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1.
Sci Rep ; 14(1): 10592, 2024 05 08.
Artículo en Inglés | MEDLINE | ID: mdl-38719900

RESUMEN

Umbelliferous (Apiaceae) vegetables are widely consumed worldwide for their nutritive and health benefits. The main goal of the current study is to explore the compositional heterogeneity in four dried umbelliferous vegetables viz, celery, coriander, dill, and parsley targeting their volatile profile using gas chromatography-mass spectrometry (GC-MS). A total of 133 volatile metabolites were detected belonging to 12 classes. Aromatic hydrocarbons were detected as the major components of the analyzed vegetables accounting ca. 64.0, 62.4, 59.5, and 47.8% in parsley, dill, celery, and coriander, respectively. Aliphatic hydrocarbons were detected at ca. 6.39, 8.21, 6.16, and 6.79% in parsley, dill, celery, and coriander, respectively. Polyunsaturated fatty acids (PUFA) of various health benefits were detected in parsley and represented by roughanic acid and α-linolenic acid at 4.99 and 0.47%, respectively. Myristicin and frambinone were detected only in parsley at 0.45 and 0.56%. Investigation of antibacterial activity of umbelliferous vegetables n-hexane extract revealed a moderate antibacterial activity against Gram-positive and Gram-negative bacteria with higher activity for celery and dill against Staphylococcus aureus with inhibition zone 20.3 mm compared to 24.3 mm of the standard antibacterial drug.


Asunto(s)
Antibacterianos , Cromatografía de Gases y Espectrometría de Masas , Hexanos , Fitoquímicos , Verduras , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/análisis , Verduras/química , Fitoquímicos/química , Fitoquímicos/análisis , Fitoquímicos/farmacología , Hexanos/química , Apiaceae/química , Pruebas de Sensibilidad Microbiana , Derivados de Alilbenceno , Ácido alfa-Linolénico/análisis , Ácido alfa-Linolénico/farmacología , Aceites Volátiles/farmacología , Aceites Volátiles/química , Aceites de Plantas/farmacología , Aceites de Plantas/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Ácidos Grasos Insaturados/análisis , Staphylococcus aureus/efectos de los fármacos , Dioxolanos
2.
Sci Rep ; 14(1): 10675, 2024 05 09.
Artículo en Inglés | MEDLINE | ID: mdl-38724667

RESUMEN

Trillium govanianum is traditionally used to treat innumerable alignments like sexual disorders, cancer, inflammation etc. Mainly rhizomes of T. govanianum have been explored for phytochemical profiling but comprehensive metabolomics of other parts has not been yet deeply investigated. Thus, current study was aimed for organs-specific (roots, rhizomes, rhizomatous buds, stems, leaves, and fruits) phytochemical profiling of T. govanianum via metabolomics approach. Targeted (steroidal saponins and free sugars) and non-targeted metabolomics were performed by UPLC-PDA/ELSD & UHPLC-Q-TOF-IMS. Among steroidal compounds, 20-hydroxyecdysone, pennogenin-3-O-ß-chacotrioside, dioscin were found predominantly in all samples while diosgenin was identified only in rhizomes. Further, four free sugars viz. 2-deoxyribose (116.24 ± 1.26 mg/g: leaves), fructose (454.76 ± 12.14 mg/g: rhizomes), glucose (243.21 ± 7.53 mg/g: fruits), and galactose (69.06 ± 2.14 mg/g: fruits) were found significant in respective parts of T. govanianum. Elemental analysis of targeted samples was determined by atomic absorption spectrophotometer. Heavy metals (Cd, Hg, Pd, As) were absent while micro- (Mn, Na, Zn, Cu) and macro- (Ca, Fe, Mg, K) elements were found in all samples. Furthermore, UHPLC-Q-TOF-IMS had identified 103 metabolites based on their mass fragmentation patterns and 839 were tentatively predicted using METLIN database. The multivariate statistical analysis showed organs specific clustering and variance of metabolites. Apart from this, extracts were evaluated for in vitro anticholinesterase activity, and found potentials inhibitors with IC50 values 2.02 ± 0.15 to 27.65 ± 0.89 mg/mL and 3.58 ± 0.12 to 16.81 ± 2.48 mg/mL of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme, respectively. Thus, comprehensive metabolomics and anti-cholinesterase activity of different parts of T. govanianum would lay the foundation for improving medicinal importance and health benefits of T. govanianum.


