Chronic disease management via modulation of cellular signaling by phytoestrogen Bavachin.

The emergence of chronic diseases, particularly cancers, cardiovascular, and bone disorders, presents a formidable challenge, as currently available synthetic drugs often result in significant side effects and incur higher costs. Phytoestrogen Bavachin, present in the Psoralea corylifolia L. plant, represents structural and functional similarity to mammalian estrogen and has recently attracted researchers for its medicinal properties. This review spotlighted the extraction methods, bioavailability and therapeutic interventions of Bavachin against diseases. Bavachin exerted estrogenic properties, demonstrating the ability to bind to estrogen receptors (ERs), mimicking the actions of human estrogen and initiating estrogen-responsive pathways. Bavachin delivered potent therapeutic ventures in abrogating chronic diseases, including cancer, neuronal, bone, cardiovascular, skin, lung, and liver disorders via targeting signaling transductions, managing calcium signaling, immune regulation, inflammation, apoptosis, and oxidative stress. In-silico analysis, including Gene ontology and pathway enrichment analysis, retrieved molecular targets of Bavachin, majorly cytochrome c oxidase (COX), nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), Nucleotide-binding domain, leucine-rich-containing family, pyrin domain-containing-3 (NLRP3), and ER, hypothesizing Bavachin's cellular mechanism in preventing crucial health ailments. Limitations of Bavachin were also summarized, evidenced by hepatotoxicity at specific dosage levels. In conclusion, Bavachin showed promising therapeutic efficacy in suppressing chronic diseases and can be considered as an adequate replacement for hormone replacement therapy, necessitating further investigations on its effectiveness, safety, and clinical outcomes.

Promotion of Raf-1/ASK1 complex formation by corylin inhibits cell apoptosis in myocardial ischemia/reperfusion injury.

Effective treatment of myocardial ischemia-reperfusion (MIR) injury remains an unmet clinical need. Cardiomyocyte apoptosis is common at this stage and poses a significant risk. Corylin, a flavonoid compound extracted from Psoralea corylifolia L., has been shown to have anti-inflammatory, anticancer, and antiatherosclerotic properties. However, whether and how corylin affects MIR injury remain unclear. In this study, we explored the mechanism of corylin as a potent therapeutic agent for MI/R injury, using a left anterior descending (LAD) coronary artery ligation and oxygen-glucose deprivation and reperfusion (OGD/R) model in vivo and in vitro. TUNEL, Annexin-V/PI double staining,Ki67 immunohistochemistry, western blot analysis, and immunofluorescence were used to validate cell apoptosis level and Raf-1/ASK1 complex activity. The interaction between corylin and Raf-1/ASK1 complex was detected using molecular docking, corylin-Raf-1 binding assays, and coimmunoprecipitation (Co-IP). Moreover, TTC staining, echocardiography, HE staining, Masson trichrome staining and serological testing were performed to assess the cardioprotective effects of corylin in vivo. These findings showed that corylin reduces MIR injury-induced cardiomyocyte apoptosis and improves cardiac function. Mechanistically, corylin can interact with Raf-1 and promote the formation of the Raf-1/ASK1 complex, thus inhibiting cardiomyocyte apoptosis. In conclusion, our results demonstrate that corylin ameliorated cardiac dysfunction after MIR injury by reducing myocardial apoptosis.

Bavachinin, a main compound of Psoraleae Fructus, facilitates GSDMD-mediated pyroptosis and causes hepatotoxicity in mice.

