS containing PSs and experimental evidence to elucidate the mechanisms of action limit the use of PSs in BPH. Moreover, the results suggest multiple research directions in this field. [ABSTRACT FROM AUTHOR]

Introduction:Chamerion angustifolium (L.) Holub (syn. Epilobium angustifolium L.) plants have been used in the treatment and alleviating symptoms of mild Benign Prostatic Hyperplasia (BPH). Plants are abundant in polyphenols, particularly ellagitannins, phenolic acids and flavonoids. Apart from polyphenols, herb of this species also contains steroids, triterpenes and fatty acids.

Plant sterols are molecules that are structurally similar to cholesterol and provided only as dietary sources (e.g., vegetables, fruits, nuts, cereals) since they cannot be synthesized by humans. Sterol-enriched diets (≥2 g/day) may decrease total and low-density lipoprotein cholesterol concentrations by 5–10%, either alone or when added to statins, since they antagonize dietary cholesterol absorption in the intestine. On the other hand, increased serum phytosterol concentrations, (including when associated with sitosterolemia, a rare genetic defect) may contribute to atherosclerotic risk, although a threshold for such a role has not been established. Medications such as ezetimibe may effectively reduce cholesterol and phytosterol absorption. Whether the therapeutic approach associated with the reduction of phytosterol absorption is also translated into a reduction in a patient's residual cardiovascular risk needs to be established. [ABSTRACT FROM AUTHOR]

ATP-Binding cassette subfamily G (ABCG) sterol transporters maintain whole body endogenous and exogenous sterol homeostasis. A substantial portion of exogenous sterols are undigestible phytosterols (plant sterols), which can introduce complications when accumulated. ABCG5/G8 is the main protein functioning to remove ingested plant sterols providing protection from their toxic effects, although, the structural features behind substrate binding in ABCG5/G8 remain poorly resolved. Within this data article, we present extended preceding in the determination of the cholesterol-bound crystal structure and the sterol docking analysis. The crystal structure was deposited in the Protein Data Bank with the accession number of 8CUB, whereas the diffraction images were deposited at the SBGrid Data Bank. This dataset follows the research article entitled as “Structural analysis of cholesterol binding and sterol selectivity by ABCG5/G8” (doi: 10.1016/j.jmb.2022.167795).

Despite the high coexistence of hyperlipidaemia and the prediabetes state, little is known about the effects of the β-sitosterol and metformin (MET) combination. This study aimed to evaluate the effects of low doses of MET (75 or 150 mg/kg bw; M75 or M150) on western-diet induced obese (WDIO) rats, in combination or not with β-sitosterol (176 mg/kg bw; SIT and N-SIT, respectively). The gains of body weight and body fat mass, calorie food intake and plasma leptin were reduced in M150 animals, both SIT and N-SIT groups. Only N-SIT animals showed that insulin levels and HOMA-IR were reduced in the M150 group. M150 group showed a tendency towards lower mRNA levels of Npy and increased Lepr mRNA levels in hypothalamus, but only in N-SIT animals. In conclusion, these results show that the co-administration of MET with β-sitosterol seems to neutralise part of the beneficial effects of MET in WDIO rats.

Background: This study describes the isolation of chemical constituents from the leaves and bark of Phyllanthus acidus, a medicinal plant widely used for the treatment of several ailments. Materials and Methods: The crude extract of P. acidus was chromatographed on a gravity column dry packed with silica gel and was fractionated by increasing proportions of acetone in CH2Cl2. The purified isolates were subjected to NMR for structure elucidation. Their structures were identified mainly by using 1H-NMR and by comparing current NMR data with those reported in the literature. Results: The results showed that the air-dried leaves extracts of the plant afforded mixture of β-sitosterol and stigmasterol while the bark yielded mixture of phyllanthol, α-amyrin, β-amyrin and lupeol. Conclusion: The air-dried of DCM extract of P. acidus resulted in the isolation of the mixture of phyllanthol, α- amyrin, β-amyrin and lupeol from the bark and mixture of β-sitosterol and stigmasterol from the leaves of the plant. It is important to conduct detailed pharmacological and toxicity investigations as well as clinical studies using different doses or concentrations to verify its traditional uses. [ABSTRACT FROM AUTHOR]