Asunto(s)
Inhibidores de la Colinesterasa , Metabolómica , Trillium , Metabolómica/métodos , Inhibidores de la Colinesterasa/farmacología , Trillium/química , Trillium/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/química , Hojas de la Planta/química , Hojas de la Planta/metabolismo , Fitoquímicos/farmacología , Fitoquímicos/química , Fitoquímicos/metabolismo , Fitoquímicos/análisis , Cromatografía Líquida de Alta Presión , Rizoma/química , Raíces de Plantas/química , Raíces de Plantas/metabolismo
3.
Int J Mol Sci ; 25(9)2024 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-38731845

RESUMEN

Moringa oleifera leaves are rich sources of bioactive compounds with potential health benefits, including antioxidants and anti-inflammatory agents. Pressurized liquid extraction (PLE) stands out as a promising technique for effectively extracting valuable compounds from natural sources. In this study, we aimed to optimize PLE parameters, such as temperature, extraction duration, and pressure, to maximize bioactive compound (polyphenols, flavonoids, and ascorbic acid) yield from M. oleifera leaves and evaluate their antioxidant and anti-inflammatory activities. According to the outcomes of this research, the maximum achieved total polyphenol content was 24.10 mg gallic acid equivalents (GAE)/g of dry weight (dw), and the total flavonoid content was increased up to 19.89 mg rutin equivalents (RtE)/g dw. Moreover, after HPLC-DAD analysis, neochlorogenic and chlorogenic acids, catechin and epicatechin, rutin, and narirutin were identified and quantified. As far as the optimum ascorbic acid content is concerned, it was found to be 4.77 mg/g dw. The antioxidant activity was evaluated by three different methods: ferric reducing antioxidant power (FRAP), the DPPH method, and the anti-hydrogen peroxide activity (AHPA) method, resulting in 124.29 µmol ascorbic acid equivalent (AAE)/g dw, 131.28 µmol AAE/g dw, and 229.38 µmol AAE/g dw values, respectively. Lastly, the albumin denaturation inhibition was found to be 37.54%. These findings underscore the potential of PLE as an efficient extraction method for preparing extracts from M. oleifera leaves with the maximum content of bioactive compounds.


Asunto(s)
Antioxidantes , Moringa oleifera , Extractos Vegetales , Hojas de la Planta , Moringa oleifera/química , Hojas de la Planta/química , Antioxidantes/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/química , Flavonoides/aislamiento & purificación , Flavonoides/análisis , Flavonoides/química , Flavonoides/farmacología , Polifenoles/aislamiento & purificación , Polifenoles/farmacología , Polifenoles/análisis , Polifenoles/química , Ácido Ascórbico/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Cromatografía Líquida de Alta Presión/métodos , Presión , Extracción Líquido-Líquido/métodos , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación
4.
Int J Mol Sci ; 25(9)2024 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-38732062

RESUMEN

Prunella vulgaris (PV) is one of the most commonly used nutraceuticals as it has been proven to have anti-inflammatory and antioxidant properties. The aim of this study was to evaluate the phytochemical composition of PV and its in vivo antioxidant properties. A phytochemical analysis measuring the total phenolic content (TPC), the identification of phenolic compounds by HPLC-DAD-ESI, and the evaluation of the in vitro antioxidant activity by the DPPH assay of the extract were performed. The antioxidant effects on inflammation induced by turpentine oil were experimentally tested in rats. Seven groups with six animals each were used: a control group, the experimental inflammation treatment group, the experimental inflammation and diclofenac sodium (DS) treatment group, and four groups with their inflammation treated using different dilutions of the extract. Serum redox balance was assessed based on total oxidative status (TOS), nitric oxide (NO), malondialdehyde (MDA), total antioxidant capacity (TAC), total thiols, and an oxidative stress index (OSI) contents. The TPC was 0.28 mg gallic acid equivalents (GAE)/mL extract, while specific representatives were represented by caffeic acid, p-coumaric acid, dihydroxybenzoic acid, gentisic acid, protocatechuic acid, rosmarinic acid, vanillic acid, apigenin-glucuronide, hesperidin, kaempferol-glucuronide. The highest amount (370.45 µg/mL) was reported for hesperidin, which is a phenolic compound belonging to the flavanone subclass. The antioxidant activity of the extracts, determined using the DPPH assay, was 27.52 mmol Trolox/mL extract. The PV treatment reduced the oxidative stress by lowering the TOS, OSI, NO, and MDA and by increasing the TAC and thiols. In acute inflammation, treatment with the PV extract reduced oxidative stress, with lower concentrations being more efficient and having a better effect than DS.


Asunto(s)
Antioxidantes , Inflamación , Estrés Oxidativo , Fitoquímicos , Extractos Vegetales , Prunella , Animales , Antioxidantes/farmacología , Antioxidantes/química , Ratas , Prunella/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Fitoquímicos/química , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Estrés Oxidativo/efectos de los fármacos , Masculino , Antiinflamatorios/farmacología , Antiinflamatorios/química , Fenoles/farmacología , Fenoles/análisis , Ratas Wistar
6.
PLoS One ; 19(5): e0302795, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38743731

