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1.
Bioorg Chem ; 150: 107604, 2024 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-38981209

RESUMO

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.

2.
Vet Sci ; 11(5)2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38787160

RESUMO

Rotavirus is the main causative agent of viral gastroenteritis among young animals worldwide. Currently, no clinically approved or effective antiviral drugs are available to combat rotavirus infections. Herein, we evaluated the anti-rotaviral activities of extracts and bavachin isolated from Psoralea corylifolia L. (Fabaceae) (P. corylifolia) against the bovine rotavirus G8P[7] and porcine rotavirus G5P[7] in vitro. Two assay strategies were performed: (1) a virucidal assay to reduce viral infectivity by virus neutralization and (2) a post-treatment assay to assess viral replication suppression. The results from the virucidal assay showed that the extracts and bavachin did not exert anti-rotaviral activities. In the follow-up analysis after treatment, bavachin exhibited robust antiviral efficacy, with 50% effective concentration (EC50) values of 10.6 µM (selectivity index [SI] = 2.38) against bovine rotavirus G8P[7] and 13.0 µM (SI = 1.94) against porcine rotavirus G5P[7]. Bavachin strongly suppressed viral RNA synthesis in the early (6 h) and late stages (18 h) after rotaviral infection. These findings strongly suggest that bavachin may have hindered the virions by effectively inhibiting the early stages of the virus replication cycle after rotaviral infection. Furthermore, confocal imaging showed that bavachin suppressed viral protein synthesis, notably that of the rotaviral protein (VP6). These results suggest that bavachin has strong antiviral activity against rotaviruses, inhibits viral replication, and is a candidate natural therapeutic drug targeting rotaviral infection. The utilization of bavachin isolated from P. corylifolia may contribute to decreased mortality rates, lower medication expenses, and enhanced economic viability in domestic farms.

3.
Bol. latinoam. Caribe plantas med. aromát ; 23(3): 336-348, mayo 2024. ilus
Artigo em Inglês | LILACS | ID: biblio-1538075

RESUMO

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.


Assuntos
Plantas Medicinais , Psoralea , Chile
4.
J Ethnopharmacol ; 329: 118130, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-38565407

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Psoraleae Fructus (Bu Gu Zhi) is the fruit of Psoralea corylifolia L. (PCL) and has been used for centuries in traditional Chinese medicine formulas to treat osteoporosis (OP). A new drug called "BX" has been developed from PCL, but its mechanism for treating OP is not yet fully understood. AIM OF THE STUDY: To explore the mechanism of action of BX in the treatment of ovariectomy-induced OP based function-oriented multi-omics analysis of gut microbiota (GM) and metabolites. MATERIALS AND METHODS: C57BL/6 mice were bilaterally ovariectomized to replicate the OP model. The therapeutic efficacy of BX was evaluated by bone parameters (BMD, BV/TV, Tb.N, Tb.Sp), hematoxylin and eosin (H&E) staining results, and determination of bone formation markers procollagen type Ⅰ amino-terminal peptide (PⅠNP) and bone-specific alkaline phosphatase (BALP). Serum and fecal metabolomics and high-throughput 16S rDNA sequencing were performed to evaluate effects on endogenous metabolites and GM. In addition, an enzyme-based functional correlation algorithm (EBFC) algorithm was used to investigate functional correlations between GM and metabolites. RESULTS: BX improved OP in OVX mice by increasing BMD, BV/TV, serum PⅠNP, BALP, and improving Tb.N and Tb.Sp. A total of 59 differential metabolites were identified, and 9 metabolic pathways, including arachidonic acid metabolism, glycerophospholipid metabolism, purine metabolism, and tryptophan metabolism, were found to be involved in the progression of OP. EBFC analysis results revealed that the enzymes related to purine and tryptophan metabolism, which are from Lachnospiraceae_NK4A136_group, Blautia, Rs-E47_termite_group, UCG-009, and Clostridia_UCG-014, were identified as the intrinsic link between GM and metabolites. CONCLUSIONS: The regulation of GM and restoration of metabolic disorders may be the mechanisms of action of BX in alleviating OP. This research provides insights into the function-oriented mechanism discovery of traditional Chinese medicine in the treatment of OP.


