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1.
BMC Complement Med Ther ; 23(1): 394, 2023 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-37924066

RESUMO

BACKGROUND: Decoctions of the root and stem of the medicinal plant Salacia reticulata is an indigenous remedy for diabetics and its complications in Sri Lanka. In diabetics, the formation of advanced glycation end products (AGEs) leads to many pathologies. Nevertheless, the anti-protein-glycation property of this plant is poorly documented. This study reports the anti-protein-glycation and radical scavenging potential of various plant parts of S. reticulata. METHODS: Hot water extracts (2g dried powder/50 ml) of root, stem, leaf, twigs, and fruits at various concentrations (15.6 to 500.0 µg/ml) were subjected to anti-glycation and glycation reversing assays in vitro. 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay was used for free radical scavenging property. RESULTS: Various plant parts of S. reticulata showed anti-protein-glycation and free-radical scavenging activities. IC50 for the anti-glycation activity of root, stem, leaf, twigs, and fruit extracts were 11.92 ± 1.14, 35.18 ± 2.79, 113.3 ± 1.91, 149.59 ± 1.06, and 1120.37 ± 229.48 µg/ml respectively. IC50 of Rutin was 21.88 ± 2.82 µg/ml. EC50 of the root, stem, twigs, and leaf extracts for glycation reversing was 102.09 ± 6.23, 116.99 ± 5.82, 154.45 ± 5.79, and 278.78 ± 14.19 µg/ml respectively. The EC50 values for the radical scavenging activity of leaf, stem, and roots were 26.4±4.7, 9.0±1.2, and 9.1±1.3 respectively. Root had significantly (p<0.05) high activity for all the parameters tested. CONCLUSION: Salacia reticulata possess anti-glycation, glycation-reversing, and free radical scavenging activities. Other than root and stem, the leaves and twigs too may be a useful source for anti-diabetic bioactive molecules.


Assuntos
Diabetes Mellitus , Plantas Medicinais , Salacia , Plantas Medicinais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Salacia/química , Sri Lanka , Hipoglicemiantes , Reação de Maillard , Radicais Livres
2.
Zhongguo Zhong Yao Za Zhi ; 48(24): 6676-6681, 2023 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-38212027

RESUMO

Nine compounds were isolated from the 90% ethanol extract of Salacia polysperma by silica gel, Sephadex LH-20 column chromatography, together with preparative HPLC methods. Based on HR-ESI-MS, MS, 1D and 2D NMR spectral analyses, the structures of the nine compounds were identified as 28-hydroxy wilforlide B(1), wilforlide A(2), 1ß,3ß-dihydroxyurs-9(11),12-diene(3),(-)-epicatechin(4),(+)-catechin(5),(-)-4'-O-methyl-ent-galloepicatechin(6), 3-hydroxy-1-(4-hydroxy-3-methoxy-phenyl)propan-1-one(7),(-)-(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(8), and vanillic acid(9). Compound 1 is a new oleanane-type triterpene lactone. Compounds 1, 3, 4, 7-9 were isolated from the Salacia genus for the first time. All compounds were assayed for their α-glucosidase inhibitory activity. The results suggested that compound 8 exhibited moderate α-glucosidase inhibitory activity, with an IC_(50) value of 37.2 µmol·L~(-1), and the other compounds showed no α-glucosidase inhibitory activity.


Assuntos
Salacia , Triterpenos , Salacia/química , alfa-Glucosidases , Triterpenos/farmacologia , Espectroscopia de Ressonância Magnética , Etanol , Estrutura Molecular
3.
Nat Prod Res ; 36(9): 2292-2299, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-33043693

RESUMO

Four new triterpene glucosides (1-4) were isolated from the 90% ethanol extract of Salacia cochinchinensis, together with five known compounds (5-9). The structures of the new compounds were elucidated by comprehensive spectroscopic analysis including HRESIMS, IR, 1 D and 2 D NMR analysis. All isolates were assayed for their α-glucosidase inhibitory activity. Compound 9 showed remarkable α-glucosidase inhibitory activity with an IC50 value of 0.31 µM, and the triterpene glycosides (1-5) exhibited moderate α-glucosidase inhibitory activity.