Psoraleae Fructus (PF, Psoralea corylifolia L.), a traditional medicine with a long history of application, is widely used clinically for the treatment of various diseases. However, the reports of PF-related adverse reactions, such as hepatotoxicity, phototoxic dermatitis, and allergy, are increasing year by year, with liver injury being the mostly common. Our previous studies have demonstrated that PF and its preparations can cause liver injury in lipopolysaccharide (LPS)-mediated susceptibility mouse model, but the mechanism of PF-related liver injury is unclear. In this study, we showed that PF and bavachinin, a major component of PF, can directly induce the expression of caspase-1 and interleukin-1ß (IL-1ß), indicating that PF and bavachinin can directly triggered the activation of inflammasome. Furthermore, pretreatment with NLR family pyrin domain-containing 3 (NLRP3), NLR family CARD domain containing 4 (NLRC4) or absent in melanoma 2 (AIM2) inflammasome inhibitors, containing MCC950, ODN TTAGGG (ODN) and carnosol, all significantly reversed bavachinin-induced inflammasome activation. Mechanistically, bavachinin dose-dependently promote Gasdermin D (GSDMD) post-shear activation and then induce mitochondrial reactive oxygen species (mtROS) production and this effect is markedly inhibited by pretreatment with N-Acetylcysteine amide (NAC). In addition, combination treatment of LPS and bavachinin significantly induced liver injury in mice, but not LPS or bavachinin alone, and transcriptome analysis further validated these results. Thus, PF and bavachinin can induce the activation of inflammasome by promoting GSDMD cleavage and cause hepatotoxicity in mice. Therefore, PF, bavachinin, and PF-related preparations should be avoided in patients with inflammasome activation-associated diseases.

The flavonoids from the fruits of Psoralea corylifolia and their potential in inhibiting metastasis of human non-small cell lung cancers.

Nineteen flavonoids were isolated from the fruits of Psoralea corylifolia L., including a novel flavanol (3) and three novel isoflavones (12-14). Their chemical structures were unequivocally determined through comprehensive spectral data analysis. The anti-proliferative effect of the isolated flavonoids was assessed in vitro using the MTT assay. Molecular docking and ELISA were employed to determine the inhibitory effects of the active compounds on ALK5. Isobavachalcone was found to inhibit TGF-ß1 induced EMT in A549 cells by Wound healing assay and Transwell chamber assay. Immunofluorescence assay and Western blot assay showed that IBC could inhibit cytoskeleton rearrangement, reduce the phosphorylation of ALK5, ERK, and Smad, down-regulate Snail expression, and up-regulate E-cadherin expression in TGF-ß1 induced A549 cells, thereby exerting the potential inhibitory effects on epithelial-mesenchymal transition (EMT) process in A549 cells. The findings presented herein establish a fundamental basis for investigating the anti-proliferative and anti-metastatic properties of psoralen flavonoids in human non-small cell lung cancer.

Past, present and future of Psoralea glandulosa Linn, Chilean medicinal plant, an inexhaustible resource: a literature review / Pasado, presente y futuro de Psoralea glandulosa Linn, planta medicinal chilena fuente inagotable de recursos: una revisión de la literatura

Culén is the popular term used in Chile for the only endemic species of the Fabaceae family, Psoralea glandulosaLinn. It is one of the most widely used medicinal plants in Chile and in some regions of South America, not only as a home remedy, but also recommended by medicine and widely used in the gastronomic industry. Many properties are known, supported by biological tests both in vitroand in vivo. Because it is so highly appreciated, it is included in the book "Medicamentos HerbariosTradicionales" (Traditional Herbal Medicines) of the Chilean Ministry of Health. Given the great interest in this plant since time immemorial, this review contains information on its history, popular uses and scientific studies, for a better knowledge, management and sustainable care of this Chilean natural resource.

Culén es el término popular utilizado en Chile para la única especie endémica de la familia Fabaceae, Psoralea glandulosaLinn. Se trata de una de las plantas medicinales más utilizadas en Chile y en algunas regiones de Sudamérica, no solamente como remedio curativo casero, sino también recomendada por la medicina y con amplia utilización en la industria gastronómica. De ella se conocen un gran número propiedades avaladas por ensayos biológicos tanto in vitrocomo in vivo. Por ser tan apreciada, se encuentra incluida en el libro "Medicamentos Herbarios Tradicionales" del Ministerio de Salud de Chile. Dado el gran interés que despierta esta planta desde tiempos inmemoriales, se recoge en este capítulo la información sobre su historia, usos populares y estudios científicos, para un mejor conocimiento, manejo y cuidado de manera sustentable de este recurso natural chileno.

Psoralen and Isopsoralen, Two Estrogen-Like Natural Products from Psoraleae Fructus, Induced Cholestasis via Activation of ERK1/2.