RESUMEN

BACKGROUND: Natural propolis has been used since decades owing to its broad-spectrum activities. Burn injuries are a global health problem with negative impacts on communities. Bacterial infections usually accompany burns, which demand implementation of antibiotics. Antibiotics abuse led to emergence of microbial drug resistance resulting in poor treatment outcomes. In such instances, the promising alternative would be natural antimicrobials such as propolis. OBJECTIVE: Full chemical profiling of propolis and evaluation of in vitro antibacterial, antioxidant and anti-inflammatory activities as well as in vivo burn healing properties. METHODS: Chemical profiling of propolis was performed using Liquid chromatography (UHPLC/MS-PDA and HPLC-PDA). In vitro assessment was done using Disc Diffusion susceptibility test against Staphylococcus aureus and infected burn wound mice model was used for in vivo assessment. In vitro antioxidant properties of propolis were assessed using DPPH, ABTS and FRAP techniques. The anti-inflammatory effect of propolis was assessed against lipopolysaccharide/interferon-gamma mediated inflammation. RESULTS: UHPLC/MS-PDA results revealed identification of 71 phytochemicals, mainly flavonoids. Upon flavonoids quantification (HPLC-PDA), Pinocembrin, chrysin and galangin recorded high content 21.58±0.84, 22.73±0.68 and 14.26±0.70 mg/g hydroalcoholic propolis extract, respectively. Propolis showed concentration dependent antibacterial activity in vitro and in vivo burn healing via wound diameter reduction and histopathological analysis without signs of skin irritation in rabbits nor sensitization in guinea pigs. Propolis showed promising antioxidant IC50 values 46.52±1.25 and 11.74±0.26 µg/mL whereas FRAP result was 445.29±29.9 µM TE/mg. Anti-inflammatory experiment results showed significant increase of Toll-like receptor 4 (TLR4), interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α) mRNA levels. Nitric oxide and iNOS were markedly increased in Griess assay and western blot respectively. However, upon testing propolis against LPS/IFN-γ-mediated inflammation, TLR4, IL-6 and TNF-α expression were downregulated at transcriptional and post-transcriptional levels. CONCLUSION: Propolis proved to be a promising natural burn healing agent through its antibacterial, antioxidant and anti-inflammatory activities.


Asunto(s)
Antibacterianos , Antiinflamatorios , Antioxidantes , Quemaduras , Própolis , Staphylococcus aureus , Cicatrización de Heridas , Própolis/química , Própolis/farmacología , Animales , Quemaduras/tratamiento farmacológico , Quemaduras/patología , Antioxidantes/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antibacterianos/farmacología , Ratones , Cicatrización de Heridas/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Masculino , Fitoquímicos/farmacología , Fitoquímicos/química , Cromatografía Líquida de Alta Presión , Flavonoides/farmacología , Pruebas de Sensibilidad Microbiana
7.
PLoS One ; 19(5): e0301201, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38743750

RESUMEN

With the rise of AMR the management of wound infections are becoming a big challenge. This has been attributed to the fact that most wound bacterial isolates have been found to possess various virulence factors like enzymes, toxins & biofilms production. Therefore, need for discovery of new lead compounds is paramount as such factors make these microbes to be resistant to already existing arsenal of antibiotics or even the immune system. This study aimed at documenting the nutritional, physicochemical, phytochemical and antibacterial properties of stingless bee honey. Isolation and characterization of bacterial isolates from 34 samples obtained from wounds of outpatients and surgical wards of Nakuru County Referral Hospital, Kenya was done. Various bacterial isolates (43) were isolated Staphylococcus aureus (34.8%) being predominant, followed by Pseudomonas aeruginosa (27.9%), Klebsiella pneumoniae (23.3%) and Escherichia coli (14.0%). A total of 36 out of the total isolates were genotypically characterized using molecular techniques detecting the prevalence of the following virulence genes; 16 srRNA (756 bp), hla (229 bp), cnf1 (426 bp), cnf2 (543 bp), hlyA (1011 bp), rmpA (461 bp), lasL (600 bp), gyrB (411 bp), khe (77 bp) and magA (128 bp). An assessment of the in vitro antibacterial activity of 26 stingless bee honey samples collected from their cerumen egg-shaped pots in Marigat sub-County, Baringo County, Kenya was done. Antibacterial properties of the stingless bee honey was done with varying susceptibility patterns being observed at different concentrations of honey impregnated discs (10x104, 20x104, 50x104 and 75x104 ml µg/ ml) giving mean inhibition diameters of 18.23 ± 0.4 mm (Staphylococcus aureus), 17.49 ± 0.3 mm (Pseudomonas aeruginosa), 16.05 ± 0.6 mm (Klebsiella pneumoniae) and 10.19 ± 0.5 mm (Escherichia coli) with a mean range of 14.54 ± 2.0 mm to 17.58 ± 3 mm. Higher susceptibility to honey was recorded across all the bacterial isolates compared to conventional antibiotics while the mean MIC and MBC of the honey were recorded at 62.5 ml µg/ ml and 250 ml µg/ ml respectively. Control bacterial isolates Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 27736 and Pseudomonas aeruginosa ATCC 27858 were used in the analysis. The stingless bee honey was found to be rich in various nutritive components like sugar (89.85 ± 5.07 g/100 g) and moisture (81.75 ± 10.35 mg/g) with a significant difference of P <0.05 as the main antibacterial components. Additionally, the stingless honey did possess water soluble vitamins, proteins and minerals of which potassium was the most dominant one. In regard to phytochemicals, on our preliminary analysis phenolic, flavonoid and carotenoid compounds were found to be present with phenolic compounds being the most dominant one. Stingless bee honey from Marigat, has antimicrobial properties which could be attributed to the rich phytochemicals it possesses and its physicochemical properties in addition to its high nutritive value.