Assuntos
Salacia , Triterpenos , Glucosídeos/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Estrutura Molecular , Salacia/química , Triterpenos/química , Triterpenos/farmacologia , alfa-Glucosidases
4.
Nat Prod Res ; 36(15): 4026-4030, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-33729063

RESUMO

Bioactivity-guided isolation of the CHCl3-soluble fraction of the stems of Salacia chinensis L. (Celastraceae) was carried out to obtain a new 7',9-epoxylignan (1) and three 7,9':7',9-diepoxylignans (2-4). The absolute configuration of 1 was elucidated based on NMR and ECD spectroscopic data interpretation. All isolated lignans showed intermediate α-glucosidase inhibitory activity with the IC50 values ranging from 28.5 to 85.6 µM.


Assuntos
Celastraceae , Lignanas , Salacia , Lignanas/farmacologia , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , Salacia/química
5.
Biomed Pharmacother ; 142: 112034, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34411914

RESUMO

Acute myeloid leukemia (AML) is the most lethal form of leukemia. Standard anti-AML treatment remains almost unchanged for decades. Tingenone (TG) and 22-hydroxytingenone (22-HTG) are quinonemethide triterpenes found in the Amazonian plant Salacia impressifolia (Celastraceae), with cytotoxic properties in different histological types of cancer cells. In the present work, we investigated the anti-AML action mechanism of TG and 22-HTG in the AML HL-60 cell line. Both compounds exhibited potent cytotoxicity in a panel of cancer cell lines. Mechanistic studies found that TG and 22-HTG reduced cell growth and caused the externalization of phosphatidylserine, the fragmentation of internucleosomal DNA and the loss of mitochondrial transmembrane potential in HL-60 cells. In addition, pre-incubation with Z-VAD(OMe)-FMK, a pan-caspase inhibitor, prevented TG- and 22-HTG-induced apoptosis, indicating cell death by apoptosis via a caspase-dependent pathway. The analysis of the RNA transcripts of several genes indicated the interruption of the cellular antioxidant system, including the downregulation of thioredoxin, as a target for TG and 22-HTG. The application of N-acetyl-cysteine, an antioxidant, completely prevented apoptosis induced by TG and 22-HTG, indicating activation of the apoptosis pathway mediated by oxidative stress. Moreover, TG and 22-HTG induced DNA double-strand break and phosphorylation of JNK2 (T183/Y185) and p38α (T180/Y182), and co-incubation with SP 600125 (JNK/SAPK inhibitor) and PD 169316 (p38 MAPK inhibitor) partially prevented apoptosis induced by TG and 22-HTG. Together, these data indicate that TG and 22-HTG are new candidate for anti-AML therapy targeting thioredoxin.


Assuntos
Leucemia Mieloide Aguda/tratamento farmacológico , Tiorredoxinas/genética , Triterpenos/farmacologia , Animais , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/metabolismo , Apoptose/efeitos dos fármacos , Linhagem Celular , Linhagem Celular Tumoral , Quebras de DNA de Cadeia Dupla/efeitos dos fármacos , Regulação para Baixo/efeitos dos fármacos , Células HL-60 , Humanos , Leucemia Mieloide Aguda/genética , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Camundongos , Estresse Oxidativo/efeitos dos fármacos , Salacia/química , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
6.
Bol. latinoam. Caribe plantas med. aromát ; 20(4): 416-426, jul. 2021. tab, ilus
Artigo em Inglês | LILACS | ID: biblio-1369485

RESUMO

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitroas well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerataand S. kraussiipossess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.


