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1.
Mar Drugs ; 22(4)2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38667792

RESUMO

Ulcerative colitis (UC) is a kind of inflammatory bowel condition characterized by inflammation within the mucous membrane, rectal bleeding, diarrhea, and pain experienced in the abdominal region. Existing medications for UC have limited treatment efficacy and primarily focus on symptom relief. Limonium bicolor (LB), an aquatic traditional Chinese medicine (TCM), exerts multi-targeted therapeutic effects with few side effects and is used to treat anemia and hemostasis. Nevertheless, the impact of LB on UC and its mechanism of action remain unclear. Therefore, the objective of this study was to investigate the anti-inflammatory effects and mechanism of action of ethanol extract of LB (LBE) in lipopolysaccharide-induced RAW 264.7 macrophages and dextran sulfate sodium (DSS)-induced UC. The results showed that LBE suppressed the secretion of cytokines in LPS-stimulated RAW 264.7 cells in a dose-dependent manner. LBE had protective effects against DSS-induced colitis in mice, decreased the disease activity index (DAI) score, alleviated symptoms, increased colon length, and improved histological characteristics, thus having protective effects against DSS-induced colitis in mice. In addition, it reversed disturbances in the abundance of proteobacteria and probiotics such as Lactobacillus and Blautia in mice with DSS-induced UC. Based on the results of network pharmacology analysis, we identified four main compounds in LBE that are associated with five inflammatory genes (Ptgs2, Plg, Ppar-γ, F2, and Gpr35). These results improve comprehension of the biological activity and functionality of LB and may facilitate the development of LB-based compounds for the treatment of UC.


Assuntos
Colite Ulcerativa , Sulfato de Dextrana , Disbiose , Etanol , Microbioma Gastrointestinal , Plumbaginaceae , Animais , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Camundongos , Células RAW 264.7 , Microbioma Gastrointestinal/efeitos dos fármacos , Disbiose/tratamento farmacológico , Plumbaginaceae/química , Etanol/química , Masculino , Anti-Inflamatórios/farmacologia , Modelos Animais de Doenças , Citocinas/metabolismo , Inflamação/tratamento farmacológico , Lipopolissacarídeos , Camundongos Endogâmicos C57BL , Colo/efeitos dos fármacos , Colo/patologia , Colo/metabolismo
2.
Int J Biol Macromol ; 260(Pt 1): 129455, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38232876

RESUMO

Plumbago zeylanica L., a traditional Chinese medicine, has anti-bacterial and anti-inflammatory effects, and it is critical important to explore the chemical compounds and evaluate their biological actions from the medicinal plant. However, the chemical structure and biological activities of polysaccharides from P. zeylanica. were still poorly understood. In this study, two water-soluble polysaccharides named WPZP-2-1 and WPZP-2-2 were purified from P. zeylanica L. Chemical and spectroscopic tests showed that the main chain of WPZP-2-1 was →4)-α-D-GalpA-(1 â†’ 2)-α-L-Rhap-(1→, and the branch chain was galactose or arabinose. The main chain of WPZP-2-2 was composed of →4)-α-D-GalpA-(1 â†’ 2)-α-L-Rhap-(1→, and the O-2 and O-3 of →4)-α-D-GalpA had a small amount of acetylation. In addition, in vitro test showed that WPZP-2-1 and WPZP-2-2 significantly improved the inflammatory damage of LPS + IFN-γ-induced THP-1 cells via reducing the protein levels of CD14, TLR4 and MyD88, thereby promoting IL-10 expression and inhibiting the mRNA levels of TNF-α and IL-1ß. Those findings indicated that WPZP-2-1 and WPZP-2-2 from the plant should be served as the potential anti-inflammatory agents.


Assuntos
Plantas Medicinais , Plumbaginaceae , Plumbaginaceae/química , Polissacarídeos/química , Anti-Inflamatórios/farmacologia , Extratos Vegetais/química
3.
Biomolecules ; 14(1)2024 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-38275763

RESUMO

Lampedusa, the largest island of the Pelagie archipelago, Sicily, Italy, has proven to be a rich source of plants and shrubs used in folk medicine. These plants, often native to the island, have been very poorly investigated for their phytochemical composition and biological potential to be translated into pharmacological applications. To start achieving this purpose, a specimen of Limonium lopadusanum, a plant native to Lampedusa, was investigated for the first time. This manuscript reports the results of a preliminary biological assay, focused on antimicrobial activity, carried out using the plant organic extracts, and the isolation and chemical and biological characterization of the secondary metabolites obtained. Thus 3-hydroxy-4-methoxybenzoic acid methyl ester (syn: methyl isovanillate, (1), methyl syringate (2), pinoresinol (3), erythrinassinate C (4) and tyrosol palmitate (5) were isolated. Their antimicrobial activity was tested on several strains and compound 4 showed promising antibacterial activity against Enterococcus faecalis. Thus, this metabolite has antibiotic potential against the drug-resistant opportunistic pathogen E. faecalis.