Asunto(s)
Antibacterianos , Miel , Pruebas de Sensibilidad Microbiana , Miel/análisis , Antibacterianos/farmacología , Animales , Abejas/microbiología , Humanos , Bacterias/efectos de los fármacos , Bacterias/aislamiento & purificación , Fitoquímicos/farmacología , Infección de Heridas/microbiología , Infección de Heridas/prevención & control , Infección de Heridas/tratamiento farmacológico , Factores de Virulencia
8.
Med Oncol ; 41(6): 144, 2024 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-38717574

RESUMEN

Peganum harmala has been extensively employed in Algerian traditional medicine practices. This study aimed to explore the impact of n-butanol (n-BuOH) extract sourced from Peganum harmala seeds on cell proliferation, cell migration, and angiogenesis inhibition. Cytotoxic potential of n-BuOH extract was evaluated using MTT (3-(4,5-dimethylthiazol-2-yl) 2,5 diphenyltetrazolium bromide) assay against human breast adenocarcinoma MCF-7 cells, cell migration was determined using scratch assay, and anti-angiogenic effect was evaluated through macroscopic and histological examinations conducted on chick embryo chorioallantoic membrane. Additionally, this research estimated the phytochemical profile of n-BuOH extract. Fifteen phenolic compounds were identified using Ultra-performance liquid chromatography UPLC-ESI-MS-MS analysis. In addition, the n-BuOH extract of P. harmala exhibited potent antioxidant and free radical scavenging properties. The n-BuOH extract showed potent cytotoxicity against MCF-7 cell with an IC50 value of 8.68 ± 1.58 µg/mL. Furthermore, n-BuOH extract significantly reduced migration. A strong anti-angiogenic activity was observed in the groups treated with n-BuOH extract in comparison to the negative control. Histological analysis confirmed the anti-angiogenic effect of the n-BuOH extract. This activity is probably a result of the synergistic effects produced by different polyphenolic classes.


Asunto(s)
Inhibidores de la Angiogénesis , Movimiento Celular , Peganum , Fenoles , Extractos Vegetales , Humanos , Movimiento Celular/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Peganum/química , Embrión de Pollo , Fenoles/farmacología , Fenoles/análisis , Inhibidores de la Angiogénesis/farmacología , Células MCF-7 , Animales , Proliferación Celular/efectos de los fármacos , Fitoquímicos/farmacología , Fitoquímicos/química , Antioxidantes/farmacología , Antioxidantes/química , Antineoplásicos Fitogénicos/farmacología , Membrana Corioalantoides/efectos de los fármacos , Membrana Corioalantoides/irrigación sanguínea
9.
Med Oncol ; 41(6): 134, 2024 May 04.
Artículo en Inglés | MEDLINE | ID: mdl-38703282

RESUMEN

Primary liver cancer is a type of cancer that develops in the liver. Hepatocellular carcinoma is a primary liver cancer that usually affects adults. Liver cancer is a fatal global condition that affects millions of people worldwide. Despite advances in technology, the mortality rate remains alarming. There is growing interest in researching alternative medicines to prevent or reduce the effects of liver cancer. Recent studies have shown growing interest in herbal products, nutraceuticals, and Chinese medicines as potential treatments for liver cancer. These substances contain unique bioactive compounds with anticancer properties. The causes of liver cancer and potential treatments are discussed in this review. This study reviews natural compounds, such as curcumin, resveratrol, green tea catechins, grape seed extracts, vitamin D, and selenium. Preclinical and clinical studies have shown that these medications reduce the risk of liver cancer through their antiviral, anti-inflammatory, antioxidant, anti-angiogenic, and antimetastatic properties. This article discusses the therapeutic properties of natural products, nutraceuticals, and Chinese compounds for the prevention and treatment of liver cancer.


Asunto(s)
Neoplasias Hepáticas , Transducción de Señal , Humanos , Neoplasias Hepáticas/prevención & control , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/metabolismo , Transducción de Señal/efectos de los fármacos , Carcinoma Hepatocelular/prevención & control , Carcinoma Hepatocelular/tratamiento farmacológico , Carcinoma Hepatocelular/metabolismo , Animales , Suplementos Dietéticos , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/uso terapéutico , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico
10.
BMC Complement Med Ther ; 24(1): 183, 2024 May 04.
Artículo en Inglés | MEDLINE | ID: mdl-38704537

