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1.
Fitoterapia ; 157: 105133, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35114336

RESUMO

Six diterpenoids including three ent-kauranes (1-2, 4) and three cleistanthanes (3, 5-6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (16S)-ent-16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent-kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4-6 displayed cytotoxic potential with IC50 values ranging from 1.96 to 29.15 µM. They also showed moderate anti-inflammatory activities (IC50 = 6.30-12.05 µM). Particularly, the new ent-kaurane 2 displayed cytotoxic potential against HL-60 (IC50 = 2.00 µM) and MCF-7 (IC50 = 3.55 µM) cells, and anti-inflammatory activity (IC50 = 6.47 µM).


Assuntos
Diterpenos do Tipo Caurano/toxicidade , Diterpenos/toxicidade , Phyllanthus/química , Extratos Vegetais/toxicidade , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/toxicidade , Linhagem Celular Tumoral , Diterpenos/química , Diterpenos do Tipo Caurano/química , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Extratos Vegetais/síntese química , Raízes de Plantas/química , Caules de Planta/química
2.
Cell Death Dis ; 13(1): 45, 2022 01 10.
Artigo em Inglês | MEDLINE | ID: mdl-35013112

RESUMO

PHY34 is a synthetic small molecule, inspired by a compound naturally occurring in tropical plants of the Phyllanthus genus. PHY34 was developed to have potent in vitro and in vivo anticancer activity against high grade serous ovarian cancer (HGSOC) cells. Mechanistically, PHY34 induced apoptosis in ovarian cancer cells by late-stage autophagy inhibition. Furthermore, PHY34 significantly reduced tumor burden in a xenograft model of ovarian cancer. In order to identify its molecular target/s, we undertook an unbiased approach utilizing mass spectrometry-based chemoproteomics. Protein targets from the nucleocytoplasmic transport pathway were identified from the pulldown assay with the cellular apoptosis susceptibility (CAS) protein, also known as CSE1L, representing a likely candidate protein. A tumor microarray confirmed data from mRNA expression data in public databases that CAS expression was elevated in HGSOC and correlated with worse clinical outcomes. Overexpression of CAS reduced PHY34 induced apoptosis in ovarian cancer cells based on PARP cleavage and Annexin V staining. Compounds with a diphyllin structure similar to PHY34 have been shown to inhibit the ATP6V0A2 subunit of V(vacuolar)-ATPase. Therefore, ATP6V0A2 wild-type and ATP6V0A2 V823 mutant cell lines were tested with PHY34, and it was able to induce cell death in the wild-type at 246 pM while the mutant cells were resistant up to 55.46 nM. Overall, our data demonstrate that PHY34 is a promising small molecule for cancer therapy that targets the ATP6V0A2 subunit to induce autophagy inhibition while interacting with CAS and altering nuclear localization of proteins.


Assuntos
Antineoplásicos/farmacologia , Autofagia/efeitos dos fármacos , Núcleo Celular/metabolismo , Proteína de Suscetibilidade a Apoptose Celular/metabolismo , Cistadenocarcinoma Seroso/metabolismo , Neoplasias Ovarianas/metabolismo , ATPases Translocadoras de Prótons/antagonistas & inibidores , Transporte Ativo do Núcleo Celular/efeitos dos fármacos , Antineoplásicos/metabolismo , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proteína de Suscetibilidade a Apoptose Celular/genética , Cistadenocarcinoma Seroso/tratamento farmacológico , Cistadenocarcinoma Seroso/patologia , Feminino , Humanos , Neoplasias Ovarianas/tratamento farmacológico , Neoplasias Ovarianas/patologia , Phyllanthus/química , Prognóstico
3.
Phytochemistry ; 194: 113028, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34847377

RESUMO

The first investigation of Phyllanthus mirabilis Müll.Arg. led to the isolation of six undescribed compounds including two tyramine derivatives: phyllatyramines A and B; three butenolide analogues, phyllantenolide, phyllantenocoside-O-gallate and epi-phyllantenocoside-O-gallate; and a flavanonol gallate, (-)-taxifolin-3-O-gallate; as well as two first isolated natural products, phyllatyramine C and phyllantenocoside; together with twenty-three known compounds. Their structures were elucidated by spectroscopic means. ECD spectra of all isolated butenolides were compared and assigned the configurations. Phyllatyramine A displayed weak cytotoxicity against the KB cell line, while phyllatyramines B and C showed weak cytotoxicity against KB and HeLa cell lines. In addition, phyllatyramine B and (-)-taxifolin-3-O-gallate showed more potent α-glucosidase inhibitory activity than the standard acarbose 3.4 and 5.8 fold, respectively.