Las especies reactivas de oxígeno están implicadas en múltiples condiciones patológicas, incluyendo la disfunción eréctil. Este estudio evaluó el potencial antioxidante in vitro e in vivo de extractos metanólicos de Inula glomeratay Salacia kraussii. Los materiales vegetales fueron pulverizados y extraídos con metanol. A estos extractos crudos se les llevó a cabo el análisis fitoquímico junto con el contenido total de fenólicos y flavonoides, así como se les investigó la capacidad in vitro para atrapar radicales (ABTS, DPPH, NO.). Los potenciales antioxidantes in vivo de los extractos crudos (50/250 mg/kg de peso corporal) se determinaron en un modelo en ratas con disfunción eréctil. El análisis fitoquímico reveló que ambas plantas contuvieron flavonoides, taninos, terpenoides y alcaloides. Los extractos crudos con un grado variable de eficiencia, atraparon a los radicales ABTS y DPPH. Los extractos crudos a bajas concentraciones (50 mg/kg p.c) significativamente (p<0.05) disminuyeron el nivel de malondialdehído, aumentaron las actividades de catalasa y elevaron los niveles de glutatión. Sin embargo, las actividades de SOD por los extractos crudos fueron significativamente dosis-dependientes. Así, los extractos de I. glomeratay S. kraussii mostraron propiedades antioxidantes, y por lo tanto, podrían servir como una alternativa terapéutica en el tratamiento de disfunción eréctil inducida por estrés oxidativo.


Assuntos
Animais , Ratos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Inula/química , Salacia/química , Antioxidantes/farmacologia , Antioxidantes/química , Ácidos Sulfônicos/metabolismo , Flavonoides/análise , Espécies Reativas de Oxigênio , Ratos Sprague-Dawley , Estresse Oxidativo/efeitos dos fármacos , Asteraceae/química , Celastraceae/química , Benzotiazóis/metabolismo , Compostos Fenólicos/análise , Compostos Fitoquímicos/análise , Óxido Nítrico/metabolismo
7.
J Nat Med ; 75(3): 449-466, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33900535

RESUMO

During our studies characterizing functional substances from food resources for the prevention and treatment of lifestyle-related diseases, we isolated the active constituents, salacinol (1) and neokotalanol (4), and related thiosugar sulfoniums, from the roots and stems of the genus Salacia plants [Celastraceae (Hippocrateaceae)] such as Salacia reticulata Wight, S. oblonga Wall., and S. chinensis L., and observed their antidiabetic effects. These plant materials have been used traditionally in Ayurvedic medicine as a specific remedy at the early stage of diabetes, and have been extensively consumed in Japan, the United States, and other countries as a food supplement for the prevention of obesity and diabetes. Here, we review our studies on the antidiabetic effects of plants from the genus Salacia, from basic chemical and pharmacological research to their application and development as new functional food ingredients.


Assuntos
Hipoglicemiantes/farmacologia , Salacia/química , Álcoois Açúcares/farmacologia , Sulfatos/farmacologia , Tioaçúcares/farmacologia , Animais , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/prevenção & controle , Humanos , Japão , Ayurveda , Estrutura Molecular , Obesidade/prevenção & controle , Raízes de Plantas/química , Caules de Planta/química , Ensaios Clínicos Controlados Aleatórios como Assunto
8.
J Ethnopharmacol ; 266: 113423, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33007390

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Pristimerin is a triterpenoid considered the main component of Salacia crassifolia extracts. This terpene has shown promising antitumor, anti-inflammatory, and antimicrobial effects. Likewise, S. crassifolia has been used in traditional medicine to treat cancer and as an antimicrobial and anti-inflammatory agent. AIM OF THE STUDY: This study aimed to evaluate the antibacterial activity of the hexane extract of Salacia crassifolia roots (HER) and its isolate, pristimerin, against pathogenic bacteria. MATERIALS AND METHODS: First, we evaluated the spectrum of action of HER and pristimerin by the determination of the minimum inhibitory concentration (MIC) and the minimal bactericidal concentration (MBC). Subsequently, we analyzed the time-kill curve of these plant-derived compounds against Staphylococcus aureus. Then, we examined their mode of action by three different assays: the crystal violet methodology, the release of intracellular material, and transmission electron microscopy methods (TEM). Finally, we evaluated the effect of HER and pristimerin on the pre-formed biofilm of S. aureus by the crystal violet assay, the synergistic effect by the checkerboard method, the cytotoxicity against Vero cells, and the in silico activity using the online software PASS. RESULTS: HER and pristimerin presented a narrow spectrum of action against Gram-positive bacteria (MIC 0.195-25 µg/mL), and their primary mode of action is the alteration of membrane permeability of S. aureus. Our results show that the compounds disrupted the pre-formed biofilm of S. aureus in a dose-dependent manner. Furthermore, HER and pristimerin presented a significant synergic effect after the combination with well-known antibiotics, which was associated with the ability of these phytomedicines to change membrane permeability. Regarding the cytotoxic effect, the selective index (SI) of HER ranged from 0.37 to 11.86, and the SI of pristimerin varied from 0.24 to 30.87, according to the bacteria tested. CONCLUSIONS: Overall, HER and pristimerin showed a promising antibacterial effect in vitro through the alteration of membrane permeability of S. aureus.


