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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.
Zhongguo Zhong Yao Za Zhi ; 48(24): 6676-6681, 2023 Dec.
Artigo em Zh | 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.
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
4.
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
5.
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
6.
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
7.
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
8.
Arch Virol ; 163(6): 1567-1576, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29478125

RESUMO

Mayaro fever, caused by Mayaro virus (MAYV) is a sub-lethal disease with symptoms that are easily confused with those of dengue fever, except for polyarthralgia, which may culminate in physical incapacitation. Recently, outbreaks of MAYV have been documented in metropolitan areas, and to date, there is no therapy or vaccine available. Moreover, there is no information regarding the three-dimensional structure of the viral proteins of MAYV, which is important in the search for antivirals. In this work, we constructed a three-dimensional model of protein C of MAYV by homology modelling, and this was employed in a manner similar to that of receptors in virtual screening studies to evaluate 590 molecules as prospective antiviral agents. In vitro bioassays were utilized to confirm the potential antiviral activity of the flavonoid epicatechin isolated from Salacia crassifolia (Celastraceae). The virtual screening showed that six flavonoids were promising ligands for protein C. The bioassays showed potent antiviral action of epicatechin, which protected the cells from almost all of the effects of viral infection. An effective concentration (EC50) of 0.247 µmol/mL was observed with a selectivity index (SI) of 7. The cytotoxicity assay showed that epicatechin has low toxicity, with a 50% cytotoxic concentration (CC50) greater than 1.723 µmol/mL. Epicatechin was found to be twice as potent as the reference antiviral ribavirin. Furthermore, a replication kinetics assay showed a strong inhibitory effect of epicatechin on MAYV growth, with a reduction of at least four logs in virus production. Our results indicate that epicatechin is a promising candidate for further testing as an antiviral agent against Mayaro virus and other alphaviruses.


Assuntos
Alphavirus/química , Antígenos Virais/química , Antivirais/farmacologia , Catequina/farmacologia , Salacia/química , Proteínas Virais/química , Alphavirus/metabolismo , Animais , Antígenos Virais/metabolismo , Antivirais/química , Antivirais/isolamento & purificação , Sítios de Ligação , Catequina/química , Catequina/isolamento & purificação , Chlorocebus aethiops , Ensaios de Triagem em Larga Escala , Humanos , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Ligação Proteica , Conformação Proteica em alfa-Hélice , Conformação Proteica em Folha beta , Domínios e Motivos de Interação entre Proteínas , Ribavirina/química , Ribavirina/farmacologia , Homologia Estrutural de Proteína , Interface Usuário-Computador , Células Vero , Proteínas Virais/antagonistas & inibidores , Proteínas Virais/metabolismo , Replicação Viral/efeitos dos fármacos
9.
Mol Biol Rep ; 45(5): 931-941, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30027475

RESUMO

Diversity and phylogenetic relationship between four closely related Salacia species, i.e., Salacia chinensis, Salacia macrosperma, Salacia fruticosa and Salacia oblonga, collected from the Western Ghats of Karnataka, India, was assessed. Ten each of RAPD and ISSR primers generated a total of 76 and 68 loci, generating polymorphisms of 92.21 and 89.71%, respectively. Maximum likelihood analysis of the ITS sequences revealed three clades. Dendrogram analyses of RAPD and ISSR revealed two and four clusters, respectively. Overall polymorphism revealed by RAPD was 41.45 ± 10%, ISSR was 33.58 ± 6.52%, and ITS was 25.50 ± 17.25%. Molecular variance revealed significant variance within and among the Salacia species. Tajima's D neutrality test and Fu's Fs were negative for all four species, implying presences of rare alleles and population expansion. Comparative study of RAPD, ISSR and ITS for Salacia species has given an insight into the efficiency of each technique in detecting diversity within and among the population sampled in the Western Ghats of Karnataka.


