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1.
Molecules ; 26(3)2021 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-33572779

RESUMO

Plants have been used for thousands of years for various purposes because they have a wide variety of activities with biological significance. Mexican oregano is an aromatic plant of great importance to Mexico and north of Jalisco state as a spice with important economic value. Chromatographic identification and quantification of phenolic compounds and evaluation of their antioxidant activity were important tools to obtain a better characterization of this spice. Phytochemical analysis indicated the presence of flavonoids, triterpenes, saponins, quinones and tannins, the latter at high concentrations. Through chromatographic assays of Mexican oregano extracts, 62 compounds were identified, the major ones being quantified as: taxifolin, apigenin 7-O-glucoside, phlorizin, eriodictyol, quercetin, naringenin, hispidulin, pinocembrin, galangin and genkwanin (compound for the first time reported for this species). The results can be useful as a precedent to establish the bases of new quality characterization parameters and they have also suggested that Mexican oregano contains a wide variety of compounds with untapped importance for the development of new high value-added products.


Assuntos
Antioxidantes/química , Origanum/química , Fenóis/química , Flavonoides/química , Humanos , Fenóis/classificação , Fenóis/isolamento & purificação , Extratos Vegetais/química , Quinonas/química , Saponinas/química , Taninos/química , Triterpenos/química
2.
Food Chem Toxicol ; 150: 112075, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33617964

RESUMO

Medicinal or herbal plants are widely used for their many favourable properties and are generally safe without any side effects. Saponins are sugar conjugated natural compounds which possess a multitude of biological activities such as medicinal properties, antimicrobial activity, antiviral activity, etc. Saponin production is a part of the normal growth and development process in a lot of plants and plant extracts such as liquorice and ginseng which are exploited as potential drug sources. Herbal compounds have shown a great potential against a wide variety of infectious agents, including viruses such as the SARS-CoV; these are all-natural products and do not show any adverse side effects. This article reviews the various aspects of saponin biosynthesis and extraction, the need for their integration into more mainstream medicinal therapies and how they could be potentially useful in treating viral diseases such as COVID-19, HIV, HSV, rotavirus etc. The literature presents a close review on the saponin efficacy in targeting mentioned viral diseases that occupy a high mortality rate worldwide. This manuscript indicates the role of saponins as a source of dynamic plant based anti-viral remedies and their various methods for extraction from different sources.


Assuntos
Antivirais/isolamento & purificação , Saponinas/isolamento & purificação , Anti-Infecciosos/farmacologia , Antifúngicos/farmacologia , Antivirais/farmacologia , HIV/efeitos dos fármacos , Estrutura Molecular , Orthomyxoviridae/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Saponinas/biossíntese , Saponinas/química , Saponinas/farmacologia
3.
Food Chem ; 337: 127949, 2021 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-32919267

RESUMO

This study compared the interfacial and emulsifying properties of purified saponins and non-purified saponin-rich extracts of Glycyrrhiza glabra, and highlighted potential mechanisms by which crude surface-active compositions, such as liquorice root extract (LRE), act as emulsifiers. LRE presented different fluid properties, in comparison to purified glycyrrhizin (PG), at equivalent glycyrrhizin concentrations. Particularly, it exhibited limited glycyrrhizin fibrilization at pH < pKa and efficiently reduced the interfacial tension at the soybean oil/water interface, independently of pH. LRE also presented better emulsification properties, in comparison to PG samples. Emulsions prepared using LRE had lower droplet sizes when using higher oil mass fractions or lower homogenization pressures, which was attributed to 2 main factors: (i) efficient adsorption of glycyrrhizin molecules at relatively low interfacial curvatures, thus accelerating oil phase breakup during homogenization and (ii) sufficient coverage of newly generated droplets due to adsorption of residual surface-active components (e.g. proteins), thus minimizing droplet coalescence.


