BAKUCHIOL

Bakuchiol (BAK), a meroterpene phenol abundant in the plant Psoralea corylifolia, is an emerging cosmeceutical agent with promising anti-aging, anti-inflammatory, and antibacterial properties. The trend for "clean" skincare products and search for anti-aging retinoid alternatives have poised BAK as a "must-have" ingredient in skincare. Our aim was to review the data for the applications of BAK in dermatology. This is a systematic review of PubMed. Thirty articles matched our search terms ["Bakuchiol" and "Dermatology"] or ["Bakuchiol" and "Skin"] of which one did not meet inclusion criteria, 16 were pre-clinical studies, seven clinical studies, three commentaries, two narrative reviews, and one report on adverse events. BAK has been mostly studied for its effects on photoaging, acne, and post-inflammatory hyperpigmentation (PIH), showing beneficial results comparable to those achieved by topical retinoids. While having no structural resemblance to retinoids, BAK can function as a retinol analog, through retinol-like regulation of gene expression. In in vivo studies, BAK was used alone or in combination with other products resulting in a significant reduction in photodamage, hyperpigmentation, wrinkle scores, and acne severity. Additionally, in vitro studies hinted at its anti-cancer properties by inhibiting epidermal growth factor induced neoplastic cell transformation. Also, demonstrated potential applications in psoriasis by normalizing keratinocyte activity and in pigmentary disorders through inhibition of melanogenesis. There was one adverse event case reported of contact dermatitis in the literature. Bakuchiol is a retinol alternative with anti-aging, antibacterial, and anti-inflammatory properties. Additional studies are warranted to better understand its applications in dermatology.

Natural compounds extracted from medicinal plants have recently gained attention in therapeutics as they are considered to have lower Toxicity and higher tolerability relative to chemically synthesized compounds. Bakuchiol from Psoralea corylifolia L. is one such compound; it is a type of meroterpene derived from the leaves and seeds of Psoralea corylifolia plants. Natural sources of bakuchiol have been used in traditional Chinese and Indian medicine for centuries due to its preventive benefits against tumors and inflammation. It plays a strong potential role as an antioxidant with impressive abilities to remove Reactive Oxygen Species (ROS). This review has focused on bakuchiol's extraction, therapeutic applications, and pharmacological benefits. A search strategy has been followed to retrieve the relevant newly published literature on the pharmacological benefits of bakuchiol. After an extensive study of the retrieved articles and maintaining the inclusion and exclusion criteria, 110 articles were finally selected for this review. Strong support of primary research on the protective effects via antitumorigenic, anti-inflammatory, antioxidative, antimicrobial, and antiviral activities are delineated. From ancient to modern life, medicinal plants have always been drawing the attention of human beings to alleviate ailments for a healthy and balanced lifestyle. This review is a comprehensive approach to highlighting bona fide essential pharmacological benefits and mechanisms underlying their therapeutic applications.

Bakuchiol is a topical cosmeceutical marketed as a retinoid alternative. Human clinical trial data on bakuchiol’s efficacy for the treatment of dermatologic conditions has not been thoroughly evaluated. To review human clinical trials using topical formulations containing bakuchiol in the treatment of facial skin disorders. A comprehensive electronic search of Cochrane Library, PubMed, EMBASE, and Web of Science was conducted on August 28, 2022, using the search terms “bakuchiol” and “UP256.” Study characteristics, measured outcomes, significant results, and stated limitations were extracted.  Results: Fifteen human clinical trials were analyzed. Dermatologic conditions treated included aging, acne, and post-inflammatory hyperpigmentation. Twelve trials were unblinded, open-label trials without a control group. Ten trials used a combination therapy containing bakuchiol. Four trials did not specify the dose or concentration of bakuchiol in treatment regimens. The heterogeneity of treatments, study designs, and measured outcomes makes meta-analysis unfeasible.  Conclusion: Trials lack methodologic rigor, which introduces a high risk of bias in reported outcomes. The use of combination topical formulations containing bakuchiol limits the comparison of bakuchiol’s efficacy with retinoids. Continued research with an improved trial design is needed.J Drugs Dermatol. 2024;23(4): doi:10.36849/JDD.7763.