Assuntos
Marcadores Genéticos , Variação Genética , Técnica de Amplificação ao Acaso de DNA Polimórfico/métodos , Salacia/genética , DNA de Plantas/genética , Funções Verossimilhança , Repetições de Microssatélites , Filogenia , Salacia/classificação
10.
Molecules ; 23(6)2018 06 20.
Artigo em Inglês | MEDLINE | ID: mdl-29925807

RESUMO

The new pentacyclic triterpene 11ß-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both the extract and the purified triterpenes displayed pronounced cytotoxic activity against human cancer cell lines. The NCI-60 cell line screen revealed that compound 2 was the most active, with a mean GI50 of 0.17 µM, while compound 1 had a mean GI50 of 8.7 µM. A COMPARE analysis of the screening results showed that pristimerin is likely to be the main compound responsible for the cytotoxic activity of the extract (mean GI50 of 0.3 µg·mL−1). A targeted search for pristimerin and related derivatives using LC-MS/MS revealed the presence of pristimerin (2) and 6-oxopristimerol (3) in all Celastraceae species examined and in all plant parts tested, while vitideasin (4) was only detected in the genus Salacia.


Assuntos
Celastraceae/metabolismo , Metabolômica/métodos , Extratos Vegetais/química , Salacia/química , Triterpenos/química , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/metabolismo , Antineoplásicos/uso terapêutico , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Triterpenos Pentacíclicos , Raízes de Plantas/química , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação , Triterpenos/metabolismo , Triterpenos/uso terapêutico
11.
J Org Chem ; 81(8): 3407-15, 2016 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-27015084

RESUMO

A facile and highly diastereoselective route to potent natural α-glucosidase inhibitors, i.e., neosalacinol (4) and neoponkoranol (6), isolated from the traditional Ayurvedic medicine "Salacia" was developed by intramolecular cyclization of appropriately substituted sulfides (9 and 12).


Assuntos
Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/química , Salacia/química , Álcoois Açúcares/química , Álcoois Açúcares/farmacologia , Sulfatos/química , Sulfatos/farmacologia , Sulfetos/química , Tiofenos/química , Tiofenos/farmacologia , Ciclização , Extratos Vegetais/isolamento & purificação , Estereoisomerismo , Relação Estrutura-Atividade
12.
Pharm Biol ; 54(3): 458-64, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25973644

RESUMO

CONTEXT: Tobacco smoking generates a tremendous amount of free radicals that induce oxidative stress (OS) in diabetics (pancreatic islet cells are defective). Salacia oblonga Wall. (Celastraceae) is a proven antioxidant and antidiabetic plant whose mechanism of action is yet to be explored. OBJECTIVE: The present study focuses on the protective ability of S. oblonga in tobacco smoke-induced oxidatively stressed pancreatic ß-cell line. MATERIALS AND METHODS: The RINm5f cell line was exposed to tobacco smoke concentrate (TSC) (0.5-10%, 24 h), plant extract (1-75 µg/ml, 3 h), and their combinations. Cell viability was determined through MTT assay. Microscopic analysis was carried out in unstained and nonyl acridine orange-stained cells. The effect of toxic doses of TSC on DNA integrity was analyzed through DNA fragmentation assay. The TSC-induced nitric oxide generation was determined spectrophototmetrically. The expression of anti-apoptotic protein Bcl-X under the above treatment conditions was carried out through RT-PCR. RESULTS: The LD50 dose for TSC was found to be 1% TSC. Salacia oblonga extracts (10 and 15 µg/ml) were found to be optimum safe doses that significantly increased cell viability and decreased the nitric oxide production in TSC-treated cells. Pre-treatment with plant extract suppressed apoptosis through probable increase in the expression of anti-apoptotic protein Bcl-X in TSC-treated cells. Thus, the overall efficiency of plant extract in recovering cellular damage was proven. DISCUSSION AND CONCLUSION: The results suggest that TSC-induced cellular alterations are related to rise in nitric oxide and Bcl-X mRNA expression and propose that S. oblonga may confer significant cytoprotection against OS-mediated injury in ß-cells.