Assuntos
Antibacterianos/farmacologia , Salacia/química , Staphylococcus aureus/efeitos dos fármacos , Triterpenos/farmacologia , Animais , Antibacterianos/isolamento & purificação , Biofilmes/efeitos dos fármacos , Chlorocebus aethiops , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Triterpenos Pentacíclicos , Raízes de Plantas , Infecções Estafilocócicas/tratamento farmacológico , Triterpenos/isolamento & purificação , Células Vero
9.
Bioorg Med Chem Lett ; 33: 127751, 2021 02 01.
Artigo em Inglês | MEDLINE | ID: mdl-33347966

RESUMO

Four chain-extended analogs (12a-12d) and two related de-O-sulfonated analogs (13a and 13c) by introducing alkyl groups (a: R = C3H7, b R = C6H13, c: R = C8H17, d: R = C10H21) to the side chains of salacinol (1), a natural α-glucosidase inhibitor from Ayurvedic traditional medicine "Salacia", were synthesized. The α-glucosidase inhibitory activities of all the synthesized analogs were evaluated in vitro. Against human intestinal maltase, the inhibitory activities of 12a and 13a with seven-carbon side chain were equal to that of 1. In contrast, analogs (12b-12d, and 13c) exhibited higher level of inhibitory activity against the same enzyme than 1 and had equal or higher potency than those of the clinically used anti-diabetics, voglibose, acarbose, and miglitol. Thus, elongation of the side chains of 1 was effective for specifically increasing the inhibitory activity against human intestinal maltase.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Intestinos/enzimologia , Salacia/química , Álcoois Açúcares/farmacologia , Sulfatos/farmacologia , alfa-Glucosidases/metabolismo , Animais , Relação Dose-Resposta a Droga , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Ayurveda , Conformação Molecular , Ratos , Relação Estrutura-Atividade , Álcoois Açúcares/síntese química , Álcoois Açúcares/química , Sulfatos/síntese química , Sulfatos/química
10.
J Med Food ; 24(1): 10-17, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33370165

RESUMO

The number of diabetes mellitus and borderline diabetes cases is increasing and poses a serious problem worldwide. Plants of the genus Salacia are known to have α-glucosidase inhibitory activity and to lower postprandial hyperglycemia. Two randomized, double-blind, placebo-controlled clinical trials were conducted to evaluate the efficacy of Salacia chinensis extract. Study 1 was a single-dose crossover study of 150, 300, or 600 mg of Salacia extract or placebo to determine the dose dependency of the effect on postprandial hyperglycemia. The duration of the washout period between each experimental day was a minimum of 6 days. Study 2 was a 12-week, multiple-dose, parallel-group study to evaluate the effects of 600 mg/day of Salacia extract on blood glucose parameters. In Study 1, Salacia induced significant dose-dependent suppression of postprandial blood glucose, insulin, and their incremental area under the curve values. The dose of 600 mg appeared to have the most significant effect. In Study 2, Salacia significantly improved several blood glucose-related parameters, such as hemoglobin A1c, and glucose tolerance after glucose challenge. These results suggest that S. chinensis extract may have beneficial effects in patients with diabetes.


