베타-시토스테롤 (탈모 · DHT 완충)

PURPOSE: This research aimed to investigate the protective role as well as molecular mechanisms of Rehmanniae Radix Praeparata and its bioactive compound β-sitosterol in preventing CIHL. METHODS: Network pharmacology and bioinformatic analyses were used to identify the pharmacologically active constituents of Rehmanniae Radix Praeparata and predict their potential molecular targets. The influence of β-sitosterol on hair cell damage, apoptosis, reactive oxygen species (ROS) levels, and target protein expression were evaluated in vitro as well as in vivo. RESULTS: The primary active constituents of Rehmanniae Radix Praeparata were β-sitosterol and stigmasterol. They shared 50 potential targets with CIHL, with MAPK3, SRC, and ESR1 as the top three. Molecular docking combined with dynamics simulations demonstrated strong binding and stable complex formation between β-sitosterol and MAPK3. In vitro, β-sitosterol mitigated cisplatin-induced hair cell death, reduced ROS levels, and restored phosphorylated MAPK3. In vivo, it enhanced hearing, decreased hair cell loss, and partially restored phosphorylated MAPK3 in the cochleae of cisplatin-treat

This systematic review assessed the potential effectiveness and safety of Serenoa repens (saw palmetto) for benign prostatic disorders, mainly benign prostatic hyperplasia and associated lower urinary tract symptoms. Following PRISMA guidance (PROSPERO: CRD420251032255), we searched PubMed, Cochrane and ScienceDirect for human studies from January 2020 to May 2025. Sixteen studies (>3000 participants) met criteria, including randomized trials, observational cohorts, a post hoc analysis, an open-label comparative study and a pharmacovigilance analysis. Overall, S. repens was associated with improvements in symptom severity (International Prostate Symptom Score) in several trials, with variable effects on urinary flow, post-void residual volume, and patient-reported quality of life. Signals of benefit appeared more consistently with hexanic lipidosterolic extracts and β-sitosterol-enriched preparations, and some real-world and head-to-head comparisons suggested outcomes comparable to alpha-blockers with fewer adverse events. Combination therapy, especially with the addition of alpha-blockers, showed larger symptom reductions in select populations, particularly with more pronounced baseline symptoms or prostatic inflammation. However, heterogeneity in extract formulations, dosing, study design, and outcome reporting limited cross-study comparability. Safety findings were generally favourable, with mostly mild gastrointestinal events and fewer sexual adverse effects than reported for conventional pharmacotherapies. Taken together, recent evidence supports S. repens as a potentially useful, well-tolerated option for benign prostatic hyperplasia-related symptoms - especially in certain formulations and as part of combination strategies -

Studies suggest that vegetarians and Asians have lower mortality rates from prostate cancer compared to men who follow a Western diet. β-sitosterol, a key compound of plant-based diets, has been found to induce significant changes in the ultrasonic structure of the prostatic adenomas, making it a promising candidate for further prostate cancer research. Consequently, we investigated the potential of β-sitosterol and the synthetic derivative 2 as potent inhibitors of androgen synthesis, a critical process for the growth and survival of prostate tumor LNCaP cells. Solubilized LNCaP microsomes were used as a source of SRD5A1 and AKR1C3 to monitor androgen synthesis from labeled androstenedione, both in the presence and absence of β-sitosterol or 2. Furthermore, the effect of these steroids on LNCaP viability was determined using the MTT method. Our findings revealed significant insights into the androgen synthesis pathways in LNCaP cells. The most efficient metabolic route for dihydrotestosterone formation was the conversion of androstenedione to 5α-androstanedione rather than from testosterone in LNCaP. This conclusion is supported by the Vmax values for 5α-androstanedione formation (271.05 ± 5.0 ng/mg protein/min) and the Vmax of testosterone formation (80.1 ± 8.0 ng/mg protein/min). Both β-sitosterol and 2 demonstrated substantial inhibitory effects of these enzymes for dihydrotestosterone formation and significantly reduced cell viability, highlighting their therapeutic potential. These findings enhance our understanding of the inhibitory effects of β-sitosterol and 2 on LNCaP cells and suggest their promising application in the