Assuntos
Emulsificantes/química , Ácido Glicirrízico/química , Extratos Vegetais/química , Emulsões/química , Glycyrrhiza/química , Saponinas/química , Óleo de Soja/química , Tensão Superficial , Água/química
4.
Food Chem ; 338: 128113, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33092009

RESUMO

Saponins are promising compounds for ameliorating hyperlipidemia but scarce information exists about sapogenins, the hydrolyzed forms of saponins. Saponin-rich extracts and their hydrolysates from fenugreek (FE, HFE) and quinoa (QE, HQE), and saponin and sapogenin standards, were assessed on the inhibition of pancreatic lipase and interference on the bioaccessibility of cholesterol by in vitro digestion models. All extracts inhibited pancreatic lipase (IC50 between 1.15 and 0.59 mg/mL), although the hydrolysis enhanced the bioactivity of HQE (p = 0.014). The IC50 value significantly correlated to the saponin content (r = -0.82; p = 0.001). Only the hydrolyzed extracts showed a reduction of bioaccessible cholesterol (p < 0.001) higher than that of phytosterols (35% reduction). Sapogenin standards exhibited no bioactivities, protodioscin and hederacoside C slightly inhibited the lipase (around 10%) and protodioscin reduced the bioaccessible cholesterol (23% reduction, p = 0.035). The hydrolysis process of saponin-rich extracts enhances the bioactivity and allows developing multibioactive products against pancreatic lipase and cholesterol absorption simultaneously.


Assuntos
Chenopodium quinoa/química , Lipase/antagonistas & inibidores , Pâncreas/enzimologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Saponinas/química , Trigonella/química , Anticolesterolemiantes/química , Anticolesterolemiantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Hidrólise
5.
PLoS One ; 15(12): e0244654, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33382809

RESUMO

BACKGROUND: Saponins are secondary metabolites from plants added to shampoos and beverages to make them foam, and the sapogenins released from them upon acid hydrolysis are commonly used as starting materials for steroidal drugs. However, current methods embed the saponin in a thick "gum" material consisting of multiple impurities. This gum limits access to the saponin, reducing the efficiency of hydrolysis and requiring large amounts of heat, organic solvents and effort to recover the sapogenin. For centuries, herbalists have been making tinctures by soaking plant materials at room temperature, in mixtures of alcohol and water. Many herbal tinctures contain saponins floating freely in solution, gum free. The saponin from sarsaparilla (Smilax spp), sarsasaponin, yields the sapogenin, sarsasapogenin, upon acid hydrolysis. The retail price of sarsasapogenin is very high but would be lower if the "gum problem" could be avoided. MATERIALS AND METHODS: We incubated sarsaparilla tincture under different conditions of temperature, acidity and duration then used quantitative nuclear magnetic resonance (qNMR) to measure the amount of sarsasapogenin produced by hydrolysis as well as the amount of its epimer, smilagenin. RESULTS AND DISCUSSION: Most, if not all the sarsasaponin in sarsaparilla root powder is extracted into a solution of 45% ethanol (55% water) at room temperature and stays suspended without formation of any particles (gum). Acid hydrolysis of the saponin in this solution is very efficient, approaching 100%. The sarsasapogenin released by hydrolysis and the smilagenin produced by its epimerisation, migrate into the chloroform phase. CONCLUSION: Sarsaparilla saponin diffuses into and disperses in a solution of alcohol:water (45:55) at room temperature. Hydrolysis of saponins in tincture provides a simple, inexpensive and environmentally friendly alternative.


Assuntos
Saponinas/química , Smilax/química , Ácidos/química , Hidrólise , Raízes de Plantas/química , Sapogeninas/química , Saponinas/isolamento & purificação , Metabolismo Secundário
6.
J Immunoassay Immunochem ; 41(6): 976-999, 2020 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-33356860

RESUMO

At present, specific therapies for COVID-19 are not well established, being certain only that the immune system plays a decisive role in the initiation and progression of the disease. Plants have given and continue to give compounds with great efficiency and low toxicity, some of them being a starting point for extremely effective synthetic substances. Although herbal remedies are used mainly for preventive purposes, there are also guidelines issued by some countries that indicate the use of traditional remedies for different stages of COVID-19 disease.Europe has a long and strong tradition of using medicinal plants for therapeutic purposes, but clinical trials for this type of approach are scarce, compared to Asia. In this regard, a bridge between tradition and science, would have a strong impact on the capacity for prevention and treatment of COVID-19. The paper reviews compounds of plant origin that have previously proven effective in counteracting some coronaviruses but also some of their major effects - direct action on virus replicative apparatus (viral entry or replication, action on the viral enzymatic system), collateral action of natural compounds on the immune system and also the contribution of herbal medicine as vaccine adjuvants are tackled.