This study aims at investigation of antibacterial property of Parthenium hysterophorous against aquatic bacterial pathogens and to identify the key bioactive compound of the same. Antibacterial activity of the crude extracts confirmed that chloroform extract PHC has strong antibacterial activity against aquatic pathogens V.anguillarum and V.harveyi with 16mm and 15mm ZOI at 1mg/well concentration. The crude extracts were subjected for GC-MS analysis to identify the secondary metabolites. PHC was subjected to silica-gel column chromatography to separate the individual phytochemicals. PHC was separated into 9 fractions, among which Fraction No.2 demonstrated significant antibacterial activity against V.anguillarum and V.harveyi with 19mm and 17mm ZOI at 10µg/well concentration. Fraction No.2 was identified to be β-sitosterol based on mass spectrometry analysis and fragmentation analysis. In-silico protein ligand docking demonstrated that β-sitosterol has highest affinity to inhibit dihydrofolate reductase (DHFR) enzyme with -10.10Kcal/mol binding energy. This prediction was further validated using molecular dynamic simulation for 20ns. Based on these computational analyses, it was proposed that β-sitosterol exhibits antibacterial activity via inhibition of DHFR enzyme. β-sitosterol is a well known nutritionally valuable compound that reduces cholesterol levels in humans. It is also been used as supplement feed to increase the nutritional value of cultured fishes. β-sitosterol has also been proven to have positive effect in growth and reproduction of cultivated fishes. Findings of this study strongly suggest the usage of β-sitosterol in aquaculture, as nutritional supplement and also as disease control agent to prevent and control fish diseases caused by Vibrio species.

Replacement with the cheaper animal fats or vegetable oils is conventional in milk through direct incorporation or homogenization of skimmed milk with less expensive foreign fats. The main objective of the present study was to evaluate the capability of a simple, fast, and reliable method for the detection of added palm oil in butter. The butter samples were mixed with palm oil (0.5-50 wt%) followed by gas chromatography analysis of fatty acids and sterols. The results confirmed the potential of discrimination based on a significant increase in the content of unsaturated fatty acids (C18:1 and C18:2) and a decrease in saturated fatty acids (mainly C10:0, C12:0, and C14:0). The differences are detectable for at least 10.0 wt% of the palm oil. Also, significant variations were observed in the cholesterol and sitosterol as marker sterols in the butter and palm oil, respectively. The study demonstrates the high potential of the procedure to rapidly detect and discriminate between butter-palm oil blends among pure samples.

The prevalence of benign prostatic hyperplasia (BPH) markedly increases with age. Phytotherapeutic approaches have been developed over time owing to the adverse side effects of conventional medications such as 5-reductase inhibitors and α1-adrenergic receptor antagonists. Therefore, dietary supplements (DS) containing active compounds that benefit BPH are widely available. Phytosterols (PSs) are well recognized for their role in maintaining blood cholesterol levels; however, their potential in BPH treatment remains unexplored. This review aims to provide a general overview of the available data regarding the clinical evidence and a good understanding of the detailed pharmacological roles of PSs-induced activities at a molecular level in BPH. Furthermore, we will explore the authenticity of PSs content in DS used by patients with BPH compared to the current legislation and appropriate analytical methods for tracking DS containing PSs. The results showed that PSs might be a useful pharmacological treatment option for men with mild to moderate BPH, but the lack of standardized extracts linked with the regulation of DS containing PSs and experimental evidence to elucidate the mechanisms of action limit the use of PSs in BPH. Moreover, the results suggest multiple research directions in this field.

Non-cholesterol sterols are transported in plasma lipoproteins and are consequently important in cholesterol metabolism. We investigated the distribution of non-cholesterol sterol precursors of cholesterol synthesis (NCSPCS), oxysterols, and phytosterols in lipoproteins of healthy subjects differing according to HDL-Cholesterol (HDL-C) plasma levels. Elevated NCSPCS (desmosterol, lathosterol) in the High HDL group suggests that HDL exports these sterols from cells, but not the cholesterol metabolite 24-OHC which was higher in the Low HDL group than in the High HDL group. 27-hydroxycholesterol (27OH-C) plasma levels did not differ between groups. Percentage of NCSPCS and phytosterols predominates in LDL, but did not differ between groups. Thirty percent of desmosterol and lathosterol are present in HDL, with the High HDL group carrying higher percentage of these sterols. A high percentage of campesterol and sitosterol in HDL suggests that phytosterols are absorbed by enterocytes, and that HDL could be a marker of the ABCA1/ApoA1 intestinal activity.

