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Cyclodextrins, representing a versatile family of cyclic oligosaccharides, have extensive pharmaceutical applications due to their unique truncated cone-shaped structure with a hydrophilic outer surface and a hydrophobic cavity, which enables them to form non-covalent host–guest inclusion complexes in pharmaceutical formulations to enhance the solubility, stability and bioavailability of numerous drug molecules. As a result, cyclodextrins are mostly considered as inert carriers during their medical application, while their ability to interact not only with small molecules but also with lipids and proteins is largely neglected. By forming inclusion complexes with cholesterol, cyclodextrins deplete cholesterol from cellular membranes and thereby influence protein function indirectly through alterations in biophysical properties and lateral heterogeneity of bilayers. In this review, we summarize the general chemical principles of direct cyclodextrin–protein interactions and highlight, through relevant examples, how these interactions can modify protein functions in vivo, which, despite their huge potential, have been completely unexploited in therapy so far. Finally, we give a brief overview of disorders such as Niemann–Pick type C disease, atherosclerosis, Alzheimer’s and Parkinson’s disease, in which cyclodextrins already have or could have the potential to be active therapeutic agents due to their cholesterol-complexing or direct protein-targeting properties.

Egg yolk is used as an emulsifying agent. Nevertheless, its high concentration of cholesterol is linked to chronic degenerative diseases that cause cardiovascular disease. In this study, three methods for reducing the level of cholesterol in egg yolks were studied. The first method consisted of physical separation of the granules contained in the yolk (NaG). The second method applied was the use of anionic chelating biopolymers, such as arabic gum solution (AG) and mesquite gum solution (MG), and the third method was extraction with a solvent (SA). For this purpose, the cholesterol present in egg yolks, the microstructure, particle size, zeta potential, and its emulsifying capacity were determined. The amount of cholesterol removed was 97.24% using 1% mesquite gum (MG1%), and 93.26% using 1% Arabic gum (AG1%). The zeta potential was determined, and the isoelectric point (ζ = 0) of egg yolk was identified as pH 4.6. While, at this pH, the zeta potential of mesquite gum was −14.8 mV, the zeta potential for the arabic gum was −16 mV. The emulsifying capacity of MG1% was 62.95%, while the emulsifying capacity of AG1% was 63.57%. The complex obtained can be used in the development of functional foods reduced in cholesterol.

This work is devoted to the chemical synthesis of sulfated chitosan and its experimental verification in an animal model of early atherosclerosis. The method of chitosan quaternization with sulfate-containing ingredients resulted in a product with a high content of sulfate groups. Implantation of this product into the fascial-muscular sheath of the main limb artery along the leg and thigh in rabbits led to the extraction of cholesterol from the subintimal region. Simplified methods for the chemical synthesis of quaternized sulfated chitosan and the use of these products in a model of experimental atherosclerosis made it possible to perform a comparative morphological analysis of the vascular walls of the experimental and control limbs under conditions of a long-term high-cholesterol diet. The sulfated chitosan samples after implantation were shown to change the morphological pattern of the intimal and middle membranes of the experimental limb artery. The implantation led to the degradation of soft plaques within 30 days after surgical intervention, which significantly increased collateral blood flow. The implantation of sulfated chitosan into the local area of the atherosclerotic lesions in the artery can regulate the cholesterol content in the vascular wall and destroy soft plaques in the subintimal region.

