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Molecules (Basel, Switzerland) Jun 2022(L.) Britton, an important pharmaceutical and nutraceutical crop, is widely cultivated in East Asian countries. In this review, we present the latest research findings... (Review)
Review
(L.) Britton, an important pharmaceutical and nutraceutical crop, is widely cultivated in East Asian countries. In this review, we present the latest research findings on the phytochemistry and pharmacological activities of . Different databases, including PubMed, Scopus, CNKI, Agricola, Scifinder, Embase, ScienceDirect, DOAJ, and Web of Science, were searched to present the best review. In this review, we clearly represent the active constituents responsible for each and every pharmacological activity, plausible mechanism of action, and maximum inhibitory concentrations, as well as IC values. Approximately 400 different bioactive compounds, including alkaloids, terpenoids, quinines, phenylpropanoids, polyphenolic compounds, flavonoids, coumarins, anthocyanins, carotenoids, neolignans, fatty acids, polycosanols, tocopherols, and sitosterols, have been reported in the leaves, seeds, roots, and aerial parts of . The bioactive constituents of exhibited different enzyme-inhibition properties, including antihyaluronidase effects and aldose reductase inhibitory, α-glucosidase inhibitory, xanthine oxidase inhibitory, and tyrosinase inhibitory properties. showed strong anti-inflammatory, antidepressant, anti-spasmodic, anticancer, antioxidant, antimicrobial, insecticidal, neuroprotective, and hepatoprotective effects. Hence, the active constituents of used in the treatment of diabetes and diabetic complications (retinopathy, neuropathy, and nephropathy), prevention of hyperuricemia in gout patients, hyper pigmentation, allergic conditions, skin inflammation, skin allergy, atopic dermatitis, periodontosis, androgenic alopecia, gastric inflammation, oesophagitis, carcinogenesis, cardiovascular, Alzheimer's, Parkinson's, and cerebral ischemic disorders. Furthermore, we revealed the most active constituents and possible mechanisms of the pharmacological properties of .
Topics: Anthocyanins; Humans; Inflammation; Perilla frutescens; Plant Leaves; Xanthine Oxidase
PubMed: 35684514
DOI: 10.3390/molecules27113578 -
Biomedicine & Pharmacotherapy =... Nov 2020Phytosterols are bioactive compounds that are naturally present in plant cell membranes with chemical structure similar to the mammalian cell- derived cholesterol. They... (Review)
Review
Phytosterols are bioactive compounds that are naturally present in plant cell membranes with chemical structure similar to the mammalian cell- derived cholesterol. They are highly present in lipid-rich plant foods such as nuts, seed, legumes and olive oil. Among various phytosterols, β-sitosterol (SIT) is the major compound, found plentiful in plants. It has been evidenced in many in-vitro and in-vivo studies that SIT possesses various biological actions such as anxiolytic & sedative effects, analgesic, immunomodulatory, antimicrobial, anticancer, anti - inflammatory, lipid lowering effect, hepatoprotective, protective effect against NAFLD and respiratory diseases, wound healing effect, antioxidant and anti-diabetic activities. In this review, in order to compile the sources, characterization, biosynthesis, pharmacokinetics, antioxidant and anti-diabetic activities of SIT, classical and online-literature were studied which includes the electronic search (Sci Finder, Pubmed, Google Scholar, Scopus, and Web of Science etc) and books on photochemistry. The experimental studies on SIT gives a clear evidence that the potential phytosterol can be used as supplements to fight against life threatening diseases. High potential of this compound, classifies it as the notable drug of the future. Therefore, immense researches regarding its action at molecular level on life threatening diseases in humans are highly endorsed.
Topics: Animals; Antioxidants; Diabetes Mellitus; Dietary Supplements; Humans; Sitosterols
PubMed: 32882583
DOI: 10.1016/j.biopha.2020.110702 -
Food Science and Biotechnology Dec 2019Benign prostatic hyperplasia (BPH) is a noncancerous growth of the prostate. BPH commonly occurs in elderly men. Lower urinary tract symptoms (LUTS) secondary to BPH... (Review)
Review
Benign prostatic hyperplasia (BPH) is a noncancerous growth of the prostate. BPH commonly occurs in elderly men. Lower urinary tract symptoms (LUTS) secondary to BPH (LUTS/BPH) have significant impacts on their health. Saw palmetto () extract (SPE) has been evaluated for its effectiveness in improvement of LUTS/BPH at preclinical and clinical levels. Potential mechanisms of actions include anti-androgenic, pro-apoptotic, and anti-inflammatory effects. However, SPE efficacy was inconsistent, at least partly due to a lack of a standardized SPE formula. A hexane extract (free fatty acids, > 80%) provided more consistent results. Free fatty acids (lauric acid) were effective in inhibition of 5α-reductase, and phytosterol (β-sitosterol) reduced prostatic inflammation. Multiple actions derived from different constituents may contribute to SPE efficacy. Evaluation of the clinical relevance of these bioactive components is required for standardization of SPE, thereby enabling consistent efficacy and recommendations for the use in the prevention and treatment of BPH.