While the properties of edible pomegranate varieties have been widely explored, there is little information on ornamental types. In this study, possible alternatives for the valorization of dwarf pomegranate fruits have been explored. The characterization of their hydromethanolic extract by gas chromatography−mass spectrometry evidenced the presence of high contents of 5-hydroxymethylfurfural (a carbon-neutral feedstock for the production of fuels and other chemicals) and β- and γ-sitosterol stereoisomers. The microbicidal activity of the crude extract, both alone and in a conjugate complex with chitosan oligomers (COS), was investigated against three plant pathogenic microorganisms that cause significant losses in woody crops: Erwinia amylovora, E. vitivora, and Diplodia seriata. In in vitro assays, a strong synergistic behavior was found after conjugation of the bioactive constituents of the fruit extract with COS, resulting in minimum inhibitory concentration (MIC) values of 750 and 375 μg·mL−1 against E. amylovora and E. vitivora, respectively, and an EC90 value of 993 μg·mL−1 against D. seriata. Hence, extracts from the non-edible fruits of this Punicaceae may hold promise as a source of high value-added phytochemicals or as environmentally friendly agrochemicals. [ABSTRACT FROM AUTHOR]

Qingfei Paidu decoction (QFPD) has been repeatedly recommended for the clinical treatment of novel coronavirus disease 2019 (COVID-19) in multiple provinces throughout China. A possible complication of COVID-19 lung involvement is pulmonary fibrosis, which causes chronic breathing difficulties and affects the patient's quality of life. Therefore, there is an important question regarding whether QFPD can alleviate the process of pulmonary fibrosis and its potential mechanisms. To explore this issue, this study demonstrated the anti-pulmonary fibrosis activity and mode of action of QFPD in vivo and in vitro pulmonary fibrosis models and network pharmacology. The results showed that QFPD effectively ameliorated the bleomycin-induced inflammation and collagen deposition in mice and significantly improved the epithelial-mesenchymal transition in pulmonary fibrosis in mice. In addition, QFPD inhibited bleomycin-induced M2 polarization of macrophages in pulmonary tissues. An in-depth study of the mechanism of QFPD in the treatment of pulmonary fibrosis based on network pharmacology and molecular simulation revealed that SRC was the main target of QFPD and sitosterol (a key compound in QFPD). QFPD and sitosterol regulate the EMT process and M2 polarization of macrophages by inhibiting the activation of SRC, thereby alleviating pulmonary fibrosis in mice. COVID-19 infection might produce severe fibrosis, and antifibrotic therapy with QFPD may be valuable in preventing severe neocoronavirus disease in patients with IPF, which could be a key factor explaining the role of QFPD in the treatment of COVID-19. [ABSTRACT FROM AUTHOR]

The role of selected minor oil components on sterol/sterol ester oleogels was studied. Therefore, oleic acid, tocopheryl acetate and monoglycerides were admixed with three vegetable oils, having different fatty acid compositions. Before that, minor natural components were removed from untreated oils (purification). Moreover, purified oils were subjected to a humidity treatment to increase their water content. All additives retarded the molecular self‐assembly of sitosterol with oryzanol, and the effect was dose‐dependent. Gel hardness only increased at low concentrations of tocopheryl acetate and decreased in all gels at higher concentrations. In contrast, Gmax′ was invariable in samples with oleic acid and monoglycerides and increased in gels containing tocopheryl acetate and water. Therefore, Gmax′ does not necessarily relate to the gels' compression firmness. Atomic force microscopy showed that the microstructure of oleogels was considerably modified by the additives. In general, a packed surface of twisted, thick bundles of tubules may be associated with a stiffer gel. Moreover, a composite structure in gels with monoglycerides was visible and confirmed by differential scanning calorimetry (DSC). DSC was used to determine gel–sol transition temperature and was associated with the number of tubules in the gel. The gel–sol temperature increased in samples 1.0% w/w oleic acid and tocopheryl acetate and decreased in gels with monoglycerides and water. The results show that oleogel properties can be significantly modified by minor components with functional groups. That was associated with interactions with the sterol and sterol ester in solution and with the surface of the tubules (ferulic acid moieties of oryzanol) in oleogels. [ABSTRACT FROM AUTHOR]