Assuntos
Cumarínicos , Microbioma Gastrointestinal , Camundongos Endogâmicos C57BL , Osteoporose , Ovariectomia , Psoralea , Animais , Psoralea/química , Feminino , Osteoporose/tratamento farmacológico , Cumarínicos/farmacologia , Cumarínicos/isolamento & purificação , Cumarínicos/uso terapêutico , Microbioma Gastrointestinal/efeitos dos fármacos , Camundongos , Densidade Óssea/efeitos dos fármacos , Metabolômica , Modelos Animais de Doenças , Frutas , Multiômica
5.
Front Pharmacol ; 15: 1308655, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38449808

RESUMO

Objective: Psoralea corylifolia L. (FP) has received increasing attention due to its potential hepatotoxicity. Methods: In this study, zebrafish were treated with different concentrations of an aqueous extract of FP (AEFP; 40, 50, or 60 µg/mL), and the hepatotoxic effects of tonicity were determined by the mortality rate, liver morphology, fluorescence area and intensity of the liver, biochemical indices, and pathological tissue staining. The mRNA expression of target genes in the bile acid metabolic signaling pathway and lipid metabolic pathway was detected by qPCR, and the mechanism of toxicity was initially investigated. AEFP (50 µg/mL) was administered in combination with FXR or a peroxisome proliferator-activated receptor α (PPARα) agonist/inhibitor to further define the target of toxicity. Results: Experiments on toxic effects showed that, compared with no treatment, AEFP administration resulted in liver atrophy, a smaller fluorescence area in the liver, and a lower fluorescence intensity (p < 0.05); alanine transaminase (ALT), aspartate transaminase (AST), and γ-GT levels were significantly elevated in zebrafish (p < 0.01), and TBA, TBIL, total cholesterol (TC), TG, low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C) levels were elevated to different degrees (p < 0.05); and increased lipid droplets in the liver appeared as fatty deposits. Molecular biological validation revealed that AEFP inhibited the expression of the FXR gene, causing an increase in the expression of the downstream genes SHP, CYP7A1, CYP8B1, BSEP, MRP2, NTCP, peroxisome proliferator-activated receptor γ (PPARγ), ME-1, SCD-1, lipoprotein lipase (LPL), CPT-1, and CPT-2 and a decrease in the expression of PPARα (p < 0.05). Conclusion: This study demonstrated that tonic acid extracts are hepatotoxic to zebrafish through the inhibition of FXR and PPARα expression, thereby causing bile acid and lipid metabolism disorders.

6.
J Asian Nat Prod Res ; 26(1): 120-129, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38509697

RESUMO

Three new monoterpene phenol dimers, bisbakuchiols V-X (1-3), and two bakuchiol ethers (4 and 5), along with four known compounds (6-9) were isolated from the fruits of Psoralea corylifolia. Their structures were elucidated based on extensive spectral analysis. The absolute configurations of 1, 2, 4, and 5 were specified by quantum chemical calculations of ECD spectra.


Assuntos
Fenol , Psoralea , Fenol/análise , Frutas/química , Psoralea/química , Monoterpenos , Estrutura Molecular , Fenóis/química
7.
Vet Parasitol ; 328: 110167, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38518713

RESUMO

Tetrahymena piriformis belongs to the ciliated protists (ciliates), causing severe economic losses in aquaculture. Chemical drugs currently used usually have toxic side effects, and there is no specific drug against Tetrahymena. Therefore, it is an urgent need to identify new antiparasitic lead compounds. In the present study, the in vitro parasiticidal activity of ethyl acetate (EtOAc) extracts and water extracts from 22 selected traditional Chinese medicines (TCMs) were evaluated against T. piriformis. The EtOAc extract of P. corylifolia turned out to be the most active with the minimum parasiticidal concentration of 100 mg/L within 3 h. Thus, it was separated into 12 fractions by the first-dimensional (D1) normal phase liquid chromatography (NPLC), meanwhile combining with in vitro antiparasitic tests for activity tracking. Subsequently, 8 flavonoids were identified in the active fractions by the second-dimensional (D2) reverse phase liquid chromatography (RPLC) tandem high-resolution mass spectrometry. According to the results, 5 flavonoids were selected for in vitro antiparasitic test, of which isobavachalcone showed the minimum parasiticidal concentration of 3.125 mg/L in 2 h. Bathing treatment of infected guppies with isobavachalcone could significantly reduce the burden of T. piriformis, obtaining a 24-h median effective concentration (24-h EC50) value of 1.916 mg/L. And the concentration of isobavachalcone causing guppies to die within 24 h is 39 times than that of 24-h EC50. The results demonstrated that isobavachalcone has the potential to be developed into a novel commercial fish drug against T. piriformis.