Assuntos
Plumbaginaceae , Plumbaginaceae/química , Antibacterianos/farmacologia , Extratos Vegetais/química , Medicina Tradicional , Itália , Testes de Sensibilidade Microbiana
4.
Chem Biodivers ; 20(12): e202301177, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37926684

RESUMO

Limonium. Mill is a genus of flowering plants belonging to the Plumbaginaceae family. The present study aimed to compare two Limonium species (L. pruinosum Kuntze and L. tunetanum (Barratte & Bonnet) Maire) in terms of their chemical composition and bioactivity. Chemical profiling showed that the methanolic (MeOH) extracts of both species were the most enriched with total phenolic (TP) and total flavonoid (TF) contents. The TFC were higher in L. tunetanum compared to L. pruinosum. HPLC-DAD analysis showed that distinctly the gallic acid and L-tyrosine 7-amido-4-methylcoumarin were the main compounds for L. pruinosum and L. tunetanum, respectively. For both Limonium. Mil species, the MeOH extracts displayed the highest antioxidant with IC50 of 7.7 and 8.4 µg/mL for L. pruinosum and L. tunetanum, respectively. The highest anti-15-lipoxygnase activity was recorded in the ethyl acetate (IC50 =14.2 µg/mL) and Methanol (IC50 =15.6 µg/mL) extracts for L. pruinosum. However, for L. tunetanum the best activity was recorded for dichloromethane extract (IC50 =10.4 µg/mL). L. pruinosum extracts displayed the highest cytotoxic activity against MCF-7 and HCT-116 cell lines compared to L. tunetanum ones. The obtained bioactivity discrepancy between Limonium. Mill species was discussed in relation to the organic extract chemical richness.


Assuntos
Antineoplásicos , Plumbaginaceae , Antioxidantes/farmacologia , Antioxidantes/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Plumbaginaceae/química , Áreas Alagadas , Flavonoides/química , Flavonoides/farmacologia
5.
Fitoterapia ; 168: 105538, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37178808

RESUMO

Five undescribed guanidine alkaloids, plumbagines HK (1-4) and plumbagoside E (5), as well as five known analogues (6-10) were isolated from the roots of Plumbago zeylanica. Their structures were established by extensive spectroscopic analyses and chemical methods. In addition, 1-10 were accessed their anti-inflammatory activities by measuring nitric oxide (NO) concentrations in LPS-induced RAW 264.7 cells. However, all compounds especially 1 and 3-5 could not inhibit the secretion of NO but significant increase the secretion of NO. The result reminded us that 1-10 may become potential novel immune potentiators.


Assuntos
Alcaloides , Plumbaginaceae , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Guanidinas/química , Guanidinas/isolamento & purificação , Guanidinas/farmacologia , Estrutura Molecular , Raízes de Plantas/química , Plumbaginaceae/química , Células RAW 264.7 , Animais , Camundongos , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Óxido Nítrico/metabolismo , Macrófagos/efeitos dos fármacos , Espectroscopia de Ressonância Magnética
6.
Planta Med ; 89(11): 1074-1086, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35598603

RESUMO

Periodontal diseases are a global oral health problem affecting almost 10% of the global population. Porphyromonas gingivalis is one of the main bacteria involved in the initiation and progression of inflammatory processes as a result of the action of the cysteine proteases lysin- and arginine-gingipain. Surelease/polycarbophil microparticles containing a lyophilized proanthocyanidin-enriched fraction from the rhizomes of Limonium brasiliense, traditionally named "baicuru" (ethyl acetate fraction), were manufactured. The ethyl acetate fraction was characterized by UHPLC by the presence of samarangenins A and B (12.10 ± 0.07 and 21.05 ± 0.44%, respectively) and epigallocatechin-3-O-gallate (13.44 ± 0.27%). Physiochemical aspects of Surelease/polycarbophil microparticles were characterized concerning particle size, zeta potential, entrapment efficiency, ethyl acetate fraction release, and mucoadhesion. Additionally, the presence of the ethyl acetate fraction-loaded microparticles was performed concerning potential influence on viability of human buccal KB cells, P. gingivalis adhesion to KB cells, gingipain activity, and P. gingivalis biofilm formation. In general, all Surelease/polycarbophil microparticles tested showed strong adhesion to porcine cheek mucosa (93.1 ± 4.2% in a 30-min test), associated with a prolonged release of the ethyl acetate fraction (up to 16.5 ± 0.8% in 24 h). Preincubation of KB cells with Surelease/polycarbophil microparticles (25 µg/mL) resulted in an up to 93 ± 2% reduced infection rate by P. gingivalis. Decreased activity of the P. gingivalis-specific virulence factors lysin- and arginine-gingipain proteases by Surelease/polycarbophil microparticles was confirmed. Surelease/polycarbophil microparticles decreased biofilm formation of P. gingivalis (97 ± 2% at 60 µg/mL). Results from this study prove the promising activity of Surelease/polycarbophil microparticles containing ethyl acetate fraction microparticles as a prophylaxis strategy to prevent the recurrence of P. gingivalis.