Assuntos
Dano ao DNA/efeitos dos fármacos , Células Secretoras de Insulina/efeitos dos fármacos , Nicotiana/toxicidade , Extratos Vegetais/farmacologia , Salacia , Fumaça/efeitos adversos , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Dano ao DNA/fisiologia , Relação Dose-Resposta a Droga , Células Secretoras de Insulina/patologia , Extratos Vegetais/isolamento & purificação , Substâncias Protetoras/isolamento & purificação , Substâncias Protetoras/farmacologia , Ratos
13.
Nutr J ; 14: 21, 2015 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-25889885

RESUMO

BACKGROUND: Nearly 50% of diabetic patients worldwide use complementary medicines to treat or supplement their conventional diabetes treatment. Salacia reticulata (Kothala himbutu) is a woody climber used widely in the Ayurvedic system to treat diabetes and obesity. OBJECTIVE: In this review I critically analyze the evidence for using Salacia reticulata for treating type 2 diabetes and obesity. The available evidence is described in terms of in-vitro studies, animal studies and clinical trials. RESULTS AND CONCLUSIONS: In vitro studies demonstrate the ability of Salacia to inhibit intestinal alpha glucosidase. In mouse mesenteric fat it enhances the mRNA expression for hormone sensitive lipase (HSL) and adiponectin; thus increasing lipolysis and reducing insulin resistance respectively. In 3 T3-L-1 adipocytes lipogenesis factors are down regulated and lipolysis factors are up regulated with Salacia reticulata treatment. Animal studies and clinical trials are consistent in demonstrating improvement of glucose concentrations in the fasted and sucrose and maltose loaded states. Clinically significant reductions of HbA1C and plasma Insulin are reported with treatment of 6 weeks to 3 months. One clinical trial reported significant reduction of weight and BMI when Salacia is used in combination with vitamin D. Salacia reticulata effectively improves insulin resistance, glucose metabolism and reduces obesity. A larger evidence base is required from well-planned studies to confirm its efficacy and safety.


Assuntos
Glicemia/efeitos dos fármacos , Diabetes Mellitus Tipo 2/dietoterapia , Resistência à Insulina , Obesidade/dietoterapia , Extratos Vegetais , Salacia , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Adiponectina/genética , Adiponectina/metabolismo , Animais , Peso Corporal/efeitos dos fármacos , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/metabolismo , Hemoglobinas Glicadas/análise , Humanos , Insulina/sangue , Lipogênese/efeitos dos fármacos , Lipólise/efeitos dos fármacos , Camundongos , Obesidade/sangue , Obesidade/metabolismo , RNA Mensageiro/efeitos dos fármacos , Esterol Esterase/genética , Esterol Esterase/metabolismo , Resultado do Tratamento , alfa-Glucosidases/sangue
14.
Phytother Res ; 29(7): 986-95, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26031882

RESUMO

Extracts of Salacia reticulata Wight (Hypocrataceae) roots, stems, and leaves have been used in Asia for hundreds of years for the folkloric treatment of diabetes and other health problems. Constituents that have been identified as exhibiting anti-diabetic effects include salacinol, kotalanol, ponkorinol, salaprinol, and their corresponding de-0-sulfonated compounds. Mangiferin, kotalagenin 16-acetate and various proanthocyanidin oligomers have also been isolated. Studies indicate that Salacia extracts modulate multiple targets that influence carbohydrate and lipid metabolism including α-glucosidase, aldose reductase, pancreatic lipase, peroxisomal proliferator-activated receptor-α, glucose transporter-4 mediated glucose uptake, and angiotensin II type 1 receptor. Furthermore, Salacia extracts exhibit free radical scavenging, antioxidant and hepatoprotectant activities. In human studies, Salacia extracts have been shown to decrease plasma glucose and insulin levels, decrease HbA1c, and modulate serum lipid levels with no adverse effects being reported. Similar results have been demonstrated in rat and mouse models as well as in vitro systems. Safety of S. reticulata and other Salacia species as S. oblonga and S. chinensis in rats and mice indicate that extracts are exceedingly safe. No clinical studies have examined the effects of Salacia extracts on human weight loss, although weight loss and decreases in weight gain have been demonstrated in animal models. Because of the large number of pharmacologically active compounds, it is difficult to establish standards for extracts.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Salacia/química , Animais , Antioxidantes/farmacologia , Metabolismo dos Carboidratos/efeitos dos fármacos , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos , Monossacarídeos/farmacologia , Folhas de Planta/química , Raízes de Plantas/química , Proantocianidinas/farmacologia , Ensaios Clínicos Controlados Aleatórios como Assunto , Ratos , Álcoois Açúcares/farmacologia , Sulfatos/farmacologia , Triterpenos/farmacologia , Xantonas/farmacologia
15.
AAPS PharmSciTech ; 16(2): 250-8, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25273025