Steroidal 5α-reductase type 2 (S5αR2) is a key enzyme involved in the conversion of testosterone (TST) to dihydrotestosterone (DHT), a crucial process in the development of benign prostatic hyperplasia (BPH). Phytosterols (PSs), natural plant-derived compounds, have been proposed as potential inhibitors of S5αR2, but studies on their efficacy are limited. This study evaluates the inhibitory effects of three PSs (β-sitosterol, stigmasterol, and campesterol) on S5αR2 activity using a combined in vitro and in silico approach. The inhibitory activity of the respective PSs was assessed in vitro, by measuring TST and DHT, while molecular docking and dynamics explored PS interactions with S5αR2's active site. The in vitro tests indicated significantly higher IC50 values (β-sitosterol, 3.24 ± 0.32 µM; stigmasterol, 31.89 ± 4.26 µM; and campesterol, 15.75 ± 5.56 µM) for PSs compared to dutasteride (4.88 × 10-3 ± 0.33 µM), suggesting a lower efficiency in inhibiting S5αR2. The in silico studies confirmed these observations, explained by the lower binding affinity identified for PSs to the enzyme's active site in the molecular

ETHNOPHARMACOLOGICAL RELEVANCE: Benign prostatic hyperplasia (BPH), characterized by prostate enlargement due to cell proliferation, is a common urinary disorder in men over 50, manifesting as lower urinary tract symptoms (LUTS). Currently, several therapeutic options are accessible for treating BPH, including medication therapy, surgery and watchful waiting. Conventional drugs such as finasteride and dutasteride are used as 5α-reductase inhibitors for the treatment of BPH. However long-term use of these drugs is restricted due to their unpleasant side effects. Despite the range of available medical therapies, the effective treatment against BPH is still inadequate. Certain therapeutic plants and their phytochemicals have the aforementioned goals and work by regulating this enzyme. AIM OF THE STUDY: This review aims to provide a comprehensive insight to advancements in diagnosis of BPH, modern treatment methods and the significance of ethnobotanically relevant medicinal plants as alternative therapeutics for managing BPH. MATERIAL AND METHODS: A thorough and systematic literature search was performed using electronic databases and search engines suc

PURPOSE: Androgenetic alopecia (AGA) is the most common type of hair loss in humans, affecting self-esteem and emotional well-being. This study aimed to assess the safety and efficacy of VISPOTM, a standardized saw palmetto oil (2-3% β-sitosterol), in subjects with mild-to-moderate AGA. METHODS: In a double-blind, placebo-controlled, four-arm clinical study, 80 healthy male and female subjects aged 18-50 years were randomly allocated (1:1:1:1) to receive either 400 mg capsules of VISPO or 5 mL of a topical formulation containing 20% VISPO or the respective placebo once daily for 16 weeks. The primary endpoints included hair count (hair comb and hair pull tests) and the self-assessment of perceived efficacy. Objective evaluation was performed using the global photographic assessment score. Hair density, thickness, and anagen/telogen ratio were evaluated using phototrichogram analysis. RESULTS: At the end of the study, oral and topical formulations of VISPO reduced hair fall by up to 29% (p<0.001) and 22.19% (p<0.01) from the baseline, respectively. Hair density increased by 5.17% and 7.61% in the oral and topical VISPO groups, respectively (p<0.001). In addition, oral ingestion of VISPO resulted in a marked reduction in serum dihydrotestosterone (DHT) levels in the subjects compared to placebo (p<0.001). However, the effect of the VISPO formulati

Lower urinary tract symptoms from benign prostatic hyperplasia affect 25% of U.S. men, nearly one-half of whom have at least moderate symptoms. Sedentary lifestyle, hypertension, and diabetes mellitus increase risk of symptoms. Evaluation is focused on determining severity of symptoms and therapy to improve symptoms. Rectal examination has limited accuracy in evaluating prostate size. Transrectal ultrasonography is preferred to verify size when starting 5-alpha reductase therapy or considering surgery. Serum prostate-specific antigen testing is not recommended in routine evaluation of lower urinary tract symptoms, and shared decision-making should be used for cancer screening decisions. The International Prostate Symptom Score is the best way to track symptoms. Self-management methods, including limiting evening fluid intake, reducing caffeine and alcohol intake, toilet and bladder training, pelvic floor exercises, and mindfulness techniques, can improve symptoms. Although saw palmetto is not effective, the herbal treatments Pygeum africanum and beta-sitosterol may be effective. Primary medical treatment involves alpha blockers or phosphodiesterase-5 inhibitors. Alpha blockers offer rapid benefit and can be used for acute urinary retention. Combining alpha blockers and phosphodiesterase-5 inhibitors is not beneficial. For uncontrolled symptoms, 5-alpha reductase inhibitors should be started if the prostate volume is 30 mL or greater by ultrasonography. 5-Alpha reductase inhibitors take up to one year to be fully beneficial and are more effective when taken with alpha blockers. Only 1% of patients with lower urinary tract symptoms require surgery. Although transurethral resection of the prostate improves symptoms, many less invasive options with varying effectiveness can be considered.