Bakuchiol, is a principal bioactive component present in seeds of Psoralea corylifolia. It is one of the important monoterpene phenols and has been reported to possess extensive pharmacological properties like antioxidant, anti-inflammatory, anticancer, and hepatoprotective. Bakuchiol also plays a significant role in mental disorders. With an aim to explore the pharmacological potential of plant Psoralea corylifolia and its bioactive constituent, Bakuchiol; which may act as a lead to develop new molecular entities as drugs. A substantial literature survey was performed by scientific search engines like PubMed, Scopus,Web of Science, Science Direct, etc., and were reviewed with particular emphasis on their scientific impact and novelty. The study concludes that both Psoralea and bakuchiol possess innumerable pharmacological potentials to treat multiple disorders. Altogether, the promising pharmacological activities of bakuchiol may open new probes for therapeutic invention in the management of numerous ailments. Thus, the present review gives the erudition of bakuchiol as d foundation for further studies on the molecular mechanisms of BXXXD in the treatment of T2DM.

Bakuchiol is a phytochemical that has demonstrated cutaneous antiageing effects when applied topically. Early studies have suggested that bakuchiol is a functional analogue of topical retinoids, as both compounds have been shown to induce similar gene expression in the skin and lead to improvement of cutaneous photodamage. No in vivo studies have compared the two compounds for efficacy and side-effects. To compare the clinical efficacy and side-effect profiles of bakuchiol and retinol in improving common signs of cutaneous facial ageing. This was a randomized, double-blind, 12-week study in which 44 patients were asked to apply either bakuchiol 0·5% cream twice daily or retinol 0·5% cream daily. A facial photograph and analytical system was used to obtain and analyse high-resolution photographs of patients at 0, 4, 8 and 12 weeks. Patients also completed tolerability assessment questions to review side-effects. During study visits, a board-certified dermatologist, blinded to study group assignments, graded pigmentation and redness. Bakuchiol and retinol both significantly decreased wrinkle surface area and hyperpigmentation, with no statistical difference between the compounds. The retinol users reported more facial skin scaling and stinging. Our study demonstrates that bakuchiol is comparable with retinol in its ability to improve photoageing and is better tolerated than retinol. Bakuchiol is promising as a more tolerable alternative to retinol.

The study was undertaken to compare the skin care related activities of retinol and bakuchiol, a potential alternative to retinoids. Retinol is a pivotal regulator of differentiation and growth of developing as well as adult skin. Retinoic acid is the major physiologically active metabolite of retinol regulating gene expression through retinoic acid receptor - dependant and independent pathways. Comparative gene expression profiling of both substances in the EpiDerm FT full thickness skin substitute model was undertaken. Furthermore, type I, III and IV collagen, as well as aquaporin 3 expression was analyzed by ELISA and/or histochemistry in human dermal fibroblasts and/or Epiderm FT skin substitutes. Bakuchiol is a meroterpene phenol abundant in seeds and leaves of the plant Psoralea corylifolia. We present evidence that bakuchiol, having no structural resemblance to retinoids, can function as a functional analogue of retinol. Volcano plots showed great overall similarity of retinol and bakuchiol effects on the gene expression profile. This similarity was confirmed by the side-by-side comparison of the modulation of individual genes, as well as on the protein level by ELISA and histochemistry. Retinol-like functionality was further confirmed for the upregulation of types I and IV collagen in DNA microarray study and also show stimulation of type III collagen in the mature fibroblast model. Bakuchiol was also formulated into a finished skin care product and was tested in clinical case study by twice-a-day facial application. The results showed that, after 12 weeks treatment, significant improvement in lines and wrinkles, pigmentation, elasticity, firmness and overall reduction in photo-damage was observed, without usual retinol therapy-associated undesirable effects. Based on these data, we propose that bakuchiol can function as an anti-ageing compound through retinol-like regulation of gene expression.

Fructus Psoraleae (FP) is an herbal medicine widely used in East Asia. Nevertheless, numerous reports have documented its toxicity, including adverse reactions involving the liver, kidney, and skin. The underlying toxic components and mechanisms remain unclear, which severely limits its clinical application. This study aimed to identify potentially toxic components in FP and to further elucidate their mechanism of toxicity. Potentially toxic components in FP were rapidly screened using a zebrafish model. Potential hepatotoxicity-related targets and pathways were identified by integrating network toxicology with molecular docking, and the candidate targets were subsequently validated. Fifteen components of FP were evaluated for acute toxicity in zebrafish. Bakuchiol, bavachinin and corylifolinin - the three compounds exhibiting the highest c/LC 50 values - adversely affected normal hepatic function in zebrafish and induced oxidative stress responses. Bakuchiol was further identified as the component with the greatest hepatotoxic potential and was demonstrated to disrupt the homeostasis of the γ-aminobutyric acid (GABA) signalling system in the liver at 1, 5 and 10 μM by altering Cl - levels and upregulating GABA A receptor expression. Moreover, the GABA A receptor antagonist flumazenil was able to counteract bakuchiol-induced hepatotoxicity. Bakuchiol, by virtue of its high content and potent toxicity, is a potential hepatotoxic component of FP. It disrupts hepatic GABA system homeostasis by affecting Cl - channel and GABA A receptor expression.