Assuntos
Plumbaginaceae , Proantocianidinas , Humanos , Animais , Suínos , Cisteína Endopeptidases Gingipaínas , Porphyromonas gingivalis , Adesinas Bacterianas , Proantocianidinas/farmacologia , Cisteína Endopeptidases , Plumbaginaceae/química
7.
Nutrients ; 14(19)2022 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-36235564

RESUMO

The purpose of this study was to examine whether Limonium tetragonum, cultivated in a smart-farming system with LED lamps, could increase exercise capacity in mice. C57BL/6 male mice were orally administered vehicle or Limonium tetragonum water extract (LTE), either 30 or 100 mg/kg, and were subjected to moderate intensity treadmill exercise for 4 weeks. Running distance markedly increased in the LTE group (100 mg/kg) by 80 ± 4% compared to the vehicle group, which was accompanied by a higher proportion of oxidative fibers (6 ± 6% vs. 10 ± 4%). Mitochondrial DNA content and gene expressions related to mitochondrial biogenesis were significantly increased in LTE-supplemented gastrocnemius muscles. At the molecular level, the expression of PGC-1α, a master regulator of fast-to-slow fiber-type transition, was increased downstream of the PKA/CREB signaling pathway. LTE induction of the PKA/CREB signaling pathway was also observed in C2C12 cells, which was effectively suppressed by PKA inhibitors H89 and Rp-cAMP. Altogether, these findings indicate that LTE treatment enhanced endurance exercise capacity via an improvement in mitochondrial biosynthesis and the increases in the formation of oxidative slow-twitch fibers. Future study is warranted to validate the exercise-enhancing effect of LTE in the human.


Assuntos
Condicionamento Físico Animal , Extratos Vegetais , Plumbaginaceae , Corrida , Animais , DNA Mitocondrial/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Músculo Esquelético/metabolismo , Biogênese de Organelas , Estresse Oxidativo , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/genética , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/metabolismo , Condicionamento Físico Animal/fisiologia , Resistência Física , Extratos Vegetais/farmacologia , Plumbaginaceae/química
8.
Int J Nanomedicine ; 16: 8221-8233, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34955639

RESUMO

INTRODUCTION: Plumbago indica L. is considered a valuable source in the Plumbaginaceae family for various types of active compound such as alkaloids, phenolics and saponins. To promote the usage of P. indica in the bionanotechnology field, zinc oxide nanoparticles (ZnONPs) were biosynthesized by using its alcoholic extract. The inhibitory effects of ZnONPs and the plant extract were also evaluated against HSV-1. METHODS: ZnONPs were described by the following techniques, UV-visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), zeta potential, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and x-ray diffraction (XRD). The phenolic and flavonoid contents of P. indica extract, which are accountable for bioreduction, formation and stabilization of the nanoparticles, were analyzed by HPLC technique. The antiviral assessment was implemented on both agents by using Vero cell lines. RESULTS: DLS revealed that the average size of ZnONPs was 32.58 ± 7.98 nm and the zeta potential was -20.8 mV. The observation of TEM analysis revealed that the particle size of ZnONPs varied from 2.56 to 8.83 nm. The XRD analysis verified the existence of pure crystals of hexagonal shapes of nanoparticles of ZnO with a main average size of 35.28 nm that is approximating to the values of particle size acquired by SEM analysis (19.64 and 23.21 nm). The HPLC analysis of P. indica ethanolic extract showed that gallic acid, chlorogenic acid and rutin were the major compounds, with concentrations equal to 8203.99, 2965.95 and 1144.99 µg/g, respectively. Regarding the antiviral assessment, the synthesized uncalcinated ZnONPs were found to exhibit a promising activity against HSV-1, with CC50 and IC50 values equal to 43.96 ± 1.39 and 23.17 ± 2.29 µg/mL, respectively. CONCLUSION: The green synthesized ZnONPs are considered promising adjuvants to enhance the efficacy of HSV-1 drugs.