PubMed: 31807332
DOI: 10.1007/s10068-019-00605-9 -
ACS Nano Sep 2022Despite lipid nanoparticles' (LNPs) success in the effective and safe delivery of mRNA vaccines, an inhalation-based mRNA therapy for lung diseases remains challenging....
Despite lipid nanoparticles' (LNPs) success in the effective and safe delivery of mRNA vaccines, an inhalation-based mRNA therapy for lung diseases remains challenging. LNPs tend to disintegrate due to shear stress during aerosolization, leading to ineffective delivery. Therefore, LNPs need to remain stable through the process of nebulization and mucus penetration, yet labile enough for endosomal escape. To meet these opposing needs, we utilized PEG lipid to enhance the surficial stability of LNPs with the inclusion of a cholesterol analog, β-sitosterol, to improve endosomal escape. Increased PEG concentrations in LNPs enhanced the shear resistance and mucus penetration, while β-sitosterol provided LNPs with a polyhedral shape, facilitating endosomal escape. The optimized LNPs exhibited a uniform particle distribution, a polyhedral morphology, and a rapid mucosal diffusion with enhanced gene transfection. Inhaled LNPs led to localized protein production in the mouse lung without pulmonary or systemic toxicity. Repeated administration of these LNPs led to sustained protein production in the lungs. Lastly, mRNA encoding the cystic fibrosis transmembrane conductance regulator (CFTR) was delivered after nebulization to a CFTR-deficient animal model, resulting in the pulmonary expression of this therapeutic protein. This study demonstrated the rational design approach for clinical translation of inhalable LNP-based mRNA therapies.
Topics: Animals; Cholesterol; Cystic Fibrosis Transmembrane Conductance Regulator; Lipids; Liposomes; Mice; Nanoparticles; RNA, Messenger
PubMed: 36038136
DOI: 10.1021/acsnano.2c05647 -
Nutrients Jul 2022Sarcopenia refers to a decline in muscle mass and strength with age, causing significant impairment in the ability to carry out normal daily functions and increased risk...
Sarcopenia refers to a decline in muscle mass and strength with age, causing significant impairment in the ability to carry out normal daily functions and increased risk of falls and fractures, eventually leading to loss of independence. Maintaining protein homeostasis is an important factor in preventing muscle loss, and the decrease in muscle mass is caused by an imbalance between anabolism and catabolism of muscle proteins. Although β-sitosterol has various effects such as anti-inflammatory, protective effect against nonalcoholic fatty liver disease (NAFLD), antioxidant, and antidiabetic activity, the mechanism of β-sitosterol effect on the catabolic pathway was not well known. β-sitosterol was assessed in vitro and in vivo using a dexamethasone-induced muscle atrophy mice model and C2C12 myoblasts. β-sitosterol protected mice from dexamethasone-induced muscle mass loss. The thickness of gastrocnemius muscle myofibers was increased in dexamethasone with the β-sitosterol treatment group (DS). Grip strength and creatine kinase (CK) activity were also recovered when β-sitosterol was treated. The muscle loss inhibitory efficacy of β-sitosterol in dexamethasone-induced muscle atrophy in C2C12 myotube was also verified in C2C12 myoblast. β-sitosterol also recovered the width of myotubes. The protein expression of muscle atrophy F-box (MAFbx) was increased in dexamethasone-treated animal models and C2C12 myoblast, but it was reduced when β-sitosterol was treated. MuRF1 also showed similar results to MAFbx in the mRNA level of C2C12 myotubes. In addition, in the gastrocnemius and tibialis anterior muscles of mouse models, Forkhead Box O1 (FoxO1) protein was increased in the dexamethasone-treated group (Dexa) compared with the control group and reduced in the DS group. Therefore, β-sitosterol would be a potential treatment agent for aging sarcopenia.
Topics: Animals; Dexamethasone; Disease Models, Animal; Forkhead Box Protein O1; Forkhead Transcription Factors; Mice; Muscle Fibers, Skeletal; Muscle, Skeletal; Muscular Atrophy; Sarcopenia; Sitosterols; Ubiquitin-Protein Ligases
PubMed: 35889851
DOI: 10.3390/nu14142894 -
BMC Urology Jul 2020The present clinical trial was conducted to evaluate the efficacy and tolerability of a standardized saw palmetto oil containing 3% β-sitosterol in the treatment of... (Comparative Study)
Comparative Study Randomized Controlled Trial
A double blind, placebo-controlled randomized comparative study on the efficacy of phytosterol-enriched and conventional saw palmetto oil in mitigating benign prostate hyperplasia and androgen deficiency.
BACKGROUND
The present clinical trial was conducted to evaluate the efficacy and tolerability of a standardized saw palmetto oil containing 3% β-sitosterol in the treatment of benign prostate hyperplasia (BPH) and androgen deficiency.