Assuntos
/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Preparações de Plantas/uso terapêutico , Plantas Medicinais/química , /efeitos dos fármacos , Ensaios Clínicos como Assunto , Europa (Continente) , Humanos , Sistema Imunitário/efeitos dos fármacos , Lectinas/química , Óleos Voláteis/química , Fenóis/química , Fitoterapia , Saponinas/química , Internalização do Vírus/efeitos dos fármacos , Replicação Viral/efeitos dos fármacos
7.
Nat Commun ; 11(1): 5664, 2020 11 16.
Artigo em Inglês | MEDLINE | ID: mdl-33199711

RESUMO

Triterpenoid saponins are specialised metabolites distributed widely in the plant kingdom that consist of one or more sugar moieties attached to triterpenoid aglycones. Despite the widely accepted view that glycosylation is catalysed by UDP-dependent glycosyltransferase (UGT), the UGT which catalyses the transfer of the conserved glucuronic acid moiety at the C-3 position of glycyrrhizin and various soyasaponins has not been determined. Here, we report that a cellulose synthase superfamily-derived glycosyltransferase (CSyGT) catalyses 3-O-glucuronosylation of triterpenoid aglycones. Gene co-expression analyses of three legume species (Glycyrrhiza uralensis, Glycine max, and Lotus japonicus) reveal the involvement of CSyGTs in saponin biosynthesis, and we characterise CSyGTs in vivo using Saccharomyces cerevisiae. CSyGT mutants of L. japonicus do not accumulate soyasaponin, but the ectopic expression of endoplasmic reticulum membrane-localised CSyGTs in a L. japonicus mutant background successfully complement soyasaponin biosynthesis. Finally, we produced glycyrrhizin de novo in yeast, paving the way for sustainable production of high-value saponins.


Assuntos
Biocatálise , Glucosiltransferases/metabolismo , Ácido Glucurônico/metabolismo , Saponinas/biossíntese , Vias Biossintéticas , Retículo Endoplasmático/metabolismo , Regulação da Expressão Gênica de Plantas , Glicosilação , Glycyrrhiza uralensis/genética , Ácido Glicirrízico/metabolismo , Funções Verossimilhança , Lotus/genética , Filogenia , Saccharomyces cerevisiae/metabolismo , Saponinas/química , Soja/genética , Especificidade por Substrato , Triterpenos/metabolismo , Uridina Difosfato Ácido Glucurônico/metabolismo
8.
Yakugaku Zasshi ; 140(8): 1063-1069, 2020.
Artigo em Japonês | MEDLINE | ID: mdl-32741864

RESUMO

Quantitative NMR (qNMR) has been developed as an absolute quantitation method to determine the purity or content of organic compounds including marker compounds in crude drugs. The "qNMR test" has been introduced into the crude-drug section of the Japanese Pharmacopoeia (JP) for determining the purity of reagents used for the assay in the JP. In Supplement II to the JP 17th edition published in June 2019, fifteen compounds adopted qNMR test were listed as the reagents for the assay. To establish the "qNMR test" in the crude drug section of the JP, there were several problems to be solved. Previously, we reported that the handling impurity signals from reference substances and targeted marker compounds, chemical shifts of reference substances, and peak unity of signals of targeted marker compounds are important factors to conduct qNMR measurements with intended accuracy. In this study, we investigated that the hygroscopicity of reagents could cause the changes in the compounds' purity depending on increasing their water content. Twenty-one standard products used for the crude-drug test in JP were examined by water sorption-desorption analysis, and ginsenosides and saikosaponins were found to be hygroscopic. To prepare a sample solution of saikosaponin b2 for qNMR analysis, samples need to be maintained for 18 h at 25°C and 76% relative humidity; further, samples need to be weighed at the same humidity for the qNMR analysis.