Assuntos
Hiperglicemia , Hipoglicemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Salacia/química , Glicemia , Estudos Cross-Over , Diabetes Mellitus Tipo 2 , Relação Dose-Resposta a Droga , Método Duplo-Cego , Humanos , Hiperglicemia/tratamento farmacológico , Hiperglicemia/prevenção & controle , Hipoglicemiantes/administração & dosagem , Extratos Vegetais/administração & dosagem , Período Pós-Prandial
11.
IET Nanobiotechnol ; 14(6): 485-490, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32755958

RESUMO

In this examination, we researched the advantages of DNA fragmentation and metallic nanoparticles well-appointed with biomolecules. A novel interpretation of DNA damage by Silver Nano-Clusters (AgNCs) which were developed by the utilization of green synthesis method was demonstrated. The green synthesis of AgNCs was accomplished by utilizing the leaf extract of Salacia mulbarica (SM). The preparation of SM-AgNCs was developed by estimating surface plasmon resonance peak around 449 nm by using a UV-Visible spectrophotometer. The effect of phytochemicals in SM leaf extract on the development of stable SM-AgNCs was confirmed by FTIR spectroscopy. The size of the fabricated SM-AgNCs was estimated by dynamic light scattering and zeta-sizer analysis and the morphology of the SM-AgNCs was examined by transmission electron microscopy. The presence of clusters of Ag particles in the prepared SM-AgNCs was recognized by energy dispersion X-ray analysis. The results show that saponins, phytosterols, and phenolic compounds present in plant extract may play a great part in developing the SM-AgNCs in their specialized particles. The succeeded SM-AgNCs shows incredible anti-bacterial action towards Escherichia coli and Bacillus subtilis. In-light of the antibacterial study, these SM-AgNCs were analyzed with calf thymus-DNA and found significant damage to the strand of thymus-DNA.


Assuntos
Antibacterianos , Dano ao DNA/efeitos dos fármacos , Nanopartículas Metálicas/química , Extratos Vegetais , Salacia/química , Antibacterianos/química , Antibacterianos/metabolismo , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , DNA/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo , Prata/química , Prata/metabolismo , Prata/farmacologia
12.
J Biochem ; 167(5): 503-511, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-31883005

RESUMO

Hyperpigmentation that manifests through melasma and solar lentigo (age spots), although mostly harmless for health, bothers many people. Controlling the rate-limiting activity of tyrosinase is most effective for suppressing excessive melanin formation and accordingly recent research has focused on the maturation of tyrosinase. Salacia, a medicinal plant, has been used to treat diabetes in India and Sri Lanka. Salacia extract reportedly contains components that inhibit the activity of α-glucosidase. Salacinol, the active ingredient in Salacia extract, has unique thiosugar sulphonium sulphate inner salt structure. Here, we observed that the salacinol component of Salacia extract possesses anti-melanogenic activity in comparison to various existing whitening agents. Although the anti-melanogenic mechanism of salacinol is presumably medicated by inhibition of tyrosinase activity, which is often found in existing whitening agents, salacinol did not inhibit tyrosinase activity in vitro. Analysis of the intracellular state of tyrosinase showed a decrease in the mature tyrosinase form due to inhibition of N-linked oligosaccharide processing. Salacinol inhibited the processing glucosidase I/II, which are involved in the initial stage of N-linked glycosylation. Owing to high activity, low cytotoxicity and high hydrophilicity, salacinol is a promising candidate compound in whitening agents aimed for external application on skin.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Melanoma/tratamento farmacológico , Monofenol Mono-Oxigenase/antagonistas & inibidores , Oligossacarídeos/antagonistas & inibidores , Neoplasias Cutâneas/tratamento farmacológico , Álcoois Açúcares/farmacologia , Sulfatos/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Relação Dose-Resposta a Droga , Glicosilação , Humanos , Melaninas/antagonistas & inibidores , Melaninas/biossíntese , Melanoma/metabolismo , Melanoma/patologia , Camundongos , Conformação Molecular , Monofenol Mono-Oxigenase/metabolismo , Oligossacarídeos/metabolismo , Salacia/química , Neoplasias Cutâneas/metabolismo , Neoplasias Cutâneas/patologia , Relação Estrutura-Atividade , Álcoois Açúcares/química , Álcoois Açúcares/isolamento & purificação , Sulfatos/química , Sulfatos/isolamento & purificação , Células Tumorais Cultivadas
13.
Int J Mol Sci ; 20(24)2019 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-31847284