Assuntos
Mirabilis , Phyllanthus , Carbonato de Cálcio , Células HeLa , Humanos , Folhas de Planta , alfa-Glucosidases
4.
Drug Chem Toxicol ; 45(1): 407-416, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31899970

RESUMO

Aluminum (Al)-induced toxicity in fruit fly (Drosophila melanogaster) is one of the established models for studying neurotoxicity and neurodegenerative diseases. Alkaloid phytochemicals have been reported to exhibit neuroprotective effects. Therefore, the aim of this study is to determine the effect of alkaloid extracts of Andrographis paniculata and Phyllanthus amarus leaves on Al-induced toxicity in wild type Drosophila melanogaster. The flies were exposed to diets containing 40 mM AlCl3, and the alkaloid extracts (0.1 and 1 mg/ml). Thereafter, the flies were assessed for learning and memory, as well as locomotor performance 14 days post-treatment. This was followed by homogenizing the flies and the homogenates were assayed for acetylcholinesterase, monoamine oxidase and catalase activities, as well as the malondialdehyde content. The results showed that the alkaloid extracts of both leaves could ameliorate the aluminum-induced behavioral and biochemical impairments in the flies. The HPLC analysis of the alkaloid contents revealed that there is an abundance of Amaryllidaceae alkaloids, caffeine and carpaine. Thus, alkaloid extracts from these leaves could serve as promising therapeutic candidates for the management of neurodegenerative disease.


Assuntos
Andrographis , Doenças Neurodegenerativas , Phyllanthus , Acetilcolinesterase , Animais , Drosophila melanogaster , Extratos Vegetais/toxicidade
5.
Nat Prod Res ; 36(2): 539-545, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32643407

RESUMO

A new diterpenoid, phyllane C (1), along with three known compounds, ovoideal E (2), spruceanol (3), and fluacinoid B (4) were isolated from the leaves of Phyllanthus acidus growing in Thailand. The structures were determined by analysis of their MS and NMR data as well as by comparison with literature values. DFT-NMR chemical shift calculations and subsequent DP4/DP4+ probability methods were applied to define the relative configuration of 1. Compound 3 showed a weak cytotoxicity against K562 cell line (IC50 41.9 ± 2.31 µg/mL).


Assuntos
Diterpenos , Phyllanthus , Linhagem Celular , Diterpenos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta
6.
Asian Pac J Cancer Prev ; 22(11): 3561-3568, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34837913

RESUMO

BACKGROUND: Chemotherapy as part of colorectal cancer management can cause death to immunologically active tumor cell, but also it has immune suppressive effect. Phyllanthus niruri Linn is known to has immunomodulatory effect. This study was intended to prove P. niruri Linn effect on infiltrating dendritic cells and Neutrophil/lymphocyte ratios (NLRs) in Sprague-Dawley rats with colorectal cancer which were given capecitabine chemotherapy. METHODS: The study was randomized post-test only control group design. The samples were 39 Sprague-Dawley male rats, with body weight around 170-220 grams, induced by 1,2-dimetylhydrazine (DMH) 30 mg/kgBW once per week subcutaneously. On 9th,11th and 13th week, there were four induced rats sacrificed each week to detect colorectal cancer (CRC) development. On the 13th week, all of the 4 sacrificed rats developed colon cancer, so the induction had to be stopped. The rest of 27 induced rats were randomly divided into three groups: control-group (K) were left untreated (9 rats), group P1 (9 rats) were given Capecitabine and group P2 (9 rats) were given Capecitabine with combination of P. niruri Linn extract 13.5 mg/kgBW orally. After 17th week, all rats were terminated and tumor lesion of colon were processed to be paraffin blocks and were stained with HE for evaluating the NLRs, and immunohistochemistry (S100) for evaluating infiltrating dendritic cells. Data was analyzed by using Oneway-Anova-test and post-Hoc LSD-test. Considered significant if p was <0.05. RESULTS: The mean±standard deviation of infiltrating dendritic cells showed increasing value in group P2 (62.11±31.35) compared to group P1 (52.78±29.24) though not statistically significant. The mean of NLRs also showed statistically significant elevation of value in group P2 (0.13±0.05) compared to group P1 (0.04±0.01). CONCLUSION: Extract of Phyllanthus niruri Linn increasing immunologic status through elevation of infiltrating dendritic cells and NLRs in animal model colorectal cancer with Capecitabine chemotherapy.