With the increasing use of oral contraceptives and estrogen replacement therapy, the incidence of estrogen-induced cholestasis (EC) has tended to rise. Psoralen (P) and isopsoralen (IP) are the major bioactive components in Psoraleae Fructus, and their estrogen-like activities have already been recognized. Recent studies have also reported that ERK1/2 plays a critical role in EC in mice. This study aimed to investigate whether P and IP induce EC and reveal specific mechanisms. It was found that P and IP increased the expression of esr1, cyp19a1b and the levels of E2 and VTG at 80 µM in zebrafish larvae. Exemestane (Exe), an aromatase antagonist, blocked estrogen-like activities of P and IP. At the same time, P and IP induced cholestatic hepatotoxicity in zebrafish larvae with increasing liver fluorescence areas and bile flow inhibition rates. Further mechanistic analysis revealed that P and IP significantly decreased the expression of bile acids (BAs) synthesis genes cyp7a1 and cyp8b1, BAs transport genes abcb11b and slc10a1, and BAs receptor genes nr1h4 and nr0b2a. In addition, P and IP caused EC by increasing the level of phosphorylation of ERK1/2. The ERK1/2 antagonists GDC0994 and Exe both showed significant rescue effects in terms of cholestatic liver injury. In conclusion, we comprehensively studied the specific mechanisms of P- and IP-induced EC and speculated that ERK1/2 may represent an important therapeutic target for EC induced by phytoestrogens.

Isobavachin, a main bioavailable compound in Psoralea corylifolia, alleviates lipopolysaccharide-induced inflammatory responses in macrophages and zebrafish by suppressing the MAPK and NF-κB signaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Psoralea corylifolia L. (PC) is widely used in traditional medicines to treat inflammatory and infectious diseases. Isobavachin (IBC) is a bioavailable prenylated flavonoid derived from PC that has various biological properties. However, little information is available on its anti-inflammatory effects and mechanisms of action. AIM OF THE STUDY: In this study, we aimed to determine the anti-inflammatory effects of IBC in vitro and in vivo by conducting a mechanistic study using murine macrophages. MATERIALS AND METHODS: We evaluated the modulatory effects of IBC on the production of pro-inflammatory cytokines and mediators in murine macrophages. In addition, we examined whether IBC inhibits lipopolysaccharide (LPS)-induced inflammatory responses in a zebrafish model. Alterations in inflammatory response-associated genes and proteins were determined using quantitative reverse transcriptional polymerase chain reaction (RT-qPCR) and Western blotting analysis. RESULTS: IBC markedly reduced the overproduction of inflammatory mediators, pro-inflammatory cytokines, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), phosphorylation of mitogen-activated protein kinase (MAPK) and nuclear translocation of nuclear factor-kappa B (NF-κB) in macrophages induced by lipopolysaccharides (LPS). In addition, excessive NO, ROS, and neutrophil level induced by LPS, were suppressed by IBC treatment in a zebrafish inflammation model. CONCLUSIONS: Collectively, bioavailable IBC inhibited on the inflammatory responses by LPS via MAPK and NF-κB signaling pathways in vitro and in vivo, suggesting that it may be a potential modulatory agent against inflammatory disorders.

Bakuchiol, a natural constituent and its pharmacological benefits.

Background and aims: 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. Methods: 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. Results: Strong support of primary research on the protective effects via antitumorigenic, anti-inflammatory, antioxidative, antimicrobial, and antiviral activities are delineated. Conclusions: 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.

Phytochemical and Pharmacological Aspects of Psoralen - A Bioactive Furanocoumarin from Psoralea corylifolia Linn.