RESUMO

The US patented polyherbal formulation for the prevention and management of type II diabetes and its vascular complications was used for the present study. The xanthone glycoside mangiferin is one of the major effector constituents in the Salacia species with potential anti-diabetic activity. The pharmacokinetic differences of mangiferin following oral administration of pure mangiferin and polyherbal formulation containing Salacia species were studied with approximately the same dose 30 mg/kg mangiferin and its distribution among the major tissue in Wistar rats. Plasma samples were collected at different time points (15, 30, 60, 120, 180, 240, 360, 480, 600, 1,440, 2,160, and 2880 min) and subsequently analyzed using a validated simple and rapid LC-MS method. Plasma concentration versus time profiles were explored by non-compartmental analysis. Mangiferin plasma exposure was significantly increased when administered from formulation compared to the standard mangiferin. Mangiferin resided significantly longer in the body (last mean residence time (MRTlast)) when given in the form of the formulation (3.65 h). Cmax values of formulation (44.16 µg/mL) administration were elevated when compared to equivalent dose of the pure mangiferin (15.23 µg/mL). Tissue distribution study of mangiferin from polyherbal formulation was also studied. In conclusion, the exposure of mangiferin is enhanced after formulation and administration and could result in superior efficacy of polyherbal formulation when compared to an equivalent dose of mangiferin. The results indicate that the reason which delays the elimination of mangiferin and enhances its bioavailability might the interactions of the some other constituents present in the polyherbal formulation. Distribution study results indicate that mangiferin was extensively bound to the various tissues like the small intestine, heart, kidney, spleen, and liver except brain tissue.


Assuntos
Medicamentos sem Prescrição/farmacocinética , Extratos Vegetais/farmacocinética , Xantonas/farmacocinética , Administração Oral , Animais , Disponibilidade Biológica , Química Farmacêutica/métodos , Diabetes Mellitus Tipo 2 , Hipoglicemiantes/farmacocinética , Masculino , Ratos , Ratos Wistar , Salacia/química , Distribuição Tecidual , Estados Unidos
16.
Phytochem Anal ; 25(6): 544-50, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24816820

RESUMO

INTRODUCTION: Stems and roots of Salacia genus plants have been used in Ayurveda as a specific remedy for early stage diabetes. Previous investigations identified four sulphonium sulphates, that is, salacinol (1), kotalanol (3), ponkoranol (5) and salaprinol (7), as the compounds responsible for the anti-diabetic activity. Their desulphonates (2, 4, 6 and 8) were also isolated as active constituents. Two separate quantitative analytical protocols, that is, for 1 and 3 and for 2 and 4, have been developed recently. OBJECTIVE: To: validate the two analytical protocols with respect to all eight sulphoniums; evaluate the quality of a variety of Salacia samples collected in different geographical regions, that is, Thailand, Sri Lanka and India; and determine their distribution in each part of the plant, that is, stems/roots, leaves and fruits. METHODS: Analyses of four sulphonium sulphates in 32 Salacia extracts were carried out on an Asahipak NH2P-50 column, and those of the corresponding desulphonates were conducted on an Inertsil ODS-3 column. RESULTS: Neokotalanol (4) was the major constituent in Salacia samples from Thailand, whereas 1 was the primary constituent in extracts of the stems/roots of plants from Sri Lanka and India. These sulphoniums were only present in trace amounts in leaves and fruits of the plants. CONCLUSION: Two analytical protocols were successfully applied to analyse 32 Salacia samples, and revealed that sulphoniums (1-8) had characteristic distributions due to the plant part and/or due to geographical region.