Plant sterols are molecules that are structurally similar to cholesterol and provided only as dietary sources (e.g., vegetables, fruits, nuts, cereals) since they cannot be synthesized by humans. Sterol-enriched diets (≥2 g/day) may decrease total and low-density lipoprotein cholesterol concentrations by 5–10%, either alone or when added to statins, since they antagonize dietary cholesterol absorption in the intestine. On the other hand, increased serum phytosterol concentrations, (including when associated with sitosterolemia, a rare genetic defect) may contribute to atherosclerotic risk, although a threshold for such a role has not been established. Medications such as ezetimibe may effectively reduce cholesterol and phytosterol absorption. Whether the therapeutic approach associated with the reduction of phytosterol absorption is also translated into a reduction in a patient’s residual cardiovascular risk needs to be established.

β‐Sitosterol is a major bioactive constituent in plants with potent anticancer effects against many human cancer cells, but its bioavailability and therapeutic efficacy are limited by its poor solubility in water. In this study, C6‐imidazole chitosan, C6‐1‐methylimidazole chitosan, C6‐1‐ethylimidazole chitosan, C6‐1‐vinylimidazole chitosan, C6‐1‐allylimidazole chitosan, and C6‐1‐butylimidazole chitosan were prepared to extract β‐sitosterol from edible oil samples via ultrasonic‐assisted solid liquid extraction. The structures and properties of the newly synthesized products were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, and elemental analysis. The extraction abilities of the derivatives were tested in the experiment with high‐performance liquid chromatography (limit of detection 0.21 μg/g and limit of quantification 0.67 μg/g), and the % relative standard deviation (<3.25%) and recovery values of the prepared chitosan derivatives toward β‐sitosterol (average: 100.20%) were acceptable. The spiked interday and intraday recoveries of β‐sitosterol were 102.60 ± 2.78 and 103.90 ± 3.04%, respectively. The actual amounts of β‐sitosterol extracted from three real samples using C6‐imidazole chitosan according to the solid phase extraction method were 3302.40, 901.70, and 2045.60 mg/kg for corn oil, olive oil, and pea oil, respectively. [ABSTRACT FROM AUTHOR]

• There is no feasible diagnostic tool in primary care screening for sitosterolemia. • Endogenous and plant sterols in dried blood spot (DBS) was evaluated by GC–MS. • The DBS levels of plant sterols accurately identified patients with sitosterolemia. • Molecular ratios of sitosterol to endogenous sterols could be diagnostic biomarkers. • A DBS/GC–MS assay provides diagnostic sterol cut-off values for sitosterolemia. Sitosterolemia is a rare inherited lipid metabolic disorder characterized by increased levels of plant sterols and accelerated atherosclerosis. Although early detection is beneficial for the prevention of disease progression, it is largely underdiagnosed by routine screening based on conventional lipid profiles. A gas chromatography-mass spectrometry (GC–MS)-based profiling has been developed and validated to measure the levels of biologically active free sterols, including five endogenous sterols and three plant sterols (sitosterol, campesterol, and stigmasterol) in dried blood spot (DBS). Within- and between-run precisions were 1.4–11.1 % and 2.2–14.1 %, respectively, while the accuracies were all 86.3 ∼ 121.9 % with the correlation coefficients (r 2) > 0.988 for all the sterols. In the patients (four girls and two boys, 6.5 ± 2.8 years), sitosterol levels were significantly increased, with an optimal cut-off value of 2.5 µg/mL distinguishing them from ninety-three age-matched healthy children. A cut-off value of 31.9 µg/mL differentiated the patients from six ABCG5/ABCG8 heterozygous carriers. In addition, the molecular ratios of sitosterol to cholesterol, desmosterol, and 7-dehydrocholesterol provided excellent cut-off values of 26.3, 67.6, and 21.6, respectively, to distinguish patients from both healthy controls and heterozygous carriers. The novel DBS-based GC–MS profiling of free sterols accurately identified patients with sitosterolemia, with a performance comparable to that of a serum assay. The DBS profiling could be more feasible method in clinical practice as well as population screening programs, and it can provide diagnostic cut-off values for individual plant sterols. [ABSTRACT FROM AUTHOR]