Assuntos
Antivirais , Herpesvirus Humano 1 , Nanopartículas Metálicas , Plumbaginaceae , Óxido de Zinco , Antivirais/farmacologia , Herpesvirus Humano 1/efeitos dos fármacos , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Óxido de Zinco/farmacologia
9.
Molecules ; 26(13)2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-34279385

RESUMO

This work aimed to evaluate the phenolic content and in vitro antioxidant, antimicrobial and enzyme inhibitory activities of the methanol extracts and their fractions of two edible halophytic Limonium species, L. effusum (LE) and L. sinuatum (LS). The total phenolic content resulted about two-fold higher in the ethyl acetate fraction of LE (522.82 ± 5.67 mg GAE/g extract) than in that of LS (274.87 ± 1.87 mg GAE/g extract). LC-MS/MS analysis indicated that tannic acid was the most abundant phenolic acid in both species (71,439.56 ± 3643.3 µg/g extract in LE and 105,453.5 ± 5328.1 µg/g extract in LS), whereas hyperoside was the most abundant flavonoid (14,006.90 ± 686.1 µg/g extract in LE and 1708.51 ± 83.6 µg/g extract in LS). The antioxidant capacity was evaluated by DPPH and TAC assays, and the stronger antioxidant activity in ethyl acetate fractions was highlighted. Both species were more active against Gram-positive bacteria than Gram negatives and showed considerable growth inhibitions against tested fungi. Interestingly, selective acetylcholinesterase (AChE) activity was observed with LE and LS. Particularly, the water fraction of LS strongly inhibited AChE (IC50 = 0.199 ± 0.009 µg/mL). The ethyl acetate fractions of LE and LS, as well as the n-hexane fraction of LE, exhibited significant antityrosinase activity (IC50 = 245.56 ± 3.6, 295.18 ± 10.57 and 148.27 ± 3.33 µg/mL, respectively). The ethyl acetate fraction and methanol extract of LS also significantly inhibited pancreatic lipase (IC50 = 83.76 ± 4.19 and 162.2 ± 7.29 µg/mL, respectively). Taken together, these findings warrant further investigations to assess the potential of LE and LS as a bioactive source that can be exploited in pharmaceutical, cosmetics and food industries.


Assuntos
Compostos Fitoquímicos/química , Extratos Vegetais/química , Plumbaginaceae/química , Polifenóis/análise , Acetilcolinesterase/metabolismo , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Proteínas de Peixes/antagonistas & inibidores , Proteínas de Peixes/metabolismo , Lipase/antagonistas & inibidores , Monofenol Mono-Oxigenase/antagonistas & inibidores , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia
10.
Chem Biodivers ; 18(9): e2100278, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34227240

RESUMO

This work aimed to investigate, for the first time, the chemical composition, antioxidant, antiparasitic, cytotoxicity, and antimicrobial activities of the aromatic plant Limonium oleifolium Mill. essential oil (EO) and organic extracts. L. oleifolium aerial parts essential oil was analyzed by GC-FID and GC-MS, and 46 constituents representing 98.25±1.12 % of the oil were identified. γ-Muurolene (10.81±0.07 %), cis-caryophyllene (7.71±0.06 %), o-cymene (7.07±0.01 %) and α-copaene (5.02±0.05 %) were the essential oil main compounds. The antioxidant activity of L. oleifolium EO and organic extracts (MeOH, CHCl3 , AcOEt, BuOH) was explored using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS, ß-carotene/linoleic acid, cupric reducing antioxidant capacity (CUPRAC), and ferric reducing power assays. The results showed that L. oleifolium EO exhibit antioxidant capacity (IC50 =17.40±1.32 µg/mL for DPPH assay, IC50 =29.82±1.08 µg/mL for ß-carotene assay, IC50 =25.23±1.01 µg/mL for ABTS assay, IC50 =9.11±0.08 µg/mL for CUPRAC assay and IC50 =19.41±2.06 mg/mL for reducing power assay). Additionally, the EO showed significant activity against trophozoite form of Acanthamoeba castellanii (IC50 =7.48±0.41 µg/mL) and promastigote form of Leishmania amazonensis (IC50 =19.36±1.06 µg/mL) and low cytotoxicity on murine macrophages (LC50  90.23±1.09 µg/mL), as well as good antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella oxytoca, and Pseudomonas aeruginosa. These results suggest that L. oleifolium essential oil is a valuable source of bioactive compounds presenting antioxidant, antiparasitic, and antimicrobial activities. Furthermore, it is considered nontoxic.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Antiparasitários/farmacologia , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Acanthamoeba castellanii/efeitos dos fármacos , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antiparasitários/química , Antiparasitários/isolamento & purificação , Bactérias/efeitos dos fármacos , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Leishmania/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Testes de Sensibilidade Parasitária , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ácidos Sulfônicos/antagonistas & inibidores
11.
Food Funct ; 12(8): 3443-3454, 2021 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-33900332