Assuntos
Neoplasias Colorretais/tratamento farmacológico , Células Dendríticas/efeitos dos fármacos , Linfócitos/efeitos dos fármacos , Neutrófilos/efeitos dos fármacos , Phyllanthus , Animais , Antimetabólitos Antineoplásicos/uso terapêutico , Capecitabina/uso terapêutico , Neoplasias Colorretais/sangue , Modelos Animais de Doenças , Contagem de Leucócitos , Masculino , Ratos , Ratos Sprague-Dawley
7.
IET Nanobiotechnol ; 15(2): 164-172, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34694700

RESUMO

Herein, the green synthesis of TiO2 nanoparticles using Phyllanthus niruri leaf extract was accomplished by the sol-gel method. The structure and particle size of the synthesised TiO2 nanoparticles were characterised by X-ray diffraction (XRD) analysis and the size was found to be 20 nm. The Fourier-transform infrared spectra determined the existence of carboxyl and hydroxyl functional groups. The images from SEM analysis recommended a porous and heterogeneous surface. The methyl orange (MO) dye removal was examined using different parameters such as pH, time, dose, temperature and dye concentration. Maximum dye elimination percentage was achieved at pH 6.0 and 0.02 g as the optimum adsorbent dose. The kinetic analysis suggested that the pseudo-second-order kinetic model finely defines adsorption dynamics. Langmuir adsorption isotherm studies revealed endothermic monolayer adsorption of the methyl Orange dye. The negative value of ∆G° and positive value of ∆H° showed the spontaneous and endothermic adsorption method.


Assuntos
Nanopartículas , Phyllanthus , Poluentes Químicos da Água , Adsorção , Concentração de Íons de Hidrogênio , Cinética , Extratos Vegetais , Espectroscopia de Infravermelho com Transformada de Fourier , Titânio
8.
Sci Rep ; 11(1): 20888, 2021 10 22.
Artigo em Inglês | MEDLINE | ID: mdl-34686666

RESUMO

Rapid and accurate species diagnosis accelerates performance in numerous biological fields and associated areas. However, morphology-based species taxonomy/identification might hinder study and lead to ambiguous results. DNA barcodes (Bar) has been employed extensively for plant species identification. Recently, CRISPR-cas system can be applied for diagnostic tool to detect pathogen's DNA based on the collateral activity of cas12a or cas13. Here, we developed barcode-coupled with cas12a assay, "Bar-cas12a" for species authentication using Phyllanthus amarus as a model. The gRNAs were designed from trnL region, namely gRNA-A and gRNA-B. As a result, gRNA-A was highly specific to P. amarus amplified by RPA in contrast to gRNA-B even in contaminated condition. Apart from the large variation of gRNA-A binding in DNA target, cas12a- specific PAM's gRNA-A as TTTN can be found only in P. amarus. PAM site may be recognized one of the potential regions for increasing specificity to authenticate species. In addition, the sensitivity of Bar-cas12a using both gRNAs gave the same detection limit at 0.8 fg and it was 1,000 times more sensitive compared to agarose gel electrophoresis. This approach displayed the accuracy degree of 90% for species authentication. Overall, Bar-cas12a using trnL-designed gRNA offer a highly specific, sensitive, speed, and simple approach for plant species authentication. Therefore, the current method serves as a promising tool for species determination which is likely to be implemented for onsite testing.