Plants stand out among eukaryotes due to the large variety of sterols and sterol derivatives that they can produce. These metabolites not only serve as critical determinants of membrane structures, but also act as signaling molecules, as growth-regulating hormones, or as modulators of enzyme activities. Therefore, it is critical to understand the wiring of the biosynthetic pathways by which plants generate these distinct sterols, to allow their manipulation and to dissect their precise physiological roles. Here, we review the complexity and variation of the biosynthetic routes of the most abundant phytosterols and cholesterol in the green lineage and how different enzymes in these pathways are conserved and diverged from humans, yeast, and even bacteria. Many enzymatic steps show a deep evolutionary conservation, while others are executed by completely different enzymes. This has important implications for the use and specificity of available human and yeast sterol biosynthesis inhibitors in plants, and argues for the development of plant-tailored inhibitors of sterol biosynthesis. [ABSTRACT FROM AUTHOR]

This study aims at investigation of antibacterial property of Parthenium hysterophorous against aquatic bacterial pathogens and to identify the key bioactive compound of the same. Antibacterial activity of the crude extracts confirmed that chloroform extract PHC has strong antibacterial activity against aquatic pathogens V.anguillarum and V.harveyi with 16mm and 15mm ZOI at 1mg/well concentration. The crude extracts were subjected for GC-MS analysis to identify the secondary metabolites. PHC was subjected to silica-gel column chromatography to separate the individual phytochemicals. PHC was separated into 9 fractions, among which Fraction No.2 demonstrated significant antibacterial activity against V.anguillarum and V.harveyi with 19mm and 17mm ZOI at 10μg/well concentration. Fraction No.2 was identified to be β-sitosterol based on mass spectrometry analysis and fragmentation analysis. In-silico protein ligand docking demonstrated that β-sitosterol has highest affinity to inhibit dihydrofolate reductase (DHFR) enzyme with -10.10Kcal/mol binding energy. This prediction was further validated using molecular dynamic simulation for 20ns. Based on these computational analyses, it was proposed that β-sitosterol exhibits antibacterial activity via inhibition of DHFR enzyme. β-sitosterol is a well known nutritionally valuable compound that reduces cholesterol levels in humans. It is also been used as supplement feed to increase the nutritional value of cultured fishes. β-sitosterol has also been proven to have positive effect in growth and reproduction of cultivated fishes. Findings of this study strongly suggest the usage of β-sitosterol in aquaculture, as nutritional supplement and also as disease control agent to prevent and control fish diseases caused by Vibrio species. [ABSTRACT FROM AUTHOR]

Two new steroidal saponins, β-sitosterol-3-O-α-l-glucopyranoside (3) and β-sitosterol-3-O-β-d-glucopyranosyl-(1→6)-β-d-glucopyranoside (4), were isolated and identified from the bark of Neolamarckia cadamba, along with 13 known compounds. Their structures were established on the basis of spectral data. [ABSTRACT FROM AUTHOR]

Cholesterol and sitosterol are two members of the steroid family, which molecular structures differ only by the presence of an ethyl substituent at the position 24 of the steroid skeleton. Cholesterol is mainly synthesized in large quantities in the liver of animals and only in small quantities by plants. In contrast sitosterol is only synthesized by plants. This tiny difference of an ethyl group between the two steroids structures have induced profound effects on the climatic changes during evolution, but plant sterols still have important effects on cholesterol metabolism on humans. [ABSTRACT FROM AUTHOR]