Cyclodextrins (CDs) have traditionally been recognized as excipients that enhance solubility and stability of drugs. However, growing evidence shows that CDs themselves can act as active therapeutic agents. Their unique supramolecular properties enable them to interact with biological membranes, mobilize cholesterol, and modulate immune responses. This review highlights four therapeutic areas where CDs demonstrate particular promise. First, in gene and mRNA therapy, cationic CD derivatives form nanoparticles that protect nucleic acids, promote endosomal escape, and achieve targeted delivery. Second, in neurodegenerative disorders such as Niemann–Pick type C and Alzheimer’s disease, hydroxypropyl-β-CD facilitates cholesterol clearance and reduces pathological lipid accumulation. Third, in detoxification, the γ-CD derivative sugammadex exemplifies a clinically approved agent that encapsulates neuromuscular blockers to reverse anesthesia. Finally, CDs have emerged as safe vaccine adjuvants, inducing robust systemic and mucosal immunity with reduced IgE responses compared to alum. Together, these examples illustrate a paradigm shift: CDs are not only versatile excipients but also active molecules with direct therapeutic effects. Future translation will require careful optimization of safety, scalability, and regulatory compliance, but CDs are poised to contribute meaningfully to next-generation medicines.

The cholesterol-lowering effects of garlic as part of a healthy diet remain controversial. The aim of this study was to investigate whether supplementation with aged black garlic (ABG) could improve blood lipid profiles in patients with mild hypercholesterolemia. We conducted a double-blind, randomized placebo-controlled trial. Sixty participants were randomly assigned to receive either ABG or placebo twice daily (total 6 g/d) before consumption of a meal every morning and evening for 12 wk. During the study, two participants dropped out of the ABG group, and three participants dropped out of the placebo group. Thus, the effects of AGB on fasting blood levels of lipids were evaluated in 28 participants and compared with the placebo group (n = 27). Among lipid components, no significant differences in triglycerides, low-density lipoprotein cholesterol, total cholesterol, or free fatty acid levels were observed between the two groups. However, ABG increased high-density lipoprotein cholesterol levels compared with the placebo group at the end of the study. Moreover, a significant decrease in the levels of alipoprotein B and a significant increase in the ratio of low-density lipoprotein cholesterol/alipoprotein B were observed in the ABG group. No adverse effects were reported in any of the patients. ABG supplementation reduced atherogenic markers and thus may have a cardioprotective effect beyond the gold standard medication in patients with mild hypercholesterolemia.

Crude rice bran oils from different rice cultivars and extraction methods bear different contents of nutraceuticals. The health benefits of lowering cholesterol activity of rice bran oil being confirmed by many reports are partly attributed to non-nutrient nutraceuticals, especially γ-oryzanol, phytosterols, and policosanols. As the world has been facing the global warming crisis, green extraction technology is gaining attention from many sectors. The current study aims to compare the nutraceutical composition with respect to γ-oryzanol, phytosterol, and policosanol content as well as the antioxidant properties of crude rice bran oils extracted from white and red rice bran using three green technologies, comparing with conventional hexane extraction. The data show that the traditional solvent extraction gave the highest oil yield percentage (26%), but it was not significantly different from subcritical liquefied dimethyl ether extraction (24.6%). Subcritical liquefied dimethyl ether extraction gave higher oil yield than supercritical CO2 extraction (15.5–16.2%). The crude rice bran oil extracted using subcritical liquefied dimethyl ether extraction produced the highest total phenolic contents and antioxidant activities. The highest γ-oryzanol content of the crude rice bran oil was found in oil extracted by conventional cold press (1370.43 mg/100 g). The γ-oryzanol content of the oil obtained via subcritical liquefied dimethyl ether extraction was high (1213.64 mg/100 g) compared with supercritical CO2 extraction. The red rice bran yielded the crude rice bran oil with the highest total phytosterol content compared with the white bran, and the oil from red rice bran extracted with subcritical liquefied dimethyl ether generated the highest total phytosterol content (1784.17 mg/100 g). The highest policosanol content (274.40 mg/100 g) was also found in oil obtained via subcritical liquefied dimethyl ether extraction.

Betaine is a non-essential amino acid with proven functional properties and underutilized potential. The most common dietary sources of betaine are beets, spinach, and whole grains. Whole grains—such as quinoa, wheat and oat brans, brown rice, barley, etc.—are generally considered rich sources of betaine. This valuable compound has gained popularity as an ingredient in novel and functional foods due to the demonstrated health benefits that it may provide. This review study will provide an overview of the various natural sources of betaine, including different types of food products, and explore the potential of betaine as an innovative functional ingredient. It will thoroughly discuss its metabolic pathways and physiology, disease-preventing and health-promoting properties, and further highlight the extraction procedures and detection methods in different matrices. In addition, gaps in the existing scientific literature will be emphasized.