Assuntos
Sistemas CRISPR-Cas/genética , Código de Barras de DNA Taxonômico/métodos , Phyllanthus/genética , DNA/genética , RNA Guia/genética
9.
Int J Mol Sci ; 22(18)2021 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-34576229

RESUMO

The prevalence of non-alcoholic fatty liver disease (NAFLD) is one of the leading causes of chronic liver diseases worldwide. This study examined the potential protective effects of a naturally occurring polyphenolic compound, methyl brevifolincarboxylate (MBC) on fatty liver injury in vitro. The results showed that MBC at its non-cytotoxic concentrations, reduced lipid droplet accumulation and triglyceride (TG) levels in the oleic acid (OA)-treated human hepatocarcinoma cell line, SK-HEP-1 and murine primary hepatocytes. In OA-treated SK-HEP-1 cells and primary murine hepatocytes, MBC attenuated the mRNA expression levels of the de novo lipogenesis molecules, acetyl-coenzyme A carboxylase (Acc1), fatty acid synthase (Fasn) and sterol regulatory element binding protein 1c (Srebp1c). MBC promoted the lipid oxidation factor peroxisome proliferator activated receptor-α (Pparα), and its target genes, carnitine palmitoyl transferase 1 (Cpt1) and acyl-coenzyme A oxidase 1 (Acox1) in both the SK-HEP-1 cells and primary murine hepatocytes. The mRNA results were further supported by the attenuated protein expression of lipogenesis and lipid oxidation molecules in OA-treated SK-HEP-1 cells. The MBC increased the expression of AMP activated protein kinase (AMPK) phosphorylation. On the other hand, MBC treatment dampened the inflammatory mediator's, tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-8, and IL-1ß secretion, and nuclear factor (NF)-κB expression (mRNA and protein) through reduced reactive oxygen species production in OA-treated SK-HEP-1 cells. Taken together, our results demonstrated that MBC possessed potential protective effects against NAFLD in vitro by amelioration of lipid metabolism and inflammatory markers through the AMPK/NF-κB signaling pathway.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Benzopiranos/farmacologia , Ácidos Graxos não Esterificados/metabolismo , Hepatócitos/efeitos dos fármacos , Inflamação/tratamento farmacológico , Metabolismo dos Lipídeos , NF-kappa B/metabolismo , Animais , Linhagem Celular Tumoral , Hepatócitos/metabolismo , Humanos , Lipídeos/química , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Ácido Oleico/química , Phyllanthus/efeitos dos fármacos , Espécies Reativas de Oxigênio , Transdução de Sinais , Triglicerídeos/metabolismo
10.
ScientificWorldJournal ; 2021: 6650704, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34194288

RESUMO

BACKGROUND: Ethnobotanical knowledge on four herbaceous species, Acmella uliginosa (Sw.) Cass., Momordica charantia L., Phyllanthus amarus Schumach. & Thonn., and Scoparia dulcis L., in Benin was investigated. METHODS: Herbal medicine traders in six different markets were interviewed using a semi-structured questionnaire. The linear regression test was performed to check for the influence of respondent's age on ethnobotanical uses they hold. Relative frequency citation, fidelity level, use value, and Rahman similarity index were calculated to assess the diversity of medico-magic knowledge. The Informant Consensus Factor is not applicable in this study since we are dealing neither with the diversity of medicinal plants used by a community of people nor with a great number of plant species used for medicinal purposes, nor the diversity of plant species used in the treatment of a specific or group of ailments. RESULTS: The respondent's age did not influence the ethnobotanical uses they hold on the species. All thirty-six informants surveyed traded Phyllanthus amarus Schumach. & Thonn., Momordica charantia L., and Scoparia dulcis L., and the majority traded Acmella uliginosa (Sw.) Cass. The respondent's age does not influence the diversity of ethnobotanical uses they hold on the study species. Purchase in traders' own markets was the predominant source of Phyllanthus amarus Schumach. & Thonn., Momordica charantia L., and Scoparia dulcis L. while Acmella uliginosa (Sw.) Cass. was mostly purchased in other more distant markets. A noticeable proportion of traders also collect Phyllanthus amarus Schumach. & Thonn. and Momordica charantia L. from wild populations. Phyllanthus amarus Schumach. & Thonn. was the species most demanded by customers followed by Momordica charantia L. Traders confirmed the scarcity of all species in recent years and climate change and destruction of natural habitats for logging were the most cited causes. The entire plant of Phyllanthus amarus Schumach. & Thonn. was used mainly to treat malaria, diabetes, and constipation, and decoction with oral administration was the most frequent preparation for malaria treatment. To treat diabetes, informants mixed Phyllanthus amarus Schumach. & Thonn. with Momordica charantia L. used as a decoction with oral administration. Momordica charantia L. was also used to treat measles and chicken pox. Acmella uliginosa (Sw.) Cass. and Scoparia dulcis L. were mostly used for their spiritual use for luck, predominantly by chewing fresh leaves or flowers, and by bathing with the ground plant mixed with soap, respectively. Overall, Momordica charantia L. had the greatest use value followed by Phyllanthus amarus Schumach. & Thonn. The majority of traders do not plant the species. CONCLUSIONS: The harvesting and trade of the species threaten their natural populations and urgent tools, including in situ and ex situ conservation, are needed to ensure their long-term sustainable exploitation.