• Some of the heterozygous mutation carriers showed serum sitosterol level >10 μg/ml. • A cutoff value of sitosterol 15 μg/ml appears to be best predicting ABCG5 / ABCG8 mutations. • Genetic analysis should be considered when sitosterol level >15 μg/ml. Currently, serum concentrations of sitosterol above 10 μg/ml are considered to be one of the major diagnostic criteria of sitosterolemia. We retrospectively investigated consecutive 206 Japanese dyslipidemic subjects (mean age = 46 yr, male n = 94) with the assessments of serum sitosterol level and the presence of ABCG5 or ABCG8 genetic mutations in our institute since 2009–2018. We divided the subjects into 3 groups based on the number of pathogenic mutations in ABCG5 or ABCG8 genes. We compared serum lipids and serum sitosterol among those groups, and tried to validate the cutoff value discriminating patients of sitosterolemia with double mutations from others. We identified 8 individuals with sitosterolemia with double mutations (affected), 26 individuals with a single mutation (carrier), and 172 individuals without any mutations (wildtype control). Serum sitosterol level of patients with sitosterolemia with double mutations (affected) exhibited significantly higher than those of any other groups (45.2. vs. 7.9 μg/ml, p = 2.5 × 10-2, 45.2 vs. 3.1 μg/ml, p = 1.8 × 10-2). Under these conditions, a cutoff value of sitosterol 10 μg/ml could discriminate the patients with sitosterolemia with double mutations in ABCG5 or ABCG8 gene from no mutation carrier (wildtype control) perfectly, although 6 heterozygous mutation carries exhibited sitosterol level greater than 10 μg/ml. Receiver-operating characteristic (ROC) analysis predicting double mutation status showed that the best cut-off value was 14.81 μg/ml. We suggest a cutoff value of sitosterol 15 μg/ml that shows higher positive predictive value than 10 μg/ml. [ABSTRACT FROM AUTHOR]

Purpose: Lowering of LDL cholesterol levels by plant sterols and stanols is associated with decreased risk of cardiovascular disease in humans. Plant sterols and stanols also lower triacylglycerol (TG). However, it is not fully understood how reduction in TG is achieved and what the full potential of plant sterols and stanols is on whole-body metabolism. We here hypothesize that high levels of plant sterols and stanols stimulate whole-body energy expenditure, which can be attributed to changes in mitochondrial function of brown adipose tissue (BAT), skeletal muscle and liver. Methods: Phytosterolemic mice were fed chow diets for 32 weeks to examine whole-body weight gain. In vitro, 24-h incubation were performed in adipocytes derived from human BAT, human myotubes or HepG2 human hepatocytes using sitosterol or sitostanol. Following mitochondrial function was assessed using seahorse bioanalyzer. Results: Chow feeding in phytosterolemic mice resulted in diminished increase in body weight compared to control mice. In vitro, sitosterol or sitostanol did not change mitochondrial function in adipocytes derived from human BAT or in cultured human myotubes. Interestingly, maximal mitochondrial function in HepG2 human hepatocytes was decreased following sitosterol or sitostanol incubation, however, only when mitochondrial function was assessed in low glucose-containing medium. Conclusions: Beneficial in vivo effects of plant sterols and stanols on lipid and lipoprotein metabolism are well recognized. Our results indicate that alterations in human mitochondrial function are apparently not involved to explain these beneficial effects. [ABSTRACT FROM AUTHOR]

HepG2 cells were incubated with a 16.5:1.7:1 ratio of cholesterol:sitosterol:campesterol (CSC), a ratio of the major sterols observed in the plasma of phytosterolemia patients, or with cholesterol alone in combination with [14C]acetate for 24 h and the radioactivity incorporated into lipids determined. Cells incubated with CSC exhibited a 40% reduction in cholesterol esterification (p < 0.05) compared to cells incubated with cholesterol alone. In addition, a 17.5‐fold reduction (p < 0.05) in total cholesterol (cholesterol plus cholesteryl ester) synthesis from [14C]acetate was observed in cells incubated with CSC compared to cholesterol alone. Low‐density lipoprotein receptor (LDLR) mRNA abundance was lower in cells incubated with CSC compared to cells incubated with cholesterol alone. Our results suggest that incubation of HepG2 cells with a ratio of sterols that mimic the plasma concentration seen in phytosterolemia patients reduces cholesterol esterification, total cholesterol synthesis, and inhibits LDLR mRNA abundance. We suggest that future cell and animal‐based work on phytostosterolemia might employ this methodology to serve as a novel paradigm of the disease. [ABSTRACT FROM AUTHOR]