RESUMEN

BACKGROUND: Highlighting affordable alternative crops that are rich in bioactive phytoconstituents is essential for advancing nutrition and ensuring food security. Amaranthus blitum L. (AB) stands out as one such crop with a traditional history of being used to treat intestinal disorders, roundworm infections, and hemorrhage. This study aimed to evaluate the anthelmintic and hematologic activities across various extracts of AB and investigate the phytoconstituents responsible for these activities. METHODS: In vitro anthelmintic activity against Trichinella spiralis was evaluated in terms of larval viability reduction. The anti-platelet activities were assessed based on the inhibitory effect against induced platelet aggregation. Further, effects on the extrinsic pathway, the intrinsic pathway, and the ultimate common stage of blood coagulation, were monitored through measuring blood coagulation parameters: prothrombin time (PT), activated partial thromboplastin time (aPTT), and thrombin time (TT), respectively. The structures of isolated compounds were elucidated by spectroscopic analysis. RESULTS: Interestingly, a previously undescribed compound (19), N-(cis-p-coumaroyl)-ʟ-tryptophan, was isolated and identified along with 21 known compounds. Significant in vitro larvicidal activities were demonstrated by the investigated AB extracts at 1 mg/mL. Among tested compounds, compound 18 (rutin) displayed the highest larvicidal activity. Moreover, compounds 19 and 20 (N-(trans-p-coumaroyl)-ʟ-tryptophan) induced complete larval death within 48 h. The crude extract exhibited the minimal platelet aggregation of 43.42 ± 11.69%, compared with 76.22 ± 14.34% in the control plasma. Additionally, the crude extract and two compounds 19 and 20 significantly inhibited the extrinsic coagulation pathway. CONCLUSIONS: These findings extend awareness about the nutritional value of AB as a food, with thrombosis-preventing capabilities and introducing a promising source for new anthelmintic and anticoagulant agents.


Asunto(s)
Amaranthus , Antihelmínticos , Anticoagulantes , Fitoquímicos , Extractos Vegetales , Inhibidores de Agregación Plaquetaria , Animales , Antihelmínticos/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Inhibidores de Agregación Plaquetaria/farmacología , Anticoagulantes/farmacología , Larva/efectos de los fármacos
11.
Malar J ; 23(1): 141, 2024 May 11.
Artículo en Inglés | MEDLINE | ID: mdl-38734650

RESUMEN

BACKGROUND: The development of resistance by Plasmodium falciparum is a burdening hazard that continues to undermine the strides made to alleviate malaria. As such, there is an increasing need to find new alternative strategies. This study evaluated and validated 2 medicinal plants used in traditional medicine to treat malaria. METHODS: Inspired by their ethnobotanical reputation of being effective against malaria, Ziziphus mucronata and Xysmalobium undulutum were collected and sequentially extracted using hexane (HEX), ethyl acetate (ETA), Dichloromethane (DCM) and methanol (MTL). The resulting crude extracts were screened for their anti-malarial and cytotoxic potential using the parasite lactate dehydrogenase (pLDH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, respectively. This was followed by isolating the active compounds from the DCM extract of Z. mucronata using silica gel chromatography and structural elucidation using spectroscopic techniques (NMR: 1H, 12C, and DEPT). The active compounds were then targeted against P. falciparum heat shock protein 70-1 (PfHsp70-1) using Autodock Vina, followed by in vitro validation assays using ultraviolet-visible (UV-VIS) spectroscopy and the malate dehydrogenase (MDH) chaperone activity assay. RESULTS: The extracts except those of methanol displayed anti-malarial potential with varying IC50 values, Z. mucronata HEX (11.69 ± 3.84 µg/mL), ETA (7.25 ± 1.41 µg/mL), DCM (5.49 ± 0.03 µg/mL), and X. undulutum HEX (4.9 ± 0.037 µg/mL), ETA (17.46 ± 0.024 µg/mL) and DCM (19.27 ± 0.492 µg/mL). The extracts exhibited minimal cytotoxicity except for the ETA and DCM of Z. mucronata with CC50 values of 10.96 and 10.01 µg/mL, respectively. Isolation and structural characterization of the active compounds from the DCM extracts revealed that betulinic acid (19.95 ± 1.53 µg/mL) and lupeol (7.56 ± 2.03 µg/mL) were responsible for the anti-malarial activity and had no considerable cytotoxicity (CC50 > µg/mL). Molecular docking suggested strong binding between PfHsp70-1, betulinic acid (- 6.8 kcal/mol), and lupeol (- 6.9 kcal/mol). Meanwhile, the in vitro validation assays revealed the disruption of the protein structural elements and chaperone function. CONCLUSION: This study proves that X undulutum and Z. mucronata have anti-malarial potential and that betulinic acid and lupeol are responsible for the activity seen on Z. mucronata. They also make a case for guided purification of new phytochemicals in the other extracts and support the notion of considering medicinal plants to discover new anti-malarials.