Assuntos
Infecções por Cilióforos , Doenças dos Peixes , Flavonoides , Poecilia , Psoralea , Animais , Flavonoides/farmacologia , Flavonoides/química , Poecilia/parasitologia , Doenças dos Peixes/parasitologia , Doenças dos Peixes/tratamento farmacológico , Infecções por Cilióforos/veterinária , Infecções por Cilióforos/tratamento farmacológico , Infecções por Cilióforos/parasitologia , Psoralea/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antiparasitários/farmacologia , Antiparasitários/química
9.
Chem Biodivers ; 21(2): e202301841, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38226737

RESUMO

Psoralea corylifolia (syn. Cullen corylifolium), commonly called bawachi, is a medicinal plant extensively used for skin conditions like leukoderma, vitiligo, and psoriasis. It is notably rich in valuable bioactive compounds, particularly coumarins and furanocoumarins. This study isolated fourteen coumarins from P. corylifolia which were tested for cytotoxicity using the MTT assay, with compound 10 showing good cytotoxicity against A549 cells (IC50 0.9 µM), while compound 1, compound 2, and compound 3 displaying potential cytotoxicity against MDA-MB-231 cells (IC50 0.49 µM, 0.56 µM, and 0.84 µM respectively). Additionally, the compounds' interaction with Epidermal Growth Factor Receptor (EGFR) protein, highly expressed in both cell lines, was investigated through molecular modeling studies, that aligned well with cytotoxicity results. The findings revealed the remarkable cytotoxic potential of four coumarins 1, 2, 3, and 10 against A549 and MDA-MB-231 cell lines.


Assuntos
Furocumarinas , Plantas Medicinais , Psoralea , Cumarínicos/farmacologia , Extratos Vegetais/farmacologia
10.
J Ethnopharmacol ; 321: 117501, 2024 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-38012970

RESUMO

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.


Assuntos
Proteínas Quinases Ativadas por Mitógeno , Psoralea , Animais , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Lipopolissacarídeos/farmacologia , Peixe-Zebra , Psoralea/metabolismo , Transdução de Sinais , Flavonoides/farmacologia , Citocinas/metabolismo , Macrófagos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo
11.
F1000Res ; 12: 29, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38021404

RESUMO

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.


Assuntos
Fabaceae , Plantas Medicinais , Psoralea , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Psoralea/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico
12.
Chem Biodivers ; 20(11): e202300867, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37752710

RESUMO

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.


Assuntos
Fabaceae , Furocumarinas , Plantas Medicinais , Psoralea , Humanos , Furocumarinas/farmacologia , Ficusina/farmacologia , Extratos Vegetais/farmacologia , Compostos Fitoquímicos/farmacologia
13.
Toxicol Lett ; 385: 31-41, 2023 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-37598872

RESUMO

Psoralea corylifolia L. (P. corylifolia) has attracted increasing attention because of its potential hepatotoxicity. In this study, we used network analysis (toxic component and hepatotoxic target prediction, proteinprotein interaction, GO enrichment analysis, KEGG pathway analysis, and molecular docking) to predict the components and mechanism of P. corylifolia-induced hepatotoxicity and then selected 4-hydroxylonchocarpin and corylifol A for experimental verification. HepG2 cells were treated with low, medium, and high concentrations of 4-hydroxylonchocarpin or corylifol A. The activities of ALT, AST, and LDH in cell culture media and the MDA level, SOD activity, and GSH level in cell extracts were measured. Moreover, apoptosis, ROS levels, and mitochondrial membrane potential were evaluated. The results showed that the activities of ALT, AST, and LDH in the culture medium increased, and hepatocyte apoptosis increased. The level of MDA increased, and the activity of SOD and level of GSH decreased, and the ROS level increased with 4-hydroxylonchocarpin and corylifol A intervention. Furthermore, the mitochondrial membrane potential decreased in the 4-hydroxylonchocarpin and corylifol A groups. This study suggests that 4-hydroxylonchocarpin and corylifol A cause hepatocyte injury and apoptosis by inducing oxidative stress and mitochondrial dysfunction, suggesting that these compounds may be the potential hepatotoxic components of P. corylifolia.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas , Psoralea , Simulação de Acoplamento Molecular , Espécies Reativas de Oxigênio , Superóxido Dismutase
14.
Chin Herb Med ; 15(2): 263-270, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37265757