Assuntos
Hipoglicemiantes/análise , Medicina Tradicional do Leste Asiático , Extratos Vegetais/análise , Salacia/química , Compostos de Sulfônio/análise , Calibragem , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Índia , Monossacarídeos/análise , Monossacarídeos/química , Monossacarídeos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Caules de Planta/química , Sri Lanka , Álcoois Açúcares/análise , Álcoois Açúcares/química , Álcoois Açúcares/isolamento & purificação , Sulfatos/análise , Sulfatos/química , Sulfatos/isolamento & purificação , Compostos de Sulfônio/química , Compostos de Sulfônio/isolamento & purificação , Tailândia
17.
Pak J Pharm Sci ; 27(1): 161-7, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24374436

RESUMO

Salacia chinensis L. is a traditional Southeast Asian herbal medicine and used in the treatment of diabetes. To investigate the antidiabetic properties of mangiferin from Salacia chinensis and its beneficial effect on toxicological and hematological parameters in streptozotocin induced diabetic rats. Mangiferin was orally treated with the dose of 40 mg/kg body weight/day for 30 days to diabetic rats. Biochemical (blood glucose, uric acid, urea and creatinine), toxicological (AST, ALT and ALP) and hematological parameters (red and white blood cells) and their functional indices were evaluated in diabetic treated groups with mangiferin and glibenclamide. Mangiferin treated diabetic rats significantly (p<0.05) lowered the level of blood glucose, in addition, altered the levels of biochemical parameters including urea, uric acid, and creatinine. Toxicological parameters including AST, ALT and ALP were also significantly reduced after treatment with mangiferin in diabetic rats. Similarly, the levels of red blood, white blood cells and their functional indices were significantly improved through the administration of mangiferin. Thus, our results indicate that mangiferin present in S. chinensis possesses antidiabetic properties and nontoxic nature against chemically induced diabetic rats. Further experimental investigations are warrant to make use of its relevant therapeutic effect to substantiate its ethno-medicinal usage.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Fitoterapia , Salacia/química , Xantonas/uso terapêutico , Animais , Glicemia/análise , Creatinina/sangue , Diabetes Mellitus Experimental/sangue , Masculino , Ratos , Ratos Wistar , Estreptozocina , Ácido Úrico/sangue
18.
Biol Pharm Bull ; 36(2): 316-25, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23370361

RESUMO

Pristimerin is a naturally occurring triterpenoid that causes cytotoxicity in several cancer cell lines. However, the mechanism of action for the cytotoxic effect of pristimerin has not been unexplored. The purpose of this study was to investigate the effect of pristimerin on cytotoxicity using the epidermal growth factor receptor 2 (HER2)-positive SKBR3 human breast cancer cell line. Pristimerin inhibited proliferation in dose- and time-dependent manners in cells. We found it to be effective for suppressing HER2 protein and mRNA expression. Fatty acid synthase (FASN) expression and FASN activity were downregulated by pristimerin. Adding of exogenous palmitate, the end product of de novo fatty acid synthesis, reduced the proliferation activity of pristimerin. The changes in HER2 and FASN expression induced by pristimerin altered the levels of Akt and mitogen-activated protein kinase (MAPK) phosphorylation (Erk1/2, p38, and c-Jun N-terminal kinase (JNK)). Pristimerin lowered the levels of phosphorylated mammalian target of rapamycin (mTOR) and its downstream targets such as phosphoprotein 70 ribosomal protein S6 kinase and 4E binding protein1. Pristimerin inhibited migration and invasion of cells, and co-treatment with the mTOR inhibitor rapamycin additionally suppressed these activities. Pristimerin-induced apoptosis was evaluated using Western blotting for caspase-3, -8, -9, and poly (ADP-ribose) polymerase expression and flow cytometric analysis for propidium iodide labeling. These results suggest that pristimerin is a novel HER2-downregulated compound that is able to decrease fatty acid synthase and modulate the Akt, MAPK, and mTOR signaling pathways to influence metastasis and apoptosis. Pristimerin may be further evaluated as a chemotherapeutic agent for HER2-positive breast cancers.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Receptor ErbB-2/metabolismo , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Neoplasias da Mama/metabolismo , Caspases/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ácido Graxo Sintase Tipo I/antagonistas & inibidores , Humanos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Triterpenos Pentacíclicos , Extratos Vegetais , Raízes de Plantas , Poli(ADP-Ribose) Polimerases/metabolismo , RNA Mensageiro/metabolismo , Receptor ErbB-2/genética , Salacia , Serina-Treonina Quinases TOR/antagonistas & inibidores , Triterpenos/isolamento & purificação , Cicatrização
19.
Genet Mol Res ; 12(3): 2167-77, 2013 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-23884760