RESUMO

: Salacia chinensis L. (SC) stems have been used as an ingredient in Thai traditional medicine for treating patients with hepatic fibrosis and liver cirrhosis. However, there is no scientific evidence supporting the antifibrotic effects of SC extract. Therefore, this study aimed to determine the antifibrotic activity of SC stem extract in human hepatic stellate cell-line called LX-2. We found that upon TGF-ß1 stimulation, LX-2 cells transformed to a myofibroblast-like phenotype with a noticeable increase in α-SMA and collagen type I production. Interestingly, cells treated with SC extract significantly suppressed α-SMA and collagen type I production and reversed the myofibroblast-like characteristics back to normal. Additionally, TGF-ß1 also influenced the development of fibrogenesis by upregulation of MMP-2, TIMP-1, and TIMP-2 and related cellular signaling, such as pSmad2/3, pErk1/2, and pJNK. Surprisingly, SC possesses antifibrotic activity through the suppression of TGF-ß1-mediated production of collagen type 1, α-SMA, and the phosphorylation status of Smad2/3, Erk1/2, and JNK. Taken together, the present study provides accumulated information demonstrating the antifibrotic effects of SC stem extract and revealing its potential for development for hepatic fibrosis patients.


Assuntos
Células Estreladas do Fígado/metabolismo , Cirrose Hepática/tratamento farmacológico , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Extratos Vegetais/farmacologia , Caules de Planta/química , Salacia/química , Proteína Smad2/metabolismo , Proteína Smad3/metabolismo , Fator de Crescimento Transformador beta1/metabolismo , Linhagem Celular , Células Estreladas do Fígado/patologia , Humanos , Cirrose Hepática/metabolismo , Cirrose Hepática/patologia , Extratos Vegetais/química
14.
Carbohydr Res ; 484: 107777, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31446303

RESUMO

Four new triterpene glycosides, named salaciacochinosides A-D (1-4) were isolated from the 90% ethanol extract of Salacia cochinchinensis, together with five known compounds 2α,3ß,23-trihydroxyurs-12,18-dien-28-oic acid 28-O-ß-d-glucopyranoside (5), racemiside (6), alangiplatanoside (7), acantrifoside E (8), and syringin (9). The structures of the four new triterpenoids were characterized by chemical methods and MS, IR, 1D and 2D NMR spectral analyses. The α-glucosidase inhibitory activities of the nine compounds were assessed, compounds 6 and 7 showed remarkable α-glucosidase inhibitory activities, with IC50 values of 0.44 and 0.75 µM, respectively. Compounds 1-5 exhibited moderate α-glucosidase inhibitory activities, and compounds 8 and 9 showed none α-glucosidase inhibitory activity in our current experiments.


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Glicosídeos/química , Salacia/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos/farmacologia , Concentração Inibidora 50 , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Triterpenos/química , Triterpenos/farmacologia
15.
Drug Discov Ther ; 13(3): 133-136, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31327788

RESUMO

Using a silkworm evaluation system, we previously evaluated various substances that suppress postprandial hyperglycemia. Enterococcus faecalis YM0831, a lactic acid bacterium that inhibits glucose uptake by the human intestinal Caco-2 cell line, exhibited hyperglycemia-suppressing effects in the silkworm system. In the present study, we found that Kothala himbutu (Salacia reticulata) extract, a traditional medicine containing α-glucosidase inhibitors, suppressed sucrose-induced hyperglycemia in the silkworm system. Moreover, combined oral administration of lactic acid bacteria YM0831 with Kothala himbutu extract had stronger suppressive effects on sucrose-induced hyperglycemia than single administration of either component. These findings suggest that the silkworm system provides a simple way to evaluate the effects of supplements on the suppression of blood glucose level induced by sucrose ingestion.