With increasing life expectancy, the aging population, particularly in Asia, is expanding rapidly. Combined with intense year-round ultraviolet exposure, this accelerates skin aging. Male skin also exhibits distinct aging characteristics. This study aims to evaluate the efficacy and safety of the Genistein Plus Bakuchiol and Vitamins (GEN + ) product on male facial skin. A randomized, double-blind, placebo-controlled trial was conducted in men aged 45-65 years. Participants were assigned to receive either the GEN + or placebo (PLA) product in a 1:1 ratio and applied the product twice daily for 12 weeks. Facial skin assessments were performed at baseline and at weeks 4, 8, and 12. Evaluated parameters included skin color and consistency, spots, pigmentation, redness, acne, elasticity, hydration, barrier function, and wrinkles. Compliance and satisfaction were also monitored. Eighty male participants were enrolled (GEN + : n = 40; PLA: n = 40). After 12 weeks, the GEN + group demonstrated significant improvements in cheek skin lightening (MD = 0.55, 95% CI: 0.03 to 1.08, p = 0.04) and color consistency (MD = -0.56, 95% CI: -1.06 to -0.06, p = 0.03), along with a reduction in forehead spots (MD = -0.60, 95% CI: -1.15 to -0.06, p = 0.03). No significant differences were observed in melanin-, erythema-, or acne-related parameters. Skin property parameters did not differ significantly between groups, except for skin roughness. Adverse events were mild and self-resolving. While satisfaction scores did not differ significantly, the GEN + group reported higher scores across most domains. The GEN + product demonstrated promising improvements in male facial skin appearance, including skin lightening, color consistency, and spot reduction. The product was well-tolerated and offered a safe, targeted skincare solution for men. ClinicalTrials.gov identifier: TCTR20240312001.

Asian skin is more sensitive than Caucasian. When it comes to anti-aging treatments, some classic actives like Retinoids, are not friendly to Asian skin due to irritation issues. Therefore, it becomes more important to research new active ingredients to address the aging concern of sensitive skin. To clinically assess the anti-aging, skin soothing, barrier function improvement efficacy of one novel formulation containing supramolecular Bakuchiol and Terminalia chebula extract in Chinese sensitive skin population. A total of 34 sensitive skin subjects were enrolled in this clinical efficacy study. A routine consisting of twice daily topical applications of the test serum was followed for 28 days, evaluations were performed at baseline (D0) and after 8 h (T8h), 14 days (D14) and 28 days (D28) of using the regime. Objective skin assessment principles are skin sensitivity, barrier and aging. Sensitivity was evaluated by lactic acid sting test (LAST). Skin barrier evaluation, including transepidermal water loss (TEWL), a* value, and redness percentage. Aging evaluation, including wrinkle area, skin wrinkle (SEw), elasticity (R2), firmness (F4). As well as dermatologist evaluation of skin sensitivity and aging parameters and safety assessment. TEWL, a* value, redness percentage and mean score of LAST significantly reduced by 24.90%, 10.76%, 31.81%, 28.09%, respectively, and Dermatologist assessment significant decrease in facial redness, after 28 days of skin care treatment with the test serum. Wrinkle area, SEw, F4 significantly reduced by 16.06%, 16.71%, 25.60%, respectively, and Dermatologist assessment significant decrease in facial wrinkles, while R2 significantly increased by 23.04% after 28 days. No adverse events were reported. The serum containing supramolecular Bakuchiol and Terminalia chebula extract achieved skin rejuvenation in sensitive skin by improving sensitive and aging skin.