Assuntos
Conhecimentos, Atitudes e Prática em Saúde/etnologia , Medicina Tradicional Africana , Plantas Medicinais , Asteraceae , Benin , Etnobotânica , Humanos , Medicina Tradicional Africana/métodos , Medicina Tradicional Africana/psicologia , Momordica charantia , Phyllanthus , Scoparia
11.
Molecules ; 26(14)2021 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-34299650

RESUMO

A combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from Phyllanthus muellarianus. Phytocomponents responsible for the anti-cholinesterase activity of subfractions PMF1 and PMF4 were identified and re-assayed to confirm their activity. Magnoflorine was identified as an active phytocomponent from PMF1 while nitidine was isolated from PMF4. Magnoflorine was shown to be a selective inhibitor of human butyrylcholinesterase-hBChE (IC50 = 131 ± 9 µM and IC50 = 1120 ± 83 µM, for hBuChE and human acetylcholinesterase-hAChE, respectively), while nitidine showed comparable inhibitory potencies against both enzymes (IC50 = 6.68 ± 0.13 µM and IC50 = 5.31 ± 0.50 µM, for hBChE and hAChE, respectively). When compared with the commercial anti-Alzheimer drug galanthamine, nitidine was as potent as galanthamine against hAChE and one order of magnitude more potent against hBuChE. Furthermore, nitidine also showed significant, although weak, antiaggregating activity towards amyloid-ß self-aggregation.


Assuntos
Acetilcolinesterase , Butirilcolinesterase/química , Inibidores da Colinesterase , Simulação de Acoplamento Molecular , Phyllanthus/química , Casca de Planta/química , Extratos Vegetais/química , Acetilcolinesterase/química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Proteínas Ligadas por GPI/antagonistas & inibidores , Proteínas Ligadas por GPI/química , Humanos , Estrutura Molecular
12.
Comput Biol Med ; 136: 104683, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34329860

RESUMO

Coronavirus Disease-2019 (COVID-19), a viral disease caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) was declared a global pandemic by WHO in 2020. In this scenario, SARS-CoV-2 main protease (COVID-19 Mpro), an enzyme mainly involved in viral replication and transcription is identified as a crucial target for drug discovery. Traditionally used medicinal plants contain a large amount of bioactives and pave a new path to develop drugs and medications for COVID-19. The present study was aimed to examine the potential of Emblica officinalis (amla), Phyllanthus niruri Linn. (bhumi amla) and Tinospora cordifolia (giloy) bioactive compounds to inhibit the enzymatic activity of COVID-19 Mpro. In total, 96 bioactive compounds were selected and docked with COVID-19 Mpro and further validated by molecular dynamics study. From the docking and molecular dynamics study, it was revealed that the bioactives namely amritoside, apigenin-6-C-glucosyl7-O-glucoside, pectolinarin and astragalin showed better binding affinities with COVID-19 Mpro. Drug-likeness, ADEMT and bioactivity score prediction of best drug candidates were evaluated by DruLiTo, pkCSM and Molinspiration servers, respectively. Overall, the in silico results confirmed that the validated bioactives could be exploited as promising COVID-19 Mpro inhibitors.