Assuntos
Contaminação de Medicamentos/prevenção & controle , Higroscópicos/química , Higroscópicos/normas , Indicadores e Reagentes/normas , Espectroscopia de Ressonância Magnética/métodos , Farmacopeias como Assunto/normas , Ginsenosídeos/química , Ginsenosídeos/normas , Umidade , Japão , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Ácido Oleanólico/normas , Psicoterapia Breve , Saponinas/química , Saponinas/normas , Temperatura , Água/análise
9.
Int J Nanomedicine ; 15: 5839-5853, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32848393

RESUMO

Background: The development of paclitaxel (PTX) resistance seriously restricts its clinical efficacy. An attractive option for combating resistance is inhibiting the expression of P-glycoprotein (P-gp) in tumor cells. We have reported that flavokawain A (FKA) inhibited P-gp protein expression in PTX-resistant A549 (A549/T) cells, indicating that FKA combined with PTX may reverse PTX resistance. However, due to the variable pharmacokinetics of FKA and PTX, the conventional cocktail combination in clinics may cause uncertainty of treatment efficacy in vivo. Materials and Methods: To synergistically elevate the anti-cancer activity of PTX and FKA in vivo, the national medical products administration (NMPA) approved sodium aescinate (Aes) was utilized to stabilize hydrophobic PTX and FKA to form polymer-free twin like PTX-A nanoparticles (NPs) and FKA-A NPs. Results: The resulting nanoparticles prepared simply by nanoprecipitation possessed similar particle size, good stability and ultrahigh drug loadings of up to 50%. With the aid of Aes, these two drugs accumulated in tumor tissue by passive targeting and were efficiently taken up by A549/T cells; this resulted in significant suppression of tumor growth in A549/T homograft mice at a low PTX dose (2.5 mg·kg-1). Synergistic effects and reversed PTX resistance were achieved by the combination of PTX-A NPs and FKA-A NPs by inhibiting P-gp expression in tumor cells. Conclusion: Using NMPA-approved Aes to prepare twin-like nanoparticles without introducing any new materials provides an efficient platform for combination chemotherapy and clinical translation.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Nanopartículas/química , Paclitaxel/farmacologia , Saponinas/química , Triterpenos/química , Células A549 , Animais , Protocolos de Quimioterapia Combinada Antineoplásica/química , Protocolos de Quimioterapia Combinada Antineoplásica/farmacocinética , Linhagem Celular Tumoral , Chalcona/administração & dosagem , Chalcona/análogos & derivados , Chalcona/farmacocinética , Estabilidade de Medicamentos , Sinergismo Farmacológico , Feminino , Humanos , Interações Hidrofóbicas e Hidrofílicas , Camundongos Endogâmicos BALB C , Nanopartículas/administração & dosagem , Nanopartículas/uso terapêutico , Paclitaxel/administração & dosagem , Paclitaxel/farmacocinética , Tamanho da Partícula , Polímeros/química , Ensaios Antitumorais Modelo de Xenoenxerto
10.
J Nat Med ; 74(4): 732-740, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32643027

RESUMO

AG36 is a triterpenoid saponin from Ardisia gigantifolia stapf. Our recent studies proved that AG36 displayed prominent cytotoxicity against breast cancer cells both in vitro and in vivo. However, whether AG36 has antiangiogenic properties is unknown. Therefore, in the present study, we evaluated the antiangiogenic effect of AG36 and the underlying mechanism. The results indicated that AG36 could significantly inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC). Further antiangiogenic molecular mechanism investigation showed that AG36 significantly suppressed phosphorylated FAK and AKT, and downregulated the expressions of vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptor 2 (VEGFR2) in HUVECs. PI3K inhibitor (LY294002) and FAK inhibitor (PF562271) pretreatment could markedly enhance AG36-induced inhibition of HUVEC proliferation and p-FAK suppression, respectively. In addition, AG36 inhibited the tumor growth in xenograft model and expressions of p-VEGFR2 and p-Akt in vivo. Molecular docking simulation indicated that AG36 formed hydrogen bonds and hydrophobic interactions within the ATP binding pocket of VEGFR2 kinase domain. The present study firstly revealed the high antiangiogenic potency and related underlying molecular of AG36, demonstrating that AG36 maybe a potential antiangiogenic cancer therapy agent or lead candidate.