RESUMO

The genus Limonium includes important halophyte plants containing a variety of bioactive compounds of therapeutic interest. In the present work, the untargeted phytochemical profiles of both aerial part and root extracts from six Limonium species namely, L. bellidifolium, L. globuliferum, L. gmelinii, L. lilacinum, L. sinuatum and L. iconicum from Turkey were determined. Furthermore, several biological activities (in vitro antioxidant and enzyme inhibitory effects) were investigated. Overall, significant amounts of total phenolics (43.64-238.18 mg g-1) and flavonoids (1.61-129.69 mg g-1) were recorded. Particularly, the root extracts of L. gmelinii, L. iconicum and L. globuliferum showed the highest total phenolic content (204.13-238.18 mg g-1), whilst the highest total flavonoid content was recorded in the root extracts of L. gmelinii (129.69 mg g-1). Overall, the tested extracts demonstrated potent radical scavenging activities in both DPPH (2,2- diphenyl-1-picrylhydrazyl) and ABTS (3-ethylbenzothiazoline-6-sulphonic acid) (90.10-507.94 mg g-1 and 163.39-1175.34 mg g-1, respectively). However, the highest scavenging potential (p < 0.05) was displayed by the root extracts of L. iconicum. Conversely, the metal chelating ability assay revealed that L. lilacinum root extract showed the highest activity (21.03 mg g-1). Interestingly, all the extracts were found to be active inhibitors of cholinesterases (AChE (acetylcholinesterase): 4.20-5.11 mg GALAE (galantamine equivalent) per g; BChE (butyrylcholinesterase): 3.89-10.75 mg GALAE per g), amylase (0.52-1.09 mmol ACAE (acarbose equivalent) per g) and tyrosinase (119.41-155.67 mg KAE (kojic acid equivalent) per g), unlike for glucosidase (2.31-2.41 mmol ACAE per g). Taken together, these findings demonstrated a diverse chemical profiles and biological of the extracts, to be potentially considered as phytotherapeutic or functional ingredients due to their antioxidant properties and inhibition of key enzymes involved in several diseases.


Assuntos
Suplementos Nutricionais/análise , Metaboloma , Plumbaginaceae/química , Antioxidantes/análise , Inibidores Enzimáticos/análise , Flavonoides/análise , Fenóis/análise , Compostos Fitoquímicos/análise , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Raízes de Plantas/química , Plumbaginaceae/classificação , Especificidade da Espécie , Turquia
12.
Nat Prod Res ; 35(5): 880-883, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31084209

RESUMO

Ikonnikovia kaufmanniana is an endemic plant of Kazakhstan of which phytochemical analysis has not been reported. The present study found out that this species enriched with antioxidant chemicals. Isolation and structural identification processes reveal twelve phenolic compounds (1-12) having dihydroflavanonol, flavonol, isoflavone and flavanol skeletons. The annotation of individual components in the extract was carried out by LC-ESI-MS/MS to represent a chemotaxonomic marker of the target plant. The antioxidant activities of all compounds were screened using three different radical sources (DPPH, ORAC, and hydroxyl radicals). Most compounds (1-11) had significant antioxidant activity against three radical sources, and their efficacies were found to differ by their functionality and skeleton. The potential of the isolated compounds in preventing oxidative damage of DNA was evaluated with pBR322 plasmid DNA. Compounds (1, 5, 7, and 8) had protective effects on DNA damaged with 80% efficacy at 60 µM concentration.


Assuntos
Dano ao DNA , Compostos Fitoquímicos/análise , Componentes Aéreos da Planta/química , Plumbaginaceae/química , Antioxidantes/química , Flavonóis/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Plasmídeos/genética , Polifenóis/análise , Espectrometria de Massas em Tandem
13.
J Ethnopharmacol ; 266: 113457, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33039629

