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1.
Appl Microbiol Biotechnol ; 108(1): 200, 2024 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-38326604

RESUMO

The plants of the genus Salacia L. are the storehouse of several bioactive compounds, and are involved in treating human diseases and disorders. Hitherto, a number of reports have been published on in vitro biotechnology as well as microbial involvement in the improvement of Salacia spp. The present review provides comprehensive insights into biotechnological interventions such as tissue culture for plant propagation, in vitro cultures, and endophytic microbes for up-scaling the secondary metabolites and biological potential of Salacia spp. Other biotechnological interventions such as molecular markers and bio-nanomaterials for up-grading the prospective of Salacia spp. are also considered. The in vitro biotechnology of Salacia spp. is largely focused on plant regeneration, callus culture, cell suspension culture, somatic embryogenesis, and subsequent ex vitro establishment of the in vitro-raised plantlets. The compiled information on tissue cultural strategies, involvement of endophytes, molecular markers, and nanomaterials will assist the advanced research related to in vitro manipulation, domestication, and commercial cultivation of elite clones of Salacia spp. Moreover, the genetic diversity and other molecular-marker based assessments will aid in designing conservation policies as well as support upgrading and breeding initiatives for Salacia spp. KEY POINTS: • Salacia spp. plays a multifaceted role in human health and disease management. • Critical and updated assessment of tissue culture, endophytic microbes, metabolites, molecular markers, and bio-nanomaterials of Salacia spp. • Key shortcomings and future research directions for Salacia biotechnology.


Assuntos
Salacia , Humanos , Biotecnologia , Plantas , Técnicas de Cultura de Células , Endófitos
2.
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
3.
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
4.
Curr Microbiol ; 79(7): 204, 2022 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-35612657

RESUMO

Antibiotic resistance and the hazardous nature of synthetic drugs is threatening issue in the health sector. The alternative for this problem is to focus on plants that attribute to various compounds that exhibit therapeutic properties. Therefore, the study aims to evaluate the antimicrobial efficacy of Salacia oblonga leaf and root extracts against tested human pathogens. The S. oblonga extracts showed a significant zone of inhibition against bacteria and fungi. The leaf and root extracts of S. oblonga are prepared using low polar to high polar solvents in the Soxhlet apparatus and tested on the selected bacterial and fungal strains. Agar well diffusion and broth dilution methods evaluate antibacterial activity, antifungal activity, and Minimum Inhibitory Concentration (MIC) of extracts. Among the extracts tested, the ethyl acetate extract of root showed more antimicrobial activity against the tested bacterial and fungal strains. The most susceptible bacterial and fungal species against ethyl acetate extract are Micrococcus luteus, Mycobacterium tuberculosis, Microsporum canis, Trichophyton interdigitale, and Microsporum gypseum. The MIC for bacteria ranged from 13.0 to > 200 µg/ml, whereas for fungi, the MIC ranged from 25.9 to > 200 µg/ml. Ethyl acetate extract of root with 100 µg/ml concentration showed 29.1 mm and 28.7 mm zone of inhibition against bacterial strains M. luteus and M. tuberculosis, respectively. The ethyl acetate extract of root with a 100 µg/ml concentration showed 15.8, 15.2, and 15.6 mm zone of inhibition against fungal isolates M. canis, T. interdigitale, and M. gypseum, respectively. The activity of root and leaf extracts increased in a concentration-dependent manner, and further, the compounds isolated from the crude extracts of leaf and root showed antimicrobial activity. Structural elucidation of isolated compounds Lambertic acid and Ferruginol was done using NMR spectroscopy. Reports indicate that Lambertic acid was isolated previously, but the isolation of hydroxy Ferruginol from S. oblonga leaf extract was reported unprecedented.


Assuntos
Anti-Infecciosos , Salacia , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Bactérias , Humanos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
5.
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
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 ; 274: 113909, 2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-33588011