Assuntos
Inibidores da Angiogênese/uso terapêutico , Ardisia/química , Medicina Tradicional Chinesa/métodos , Saponinas/química , Inibidores da Angiogênese/farmacologia , Animais , Humanos
11.
J Food Sci ; 85(7): 2198-2206, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32614078

RESUMO

The hemolytic property discourages the development of sea cucumber saponins on alleviating lipids metabolism disturbance. The hemolytic activity of saponins has been reported to be highly correlative to their chemical structures. The aim of this study was to reduce the hemolytic activity of sea cucumber-derived saponins echinoside A (EA) and simultaneously remain its effect on alleviating non-alcoholic fatty liver disease (NAFLD) by structural modifications. Administration with EA and its derivatives for 8 weeks remarkably mitigated orotic acid-induced NAFLD via inhibiting the activities and mRNA expressions of enzymes involved in lipogenesis, enhancing the activities and expressions of enzymes related to hepatic lipolysis in a rat model. Importantly, aglycone exhibited a distinct advantage in stimulating hepatic lipolysis compared with EA and dsEA, meanwhile possessed lowest hemolytic activity. This study may provide the theoretical basis to strengthen the application of sea cucumber saponins as food supplements and/or functional ingredients.


Assuntos
Holoturina/análogos & derivados , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Pepinos-do-Mar/química , Animais , Holoturina/administração & dosagem , Holoturina/química , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Lipólise/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Hepatopatia Gordurosa não Alcoólica/metabolismo , Hepatopatia Gordurosa não Alcoólica/fisiopatologia , Ratos , Ratos Wistar , Saponinas/administração & dosagem , Saponinas/química
12.
Food Chem ; 327: 127029, 2020 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-32450486

RESUMO

Platycodonis Radix, the root of Platycodon grandiflorum (Jacq.) A. DC., is a well-known edible herbal medicine. It is a common vegetable used for the preparation of side dish, kimchi, dessert, and tea. Besides, it has been used to treat respiratory disease including cough, excessive phlegm, and sore throat for a long history. In the past decades, the bioactive components and the pharmacological activities of Platycodonis Radix have been widely investigated. Thereinto, platycodins, the oleanane-type triterpenoid saponins were demonstrated to be the main bioactive components in Platycodonis Radix, and more than 70 platycodins have been identified up to date. This paper mainly reviewed the phytochemistry, pharmacological activities (apophlegmatic, anti-tussive, anti-inflammatory, anti-cancer, anti-obesity, anti-diabetic, immunomodulatory, cardiovascular protective, and hepatoprotective activities, etc.), toxicology and pharmacokinetics of platycodins isolated from Platycodonis Radix, aiming to promote further investigation on therapeutic potential of these platycodins.


Assuntos
Platycodon/química , Saponinas/química , Saponinas/farmacologia , Animais , Humanos , Fitoterapia , Saponinas/farmacocinética , Saponinas/toxicidade
13.
Food Chem ; 327: 127062, 2020 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-32454279

RESUMO

Soy glycinin (11S) was mixed with soyasaponin (Ssa) to elucidate the mechanism(s) involved in the stabilization of emulsions by mixed systems based on dynamic interfacial tension and dilatational rheology at the oil-water interface. The short/long-term properties of oil-in-water emulsions stabilized by 11S-Ssa mixtures included droplet-size distribution, droplet ζ-potential, microstructure, and Turbiscan stability index. The combination of Ssa (0.05%) with 11S significantly affected the interfacial dilatational and emulsion properties although the interfacial properties were still dominated by the protein. Higher concentrations (0.1% and 0.2%) of Ssa combined with 11S synergistically decreased the interfacial tension, which was attributed to the interaction between 11S and Ssa. Using high Ssa concentrations (0.25%-0.5%) enhanced the long-term stability of emulsions (in response to external deformations) after 42 d. These results will aid the basic understanding of protein-Ssa interfacial adsorption during emulsion formation and can help prepare natural food additives for designing emulsions.