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Trimada is well-known polyherbal Ayurvedic formulation used in Indian Traditional medicine since ancient times. It consisted of three inebriant herbs including "Chitraka" (Plumbago zeylanica Linn. Family- Plumabaginaceae), "Musta" (Cyperus rotundus Linn. Family- Cyperaceae) and Vidanga (Embelia ribes Burm. F. Family- Myrsinaceae) in equal ratios as mentioned in Ayurveda. Trimada is traditionally used to increase the functioning of the digestive system and metabolism. Along with these, it also assists in the reduction of cholesterol as well as reduces stomach aches and chest pain. AIM OF THE STUDY: This study is aimed to identify the metabolites present in this polyherbal formulation. Further, the cytotoxicity and interaction potential of the formulation and individual herbs with Cytochrome P450 isozymes (CYP3A4, 2D6, 2C9, 1A2) was evaluated by MTT assay and CYP450 enzyme inhibition. The concentration of heavy metals was also determined. MATERIAL AND METHODS: Ultra-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UPLC-QTOF-MS) analysis was performed to detect and identify the phytoconstituents in the formulation. Cytotoxicity of the formulation was evaluated by MTT assay. CYP450 enzyme interaction potential of the individual herbs and the Trimada formulation was carried out through CYP-CO assay and fluorometric high throughput screening (HTS) assay for individual isozymes. The content of heavy metal in the formulation was quantified by Atomic Absorption Spectroscopy. RESULTS: Trimada formulation exhibited lower cytotoxicity to human liver carcinoma cell line (HepG2). CYP-CO assay revealed that the interaction potential of individual herbs and Trimada on the liver microsomes was found to be lesser than the standard inhibitor ketoconazole. Individual herbs and Trimada formulation displayed higher IC50 values than the respective standard inhibitors in the fluorimetric assay. UPLC-QTOF-MS analysis showed the presence of a number of active phytoconstituents including sesquiterpenes, phenolic acids, benzoquinones, triterpenes and flavonoids. The heavy metal concentration in the traditional medicinal herbal formulation was found within the approved limit. CONCLUSIONS: This study suggested that the individual herbs and Trimada formulation exhibited low cytotoxicity and contributes insignificant interaction with CYP450 isozymes. So, the formulation is considered to be safe for its therapeutic management without any potential drug interaction involving CYP 450 isozymes.


Assuntos
Sistema Enzimático do Citocromo P-450/efeitos dos fármacos , Ayurveda , Microssomos Hepáticos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Cromatografia Líquida de Alta Pressão , Cyperus/química , Sistema Enzimático do Citocromo P-450/metabolismo , Embelia/química , Células Hep G2 , Ensaios de Triagem em Larga Escala , Humanos , Concentração Inibidora 50 , Isoenzimas , Metais Pesados/análise , Metais Pesados/química , Metais Pesados/isolamento & purificação , Microssomos Hepáticos/metabolismo , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Plumbaginaceae/química
14.
Mini Rev Med Chem ; 21(6): 731-737, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33200707

RESUMO

Cancer is a deadly disease, which has significantly increased in both developed and developing nations. Treatment of cancer utilizing radiotherapy or chemotherapy actuates a few issues which incorporate spewing, sickness, unpalatable reactions, and so forth. In this specific situation, an alternative drug source, which can effectively treat cancer is of prime importance. Products that are obtained from plant sources are utilized for the treatment of various diseases due to their non-harmful nature. Medicinal plants contain different bioactive compounds, which possess an important role in the prevention of different diseases such as cancer. Plumbagin is a bioactive compound, which is mainly present in Plumbaginaceae family and has been explored for its anticancer activity. Plumbagin basically inactivates the Akt/NF-kB, MMP-9 and VEGF pathways that are essential for cancer cell development. Therefore, it is important to review the role of plumbagin in different cancer cells in order to find an alternative drug to overcome this disease. The present review provides a summary of anticancer activity of plumbagin in various cancers and its mode of action.


Assuntos
Antineoplásicos Fitogênicos/química , Naftoquinonas/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Humanos , NF-kappa B/metabolismo , Naftoquinonas/isolamento & purificação , Naftoquinonas/farmacologia , Naftoquinonas/uso terapêutico , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Plumbaginaceae/química , Plumbaginaceae/metabolismo , Transdução de Sinais/efeitos dos fármacos
15.
Braz. arch. biol. technol ; 64: e21200179, 2021. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1153293

RESUMO

HIGHLIGHTS L. duriusculum n-BuOH extract reduces inflammatory responses both in vitro and in vivo. L. duriusculum n-BuOH extract inhibits NF-κB-dependent transcriptional responses. L. duriusculum n-BuOH extract decreases the expression of TNF-α and IL-6 genes.