Asunto(s)
Antimaláricos , Fitoquímicos , Extractos Vegetales , Plasmodium falciparum , Ziziphus , Antimaláricos/farmacología , Antimaláricos/química , Ziziphus/química , Plasmodium falciparum/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Descubrimiento de Drogas
12.
Nat Prod Res ; 38(11): 1956-1960, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38739565

RESUMEN

Magonia pubescens is a natural species from the Brazilian cerrado biome. Its fruits and seeds are used in the treatment of seborrheic dermatitis, a common inflammatory skin disease. In this work, the known compounds lapachol, stigmasterol, maniladiol and scopoletin were isolated from hexane and dichloromethane extracts of M. pubescens branches. The aqueous extract of this material was fractioned through a liquid-liquid partition and the obtained fractions were analyzed by UHPLC-MS/MS. The results obtained were compared with data from three databases, leading to the putative identification of 51 compounds from different classes, including flavonoids, saponins and triterpenes. The cytotoxicity of aqueous fractions was assayed against breast cancer (MDA-MB-231) and leukemia (THP-1 and K562) cells. The best activity was observed for fraction AE3 against MDA-MB-231 cells (IC50 30.72 µg.mL-1).


Asunto(s)
Antineoplásicos Fitogénicos , Neoplasias de la Mama , Fitoquímicos , Extractos Vegetales , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Neoplasias de la Mama/tratamiento farmacológico , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Femenino , Fitoquímicos/farmacología , Fitoquímicos/química , Triterpenos/farmacología , Triterpenos/química , Brasil , Leucemia/tratamiento farmacológico , Flavonoides/farmacología , Flavonoides/química , Células K562 , Cromatografía Líquida de Alta Presión , Espectrometría de Masas en Tándem , Saponinas/farmacología , Saponinas/química , Células THP-1 , Estructura Molecular
13.
Nutrients ; 16(9)2024 May 06.
Artículo en Inglés | MEDLINE | ID: mdl-38732642

RESUMEN

Vernonia cinerea (L.) Less. is a perennial herbaceous plant found mainly in tropical areas, particularly in Southeast Asia, South America, and India. Various parts of V. cinerea have traditionally been used in folk medicine to treat several diseases, such as malaria, fever, and liver diseases. V. cinerea has so far yielded about 92 secondary metabolites. The majority of these are sesquiterpene lactones, but triterpenes, flavonoids, steroids, phenolics, and other compounds are present as well. V. cinerea crude extracts reportedly exhibit anti-inflammatory, antiprotozoal, antidiabetic, anticancer, antimicrobial, antioxidant, and renoprotective activities. This study aims to provide the latest up-to-date information on the botanical characterization, distribution, traditional uses, phytochemistry, and pharmacological activity of V. cinerea. Information on V. cinerea was thoroughly reviewed. The literature published between 1950 and 2024 was compiled through online bibliographic databases, including SciFinder, Web of Science, Google Scholar, PubMed, ScienceDirect, Springer Link, Wiley, and the MDPI online library. The keywords used for the literature search included Vernonia cinerea (L.) Less. and the synonyms Cyanthillium cinereum (L.) H.Rob., Conyza cinerea L., and various others.


Asunto(s)
Medicina Tradicional , Fitoquímicos , Extractos Vegetales , Vernonia , Vernonia/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Humanos , Fitoquímicos/farmacología , Fitoterapia , Animales , América del Sur , Asia Sudoriental
14.
Pak J Pharm Sci ; 37(1): 163-171, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-38741413

RESUMEN

Medicinal plants contain a wide variety of bioactive phytoconstituents which can serve as new therapeutic agents for several diseases. This study examines the antidiabetic potential of Aitchisonia rosea in alloxan-induced diabetic rats and identifies its bioactive phytoconstituents using GC-MS. In vitro, antidiabetic potential was established using the α-amylase inhibition assay. In vivo, antidiabetic potential was investigated by employing the oral glucose tolerance test (OGTT). GC-MS analysis was used to identify the bioactive phytoconstituents. The in vitro and in vivo tests showed that the aqueous extract of A. rosea possesses better antidiabetic potential. The α-amylase inhibition assay highlighted an IC50 value of 134.87µg/ml. In an oral glucose tolerance test, rats given an aqueous A. rosea extract significantly lowered their blood sugar levels significant reduction in the blood glucose concentration was observed in the oral glucose tolerance test in rats treated with the aqueous A. rosea extract. GC-MS investigation revealed many phytoconstituents, with serverogenin acetate and cycloheptasiloxane tetradecamethyl being important antidiabetic agents. This study found anti-diabetic properties in A. rosea extract. The phytochemical and GC-MS investigation also found serverogenin acetate and cycloheptasiloxane tetradecamethyl, which could be used to develop new antidiabetic drugs.