Since long ago, medicinal plants have played a vital role in drug discovery. Being blessed and rich in chemovars with diverse scaffolds, they have unique characteristics of evolving based on the need. The World Health Organization also mentions that medicinal plants remain at the center for meeting primary healthcare needs as the population relies on them. The plant-derived natural products have remained an attractive choice for drug development owing to their specific biological functions relevant to human health and also the high degree of potency and specificity they offer. In this context, one such esteemed phytoconstituent with inexplicable biological potential is psoralen, a furanocoumarin. Psoralen was the first constituent isolated from the plant Psoralea corylifolia, commonly known as Bauchi. Despite being a life-saver for psoriasis, vitiligo, and leukoderma, it also showed immense anticancer, anti-inflammatory, and anti-osteoporotic potential. This review brings attention to the possible application of psoralen as an attractive target for rational drug design and medicinal chemistry. It discusses the various methods for the total synthesis of psoralen, its extraction, the pharmacological spectrum of psoralen, and the derivatization done on psoralen.

Network pharmacology-based identification of bioavailable anti-inflammatory agents from Psoralea corylifolia L. in an experimental colitis model.

ETHNOPHARMACOLOGICAL RELEVANCE: In traditional oriental medicine, the dried seeds of Psoralea corylifolia L. (PC) have been used to treat various diseases, including gastrointestinal, urinary, orthopedic, diarrheal, ulcer, and inflammatory disorders. AIM OF THE STUDY: Although its various biological properties are well-known, there is no information on the therapeutic effects and bioavailable components of PC against inflammatory bowel disease. Therefore, we focused on the relationship between hydroethanolic extract of PC (EPC) that ameliorates colitis in mice and bioactive constituents of EPC that suppress pro-inflammatory cytokines in macrophages. MATERIALS AND METHODS: We investigated the therapeutic effects of EPC in a dextran sulfate sodium-induced colitis mouse model and identified the orally absorbed components of EPC using UPLC-MS/MS analysis. In addition, we evaluated and validated the mechanism of action of the bioavailable constituents of EPC using network pharmacology analysis. The effects on nitric oxide (NO) and inflammatory cytokines were measured by Griess reagent and enzyme linked immunosorbent assay in lipopolysaccharide (LPS)-induced macrophages. RESULTS: In experimental colitis, EPC improved body weight loss, colon length shortening, and disease activity index. Moreover, EPC reduced the serum levels of pro-inflammatory cytokines and histopathological damage to the colon. Network pharmacological analysis identified 13 phytochemicals that were bioavailable following oral administration of EPC, as well as their potential anti-inflammatory effects. 11 identified EPC constituents markedly reduced the overproduction of NO, tumor necrosis factor-α, and/or interleukin-6 in macrophages induced by LPS. The LPS-induced expression of the nuclear factor kappa-light-chain-enhancer of activated B cells reporter gene was reduced by the 4 EPC constituents. CONCLUSIONS: The results indicate that the protective activity of EPC against colitis is a result of the additive effects of each constituent on the expression of inflammatory cytokines. Therefore, it suggests that 11 bioavailable phytochemicals of EPC could aid in the management of intestinal inflammation, and also provides useful insights into the clinical application of PC for the treatment of inflammatory bowel diseases.

Therapeutic and Health Promoting Potential of Bakuchiol from Psoralea corylifolia: A Comprehensive Review.

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: A Potential Anticancer Compound from Psoralea corylifolia Linn.

BACKGROUND: Bakuchiol is a monoterpene phenol isolated from the seeds of Psoralea corylifolia Linn. It is used traditionally in Indian and Chinese medicine and has been reported to possess extensive pharmacological potential against a variety of ailments. A recent study enumerates the anticancer potential of bakuchiol. OBJECTIVE: The objective of the present review study is to explore the anticancer potential of bakuchiol which provides insight into the design and develop novel molecular entities against various disorders. METHODS: Current prose and patents emphasizing the anticancer potential of bakuchiol have been identified and reviewed with particular emphasis on their scientific impact and novelty. An extensive literature survey was performed and compiled via the search engine, PubMed, Science Direct, and from many reputed foundations. RESULTS: The study's findings suggested and verified the anticancer potential that Psoralea and bakuchiol against a variety of cancer. Both Psoralea and bakuchiol also portrayed synergistic or potentiating effects when given in combination with other anticancer drugs or natural compounds. CONCLUSION: Altogether, the promising anticancer potential of bakuchiol may open new probes for therapeutic invention in various types of tumors. Thus, the present review gives the erudition of bakuchiol and Psoralea as anticancer which paves the way for further work in exploring their potential.