Assuntos
Globulinas/química , Saponinas/química , Proteínas de Soja/química , Soja/química , Adsorção , Óleo de Milho/química , Emulsões/química , Tensão Superficial , Água/química
14.
Food Chem ; 321: 126706, 2020 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-32234636

RESUMO

The purpose of this study was to fabricate ternary complexes composed of pea protein isolate (PPI), high methoxyl pectin (HMP) and individual surfactants including rhamnolipid (Rha), tea saponin (TS) and Ethyl lauroyl arginate (LAE), for the delivery of resveratrol (Res). A combination of electrostatic attraction and hydrophobic interaction was dominantly responsible for the formation of HMP-surfactant-PPI complexes. The physicochemical properties of the ternary complexes were affected by surfactant types as well as mass ratios of individual surfactant to PPI. HMP-Rha-PPI1:1, HMP-TS-PPI1:1 and HMP-LAE-PPI1:25 complexes had higher denaturation temperatures of 82.78 ± 0.31, 80.21 ± 0.02 and 79.98 ± 0.86 ℃, respectively. The HMP-Rha-PPI1:1 ternary complex could be an effective delivery system, which were effective to retard photo- and thermal- degradation of Res as well as delayed the release of Res in in vitro digestion.


Assuntos
Glicolipídeos/química , Proteínas de Ervilha/química , Pectinas/química , Resveratrol/química , Tensoativos/química , Interações Hidrofóbicas e Hidrofílicas , Saponinas/química
15.
J Nat Med ; 74(3): 591-598, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32200514

RESUMO

Three new steroidal saponins, aspiletreins A-C (1-3), together with 2H-chromen-2-one (4), and α-tocopherol (5), were isolated from whole Aspidistra letreae plants collected in Vietnam. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR, IR, and HRESIMS, and by comparison with the reported data in the literature. Compounds 1-3 exhibited moderate cytotoxicities against the LU-1, HeLa, MDA-MB-231, HepG2, and MKN-7 human cancer cell lines, with IC50 values ranging from 7.69 ± 0.40 to 20.46 ± 3.11 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Asparagaceae/química , Proliferação de Células/efeitos dos fármacos , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Células HeLa , Células Hep G2 , Humanos , Estrutura Molecular , Neoplasias/tratamento farmacológico , Extratos Vegetais/química , Saponinas/química , Vietnã
16.
Sci Rep ; 10(1): 4967, 2020 03 18.
Artigo em Inglês | MEDLINE | ID: mdl-32188912

RESUMO

Aging is associated with increased prevalence of skeletal and cardiac muscle disorders, such as sarcopenia and cardiac infarction. In this study, we constructed a compendium of purified ginsenoside compounds from Panax ginseng C.A. Meyer, which is a traditional Korean medicinal plant used to treat for muscle weakness. Skeletal muscle progenitor cell-based screening identified three compounds that enhance cell viability, of which 20(R)-ginsenoside Rh2 showed the most robust response. 20(R)-ginsenoside Rh2 increased viability in myoblasts and cardiomyocytes, but not fibroblasts or disease-related cells. The cellular mechanism was identified as downregulation of cyclin-dependent kinase inhibitor 1B (p27Kip1) via upregulation of Akt1/PKB phosphorylation at serine 473, with the orientation of the 20 carbon epimer being crucially important for biological activity. In zebrafish and mammalian models, 20(R)-ginsenoside Rh2 enhanced muscle cell proliferation and accelerated recovery from degeneration. Thus, we have identified 20(R)-ginsenoside Rh2 as a p27Kip1 inhibitor that may be developed as a natural therapeutic for muscle degeneration.