Asunto(s)
Glucemia , Diabetes Mellitus Experimental , Cromatografía de Gases y Espectrometría de Masas , Hipoglucemiantes , Componentes Aéreos de las Plantas , Extractos Vegetales , Animales , Hipoglucemiantes/farmacología , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/inducido químicamente , Componentes Aéreos de las Plantas/química , Masculino , Glucemia/efectos de los fármacos , Ratas , Prueba de Tolerancia a la Glucosa , alfa-Amilasas/antagonistas & inhibidores , alfa-Amilasas/metabolismo , Ratas Wistar , Fitoquímicos/farmacología , Fitoquímicos/análisis , Aloxano
15.
Molecules ; 29(9)2024 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-38731401

RESUMEN

The burden of human schistosomiasis, a known but neglected tropical disease in Sub-Saharan Africa, has been worrisome in recent years. It is becoming increasingly difficult to tackle schistosomiasis with praziquantel, a drug known to be effective against all Schistosoma species, due to reports of reduced efficacy and resistance. Therefore, this study seeks to investigate the antischistosomal potential of phytochemicals from Azadirachta indica against proteins that have been implicated as druggable targets for the treatment of schistosomiasis using computational techniques. In this study, sixty-three (63) previously isolated and characterized phytochemicals from A. indica were identified from the literature and retrieved from the PubChem database. In silico screening was conducted to assess the inhibitory potential of these phytochemicals against three receptors (Schistosoma mansoni Thioredoxin glutathione reductase, dihydroorotate dehydrogenase, and Arginase) that may serve as therapeutic targets for schistosomiasis treatment. Molecular docking, ADMET prediction, ligand interaction, MMGBSA, and molecular dynamics simulation of the hit compounds were conducted using the Schrodinger molecular drug discovery suite. The results show that Andrographolide possesses a satisfactory pharmacokinetic profile, does not violate the Lipinski rule of five, binds with favourable affinity with the receptors, and interacts with key amino acids at the active site. Importantly, its interaction with dihydroorotate dehydrogenase, an enzyme responsible for the catalysis of the de novo pyrimidine nucleotide biosynthetic pathway rate-limiting step, shows a glide score and MMGBSA of -10.19 and -45.75 Kcal/mol, respectively. In addition, the MD simulation shows its stability at the active site of the receptor. Overall, this study revealed that Andrographolide from Azadirachta indica could serve as a potential lead compound for the development of an anti-schistosomal drug.


Asunto(s)
Azadirachta , Dihidroorotato Deshidrogenasa , Simulación del Acoplamiento Molecular , Oxidorreductasas actuantes sobre Donantes de Grupo CH-CH , Esquistosomiasis , Azadirachta/química , Animales , Esquistosomiasis/tratamiento farmacológico , Oxidorreductasas actuantes sobre Donantes de Grupo CH-CH/antagonistas & inhibidores , Oxidorreductasas actuantes sobre Donantes de Grupo CH-CH/metabolismo , Humanos , Fitoquímicos/farmacología , Fitoquímicos/química , Simulación de Dinámica Molecular , Schistosoma mansoni/efectos de los fármacos , Schistosoma mansoni/enzimología , NADH NADPH Oxidorreductasas/antagonistas & inhibidores , NADH NADPH Oxidorreductasas/metabolismo , Extractos Vegetales/química , Extractos Vegetales/farmacología , Simulación por Computador , Esquistosomicidas/farmacología , Esquistosomicidas/química , Esquistosomicidas/uso terapéutico , Complejos Multienzimáticos/antagonistas & inhibidores , Complejos Multienzimáticos/metabolismo , Praziquantel/farmacología , Praziquantel/química , Praziquantel/uso terapéutico
16.
Molecules ; 29(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731500

RESUMEN

A robust, well-functioning immune system is the cornerstone of good health. Various factors may influence the immune system's effectiveness, potentially leading to immune system failure. This review aims to provide an overview of the structure and action of immunomodulators isolated from African medicinal plants. The research was conducted according to PRISMA guidelines. Full-text access research articles published in English up to December 2023, including plant characteristics, isolated phytochemicals, and immuno-modulatory activities, were screened. The chemical structures of the isolated compounds were generated using ChemDraw® (version 12.0.1076), and convergent and distinctive signaling pathways were highlighted. These phytochemicals with demonstrated immunostimulatory activity include alkaloids (berberine, piperine, magnoflorine), polysaccharides (pectin, glucan, acemannan, CALB-4, GMP90-1), glycosides (syringin, cordifolioside, tinocordiside, aucubin), phenolic compounds (ferulic acid, vanillic acid, eupalitin), flavonoids (curcumin, centaurein, kaempferin, luteolin, guajaverin, etc.), terpenoids (oleanolic acid, ursolic acid, betulinic acid, boswellic acids, corosolic acid, nimbidin, andrographolides). These discussed compounds exert their effects through various mechanisms, targeting the modulation of MAPKs, PI3K-Akt, and NF-kB. These mechanisms can support the traditional use of medicinal plants to treat immune-related diseases. The outcomes of this overview are to provoke structural action optimization, to orient research on particular natural chemicals for managing inflammatory, infectious diseases and cancers, or to boost vaccine immunogenicity.