Biological Importance, Therapeutic Benefits, and Analytical Aspects of Active Flavonoidal Compounds 'Corylin' from Psoralea corylifolia in the Field of Medicine.

BACKGROUND: Flavonoidal class phytochemicals are the best examples of secondary metabolite found in different natural sources, including 'fruits, grains, vegetables, broccoli, tea, berries, wine, strawberries, apples, grapes, lettuce, and citrus fruit. Natural products are a rich source of flavonoidal compounds present in our diet source. OBJECTIVE: Flavonoidal class chemicals can be subcategorized into chalcones, isoflavone, flavonols, catechin, flavones, flavanones, and anthocyanidin with respect to their basic chemical structures. Psoralea corylifolia L. belongs to the family Fabaceae and is an herbal medicine used in traditional Chinese Medicine for the treatment of inflammatory disorders, bacterial infections, and cancerous disorders. METHODS: In the present work, scientific data have been collected from different databases and analyzed in order to find the therapeutic potential of corylin in medicine. Different scientific databases such as Google, Scopus, PubMed, Science Direct, etc., have been searched to collect the needed scientific information on corylin. Scientific information on corylin has been collected in the present work in order to know the pharmacological activities and medicinal uses of corylin in the scientific fields. However, analytical techniques data of corylin have also been collected and analyzed for standardization of Psoralea corylifolia and other medicinal plants. RESULTS: Scientific data analysis of research works revealed the medicinal importance of Psoralea corylifolia and its important phytoconstituents corylin in medicine. Scientific data analysis revealed that corylin is a flavonoidal class phytochemical found in the nuts of Psoralea corylifolia L. Biological importance of corylin in bone differentiation, bone growth, and osteoporosis has been proven in this scientific research work. The anti-inflammatory, anti-oxidant, and antitumor activity of corylin has been also described in this medical literature. The biological importance of corylin in hyperlipidemia, insulin resistance, atherosclerosis, hepatocellular carcinoma, and neurodisorders have also been presented in this work. CONCLUSION: Scientific data analysis revealed the biological importance and therapeutic potential of corylin in the field of medicine.

Individual and combined effects of chromium and ultraviolet-B radiation on defense system, ultrastructural changes, and production of secondary metabolite psoralen in a medicinal plant Psoralea corylifolia L.

The present study focuses on the effects of individual and combined stress of chromium (Cr) and ultraviolet-B (UV-B) radiation on Psoralea corylifolia L. The experiment comprised four sets: (i) control, (ii) eUV-B (elevated UV-B i.e., ambient + 7.2 kJ m-2 day-1 UV-B), (iii) Cr (chromium; 30 mg kg-1 soil), and (iv) Cr + eUV-B (chromium and elevated UV-B; Cr 30 mg kg-1 and ambient + 7.2 kJ m-2 day-1 UV-B). The eUV-B and Cr individually and in combination showed the variable responses on ultrastructure, physiology and biomass however, the impact was more prominent under individual Cr treatment followed by Cr + eUV-B and eUV-B. Higher bioconcentration factor and the lowered translocation factor consequently led to a higher reduction in the below ground biomass and the lesser reduction in above ground biomass under Cr + eUV-B treatment as compared to individual Cr treatment. In addition, higher induction in the enzymatic (glutathione reductase, ascorbate peroxidase, superoxide dismutase, and glutathione-S-transferase) and non-enzymatic antioxidants (glutathione reduced) were found to be responsible for efficient scavenging of hydrogen peroxide and superoxide radical leading to lowered MDA content under combined treatment as compared to Cr treatment. Deposition of Cr as electron dense granules in the cytoplasm, vacuoles, and cell wall under Cr and Cr + eUV-B is contemplated as one of the cellular mechanisms of P. corylifolia against the toxicity of Cr. Psoralen increased under all treatments with a maximum increase under Cr + eUV-B treatment. Taken together our results accentuated that P. corylifolia can be grown in an area contaminated with Cr and has a higher influx of UV-B for the attainment of psoralen considering its pharmaceutical perspectives.