BACKGROUND/OBJECTIVES: In many studies, low serum cholesterol is paradoxically associated with a higher mortality risk among older adults. Therefore, we studied whole‐body cholesterol metabolism and its role in all‐cause mortality of older men in two subcohorts of different ages. DESIGN: Prospective long‐term cohort. SETTING: Home‐dwelling men of the Helsinki Businessmen Study. PARTICIPANTS: Two partly overlapping subcohorts were recruited, in 2003 (n = 660; mean age = 76 years) and in 2011 (n = 398; mean age = 83 years). The younger subcohort was followed up after 3 and 11 years, and the older subcohort was followed up after 3 years. MEASUREMENTS: Cholesterol metabolism was assessed via serum noncholesterol sterol‐cholesterol ratios, and quantification was performed by gas‐liquid chromatography with flame ionization detection. All statistical analyses were performed with age and statin treatment as covariates. RESULTS: At the end of the 3‐year follow‐up, 10% of the younger and 13% of the older subcohort had died; and at the end of the 11‐year follow‐up, 40% of the younger subcohort had died. Serum total and low‐density lipoprotein (LDL) cholesterol and cholesterol precursors reflecting cholesterol synthesis were lower in the older than in the younger subcohort (P <.001 for all). In the older subcohort, low serum campesterol and sitosterol, reflecting decreased cholesterol absorption efficiency, predicted all‐cause mortality (P <.05). This was supported by a trend toward low serum campesterol and sitosterol predicting mortality (P =.088 and P =.079, respectively) in the younger subcohort after 11 years. Cholesterol synthesis did not predict mortality, but in the older subcohort, decreased cholesterol absorption was less efficiently compensated for by decreased cholesterol synthesis. CONCLUSIONS: Low cholesterol absorption efficiency predicted all‐cause mortality, especially in men aged 83 years on average, and cholesterol synthesis was lowered. These metabolic changes could contribute to the lowering of serum total and LDL‐cholesterol in older men. J Am Geriatr Soc 68:281–287, 2020 See related editorial by Ariela R. Orkaby in this issue. See related article by Maihofer et al. [ABSTRACT FROM AUTHOR]

Using cholesterol, stigmasterol and sitosterol as starting materials, a series of 7-subsitituted-ster-3-yl 2-methoxybenzoate analogs were prepared through reacting with 2-methoxybenzoyl chloride and introducing some function groups, such as carbonyl, hydroxyl and various thiosemicarbazones, at 7-position of steroidal nucleus. The structures of these new compounds were characterized by IR, NMR and HRMS. Their antiproliferative activities were evaluated by using several types of cancer cells. Interestingly, the compounds displayed potent antiproliferative activity against CNE-2 (nasopharyngeal carcinoma cell lines), BEL-7402 (human liver cancer cell lines) and HepG2 (human liver cancer cell lines), suggesting that they have potential to be drug candidates for cancer treatment. [ABSTRACT FROM AUTHOR]

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The effect of β-Sitosterol to the levels of male,s hormones was carried out in sera of adult male rabbit, twenty eight of local rabbite, weigh aging range between (800-1500)g. The animals was divided randomly into 4 groups (7 rabbits in each group) . The control wene treated orally corn oil but the Three groups G1,G2 and G3 wene treated orally with (40,60,80) mg/kg of β-Sitosterol respectively for a period of 30 days. Their sera were taken so as to conducting the biochemical tests, including the estimate of testosterone hormone ,Lutein hormone ,Follice stimulating hormone and estradiol hormone . The results showed that the LH hormone level was significantly increased in sera of G2andG3 as compared with control group, while the FSH level did not show any significant differences compared with control group, whereas the control group. The estradiol hormone level did not show any significant changes in sera of all groups under testosterone hormone level showed a significant decrease in sera of G1 and G3 compared with investigation , The effect of β-sitosterol on the testicle tissue had showed that there were necrosis and vaculation between seminiferous tubules with the deposition of fibrin between and within the seminiferous tubules in the transaction in all groups treated with β-sitosterol .