Assuntos
Ginsenosídeos/farmacologia , Músculo Esquelético/citologia , Infarto do Miocárdio/tratamento farmacológico , Miocárdio/citologia , Panax/química , Saponinas/química , Células-Tronco/metabolismo , Adulto , Animais , Sobrevivência Celular , Ginsenosídeos/química , Ensaios de Triagem em Larga Escala , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/metabolismo , Infarto do Miocárdio/metabolismo , Infarto do Miocárdio/patologia , Miocárdio/metabolismo , Fosforilação , Ratos , Ratos Sprague-Dawley , Regeneração , Peixe-Zebra
17.
Int J Mol Med ; 45(4): 1225-1236, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32124939

RESUMO

Panax notoginseng saponins (PNS) are active extracts obtained from the P. notoginseng plant. PNS exhibit various anti­inflammatory, anti­oxidant and anti­aging pharmacological properties in some cells. However, the effects of PNS on senescence and apoptosis in chondrocytes have not been studied to date. In the present study, whether PNS could limit tumor necrosis factor (TNF)­α­induced senescence and apoptosis in chondrocytes and whether they could slow down cartilage degeneration in a surgery­induced rat osteoarthritis (OA) model by regulating the phosphatidyl inositol 3 kinase (PI3K)­protein kinase B (AKT)­mammalian target of rapamycin (mTOR) signaling pathway was examined. A potential mechanism underlying these effects was further elucidated. The present in vitro experiments showed that PNS significantly inhibited senescence and apoptosis in OA chondrocytes and prevented a decrease in the mitochondrial membrane potential and excessive mitochondrial permeability. In addition, the expression levels of autophagy­related proteins and the anti­apoptotic protein Bcl­2 were significantly increased in PNS­treated OA chondrocytes, but the expression levels of Bax and caspase­3 were decreased; these effects were concentration­dependent. TNF­α significantly increased the expression of p­PI3K/p­AKT/p­mTOR in OA chondrocytes, whereas PNS reduced PI3K, AKT and mTOR phosphorylation. The results of the in vivo experiments demonstrated that PNS significantly inhibited the PI3K­AKT­mTOR signaling pathway and collagen II degradation, as well as reduced matrix metalloproteinase (MMP)­3 and MMP­13 expression in chondrocytes in a rat OA model, thus attenuating cartilage destruction in OA. The results obtained in the rat model were consistent with the in vitro experimental results. Furthermore, histological analyses and ultrastructural observations confirmed these results. Taken together, the results of the present study demonstrated that PNS may protect osteoarthritic chondrocytes from senescence and apoptosis by inhibiting the PI3K­AKT pathway, thus delaying the degradation of articular cartilage.


Assuntos
Apoptose/efeitos dos fármacos , Senescência Celular/efeitos dos fármacos , Condrócitos/metabolismo , Osteoartrite/metabolismo , Panax notoginseng/química , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Saponinas/farmacologia , Serina-Treonina Quinases TOR/metabolismo , Animais , Condrócitos/patologia , Modelos Animais de Doenças , Humanos , Masculino , Osteoartrite/tratamento farmacológico , Osteoartrite/patologia , Ratos , Ratos Sprague-Dawley , Saponinas/química
18.
J Immunol Res ; 2020: 2714257, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32149156

RESUMO

Pseudorabies is an important infectious disease of swine, and immunization using attenuated pseudorabies virus (aPrV) vaccine is a routine practice to control this disease in swine herds. This study was to evaluate a saline solution containing ginseng stem-leaf saponins (GSLS) and sodium selenite (Se) as a vaccine adjuvant for its enhancement of immune response to aPrV vaccine. The results showed that aPrV vaccine diluted with saline containing GSLS-Se (aP-GSe) induced significantly higher immune responses than that of the vaccine diluted with saline alone (aP-S). The aP-GSe promoted higher production of gB-specific IgG, IgG1, and IgG2a, neutralizing antibody titers, secretion of Th1-type (IFN-γ, IL-2, IL-12), and Th2-type (IL-4, IL-6, IL-10) cytokines, and upregulated the T-bet/GATA-3 mRNA expression when compared to aP-S. In addition, cytolytic activity of NK cells, lymphocyte proliferation, and CD4+/CD8+ ratio was also significantly increased by aP-GSe. More importantly, aP-GSe conferred a much higher resistance of mice to a field virulent pseudorabies virus (fPrV) challenge. As the present study was conducted in mice, further study is required to evaluate the aP-GSe to improve the vaccination against PrV in swine.