RESUMO

Objective: The compatibility of Eucommia ulmoides (Eu) and Psoralea corylifolia (Pc) on the pharmacokinetic (PK) properties in the rat was explored in this study. Methods: Eu extract, Pc extract and the combined extracts (crude drug ratio was 2:1) was administered by gavage, respectively. Two PK experiments were conducted. In first one, the blood samples were collected via the occuli chorioideae vein to get the PK properties of the components. In second one, the blood samples were simultaneously collected via the internal jugular vein or portal vein at different time points and the concentrations of target ingredients were detected by LC/MS/MS to clear the location where the interaction of Eu and Pc took place in vivo. Results: Eight of 11 ingredients in Eu and Pc extract were determined in rat plasma. The exposure levels of geniposidic acid (GPA), aucubin (AU), geniposide (GP), pinoresinol diglucoside (PDG), psoralen glycosides (PLG) and isopsoralen glycosides (IPLG) were decreased 1/5-2/3 after administration of combined extracts. Comparing to the combined administration, the exposure of GPA and AU in plasma of single Eu administration collected via the portal vein were decreased 1/3-2/3, and the values of AUC0-24h and AUC0-∞ of GP collected from the portal vein or internal jugular vein were double increased. The other components' parameters were not significantly changed. Conclusion: In summary, the Pc and Eu combined administration could affect the exposure of the main components of Eu extract in rats due to the changed intestinal absorption. The research on the compatibility of Pc and Eu was helpful to guide the clinical administration of Eu and Pc simultaneously.

15.
J Ethnopharmacol ; 313: 116534, 2023 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-37127140

RESUMO

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.


Assuntos
Colite Ulcerativa , Colite , Fabaceae , Psoralea , Camundongos , Animais , Psoralea/metabolismo , Lipopolissacarídeos/farmacologia , Cromatografia Líquida , Farmacologia em Rede , Espectrometria de Massas em Tandem , Colite/induzido quimicamente , Colite/tratamento farmacológico , Colite/patologia , Anti-Inflamatórios/efeitos adversos , Colo , Citocinas/metabolismo , Sulfato de Dextrana , Colite Ulcerativa/tratamento farmacológico , NF-kappa B/metabolismo
16.
Naunyn Schmiedebergs Arch Pharmacol ; 396(9): 2105-2125, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-36929274

RESUMO

The aim of the current study is to evaluate the anti-psoriatic potential of bakuchiol (Bak) loaded solid lipid nanoparticles (SLNs) via modulating inflammatory and oxidative pathways. Bak-loaded SLNs were prepared using hot homogenization method and characterized by various spectroscopic techniques. Bak-SLNs suspension was formulated into gel using Carbopol. Different in vivo assays were executed to explore the role of inflammatory markers and oxidative enzymes in psoriasis. DLS (dynamic light scattering) analysis showed suitable particle size, zeta potential, and polydispersity index (PDI) of developed formulation. TEM (transmission electron microscopy) reveal the spherical shape of Bak-SLNs particles. The release studies confirmed the sustained release of Bak-SLNs-based gel. UV-B-induced psoriatic Wistar rat model showed significant anti-psoriatic effect of Bak via regulating inflammatory markers (NF-kB, IL-6, IL-4, and IL-10) and levels of anti-oxidant enzymes, superoxide dismutase (SOD), catalase (CAT), glutathione (GSH), and glutathione-S-transferase (GST). Furthermore, RT-qPCR analysis confirms that Bak downregulates the expression of inflammatory markers, while histology and immunohistology results also confirm the anti-psoriatic effect of Bak. The study indicates that Bak-loaded SLNs-based gel significantly downregulates the level of cytokines and interleukins involve in NF-kB signaling cascade; hence, it can prove to be a novel therapeutic approach to cure psoriasis.


Assuntos
Nanopartículas , Psoríase , Ratos , Animais , NF-kappa B , Ratos Wistar , Psoríase/tratamento farmacológico , Nanopartículas/química , Glutationa , Transdução de Sinais , Portadores de Fármacos/química
17.
Biomed Pharmacother ; 161: 114479, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36921531