Assuntos
Phyllanthus emblica , Phyllanthus , Inibidores de Proteases/farmacologia , SARS-CoV-2/efeitos dos fármacos , Tinospora , COVID-19 , Proteases 3C de Coronavírus/antagonistas & inibidores , Humanos , Medicina Ayurvédica , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Peptídeo Hidrolases , Phyllanthus/química , Phyllanthus emblica/química , Compostos Fitoquímicos/farmacologia , Plantas Medicinais/química , Tinospora/química
13.
Int J Biol Macromol ; 187: 451-461, 2021 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-34324903

RESUMO

The current work aims to prepare biologically active and pH responsive smart films based on Chitosan (CS)/Methylcellulose (MC) matrix integrated with Phyllanthus reticulatus (PR) ripen fruit anthocyanin. The prepared smart films (CMPR) were fabricated through a cost-effective solvent casting technique. The existences of secondary interactions were confirmed by the FT-IR analysis. The smooth SEM images revealed the miscibility and compatibility of the CS/MC matrix with PR anthocyanin. The incorporation of PR anthocyanin significantly blocked the UV light transmission of the CS/MC films while slight decrease in the transparency was observed. The water solubility, moisture retention capacity, and water vapor transmission rate were significantly enhanced with an increase in the PR anthocyanin content. Additionally, the prepared CMPR smart films showed pink color in acidic pH while yellowish in basic pH solution and further exhibited strong antioxidant activity as well as antibacterial activity against the common foodborne pathogens such as S. aureus, P. aeruginosa, and E. coli. The CMPR smart film also displayed potential result for monitoring the fish fillet freshness at room temperature. The results proclaim that the prepared CMPR smart films could be utilized for quality assurance as well as shelf life extension of the marine food products.


Assuntos
Antocianinas/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Quitosana/farmacologia , Peixes , Embalagem de Alimentos , Qualidade dos Alimentos , Metilcelulose/farmacologia , Phyllanthus , Alimentos Marinhos , Polímeros Responsivos a Estímulos/farmacologia , Animais , Antocianinas/química , Antocianinas/isolamento & purificação , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Compostos de Bifenilo/química , Quitosana/química , Cor , Peixes/metabolismo , Peixes/microbiologia , Microbiologia de Alimentos , Concentração de Íons de Hidrogênio , Metilcelulose/química , Phyllanthus/química , Picratos/química , Alimentos Marinhos/microbiologia , Polímeros Responsivos a Estímulos/química
14.
Molecules ; 26(13)2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-34203560

RESUMO

A number of plants used in folk medicine in Thailand and Eastern Asia are attracting interest due to the high bioactivities of their extracts. The aim of this study was to screen the edible leaf extracts of 20 plants found in Thailand and investigate the potential neuroprotective effects of the most bioactive sample. The total phenol and flavonoid content and 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity were determined for all 20 leaf extracts. Based on these assays, Glochidion littorale leaf extract (GLE), which showed a high value in all tested parameters, was used in further experiments to evaluate its effects on neurodegeneration in Caenorhabditis elegans. GLE treatment ameliorated H2O2-induced oxidative stress by attenuating the accumulation of reactive oxygen species and protected the worms against 1-methyl-4-phenylpyridinium-induced neurodegeneration. The neuroprotective effects observed may be associated with the activation of the transcription factor DAF-16. The characterization of this extract by LC-MS identified several phenolic compounds, including myricetin, coumestrin, chlorogenic acid, and hesperidin, which may play a key role in neuroprotection. This study reports the novel neuroprotective activity of GLE, which may be used to develop treatments for neurodegenerative diseases such as Parkinson's syndrome.


Assuntos
Proteínas de Caenorhabditis elegans/metabolismo , Caenorhabditis elegans/metabolismo , Fatores de Transcrição Forkhead/metabolismo , Fármacos Neuroprotetores , Estresse Oxidativo/efeitos dos fármacos , Phyllanthus/química , Extratos Vegetais , Animais , Peróxido de Hidrogênio/farmacologia , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
15.
J Basic Clin Physiol Pharmacol ; 32(4): 809-815, 2021 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-34214339