Skin ageing, hyperpigmentation, and texture are common dermatological concerns. Retinoids, including retinol, are widely used for their efficacy in treating these conditions. However, their side effects, such as irritation, often limit their use. Bakuchiol, a plant-derived retinoid alternative, has gained attention for its gentler profile, but its efficacy remains a subject of comparison with traditional retinoids. The aim of the present study was to evaluate the efficacy of a novel microalgae-derived bioretinoid (MBR) in comparison to retinol and bakuchiol in promoting skin regeneration, reducing ageing signs, and addressing hyperpigmentation. The effects of MBR were evaluated in vitro for cell proliferation, melanin production, and extracellular matrix modulation. Clinically, MBR was applied to assess improvements in skin texture, firmness, elasticity, and pigmentation compared with reference treatments. In vitro, MBR significantly outperformed both retinol and bakuchiol in cell proliferation, melanin reduction, and ECM modulation. In vivo, MBR improved skin texture, firmness, and pigmentation, showing results comparable to retinol. MBR also synergistically enhanced retinol's effects, improving hydration and reducing irritation. MBR is a promising alternative to traditional retinoids, offering enhanced efficacy in skin regeneration and pigmentation control with a more favourable safety profile, especially when combined with retinol. Le vieillissement cutané, l'hyperpigmentation et la texturation de la peau sont des problèmes dermatologiques courants. Les rétinoïdes, dont le rétinol, sont largement utilisés pour leur efficacité dans le traitement de ces affections. Cependant, leurs effets secondaires, tels que l'irritation, limitent souvent leur utilization. Le bakuchiol, une alternative d'origine végétale au rétinol, a attiré l'attention pour son profil plus doux, mais son efficacité reste sujette à comparaison avec les rétinoïdes traditionnels. Cette étude avait pour objectif d'évaluer l'efficacité d'un nouveau bio‐rétinoïde dérivé de microalgues (BRM) par rapport au rétinol et au bakuchiol dans la promotion de la régénération cutanée, la réduction des signes de vieillissement et le traitement de l'hyperpigmentation. MÉTHODES: Les effets du BRM ont été évalués in vitro pour la prolifération cellulaire, la production de mélanine et la modulation de la matrice extracellulaire. Sur le plan clinique, le BRM a été utilisé pour évaluer les améliorations de la texture, de la fermeté, de l'élasticité et de la pigmentation de la peau par rapport aux traitements de référence. RÉSULTATS: In vitro, le BRM a largement surpassé le rétinol et le bakuchiol en termes de prolifération cellulaire, de réduction de la mélanine et de modulation de la MEC. In vivo, le BRM a amélioré la texture, la fermeté et la pigmentation de la peau, avec des résultats comparables à ceux du rétinol. Le BRM a également renforcé de manière synergique les effets du rétinol, améliorant l'hydratation et réduisant l'irritation. Le BRM est une alternative prometteuse aux rétinoïdes traditionnels, offrant une efficacité accrue dans la régénération cutanée et le contrôle de la pigmentation, avec un profil d'innocuité plus favourable, en particulier lorsqu'il est associé au rétinol.

Retinoids are used in cosmetics as anti-aging ingredients, along with other substances. However, due to limitations in use (such as photodegradation), it seems necessary to look for retinoid alternatives to be applied in cosmetic products. Bakuchiol, a natural alternative of retinoids, isolated from Psolarea corylifolia , is one such compound. It has great cosmetic potential and its mechanism of action is not yet fully explored. From the point of view of the bioactive compound, it is also essential to develop a method for rapid quality control of cosmetic preparations containing bakuchiol. The aim of this study was to apply and compare methods for the quantification of bakuchiol in cosmetic products using UV-Vis, 1 H qNMR, and HPLC. The results show the possibility of using the 1 H NMR method in the routine quality control of cosmetics with bakuchiol because of its comparable results with HPLC analysis and significantly shorter analysis time.

Bakuchiol (BAK) is a natural bioactive agent described as a functional analogue of retinol that acts through the same cellular pathways. Its lipophilicity (log K o/w 6.1) and oily state at ambient temperature pose significant challenges in formulation development. This study investigated the use of different nanocarriers to develop primarily aqueous formulations of BAK and their ability to facilitate its cutaneous delivery. Micelles were prepared using solvent evaporation, microemulsions (ME) were formulated using the water titration method, and nanoemulsions (NE1 and NE2 - with and without oleic acid, respectively) were produced using ultrasonication. Optimized micelles formed using D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) and Poloxamer 407 demonstrated encapsulation efficiencies of 96.6 ± 3.2 % and 101.5 ± 0.3 %, with particle sizes of 28 nm (PDI 0.21) and 27 nm (PDI 0.092), respectively. NE2 had a higher encapsulation efficiency (106.8 ± 5.7 %) than either NE1 (90.2 ± 2.4 %) or ME (86.3 ± 4.6 %). The micro- and nanoemulsions exhibited larger sizes than the micelles (ME: 108 nm; NE1: 129. nm; NE2: 68 nm). Cutaneous delivery experiments demonstrated that NE1 and NE2 resulted in 3-4 fold higher BAK deposition than either the micelles or microemulsion; thus, oleic acid content was not determining BAK delivery. These findings suggest that the thermodynamic activity and molecular physicochemical properties are more important for skin delivery, than simply considering the size of the nanocarrier; which will not necessarily retain its structure upon contact with skin. Cutaneous biodistribution experiments to determine the spatial distribution of BAK confirmed that nanoemulsions effectively targeted the viable epidermis and dermis - key sites for BAK's biological effects, with concentrations 36-fold higher than the minimum effective concentration.