RESUMO

Diabetic nephropathy (DN) is a major complication of diabetes mellitus. Psoralea corylifolia L. seed (PCS) is a traditional medicine effective against various diseases. In this study, we aimed to investigate the effect of bavachin, the major active component of PCS, on DN in db/db mice. Bavachin (10 mg/kg/day) was administered orally to 12-week-old male db/db mice for 6 wk. For in vitro experiments, SV40 MES13 cells were treated with bavachin in the presence of 25 mM glucose. Food and water intake and urine mass were significantly increased in db/db mice compared to wild-type CON mice, but bavachin administration significantly reduced these increases. Urinary microalbumin, blood urea nitrogen, and creatinine clearance which were significantly increased in db/db mice, were also decreased by bavachin administration. Glomerular area and collagen deposition in the kidney were significantly decreased in db/db mice following bavachin administration. Increased renal levels of fibrotic factors, fibronectin, COL1A1, and α-SMA, were reduced following bavachin administration. Protein expressions of antioxidant enzymes, namely SOD2, catalase, and HO-1, and mitochondrial function-related factors, namely SIRT1, PGC1α, Nrf1, and mtTFA, were reduced in the kidney tissues of db/db mice compared to wild-type CON mice, and bavachin administration upregulated these protein expressions. In vitro studies also showed that bavachin decreases mitochondria ROS production, increases the expression of PGC-1α and SIRT1, and decreases the expression of α-SMA in high glucose-treated SV40 MES13 cells. Based on these results, bavachin improved DN by inhibiting oxidative stress and enhancing mitochondrial function.


Assuntos
Diabetes Mellitus , Nefropatias Diabéticas , Camundongos , Masculino , Animais , Nefropatias Diabéticas/tratamento farmacológico , Nefropatias Diabéticas/metabolismo , Sirtuína 1/metabolismo , Estresse Oxidativo , Mitocôndrias/metabolismo , Rim/metabolismo , Camundongos Endogâmicos , Glucose/metabolismo , Diabetes Mellitus/metabolismo
18.
Artigo em Inglês | MEDLINE | ID: mdl-36748816

RESUMO

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.


Assuntos
Fabaceae , Psoralea , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Fenóis/farmacologia , Fenóis/uso terapêutico , Promoção da Saúde
19.
Chin Med ; 18(1): 4, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36627680

RESUMO

Psoralea corylifolia L. (PCL), referred to as "Bu-gu-zhi" in Chinese, has great medicinal values since ancient times. PCL is the dried ripe fruit of Psoralea corylifolia L., which has been widely used in traditional Chinese medicine (TCM) for the treatment of kidney-yang deficiency, enuresis and urinary frequency, chills and pain of the waist and knees, dawn diarrhea and vitiligo. In this paper, a systematic of the botany, traditional uses, phytochemistry, pharmacology, toxicology, quality control and pharmacokinetics of PCL was presented, along with future research directions. According to the results, PCL contains approximately 163 chemical components, including coumarins, flavonoids, monoterpene phenols, benzofurans, glycosides, lipids, fatty acids, and volatile oils. PCL and its active ingredients have a variety of pharmacological activities, such as anti-inflammatory, antibacterial, antiviral, antioxidant, antitumor, antiosteoporosis, cardioprotective, neuroprotective, and immunomodulatory. Further study of quality control standards and potential mechanisms of PCL is also needed. In addition, more toxicological studies will also contribute to the progress of clinical trials.

20.
Antioxidants (Basel) ; 12(1)2023 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-36671000

RESUMO

Type 2 diabetes reduces muscle mass and function. Chronic inflammation and mitochondrial dysfunction play critical roles in muscle atrophy pathogenesis. Here, we investigated the effects of bavachin and corylifol A from Psoralea corylifolia L. seeds on muscle atrophy in dexamethasone-treated mice and in db/db mice. Bavachin and corylifol A enhanced muscle strength and muscle mass in dexamethasone-treated mice. In diabetic mice, they enhanced muscle strength and cross-sectional areas. Bavachin and corylifol A suppressed inflammatory cytokine (interleukin-6 and tumor necrosis factor-α) expression levels by downregulating nuclear factor-κB phosphorylation. They decreased the muscle atrophic factor (myostatin, atrogin-1, and muscle RING finger-1) expression levels. They activated the AKT synthetic signaling pathway and induced a switch from fast-type glycolytic fibers (type 2B) to slow-type oxidative fibers (types I and 2A). They increased mitochondrial biogenesis and dynamic factor (optic atrophy-1, mitofusin-1/2, fission, mitochondrial 1, and dynamin 1-like) expression levels via the AMP-activated protein kinase-peroxisome proliferator-activated receptor gamma coactivator 1-alpha signaling pathway. They also improved mitochondrial quality by upregulating the mitophagy factor (p62, parkin, PTEN-induced kinase-1, and BCL2-interacting protein-3) expression levels. Therefore, bavachin and corylifol A exert potential therapeutic effects on muscle atrophy by suppressing inflammation and improving mitochondrial function.

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