Asunto(s)
Fitoquímicos , Plantas Medicinales , Plantas Medicinales/química , Fitoquímicos/farmacología , Fitoquímicos/química , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Agentes Inmunomoduladores/farmacología , Agentes Inmunomoduladores/química , Agentes Inmunomoduladores/aislamiento & purificación , Factores Inmunológicos/farmacología , Factores Inmunológicos/química , Factores Inmunológicos/aislamiento & purificación , África , Animales
17.
Molecules ; 29(9)2024 Apr 27.
Artículo en Inglés | MEDLINE | ID: mdl-38731504

RESUMEN

Polyphenols are ubiquitous plant metabolites that demonstrate biological activities essential to plant-environment interactions. They are of interest to plant food consumers, as well as to the food, pharmaceutical and cosmetic industry. The class of the plant metabolites comprises both widespread (chlorogenic acids, luteolin, quercetin) and unique compounds of diverse chemical structures but of the common biosynthetic origin. Polyphenols next to sesquiterpenoids are regarded as the major class of the Inuleae-Inulinae metabolites responsible for the pharmacological activity of medicinal plants from the subtribe (Blumea spp., Dittrichia spp., Inula spp., Pulicaria spp. and others). Recent decades have brought a rapid development of molecular and analytical techniques which resulted in better understanding of the taxonomic relationships within the Inuleae tribe and in a plethora of data concerning the chemical constituents of the Inuleae-Inulinae. The current taxonomical classification has introduced changes in the well-established botanical names and rearranged the genera based on molecular plant genetic studies. The newly created chemical data together with the earlier phytochemical studies may provide some complementary information on biochemical relationships within the subtribe. Moreover, they may at least partly explain pharmacological activities of the plant preparations traditionally used in therapy. The current review aimed to systematize the knowledge on the polyphenols of the Inulae-Inulinae.


Asunto(s)
Polifenoles , Polifenoles/química , Polifenoles/farmacología , Humanos , Plantas Medicinales/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Fitoquímicos/química , Fitoquímicos/farmacología , Asteraceae/química
18.
Molecules ; 29(9)2024 May 03.
Artículo en Inglés | MEDLINE | ID: mdl-38731619

RESUMEN

This study aims to investigate the vegetative buds from Picea abies (spruce), naturally found in a central region of Romania, through a comprehensive analysis of the chemical composition to identify bioactive compounds responsible for pharmacological properties. Using HPLC/derivatization technique of GC-MS and quantitative spectrophotometric assays, the phenolic profile, and main components of an ethanolic extract from the buds were investigated. The essential oil was characterized by GC-MS. Moreover, the antioxidant activity with the DPPH method, and the antimicrobial activity were tested. Heavy metal detection was performed by graphite furnace atomic absorption spectrometry. The main components of the alcoholic extract were astragalin, quercetin, kaempferol, shikimic acid, and quinic acid. A total content of 25.32 ± 2.65 mg gallic acid equivalent per gram of dry plant (mg GAE/g DW) and of 10.54 ± 0.083 mg rutin equivalents/g of dry plant (mg RE/g DW) were found. The essential oil had D-limonene, α-cadinol, δ-cadinene, 13-epimanool, and δ-3-carene as predominant components. The spruce vegetative buds exhibited significant antioxidant activity (IC50 of 53 µg/mL) and antimicrobial effects against Staphylococcus aureus. Furthermore, concentrations of heavy metals Pb and Cd were below detection limits, suggesting that the material was free from potentially harmful contaminants. The results confirmed the potential of this indigenous species to be used as a source of compounds with pharmacological utilities.


Asunto(s)
Antiinfecciosos , Antioxidantes , Aceites Volátiles , Fitoquímicos , Picea , Extractos Vegetales , Picea/química , Antioxidantes/farmacología , Antioxidantes/química , Fitoquímicos/farmacología , Fitoquímicos/química , Antiinfecciosos/farmacología , Antiinfecciosos/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Aceites Volátiles/farmacología , Aceites Volátiles/química , Pruebas de Sensibilidad Microbiana , Cromatografía de Gases y Espectrometría de Masas , Rumanía , Fenoles/análisis , Fenoles/farmacología , Fenoles/química
20.
Molecules ; 29(8)2024 Apr 10.
Artículo en Inglés | MEDLINE | ID: mdl-38675535

RESUMEN

Moslae Herba (MH) can be used for both medicine and food and has a long history of medicine. MH has the effects of sweating and relieving the exterior, removing dampness and harmonizing, and is mainly used for colds caused by damp heat in summer. It is called "Xiayue Zhi Mahuang" in China. So far, 123 chemical compounds have been isolated and identified from MH, including flavonoids, terpenoids, phenolic acids, phenylpropanoids, and other chemical compounds. Its chemical components have a wide range of pharmacological activities, including antibacterial, antiviral, anti-inflammatory, antioxidant, analgesic sedation, antipyretic, immune regulation, insecticidal, and other effects. In addition, because of its aromatic odor and health care function, MH also has development and utilization value in food, chemical, and other fields. This paper reviewed the research progress of MH in botany, traditional uses, phytochemistry, and pharmacology and provided a possible direction for further research.


Asunto(s)
Medicina Tradicional China , Fitoquímicos , Animales , Humanos , Antioxidantes/química , Antioxidantes/farmacología , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico
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