The use of synthetic medication for treating alopecia is restricted because of systemic exposure and related negative effects. Beta-sitosterol (β-ST), a natural chemical, has lately been studied for its potential to promote hair development. The cubosomes with dissolving microneedles (CUBs-MND) created in this study may be a useful starting point for the creation of a sophisticated dermal delivery system for β-ST. Cubosomes (CUBs) were prepared by the emulsification method, using glyceryl monooleate (GMO) as a lipid polymer. CUBs were loaded with dissolving microneedles (MND) fabricated with HA and a PVP-K90 matrix. An ex vivo skin permeation study and an in vivo hair growth efficacy test of β-ST were performed with both CUB and CUB-MND. The average particle size of the CUBs was determined to be 173.67 ± 0.52 nm, with a low polydispersity index (0.3) and a high zeta potential value that prevents the aggregate formation of dispersed particles. When compared to CUBs alone, CUBs-MND displayed higher permeating levels of β-ST at all-time points. In the animals from the CUB-MND group, significant hair development was observed. According to the results of the current investigati

Plant-derived 5 α-reductase inhibitors, such as β-sitosterol and phytosterol glycosides, have been used to treat androgenic alopecia, but their oral absolute bioavailability is poor. This study aimed to develop a transdermal drug delivery system of β-sitosterol (BS) using a nanostructured lipid carrier (NLC) incorporated into polymeric microneedles (MN). Using a high-speed homogenization method, NLC was formulated variables were optimized by Box-Behnken statistical design. The optimized formulation of BS-loaded NLCs was incorporated into the chitosan-based MNs to prepare NLC-loaded polymeric MNs (NLC-MNs) and evaluated using testosterone induced alopecia rats. The cumulative amount of β-sitosterol associated with NLC- MN which penetrated the rat skin in-vitro was 3612.27 ± 120.81 μg/cm2, while from the NLC preparation was 2402.35 ± 162.5 μg/cm2. The steady state flux (Jss) of NLC-MN was significantly higher than that of the optimized NLC formulation (P < 0.05). Anagen/telogen ratio was significantly affected by NLC and NLC-MN, which was 2.22 ± 0.34, 1.24 ± 0.18 respectively compared to 0.26 ± 0.08 for animal group treated with testosterone. The reversal of androgen-i

The application of the seed oil of Prunus mira Koehne (Tibetan name ཁམབུ།), a plant belonging to the Rosaceae family, for the treatment of alopecia has been recorded in Jingzhu Materia Medica (ཤེལ་གོང་ཤེལ་ཕྲེང་།) (the classic of Tibetan medicine) and Dictionary of Chinese Ethnic Medicine. This study aims to reveal the effective components and mechanism of hair growth promotion in the kernel of Prunus mira Koehne. Network pharmacology was used to predict the mechanism of action and effective components in the treatment of the kernel of Prunus mira Koehne. The contents of amygdalin in 12 batches of the kernel of Prunus mira Koehne were determined by HPLC. An animal model of the depilation of KM mice induced by sodium sulfide was created, and five effective components that promoted hair growth were initially screened. In the study of the effectiveness and mechanism of action, KM and C57BL/6 mice are selected as experimental objects, three screening tests for active components of the kernel of P. mira are performed, and three effective components are screened out from the eight components. HE staining was used to detect the number of hair follicles and the thickness of the dermis. RT-PCR and immunohistochemistry were used to evaluate the influence of the expression of indicators in the Wnt/β-catenin signaling pathway in skin, including β-catenin, GSK-3β, and mRNA and protein expression levels of Cyclin D 1 and LEF 1. The network pharmacology study showed 12 signaling pathways involving 25 targets in the treatment of alopecia by the kernel of Prunus mira Koehne. vitamin E (3.125 mg/cm2/d), β-sitosterol (0.061