Assuntos
Enterococcus faecalis/fisiologia , Hiperglicemia/terapia , Extratos Vegetais/administração & dosagem , Salacia/química , Animais , Glicemia/metabolismo , Bombyx , Terapia Combinada , Modelos Animais de Doenças , Hiperglicemia/induzido quimicamente , Hiperglicemia/metabolismo , Extratos Vegetais/uso terapêutico , Sacarose/efeitos adversos , Resultado do Tratamento
16.
Molecules ; 24(14)2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31295972

RESUMO

Predominantly spread in West Tropical Africa, the shrub Salacia senegalensis (Lam.) DC. is known because of its medicinal properties, the leaves being used in the treatment of skin diseases. Prompted by the ethnomedicinal use, a hydroethanolic extract obtained from the leaves of the plant was screened against a panel of microbial strains, the majority of which involved in superficial infections. The extract was found to be active against the dermatophytes Trichophyton rubrum and Epidermophyton floccosum. Notable results were also recorded regarding the attenuation of the inflammatory response, namely the inhibitory effects observed against soybean 5-lipoxygenase (IC50 = 71.14 µg mL-1), no interference being recorded in the cellular viability of RAW 264.7 macrophages and NO levels. Relevantly, the extract did not lead to detrimental effects against the keratinocyte cell line HaCaT, at concentrations displaying antidermatophytic and anti-inflammatory effects. Flavonoid profiling of S. senegalensis leaves was achieved for the first time, allowing the identification and quantitation of myricitrin, three 3-O-substituted quercetin derivatives, and three other flavonoid derivatives, which may contribute, at least partially, to the observed antidermatophytic and anti-inflammatory effects. In the current study, the plant S. senegalensis is assessed concerning its antidermatophytic and anti-inflammatory properties.


Assuntos
Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Arthrodermataceae/efeitos dos fármacos , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Salacia/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Antifúngicos/química , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Flavonoides/química , Humanos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/química , Células RAW 264.7 , Análise Espectral
17.
J Nat Med ; 73(3): 584-588, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31028661

RESUMO

The antidiabetic effects of a hot water extract of the stems of Salacia chinensis (SCE) were evaluated in vivo in ob/ob mice (genetically obese hyperglycemic mice). Administration of dietary feed containing 0.20 and 0.50% of SCE for 23 days to ob/ob mice significantly suppressed the elevation of both blood glucose and HbA1c levels, without significantly changing body weight and food intake. To characterize the antidiabetic effects of the thiosugar sulfonium constituent neokotalanol (1), which has potent α-glucosidase inhibitory activity, we performed a similar in vivo study. HbA1c levels were significantly suppressed in ob/ob mice after the administration of dietary feed containing 0.0003% of neokotalanol (1) for 20 days. These results indicate that SCE and neokotalanol (1) are potential leads for the development of novel antidiabetic agents.


Assuntos
Hemoglobinas Glicadas/metabolismo , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , Salacia/química , Tioaçúcares/farmacologia , Animais , Glicemia/análise , Glicemia/efeitos dos fármacos , Peso Corporal , Hipoglicemiantes/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos , Camundongos Obesos , Obesidade , Tioaçúcares/química
18.
J Basic Clin Physiol Pharmacol ; 30(2): 239-244, 2018 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-30367801

RESUMO

Background Salacial lehmbachii stem bark is used traditionally for the treatment of diabetes mellitus and its associated complications. Treatment of diabetes is necessary to reduce these complications. Methods In this study, the antidiabetic and antihyperlipidemic potential of S. lehmbachii ethanol stem bark extract was evaluated in alloxan-induced diabetic rats at a dose of 100 mg/kg, 200 mg/kg, and 400 mg/kg p.o. daily for 21 days. Blood glucose levels, serum total cholesterol (TC), triglycerides (TG), high density lipoprotein (HDL), low density lipoprotein (LDL), and very low density lipoprotein (VLDL) were assessed in the animals. Results Treatment of alloxan-induced diabetic rats with S. lehmbachii stem bark extract showed significant (p<0.01) reduction in blood glucose levels when compared with diabetic control. The elevated levels of serum cholesterol, triglycerides, LDL, and VLDL were significantly (p<0.01) reduced by S. lehmbachii stem bark extract, while the level of HDL significantly (p<0.01) increased. Conclusions The results obtained suggest that S. lehmbachii stem bark extract has the potential to treat diabetes condition and hyperlipidemic disorders.