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The roots and stems of several Salacia species have been used as traditional medicines, especially in Ayurvedic medical system for the treatment of diabetes, rheumatism, gonorrhea, amenorrhea, skin diseases, etc. Due to reported evidence supporting Salacia's beneficial effects in early-stage diabetes and other lifestyle-related diseases, Salacia-based dietary supplements and health foods have been gaining popularity in Japan and other countries in recent years. However, due to the morphological similarities between Salacia plants, particularly in the medicinally used parts (roots and stems), the authentication of the botanical identities of Salacia-derived products is challenging. AIM OF THIS STUDY: This study aims to develop a genetic approach to authenticate the medicinally used Salacia species and to determine the botanical sources of the commercially available Salacia-derived products. MATERIALS AND METHODS: The sequences of nuclear DNA internal transcribed spacer (ITS) and chloroplast trnK-rps16 region were determined and compared between 10 plant specimens from three medicinally used Salacia species as well as 48 samples of commercial crude drugs. Moreover, a PCR-restriction fragment length polymorphism (RFLP) assay was developed for rapid identification based on the ITS sequences. RESULTS: The plant specimens from the three medicinally used Salacia species showed three main types of sequences in both ITS (types I, II, III) and trnK-rps16 (i, ii, iii) regions. Combined the sequences of ITS and trnK-rps16 regions, S. reticulata and S. oblonga had type I-i and type III-iii or similar sequences, respectively. S. chinensis had type II-ii or II(536M)-i sequences. Forty-eight samples of commercial crude drugs were identified based on ITS and trnK-rps16 DNA barcode. A convenient PCR-RFLP assay using Cac8I restriction enzyme was established and applied to identify the botanical sources of health food products purchased from online retailers. All the twelve samples were identified as S. chinensis. CONCLUSION: The nrDNA ITS sequences provided useful information to authenticate Salacia species and to elucidate the phylogenetic relationship within the Salacia genus. Genetic identification results revealed that S. chinensis and S. reticulata are the major sources of commercially available Salacia-products. Based on the ITS sequences, a convenient PCR-RFLP assay was established for the identification of the medicinally used Salacia species as well as their derived health food products.


Assuntos
Código de Barras de DNA Taxonômico/métodos , DNA de Plantas/genética , DNA Espaçador Ribossômico/genética , DNA Espaçador Ribossômico/isolamento & purificação , Reação em Cadeia da Polimerase/métodos , Salacia/classificação , Salacia/genética , DNA de Cloroplastos/análise , DNA de Cloroplastos/genética , DNA Espaçador Ribossômico/análise , Suplementos Nutricionais/análise , Análise de Alimentos , Filogenia , Polimorfismo de Fragmento de Restrição
9.
Comput Biol Chem ; 91: 107438, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33524844

RESUMO

The genus Salacia (Celastraceae) consists of many important medicinal plants used mainly against type II diabetes. Segregation and delimitation of species is difficult based on morphological features alone. DNA barcoding is the most effective and emerging method of molecular identification. It was reported that ITS2 has better discriminating power in the genus Salacia in comparison to other barcode loci. This paper describe the analysis of sequence and structural information of ITS2 to discriminate the species of Salacia. A total of 8 species of Salacia in South India and the available sequences in NCBI database were taken for the present study. NJ method based phylogenetic trees were constructed using MEGAX with primary sequence as well as using sequence and secondary structural information. Primary structure based phylogeny did not give much information whereas the dendrogram based on sequence and structural information was more informative to decipher the phylogeny of South Asian species of Salacia. The present study revealed some interesting facts regarding the genus. Secondary structure of the ITS2 sequence of S. chinensis reported from Kerala differs consistently from that of S. chinensis reported from other parts of India and of South Asia. Probably the S. chinensis in Kerala, India has diverged a lot from the original S. chinensis. ITS2 sequence of S. reticulata reported from Sri Lanka was identical to S. chinensis reported by other groups from Thailand and Udupi, India. The molecular level identity of ITS2 sequence of S. chinensis with S. reticulata suggest merger of the two species. ITS2 sequence of S. beddomei is only reported from Kerala, India showed it to be identical to S. macrosperma. This observation points to a mistaken identity of S. beddomei which could be elusive from Kerala. Phylogenetic trees constructed based on sequence and structural features of ITS2 suggest that the ancestor species of S.chinensis diversified in two evolutionary lines. One line leads to the present day S. chinensis and the other line further diversified and lead to the rest of the present day Salacia species.