Interactions between the diet and intestinal microbiota play a role in health and disease, including obesity and related metabolic complications. There is great interest to use dietary means to manipulate the microbiota to promote health. Currently, the impact of dietary change on the microbiota and the host metabolism is poorly predictable and highly individual. We propose that the responsiveness of the gut microbiota may depend on its composition, and associate with metabolic changes in the host. Our study involved three independent cohorts of obese adults (n = 78) from Belgium, Finland, and Britain, participating in different dietary interventions aiming to improve metabolic health. We used a phylogenetic microarray for comprehensive fecal microbiota analysis at baseline and after the intervention. Blood cholesterol, insulin and inflammation markers were analyzed as indicators of host response. The data were divided into four training set - test set pairs; each intervention acted both as a part of a training set and as an independent test set. We used linear models to predict the responsiveness of the microbiota and the host, and logistic regression to predict responder vs. non-responder status, or increase vs. decrease of the health parameters. Our models, based on the abundance of several, mainly Firmicute species at baseline, predicted the responsiveness of the microbiota (AUC  =  0.77-1; predicted vs. observed correlation  =  0.67-0.88). Many of the predictive taxa showed a non-linear relationship with the responsiveness. The microbiota response associated with the change in serum cholesterol levels with an AUC of 0.96, highlighting the involvement of the intestinal microbiota in metabolic health. This proof-of-principle study introduces the first potential microbial biomarkers for dietary responsiveness in obese individuals with impaired metabolic health, and reveals the potential of microbiota signatures for personalized nutrition.

An ultrahigh-pressure supercritical fluid extraction method was optimized and applied to extract seed oil lipids from two moringa species, namely Moringa oleifera (MO) and Moringa peregrina (MP). A full-factorial design was used to investigate the direct and interaction influence of pressure and temperature in the range of 40 to 80 MPa and 40 to 70 °C, respectively, on the extracted amount of oil from crushed seeds. The results revealed that pressure has a significant positive influence on the extracted amount of oil. The best extraction condition using neat CO2 was found at 80 MPa and 57 °C, yielding 396 ± 23 and 529 ± 26 mg oil per gram of seeds for MO and MP, respectively. An extraction kinetics study revealed a mainly solubility-controlled extraction of oil, and 28 g of CO2 was required to extract 400 mg of oil per gram of seeds of MO using the developed method. Addition of ethanol to the sample prior to the extraction increased the proportion of extractable polar lipids as well as the total amount of extracted oil. The developed method increased the extracted amount of oil twofold compared to a reference method based on solvent sonication. The obtained oil consisted mainly of glycerolipids, sterol esters, and phospholipids. Phospholipids, campesterol, and stigmasterol ester concentrations were found to be higher in MO while cholesterol ester was more abundant in MP.

Ginkgo biloba L. has always been a popular area of research due to its various active ingredients and pharmacological effects. Ginkgo biloba is rich in ginkgo flavonoids, ginkgolides, and ginkgolic acid, with anti-inflammation, antioxidation, neuroprotection, anti-platelet agglutination, hypolipidemic effect, anti-cancer, and anti-radiation properties. There are many methods to extract and separate the active components of ginkgo. Among them, supercritical carbon dioxide fluid extraction (SFE-CO2) is known for its green, clean, and environment-friendly properties. In this paper, the pharmacological activities, the active components, and structures of different parts of ginkgo, the extraction methods of its effective ingredients, and the application of the SFE-CO2 method for the extraction and separation of active ingredients in Ginkgo biloba from leaves, seeds, pollen, and roots were reviewed, in order to make best use of ginkgo resources, and provide support and references for the development of SFE-CO2 of active components from Ginkgo biloba.