Assuntos
Aloxano/farmacologia , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Salacia/química , Animais , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Colesterol/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/metabolismo , Etanol/química , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fitoterapia/métodos , Casca de Planta/química , Ratos
19.
Fitoterapia ; 131: 174-181, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30352292

RESUMO

Phytochemical studies of the seeds of the Cameroonian medicinal plant, Salacia staudtiana, resulted in the isolation and identification of five new cardenolides (1-5) as well as a new dihydro-ß-agarofuran (9), along with eight known compounds. The structures of all compounds were elucidated by 1D/2D NMR, ESI-HRMS data and comparison with literature data. The relative configurations of the new compounds were defined by X-ray crystallography analysis, NOESY correlations and coupling constants. We evaluated their antibacterial efficacy against two commonly dispersed environmental strains of Escherichia coli and Bacillus subtilis, and two pathogenic strains of Staphylococcus aureus and Pseudomonas aeruginosa, compared to the standard antibiotics, streptomycin and gentamicin. Moreover, we assessed the antibacterial activity of the crude extract of the seeds in parallel to evaluate the plausible synergistic effects of the compounds in chemical defense of the seeds during germination and plant reproduction. The isolated compounds showed moderate antibacterial activities against the tested organisms. Compounds 1 and 3 and the crude extract exhibited distinct antibacterial activities against B. subtilis and S. aureus. The isolated compounds showed weak DPPH radical scavenging properties compared to the reference standard (Trolox). Our study lends evidence to the antibacterial chemical defense of S. staudtiana seeds by seed-borne compounds.


Assuntos
Antibacterianos/farmacologia , Cardenolídeos/farmacologia , Salacia/química , Sementes/química , Sesquiterpenos/farmacologia , Antibacterianos/isolamento & purificação , Camarões , Cardenolídeos/isolamento & purificação , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Plantas Medicinais/química , Sesquiterpenos/isolamento & purificação
20.
Mater Sci Eng C Mater Biol Appl ; 93: 664-670, 2018 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-30274099

RESUMO

Gold nanoparticles have been extensively used in diagnostics, biomedical imaging, and drug delivery owing to simple method of synthesis and versatile surface functionalization. Present investigation aims to evaluate the osteoinductive property of Salacia chinensis (SC) mediated gold nanoparticles (GNPs) for its application in implant dentistry. The formation of GNPs was assessed initially using the visual method and characterized analytically by using UV-visible spectroscopy, Zetasizer, X-RD, ICP-AES, AFM, and TEM. Green synthesized GNPs exhibited a remarkable stability in various blood components (0.2 M histidine, 0.2 M cysteine 2% bovine serum albumin, and 2% human serum albumin) and were found to be nontoxic when evaluated for their cytocompatibility and blood compatibility using periodontal fibroblasts and erythrocytes respectively. Exposure of GNPs to MG-63 cell lines displayed increased percent cell viability (138 ±â€¯27.4) compared to the control group (96 ±â€¯3.7) which confirms its osteoinductive potential. Herein, it can be concluded that the stable, biocompatible and eco-friendly GNPs can be used as an effective bone inductive agent during dental implant therapy.


Assuntos
Implantes Dentários , Fibroblastos/metabolismo , Ouro/química , Teste de Materiais , Nanopartículas Metálicas/química , Periodonto/metabolismo , Processos Fotoquímicos , Salacia/química , Linhagem Celular Tumoral , Fibroblastos/citologia , Humanos , Periodonto/citologia
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