Abstract Limonium duriusculum is used in folk medicine to treat inflammatory disorders and has gained attention due to its richness in apigenin. The present investigation was performed to evaluate and confirm its anti-inflammatory properties, in cell lines and animal models. The potential anti-inflammatory properties of n-butanol (n-BuOH) extract of L. duriusculum (BEL) and isolated apigenins were examined on NF-κB transcriptional activity in TNFα- or LPS-stimulated cells, and on in vivo acute inflammatory models (carrageenan induced paw edema and peritonitis). BEL treatment was able to inhibit the activity of an NF-κB reporter gene in HCT116 cells both in the absence and in the presence of exogenous TNFα, used as NF-κB pathway inducer. This anti-inflammatory effect was even more potent compared to Apigenin (APG1) and was confirmed using monocyte-derived THP-1 cells treated with LPS to stimulate NF-κB-dependent transcription of IL-6 and TNFα mRNAs. Apigenin7-O-β-(6''-methylglucuronide) (APG2) was instead inactive both in HCT116 and THP-1 cells. BEL (oral, 200 mg/kg) led to paw swelling inhibition, vascular permeability and peritoneal leukocyte and PN migration diminution. Apigenins (intraperitoneal, APG1, APG2: 20 mg/kg) also evoked a significant anti-edema effect, early vascular permeability and leukocyte influx reduction. Collectively, this study demonstrates for the first time the effectiveness of L. duriusculum to inhibit NF-κB-dependent transcriptional responses in HCT116 and THP-1 cells. In vivo studies also established that L. duriusculum possesses a potential anti-inflammatory effect, confirm its traditional, empirical use, that could be attributed to its richness in apigenin.


Assuntos
Humanos , Animais , Masculino , Ratos , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Imunomodulação/efeitos dos fármacos , Anti-Inflamatórios/farmacologia , Interleucina-6 , Ratos Wistar , Modelos Animais , Células THP-1
16.
Folia Med (Plovdiv) ; 62(2): 308-313, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32666745

RESUMO

BACKGROUND: Plumbago zeylanica plant belongs to Plumbaginaceae. The plant is reported for many pharmacological activities. AIM: The objective of the study was to identify fatty acids and non-polar chemical compounds in Plumbago zeylanica leaves. MATERIALS AND METHODS: Petroleum ether extract was prepared using soxhlet apparatus. Saponifiable and unsaponifiable matter was separated with saponification process. To identify fatty acids in saponifiable matter further esterification was performed. Gas chromatography and mass spectrometry analysis was performed of both saponifiable and unsaponifiable fractions. All the fatty acid methyl esters and non-polar chemical compounds were identified using NIST library data. RESULTS: A total of 14 compounds were identified with comparison of NIST data. From that, 8 fatty acid methyl esters and 6 non-polar chemical compounds were identified. Here we have analyzed fatty acids and non-polar chemical compounds by the same GC-MS method. CONCLUSIONS: The present analysis showed that Plumbago Zeylanica leaves contain 8 fatty acids and 6 non-polar chemical compounds. Principal determination of the research was development of efficient method to identify non-polar compound from plant by single injection using chromatographic technique.


Assuntos
Extratos Vegetais/química , Folhas de Planta/química , Plumbaginaceae/química , Ésteres/análise , Ésteres/química , Ácidos Graxos/análise , Ácidos Graxos/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Extratos Vegetais/análise
17.
J Med Food ; 23(6): 633-640, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32311286

RESUMO

Idiopathic pulmonary fibrosis (IPF) is a chronic fibrosing interstitial lung disease with a poor prognosis similar to that of malignancy. The causes of IPF are not clearly known, and there is no effective therapy to date. In this study, the natural compound plumbagin, which was isolated from Plumbago rosea root extract, was screened for p300 inhibitory activity. Plumbagin specifically inhibited the activity of p300 toward histone acetyltransferases. Plumbagin treatment significantly suppressed transforming growth factor-ß-induced profibrotic target-gene expression and proliferation of fibroblast cell lines. Moreover, plumbagin significantly inhibited bleomycin-induced pulmonary fibrosis in mice. Taken together, these data demonstrate the inhibitory effects of plumbagin on lung fibrosis and its promise as a therapeutic agent for IPF.


Assuntos
Naftoquinonas/uso terapêutico , Fibrose Pulmonar/tratamento farmacológico , Fatores de Transcrição de p300-CBP/antagonistas & inibidores , Animais , Bleomicina , Linhagem Celular , Fibroblastos/efeitos dos fármacos , Pulmão/efeitos dos fármacos , Pulmão/patologia , Camundongos , Raízes de Plantas/química , Plumbaginaceae/química , Fibrose Pulmonar/induzido quimicamente
18.
Biosci Biotechnol Biochem ; 84(1): 134-142, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31490096

RESUMO

Plumbagin (PLB), an alkaloid obtained from the roots of the plants of Plumbago genus, is an inhibitor of NADPH oxidase 4 (NOX4). This study aimed to investigate the beneficial effect of PLB against oxygen-glucose deprivation/reoxygenation (OGDR)-induced neuroinjury in human SH-SY5Y neuronal cultures. Our results showed that OGD/R stimulated NOX4 protein expression and reactive oxygen species (ROS) production in SH-SY5Y cells, whereas increased 4-hydroxynonenal (4-HNE) and malondialdehyde (MDA) production, resulting in the activation of the NLRP3 inflammasome. And PLB pretreatment reduced the ROS production by regulating the expression of NOX4 and downregulated NF-κB signaling which was induced by OGDR. Furthermore, PLB inhibited OGDR induced NLRP3 inflammasome activation but not PARP1. Overall, PLB improved OGDR induced neuroinjury by inhibiting NOX4-derived ROS-activated NLRP3 inflammasome.