RESUMO

OBJECTIVES: Phyllanthus niruri has been known as an immunomodulator and also reported to possess an antiviral activity against several RNA viruses, such as hepatitis B virus and hepatitis C virus by inhibiting viral entry and replication. Since the current situation of Coronavirus Disease 2019 (COVID-19) which infected among the world and caused severe disease and high morbidity, it urgently needed to find new agents against COVID-19. Therefore, in silico screening against COVID-19 receptors is carried out as an initial stage of drug discovery by evaluating the activity of phyllanthin and hypophyllanthin, an isolated from Phyllanthus niruri, in inhibiting spike glycoprotein (6LZG) and main protease (5R7Y) which play as target receptors of COVID-19. METHODS: Molegro Virtual Docker 6.0 used to determine the best binding energy through the rerank score which shows the total energy bonds calculation. RESULTS: Phyllanthin and hypophyllanthin demonstrated to possess greater binding affinity toward the COVID-19 inhibition sites than their native ligand. The rerank score of phyllanthin and hypophyllanthin are lower than the native ligands 6LZG and 5R7Y. This result indicated that phyllanthin and hypophyllanthin have a stronger interaction than the native ligands both in spike glycoprotein (entry inhibitor) and main protease (translation and replication inhibitor). CONCLUSIONS: In conclusion, phyllanthin and hypophyllanthin are predicted to have strong activity against COVID-19 through inhibiting spike glycoprotein and main protease under in silico study. Further research is needed to support the development of P. niruri as inhibitor agents of COVID-19 through bioassay studies.


Assuntos
Lignanas/farmacologia , Phyllanthus/química , COVID-19/tratamento farmacológico , Simulação por Computador , Humanos , Ligantes , Lignanas/toxicidade , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/farmacologia , SARS-CoV-2/efeitos dos fármacos
16.
Bioorg Chem ; 114: 105125, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34217976

RESUMO

The young leaves of Phyllanthus acidus (Euphorbiaceae) are commonly used as edible vegetables in Indonesia, Thailand, and India, and their water infusions as dieting aids for people trying to remain slim. However, it is regarded as a poisonous plant in Malaya, and current researches are insufficient to provide a conclusion on its toxicity and safety under large doses. In this study, we firstly found that the refined nonpolar extracts of P. acidus leaves showed significant cytotoxic effect against BEAS-2B and L02 normal cell lines with IC50 values of 2.15 and 1.64 mg/mL, respectively. Further bioactivity-guided isolation produced four new rare dichapetalins (pacidusins A-D) from the most active fraction. Their structures including absolute configurations were elucidated by extensive spectroscopic data and X-ray diffraction analysis. All the isolated dichapetalins exhibited moderate cytotoxicity against, BEAS-2B and L02 normal cell lines with IC50 values ranging from 12.44 to 22.55 µM, as well as five human cancer cell lines with IC50 values ranging from 3.38 to 22.38 µM. Furthermore, the content of the main dichapetalins in the leaves were determined by analytical HPLC, which showed that the leaves contained a very high amount of the four isolated dichapetalins with a total yield of 0.488 mg/g of dry plant material. These toxic dichapetalins may lead to adverse health effects in higher doses. Our findings indicate that the dichapetalin containing leaves may not be suitable for consumption in large quantities as food, but demonstrate their potency as anti-cancer agents for new drug discovery.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Phyllanthus/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade
17.
Arch Ital Urol Androl ; 93(2): 184-188, 2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-34286553

RESUMO

OBJECTIVE: The aim of this study is to evaluate the efficacy of a food supplement containing Phyllanthus niruri and Chrysanthellum americanum in association with potassium and magnesium citrates in the treatment and prophylaxis of urinary stones. MATERIALS AND METHODS: Eighty-two patients (mean age 49.7 ± 11.2) with history of urinary stones received this food supplement, one capsule a day for 6 months. Each administration contained a combination of the following ingredients: 244 mg Potassium citrate, 735 mg Magnesium citrate, Phyllanthus (Phyllantus niruri) herb d.e. 15% mg Tannins 220 mg, Chrysanthellum (Chrysanthellum americanum Vatke) plant d.e. » 55 mg. After 6 months, all patients underwent urologic visit, urinalysis, imaging and quality of life (QoL) questionnaires evaluation. Each patient was also evaluated by computed tomography (CT) scan at baseline and at 6 months. RESULT: From January 2018 to March 2019, 82 patients (mean age 49.7 ± 11.2) completed the follow-up period and were analyzed. Fifty patients showed lower stone dimensions (60.9%). The average stone size was 0.9 mm, with a significant reduction in comparison with the baseline (-6.7 mm ± 3 mm) (p < 0.001). Forty-nine patients (59.7%) did not show any symptomatic episode with an improving in QoL (+0.4 ± 0.1) (p < 0.001) in comparison with the baseline. At the end of the follow-up period, 27 patients out of 82 were stone-free (32.9%). Moreover, we report a significant reduction of patients with asymptomatic bacteriuria (ABU) between the baseline and the end of the follow-up evaluation (p < 0.001). CONCLUSIONS: In conclusion, this food supplement is able to improve quality of life in patients with urinary stones, reducing symptomatic episodes and the prevalence of ABU.