METHODS
Subjects aged 40-65 years with symptomatic BPH were randomized to 12-week double-blind treatment with 500 mg doses of β-sitosterol enriched saw palmetto oil, conventional saw palmetto oil and placebo orally in the form of capsules (n = 33 in each group). BPH severity was determined using the International Prostate Symptom Score (IPSS), uroflowmetry, serum measurement of prostate specific antigen (PSA), testosterone and 5α-reductase. During the trial, the androgen deficiency was evaluated using Aging Male Symptoms (AMS) scale, the Androgen Deficiency in the Aging Male (ADAM) questionnaire, serum levels of free testosterone.
RESULTS
Subjects treated with β-sitosterol enriched saw palmetto oil showed significant decrease in IPSS, AMS and ADAM scores along with reduced postvoiding residual volume (p < 0.001), PSA (p < 0.01) and 5α-reductase from baseline to end of 12-week treatment as compared to placebo. There was also a significant increment in the maximum and average urine flow rate (p < 0.001), and serum free testosterone level of subjects treated with enriched saw palmetto oil as compared to placebo.
CONCLUSION
This study demonstrates the efficacy of β-sitosterol enriched saw palmetto oil superior to conventional oil thus extending the scope of effective BPH and androgen deficiency treatment with improved quality of life through the intake of functional ingredients.
TRIAL REGISTRATION
CTRI/2018/12/016724 dated 19/12/2018 prospectively registered. URL: http://ctri.nic.in/Clinicaltrials/advsearch.php.
Topics: Adult; Aged; Androgens; Double-Blind Method; Humans; Male; Middle Aged; Phytosterols; Phytotherapy; Plant Extracts; Plant Oils; Prostatic Hyperplasia; Serenoa; Sitosterols; Treatment Outcome; Urological Agents
PubMed: 32620155
DOI: 10.1186/s12894-020-00648-9 -
Journal of Food Science and Technology Jul 2020Plants consist of triterpenoids such as phytosterols (PT) (CHO) with steroidal nuclei, including sitosterol, stigmasterol, brassicasterol and campesterol. They are... (Review)
Review
Plants consist of triterpenoids such as phytosterols (PT) (CHO) with steroidal nuclei, including sitosterol, stigmasterol, brassicasterol and campesterol. They are hydrophobic but soluble in alcohol and other organic solvents and are isolated from industrial waste deodorizer distillates of various edible oil industries. They exist as free PT or their ester derivatives in soybean, rice, wheat, oat, cottonseed and corn fiber, and other cereals and grains. Conventional isolation techniques such as solvent extraction, distillation, evaporative fractionation, saponification and chemical esterification are employed for isolation and purification of PT. The present article reviews the various advanced separation techniques like solvent crystallization, supercritical fluid extraction, high speed counter-current chromatography and enzymatic process as strategic methods to isolate and purify sterols.
PubMed: 32549589
DOI: 10.1007/s13197-019-04209-3 -
International Journal of Molecular... Nov 2021Phytosterols constitute a class of natural products that are an important component of diet and have vast applications in foods, cosmetics, and herbal medicines. With... (Review)
Review
Phytosterols constitute a class of natural products that are an important component of diet and have vast applications in foods, cosmetics, and herbal medicines. With many and diverse isolated structures in nature, they exhibit a broad range of biological and pharmacological activities. Among over 200 types of phytosterols, stigmasterol and β-sitosterol were ubiquitous in many plant species, exhibiting important aspects of activities related to neurodegenerative diseases. Hence, this mini-review presented an overview of the reported studies on selected phytosterols related to neurodegenerative diseases. It covered the major phytosterols based on biosynthetic considerations, including other phytosterols with significant in vitro and in vivo biological activities.
Topics: Brain; Humans; Molecular Structure; Neurodegenerative Diseases; Neuroprotective Agents; Phytosterols; Phytotherapy; Plants, Medicinal; Sitosterols; Stigmasterol
PubMed: 34830148
DOI: 10.3390/ijms222212255 -
Frontiers in Pharmacology 2020Phytosterols (PSs) are plant-originated steroids. Over 250 PSs have been isolated, and each plant species contains a characteristic phytosterol composition. A wide... (Review)
Review
Phytosterols (PSs) are plant-originated steroids. Over 250 PSs have been isolated, and each plant species contains a characteristic phytosterol composition. A wide number of studies have reported remarkable pharmacological effects of PSs, acting as chemopreventive, anti-inflammatory, antioxidant, antidiabetic, and antiatherosclerotic agents. However, PS bioavailability is a key issue, as it can be influenced by several factors (type, source, processing, preparation, delivery method, food matrix, dose, time of administration into the body, and genetic factors), and the existence of a close relationship between their chemical structures (e.g., saturation degree and side-chain length) and low absorption rates has been stated. In this sense, the present review intends to provide in-depth data on PS therapeutic potential for human health, also emphasizing their preclinical effects and bioavailability-related issues.
PubMed: 33519459
DOI: 10.3389/fphar.2020.599959