Assuntos
Adjuvantes Imunológicos , Panax/química , Saponinas/farmacologia , Selênio/farmacologia , Células Th1/efeitos dos fármacos , Células Th1/imunologia , Células Th2/efeitos dos fármacos , Células Th2/imunologia , Vacinas/imunologia , Animais , Anticorpos Neutralizantes/imunologia , Biomarcadores , Relação CD4-CD8 , Citocinas/metabolismo , Feminino , Expressão Gênica , Imunoglobulina G/imunologia , Camundongos , Vacinas contra Pseudorraiva/imunologia , Saponinas/química , Selênio/química , Soluções , Baço/efeitos dos fármacos , Baço/imunologia , Baço/metabolismo , Suínos , Subpopulações de Linfócitos T/efeitos dos fármacos , Subpopulações de Linfócitos T/imunologia , Subpopulações de Linfócitos T/metabolismo , Células Th1/metabolismo , Células Th2/metabolismo
19.
Food Chem ; 318: 126474, 2020 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-32151922

RESUMO

Excessive energy intake, poor physical exercise and genetics/epigenetics are instrumental for the development of obesity. Because of rapidly emerging evidences related to off-target effects and toxicity of anti-obesity drugs, there is a need to search for more effective and targeted drugs for treatment of obesity. Substantial studies have found the nutritional effects of dietary saponins (bio-detergents) in terms of decreasing the synthesis of lipids, suppressing adipogenesis, inhibiting intestinal absorption of lipids, and promoting fecal excretion of bile acids and triglycerides. Dietary saponin have been approved as potent pancreatic lipase inhibitors, disaccharidase enzyme inhibitors, antagonistic to in vitro lipogenesis and in vivo appetite suppressants, antioxidants, immune-regulators, prevent fatty liver formation, protects epithelial vasculature and regulate body weight. Many dietary saponins, such as sibutramine, morgoside, sessiloside, soysaponin B, and diosgenin, have treatment potential against the development of obesity. Excellent scientific achievements have been developed for a better understanding the mechanism of saponins in preventing obesity.


Assuntos
Fármacos Antiobesidade/farmacologia , Obesidade/prevenção & controle , Saponinas/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Suplementos Nutricionais , Inibidores Enzimáticos/farmacologia , Humanos , Lipase/antagonistas & inibidores , Obesidade/dietoterapia , Saponinas/química
20.
J Chromatogr A ; 1620: 461010, 2020 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-32173025

RESUMO

In this paper, adsorption mechanism of triterpenoid saponins in reversed-phase liquid chromatography (RPLC) and hydrophilic interaction liquid chromatography (HILIC) was proposed based on the study of the retention behavior of mogroside V as test substance. The change of peak shape of mogroside V and its influencing factors was first investigated. As the increase of sample loading, a tailing peak of mogroside V was observed in MeOHH2O of both two modes. It was the fronting peak in ACNH2O of HILIC while there was a transition from fronting peak to tailing peak in ACNH2O of RPLC that was largely affected by column temperature and ACN concentration. The adsorption isotherm of mogroside V in ACNH2O of RPLC was fitted by Moreau model, where a monolayer adsorption with large inter-molecular interaction was formed on the C18 surface. While in ACNH2O of HILIC, the adsorption of mogroside V was in accordance with BET model, showing multilayer adsorption behavior. In MeOHH2O of both HILIC and RPLC, there was always monolayer adsorption, which was fitted by Langmuir model. At last, by choosing the suitable chromatographic mode, controlling the key factors such as the solvent concentration and column temperature, and predicting the broadening trend of peak, three methods were screened out, namely, C18 column with 22% ACN (30 °C), Click XIon column with 90% MeOH or 70% ACN, to get mogroside V of purity greater than 98% from Siraitia grosvenorii extract. Among them, the RPLC method of 22% ACN that showed the highest loading sample per hour (1.92%) and the lowest solvent consumption emerged as the best approach.


Assuntos
Cromatografia Líquida/métodos , Cromatografia de Fase Reversa/métodos , Interações Hidrofóbicas e Hidrofílicas , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Adsorção , Saponinas/química , Solventes , Temperatura , Triterpenos/química
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