Assuntos
Cálculos Renais , Phyllanthus , Cálculos Urinários , Adulto , Citratos , Ácido Cítrico , Humanos , Pessoa de Meia-Idade , Compostos Organometálicos , Potássio , Estudos Prospectivos , Qualidade de Vida , Cálculos Urinários/tratamento farmacológico , Cálculos Urinários/prevenção & controle
18.
Bioprocess Biosyst Eng ; 44(8): 1593-1616, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34075470

RESUMO

Titanium dioxide nanoparticles exhibit good anticancer and antibacterial activities. They are known to be environmentally friendly, stable, less toxic, and have excellent biocompatibility nature. Due to these properties, they are well suited for biological applications particularly in biomedical applications such as drug delivery and cancer therapy. In this research article, three medicinal herbs namely, Plectranthus amboinicus (Karpooravalli), Phyllanthus niruri (Keezhanelli), and Euphorbia hirta (Amman Pacharisi), were used to modify the surface of the TiO2 nanoparticles. The synthesized nanoparticles were subjected to various characterization techniques. The samples are then subjected to MTT assay to determine cell viability. KB oral cancer cells are used for the determination of the anticancer nature of the pure and bio modified nanoparticles. It is observed that Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nanoparticles exhibit excellent anticancer activities among other bio modified and pure samples. The samples are then examined for antibacterial activities against three Gram-negative bacterial strains namely, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and two Gram-positive bacterial strains namely, Staphylococcus aureus and Streptococcus mutans, respectively. Among the modified and pure samples, Plectranthus amboinicus showed good antibacterial activity against Gram-positive and Gram-negative bacteria. In the Flow cytometry analysis, the generation of p53 protein expression from Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nano herbal particles shows the anti-cancerous nature of the sample. Then to determine the toxic nature of the Plectranthus amboinicus-Phyllanthus niruri modified TiO2 nano herbal particles against normal cells, the NPs were subjected to MTT assay against normal L929 cells, and it was found to be safer and less toxic towards the normal cells.


Assuntos
Euphorbia/metabolismo , Phyllanthus/metabolismo , Plectranthus/metabolismo , Titânio/química , Ágar/química , Animais , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular , Sobrevivência Celular , Células HEK293 , Humanos , Concentração de Íons de Hidrogênio , Nanopartículas Metálicas/química , Camundongos , Testes de Sensibilidade Microbiana , Modelos Químicos , Nanotecnologia/métodos , Extratos Vegetais , Folhas de Planta , Preparações de Plantas/farmacologia , Pós , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Sais de Tetrazólio/farmacologia , Tiazóis/farmacologia , Difração de Raios X
19.
BJU Int ; 128(6): 661-666, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34192414

RESUMO

Despite high-level evidence supporting the use of pharmacotherapy therapy for the prevention of kidney stones, adherence to medications is often poor because of side-effects, inconvenience and cost. Furthermore, with a desire for more 'natural' products, patients seek dietary and herbal remedies over pharmacotherapy. However, patients are often unaware of the potential side-effects, lack of evidence and cost of these remedies. Therefore, in the present review we examine the evidence for a few of the commonly espoused non-prescription agents or dietary recommendations that are thought to prevent stone formation, including lemonade, fish oil (omega fatty acids), Phyllanthus niruri and the Dietary Approaches to Stop Hypertension (DASH) diet. While the present review includes only a few of the stone-modulating recommendations available to the lay community, we focussed on these four due to their prevalent use. Our goal is not to only dispel commonly held notions about stone disease, but also to highlight the lack of high-level evidence for many commonly utilised treatments.


Assuntos
Citrus , Abordagens Dietéticas para Conter a Hipertensão , Óleos de Peixe/uso terapêutico , Cálculos Renais/prevenção & controle , Phyllanthus , Fitoterapia , Humanos , Cálculos Renais/tratamento farmacológico , Cálculos Renais/etiologia , Extratos Vegetais/uso terapêutico
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