Anti-tyrosinase and antioxidant activity of meroterpene bakuchiol from Psoralea corylifolia (L.).

Bakuchiol is gaining major interest for treatments against skin photoaging. The kinetics of mushroom tyrosinase inhibition by bakuchiol, by real-time oxygen sensing and UV-vis monitoring (475 nm), showed competitive inhibition with average Ki constant (µM, 30 °C, pH 6.8) of 6.71 ± 1.23 and 1.15 ± 0.34 for monophenolase and diphenolase reactions respectively, with respective IC50 37.22 ± 5.18 and 6.91 ± 0.96 âˆ¼ at 1 mM substrate, compared to kojic acid IC50 34.02 ± 5.51 and 16.86 ± 3.28 µM. Fluorescence quenching showed a single binding mode with formation constant Ka 1.02 × 106 M-1. The antioxidant activity was studied by inhibited autoxidation of styrene and cumene (PhCl, 30 °C) affording inhibition constant kinh = 18.1 ± 6.6 (104M-1s-1, 30 °C) and of MeLin in Triton™ X-100 micelles giving kinh = 0.16 ± 0.03 (104M-1s-1, 37 °C). Stoichiometric factor was 1.9 ± 0.1. ReqEPR spectroscopy afforded the BDE(OH) as 81.7 ± 0.1 kcal/mol. Bakuchiol is a potent tyrosinase inhibitor with good antioxidant activity having major potential as natural food preservative against oxidation and food-browning.

Flavonoids dimers from the fruits of Psoralea corylifolia and their cytotoxicity against MCF-7 cells.

Nine new flavonoids dimers, psocorylins R-Z (1-9), were isolated from the fruits of Psoralea corylifolia L. (Psoraleae Fructus), a traditional Chinese medicine. The structures of these compounds were elucidated via multiple spectroscopic techniques and X-ray diffraction. Psocorylins R (1) and S (2) were rare cyclobutane-containing chalcone dimers, and psocorylins T-Z (3-9) were established by CC or COC bond of two flavonoid monomers. The structural-types, flavonoids dimers, were isolated from the plant for the first time, enriching the chemical diversity. The cytotoxicity assay suggested that compounds 1, 2, 4, 5, 6 and 8 exhibited cytotoxic activities against MCF-7 cells. Furthermore, compounds 1 and 8 significantly increased intracellular ROS levels, decreased MMP and induced apoptosis of MCF-7 cells. They markedly upregulated the expression of Bax and cleaved caspase-3, and suppressed Bcl-2 and caspase-3 levels, indicating their mechanism of Bcl-2/Bax/Cleaved caspase-3 pathway. Hence, our findings not only promoted the chemical investigation of Psoraleae Fructus, but also provided potential bioactive natural products for anti-cancer.

Exploration of Antimicrobial Ingredients in Psoralea corylifolia L. Seed and Related Mechanism against Methicillin-Resistant Staphylococcus aureus.

With the abuse of antibiotics, bacterial antibiotic resistance is becoming a major public healthcare issue. Natural plants, especially traditional Chinese herbal medicines, which have antibacterial activity, are important sources for discovering potential bacteriostatic agents. This study aimed to develop a fast and reliable method for screening out antimicrobial compounds targeting the MRSA membrane from Psoralea corylifolia Linn. seed. A UPLC-MS/MS method was applied to identify the prenylated flavonoids in major fractions from the extracts of Psoralea corylifolia Linn. seed. The broth microdilution method was used to determine the minimum inhibitory concentrations (MICs) of different fractions and compounds. The morphological and ultrastructural changes of MRSA were determined by scanning electron microscopy (SEM). The membrane-targeting mechanism of the active ingredients was explored by membrane integrity assays, membrane fluidity assays, membrane potential assays, ATP, and ROS determination. We identified eight prenylated flavonoids in Psoralea corylifolia Linn. seed. The antibacterial activity and mechanism studies showed that this type of compound has a unique destructive effect on MRSA cell membranes and does not result in drug resistance. The results revealed that prenylated flavonoids in Psoralea corylifolia Linn. seeds are promising candidates for the development of novel antibiotic agents to combat MRSA-associated infections.