Bakuchiol (BK), a natural meroterpene isolated from Psoralea corylifolia, has gained significant attention as a functional cosmetic ingredient due to its antioxidant, anti-inflammatory, and antibacterial properties. However, its high hydrophobicity and chemical instability limit its practical application. In this study, we developed a robust and efficient delivery system for BK using polyglyceryl-10 laurate (PG10-L), an amphiphilic polymer, via a simple and scalable nanoprecipitation strategy. This approach helps address an important challenge in achieving stable long-term aqueous formulations of BK without relying on complex synthetic processes. The resulting BK-loaded nanoparticles (BK@NPs) exhibited a small particle size (< 200 nm), high encapsulation efficiency (≈ 99%), and remarkable colloidal stability for over 12 weeks. Notably, BK@NPs significantly enhanced biological efficacy compared to free BK, resulting in markedly improved antioxidant and antibacterial performance. Furthermore, the formulation demonstrated excellent cytocompatibility in NIH-3T3 murine fibroblasts along with effective suppression of intracellular reactive oxygen species (ROS). These findings highlight that the PG10-L-based nanoprecipitation strategy provides a robust and green platform to enhance the multifunctional potential of bakuchiol for advanced dermo-cosmetic applications.

Acne vulgaris is a prevalent inflammatory skin disorder influenced by sebaceous gland activity, hormonal regulation, and microbial proliferation. Dietary factors, including sweetening agents, may modulate acne pathophysiology, affecting sebum production, inflammatory responses, and the skin microbiome. This systematic review summarizes the effects of nutritive and non-nutritive sweeteners on acne-related markers, with a focus on Cutibacterium acnes activity and associated inflammatory pathways. Non-nutritive sweeteners such as mannitol and xylitol show potential in regulating acne pathogenesis and exhibiting antibacterial activity against C. acnes. Strategic combinations of sweeteners with bioactive compounds, such as mannitol with bakuchiol or Ginkgo biloba extract, and xylitol with propanediol and caprylic acid, further enhance anti-inflammatory and antimicrobial effects, offering a multifaceted approach to acne management. For nutritive sweeteners, experimental evidence suggests that glucose may enhance C. acnes biofilm susceptibility when combined with certain antibiotics. These findings emphasize the importance of careful selection and formulation of sweetening agents in dermatological interventions. Incorporating sweeteners, alone or in combination with bioactive compounds, could complement conventional acne therapies, reduce microbial proliferation, modulate inflammatory pathways, and support overall skin health. This review provides a scientific basis for dietary recommendations and the development of adjunctive acne treatments, highlighting sweetening agents as emerging functional modulators of acne pathogenesis.

Patients experiencing signs of pre-aging in their 20s and early 30s desire solutions including topical skincare and cosmetic procedures to help preserve skin quality and function. Methods: A series of studies was conducted to define, evaluate, and treat pre-aging skin. A total of 180 subjects were assessed to identify clinical features of pre-aging across all Fitzpatrick Skin Types (FSTs). In vitro studies compared the response of young and old dermal fibroblasts to ultraviolet A (UVA) exposure and retinoid treatment and evaluated the beneficial effects of acetyl dipeptide-31 amide, for pre-aging treatment. A 12-week clinical study of 46 patients (mild to moderate photoaging) was conducted to assess the efficacy and tolerability of a skincare regimen to treat pre-aging. Skin glycation index was assessed via UV-fluorescence and cross-polarized images. Clinical evaluation revealed that the earliest signs of skin aging were consistent across FSTs and included uneven skin tone, fine lines, and roughness. Aging turning points were seen in the mid-twenties in lighter FSTs and mid-thirties in darker FSTs. A reduction in elasticity began in the 20s and collagen content decreased progressively with age. Younger dermal fibroblasts produced more ROS after UVA exposure but were also more responsive to retinoids. Acetyl dipeptide-31 amide demonstrated anti-inflammatory and extracellular matrix (eg, collagen, elastin, etc) building effects. Clinical testing revealed an AM/PM regimen containing acetyl dipeptide-31 amide, sunscreen, and bakuchiol significantly improved early signs of pre-aging and reduced skin glycation index. These data support the need for and benefit of early intervention to protect and preserve youthful skin.  J Drugs Dermatol. 2025;24:5(Suppl 2):s4-14.&nbsp.