RESUMO

Salacia crassifolia (Mart. Ex. Schult.) G. Don., popularly known in Brazil as "bacupari", "cascudo", and "saputá", is a shrub of the Celastraceae family that is unique to the Brazilian Cerrado region. In folk medicine, this plant has been mainly used to treat skin cancer and gastric ulcers. In the present study, the genotoxic, cytotoxic, antigenotoxic, and anticytotoxic effects of S. crassifolia stem bark fractions (hexane, ethyl acetate, and hydroalcoholic extracts) were evaluated using the mouse bone marrow micronucleus test. Our results showed that none of the S. crassifolia fractions led to a significant increase in the frequency of micronucleated polychromatic erythrocytes (MNPCE) (P > 0.05), suggesting the absence of genotoxicity. In the antigenotoxicity assessment, a significant decrease in the MNPCE frequency was observed in all fractions of this plant (P < 0.05), demonstrating its protective action against genotoxicity induced by mitomycin C (MMC), which was used as the positive control. Only the hexane fraction of S. crassifolia significantly decreased the poly- and normochromatic erythrocyte ratio (PCE/NCE) in all doses tested (P < 0.05), demonstrating its cytotoxic activity. In association with MMC, both ethyl acetate and hydroalcoholic fractions significantly increased the PCE/NCE ratio in almost all doses tested (P < 0.05), demonstrating the protective action of S. crassifolia against the cytotoxic effect of the positive control. In contrast, the hexane fraction presented a significant decrease in the PCE/NCE ratio in all treatments (P < 0.05), demonstrating an increase in this plant's cytotoxicity in mouse bone marrow cells.


Assuntos
Citotoxinas/farmacologia , Dano ao DNA , Casca de Planta/química , Extratos Vegetais/farmacologia , Salacia/química , Animais , Antibióticos Antineoplásicos/farmacologia , Células da Medula Óssea/efeitos dos fármacos , Fracionamento Químico , Citotoxinas/química , Citotoxinas/toxicidade , Eritrócitos/efeitos dos fármacos , Camundongos , Micronúcleos com Defeito Cromossômico/efeitos dos fármacos , Mitomicina/farmacologia , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Caules de Planta/química , Salacia/anatomia & histologia
20.
Int J Vitam Nutr Res ; 83(4): 216-23, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-25008011

RESUMO

BACKGROUND: The Indian plant root Salacia reticulata, which is rich in alpha-glucosidase inhibitors, is used for metabolic disorders in Ayurvedic medicine. Vitamin D3 is also used in the treatment of some metabolic diseases. Our goal was to determine its potential effect for humans with obesity. MATERIAL: In a randomized open-label study, we investigated 40 healthy participants aged 30 - 60 years, physically active, with a body mass index (BMI) of 25 - 45. The participants were randomly allocated into two groups. Body weight, BMI, and body composition were measured. Both groups (A and B) received a guideline for lifestyle and fitness training for 4 weeks. Group B additionally took one capsule containing 200 mg of Salacia reticulata and 1.6 µg (i. e. 64 IU) Vitamin D3 (SRD) 3 times/day with the meals. RESULTS: Significant weight and body-fat reduction within 4 weeks was observed. Group A lost 1.8 kg or 2.1 %, group B lost 5.3 kg or 6.1 % (p = 0.03), therefore BMI reduction was achieved. While Group A lost 1.4 % of body fat, group B reduced it by 4.5 % (p = 0.01). CONCLUSION: These promising results suggest that the combination of Salacia reticulata and Vitamin D3 might be highly valuable and potent to treat overweight and obesity, especially in addition to a modifying lifestyle program. Further research is needed in addition to this study to clarify pathways and effect mechanisms.


Assuntos
Obesidade/tratamento farmacológico , Sobrepeso/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Salacia/química , Vitamina D/uso terapêutico , Adulto , Composição Corporal , Índice de Massa Corporal , Exercício Físico , Feminino , Humanos , Estilo de Vida , Masculino , Pessoa de Meia-Idade , Extratos Vegetais/administração & dosagem , Vitamina D/administração & dosagem , Redução de Peso
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