Total Syntheses and Cytotoxicity Evaluation of Coryaurone A and Representative Analogues.

The first total synthesis of coryaurone A, which was originally obtained from Psoralea corylifolia L., was achieved via an efficient route with the longest linear sequence of six steps from the commercially available 6-hydroxy-2H-benzofuran-3-one in 37% overall yield. A series of representative analogues were synthesized from the same starting material in 4-7 steps with overall yields of 27-56%. The cytotoxicities of these compounds against the leukemia cell line HL-60 and the colon cancer cell line SW480 were determined. Among them, compounds 12, 14, 21, and 27 exhibited different levels of cytotoxic activity, which were greater than the positive control cisplatin.

The Use of Bakuchiol in Dermatology: A Review of In Vitro and In Vivo Evidence.

The plant Psoralea corylfolia contains compounds such as psoralens that are useful for the treatment of psoriasis and vitiligo, and the plant is used in Chinese and Indian traditional medicine for diseases such as psoriasis and leprosy. Bakuchiol, a meroterpene phenol in Psoralea corylfolia, has similar functional properties to topical retinoids, which are commonly used to treat acne, post-inflammatory hyperpigmentation, and wrinkles. Bakuchiol’s anti-inflammatory and anti-proliferative properties also may lead to improvement in psoriasis and skin cancers, yet more clinical evidence is needed to elucidate these effects. Notably, bakuchiol does not cause common adverse effects seen with topical retinoids such as burning and scaling, permitting wider use in patients with sensitive skin. This review will detail the current evidence for bakuchiol as an alternative treatment in dermatologic conditions. J Drugs Dermatol. 2022;21(6):624-629. doi:10.36849/JDD.6740.

Psoralea corylifolia L. seed extract attenuates dexamethasone-induced muscle atrophy in mice by inhibition of oxidative stress and inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: The seeds of Psoralea corylifolia (PCS), also called "Boh-Gol-Zhee" in Korean, have been used in traditional medicine. PCS is effective for the treatment of vitiligo, cancer, inflammatory diseases, neurodegenerative diseases, kidney diseases, and musculoskeletal diseases. AIM OF THE STUDY: In this study, we validated the beneficial effects of PCS extract on dexamethasone (DEX)-induced muscle atrophy in mice. MATERIALS AND METHODS: DEX (20 mg/kg/day, 10 days) was intraperitoneally injected into C57BL/6 male mice to induce muscular atrophy. Oral administration of PCS extract (200 or 500 mg/kg/day) was started 2 days before DEX injection and continued for 12 days. RESULTS: PCS extract inhibited DEX-induced decrease in body and muscle weight, grip strength, and cross-sectional area of the tibialis anterior. PCS extract significantly increased the mRNA and protein expression levels of myosin heavy chain 1, 2A, and 2X in DEX-administered mice. DEX administration significantly increased the levels of muscle atrophy factors atrogin-1, muscle RING-finger protein-1, and myostatin, which were inhibited by the PCS extract. Additionally, PCS extract increased the expression of muscle regeneration factors, such as myoblast determination protein 1, myogenin, and embryonic myosin heavy chain, and muscle synthesis markers, such as protein kinase B and mammalian target of rapamycin signaling molecules. PCS extract also significantly decreased the DEX-induced production of 4-hydroxynonenal, an oxidative stress marker. Furthermore, PCS extract recovered superoxide dismutase 2, glutathione peroxidase, and catalase activities, which were significantly reduced by DEX administration. Moreover, DEX-induced activation of nuclear factor kappa-light-chain-enhancer of activated B cells and expression of cytokines, such as tumor necrosis factor α and monocyte chemoattractant protein-1, significantly decreased after PCS extract administration. CONCLUSIONS: Here, we demonstrated that PCS extract administration protected against DEX-induced muscle atrophy. This beneficial effect was mediated by suppressing the expression of muscle degradation factors and increasing the expression of muscle regeneration and synthesis factors. This effect was probably due to the inhibition of oxidative stress and inflammation. These results highlight the potential of PCS extract as a protective and therapeutic agent against muscle dysfunction and atrophy.