Assuntos
Hipóxia Celular/efeitos dos fármacos , Glucose/deficiência , Inflamassomos/metabolismo , NADPH Oxidase 4/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Naftoquinonas/farmacologia , Neurônios/metabolismo , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Apoptose/efeitos dos fármacos , Isquemia Encefálica/metabolismo , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , NF-kappa B/antagonistas & inibidores , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas/química , Plumbaginaceae/química
19.
An Acad Bras Cienc ; 91(2): e20180468, 2019 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-31241699

RESUMO

This study evaluates the antibacterial, cytotoxic activities, and phytochemical composition, of Callistemon citrinus, Hibiscus rosa-sinensis and Plumbago auriculata leaves and flowers, three ornamental plants in Mexico. However, in other countries offers a range of other uses. Ethanol extracts of C. citrinus leaf and flower presented stronger antibacterial activity than the extracts obtained from the other two plants. C. citrinus leaf showed low cytotoxicity (LC50 <600 µg/mL) on the brine shrimp test, whereas the ethanol extracts of H. rosa-sinensis and P. auriculata leaves showed no cytotoxic activity. Flower extracts obtained from the three plants did no exhibit cytotoxicity. GC-MS analysis revealed that the ethanol extract of P. auriculata leaf contained lupeol triterpene and lupeol acetate, neither of them have been previously reported in this genus. Gamma sitosterol was present in the leaf and flower extracts of P. auriculata. Higher contents of linoleic and linolenic acids were found in extracts of H. rosa-sinensis leaves and flowers. The ability of the ethanol extracts of C. citrinus leaves and flowers to inhibit the growth of Gram-positive and Gram-negative bacteria indicates a potentially broad antimicrobial spectrum. Moreover, the absence of cytotoxicity suggests the potential use of this plant to treat microbial infections.


Assuntos
Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hibiscus/química , Myrtaceae/química , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Animais , Antibacterianos/toxicidade , Artemia/efeitos dos fármacos , México , Testes de Sensibilidade Microbiana , Extratos Vegetais/toxicidade , Testes de Toxicidade
20.
Lett Appl Microbiol ; 69(1): 41-49, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31044446

RESUMO

Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) is a bicyclic naphthoquinone, found in three major plant families viz. Plumbaginaceae, Ebenceae and Droseraceae. The phytochemical is reported to exhibit various pharmacological properties. In this study, plumbagin isolated from Plumbago zeylanica L. was investigated for its in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA). Against 100 MRSA isolates that included multi-drug-resistant phenotypes, plumbagin showed consistent activity with a narrow minimum inhibitory concentration (MIC) range of 4-8 µg ml-1 . The time-kill study revealed 99% kill of a reference MRSA strain, 8 h after exposure to plumbagin. In the combination MIC study using the reference MRSA strain, plumbagin showed synergistic effect with ciprofloxacin and piperacillin while additive or indifference effect with other commonly used antibiotics. The transmission electron micrograph of the reference MRSA strain treated with plumbagin confirmed cell wall and cytoplasmic changes. Our results demonstrated potent anti-MRSA activity of plumbagin which was not impacted by multi-drug resistance. This is a first ever study that evaluated in vitro anti-MRSA activity of plumbagin employing large number of MRSA isolates. The findings of this study support the need for the further investigation on this phytochemical agent for therapeutic application. SIGNIFICANCE AND IMPACT OF THE STUDY: This study revealed phytochemical plumbagin's potent and consistent in vitro antibacterial activity against clinically problematic methicillin-resistant Staphylococcus aureus (MRSA) including multi-drug-resistant (MDR) phenotypes. The study results support further research to assess the clinical scope of plumbagin.


Assuntos
Antibacterianos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Naftoquinonas/farmacologia , Extratos Vegetais/farmacologia , Plumbaginaceae/química , Parede Celular/efeitos dos fármacos , Ciprofloxacina/farmacologia , Citoplasma/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Staphylococcus aureus Resistente à Meticilina/isolamento & purificação , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/farmacologia , Piperacilina/farmacologia
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