Assuntos
Genes de Plantas , Marcadores Genéticos , Conformação de Ácido Nucleico , Filogenia , RNA de Plantas/química , Salacia/classificação , Código de Barras de DNA Taxonômico , Índia , Reação em Cadeia da Polimerase/métodos , RNA de Plantas/genética , Salacia/genética
10.
Niger J Physiol Sci ; 36(2): 195-201, 2021 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-35947737

RESUMO

The root bark of Salacia nitida L.benth (celastraceae) is used as remedy for malaria and typhoid fever in Southern part of Nigeria. This study is designed to evaluate the effect of treatment with ethanolic extract from root bark of S. nitida on lipid peroxidation, hepatomegaly and splenomegaly in Plasmodium berghei-malaria infected mice. Thirty malaria-infected and six uninfected mice were used for the study. 280, 430, and 580 mg kg-1 body weight day-1 of ethanolic extract and 4 mg kg-1 body weight day-1 of artesunate were administered orally to infected mice in groups B, C, D, and E, while 4 ml kg-1 body weight day-1 of physiological saline was given to infected untreated mice in group A and the uninfected untreated mice in group F. Treatments were done for five days. Levels of malondialdehyde were measured as means of assessing lipid peroxidation in the experimental animals. Weights of experimental animals, liver, and spleen, and the length of spleen from experimental animals were also measured. Animal's liver and spleen-body weight ratios were determined. Results from the study showed significant decrease (P < 0.05) in levels of malondialdehyde, and significant increase (P < 0.05) in body weights. Also, significant decreases (P < 0.05) were seen in the weights of liver and spleen, lengths of spleen, and organ-body weight ratios of malaria-infected treated mice. Therefore, this study confirmed that ethanolic extract from root bark of S. nitida is effective in the treatment of malaria, as it is seen in its ability to attenuate lipid peroxidation and hepatosplenomegaly in mice, thus corroborating its traditional use for the treatment of malaria.


Assuntos
Antimaláricos , Malária , Salacia , Animais , Antimaláricos/farmacologia , Antimaláricos/uso terapêutico , Peso Corporal , Etanol/uso terapêutico , Hepatomegalia/tratamento farmacológico , Peroxidação de Lipídeos , Malária/tratamento farmacológico , Malondialdeído/farmacologia , Camundongos , Casca de Planta , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Plasmodium berghei , Esplenomegalia/tratamento farmacológico
11.
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
12.
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
13.
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
14.
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
15.
J Asian Nat Prod Res ; 22(8): 738-745, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31131622

RESUMO

Two new isopimarane diterpenoids, named 1α-hydroxy-7-oxoisopimara-8, 15-diene (1), 11ß-hydroxy-7-oxoisopimara-8(14), 15-diene (2), together with six known compounds (3-8), were isolated from the medicinal plant Salacia cochinchinensis. All isolates were assayed for their cytotoxicity and α-glucosidase inhibitory activity. Results suggested compounds 1, 3 possessed significant cytotoxic activity against HepG2, HL60, and Hela cell lines with IC50 values ranging from 0.23 to 0.35 µM, and compounds 7, 8 exhibited noticeable α-glucosidase inhibitory ability with IC50 values of 0.25 and 0.31 µM, respectively.


Assuntos
Diterpenos , Salacia , Células HeLa , Humanos , Estrutura Molecular , alfa-Glucosidases
16.
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
17.
Pol J Microbiol ; 69(4): 453-462, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33574873

RESUMO

Stems and roots of Salacia genus plants have been used as a specific remedy for early-stage diabetes, and one of the four sulphonium sulphates, salacinol is the compound responsible for the anti-diabetic activity. Salacia is prone to microbial contamination and insect infestation; hence, methods to estimate the microbial load in such plants will enhance its nutritional value. This paper highlights the novel use of Soleris® to quantify microbes of all types, namely bacteria, yeasts, molds, and coliforms in herbal extracts. The microbial analysis results obtained with Soleris® test vial have been compared with the conventional method, and the results indicate that Soleris® is equally efficient as the conventional method and in fact displays several advantages over the traditional method. The Soleris® method is a real time monitoring system that is highly sensitive, user-friendly, and environmentally friendly since it generates very little biomedical waste and saves a large amount of time. The data presented here demonstrate that for highly contaminated samples, results are available within 24 h. For yeasts and molds, the Soleris® method produces results in 48 h, thus offering considerable time savings compared to other commonly used methods.


Assuntos
Bactérias/crescimento & desenvolvimento , Carga Bacteriana , Contaminação de Medicamentos , Fungos/crescimento & desenvolvimento , Técnicas Microbiológicas , Extratos Vegetais , Salacia/microbiologia , Dióxido de Carbono/análise , Raízes de Plantas/microbiologia , Caules de Planta/microbiologia , Plantas Medicinais/microbiologia , Software
18.
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
19.
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
20.
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
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