Abstract Amazonian aquatic systems are usually associated with pristine waters, however, irregular urban occupation of the hydrographic basins and sewerage deficiencies may lead to point and diffuse contamination. Sewage contamination in intertidal surface sediments from the Guajará Estuary, Brazilian Amazon coast, was evaluated using a set of steroids as biomarkers. Sediments collected along the urbanized margin were also analyzed for chlorophyll a, total organic carbon and grain sizes. Coprostanol, the main fecal sterol, was found at concentrations varying from 0.06 to 7.93 µg g-1 dry sediment, following the sequence Tucunduba > Ver-o-Peso > Porto da Palha > Tamandaré > Icoaraci > Miramar. Mixed sources of organic matter and coastal process probably concurred to produce weak correlations among the parameters. Plant derived sterols, including n-C30 alcohol and β-amyrinyl alkanoates, were clearly abundant, but they did not preclude the use of other steroid signals to the assessment of sewage contamination. High values of the steroid indexes involving 5α and 5β stanols and stanones highlighted sewage contamination at the sites with the lowest absolute coprostanol concentrations. The predominance of 5β stanols indicated a chronically sewage contamination of the area.

Graphical abstract Highlights • Thirteen phytosterols were identified in the kernels of six black walnut cultivars. • Black walnuts and English walnut did not vary significantly on total phytosterol levels. • Untargeted metabolomics analysis showed the presence of conjugated phytosterols. Abstract This study aimed to identify and quantify phytosterols of six black walnut (Juglans nigra L.) varieties, and compare the levels of these phytosterols between black walnuts and English walnut (Juglans regia L.). Totally, 13 phytosterols were identified in the black walnut kernels, with β-sitosterol predominating over the other sterols. The analysis also revealed the presence of 3 phytosterols, Δ5,23-stigmastadienol, cycloeucalenol and 28-methylobtusifoliol, which have never been reported in black walnuts. The average levels of total sterols ranged from 1236.0 mg/kg to 1542.3 mg/kg. No significant differences were noted in total sterol levels between the studied black walnut varieties and English walnut. Through untargeted metabolomics analysis, five additional glycosylates and hydroxycinnamates of phytosterols were putatively identified in the black walnuts. The findings from this research suggest black walnuts are rich in phytosterols most of which have been demonstrated to exert bioactivities. Future studies should be focused on seasonal and geographic variations in phytosterol content of black walnuts, and bioassay-guided purification to assess potential health-promoting properties of these phytosterols. [ABSTRACT FROM AUTHOR]

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Background and aims We aimed to examine the effect of serum sitosterol, a cholesterol absorption marker, on clinical outcomes in acute coronary syndrome patients with dyslipidaemia. Methods This is a sub-analysis of the HIJ-PROPER trial that assesses the effect of aggressive low-density lipoprotein cholesterol (LDL-C) lowering treatment with pitavastatin + ezetimibe in 1734 acute coronary syndrome (ACS) patients with dyslipidaemia. Patients were divided into two groups based on sitosterol level at enrolment (cut-off value was 2.2 μg/mL; a median of baseline sitosterol level), and clinical outcomes were examined. Results The mean LDL-C level after 3 years in the low sitosterol group was 84.8 ± 20.1 mg/dL with pitavastatin-monotherapy and 64.6 ± 20.3 mg/dL with pitavastatin + ezetimibe, while corresponding values in the high sitosterol group were 91.0 ± 22.9 mg/dL and 71.1 ± 23.3 mg/dL, respectively. In the high sitosterol group, the Kaplan-Meier event rate for the primary endpoint at 3 years was 26.0% in the pitavastatin + ezetimibe group, as compared with 34.3% in the pitavastatin-monotherapy group (hazard ratio, 0.71; 95% confidence interval, 0.56–0.91; p  = 0.006, p -value for interaction = 0.010). However, in the low sitosterol group, there was no significant reduction of the primary endpoint by pitavastatin + ezetimibe therapy. Conclusions Aggressive lipid-lowering treatment with ezetimibe had a positive effect on clinical outcomes in the high sitosterol subset of ACS patients with dyslipidaemia, but not in the low sitosterol subset. This effect was independent of LDL-C reduction and suggests that sitosterol measurement on admission in ACS patients might contribute to a “personalised” lipid-lowering approach. [ABSTRACT FROM AUTHOR]

Copyright of Egyptian Journal of Botany is the property of Egyptian National Agricultural Library (ENAL) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Shipin Kexue/ Food Science is the property of Food Science Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)